Term
| Class of Drug? Lysergic and diethylamide |
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Definition
| This is LSD, and it is an indole (hallucinogen) |
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Term
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Definition
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Term
| Class of Drug? Psilocybin |
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Definition
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Term
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Definition
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Term
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Definition
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Term
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Definition
| Phenylethylamine (Hallucinogen) |
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Term
| Class of Drug? Methylenedioxymethamphetamine |
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Definition
| aka MDMA, ECstasy--Phenylethylamine (Hallucinogen) |
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Term
| initial and later effects of LSD (prototype hallucinogen) |
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Definition
INITIAL EFFECTS (within 30 min-2 hours)
1.) SYMPATHOMIMETIC EFFECTS
-pupillary dilation
-increase in BP
-tachycardia
-piloerection
-hyperflexia
-tremors
-increase in body temp
2.) Miscellaneous Somatic Effects
-dizziness
-weakness
-paresthesias
-nausea
3.) SUBJECTIVE PSYCHIC CHANGES
-anxiety
-euphoria, giddiness
-emotional lability
-in general..the early stage subjective effects are usually perceived as pleasant
LATER EFFECTS (1-3 hours
1.) HALLUCINOGENIC EFFECTS
-Sensory distortions--heightened awareness of sensory input, auditory and visual disturbances, hallucinations (primarily visual), synesthesias
-Depersonalization-out of body experiences
-difficulty differentiating drug effects from reality
-anxiety, fear, paranoia, panic, emotional "lability"
-panic reactions, psychotic reactions |
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Term
| Where found, main effects? Psilocin and psilocybin |
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Definition
| Both are found in hallucinogenic mushrooms--effects are qualitatively similar to those of LSD |
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Term
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Definition
| found in some mushrooms and in the skin of some amphibians (TOAD LICKING!!!) |
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Term
| Where found? Main effects? Mescaline |
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Definition
| Mescaline is found in buttons of the peyote cactus...effects are similar to those of LSD but the somatic autonomic changes are more pronounced |
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Term
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Definition
| This is Ecstasy--has both hallucinogenic and stimulant effects...NOW one of the more common hallucinogens |
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Term
| Ibogaine--where from? main effects? |
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Definition
| Ibogaine is an alkaloid found in the roots of an African shrub (Tabernanthe iboga) It is a powerful hallucinogen that has recently been reported to suppress the craving for heroin, cocaine, and other drugs in addicted individuals...this is extremely controversial though |
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Term
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Definition
| not well understood MOA--act as agonists at presynaptic 5-HT2 receptors and thereby decrease the rate of firing of 5-HT neurons in the dorsal raphe nucleus, which leads to alterations in the functioning of the reticular sensory filtering system...in addition, there is evidence that the drugs may affect other NT systems such as dopamine and the enkephalins |
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Term
| Other names for Phencyclidine |
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Definition
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Term
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Definition
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Term
| Pharmacokinetics of PCP/Ketamine |
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Definition
PCP may be taken orally, snorted, injected, or most commonly smoked
-it is often mixed with weed
-PCP is rapidly absorbed and distributed
-it is slowly metabolized and excreted--in overdose situations the T1/2 may be 2-3 days |
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Term
| Major Pharmacologic effects of PCP/Ketamine |
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Definition
-Low doses produce subjective effects similar to those of weed
-slightly higher doses cause amphetamine-like stimulant effects that are restlessness, irritability, and hostility...
--at even higher doses, hallucinations, psychotic reactions and rage reactions can occur
-Social withdrawl, isolation and cognitive disturbances are common among heavy users
-Phenylcyclidine causes some degree of hyperflexia and has been reported to increase muscle strength --Phenylcyclidine has significant analgesic activity--Besides acting crazy and feeling strong, an individual under the influence of PCP "feels no pain"--uhoh!
NOTE: the effects of phencyclidine vary markedly from one individual to another...psychotic reactions are much more common with phencyclidine than with other drugs |
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Term
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Definition
| very complex and not well understood--Blockade of NMDA receptors |
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Term
| Symptoms of acute poisoning with PCP |
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Definition
slurred speech, ataxia, stupor
***Hyperreflexia, increased muscle tone and HTN may be useful in differentiating PCP poisoning from that of sedative hypnotics. In addition, PCP is unique in that it can cause VERTICAL NYSTAGMUS, which may be useful in the diagnosis of poisoning
-psychotic reactions-hostility, aggression, hallucinations
-convulsions
-cardiac and respiratory depression
-coma and cardiovascular collapse |
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Term
| Treatment of acute poisoning with PCP |
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Definition
Calm and reassure the patient--decrease sensory stimulation
-Symptomatic support for psychotic reactions-antipsychotics as needed
-support respiration
-use anticonvulsants and antihypertensives as needed
-acidify urine to hasten excretion of drug |
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Term
| Symptoms of PCP withdrawl |
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Definition
craving for drug
-fear, anxiety, restlessness |
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Term
| Hazards assoc with long term use of PCP |
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Definition
| Psychosis and cognitive impairment may persist even after the drug has been stopped |
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Term
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Definition
| Marijuana, Hashish, K-2, Spice |
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Term
| Pharmacokinetics of Cannabinoids |
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Definition
THC is very lipid soluble and is rapidly absorbed and distributed to the brain and other fatty tissue
Because of its high lipid solubility, THC accumulates in fat and is slowly released over time
Although the duration of action is only 2-3 hours, low levels of the drug and its metabolites may be present for several weeks |
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Term
| Pharmacologic Effects of Cannabinoids |
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Definition
Relaxation and inreased sense of well-being, giddiness
sedation and drowsiness
memory and cognitive impairment, confusion
psychomotor slowing, loss of coordination, decreased ability to perform complex tasks
high doses can cause hallucinations, paranoia, psychotic reactions
increase in appetite
**tachycardia, postural hypotension
reddening of the conjunctiva (tell tale sign)
decrease in intraocular pressure ( treatment of glaucoma?)
inhibition of vomiting reflex (THC avaliable for pts undergoing cancer chemotherapy) |
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Term
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Definition
| Not well understood but recent studies have shown that specific canabinoid receptors are present in the CNS--investigators are trying to identify the endogenous compounds that act on these receptors..one such sompound that has been identified is an analog of arachidonic acid, arachidonylethanolamide. New drugs that modulate "endcanabinoids" and canabinoid receptors are under development |
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Term
| Toxic effects of cannabinoids |
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Definition
1.) Suppression of immune function-significance in humans is unclear
2.) Lowering of testosterone levels in males--decreased libido, gynecomastia
3.) Teratogenic effects-decreased birthweight, increased incidence of birth defects, learning disabilities in offspring
4.) A so called "amotivational syndrome"has been associated with heavy use-not sure wheter the cause or effect of drug use
5.) Damage to lungs similar to that seen in tobacco smokers--lung damage might be severe if marijuana is treated with herbicides such as paraquat
6.) Severe poisoning is rare--may get paranoid though |
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Term
| Tolerance and Physical Dependence on Cannabinoids |
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Definition
Marijuana appears to produce some degree of tolerance with chronic use, although paradoxically, some users may actually become sensitized to the effects of marijuana--may be due to increased awareness of drugs effects OR saturation of body fat with THC over time
Some lab studies suggest that heavy use can result in physical dependence with a withdrawl syndrome characterized by irritabiilty, tremors, nausea and vomiting...however, such withdrawl symptoms are almost never seen outside of research lab |
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Term
| Medical uses of cannabinoids |
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Definition
prevention of nausea and vomiting during cancer chemo
prevention of "wasting" in AIDS pts
treatment of glaucoma and asthma (proposed but not approved)--actually alot of data says weed doesnt help glaucoma |
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Term
Salvia
Source, Use, MOA, mode of administration, |
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Definition
Salvia comes from a plant known as Salvia divinorum (related to mint family) which grows wild in many parts of N. America..it has been used in religious rituals by native ppl of Mexico and is now being abused for its hallucinogenic effects
Active agent: salvinorin A, which is an agonist at kappa opioid and D2 dopamine receptors. It has hallucinogenic activities that are qualitatively different from classic hallucinogens, such as LSD
Usually taken by smoking leafy material in bong or water piper
Readily avaliable via internet
has been criminalized in many states and banned by the DEA
Responses to the drug vary markedly from one person to another--many ppl report dysphoric effects and "bad trip" symptoms...many videos of ppl having bad reactions to salvia are posted on the web |
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Term
Kratom
where from, use, MOA, |
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Definition
Kratom is indigenous to regions of Thiland, where it has been used as a stimulant and pain reliever...it has been reported to have opioid-like effects...
contains several active pharmacological agents that are chemically different from morphine and other opioids. A few of the compounds (mitragynine and 7-hydroxyragynine) have agonist activity at mu-opioid receptors
Touted as a LEGAL opioid and being useful for controlling opioid withdrawl symptoms
Responses vary markedly from one person to another (euphoria to dysphoria to not effect)
Plant material and extracts are readily avaliable over the internet and in some "head shops"
Being used in US for sefl directed management of pain and opioid withdrawal...also abused
Currentyl legal in most parts of the US but has drawn attn of the DEA and some local governments |
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Term
| Class of drug/use: Rivastigmine |
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Definition
| Acetylcholinesterase inhibitor used in treatmnet of Alzheimers and some types of dementia |
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Term
| Class of Drug/use: Donepezil |
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Definition
| Acetylcholinesterase inhibitor used in treatmnet of Alzheimers and some types of dementia |
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Term
| Side effects: Rivastigmine |
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Definition
| Significant cholinergic side effects such as salivation, sweating, nausea, diarrhea, intestinal cramping, urinary incontinence, bradycardia, bronchoconstriction, etc. |
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Term
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Definition
Significant cholinergic side effects such as salivation, sweating, nausea, diarrhea, intestinal cramping, urinary incontinence, bradycardia, bronchoconstriction, etc.
BUT Donepazil has the lowest tendency to cause these side effects |
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Term
| Class of Drug/use: Memantine |
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Definition
| Memantine is a NMDA receptor antagonist approved for the treatemnet of Alzheimers disease in the US |
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Term
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Definition
| Acts by blocking the excitatory actions of glutamate at NMDA receptors in the hippocampus and frontal cortex...this can improve cognitive function in patients with AD and may also prevent some of the excitoneurotoxic effects of glutamate (which are thought to contribute to the neurodegenerative changes seen in AD). In general, memantine is fairly well tolerated. the most common side effects include increased BP, dizziness,GI distress and cough |
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Term
| Antioxidants which reduce the degenerative changes seen in Alzheimers Disease |
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Definition
| Vitamin E and Seligiline/deprenyl have been reported to reduce some of the degenerative changes and slow the progression of AD. Other studies have shown only modest effects or no benefit....All of this is very controversial |
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Term
| Drug used to treat ALS (Lou Gehrig's Disease) |
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Definition
Riluzole (Rilutek):
This is the only drug currently avaliable that has been shown to slow the progression of the disease. It is thought to act by inhibiting the release of glutamate from nerve endings and reducing the so called "excitotoxicity"
Is avaliable as an "orphan drug" and seems to be most beneficial if started early in the course of the disease |
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Term
| Main MOA: Stimulants for treatment of ADHD |
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Definition
Drugs related to the stimulant amphetamine have been the mainstay agents for the treatment of ADHD over the years...
These act by stimulating areas of the brain (esp locus ceruleus) that enable an individual to focus their attention on the task at hand. In an individual with ADHD, this may appear to represent a "calming" effect but it actually results from a stimulatory action of the drug
At the molecular level, all of the stimulants act by causing the release and/or inhibiting the reuptake of dopamine and norepinephrine from synaptic nerve endings.. |
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Term
| Side Effects of the ADHD Stimulant Drugs |
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Definition
| Suppression of appetite resulting in slowed growth, sympathomimetic effects including HTN and tacycardia, tremors and emotional lability..also all of the ADHD stimulants have a significant abuse potential |
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Term
| Methylphenidate: use, MOA, duration of action |
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Definition
This is AKA Ritalin
this is the mainstay stimulant drug used for the treatment of ADHD
relatively short duration of action alone, although sustained release preps are now avaliable |
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Term
d-amphetamine, d,l-amphetamine and their salts
use, brand name, what complicates their prescribing? |
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Definition
These are powerful stimulants generally reserved for ADHD patients who dont show an adequate response to methylphenidate (Ritalin)
ADDERALL is a brand name product that contains a complex mixture of amphetamine salts
The fact that they are schedule 2 drugs complicates prescribing |
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Term
| Atomoxatime: use, MOA, concern? |
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Definition
Atomoxatine is a non stimulating agent approved for the treatment of ADHD in adults and kids...it is thought to act by inhibiting the synaptic reuptake of NE. Clinical trials have shown that it can greatly benefit some pts who dont respond well to stimulants
However, there are increasing concerns about the potential for this drug to cause serious hepatotoxicity in a small percentage of pts |
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Term
| Class of Anesthetic: Nitrous Oxide |
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Definition
| inhaled general anesthetics |
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Term
| Class of Anesthetic: Isoflurane |
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Definition
| inhaled general anesthetics |
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Term
| Class of Anesthetic: Enflurane |
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Definition
| inhaled general anesthetics |
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Term
| Class of Anesthetic: Desflurane |
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Definition
| inhaled general anesthetics |
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Term
| Class of Anesthetic: Sevoflurane |
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Definition
| inhaled general anesthetics |
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Term
| Class of Anesthetic: Propofol |
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Definition
| Intravenous General Anesthetic |
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Term
| Class of Anesthetic: Etomidate |
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Definition
| Intravenous General Anesthetic |
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Term
| Class of Anesthetic: Ketamine |
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Definition
| Intravenous General Anesthetic |
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Term
| Class of Anesthetic: Midazolam |
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Definition
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Term
| Class of Anesthetic: Fentanyl |
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Definition
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Term
| Class of Anesthetic: Dexmedetomidine |
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Definition
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Term
| General MOA of General Anesthetics |
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Definition
GAs inhibit neuronal activity by causing:
1.) neuronal hyperpolarization
2.) inhibition of excitatory synapses
3.) enhancing inhibitory synapses |
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Term
| Lipid Theory of General Anesthetics' MOA |
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Definition
States tha GAs swell lipid membranes causing a general alteration in ion channel conduction
Myer-Overton rule: anesthetic potency correlates with its solubility in olive oil |
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Term
| Specific protein theory of General anesthetics' MOA |
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Definition
| states that general anesthetics interact specifically with ion channels/receptors |
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Term
Nitrous Oxide:
Use, Pharmacokinetics, and side effects |
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Definition
The MAC of Nitrous oxide is 105%, meaning that N2O by itself cannot achieve the desired depth of anesthesia. It is a weak anesthetic, producing analgesia at 20% concentration of inhaled air and sedation at 30-80%...it is a colorless, odorless gas that can be used to induce analgesia in the dentist office
Pharmacokinetics: rapid induction and recovery (low blood/water solubility and low blood/gas partition coefficient)
Side Effects: air pockets (in middle ear) may expand
can change BP depending on what is co-administered
depresses ventillary response to hypoxia
doesnt trigger malignant hyperthermia |
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Term
| Enflurane: odor, side effects |
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Definition
this is a general anesthetic with a sweet odor
Side effects:
decrease in BP, decreased cardiomyocyte contractility, peripheral vasodilation (cerebral vasculature), no change in heart
**Produces electrical seizure activity, though no evidence, contraindicated for epileptics**
muscle relaxation enhanced with neuromuscular junction blockers
decrease in ventilation rate |
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Term
| Isoflurane: scent, how eliminated, side effects |
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Definition
Isoflurane is a General anesthetic with a pungent odor
>99% is eliminated unchanged via the lungs
Side Effects:
Decrease in BP
vasodilation only (cerebral vasculature)
cardiac output maintained
mild tachycardia
Decreased ventilary response reflex to hypoxia/hypercapnia
modest vasodilation in cerebral vasculature, however metabolic rate of brain is decreased
preferred GA for neurosurgery
muscle relaxation enhanced with Neuromuscular junciton blockers
decreased renal blood flow |
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Term
| Desflurane: how eliminated, side effects |
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Definition
General anesthetic
>99% eliminated unchanged via the lungs
Side effects:
Irritating gas--coughing and respiratory secretions occur when inhaled so thus must be used IV to induce anesthesia
Decrease in BP, CO is well preserved
Decrease in ventilation rate |
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Term
| Sevoflurane: Pharmacokinetics and Side effects |
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Definition
Sevoflurane is a general anesthesia drug that reacts with dried soda lime to produce CO...is non-irritating alone to airways
Pharmacokinetics: >99% eliminated unchanged via lungs
Side effects:
decrease in BP
systemic vasodilation
no change in cardiac output
preferred GA for pts prone to myocardial ischemia
renal effects
sevoflurane and soda lime combine to produce "COMPOUND A" which may cause short term renal damage--because of this, the FDA recommends sevoflurane administered with fresh gas at a rate of 2 L/min, semi closed or open gas administration |
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Term
| Propofol: use, who to be careful using with, MOA, Side effects |
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Definition
**cause of Michael Jacksons death
This is the most common induction agent of general anesthesia in the US
Not water soluble (may be dissolved in vegetable oil) very fatty, must be used with caution in patients with high triglyceride levels
--Patients discharged faster than other GAs, lack of hangover effects as compared to Na thiopental
-Anti-emetic effects properties, used for patients prone to vomiting
--doesnt cross the placenta so safe for pregnant women
MOA:
Enhance effects of GABA at GABAa inhibitory receptors
Side Effects
Major decrease in blood pressure in BP, vasodilation and decrease myocardial contractility
Pain of injection, reduced with local anesthetic or injecting into a large vessel
Decrease in ventilation rate |
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Term
Etomidate
Use, MOA, Side effects |
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Definition
Etomidate is a non-water soluble general anesthetic drug used for patients at risk for hypotension and used for induction and maintenance of anesthesia
MOA:
-enhance effects of GABA at GABAa inhibitory receptor
-activates GABAa receptor without GABA present
-Metabolized in the liver, metabolites eliminated in urine
Side Effects:
pain of injection, reduced with local anesthetic or injecting into a large vessel
myoclinic movements, benzodiazepines co-administered to prevent
assoc with nausea and vomiting
inhibition of adrenal gland synthetic enzymes
no decrease in BP or CO |
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Term
| Ketamine: Use, MOA and Side Effects |
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Definition
A general anesthetic that PRODUCES PROFOUND ANALGESIA and is used in the battlefield and in veterinary medicine
Like Etomidate, good for pts at risk for hypotension
given oral, rectal and intramuscular
MOA:
competative antagonist of NMDA receptor
inhibition of voltage sensitive Na, K channels...metabolized in liver to norketamine (has further actions on the CNS, rapid clearance
Side effects: no pain of injection
increase cerebral blood flow, no change in brain metabolism
emergence delirium
hallucinations, vivid dreams, illusions
benzodiazepines lessen these effects
**Ventilation-only modest decrease in ventilation rate and is a potent bronchodilator
**Cardiovascular: increase BP, increase CO, increase HR...This makes ketamine useful in pts at risk for hypotension |
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Term
| Midazolam: use, benefit of use |
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Definition
Miazolam is a general anesthetic adjunct...decreases the dose of GA needed to reach desired depth of anesthesia (balanced anesthesia)
Midazolam is water soluble, unlike the benzodiazepines
Midazolam causes no pain on injection, while other benzodiazepines do and they also irritate vessels
Midazolam causes a more rapid onset of anesthesia and a more rapid recovery |
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Term
| Fentanyl: Use, duration of action |
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Definition
| a general anesthetic used in hostage/terrorist action to incapacitate individuals...duration of action 30 min |
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Term
| Dexmedetomidine: Use, MOA, Side Effects |
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Definition
FDA approved for sedation in critically ill adults, off label use as a GeneralAnesthetic adjunct...IV use only, produces no amnesia
MOA: alpha 2 adrenergic agonist...alpha 2 adrenergic receptor activation decreases catecholamine release
Side Effects: decrease in BP, bradycardia..no change in ventilation rate
**USEFUL IN non-intubated patients |
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Term
| Use of Dantrolene, MOA, Sde effects |
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Definition
Dantrolene is used to treat malignant hyperthermia and is a Ryanodine receptor inhibitor (in malignant hyperthermia ryanodine calcium channels in muscles do not close resulting in uncontrolled muscle contraction leading to heat generation
Side effects: muscle weakness and hepatotoxicity--liver function must be tested |
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Term
Depolarizing or Non-Depolarizing NMJ Blocker?
Atracurium |
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Definition
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Term
Depolarizing or Non-Depolarizing NMJ Blocker?
Mivacurium |
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Definition
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Term
Depolarizing or Non-Depolarizing NMJ Blocker?
Pancuronium |
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Definition
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Term
Depolarizing or Non-Depolarizing NMJ Blocker?
Rocuronium |
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Definition
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Term
Depolarizing or Non-Depolarizing NMJ Blocker?
Succinylcholine |
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Definition
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Term
| Class of Local anesthetic: Bupivacaine |
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Definition
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Term
| Class of local anesthetic: Lidocaine |
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Definition
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Term
| Class of local anesthetic: Ropivacaine |
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Definition
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Term
| Class of General Anesthetic: Articaine |
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Definition
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Term
| Class of local anesthetic: Benzocaine |
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Definition
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Term
| Class of Local anesthetic: Cocaine Hydrochloride |
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Definition
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Term
| Neuromuscular Junction Blockers--which are Benzylisoquinonlines and which are steroidal compounds and side effects for each |
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Definition
Describe the non-depolarizing neuromuscular junction blockers. The Benzylisoquinonlines are the "-curium" named ones and the Steroidal compounds are the "-curonium" named ones
Side Effects Benzylisoquinonlines
Histamine release, few vagal/ganglionic blocking effects
Side Effects Steroidal compounds
block of ganglionic muscarinic receptors can occur resulting in tachycardia due to effects on vagus
Rocuronium is a newer agent however with little to no associated tachycardia or histmine release |
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Term
| Mivacurium: what is it? time to onset of action, duration of action, pharmacokinetics/metabolism, who might not want to give to? |
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Definition
This is a Benzylisoquinoline non-depolarizing NMJ blocker
Time to onset of action: 2-4 min
Duration of aciton: 12-28 min
Pharmacokinetics: metabolized by plasma cholinesterase. this is why mivacurium has such a short duration of action
Problems can occur when patients are given mivacurium if there is decreased plasma cholinesterase activity. Patients with liver disease or nutritional deficiencies may have abnormal plasma cholinesterase activity |
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Term
| Rocuronium: Type of drug, how metabolized, time to onset of action, use, duration of action, |
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Definition
| This is a steroidal non-depolarizing NMJ blocker metabolized in liver time to onset of action: very rapid (1-2 min) similar to succinylcholine and used to RAPIDLY relax laryngeal and jaw muscles for tracheal intubation Duration of action 30-90 minutes |
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Term
| Atracurium: What is it? Time to onset of action, duration of action, pharmacokinetics and who might be useful in |
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Definition
Atracurium is a Benzylisoquinoline non-depolarizing NMJ blocker
time to onset of action: 2-4 minutes
Duration of action 30-90 minutes
Pharmacokinetics: degraded by the temperature and PH dependent Hofmann reaction. Since these drugs are not metabolized by enzymes may be useful in patients with liver and or renal failure |
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Term
| Pancuronium: What is it? use, time to onset of action, duration of action, pharmacokinetics, side effects |
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Definition
This is a steroidal non-depolarizing NMJ blocker
Time to onset of action: 4-6 minutes
Duration of action: 120-180 minutes
Use: very old drug that has been around for decades...not used much anymore...2nd drug used in most states lethal injection protocol
Pharmacokinetics: 40% excreted unchanged in urine, therefore pt needs adequate renal function..11%excreted unchanged in bile
Side effects: modest increase in heart rate, BP |
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Term
| Succinylcholine: what is it? Use, time to onset, duration of action, visible effects of the drug, MOA, Pharmacokinetics |
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Definition
Succinylcholine is a DEPOLARIZING NMJ Blocker
Time to onset of action: 1-1.5 minutes (very fast)
Duration of action: 5-8 minutes
use: used for very short procedures (ex: intubation)
The effects of Succinylcholine are characterized by initial fasciculations mostly in the chest and abdomen. these fasciculations are minor twitching of muscles and occur immediately after drug administration
Pharmacokinetics: degraded by plasma choline esterase (butyrylcholinesterase) Problems occur in pts with decreased levels of this enzyme, or those with atypical or deficient plasma cholinesterase, hepatic or liver disease, or nutritional deficiencies
MOA: Succinylcholine alters electrochemical driving forces. normally, positive ions readily enter negatively charged cell interior...excessive opening of nicotinic ACh receptors by SCh results in decreased electro-chemical driving forces and therefore less positive ion entry in presence of ACh resulting in less positive ion entry in presence of ACh resulting in less muscle response to motor neuron activity |
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Term
| Side Effects of Local Anesthetics on the CNS at low concentrations and high concentrations |
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Definition
in general, Local anesthetics cause initial stimulatory effects on the CNS, then depression
@low concentrations: Sleepiness, dizziness, restlessness..lidocaine may produce euphoria
@high concentrations: Nystagmus, shivering..CNS depression, resp. failure leading to death, also restlessness and tremor, leading to tonic-clonic convulsions (Barbituates and Benzos used to treat convulsions) |
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Term
| Side Effects of Local Anesthetics on the Cardiovascular system |
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Definition
At blood concentrations resulting from normal therapeutic doses; minimal changes in electrical excitability, conduction rate, force of contraction
at higher, toxic levels--depression of cardiac excitability, leading to cardiovascular collapse and death
All local anesthetics are vasodilators, except cocaine
Buprivacaine is more cardiotoxic than others and is associated with arrythmias and hypotension |
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Term
| Side Effects of Local Anesthetics on the PNS |
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Definition
| prolonged sensory and motor defecits |
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Term
| Side Effects of Local Anesthetics on the blood |
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Definition
| high doses of prilocaine or benzocaine can result in the conversion of hemoglobin to methemoglobin which doesnt carry O2 |
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Term
| Allergic reactions possible with Local anesthetics |
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Definition
| Allergic reactions are rare but most common in esters..allergic dermatitis, asthmatic attack mostly |
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Term
| Considerations for the use of local anesthetics during pregnancy |
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Definition
| Local anesthetics cross the placental barrier, as a result CNS, peripheral vascular tone and cardiac function can all be affected in the neonate |
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Term
| Use and benefits of use: Lidocaine |
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Definition
Lidocaine is the most widely used Local anesthetic
Used for infiltration, nerve block, spinal, epidural, topical, and intravenous anesthetic |
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Term
|
Definition
This is a local anesthetic with a LONG duration of action
Used for infiltration, nerve block, spinal, and epidural anesthetic...more sensory than motor block so it is useful in providing analgesia during labor
Not recommended for intravenous injection due to its cardiotoxic potential |
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Term
| Ropivacaine: What is it and use? |
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Definition
Ropivacaine is a newer, long acting amide local anesthetic that is the first local anesthetic that is a pure enantiomer
Has less lipophillic action compared to bupivacaine so there is less effect on myelinated motor neurons resulting in less effect on motor neurons **useful for procedures where motor block is undesireable (ex: labor anesthesia) |
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Term
| Articaine: uses, benefit of use, duration of action |
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Definition
Articaine is an amide local anesthetic approved in 2000 by the FDA which has quickly become the LA of choice for dentists supplanting prilocaine
Articaine is safer than prilocaine because it is rapidly metabolized to an inactive metabolite by plasma carboxyesterase only 5-10% is metabolized in the liver
Duration of action is 1 hour |
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Term
| Benzocaine: use, toxicity, pharmacokinetics |
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Definition
Benzocaine is used topically for suraface anesthesia..
Toxicity dur to methemoglobin production, but low toxicity in general
it is poorly water soluble and not well absorbed |
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Term
| Cocaine Hydrochloride: use, toxicity, what might increase cardiac toxicity |
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Definition
Cocaine Hydrochloride is used for topical use only..the drug is well absorbed via mucous membranes and has a high abuse potential...this is the only local anesthetic with vasoconstrictive properties
Toxicity is low if applied topically but include nervousness, convulsions and cardiac failure
Co-administration with epinephrine is unnecessary and may increase cardiac toxicity |
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Term
| Generally, what size axon is blocked first with local anesthetics |
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Definition
| neurons with small axons are the first to be blocked (ex: C fibers that convey pain sensation) Large neurons (ex: motor neurons) are the last to be blocked |
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Term
| Class of Combination Oral contraceptive: Ethinyl Estradiol |
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Definition
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Term
| Class of Combination Oral contraceptive: Levonorgestrel |
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Definition
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Term
| Class of Combination Oral contraceptive: Desogestrel |
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Definition
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Term
| Class of Combination Oral contraceptive: Drospirenone |
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Definition
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Term
| Class of Combination Oral contraceptive: Etonogestrel |
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Definition
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Term
| Class of Combination Oral contraceptive: Norgestimate |
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Definition
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Term
| Class of Combination Oral contraceptive: Norgestrel |
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Definition
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Term
| Class of Combination Oral contraceptive: Norethindrone |
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Definition
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Term
| Class of Combination Oral contraceptive: Medroxyprogesterone |
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Definition
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Term
| Class of contraceptive: ethinyl estradiol plus norelgestromin (Ortho Evera) |
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Definition
| Topical-transdermal system |
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Term
| Class of contraceptive: ethinyl estradiol plus etonogestrel |
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Definition
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Term
| Class of Oral contraceptive: Micronor, Norethindrone tablets |
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Definition
| Progestin-only contraceptive |
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Term
| Class of Oral contraceptive: Depo-Provera Medroxyprogesterone acetate |
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Definition
| progestin only contraceptives |
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Term
| Class of Oral contraceptive:Implanton Etonogestrel |
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Definition
| progestin only contraceptives |
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Term
| progestin only contraceptives |
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Definition
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Term
| Class of Contraception: Paraguard-Copper |
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Definition
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Term
| Class of Contraception: Mirena-Levonorgestrel |
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Definition
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Term
| Class of Contraception: One tablet levonorgestrel 1.5mg |
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Definition
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Term
| Class of Contraception: Ulipristal acetate (Ella) |
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Definition
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Term
| Class of contraception: 2 tablets of levonorgestrel at 0.75mg each |
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Definition
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Term
How Applied? Risk of Pregnancy? Who is it less effective in?
Topical - Transdermal System
Ortho Evra- ethinyl estradiol (0.75mg) + norelgestromin (6mg)/20 cm2 |
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Definition
-Placed on abdomen, buttocks, upper arm or torso
-Patch placed on first day of menses and replaced every week for 3 weeks, then removed for 4th week so bleeding can occur.
Falls off >1day →start a new system & use backup contraception for 7 days
1 pregnancy per 100 women yrs of use
Less effective > 90 kg (~198 lbs)
***Use of this patch increases exposure to ethinyl estradiol and norelgestromin compared to COCs, and thus Increased hormone exposure → concerns about thromboembolism |
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Term
How to use, Risk of pregnancy with use, pt complaints with use
NuvaRing ethinyl estradiol (0.015 mg) + etonogestrel (0.12 mg)/24hours ethinyl estradiol (2.7mg) + etonogestrel (11.7 mg)/Ring |
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Definition
The ring can be inserted prior to the 5th day of the menstrual cycle and stays inserted for 3 weeks..after 3wk remove and have period
1-2 pregnancies per 100 women yrs of use
Complaints of foreign body sensation
Ring can pop out
Out > 3 hrs → back up contraception until ring has been in place for 7 days |
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Term
Who might want to use? How to use? what to do if take pill late? Inhibit ovulation? rate of pregnancy with use, side effects
Progestin only contraceptive pills |
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Definition
Progestin only pills are used in women with some contraindications for estrogen (Age, smoking, thromboembolism)
OR *****Used when women are lactating and want contraception
There are no pill-free days → start taking pills on first day of menstruation and take continuously AT THE SAME TIME EACH DAY
3 hr late taking pill use backup contraception for 48 hours
Don’t consistently inhibit ovulation (~40% cycles are ovulatory)...therefore other mechanism of contraception must be occurring with these drugs...such as
↑ viscosity of cervical mucous → ↓ sperm migration,
Inhospitable environment for ovum implantation
~3 pregnancies per 100 women years of use
Sex Hormones & Gonadotropins Part 1: Contraceptives
Progestin Only Preparations
Adverse effects
Menstrual irregularities – unpredictable spotting
Weight gain |
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Term
how administered? Rate of pregnancy with use? Risks of use?
Progestin Only Preparations
Depo-Provera® contraceptive
Medroxyprogesterone acetate 150 mg/mL |
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Definition
Progestin Only Preparations
Depo-Provera® contraceptive
Medroxyprogesterone acetate 150 mg/mL
IM injection into the gluteal or deltoid every 3 months..IM injections should occur within 5 days of the beginning of menstrual bleeding
~1 pregnancy per 100 women years of use
medroxyprogesterone acetate levels Inhibit ovulation in most pts
Pts using medroxyprogesterone have ↓ [estrogen] → bone loss--****pts at risk for osteoporosis should consider other contraceptives!
**Most frequent adverse effects: Menstrual irregularities – unpredictable spotting
Other adverse effects: WEIGHT GAIN, breast tenderness, HA, depression, nervousness, ectopic pregnancy |
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Term
Pros/Cons over reg Depo-Provera?
Depo-subQ Provera 104® contraceptive
Medroxyprogesterone acetate 104 mg/mL |
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Definition
(progestin only)
Depo-subQ Provera 104® contraceptive
Medroxyprogesterone acetate 104 mg/mL
Subcutaneous injection allows for self injection
More expensive than Depo-Provera, • $100 per injection while Depo-provera is $10/injection |
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Term
How to use?
Implanon (Etonogestrel) |
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Definition
Progestin Only Preparations
Implanon (Etonogestrel)
A rod containing etonogestrel is placed under skin (subdermal) and releases drug over time. The rod must be replaced at or before the end of the third year of implantation. |
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Term
How to use, MOA, pregnancy rate with use, Risks of use
Intrauterine devices
ParaGuard - intrauterine Copper release
Mirena -Levonorgestrel – intrauterine 52 mg |
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Definition
Not popular forms of birth control in USA
Dalkon shield pulled from market in 1974 ~ tubal scarring, infertility & pelvic inflammatory disease (PID)
Inserted by a health care provider
ParaGuard: left in place for ~10 years
Mirena: release progestin for ~5 years
Produce a low grade inflammation that ↑ prostaglandins → spermicidal
Paraguard: prevent fertilization, prevent implantation, interfere with sperm transport and viability
Mirena: thick cervical mucous, ↓ sperm transport & activity, inhospitable endometrium, preventing ovulation
Pregnancy rates:
Paraguard: 0.6 – 0.8 pregnancies per 100 women years of use
Mirena: 0.1 pregnancies per 100 women years of use
Adverse effects:
Insertion may introduce bacteria into the genital tract → PID
PID risk ~1 - 2.5% and occurs ~ 20 days after insertion
Insertion of the devices must be done by a trained and experienced professional |
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Term
How to take? Effectiveness? MOA? Adverse side effects?
Plan B kit
One tablet of levonorgestrel 1.5 mg
Ella
Ulipristal acetate 30 mg
Next Choice
2 tablets of 0.75 levonorgestrel 0.75 mg each |
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Definition
Emergency contraception = Morning after pill
Must be taken within 120 hours after intercourse
75% - 98% effective in reducing pregnancy
MOA – Not well understood (delay in ovulation, Decreased endometrial receptivity, Altered transport of sperm, egg or embryo)
Adverse side effects:
Nausea and vomiting – if vomiting occurred within 1-3 hours, then tablet must be taken again
Prescribe an antiemetic |
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Term
| What Class of Drug? Conjugated equine estrogens (0.625 mg) Premarin |
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Definition
| ERT and HRT Replacement Therapy: Oral administration estrogen pills |
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Term
| What Class of drug? Conjugated equine estrogens + medroxyprogesterone acetate Prempro |
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Definition
| ERT and HRT Replacement Therapy: Estrogen and Progestin Pills |
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Term
| Class of Drug: Raloxifene Hydrochloride |
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Definition
| Selective Estrogen Receptor Modulators (SERMS) and Anti-Estrogens |
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Term
| Class of Drug: Clomiphene |
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Definition
| Selective Estrogen Receptor Modulators (SERMS) and Anti-Estrogens |
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Term
| Class of Drug: Leuprolide acetate |
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Definition
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Term
| Class of Drug: menotropins (Pergonal) |
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Definition
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Term
| Class of Drug? recombinant FSH preparations-Follitropin alpha; Follitropin Beta |
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Definition
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Term
| Class of Drug: chorionic gonadotropin |
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Definition
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Term
| Class of Drug: recombinant HCG-choriogonadotropin alfa |
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Definition
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Term
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Definition
| Topical--Transdermal Androgen and antiandrogen |
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Term
| Class of Drug? Finasteride |
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Definition
| 5-alpha reductase inhibitors |
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Term
| Class of Drug: Dutasteride |
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Definition
| 5-alpha reductase inhibitors |
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Term
| Pharmacodynamics of Raloxifene |
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Definition
| Raloxifene acts as an estrogen agonist in bone and inhibits the proliferation of pro-osteoclastic cells, increases expression of anti-osteoclastic factors and decreases teh expression of bone-resorbing cytokines and as such it exerts an anti-resorptive effect. Raloxifene therapy is not associated with endometrial proliferation or increased risk of breast cancer and it has estrogenic effects on lipid metabolism |
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Term
| Therapeutic uses of Raloxifene |
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Definition
Raloxifene is used to prevent osteoporosis in postmenopausal women....Raloxifene-treated patients show increases in total bone mineral density of 1.3-2% and raloxifene may decrease vertebral fracture by 50%
Raloxifene should be used with other pharmacological (Vitamin D) and non pharmacological (weight bearing exercise) measures to prevent osteoporosis |
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Term
| Adverse effects of Raloxifene |
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Definition
MAJOR EFFECTS
1.) Vasomotor symptoms (hot flashes)..starts in the first 6 months
2.) Thromboembolism (~3x greater risk).. occurs during first 4 mo of therapy
OTHER EFFECTS
3.) Breast pain
4.) nausea
5.) musculoskeleta
6.) CNS depression and insomnia
7.) Respiratory--sinusitis, bronchitis, pharyngitis, cough, pneumonia |
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Term
| Drug interactions with Raloxifene |
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Definition
| Abx can kill off normal microbial flora resulting in decreased enterohepatic recirculation of raloxifene |
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Term
| Contraindications to Raloxifene use |
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Definition
-active or past episodes of venous thrombosis
-drug shouldnt be used during periods of prolonged immobilization (e.g.: recovery from surgery) due to risk of thromboembolism |
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Term
| Pharmacodynamics of Clomiphene Citrate |
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Definition
Clomiphene citrate has potent enti-estrogenic activity (trans isomer) and weak estrogenic activity (cis isomer) and binds to ERalpha and ER beta
Clomiphene inhibits the negative feedback effects of estrogen at the hypothalamic and pituitary level...therefore, therapy with Clomiphene promotes the release of FSH and LH which promotes the maturation of an ovarian follicle, ovulation, adn the generation of the corpus luteum |
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Term
| Therapeutic uses of Clomiphene citrate |
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Definition
| Female infertility: induce ovulation in anovulatory women who want to become pregnant |
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Term
| Toxicity, Adverse reactions, and contraindications to use of Clomiphene Citrate |
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Definition
1.) Hot flushes-most common side effect
2.) Multiple ovulations with pleural pregnancies
3.) Ovarian enlargement and cyst formation are the most common side effects
4.) Visual-Blurren vision, photophobia, avoid bright light
5.) Ovarian cancer-prolonged use may be associated with increased risk of ovarian cancer
other--nausea, vomiting, increased urinary frequency
Contraindications: liver disease, preexisting ovarian cyst, contraindicated during pregnancy due to teratogenic effects in rats and rabbits |
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Term
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Definition
1.) Prostate cancer: The GnRH agonist Leuprolide is used for the palliative treatment of advanced stage D2 (tumor with metastases to lymph nodes, bone, and/or viscera) androgen-dependent prostate cancer. **When a GnRH agonist is used there will be a transient increase in sex hormone concentrations especially in the first couple weeks of therapy. This could be problematic since there could be an increase in tumor growth during this period.....combined therapy with an antiandrogen might alleviate this problem
2.) Endometriosis: Leuprolide produces a reversible hypoestrogenic state--dont use long term because can decrease bone density
3.) Percocious Puberty--Drug of choice for treating central precocious puberty--goal is to prevent rapid sexual maturation, prevent early menarche in females and achieve a normal adult height--discontinued at age 11 in females and age 12 for males |
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Term
| Adverse Effects of Leuprolide |
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Definition
In general Leuprolide is well tolerated and many of the side effects reflect the endocrine effects of the drug:
****hot flashes and night sweats are teh most prequent adverse effect
-decreased bone density in women
-vaginal dryness and atrophy
-impotence and decreased libido in men
-increased bone pain in pts with prostate cancer during first 1-2 weeks of therapy
-immediate allergic reactions |
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Term
| Menotropins: What are they? how to prevent adverse reactions with them? |
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Definition
| Menotropins are LH and FSH isolated from the urine of postmenopausal women. Due to low purity, menotropins are administered IM rather than subcutaneously to prevent hypersensitivity reactions |
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Term
| Uses of Menotropins in males and females |
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Definition
females: Menotropins are used sequentially with chorionic gonadotropin to induce ovulation in infertile anovulatory women with hypogonadotropic hypogonadism but to hypothalamic or pituitary dysfunction
Males: Menotropins can be used with chorionic gonadotropin to stimulate spermatogenesis in males with hypogonadotropic hypogonadism |
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Term
| Adverse effects of Menotropins |
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Definition
Ovarian enlargement is the most frequent adverse effect. Patients may experience abdominal distension and pain which usually goes away 2-3 weeks after treatment...more rarely-ovarian hyper stimulation syndrome=sudden ovarian enlargement and ascites
**Plural gestations (mostly twins) due to multiple ovulations |
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Term
What are they? Pros/Cons over Menotropins,
Follitropin alpha, Follitropin Beta |
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Definition
These are 2 recombinant FSH preparations that are made by expressing cDNA clones for the alpha and beta subunits in mammalian cells. The two products differ in the structure of their carbohydrate structures...The recombinant drugs are more expensive than menotropins, but they can be administered SUBQ since they are more pure than menotropins
; used to treat infertility in women and increase spermatogenesis in men
unclear if greater efficacy or decreased side effects from menotropins |
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Term
What is it? How standardized? How administered? how distributed in body? Pharmacokinetics?
Chorionic gonadotropin |
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Definition
Chorionic Gonadotropin is obtained from the urine of pregnant women. The activity of Chorionic gonadotropin is standardized by its ability to increase the weight of an immature female rat uterus compared to a chorionic gonadotropin reference std.
Administered IM and distributed mostly to tested and ovaries...
Concentrations decline in a biphasic manner with the half life of the initial phase being about 11 hours and the half life of th esecond phase being about 23 hours..drug is excreted in urine |
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Term
| Uses of Chorionic gonadotropin |
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Definition
1.) Treatment of Prepubertal cryptochidism--CG can be used to promote testicular descent
2.) Used to promote spermatogenesis
3.) Used topromote ovulation in anovulatory infertile women |
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Term
| Adverse effects of Chorionic gonadotropin |
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Definition
CG is generally well tolerated...might see:
-HA, irritability, restlessness, depression, fatigue, and edema
-precocious puberty in males taking CG for cryptochidism--if this occurs discontinue use
**Ovarian hyperstimulation and multiple pregnancies |
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Term
How made? Use?
Choriogonadotropin Alfa |
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Definition
| Choriogonadotropin Alfa is produced in mammalian cells using recombinant DNA technology. It is different from urinary derived CG mainly in the carbohydrate moiety. It can be used for ovulation induction by SUBQ injection |
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Term
| Benefits of Androderm over oral testosterone or IM testosterone injections |
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Definition
| Androderm is a topical/Transdermal testosterone prep and provides a more stable serum testosterone concentration vs. IM injections |
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Term
| Adverse Effects of high levels of androgens (testosterone) |
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Definition
When testosterone is administered as a transdermal prep (Androderm) or IM as an ester that get hydrolyzed to testosterone, as long as dose not excessive, no adverse effects other than the normal effects of testosterone in healthy adults
When taken at high enough dose all androgens can supress gonadotropin secretion which will supress endogenous testicular function and cause testicular atrophy
High doses of androgens can cause erythrocytosis
The 17alpha alkylated androgens have adverse effects even at doses targeted for physical replacement... the adverse hepatic effects include: cholestasis, blood filled hepatic cysts and more rarely hepatic cancer....large amounts may also decrease HDL and increase LDL
when a man has normal serum testosterone for many years and is over 40 he is more prone to testosterone-dependent diseases such as benign prostatic hyperplasia and prostate cancer |
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Term
| Finasteride and Dutasteride: what are they? What used to treat? |
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Definition
Finasteride and Dutasteride are competative inhibitors of the type 2 5alpha reductase enzyme, and thus block the conversion of testosterone to dihydroterstoserone... Finasteride inhibits the Type 1 enzyme while Dutasteride inhibits the type 2 enzyme
These drugs are used to treat BPH since they block the conversion of testosterone to the more potent dihydrotestosterone in the male reproductive system....they can cause a decrease in prostate size and an increase in urine flow in pts with BPH and also can cause impotence in men
Finasteride is also used for the treatment of male pattern baldness |
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Term
| Main action on the body: Oxytocin |
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Definition
| Stimulates uterine activity |
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Term
| Main action on the body: PGE2 (Dinoprostone) |
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Definition
| Stimulates uterine activity |
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Term
| Main action on the body: PGE1 analog (Misoprostol) |
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Definition
| Stimulates uterine activity |
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Term
| Main action on the body: Ergonovine Maleate/Methylergonovine Maleate |
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Definition
| Stimulates uterine activity |
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Term
| Main action on the body: Mifepristone |
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Definition
| Stimulates uterine activity |
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Term
| Main action on the body: Terbutaline sulfate |
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Definition
| Inhibits uterine activity |
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Term
| Main action on the body: Magnesium sulfate |
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Definition
| Inhibits uterine activity |
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Term
| Main action on the body: Prostaglandin-Synthetase Inhibitors (Indomethacin) |
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Definition
| Inhibits uterine activity |
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Term
| Physiological Production of Oxytocin |
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Definition
Oxytocin is produced as a prohormone my magnocellular neurons in the supraoptic and paraventricular nuclei of the hypothalamus. The neurons that produce oxytocin send axonal projections to the posterior pituitary....
Sensory stimuli (stretching) from the cervix, vagina, and breast causes the release of oxytocin from these nerve terminals into the circulation
oxytocin may also be produced locally in the uterus at the time of partuition |
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Term
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Definition
Oxytocin binds to oxytocin receptors in the myometrium and endometrium....activation of these receptors on myometrial Smooth muscle cells increases intracellular calcium which leads to the activation of myosin light chain kinases which promotes actin-myosin interactions. The net effect is to cause CONTRACTION of myometrial smooth muscle
Activated oxytocin receptors in the endometrium stimulate prostaglandin production...these prostaglandins also stimulate uterine contractions by increasing myometrial intracellular levels
The sensitivity of the uterus to oxytocin increases as gestation progresses...this increased sensitivity is thought to be due to an estrogen-induced increase in the number of oxytocin receptors, and also to elevated levels of oxytocin at the time of parturition |
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Term
| Indications for use of oxytocin for labor induction |
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Definition
--if continuation of the pregnancy presents a risk to the mother, fetus, or both
--premature rupture of membranes
--Erythroblastosis fetalis (HDN--anemia, jaundice, edema)
--Antepartum bleeding
--placental insufficiency (DM, pre-eclampsia, eclampsia)
--prolonged pregnancy (42 weeks) |
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Term
| Influence of oxytocin on breast tissue |
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Definition
Oxytocin stimulates contraction of myoepithelial cells in the breast which forces milk from the alveoli of the breast (milk letdown/ejection)
Oxytocin has been used for inadequacy of breastfeeding by intranasal administration 2-3 minutes before feeding. not useful if inadequate milk production is the problem |
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Term
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Definition
| in high-risk pregnancies, oxytocin can be administered to test for fetal respiratory capabilities |
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Term
| Uses of oxytocin besides induction pregnancy, breastfeeding, and oxytocin challenge test |
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Definition
Oxytocin may reduce postpartum hemorrhage following delivery of the fetus and placenta
Oxytocin can also be used with hypertonic urea or Dinoprostone for inducing abortions |
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Term
| Toxic, adverse effects, and contraindications for the use of Oxytocin |
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Definition
-Decrease in systolic and diastolic BP, increased heart rate, and arrhythmia
-Antidiuretic effect and hyponatremia secondary to water retention--Vasopressin V2 receptor mediated event....Esp seen with prolonged infusion of excess amounts of IV fluid
--sustained uterine contractions can interfere with fetal circulation (oxytocin challenge test)---but not sooo risky to use because oxytocin has a short half life and thus you can just stop the IV infusion
--Contraindicated for labor induction with abnormal fetal position, fetal distress/placental abnormalities, and previous uterine surgery |
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Term
| PGE2 (Dinoprostone) Use, MOA, mode of administration |
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Definition
PGE2 stimulates uterine contractions and causes sofetening and dilation of the cervix (cervical ripening)
MOA for cervical ripening appears to be due in part to increased secretion of the enzyme collagenase...like oxytocin, dinoprostone can also stimulate uterine contractions by causing an increase in myometrial intracellular free calcium
Cervical gel containing Dinoprostone is supplied in a syringe with a catheter for intravaginal administration to the cervical canal to induce cervical ripening..if there is no cervical ripening with the first dose a second dose may be given after 6-12 hours..***This product is used to induce cervical ripening in cases where labor is going to be induced with oxytocin ***also avaliable are Dinoprostone vaginal inserts
Intravaginal suppositories of Dinoprostone are used to induce second trimester abortions and also to expel uterine products |
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Term
| Toxic and adverse effects. and contraindications for use of PGE2/Dinoprostone |
|
Definition
-GI disturbances are the most commonly reported side effects and include symptoms such as nausea and vomiting...pts can be premedicated with an antiemetic and antidiarrheal
--Uterine hyperstimulation contractions lasting greater than 2 min or greater than 5 contractions within 10 minutes
--other potential adverse effects: transient temp elevation, HA, chills, hot flashes, transient decrease in diastolic BP, cardiac arrythmias, wheezing, cough and chest pain
Contraindications for the use of PGE2 for inducing cervical ripening include abnormal fetal position, fetal distress/placental abnormalities, previous uterine surgery |
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Term
| Use of 15-methyl PGF2alpha (Carboprost Tromethamine) |
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Definition
IM administration can be used to control postpartum bleeding that doesnt respond to oxytocin or ergot alkaloids
IM administration can be used to induce abortion in the second trimester --esp useful when fetal membranes are ruptured but the uterine contents have not been eliminated |
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Term
| Use of PGE1 analog (Misoprostel) |
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Definition
| can be used with the antiprogestin Mifepristone RU 486 for early termination of pregnancy Misopristel is administered 2 days after administration of Mifepristone RU486 to induce contractions and expulsion of the products of conception--it is also used for labor induction and postpartum hemorrhage |
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Term
| Use: Ergot Alkaloids Ergonovine Maleate and Methylergonovine Maleate |
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Definition
These amine ergot alkaloids induce intense contractions of the uterus---were originally used in the 1800s in the USA to facilitate childbirth...However, it was soon recognized that use of ergot alkaloids increased the # of stillborn kids
TODAY:
The ergot alkaloids should NOT be used for the induction or augmentation of labor
They might be used for: postpartum or postabortion hemorrhage |
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Term
| MOA: Ergot Alkaloids Ergonovine Maleate and Methylergonovine Maleate |
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Definition
| The ability of ergot alkaloids to stimulate uterine contractions appears to be due to the ability of these compounds to activate alpha 1 adrenergic receptors located in the myometrium of the uterus |
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Term
| Toxic, adverse effects, and contraindications of ergot alkaloids |
|
Definition
Ergot alkaloids can cause hypertension due to vasoconstriction (methylergonovine preferred because it produces HTN less frequently)
-Contraindicated with hypertension and cardiovascular disease, hepatic and renal disease
--can cause nausea, vomiting, and diarrhea, and seizures, and gangrene of the fingers and toes |
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Term
| Class of Anticancer drug: Mecholrethamine |
|
Definition
| Alkylating agent--Nitrogen Mustard |
|
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Term
| Class of Anticancer drug: Cyclophosphamide |
|
Definition
| Alkylating agent--Nitrogen Mustard |
|
|
Term
| Class of Anticancer drug: Carmustine |
|
Definition
| Alkylating agent-Nitrosourea |
|
|
Term
| Class of Anticancer drug: Cisplatin |
|
Definition
| Alkylating Agent-Platinum Complexes |
|
|
Term
| Class of Anticancer drug: Methotrexate |
|
Definition
| Antimetabolite-Folic Acid Analog |
|
|
Term
| Class of Anticancer drug: Mercaptopurine |
|
Definition
| Antimetabolite--Purine Analog |
|
|
Term
| Class of Anticancer drug: Fluorouracil |
|
Definition
| Antimetabolite--Pyrimidine Analog |
|
|
Term
| Class of Anticancer drug: Cytarabine |
|
Definition
| Antimetabolite-Cytarabine |
|
|
Term
| Class of Anticancer drug: Daunorubicin Hydrochloride |
|
Definition
|
|
Term
| Class of Anticancer drug: Doxorubicin Hydrochloride |
|
Definition
|
|
Term
| Class of Anticancer drug: Vinblastine Sulfate |
|
Definition
| Vinca Alkaloids, Epipodophylotoxins, and Taxanes |
|
|
Term
| Class of Anticancer drug: Vincristine Sulfate |
|
Definition
| Vinca Alkaloids, Epipodophylotoxins, and Taxanes |
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Term
| Class of Anticancer drug: Etoposide |
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Definition
| Vinca Alkaloids, Epipodophylotoxins, and Taxanes |
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Term
| Class of Anticancer drug: Paclitaxel |
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Definition
| Vinca Alkaloids, Epipodophylotoxins, and Taxanes |
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Term
| Class of Anticancer drug: Prednisone |
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Definition
| Hormonal Agent: Andrenocorticosteroid |
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Term
| Class of Anticancer drug: Dexamethasone |
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Definition
| Hormonal Agent: Andrenocorticosteroid |
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Term
| Class of Anticancer drug: Tamoxifen |
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Definition
| Hormonal Agent: Estrogens and Antiestrogens |
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Term
| Class of Anticancer drug: Imatinib Mesylate |
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Definition
| Tyrosine Kinase Inhibitor |
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Term
| Class of Anticancer drug: Trastuzumab |
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Definition
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Term
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Definition
| non-specific drug chelator, limits drug absorption, not as efficacious if the drug is rapidly absorbed (ex: alcohol) |
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Term
| Use: Polyethylene glycol (PEG 3350) |
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Definition
Used in Whole bowel irrigation in balanced electrolyte solution
This is very useful when the ingestion of a drug occurs that is poorly absorbed by activated charcoal (ex: lithium) |
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Term
MOA, S/S:
Organophosphates |
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Definition
Organophosphates all act as IRREVERSIBLE acetylcholine esterase inhibitors
S/S: miosis, HA, nausea, dizziness, loss of muscle control, SLUD (salivation, lactrimation, urination, defacation), constant depression, mental confusion, acute fatigue, blurred vision
Eventual respiratory failure due to diaphragm muscle paralysis and central depression of resp. centers in CNS can also cause bronchoconstriction. Unknown MOA for behavioral effects |
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Term
| Treatment of organophosphate poisoning |
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Definition
Pralidoxime (2-PAM)
This acts to reactivate cholinesterase enzymes (mostly outside of the CNS)...must be given at time of exposure to be effective! |
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Term
| Methanol: Sources, S/D, MOA |
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Definition
Methanol is found in windshield wiper solvent for cars also found in mixed solvents (paint removers)
s/s: CNS depression like ethanol
MOA: metabolized to formaldehyde by alcohol dehydrogenase (ADH) to formate by aldehyde dehydrogenase leading to--blindness, metabolic acidosis |
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Term
| Treatment of methanol poisoning |
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Definition
Metabolic acidosis with Na bicarbonate IV....Folic acid B vitamin complex, converts formate to CO2 and H2O, preventing blindness!
ADH inhibitors: *****FOMEPIZOLE***
can also give ethanol--this reduces toxic metabolite production because it out competes methanol at the ADH enzyme |
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Term
| Ethylene Glycol-sources, S/S |
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Definition
Ethylene Glycol is found in auto antifreeze adn other industrial solvents
S/S: CNS depression like ethanol...the metabolites are more toxic with ethylene glycol being metabolized eventually to oxalic acid...Oxalic acid has high affinity for calcium causing hypocalcemic tetany. When calcium is bound to oxalic acid the result is crystal formation. Renal injury occurs as these crystals pass thru the renal tubules and eventually end up in urine. When crystals present in urine it is called oxalicaciduria and is indicative of ethylene glycol exposure |
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Term
| Treatment of Ethylene Glycol poisoning |
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Definition
Treat hypocalcemia with Calcium IV
also treat with pyridoxine, folate, thiamine--cofactors for ethylene glycol metabolism...also with ADH inhibitors such as Fomepizole*** and also ethanol works to out compete ethylene glycol at the ADH enzyme |
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Term
| Source, S/S Diethylene Glycol |
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Definition
Source: Improperly used as a low-cost substitute for glycerin and propylene glycol in pharmaceutical products...also as an industrial solvent
S/S: nausea, ANURIC RENAL FAILURE, hepatitis, pancreatitis |
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Term
| Treatment: Diethylene Glycol poisoning |
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Definition
| Treat with supportive and symptomatic care---important to obtain EARLY diagnosis to prevent multi organ failure |
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Term
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Definition
Sources of Lead: contaminated food (chocolate from factories), ingestion of paint chips, inhalation of lead dust, contaminated drinking water, toys from other countries, gasoline, occupational exposure
S/S:
Blood: hypo chromic microcytic anemia
PNS: weak wrist or ankle extensor muscles
CNS: lead encephalopathy
GI: colic, loss of appetite
Kidney: increased uric acid-gout
Reproductive: stillbirths in women, decreased sperm count and motility
MOA: Believed to mimic and replace endogenous ions--"molecular mimicry"
Lead is very effective at inhibiting Hgb synthesis resulting in anemia and a buildup of precursors of Hgb, esp protoporphyrin |
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Term
| Treatment of lead poisoning |
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Definition
For severe cases where blood levels are very high (greater than 25ug/dl in kids and >50ug/dl in adults), metal chelators are given with SUCCIMER being the first line drug and EDTA the second line. The steroidal anti-inflammatory drug dexamethasone can be given for cerebral edema
**kids are mor susceptible than adults to the toxic effects of lead. Approx 10% of ingested inorganic lead is absorbed in adults. However, up to 40% of ingested lead is absorbed in kids. The BBB deteriorates with Pb exposure, more so in kids who dont have a fully formed BBB!!!---Childhood Pb exposure is associated with low IQ, increase in ADHD, aggressive behavior, and juvenile delinquincy |
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Term
| Sources, S/S, MOA: ARSENIC |
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Definition
Sources: contaminant of coal, metal ores, rural/muicipal water supplies in the US but especially in Bangledesh where "tube wells" were dug in the 1980s...occupational exposure can occur in industrial workers in semiconductor industry and CPU manufacturing
SS:
ACUTE: hemorrhagic gastroenteritis (rice water diarrhea), violent nausea, laryngitis, bronchitis, garlic odor on breath, capillary damage (dehydration, shock, death)...if pt survives-sensory neuropathy folllows
CHRONIC: insidious and irreversible before S/S start to show...hyperkeratosis exfoliative dermatitis, vesicular lesions on the feet, peripheral neuropathy, cutaneous vasodilation "Milk and Roses" complexion, BM depression, fatty liver degeneration, increased risk of skin, liver, lung, kidney, and bladder cancers
MOA: High affinity for -SH groups..Likely causes severe oxidative stress and disrupts protein function by binding to -SH containing AA |
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Term
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Definition
| Lead has a short 1/2 life in soft tissue, but the 1/2 life in bone is from years to decades!!! |
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Term
| Methylmercury: Sources, S/S |
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Definition
Sources: consumption of contaminated fish and grain fungicide, metal in old dental labs, old thermometers, gold mining...used as medical specimen preservatives, insecticides...making felt hats (Mad HAtters)
S/S: Methylmercury readily causes neurotoxicity in particular in the cerebellum=cerebellar ataxia and movement disorders are common in people with MeHG exposure. also loss of balance, sensory deficits, loss of visual field, deafness, dysarthria---all are irreversible |
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Term
| Prevention of Methylmercury poisoning |
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Definition
people should eat no more than 1 serving of swordfish or shark or other predatory fish per week....Women who are nursing or preggers should avoid consuming ALL predatory fish species, due to the teratogenic effects of MeHg
in one study, co-administration with Selenium significantly reduced neurotoxic effects of MeHg |
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Term
| Use and MOA in general: Metal Chelators |
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Definition
| Metal Chelators are used only in pts with highly elevated levels of metal or severe toxicity. Chelators bind metals then the metal/chelator complex can be excreted form the body. Chelation therapy only reduces the readily accesible pool of metal...After chelation therapy ends...blood metal levels can rebound! |
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Term
| Calcium EDTA: how administered, side effects, controversy |
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Definition
Calcium EDTA is given IV or IM for severe lead poisoning. it is toxic to the kidney at high doses...side effects include chills, fever, nausea, vomiting, allergies...
Controversial use in chelation therapy to produce general detoxification of various metals, lack of selectivity, blood levels of metals rebound after discontinuation of therapy.
Rapid and severe hypocalcemia can occur if disodium EDTA is given by mistake. |
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Term
| Succimer: how administered, uses, side effects |
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Definition
Succimer is the first orally effective metal chelator
it is more rapidly effective than EDTA for lead, also may be useful for treating mercury and arsenic poisoning
Side Effects: GI distress, rash, diarrhea, increase in serum transaminases |
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Term
| Carbon Monoxide: sources, S/S, MOA, treatment |
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Definition
Carbon Monoxide can be produced from any burning or combustion process...in the fall when home furnaces are turned on the furnace fume vent may have become plugged due to animal activity and houses can thus fill with lethal levels of CO!! it is colorless, odorless, tasteless, nonirritating and ubiquitous
S/S: organs with the greatest oxygen demand will show signs of CO exposure first (Headache, dizziness, and increased heart rate)...chronic exposure=possible cardiovascular problems
MOA: out competes O2 binding to Hgb....220x greater affinity than oxygen. In addition, CO when bound to one of the four oxygen binding sites on Hgb forms carboxyhemoglobin...This form of Hgb reduces the ability of oxygen to dissociate from Hgb and be delivered to the deep tissues needing oxygen
Treatement: remove pt from CO environment, then givehyperbaric oxygen |
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Term
| Cyanide: sources, S/S, MOA, Treatment |
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Definition
Sources of cyanide: present in smoke (burning of plastics, wool), industrial exposure (plastics and metal plating) chemical warfare agent
S/S: "bitter almond breath" HA, nausea, tachypnea, apnea, loss of consciousness, seizures, coma
MOA: binds to cytochrome oxidase resulting in the inhibition of the ETC and reduces the ability of the cell to utilize oxygen in producing ATP
Treatment: 2 different ways to treat--if there is a shortage of cyanokits in the ER the "older" method may be used
Older method (2 steps)
-Na nitrite to form methemoglobin--which binds CN- to form cyanomethemoglobin
-Sodium thiosulfate then given to convert cyanomethemoglobin to thiocynate--excreted in urine
--As of 2006 in the US, 1 step-can be given if cyanide exposure is suspected regardless of CO coexposure (**in smoke inhalation, cyanide exposure is often assoc with CO exposure) |
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Term
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Definition
Source: working in or around products that contain asbestos (older buildings)
S/S: no real S/S...Mesothelioma lung cancer may occur 15-20 yrs after exposure, may see pleural plaques (sections of lung scar tissue) and Pleural effusions associated with plural plaques and accumulation of fluid around lung |
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Term
| Sources, S/S: PCBs and Dioxin |
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Definition
Flame retardants, plasticizers, insulating material in electric transformers...farm raised salmon...Dioxin is a contaminant of agent orange and of industrial processes (herbicide and germicide)
S/S: dermal acne-like eruptions called chloracne, nausea, HA, vomiting |
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Term
| Bisphenol A (BPA): Source, S/S, |
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Definition
Sources: leaching from plastic water bottles (with number 7 on bottom), plastic-lined canned food--93% of Americans have BPA in urine
S/S: unknown--possible link to obesity and DM? |
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Term
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Definition
Ternutaline sulfate is a Beta-2 adrenergic receptor agonist
The uterine smooth muscle contains beta-2 adrenergic receptors...when beta2agonists bind to these receptors adenylyl cyclase is activated and cAMP is generated. An increase in cAMP may decrease contraction of smooth muscle by modulating myosin light chain kinase and sequestering intracellular calcium. Failure of these drugs to inhibit uterine contractions may be due to rapid receptor desensitization |
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Term
| Toxic, adverse effects, and contraindications for Terbutaline sulfate |
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Definition
Terbutaline sulfate is a bets2-adrenergic receptor agonist
1.) Fetal and maternal tachycardia (reflex response to lowered diastolic pressure and direct action on Beta1 receptors in the heart)
2.) Maternal pulmonary edema--increased risk with co-administration of a corticosteroid
3.) Mathernal hyperglycemia...use w/ caution in pts with DM |
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Term
| Use, MOA, adverse effects: Magnesium sulfate |
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Definition
Magnesium sulfate relaxes uterine smooth muscle, although the exact MOA no known...research suggests that Mg can decrease teh levels of myometrial intracellular free calcium and therefore can decrease uterine contractions....if cervical dilation progresses beyond 5cm Mg sulfate is discontinued...
***DRUG of choice in pts with contraindications for using Ritodrine hydrochloride
Adverse effects: flushing, sweating, hypotension, depressed reflexes, hypothermia, cardiac and CNS depression, respiratory paralysis |
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Term
| Indomethacin: MOA, uses, adverse effects |
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Definition
Indomethacin is a prostaglandin synthetase inhibitor--it inhibits the production of prostagalandins which are important for cervical ripening and myometrial contraction.
Uses: Tocolytic agent (stops uterine contractions), to cause closure of ductus arteriosus, to threat painful menstrual cramps associated with primary dysmenorrhea
Adverse effects: pulmonary HTN |
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