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Pharmacology - Drugs of Abuse
DRUGS OF ABUSE
41
Medical
Not Applicable
08/10/2009

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Cards

Term
What is the MoA for cocaine?
Definition
Cocaine blocks the cotransporter involved in the reuptake of catecholamines (DA, NE) and 5-HT.  This leads to increased concentrations of these in the synapse.  Cocaine therefore has a stimulating effect on the CNS. 
Term
What are Schedule I drugs?
Definition

Schedule I drugs are those with a high potential for abuse and have no accepted medical use.

It is illegal to buy, sell, or possess thise drugs!

Ex: Heroin, Mescaline, PCP, LSD, Ecstasy

Term
What are Schedule II drugs?
Definition

Schedule II drugs are drugs that have accepted medical uses (with severe restrictions) and have a high potential for abuse.

 

Ex: Amphetamine (Adderall), Methamphetamine, morphine, oxycodone, Methylphenidate (Ritalin), Nabilone (THC)

Term
What are some effects of cocaine on the cardiovascular system, hunger, fatigue, and mental function?
Definition

Cocaine stimulates the cardiovascular system, producing increased heart rate and blood pressure (recall NE increase!) 
Also remember that NE has vasoconstrictive properties through its actions on alpha-1 receptors.  This can cause ischemic necrosis.  When people snort cocaine, the vasoconstrictive effects cause death of nasal tissue leading to a perforated nasal septum!  It can also cause vasospasms that lead to MI.

 

Cocaine eliminates fatigue and hunger

 

Cocaine may induce schizophrenic behavior (DA) and leads to a state of euphoria (DA reward system) and rapid speech.

Term
What are symptoms of cocaine withdrawal?
Definition

Remember, withdrawal symptoms are opposite to the symptoms of the drug.  Because cocaine is normally stimulatory and euphoria producing, withdrawal will include sleepiness, dysphoria, depression, and bradycardia.

 

For severe withdrawal symptoms, the drug Modafinil may be useful.  It is also used in narcoleptics because it prolongs wakefulness... this will help with the fatigue experienced during cocaine withdrawal.

Term
What drug could help with the sleepiness associated with severe cocaine withdrawal?
Definition
Modafinil prolongs wakefulness
Term
What is the MoA for amphetamines?
Definition
Amphetamines are indirect acting sympathomimetic drugs.  They enter the nerve terminal and displace neurotransmitters into the synaptic space.  This increases the level of the neurotransmitters NE, DA, 5-HT.
Term
What are the uses for amphetamines?
Definition

Amphetamines are used in the pharmacological agents Adderall and Ritalin.  These are used for ADHD prescriptions.

 

As CNS stimulants, amphetamines also find use in narcolepsy treatment (but remember: modafinil can also be used)

Term
What should you do in the case of amphetamine toxicity?
Definition
Because amphetamines are highly basic, making the urine acidic is a useful way to help remove excess drug.  50% of the drug is excreted renally...
Term
What are the effects of amphetamines?
Definition
The effects of amphetamines are similar to those of cocaine, as they both result in increased neurotransmitter in the synapse.
Term
Describe acute amphetamine intoxication
Definition

Acute amphetamine intoxication produces tachycardia, hypertension, confusion, tremors, and euphoria.  Stroke or seizure may occur.

 

Remember, amphetamines are stimulatory (like cocaine) and displace NTs (DA, NE, 5-HT) into the synapse.

Term
What are some drugs with which amphetamines should not be coadministered?
Definition

MAOIs should not be used with amphetamines, as this could precipitate a hypertensive crisis.

 

Adrenergic neuron blockers (antihypertensives) will be counteracted.  So don't give amphetamines to controlled hypertensives on these medications.

 

Hypertensives in general should not use amphetamine, as this will only raise their blood pressure even more.

Term
What is methylphenidate used to treat?
Definition

Methylphenidate is an amphetamine derivative.  It is most commonnly known as Ritalin and is prescribed in cases of ADHD. 

 

It is often abused by students as a neuroenhancer.

Term
What is theophylline?
Definition

Theophylline is a methyl-xanthine.  It is used in cases of respiratory distress, and in cases where opioids have depressed respiration.  (Methyl-xanthines increase the sensitivity of the respiratory center of the medulla to CO2)

 

Methyl-xanthines (caffeine, theophylline) work by blocking the adenosine receptor 

Term
What is the MoA of caffeine or theophylline?
Definition

Caffeine and theophylline are methyl-xanthines, and therefore work by blocking the adenosine receptor.

 

This causes increased cortical arousal, awareness, restlessness.  It increases heart rate.  It also causes diuresis.

Term
What drug of abuse, which has no clinical use, is associated with altered water dynamics, serotonin syndrome risk, heart attacks, and brain hemorrhage?
Definition
Ecstasy
Term
A man tells you he had a bad trip on some acid... what drug did he take?
Definition
LSD (lysergic acid diethylamide)
Term
What drug is also called angel dust?
Definition
(phencyclidine) PCP is known as angel dust
Term

A man jumped from a second story building, breaking his ankle, and continued to run down the street, yelling at passersby and breaking car windows.  Later, in the hospital, he states that he had an "out-of-body" experience.

What drug was he likely on?

Definition

PCP (phencyclidine aka phencyclohexylpiperidine) is a schedule 1 psychotomimetic drug.  It produces vivid dreams, out of body experiences, aggressive behavior, and a lack of pain!

 

It causes both vertical and horizontal nystagmus (a pathognomonic/characteristic sign)

Term
What are effects of LSD?
Definition
LSD (lysergic acid diethylamide) is a psychotropic drug that produces synesthesias.  Synesthesia is the mixing of senses... for example someone might see colors, shapes, and patterns when they hear music...
LSD is known as 'acid'
Term
What are therapeutic forms of cannabinoids?
Definition

Cannabinoids are schedule II drugs and are prescribed for the treatment of nausea related to chemotherapy...cannabinoid receptors (CB-1) are found in the vomiting center..., glaucoma, spasticity, and anorexia. 

 

The therapeutic drugs are Dronabinol and Nabilone

Term
What are side effects of anabolic steroid abuse?
Definition

Anabolic steroids are androgenic-steroids.  Androgens suppress gonadotropin production in a classical negative feedback system.  This decreases testosterone levels, causing a reduction in sperm production and decreased fertility.

 

Eventually, this leads to small testicles

 

Gynecomastia results when the androgens (steroids) are converted to estrogen.

 

Large doses can be hepatotoxic

 

Roid Rage is a behavioral change that results in aggresion in susceptible individuals.

Term
can you list some opioids that are abused?
Definition

Heroin

oxycodone

morphine

methadone

meperidine

 

These are all opioids (pain relievers) that are regularly abused.

Term
What class of drug is flunitrazepam, and what is its most common form of abuse?
Definition
Flunitrazepam is a benzodiazepine.  It is also known as Rohypnol and is abused as a date rape drug (roofies).  This is because it incapacitates people and produces amnesia so that they cannot recall what happened.
Term
What is the normal use of GHB?
Definition

GHB is gamma-hydroxybutyrate.  It is a CNS depressant that is believed to have an inhibitory role in the dopaminergic pathways of the brain.

 

It is a treatment for narcolepsy... recall: can also use modafinil and amphetamines. 

It is also a treatment for cateplexy

Term
How is GHB abused on the street as 'G' ?
Definition

GHB, gamma-hydroxybutyrate, causes intoxication that mimics alcohol intoxication.  It produces euphoria and an increased sexual desire.  Because it causes amnesia, it is also used as a date-rape drug, and is rivaling Rohypnol in this regard.

 

 

 

Term
What is the general strategy behind treatment for overdose toxicity
Definition
For overdoses, give an ANTAGONIST!
Term
What is the general strategy behind treatment for withdawal?
Definition
for withdrawal symptoms, give a CROSS-TOLERANT drug... (a drug that acts at the same receptor, but is not associated with the same toxicities)
Term
What is the treatment for Heroin overdose?
Definition
Heroin is an opioid.  For Heroin overdose, and opioid overdose in general, give Naloxone (Narcan), which acts as an antagonist at the opioid mu receptur.
Term
What drug would you give in the case of benzodiazepine overdose?
Definition
Give Flumazenil, the benzo antagonist in cases of benzodiazepine overdose.
Term

What are signs of opioid overdose?

What do you treat it with?

Definition

Pinpoint pupils, loss of consciousness, decreased respiration leading to cyanosis.  (everything DOWN)

 

Give IV naloxone (Narcan) to treat opioid overdose toxicity.  Give it by IV and slowly to avoid precipitating withdrawal symptoms.  for long half-life opioids like methadone, serial dosing of naltrexone (another opioid antagonist) may be necessary

Term
How would you treat the withdrawal of a chronic opioid abuser?
Definition

Detoxification of opioid abusers involves giving gradually decreasing doses of the opioid agonist methadone.

 

Additionally, you could use clonidine to decrease withdrawal rebound NE release by its actions at a-2 receptors, or a clonidine-naltrexone combination.  In this last option, clonidine acts to prevent the withdrawal that naltrexone would normally precipitate.  Eventually, clonidine is decreased and naltrexone increased.

Term
why is naltrexone a good maintenance drug to give an opioid user after they have been through detox?
Definition
Naltrexone is a long lasting opioid antagonist.  This means that the opioid receptors are blocked and the patient will not be able to get their desired effect even if they do try to abuse opioids again.  Additionally, naltrexone is able to REDUCE CRAVINGS!  Naloxone is not good for maintenance because of its short half life.
Term
Why does Buprenorphine have a higher compliance than naltrexone in opioid mantenance treatment?
Definition
Buprenorphine is a partial agonist at opioid receptors, giving patients some pleasure/reward.  Contrary to this, naltrexone is an opioid antagonist!
Term
What drugs could you prescribe as maintenance therapy to keep patients from abusing opioids again?
Definition

Naltrexone or Buprenorphine are used for opioid maintenance therapy.  Buprenorphine is a partial agonist with a very high affinity for the receptors, thus inhibiting the opiates from binding, even if the patient does try to use them again.

 

Naltrexone is a long-lived antagonist and also reduces cravings.

Term
On opiate withdrawal, what neurotransmitter release is enhanced?
Definition

Norepinephrine

 

opiate action at presynaptic receptors causes decreased NE release.  This upregulates postsynaptic NE receptors.  When opiates are withdrawn, the increased post-synaptic NE receptor density results in an supersensitivity to the effects of NE.  This manifests as an 'adrenergic storm'.  This is why clonidine, which decreases NE release, is useful in opiate withdrawal!

Term
What are some effects of cocaine overdose?
Definition

Cocaine overdose can cause cardiac arrhythmias, tachycardia, hypertension, and seizures.

 

Treat the symptoms with beta and alpha blockers.  Nitroglycerine is useful in cocaine-induced cardiac ischemia. (this is secondary to the vasospastic influence of cocaine on the coronary arteries)

Term
What would you see in barbiturate overdose?
Definition

Barbiturates are CNS depressants.  You would see sedation, reduced BP, cardiac and respiratory depression, and coma.

 

Don't give CNS stimulants to try to fix it, this strangely increases the mortality from barbiturate overdose.  Instead, use a gastric lavage and activated charcoal.  Hemodialysis if necessary.

Term
what drug may be useful to sedate a patient on a bad trip from LSD?
Definition
The classical neuroleptic Chlorpromazine has a strong sedatory quality, and is useful in these circumstances.
Term
What is the treament for overdose, withdrawal, and maintenace in an opioid abuser?
Definition

Overdose = Naloxone (Narcan)

 

Withdrawal = Methadone, clonidine, or clonidine&naltrexone

 

Maintenance = Naltrexone or Buprenorphine

Term
What is the treatment for methanol or ethylene glycol poisoning?
Definition
Use ethanol or fomepizole for methanol/ethylyne glycol poisoning.
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