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Block 5 Drugs (Drugs only)
Uses, Side Effects, considerations
125
Medical
Graduate
03/25/2013

Additional Medical Flashcards

 


 

Cards

Term
Buspirone
Definition

Anti-anxiety drug. Partial 5-HT1a agonist. No sedation, abuse potential, depressant effects. Slow onset and safe in pregnanc

Metabolized by 3A4. 

Term
Fluoxetine
Definition
SSRI. Used for GAD and depression. Most stimulating
SE - sexual dysfunction, bruxism, akathesia (agitation), headache, sedation, weight gain, w/ clozapine or lithium -> seizures. Very long half life
May induce mania in misdiagnosed bipolar pt.
Term
Sertraline
Definition
SSRI. Used for anxiety and depression
SE - sexual dysfunction, bruxism, headache, sedation, weight gain, w/ clozapine/lithium -> seizures
May induce mania in misdiagnosed bipolar pt.
Term
Paroxetine
Definition
SSRI. approved for GAD and depression. most sedating.
SE - sexual dysfunction, bruxism, headache, sedation, weight gain, w/ clozapine or lithium -> seizures
May induce mania in misdiagnosed bipolar pt.
Term
Citalopram
Definition
SSRI. Used for anxiety and depression
SE - sexual dysfunction, bruxism, headache, sedation, weight gain, w/ clozapine or lithium -> seizures
May induce mania in misdiagnosed bipolar pt.
Term
Escitalopram
Definition
SSRI. Approved for GAD and depression
SE - sexual dysfunction, bruxism, headache, sedation, weight gain
May induce mania in misdiagnosed bipolar pt.
Term
Duloxetine
Definition
SNRI. Used for GAD and depression
CI'd in BPH due to urine retention and in hepatic insufficiency.
SE - sexual dysfunction, bruxism, headache, sedation, weight gain
Term
Venlafaxine
Definition
SNRI. Approved for GAD.
Causes HTN at high doses.
SE - sexual dysfunction, bruxism, headache, sedation, weight gain
Term
alprozolam
Definition
BZD. Approved for panic attacks.
Highly lipophilic and metabolized by P450.
SE - CNS depression, anterograde amnesia and respiratory depression.
Term
Clonazepam
Definition
BZD and AED. Approved for panic attacks, ethosuximide/depakote resistant seizures, Lennox-Gastaut, restless legs
Highly lipophilic and metabolized by P450.
SE - CNS depression, anterograde amnesia, respiratory depression, children -> congestions and behavioral problems, withdrawal -> status epilepticus
Term
Diazepam
Definition
BZD. Used for anxiety, epilepsy (seizures), and chronic spasms. Very long acting.
Highly lipophilic and metabolized by P450. indicated in first line treatment of status epilepticus and febrile seizures
SE - CNS depression, anterograde amnesia and respiratory depression.
Term
Lorazepam
Definition
BZD and AED. along w/ diazepam, DOC for status epilepticus. Preferred for elderly and post menopausal women. Highly lipophilic and metabolized by P450.
SE - CNS depression, anterograde amnesia and respiratory depression.
Term
Oxazepam
Definition
BZD. Preferred for elderly and post menopausal women. Short acting
Highly lipophilic and metabolized by P450.
SE - CNS depression, anterograde amnesia and respiratory depression.
Term
Triazolam
Definition
BZD. Short acting. Used to induce sleep.
Highly lipophilic and metabolized by P450.
SE - CNS depression, anterograde amnesia and respiratory depression.
Term
zolpidem and zaleplon
Definition
BZD receptor agonists.
fast onset w/ T1/2 4-6 hrs.
Only used for short term insomnia treatment
CI'd in elderly pts b/c increase confusion
Term
Fentanyl
Definition
Strong Opioid
Term
Hydromorphone
Definition
Strong Opioid
Term
Oxymorphone
Definition
Strong opioid
Term
Meperidine
Definition
Strong opioid
Term
Methadone
Definition
strong opioid
Term
Morphine sulphate
Definition
strong opioid
Term
Oxycodone
Definition
strong opioid
Term
Heroin
Definition
strong opioid
Term
Codeine
Definition
moderate opioid
Term
Hydrocodone
Definition
moderate opioid
Term
Buprenorphine
Definition
partial agonist
Used for outpatient detoxification
Term
Vicodin/Lortab
Definition
moderate opioid
Term
Vicoprofen
Definition
moderate opioid
Term
Percocet
Definition
moderate opioid
Term
loperamide
Definition
weak opioid
Term
Diphenoxylate
Definition
weak opioid
Term
Dextromethorphan
Definition
weak opioid
Term
Tramadol
Definition
weak opioid also inhibits serotinin and norepi reuptake -> CI'd w/ antidepressants Low dependence and not completely antagonized by naloxone.
Term
Pentazocine
Definition
opioid agonist/antagonist
Mu antagonist and kappa agonist.
Only benefit is no respiratory depression.
Term
Nalbuphine
Definition
opioid agonist/antagonist
Mu antagonist and kappa agonist.
Only advantage is lack of respiratory depression.
Term
Butorphanol
Definition
opioid agonist/antagonist
Mu agonist and kappa antagonist
doesn't cause respiratory depression
Term
Naloxone
Definition
opioid antagonist
binds to all receptors but is strongest at the mu receptor. Duration 1-2 hours.
Term
Naltrexone
Definition
oral form of naloxone
Long half life (48 hours)
highly hepatotoxic
Term
Endorphins
Definition
endogenous opioids that bind to mu receptors
Term
Dynorphins
Definition
endogenous opioid that binds to the kappa receptors
Term
Enkephalins
Definition
endogenous opioid that binds to the delta receptors
Term
Tapentadol
Definition
Opioid. synthetic drug w/ modest mu activity. Inhibits uptake of norepi.
basically same as tramadol
Term
imipramine
Definition
TCA. Used for depression and enuresis. has anticholinergic, sedative, orthostatics, QT prolongation, weight gain, sexual dysfunction, enhances insulin/hypoglycemic effects. Long Half lives
Term
desipramine
Definition
TCA. orthostatics, QT prolongation, weight gain, sexual dysfunction, enhances insulin/hypoglycemia. Long half life
Term
Amitriptyline
Definition
TCA. Treats depression or neuropathic pain. Anticholinergic, highly sedative. QT prolongation, orthostatics, weight gain, sexual dysfunction, enhances insulin/hypoglycemics. Long half lives
Term
Nortriptyline
Definition
TCA. orthostatics, QT prolongation, weight gain, sexual dysfunction, enhances insulin/hypoglycemics, long half lives.
Term
desvenlafaxine
Definition
SNRI (mixed NE and 5-HT rekuptake inhibitor). Same SE as SSRI's except more minor. However, increased risk of serotonin syndrome. May cause HTN.
Don't give w/ stimulants, things that increase 5-HT.
Short half lives but long tissue life
Term
phenelzine
Definition
MAO A and B irreversible inhibitor. Treat depression after other treatments fail.
SE - orthostatics, insomnia, weight gain, sex dysfuncion, anticholinergic, overdose -> convulsions
Phenelzine is a/w hepatotoxic damage.
Tyramine induced HTN crisis
Don't give w/ stimulants, things that increase 5-HT.
Short half lives but long tissue life
Term
tranylcypromine
Definition
MAO A and B irreversible inhibitor.
Treat depression after other treatments fail.
SE - orthostatics, insomnia, anticholinergics, weight gain, sexual dysfunction, overdose -> convulsions
Tyramine induced HTN crisis.
Don't give w/ stimulants, things that increase 5-HT.
Short half lives but long tissue life
Term
Selegiline
Definition
MAO B inhibitor. Used for treatment of parkinsons disease. Can be safely combined w/ sinemet or as monotherapy in early/mild PD. If used in higher dose, will inhibit MAO A. Selegiline is metabolized to amphetamine
Don't give w/ stimulants, or things that increase 5-HT.
Short half lives but long tissue life
Does not cause HTN crisis like non selectives do
Term
Buproprion
Definition
aka wellbutrin. atypical anti-depressant
Blocks NE and Dopamine reuptake.
NE increase treats depression and increased DA is for smoking cessation
SE - headache, and CNS DA effects ->hallucinations, delusions, catatonia, delirium.
CI'd w/ MAOIs -> HTN crisis
Advantages over SSRI -> no weight gain, drowsiness or sexual dysfunction
Term
Nefazodone
Definition
atypical antidepressant. 5-HT2 and 5-HT1 autoreceptor antagonist
SE - orthostatics, dizziness, light headedness, hepatotoxic. Thus is CI in elderly
Strong inhibitor of 3A4.
Term
Mirtazapine
Definition
Atypical Anti-depressant.
structurally a TCA but acts like an a2 autoreceptor antagonist -> increase 5-HT and NE concentration.
SE - MC is muscarinic effects, weight gain, somnolence, agranulocytosis is rare.
Avoid MAOs b/c of HTN crisis
Term
Lithium
Definition
Treats acute mania, DOC bipolar, adjunct in depression Mimics Na but can't be pumped out -> depolarization
Depletes inositol in the brain, decreases GSK3
Oral absorption good w/ full body distribution. 24 hr half life.
increased reabsorption in Na depleting diuretics and NSAIDs --> toxicity. Flip side - volume depleting diuretics -> increase Li excretion
SE - nephrogenic DI, CI'd in preg, N/V/D, abd pain, sedation, acne, alopecia, WEIGHT GAIN. If severe -> confusion, hyperreflexia, seizure, coma/death
Term
Valproic acid
Definition
anticonvulsant. Na and Ca channel blocker and GABA T inhibitor. DOC in kids w/ grand mal and petite (aka abscence). Backup drug for acute mania
Milder SE than lithium but only good for a few weeks.
Li is still used for maintenance
The only established anti-epileptic that does not induce p450!!! It inhibits it instead.
SE - **Hepatotoxicity** (measure LFTs), GI, CNS depression effects,weight gain, suicidal behavior, hypersensitivity reaction, birth defects
Term
Carbamazepine
Definition
anti-convulsant. Na sodium channel blocker. Used for all partials, TC, neuralgia and w/ Li in bipolar or acute mania
SE milder than Li. Intoxication -> coma, resp depression. possible a/w blood dyscrasia
SE - induces p450 -> autometabolism thus needed adjustment in first weeks of treatment, similar structure to TCA -> CI'd along w/ MAOI, fluid retention -> hyponatremia, teratogenic, TEN and SJS a/w HLA-B1502
Term
Oxcarbazepine
Definition
AED. same as carbamazepine except has less autometabolism but w/ more fluid retention and hyponatremia.
Term
Phenobarbital
Definition
barbituate w/ anti-seizure activity, prolongs duration of GABA-a opening
Used in FEBRILE SEIZURES IN CHILDREN and status epilepticus
SE - sedation, hypersensitivity, habit forming, behavioral problems in children, agitation, overdose -> respiratory depression, coma, death
Term
Primidone
Definition
prodrug of phenobarbital
Term
Phenytoin
Definition
Anti-epileptic. (all partials and TC)
Use dependent block of Na channels
saturable metabolism -> toxicity -> measure levels!!!
SE - induces p450, Nystagmus, vertigo, ataxia, blurred vision, gingival hyperplaxia, hirsutism, rash, hyperglycemia and osteomalacia, cleft palate, heart malformations
Term
Ethosuximide
Definition
Anti-epileptic and T Type Ca channel blocker to treat abscence seizures as monotherapy BUT may exacerbate TC and complex partial seizures, so use depakote instead
SE - induces p450, N/V, weight loss
Term
Lamotrigine
Definition
Atypical Anti-epileptic blocks Na channels. approved monotherapy for partial seizures, Lennox-Gastaut, and bipolar
SE - hypersensitivity reactions, thrombocytopenia, hepatotoxicity, sedation.
Term
Topiramate
Definition
Anti-epileptic
Use dependent block of Na channels
Term
Zonisamide
Definition
anti-epileptic.
Use dependent block of Na channels and Ca channel inhibitor (N and T type) Thus, useful in absence seizures, partial seizures, bipolar, and migraines
SE - sulphur allergies, hyperthermia, aplastic anemia, renal stones
Term
Mephobarbital
Definition
a barbituate that has been shown to have anti-seizure effects
Term
Levetiracetam
Definition
approved for TC, partial and myoclonic in children >6 as monotherapy
Non known hypersensitivity reactions
commonly used in pregnant women
unknown MOA
Term
Gabapentin
Definition

AED and spasmolytic (used in MS). analog of GABA, crosses BBB (and placenta) but no GABA mimetic effects. Potentiates GABA. Inhibits GABA-T. GI absorption is saturable. excreted in urine unchanged

 

Term
Felbamate
Definition
similar to phenytoin.
Limited use to Lennox-Gastaux in children, adjunct in partial seizures
BLACK BOX WARNING FOR HEPATOTOXICITY
Term
Tiagabine
Definition
atypical anti-epileptic.
Blocks GABA reuptake to increase GABA effectiveness.
Used for partial seizures.
SE - dizziness and tremors
Term
Levodopa (L-Dopa)
Definition
converted to dopamine via AAD aka dopa decarboxylase.
The dopamine made in periphery -> N/V, and CV effects.
Term
carbidopa
Definition
inhibits peripheral AAD, does not cross BBB and reduces all the side effects of L-dopa alone
Term
sinemet
Definition
combination L-Dopa and carbidopa. MC prescribed TID 25/100 (C/L). if GI symptoms persist, increase carbidopa. relief typically lasts 2.5 years
SE - more common w/ higher doses -> N/V, hypotension from vasodilation, arrhythmias, dyskinesia, somnolence. Schizo symptoms, confusion, insomnia, nightmares (treat w/ atypical antipsycotics). Mydriasis and increase IOP
CI'd - psychosis, narrow angle glaucoma, PUD.
w/ non specific MAOI -> HTN crisis
Long term complications: on/off phenomena and dyskinesia during "on" period(irreversible)
Term
Bromocriptine
Definition
1st gen ergot alkaloid DR agonists. Used to treat parkinsons. Strong D2 and weak D1 agonism.
Initial treatment -> hypotension, nausea and fatigue. start on low dose
Term
Pergolide
Definition
1st gen ergot alkaloid DR agonist
no longer on the market due to damage to cardiac valves
Term
Cabergoline
Definition
Treats parkinsons. 2nd gen ergot alkaloid agonist. Specific to just the D2 receptor. single dose lasts for days
Term
Ropirinole
Definition

Treats parkinsons. selective D2 receptor agonist. Faster titration and effects. treatment is effective quickly w/in 1 week

SE - hallucinations and somnolence Metabolized by p450 -> dose adjustment typically used in younger pts w/ parkinsons

Term
Pramipexole
Definition
Treats parkinsons. non-selective D2 receptor agonist. Faster titration and effects. Selective for D2
SE - hallucinations and somnolence
Excreted unchanged -> dose adjust in renal pts
Typically used in younger pts w/ parkinsons
Term
Apomorphine
Definition
Used as rescue in off episodes in parkinsons. non-selective D2 receptor agonist. Faster titration and effects. Can be given SubQ.
High affinity for D4
Used as rescue therapy during off episodes.
SE - high potential for N/V -> must pretreat w/ trimethobenzamide. DO NOT USE 5-HT3 ANTAGONISTS (ONDASETRON) -> hhypotension
Term
Entacapone
Definition
COMT inhibitor used in parkinsons. blocks peripheral conversion of L-Dopa to 3-o-methyldopa
Adjunct to sinemet to reduce wearing off and on/off effects.
short duration, no incidence of hepatotoxicity
Term
Tolcapone
Definition
COMT inhibitor used in parkinsons. Blocks peripheral and central COMT
Adjunct to sinemet to reduce wearing off and on/off effects
longer duration than entacapone
SE - nausea, orthostatics, confusion, hallucination, HEPATOTOXICITY (monitor).
Only used as last line
Term
Diphenhydramine Hydrochloride
Definition
benadryl. a muscarinic receptor antagonist to turn down Ach activity in PD. used as rescue in parkinsons
Useful in early PD or as adjunct.
Reduces tremor more than bradykinesia
SE-sedation, confusion, blurred vision, constipation, urinary retention
also used for treatment of acute EPS in psychosis treatment w/ typical anti-psychotics
Term
Amantadine
Definition
anti-viral that is now used to block NMDA receptors preventing excitotoxicity a/w parkinsons.
Used as initial therapy for mild PD
SE - dizziness, lethargy, sleep disturbance, anti-cholinergic, N/V.
Term
Chlorpromazine
Definition
Typical anti-psychotic thus -> potent D2 blocker, effective against + symptoms, significant EPS (dystonia, akathisia, parkinsons like, dyskinesia) and hyperprolactinemia
Term
Perphenazine/Fluphenazine
Definition
Typical anti-psychotic thus -> potent D2 blocker, effective against + symptoms, significant EPS (dystonia, akathisia, parkinsons like, dyskinesia) and hyperprolactinemia
Term
Haloperidol
Definition
Typical anti-psychotic thus -> potent D2 blocker, effective against + symptoms, significant EPS (dystonia, akathisia, parkinsons like, dyskinesia) and hyperprolactinemia
Term
Clozapine
Definition
5-HT2a blocker w/ mild D2 block. Treats - symptoms best. Minimal EPS and hyperprolactinemia. SE-known to cause seizures,cardiac arrhythmias and fatal neutropenia (must monitor CBC)
Only used if pt failed 2 other drugs and has dyskinesia and severe EPS.
opposite effect on salivation -> sialorrhea
Term
Risperidone
Definition
5-HT2a blocker w/ mild D2 block. Commonly used for acute psychotic breaks. Treats - symptoms best. Minimal EPS and hyperprolactinemia
Term
Olanzapine
Definition
5-HT2a blocker w/ mild D2 block. MC used during acute psychotic break Treats neg symptoms best. Minimal EPS and hyperprolactinemia. known to cause seizures
Term
Quetiapine
Definition
5-HT2a blocker w/ no D2 block. Treats psychoses in PD. Treats neg symptoms best. Minimal EPS and hyperprolactinemia but more sedation and orthostatics
Term
Ziprasidone
Definition
5-HT2a blocker w/ mild D2 block. Treats - symptoms best. Minimal EPS and hyperprolactinemia. SE - known to cause cardiac arrhythmia in at risk pts. Less weight gain than usual.
Term
Aripiprazole
Definition
5-HT2a blocker, mild 5-HT1a and D2 agonist, and some SSRI. Used as adjunct treatment for depression. Treats - symptoms best. Minimal EPS and hyperprolactinemia. Biggest advantage -> minimal weight gain. Black box warning - increased risk of stroke and MI in dementia patients.
Term
Thiopental
Definition
only barbituate still used.
Highly lipophilic (and what is the point of lipophilicity in anesthetics?
Duration-5 min b/c redistribution. Prone to accumulation. given as an alkali (the point? flush iv lines). narrow TW -> CV depression
Term
Propofol
Definition
Administered IV. onset w/in 30 sec. Rapidly metabolized -> no hangover. Low N/V. CV and resp depression possible. Only IV anesthetic that can be used for maintaining anesthesia.
Term
Etomidate
Definition
similar to thiopental w/ less CV depression. Down side -> very nauseating, involuntary movements, adrenocortical suppression
Term
Ketamine
Definition
Block NMDA. 1-2 min onset, good analgesic. causes dissociative anesthesia.
SE- can raise ICP and cause hallucinations
Term
Isoflurane
Definition
open K channels. Very common. Can lead to myocardial ischemia and has low respiratory irritation potential.
Strongly potentiates NMJ blockers
Term
Desflurane
Definition
Open K channels. Rapid onset/recovery and respiratory irritant -> cough/spasm
Term
Sevoflurane
Definition
may lead to fluoride in the kidney but no real proof. no respiratory irritation. Similar to desflurane (meaning fast induction/recovery)
Term
Nitrous Oxide
Definition
Block NMDA. Always given with oxygen good analgesic w/ low potency (need high levels) Used as an anesthesia adjunct, for preg woman and childbirth. Chronic use a/w -> fetal toxicity, and Vit B12 def symptoms (neuropathy, tinnitus, numbness) SE - increases cerebral blood flow -> CI'd in high ICP, expands air filled cavities -> CI'd in bowel obstruction, pneumothorax, middle ear/sinus disease, eye procedures
Term
Halothane
Definition
old. not used. hepatotoxicity
Term
Dantrolene
Definition
used in treatment of malignant hyperthermia and chronic spasms (via blocking the ryanodine receptor) along w/ electrolyte, acid/base, and temp control. What two drugs are known to cause malignant HTN?
Term
Enflurane
Definition
older drug similar to halothane w/ less hepatic metabolism and toxicity. May cause seizures and malignant HTN
Term
Cocaine
Definition
Local anesthetic. Blocks dopa reuptake in midbrain -> reward. Only local anesthetic w/ vasoconstriction properties via blocking NE uptake.
Term
Chlorprocaine
Definition
local anesthetic. tends -> neurotoxicity in continuous spinal block
Term
Tetracaine
Definition
commonly used for spinal and corneal anesthesia
Term
Bupivacaine
Definition
local anesthetic w/ slow onset but long duration. No longer used in obstetrics b/c death if injected into epidural vein. These veins enlarge during pregnancy.
H/w, widely used for infiltration. Slightly higher cardiotoxicity
Term
Lidocaine
Definition
Use dependent Na channel blocker
Term
Lidocaine
Definition
LA. DOC for digitalis induced arrhythmias. Neurotoxic if used for spinal block
Some CNS effects
Term
Mepivacaine
Definition
local anesthetic. has less vasodilation so can be used w/o epi.
Term
Prilocaine
Definition
Commonly used. h/w tends to cause accumulationof o-toludine -> methhemoglobinemia and can cause methhemoblobinemia in neonates. Blood looks black and pt is cyanotic. Tx w/ iv ??
Term
Methylene Blue
Definition
treats methhemoglobinemia
Term
Succinylcholine
Definition
a depolarizing NMJ blocker. Phase 1 - nicotinic agonist -> fasciculations. Phase 2 - Ca back into SR -> relaxation and paralysis b/c it stays around. AchI's will worsen phase 1.
two AcH attached together.
metabolized peripherally but not by the Achesterase in the NMJ. Rapid onset w/ short duration.
SE - post-op muscle pain, hyperkalemia, decrease HR, increase IOP, possible malignant hyperthermia (do you remember the tx for it?
Term
Pancuronium
Definition
Long acting non-depolarizing NMJ blocker
liver metabolism and renal clearance.
Fewer SE. only slight tachycardia. No hypotension
Term
atracurium
Definition
Non-depolarizing NMJ blocker. short acting (30 min).
SE - histamine release, hypotension, accumulation of toxic metabolites formed from Hoffman's elimination.
Term
cistracurium
Definition
Commonly used non-depolarizing NMJ blocker. onset fastest (1-3 min)
SE - similar to atracurium w/ less hypotension, histamine release, and toxic metabolites
Term
rocuronium
Definition
Non-depolarizing NMJ blocker.
Fast onset.
Liver metabolism and renal clearance
SE - may cause muscarinic block
Term
tubocurarine
Definition
Non-depolarizing NMJ blocker
Renal elimination
SE - hypotension from ganglion block, Most likely NMJ blocker to cause histamine release -> bronchoconstriction
Term
baclofen
Definition
a GABA-B agonist in the spinal cord used for treatment of chronic spasms. also closes Ca channels and decreases Substance P release.
Term
Tizanidine
Definition

analog of clonidine used in the treatment of chronic spasms.

SE - drowsiness and hypotension

Term
Botulinum Toxin
Definition
Anti-spasmotic
injected into muscles
Used in cerebral palsy
MOA - prevents synaptic vesicle fusion/release
Term
Cyclobenzaprine
Definition

Spasmolytic. used for acute muscle spasms from injury. For example, a pulled muscle. acts in the brain stem to inhibit polysynaptic reflexes.

Not effective in spasms from spinal injury or cerebral palsy

SE - if combined with SSRI/SNRI -> serotonin syndrome, highly sedative and anti-muscarinic. 

Term
Metaxalone
Definition

acute spasmolytic. for relief of discomfort w/ acute painful MSK conditions. Effects CNS, not periphery

SE - drowsiness, dizziness, and irritability

Term
Carisoprodol
Definition

aka soma.

Acute spasmolytic. treats muscle spasms and promote sleep MOA not known and don't be on other depressants CI'd- elderly b/c CNS affects

Term
Methocarbamol
Definition
treats spasms in acute painful MSK conditions. ex tetanus. relaxation is via CNS depression. SE - fowsy, dizzy, hypotension, syncope CI'd - renal impairment.
Term
Flumazenil
Definition
competitive antagonist of BZD receptor. Used as the antidote for BZD overdose.
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