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75 Cards in this Set
- Front
- Back
what is the effect of barbiturates?
mechanism? |
•generalized CNS depressant
•binds GABA-a receptor ⇒ ↑duration of GABA action •also ↑Cl- influx to ⇒ inhibition *independent of GABA* |
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what are the SEs of barbiturates?
how do you treat OD? |
•↓ respiratory drive
•↓ BP (w/ OD) •porphyria •tx OD w/ urine alkalinization |
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what are the CIs for barbiturates?
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porphyria
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what are other uses for phenobarbital (besides CNS depression)?
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partial seizures, generalized tonic-clonic seizures
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how do the benzodiazepines act?
how does this compare to barbs? |
•facilitate GABA - bind specific receptor assoc. w/ GABA-a complex
•benzo acts ONLY when GABA is present; much safer than barbs |
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what are the uses for benzos?
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•anxiolytic (DOC)
•acute mm relaxation at high dose (diazepam) •alcohol & barb w/d •status epilepticus •DTs- diazepam, chloridiazepoxide, lorazepam |
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what are the long & short acting benzos?
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long acting:
•diazepam •chlordiazepoxide •flurazepam short acting: •midazolam •triazolam |
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which benzo is given IV?
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midazolam
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what are the CIs of benzos?
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pregnancy (teratogenic), kids & elderly, sleep apnea, with alcohol, caution in recovering addicts
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what are the effects of flumazenil?
what drugs can cause seizures in combo w/ flumazenil? |
•benzo antagonist; also reverses effects of the "z drugs"
•seizures possible w/ benzo, barb, alcohol dependence, epilepsy, and TCA OD |
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what are the pharmacokinetics of zolpidem & zaleplon?
what are the possible adverse effects? |
•very rapid action, very short half life
•may cause sleep behaviors - walking, driving, eating |
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how is eszopiclone different from zolpidem & zaleplon?
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•eszopiclone has longer half life
•also can have w/d after chronic use |
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what class is ramelteon?
how does it work? |
•melatonin analogue
•binds MT 1&2 receptors •NO EFFECT on GABA-a |
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what is buspirone?
what are its effects? |
•partial agonist at 5-HT1A
•acts as anxiolytic w/o sedation |
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how does alcohol act?
how is it metabolized? |
•binds GABA-a receptor complex
•inhibits NMDA receptor •metabolized by alcohol dehydrogenase first, followed by aldehyde DH •zero order kinetics |
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what happens w/ chronic alcohol use?
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•induce CYP2E1
•long term use down-regulates GABA & up-regulates NMDA •pharmacodynamic & pharmacokinetic tolerance •other effects: gastritis, hepatotoxicity, FAS, wernicke, korsakoff, cardiomyopathy |
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what are the drug interactions for alcohol?
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tylenol ⇒ liver toxicity
(others: benzos, barbs, phenothiazines, TCAs) |
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how do you treat alcohol w/d?
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•benzos
•also phenytoin, antipsychotics, ibuprofen |
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what is naltrexone?
what is the bad SE? |
•opioid receptor antagonist
•reduces craving (block reward pathway) •causes liver damage |
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what is acamprosate?
what makes it a good choice? |
•restores GABA & glutamate balance in alcoholic
•good choice b/c NO liver toxicity |
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how does disulfiram act?
how long do its effects last? |
•blocks aldehyde dehydrogenase
•must avoid all sources of alcohol •3-4 day effects |
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how does fomepizole act?
what are its uses? |
•blocks alcohol dehydrogenase
•used to treat methanol & ethylene glycol poisoning |
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how does you treat methanol or ethylene glycol poisoning?
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•fomepizole - blocks alcohol DH
•or use alcohol to compete for the enzyme |
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what class is imipramine?
how does it act? uses? |
•TCA
•inhibits reuptake of NE & 5HT •also blocks alpha1, histamine, and muscarinic receptors •now used for chronic pain •analgesia of spinal cord |
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what are major SEs of TCAs?
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•weight gain
•↓seizure threshold •SIADH •sexual dysfunction •sedation (antihistamine) •anticholinergic, esp. impaired memory/cognition •alpha1 postural hypotension ***torsades w/ OD |
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what are the drug interactions for TCAs?
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•MAOIs ⇒ severe CNS toxicity, serotonin syndrome
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what class is desipramine?
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•TCA
•2° amine, so less sedation than imipramine |
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what class is phenelzine?
what are the SEs? |
•MAOI
•HTN crisis when combined w/ tyramine from many foods - tx w/ alpha block •also get muscarinic block |
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what are the drug interactions of phenelzine?
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meperidone, dextomethorphan (OTC cold), TCAs, SSRIs (serotonin syndrome)
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what are the sx of serotonin syndrome?
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•CNS toxicity
•hyperpyrexia •restlessness •mm twitch •can be fatal |
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what class is fluoxetine?
long or short duration of action? what are the SEs? |
•SSRI w/ a long duration of action
•GI - nausea, loss of appetite •sexual disinterest •SIADH |
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what drugs inhibit CYP2D6?
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•fluoxetine
•duloxetine (moderate) |
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what 3 drugs are SNRIs?
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venlafaxine
desvenlafaxine duloxetine |
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how does venlafaxine act?
SEs? |
•blocks uptake of both NE & 5HT
•similar to TCA w/o muscarinic or alpha block •may ↑BP |
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what are the uses and SEs for trazodone?
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•pain management
•significant sedation •priapism** |
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how does bupropion act?
SEs? |
•inhibits DA reuptake (no effect on 5HT, minor on NE)
•may cause wt loss •few sexual SEs (can combine w/ SSRI) •anxiety, insomnia, seizures |
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st johns wort interactions?
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•used OTC for mild depression
•do not combine w/ other antidepressants •reduced efficacy of protease inhibitors, OCP, digoxin, warfarin |
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how does chlorpromazine act?
side effects? |
•inhibits D2 receptors to inhibit + sx of schizophrenia
•extrapyramidal sx- parkinson like •tardive dyskinesia •weight gain •↑prolactin •alpha, muscarinic, histamine block •↓sz threshold •jaundice •neuroleptic malignant syndrome |
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what drug causes neuroleptic malignant syndrome?
how do you treat? |
chlorpromazine
tx w/ dantrolene |
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how to treat EPS?
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anticholinergic
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major SE of thioridazine?
|
retinal deposits
|
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how does haloperidol act?
major SEs? |
•selective D2 receptor blockade
•no anticholinergic activity •highest incidence of EPS •highly sedating |
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how does clozapine act?
what is its advantage? major SE? |
•"atypical" antipsychotic
•block D4 & 5HT2A receptors •advantage: very rare to get EPS or tardive dyskinesia •major issue: agranulocytosis |
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class and major SE of risperidone?
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•"atypical" antipsychotic
•prolongs QT interval •may ↑ mortality in Alzheimer's |
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class and major SEs of olanzapine?
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•"atypical" antipsychotic
•weight gain ***the WORST for hyperglycemia |
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uses and SEs for quetiapine?
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•"atypical" antipsychotic
•used for sedation, antidepressant adjunct •SEs: weight gain, extreme sedation •little effect on prolactin, no agranulocytosis |
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how does aripiprazole act?
major uses & SEs? |
•DA & 5HT-1A partial agonist
•used for schizophrenia & depression ***↓esophageal motility also, no effect on prolactin, QT, weight, or EPS |
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pharmacokinetics of lithium?
interactions? |
•excreted by kidneys
•narrow therapeutic range •things that ↓Na will ↑Li -- thiazides •NSAIDs will ↓Li clearance •interactions: antidepressants, antipsychotics, thiazides, NSAIDs, sodium |
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how to treat DI?
what drug can cause it? |
•amiloride
•caused by lithium |
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signs for Li toxicity?
how to treat lithium OD? |
•N/V, tremor
•infuse Na |
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what are the use & SEs for valproic acid?
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•good for multiple seizure disorders
•liver toxicity, weight gain |
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how does topiramate act?
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•acts on Na channels
•not as teratogenic as the other anticonvulsants |
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how does phenytoin act?
uses? major SE? |
•prolongs inactivation of Na channels
•used for partial sz, generalized tonic-clonic sz •narrow therapeutic range ***gingival hyperplasia |
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what is the DOC for partial seizures?
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carbamazepine
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uses for carbamazepine?
SE? |
•DOC for parial sz
•tonic-clonic •trigeminal neuralgia **idiosyncratic blood dyscrasias |
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use and SEs for gabapentin?
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•neuropathic pain
•drowsiness & weight gain •pregnancy category C |
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how does ethosuximide act?
use? SE? |
•reduces low threshold Ca current in thalamic neurons
•DOC for absence sz •can cause SJ syndrome (rare) |
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how does levodopa act?
SEs? |
•↑DA levels by replacement
•readily crosses BBB and is converted to DA in neuron •see peripheral effects in 80% - N/V, vasodilation |
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how does carbidopa/levodopa act?
SEs? |
•carbidopa inhibits DA decarboxylase, but is unable to cross BBB
•prevents the peripheral conversion of l-dopa •can still get some GI effects (N/V) •dyskinesias develop w/ time •may cause psychosis |
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what class is selegiline?
how does it act? use? SE? |
•MAOI
•inhibits MAO-B, reducing striatal metabolism of DA •can help w/ on/off phenomenon •fewer food interactions than phenelzine •may cause insomnia |
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what is bromocriptine used for?
what is the SE? |
•on/off periods
•erythromelagia - red, swollen feet |
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what drug class is pramipexole?
what is the major SE? |
•DA agonist
•may cause sudden sleep during the day |
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what class is benzotropine?
how does it act? |
•anticholinergic
•restores DA/Ach balance to help improve rigidity in parkinsons |
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what class is donepezil?
how does it act? major SEs? |
•cholinesterase inhibitor
•increases the amount of Ach in nerve terminal •this is indirect action, so it loses effectiveness as the neurons are lost w/ progression of Alzheimer's •SEs: GI- N/V/D, stomach cramps |
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what class is memantine?
how does it act? use? SE? |
•NMDA receptor antagonist
•may reduce neurotoxic effect of glutamate •Alzheimer's disease •incontinence |
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how does baclofen work?
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•acts as agonist on GABAb receptor
•results in hyperpolarization and inhibition of release of excitatory NT (glutamate) from presynapse in both brain & SC |
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which drug is administered intrathecally?
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baclofen
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what are the uses for baclofen?
SEs? |
•used for chronic spasticity
•SE- some drowsiness |
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what class is cyclobenzaprine?
what major SE? |
•acts as a sedative at the level of the brain stem
•SE- confusion, transient visual hallucinations |
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what is carisoprodol?
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•central sedative activity
•popular drug of abuse |
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what is dantrolene used for?
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malignant hyperthermia
neuroleptic malignant syndrome |
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how does botulinum toxin act?
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blocks release of Ach from presynaptic terminal
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how does methylphenidate act?
uses? |
•promote release of newly synthesized catecholamines
•DA neurons in brain mostly affected •use for narcolepsy and ADHD |
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what are the SEs of amphetamine?
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•NE effects in the periphery
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how does caffeine act?
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blocks adenosine receptors and ↑cAMP by inhibiting PDE
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