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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*
what are the SEs of barbiturates?
how do you treat OD?
•↓ respiratory drive
•↓ BP (w/ OD)
•porphyria
•tx OD w/ urine alkalinization
what are the CIs for barbiturates?
porphyria
what are other uses for phenobarbital (besides CNS depression)?
partial seizures, generalized tonic-clonic seizures
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
what are the uses for benzos?
•anxiolytic (DOC)
•acute mm relaxation at high dose (diazepam)
•alcohol & barb w/d
•status epilepticus
•DTs- diazepam, chloridiazepoxide, lorazepam
what are the long & short acting benzos?
long acting:
•diazepam
•chlordiazepoxide
•flurazepam

short acting:
•midazolam
•triazolam
which benzo is given IV?
midazolam
what are the CIs of benzos?
pregnancy (teratogenic), kids & elderly, sleep apnea, with alcohol, caution in recovering addicts
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
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
how is eszopiclone different from zolpidem & zaleplon?
•eszopiclone has longer half life
•also can have w/d after chronic use
what class is ramelteon?
how does it work?
•melatonin analogue
•binds MT 1&2 receptors
•NO EFFECT on GABA-a
what is buspirone?
what are its effects?
•partial agonist at 5-HT1A
•acts as anxiolytic w/o sedation
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
what happens w/ chronic alcohol use?
•induce CYP2E1
•long term use down-regulates GABA & up-regulates NMDA
•pharmacodynamic & pharmacokinetic tolerance
•other effects: gastritis, hepatotoxicity, FAS, wernicke, korsakoff, cardiomyopathy
what are the drug interactions for alcohol?
tylenol ⇒ liver toxicity

(others: benzos, barbs, phenothiazines, TCAs)
how do you treat alcohol w/d?
•benzos
•also phenytoin, antipsychotics, ibuprofen
what is naltrexone?
what is the bad SE?
•opioid receptor antagonist
•reduces craving (block reward pathway)
•causes liver damage
what is acamprosate?
what makes it a good choice?
•restores GABA & glutamate balance in alcoholic
•good choice b/c NO liver toxicity
how does disulfiram act?
how long do its effects last?
•blocks aldehyde dehydrogenase
•must avoid all sources of alcohol
•3-4 day effects
how does fomepizole act?
what are its uses?
•blocks alcohol dehydrogenase
•used to treat methanol & ethylene glycol poisoning
how does you treat methanol or ethylene glycol poisoning?
•fomepizole - blocks alcohol DH
•or use alcohol to compete for the enzyme
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
what are major SEs of TCAs?
•weight gain
•↓seizure threshold
•SIADH
•sexual dysfunction
•sedation (antihistamine)
•anticholinergic, esp. impaired memory/cognition
•alpha1 postural hypotension

***torsades w/ OD
what are the drug interactions for TCAs?
•MAOIs ⇒ severe CNS toxicity, serotonin syndrome
what class is desipramine?
•TCA
•2° amine, so less sedation than imipramine
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
what are the drug interactions of phenelzine?
meperidone, dextomethorphan (OTC cold), TCAs, SSRIs (serotonin syndrome)
what are the sx of serotonin syndrome?
•CNS toxicity
•hyperpyrexia
•restlessness
•mm twitch
•can be fatal
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
what drugs inhibit CYP2D6?
•fluoxetine
•duloxetine (moderate)
what 3 drugs are SNRIs?
venlafaxine
desvenlafaxine
duloxetine
how does venlafaxine act?
SEs?
•blocks uptake of both NE & 5HT
•similar to TCA w/o muscarinic or alpha block

•may ↑BP
what are the uses and SEs for trazodone?
•pain management
•significant sedation
•priapism**
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
st johns wort interactions?
•used OTC for mild depression
•do not combine w/ other antidepressants
•reduced efficacy of protease inhibitors, OCP, digoxin, warfarin
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
what drug causes neuroleptic malignant syndrome?
how do you treat?
chlorpromazine
tx w/ dantrolene
how to treat EPS?
anticholinergic
major SE of thioridazine?
retinal deposits
how does haloperidol act?
major SEs?
•selective D2 receptor blockade
•no anticholinergic activity

•highest incidence of EPS
•highly sedating
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
class and major SE of risperidone?
•"atypical" antipsychotic
•prolongs QT interval
•may ↑ mortality in Alzheimer's
class and major SEs of olanzapine?
•"atypical" antipsychotic
•weight gain
***the WORST for hyperglycemia
uses and SEs for quetiapine?
•"atypical" antipsychotic
•used for sedation, antidepressant adjunct
•SEs: weight gain, extreme sedation
•little effect on prolactin, no agranulocytosis
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
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
how to treat DI?
what drug can cause it?
•amiloride
•caused by lithium
signs for Li toxicity?
how to treat lithium OD?
•N/V, tremor
•infuse Na
what are the use & SEs for valproic acid?
•good for multiple seizure disorders
•liver toxicity, weight gain
how does topiramate act?
•acts on Na channels
•not as teratogenic as the other anticonvulsants
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
what is the DOC for partial seizures?
carbamazepine
uses for carbamazepine?
SE?
•DOC for parial sz
•tonic-clonic
•trigeminal neuralgia

**idiosyncratic blood dyscrasias
use and SEs for gabapentin?
•neuropathic pain
•drowsiness & weight gain
•pregnancy category C
how does ethosuximide act?
use?
SE?
•reduces low threshold Ca current in thalamic neurons
•DOC for absence sz
•can cause SJ syndrome (rare)
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
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
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
what is bromocriptine used for?
what is the SE?
•on/off periods
•erythromelagia - red, swollen feet
what drug class is pramipexole?
what is the major SE?
•DA agonist
•may cause sudden sleep during the day
what class is benzotropine?
how does it act?
•anticholinergic
•restores DA/Ach balance to help improve rigidity in parkinsons
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
what class is memantine?
how does it act?
use?
SE?
•NMDA receptor antagonist
•may reduce neurotoxic effect of glutamate
•Alzheimer's disease
•incontinence
how does baclofen work?
•acts as agonist on GABAb receptor
•results in hyperpolarization and inhibition of release of excitatory NT (glutamate) from presynapse in both brain & SC
which drug is administered intrathecally?
baclofen
what are the uses for baclofen?
SEs?
•used for chronic spasticity
•SE- some drowsiness
what class is cyclobenzaprine?
what major SE?
•acts as a sedative at the level of the brain stem
•SE- confusion, transient visual hallucinations
what is carisoprodol?
•central sedative activity
•popular drug of abuse
what is dantrolene used for?
malignant hyperthermia
neuroleptic malignant syndrome
how does botulinum toxin act?
blocks release of Ach from presynaptic terminal
how does methylphenidate act?
uses?
•promote release of newly synthesized catecholamines
•DA neurons in brain mostly affected

•use for narcolepsy and ADHD
what are the SEs of amphetamine?
•NE effects in the periphery
how does caffeine act?
blocks adenosine receptors and ↑cAMP by inhibiting PDE