Exam Review Flashcards

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1
Q

LDopa: use, mech, side effects, things to know

A

Use: PD

Mech: converted to dopamine by dopa decarboxylase, give with carbidopa

Side: arrhythmia, on-off effect + wearing off effect with long term use, dyskinesia

Other: if admin with high proten meal = reduce peak plasma conc

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2
Q

Carbidopa: use, mech

A

Use: co-admin with LDopa

Mech: decrease systemic conversion LDopa to dopamine so more LDopa reaches brain + limit peripheral side effects

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3
Q

Pramipexole: use, mech, side effects, things to know

A

Use: alone in early/mild PD; adjunct with LDopa later –> allow reduced LDopa dose = less severity on-off effect

Mech: selective D2 agonist

Side: somnolence [sleepiness]

Other: longer duration than LDopa, available extended release

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4
Q

Ropinirole: use, mech, side effects, things to know

A

Use: use alone in early/mild PD; adjunct with LDopa later –> allow reduced LDopa dose = less severity on-off effect

Mech: selective D2 agonist

Side: metabolized by CYP1a2 –> caffeine + warfarin interactions

Other: longer duration than LDopa, available extended release

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5
Q

Selegiline: use, mech, side effects, things to know

A

Use: adjunct to LDopa to prolong elevation of central DA

Mech: irreversible inhibitor of MAO in brain that breaks down dopamine, selective for MAO-B

Side: metabolites = amphetamine/ meth causes anxiety/insomnia [reduce w/ transderm patch]; interacts with meperidine [opioid analgestic] –> serotonin syndrome

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6
Q

Apomorphine: use, mech, side effects, things to know

A

Use: rescue drug to terminate “off” periods during LDopa therapy

Mech: non-selective agonist against most DA receptors

Side: emetics [N/V], CV [angina, orthostatic HT], somnolence, hallucinations

Other: rapid elim unchanged in urine; subcutaneous injection

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7
Q

Rasagiline: use, mech, side effects, things to know

A

Use: prolong elevation of central DA, adjunct to LDopa, give alone for early/mild PD

Mech: irreversible MAO-B inhibitor

Side: interacts with meperidine [opioid analgestic] –> serotonin syndrome

Other: more selective for MAO-B than selegiline; no amphetamine metabolites

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8
Q

Which parkinsons drug is metabolized to amphetamine?

A

selegiline

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9
Q

Which parkinsons drug is metabolized by CYP1A2?

A

ropinirole

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10
Q

Which parkinsons drug is a potent emetic?

A

apomorphine

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11
Q

Amantadine: use, mech, side effects

A

Use: give alone early/mild; adjunct to LDopa later, antiviral

Mech: increase DA synthesis/release, anti-ACh activity

Side: few side effects, ataxia

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12
Q

Entacapone: use, mech, side effects, things to know

A

Use: adjunct to LDopa to treat response fluctuations

Mech: Inhibits COMT only in periphery

Side: similtar to LDopa

Other: short duration of action, give with ever dose of LDopa

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13
Q

Trihexyphenidyl: use, mech, side effects, things to know

A

Use: adjunct to dopaminergic drugs

Mech: muscarinic antagonist

Side: CNS effects [confusiong, sedations, poor toleration in elderly], don’t give in closed angle glaucoma

Other:

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14
Q

Tetrabenazine: use, mech, side effects, things to know

A

Use: treats huntingtons motor symptoms

Mech: block DA release, deplete neuron catecholamines

Side: depression, suicidal ideation, hypotension, sedation

Other: does not treat psychiatric symptoms –> give anti-depressants/psychotics/anxiolytics

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15
Q

Baclofen: use, mech, things to know

A

Use: anti-spasticity

Mech: GABA-A agonist, dampens corticospinal input to motor neurons + directly inhibits

Other: oral

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16
Q

Tizanidine: use, mech, things to know

A

Use: anti-spasticity

Mech: A2 agonist, inhibits motor neuron directly + through inhibition corticospinal inputs

Other: oral

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17
Q

Dantrolene: use, mech, things to know

A

Use: anti-spasticity + malignant hyperthermia

Mech: prevents release CA from SR of skeletal muscle

Other: oral

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18
Q

Botulinum toxin: use, mech, things to know

A

Use: anti-spasiticity = best treatment

Mech: prevent ACh release from NMJ

Other: inject IM

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19
Q

Phenytoin: use, mech, side effects, things to know

A

Use: narrow spectrum [partial, tonic-clonic, status epilepticus], first line for status epilepticus with benzo; first line for tonic-clonic

Mech: inhibit NA channel

Side effects: nystagmus, teratogen [hydantoin syndrome], steven johnson, gingival hyperplasia, CYP450 inducer

Other: zero order kinetics

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20
Q

Phenobarbital: use, mech, side effects, things to know

A

Use: narrow [partial, tonic-clonic]

Mech: activate GABA-A

Side effects: teratogen, CNS depression/sedation, paradoxical excitatory in kids, megaloblastic anemia, CYP450 inhibitor

Other: first line in neonates/ pregnant

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21
Q

Carbamazepine: use, mech, side effects, things to know

A

Use: narrow [partial, tonic-clonic]; drug of choice for all 3, trigeminal neuralgia

Mech: inactivation NA channel

Side effects: CYP450 inducer

Other: diplopia, ataxia, dizziness, N/V, Steven Johnson

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22
Q

Gabapentin: use, mech, side effects, things to know

A

Use: narrow [partial, tonic-clonic], neuropathic pain

Mech: mech unclear – maybe increase GABA, maybe block Ca channel

Side effects: sedation, ataxia, weight gain

Other: 100% renal excretion

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23
Q

Tiagabine: use, mech, side effects

A

Use: narrow [partial]

Mech: inhibit GABA reuptake

Side effects: can induce seizure, usually mild = dizzy, somnolence

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24
Q

Valproate : use, mech, side effects

A

Use: broad [partial, tonic-clonic, absence]; first line tonic-clonic

Mech: block Na channel [may also decrease T-type Ca and increase GABA]

Side effects: teratogen, hepatotoxicity, N/V

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25
Q

Clonazepam: use, mech, side effects, things to know

A

Use: broad [absence, myoclonic, atonic]

Mech: increase GABA-A

Side effects: resp depression, sedation, tolerance, dependence

Other: benzodiazepine

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26
Q

Topiramate: use, mech, side effects, things to know

A

Use: broad [partial, tonic-clonic]

Mech: blocks Na channel, inhibits glutamate AMPA receptors, increase GABA

Side effects: confusion, cognitive slowing

Other: elimination 80% renal

27
Q

Lamotrigine: use, mech, side effects

A

Use: broad [partial, tonic clonic, absence]

Mech: blocks Na channel

Side effects: titrate slowly = Steven johnson. especially be careful if give with valproate causes increase lamotrigine conc

28
Q

Lorazepam: use, mech, side effects, things to know

A

Use: status epilepticus

Mech: increase GABA-A

Side effects: resp depression, sedation, tolerance, dependence

Other: benzodiazepine, for acute use only

29
Q

Ethosuximide: use, mech, side effects, things to know

A

Use: absence

Mech: inhibit thalamic T-type Ca channels

Side effects: fatigue, GI distress, headache, itching, steven-johnson

30
Q

Cocaine: use, mech, side effects, things to know

A

Use: local anesthesia eye/ear/nose/throat

Mech: inhibit DAT reuptake –> more DA/NE/5HT

Side effects: vasoconstriction, tachycardia, high BP, impaired judgement, pupil dilation, hallucination, paranoia, sudden cardiac arrest

Other: half life 1 hr, highly addictive; eliminate plasma + hepatic esterases

31
Q

Amphetamine/Methamphetamine: use, mech, side effects, things to know

A

Use: ADHD, narcolepsy [+ meth = exogenous obesity]

Mech: competitively inhibit reuptake DA/NE and enhance release –> synaptic depletion

Side effects: HT but reflex bradycardia, euphoria, pupil dilation, tachycardia, paranoia, anorexia

Other: eliminate mostly kidney, half life 10 hr

32
Q

Methylphenidate: use, mech, side effects, things to know

A

Use: ADHD, narcolespy

Mech: competitively inhibit reuptake, enhance DA/NE release

Side effects: same as amphetamine = HT but reflex bradycardia, euphoria, pupil dilation, tachycardia, paranoia, anorexia

Other: eliminate mostly kidney, half life 5 hr

33
Q

Phentermine: use, mech, side effects, things to know

A

Use: exogenous obesity

Mech: competitively inhibit reuptake, enhance DA/NE release

Side effects: same as amphetamine = HT but reflex bradycardia, euphoria, pupil dilation, tachycardia, paranoia, anorexia

Other: eliminate mostly by kidney; half life 20 hr

34
Q

Modafinil: use, mech, side effects, things to know

A

Use: narcolespy, obstructive sleep apnea, daytime shift disorder

Mech: not understood

Side effects: sympathomimetics [tachycardia, HT, etc], headache, nausea

Other: less risk of addiction than amphetatimes

35
Q

Caffeine: use, mech, side effects, things to know

A

Use: fatigue

Mech: adenosine receptor antagonist

Side effects: withdrawal = fatigue, sedation, headache/nausea

Other: tolerance develops

36
Q

Nicotine: use, mech, side effects, things to know

A

Use: tobacco addiction

Mech: direct agonist at central nicotinic ACh receptors

Side effects: arousal, relaxation, enhanced mood; low dose - high BP/HR/CO; high = release adrenal catecholamines; really high = hypotension

Other: highly addictive, excitation of DA neurons, causes nAChR desensitization

37
Q

Synthetic cathinones: mech, things to know

A

Mech: inhibit re-uptake/enhance NT release = similar to amphetamines

Other: constituent of bath salts

38
Q

LSD [lysergic acid diethylamide]: mech, side effects, things to know

A

Mech: 5HT2A partial agonist

Side effects: excitation of glutamate actions – hallucinations, synesthesias

Other: hepatic elimination 2.5-4 hrs; no withdrawal

39
Q

MDMA [methylenedioxyamphetamine] : mech, side effects, things to know

A

Mech: 5HT2A receptor partial agonist

Side effects: hallucinations = primarily visual, synesthesias

Other: hepatic metabolism 7 hrs, no withdrawal

40
Q

PCP [phencyclidine]: mech, side effects, things to know

A

Mech: non-competitive glutamate receptor antagonist

Side effects: visual/auditory hallucinations, paranoid delusions, numbness, insensitivity to pain, tachycardia, HT, sweating; at high dose = anesthesia, coma with mydriasis

Other: high risk of addiction

41
Q

marijuana: use, mech, side effects, things to know

A

Use: appetite stimulation; nausea; reduce intraocular pressure; reduce spasticity

Mech: agonist CB1 [and some CB2] receptor

Side effects: mellow high, with high doses -> anxiety/panic, psychomotor impairment

Other: hepatic metabolism; half like 1-1.5 days; 2 compartment kinetics

42
Q

dronabinol: use, mech

A

Use: anorexia “wasting” in AIDS, antiemetic for chemo, post surgery nausea

Mech: controlled synthetic cannabinoid = agonist CB1

43
Q

barbiturates : use, mech, side effects, things to know

A

Use: anxiety, insomnia, anesthesia induction [thiopental], headache [butalbital], resp/CNS depression, dependence

Mech: activate GABA-A

Side effects: CYP450 induction, small pupils, diminished reflexes

Other: rapid absorption, distribution, slow metabolism, renal elimination

44
Q

Benzodiazepines : use, mech, side effects, things to know

A

Use: anxiety, spasticity, status epilepticus [lorazepam/diaz.], detox alc withdrawal, insomnia, general anesthesia

Mech: activate GABA-A, decrease REM sleep

Side effects: dependence, CNS depression, less resp depression/coma than barbs, life threatening withdrawal

Other: 2 phase metabolism 1. ox by CYP3A4 (except lorazepam) 2. slow renal excretion

45
Q

What is time frame of action of benzos?

  • clonazepam
  • alprazolam
  • midazolap
  • diazepam
  • lorazepam
A
midazolam = short, IV
alprazolam = intermediate
lorazepam = intermediate
clonazepam = long
diazepam = longest
46
Q

What are the 5 Na channel blockers for epilepsy treatment?

A
Carbamazapine
Phenytoin
Valproate
Topirimate
Lamotrigine
47
Q

What are the 4 GABA enhancers for epilepsy treatmetn?

A

clonazepam
phenobarbital
tiagabine
lorazepam

48
Q

What 4 epilepsy drugs are teratogenic?

A

carbamazepine
phenytoin
phenobarbital
valproate

49
Q

What 3 epilepsy drugs are CYP450 inducers?

A

carbamazipine
phenytoin
phenobarbital

50
Q

flumazenil: use, mech, side effects

A

Use: benzo or newer hypnotic overdose

Mech: competitive antagonist with benzo for GABA-A receptor

Side effects: agitation, confusion, seizure

51
Q

zolpidem: use, mech, side effects, things to know

A

Use: insomnia

Mech: activate BZ1 subtype of GABA-A

Side effects: greater risk of dependence than benzos, hangover the next day

Other: quick onset, rapid CYP3A4 met, 3.5 hrs

52
Q

dexmedetomidine: use, mech, side effects, things to know

A

Use: sedation prior to surgery, analgesia

Mech: alpha 2 agonist = decreases NE secretion

Side effects: severe bradycardia, hypotension, sinus arrest

Other: IV

53
Q

busprione: use, mech, side effects, things to know

A

Use: generalized anxiety disorder

Mech: 5HT 1a partial agonist

Side effects: chest pain; tachycardia; dizziness; nervousness

Other: can take wks to be useful, no sedation/addiction/tolerance; does not interact with alcohol; eliminate: 1st pass CYP3A4 inhibitors; 2-4 hrs

54
Q

ethanol: mech, side effects, things to know

A

Mech: affects lots of membrane proteins; increase GABA-A; inhibit glutamate NMDA

Side effects: less myocardial contractility, tachycardia, vasodilation –> hyperthermia, uterine relaxation, N/V

Other: peak BAC within 30 min zero order kinetics = independent of time and conc

55
Q

disulfiram: use, mech, side effects, things to know

A

Use: alcoholism

Mech: inhibits aldehyde dehydrogenase

Side effects: causes accumulation of acetaldehyde if you drink –> facial flushing, N/V, dizziness, headache

Other: poor adherence weak efficacy

56
Q

naltrexone: use, mech, side effects, things to know

A

Use: alcoholism

Mech: long acting opioid antagonist

Side effects: hepatotoxicity

Other: daily oral/monthyl extendend release; avoid in pts on opioids or disulfiram or liver disease

57
Q

acamprosate: use, mech, side effects, things to know

A

Use: alcoholism

Mech: weak NMDA-antgonist + GABA-A agonist

Side effects: GI [N/V, diarrhea], rash, poor absorption with food

Other: renal elimination = avoid in severe renal disease; no drug-drug interactions; safe in liver disease

58
Q

desflurane/isoflurane/sevoflurane: use, mech, side effects, things to know, difference

A

Use: inhalation anesthetic

Mech: not well known

Side effects: malignant hyperthermia [fever + muscle contraction], myocardial depression, dose dependent resp depression, induce muscle relaxation [so give lower dose NMJ blocker]

Other: desflurane/isoflurane = no change
sevoflurane = decrease CO

59
Q

N2O: use, mech, side effects, things to know

A

Use: inhalation anesthetic

Mech: not well known

Side effects: expansion of trapped gas in body cavity; second gas effect; diffusion hypoxia; induce muscle relaxation –> lower dosea of NMJ blocker; no change in CO

Other: low solubility in blood –> rapid induction anesthesia;

60
Q

Propofol: use, mech, side effects, things to know

A

Use: IV anesthetic; sedation in ICU; rapid anesthesia induction; short procedures

Mech: activate GABA-A

Side effects: decrease BP, vasodilation, resp depression

Other: context sensitive half life–> longer in infusion than bolus b/c bolus has 2 phase metabolism. bolus = too short for surgery; not analgesic

61
Q

Etomidate: use, mech, side effects, things to know

A

Use: IV anesthetic

Mech: enhances GABA-A

Side effects: pain on injection; unlike propofol –> minimal effect on BP/HR/CO = preferred in pt with CV disease or risk of hypotension

Other: metabolized by esterases in blood + liver; not alagesic; not good for prolonged anesthesia b/c suppresses synthesis adrenal hormones

62
Q

Ketamine: use, mech, side effects, things to know

A

Use: IV/IM/oral/rectal/epidural

Mech: blocks NMDA receptors

Side effects: analgesic even at sub-anasthetic levels; dissociative anesthesia = cataleptic state, pts eyes open, slow nystagmus, increase HR /BP/ bronchodilation /cerebral blood flow

Other: hepatic metabolism, abused as hallucinogen

63
Q

Dantrolene: use, mech

A

Use: huntingtons, malignant hyperthermia associated wtih inhalaltion anesthetic intoxication

Mech: interferes with Ca release from SR via ryanodine