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Brain and Behavior Exam 3 > 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
Clonazepam: use, mech, side effects, things to know
Use: broad [absence, myoclonic, atonic] Mech: increase GABA-A Side effects: resp depression, sedation, tolerance, dependence Other: benzodiazepine
26
Topiramate: use, mech, side effects, things to know
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
Lamotrigine: use, mech, side effects
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
Lorazepam: use, mech, side effects, things to know
Use: status epilepticus Mech: increase GABA-A Side effects: resp depression, sedation, tolerance, dependence Other: benzodiazepine, for acute use only
29
Ethosuximide: use, mech, side effects, things to know
Use: absence Mech: inhibit thalamic T-type Ca channels Side effects: fatigue, GI distress, headache, itching, steven-johnson
30
Cocaine: use, mech, side effects, things to know
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
Amphetamine/Methamphetamine: use, mech, side effects, things to know
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
Methylphenidate: use, mech, side effects, things to know
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
Phentermine: use, mech, side effects, things to know
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
Modafinil: use, mech, side effects, things to know
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
Caffeine: use, mech, side effects, things to know
Use: fatigue Mech: adenosine receptor antagonist Side effects: withdrawal = fatigue, sedation, headache/nausea Other: tolerance develops
36
Nicotine: use, mech, side effects, things to know
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
Synthetic cathinones: mech, things to know
Mech: inhibit re-uptake/enhance NT release = similar to amphetamines Other: constituent of bath salts
38
LSD [lysergic acid diethylamide]: mech, side effects, things to know
Mech: 5HT2A partial agonist Side effects: excitation of glutamate actions -- hallucinations, synesthesias Other: hepatic elimination 2.5-4 hrs; no withdrawal
39
MDMA [methylenedioxyamphetamine] : mech, side effects, things to know
Mech: 5HT2A receptor partial agonist Side effects: hallucinations = primarily visual, synesthesias Other: hepatic metabolism 7 hrs, no withdrawal
40
PCP [phencyclidine]: mech, side effects, things to know
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
marijuana: use, mech, side effects, things to know
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
dronabinol: use, mech
Use: anorexia "wasting" in AIDS, antiemetic for chemo, post surgery nausea Mech: controlled synthetic cannabinoid = agonist CB1
43
barbiturates : use, mech, side effects, things to know
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
Benzodiazepines : use, mech, side effects, things to know
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
What is time frame of action of benzos? - clonazepam - alprazolam - midazolap - diazepam - lorazepam
``` midazolam = short, IV alprazolam = intermediate lorazepam = intermediate clonazepam = long diazepam = longest ```
46
What are the 5 Na channel blockers for epilepsy treatment?
``` Carbamazapine Phenytoin Valproate Topirimate Lamotrigine ```
47
What are the 4 GABA enhancers for epilepsy treatmetn?
clonazepam phenobarbital tiagabine lorazepam
48
What 4 epilepsy drugs are teratogenic?
carbamazepine phenytoin phenobarbital valproate
49
What 3 epilepsy drugs are CYP450 inducers?
carbamazipine phenytoin phenobarbital
50
flumazenil: use, mech, side effects
Use: benzo or newer hypnotic overdose Mech: competitive antagonist with benzo for GABA-A receptor Side effects: agitation, confusion, seizure
51
zolpidem: use, mech, side effects, things to know
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
dexmedetomidine: use, mech, side effects, things to know
Use: sedation prior to surgery, analgesia Mech: alpha 2 agonist = decreases NE secretion Side effects: severe bradycardia, hypotension, sinus arrest Other: IV
53
busprione: use, mech, side effects, things to know
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
ethanol: mech, side effects, things to know
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
disulfiram: use, mech, side effects, things to know
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
naltrexone: use, mech, side effects, things to know
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
acamprosate: use, mech, side effects, things to know
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
desflurane/isoflurane/sevoflurane: use, mech, side effects, things to know, difference
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
N2O: use, mech, side effects, things to know
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
Propofol: use, mech, side effects, things to know
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
Etomidate: use, mech, side effects, things to know
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
Ketamine: use, mech, side effects, things to know
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
Dantrolene: use, mech
Use: huntingtons, malignant hyperthermia associated wtih inhalaltion anesthetic intoxication Mech: interferes with Ca release from SR via ryanodine

Brain and Behavior Exam 3 (32 decks)

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