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Human Disease Systems > Neuro+Psych Pharmacology (Categories) > Flashcards

Neuro+Psych Pharmacology (Categories) Flashcards

1
Q

triptans

A

sumatriptan, zolmitriptan

acute migraine attack

MOA: 5HT1B/D agonist => block release of vasoactive peptides from perivascular trigeminal neurons

AE: nausea, dizziness, paresthesias, somnolence, chest tightness

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2
Q

lasmiditan

A

acute migraine attack

MOA: 5HT1F agonist => block release of vasoactive peptides from vascular trigeminal neurons

AE: nausea, dizziness, paresthesias, somnolence

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3
Q

CGRP receptor antagonists

A

ubrogepant, rimegepant

acute migraine attack

MOA: small molecule antagonist of CGRP receptors

AE: nausea, sedation

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4
Q

dihydroergotamine

A

acute migraine attack

MOA: structurally similar to LSD; mostly 5HT1D agonist, but also 5HT2A/B/C agonist, dopamine agonist, a receptor agonist

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5
Q

CGRP or CGRP receptor antibodies

A

galcanezumab, erenumab

migraine prophylaxis

MOA: antibodies to CGRP (galcanezumab) or to CGRP receptor (erenumab)

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6
Q

beta blockers for migraine prophylaxis

A

propranolol, timolol

migraineurs with hypertension/angina or with performance anxiety/aggressive behavior

MOA: unknown in migraine

AE: fatigue, exercise intolerance, cold extremities, diarrhea, constipation, dizziness, worsening depression

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7
Q

calcium channel blockers for migraine prophylaxis

A

verapamil

migraineurs with hypertension, hemiplegic migraine

MOA: block transmembrane influx of calcium => affects neurotransmission

AE: constipation, hypotension, AV block, edema, nausea

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8
Q

tricyclic antidepressants for migraine prophylaxis

A

amitriptyline, nortriptyline

headaches associated with depressive disorders or migraineurs with depression/anxiety

MOA: inhibit 5HT and NE reuptake

AE: antimuscarinic effects (increased HR, blurred vision, difficulty urinating, dry mouth, constipation), weight loss/gain, orthostatic hypotension

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9
Q

antiepileptics used for migraine prophylaxis

A

topiramate, valproic acid

migraineurs that are overweight or have bipolar disorder

MOA: AMPA receptors/sodium channel antagonist, GABA agonist (topiramate); inhibit T-type calcium channels (valproic acid)

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10
Q

fusion inhibitor (HIV)

A

enfuviritide

HIV patients resistant to other drugs

MOA: binds gp41 => prevents entry

AE: local injection site reaction, increased rate of bacterial pneumonia, hypersensitivity

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11
Q

CCR5 antagonist (HIV)

A

maraviroc

HIV patients resistant to other drugs

MOA: blocks CCR5 co-receptor => prevents entry

AE: cough, fever, rash, URT infection, musculoskeletal pain, postural dizziness, hepatotoxicity, cardiovascular events

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12
Q

nucleoside reverse transcriptase inhibitors (HIV)

A

lamivudine, emtricitabine, abacavir, zidovudine, tenofovir

HIV

MOA: nucleoside analogues phosphorylated (tenofovir does not need to be phosphorylated) to triphosphates => cause chain termination of DNA as it is being transcribed from RNA

AE: mitochondrial toxicity (lactic acidosis, pancreatitis, peripheral neuropathy, myopathy, cardiomyopathy, hepatic steatosis, lipid dystrophy)

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13
Q

non-nucleoside reverse transcriptase inhibitors

A

efavirenz

HIV

MOA: inhibit reverse transcriptase

AE: rash, Steven-Johnson syndrome, hepatitis, CNS effects

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14
Q

integrase inhibitors

A

bictegravir, dolutegravir, elvitegravir, raltegravir, cabotegravir/rilpivirine

HIV

MOA: target viral integrase

AE: hypersensitivity reactions or serious dermatological reactions, rhabdomyolysis, diarrhea, headache

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15
Q

protease inhibitors

A

darunavir, ritonavir

HIV

MOA: target a dipeptide region in HIV aspartate protease (not seen in mammalian proteins)

AE: nausea, vomiting, diarrhea, hyperglycemia, hepatotoxicity

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16
Q

fostemsavir

A

HIV

MOA: binds gp120 => prevents viral attachment

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17
Q

ibalizumab

A

HIV

MOA: recombinant mAb against domain 2 of CD4 T cells => prevents entry

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18
Q

depolarizing neuromuscular blockers

A

succinylcholine

used for brief procedures (mainly intubation)

MOA: more stable agonist than acetylcholine; cause persistent depolarization and then desensitization and finally inactivation of nicotinic receptors

AE: apnea, hyperkalemia (precludes use in children), increased IOP, increased gastric pressure, malignant hyperthermia

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19
Q

non-depolarizing neuromuscular blockers

A

tubucurarine, pancuronium (longer duration; kidney metabolism)

cisatracurium, atracurium (widely used in surgery, intermediate duration, spontaneous hydrolysis)

verconium (widely used in surgery, intermediate duration, liver metabolism)

rocuronium (rapid onset for brief procedures, liver metabolism)

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20
Q

drugs used for non-depolarizing NMJ blocker reversal

A

neostigmine (cholinesterase inhibitor) and atropine/glycopyrrolate (antimuscarinic to prevent concomitant ACh excess)

21
Q

inhaled anesthetics

A

nitrous oxide

isoflurane, sevoflurane, desflurane, enflurane, halothane

AE: renal toxicity (enflurane), hepatic toxicity (halothane), respiratory toxicity (sevoflurane)

22
Q

intravenous anesthetics

A

thiopental, methohexital, etomidate, propofol, ketamine

23
Q

dopamine precursors (Parkinson’s)

A

L-DOPA, sinemet

MOA: taken up by neuron, converted to dopamine, stored in vesicle, released (sinemet = controlled release formation)

AE: GI effects (anorexia, nausea, vomiting), cardiovascular effects (orthostatic hypotension, tachycardia), dyskinesias, psychiatric side effects, on-off phenomena

24
Q

dopamine agonists (Parkinson’s)

A

bromocriptine (D2, D3), pramipexole (D3>D2), ropinirole (D2, D3)

AE: cardiovascular effects (postural hypotension, erythromelalgia, digital vasospasm), GI effects (anorexia, nausea, vomiting, constipation, peptic ulceration, reflux esophagitis), dyskinesia, mental disturbance

25
Q

dopamine releasing agent (Parkinson’s)

A

amantadine

to control L-DOPA dyskinesias

MOA: antiviral drug that causes DA release in striatum

AE: restlessness, agitation, hallucination, livedo reticularis, peripheral edema

26
Q

monoamine oxidase inhibitor (Parkinson’s)

A

selegiline

adjunctive therapy for Parkinson’s

MOA: MAO-B inhibitor => retards breakdown of dopamine, prolongs effect of DOPA

AE: insomnia

27
Q

anticholinergics (Parkinson’s)

A

benzotropine, trihexyphenidyl

improves rigidity/tremor, minor effect on bradykinesia

MOA: restores dopamine/cholinergic balance within striatum

AE: restlessness, hallucinations, confusion, antimuscarinic effects

28
Q

COMT inhibitors (Parkinson’s)

A

tolcapone, entacapone

increase duration of DOPA dose (adjunctive)

MOA: enhance delivery of L-DOPA to brain and stabilize dopamine

AE: dyskinesias, tolcapone can cause liver toxicity

29
Q

cholinesterase inhibitors (Alzheimer’s)

A

tacrine, donepezil, galantamine, rivastigmine

AE: hepatotoxicity (tacrine); nausea, diarrhea, headache, insomnia, anorexia, pain, urinary incontinence (others)

30
Q

NMDAR antagonist (Alzheimer’s)

A

memantine

AD, Huntington disease, AIDS-related dementia, vascular dementia

MOA: NMDAR antagonist that blocks “open” NMDA channels with low to moderate affinity

AE: dizziness, constipation, confusion, headache, hypertension

31
Q

typical antipsychotics

A

high potency: haloperidol, fluphenazine

medium potency: periphenazine

low potency: chlorpromazine, thioridazine

MOA: D2 blockade; increasing anticholinergic effect with decreasing potency

AE: acute dystonia (treated with diphenhydramine), parkinsonism (treated with amantadine), akathesia (treated with propranolol), tardive dyskinesia (treated with valbenazine), orthostatic hypotension, male sexual dysfunction, constipation, dry mouth, urinary retention, visual problems, sedation, galactorrhea, amenorrhea, neuroleptic malignant syndrome (treated with dantrolene or bromocriptine)

32
Q

atypical antipsychotics

A

clozapine, risperidone, olanzapine, quetiapine, ziprasidone, ariprazole

MOA: 5HT2A antagonist, D2 antagonist with rapid dissociation, dopamine D2 partial agonist (ariprazole only)

AE: increased appetite and increased weight, sedation, somnolence; agranulocytosis, salivation, seizures (clozapine); cardiac arrhythmia (ziprasidone); EPS at higher doses (risperidone)

33
Q

selective serotonin reuptake inhibitors

A

fluoxetine, sertraline, citalopram, fluvoxamine, paroxetine

MOA: inhibit reuptake of 5HT

AE: nausea, diarrhea, sexual dysfunction, discontinuation syndrome, serotonin syndrome, reduced platelet aggregation, sweating, suicide

34
Q

serotonin/ norepinephrine reuptake inhibitors

A

venlafaxine, duloxetine

MOA: inhibit 5HT and NE (venlafaxine only at higher doses) transporter

AE: nausea, discontinuation syndrome, serotonin syndrome, increased BP and HR, CNS activation

35
Q

tricyclic antidepressants

A

amitriptyline, nortriptyline, imipramine, desipramine, clomipramine

MOA: inhibit NE and 5HT reuptake to varying degrees

AE: anticholinergic effects, postural hypotension, weight gain, sedation, sexual side effects, discontinuation and serotonin syndromes

toxicity treated with: sodium bicarbonate

36
Q

5HT2A receptor antagonists

A

trazadone, mirtazapine

insomnia, melancholic depression, depression with insomnia

AE: sedation, GI upset, hypotension and priapism, increased appetite and weight gain, sedation

37
Q

unicycle antidepressant

A

bupropion

MOA: resembles amphetamine (CNS activating effects), cause NE release and DA release to a lesser extent; moderate inhibitor of NE and DA reuptake

AE: agitation, insomnia, anorexia

38
Q

MOAIs

A

phelezine, tranylcyproamine, isocarboxazid, selegiline

MOA: inhibit MAO-A and MAO-B (selegiline only B) => increase monoamine transmission

AE: tyramine escapes destruction, causing dramatic hypertension; serotonin syndrome, CNS stimulation in overdose, postural hypotension, weight gain

39
Q

lithium

A

mood stabilizer

MOA: unknown

AE: tremor, sedation, decreased cognition, decreased thyroid function, polydipsia and polyuria, tubulointerstitial nephropathy, nausea, vomiting, diarrhea, weight gain, dermatitis, hair loss, acne, reversible increase in PMNs

40
Q

benzodiazepines

A

diazepam, chlordiazepam, flurazepam (longer acting due to phase I metabolism); clonazepam, alprazolam, temazepam, triazolam, lorazepam, oxazepam

anxiolytics, insomnia

AE: sedation, physical/psychological dependence, toxicity (treated with flumenazil)

41
Q

non-benzodiazepine anxiolytic

A

buspirone

MOA: partial agonist at both presynaptic and postsynaptic 5HT1A receptors => may inhibit normal inhibitory feedback

relatively non-sedating

42
Q

benzodiazepines used for insomnia

A

diazepam, flurazepam, temazepam, triazolam

43
Q

non-benzodiazepines for insomnia

A

zolpidem, zaleplon, eszopiclone, suvorexant (orexin antagonist), ramelteon (melatonin agonist)

AE: sleep driving, ataxia, nightmares, headache, confusion, next day drowsiness

44
Q

stimulants used for ADHD

A

methylphenidate, dexmethylphenidate (block DA and NE reuptake; for 6+)

detroamphetamine, lisdextamfetamine (enhance release and block reuptake of DA and NE; for 3+)

AE: anorexia, nervousness, growth suppression, GI distress, irritability, tachycardia, increased BP, tics, sudden death in children with cardiac abnormalities (amphetamines only)

45
Q

non-stimulants for ADHD

A

atomoxetine (NE reuptake inhibitor); clonidine, guanfacine (central a2 agonist); bupropion (DA and NE reuptake inhibitor)

AE: nausea, anorexia, increased HR and BP, constipation, hepatotoxicity, sedation, orthostatic hypotension, dry mouth

46
Q

cocaine MOA

A

blocks reuptake of monoamines in presynaptic terminal; predominantly DA

47
Q

amphetamine MOA

A

substrate for monoamine transporter; displaces NE => NE release

48
Q

methamphetamine MOA

A

decreased DA reuptake and increased DA release

Human Disease Systems (11 decks)

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