Neuro+Psych Pharmacology (Categories) Flashcards
triptans
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
lasmiditan
acute migraine attack
MOA: 5HT1F agonist => block release of vasoactive peptides from vascular trigeminal neurons
AE: nausea, dizziness, paresthesias, somnolence
CGRP receptor antagonists
ubrogepant, rimegepant
acute migraine attack
MOA: small molecule antagonist of CGRP receptors
AE: nausea, sedation
dihydroergotamine
acute migraine attack
MOA: structurally similar to LSD; mostly 5HT1D agonist, but also 5HT2A/B/C agonist, dopamine agonist, a receptor agonist
CGRP or CGRP receptor antibodies
galcanezumab, erenumab
migraine prophylaxis
MOA: antibodies to CGRP (galcanezumab) or to CGRP receptor (erenumab)
beta blockers for migraine prophylaxis
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
calcium channel blockers for migraine prophylaxis
verapamil
migraineurs with hypertension, hemiplegic migraine
MOA: block transmembrane influx of calcium => affects neurotransmission
AE: constipation, hypotension, AV block, edema, nausea
tricyclic antidepressants for migraine prophylaxis
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
antiepileptics used for migraine prophylaxis
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)
fusion inhibitor (HIV)
enfuviritide
HIV patients resistant to other drugs
MOA: binds gp41 => prevents entry
AE: local injection site reaction, increased rate of bacterial pneumonia, hypersensitivity
CCR5 antagonist (HIV)
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
nucleoside reverse transcriptase inhibitors (HIV)
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)
non-nucleoside reverse transcriptase inhibitors
efavirenz
HIV
MOA: inhibit reverse transcriptase
AE: rash, Steven-Johnson syndrome, hepatitis, CNS effects
integrase inhibitors
bictegravir, dolutegravir, elvitegravir, raltegravir, cabotegravir/rilpivirine
HIV
MOA: target viral integrase
AE: hypersensitivity reactions or serious dermatological reactions, rhabdomyolysis, diarrhea, headache
protease inhibitors
darunavir, ritonavir
HIV
MOA: target a dipeptide region in HIV aspartate protease (not seen in mammalian proteins)
AE: nausea, vomiting, diarrhea, hyperglycemia, hepatotoxicity
fostemsavir
HIV
MOA: binds gp120 => prevents viral attachment
ibalizumab
HIV
MOA: recombinant mAb against domain 2 of CD4 T cells => prevents entry
depolarizing neuromuscular blockers
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
non-depolarizing neuromuscular blockers
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)
drugs used for non-depolarizing NMJ blocker reversal
neostigmine (cholinesterase inhibitor) and atropine/glycopyrrolate (antimuscarinic to prevent concomitant ACh excess)
inhaled anesthetics
nitrous oxide
isoflurane, sevoflurane, desflurane, enflurane, halothane
AE: renal toxicity (enflurane), hepatic toxicity (halothane), respiratory toxicity (sevoflurane)
intravenous anesthetics
thiopental, methohexital, etomidate, propofol, ketamine
dopamine precursors (Parkinson’s)
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
dopamine agonists (Parkinson’s)
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
dopamine releasing agent (Parkinson’s)
amantadine
to control L-DOPA dyskinesias
MOA: antiviral drug that causes DA release in striatum
AE: restlessness, agitation, hallucination, livedo reticularis, peripheral edema
monoamine oxidase inhibitor (Parkinson’s)
selegiline
adjunctive therapy for Parkinson’s
MOA: MAO-B inhibitor => retards breakdown of dopamine, prolongs effect of DOPA
AE: insomnia
anticholinergics (Parkinson’s)
benzotropine, trihexyphenidyl
improves rigidity/tremor, minor effect on bradykinesia
MOA: restores dopamine/cholinergic balance within striatum
AE: restlessness, hallucinations, confusion, antimuscarinic effects
COMT inhibitors (Parkinson’s)
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
cholinesterase inhibitors (Alzheimer’s)
tacrine, donepezil, galantamine, rivastigmine
AE: hepatotoxicity (tacrine); nausea, diarrhea, headache, insomnia, anorexia, pain, urinary incontinence (others)
NMDAR antagonist (Alzheimer’s)
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
typical antipsychotics
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)
atypical antipsychotics
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)
selective serotonin reuptake inhibitors
fluoxetine, sertraline, citalopram, fluvoxamine, paroxetine
MOA: inhibit reuptake of 5HT
AE: nausea, diarrhea, sexual dysfunction, discontinuation syndrome, serotonin syndrome, reduced platelet aggregation, sweating, suicide
serotonin/ norepinephrine reuptake inhibitors
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
tricyclic antidepressants
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
5HT2A receptor antagonists
trazadone, mirtazapine
insomnia, melancholic depression, depression with insomnia
AE: sedation, GI upset, hypotension and priapism, increased appetite and weight gain, sedation
unicycle antidepressant
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
MOAIs
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
lithium
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
benzodiazepines
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)
non-benzodiazepine anxiolytic
buspirone
MOA: partial agonist at both presynaptic and postsynaptic 5HT1A receptors => may inhibit normal inhibitory feedback
relatively non-sedating
benzodiazepines used for insomnia
diazepam, flurazepam, temazepam, triazolam
non-benzodiazepines for insomnia
zolpidem, zaleplon, eszopiclone, suvorexant (orexin antagonist), ramelteon (melatonin agonist)
AE: sleep driving, ataxia, nightmares, headache, confusion, next day drowsiness
stimulants used for ADHD
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)
non-stimulants for ADHD
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
cocaine MOA
blocks reuptake of monoamines in presynaptic terminal; predominantly DA
amphetamine MOA
substrate for monoamine transporter; displaces NE => NE release
methamphetamine MOA
decreased DA reuptake and increased DA release
