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Neuro Pharmacology Flashcards

1
Q

L-DOPA

A

uses: Parkinson’s disease
MoA: restores dopamine in the basal ganglia; enters brain via amino acid transporters; poor bioavailability (metabolized by L-AAAD or COMT), administered with carbidopa or entacapone; beneficial effects outlive half-life (dopamine accumulates in vesicles)
side effects: effectivity declines after a few years of treatment, dyskinesia, dementia, confusion, nausea, postural hypotension, arrhythmias, hypertension
drug interactions: pyridoxine, MAO inhibitors (except selegiline), halothane, DA-antagonist antipsychotics
contraindications: glaucoma, psychosis, arrhythmia, melanoma

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2
Q

carbidopa

A

uses: Parkinson’s disease
MoA: co-administered with L-DOPA, inhibits peripheral L-AAAD to prevent dopamine degradation (does not cross BBB)
side effects:

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3
Q

ropinerole

A

uses: Parkinson’s disease
MoA: selective D2 agonist
side effects: nausea, fatigue, sudden daytime sleep attacks, confusion, dyskinesia

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4
Q

pramipexole

A

uses: Parkinson’s disease
MoA: selective D2 agonist
side effects: nausea, fatigue, sudden daytime sleep attacks, confusion, dyskinesia

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5
Q

apomorphine

A

uses: Parkinson’s disease: immediate therapy for an “off” episode, reserved for pts refractory to other treatments
MoA: high-affinity D4 agonist, moderate D2, D3, D5 agonist (SQ)
side effects: nausea, fatigue, sudden daytime sleep attacks, confusion, dyskinesia, QT prolongation, injection site rxn

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6
Q

amantadine

A

uses: Parkinson’s disease (less effective, short-lived benefit)
MoA: increases dopamine release, mildly anti-cholinergic, blocks NMDA receptors; often co-administered with L-DOPA or anticholinergics, but not helpful if L-DOPA is ineffective
side effects: dizziness, lethargy, sleep disturbances, peripheral edema, sympathomimetic effects; contraindicated in CHF

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7
Q

trihexyphenidyl

A

uses: Parkinson’s disease (modest efficacy: not helpful for bradykinesia, third-choice when dopaminergic tx is contraindicated)
MoA: striatal muscarinic antagonist; inhibits cholinergic interneurons that lose dopaminergic inhibition in PD; may be used in combination with L-DOPA
side effects: sedation, mental confusion, atropine-like effects

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8
Q

benztropine

A

uses: Parkinson’s disease (modest efficacy: not helpful for bradykinesia, third-choice when dopaminergic tx is contraindicated)
MoA: striatal muscarinic antagonist; inhibits cholinergic interneurons that lose dopaminergic inhibition in PD; may be used in combination with L-DOPA
side effects: sedation, mental confusion, atropine-like effects

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9
Q

selegiline

A

uses: Parkinson’s disease (modest effect; may be used in combination with L-DOPA)
MoA: selective, irreversible MAO-B inhibitor; prolongs action of dopamine in the brain, may also reduce oxidative stress due to dopamine metabolism
side effects: well-tolerated in early disease; in late disease, worsens side effects of L-DOPA, metabolized to amphetamine/methamphetamine (anxiety, insomnia)
drug interactions: meperidine, tricyclic antidepressants, SSRIs (cause serotonin syndrome: stupor, rigidity, agitation, hyperthermia)

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10
Q

rasagiline

A

uses: Parkinson’s disease (modest effect; may be used in combination with L-DOPA)
MoA: selective, irreversible MAO-B inhibitor; prolongs action of dopamine in the brain, may also reduce oxidative stress due to dopamine metabolism
side effects: well-tolerated in early disease; in late disease, worsens side effects of L-DOPA, metabolized to amphetamine/methamphetamine (anxiety, insomnia)
drug interactions: meperidine, tricyclic antidepressants, SSRIs (cause serotonin syndrome: stupor, rigidity, agitation, hyperthermia)

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11
Q

entacapone

A

uses: Parkinson’s disease
MoA: inhibits COMT (both peripheral and central) to increase half-life/bioavailability of dopamine; co-administered with L-DOPA
side effects: nausea, orthostatic hypotension, vivid dreams, confusion, hallucinations

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12
Q

donepezil

A

uses: Alzheimer’s disease
MoA: acetylcholinesterase inhibitor

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13
Q

galantamine

A

uses: Alzheimer’s disease
MoA: acetylcholinesterase inhibitor

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14
Q

memantine

A

uses: Alzheimer’s disease
MoA: NMDA channel blocker

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15
Q

rivastigmine

A

uses: Alzheimer’s disease
MoA: acetylcholinesterase inhibitor

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16
Q

riluzole

A

uses: ALS (increases life span 2-3 months)
MoA: inhibits NMDA channels, inhibits glutamate release, increases uptake

17
Q

lysergic acid diethylamide

A

uses: recreational hallucinogen
MoA: 5-HT2 receptor agonist, highly potent

18
Q

buspirone

A

uses: anxiety
MoA: 5-HT1A receptor partial agonist

19
Q

sumatriptan

A

uses: migraine headaches (abortive tx)
MoA: 5-HT1B/D agonist, leads to cerebral blood vessel constriction, brainstem pathway blockage, inhibition of trigeminal nucleus caudalis; inhibits release of vasoactive peptides (CGRP); available orally, SQ, or as nasal spray and in combination with naproxen
side effects: peripheral vasoconstriction, nausea, angina, dizziness, flushing
contraindications: stroke, MI, uncontrolled HTN, ischemic heart disease

20
Q

alternative migraine abortive treatments to triptans

A

NSAIDs, caffeine, steroids, ergots

21
Q

drugs used for migraine prophylaxis

A

tricyclic antidepressants, SNRIs, antiseizure agents (valproic acid, topiramate, gabapentin, pregabalin, lamotrigine), beta blockers, calcium channel blockers

22
Q

phenytoin

A

uses: generalized tonic-clonic seizures, partial seizures (not absence seizures)
MoA: use-dependent blockade of sodium channels - stabilizes closure of inactivation gate, which prevents repetitive neuron firing
kinetics: dose-dependent - first-order at low doses, zero-order at high doses
side effects: nausea, anorexia, apathy, sedation, ataxia, nystagmus, diplopia, gingival hyperplasia, hirsutism, teratogenic, rash, bone marrow and hepatic effects
drug interactions: those that are metabolized by microsomal enzymes or protein-bound

23
Q

carbamazepine

A

uses: partial seizures (not absence seizures), bipolar disorder
MoA: blocks sodium channels
kinetics: induces hepatic enzymes
side effects: rash, diplopia, ataxia, GI upset, drowsiness, blood dycrasias, teratogenic, hepatic toxicity

24
Q

ethosuximide

A

uses: absence seizures
MoA: reduces T-type calcium currents in thalamic neurons
kinetics: not protein-bound (volume of distribution = TBW), liver metabolism inhibited by valproic acid, long half-life (but 1X daily dosing may increase side effects)
side effects: GI upset, lethargy, fatigue, bone marrow effects

25
valproic acid
uses: absence seizures, tonic-clonic seizures, partial seizures, myoclonic seizures MoA: blocks repetitive neuronal firing, reduces T-type calcium currents, increases GABA concentration kinetics: competes with phenytoin for protein binding; distributes to ECF; inhibits metabolism of phenobarbital, phenytoin, and carbamazepine side effects: GI upset, weight gain, hair loss, hepatotoxicity, teratogenic, bone marrow effects
26
felbamate
uses: partial seizures that are refractory to other tx MoA: NMDA receptor antagonist - binds allosterically at glycine modulatory site; potentiates GABA side effects: aplastic anemia, hepatic failure
27
gabapentin
uses: partial seizures w/ or w/o generalized tonic-clonic seizures (adjunct), neuropathic pain, ALS MoA: GABA analog, specific role is unclear (not an agonist) kinetics: not metabolized and does not bind protein, i.e. no drug interactions
28
pregabalin
uses: partial seizures (adjunct), neuropathic pain associated with diabetes, postherpetic neuralgia, and fibromyalgia MoA: structurally similar to gabapentin but more potent; may inhibit neurotransmitter release via interaction with voltage-gated calcium channels side effects: limited abuse potential
29
lamotrigine
uses: partial seizures, generalized tonic-clonic seizures, absence seizures, bipolar disorder MoA: blocks repetitive action channels, may block sodium channels kinetics: does not interfere with other drugs side effects: rash, Stevens-Johnson syndrome
30
topiramate
uses: add-on tx for adults with partial seizures, migraine prophylaxis MoA: derivative of D-fructose; inhibits activity of excitatory amino acids on kainate/AMPA glutamate receptors; may also block sodium channels; blocks spread of seizures (rather than raising seizure threshold) side effects: fatigue, nausea, confusion, weight loss
31
tiagabine
uses: add-on tx for partial seizures MoA: inhibits reuptake of GABA by blocking GABA transporter GAT-1 side effects: dizziness, tremor, somnolence
32
levetiracetam
uses: adjunctive tx for partial seizures, myoclonic seizures, generalized tonic-clonic seizures MoA: unknown; may involve SV2A (synaptic vesicle protein) side effects: somnolence, asthenia, dizziness
33
zonisamide
uses: adjunctive tx for adults with partial seizures MoA: reduces voltage-dependent transient inward currents at sodium and T-type calcium channels; stops spread of seizures and suppresses their focus side effects: ataxia, anorexia, nervousness, fatigue, speech impairment, bone marrow effects
34
vigabatrin
uses: adjunctive tx for refractory complex partial seizures and infantile spasms MoA: irreversibly inhibits GABA metabolism (GABA-transaminase) side effects: possible permanent vision loss
35
clobazam
uses: adjunctive tx for Lennox-Gastaut syndrome in pts older than 2 y.o. MoA: enhances GABA action at GABA receptor chloride channel complex
36
lactosamide
uses: adjunctive tx for partial seizures MoA: enhances slow inactivation of voltage-gated sodium channels; effects are additive to other AEDs
37
perampanel
uses: partial seizures MoA: antagonizes post-synaptic AMPA receptors at an allosteric site (noncompetitive); ultimately prevents NMDA receptor discharge drug interactions: potent CYP3A inducers (carbamazepine, oxcarbazepine, phenytoin)
38
ezogabine
uses: adjunctive tx for partial seizures in adults (last-resort) MoA: potassium channel facilitator side effects: retinal abnormalities, possible vision loss, bluish skin discoloration
39
rufinamide
uses: adjunctive tx for Lennox-Gastaut syndrome in pts 4 y.o. and older; particularly effective against tonic-atonic seizures MoA: decreases sustained high-frequency firing of neurons via prolongation of inactive state of sodium channel

Neuro/Psych (2 decks)

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