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USMLE Pharmacology > Neurology > Flashcards

Neurology Flashcards

1
Q

Glaucoma drugs

Decrease IOP and amount of aqueous humor

A 
a-agonists (epinephrine, brimonidine/a2)
B-blockers (timolol, betaxol, carteolol)
Diuretics (acetazolamide)
Cholinomimetics (direct = pilocarpine, carbachol; indirect = physostigmine, echothiophate)
Prostaglandin = latanoprost (PGF2a)
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2
Q

Epinephrine and Brimonidine (a2)

Use/MOA/SE

A

Glaucoma
Decrease aqueous humor synthesis via vasoconstriction
SE = mydriasis (don’t use in closed angle glaucoma); blurry vision, ocular hyperemia, foreign body sensation, ocular allergic reactions, ocular pruritus

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3
Q

Timolol, betaxolol, carteolol

Use/MOA/SE

A

Glaucoma
Decrease aqueous humor synthesis
SE = no pupillary or vision changes

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4
Q

Acetazolamide

A

Glaucoma
Decrease aqueous humor synthesis via inhibition of carbonic anhydrase
SE = no pupillary or vision changes

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5
Q

Direct and indirect cholinomimetics for glaucoma

A

D = Pilocarpine, Carbachol
I = Physostigmine, Echothiophate
Increase outflow of aqueous humor via contraction of ciliary muscle and opening of trabecular meshwork
SE = miosis and cyclospasm (contraction of ciliary muscle)

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6
Q

Drug used in glaucoma emergencies

A

Pilocarpine

Very effective at opening meshwork into canal of Schlemm

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7
Q

Latanoprost

A

PGF2a for glaucoma
Increase outflow of aqueous humor
SE = darkens color of iris (browning)

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8
Q

Opioid analgesics

A

Morphine, fentanyl, codeine, loperamide, methadone, meperidine, dextromethorphan, diphenoxylate
Agonists at opioid receptors (mu = morphine, delta = enkephalin, kappa = dynorphin)
Modulate synaptic transmission = open K, close Ca channels = decrease transmission
Inhibit release of ACh, NE, 5HT, glutamate, substance P

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9
Q

Opioid analgesic - pain and cough suppression

A

Dextromethorphan

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10
Q

Opioid analgesic - diarrhea

A

Loperamide

Diphenoxylate

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11
Q

Acute pulmonary edema and maintenance programs for heroin addicts

A

Methadone

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12
Q

Opioid analgesic toxicity

A 
Addiction
Respiratory depression
CONSTIPATION
MIOSIS (PINPOINT PUPILS)
Additive CNS depression with other drugs
Tolerance does not develop to miosis and constipation
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13
Q

Treatment for opioid toxicity

A

Naloxone

Naltrexone (opioid receptor antagonist)

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14
Q

Butorphanol

A

Mu opioid receptor partial agonist and kappa-opioid receptor agonist
Produces analgesia
Use = severe pain (migraine, labor)
Less respiratory depression

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15
Q

Butorphanol toxicity

A

Opioid withdrawal symptoms if also taking full opioid agonist
Overdose NOT easily reversed with naloxone

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16
Q

Tramadol

A 
Weak opioid agonist
Also inhibits 5HT and NE reuptake
"Tram it all with Tramadol"
Use = chronic pain
Toxicity = decreases seizure threshold, serotonin syndrome
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17
Q

Ethosuximide

A

Absence
Blocks thalamic T-type Ca channels
SE = fatigue, GI distress, headache, itching (urticaria), Stevens-Johnson syndrome

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18
Q

Benzodiazepines

A

Status epilepticus
Increase GABAa action
SE = sedation, tolerance, dependence, respiratory depression

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19
Q

Eclampsia seizures

A

MgSO4

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20
Q

Phenytoin

A

All seizures
Prophylaxis status epilepticus, first line tonic-clonic
Increase Na channel inactivation; zero-order kinetics
SE = gingival hyperplasia, megaloblastic anemia, teratogenic (fetal hydantoin syndrome), SLE like syn, induction P450, Stevens Johnson, osteopenia, nystagmus/diplopia, ataxia, sedation

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21
Q

Carbamazepine

A

First line simple, complex, tonic-clonic
Increase Na channel inactivation
SE = blood dyscrasias (agranulocytosis, aplastic anemia), induction P450, SIADH, Stevens-Johnson syn

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22
Q

Trigeminal neuralgia

A

Carbamazepine

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23
Q

Valproic acid

A

All, first line tonic clonic
Increase Na channel inactivation
Increase GABA concentration by inhibiting GABA transaminase
SE = fatal hepatotoxicity (measure LFTs!!!), NTD, tremor, WG

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24
Q

Myoclonic seizures, bipolar disorder

A

Valproic acid

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25
Gabapentin
Simple, complex, tonic-clonic Inhibits high-voltage-activated Ca channels Designed as GABA analog SE = sedation, ataxia
26
Peripheral neuropathy, postherpetic neuralgia, migraine prophylaxis, bipolar disorder
Gabapentin
27
Phenobarbital
Simple, complex, tonic-clonic Increase GABAa action SE = sedation, induction P450, cardiorespiratory depression First line in neonates
28
Topiramate
Simple, complex, tonic-clonic Blocks Na channels, increase GABA action SE = sedation, MENTAL DULLING, kidney stones, WL
29
Migraine prevention
Topiramate
30
Lamotrigine
All Blocks voltage-gated Na channels SE = Stevens-Johnson syn (titrate slowly)
31
Levetiracetam
Simple, complex, tonic-clonic | May modulate GABA and glutamate release
32
Tiagabine
Simple, complex | Increase GABA by inhibiting reuptake
33
Vigabatrin
Simple, complex | Increase GABA by irreversibly inhibiting GABA transaminase
34
Stevens-Johnson syndrome
Prodrome of malaise and fever followed by rapid onset of erythematous/purpuric macules (oral, ocular, genital) Skin lesions progress to epidermal necrosis and sloughing
35
Barbiturates (4)
Phenobarbital, pentobarbital, thiopental, secobarbital Facilitate GABAa action by INCREASING DURATION of Cl- channel opening = decreases neuron firing Sedative (anxiety, seizures, insomnia); induction anesthesia (thiopental)
36
Barbiturate toxicity
Respiratory and cardiovascular depression CNS depression (exacerbated by EtOH) Dependence Induces P450 = drug interactions
37
Barbiturate overdose treatment
Supportive = assist respiration and maintain BP
38
Benzodiazepines
Diazepam, lorazepam, triazolam, temazepam, oxazepam, midazolam, chlordiazepoxide, alprazolam Facilitate GABAa action by INCREASING FREQUENCY of Cl- channel opening Decrease REM sleep Long half-lives and active metabolites (except short acting "TOM" = trizolam, oxazepam, midazolam = higher addictive potential)
39
Benzo use
Anxiety, spasticity, status epilepticus (lorazepam/diazepam) Detox = alcohol withdrawal DTs Night terrors, sleepwalking, general anesthetic, hypnotic
40
Benzo toxicity
Additive with alcohol Less risk respiratory depression and coma than barbs Overdose = FLUMAZENIL (comp antag at GABA benzo receptor)
41
Which three substances bind GABA a receptor
Benzos Barbs EtOH
42
Nonbenzodiazepine hypnotics | "All ZZZs put you to sleep"
``` Zolpidem = Ambien Zaleplon = Sonata esZopiclone = Lunesta Act via BZ1 subtype of GABA receptor Effects reversed by flumazenil Use = insomnia ```
43
Zolpidem, Zaleplon, Eszopiclone toxicity
Ataxia, HA, confusion Short duration = rapid met by liver Cause only modest day-after psychomotor depression and few amnestic effects Decreased dependence risk
44
Anesthetic general principles CNS drugs must be ___ or ___ Drugs with decreased solubility in blood have ___ induction and recovery times Drugs with increased solubility in lipids have ___ potency MAC?
CNS drugs must be LIPID soluble (cross BBB) or actively transported Drugs with DECREASED solubility in BLOOD = RAPID induction/recovery times Drugs with INCREASED solubility in LIPIDS = INCREASED potency = 1/MAC MAC = minimal alveolar concentration of inhaled anesthetic required to prevent 50% of subjects from moving in response to noxious stimuli
45
N2O with decreased blood and lipid solubility
Fast induction | Low potency
46
Halothane with high blood and lipid solubility
Slow induction | High potency
47
Inhaled anesthetics
Halothane, enflurane, isoflurane, sevoflurane, methoxyflurane, nitrous oxide MOA unknown Effects = myocardial depression, respiratory depression, nausea/emesis, INCREASED cerebral blood flow (decreased metabolic demand)
48
Inhaled anesthetic toxicity
Malignant hyperthermia = rare, life-threatening hereditary condition in which inhaled anesthetics (except NO) and succinylcholine induce fever and severe muscle contractions Tx = DANTROLENE
49
Treatment for malignant hyperthermia induced by inhaled anesthetic + succinylcholine?
Dantrolene
50
IV anesthetics
Barbiturates = thiopental (induction, short procedures) Benzodiazepines = midazolam (endoscopy; can cause resp depression, hypotension, anterograde amnesia) Arylcyclohexylamines (Ketamine) = PCP analogs, dissociative anesthetics, block NMDA receptors (CV stimulant; disorientation, hallucination, bad dreams) Opioids = morphine, fentanyl (general anesthesia) Propofol = RAPID INDUCTION, sedation ICU, short procedure (potentiates GABA a, less post op nausea)
51
Local anesthetic esters
Procaine Cocaine Tetracaine One "i"
52
Local anesthetic amides
Lidocaine Mepivacaine Bupivacaine Two "i's"
53
Local anesthetics
Block Na channels (bind activated so effective in rapidly firing neurons) Given with vasoconstrictors (epi) to enhance local action = decrease bleeding and increase anesthesia by decreasing systemic concentration
54
Order of nerve blockage - local anesthetics
Small diameter fibers > large Myelinated fibers > unmyelinated Small myelinated fibers > small unmyelinated fibers > large myelinated fibers > large unmyelinated fibers
55
Order of sensation loss - local anesthetics
Pain Temperature Touch Pressure
56
Local anesthetic toxicity
CNS excitation Severe CV toxicity (bupivacaine) HTN/hypotension Arrhythmias (cocaine)
57
Neuromuscular blocking drugs
Muscle paralysis in surgery or mechanical ventilation | Motor nicotinic receptor specific
58
Depolarizing NM blocking drugs
``` Succinylcholine = strong ACh receptor AGONIST = produces sustained depolarization and prevents muscle contraction Complications = hypercalcemia, hyperkalemia, malignant hyperthermia ```
59
Reversal of depolarizing NM blockers/succinylcholine (2 phases)
``` Phase I (prolonged depol) = no antidote; block potentiated by cholinesterase inhibitors Phase II (repolarized by blocked; ACh receptors available but desensitized) = antidote of CHOLINESTERASE INHIBITORS ```
60
Nondepolarizing NM blocking drugs
Tubocurarine, atracurium, mivacurium, pancuronium, vecuronium, rocuronium Competitive antagonists = compete with ACh for receptors
61
Reversal of nondepolarizing NM blockers
Neostigmine (given with atropine), edrophonium, and other cholinesterase inhibitors
62
Dantrolene
Muscle relaxant Prevents release of Ca from sarcoplasmic reticulum of skeletal muscle Use = tx malignant hyperthermia and neuroleptic malignant syndrome (toxicity of antipsychotic drugs)
63
Parkinson disease
Loss dopaminergic neurons and excess cholinergic activity | Decreased Da, increased ACh
64
Parkinson drugs
Dopamine agonists = Bromocriptine (ergot); pramipexole, ropinirole (non-ergot, preferred) Increase dopamine = Amantadine; L-dopa/carbidopa Prevent breakdown = Selegiline (MAO B inhibitor); entacapone, tolcapone (COMT inhibitors = prevent L-dopa degradation) Curb excess cholinergic acitivity = Benztropine (antimuscarinic; improves tremor and rigidity but has little effect on bradykinesia)
65
Bromocriptine, pramipexole, ropinirole
Da agonists | Parkinsons
66
Amantadine, L-dopa/carbidopa
Increase Da | Parkinsons
67
Selegiline
MAO B inhibitor = preferentially metabolizes Da over NE and 5HT Parkinsons
68
Entacapone, tolcapone
COMT inhibitors | Parkinsons
69
Benztropine
Antimuscarinic = improves Parkinson tremor and rigidity; little effect on bradykinesia
70
L-dopa (levodopa)/carbidopa
Increase dopamine in brain Levodopa = crosses BBB and is converted by dopa decarboxylase to dopamine Carbidopa = peripheral decarboxylase inhibitor; increases bioavailability in brain and limits peripheral SE Car
71
Levodopa/carbidopa SE
Arrhythmias from peripheral formation catecholamines Dyskinesia following administration (on-off phenomenon) Akinesia between doses
72
Alzheimer drugs
Alzheimer = decreased ACh Memantine Donepezil, galantamine, rivastigmine
73
Memantine
NMDA receptor antagonist for Alzheimer disease Helps prevent excitotoxicity (mediated by Ca) Tox = dizziness, confusion, hallucinations
74
Donepezil, galantamine, rivastigmine
AChE inhibitors for Alzheimer disease | Tox = nausea, dizziness, insomnia
75
Huntington drugs
Decreased GABA and ACh Increased Da Tetrabenazine and reserpine = inhibit vesicular monoamine transporter (VMAT); limit Da vesicle packaging and release Haloperidol = dopamine receptor antagonist
76
Sumatriptan
5HT1B/1D AGONIST Inhibits trigeminal nerve activation, prevents vasoactive peptide release, induces VASOCONSTRICTION Half life
77
Sumatriptan contraindications
Patients with CAD or Prinzmetal angina due to SE of coronary vasospasm

USMLE Pharmacology (15 decks)

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