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USMLE 1 > Neurology- Pharmacology > Flashcards

Neurology- Pharmacology Flashcards

1
Q

Epilepsy drugs

A

Pag. 528

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2
Q

Eclampsia seizures 1st line treatment

A

MgSO4

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3
Q

Seizures 1st line in neonates

A

Phenobarbital (phenoBABYthal)

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4
Q

Phenytoin, fosphenytoin

- Adverse effects

A 
PHENYTOIN: 
P450 induction, 
Hirsutism, 
Enlarged gums, 
Nystagmus, 
Yellow-brown skin, 
Teratogenicity (fetal hydantoin syndrome),
Osteopenia, 
Inhibited folate absorption,
Neuropathy
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5
Q

Vigabatrin action mechanism

A

Irreversible GABA TRansaminase INihibitor:

viGABATRIN

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6
Q

Barbiturates

  • Names
  • Mechanism
  • Clinical uses
A

Phenobarbital, pentobarbital, thiopental, secobarbital

Facilitate GABA-A action

Sedative for anxiety, seizures, insomnia, induction of anesthesia (thiopental).

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7
Q

Barbiturates

- Adverse effects

A

Respiratory and cardiovascular depression; CNS depression (can be exacerbated by alcohol use); dependence; drug interactions (induces cytochrome P-450).

Overdose treatment is supportive (assist respiration and maintain BP). Contraindicated in porphyria

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8
Q

Benzodiazepines

  • Mechanism
  • Short acting benzoodiazepines
A

Facilitate GABAA action

Mosthave long half-lives and active metabolites (exceptions [ATOM]: Alprazolam, Triazolam, Oxazepam, and Midazolam are short acting)

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9
Q

Benzodiazepines

  • Adverse effects
  • Benzodiazepines with liver disease
A

Dependence, additive CNS depression effects with alcohol. Treat overdose with flumazenil

“OK for Terrible Livers”
Oxazepam, Temazepam, and Lorazepam: they can be used to treat alcohol withdrawal in patients with liver disease due to minimal first-pass metabolism.

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10
Q

Nonbenzodiazepine hypnotics

  • Names
  • Mechanism
  • Clinical use
  • Adverse effects
A

hypnotics Zolpidem, Zaleplon, esZopiclone

Act via the BZ1 subtype of the GABA receptor. Effects reversed by flumazenil. Sleep cycle less affected.

Insomnia

Ataxia, headaches, confusion, low dependence risk.

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11
Q

Suvorexant

  • Mechanism
  • Clinical use
  • Adverse effects
A

Orexin (hypocretin) receptor antagonist

Insomnia

CNS depression, headache, dizziness, abnormal dreams, upper respiratory tract infection. Contraindicated with strong CYP3A4 inhibitors

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12
Q

Ramelteon

  • Mechanism
  • Clinical use
  • Adverse effects
A

Melatonin receptor agonist, binds MT1 and MT2 in suprachiasmatic nucleus.

Insomnia

Dizziness, nausea, fatigue, headache. No dependence

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13
Q

Triptans (sumatriptan)

  • Mechanism
  • Clinical use
  • Adverse effects
A

5-HT1B/1D agonists. Inhibit trigeminal nerve activation; prevent vasoactive peptide release; induce vasoconstriction.

Acute migraine, cluster headache attacks.

Coronary vasospasm, mild paresthesia, serotonin syndrome

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14
Q

Parkinson disease drugs

A

BALSA

Bromocriptine, Amantadine, Levodopa (with carbidopa), Selegiline (and COMT inhibitors), Antimuscarinics

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15
Q

Dopamine agonists

A

Ergot—Bromocriptine.

Non-ergot (preferred)—pramipexole, ropinirole; toxicity includes impulse control disorder, postural hypotension, hallucinations/confusion.

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16
Q

Drugs increasing dopamine availability

A

Amantadine; toxicity = ataxia, livedo reticularis

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17
Q

Drugs increasing l-DOPA availability (agents act peripheral)

A

ƒ Levodopa (l-DOPA)/carbidopa—carbidopa blocks peripheral conversion of l-DOPA to dopamine by inhibiting DOPA decarboxylase

ƒ Entacapone prevents peripheral l-DOPA degradation by inhibiting COMT. Used in conjunction with levodopa.

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18
Q

Drugs: Prevent dopamine breakdown (agents act centrally)

A

ƒƒ Selegiline, rasagiline—block conversion of dopamine into DOPAC by selectively inhibiting MAO-B.

ƒƒ Entacapone—blocks conversion of dopamine by inhibiting central COMT.

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19
Q

Drugs: Curb excess cholinergic activity

A

Benztropine, trihexyphenidyl (Antimuscarinic; improves tremor and rigidity but has little effect on bradykinesia in Parkinson disease).

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20
Q

Levodopa/carbidopa

- Adverse effects

A

Nausea, hallucinations, postural hypotension from increase peripheral formation of catecholamines.

Long-term use can lead to dyskinesia following administration (“on-off” phenomenon), akinesia between doses.

21
Q

Tetrabenazine, reserpine

A

Inhibit vesicular monoamine transporter (VMAT) dopamine.

Huntington chorea, tardive dyskinesia

22
Q

Riluzole

A

Decrease neuron glutamate excitotoxicity

ALS (Lou Gehrig)

23
Q

Alzheimer disease drugs

A

Memantine: NMDA receptor antagonist; helps prevent
excitotoxicity

Donepezil, rivastigmine, galantamine: AChE inhibitors.

24
Q

Anesthetics—general principles

- MAC

A

Minimal Alveolar Concentration (of inhaled anesthetic) required to prevent 50% of subjects from moving in response to noxious stimulus (eg, skin incision).

25
Q

Anesthetics—general principles

  • Low solubility in blood
  • High solubility
A

Rapid induction and recovery times: Nitous oxide

High potency = 1/MAC: Halothane, propofol, and thiopental (high potency and slow induction)

26
Q

Inhaled anesthetics

  • Names
  • Mechanism
  • Effects
A

Desflurane, halothane, enflurane, isoflurane, sevoflurane, methoxyflurane, N2O.

Mechanism unknown.

Myocardial depression, respiratory depression, nausea/emesis, increase cerebral blood flow.

27
Q

Inhaled anesthetics

- Adverse efects

A

Hepatotoxicity (halothane),
Nephrotoxicity (methoxyflurane),
Proconvulsant (enflurane, epileptogenic),
Expansion of trapped gas in a body cavity (N2O).

28
Q

Malignant hyperthermia

  • Cause
  • Mutation
  • Treatment
A

inhaled anesthetics or succinylcholine induce fever and severe muscle contraction.

Mutations in voltage-sensitive ryanodine receptor (RYR1 gene) cause  Ca2+ release from sarcoplasmic
reticulum. AD

Treatment: dantrolene

29
Q

Intravenous anesthetics

A

Thiopental, Midazolam, Propofol (potentiates GABA A), Ketamine (NMDA antagonist)

30
Q

Anesthesia use

  • Thiopental
  • Midazolam
  • Propofol
  • Ketamine
A

Induction of anesthesia, short surgical procedures

Procedural sedation (eg, endoscopy), anesthesia induction

Rapid anesthesia induction, short procedures, ICU
sedation

Dissociative anesthesia. Sympathomimetic

31
Q

Anesthesia characteristics

  • Thiopental
  • Midazolam
  • Ketamine
A

Decrease cerebral blood flow. High lipid solubility. Effect terminated by rapid redistribution into tissue and fat

May cause severe postoperative respiratory depression, low BP, anterograde amnesia.

Increase cerebral blood flow. Emergence reaction
possible with disorientation, hallucination, vivid dreams.

32
Q

Local anesthetics

  • Esters
  • Amides
A

Esters—procaine, tetracaine, benzocaine, chloroprocaine.

Amides—lidocaIne, mepivacaIne, bupivacaIne, ropivacaIne (amIdes have 2 I’s in name).

33
Q

Local anesthetics

- Mechanism

A

Block Na+ channels by binding to specific receptors on inner portion of channel. Most effective in rapidly firing neurons.

  • Can be given with vasoconstrictors (usually epinephrine) to enhance local action
  • In infected (acidic) tissue, alkaline anesthetics are charged and cannot penetrate membrane effectively
34
Q

Local anesthetics

- Order of loss

A

(1) pain, (2) temperature, (3) touch, (4) pressure.

35
Q

Local anesthetics

- Adverse effects

A

CNS excitation, severe cardiovascular toxicity (bupivacaine), hypertension, hypotension, arrhythmias (cocaine), methemoglobinemia (benzocaine).

36
Q

Neuromuscular blocking drugs

  • Mechanism
  • Depolarizing drugs
A

Muscle paralysis in surgery or mechanical ventilation. Selective for Nm nicotinic receptors.

Succinilcoline

37
Q

Nondepolarizing neuromuscular blocking drugs

A

Atracurium, cisatracurium, pancuronium, rocuronium, tubocurarine, vecuronium—competitive with ACh for receptors

Reversal of blockade—neostigmine (must be given with atropine or glycopyrrolate), edrophonium, and other cholinesterase inhibitors.

38
Q

Dantrolene

  • Mechanism
  • Clinical use
A

binding to the ryanodine receptor.

Malignant hyperthermia and neuroleptic malignant syndrome (a toxicity of antipsychotic drugs).

39
Q

Baclofen

  • Mechanism
  • Clinical use
A

Skeletal muscle relaxant. GABAB receptor agonist

Muscle spasticity, dystonia, multiple sclerosis

40
Q

Cyclobenzaprine

  • Mechanism
  • Clinical use
  • Adverse effects
A

Skeletal muscle relaxant. Acts within CNS.

Muscle spasms.

Anticholinergic side effects. Sedation.

41
Q

Opioid analgesics

  • Full agonist
  • Partial agonist
  • Mixed agonist/antagonist
  • Antagonist
A

Morphine, heroin, meperidine, methadone, codeine.

buprenorphine

nalbuphine, pentazocine.

naloxone, naltrexone, methylnaltrexone

42
Q

Opioid analgesics

- Mechanism

A

Act as agonists at opioid receptors (μ = β-endorphin, δ = enkephalin, κ = dynorphin) to modulate synaptic transmission

43
Q

Opioid analgesics

- Clinical use

A
  • Moderate to severe or refractory pain,
  • Cough suppression (dextromethorphan),
  • Diarrhea (loperamide, diphenoxylate),
  • Acute pulmonary edema,
  • Maintenance programs for heroin addicts (methadone, buprenorphine + naloxone).
44
Q

Opioid analgesics

- Adverse effects

A

Nausea, vomiting, pruritus, addiction, respiratory depression, constipation, sphincter of Oddi spasm, miosis (except meperidine Ž mydriasis), additive CNS depression with other drugs

45
Q

Pentazocine

  • Mechanism
  • Clinical use
  • Adverse effects
A

κ-opioid receptor agonist and μ-opioid receptor weak antagonist or partial agonist.

Analgesia for moderate to severe pain.

Can cause opioid withdrawal symptoms

46
Q

Butorphanol

  • Mechanism
  • Clinical use
  • Adverse effects
A

κ-opioid receptor agonist and μ-opioid receptor partial agonist.

Severe pain (eg, migraine, labor). Causes less respiratory depression than full opioid agonists.

can precipitate withdrawal. Not easily reversed with naloxone

47
Q

Tramadol

  • Mechanism
  • Clinical use
  • Adverse effects
A

Very weak opioid agonist; also inhibits 5-HT receptors.

Chronic pain

Similar to opioids. Decreases seizure threshold. Serotonin syndrome.

48
Q

Glaucoma drugs

  • β-blockers
  • α-agonists
  • Diuretics
A

Timolol, betaxolol, carteolol

Epinephrine (α1), apraclonidine, brimonidine (α2)

Acetazolamide

49
Q

Glaucoma drugs

  • Prostaglandins
  • Cholinomimetics (M3)
A

Bimatoprost, latanoprost (PGF2α)

Direct: pilocarpine, carbachol
Indirect: physostigmine, echothiophate

USMLE 1 (73 decks)

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