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USMLE Step 1 Pharmacology | High-Yield Drug Review & Practice Questions | 2026/2027

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Complete USMLE Step 1 pharmacology review covering high-yield drugs, mechanisms of action, adverse effects, indications, contraindications, drug interactions and clinical applications with practice questions and verified answers for 2026/2027.

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USMLE Step 1 Drugs | High-Yield Pharmacology Review | Complete Practice Questions & Verified Answers

General MOA of local anesthetics block VGNCs, blocking initiation and propagation of action potentials




Name the ester local anesthetics cocaine, benzocaine, procaine




Name the amide local anesthetics lidocaine, bupivacaine, mepivacaine, ropivacaine, prilocaine




Why is epinephrine or NE often given with local local anesthetics cause vasodilation leading to short duration of action, epi and
anesthetics? NE cause vasoconstriction causing increased DOA



What are common ADRs of local anesthetics antihistaminic, anticholinergic, antiarrhythmic actions (esp Lidocaine)

methemoglobinemia (prilocaine)
transient neurological symptoms
LAST (local anesthetic systemic toxicity)
LAST cardiotoxicity in bupivacaine
allergic reactions to ester LA due to PABA metabolites


Blood/gas partition coefficient determines the solubility of a gas in anesthetic in the blood which in turn
determines the onset of action of the drug. Drugs with high coefficients are more
soluble in the blood, demonstrate slower equilibration in the brain/tissues, and
have longer onset times.


Nitrous Oxide Use: induction of general anesthesia

MOA: NMDA antagonist

ADRs: loss of balance, ataxia, peripheral neuropathy


Common ADRs of inhaled anesthetics myocardial depression (decreased CO + hypotension)
respiratory depression
malignant hyperthermia (except N2O)
increased cerebral blood flow


Fluorinated inhaled anesthetics Isoflurane, desflurane, halothane




Thiopental Use: induction of anesthesia for procedures without significant pain

MOA: ultra-short acting barbiturate (increases duration GABA-A channel)

ADRs: poor analgesia, respiratory depression, poor skeletal muscle relaxation


Etomidate Use: IV for induction of general anesthesia that is hemodynamically neutral
(minimal effect on HR, CO, peripheral circulation)

MOA: increases GABA-A (non-barbiturate)

ADRs: adrenal suppression, not an analgesic


Propofol Use: induction, maintenance of anesthesia, increased lipophilicity = quick onset

MOA: emulsion, increases GABA-A activity (non-barbiturate)

ADRs: vasodilation, increased TGs, respiratory depression, anaphylaxis

,USMLE Step 1 Drugs | High-Yield Pharmacology Review | Complete Practice Questions & Verified Answers
Ketamine, PCP Use: emergency surgeries, outpatient procedures - dissociative anesthesia,
increases sympathetics (HR, BP) - good for hypovolemic, cardiogenic shock,
asthmatics

MOA: NMDAr antagonist

ADRs: prolonged retention in body, Psych emergence symptoms- nightmares,
flashbacks


Dantrolene Use: cure for malignant hyperthermia (inhaled anesthetics, succinylcholine)

MOA: blocks ryanodine receptor and Ca release from sarcoplasmic reticulum in
skeletal muscle

ADRs: hepatotoxicity


Sugammadex cure for NMJ blockade by nondepolarizing NMB (rocuronium, vecuronium)




Spasmolytic Drugs Benzos
Barbs
Gabapentin
Riluzole
Tizanidine
Dantrolene
Botulinum toxin


L-DOPA (levodopa) Use: PD

MOA: DA precursor in blood that can be converted to DA in the brain

ADRs:
L-dopa induced dyskinesias (choreoathetosis of face and distal extremities)
cardiac arrhythmias: tachycardia, ventricular extrasystoles
HTN
anorexia, n/v
depression, anxiety, psychosis (tx w/ pimavanserin)


Carbidopa, Benserazide Use: PD

MOA: prevents breakdown of L-DOPA by dopa-decarboxylase in periphery


Entacapone, Tolcapone Use: PD

MOA: COMT inhibitors, prevent breakdown of L-dopa in periphery

ADRs: tolcapone - hepatotoxic, can cross BBB

"Al Capone COMiTs crime"


Selegilline, Rasagilline Use: PD

MOA: MAO-B inhibitors, prevents breakdown of DA in the brain

ADRs: Selegilline can cause hallucinations, rasagilline - impulse control
disorders

"you want LINEs when you MAO the lawn"


Bromocriptine, Pramipexole, Ropinirole Use: PD for younger pts with less severe PD

MOA: DA agonists

ADRs: dyspepsia, reflux esophagitis, CV, impulse control, CNS effects
withdrawal symptoms


Amantadine Use: PD, antiviral

MOA: NMDAr antagonist, blocks reuptake of DA into presynaptic neuron and
increases DA synthesis

ADRs: peripheral edema, livedo reticularis

, USMLE Step 1 Drugs | High-Yield Pharmacology Review | Complete Practice Questions & Verified Answers
Tetrabenazine Use: Huntington's

MOA: synaptic vesicular amine transporter inhibitor, decreases cerebral DA and
therefore chorea


Benztropine, Trihexyphenidyl anticholinergics (antimuscarinics) used to treat PD tremors and rigidity but not
bradykinesia



Donepezil, Rivastigmine, Galantamine Use: Alzheimer's

MOA: cholinesterase inhibitors

ADRs: GI, bradycardia, hypotension, sleep disturbances


Memantine Use: AD

MOA: NMDAr antagonist

ADRs: HA, dizziness, constipation


Aducanumab, lecanemab Use: AD

MOA: bind amyloid beta plaques, slows progression


Riluzole Use: ALS

MOA: reduces glutamate-induced excitotoxicity (inhibits glutamate release,
blocks NMDAr, blocks VGNC)


Drugs for bipolar disorder (mood stabilizers) lithium
VPA
lamotrigine
carbamazepine
oxcarbazepine


Lithium Use: bipolar disorder mania

MOA: Li ion inhibits IP3 and DAG signaling

ADRs:
hypothyroidism with goiter
polyuria, polydipsia
nephrogenic DI
teratogen: Ebstein's anomaly, malformed tricuspid

DI: decreased clearance with thiazides, NSAIDs, ACEIs


Lamotrigine Use: broad spec antiepileptic, bipolar disorder depressed phase

MOA: glutamate inhibition, blocks VGNC

ADRs: SJS

"Lame-O both glutamate and sodium channel block"


VPA (valproic acid) Use: first line antiepileptic, focal + generalized, bipolar disorder

MOA: inactivates Na channels, increases GABA concentration

ADRs:
anemia
thrombocytopenia
LFT elevation (hepatotoxic)
NTD
pancreatitis

"ALPRO - anemia, liver, pancreatotis, rO (hole NTD)"

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