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)"