1. Aspirin: acidic or basic? 0- or 1st- order elimination?
    Weakly acidic (give bicarbonate), 0-order elimination (PEA)
  2. Amphetamines: acidic or basic?
    Weakly basic
  3. Loading dose
    Target dose * Vd / bioavailability
  4. Overdose of a weakly basic drug (ex. amphetamines)
    Give ammonium chloride, since it's trapped in another acidic environment.
  5. Phase 1 metabolism
    CYP450: redox, hydrolysis. Afterward, the metabolite will be slightly water-soluble & polar. Old people lose Phase I first.
  6. Phase 2 metabolism
    Conjugation to make it more water-soluble for excretion: metabolites are now very polar & inactive. Acetylation, glucuronidation, sulfation.
  7. Bethanechol
    • Activates bowel & bladder smooth muscle -- for ileus (post-op or neurogenic) or urinary retention.
    • BethAnne, call me...
  8. Pilocarpine
    Pile on the sweat & tears... and weight (b/c saliva stimulated too).
  9. Carbachol
    Eyes: for glaucoma, pupil contraction, release intraocular pressure
  10. Methacholine
    For asthma dx. A challenge test, b/c this drug stimulates muscarinic receptors in airway.
  11. The -stigmines
    • "Keep, the stale, stagnant one around longer" = parasympathetic. Very stagnant & boring, b/c they don't even work directly... they slow the ACh breakdown enzyme (anti-cholinesterase), so ACh stays around longer to stimulate muscarinic receptors.
    • All are good for either m.gravis (where you're losing ACh receptors) or glaucoma.
  12. Neostigmine
    • For: ileus & urinary retention (same as bethanechol), m.gravis, reverse NMJ blockade post-operatively.
    • NO CNS penetration.
  13. Name the muscarinic antagonists useful for: eyes, CNS, respiratory, GU, GI
    • Eyes = atropine, tropicamide, homatropine (pupil dilators)
    • CNS = benztropine (Parkinson's -- park my Benz), scopolamine (motion sickness)
    • Respiratory = ipratropium bromide inhaler
    • GU = oxybutynin, glycopyrrolate
    • GI = methscopolamine, pirenzepine, propantheline
  14. Antidote for cholinesterase inhibitor poisoning (ex. neostigmine)
    Atropine, an antagonist.
  15. Epinephrine
    Stimulates all 4 (alpha 1&2, beta 1&2)... but at low doses, B1 predominates. Used for glaucoma, anaphylaxis, severe asthma, hypotension.
  16. Norepinephrine
    Alpha-1 and -2 > B1
  17. Dopamine
    All 3: D > B > A. Used for HF and shock (due to dec'd renal perfusion).
  18. Amphetamine
    General sympathetic agonist. Weak base. Used for ADD, narcolepsy, obesity.
  19. The 4 selective B-2 agonists
    • Metaproterenol
    • Albuterol
    • Salmeterol
    • Terbutaline
    • (MAST)
  20. Mirtazapine
    Alpha-2-selective antagonist, used for depression. Inc'd serum cholesterol & appetite.
  21. DHPR Ca++ channel blockers
    • More potent than non-DHPR, because the DHPR ones control many RyR channels in sarcoplasmic reticulum.
    • Amlodipine, nifedipine.
  22. Non-DHPR Ca++ channel blockers
    Verapamil, diltiazem. Not as potent. Decreased inotropy, so watch for excess bradycardia with Ca++ channel blocker + B-blocker.
  23. Methanol vs. ethylene glycol: what do they become, & what are the consequences?
    • Methanol --> formaldehyde: blindness (retinal damage) + acidosis
    • Ethylene glycol --> oxalic acid: toxic to kidneys/acidosis. (Makes sense; salicylic acid is also nephrotoxic.)

    Both use alcohol dehydrogenase.
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