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SGU Pharmacology basics

  1. Dosing Rate = 
    Image Upload 2

    • TC = target concentration
    • F = bioavailability
  2. Loading Dose = 
    Image Upload 4

    • TC = target concentration
    • F = bioavailability
  3. Vd =
    Image Upload 6

    or

    Image Upload 8
  4. CL =
    Image Upload 10

    or

    Image Upload 12  (for first order)

    or

    Image Upload 14  (for zero order)
  5. t1/2 =
    Image Upload 16
  6. Efficacy
    The maximal effect (Emax) an agonist can produce.
  7. Potency
    The concentration (EC50) of a drug required to produce 50% of the maximal effect.
  8. Chemical antagonism example:
    Protamine - positively charged and counteracts the negatively charged heparin.
  9. Inverse antagonist examples (2):
    Famotidine & Metoprolol
  10. Tachyphylaxis
    Desensitization, or the effect of a drug to gradually diminish when given continuously or repeatedly.
  11. Therapeutic index = 
    Image Upload 18

    or

    Image Upload 20
  12. Henderson-Hasselbalch equation:
    pH = pK + logImage Upload 22
  13. F =
    Image Upload 24

    F = bioavailability
  14. Bioequivalence = 
    If the two concentration-time plots are nearly superimposable, the preparations are said to be bioequivalent:  one can replace the other safely.
  15. In plasma:

    acidic drugs bind =

    basic drugs bind =
    acidic = albumin

    basic = alpha1-acid glycoprotein
  16. Warfarin-sulfonamide interaction:
    Sulfonamide displaces warfarin from albumin, causing a massive increase in plasma concentration, which may lead to bleeding.
  17. Enzyme systems involved in phase I conjugation reactions are located in:
    the ER
  18. Enzyme systems involved in phase II conjugation reactions are located in:
    the cytosol
  19. xenobiotic receptors (3):
    aryl hydrocarbon receptor (AhR)

    pregnane X receptor (PXR)

    constitutively active receptor (CAR)

    [all promote CYP induction]
  20. carbamazepine
    antiepileptic that induces CYP3A4 and is metabolized by CYP3A4.
  21. Drugs that increase the synthesis of one or more P450 isoforms (3):
    phenobarbital

    rifampin

    carbamazepine
  22. Drugs that significantly inhibit P450 isoforms:
    amiodarone, cimetidine, azole antifungals (ketoconazole), macrolide antibiotics (erythromycin), chloramphenicol, ritonavir, grapefruit juice (furanocoumarins)

    bold: appears on drug list
  23. Acetaminophen metabolism:
    5% metabolized by CYP2E1 to NAPQI, which is toxic to liver tissues
  24. Antidote to acetaminophen poisoning:
    N-acetylcysteine
  25. Glomerular capillary filtration size:
    MW < 20,000
  26. Zero-order elimination is reached with (3):
    aspirin

    ethanol

    phenytoin

    A constant amount of drug is eliminated per unit time.
  27. Accumulation Factor (AF) =
    Image Upload 26
  28. PCss =
    PC1 x AF
Author
SGU
ID
193666
Card Set
SGU Pharmacology basics
Description
Flash cards for pharmacology at St. George's University SOM.
Updated

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