PK - drugs

omeprazole

acid unstable drug that requires enteric coating

aspirin

irritating drug that is formulated with enteric coating that only dissolves in the SI

2-4 hrs + 6 times

half life of morphine and no. of adm. times

heparin

drug poorly absorbed in the GI tract and adm. parenterally

insulin

• drug that is unstable in the GI tract and adm. parenterally

• destroyed in the GI tract by degradative enzymes

rocuronium

neuromuscular blocker not absorbed orally and adm. IV

polyethylene glycol

Depot preparations often consist of a suspension of the drug in a nonaqueous vehicle such as ____

• haloperidol

• depot medroxyprogesterone

2 ex. of sustained-release drugs

• insulin

• heparin

2 drugs commonly adm. subcutaenously

• albuterol (bronchodilator)

• fluticasone (corticosteroid)

2 ex. of oral inhalation drugs

• oxymetazoline (nasal decongestant)

• mometasone furoate (corticosteroid)

2 ex. of nasal inhalation drugs

desmopressin

drug adm. intranasally in the treatment of diabetes insipidus

(intrathecal) amphotericin B

used in treating cryptococcal meningitis

clotrimazole

cream applied directly to the skin for the treatment of fungal infections

• nitroglycerin (antianginal)

• scopolamine (antiemetic)

• nicotine (smoking cessation)

3 drugs used transdermally

vitamin B12

vitamin that is transported across the gut wall by endocytosis

norepinephrine

neurotransmitter stored in intracellular vesicles in the nerve terminal and released by exocytosis.

90%

% of nitroglycerin cleared during first pass metabolism

penicillin G

antibiotic that is unstable in pH of gastric contents

propofol

Variation in blood flow partly explains the short duration of hypnosis produced by an IV bolus of ____

acrolein

• metabolite of cyclophosphamide

• can cause hemorrhagic cystitis because it accumulates in the bladder

zero-order / nonlinear

In high doses, aspirin, ethanol, and phenytoin is eliminated according to ____ kinetics

Michaelis-Menten kinetics

The metabolic transformation of drugs catalyzed by enzymes

CYP2D6

some individuals obtain no benefit from the analgesic codeine as they lack the _____ enzyme

clopidogrel

prodrug that carries a warning that patients who are poor CYP2C19 metabolizers have a higher incidence of cardiovascular events

• phenobarbital

• rifampin

• carbamazepine

• 3 drugs capable of increasing the synthesis of one or more CYP isozymes

• results in increased biotransformation of drugs

• can lead to significant decreases in plasma concentrations of drugs metabolized by these CYP isozymes + concurrent loss of pharmacologic effect

rifampin

antituberculosis drug that decreases the plasma concentrations of HIV protease inhibitors, thereby diminishing their ability to suppress HIV replication

St. John’s wort

herbal product that is a potent CYP3A4 inducer

omeprazole

drug which is a potent inhibitor of three of the CYP isozymes responsible for warfarin metabolism

• erythromycin

• ketoconazole

• ritonavir

3 important CYP inhibitors as each inhibit several CYP isoenzymes

grapefruit

juice which inhibits CYP3A4 and leads to higher levels of drugs (ex. nifedipine,clarithromycin, simvastatin)

morphine-6-glucuronide

compound more potent than morphine

• phenobarbital

• bicarbonate

patient presenting with _____ (weak acid) overdose can

be given _____, which alkalinizes the urine and keeps the

drug ionized, thereby decreasing its reabsorption

zolpidem

single dose sleep inducing agent

• digoxin

• warfarin

• cyclosporine

3 drugs with small therapeutic window