Chapter 7 - Medicines and Pharmacology Flashcards
Requirement for skin absorption?
Lipid solubility through the epidermis
Requirement for CSF absorption?
Nonionized, lipid-soluble drugs
Sulfonamides will do what in newborns?
Displace unconjugated bilirubin
What is 0 order kinetics?
Constant amount of drug is eliminated regardless of dose
What is 1st order kinetics?
Drug eliminated proportional to dose
How many half-lives for a drug to reach steady state?
5
Where are tetracycline and heavy metals stored?
In bone
Volume of distribution is equal to what?
Amnt of drug in the body divided by amnt of drug in plasma or blood
High volume of distribution means what?
Higher concentrations in the extravascular compartment compared with intravascular concentrations
What is bioavailability?
Fraction of unchanged drug reaching the systemic circulation; 100% for IV drugs
What is ED50?
Drug level at which desired effect occurs in 50% of patients
What is LD50?
Drug level at which death occurs in 50% of patients
What is tachyphylaxis?
Tolerance after only a few doses
What is potency?
Dose required for effect
What is efficacy?
Ability to achieve result without untoward effect
What is Phase I of microsomal drug metabolism?
Demethylation, oxidation, reduction, hydrolysis reaction (requries NADPH/O2)
What is Phase II of microsomal drug metabolism?
Glucuronic acid (#1) and sulfates attached (forms water-soluble metabolite)
Inhibitors of P-450?
Cimetidine, isoniazid, ketoconazole, erythromycin, Cipro, Flagyl, allopurinol, verapamil, amiodarone, MAOIs, disulfiram
Inducers of P-450?
Cruciform vegetables, ETOH, insecticides, cigarette smoke, phenobarbital, dilantin, theophylline, warfarin
Most important organ for eliminating most drugs?
Kidney
How are polar (ionized) drugs eliminated?
More water soluble, more likely to be eliminated in unaltered form
How are nonpolar (nonionized) drugs eliminated?
More fat soluble, more likely to be metabolized before excretion
What causes gout?
Uric acid buildup; end product of purine metabolism
Colchicine MOA?
Anti-inflammatory; binds tubulin, inhibits migration
Allopurinol MOA?
Xanthine oxidase inhibitor, blocks uric acid formation from xanthine
Probenecid MOA?
Increases renal secretion of uric acid
Side effect of cholestyramine?
Can bind Vit K and cause bleeding tendency
Side effect of HMG-CoA reductase inhibitors?
Liver dysfunction, rhabdo
Side effect of niacin?
Flushing (Tx: ASA)
Side effect of promethazine?
Tardive dyskinesia (inhibits dopamine receptors); Tx: Benadryl
Metoclopramide MOA?
Dopamine receptor blocker, used to increase gastric/gut motility
Ondansetron MOA?
Serotonin receptor inhibitor
Digoxin MOA?
Inhibits Na/K ATPase and increases myocardial calcium; increases atrial contraction rate but slows AV conduction
Side effects of digoxin?
Decreased blood flow to intestines, has been implicated in causing mesenteric ischemia; hypokalemia, increases sensitivity of heart to digitalis causing arrhythmias/AV block; visual changes (yellow hue), fatigue
Side effects of procainamide?
Lupus-like syndrome, pulmonary fibrosis, torsades (follow drug levels and QT intervals, torsades treated w/ Mg2+)
Adenoside MOA?
Transient interruption of the AV node
What is the best single agent shown to reduce mortality in pts with CHF?
ACE-I
When can ACE-I precipitate renal failure?
In pts with renal artery stenosis
What medication can reduce the risk of MI and a fib post-op?
Beta-blockers
Atropine MOA?
ACh antagonist; increases heart rate
Leuprolide MOA?
Analogue of GnRH and LHRH; inhibits release of LH and FSH from pituitary when given continuously (paradoxic effect)
Vasopressin MOA?
Acts on V-1 receptors found on vascular smooth muscle causing constriction
Indomethacin MOA and uses?
Inhibits prostaglandin production; used to close PDA in children and used in pts with gout
Misoprostol MOA and uses?
PGE1 derivative; protective prostaglandin used to prevent PUD
Mechanism of ulcer formation in patients on NSAIDs?
Inhibits prostaglandin synthesis and leads to decreased mucus and HCO3- secretion and increases acid production
Haldol side effect?
Extrapyramidal manifestations
Symptoms of ASA poisoning?
Tinnitus, headaches, nausea, vomiting; 1st respiratory alkalosis, 2nd metabolic acidosis
Side effect of gadolinium?
Nausea