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Drug administration routes that do not require passage through the liver first
Sublingual, rectal
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Drug absorption limited to nonionized, lipid soluble drugs
CSF absorption
-
Molecule largely responsible for binding drugs
Albumin (PCN and warfarin are 90% bound)
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Drug pharmacokinetics where a constant amount is eliminated regardless of dose
0 order kinetics
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drug pharmacokinetics where drug elimination is proportional to dose
1st order kinetics
-
number of half lives to reach a steady state
5
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amount of drug in body/amount of drug in plasma
volume of distribution
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fraction of unchanged drug reaching the systemic circulation
bioavailability
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drug level at which desired effect occurs in 50% of patients
ED50
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Drug level at which death occurs in 50% of patients
LD50
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Tolerance gained after only a few doses
Tachyphylaxis
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Dose required for drug to take effect
Potency
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Ability of a drug to achieve results without untoward effects
Efficacy
-
Inhibitors of P-450 (11)
Cimetidine, isoniazid, ketoconazole, erythromycin, cipro, flagyl, allopurinol, verapamil, amiodarone, MAOIs, disulfuram
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Inducers of P-450 (7)
ETOH, insecticides, cigarette smoke, Phenobarbital, dilantin, theophylline, warfarin
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Most important organ for eliminating drugs
Kidney
-
Water soluble drugs, more likely to be eliminated unaltered
Polar (ionized) drugs
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Fat soluble drugs, more likely to be metabolized before excretion
Nonpolar (nonionized) drugs
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Anti-inflammatory that binds tubulin and inhibits migration
Colchicine
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Anti-inflammatory used in gout
Indomethacin
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Xanthine oxidase inhibitor that blocks uric acid formation from xanthene, used in uric acid chronic overproducers
Allopurinol
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Gout drug that increases renal secretion of uric acid; used for undersecreters
Probenecid
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Dopamine receptor blocker that can be used to increase gastric motility
Metoclopramide
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Serotonin receptor inhibitor used as an antiemetic
Zofran
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Long-acting somatostatin analog
Octreotide
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Drug that inhibits Na/K ATPase and increases myocardial calcium, increasing atrial contraction but slowing AV conduction
Digoxin
-
Drug used to treat torsades
Magnesium
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Drug that causes transient disruption of the AV node
Adenosine
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Best single agent shown to reduce mortality in CHF patients
ACE inhibitors
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Drugs that reduce risk of MI and Afib postoperatively
Beta blockers
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Acetylcholine antagonist that increases heart rate
Atropine
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2 drugs that inhibit adrenal steroid synthesis
metyrapone, aminoglutethimide
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GnRH analog that inhibits LH and FSH release from pituitary
Leuprolide
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Drug that acts on V1 receptors as a contrictor; can be used in GI bleeding by reducing blood flow
Vasopressin
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Prostaglandin inhibitor used to close PDA in children; also used in gout
Indomethacin
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PGE1 derivative used to prevent PUD
Misoprostol
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Prostaglandin synthesis inhibitors, lead to dec mucus and HCO3- secretion and inc acid production
NSAIDs
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Symptoms of ASA poisoning (5)
Tinnitus, headache, nausea, vomiting, respiratory alkalosis then metabolic acidosis
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Treatment of Tylenol overdose
N-acetylcysteine
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Fibrinolytic used in sepsis; inactivates the inhibitor of protein C
Xigris (activated protein C)
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