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25 Cards in this Set

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After normal dose, which would be the cause of altered drug levels (other than normal), pharmacodynamics or pharmacokinetics?
Pharmacokinetics (altered drug disposition)
If there are no changes in dose and plasma levels, and response is changed, what is the cause pharmacodynamics or pharmacokinetics?
pharmacodynamic (altered drug sensitivity)
Name 7 causes of altered drug disposition in neonates.
Absorptions: 1) Prolonged gastric emptying and fluctuation pH. 2) erratic intramuscular absorption (due to small muscles), 3) greater cutaneous absorption (high surface area ratio)... Distribution: 4) Body water and fat ratio changes in first year of life (they have more water at birth), 5) less plasma proteins... Elimination: 6) immature CYP in liver, 7) poor renal blood flow, filtration and secretion

REWIEW THE HANDOUT!!!!!
None
Why do neonates of addicted mothers get jaundice?
they are deficient in glucuronyl transferase to metabolis the drug
Give 9 problems associated with aging and metabolism of drugs.
1) Decreased CO, 2) decreased liver blood flow, 3) decreased renal blood flow, 4) increased gastric pH and slowing of gastric emptying intestinal absorption --> slower absorption, 5) decrease in Phase I metabolism, 6) increase fat in organs, 7) decreased muscle mass, 8) decreased water compartment, 9) altered Vd
Because of a greater proportion of fat in elderly, what happens to Vd and plasma concentration in WATER soluble drugs?
decrease in Vd, and increased plasma concentration
Because of a greater proportion of fat in elderly, what happens to Vd and plasma concentration in LIPID soluble drugs?
higher Vd and lower [plasma]
In obese people, drugs that are limited to plasma and/or total body fluid are dosed based on what?
Ideal body weight or idea body weight plus a little extra for increased body fluid
Stop here
What effect on drug half-life does liver and renal disease have?
increased half-life for many drugs
What is the adverse side effect of antibiotic use with digoxin in some patients? Why?
digoxin intoxication, the antibiotic kills a type of bacteria that inactivates digoxin, so kill it off and overdose occurs… due to polymorphism
What effect does the suppression of gut bacteria (via oral antibiotics) have on half life on drugs that undergo extensive enterohepatic circulation?
Decreases half-life
what drug does grapefruit juice inhibit the metabolism?
cyclosporin
What can selectively induce CYPs in phase I and glucuronic acid and glutathioine in phase II?
chronic exposure to drugs, via increased DNA transcription.
What does ketoconazole inhibit?
terfenadine (seldane): drug-drug inhibition interaction
Which two drugs induce the metabolism of cyclosporin?
Barbituates and St. Johns wort induce the metabolism of cyclosporin
None
What effect do barbequed meat and environmental toxins have on many drugs
induce metabolism
Which CYP does phenobarbital induce?
CYP2B6
Which CYP does ethanol/ isoniazid induce?
CYP2E1
Which CYP do barbituates and glucocorticoids induce?
CYP3A4/5
A) Slow acetylation of Isoniazid is caused by lower levels of which which enzyme? B) What causes this deficient production? C) Which ethnic group has more slow acetylizers, Europeans or Asians? D) Which ethnics group, in general, requires larger doses of isoniazid? E) Which group would be suseptible to toxicity?
A) Slow acetylation of Isoniazid is caused by lower levels of which which enzyme? NAT2 (in liver)

B) What causes this deficient production? single recessive gene

C) Which ethnic group has more slow acetylizers, Europeans or Asians?: EUROPEANS

D) Which ethnics group, in general, requires larger doses of isoniazid? ASIANS

E) Which group would be suseptible to toxicity? EUROPEANS
None
a) 5-10% of caucasian fail to synthesize CYP2D6, which drugs are effected in these individuals? B) What consideration must be taken given this deficit?
a) anitdepressants, antihyperglycemic, and beta blockers…b) give less drug to these patients if the drug is inactivated by cYP2D6 -or- realize that some of these drugs will not work at all in some patients because the the active drug is metabolized (i.e., codeine).
codeine --( ?)--> morphine
CYP2D6
In terms of ethanol metabolism, which ethnic group is deficient in high affinity isozyme and thus exhibit acetaldehyde toxicity (flushing)
Asians
People that are completely deficient for TPMT, which along with xanthine oxidase metabolizes 6-MP to an inactive metabolite are at risk for______.
severe myelosuppression (1 out 300)