(3) Kinetics SLO Flashcards
Acetylation is a type of Phase II conjugation reaction. There are people who genetically, are fast acetylators and others whose enzymes work slowly. In a fast acetylator, given a normal amount of a drug metabolized by this route, you would expect (assumes drug is NOT a prodrug):
A. Not enough information to answer
B. The drug will be metabolized slower than normal
C. Treatment failure
D. Toxicity or “over dose”
E. No effect
Treatment failure
Albumin is important for: A. Plasma protein binding B. Excretion of drugs C. Metabolism of drugs D. Absorption of drugs E. None of the listed answers is correct
Plasma protein binding
Barbiturates, including Phenobarbital, an antiepileptic drug (AED), are potent inducers of P450 enzymes (especially CYP3A and CYP2B isozymes). Atorvastatin (Lipitor, a statin drug used to reduce cholesterol) is metabolized by CYP3A4. What do you expect to occur in a person using Phenobarbital to control seizures who is prescribed atorvastatin?
A. Toxicity or “over dose”
B. No effect
C. The drug will be metabolized slower than normal
D. Not enough information to answer
E. Treatment failure
Treatment failure
Chloramphenicol, an antibiotic, is known to cause “Grey” baby syndrome in neonates. This is because young babies are/have:
A. On at least 10 different medications on average
B. All of the answers listed are correct
C. Metabolically underdeveloped and lacking virtually all Phase 2 metabolism
D. A strongly induced set of metabolic enzymes from mom
E. Non-functional kidneys and can’t excrete drugs
Metabolically underdeveloped and lacking virtually all Phase 2 metabolism
CYP3A4 in the gut is inhibited by grapefruit juice. Atorvastatin (Lipitor, a statin drug used to reduce cholesterol in the body) is primarily metabolized by CYP3A4. What would you expect to occur in a person consuming grapefruit juice who is prescribed atorvastatin?
A. No effect
B. Not enough information to answer
C. Treatment failure
D. The drug will be metabolized slower than normal
E. Toxicity or “over dose”
Toxicity or “over dose”
CYP3A4 inducers tend to cause \_\_?\_\_ in drugs that are CYP3A4 substrates. A. No effect B. More beneficial effects C. Synergistic effects D. Treatment failure E. Toxicity
Treatment failure
Ion trapping of weakly basic drugs may occur: A. Only in the stomach B. Only in the intestines C. In the stomach and fetus D. In the stomach and intestines E. Only in the fetus
In the stomach and fetus
Metabolism may produce metabolites (daughters) that (are): A. Only in the stomach B. Only in the intestines C. In the stomach and fetus D. In the stomach and intestines E. Only in the fetus
More, or less, active than the parent More, or less, toxic than the parent Have a new action or effect Similar to the parent ***ALL***
Morphine is an opioid analgesic that has significant 1st pass losses. This can be avoided by giving the drug: A. Orally B. Enterally C. Parenterally D. 2 Hours after eating E. With Meals
Parenterally
Most penicillins have very high extraction ratios in the kidneys. This means most penicillins have (are): A. No effect on the kidneys B. A short half-life C. Not excreted into urine D. An unpredictable half-life E. A long half-life
A short half-life
Phase 1 reactions are: A. P450 mediated B. Mediated by membrane-bound enzymes C. REDOX reactions D. Often "activation" reactions for Phase 2 metabolism, creating sites for conjugation to occur E. All the above
P450 mediated REDOX reactions Mediated by membrane-bound enzymes Often "activation" reactions for Phase 2 metabolism, creating sites for conjugation to occur ***ALL***
Phase 2 reactions are:
A. Conjugation reactions
B. Mediated by cytosolic and membrane-bound enzymes
C. Reactions used by the body to improve the excretion of wastes
D. Mediated by enzymes that, like the P450s, can be induced or inhibited by drugs and are subject to individual genetic differences in expression
E. All the above
Conjugation reactions
Mediated by cytosolic and membrane-bound enzyme
Reactions used by the body to improve the excretion of wastes
Mediated by enzymes that, like the P450s, can be induced or inhibited by drugs and are subject to individual genetic differences in expression
ALL
Probenecid (Benuryl) is important because it:
A. Inhibits absorbtion of drugs in the GIT
B. Reduces renal tubular secretion of certain drugs
C. Induces P450 enzymes
D. Inhibits P450 enzymes
E. Stimulates urinary excretion of drugs
Reduces renal tubular secretion of certain drugs
The elderly generally require lower doses or more careful monitoring because:
A. They have experienced age-related alterations n body water and lean body mass
B. Their cardiac function is often reduced leading to poor perfusion of tissues
C. Their kidney function is significantly reduced due to age
D. All of the listed answers are correct
E. Their livers are no longer synthesizing normal amounts of proteins including plasma proteins and metabolic enzymes
Their cardiac function is often reduced leading to poor perfusion of tissues, They have experienced age-related alterations n body water and lean body mass, Their kidney function is significantly reduced due to age, Their livers are no longer synthesizing normal amounts of proteins including plasma proteins and metabolic enzymes
ALL
Which of these is an insignificant route of excretion, for the most part? A. Liver (feces) B. Skin (Sweat) C. Liver (bile) D. Kidneys (urine) E. Lungs (exhaled air)
Skin (Sweat)
