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Pharm - 1st Week > 3 Kruse DSA's - 8/3 Kruse > Flashcards

3 Kruse DSA's - 8/3 Kruse Flashcards

1
Q

What is the chemical modification of lipophilic, unionized, or large compounds to terminate their actions and facilitate elimination called?

A

Biotransformation

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2
Q

What is an example of Biotransformation activation?

Active -> active compound?

Inactivation?

A

L-dopa -> dopamine

Diazepam -> oxazepam

Aspirin -> acetic acid + salicylate

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3
Q

Major site of Biotransformation?

Additional sites?

A

Liver

Gi tract, lungs, skin, kidneys

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4
Q

What is described by the process by which oral drugs are absorbed in the small intestine and transported into the liver via the hepatic portal system, undergoing extensive metabolism?

A

1st-pass effect

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5
Q

Phase I reactions include what kinds of reactions?

A

PCONS oxidation
Reduction hydrolysis

Less commonly: hydroxylation, epoxidation, dealkylation, deamination, desulfuration, dechlorination

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6
Q

What carries out Phase 1 reactions?

A

CYP
FMO
mEH, sEH

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7
Q

Where are phase I enzymes located?

Phase 2?

A

Lipophilic ER membranes of liver

Liver

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8
Q

What is the most important CYP subtype?

What do all CYPs contain?

A

CYP3A4

Molecule of heme that is noncovalently bound to the polypeptide chain

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9
Q

What do P450s need to carry out oxidation of substrates?

A

NADPH (O2 and H+)

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10
Q

Name the most common enzyme inducers

A 
Phenytoin 
Ethanol
Benzo[a]pyrene
Rifampin
Phenobarbital
ST John's wort
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11
Q

What effect does grapefruit juice have on drugs taken orally?

A

Irreversibly inhibit intestinal CYP3A4

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12
Q

What effect does allopurinol have on mercaptopurine?

A

Prolongs the action of mercaptopurine and enhances its chemotherapeutic and toxic effects by inhibiting xanthine oxidase

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13
Q

What predisposes neonates to drug toxicity?

A

Poorly developed BB barrier
Weak Biotransforming activity
Immature excretion mechanisms

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14
Q

Toxic doses of acetaminophen can lead to what?

Why?

A

Hepatotoxicity

GSH is depleted to quickly

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15
Q

What are the most common enzyme inhibitors?

A 
Amiodarone
Cimetidine
Grapefruit juice
Azole anti fungal 
Ritonavir (HIV protease inhibitor)
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16
Q

What are the P-GP inhibitors?

A

Verapamil
Mibefradil
Grapefruit juice

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17
Q

What drugs are expelled by P-gp and more toxic when given with a P-gp inhibitor?

A

Digoxin
Cyclosporine
Saquinavir

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18
Q

1st pass metabolism of what is greater in men than women?

A

Ethanol

19
Q

Polymorphisms in what enzyme result in increased toxicity and require reduced dosage which causes diarrhea and neutropenia due to decreased clearance of 5-FU?

A

DPD

20
Q

CYP2C19 polymorphisms can affect what drugs?

A 
Clopidogrel
Propanolol
Omeprazole
Diazepam
Tricyclics
21
Q

Reduced efficacy (LOF) of clopidogrel results in what?

A

INC risk of clotting in Pts with CAD

22
Q

What polymorphism is associated with GOF and increased effect and toxicity of codeine?

A

CYP2D6

23
Q

What is associated with reduced Warfarin clearance?

A

CYP2C9 with reduced function allele of VCORC1

24
Q

Reduced function of OATPs like SLCO1B1 result in what?

A

Increased risk of simvastatin myopathy and increased risk of skeletal muscle myopathy

25
Q

What polymorphism is associated with risk of hemolysis and increased resistance to malaria?

A

G6PD

26
Q

A polymorphism of UGT1A1 results in what?

A

Decreased clearance and increased toxicity of SN-38

27
Q

What is associated with decreased clearance of 6-mercaptopurine and increased toxicity?

A

TPMT*2

28
Q

What can increase the metabolism of codeine?

What is the active metabolite?

Can result in what?

A

CYP2D6

Morphine

Respiratory depression (cyanosis)

29
Q

What kind of design consists of patients receiving each therapy in sequence so that the patients serve as their own controls?

A

Crossover design

30
Q

What characterizes phase 0 testing in humans?

A

Micro dosing

31
Q

What phase drug testing examines absorption, half-life, and metabolism?

A

Phase I

32
Q

How many volunteers is typical of phase I testing?

A

25-50

33
Q

How many volunteers are used in phase II testing?

Primarily looking for what?

A

100-200

Efficacy, dosing requirements, toxicities

34
Q

How large of a group is used in phase III testing?

What techniques are used?

A

300-3000

Crossover, double-blind

35
Q

When does phase IV testing occur?

A

After approval to market

36
Q

What does the dominant lethal test assess?

A

In vivo mutagenicity (loss of embryos or deformed fetus)

37
Q

What test is used for mutagenicity in bacteria?

A

Ames test

38
Q

Give the order in which they occur of the following:

NDA
IND
Clinical trials

A
  1. IND
  2. clinical trial
  3. NDA
39
Q

When are the results of chronic toxicity studies in animals required?

When do they usually begin?

A

NDA

At the time of the IND submission

40
Q

What SNP is associated with codeine?

A

CYP2D6

41
Q

What is associated with CYP2C19?

A

Clopidogrel

42
Q

N-acetyltransferase SNP is associated with what drug?

A

Isoniazid

43
Q

TPMT SNPs are associated with drugs?

A

6-mercaptopurine

44
Q

Butyrylcholinesterase SNPs are associated with drug?

A

Succinylcholine

Pharm - 1st Week (4 decks)

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