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PDA 2 > 2.6 > Flashcards

2.6 Flashcards

1
Q

Reactions that increase polarity?

A

Phase 1

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2
Q

What type of functional groups do Phase 1 add?

A

Polar

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3
Q

Which phase generally terminates biological activity?

A

Phase 1

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4
Q

Oxidation, Reduction, Hydrolysis

A

Phase 1 reactions

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5
Q

Most frequently occuring type of Phase 1 reaction?

A

Oxidation

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6
Q

A subcellular fraction

A

Microsomes

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7
Q

Microsomes contain?

A

fragments of the endoplasmic reticulum

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8
Q

A multicomponent electron transport system?

A

Cytochorome P450

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9
Q

Cyt 450

A

Serves as substrate binding site and Oxygen binding site

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10
Q

NADPH Cytochrome P 450 Reductase

A

Contains FAD and FMN. Shuttles electrons from NADPH to P450

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11
Q

Where do different isoforms of Cyt P450 exist?

A

liver

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12
Q

Each Cyt P450 has a different?

A

substrate selectivity

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13
Q

What are MFO’s made up of?

A

A family of heme proteins known as Cytochromes P450

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14
Q

Hydroxylation

A

Microsomes

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15
Q

Dealkylation

A

Microsomes

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16
Q

Oxide formation

A

Microsomes

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17
Q

Desulfurization

A

Microsomes

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18
Q

Dehalogenation

A

Microsomes

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19
Q

Alcohol oxidation

A

Soluble and Microsomes

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20
Q

Aldehyde oxidation

A

soluble

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21
Q

Deamination

A

Microsomes and Mitochondria

22
Q

Reductive Reactions

A
  1. May be reversible when coupled with oxidative reactions
  2. Usually occur at groups with multiple bonds
  3. Usually seen when one or both atoms are heteroatoms
23
Q

Aldehyde reduction

A

soluble

24
Q

Azoreduction

A

Microsomes

25
Q

Nitroreduction

A

microsomes, soluble

26
Q

What do phase II reactions do?

A

increase solubility, by bringing things together

27
Q

What type of groups does a Phase II attach?

A

small, polar, ionizable endogenous compounds such as glucuronic acid, glycine, and sulfate

28
Q

Where does Phase II reactions attach the conjugating groups?

A

To polar functional group generated in Phase I

29
Q

What type of reaction is Glutathione (GSH)

A

Phase II

30
Q

What does a Glutathione conjugation do?

A

protects the body from toxic, electrophilic compounds and metabolic activation products.

31
Q

Type of molecule is GSH?

A

nucleophilie

32
Q

What phase increases the H2O solubility more?

A

Phase II

33
Q

What 2 reactions decrease the H2O solubility?

A

Methylation and acetylation

34
Q

What is the most important organ in drug metabolism?

A

The liver

35
Q

Drugs taken orally travel to the liver via the?

A

Portal vein system after absorption

36
Q

First past effect.

A

Following absorption from the gi tract drugs travel directly to the liver, where some are extensively metabolized before reaching the systemic circulation.

37
Q

Which drug is not an effective on oral administration because of the first pass effect?

A

Lidocaine

38
Q

Extrahepatic metabolism

A

Anywhere besides the liver

39
Q

What is in the intestinal wall that hydroyzes glucuronide conjugates found in the bile and release free drug?

A

Beta-glucuronidases

40
Q

Enterohepatic recirculation

A

reabsorption of free drug back across the gut wall into the systemic circulation

41
Q

What enzymes are contained in the lumen?

A

Azoreductases
Nitroreductases
Sulfatases

42
Q

Mammal that doesnt acetylate?

A

Dogs

43
Q

Mammal that makes sulfates, but not glucuronides?

A

Cats

44
Q

Mammal that makes glucuronides, but not sulfates?

A

Pig

45
Q

Mammal that acetylates, makes glucuronidate and sulfate?

A

Humans

46
Q

What ethnic groups are rapid acetylators of isoniazid?

A

Eskimos and Asians

47
Q

5 factors influencing metabolism

A
  1. Genetic Factors
  2. Sex
  3. Physiological Differences
  4. Pharmacodynamic factors
  5. Environmental factors
48
Q

Example of pharmacodynamic factors?

A

Dose of drug. The concentration could saturate all the enzymes.

49
Q

Enzyme Inhibitors

A

Poisoning of enzymes by toxic chemicals such as carbon monoxide, or pesticides may alter metabolism

50
Q

Enzyme Inducers

A

Prolonged treatment with phenobarbital or phenytoin will increase the concentration of microsomal enzymes and thus, decrease the half-life of many drugs.

51
Q

Examples of enzyme inducers

A

Phenobarbital
Benzopyrene
3-methylcholanthrine

52
Q

Largest CYP 450 Isoform

A

2A4/5

PDA 2 (6 decks)

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