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Phamacology > Pharmacokinetics- Metabolism > Flashcards

Pharmacokinetics- Metabolism Flashcards

1
Q

Physiological factors affecting metabolism?

A 
Blood flow
Plasma protein binding
Nutrition
Age
Disease
Sex hormones
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2
Q

What are the organs of metabolism?

A 
Liver
Kidneys
Skin
Plasma
Brain/nervous tissue
Epithelial cells of GIT
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3
Q

What is First pass metabolism?

A

GIT->Drug in->Liver->Drug out-> circulation

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4
Q

What is the extraction equation?

A

E = Cblood in- Cblood out / Cblood in

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5
Q

What drugs go through first pass metabolism?

A 
Aspirin 
Metoprolol
Morphine
Propranolol
Salbutamol 
Verapamil 
Glycerol trinitrate
Isosorbide dinitrate
Levadopa
Lidocaine
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6
Q

What is phase 1 metabolism?

A

Catabolic- products are more chemically reactive

Oxidation- demethylation, reduction, hydrolysis

Liver microsomes- Cytochrome P450

Specific enzymes- Pseudocholinesterase, alcohol dehydrogenase

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7
Q

What is phase 2 metabolism?

A

Synthetic- normally inactive

Conjugation- Glucoronidation, acetylation, sulfation, methylation

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8
Q

What are Cytochrome P450 enzymes?

A 
Haem proteins
Large family
Differ in amino acid sequence
Differ in sensitivity to inhibition and induction 
Overlapping substrate specificities
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9
Q

What is the CYP 450 system?

A

Families 1-3 - catalyse xenobiotic compounds

Families >4 - Biosynthesis and degradation of hormones, signalling molecules and retinoids acid derivatives

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10
Q

P450 enzyme drug substrates?

CYP1A2
CYP2B6
CYP2C8
CYP2C9 
CYP2C19
CYP2D6
CYP2E1
CYP3A4
A 
Caffeine
Methadrone
Repaglinide 
Ibuprofen 
Phenytoin
Codeine
Paracetamol 
Warfarin
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11
Q

3A4 Isoenzymes induction and substrates

A 
Induction:  
Steroids
Herbals
Phenobarb 
Rifamycins
Phenytoin 
Substrates:
Statins
Oral contraceptives 
Macrolides
HIV protease
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12
Q

CYP isoenzyme systems?

A 
Macrolides
Azoles 
Ca+ blockers
Ritonavir
Cyclosporin
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13
Q

Herbal and nutraceutical impacts on metabolism?

A 
Chamomile 
Garlic
Grapefruit juice
Seville orange juice 
Milk thistle
St Johns wart

Will alter the metabolism of the substrates of 3A4 system

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14
Q

What is enzyme induction in metabolism?

A

Can cause drug interactions
Not immediate
Can be clinically significant
Drugs with narrow therapeutic range

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15
Q

Enzyme in inhibition in metabolism?

A 
Cause drug interactions 
Immediate
Can be clinically significant 
Drugs with narrow therapeutic range
Can be stereoselective
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16
Q

What are the deficiency of 2C9?

A
  • 2C9 deficiency (chromosome 10)

- 1-3% Caucasian

17
Q

What causes a 2C19 deficiency?

A

Chromosome 10
2-4% Caucasian
10-18% Afro-Caribbean
10-25% Asia

18
Q

What causes a 2D6 deficiency?

A

Chromosome 22
5-10% Caucasian
>53 alleles of the gene identified

19
Q

Warfarin toxicity and CYP2C9

A 
S-Warafin metabolised by 2C9
Wild type 2C9*1*1 present in 68% of population 
Variety *1*2 and *1*3 present in 32%
*1*2 reduces enzyme activity- 30%
*1*3 reduces enzyme activity-80%

Phamacology (6 decks)

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