ADME Flashcards

1
Q

Drugs must be dissolved before being absorbed T/F

A

True

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2
Q

The proteins found in the plasma lipid membrane are

A

Integral protein
Lipid anchored protein
Peripheral protein
Transmembrane protein

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3
Q

90% of drugs in clinical practice uses what mechanisms of drug transport

A

Passive diffusion
Facilitated diffusion

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4
Q

Facilitated diffusion is faster than passive diffusion T/F

A

True

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5
Q

The membrane physiology that affects drug absorption include

A

Thickness of the membrane
Surface area of the membrane
Transport mechanism in the membrane

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6
Q

What is gastric emptying

A

This is the process by which the content of the stomach is emptied into the small intestine particularly the duodenum

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7
Q

The principal site of absorption of most orally ingested drugs is …………..

A

Duodenum

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8
Q

A rapid gastric emptying favours drugs absorbed in ……..

A

Small intestine

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9
Q

Metoclopramide and domperidone are ………

A

Dopaminergic antagonist used to emesis and it increases peristaltic movement thus gastric emptying

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10
Q

Factors that decrease gastric emptying include

A

Drugs
Anticholinergic( atropine)
Analgesics(Aspirin)
Narcotics( morphine)
High calorie foods and fatty foods like carbohydrate

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11
Q

Proteins increases gastric pH T/F

A

True

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12
Q

Lipid food increases the solubility of lipid soluble drugs like ………

A

Griseofulvin
Arthemeter

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13
Q

Drugs like tetracycline are chelated by ……..

A

Milk
Calcium-rich foods

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14
Q

A commonly known CYP450 inhibition and drug efflux transporter inhibitor is ……..

A

Grape fruit

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15
Q

Ways in which food can affect the absorption of a drug are

A

Through gastric emptying
pH of the stomach
Solubility of the drug
Chelation of the drug
Metabolism/first pass effect on the drug

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16
Q

What is GI motility

A

The overall speed with which food moves along the alimentary canal

17
Q

Laxatives Cathartics that increases GI motility reduces the overall absorption of …… when co administered

A

Drugs

18
Q

How does GI blood flow affect drug absorption

A

Directly proportional I.e the more the GI flow the greater the absorption of drug

19
Q

Mechanism of pre systemic metabolism include

A

Intestinal bacteria
Enzymes in alimentary canal
Hepatic enzyme

20
Q

Pathologic conditions that affect drug absorption include

A

Diseases
Surgery
Inflammation
Drug interaction

21
Q

List the diseases of the GI and how they affect absorption of drug

A

Achlohydra - diseases that leads to reduction in secretion of hydrochloric acid hence Decreased absorption of weakly acidic drugs e.g aspirin

Celiac or crohn’s causes malabsorption hence general defects in absorption

Congestive heart disease - edema of the intestine, Decreased blood flow which leads to decreased absorption

Hepatic disease and liver cirrhosis which increases the availability of drugs that should undergo first pass effect

22
Q

What is the effect of Gastrectomy and intestinal resection on drug absorption

A

Gastrectomy and intestinal resection increases gastric emptying and gastric motility

23
Q

What is the effectbof inflammation on drug absorption

A

It decrease GI transit time hence decreases absorption

24
Q

Drug -drug interaction that affects absorption is similar to the effect f food on drug absorption

A
25
Q

Order of absorption of drugs in terms of physical state is

A

Solid <powder<suspension <syrup

26
Q

The pharmaceutical factors that affects the absorption of drugs include

A

A. Solubility of drug and formulation
B. Permeability and size of drug
C. Dissolution of the drug
D. Drug-drug interaction
E. Degree of ionisation of the drug

27
Q

A drug has to be …….. size in order to cross to the endothelium

A

</=500D

28
Q

A drug has to be ……. . Size to cross into the intracellular compartment

A

</=50

29
Q

What in o/w partition coefficient

A

It is ratio of concentration of a drug in n-octanol to the conc in water

It measures the lipophillicity of a drug

The greater the partition coefficient the more soluble the drug

30
Q

The pKa of strong acids and bases are ………. respectively

A

Low
High

31
Q

The size requirements for drugs to cross the cell membrane barrier is

A

</=50 Da for hydrophilic drugs

</=500 Da lipophyllic drugs by diffusion or Facilitated diffusion

32
Q

Means by which polar substances cross the BBB include

A

Dimethyl sulfoxide DMSO
osmotic disruptors - mannitol, etc
Dihydropyridine redox system