Pharmacokinetics Flashcards

1
Q

Absorption

A

Process by which drug enters a system in circulation followed by illustration of mouth inhalation, through skin or injection

Passage of drug from site of administration into plasma

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2
Q

What are the 4 main mechanisms for movement of small molecules?

A

Passive diffusion through lipid- conc gradient, best small and hydrophobic
Facilitated passive diffusion- molecules more polar, charged, carried molecule, with conc gradient
Active transport
Pinocytosis

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3
Q

Acidic drug best absorbed at which levels?

A

Acidic environments

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4
Q

What is sublingual administration?

A

Placing drug under tongue, to dissolve, absorb into blood stream through tissue there

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5
Q

What is transdermal administation?

A

Through skin to bloodstream

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6
Q

What are the factors affecting absorption from GI tract?

A

Particle size and formulation- liquid dissolve more quickly
Physiochemical factors- molecular sizing
Gut content- faster absorption on empty
GI motility- gastric emptying determines how quickly drug delivered to small intestine
Splanchnic blood flow- reduced in heart failure, give reduced absorption

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7
Q

What is IV administration?

A

Direct administration into plasma

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8
Q

Bioavailability

A

The fraction of the administered dose that reached the systemic circulation as the parent drug

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9
Q

Reason for incomplete bioavailability for oral admin

A

Incomplete absorption and loss in faeces

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10
Q

How does bioavailability of a drug affect the dose

A

Poor bioavailability will need a higher dose

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11
Q

Distribution

A

Process by which drug is transferred reversibly between the plasma and the tissues

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12
Q

Distribution is dependent on which 2 factors

A

Blood flow

Lipid solubility - lipid soluble more likely to cross blood brain barrier causing less side effects

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13
Q

Why are lipid soluble drugs more likely to be more slowly released from body

A

Tissue store of lipid soluble drug will be higheer resulting in slower elimination

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14
Q

Oral distribution of drug

A

Gradual increase in blood

Even filling of all compartments

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15
Q

IV distribution of drug

A

Rapid rise of drug in blood
Rapid rise in vessel rich
Slow rise in intermediate and poor vessel
Drug redistributed from vessel rich so become equal

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16
Q

Volume of distribution

A

Theoretical volume necessary to contain total amount of an administered drug at same conc that is observed in blood plasma

17
Q

Volume of distribution equation

A

total amount of drug in body/ plasma conc

18
Q

Low volume distribution drugs

A

Large, water soluble

Stay within plasma

19
Q

High volume distribution drugs

A

Small lipid soluble

Distribute into all compartments

20
Q

What is principle site of drug metabolism?

A

Liver

21
Q

What does liver do?

A

Aim to make drug more soluble for elimination via kidneys

22
Q

Metabolism of drug affected by 3 factors

A

Enzyme induction or inhibition
Blood flow to liver
Genetic variation in enzymes

23
Q

How do enzyme inhibitors affect activity of drug?

A

Increase activity

24
Q

How do enzyme inducers affect activity of drug?

A

Reduce activity

25
Q

Pro-drug

A

Drug that is metabolised after administration to a pharmacologically active metabolite
adminstered inactive form, reduces undersirable effects

26
Q

Larger molecules are excreted how?

A

By bile (removed in faeces)

27
Q

Smaller moelcules are excreted how?

A

Renally (urine)

28
Q

What is first order drug elimination

A

Metabolism rate is proportional to drug plasma conc

Drug conc drops by fixed percentage in given time

29
Q

What is zero order drug elimination?

A

Metabolism removes fixed amount of drug in given period

30
Q

Half life of drug

A

Time it takes for plasma conc or amount of drug in body to be reduced by 50%

31
Q

Clearance equation

A

Rate of elimination from body/ drug conc in plasma

32
Q

Cl total equation

A

Cl renal + clearance non renal

33
Q

Repeated administration

A

Drug administration of fixed dose at regular time interval through given route

34
Q

Drug drug interactions

A

When one drug affects the activity of another when 2 are given in combination

35
Q

Therapeutic index equation

A

Dose resulting in toxicity/ dose giving therapeutic response

36
Q

High TI indicates what toxicity

A

Low risk of toxicity

37
Q

Low TI or narrow indicated what

A

High risk of toxicity