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Pharmacology - kinetics, dynamics, ADRs > Pharmacokinetics > Flashcards

Pharmacokinetics Flashcards

1
Q

What is Pharmacokinetics

A

How the drug is handled within the body

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2
Q

What is permeation

A

How the drug enters systemic circulation and barriers it goes through

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3
Q

What is facilitated diffusion

A

passive movement
molecules move across the cell membrane via the aid of a membrane protein.
It is utilised by molecules that are unable to freely cross the phospholipid bilayer (e.g. large, polar molecules and ions)

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4
Q

What is Pinocytosis

A

Cellular drinking
Big molecules - hormones and proteins

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5
Q

What are the main components of pharmacokinetics

A

Absorption
Distribution
Metabolism
Excretion

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6
Q

What is absorption

A

Drugs into systemic circulation

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7
Q

What’s effects absorption

A

PH
Food
Blood flow to the GI tract
Gastric emptying
Permeation

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8
Q

What is first pass effect

A

first pass effect occurs when a drug is metabolized at a specific spot in the body, resulting in a lower concentration of the active substance when it reaches its site of action or the systemic circulation.

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9
Q

What is Bioavailability

A

Proportion of drug available to the body

Drugs given orally under the curve

I’ve route 100% bioavailability

Is not a measurement of effectiveness

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10
Q

What is Bioequivalance

A

Therapeutic equivalence between two drugs - same clinical response - the same drug

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11
Q

What is Bioinequivalance

A

2 main brands - not swappable

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12
Q

What is drug half life

A

Drug concentration in plasma falls 50%

Metabolism and excretion determines half life

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13
Q

What is Steady State

A

Drug input is equal to drug elimination

5 half life’s = Steady State

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14
Q

What is flicks first law

A

Rate of permeation depends on surface area and concentration gradient

Small molecules
Small area
Gas exchange takes longer if fluid present in the lung, prolonging diffusion

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15
Q

What is distribution

A

Drug > plasma protein > good blood flow > lipid soluble > PH > degree of ionisation

If albumin low takes longer to distribute

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16
Q

What is Volume distribution

A

How far the drugs distribute
High volume - gets everywhere

Small VD (0.1-1l/kg) - does not go far
Large VD (1-10l/kg) reach wide and far

17
Q

Exam:
What are the summary factors influencing drug distribution

A

Drugs need to cross cell membrane
1, low degree of ionisation
2, low molecular weight
3, high lipid solubility
4, high concentration gradient

18
Q

What is Metabolism

A

Metabolism occurs in the liver
Lipophilic drugs

Gi tract > skin > lungs > kidneys

Metabolism may produce toxic metabolites

19
Q

What is metabolism 2

A

Influence drug metabolism
Cytochrome p450 enzyme
Young and old age
Liver size and function
Circadian rhythm
Body temp
Smokers metabolise quicker

20
Q

The role of the liver

Slide 44

A

Phase 1 - CP450 - Superfamily of enzymes
Phase 2 - reactions by enzymes
Phase 3 - active drug transport across cel membranes

21
Q

What are the 2 phases of metabolism

A

Phase 1 - produces toxic metabolites

Phase 2 - turns toxic into soluble metabolites for excretion

22
Q

What are the inhibitors and inducers of microsomal enzymes

A

Inhibitors- grapefruit, cimetidine, prolongs or stops

Inducers - barbiturates, carbamazepine
Speeds up drugs shortens therapy

23
Q

What is renal excretion

A

Water soluble
Eliminated in urine
Small enough to fit through kidney glomerlus
Not rapidly diffused in lipid membranes

24
Q

What is biliary secretion

A

Water soluble
Too large to fit through glomerular
Lipophilic
Can be excreted in bile

25
Q

What is clearance

A

Clearance is the amount of drug given at any given time

26
Q

Exam:

What is Zero order

A

The rate of excretion of a drug is independent of its concentration

5% - cannot be altered

27
Q

Exam:

What is first order

A

The rate of excretion is directly proportional to its concentration

Most drugs - first order can be altered

95% of drugs at therapeutic level

Pharmacology - kinetics, dynamics, ADRs (9 decks)

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