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ELM2 - clinical pharmacology > lecture 1 - intro to pharmacokinetics > Flashcards

lecture 1 - intro to pharmacokinetics Flashcards

1
Q

What are the 4 stages of pharmacokinetics when a drug enters the body?

A

ADME - absorption, distribution, metabolism, excretion

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2
Q

What is the aim of drug dosing?

A

To ensure the drug plasma concentration is within the optimal therapeutic range for a sufficient duration.

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3
Q

What is the symbol for Drug plasma concentration?

A

Cₚ

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4
Q

What is the ‘AUC’ in drug dosing?

A

Area Under the Curve

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5
Q

What does the AUC in a drug dosing curve correspond to?

A

The fraction of the dose administered that reaches the systemic circulation, i.e. body exposure

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6
Q

What is the Cₚ AUC dependent on?

A

The dose administered, and the rate of drug elimination

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7
Q

What is the unit of AUC?

A

Conc. (mg) * hours / volume (L)

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8
Q

What are the 2 overall routes of drug administration?

A

Enteral, parenteral

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9
Q

What is enteral drug administration?

A

Absorption via any part of the enteric system/GI tract

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10
Q

What are the 3 routes of enteral drug administration?

A

oral, sublingual, rectal

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11
Q

What is parental drug administration?

A

non-enteral, systemic delivery

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12
Q

What are the methods of parenteral drug administration?

A

IV bolus/infusion, Injections (Intraarterial, intramuscular, subcutaneous), topical, inhalation

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13
Q

What is the metabolic disadvantage of oral enteral delivery?

A

Drug is subject to 1st pass metabolism - by the liver.

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14
Q

What measure is used to measure the amount of a drug that reaches the systemic circulation in its active form?

A

Fraction of dose (F)

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15
Q

What does Fraction of dose (F) measure?

A

Oral availability - the proportion of a dose that reaches the systemic circulation in its active form

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16
Q

What is the Fraction of dose (F) for an intravenously administered drug?

A

1 - all of the drug enters the circulation directly

17
Q

What is the equation for Fraction of dose (F)?

A

F% = AUC(oral)/AUC(IV) *100

18
Q

What is the oral availability of a drug dependent on?

A

drug absorption, first pass metabolism

19
Q

What is drug absorption?

A

transport of the drug from site of absorption into the systemic circulation

20
Q

What is the rate of drug absorption dependent on?

A

drug lipid solubility, gastric pH, pKa, surface area, blood flow, GIT transit time, presence of other drugs

21
Q

What is the rate of the first pass metabolism of drugs dependent on?

A

gastric pH, GIT motility, metabolic enzymes in gut and liver, drug breakdown, hepatic mass & perfusion

22
Q

What type of lipid membrane transport do most drugs use?

A

passive transport (non-energetic)

23
Q

What metabolic enzyme systems are involved in the first pass metabolism of drugs?

A

GI lumenal enzymes, gut wall enzymes, bacterial enzymes, hepatic enzymes

24
Q

What physico-chemical properties of drugs affect their absorption?

A

molecular weight, hydrophilicity/lypophilicity, ionisation status

25
Q

What is the unit for drug clearance?

A

vol of plasma cleared/unit time

26
Q

What are the 2 key types of drug clearance?

A

metabolic, renal

27
Q

Where does metabolic drug clearance predominantly occur?

A

The liver

28
Q

What is the relationship between AUC and drug clearance?

A

Inversely proportional - increasing clearance decreases AUC

29
Q

What is the rate of drug distribution dependent on?

A

membrane permeability, organ perfusion

30
Q

What measure is used to quantify how well a drug is distributed throughout the body?

A

Volume of distribution (Vd)

31
Q

How is volume of distribution of a drug calculated?

A

amount administered/concentration in plasma

32
Q

What is the purpose of calculating loading dose?

A

Allows a steady plasma concentration to be achieved quickly

33
Q

What is the equation for calculating loading dose?

A

LD = volume of distribution * target plasma conc.

34
Q

What is the reciprocal of pharmacokinetic half life?

A

The drug elimination rate constant

35
Q

How is the drug elimination rate constant calculated?

A

k = 0.693/t1/2

36
Q

How is half life calculated from volume of distribution & drug clearance?

A

t1/2 = (0.693 * Vd)/Cl

ELM2 - clinical pharmacology (20 decks)

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