Chapter 4 - Properties of Drugs Flashcards

1
Q

What is pharmacokinetics?

A

study of how drugs pass through the body (absorption in blood stream to elimination)
steps: absorption, distribution, metabolism, elimination

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2
Q

Absorption stage

A

refers to passage of a drug into the bloodstream; in most cases drug must pass through cell membrane(s); depends of route of administration
ex. intravenous goes to blood directly, orally must pass through mucous membranes in mouth or wall of intestine

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3
Q

Route of administration

A

affects how much drug reaches blood stream and the speed of absorption (may contribute to abuse)
common routes: inhalation, intramuscular, intravenous, oral

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4
Q

Absorption into body depends on

A

how well pH of an environment matches the drug’s pKa (acidity of drug)

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5
Q

Henderson-Hasselbalch equation

A

the closer the pKa and pH, the more non-ionized particles (better diffusion into blood stream)
ex. pKa=3 better absorbed in the stomach (pH=1) than intestine (pH=7)

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6
Q

Liberation (process during absorption)

A

the process of drug molecules separating form the pill or solution it was dissolved in; many oral drugs are meant to be liberated in small intestines

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7
Q

Distribution stage

A

after absorption into blood stream, passage of drug from bloodstream into intended body sites

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8
Q

Bioavailability

A

ability of a drug to reach its intended target

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9
Q

blood-brain barrier

A

protective layer of cells surrounding blood capillaries in brain that prevent many substances in blood from entering brain; nutrients and some molecules can penetrate it through passive diffusion or active transport

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10
Q

Passive diffusion

A

fat soluble, neutrally charged, and small in size chemicals can diffuse across the blood brain barrier

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11
Q

Active Transport

A

consists of membrane channels or transporters that facilitate passage of chemicals through cell membranes
ex. glucose transporter, large amino-acid transporter

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12
Q

Non-specific binding

A

drugs can sometimes bind to other unintended targets which reduces amount delivered to intended targets

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13
Q

Protein binding

A

drug may bind to proteins in blood stream (not free to cross blood-brain barrier)

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14
Q

Depot binding

A

drug may bind to other tissues which reduces amount in blood available to intended target (ex. TCH in fatty tissues)

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15
Q

Metabolizing stage (biotransformation)

A

process of converting a drug into one or more metabolites

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16
Q

metabolites

A

products resulting from transformation of a drug via enzymes
mostly smaller molecules; water soluble; may be active or inactive

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17
Q

Individual differences

A

rapid metabolizers: more metabolic enzymes; decreased amount of drug (have to use high dose or use different class of drugs)
poor metabolizers: fewer metabolic enzymes; prolongs drug life-span

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18
Q

Personalized medicine

A

prescribe treatments based on patient’s unique biological make up

19
Q

Elimination stage

A

process by which drug leaves the body; final stage of pharmacokinetics; several channels, depends on drug (urine/sweat/breath/feces)

20
Q

Elimination rate

A

amount of drug eliminated from the body over time

21
Q

Half life

A

amount of time required to eliminate half the amount of drug; amount eliminated per unit of time varies; can vary considerably; determines dosing frequency; used if drugs follow first-order kinetics

22
Q

Zero-order kinetics

A

drug is eliminated at a fixed amount per unit time (ex. alcohol is eliminated at about 10-14mg per hour)

23
Q

Pharmacodynamics

A

mechanisms of action for drug which accounts for its (psychological) effects; some alter neurotransmission directly; some may interfere with neurotransmitter storage/reuptake mechanisms/metabolic enzymes

24
Q

Binding affinity

A

The drug’s strength of binding to a receptor; some drugs have a stronger binding to a receptor than a neurotransmitter

25
Q

Receptor efficacy

A

The drugs ability to activate a receptor; some drugs exert weak effects, others exert strong effects

26
Q

Agonist

A

Binds to a receptor and exerts actions similar to the neurotransmitter

27
Q

Partial agonist

A

Binds to the same receptor that the neurotransmitter binds to but has a weaker effect than the NT; functionally reduces the action of the NT

28
Q

Antagonist

A

Binds to a receptor and blocks the action of a NT

29
Q

Competitive antagonist

A

Binds to the same receptor that the neurotransmitter binds to and blocks the action of the NT; direct competition for receptor

30
Q

Non-competitive antagonist

A

Binds to a different receptor than the NT (usually on a complex) and blocks action of NT

31
Q

Allosteric regulators

A

Bind to a receptor other than a NT and affects action of NT; usually receptor for drug is part of a larger receptor complex

32
Q

Positive modulator

A

Drug enhances the action of the NT

33
Q

Negative modulator

A

Drug decreases the action of the NT

34
Q

A good example of allosteric regulation is ____ because ____

A

GABAA receptors; several drugs increase GABA binding to GABAA receptors which enhances action of GABA (benzodiazepines, barbiturates, alcohol)

35
Q

Sensitization (chronic drug use)

A

Increased effects of drugs; lower dose necessary for a given level of effect; dose-response curve shifted left

36
Q

Tolerance (chronic drug use)

A

Decreased effect of a drug; larger dose necessary for a given level of effect; dose-response curve shifted right

37
Q

Pharmacokinetic tolerance (types of tolerance)

A

Reduction in the amount of drug reaching target
Ex. Increased production of metabolic enzymes

38
Q

Pharmacodynamic tolerance

A

Changes in the number of neurotransmitter receptors

39
Q

Down-regulation

A

Decreased number of receptors

40
Q

Behavioural tolerance (types of tolerance)

A

Decreased behavioural response (learn to perform tasks better under effects of drug)

41
Q

Conditioned/contingent tolerance (types of tolerance)

A

Tolerance due to conditioned physiological responses that counteract the drug effects; stimuli associated with drug use may activate a pharmacokinetic response that reduces drug’s effect; in presence of conditioned stimulus, drug effect decreases; in absence of CS, drug affect is much stronger

42
Q

Cross tolerance (types of tolerance)

A

Tolerance to one drug may result in tolerance to another drug
Ex. Someone with high tolerance to heroin may be tolerant to methadone

43
Q

Withdrawal syndrome

A

Collection of responses that occur when a drug is no longer administered; severity of physical effects depends on length/amount of use; psychological effects commonly include drug cravings or mood changes
Ex. Alcohol withdrawal can lead to seizures; heroin withdrawal can lead to increased pain sensitivity