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Neuro-pharmacology > Pharmacology: pharmokinetics > Flashcards

Pharmacology: pharmokinetics Flashcards

1
Q

Neuro-psychopharmacology

A

the study of the actions of drugs on the CNS and their effects on human behavior

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2
Q

Drug actions

A

specific molecular changes resulting from drug binding to the target site receptor

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3
Q

Drug effects

A

widespread alterations in physiology or psychology resulting from drug action

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4
Q

Therapeutic effects

A

drug-target interactions producing the desired physiological or behavioral changes

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5
Q

Side effects

A

any effect that isn’t the therapeutic effect

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6
Q

Adverse effects

A

undesirable or harmful drug effects

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7
Q

Specific effects

A

biochemical interaction between the drug and the receptor

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8
Q

Non-specific effects

A

interactions that go beyond the interaction between the drug and the receptor

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9
Q

Placebo

A

Measurable therapeutic effect of a treatment without specific activity for the receptive condition

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10
Q

Pharmacokinetics

A

factors contributing to bioavailability and efficacy of drugs in the human body. Provides performance guidelines for efficacy, efficiency, and drug use in clinical settings

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11
Q

ADME

A

Absorption, distribution, metabolism, excretion

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12
Q

Absorption

A

movement of the drug from site of administration to the circulatory system

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13
Q

Distribution

A

dispersal of the drug through body fluids to the target tissues of the body

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14
Q

Depot binding

A

when the drug binds to non-target tissues

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15
Q

Metabolism

A

biotransformation or inactivation of drugs in the body into metabolites

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16
Q

Excretion

A

removal of substances or metabolites from the body

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17
Q

First pass effect

A

blood flow from the stomach/intestines goes directly to the liver for detox, drug gets metabolised into a usable form for the body

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18
Q

the more of a drug you take the more

A

adverse the effects become

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19
Q

Nonspecific effects may occur as a result of

A

unique characteristics of the individual or an individuals state

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20
Q

Placebo effect is affected by

A

expectancy and conditioning

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21
Q

Placebo is a

A

confound in neuropsychopharmacology

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22
Q

PO =

A

oral administration

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23
Q

IV =

A

intravenous

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24
Q

IM =

A

intramuscular

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25
Q

Inhalation

A

intake of drugs through the nose

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26
Q

Advantages and disadvantages of oral Administration

A

Advantages: self administered, economical
Disadvantages: slow, variable absorption, subject to first pass metabolism

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27
Q

Advantages and disadvantages of intravenous Administration

A

advantages: Rapid, accurate blood concentration
Disadvantage: overdose danger, cannot be readily reversed, sterility

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28
Q

Advantages and disadvantages of intramuscular Administration

A

Advantages: slow and even absorption
Disadvantages: irritation at injection site, sterility

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29
Q

Advantages and disadvantages of subcutaneous Administration

A

Advantages: slow and prolonged absorption
Disadvantages: variable absorption depending on blood flow

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30
Q

Advantages and disadvantages of inhilation Administration

A

Advantages: most rapid, large absorption surface
Disadvantages: irritation of nasal passages, could damage lungs

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31
Q

Advantages and disadvantages of topical Administration

A

Advantages: localized action and effects, easy to self-administer
Disadvantages: may be absorbed into general circulation

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32
Q

Advantages and disadvantages of transdermal Administration

A

Advantages: controlled and prolonged absorption
Disadvantages: local irritation, useful only for lipid soluble drugs

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33
Q

Advantages and disadvantages of epidural Administration

A

Advantages: bypass blood brain barrier, very rapid effects of the CNS
Disadvantages: not reversible, need a trained anesthesiologist, possible nerve damage

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34
Q

Oral rout has the greatest

A

breakdown of a drug

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35
Q

Absorption is affected by

A

drug concentration, breakdown by metabolic or digestive processes, solubility and ionizing of the drug

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36
Q

Absorption is dependent on

A

passive diffusion

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37
Q

Drug concentration is affected by

A

age, sex, body size, body fat content

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38
Q

Polar molecules

A

Water soluble
Hydrophilic - water loving
Lipophobic - fat hating

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39
Q

Non-polar molecules

A

Lipid-soluble Hydrophobic - fear water
Lipophilic - fat loving

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40
Q

polar molecules are transported through

A

aqueous compartments

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41
Q

Non-polar molecules freely diffuse across

A

semi-permeable membranes

42
Q

aqueous compartments

A

blood, CSF, ECF

43
Q

semi-permeable membranes

A

intestinal wall, BBB, cell membranes

44
Q

Non-polar molecules tend to be

A

less soluble in water

45
Q

Polar or charged (ionized) drugs are prevented from

A

diffusing through membranes

46
Q

Many orally administered drugs are weak acids or bases

A

gaining or losing charges based on the pH of the external environment

47
Q

How aspirin moved through the system

A

stomach - around the same acidity to freely moves across the cell membrane - becomes ionized in the blood and is readily soluble - in the intestines’ it alternates between ionized and non-ionized forms and diffuseness more slowly across the membranes

48
Q

Surface area of body compartments

A

surface area affects drug absorption

49
Q

Stomach has a relatively small surface area

A

slow absorption

50
Q

Intestines have relatively large surface area

A

(fast absorption) and are the site of most (oral) drug absorption

51
Q

Once in the bloodstream drugs circulate to the entire body within

A

minutes

52
Q

Drug concentration is highest in tissues with

A

greatest blood flow

53
Q

Drug concentration is highest in tissues with greatest blood flow

A

Heart, brain, kidneys, liver

54
Q

Peripheral capillaries are highly

A

porous allowing ready distribution of drugs (lipophilic or hydrophilic) into tissues

55
Q

Blood-brain barrier

A

permits passive diffusion of only lipophilic drugs

56
Q

Three main compartments affect drug concentration in the brain

A

Blood plasma, Cerebral spinal fluid, extracellular fluid

57
Q

Blood plasma

A

Permeates entire brain
Carries soluble drugs and nutrients (glucose, oxygen, amino acids)
Removes waste products and gases

58
Q

Cerebral spinal fluid (CSF)

A

Fills subarachnoid space, ventricles, cisternae
Highly regulated concentration of solutes, glucose, very low protein
Isolated from systemic circulation

59
Q

Extracellular fluid (ECF)

A

Interstitial space between cells in the brain
Similar composition to CSF but more varied between brain regions
Isolated from systemic circulation by the blood-brain barrier (BBB)

60
Q

Astrocytes are to blame for

A

hydrophilic substances being unable to pass through the blood brain barrier

61
Q

typical capillary

A

capillaries are porous, allowing hydrophilic drugs to freely enter tissues

62
Q

Brain capillaries are

A

are coupled by tight junctions and lined by astrocyte endfeet creating a highly impermeable barrier

63
Q

The BBB limits access to

A

98% of small molecule pharmaceuticals (and 100% of large molecule pharmaceuticals

64
Q

Passage of solutes through the BBB often occurs at

A

specific transporters (e.g. glucose and amino acid transporters)

65
Q

Some drugs are actively removed from the ECF by

A

efflux transporters (i.e. p-glycoprotein, a.k.a. multidrug resistance protein-1)

66
Q

BBB is not a complete barrier

A

certain sites have direct access to the circulatory system

67
Q

Chemoreceptor trigger zone

A

allows direct detection of toxins in the blood

68
Q

where is the Chemoreceptor trigger zone located

A

the medulla (vomit center)`

69
Q

Hypothalamus

A

allows direct access to capillaries for secretion of neurohormones and hormone-releasing factors

70
Q

some drugs get into the brain Via the

A

passage way the hypothalamus uses

71
Q

Drugs (licit and illicit), alcohol, gaseous anaesthetics, and gases (e.g. carbon monoxide) readily cross the placental barrier and can cause

A

acute toxicity or teratogenic effects to the fetus

72
Q

the placenta is

A

Slightly more permeable than the BBB

73
Q

drug depot sites

A

Adipose tissue (lipid-soluble drugs)
Muscle tissue
Albumin (plasma protein)

74
Q

drug depot sites and circulation

A

Decreases circulating drug concentration

75
Q

drug depot sites and Prolongs drug action

A

Can function as reservoirs for drug release
Protects stored drug from metabolism

76
Q

depot binding and drug efficacy

A

Can explain individual differences in drug efficacy

77
Q

rapid binding to depot before reaching target tissue = what therapeutic effect

A

slower onset and reduced effects

78
Q

individual differences in the amount of binding = what therapeutic effect?

A

less free drug, so some need higher doses, low binding means more free drug so some individuals are more sensitive

79
Q

competition among drugs for depot binding sites = what therapeutic effect

A

higher than expected blood levels of the displaced drug, possibly causing greater side effects even toxicity

80
Q

bound drug is not metabolized = what therapeutic effect?

A

drug remains in the body for prolonged action

81
Q

binding to depots follows the rapid action at targets (redistribution) = what therapeutic effect?

A

rapid termination of drug action

82
Q

Metabolism occurs primarily in the

A

the liver under control of microsomal enzymes

83
Q

cytochrome P450 family (CYP ~ 57 in total)

A

oxidize the majority of psychoactive drugs (incl. opioids, antidepressants, amphetamines, nicotine)

84
Q

CYP1A2

A

metabolizes many antidepressants and antipsychotics – induced by smoking

85
Q

CYP3A4

A

metabolizes many opioids, antidepressants, statins, anxiolytics – inhibited by grapefruit juice

86
Q

Metabolism is a non-specific

A

detoxification process that occurs in two distinct types or phases

87
Q

Metabolism is a non-specific detoxification process that occurs in two distinct types or phases (type 1)

A

non-synthetic modifications, oxidation, reduction, and hydrolysis

88
Q

Metabolism is a non-specific detoxification process that occurs in two distinct types or phases (type 2)

A

synthetic modifications. conjugation with glucuronide, sulfate, or methyl groups

89
Q

Type I metabolism during first pass can produce

A

active metabolites of the pharmaceutical preparation of drugs

90
Q

Metabolic products (active and inactive) are returned to circulation from

A

the liver and can reach target sites of action or sites for excretion (kidneys, biliary, or fecal excretion)

91
Q

4 factors that influence metabolism

A

Enzyme induction
Enzyme inhibition
Drug competition
Individual differences (age, sex, genetics)

92
Q

Enzyme induction

A

repeated use results in increase in liver enzymes (contributes to tolerance and cross tolerance)

93
Q

Enzyme inhibition

A

drugs targeting enzymes (e.g. monoamine oxidase inhibitors - MAOI) decrease their own clearance and other drugs

94
Q

Drug competition

A

competition for enzymes may prevent some drugs being metabolized in a safe fashion

95
Q

Individual differences

A

genetic polymorphisms have been identified in metabolic enzymes
different individuals have different rates of clearance for drugs

96
Q

Routes of excretion include

A

breath, sweat, saliva, feces, breast milk, and urine

97
Q

Primary means of excretion is

A

filtration by kidney and excretion through urine

98
Q

Most drugs are excreted by

A

first-order kinetics

99
Q

Exponential elimination

A

constant fraction removed in a given time

100
Q

Half-life (t½)

A

describes the interval required to eliminate half of the drug from circulation

101
Q

Very few drugs removed by

A

zero-order kinetics (constant rate)
- alcohol is

Neuro-pharmacology (26 decks)

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