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Psychopharmacology > Principles of Pharmacology > Flashcards

Principles of Pharmacology Flashcards

1
Q

Pharmacology

A

The scientific study of the actions of drugs and their effects on a living organism

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2
Q

The WHO estimates that as many as _% of people in developing countries are entirely dependent on herbs or plant-derived medicinals

A

80%

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3
Q

What is the focus of neuropharmacology

A

Drug-induced changes in the functioning of cells in the nervous system

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4
Q

What is the focus of psychopharmacology?

A

Drug-induced changes in mood, thinking, and behaviour

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5
Q

What is the focus of neuropsychopharmacology?

A

Identifying chemical substances that act on the nervous system to alter behaviour that is disturbed because of injury, disease, or environmental factors

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6
Q

Drug action

A

The specific molecular changes produced by a drug when it binds to a particular target site or receptor

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7
Q

Drug effects

A

The more widespread changes in physiological or psychological function as a result of drug action

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8
Q

Therapeutic effects

A

The drug-receptor interaction produces the desired effect

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9
Q

Side effects

A

All non-therapeutic effects

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10
Q

Specific drug effects

A

Those effects based the physical and biochemical interactions a drug with a target site in living tissue

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11
Q

Nonspecific drug effects

A

Those effects that are based on certain unique characteristics of the individual, rather than the chemical activity of a drug-receptor interaction

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12
Q

What is an example of a nonspecific drug effect?

A

A placebo

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13
Q

Placebo

A

A pharmacologically inert compound

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14
Q

Bioavailability

A

The amount of drug in the blood that is free to bind at specific target sites to elicit drug action

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15
Q

Is bioavailability more important than dosage? Why or why not?

A

Yes, because many different factors are involved

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16
Q

Pharmacokinetic factors

A

Factors that contribute to bioavailability

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17
Q

What are 5 pharmacokinetic components of drug action?

A
  • Routes of administration
  • Absorption and distribution
  • Binding
  • Inactivation
  • Excretion
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18
Q

What is determined by the route of administration?

A

How quickly and how completely the drug is absorbed into the blood

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19
Q

What happens once the drug is in the blood plasma?

A

Some drug molecules move to tissues to bind to active target sites (receptors) or to plasma proteins or may be stored temporarily in bone or fat, where it is inactive

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20
Q

Depot binding

A

Type of drug interaction involving binding to an inactive site

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21
Q

Drug inactivation occurs primarily as a result of what?

A

Metabolic processes in the liver

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22
Q

The amount of drug in the body is dependent on what?

A

The dynamic balance between absorption and inactivation

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23
Q

Inactivation influences what?

A

The intensity and duration of side effects

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24
Q

What are the two major categories of administration methods?

A

Enteral and parenteral

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25
Q

Enteral methods use what route?

A

The gastrointestinal (GI) tract

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26
Q

Agents administered by which method are generally slow in onset and produce highly variable blood levels of drug?

A

Enteral

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27
Q

What is the most common enteral method?

A

Oral

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28
Q

Why is oral administration (PO) the most popular route?

A
  • Safe
  • Self-administered
  • Economical
  • Avoids complications and discomfort of injection methods
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29
Q

In order for orally administered drugs to be effective, what needs to happen?

A
  • Must dissolve in the stomach fluids and pass through the stomach wall to read blood capillaries
  • Must be resistant to destruction by stomach acid and enzymes
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30
Q

What is an example of a drug that cannot be administered orally? Why?

A

Insulin, because it can be destroyed by digestive processes

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31
Q

Absorption

A

Movement of the drug from the site of administration to the blood circulation

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32
Q

Most drugs are not fully absorbed until they reach what part of the GI tract?

A

The small intestine

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33
Q

First-pass metabolism

A

Phenomenon in which the liver metabolizes some of a drug before it can circulate through the body

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34
Q

What must be done for drugs that show extensive first-pass effects?

A

Must be administered at higher doses or in an alternative method

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35
Q

Why is the first-pass metabolism beneficial?

A

Potentially harmful chemicals/toxins can be chemically altered before passing to the heart for circulation throughout the body

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36
Q

Rectal administration

A

The placement of a drug-filled suppository in the rectum, where it melts or dissolves, releasing the drug to be absorbed into the blood

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37
Q

Why is bioavailability of drugs administered rectally hard to predict?

A

Depending on the placement of the suppository, the drug may avoid some first-pass metabolism

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38
Q

What happens with drugs absorbed from the lower rectum into the hemorrhoidal vein?

A

They bypass the liver

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39
Q

What happens with drugs placed deeper in the rectum?

A

They are absorbed by veins that drain into the portal vein, going to the liver before circulation

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40
Q

What is the most rapid and accurate method of drug administration?

A

Intravenous (IV) injection

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41
Q

Why is IV injection so effective?

A

A precise quantity of the agent is placed directly into the blood and passage through cell membranes is eliminated

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42
Q

Why is the quick onset of IV administered drugs also a hazard?

A

It leaves little time for corrective measures and cannot be removed from the body

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43
Q

Why is the IV administration of street drugs particularly dangerous?

A
  • Drugs that are impure or poor quality provide uncertain doses and reactions are likely
  • Lack of sterile equipment can lead to infection
  • Users may attempt to dissolve drugs that have insoluble filler materials, which, when injected, may become trapped in the small blood vessels in the lungs, leading to reduced respiratory capacity or death
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44
Q

What is the advantage of intramuscular (IM) injection?

A

Slower, more even absorption over a period of time

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45
Q

Drugs administered by IM injection are typically absorbed within how long?

A

10-30 minutes

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46
Q

How can absorption be slowed with IM injection?

A

By combining it with a second drug that constricts blood vessels

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47
Q

What is a disadvantage of IM injections?

A

Sometimes the solution can be very irritating and cause significant muscle discomfort

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48
Q

What method of administration is the most common route for small lab animals?

A

Intraperitoneal (IP) injection

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49
Q

How are drugs administered in IP injection?

A

The drug is administered through the abdominal wall into the peritoneal cavity

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50
Q

Peritoneal cavity

A

The space that surrounds the abdominal organs

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51
Q

Which route of administration allows for drugs to be absorbed at a rate that is dependent on the blood flow to the site?

A

Subcutaneous (SC) administration

52
Q

Why is the effect on the brain so rapid with inhalation methods?

A

Because the blood has a short distance to travel to the heart

53
Q

What are the disadvantages of inhalation methods?

A
  • Irritation of nasal passages

- Damage to lungs

54
Q

Intranasal administration

A

Topical administration of a drug to the nasal mucosa

55
Q

What method can allow a drug to skip first-pass metabolism and bypass the blood-brain barrier?

A

Intranasal topical administration

56
Q

What method of administration allows for a controlled and sustained delivery of a drug at a pre-programmed rate?

A

Transdermal administration

57
Q

What are some advantages to transdermal administration?

A
  • Don’t have to remember pills
  • Painless
  • Avoids first-pass effect
58
Q

What method of administration is preferable in cases of mass vaccination campaigns?

A

Transdermal administration

59
Q

What is the disadvantage of transdermal administration?

A

Only a limited number of drugs are able to penetrate the skin

60
Q

What is possibly the most important factor in determining plasma drug levels?

A

The rate of passage through cell layers between the site of administration and the blood

61
Q

Phospholipids

A

Lipid molecules that are major constituents of the cell membrane; composed of a polar head and two lipid tails

62
Q

Movement across the membranes is always in what direction?

A

From higher to lower concentration

63
Q

The larger the concentration difference on each side of the membrane, the….

A

More rapid the diffusion

64
Q

Does lipid solubility increase or decrease the absorption of drug into the blood?

A

Increase

65
Q

What determines how readily a drug will pass the lipid barriers to enter the brain?

A

The lipid solubility

66
Q

What is one way to predict the relative rate of movement of a drug through cell membranes?

A

Estimate its lipid solubility using its partition coefficient

67
Q

How does one measure the partition coefficient?

A
  • Mix the drug with water
  • Combine it with the same volume of oil or a lipid solvent
  • After settling, the oil and water form two distinct layers, which are then separated and the amount of drug found in each is compared
  • The ratio of the amount of drug dissolved in oil divided by its concentration is the oil/water partition coefficient
68
Q

A higher concentration of drug in the oil compared with that in the water indicates what?

A

Greater lipid solubility and more rapid passage through cell membranes

69
Q

Why are most drugs not readily lipid soluble?

A

Because they are weak acids or weak bases that can become ionized when dissolved in water

70
Q

The extent of ionization depends on what two factors?

A
  • The relative acidity/alkalinity (pH) of the solution

- An intrinsic property of the molecule (pKa)

71
Q

Regardless of the route of administration, once the drug has entered the blood, how long does it take to be carried throughout the body?

A

1 to 2 minutes

72
Q

In general, which parts of the body will have the highest concentration of drug?

A

The parts of the body in which blood flow is greatest

73
Q

Cerebrospinal fluid (CSF)

A

A clear, colourless liquid that fills the subarachnoid space that surrounds the entire bulk of the bran and spinal cord and also fills the hollow spaces (ventricles) and their interconnecting channels (aqueducts), as well as the central canal

74
Q

What is the second barrier that is unique to women?

A

The placental barrier

75
Q

Teratogens

A

Agents that induce developmental abnormalities in the fetus

76
Q

The effect of teratogens are dependent on what?

A

The timing of exposure

77
Q

What are some effects of drug depot binding on therapeutic outcome?

A
  • Reduction in the concentration of drug at its site
  • Slower onset
  • Reduction in effects
  • Higher than expected blood levels of the displaced drug, possibly causing greater side effects
78
Q

First-order kinetics

A

Term used to describe exponential elimination of drugs from the bloodstream

79
Q

Half-life

A

The amount of time required for removal of 50% of the drug in blood

80
Q

Why is half-life important?

A

Because it determines the time interval between doses

81
Q

Why is half-life important?

A

Because it determines the time interval between doses

82
Q

Steady state plasma level

A

The desired blood concentration of drug achieved when the absorption/distribution phases is equal to the metabolism/excretion phase

83
Q

For any given daily dose of a drug, the steady state plasma level is approached after a period of time equal to what?

A

Five half-lives

84
Q

Zero-order kinetics

A

Term used to describe a constant rate of drug removal from the body, regardless of drug concentration in the blood

85
Q

What is the most common reaction in biotransformation?

A

Oxidation

86
Q

What does oxidation produce usually?

A

A metabolite that is less lipid soluble and less active

87
Q

Type II/Phase II involve what kind of modification of the drug molecule?

A

Synthetic

88
Q

Members of the cytochrome P450 (CYO450) class are responsible for what important activity?

A

Oxidizing most psychoactive drugs

89
Q

Microsomal enzymes

A

Enzymes in liver cells responsible for metabolizing exogenous substances such as drugs

90
Q

What can happen with increased numbers of enzyme molecules?

A
  • The drugs speed up their own rate of biotransformation (2-3x)
  • Increase the rate of metabolism of all other drugs modified by the same enzyme
91
Q

What can happen with increased numbers of enzyme molecules?

A
  • The drugs speed up their own rate of biotransformation (2-3x)
  • Increase the rate of metabolism of all other drugs modified by the same enzyme
92
Q

Enzyme induction

A

Increase in liver drug-metabolizing enzymes associated with repeated drug use

93
Q

Genetic polymorphisms

A

Genetic variations among individuals that produce multiple forms of a given protein

94
Q

Enzyme inhibition

A

Reduction in liver enzyme activity associated with a specific drug

95
Q

Receptors

A

Large protein molecules located on the surface of or within cells, and are the initial sites of action of biologically active agents such as neurotransmitters, hormones, and drugs

96
Q

Drug competition

A

Interaction between two drugs that share a metabolic system and compete for the same metabolic enzymes; bioavailability of one or both increases

97
Q

Ligand

A

Any molecule that binds to a receptor with some selectivity

98
Q

What types of molecules attach most readily to the receptor?

A

Those with the highest affinity

99
Q

Dose-response curve

A

A method used to evaluate receptor activity which describes the extent of biological or behavioural effect (response) produced by a given drug concentration (dose)

100
Q

Dose-response curve

A

A method used to evaluate receptor activity which describes the extent of biological or behavioural effect (response) produced by a given drug concentration (dose)

101
Q

Affinity

A

Attraction between a molecule and a receptor

102
Q

Receptor agonists

A

A neurochemical or drug that can bind to a particular receptor protein and alter the shape of the receptor to initiate a cellular response

103
Q

Drug disposition tolerance/Metabolic tolerance

A

Occurs when repeated use of a drug reduces the amount of that drug that is available at the target tissue

104
Q

Receptor antagonists

A

A molecule that interacts with a receptor protein and produces no cellular effect after binding, and also prevents an “active” ligand from binding

105
Q

Partial agonists

A

Drug that acts as an agonist to some receptors, but an antagonist to others

106
Q

Up-regulation

A

Increase in the number of receptors, which may be a consequence of denervation or of chronic antagonist treatment

107
Q

Inverse agonists

A

Substance that activates a receptor but produces the opposite effect of a typical agonist at that receptor

108
Q

Down-regulation

A

Decrease in the number of receptors, which may be a consequence of chronic agonist treatment

109
Q

Cross-tolerance

A

Tolerance to a specific drug can reduce the effectiveness of another drug in the same class

110
Q

Acute tolerance

A

Rapid tolerance formed during a single administration of a drug

111
Q

Sensitization

A

The enhancement of particular drug effects after repeated administration of the same dose of drug

112
Q

Noncompetitive antagonists

A

Drug that reduces the effect of an agonist, but does not compete at the receptor site

113
Q

Physiological antagonism

A

Drug interaction characterized by two drugs reducing each other’s effectiveness in the body

114
Q

Identify the five factors that affect drug action, and very briefly explain an example of how each one

A
  • Route of administration
  • Absorption and distribution
  • Binding
  • Inactivation
  • Excretion
115
Q

What are the five gross categories of drugs?

A
  • CNS stimulants
  • CNS depressants
  • Analgesics
  • Hallucinogens
  • Psychotherapeutics
116
Q

What is an example of a CNS stimulant?

A
  • Amphetamine
  • Cocaine
  • Nicotine
117
Q

What is an example of a CNS depressant?

A
  • Barbiturates

- Alcohol

118
Q

What is an example of an analgesic?

A
  • Morphine

- Codeine

119
Q

What is an example of a hallucinogen?

A
  • Mescaline
  • LSD
  • Psilocybin
120
Q

What is an example of a psychotherapeutic?

A
  • Prozac

- Thorazine

121
Q

Describe a psychological effect of a CNS stimulant at a typical dose

A

Increased electrical activity in the brain and behavioural arousal, alertness, and a sense of well-being in the individual

122
Q

Describe a psychological effect of a CNS depressant at a typical dose

A

Depress CNS function and behaviour to cause a sense of relaxation and drowsiness

123
Q

Describe a psychological effect of an analgesic at a typical dose

A

Reduce the perception of pain

124
Q

Describe a psychological effect of a hallucinogen at a typical dose

A

Alter one’s perceptions, leading to vivid visual illusions of distortions of objects and body image

125
Q

Describe a psychological effect of a psychotherapeutic at a typical dose

A

Treat clinical disorders of mood or behaviour

Psychopharmacology (10 decks)

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