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PSY 2120 > Basic Pharmacology and Tolerance > Flashcards

Basic Pharmacology and Tolerance Flashcards

1
Q

Drugs

A

any substance that alters the physiology of the body except food and nutrients

intention of user must be taken into account

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2
Q

Psychoactive Drugs

A

substances that impact the NS to alter mood, perceptions, and level of consciousness

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3
Q

Chemical Name

A

describes a drug’s chemical structure

e.g. 5-ethyl-5-phenyl-1,3-diazinane-2,4,6-trione

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4
Q

Generic Name

A

describes a drug’s chemical structure and similarity to other drugs in its class

stem-; -stem-; -stem

e.g. pheno-barb-ital is a part of the sedative/hypnotic barbituates

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5
Q

Excipients

A

fillers, colouring agents, binding agents, flavours, preservatives, coating, etc.

affect absorption and distribution of drugs
-different formulations with the same active
ingredient may not be equally effective

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6
Q

Trade Name

A

for marketing a drug

refers to the drugs active ingredients and excipients

always capitalized

belongs to a company

e.g. Luminal (Bayer)

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7
Q

Street Name

A

selling names for recreational drugs

e.g. purple hearts, goof balls

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8
Q

How are dosages described?

A

ratio of the amount of drug per body weight

e.g. mg/kg

a certain concentration is needed for an effect to be present; taking more doesn’t increase the therapeutic benefit but can increase/add side effects

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9
Q

Dose-Response Curves

A

describe the level of drug effect by dose

horizontal axis represents dosage
vertical axis represents either the percent effect or the percent of subjects showing response

measures one effect at a time

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10
Q

Efficacy

A

maximum response a drug is able to produce

e.g. Aspirin and Morphine both have analgesic effects, but Morphine is much more effective

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11
Q

Potency

A

the dosage of a drug required to produce a particular response

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12
Q

ED50

A

dose at which 50% of an effect is observed or dose at which the effect is present in 50% of subjects

a lower ED50 means a higher potency

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13
Q

LD50

A

dose at which 50% of subjects die

represented on lethality dose-response curves

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14
Q

Therapeutic Index

A

ratio of a drug’s lethal dose-effect to its therapeutic dose-effect value

Standard: LD50/ED50
Ideal: LD1/ED99

Generally speaking, the higher the TI, the safer the drug

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15
Q

Drug Interactions

A

when you add a second drug in the mix, you could increase or decrease the effects of the first drug

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16
Q

Potentiation

A

lowering the ED50 of a drug

raising a drug’s potency

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17
Q

Antagonism

A

raises the ED50 of a drug (lowers potency)
and/or
reduces the efficacy of a drug (lowers max. effect)

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18
Q

Primary Effect

A

the intended effect(s) of a drug

the reason a drug was taken

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19
Q

Side Effect

A

any effect produced unintentionally by the administration of a drug

not necessarily negative

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20
Q

Pharmacokinetics

A

the study of how drugs move into, get around in, and are eliminated from the body

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21
Q

Absorption

A

the entry of a drug into the circulatory system

Route of Administration (RoA) has major effect on absorption

    - it impacts the # of membranes the drug has to pass through
    - since most drugs are hydrophilic, they cannot utilize simple diffusion to pass through membranes
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22
Q

Parenteral Administration

A

injection through the skin into various parts of the body

farther subdivided depending on specific point in body where bolus is left by needle
e.g. intravenous, subcutaneous, intraperitoneal, intramuscular, intracerebral, etc.

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23
Q

Vehicle

A

the liquid into which a drug is dissolved/suspended

necessary because most drugs are naturally powders

injected to form a bolus

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24
Q

Rate of Absorption (Parenteral Administration)

A

determined by…
volume of blood flow (can be increased with heat and exercise)
richness of capillary supply (drug must pass through capillary walls by diffusing through intercellular gaps/fenestrations to enter circulation)

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25
Q

Depot Injections

A

drug is dissolved in a high concentration of viscous oil and then injected into muscle
drug slowly diffuses from the oil into the body fluids over a long period of time
used for drugs that need to be taken continuously or chronically to prevent symptoms from reappearing (e.g. antipsychotics)

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26
Q

Inhalation

A

RoA
lungs are high surface area gas exchange system with a direct connection to the heart and brain
inhalation is regulated by diffusion and can thus be controlled with precision
when ash, vapour, or smoke make contact with surface of lungs, the drug dissolves and diffuses into the blood

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27
Q

Difference between smoke and gasses

A

drugs in smoke particles will not revapourize when dissolved in blood
they cannot be exhaled and must be eliminated by alternative means

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28
Q

Challenges with Oral Administration

A

low stomach pH can destroy some drug molecules
liver enzymes can break down drug molecules

these two combined are an example of First Pass Metabolism

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29
Q

First Pass Metabolism

A

a phenomenon in which the concentration of a drug in the body will be greatly reduced before it reaches general circulation

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30
Q

Oral Absorption and pH

A

an acidic molecule carries a charge, if it is protonated it becomes neutral
a basic molecule on its own is neutral, if it is protonated it carries a positive charge
the pH of the GI tract is acidic, and as such basic drugs do not absorb well from it
acidic drugs absorb well from an acidic environment and vice versa

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31
Q

PKa

A

the pH of the solution at which 50% of drug molecules will be ionized

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32
Q

Distribution

A

passage of a drug through the body

impacts a drug’s bioavailability

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33
Q

Bioavailability

A

the ability of a drug to reach its intended site of action

for psychoactive drugs; the drug’s ability to reach the brain
drugs cannot produce desired effects if they can’t get to where they need to be

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34
Q

Factors that affect drug distribution

A 
Lipid solubility
Ion trapping
Distribution to CNS (central nervous system)
Active/passive transport
Protein binding
The placental barrier
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35
Q

Lipid Solubility

A

hydrophilic substances cannot use simple diffusion to get through membranes; lipid soluble drugs can

if a drug is extremely lipophilic it will stay in a lipid, meaning it doesn’t reach the site of action at least not quickly (this is the principle behind depot injections)

36
Q

Ion Trapping

A

weak acids ionize in basic solutions, weak bases ionize in acidic solutions

once a drug is ionized on one side of a membrane, it cannot diffuse back across

happens where different pHs are separated by a membrane
e.g. GI Tract/Blood or Blood/Urine

37
Q

Blood-Brain Barrier

A

protects the brain from harmful substances in the circulatory system

there are no pores in the capillary endothelial cells (tight junctions instead)
- makes simple diffusion impossible for non-lipid-soluble drugs
astrocytes extend processes that wrap around capillaries creating an extra layer of membrane through which to pass
- makes it harder for lipid-soluble drugs to diffuse

38
Q

Active and Passive Transport

A

transport mechanisms needed depend on solubility, concentration gradient, and electrostatic pressure

39
Q

Simple Diffusion

A

passive transport
moves down concentration gradients
possible for lipid-soluble or small, uncharged molecules

40
Q

Channel Proteins

A

passive transport mechanism
filled with water
allow water-soluble molecules in

41
Q

Carrier Proteins

A

passive transport mechanism
molecule that cannot diffuse binds to a transmembrane protein
protein flips conformation to allow molecules to cross membranes

42
Q

Active Transport

A

utilizes carrier proteins

requires energy input to move substances against their electrochemical gradients

43
Q

Protein Binding

A

some drug molecules have an affinity for plasma proteins in blood
while bound to a protein, the drug is unavailable
reduces the concentration of usable drug in the body at any given time
can be impermanent

44
Q

Placental Barrier

A

similar to blood-brain barrier
usually ineffective against psychoactive drugs
concentration in fetus can be equal to mother’s bloodstream

45
Q

Drug Metabolism

A

process of converting drugs into metabolites
most often takes place in the liver with the helpy of Cytochrome P450 Enzymes
purpose is to make drugs more water-soluble and/or more likely to ionize to make it easier to extrete from kidneys

46
Q

Factors that alter Drug Metabolism

A

depression of enzyme systems
stimulation of enzyme systems
age (systems slow with age)
species (smaller species tend to have faster metabolisms)

47
Q

Elimination

A

prepping/removing the drug from the body

mostly done using the kidneys

48
Q

Pharmacokinetics

A

the study of how drugs move into, get around in, and are eliminated from the body

49
Q

Function of the Kidneys

A

filter everything out of the blood and selectively reabsorb what is required via diffusion and active/passive transport

unless reabsorbed by special transport systems, ionized or non-lipid-soluble drug molecules will be excreted

50
Q

Nephron

A

the basic functional unit of the kidney

51
Q

Peritubular Capillaries

A

capillaries responsible for reabsorption and secretion

52
Q

Afferent Arterioles

A

provide blood supply to nephrons

53
Q

Efferent Arterioles

A

how blood leaves nephrons after filtration

54
Q

Bowman’s Capsule

A

where filtered blood goes

55
Q

Renal Tubule

A

leads to collecting duct, from which filtered substances will be excreted in urine

56
Q

pH of Urine

A

Acidic (approx. 6.0) while blood is basic

basic metabolites become ionized and remain in urine (unable to diffuse) while acidic metabolies concentrate in the blood

if sodium bicarbonate is taken to alkalinize urine, more basic drugs such as barbiturates may be reabsorbed

57
Q

Half-Life

A

the amount of time it takes to reduce the concentration of a substance in the blood by half

58
Q

First Order Kinetics

A

100%-50%-25%-12.5% etc. over consecutive and consistent time intervals

usually takes 5-6 half lives of drugs that reduce via first-order kinetics to eliminate the drug from the body

creates a curve

59
Q

Zero Order Kinetics

A

some drugs (e.g. alcohol) are eliminated at a constant rate (e.g. 15 mg/ 100mL blood/ hr.)

creates a linear graph

60
Q

Elimination Rate

A

amount of drug eliminated from the body over time

typically occurs in half-lives as demonstrated by first order kinetics

determines how long a drug’s effects will last
(i.e. how frequently meds should be taken to produce a
steady state… want to maintain a high enough
concentration to be effective but not high enough to
have adverse effects)

61
Q

Combining absorption and elimination rates

A

rapid absorption=rapid elimination

slower absorption=longer-lasting effects

62
Q

Therapeutic Window

A

the range of blood concentrations of a drug between the level that it is minimally effective and the level that has adverse side effects (between therapeutic and toxic levels)

63
Q

Mechanisms of Tolerance

A

3 mechanisms by which tolerance develops

Pharmacokinetic tolerance
Pharmacodynamic tolerance
Behavioural tolerance

64
Q

Tolerance

A

decreased effectiveness or potency of a drug that results from repeated administrations
or
the necessity of increasingly large doses of a drug to maintain its effectiveness after repeated administrations

65
Q

How tolerance works

A

some effects of a drug develop tolerance more quickly than others, some do not develop tolerance at all

the tolerance develops to drug effects not the drug

66
Q

Other relevant factors that affect tolerance

A

functional disturbances
cross tolerance
acute tolerance

67
Q

Pharmacokinetic tolerance

A

increase in the rate or ability of the body to metabolize a drug, resulting in fewer drug molecules reaching their intended site of action

results from enzyme induction

68
Q

Enzyme Induction

A

increasing number or activity of enzymes

reduces all drug effects because less of the drug reaches its site of action

69
Q

Homeostasis

A

the ability of a living organism to keep conditions inside it the same despite any changes in the conditions around it

maintained via feedback loops

70
Q

Pharmacodynamic tolerance

A

arises from adjustments made by the body to compensate for an effect of the continued presence of a drug
- result of homeostasis

if a drug is repeatedly administered, the body gets better and better at restoring normal function and diminishing the disruptive effects of the drug

71
Q

Up/downregulation of receptors (Pharmacodynamic Tolerance)

A

Neurotransmitters (NTs) work on NT receptor proteins
- the neuronal response depends on the presence of
receptors

If there is more communication desired, more receptors may become available (upregulation) and the opposite can also occur (downregulation)

Many psychoactive drugs mimic NTs and therefore can influence receptor population

72
Q

Behavioural Tolerance

A

through exposure with a drug, an organism can learn to decrease the effect that the drug is having through operant and classical conditioning

aka learned tolerance

73
Q

Classical Conditioning

A

the association of an unconditioned response with a stimulus to create a conditioned response

NS+US=UR

CS=CR

74
Q

Operant Conditioning

A

association of a voluntary behaviour with a consequence (reward or punishment)

75
Q

Acute Tolerance

A

with some drug effects, the effect can be greater at a given blood level during absorption than it is at the same blood level during elimination

this does not require repeated administrations

e.g. alcohol: you are more intoxicated during the absorption

76
Q

Brain Mechanisms responsible for Sensitization

A

there is no single neuronal effect responsible

mesocorticolimbic dopamine (DA) system

 - general motivation system
 - responsible for reinforcement
77
Q

Functional Disturbances

A

physiological disruptions alone are not sufficient to cause tolerance, the change must be MEANINGFUL

e.g. amphetamine supresses appetite in rats, but if a rat is starving and food is available it will develop a tolerance to this effect. if no food is available this tolerance will not develop

78
Q

Sterotypies

A

repetitive or ritualistic movements, postures, or utterances
e.g. body rocking, self-caressing, etc.

can be induced by amphetamine consumption

repeat administrations of dosages causing only behavioural activation will cause stereotyped behaviour

79
Q

Sensitization

A

in some circumstances an effect of a drug can increase with repeat administrations
seen primarily with drugs that at high doses cause stereotypies

80
Q

Withdrawal

A

physiological symptoms/changes that occur when the use of a drug is stopped or the dosage is decreased
symptoms may vary in intensity
drugs of the same family tend to produce ssimilar symptoms
can be stopped by giving the drug or one of the same family

81
Q

Dependence

A

a state in which withdrawal symptoms occur when drug use stops
physiological state does not equal addiction

82
Q

Cross Tolerance

A

tolerance to one drug diminishes the effects of another

e. g. by acting on the same receptors or processed by the same enzymes
e. g. alcohol and sedatives

83
Q

Opponent Process Theory

A

views withdrawal symptoms as a compensatory adjustment made by homeostatic mechanisms to a drug effect after repeat exposure
with the repeat administration of a drug, the body changes its functioning
when a drug is discontinued and its effects disappear it takes the body some time to readjust to the drug’s absence (withdrawal occurs)

A-process (euphoric drug effect)
B-process (dysphoric homeostatic mechanism)

Over time, the user requires more of a drug to feel normal because the B-process acts more quickly and increases in magnitude

84
Q

Placebo Effect

A

inert substances can improve a patient’s condition because the patient expects them to help

85
Q

Nocebo Effect

A

inert substances/suggestions of them can have a negative effect on a patient if they expect it to

psychogenic in nature but can cause real and measurable physiological changes

86
Q

Top-down processing

A

voluntarily engaged, higher abstract modalities of thought and expectations coloured by perceptions

87
Q

Bottom-up processing

A

stimuli reaching receptors

PSY 2120 (4 decks)

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