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Biomedical Lab III > Lab 6 > Flashcards

Lab 6 Flashcards

1
Q

Pharmacology includes…..

A

The biochemical and physiologic study of drug effects related to mechanisms of drug action, absorption, distribution, metabolism, elimination, adverse effects, and toxicity

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2
Q

What is first studied in pharmacological studies?

A

The chemical and physical properties of the molecule

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3
Q

_____ are used to conduct the non clinical experiments

A

Animals

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4
Q

When are clinical studies in humans conducted?

A

Before use in the general population

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5
Q

Pharmacokinetics relates to….

A

The action of the BODY on the drug such as drug absorption, distribution, metabolism, and excretion

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6
Q

Pharmacodynamics relates to…..

A

The action of DRUGS ON THE BODY based on its biochemical, physiological, and pharmacological mechanisms of action

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7
Q

How do most drugs produce their effects?

A

By binding to specific receptors present in the tissue cells

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8
Q

As mentioned, most drugs produce their effects by binding to specific receptors present in tissue cells.
The predicted effect is unlikely to occur if what?

A

If the receptor is not present in the tissue OR if the drug is not present in the effective concentration

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9
Q

What is an agonist

A

An endogenous molecule or a drug that interacts with the specific receptor and produces its intrinsic activity

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10
Q

What is an antagonist

A

A chemical that can bind to the specific receptor and BLOCK its intrinsic activity

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11
Q

What can you say about partial agonists and partial antagonists

A

They may not produce the full effects in their effective concentrations

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12
Q

what is the dose-response relationship?

A

it combines the principles of pharmacokinetics and pharmacodynamics to determine the therapeutic dose and frequency and evaluate toxic effects

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13
Q

how is the dose response curve plotted?

A

measured response vs log dose

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14
Q

What is another name for a cholinergic agonist

A

cholinomimetics

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15
Q

cholinomimetics have agonist activity where?

A

at muscarinic acetylcholine receptors. They augment (add to) parasympathetic nervous system activity

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16
Q

cholinergic agonists aument activity of the parasympathetic nervous system.
what is the result of this?

A

INCREASED GI motility and DECREASED intraocular pressure

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17
Q

the anticholinergic agent works to…

A

inhibit PSNS (parasympathetic nervous system) activity

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18
Q

explain the mechanism of anticholinergics

A

they are ANTAGONISTS of muscarinic receptors, resulting in increased heart rate, increased conduction velocity, and stimulates bronchodilation

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19
Q

name 3 cholinomimetics and their uses

A

bethanechol – neurogenic ileus and urinary retention

pilocarpine - glaucoma and alleviating the symptoms of
Sjorgen’s syndrome

nicotine - in smoking cessation regimens

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20
Q

name 4 anticholinergics and their uses

A

oxybutynin - urge incontinence and postoperative bladder spasm

scopolamine - prevent motion sickness and postoperative nausea/vomiting

atropine - used in ACLS guidelines to treat bradyarrythmia and retinal dilator (in ophthalmic surgery)

ipratropium and tiotropium - correct acute exacerbations of bronchospasm (asthma, COPD) and exacerbation prophylaxis for these conditions

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21
Q

what is dopamine?

A

a monoamine catecholamine neurotransmitter and hormone

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22
Q

what does dopamine bind to? what is its function?

A

D1 and D2 dopamine receptor

D1 - memory, attention, impulse control, regulate renal function, locomotion

D2 - locomotion, attention, sleep, memory, learning, emesis

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23
Q

name a dopaminergic agonist

A

Levodopa - the precursor of dopamine

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24
Q

name a dopaminergic antagonist class of drugs

in which dosage forms are they available?

A

phenothiazine class of drugs
-prochlorperazine
-chlorpromazine

IV. rectal, PO

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25
Q

dopaminergic antagonists can block which 3 receptors?

A

histaminergic
cholinergic
noradrenergic

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26
Q

what does GABA stand for

A

Gamma-aminobutyric acid

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27
Q

explain what GABA is

A

an amino acid that is the primary inhibiter neurotransmitter for the CNS

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28
Q

what is the function of GABA

A

to reduce neuronal excitability by INHIBITING NERVE TRANSMISSION

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29
Q

what are GABA receptors?

A

receptors that respond when GABA is released into the post-synaptic nerve terminal

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30
Q

what are the chief inhibitory receptors for the central nervous system?

A

GABA receptors

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31
Q

how are GABA receptors subdivided?

A

GABAa
GABAb

GABAa = ligand gated ion channel. inotropic receptor

32
Q

name 3 GABA receptor agonists

A

alcohol (ethanol), barbiturates, benzodiazepines

33
Q

name 3 barbiturates

A

phenobarbital
pentobarbital
sodium thiopental

34
Q

between benzodiazepines and barbiturates – which are used more frequently now? why?

A

benzodiazepines are used more frequently because barbiturates have high addiction potential and lack of antidote

35
Q

what are GABA antagonists

A

drugs that bind to GABA receptors but do NOT increase the amount of GABA

36
Q

give 2 examples of GABA antagonists

A

picrotoxin
bicuclline methiodide

37
Q

the 2 GABA antagonists mentioned – picrotoxin and bicuclline methiodide – are mainly used for what?

A

research

38
Q

GABA antagonists are ___ and ____

A

proconvulsants and stimulants

39
Q

volume drug solution (normal saline) to be injected formula

A

mL = body weight (kg) * Dose (mg/kg)

/concentration (mg/mL)

40
Q

why is non-clinical testing performed during drug development?

A

to assess the safety profile and PK/TK (pharmacokinetic and toxicokinetic) characteristics of the drug candidate

41
Q

non-clinical testing is performed how?

A

both in vitro and in vivo

42
Q

name 4 types of non clinical studies

A

pharmacodynamics
safety studies
pharmacokinetics
toxicokinetics

43
Q

what is the purpose of non-clinical testing: pharmacodynamics? how is it performed?

A

to test the effect of the drug on the body

can be done in vivo and/or in vitro

44
Q

safety studies are generally conduced how?

A

in vitro

45
Q

in vivo vs in vitro

A

in vivo = in a living organism

in vitro = in a test tube or equivalent

46
Q

safety studies identify what?

A

undesirable effects on the respiratory, CNS, and cardiovascular functions (within the recommended dose AND higher doses)

47
Q

toxicokinetics evaluates what

A

ADME under condtions that produce toxicity

48
Q

how are toxicology studies performed

A

initially in rodents, and then studies in a larger animal species (dogs for ex)

49
Q

toxicity studies evaluate the toxicity profile of the compound using…..

A

single dose and repeated doses

-genotoxicity
-carcinogenity
-development and reproductive toxicity

50
Q

animals are critical in…..

A

evaluating potential usefulness and safety of new drugs prior to trial in humans

51
Q

what 3 guidance and regulatory documents outline the use of animals to evaluate pharmacology and safety risk of drug candidates?

A

-institutional animal care and use committee (IUPAC)

-OSH guidelines (occupational safety and health)

-international conference on harmonization

52
Q

define a drug

A

a substance that brings about a change in biologic functions through its actions on the body

53
Q

how do most drugs produce their effects

A

by binding to a receptor

54
Q

define diluent

A

substances or solutions added to drug to obtain required drug concentration and/or dosage form

55
Q

the PHARMACOLOGIC CLASS is based on what 3 things

A

mechanism of action
physiologic effect
chemical structure

56
Q

define mechanism of action

A

the pharmacologic action at the receptor, membrane, or tissue level

57
Q

define physiologic effect

A

the pharmacologic effect at the organ, system, or whole body level

58
Q

what is the mechanism of action of diazepam

A

GABAa - increase the frequency, but not duration of openings at GABA-activated Cl- channels

59
Q

what is the physiologic effect of diazepam

A

increased GABA activity

60
Q

what is the chemical structure of diazepam

A

benzodiazepine

61
Q

the pharmacokinetic properties of a drug are important when selecting what?

A

the route and dose of the drug (as ADME is affected by age, disease, etc)

62
Q

drug-receptor interactions
-pharmacokinetics or pharmacodynamics

A

pharmacodynamics

63
Q

define drug dose

A

the specific amount of drug administered at one time or at defined intervals to obtain a therapeutic effect

64
Q

the drug dose varies with what 3 factors

A

route
weight
age

65
Q

in toxicology, what is the “toxic dose”

A

the amount of drug that causes harmful or toxic effects

66
Q

what is the difference between side (adverse) effects and toxic effects?

A

side effects are an unexpected effect when the drug is administered in the RECOMMENDED dose

toxic effects are the result of harmful effects when greater than the therapeutic dose is given

67
Q

what is the therapeutic window

A

safe range between the minimum therapeutic concentration and the minimum toxic concentration

68
Q

when does systemic action occur

A

when the drug is absorbed into the circulatory system and affects organs and tissues away from the site of administration

69
Q

true or false

systemic absorption can affect multiple organs

A

true

70
Q

local action is to the area ______ to the application

A

proximal

71
Q

where local action is intended, systemic absorption is…….

A

not typically desired and is unnecessary for therapeutic effect

72
Q

what are the primary routes of administration for pharmaceutical products (as defined by USP)

A

enteral
parenteral
topical
mucosal

73
Q

volume administered =

A

body weight (kg) * dose (mg/kg)

/

concentration (mg/mL)

74
Q

normal saline injection volume =

A

10mL/kg

75
Q
A

Biomedical Lab III (10 decks)

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