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Biomedical Lab III > Lab 6 > Flashcards

Lab 6 Flashcards

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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
dopaminergic antagonists can block which 3 receptors?
histaminergic cholinergic noradrenergic
26
what does GABA stand for
Gamma-aminobutyric acid
27
explain what GABA is
an amino acid that is the primary inhibiter neurotransmitter for the CNS
28
what is the function of GABA
to reduce neuronal excitability by INHIBITING NERVE TRANSMISSION
29
what are GABA receptors?
receptors that respond when GABA is released into the post-synaptic nerve terminal
30
what are the chief inhibitory receptors for the central nervous system?
GABA receptors
31
how are GABA receptors subdivided?
GABAa GABAb GABAa = ligand gated ion channel. inotropic receptor
32
name 3 GABA receptor agonists
alcohol (ethanol), barbiturates, benzodiazepines
33
name 3 barbiturates
phenobarbital pentobarbital sodium thiopental
34
between benzodiazepines and barbiturates -- which are used more frequently now? why?
benzodiazepines are used more frequently because barbiturates have high addiction potential and lack of antidote
35
what are GABA antagonists
drugs that bind to GABA receptors but do NOT increase the amount of GABA
36
give 2 examples of GABA antagonists
picrotoxin bicuclline methiodide
37
the 2 GABA antagonists mentioned -- picrotoxin and bicuclline methiodide -- are mainly used for what?
research
38
GABA antagonists are ___ and ____
proconvulsants and stimulants
39
volume drug solution (normal saline) to be injected formula
mL = body weight (kg) * Dose (mg/kg) /concentration (mg/mL)
40
why is non-clinical testing performed during drug development?
to assess the safety profile and PK/TK (pharmacokinetic and toxicokinetic) characteristics of the drug candidate
41
non-clinical testing is performed how?
both in vitro and in vivo
42
name 4 types of non clinical studies
pharmacodynamics safety studies pharmacokinetics toxicokinetics
43
what is the purpose of non-clinical testing: pharmacodynamics? how is it performed?
to test the effect of the drug on the body can be done in vivo and/or in vitro
44
safety studies are generally conduced how?
in vitro
45
in vivo vs in vitro
in vivo = in a living organism in vitro = in a test tube or equivalent
46
safety studies identify what?
undesirable effects on the respiratory, CNS, and cardiovascular functions (within the recommended dose AND higher doses)
47
toxicokinetics evaluates what
ADME under condtions that produce toxicity
48
how are toxicology studies performed
initially in rodents, and then studies in a larger animal species (dogs for ex)
49
toxicity studies evaluate the toxicity profile of the compound using.....
single dose and repeated doses -genotoxicity -carcinogenity -development and reproductive toxicity
50
animals are critical in.....
evaluating potential usefulness and safety of new drugs prior to trial in humans
51
what 3 guidance and regulatory documents outline the use of animals to evaluate pharmacology and safety risk of drug candidates?
-institutional animal care and use committee (IUPAC) -OSH guidelines (occupational safety and health) -international conference on harmonization
52
define a drug
a substance that brings about a change in biologic functions through its actions on the body
53
how do most drugs produce their effects
by binding to a receptor
54
define diluent
substances or solutions added to drug to obtain required drug concentration and/or dosage form
55
the PHARMACOLOGIC CLASS is based on what 3 things
mechanism of action physiologic effect chemical structure
56
define mechanism of action
the pharmacologic action at the receptor, membrane, or tissue level
57
define physiologic effect
the pharmacologic effect at the organ, system, or whole body level
58
what is the mechanism of action of diazepam
GABAa - increase the frequency, but not duration of openings at GABA-activated Cl- channels
59
what is the physiologic effect of diazepam
increased GABA activity
60
what is the chemical structure of diazepam
benzodiazepine
61
the pharmacokinetic properties of a drug are important when selecting what?
the route and dose of the drug (as ADME is affected by age, disease, etc)
62
drug-receptor interactions -pharmacokinetics or pharmacodynamics
pharmacodynamics
63
define drug dose
the specific amount of drug administered at one time or at defined intervals to obtain a therapeutic effect
64
the drug dose varies with what 3 factors
route weight age
65
in toxicology, what is the "toxic dose"
the amount of drug that causes harmful or toxic effects
66
what is the difference between side (adverse) effects and toxic effects?
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
what is the therapeutic window
safe range between the minimum therapeutic concentration and the minimum toxic concentration
68
when does systemic action occur
when the drug is absorbed into the circulatory system and affects organs and tissues away from the site of administration
69
true or false systemic absorption can affect multiple organs
true
70
local action is to the area ______ to the application
proximal
71
where local action is intended, systemic absorption is.......
not typically desired and is unnecessary for therapeutic effect
72
what are the primary routes of administration for pharmaceutical products (as defined by USP)
enteral parenteral topical mucosal
73
volume administered =
body weight (kg) * dose (mg/kg) / concentration (mg/mL)
74
normal saline injection volume =
10mL/kg
75

Biomedical Lab III (10 decks)

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