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BIOM*3090. UOG > Pharmacology Definitions > Flashcards

Pharmacology Definitions Flashcards

1
Q

define pharmacokinetics

A

how the body handles and process drugs

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2
Q

define pharmocodynamics

A

how drugs act on the body via drug receptor interactions

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3
Q

what is a drug

A

its a substance that changes physiology through its chemical actions

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4
Q

what is a toxicant

A

its a poison or poisonous agent that has almost exclusively harmful effects

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5
Q

what is a toxin?

A

its a toxicant of biological origin (eg endotoxin, venom, poison ivy toxin, ricin)

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6
Q

what is a dose?

A

is the difference between a drug and a poison, or a foodstuff and a poison

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7
Q

All drugs have 3 types of names. what are those subcategories?

A

chemical name, generic name, commercial/trade/brand names.

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8
Q

how do cells comminicate in the body?

A

they use intercellular signalling molecules, which interact with proteins and receptors in the plasma membrane to regulate biochemical pathways in the cytoplasm

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9
Q

what is the signal transduction pathway?

A

its the receptor, its cellular target and any intermediary molecules involved in a chemical message.

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10
Q

in order for drugs to interact with receptors, they need to possess adequate what?

A

size, charge and shape/atomic composition

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11
Q

what is the range of size of drug molecules?

A

lower limit ~100MW: minimyum size needed to impart specificity of action
upper limit ~1000MW: size limit allowing reasonable movement in the body to site of action
Very large drugs must be administered directly to site

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12
Q

what makes a drug receptor selective?

A

its when the chemical bind/force is weak between the drug and the receptor. they require more precise fits if the interaction were to occur.

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13
Q

how could a drug interact with the receptors that dont have optimal fits?

A

if the D-R bond is strong enough.

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14
Q

what are the 3 kinds of bonds that exist ?

A
  1. covalent (rare/strong/irreversible)
  2. Electrostatic/hydrogen/van der waals (weaker/many D-R interactions)
  3. hydrophobic (very weak/most important with lipid interactions and highly lipid-soluble drugs/many D-R interactions)
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15
Q

what is an enantiomer?

A

its a chiral centers, drugs that act this way may be more potent because the reflect better fits with receptors.

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16
Q

in what two ways do drugs modify signal transduction after binding to receptors?

A
  1. they can initiate or enhance

2. they can diminish or terminate (block)

17
Q

how can a drug be effective immediately vs. delayed?

A

depending on the signal transduction pathway being modulated. the effect is genereally proportional to the percentage of receptors occupied by the drugs.

18
Q

what is a second messenger?

A

its a cytoplasmic molecule that translates D-R interactions into a change in cellular activity. They are acted on by effortor molecules

19
Q

what is a well-established second messenger?

A

they entail reversible phosphorylation of key target (enzyme). its allows for amplification of signal, and allows for flexible regulation of signalling

20
Q

most drugs act on receptors that have what kind of lingand, (provide examples)

A

endogenous,

neurotransmitters and hormones

21
Q

why are drugs given therapeutically?

A
  1. to stimulate receptors in hypofunctional states

2. block receptors in hyperfunctional states.

22
Q

what is an agonist?

A

it activates receptors and initiates cellular responses

23
Q

what is a partial agonist?

A

an agonist that is not able to fully activate the receptor

24
Q

what is an antagonist?

A

binds but does not activate the receptor (simply prevents agonists from stimulating the receptor)

25
Q

what is an inverse agonist?

A

it reduces constitutive activity of receptor.

26
Q

waht is the dose-response curve?

A

DRC is a depiction of the observed drug effect with (% maximal response) as a function of drug concentration.

27
Q

define potency

A

its the concentration of a drug required to produce a given effect; measure of a drug’s affinity for and activity at the receptor. Normally defined by the half-maximal effective concentration (EC50)

28
Q

how do you measure realtive potency?

A

comparison of EC50 values between drugs acting at the same receptor

29
Q

is the most potent drug the most efficacious?

A

not necessarioly

30
Q

when would low potency be a concern?

A

if the volume of the required does is too large to be convenient

31
Q

what is efficacy?

A

the magnitude of the cellular response produced when all receptors of a given type are occupied by the ligand
(its defined by the maximal response (Emax) of the drug.

32
Q

how do you measure the relative efficacy?

A

comparing the maximal responses of drugs acting upon the same receptors.

33
Q

what is a non-competitive antagonism?

A

antagonist that binds irreversibly to receptor or only very slowly dissorciates. higher agonist concentrations cannot overcome the effects of a fixed dose of antagonist.

34
Q

whatr is a competitive antagonism?

A

antagonist has affinity for receptor by no efficaty, completes with agolnist at site. Higher agonist concentration can overcome the effects of a fixed dose of antagonist
antagonist produces parallel rightward shift in dose-responses curve.

35
Q

What is tolerance?

A

its the gradual decrease in responsiveness to chronic drug administration. (desensitization/down-regulation)

36
Q

what are some possible mechanisms for development tolerance?

A
  1. temporary inaccessibility of receptors (phosphorylation)
  2. sequestration of receptors in cell (internalization)
  3. Reduced synthesis of new receptors
37
Q

what is tachyphylaxis

A

refers to rapid (acute) form of tolerance

38
Q

what is supersensitivity

A

an increase response to agonist. Usually due to chronic under-stimultion of the receptor -> causes the cell to express increased receptor numbers
May occur when a receptor antagonist has been used chronically and is suddenly withdrawn

BIOM*3090. UOG (22 decks)

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