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Pharmacology #1 > Module A-1 > Flashcards

Module A-1 Flashcards

1
Q

Signal Transduction

A

Process by which a cell converts one kind of signal into another, think signal cascade or second messenger pathway

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2
Q

Types of signal Transduction:

A

Ion Channel- think acetylcholine as ligand for receptor vs voltage gated
G-coupled protein receptor-spans 7 times, w/ three subunits-conformational change with GDP-GTP
Enzyme linked-Ex. tyrosine kinase-signal molecule triggers dimerization/phosphorylation of residues with starts cascade

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3
Q

GPCR Ex.

A
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4
Q

Drug receptor Sensitivity

A

Drug response occurs from a low concentration

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5
Q

Drug receptor selectivity

A

Structurally similar chemicals illicit drug response

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6
Q

Drug receptor Specificity

A

Measure of a receptors ability to respond to a single ligand

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7
Q

Affinity VS. Potency

A

Affinity-strength of attraction
Potency-magnitude of drug effect (dose dependent)

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8
Q

Agonist

A

Binds specific receptor and triggers a response in a cell-mimics an endogenous ligand

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9
Q

Agonist

A

Binds specific receptor and triggers a response in a cell-mimics an endogenous ligand

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10
Q

Antagonist

A

Affinity for receptor but no efficacy

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11
Q

Partial agonist

A

Activates receptor but cannot produce maximum response- may also block full effect of true agonist

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12
Q

Inverse Agonist

A

Binds receptor-results in opposite action of agonist

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13
Q

Non competitive antagonism

A

Binds allosteric site- cannot be displaced

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14
Q

Allosteric modulators

A

Binding site adjacent/separate from receptor- can be agonist or antagonist!!

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15
Q

Two state model

A

Constant flux in equilibrium between resting and active states that are conformationally distinct- active state has a higher affinity for an agonist

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16
Q

Upregulation

A

An increase in number/sensitivity of receptors

In response to:
-less stimulation from ligands
-chronic antagonist exposure
Ex. Chronic use of beta adrenergic antagonists (Beta blockers)- rebound hypertension if stopped due to upregulation

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17
Q

Down regulation

A

Decrease in number/sensitivity of receptors due to:
-Repeated agonist exposure

Ex. Chronic beta-agonist use for asthma
-increase dose (side affects) or swap drugs

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18
Q

Tolerance

A

Chronic exposure- increased drug clearance. increasing dose is usually an option

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19
Q

Tachyphylaxis

A

Short term- stepwise reduction in physiological response due to down regulation of receptors-which means increasing the dose will not work

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20
Q

Therapeutic response variation with pharmacogenetics and population variation

A

-age, sex, BSA, weight, metabolic rate, pathological state and genetic profile will all impact therapeutic response

Pharmacogenetics can alter receptor sensitivity and drug metabolism between individuals

21
Q

Mean

A

Average dose to elicit a response

22
Q

Median

A

Dose on either side of which half the responses occur

23
Q

Mode

A

Dose with greatest percentage of responses

24
Q

Standard deviation

A

Variability of a response within a population

25
Q

Standard error of the mean

A

SD of the mean
Obtaining the mean on different populations with same dose response measurements….

26
Q

ED-50

A

Median effective dose

27
Q

ED95

A

95% effective dose

28
Q

Emax

A

Maximal drug effect

29
Q

LD50

A

Lethal dose 50%

30
Q

Therapeutic index

A

LD50/ED50
Therapeutic Saftey margin
Larger the index the safer the drug (how far apart are the ED and LD)

31
Q

Therapeutic window

A

The range of therapeutically effective concentrations, most of the efficacy curve and less than 10% of toxicity curve

32
Q

Addition

A

1+1=2
Drugs act in same pathway
Sulfamethoxazole+trimethoprim

33
Q

Synergism

A

1+1=4
One drug allows the other to perform its function

Ex. Carbidopa+levodopa (keeps levodopa from being degraded in peripheral tissue)

34
Q

Antagonism example:

A

Phentolamine displaces Norepinephrine

35
Q

What increases the tendency to form the drug-receptor complex?

A

Higher concentration of free drug
Presence of unoccupied receptor

36
Q

Law of mass action

A

Rate of a reaction is proportional to the product of the concentrations of each reactant

37
Q

Second messengers and response to:
Catecholamines, caffeine and milrinone

A

(cAMP)
Response: kinase release, beta receptor stimulation, inotropic and chronotropic cardiac effects, production of adrenal and sex steroids, etc…

38
Q

Second messengers and response to Lithium

A

Phosphoinositides and Calcium
Activates calmodulin

39
Q

Nitroglycerin and Nitroprusside second messengers

A

cGMP
Activates protein kinases

40
Q

Fig 5.1-major modes of signal transduction

A
41
Q

Potentiation

A

Effect of a drug is enhanced by a drug with no effect of its own 1+0=3

42
Q

Chiral

A

Not superimposable on its mirror image, optically active

43
Q

Stereoisomer

A

Isomers that differ in the 3-D dimensional arrangement of atoms

44
Q

Enantiomer

A

Stereoisomers that are non-superimposable

45
Q

Racemic mixture

A

A mixture containing two enantiomers in equal proportions will be optically inactive,
Enantiomers can differ in dosages/efficacy/side effects but are sometimes given in racemic form

46
Q

Specificity vs selectivity phrase

A

Select chemicals illicit a specific response

47
Q

Describe GPCR second messenger system

A
48
Q

Describe GPCR second messenger system

A

Pharmacology #1 (15 decks)

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