Exam 2 Material Flashcards

1
Q

Science of interactions of chemical compounds with biological systems, how and where drugs act

A

Pharmacology

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2
Q

Study of biochemical and physiological effects of drugs and the mechanisms of their actions, including the correlation of their actions and effects with their chemical structure

A

Pharmacodynamics

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3
Q

The study of absorption, distribution, biotransformation, and elimination of xenobiotics

A

Pharmacokinetics

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4
Q

Characteristics of drugs

A

Defined by actions, most act on receptors

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5
Q

Endogenous drugs

A

foreign to the body, include toxins/poisons

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6
Q

Where endogenous ligands bind

A

orthosteric site

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7
Q

Receptor where gastric acid is neutralized by antacids

A

Extracellular receptor

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8
Q

Receptor used to treat infections, cancer therapy, hormones like estrogen

A

Intracellular receptor

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9
Q

Receptor of acetylcholine, muscarinic, nicotinic, GF receptors

A

Cell surface receptor

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10
Q

Drug that binds to a receptor and stimulates a biological response

A

Agonist

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11
Q

Drug that binds to a receptor without altering receptor function, alters interaction of receptor with another drug

A

Antagonist

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12
Q

Drug must achieve adequate concentrations at site of action to produce characteristic effect

A

Purpose of drug therapy

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13
Q

T/F No drug has a single effect

A

True

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14
Q

KD measures

A

Affinity, determines potency

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15
Q

Lower KD means

A

Higher affinity

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16
Q

Cheng Prusoff

A

Ki = IC50/[1+L/KD]

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17
Q

Total number of receptors on given cell or tissue

A

Bmax

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18
Q

Affinity of ligand for the receptor identified at 1/2 Bmax

A

KD

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19
Q

DOR,KOR,MOR question

A

Most selective for DOR - low ki value for DOR, high for MOR and KOR
Least selective - close values of ki for DOR, MOR, and KOR

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20
Q

Binding of an agonist results in

A

induced fit that activates the receptor

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21
Q

Binding of an antagonist results in

A

An induced fit that does not activate the receptor

22
Q

Dose response curve for agonist

A

Highest

23
Q

Dose response curve for antagonist

A

Zero

24
Q

Dose response curve for inverse agonist

A

negative

25
Q

Potency on graph

A

Farthest left on graph

26
Q

Efficacy on graph

A

Height on graph, limited by toxicity

27
Q

Produces a reduced response even at full receptor occupancy, can’t produce same effect as full agonist regardless of concentration

A

Partial agonist

28
Q

Inverse agonist binds to

A

Orthosteric site

29
Q

Competitive antagonism on graph

A

Lines same shape spaced apart

30
Q

How to reverse competitive antagonism

A

Increase dose

31
Q

Schild plot determines

A

Affinity of agonist or receptor

32
Q

Non competitive agonist on graph

A

Lines different heights same starting point

33
Q

Non competitive agonist increases ____ an decreases ___

A

KD, Emax

34
Q

When the max response can be elicited by an agonist that does not result in 100% occupancy

A

Spare receptor

35
Q

Functional antagonism

A

Two drugs influence a physiological system in opposite directions
ex - histamine and epinephrine

36
Q

Chemical antagonism

A

Chemical reaction between agonist and antagonist that forms inactive product

37
Q

Allosteric ligand benefit in therapy

A

ceiling effect, increased specificity for receptors with similar orthosteric binding sites

38
Q

Ki value table problems

A

Ki = 50% occupied
Divide by 10 is 10% occupancy
multiply by 10 is 90% occupancy

39
Q

Men who studied GPCRs

A

Lefkowits and Brian kobilka

40
Q

G protein effectors

A

Channels, enzymes, regulatory proteins

41
Q

G protein subtypes/second messengers

A

Cyclic AMP, Ca2+, Phosphoisinotides

42
Q

Quantal log dose response

A

All or none, increasing curve, ED50, LD50, or TD50

43
Q

Graded log dose response

A

Increases with increasing concentration, progressive increase, ED50 or TD50, S shaped with center symmetry
Allows comparison of drugs with similar properties

44
Q

Calculate therapeutic indec

A

LD50/ED50, larger ratio= greater safety

45
Q

Drug tolerance

A

Decreased responsiveness to a drug

46
Q

Cross tolerance

A

Tolerance develops to one drug seen with drugs belonging to the same class

47
Q

Tachyphylaxis

A

Acute development of tolerance following rapid or repeated administration, can’t overcome with increased dose

48
Q

Behavioral sensitization

A

Increased effect of drug the more times its administered

49
Q

Idiosyncratic reaction

A

Genetically determined abnormal reactivity to a drug, sensitive to low doses or not sensitive to high doses

50
Q

Physiological variables

A

Age, Gender, Pregnancy, Food, Circadian Clock

51
Q

Pathological factors

A

Liver disease, Renal disease, Malnutrition

52
Q

Genetic factors

A

Pseudocholinesterase deficiency, malignant hyperthermia