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Pharm > Receptor Theory, Signal Transduction, And Dose-Response > Flashcards

Receptor Theory, Signal Transduction, And Dose-Response Flashcards

1
Q

Drugs

A

. Small organic molecules that have specific 3D shape and electronic charge configuration
. Interact w/ macromolecules that have complementary configurations (receptors)

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2
Q

Examples of drug receptors

A 
. NT and hormone receptors 
. Enzymes 
. Transport proteins 
. Ion channels 
. Ion receptors 
. Cell recognition and adhesion molecules
. Nuclei acids
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3
Q

For most drugs, the duration of action is directly related to ______

A

. Time in which drug is bound to receptor

. When drug is cleared from bloodstream it dissociates from receptor and it’s action ends

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4
Q

Examples of drugs that do not act at specific receptors

A

. Antacids

. Cheating agents

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5
Q

Forces involved in drug-receptor interactions

A

. Electrostatic interactions (btw functional groups w/ opposite charges
. Hydrophobic ( non polar regions of drug and receptor interact)
. Van der waals
. Covalent bonding (drugs bind irreversibly w. Receptor through covalent binding)

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6
Q

Types of Electrostatic interactions

A

. Ionic: fully charged
. Dipolar: partially charged
. H bonding

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7
Q

Drug-receptor interactions have a high degree of ____ specificity

A

. Structural

. Slight changes in structure of drug causes large changes in activity

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8
Q

Agonism

A

. Drugs interact w/ receptors that activate receptor-effector mechanism (signal transduction pathways) and alter function of target cell

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9
Q

Competitive antagonism

A

. Drug occupies receptor and prevents agonist from binding to receptor
. Need more conc. Of agonist in order to reach same intensity of response

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10
Q

Affinity

A

. Propensity of drug to bind to given receptor

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11
Q

Intrinsic activity

A

. Ability of drug to initiate a response by producing conformational changes needed to activate receptor-effector mechanism

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12
Q

. Agonist has both ___ and _____ drug-receptor interactions

A

. it has affinity and intrinsic activity

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13
Q

Does a competitive antagonist have affinity or intrinsic activity?

A

. It has affinity

. Has no intrinsic activity

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14
Q

Other types of actions besides competitive antagonism

A

. Partial agonists
. Mixed agonist/antagonists
. Inverse agonists

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15
Q

Inverse agonists

A

. Drugs that can bind to receptor and stabilize the receptor in an inactive state
. Results in effects on the signaling pathway that are opposite those of an agonist
. Drug decreases basal activity of signaling response mechanism

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16
Q

Non-competitive antagonism

A

. Antagonist on the same molecule but at different binding site than antagonist
. Never get to same intensity of response as agonist alone

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17
Q

Chemical antagonism

A

. Antagonist interacts directly with agonist drug an inactivates it

18
Q

Functional antagonism

A

. Antagonist acts through a completely different mechanism to counteract the effects of the agonist

19
Q

Concentration-effect relationships

A

. Intensity of drug effect is dependent on drug conc. At site of action

20
Q

General process and assumptions of concentration-effect relationships

A

. Relationship is reversible, equilibrium process
. One drug molecule combines w. One receptor
. Response is directly related to number of receptors occupies
. Amount of drug actually bound is negligible compared to the amount free

21
Q

Equation to determine concentration of drug to get certain intensity of drug’s effect

A

. Effect = Max effect [D]/(Kd + [D])
. [D] is free drug conc.
. KD is dissociation constant and represents drug conc. At which effect is 1/2 of the max

22
Q

Drug-receptor interactions follow principles described for ___ interactions

A

. Enzyme-substrate

23
Q

Michealis Menten equation

A

V = Vmax[S]/(Km+[S])

24
Q

Drug potency

A

. Amount of drug needed to produce given effect

25
Q

Efficacy

A

. Ability of drug to product an effect w/o regard to concentration

26
Q

Graded dose response relationship

A

. Shows intensity of a drug effect in a subject is a function of the drug dose
. Has biological variation
. Potently is the position of the curve on X axis determined by pharmacokinetics and inherent ability fo drug to bind to receptor and product effect

27
Q

. Threshold dose

A

. Any dose below that amount no effect would be seen

28
Q

Maximal effect (efficacy)

A

. Determined by pharmacokinetics of drug and inherent ability to produce an egg etc

29
Q

Quantal dose-response relationship

A

. Shows the percent of subjects in a population that exhibit a response of given intensity as a function of a drug dose
. Curves can be used to compare effect of different drugs in population os test subjects
. Useful to compare dose of single drug that produces different effects in a population of subsections

30
Q

Therapeutic index

A

LD50/ED50
. LD50: lethal dose. Where 50% of subjects died
. ED50: 50% of subjects reached efficacy in response of drug

31
Q

Toxicity index

A

. TI = TD50/ED50
. TD50: dose amount where 50% of subjects felt toxic effect
. TD50: dose amount where 50% of subject felt efficacy response

32
Q

Tolerance

A

. Dec. sensitivty to drug

. Seen after chronic treatment

33
Q

Pharmacokinetic tolerance

A

. Due to induction of enzymes that metabolize drug

34
Q

Pharmacodynamic tolerance

A

. Due to changes in sensitivity of drug receptors

. Usually involves compensatory changes in number of receptors or sensitivity of receptors (effector mechanisms)

35
Q

Tachyphylaxis

A

. Rapidly developing pharmacodynamic tolerance

36
Q

Physical drug dependence

A

. Tolerance
. Withdrawal syndrome ( physiologic symptoms that appear when drug is abruptly stopped, effects opposite of effect drug produces)

37
Q

Pharmacodynamic basis of tolerance and dependence

A

. Related to compensatory changes in receptors and effector mechanism

38
Q

Idiosyncratic effect

A

Unusual drug effect in certain individuals

39
Q

Drug allergy

A

. Drug acts as allergen to activate immune response

40
Q

Additive effects

A

. Combined drug effect is equal to sum of effects of each drug

41
Q

Synergistic effect

A

. Combined drug effect of 2 drugs is greater than sum of the effects of each drug alone

42
Q

Potentiation

A

. 1 drug enhances the toxic actions of another

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