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CMBM Exam 4 Gopi > Receptors > Flashcards

Receptors Flashcards

0
Q

Propranolol [inderal]

A

Cell surface receptor antagonist

beta adrenoceptor blockers for angina, MI, heart failure, High BP, performance anxiety

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1
Q

Drug mechanisms

A 
antagonists of cell surface receptors 
antagoinsts of nuclear receptors 
enzyme inhibitors 
ion channel blockers 
transport inhibitors 
inhibitors of signal transduction proteins
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2
Q

Tamoxifen [Nolvadex]

A

Nuclear receptor antagonist

Estrogen receptor antagonists for prevention and treatment of breast cancer

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3
Q

Aspirin, ibuprofen [Motrin]

A

Inhibits enzymes

cyclooxygenase inhibitors for pain relief, particularly due to arthritis

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4
Q

Diltiazem [Cardizem]

A

Block ion channels

calcium channel blocker for angina and High BP

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5
Q

Fluoxetine [Prozac]

A

Transport inhibitor
selective serotonin reuptake inhibitor
for treatment of depression

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6
Q

Sildenafil [Viagra]

A

inhibits signal transduction proteins
Type 5 phosphodiesterase inhibitor for erectile dysfunction
cGMP impt in vasodilation in veins
if inhibit it, builds up and causes more vasodilation

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7
Q

Phenylephrine [Neosynephrine]

A

activates cell surface receptor
alpha adrenoceptor agonists for nasal congestion
vasoconstriction of blood vessels in nose prevents exudation into tissues

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8
Q

Conjugated equine estrogen [Premarin]

A

activate nuclear receptor

estrogen receptor agonists for hormone replacement therapy in postmenopausal women

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9
Q

Pralidoxime [Protopam]

A

activates enzymes

reactivator of cholinesterase after poisoning with nerve gas or organophosphate pesticide

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10
Q

Minoxidil [Rogaine]

A

open ion channels

Potassium channel openers for hair regrowth

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11
Q

Drug that is an enzyme

A

Alteplase [Activase]

thrombolytic therapy for acute MI

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12
Q

Vincristine or Vinblastine

A

disrupt structural proteins

vinca alkaloids for cancer

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13
Q

Cyclophosphamide [Cytoxan]

A

covalently link to macromolecules

DNA alkylating agents for the treatment of cancer

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14
Q

Dimercaprol [penicillamine]

A

binds free molecules or atoms

chelating agent for heavy metal poisoning

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15
Q

Mannitol

A

exerts action due to physical property

osmotic diuretic for edema

16
Q

affinity constant

A

Kaff = k1/k2

higher the better attraction

17
Q

potency

A

amount of drug required to elicit a response
characteristic that can be compared by use of EC50 values
often expressed as dose of a drug required to achieve 50% of the desired therapeutic effect ED50 (effective dose)

18
Q

the smaller the Ec50

A

the more potent the drug

19
Q

Quantal

A

all or none response, population

20
Q

Graded

A

range of responses, individual

21
Q

analogs of active drugs are sought to

A 
be more potent 
more completely absorbed 
less rapidly metabolized 
less bound to plasma proteins 
less toxic
22
Q

Efficacy

A

ability of agonist to cause the receptor to assume an active conformation
represented by k3
maximal response a drug can produce

23
Q

Parital agonist

A

dual activity
produces biologic response but cannot produce 100% of the biologic response even at very high dose
partially inhibit the response to full agonists at the same receptor type

24
Q

spare receptor

A

presence shifts the agonist concentration effect curve to the left of the Kd for binding of agonist to receptor
makes tissue more sensitive to an agonist without changing its affinity for the receptor

25
Q

Kd

A

when 50% of drug is bound to receptor and 50% of drug is not bound to the receptor

26
Q

Therapeutic Index

A

LD50/ED50

measure of drug safety

27
Q

Margin of safety

A

LD1/ED99

more realistic measure of drug safety

28
Q

Protective index

A

is ED50

undesirable effect/ ED50 (desireable effect)

29
Q

Noncompetitve antagonist

A

reduces the maximal response that an agonist can produce

30
Q

chemical antagonist

A

interacts directly with the drug being antagonized to remove it or prevent it from binding to target

31
Q

Drug tolerance

A

diminished response to drug over time

32
Q

Desensitization

A

rapid process involving continuous exposure to drug, altering the receptor so that it cannot produce a response

33
Q

Tachyphylaxis

A

rapid development of tolerance several doses over a short time deplete the pool reducing the response to successive doses

34
Q

Potentiation

A

5+0 = 20

35
Q

Synergism

A

4+6 = 16

36
Q

Selectivity

A

confered by either
the cell type specificity of receptor subtypes
the cell type specificity of receptor effector coupling

37
Q

dose effect relationship

A

predicts the effects of changing dose
reveal the necessary trade offs between efficacy and adverse effects
facilitate comparisons of alternative meds for the same indication
ehnace understanding of how best to use receptor blockers

CMBM Exam 4 Gopi (10 decks)

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