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Pharmacology > Block 1 Pharmacodynamics > Flashcards

Block 1 Pharmacodynamics Flashcards

1
Q

5 major signaling mechanisms

A

Intracellular rec, transmembrane rec, tm cytokine rec, lig-gated ion channels, GPCR & second messengers

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2
Q

Intracellular receptor drugs

A

Steroid hormones, thyroid hormone, vit D

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3
Q

TM enzyme receptor drugs

A

Insulin, EGF

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4
Q

TM cytokine receptor drugs

A

Growth/diff regulators, GH, erythropoietin, interferon

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5
Q

Ligand-gated ion channel drugs

A

NT-mimetics like Ach, 5-HT, GABA, glutamate

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6
Q

GPCR & second messenger drugs

A

Sympathomimetic drugs

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7
Q

Gs receptor substrates and MOA

A

b-adrenergic, glucagon, 5-HT, histamine

Inc AC = inc cAMP

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8
Q

Gi receptor substrates and MOA

A

a2-adrenergic, ACh (musc), opioids, 5-HT

Dec AC = dec cAMP

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9
Q

Gq receptor substrates and MOA

A

ACh (musc), bombesin, 5-HT

Inc PLC = inc IP3, DAG, Ca2+

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10
Q

Epinephrine

A

alpha-receptor agonist

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11
Q

Albuterol

A

beta-receptor agonist

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12
Q

Morphine, hydrocodone

A

Opioid analgesic, Gi-R agonist

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13
Q

Atenolol

A

B-blocker (b-receptor antagonist)

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14
Q

Tamoxifen

A

ER antagonist (nuclear) for breast cx

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15
Q

ACE inhibitor

A

Enzyme inhibitor for heart failure & HTN

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16
Q

Statins

A

HMG-CoA reductase enzyme inhibitor for hypercholesterolemia

17
Q

Ca-channel blocker

A

Ion channel blocker for HTN & angina

18
Q

SSRI

A

NT inhibitor for depression

19
Q

Potency

A

Concentration of drug required to produce particular effect

20
Q

Median effective dose (ED50)

A

Dose that produces 50% of maximal response

21
Q

Median lethal dose (LD50)

A

Dose that causes death in 50% of subjects

22
Q

Therapeutic index (TI)

A

Ratio of LD50 to ED50, higher TI = safer, smaller risk of OD

23
Q

Dose-response relationship

A

Relationship between concentration of drug at receptor site and magnitude of response

24
Q

Graded dose-response curve vs. quantal dose-response curve

A

G: tracks percent of maximum response versus dose
Q: tracks percent of subjects with response versus dose

25
Q

How does dose-response curve change in presence of competitive and non-competitive antagonists?

A

Comp: increase dose required for ED50, no change in max effect
Non: increase dose more than comp and decrease max effect

26
Q

Tolerance

A

Same dose of drug given repeatedly loses effect, greater doses needed to provide same effect
*CNS or hormone-affecting drugs must be tapered over time

27
Q

Tachyphylaxis & example

A

Acute tolerance - oxymetazolone (Afrin) for nasal congestion

28
Q

Pharmacodynamic tolerance & example

A

Down regulation of receptors (dec synth) - morphine

29
Q

Pharmacokinetic tolerance & example

A

Up regulation of metabolic enzymes (inc synth) - carbamazepine (Tegretol) for seizure control
*Up regulates P450 = inc met of self and other drugs

30
Q

Stereoisomer variation example

A

S-warfarin is 5x more active than R-warfarin & is metabolized by CYP 2C9 instead of CYP 1A2, 3A4

31
Q

Pharmacogenetics vs. pharmacogenomics

A

Genetics: study of genetic basis for variation in drug response
Genomics: use of tools to assess multigenic determinants of drug response

32
Q

Extensive, intermediate, poor, and ultra rapid metabolizers

A

Ex: normal, homozygous for WT CYP450 allele
Int: hetero for WT and variant allele
Poor: homo for variant
Ultra: multiple copies of WT allele

33
Q

Example of variations in CYP450 metabolism

A

~20% Asians are poor 2C19 = no Dilantin b/c inc toxicity and drug intxn risk
7-10% whites poor 2D6

34
Q

Adverse drug reaction categories & dose-response relationship of each

A

Allergic (none), toxic (dose-dep), ideosyncratic (unable to predict, genetically based), alteration of biological or metabolic system

35
Q

Example of ADR by altering biological or metabolic system

A

Alteration of bacterial floor by antibiotics

Inhibition of vitamin absorption or synthesis

36
Q

Drug synergism

A

Use multiple drugs to increase effect vs. increasing dose
Ex: multiple antibiotics or HIV meds
Response: potentiation > summation > individual > antagonism

Pharmacology (4 decks)

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