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Foundations1 > Pharmacology > Flashcards

Pharmacology Flashcards

0
Q

Graded dose response curve

A

Y- effect
X- drug concentration
EC50- concentration at 50% effect

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1
Q

ligand receptor binding curve

A

Y- DR bound
X- Drug concentration
Kd = concentration at 50% binding

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2
Q

Quantal dose response curve

A

Y- % individual responding
X- dose
graph ED50, TD50, LD50

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3
Q

Therapeutic index

A

=TD50/ED50 (bigger is better)

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4
Q

Margin of safety

A

LD1/ED99 (bigger is better)

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5
Q

Receptor effector coupling

A

transduction process between binding and effect (full–>partial–>antagonist)

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6
Q

Categorize competitive vs noncompetitive antagonists

A

Allosteric (reversible/irreversible) = noncompetitive
Active (orthosteric) irreversible = noncompetitive
Active reversible = competitive

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7
Q

Effect of competitive antagonist on agonist

A

decrease potency

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8
Q

Effect of noncompetitive antagonist on agonist

A

Decreased efficacy

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9
Q

noncompetitive antagonist effect on agonist WITH spare receptors

A

first as competitive (decrease potency)

then act as noncompetitive (decrease efficacy)

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10
Q

Why allosteric ligand drugs are cool.

A
  1. ceiling effect(limit with all sites bound)
  2. selective for tissue with endogenous active
  3. subtype selectivity (more varietytoo)
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11
Q

tachyphylaxis

A

repeat same dose–> decreased effect

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12
Q

Desensitization:

A

decreased receptor ability to response (homologous vs heterologous)

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13
Q

Inactivation:

A

loss of receptor ability to respond

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14
Q

downregulation

A

receptor removal from repeated stim

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15
Q

What is therapeutic window?

A

between MEC (minimal effective concentration) for desired response to MEC for adverse

16
Q

How does pH change affect drug absorpption?

A

Decrease pH –> more protonated acids and charged bases –> charged doesnt diffuse
Henderson hasselbalch

17
Q

What is bioavailability?

A

% of oral drug that actually reaches systemic circulation (not lost before absorption or in liver or junked up in stomach)

is the total plasma of drug over time [AUC oral]/[AUC injected]

18
Q

What 3 factors impact drug distribution?

A
  1. blood flow to tissue
  2. capillary permeability at tissue
  3. binding of drug to tissues (drug reservoir)
19
Q

2 compartment model of IV drug distribution

A
  • alpha phase (fast): drug distribution to tissue (half-life 1.2 hours)
  • beta phase (slow): drug metab and excretion (half-life 30 hours)
20
Q

What is the volume of distribution?

A

Vd = [drug taken]/[drug concentration in plasma]

suggests where drug is disributed

21
Q

Metabolism usually makes drug more soluble or more insoluble?

A

more soluble

22
Q

What is phase I metabolism? Main enzyme invovled?

A 
oxidation, hydroxylation, dealkylation, deamination
cytochrome 450 (CYP)
23
Q

What is phase II metabolism?

A

Add group (conjugation); makes compound more polar

24
Q

Zero vs first order kinetics of drug elimination

A

First order: rate of elimination is roportional to drug concentration
Zero order: rate of elim is independent (constant) (usu at saturation)

25
Q

Calculating half life

A

T(1/2) = 0.7Vd/CL

37
Q

Which CYP metabolizes almost 1/2 drugs?

A

CYP3A

38
Q

Which CYPs have a lot of polymorphisms?

A

CYP2C and CYP2A6

39
Q

What is enterohepatic recirculation?

A

when drugs in bile is reabsorbed in small intestine (instead of excreted)

40
Q

What genes are involved in warfarin?

A

CYP2C9 and VKORC1

41
Q

antipsychotics, antidepressants, metoprolol, tamoxifen

are metabolized by what cyp?

A

CYP2D6

42
Q

poor, intermediate, efficient, and ultrarapid metabolizers

-variance due to what cyp?

A

CYP2D6; ultrarapid is usu *2xn –> GOF

43
Q

TPMT

A

Phase 2; methylation inactivation of thiopurines

44
Q

Mercaptopurine and azathioprine (drugs0 are affected by which enzye gene?

A

TPMT; they are thiopurines and treat leukemia, IBS, RA, transplant immune supression; normally they are high activity ((ut sme are low activity)

45
Q

Why does FDA recommend testing prior to azathioprine admin?

A

Some people have lower activity TPMT –> leukopenia (low WBC count)

Foundations1 (14 decks)

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