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Flashcards in Pharmacology Deck (293)
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1

Pramlintide

Amylin analog. MOA = decrease gastric emptying and decrease glucagon. Used for type 1 + type 2 DM.

2

Dopamine MOA

At low doses stimulates D1 receptors in the renal vasculature and tubules, thereby increasing GFR, RBF, and sodium excretion. Big heart in middle of room + normal sized christian is squeezing it/at high doses stimulates beta-1 adrenergic receptors in the heart, thereby increasing cardiac contractility + pulse pressure + systolic BP. Huge air force one plane by the left that monster Christian is driving/at highest doses stimulates alpha-1 receptors in the systemic vasculature.

3

Why do you give dopamine for shock?

To stimulate a1 receptors in the systemic vasculature, causing vasoconstriction.

4

Amiloride vs. amiodarone vs.

Amiloride --> K+ sparing diuretic.
amiodarone --> K channel blocker
amlodipine --> Ca channel blocker

5

Ergotamine

o Code: Elisabeth with Erik backpack/ergotamine. Smoking a huge blunt + walking out of air force one/MOA = partial agonist/antagonist activity at tryptaminergic + dopaminergic + alpha-adrenergic receptors. Feet and arms are gangrenous/SE’s = peripheral vascular ischemia + potentially gangrene.
o Location: /usually used for migraines.

6

How can morphine therapy lead to toxicity?

Morphine is metabolized to active metabolites that accumulate and can cause CNS depression.

7

Drugs contraindicated in CHF

Diltiazem and verapamil.

8

Hydralazine MOA

Smooth muscle relaxant and vasodilator in arteries and arterioles. Exact mechanism unclear.

9

Phenoxybenzamine MOA

Non-selective irreversible alpha blocker

10

labetalol MOA

Mixed alpha/beta adrenergic antagonist

11

What is Vmax proportional to?

Enzyme concentration

12

Relationship of Km to Vmax

Km is enzyme saturation at 1/2Vmax

13

competitive inhibitor vs. noncompetitive inhibitor

FA 236

14

What does a change in y-intercept on Lineweaver-Burk plot indicate?

Increased y-intercept = decreased Vmax since y-axis is the reciprocal of Vmax

15

What does x-intercept represent on lineweaver-Burk plot?

The further to the right (i.e. the closer to zero), the greater the Km and the lower the affinity since x-axis is reciprocal of negative Km.

16

What is slope on Lineweaver-Burk plot?

Km/Vmax

17

How do you differentiate competitive inhibitors from noncompetitive on Lineweaver-Burk plot?

Reversible competitive inhibitors cross each other competitively, whereas noncompetitive inhibitors do not.

18

Competitive inhibitors, reversible
1) resemble substrate?
2) overcome by increased saturation?
3) bind active site?
4) effect on Vmax?
5) effect on Km?
6) potency? efficacy?

1) Yes
2) Yes
3) Yes
4) Unchanged
5) Increased
6) Decreased potency

19

Competitive inhibitors, IRREVERSIBLE
1) resemble substrate?
2) overcome by increased saturation?
3) bind active site?
4) effect on Vmax?
5) effect on Km?
6) potency? efficacy?

1) Yes
2) No
3) Yes
4) Decreased
5) Unchanged
6) Decreased efficacy

20

NONcompetitive inhibitors
1) resemble substrate?
2) overcome by increased saturation?
3) bind active site?
4) effect on Vmax?
5) effect on Km?
6) potency? efficacy?

1) No
2) No
3) No
4) Decreased
5) Unchanged
6) Decreased efficacy

21

What is bioavailability?

Fraction of administered drug reaching systemic circulation unchanged

22

bioavailability of IV dose of drug

100%

23

Why is bioavailability usually less than 100%

Incomplete absorption + first pass metabolism

24

How do liver and kidney disease affect Vd?

Decreased protein binding leads to increased volume of distribution.

25

Drugs that stick to blood compartment characteristics...

Large/charged molecules; plasma protein bound

26

Relative Vd of ECF, tissue, Blood compartments

Blood = low
ECF = medium
All tissues including fat = high

27

Characteristics of drugs that stay in ECF compartment?

Small hydrophilic molecules

28

Characteristics of drugs that stay in fat/tissue compartment?

Small lipophilic molecules, especially if bound to tissue protein.

29

Steady state in a drug with first-order kinetics?

Takes 4-5 lives to reach steady state and 3.3 half lives to reach 90% of steady-state.

30

What happens to maintenance and loading dose with renal or liver disease?

You need need to decrease maintenance dose. Loading dose is usually unchanged.