Pharmacokinetics & pharmacodynamics Flashcards

1
Q

Km=

A

1/affinity

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2
Q

Vmax is ______ proportional to _____?

A

directly, enzyme concentration

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3
Q

Lineweaver burk plot: the closer the line is to X axis:___?

A

The higher the Km (lower the affinity)

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4
Q

What is the bioavailability for IV dose

A

F=100%

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5
Q

What is the bioavailability for an oral dose

A

F

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6
Q

Volume of distribution=

A

amount of drug in body/plasma drug concentration

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7
Q

High volume of distribution

A
All tissues (including fat)
Small lipophilic molecules, esp if bound to tissue protein
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8
Q

Medium volume of distribution

A

ECF

Small hydrophilic molecules

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9
Q

Low volume of distribution

A

Blood

Large/charged molecules, plasma protein bound

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10
Q

Clearance=

A

rate of elimination of drug/plasma drug concentration

=Volume of distribution*elimination constant

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11
Q

How many half lives does it take to reach steady state?

A

4-5 half lives

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12
Q

How many half lives does it take to reach 90% of the steady-state level?

A

3.3

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13
Q

T1/2=

A

(.693*Vol. of distribution)/Clearance

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14
Q

Loading dose=

A

(Target plasma concentration at steady state*Vol.ofDis)/Bioavailability

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15
Q

Maintenance dose=

A

(Target plasma concentration at steady stateClearancedosage internal)/bioavailability

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16
Q

Do you change loading dose or maintenance dose with kidney/liver disease?

A

Decrease maintenance dose

loading dose is unchanged

17
Q

Drugs that are zero order elimination

A

PEA: Phenytoin, ethanol, aspirin

18
Q

What state do you want a drug to be to “trap” it in the urine?

A

Ionized state (can’t be reabsorbed)

19
Q

Example of a weak base

A

Amphetamines

20
Q

Example of a weak acid

A

Phenobarbital, methotrexate, aspirin, TCAs

21
Q

How do you treat a weak acid overdose?

A

Bicarbonate

22
Q

How do you treat a weak base overdose?

A

Ammonium chloride

23
Q

Phase 1 of metabolism

A

Reduction and oxidation

p450

24
Q

Phase 2 of metabolism

A

Conjugation: glucuronidation, acetylation, sulfation

25
Q

How does the speed of conjugation (phase 2) affect side effects?

A

The fast the conjugation, the less the side effects

26
Q

Geriatric patients lose which drug metabolism phase first?

A

Phase I

27
Q

Diazepam+Flumazenil: Receptor types, and effect when combined

A

Diazepam (GABA agonist) + Flumazenil (GABA competitive antagonist
Flumazenil decreases potency

28
Q

NE+ phenoxybenzamine: Receptor types, and effect when combined

A

NE (a agonist) + phenoxybenzamine (a nonceompetitive antagonist)
Phenoxybenzame decreases efficacy

29
Q

Morphine + buprenorphine

A

Morphine (u agonist) + Buprenorphine (u partial agonist)

Buprenorphine decreases efficacy, potency is independent