Pharmacokinetics Absorption/Distribution Flashcards

1
Q

Pharmacokinetics relationship between what 2 things?

A

dose-concentration

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2
Q

Biophase (PK-PD link) reflects what relationship?

A

plasma-effect site

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3
Q

Pharmacodynamics reflects what relationship?

A

concentration-effect

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4
Q

What does ADME stand for?

A

Absorption, Distribution, Metabolism, Excretion

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5
Q

Simply define pharmacokinetics.

A

what the body does to a drug.

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6
Q

Name 4 drug properties that affect absorption.

A

size, shape, degree of ionization(acidic/alkaline), lipid solubility

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7
Q

What conditions at the site affect absorption?

A

blood flow, surface area, membrane thickness, presence of other substances, metabolism (1st pass hepatic metabolism), GI motility, pH

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8
Q

The rate of diffusion is directly proportional to what?

A

concentration gradient, surface area

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9
Q

The rate of diffusion is inversely proportional to what?

A

membrane thickness

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10
Q

What’s Fick’s Law of Diffusion equation?

A

Rate of diffusion= conc. grad. * SA * Diffusion Coef / membrane thicknss

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11
Q

Define Bioavailability.

A

Fraction of unchanged drug that reaches the systemic circulation following administration by any route

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12
Q

Where is the principle route of absorption for oral route?

A

largest surface area of the small intestine

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13
Q

Name 4 medications highly susceptible to first pass hepatic metabolism.

A

Aspirin, levadopa, metoprolol, morphine

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14
Q

What common medication is hydrolyzed in the stomach?

A

penicillin

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15
Q

True/False: Transmucosal meds (SL/buccal/intranasal) are subject to 1st pass hepatic effect.

A

False

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16
Q

What percentage of body weight does water make up in men? women? infants?

A

60% men; 50% women; 70% infants

17
Q

How many L is total body water?

A

42L

18
Q

How many L of fluid is intracellular? Extracellular?

A

28L, 14L

19
Q

What % of CO is central compartment?

A

75%, peripheral comp. 25%

20
Q

What % of weight is central compartment

A

10%, peripheral comp. 90%

21
Q

Define Vd and it’s equation.

A

Vd relates the amount of drug given to plasma concentration. Vd=amount of drug/desired plasma conc.

22
Q

True/False: Small plasma concentration=large Vd.

A

True.

23
Q

What kind of drugs have large Vd?

A

Lipid soluble drugs, lipophilic. Needs larger dose for effect. Propofol

24
Q

What kind of drugs have low Vd?

A

hydrophilic drugs, highly water soluble, higher plasma concentrations. Neuromuscular blocking drugs

25
Q

True/False: Aqueous Diffusion involves lipophilic substances.

A

False, Hydrophilic substances. Driven by a concentration gradient, small molecular weight, assisted by osmotic or hydrostatic pressure.

26
Q

True/False: Lipid Diffusion is most pertinent to anesthesia.

A

True. Lipid soluble drugs, cross phospholipid bilayers based on conc. gradient to aqueous side.

27
Q

True/False: acidic drugs bind to alpha1-acid glycoprotein.

A

False. Acidic (thiopental) bind to albumin. Basic drugs (local anesthetics) bind to alpha1-acid glycoprotein.

28
Q

Name things that decrease albumin thereby increasing amount of free drug in the body.

A

renal disease, liver disease, old age, malnutrition, 3rd trimester

29
Q

What causes increased alpha1-acid glycoprotein (AAG) binding?

A

surgical stress, MI, chronic pain, RA, old age.

30
Q

What causes decreased (AAG) binding?

A

Neonates, 3rd trimester

31
Q

Vd of a drug is directly/inversely proportional to a drug?

A

inversely, but only when just looking at protein binding, there are many other factors.

32
Q

A drug changes from 98% protein bound to 94% protein bound, by what percentage has the amount of free fraction increased?

A

started with 2% unbound to 6% unbound, amount doubles twice, increases 200%. In highly protein bound drugs small changes can make a big difference

33
Q

Which are more lipid soluble? ionized or non-ionized?

A

non-ionized are 1000-10000 times more lipid soluble and rapidly diffuse across cell membranes. larger Vd.

34
Q

Ionized molecules are hydrophilic/lipophilic?

A

hydrophilic, doesn’t cross membranes

35
Q

True/False: non-ionized molecules are negatively charged?

A

False, neutral charge.

36
Q

What is the order of routes of administration from fastest to slowest to reach peak plasma concentration?

A

IV, tracheal, intercostal, caudal, paracervical, epidural, brachial plexus, sciatic/subarachnoid, subcutaneous.
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