Lec 6

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pharmacokinetics

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Lecture 6

44 Terms

1

pharmacokinetics

deals with the drug disposition; “what the body does to the drug”

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2

absorption, distribution, biotransformation, excretion

bodily processes involved in drug disposition which influence drug levels in the body

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3

enteral & parenteral

routes of drug administration

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4

enteral

route of DA that initiate orally or rectally

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5

parenteral

non-oral routes

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6

absorption

passage of drug molecules from the site of administration into the blood circulation

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7

systemic & local

types of drug effect

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8

systemic

effect that occurs when a drug is absorbed into the blood circulation

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9

local

effect that is not preceded by absorption

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10

small intestine

usual site of absorption for orally administered medications

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11

TRUE

T or F.

Absorption may begin in the mouth and stomach for some drugs

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12

dissolution rate of drug

rate-limiting factor in absorption from the gut

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13

rate of injection or infusion

rate-limiting factor in absorption from IV injections

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14

blood flow

rate-limiting factor in absorption from all other routes

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15

TRUE

T or F.

The sublingual route is both enteral and parenteral.

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16

passive diffusion

it is the most important mechanism for passage of drugs; it requires the establishment of a concentration gradient across the membrane

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17

small in size, lipophilic, non-ionized/nonpolar

characteristics of a drug in order for it to move through the cell membrane by passive diffusion

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18

TRUE

T or F.

Aside from passive diffusion, a drug can also be transported across cell membrane via carrier mediated transport and pinocytosis.

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19

bioavailability

a measure of how much drug is absorbed into the blood circulation; expressed as percent of the dose administered

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20

50%

If 100 mg of a drug is administered orally and only 50 mg of the drug is absorbed unchanged, the bioavailability is:

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21

minimum effective concentration (MEC)

minimum level of a drug that should be attained in the plasma in order to induce an effect

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22

FALSE. there is none

T or F.

There is still slight pharmacological effect produced below MEC.

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23

pharmaceutical, physiological, physicochemical

factors affecting GIT absorption

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24

incorporation of excipients, micronization/nanonization

pharmaceutical factors that affect the dissolution of dosage forms

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25

micronization or nanonization

process of reducing particle size to improve the rate of drug dissolution, thus resulting in greater GIT absorption of the drug

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26

solution > suspension > capsule > tablet

arrange the following dosage forms based on their availability to be absorbed:

suspension, tablet, capsule, solution

Answer this way:

suspension > tablet > capsule > solution

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27

length of GIT, presence of food in the stomach, GIT pH

physiologic factors that affect the transit time of drug along the GIT

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28

TRUE

T or F.

Ruminants have more alkaline pH in the GIT while carnivores have more acdic pH in the GIT

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29

drug solubility, the degree of ionization of a drug

physicochemical factors affecting the absorption of drugs in the GIT

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30

oil/water partition coefficient

ration of drug solubility in oil to its solubility in water; reflects the lipid solubility of a drug

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31

FALSE

T or F.

high oil/water partition coefficient means that the drug is less lipid soluble, and thus has lower absorbability

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32

TRUE

T or F.

A drug tends to pass thru the membrane if it is uncharged.

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33

FALSE

T or F.

Uncharged drugs are less lipid-soluble than charged drugs.

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34

TRUE

T or F.

The degree of ionization of a drug is related to its acidic or basic properties.

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35

TRUE

T or F.

Drugs are mostly weak acids or weak bases.

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36

drug pH, pH of the medium, dissociation constant (pK)

factors affecting the degree of ionization

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37

TRUE

T or F.

When a weak acid reacts in an acidic environment, it becomes lipophilic which is more absorbable in the body.

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38

FALSE

T or F.

When a weak base reacts in an acidic environment, it transforms into a lipophilic form.

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39

intestine

Weak bases are best absorbed from the ___

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40

Weak acids

They are best absorbed from the stomach

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41

TRUE

T or F.

The lower the pK, the stronger the weak acid.

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42

FALSE

T or F.

The higher the pK, the stronger the weak acid.

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43

Henderson-Hasselbach equation

demonstrates the effect of drug pH, drug pKa, and the pH of the medium on the degree of drug ionization

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44

pH = pK + log [A-]/[HA]

Henderson-Hasselbach equation

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