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601 EXAM 2 > 3.14/3.15 Pharmacokinetics II > Flashcards

3.14/3.15 Pharmacokinetics II Flashcards

1
Q

what are things that can influence absorption?

A
  • molecular size
    solubility
    degree of ionization
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2
Q

large Ka = _____ acid because?

A

strong, bc it largely dissociates

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3
Q

lower pH relative to pKa = greater fraction of ______

A

drug in protonated form

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4
Q

factors that affect distribution of drugs

A

-rate of blood flow
- concentration gradient
- ability to exit vascular system
- ability to penetrate tissue

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5
Q

4 sites of drug concentration

A
  1. fat (lipid soluble drugs)
  2. tissue
  3. bone (tetracyclines)
  4. trans-cellular reservoirs (GI)
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6
Q

An active drug is a ______ drug

A

free

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7
Q

_____ is the minimum concentration required for drug effect

A

MEC

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8
Q

__________ is the minimum concentration at which toxicity usually occurs

A

MTC

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9
Q

biotransformation happens in the _____

A

liver

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10
Q

what is the equation for TW?

A

TW = MTC/MEC

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11
Q

factors that determine intensity of drug response

A

diet, co-morbitiy, age, weight, drug-drug interaction, genetics

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12
Q

what things influence metabolism?

A

Phase 1 reactions, Phase 2 reactions, genetic factors, induction of drug metabolism, inhibition of drug metabolism

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13
Q

_________ is oxidation, reduction, hydrolysis of a drug

A

phase 1 biotransformation

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14
Q

oxidative processes usually involve what kind of enzymes?

A

cytochrome P450 system

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15
Q

_____________ consists of synthesis reactions where something is added to molecule

A

Phase 2 Biotransformation:

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16
Q

_______ makes drugs more water soluble and more excretable

A

Conjugation

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17
Q

__________ makes drugs less water soluble and inactivates drug

A

Acetylation/methylation

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18
Q

what are cytochrome P450 enzymes?

A

family of super enzymes pivotal in metabolism of drugs/chemicals

19
Q

where are Cytochrome P450 enzymes found?

A

Smooth ER

20
Q

what do Inducers do?

A
  • increase enzyme levels
  • speed up metabolism
  • lower plasma levels below MEC
  • can be drugs or environmental pollutants
21
Q

what do inhibitors do?

A
  • slow metabolism
  • can cause drugs to accumulate at toxic levels
  • can be drugs, foods, chemicals
  • decreases enzyme activity
    EX: grapefruit = inhibitor of cytochrome P450 CYP3A4
22
Q

factors that affect drug bioavailability

A

first pass effect, drug-drug interaction

23
Q

3 types of drug-drug interaciton

A

additive, synergism, potentiation

24
Q

3 routes of drug excretion

A

renal, non-renal, ion-trapping

25
Q

___________ is the time required to change the amount of drug in the body by one half during elimination

A

half life

26
Q

equation for half life

A

t1/2 = (0.7 x Vd)/CL

27
Q

_________ is the removal of drug from systemic circulation

A

Clearance

28
Q

clearance equations (3 of them)

A

CL = (rate of removal of drug)/(plasma concentration of drug)
CL = dose/ AUC
CL = (.7 x Vd)/ t1/2

29
Q

what happens after 4-5 half lives

A

plasma concentrations of a given drug will be below a clinically relevant concentration and thus will be considered eliminated.

30
Q

______ is a constant fraction of drug metabolized per unit of time (most drugs)

A

First order kinetics
(straight log graph)

31
Q

__________ is a constant amount of drug is metabolized per unit of time (ethanol/phenytoin)

A

Zero order kinetics
curved line on log graph

32
Q

what does the 2 compartment model show?

A

drug can be exchanged between extravascular volume, blood or excreted

33
Q

A ______ is an initial higher dose of a drug that may be given at the beginning of a course of treatment before dropping down to a maintenance dose. useful for drugs that are eliminated from the body relatively slowly (have a long systemic half-life)

A

Loading dose

34
Q

loading dose equation

A

LD = (Vd x Desired plasma concentration) / Bioavailabilty

35
Q

A ______ is when drug levels are maintained above the MEC to maintain a steady state of drug in the body

A

Maintenance dose

36
Q

equation for Maintenance dose

A

MD = (dosing rate) x (dosing interval)

37
Q

what are the 5 factors that influence elimination

A

pH dependent ionization (ion trapping)
competition for tubular transport
age
disease
drug interactions

38
Q

weak acids/bases can only cross membrane in _______ form

A

unionized

39
Q

_________ relates amount of drug in body to plasma concentration

A

Apparent volume distribution (Vd)

40
Q

larger Vd means what?

A

more likely to leave plasma and enter extravascular compartments of body

41
Q

_______ is the fraction (F) of drug that reaches systemic circulation

A

Bioavailability

42
Q

bioavailability equation

A

F = (amt reaching systemic circulation)/(amt administered)

43
Q

_______ makes drugs more water soluble and more excretable

A

Conjugation

601 EXAM 2 (11 decks)

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