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Naplex 2023 > Pharmacokinetics > Flashcards

Pharmacokinetics Flashcards

1
Q

pharmacokinetics

A

what body does to drug
ADME

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2
Q

pharmacodynamics

A

what drug does to human body

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3
Q

drug absorption oral

A

oral
stomach
small intestine
through hepatic portal vein
liver
part recycles from liver to small intestine
part goes liver to systemic circulation

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4
Q

passive diffusion

A

high to low concentration (i.e. gut lumen to blood)

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5
Q

active transport

A

drugs moved across gut wall by transporter proteins
normally used for nutrients from food

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6
Q

disintegration

A

solid dosage form breaks into smaller pieces in GI tract

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7
Q

disolution

A

small pieces dissolve and release active ingredient
required for drug absorption

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8
Q

fastest to slowest rate of absorption

A

IV
SL
ODT
IR tablet
ER tablet

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9
Q

primary way IR formulations get destroyed in gut

A

hydrolysis

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10
Q

prevents drug degradation in stomach

A

enteric coating

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11
Q

micronized

A

drugs with very small particle diameters to increase dissolution rate by reducing particle diameter to increase surface area

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12
Q

solubility

A

how well drugs dissolve in GI fluids
typically lower for lipophilic

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13
Q

bioavailability

A

extent of drug absorption into systemic circulation
percentage of drug absorbed from extravascular compared to intravascular administration (oral vs IV)
high = >70% (levofloxacin, linezolid)
low = <10%
F x Dose = Cl x AUC

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14
Q

AUC

A

shows bioavailability
100 x (AUC extravasc/AUC intravasc) x (dose IV/dose extravasc)

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15
Q

dose of new dosage form

A

= amount absorbed from current dosage form / F of new dosage form

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16
Q

distribution

A

drug molecules move from systemic circulation to various tissues and organs
higher with high lipophilicity, low molecular weight, unionized status and low protein binding

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17
Q

albumin

A

main protein responsible for drug binding

18
Q

unbound/free drug

A

exerts therapeutic/toxic effects

19
Q

affect of low serum albumin and high protein-bound drug

A

more drug will be in unbound form than intended = higher therapeutic/toxic effects

20
Q

highly protein bound compounds examples

A

phenytoin
calcium
need correction formulas for hypoalbuminemia
do not need corrections if “free phenytoin” or “ionized calcium” reported

21
Q

calcium correction formula

A

serum Ca + [(4-albumin) x 0.8]
reports mg/dL

22
Q

phenytoin correction formula

A

serum phenytoin / [(0.2 x albumin) + 0.1]
reports mcg/mL

23
Q

volume of distribution

A

amount of drug in body / concentration of drug in plasma = dose / serum concentration

24
Q

metabolism

A

drug is converted to facilitate elimination

25
Q

primary sites for drug metabolism

A

gut
liver

26
Q

first-pass metabolism

A

metabolism of drug before it gets.to systemic circulation
reduces bioavailability of oral formulations
Phase 1 reactions (oxidation, reduction, hydrolysis - such as adding hydroxyl group to make drug more hydrophilic) then Phase 2 reactions (conjugation)

27
Q

drugs with high first-pass metabolism

A

lidocaine - cannot be given orally on IV

28
Q

excretion

A

removal of drugs from body

29
Q

pH affect on excretion

A

weak base - acidic urine increases excretion
weak acid - alkaline urine increases excretion

30
Q

clearance

A

rate of elimination / drug concentration = (drug eliminated / how many hours to eliminate) / plasma concentration
efficiency of drug removal from body

31
Q

most reliable measurement of drug’s bioavailability

A

AUC

32
Q

first-order kinetics

A

constant percentage of drug is removed per unit of time
most drugs follow this

33
Q

zero-order kinetics

A

a set of amount (mg) of drug removed per unit time

34
Q

Michael-Mentin Kinetic /non-linear/saturable

A

enzymes for metabolism get saturated
follows first-order at very low concentration
at high concentrations, approach zero-order = inc dose causes disproportionate increase i
n drug concentration

35
Q

drugs that follow Michael-Mentin Kinetics

A

phenytoin, theophylline, voriconazole
doses should be inc in small increments

36
Q

eliminatio rate constant (ke)

A

fraction of drug liminated per unit of time
ke = Cl/Vd = how much of drug remaining is cleared per hour (ke = 0.1 hr means 10% of drug is cleared every hour

37
Q

predicting drug concentration

A

C2 = C1 x e^(-ke x t)

38
Q

half-life

A

time for drug concentration to dec by 50%
t 1/2 = 0.693/ke

39
Q

steady state

A

where drug intake equals drug eliminatino
5 half-lives required to eliminate >95% or drug

40
Q

loading dose

A

rapidly achieves therapeutic concentration of drug
= [(desired concentration) x Vd] / F

Naplex 2023 (21 decks)

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