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35 Cards in this Set

  • Front
  • Back

What is Pharmacokinetics (PK)?

what the human body does to a drug

What is Pharmacodynamics (PD)?

what the drug does to the human body

PK involves

absorption, distribution, metabolism and excretion

PK is used to.. (2)

1. assess drug levels

2. optimize drug therapy

PD refers to

the relationship between the drug concentration at the site of

action and both therapeutic and adverse effects

Absorption of oral drugs occurs via 2 primary processes

1. passive diffusion

2. active transport

If the drug has a poor absorption, one of the methods used

to increase the dissolution rate is to..

reduce particle diameter, which increases surface area


Drugs with poor absorption that are micronized include.. (2)

progesterone and fenofibrate

Which equation described the rate of dissolution?

Noyes-Whitney equation

What is bioavailability?

% of drug absorbed from the extravascular administration (PO)

relative to intravascular administration (IV)

Levofloxacin has what kind of bioavailability?

high; PO and IV doses are the same

Biphosphonates have what kind of bioavailability?

low oral bioavailability

IV: 3mg q 3 mo

PO: 150mg PO q month

Absolute bioavailability (F) equation

F (%) = 100 x (AUC extravascular/AUC iv) x

( DOSE iv / DOSE extravascular)

Factors that favor passage across membranes and greater drug

distribution to the tissues include

1. high lipophilicity

2. low molecular weight

3. unionized status

4. low protein binding

Primary protein responsible for drug binding


What form of the drug is able to interact with receptors and exert

therapeutic or toxic effects

unbound (free) form

Higher % of drug would be in unbound form if it is..

highly protein bound (>90%) and low serum albumin (<3.5 g/dL)

Volume of distribution (Vd) equation

Vd = Amount of drug in the body / Concentration of drug in plasma

Phase I rxns include

oxidation, reduction and hydrolysis

Phase II rxn include

conjugation reactions (ex: glucoronidation)

What are first-pass metabolism reactions?

1. the process of partially or extensively metabolized by the liver

before they reach the systemic circulation

2. the bioavailability of the drug is the reduced

Clearance (Cl) equation

Cl = Rate of elimination / Concentration

Cl = Dose/AUC

Cl = (F x Dose) / AUC

Zero-order elimination

a constant amount of drug is removed per unit of time

First-order elimination

a constant % of drug is removed per unit of time

Michaelis-Menten kinetics (saturable kinetics)

1) begins as first-order kinetics but at higher concentrations the

rate of metabolism approaches maximum capacity

2) any increase in dose leads to a disproportionate increase

in drug concentration at steady state

At concentrations less than Km, the rate of metabolism becomes

first order

At concentrations above the Km, the rate of metabolism becomes

mixed (first and zero order)

At high concentrations relative to Km the rate of metabolism


zero order

Which medications have saturable kinetics?

Phenytoin, Theophylline and Voriconazole

How to dose adjust phenytoin?

in small increments (30-50mg) when the serum concentration is >7mg/L

Elimination rate constant (ke) is..

the fraction of the drug that is eliminated per unit of time

ke equation

ke = Cl / Vd

What is half-life?

the time required for the drug concentration to decrease by 50%

half life equation (t 1/2)

t1/2 = 0.693 / ke

Loading dose concentration

LD = (Desired concentration x Vd) / F