______ molecules are lipid soluble and pass through biologic membranes easiliy
nonionized
_____ drugs are water soluble and must pass through water pores of the biologic membrane or be transported through the membrane by specialized transport mechanisms
ionized
ionized drug movements depend on 3 types of transport?
filtration
passive diffusion
specialized transport mechanism
what are two types of specialized transport mechanisms?
facilitated diffusion
active transport
what is the process where small water soluble substances may pass through aqueous channels or water pores in cell membranes?
filtration
nonionized forms of drugs readily cross biologic membranes along a concentration gradient until equilibrium is reached, this is known as?
passive diffusion
how do large ionized water soluble drug molecules cross the biologic membrane?
specialized transport mechanisms
what process is it when a drug forms a complex with a component of the cell membrane and is carried through the membrane and release?
facilitated diffusion
what process is the movement of drug molecules across biologic membranes against both a concentration and an electrochemical gradient?
active transport
what form of specialized transport requires energy?
active transport
what are the six factors that influence absorption?
degree of ionization
formulation (liquid or solid)
concentration
circulation to area
area of absorptive surface
route of administration
what can delay dissolution of tablets until they have moved from the stomach?
enteric-coated fomrulations
what two ways are routes of administration classified?
enteral
parenteral
what type of drug is placed directly into the GI tract by oral or rectal administration?
enteral
what is the safest, most common and convenient enteral route of administration?
oral
____ _____ _____ may reduce concentration of drug molecules
first pass effect
what is it called when a drug is removed from the liver and has a low bioavailability?
first pass
_____ drugs bypass the GI tract and include various injectable routes
parenteral
what are five examples of parenteral drugs?
intravenous IV
subcutaneous SC
intramuscular IM
inhalation
topical routes
what are two examples of topical routes of parenteral drugs?
sublingual
transdermal patch
what are the 5 features of IV route?
bypasses absorption
most predictable route
used in emergency situations
less safe than oral route
injection site reactions possible
drug distribution is achieved primarily through?
the circulatory system
which organs receive the drug minutes after absorption?
liver
kidney
heart
CNS
what may affect the duration of a drug effect?
redistribution
what are four ways drugs are distributed?
redistribution
plasma protein
blood brain barrier
placenta as barrier
t/f a bound drug to a plasma protein may cross the membrane
false only a free or unbound drug is capable of crossing biologic membranes
where does the majority of metabolism occur?
liver
why does metabolism happen most frequently in the liver?
because it contains the greatest diversity and quantity of metabolic enzymes
phase I and phase II are collectively referred to as what?
biotransfermation
what does biotransformation refer to?
phase I and phase II processes
what four ways can biotransformation alter drugs?
convert an active drug to an inactive drug
convert an active drug to an active or toxic metabolite
convert an inactive drug to an active drug
convert an unexcretable (more lipophilic) drug into an excretable (more hydrophilic) metabolite
during phase I reactions a drugs chemical structure is modified through what?
oxidation, reduction or hydrolysis
what is the most commonly used pathway for phase I reactions
hepatic microsomal cytochrome P450 (CYP450)
during phase II reactions the chemical structure of a drug is modified how?
by conjugation to a large polar endogenous molecule
why is CYP450 induced or inhibited and what is it responsible for?
induced to increase drug metabolism
inhibited to reduce the rate of drugs metabolism
responsible for many adverse drug-drug interactions
what is the most common means to eliminate drug molecules?
renal excretion
what is the most important mechanism of drug elimination from the body?
renal excretion
what two ways does glomerular filtration work?
active tubular secretion
passive tubular secretion
what is the movement of drugs from the bloodstream into renal tubular fluid by a nonselective carrier system?
active tubular secretion
what is it called when drugs need to be retained by the body and the pH of the urine is manipulated?
passive tubular reabsorption
what is it called when metabolites in bile are hydrolyzed and reabsorbed from the gut and the drug action can be reestablished?
enterophepatic recirculation
what is exhalation used for during excretion?
elimination of anesthetic gases and vapors
what is the removal of most drugs from the body follows an exponential or first order kinetics (implies that a constnat fraction of the drug is eliminated per unit of time)
half-life of a drug
what is the plateau level of drug accumulates and involves over four half lives to eliminate the drug?
steady state concentration
how many half lives does it take to eliminate a drug from the body?