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37 Cards in this Set

  • Front
  • Back

Pharmacokinetics

The study of drug movment theoughout the body

Absorption

Process by which a drug moves from its site of administration into the circulatory system

Distribution

Movement of the drug in the blood to the intended site of action

Metabolism

Process by which the body breaks down (metabolizes) and converts (biotransformation) drugs into inactive substances




mainly occurs in the liver

Excretion

the removal of waste substances from body fluids




mainly occurs in the kidneys through one of three processes


Glomular filtration


Tubular secretion


Tubular reabsorption



Half-life

The time it takes for the half of a drug to be eliminated from the blood stream

Drug distribution

The process by which a drug leaves the bloodstream and enters the interstitium of the tissue's cells

Distribution depends on the drug's…

-ability to permeate capillaries


-ability to bind to plasma proteins


-fat or water soluble characteristics


-drug dissolution


-GI tract environment

Blood brain barrier

structure modifications to the brain do not allow ionized molecules to enter the brain




Non-ionized molecules not bound to plasma proteins can enter the brain easily because they are lipid soluble

P450 system

enzymes responsible for the most oxidation reactions of drugs




metabolism occurs in the liver

Biotransformation

change that occurs in a drug's chemical nature (majority occurs in the liver)



Metabolite

new or altered form/version of drug (by-product of metabolism)

Tubular secretion

most drugs filtered out through kidney this way

Tubular reabsorption

some drugs and their metabolites are reabsorbed back into the bloodstream (happens when drug attached to water)

Clearance

rate of elimination of substances from the blood



Renal clearance

total amount of drug excreted over a specific time




all drugs have a published renal clearance rate and is used to determine dosage





Onset of action

the amount of time it takes for a drug to demonstrate a therapeutic response

Peak effect

the time it takes a drug to demonstrate it's full therapeutic effect

Duration of action

the length of time the drug's therapeutic effect lasts



Peak level

the point in time when a drug is at its highest level in the body

Trough level

the point in time when a drug is at it's lowest level in the body

Minimum effective concentration

amount of a drug required to produce a therapeutic effect

Toxic concentraion

level of a drug that will result in serious adverse effects

Therapeutic range

plasma drug concentration between the minimum effective concentration and the toxic concentration




want a wide therapeutic range

Therapeutic range reached by:

repeated dosages of drug




drug accumulation in bloodstream




plateau reached




amount administered = amount eliminated

Loading dose

give patient originally a higher dose to produce therapeutic effects faster, then go by normal dose to maintain this




kick-start to get to the therapeutic range

Median effective dose (ED50)

middle of frequency distribution curve




dose that produces therapeutic response in 50% of group




average or standard dose




many patients require more or less

Potency

a measure of the ability of a set dose of an agonist or antagonist to produce its maximum pharmacological effect




higher potency produces therapeutic effect at a lower dose compared to another drug in same class

Efficacy

ability of a drug to initiate biological effect or stimulate its receptor in a way that produces a pharmacological response after it has bound to a receptor




Magnitude of maximal response that can be produced from a particular drug




more important than potency

Agonist

stimulates a drug's effects, activates cell receptors because resemble naturally occurring hormone or enzyme

Full agonist

an agonist with maximal efficacy (acts with maximal effect)

Partial agonist

an agonist with less than maximum efficacy or one that shows a low degree of activation

Antagonist

blocks a drug's effects, occupy receptor site blocking agonist

Competitive antagonist

drug that competes with an agonist for binding to a receptor




competition can be overcome by flooding receptor site with concentration of agonists

Noncompetitive antagonist

drug that binds to a receptor and stays bound




can't be displaced by increasing concentration of agonists

Selective drugs

have a preference for acting at certain binding sites or receptors




desirable because it results in the drug having less side effects

Nonselective drugs

affect all adrenoreceptors, regardless of whether they are alpha or beta receptors