General Principles of Pharmacology Flashcards Preview

RENAL II Exam 1 > General Principles of Pharmacology > Flashcards

Flashcards in General Principles of Pharmacology Deck (54):
1

pharmacology

study of actions, effects, and disposition of drugs in body

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drug

chemical
-agent used in treatment of prevention of disease or pregnancy

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pharmacodynamics

study of drugs and their mechanism of action

what drugs do**

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pharmacokinetis

time course of drug and metabolite concentration in plasma, tissue, urine

what body does to drugs

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drug fate

study of what body does to drugs

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pharmacotherapeutics

clinical pharmacology

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drug action

biochemical event at molecular level

effect on macromolecules

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drug effect

effect of drug on body
-change in physiological function

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MEC

minimum effective concentration producing therapeutic effect

-threshold concentration in plasma or other tissue compartment

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therapeutic window

range of plasma drug concentration where therapeutic effect occurs

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local, percutaneous

drug absorption through skin
-slow, sustained systemic absorption
-patches, creams, etc.
-lipid soluble drugs

other local - eyedrops, nasal sprays

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enteral

via GI tract

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sublingual

rapid absorption
-but unpleasant taste

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oral

most common used route
-barriers - epithelial cells and capillary wall
-variable absorption
-safe - can recall drug - lavage or vomiting

first pass metabolism by liver occurs

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rectal

when oral not possible
-vomiting patient

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parenteral

non-oral route
-IV
-intraarterial injection
-subQ
-IM
-perQ -patches
-intranasal
-inhalation

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intrathecal

into sheath around brain or spinal cord

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intraperitoneal

into body cavity

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intraarticular

into joint space

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epidural

for regional anesthesia

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absorption of drug

from site of admin to blood
rate - how soon effects begin
extent - how intense effects will be

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drug dissolution

faster dissolving time - faster onset of drug

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smaller size

faster it dissolves

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liquid drug form

faster dissolution

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driving force of drug diffusion

concentration gradient

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lung and small intestine

larger surface area
-more drug absorption

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more lipid soluble drug

absorbed more rapidly

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ionized drugs

charged
-cannot diffuse across hydrophobic membrane barrier

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Vd

volume into which drug is distributed

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plasma compartment

Vd - 4L
-drugs that are large and bound to plasma proteins

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extracellular fluid compartment

Vd - plasma water and interstitial fluid
-14L

drug small enough to pass endothelial slit junctions but very hydrophilic (won't diffuse to cells)

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total body water

small enough to cross into interstitium and hydrophobic enough to diffuse through plasma membrane into intracellular space

Vd - 42L

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redistribution

after dose of drug absorbed, concentration in blood falls
-at this point drug will move back out of tissue into blood
-following concentration gradient

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blood brain barrier

endothelial cells in CNS with tight junctions with no fenestrations
-lipid soluble diffuse to bran rapidly
-water soluble - more restricted

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biotransformation

drug to metabolites

major site - liver

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conjugation

add sugar, amino acid, or other residue to make drug larger and more water soluble

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free drug

unbound in solution

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concentration of free drug depends on

ADBE
-absorption
-distribution
-biotransformation
-excretion

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passive diffusion

function of lipid solubility, degree of ionization, concentration, molecular size

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rate of diffusion

directly varied with concentration gradient

rate = kD
-k = rate constant
-D = drug concentration

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lipid:water partition coefficient

means of expressing drugs solubility in lipid versus water

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weak acid at low pH

more unionized form
-more enters cells

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weak base at low pH

more ionized form
-less enters cell

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excretion of weak acids

in basic urine

more ionized form

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excretion of weak bases

in acid urine

more ionized form

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at equilibrium

relative concentration of nonionized drug is same in all compartments

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quaternary salts

permanently charged
-highly water soluble
-poorly absorbed
-rapid urine excretion

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active transport

nonspecific
-important for passage of anions and cations across renal tubules, choroid plexus, and hepatocytes

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diffuse across membranes

only free drug
-not bound to plasma proteins

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albumin

principal binding protein in plasma

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streptokinase

binding sites must be saturated with loading dose to achieve therapeutic concentrations

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plasma protein binding

elimination half time may be prolonged

glomerular filtration and renal excretion affected

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drug interactions

may result from displacement of drugs competing for binding sites

significant interactions when bound in quantity, limited Vd, slow elimination, low therapeutic index

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thiopental

rapid onset and offset

high lipid solubility
large CO to brain
absorbed by brain on first pass
concentration falls rapidly creating steep concentration gradient leading to rapid offset