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Pharm Vocabulary

NURS 430 Vocab List 1

Potency The drug dose needed to produce a given effect - usually 50% of maximum
Efficacy The goal dose for response. Usually refers to maximal effect.
The potency or efficacy can be quantifed as the quantal response or the number of patients who respond to a drug
Therapeutic index is another name for safety
Therapeutic Index is the relationship between the toxic dose and the effective dose.
Equation for Therapeutic Index Toxic Dose over Effective Dose or TD50/ED50
ED50 is the potency
the graded dose response relationship is the drug receptor complex that results in biological effect
the magnitude of the biological effect is proportional to the number of receptors occupied
affinity is the strength of binding between the drug and its receptor
an agonist is something that binds and activates a recptor
an antagonist is something that binds and prevents receptor activity
full agonist is something that activates the receptor to full extend and mimics endogenous
partial agonist is something that causes a less than full response despite receptor saturation
partial agonists can result in antagonism
an inverse agonist is something that results in reverse activity of receptors and stabilize receptors in an inactive format
a competitive antagonist competes with agonist for receptor - like narcan and morphine
irreversible antagonist binds covalently to receptor and inactivates it - blocking the amount of receptors available
allosteric antagonist prevents receptor transformation when drug binds to a site that is different than an agonist site.
allosteric agonist example benzos bind to ion channels activated by GABA and enhance effects of GABA
chemical agonist drug binds directly to substance so substance cant interact with receptor ex. iron chelators
small therapeutic index monitor more frequently because less safe
threshold for a toxic therapeutic index 2.0
pharmakokinetics is the actions of the body on the drug; absorption, distribution, metabolism and excretion of the drug in the body
first order kinetics is the same as first order elimination
first order elimination is enxymes that metabolize a drug for elimination that do not become saturated so the rate of elimination is directly proportional to the concentration of free drug
zero order kinetics is the enzyme system is saturated so rate of metabolism is constant - regardless of drug concentration. it is not affected by the rate of concentration
first pass metabolism is when a drug is administered orally and visits the liver via the bloodstream and is metabolized before going to the organ of disease
lipophillic drugs not excreted but their hydrophilic metabolites are excreted
hydrophilic drugs leads to increased renal excretion and decreased tubular reabsorption
bioavailability is determination of equivalence - the percent of drug that reaches systemic circulation, calculated by plasma level - effective dose/bioavailability. IV dose is 100% bioavailable, oral is 70% bioav.
factors that influence bioavailability first pass metabolism, solubility of drug, chemical instability, physical properties of drug
most drugs are secreted by passive diffusion
antibiotics are brought into bacteria by endocytosis
drug distribution is when a drug reversibly leaves the bloodstream and enters the interstitium and tissues/cells
when plasma proteins are lower than normal then total drug concentrations will be lower but unbound concentration will not be affected
a large volume of distribution is associated with low excretion/long half life
metabolism is the termination of drug action and has three portions - bioinactivation, detoxification and elimination
biotransformation is metabolism. both occur in the liver
most liver metabolism converts meds to more polar, less lipophilic compounds that can be eliminated by kidneys
biotransformation occurs in two phases phase 1 results in oxidation, reduction and hydrolysis, phase two results in conjugation products and are inactive
An example of a phase 1 drug metabolism is the CYP 450 system in liver mostly but also in GI and lung
you have to love this to get in the brain fat
ionic forms of drugs are more easily excreted by the kidneys
polypharmacy is 5 or more drugs
grapefruit does this inhibits CYP 450 enzyme
milk pH is 7.08
nicotine does this induce cyp450 enzymes
acidic medications are more likely to end up in this (lactating women) breast milk
alcohol and caffeine induce cyp450enzymes
grapefruit permanently does this inactivates cyp3a4 enzymesand takes 48-72 hours
half life is the amount of time it takes for 50% of the drug to be out of your system
this many half lives should be used to calculate clearance 3.3
pharmacodynamics is potency, efficacy and safety - how the drug causes a response in the body
most drugs are excreted in the kidneys
clearance refers to renal clearance - rate of drug elimination by metabolism and excretion
pharmacogenetics inherited drug response - look at phenotypes
g linked receptor interactions include prostaglandins alpha or beta receptors
refractory receptors require a rest period - ion channels only
desnsitized receptors no longer responsive to ligand - think smell
downregulated receptors receptors are sequestered, even downgraded and unable to interact (morphine + dilaudid)
tachyphylaxis rapid unresponsiveness with repeated dosing (nitro 4th dose)
phase 1 clinical trial determine max dose, toxicity 15, ppl
phase 2 clinical trial disease oriented only 50 ppl
phase 3 clinical trial
Created by: jonquil