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21 Cards in this Set

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  • Back

Lab tests to evaluate renal function

Creatinine and BUN

Lab tests to evaluate liver function

AST and ALT

Plasma half-life

-Drugs duration of action


-length of time it takes for med to ↓ concentration in plasma by ½ after admin


-Greater half-life, longer it takes to excrete the med


-Drugs with short half-lives must be given 3-4x day


-Drugs with longer half-lives need only be given once daily



Half-life and renal/liver disease

Half-life ↑ & drug concentration may reach toxic levels at normal dose→ give meds less frequently OR reduce dosages

CytochromeP-450 (CYP450) enzyme system




(4 possible functions)

-Promote & accelerate renal excretion of the drug (convert lipid-soluble drugs into less lipid-soluble)




-Inactivate the drug


(can decrease risk of toxicity)




-Transform drug to a more active form


(Can increase potency ex-codeine to morphine)


(Can increase risk of toxicity ex- Acetaminophen to hepatotoxic metabolite)




-Activate Prodrugs

Additive effect

1+1=2


Ex:one ASA and one Tylenol= relieve headache

Synergistic effect

1+1=3




Ex: combination of CNS depressants can lead to overdose

Antagonistic effect

2+2=1




Ex: Narcan for opiate OD

Agonist

Activates the receptor

Antagonist

Blocks the receptor

Affinity

Strength of a drug and its receptor site




High-affinity= high-potency (if anagonist)


(drugs with a high affinity are capable of producing effects at a lower dose)

Intrinsic Activity

Ability of a drug to activate a receptorupon binding; reflected in maximal efficacy.




-High-intrinsic activity= high receptor activation= intense responses




-Low-intrinsic activity= low receptor activation= minimal responses

How many half-lives to get to therapeutic effect?

-takesapproximately 4 half-lives to reach the drug level where the plasma therapeuticlevel is continuously maintained

Loading Dose

1 or 2 large doses given followed by maintenance doses to achieve therapeutic level.

Protein-Binding


(warfarin example)

Decreases the availability of medication due to lack of recognition by receptors



-Major protein is albumin




EXAMPLE


-99% of warfarin is bound to albumin. ASA also binds to albumin.


-ASA displaces warfarin, and puts free warfarin into the blood which increases the risk for hemorrhage

Potency

Amount of drug given to elicit an effect.




A potent drug elicits an effect at a lower dose


(ex levothyroxine)

Efficacy

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




Almost always more important than potency

Therapeutic Index

ED-50/LD-50=TI




(closer ED is to LD, the more narrow the TI)


(OTC drugs have a wide TI)

First-Pass Effect

-Phenomenon of drug metabolism whereby the concentration of a drug is greatly reduced before it reaches the systemic circulation




-Greatly reduces bioavailability

Alternatives to First-Pass

suppository, intravenous, intramuscular, inhalational aerosol, transdermal and sublingual




-avoid the first-pass effect because they allow drugs to be absorbed directly into the systemic circulation.

Enterohepatic Recirculation

Biliary recirculation prolongs the action of a drug.




May continue for several weeks after therapy has been discontinued.