 Plasma Proteins – albumin, lipoproteins, alpha-1-acid-

glycoproteing (AGP)
 Basic drugs (morphine, amantadine) binds to AGP.
 Highly protein bound drugs >90% bound to proteins
(warfarin, glyburide, sertraline, furosemide, and
diazepam).
 Weakly protein-bound drugs - <10% bound to protein
(gentamycin, metformin, metopolol, and lisinopril).
 The portion that remains unbound is free, active drug.
 Free drugs are able to exit blood vessels and reach their
site of action, causing a pharmacological response.
 Low level of plasma protein can cause drug toxicity due
to low available binding sites of the drug thus increasing
the amount of free drug.
 Pts with liver or kidney disease and malnourished have
significantly lower serum albumin levels.
 Older adults have hypoalbuminemia particularly if they
have multiple chronic illnesses.
 NOTES: prior administration of medication it is
important as a nurse to check the protein and albumin
level of the patient to prevent drug toxicity.
 Pregnancy: 1st trimester drugs can lead to spontaneous
abortion; 2nd trimester spontaneous abortion,
teratogenesis, or other subtler defects; may alter fetal
growth and development. During breastfeeding, drugs
can pass to breast milk.

Pharmacokinetics: ADME
Absorption
Distribution
Metabolism
Excretion

 Liver is the primary site of metabolism of drugs.

 P450 system – cytochrome P 450 system – convert
drugs into metabolites.
 Large percentage of drugs are lipid soluble thus the liver
metabolize the lipid-soluble drug substance into a
water-soluble substance for renal excretion.
 Liver disease that alter drug metabolism by inhibiting
the drug-metabolizing enzymes in the liver resulting to
decrease drug metabolism increasing the risk of drug
toxicity by increase amount of free drugs.
 Half life is the time it takes for a drug to be reduced in
half inside the body.
 With liver and kidney disease a half life can be
prolonged.
 Half life is used to determine dosing interval.