PHARMACOKINETICS

Pharmacokinetics is the movement of a drug through the body, from entrance to exit.
1. Absorption Common routes Bioavailability is the extent
of administration: and rate at which the drug
1 Movement from site • Oral enters the systemic
of administration to • Intravenous (IV) circulation.
bloodstream • Intramuscular (IM) Bioavailability is 100% in IV
• Subcutaneous (SubQ) administration, but varies
• Transdermal widely in all other routes.
• Pulmonary/nasal

2 2. Distribution Influenced by: Factors that may limit

• Adequate blood flow distribution:
Transport through • Ability of drug to exit • Vascular damage due to chronic
systemic circulation vascular system disease, such as diabetes
to target tissues or • Ability of drug to enter • Limited blood supply to
organs target cell abscesses or tumors
• Tight junctions of the
3 blood-brain barrier
3. Metabolism Primarily occurs in the liver:
Effects of metabolism vary by drug, may include:
Chemical alteration, • Conversion from lipid-soluble to water-soluble compound
or biotransformation,
of a drug to make it • Inactivation of drug
pharmacologically • Bioactivation of ‘prodrug’
active or to facilitate • Increased or decreased toxicity
elimination
4. Excretion Most drugs are filtered Other routes of excretion:
by the kidneys and • Bile → feces
Removal of drug eliminated in the urine. • Lungs (primarily anesthetics)
from the body Special care must be
• Sweat and saliva
4 taken in clients with
renal disease or kidney • Breast milk (caution during
failure. lactation)

1 2 First pass 3 4 Cytochrome P450 system

effect Absorption • A group of 12 closely related enzyme families
Drugs absorbed responsible for metabolism of most drugs
through the GI tract Absorption • Genetic variability in CYP450 enzyme function
pass through the liver contributes to differences in individuals’ ability
before entering the to metabolize drugs.
systemic circulation. • Many foods and medications can inhibit or induce
Hepatic metabolism the CYP450 enzyme system.
decreases
Gut wall Hepatic • It is important to counsel clients regarding the potential
bioavailability.
metabolism metabolism food and drug interactions of their specific medications.

NOTES

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