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1.Pharmacokinetics: The study of drug movement within the body, the effect
the body has the drug.
2. Four Pharmacokinetic Processes:
1. Absorption
2. Distribution
3. Metabolism
4. Excretion
*Cell membrane Structure: Drugs usually pass through the cells, instead of
between them to cross the membrane. Page 28
Transport System: Important in drug transport, only way certain oral drugs are
absorbed are when the drug reaches the site of action and speed up renal
excretion.
3. How do drugs cross membrane?
1. Channels and pores: Very small, specific for certain protein, sodium
and potassium
2. Transport Systems: Move molecules on one side of the membrane to
the other.
E.g.: P-Glycoprotein: Transmembrane protein that transport a wide variety
of drugs out of cell.
--P-Glycoprotein transports drugs to:
1. Kidney: excreted into urine
2. Liver: excreted into the bile
3. Placenta: excreted into mothers circulation
4. Intestine: excreted into intestinal lumen
5. Capillaries of the CNS: P-glycoprotein pumps drugs back into
the blood; again limiting drug access to the brain.
-Most movement of drugs throughout the body is by direct penetration of
membranes.
-Channels are too small and most drugs lack a transport system.
-In order to directly penetrate, the drug must be lipophilic, because
membranes are composed mostly of lipids.
Characteristics of Routes
ROUTES BARRIERS PATTERNS ADVANTAGES DISADVANTES
None
Instantaneous
-Rapid onset
IV
-Irreversible
- Precise control, -Large volumes
-Irritant drugs.
IM
Capillary wall
SQ
PO
Same as IM
Epithelial lining
GI wall and
capillary wall
-Easy
-Inexpensive
-Ideal for self
administration
Potentially reversible
-Expensive
-Inconvenient
-Infection
-Embolism
-Drug must water
soluble
-Discomfort
-Inconvenient
-The variability.
Gastric acid can cause
inactivation of some
drugs.
Possible for nausea and
vomiting.
Must be conscience
and cooperative
i.
3.
4.
5.
6.
We want the drug levels to stay in the middle to stay therapeutic- Take
times to get to this level if you given patient loading doses or
maintenance to keep it at this level.
Half-Life
Defined as the time required for the amount of drug in the body
to decreased by 50%.
Percentage vs. amount: a % - not a specific amount of drug
is lost during one half life.
Determines the dosing interval
Also important regarding drug reactions.
Zetia: 22 hour half-life. After 22 hours, half of that dose will be
eliminated from the body. How often would you give this
medication? Daily, because it has a half-life of 22 hours, not twice,
or three? Too often, concentration high, because half-life, it
determines the dosage.
Half-life: Gave a drug today, tomorrow when we go to give the dose
again, 50% of the drug has been eliminated from the body.
Percentage: 50%
Recommended: 10mL once daily. So 22 hours later, 5mL would be
left in circulation. Important to know the reaction of drug and
when to monitor.
Drugs Levels Produced with Repeated Doses:
Loading dose: needed to get level of drug at a therapeutic level, after that take
maintenance doses.
Antibiotic IM: Faster, then patient can take the PO after that in a smaller dose to
maintain.
Will do antibiotics, digoxin (IV loading dose) Arrhythmias, CHF
Patient has DVT or PE: Need heparin at a therapeutic level, IV push and then
maintenance doses.
PTT: Narrow window, every 6 hours, monitor PTT levels.
Will take 4 doses to decline.