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7 𝑥 𝑉)/𝐶𝐿
There are 4 half lives before administering drug
Dynamics of drug absorption, distribution and elimination Steady state- concentration builds up
Absorption
Distribution Why is it important to know the half life of the drug?
Metabolism
Excretion - The therapeutic levels of a drug can be obtained
more rapidly by delivering a loading dose
Pharmacokinetics followed by maintenance doses
Aqueous diffusion- occurs within the larger - Amount of time it takes a drug to begin working
aqueous compartments of the body and across
Duration
epithelial membrane tight junctions and
endothelial lining of the blood vessels through - The length of time for which a drug is therapeutic
aqueous pores; 20,000-30,000 MW;
concentration gradient: Fick’s law Bioavailability
Lipid diffusion- most important limiting factor
for drug permeation - The fraction of unchanged drug reaching the
Special carriers- by active transport and systemic circulation following administration by
facilitated diffusion that are selective, saturate any route
and inhibitable
Routes of administration:
Endocytosis and exocytosis- bound at cell
surface receptor (e.g Vitamin B12- upper Intravenous- best way; 100 bioavailability
jejunum and duodenum, iron- ileum) Intramuscular- 75-≤100
Subcutaneous- 75-≤ 100
Pharmacokinetic parameters
Per oral- 5- <100
Clearance- the measure of the ability of the Per rectal- 30- <100
body to eliminate the drug; mg/L or mg/hr (e.g Inhalation- 5-100
liver, kidney lungs) Transdermal- 80-100
Volume of distribution- the measure of the Sublingual
apparent space in the body available to contain Topical
the drug
𝑎𝑚𝑜𝑢𝑛𝑡 𝑜𝑓 𝑑𝑟𝑢𝑔 Intravenous
𝑉𝑑 =
𝑐𝑙𝑒𝑎𝑟𝑎𝑛𝑐𝑒
<7= plasma - Most rapid
7-15= blood - Useful in emergencies and in unconscious
>42= tissues patients
- Insoluble drugs cannot be administered through
Half life- the amount of time required for the
intravenous
plasma concentration of a drug to decrease by
50%
Lyca A.
Intramuscular - Dermatologic and ophthalmologic preparations
Inhalation ↓
Transdermal
First pass effect
- “Patch”- skin and capillary bed
- Convenient for self administration - Phenomenon that greatly reduced effect before
- Long duration the drug reach the systemic circulation
- Lack first pass effect
- Slow absorption Time course of drug effects
Sublingual Immediate
Delayed
- Good absorption
Cumulative
- Easily administered drugs
- Because the stomach is bypassed, acid-lability
and gut-permeability need not be considered
Topical