This is a draft cheat sheet. It is a work in progress and is not finished yet.
nature of the drug
- appropriate size |
- electrical charge |
-shape |
-atomic composition |
pharmacokinetics (ADME)
Absorption |
Distribution |
Metabolism |
Excretion |
oral route
advantages** |
disadvantages |
easy |
slow effect |
safe |
destruction by GIT |
self use |
first pass effect |
convenient |
food-drug interaction |
cheap |
drug-drug interaction |
no need for sterilization |
not suitable for uncurious, emergency |
sublingual administration
advantages |
disadvantages |
rapid effect |
not for irritant drugs |
no first pass metabolism |
high bioavailability |
no GIT destruction |
bo food-drug interaction |
parental administration
Advantages |
Disadvantages |
high bioavailability |
infectious |
rapid action |
sterilization |
no first pass metabolism |
pain |
no food-drug interactions |
need skill |
no gastric interaction |
anaphylaxis |
suitable for emergency |
expensive |
inhalation
Advantages |
Disadvantages |
Rapid absorption area) |
Only few drugs can be used |
Rapid effects as IV bolus |
Provide local action |
Minor systemic effect |
low bioavailability |
Less side effects. |
No first pass effect |
Dosage form: Aerosol, Nebulizer
rectal administration
Advantages |
Disadvantages |
Vomiting & children. &unconsciousness |
Irregular absorption & bioavailability |
irritant and bad tasting drugs |
Irritation of rectal mucosa |
less first pass metabolism |
Not a well accepted route |
dosage form: suppository or enema
transdermal administration
Advantages |
Disadvantages |
bypass first pass effect |
allergy to patches |
convenient and painless |
drugs must be highly lipophilic |
ideal for drugs that are lipophilic and have poor oral bioavailability |
delayed delivery of drugs |
|
limited to drugs taken in small daily dosages |
topical application
rate of absorption depends on: physical characteristics of skin at site of application and lipid solubility of the drug |
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mechanisms of drug absoption
simple diffusion= passive diffusion |
active transport |
facilitated diffusion |
pinocytosis (endocytosis) |
simple or passive diffusion characters
common |
occurs along conc gradient |
non selective |
not saturable |
low structural specificity |
no energy |
no carrier is needed |
depends on lipid solubility |
depends on pKa of drug- pH medium |
active transport characters
unusual |
occurs against conc gradient |
selective |
saturable |
require energy |
carrier is needed (protein) |
iron absorption |
uptake of levodopa by brain |
facilitated diffusion characters
occurs along conc gradient |
selective |
saturable |
no energy is required |
carrier is needed (protein) |
factors influencing aborption
1. Effect of pH on drug absorption
2. Blood flow to the absorption site
3. Total surface area available for absorption 4. Contact time at the absorption surface
5. Expression of P-glycoprotein; transmembrane transporter protein. transport drugs from tissue to blood |
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