Routes of administration

Bahaa El Merhabi
 Administration of a drug

Aiming a systemic effect: Aiming a local effect:

Waiting from the drug to enter Waiting from the drug to act near
the systemic circulation and to the site of administration
exert a function on specific
tissue/ tissues
1- Enteral: 1- oral 1-rectum : vasoconstrictor for hemorrhoids
2- buccal
3- sublingual 2- nose : decongestants

2- parenteral: 1- IV topical 3- skin: corticosteroids to decrease inflammation

2- IM
3- sub-cu 4- eye : atropine for pupillary dilation for surgery
3- nose or eye exam.
4- vagina topical 5- vagina
5- skin
6-rectal inhalation 6- lungs: bronchodilators ( beta agonists)
7- lungs inhalation
 The absorption of a drug from its site of administration depend on 2 things

1- the site characteristics : 2- the molecule characteristics:

a- the surface of absorption That will determine its mechanism of transport
whether simple or facilitated diffusion or active
b- extend of vascularization which will influence transport or endocytosis or pinocytosis……
the surface of absorption

c- the thickness of the membrane of absorption

d- pH at the site
Oral route
- mainly drugs are absorbed by passive diffusion, then facilitated , active transport and endocytosis/exocytosis.
- Drug tablet must dissolve before it’s absorbed  certain water solubility is required which may limit absorption
- Medications should be resistant to the stomach acidity

Because the majority of drugs are weak acids or weak bases

Weak acids Weak bases

Better absorbed in the Better absorbed in the
stomach because pH<pKa intestine because pH>pKa
However
Stomach : - thick mucous layer ( high d)
- small surface
- low vascularization comparing to the intestine The rate of absorption of any drug ( weak
acid or weak base) is going to be greater in
Intestine : - thin mucous layer the intestine, because majority of
- large surface absorption is by simple diffusion
- high vascularization
Factors modifying GI absorption

Gastric factors :
1- every factor that increases gastric emptying Hunger, moderate exercise, diluted
increases the rate of drug absorption solution

2- every factor that delays gastric emptying Anticholinergics ( antihistaminic)

decreases the rate of absorption

Intestinal factors :
1- factors that increase intestine motility
decrease absorption

2- factors that decrease intestine motility Anti- diarrhea

increase absorption

Expression of OATP ( pumps drug out the cell)  areas of higher expression of P-gp exhibit lower absorption of drugs
 First pass effect and
microbiota metabolism

Drug must be
lipid soluble
Drain into the SVC - Small absorption surface
 • Ideal for large doses,
irritating substances and
complex mixtures, high MW
must be proteins and peptide drugs
aqueous
solution, • Can have immediate effect
cannot be oily
• Dosage titration and control
is possible

• used when moderate dose,

oily vehicles and certain
irritating substances
• Preferrable more than IV if
self administration

lidocaine

IV must be aqueous solution, cannot be oily

IM or sub-cu can be aqueous solution, or depot ( formulation which is (aqueous or oleaginous) suspension or oleaginous solution( smaller particles ) 
sustained effect)
• Inflammation may increase blood
flow and increase absorption

Testosterone
and
estrogen