ROUTES OF DRUG ADMINISTRATION

It is the path by which a drug, fluid, poison or other substance is brought into contact with the
body.
Classification
Routes of administration can broadly be divided into:
LOCAL SYSTEMIC
Topical: Drugs are applied topically to the skin or mucous membranes, mainly for local action.
Oral: used for systemic (non-local) effect, substance is given via the digestive tract.
Parenteral: A drug administered parenterally is one injected via a hollow needle into the body
at various sites and to varying depth.
Rectal: Drugs given through the rectum by suppositories or enema.
Inhalation: The lungs provide an excellent surface for absorption when the drug is delivered
in gaseous, aerosol or ultrafine solid particle form.
Topical route:
Skin
Dermal – cream, ointment (local action)
Transdermal- absorption of drug through skin (i.e systemic action)
I. stable blood levels (controlled drug delivery system)
II. No first pass metabolism
III. Drug must be potent or patch becomes too large
Mucosal membranes
Eye drops (into the conjunctiva)
Ear drops
Intranasal route (into the nose)
Oral route:
By swallowing.
- It is intended for systemic effects resulting from drug absorption through the various epithelia
and mucosa of the gastrointestinal tract.
Advantages:
➢ Convenient - portable, no pain, easy to take.
➢ Cheap - no need to sterilize, compact, multi-dose bottles, automated machines produce
tablets in large quantities.
➢ Variety - tablets, capsules, suspensions, mixtures.
Disadvantages:
➢ 1- Sometimes inefficient - low solubility drugs may suffer poor availability
e.g., Griseofulvin
➢ 2- First-pass effect - drugs absorbed orally are transported to the general circulation
via the liver. Thus, drugs which are extensively metabolized will be metabolized in the
liver during absorption. e.g. propranolol
First pass effect
First pass effect (Cont.):
The first pass effect is the term used for the hepatic metabolism of a pharmacological agent
when it is absorbed from the gut and delivered to the liver via the portal circulation.

- The greater the first pass effect, the lower the bioavailability of the drug (the rate and
extent of the drug reaching systemic circulation).
3- Food - Food and G-I motility can affect drug absorption.
Often patient instructions include a direction to take with food or take on an empty
stomach.
- Absorption is slower with food (milk and milk products) for tetracyclines and penicillin’s,
etc. However, for propranolol bioavailability is higher after food, and for griseofulvin
absorption is higher after a fatty meal.
4- Sometimes may have adverse reactions – e.g., Antibiotics may kill normal gut flora and
allow overgrowth of fungal varieties. Thus, antifungal agent may be included with an antibiotic.
5- Not suitable for unconscious patient - Patient must be able to swallow solid dosage forms.
Liquids may be given by tube.
6- May cause irritation to gastric mucosa, nausea and vomiting.
7- Effect too slow for emergencies.
Buccal/Sublingual route:
Some drugs are taken as smaller tablets which are held in the mouth (buccal tablet) or under
the tongue (sublingual tablet).
Buccal tablets are often harder tablets [4-hour disintegration time], designed to dissolve slowly.
E.g Nitroglycerin, as a softer sublingual tablet [2 min disintegration time], may be used for the
rapid relief of angina.
Advantages
1- Avoid hepatic first pass - The liver is by-passed thus there is no loss of drug by first pass
effect for buccal administration. Bioavailability is higher.
2- Rapid absorption - Because of the good blood supply to the area, absorption is usually quite
rapid.
3- Drug stability - pH in mouth relatively neutral (gf. stomach - acidic). Thus, a drug may be
more stable.
Disadvantages
1- Holding the dose in the mouth is inconvenient.
2- Small doses only can be accommodated easily.
Parenteral route:

Intravascular (IV, IA):

placing a drug directly into blood stream.
May be - Intravenous (into a vein) or - intraarterial (into an artery).
Advantages
precise, accurate and immediate onset of action, 100% bioavailability.
Disadvantages
risk of embolism.
high concentrations attained rapidly leading to greater risk of adverse effects.
Intramuscular :(into the skeletal muscle).
Advantages
suitable for injection of drug in aqueous solution (rapid action) and drug in suspension or
emulsion (sustained release).
Disadvantages
Pain at injection sites for certain drugs.
Subcutaneous (under the skin), e.g., insulin.
Intradermal, (into the skin itself) is used for skin testing some allergens.
Intrathecal (into the spinal canal) is most commonly used for spinal anesthesia.
Intraperitoneal, (infusion or injection into the peritoneum) e.g., peritoneal dialysis in case of
renal insufficiency.

Rectal route:
Most commonly by suppository or enema.
Advantages
By-pass liver - Some of the veins draining the rectum lead directly to the general circulation,
thus by-passing the liver.
Reduced first-pass effect.
Useful - This route may be most useful for patients unable to take drugs orally (unconscious
patients) or with younger children.
- if patient is nauseous or vomiting
Disadvantages
Erratic absorption - Absorption is often incomplete and erratic.
Not well accepted.

Inhalation route:
Used for gaseous and volatile agents and aerosols.
solids and liquids are excluded if larger than 20 microns. the particles impact in the mouth and
throat. Smaller than 0.5 micron, they aren't retained.
Advantages
Large surface area
thin membranes separate alveoli from circulation
high blood flow
As result of that a rapid onset of action due to rapid access to circulation.
Disadvantages
Most addictive route of administration because it hits the brain so quickly.
Difficulties in regulating the exact amount of dosage.
Sometimes patient having difficulties in giving themselves a drug by inhaler.