Edited By:

Rabia Mahmood
Lecturer Lahore-UBAS
PharmD, M.Phil (pharmacology) PU, Lahore.
 Contents
• Definition
• Factors affecting route
• Classification
• Local Routes and their advantages and
disadvantages
• Enteral Routes and their advantages and
disadvantages
• Parenteral Routes and their advantages and
disadvantages
 Introduction:
A route of administration is the path
by which a drug, fluid, poison or
other substance is brought into
contact with the body.

No single method of drug

administration is ideal for all
drugs in all circumstances.
Enteral; oral, sub-lingual, buccal,
rectal.

Parenteral; iv, im, sc, id, it, etc.

Different rates of absorption,
different plasma peaks.
Skin; for local or systemic effect
patches
Lungs; inhalation; local or
systemic effect
Vaginal; (usually local)
Eye; (usually local)
ENTERAL

ORAL

SUBLINGUAL

BUCCAL

RECTAL
 ORAL ROUTE
 Oral refers to
swallowing for absorption along the gastrointestinal
(GI) tract into systemic circulation
Advantages of Oral Route:
• Safest route.
• Commonest.
• Convenient.
• No skill required, self medication.
• Painless, & acceptable.
• Cost effective.
• No maximal/strict sterilization
required.
Disadvantages of Oral Route:
• Slow absorption delayed onset of
action Not suitable for emergencies.
• Unpalatable and irritant drugs not
administered e.g. Chloramphenicol.
• May cause nausea and vomiting.
• Absorption of drugs  variable and
erratic e.g. Streptomycin not absorbed.
• Interactions of prescribed drug with food
and other drugs affects absorption.
• Administration difficult in unconscious
patients.
Disadvantages of Oral
Route: – cont’d
• Some drugs are destroyed by gastric
secretions e.g. Insulin.
• Some drugs undergo extensive first pass
metabolism in the liver e.g. Lidocaine,
testosterone.
 Oral Dosage Forms
 Common dosage forms for oral administration
tablets
capsules
liquids
solutions
suspensions
syrups
elixirs
 First-pass Effect:
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 less the agent will reach the systemic
circulation when the agent is administered
orally.
These drugs undergo first-pass metabolism in
the liver, where they may be extensively
metabolized before entering the systemic
circulation. First-pass metabolism by the liver
limits the efficacy of many drugs when taken
orally. For example, more than ninety percent of
nitroglycerin is cleared during a single
passage through the liver, which is the primary
reason why this agent is not administered orally.
Drugs that exhibit high first-pass metabolism
should be given in sufficient quantities to ensure
that enough of the active drug reaches the
target organ.
Ingestion of drugs with food, or in combination
with other drugs, can influence absorption. The
presence of food in the stomach delays gastric
emptying.
Drugs that are destroyed by acid (for example,
penicillin) become unavailable for absorption.
Enteric coating of a drug protects it from the acidic
environment; the coating may prevent gastric
irritation, and depending on the formulation, the
release of the drug may be prolonged, producing a
sustained release effect.
 SUBLINGUALROUTE
 Sublingual administration is
where the dosage form is
placed under the tongue.
rapidly absorbed by
sublingual mucosa.
For example
Nitroglycerine.
 SUBLINGUALROUTE
ADVANTAGES
 ECONOMICAL.
 FIRST-PASS AVOIDED.
 DRUG ABSORPTION IS QUICK.

DISADVANTAGES
 UNPALATABLE & BITTER DRUGS.
 IRRITATION OF ORAL MUCOSA.
 LARGE QUANTITIES NOT GIVEN.
 FEW DRUGS AREABSORBED.
 BUCCAL ROUTE
 Buccal
administration is
where the dosage
form is placed
between gums and
inner lining of the
cheek (buccal
pouch)
absorbed by
buccal mucosa
For example:
buprenorphine.
 BUCCAL ROUTE
ADVANTAGES
– Avoid first pass effect
– Rapid absorption

DISADVANTAGES
– Inconvenience
– advantages lost if
swallowed
– Small dose limit
 RECTAL ROUTE
 Drugs that are administered rectally are
suppository.
 In this form, a drug is mixed with a waxy
substance that dissolves or liquefies after it is
inserted into the rectum.
 Can serve as local as well as systemic route
of administration of drugs.
 Preferable in patients who are vomiting, post-
operative, when difficult to establish intravenous
access (child having seizures).
 e.g. Diazepam, indomethacin, paraldehyde,
ergotamine.
 ADVANTAGES
 Used in children.

 Little or no first pass effect.

 Used in vomiting, unconsciousness.

 Higher concentrations rapidly achieved.

 DISADVANTAGES
 Inconvenient.

 Absorption is slow, incomplete,

irregular.
 Irritation or inflammation of rectal
mucosa can occur.
 SYSTEMIC-PARENTERAL
 Parenteral administration is
injection or infusion by means of
a needle, inserted into the body.
 The term parenteral comes from
Greek words
para, meaning outside
enteron, meaning the intestine
 This route of administration
bypasses the alimentary
canal.
Parenteral- Injections

Intraderma
l

Intrarticula Intramuscula
r r

Intra-
arterial
Injection Subcutaneo
us

s
Intratheca Intravenou
l s

Intraperitonea
l
 PARENTERAL ROUTES
Direct delivery of drug in to systemic circulation
without intestinal mucosa
 Intradermal (I.D.) (into skin).
 Subcutaneous (S.C.) (into subcutaneous tissue).
 Intramuscular (I.M.) (into skeletal muscle).
 Intravenous (I.V.) (into veins).
 Intra-arterial (I.A.) (into arteries).
 Intrathecal (I.T.) (cerebrospinal fluids).
 Intraperitoneal (I.P.) (peritoneal cavity).
 Intra - articular (Synovial fluids).
A) Intradermal – inj
into skin
B)Subcutaneous -
Absorption of drugs
from the subcutaneous
tissues
C)Intramuscular (IM)
drug injected into
skeletal muscle
D)Intravascular (IV)-
placing a drug directly
into the blood stream
 Advantages Disadvantages
• high bioavailability – Infection
• Rapid action (emergency) – Sterilization.
• No first pass metabolism –Invasive
Suitable for assistance require
–Vomiting &unconsciousness – Pain
– Irritant & Bad taste drugs. – Needs skill
– No gastric irritation – Anaphylaxis
– No food-drug interaction – Expensive.
Dosage form:
Vial or ampoule
Ampoule iv infusion Vial
 INTRAVENOUS ROUTE
ADVANTAGES
 IV is the most common parenteral route. For drugs
that are not absorbed orally.
 Avoids first-pass metabolism by the liver.
 Intravenous delivery permits a rapid effect
 (100% bioavailability)
 highly irritant drugs can be injected.
 One big advantage with this route is—in case
response is accurately measurable (e.g. BP) and
the drug short acting (e.g. sodium nitroprusside),
titration of the dose with the response is possible
 DISADVANTAGES
 However, unlike drugs in the GI tract, those that are
injected cannot be recalled by strategies such as
emesis or by binding to activated charcoal.

 , this is the most risky route—vital organs like heart,

brain, etc. get exposed to high concentrations of the
drug.
 Thrombophlebitis of vein and necrosis of adjoining
tissue if extravasation occurs.
 INTRAMUSULAR ROUTE
Large skeletal muscle- Deltoid, triceps, gluteus
maximus, rectus femoris

ADVANTAGES
 Absorption is faster(vascular)
 Rapid onset of action.
 It is less painful
 Mild irritants can be given.
 First pass avoided.
 Gastric factors can be avoided.
 Depot preparations (oily solutions,
aqueous suspensions) can be injected
by this route
 DISADVANTAGES

 Only upto 10ml drug

given.
 Local pain and abcess.
 Expensive.
 Infection.
 Nerve damage.
 Self injection is often
impracticable
because deep penetration is
needed.
 Subcutaneous (s/c)
E.g. Insulin, Heparin

Advantages
SC injection provides absorption via simple diffusion
and is slower than the IV route.
Provides constant, slow, and sustained effects
Patients can be trained for self-administration.
• The drug is deposited in the loose subcutaneous
• is less vascular (absorption is slower than
intramuscular).
Disadvantages
Irritant drugs can cause severe pain- due to
rich sensory nerve supply.
Repeated injections at same site
lipoatrophy decreased absorption
 Intradermal
• Drug injected into the layers of skin.
• e.g. BCG vaccine
• Disadvantage
-small amount of drug injected.
-may be painful.
Intrathecal
Drug to be injected in the subarachnoid space for CNS action
e.g. Spinal anaesthetics
Advantages
Used for long duration surgeries
Direct and Rapid Action
Bypass BBB
Disadvantages
Strict aseptic conditions are required.
 INTRA-ARTICULAR
 injections of antibiotics
and corticosteroids are
administered in
inflammed joined
cavities by experts.
example: hydrocortisone
in rheumatoid arthritis.
Topical Routes of Administration
 Topical administration is the application of a
drug directly to the surface of the skin
 Includes administration of drugs to any
mucous membrane

 eye  vagina
 nose  urethra
 ears  colon

 lungs
Advantages and Disadvantages
of the Topical Route

 Local therapeutic effects.

 Not well absorbed into the deeper layers of the
skin or mucous membrane.
lower risk of side effects.
 Transdermal route offers steady level of drug in
the system.
sprays for inhalation through the nose
may be for local or systemic effects
 Transdermal
This route of administration achieves systemic effects by application
of
drugs to the skin, usually via a transdermal medicated adhesive patch.
The rate of absorption can vary markedly, depending on the
physical characteristics of the drug (lipid soluble) and skin at the
site of application.
Slow effect (prolonged drug action)
This route is most often used for the sustained delivery of drugs,
such
as the antianginal drug nitroglycerin, the antiemetic scopolamine.
the nicotine patches
 Inhalation
 Inhalation provides the rapid delivery of a drug across the
large surface area of the mucous membranes of the
respiratory tract and pulmonary epithelium, producing an
effect almost as rapidly as with IV injection.
 for drugs that are gases (for example, some anesthetics)
or those that can be dispersed in an aerosol.
 This route is particularly effective and convenient for
patients with respiratory complaints (such as asthma, or
chronic obstructive pulmonary disease) because the
drug is delivered directly to the site of action and
systemic side effects are minimized.
Advantages
 Large surface area.
 Serves as local route in lung diseases.
 Hepatic first pass metabolism is avoided.
 Small dose since direct delivery – less
toxicity.
 - 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.
• Drug may induce cough e.g. Cromolyn sodium.
• Pulmonary secretion may get enhanced.
 Intranasal
 This route involves administration of drugs directly into
the nose.
 Agents include nasal decongestants such as the anti-
inflammatory corticosteroid.
 Desmopressin is administered intranasally in the
treatment of diabetes insipidus; salmon calcitonin, a
peptide hormone used in the treatment of
osteoporosis, is also available as a nasal spray.
 The abused drug, cocaine, is generally taken by
intranasal sniffing.