FA C U LT Y O F A RT S & S C I E N C E S

M B G 2 1 0 - I N T R O D U C T I O N TO
PHARMACOLOGY

2023/2024 SPRING TERM

ROUTES OF DRUG ADMINISTRATION

R O U T E S O F A D M I N I S T R AT I O N
• ROA are the possible paths of drug entry into the body system.

• The route of administration is determined by:

• the physical and chemical properties of the drug(s) – liquid/solid/gas, pH, solubility, stability, irritancy
• the rate/extent in which the drug is absorbed and/or released

• the need to bypass hepatic metabolism to achieve high concentrations at a site

• accuracy of dosage

• condition of the patient

• ROA may be divided into two:

• Enteral
• Parenteral
E N T E R A L RO U T E
• Drug placed directly in the gastrointestinal tract (G.I.T)
1. Oral –Swallowed
2. Sublingual – placed under the tongue
3. Buccal – placed between the gum and cheek
3. Rectal route – Absorption through the rectum
O R A L RO U T E

• Oral route refers to:

• swallowing for absorption along the
gastrointestinal tract into systemic
circulation.
• It is the most frequently used route of drug
administration.
• p.o. ( per os) is the abbreviation use to
indicate oral route of drug administration.
ORAL ROUTE

Advantages

Convenience – can be self-administered, pain free, easy to take

Different oral dosage forms of drugs.

Cheap – compared to most other parenteral routes

ORAL ROUTE
Disadvantages

Some drugs are unpalatable and may cause irritation of the

intestinal tact resulting in nausea, vomiting and diarrhea.

Incase of emergency when quick action of drug is required,

this route is not suitable.

Can be problematic because of the unpredictable nature of

gastro-intestinal drug absorption.

There is necessity for cooperation on part of the patient..

Drug interaction may occur if two or more drugs are

administered concurrently.
SUBLINGUAL ROUTE

Sublingual administration is where the

dosage form is placed under the
tongue.
• The dosage form is rapidly absorbed
by the sublingual mucosa
• This route has special importance
for certain drugs e.g Nitroglycerin
Sublingual route contd.

• Advantages
• Sublingual route of administration is economical
• Drug absorption via this route is quick
• First pass effect is avoided - this is the major advantage of this route because venous drainage
from the mouth is poured into the superior vena cava and the drug is saved from first pass effect.

• Disadvantages
• Some drugs can cause irritation of the oral mucosa
• Large quantities of drugs are not given via this route
• Few drugs are absorbed.
BUCCAL ROUTE

• Buccal administration is where the

dosage form is placed between the
gum and inner cheek lining.
• It is absorbed by the buccal mucosa
– e.g Prochlorperazine
BUCCAL ROUTE
Advantages
• First pass effect is avoided
• There is rapid absorption
• There is drug stability

Disadvantages
• Maybe Inconvenient
• Limited to small doses
• Advantages are lost if swallowed
R E C TA L R O U T E
Rectal administration is where the dosage form is placed inside the rectum.
Advantages
• Little or no first pass effect
• Used in vomiting/unconscious, children
• Higher concentrations rapidly achieved
Disadvantages
• It is inconvenient
• Absorption can be slow and erratic
• Irritation or inflammation of the rectal mucosa can occur
Advantages of rectal route over oral therapy:
(a) Drugs destroyed or inactivated by the pH or enzymatic activity of the stomach or intestines need
not be exposed to these destructive environments

(b) Drugs irritating to the stomach may be given without causing such irritation

(c) Drugs destroyed by hepatic circulation may bypass the liver after rectal absorption

(d) This route is convenient for administration of drugs to adult or pediatric patients who may be
unable or unwilling to swallow medication

(e) It is an effective route in the treatment of patients with vomiting episodes

PA R E N T E R A L RO U T E ( S Y S T E M I C )
Parenteral Administration involves the injection or infusion of drugs by means of a
needle or catheter inserted into the body.
• It provides the most control over the actual dose of drug delivered to the target site.
• Examples:
• Intravenous
• Intramuscular
• Subcutaneous
• Intra-arterial
I N T R AV E N O U S
Administration of drug solutions directly into the lumen of a vein so that it is diluted in the venous
blood.
Advantages Disadvantages

• Bioavailability is 100% • Less safe

• Desired blood concentrations achieved • Technical assistance/expertise is required

• Large quantities can be administered • Danger of infection

• Emergency situations, Vomiting & diarrhea • Expensive

• First pass avoided. • Less convenient and painful

INTRAMUSCULAR
• The administration of drug solution into the deltoid or gluteus muscle.

Advantages Disadvantages

• Absorption is reasonably uniform • Only up to 10ml drug can be given

• Rapid onset of action • Local pain and abscess

• Mild irritants can be given • Expensive

• First pass effect is avoided • Danger of infection

• Gastric factors can be avoided • Nerve damage
INTRADERMAL

Drug is given within skin layers (dermis)

• Mainly used for testing sensitivity to drugs
• E.g: penicillin, ATS (anti-tetanus serum)
• Inoculation: administration of vaccine (like
smallpox vaccine and BCG vaccination for active
immunization against tuberculosis)
S U B C U TA N E O U S
• Subcutaneous administration involves injecting a drug into the loose connective tissue between the
dermis of the skin and the muscle layer.
Advantages:
• It is a good route of administration especially in skin infections.
• It is relatively safer than intravenous and intramuscular routes
• Absorption is slower thus; it is a good route if a prolonged effect is to be achieved.
• Self-administration is possible as the injection need not be penetrated deeply.
Disadvantages:
• If the drug is irritating, it might cause the wearing off the skin epithermal tissues.
• It is suitable only for nonirritant drugs.
• Drug absorption is slow; hence it is not suitable for emergency.
• Like the i.m. route, only small volumes can be administered
I N T R AT H E C A L
• It is sometimes necessary to introduce drugs
directly into the cerebrospinal fluid.
• For example, amphotericin B is used in treating
cryptococcal meningitis

Site: Subarachnoid space

Advantages:
• Bypass blood brain barrier and blood CSF
barrier
• Acts directly on meninges and spinal cord
Disadvantages:
• Sepsis, expertise, painful, risky
INTRA-ARTICULAR

• Drug administration directly into the joint

cavity.
• Injections of antibiotics and corticosteroids
are administered in the inflamed joint
cavities by experts.
• Example: Hydrocortisone in rheumatoid
arthritis
 T O P I C A L R O U T E S O F A D M I N I S T R AT I O N

• Topical administration is the application of a drug directly

to the surface of the skin or any mucous membrane of
the eye, ear, nose, mouth, vagina, etc.
• Drugs for topical application are usually available as
creams, ointments, gels, lotions, sprays, powders,
aerosols, liniments, and drops.
• The drug can be made available almost directly at the
intended site of action, and because the systemic
circulation is not reached in great concentration, the risk
of systemic side-effects is reduced.
Topical administration cont’d

Advantages:
• Avoidance of the risks and inconveniences of administration and the varied conditions of absorption,
like pH changes, presence of enzymes, gastric emptying time, etc. in enteral or parenteral routes.

• Used for most dermatologic and ophthalmologic preparations.

• Avoidance of first pass effect.

Disadvantages:
• Can be used only for those drugs which require low plasma concentration for action.

• Enzymes in the epidermis may denature the drugs.

• Possibility of local irritation at the site of application.
TRANSDERMAL

Transdermal patch 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
Characteristics :
• Transdermal route offers steady level of drug in the system
no first pass metabolism
• drug must be potent, or patch becomes too large
• Absorption of drug through skin (systemic action)
FACTORS INFLUENCING CHOICE OF ROUTE OF ADMINISTRATION
1. Ease of Administration

Prescribers assess characteristics to determine route of administration:

• some patients are unable swallow
• very young or older adult patients might have difficulty swallowing
• oral route of administration is not advisable for a patient experiencing nausea and vomiting.
FACTORS INFLUENCING CHOICE OF ROUTE OF ADMINISTRATION

2. Site of Action

Choice of route of administration is influenced by desired site of action.

• The term local use refers to site-specific applications of drugs

• The term systemic use refers to the application of a drug to the site of action by absorption
into the blood and subsequent transportation throughout the body

NB: even drugs meant for systemic administration are usually targeted to a specific site of action
FACTORS INFLUENCING CHOICE OF ROUTE OF ADMINISTRATION

3. Onset of Action
Onset rate varies with route of administration:

• Oral medications for systemic use must proceed through a series of steps before they exert their
therapeutic effect.

• Liquid solutions or suspensions work faster than oral tablets or capsules.

-medication is more readily available for absorption

• Tablets placed under tongue or between cheeks and gums work quickly

-Medication bypasses stomach and liver, goes directly into bloodstream

Onset of Action contd.

• Drugs injected/infused directly into bloodstream are carried immediately throughout the
body

• Topical medications work quickly because of their localized therapeutic effects, especially
those applied:
• to the skin
• inhaled into the lungs
• instilled into the eye
FACTORS INFLUENCING CHOICE OF ROUTE OF ADMINISTRATION

4. Duration of Action

• The duration of action is the length of time a drug gives the desired response or is at the therapeutic
level.

• Controlled/extended-release tablet may last for 12 to 24 hrs compared with 4 to 6 hours for same
drug in immediate-release formulation

• Transdermal patches deliver small amounts of a drug steadily over many hours or eve days

• Sustained-duration effect can be achieved by means of intravenous infusion

• Injections into the muscle and skin last longer than injections directly into the bloodstream
FACTORS INFLUENCING CHOICE OF ROUTE OF ADMINISTRATION

5. Quantity of Drug

• Sometimes route of administration is chosen because of the amount of a drug.

• IV infusion is an excellent method for systemic delivery of large quantities of material:

• rapidly diluted in the bloodstream

• IV injections and infusions can deliver a higher dose of medication to the target site (important
in serious illnesses)
FACTORS INFLUENCING CHOICE OF ROUTE OF ADMINISTRATION

6. Metabolism by the Liver or Excretion by the Kidney

Liver metabolism breaks down active drug to inactive metabolites for elimination and to prevent
drug accumulation

• Age-related or disease-related changes in liver or kidney function can cause:

• drug accumulation
• toxicity
FIRST PASS EFFECT

• First pass effect is the loss of drug as it passes

through the G.I.T membranes and the liver, for the
first time during the absorption process after oral
administration. It is also known as Pre-systemic
elimination.

• The first-pass effect influences activity of several

drugs:
• drugs with high first pass effect must be given in large
oral doses or by another route of administration to
bypass or overcome metabolism by the liver