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Topic 4 Routes of Drug Administration 1

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46 views30 pages

Topic 4 Routes of Drug Administration 1

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When does a drug exert its

pharmacological effect?
Once it reach the site of action

A route of administration is the path by


which a drug, fluid, poison or other
substance is brought into contact with the
body.
FACTORS GOVERNING
CHOICE OF ROUTE
- Physical & chemical properties of drug
- Rate & extent of absorption from various
routes
- Effect of digestive juices & first pass effect
- Site of desired action
- Rapidity of the desired response
- Accuracy of dosage
- Condition of the patient
Classification
Routes of administration can broadly be
divided into:

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.
Routes of administration
1- Topical route:
I Skin
A-Dermal – cream, ointment (local action)

B- 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

II Mucosal membranes
 eye drops (onto the conjunctiva)
 ear drops
 intranasal route (into the nose)
2- 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:

1- Convenient
2- Cheap
3- Variety
Disadvantages:
1 - Sometimes inefficient
2 – First-pass effect
First pass effect
3- Food - Food and G-I motility can affect drug
absorption.

4- Sometimes may have adverse reactions

5- Not suitable for unconscious patient

6- May cause irritation to gastric mucosa, nausea


and vomiting.

7- Effect too slow for emergencies.


3- 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.
Sublingual: beneath the tongue
Buccal: Crushed and spread over buccal mucosa
Advantages
1- Avoid hepatic first pass

2- Rapid absorption

3- Drug stability

Disadvantages

1- Holding the dose in the mouth is inconvenient.

2- Small doses only can be accommodated easily.


Parenteral Route
4- Parenteral route:
Drugs administered directly into the
systematic circulation and have direct
access to the rest of the body.

A- Intravascular (IV, IA):


- placing a drug directly into blood
stream.

-May be - Intravenous (into a vein) or


intraarterial (into an artery).
Advantages
1- precise, accurate and immediate onset of action,
100% bioavailability.

Disadvantages
1- risk of Embolism – obstruction of an artery,
typically by a clot of blood or an air bubble

2- high concentrations attained rapidly leading to


greater risk of adverse effects.
B-Intramuscular :(into the skeletal muscle)

Advantages
1- suitable for injection of drug in aqueous solution
(rapid action) and drug in suspension or emulsion
(sustained release).

Disadvantages
1- Pain at injection sites for certain drugs.
C- Subcutaneous (under the skin), e.g. insulin.

D- Intradermal, (into the skin itself) is used for


skin testing some allergens.

E- Intrathecal (into the spinal canal) is most


commonly used for spinal anesthesia .

F- Intraperitoneal, (infusion or injection into the


peritoneum) e.g. peritoneal dialysis in case of renal
insufficiency.
5-Rectal route:
Most commonly by suppository or enema.
Advantages
1- 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.

2- 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


Suppository
Disadvantages
1- Erratic absorption - Absorption is often
incomplete and erratic.

2- Not well accepted.


6- Inhalation route:
- Used for gaseous and volatile agents and
aerosols.
- solids and liquids are excluded if larger than
20 micron. the particles impact in the
mouth and throat. Smaller than 0.5 micron ,
they aren't retained.
Advantages
A- Large surface area
B- thin membranes separate alveoli from
circulation
C- high blood flow
- As result of that a rapid onset of action due
to rapid access to circulation.

Note:
Alveoli are tiny sacs within our lungs that allow
oxygen and carbon dioxide to move between the
lungs and bloodstream
Disadvantages
1- Most addictive route of administration
because it hits the brain so quickly.

2- Difficulties in regulating the exact amount


of dosage.

3- Sometimes patient having difficulties in


giving themselves a drug by inhaler.
END

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