Routes of drug administration

Routes of drug administration

 Routes of drug administration is the way through

which the dosage form is administered into the
body for treatment of various diseases and
disorders.
 For a drug to bring its beneficial effect it has to be
administered into the body by convenient route.
 Routes of drug administration can be divided into
enteral, parenteral, topical, respiratory route
(inhalation) and miscellaneous routes

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 Routes of drug administration

 Enteral routes are routes related with GIT and

include:
Oral
Sublingual
Buccal
Rectal

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 Routes of drug administration….cont’d

 Parentral route of drug administration include:

Intravenous
Subcutaneous
Intramuscular
Intraspinal
Intrarterial
Intraperitonial
 Topical route
 Respiratory route/inhalation
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 Oral route
 In this route the dosage form is placed in the mouth
and then swallowed.
 It is also called per oral (p.o.)
 This is the most commonly used route for drug
administration.
 The most popular dosage forms are tables, capsules,
solutions, suspensions & emulsions
 The oral route can produce either a systemic or a
local effect.
 For a systemic effect the drug, formulated in either a
solid or a liquid form, is absorbed from the GIT
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 Oral route

Advantages
From a patient point of view it is the simplest,
convenient (Self-administration of drug can be
carried out) and If used properly, it is also the
safest route.

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 Oral route…..Cont’d

 Disadvantages
The onset of drug action is relatively slow
Unpleasant taste of some drugs can be felt
Irritation of gastric mucosa by some drugs
Absorption from the GIT may be irregular (e.g.,
some foods delay absorption of drugs)
 Drug solubility may be altered by the presence of
other substances in the GIT( e.g., calcium forms
complex with tetracycline)

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 Oral route…..Cont’d

 Disadvantages…….
Gastric emptying is very variable and can be
influenced by factors such as food, drugs, disease
state and posture. Not only does it affect the
onset of action, but if it is extended it may cause
a drug to be inactivated by gastric juice owing to
prolonged contact.
It is an unsuitable route of administration in
unconscious or vomiting patients and for
immediate pre- or postoperative use
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 Oral route…..Cont’d

 Disadvantages…….
 Some drugs are destroyed by enzymes and other
secretions found in the GIT (e.g., insulin,
penicillin become inactivated by the action of
stomach acid)
Because of the blood supply from the GIT passes
through the liver via the hepatic portal system, it
is subject to hepatic metabolism before it enters
the systemic circulation. This is called first pass or
presystemic metabolism. e.g., lidocaine
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 Buccal route

 In the buccal route the dosage form is positioned

against the mucus membranes lining the checks.
 A drug is administered by these route by being
formulated as a tablet or spray and is absorbed
from the buccal cavity.
 The dosage form is kept in the buccal cavity where
it disintegrates and absorption occurs in the mouth
 Water is not used for taking the dosage form

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 Buccal route

 The highly vascular nature of the tongue and buccal

cavity, and the presence of saliva which can
facilitate the dissolution of the drug, make this a
highly effective and useful route for drug
administration.
 Advantages
There is a relatively quick onset of action( due to
rapid absorption of drugs)
Drugs can be administered to unconscious
patients
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 Buccal route

 No deactivation of drug by gastric fluid

Drugs are absorbed into the systemic circulation,
there by avoiding the “first-pass” effect
 Disadvantage
 Unpleasant taste of some drugs can be felt.
 It is useful for small dose drugs.
 Inconvenient

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 Sublingual route

 In the sublingulal route the dosage form is placed

on the floor of the mouth (palate) or under the
tongue.
 Formulations which have been specifically designed
for sublingual delivery include gums, fast-dissolving
dosage forms and mucoadhesive patches.
 Example of sublingual tablet is nitroglycerine
tablets.

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 Sublingual route

 Advantages
 There is a relatively quick onset of action( due to rapid
absorption of drugs)
 Drugs can be administered to unconscious patients
 No deactivation of drug by gastric fluid
 Drugs are absorbed into the systemic circulation, there by
avoiding the “first-pass” effect
 Disadvantage
 Unpleasant taste of some drugs can be felt.
 It is useful for small dose of drugs.
 Inconvenient
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 Rectal route
 In the rectal administration dosage form is placed in the
rectum of the patient from where the drug is released to
give a local effect or it may be absorbed to give systemic
effect.
 For administration by this route, drugs are formulated as
liquids, solid DFs and semi-solids.
 The rectum is supplied by three veins, namely the middle
and inferior(lower) rectal veins which drain directly into the
systemic circulation and the upper rectal vein which drains
into the portal system which flows into the liver
 This means that, depending on the position within the
rectum, only some of the drug absorbed from the rectum
will be subject to the first pass effect.
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 Rectal route………Cont’d

 Bioavailability, therefore may be less than 100% but

may be better than obtained from other parts of
the GIT.
 The amount of fluid present in the rectum is small,
estimated at approximately 3 ml of mucus.
This effect the rate of dissolution of drug
released from DFs
However, there is also muscular movement
which spreads the drug over a large area and
promote absorption
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 Rectal route………Cont’d

 Advantages of rectal route

 To provide a local effect for the treatment of infection and
inflammation, e.g. haemorrhoids, proctitis.
 To promote evacuation of the bowel to relieve constipation
or to cleanse the bowel prior to surgery.
 To provide systemic drug absorption in situations where oral
drug absorption is not recommended. Examples of such
applications include:
 patients who are unconscious, e.g. in intensive care or
who are postoperative
 patients who are vomiting, e.g. gastrointestinal infection,
migraine
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 Rectal route………Cont’d

 Advantages of rectal route……..

 gastroirritant drugs, e.g. non-steroidal anti-
inflammatory agents(NSAIDs), particularly in
chronic usage
 drugs that are prone to degradation in the
stomach
drugs that are erratically absorbed from the
upper gastrointestinal tract
 administration of drugs that are extensively first-
pass metabolised.
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 Rectal route………Cont’d

 Disadvantages of rectal route

Uncomfortable
Specialist advice is required concerning the
administration of dosage forms
The absorption of therapeutic agents from the
rectum is slow and prone to large intrasubject
and intersubject variability.
Rectal administration of therapeutic agents may
result in the development of local side effects, in
particular proctitis.
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 Vaginal route

 In the vaginal route, dosage forms are administered

in the vaginal cavity.
 For administration by this route, drugs may be
formulated as pesseries, tablets, capsules,
solutions, sprays, creams, ointments and foams
 Most often this route is used for a local effect (used
to treat vaginal infections and vaginitis)
 However, drugs absorbed from the vagina are not
subject to the first pass effect and systemic
bioavailability better than the oral route.
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 Vaginal route……..cont’d

 Advantage of vaginal route

Possibility of self-administration,
 High vascularization,
 Relatively low enzymatic activity (e.g.,trypsin
and chymotrypsin are absent)
Bypass hepatic first pass-effect,
Increased permeability for some drugs when
comparing to the oral or other routes.

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 Vaginal route……..cont’d

 Disadvantage of vaginal route

Social taboo
Removal of dosage form after administration
Only few drugs are administered by this route
Variability in drug absorption related with
menstrual cycle, menopause and pregnancy
Influence with sexual intercourse
Gender specificity

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 Parentral route

 This is the term used to describe drug administration

by injection.

 Within this general term there is a variety of different

routes. The main ones are:
 Intravenous route (IV)
 Intramuscular route (IM)
 Subcutaneous route (SC)

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 Parentral route

Intravenous route (IV route), where drugs are injected

directly into the vein.
 It is the surest way of introducing drug into systemic
circulation.
 Permit rapid onset of action (no absorption of drug ).
 Large volume of pharmaceutical preparations can be
administered than other routes.

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 Parentral route……Cont’d

Intramuscular route (IM)

 Drugs are injected into muscle from where it is
absorbed due to the perfusion of the muscle by
blood.
 Usually injected at deltoid and gluteus muscle
 This method can be used to produce a fairly fast
onset of action when the drug is formulated as
an aqueous solution.

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 Parentral route……Cont’d

Intramuscular route (IM)…

 A slower and more prolonged action will occur
when the drug is presented as a suspension or in
non aqueous vehicle such as ethylene glycol or
peanut oil.
 As the vehicle diffuses out of the muscle, the
drug precipitates at the site of injection. The
drug then dissolves slowly, providing a
sustained release over extended period of
time.
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 Parentral route……Cont’d

 E.g., haloperidole decanoate whose slow

diffusion from the muscle produce an extended
neuroleptic effect.
 Usually produce a faster effect than oral
administration
 The volume to be injected is < 10 ml
 The rate of absorption depends on the site of
injection and physiological factor at the site of
injection
 High blood flow at the site of injection
increase drug absorption 29
 Parentral route……Cont’d

Subcutaneous route (SC), where drugs are injected

into the subcutaneous layer of the skin.
 This is the easiest and least painful type of
injection to administer
It is used for administering aqueous solution and
specialized preparation
It requires absorption
Volume of preparations to be injected is smaller
than in IV and IM routes ( usually not more than
2 ml)
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 Parentral route……Cont’d

 Subcutaneous route (SC)…….

 Absorption of drug from the site of injection for both IM
and SC can be increased by massaging, heating and adding
an enzyme hyaluronidase
 The rate of absorption from IM and SC routes can be
reduced by:
 Minute amount of epinephrine are some times
administered combined with drug to restrict its area
of action.
Epinephrine acts as local vasoconstrictor and decrease
removal of drug such as lidocaine from the site of
administration.
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 Parentral route……Cont’d

 Advantage of parentral route:

 Useful to administer drugs in emergency
conditions
When patients are unconscious
In case when drugs are destroyed, inactivated or
poorly absorbed following oral administration.

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 Parentral route……Cont’d

 Disadvantages of parentral route:

 Irreversible
 Injected drugs cannot be recalled by
strategies such as emesis or binding to
activated charcoal
Painful and inconvenient

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 Respiratory/inhalation route
 Drugs are administered usually by inhalation
through the nose or mouth to produce either local
or systemic effects.
 Drugs are delivered in gaseous, aerosol mist or ultra
fine solid particle form.
 This route is used predominantly for local
administration to treat respiratory conditions such
as asthma.
 A major benefit of the respiratory route is that the
drug dose required to produce the desired effect is
much smaller than for the oral route, with a
consequent reduction in side-effects. 34
 Respiratory/inhalation route

 Importantly this route is being increasingly

recognized as a useful means of administering the
therapeutic agents emerging from biotechnology
requiring systemic distribution & targeted delivery,
such as peptides & proteins
 Because of the high blood flow to the lungs and
their large surface area, drug absorption by this
route is extremely rapid .

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 Topical route

 Drugs are applied topically, that is to the skin,

mainly for local action
 Application of drugs to surfaces such as the eye, ear
& nose are also regarded as topical administration
 Pharmaceutical topical formulations like ointments,
creams & pastes are composed of drug in a suitable
semi-solid base
 Drugs applied to the skin for local effect include:
antiseptics, antifungals, anti- inflammatory agents ,
skin emollients, protective agents, etc
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