RoD and Bioavailibility

ROUTES OF DRUG
ADMINISTRATION
dr. Siti Syarifah, M.Biomed
Faculty of Medicine
Universitas Prima Indonesia
Medan, 2017
STUDY OBJECTIVE
Know and understand routes of drug administration

Know the factors which determined route of drug
administration
Know the advantages and disadvantages every single
route
Can apply the theory for clinical application
ILUSTRASI KASUS
Seorang wanita, usia 25 tahun datang berobat ke

Klinik anda. Saat sedang memeriksa pasien lain,
anda tiba-tiba dipanggil karena wanita tersebut,
yang sedang menunggu antrian, terlihat pucat,
sesak dan memegang dadanya. Saat anda
mendekatinya, terdengar bunyi “ngik..ngik” saat
wanita tersebut bernafas. Di tas tangannya
dijumpai tablet salbutamol 10 mg dan juga
salbutamol spray tabung. Apakah tindakan yang
anda lakukan??
ROUTES OF DRUG ADMINISTRATION
A medicinal agent becomes a medication

only after formulation suitable for therapeutic use
(i.e., in an appropriate dosage form).
The route of administration (ROA) that is

chosen may have a profound effect upon the
speed and efficiency with which the drug
acts
Factors affecting choice of route
Physical and chemical properties of drugs.

Site of desired action
Rate and extent of absorption of drug from different
routes.
Effect of digestive juices and first pass metabolism.
Rapidity with which response is desired.
Condition of patient.
Accuracy of dosage required.
ROUTES OF DRUG
ADMINISTRATION
ENTERAL PARENTERAL TOPICAL

ENTERAL
ORAL
SUBLINGUA
L
BUCCAL
RECTAL
Oral Route
Oral refers to
two methods of administration:
 applying topically to the mouth
 swallowing for absorption along the gastrointestinal (GI) tract into
systemic circulation
po (from the Latin per os) is the abbreviation used to

indicate oral route of medication administration
ORAL
 Advantages
 Convenient - can be self- administered, pain
free, easy to take
 Absorption - takes place along the whole
length of the GI tract
 Cheap - compared to most other parenteral
routes
ORAL ROUTE-Cont’d
Disadvantages
 Sometimes inefficient - only part of the drug may be
absorbed
 First-pass effect - drugs absorbed orally are initially
transported to the liver via the portal vein
 irritation to gastric mucosa - nausea and vomiting
 Destruction of drugs by gastric acid and digestive juices
 Effect too slow for emergencies
 Unpleasant taste of some drugs
 Unable to use in unconscious patient
FIRST PASS EFFECT
The metabolism of orally administered drugs by

gastrointestinal and hepatic enzymes, resulting in a
significant reduction of the amount of unmetabolized
drug reaching the systemic circulation
ORAL DOSAGE FORM
Capsules
Tablets
Liquids
Solutions
Suspensions
Syrups
Elixirs
SUBLINGUAL ROUTE
Sublingual administration is where the dosage form is placed

under the tongue
 rapidly absorbed by sublingual mucosa
SUBLINGUAL ROUTE
ADVANTAGES DISADVANTAGES
 UNPALATABLE & BITTER

 ECONOMICAL
DRUGS
 QUICK TERMINATION  IRRITATION OF ORAL MUCOSA
 FIRST-PASS AVOIDED  LARGE QUANTITIES NOT
 DRUG ABSORPTION IS GIVEN
 FEW DRUGS ARE ABSORBED
QUICK
Ex: Nitroglycerine (Isosorbide dinitrate),

Nifedipine, isoprenaline
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
BUCCAL ROUTE
ADVANTAGES
– Avoid first pass effect
– Rapid absorption
– Drug stability
DISADVANTAGES
– Inconvenience
– advantages lost if
swallowed
– Small dose limit
Ex: Fentanyl
RECTAL ROUTE
ADVANTAGES DISADVANTAGES
 Used in children  Inconvenient
 Little or no first pass effect  Absorption is slow and
 Used in vomiting erratic
/unconscious  Irritation or inflammation
 Higher concentrations of rectal mucosa can occur
rapidly achieved
Ex: dulcolax, diazepam,
paracetamol (dumin®)
SYSTEMIC-PARENTERAL
Parenteral administration is injection or

infusion by means of a needle or
catheter 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
SYSTEMIC-PARENTERAL
19
 INJECTABLES
I. INTRAVENOUS (iv)
II. INTRAMUSCULAR (im)
III. SUBCUTANEOUS (sc)
IV. INTRA-ARTERIAL
V. INTRA-ARTICULAR
VI. INTRADERMAL (ic)
INHALATION - Absorption through the lungs

INTRAVENOUS
20
ADVANTAGES
 BIOAVAILABILITY 100% DISADVANTAGES

 DESIRED BLOOD
CONCENTRATIONS ACHIEVED  IRRITATION & CELLULITIS
 LARGE QUANTITIES  THROMBOPHLEBITIS
 VOMITING & DIARRHEA  REPEATED INJECTIONS NOT
 EMERGENCY SITUATIONS ALWAYS FEASIBLE
 FIRST PASS AVOIDED  LESS SAFE
 GASTRIC MANIPULATION  TECHNICAL ASSISTANCE
AVOIDED REQUIRED
 DANGER OF INFECTION
Ex: Normal Saline (Nacl  EXPENSIVE
0.9%), Glucose, dextrose,  LESS CONVENIENT AND PAINFUL
heparin, some antibiotics
INTRAMUSCULAR ROUTE
21
ADVANTAGES
 ABSORPTION
REASONABLY UNIFORM
 RAPID ONSET OF
ACTION
 MILD IRRITANTS CAN BE DISADVANTAGES
GIVEN
 FIRST PASS AVOIDED  LOCAL PAIN AND
 GASTRIC FACTORS CAN ABCESS
BE AVOIDED  EXPENSIVE
Ex: antibiotics, vaccine,  INFECTION
neuroleptics  NERVE DAMAGE
SUBCUTANEOUS
Injected under the skin.

Absorption is slow, so action is prolonged.
Ex: Insulin, vaccine

INTRADERMAL (INTRACUTAN)
 drug is given within skin layers

(dermis)
 Painful
 Mainly used for testing sensitivity
to drugs.
e.g. penicillin, ATS (anti tetanus
serum)
INOCULATION :administration of
vaccine (like small pox vaccine )
Intracutan
INTRA-ARTERIAL
Rarely used
Anticancer drugs are given for localized effects
Drugs used for diagnosis of peripheral vascular
diseases
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
 Lung
Topical Dosage Forms
Dose forms for topical administration include:

Skin:
 creams • Eye or ear:
 ointments – solutions
 lotions
– suspensions
 gels
 transdermal patches – ointments

 disks
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
absorption of drug through skin (systemic action)

i. stable blood levels
ii. no first pass metabolism
iii. drug must be potent or patch becomes too
large
Route for Administration
-Onset of action-
intravenous 30-60 seconds

inhalation 2-3 minutes
sublingual 3-5 minutes
intramuscular 10-20 minutes
subcutaneous 15-30 minutes
rectal 5-30 minutes
ingestion 30-90 minutes
transdermal (topical) variable (minutes to hours)
DOSAGE FORM
Route Bioavailibility Characteristics
IV 100% Rapid onset of action,
pain
IM 75-100% Large volume, followed by
pain
SC 75 - <100% Need less volume than
IM, pain
ORAL 5-<100% First pass effect is
(PO) intended
Rektal 30-<100% Less first pass effect than
(PR) oral
Inhalation 5-<100% Rapid onset of action
Transder 80- ≤ 100% Slow absorption, no first
mal pass effect, longer
duration of action
Seorang wanita, usia 25 tahun datang berobat ke
Klinik gigi anda. Saat sedang memeriksa pasien
lain, anda tiba-tiba dipanggil karena wanita
tersebut, yang sedang menunggu antrian, terlihat
pucat, sesak dan memegang dadanya. Saat anda
mendekatinya, terdengar bunyi “ngik..ngik” saat
wanita tersebut bernafas. Di tas tangannya
dijumpai tablet salbutamol 10 mg dan juga
salbutamol spray tabung. Apakah tindakan yang
anda lakukan??
TERIMA KASIH

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ROUTES OF DRUG

dr. Siti Syarifah, M.Biomed

Know and understand routes of drug administration

Seorang wanita, usia 25 tahun datang berobat ke

A medicinal agent becomes a medication

The route of administration (ROA) that is

Physical and chemical properties of drugs.

ENTERAL PARENTERAL TOPICAL

po (from the Latin per os) is the abbreviation used to

The metabolism of orally administered drugs by

Sublingual administration is where the dosage form is placed

 UNPALATABLE & BITTER

Ex: Nitroglycerine (Isosorbide dinitrate),

Parenteral administration is injection or

INHALATION - Absorption through the lungs

 BIOAVAILABILITY 100% DISADVANTAGES

Injected under the skin.

Ex: Insulin, vaccine

 drug is given within skin layers

Dose forms for topical administration include:

 transdermal patches – ointments

absorption of drug through skin (systemic action)

intravenous 30-60 seconds

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