MOHAMMAD SAFIQUL ISLAM

:Definition
A route of administration is the path by which a
drug, fluid, poison or other substance is brought into
.contact with the body
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
:Topical route -1
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) 
:Oral route -2
.By swallowing -
It is intended for systemic effects resulting from drug -
absorption through the various epithelia and mucosa
.of the gastrointestinal tract
2 -Oral route (Cont.)

Advantages:
1- Convenient - portable, no pain, easy to take.

2- Cheap - no need to sterilize, compact, multi-dose bottles,

automated machines produce tablets in large quantities.

3- Variety - tablets, capsules, suspensions, mixtures .

 2- Oral route (Cont.)
:Disadvantages
Sometimes inefficient - low solubility drugs may suffer -1
poor availability e.g. Griseofulvin

2- First-pass effect - drugs absorbed orally are

transported to the general circulation via the liver. Thus
drugs which are extensively metabolized will be
metabolized in the liver during absorption. e.g.
propranolol
:First pass effect
First pass effect
:First pass effect
 First pass effect (Cont.):
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 lower the -

bioavailability of the drug(the rate and extent of the
.drug reaching systemic circulation)
2-Oral route (Cont.):

Food - Food and G-I motility can affect drug -3

.absorption
Often patient instructions include a direction to take with
.food or take on an empty stomach

Absorption is slower with food(milk and milk products) -

for tetracyclines and penicillins, etc. However, for
propranolol bioavailability is higher after food, and for
.griseofulvin absorption is higher after a fatty meal
 2- Oral route (Cont.)
Sometimes may have adverse reactions – e.g. -4
Antibiotics may kill normal gut flora and allow
overgrowth of fungal varieties. Thus, antifungal agent
.may be included with an antibiotic
Not suitable for unconscious patient - Patient -5
must be able to swallow solid dosage forms. Liquids
.may be given by tube
2-Oral route (Cont.)
May cause irritation to gastric mucosa, nausea and -6
.vomiting
.Effect too slow for emergencies -7
:Buccal/Sublingual route -3

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
3- Buccal/Sublingual route (Cont.)
Advantages
Avoid hepatic first pass - The liver is by-passed thus -1
there is no loss of drug by first pass effect for buccal
.administration. Bioavailability is higher
Rapid absorption - Because of the good blood supply to -2
.the area, absorption is usually quite rapid
Drug stability - pH in mouth relatively neutral (gf. -3
.stomach - acidic). Thus a drug may be more stable
 3- Buccal/Sublingual route (Cont.)

Disadvantages
.Holding the dose in the mouth is inconvenient -1

.Small doses only can be accommodated easily -2

:Parenteral route -4
4- Parenteral route (Cont.)

:A- Intravascular (IV, IA)

.placing a drug directly into blood stream -
May be - Intravenous (into a vein) or - intraarterial (into an-
.artery)

Advantages
precise, accurate and immediate onset of action, 100% -1
.bioavailability

Disadvantages
.risk of embolism -1
high concentrations attained rapidly leading to greater risk of -2
.adverse effects
Parenteral route (Cont) -4
.B-Intramuscular :(into the skeletal muscle)
Advantages
suitable for injection of drug in aqueous solution (rapid -1
action) and drug in suspension or emulsion (sustained
.release)
Disadvantages
.Pain at injection sites for certain drugs -1
4- Parenteral route (Cont)

.insulin .C- Subcutaneous (under the skin), e.g

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 insuffeciency
:Rectal route-5
.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

 5- Rectal route (Cont.)

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

.Not well accepted -2

:Inhalation route -6
.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
 6- Inhalation route (Cont.)
Disadvantages
Most addictive route of administration because it hits the -1
.brain so quickly

.Difficulties in regulating the exact amount of dosage -2

Sometimes patient having difficulties in giving -3

.themselves a drug by inhaler
Vagina

used to treat vaginal infections and vaginitis with

creams and suppositories, e.g. Monistat suppositories,
Premarin vaginal cream; also route of administration
for vaginal contraceptive foams and gels
 Route for administration
-Time until effect-

intravenous 30-60 seconds

intraosseous 30-60 seconds
endotracheal 2-3 minutes
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)
 PHARMACOGENETICS

Pharmacogenetics can be described as the study of

individual genetic profiles in response to
pharmaceuticals.
It is the study of how individual genetic differences
affect drug responses. It may enable us to personalize
medicine by delivering the correct drug at the correct
dosage to the correct patient at the correct time.
 PHARMACOGENETICS
A Single Nucleotide Polymorphism is a source of variance in a
genome. A SNP ("snip") is a single base mutation in DNA.
SNPs are the most simple form and most common source of
genetic polymorphism in the human genome (90% of all
human DNA polymorphisms).
There are two types of nucleotide base substitutions resulting
in SNPs:
 
A transition substitution occurs between purines (A, G) or
between pyrimidines (C, T).
This type of substitution constitutes two thirds of all SNPs.
A transversion substitution occurs between a purine and a
pyrimidine.
Every SNP has a reference number.
 GENETIC POLYMORPHISM

Genetic polymorphisms are natural

variations in the DNA sequence present in
at least or more than 1% of the population.

Almost 90% genetic changes are due to

single nucleotide polymorphisms (SNPs)
with the remainder of the variation caused
by insertions and deletions (indels),
sequence repeats and recombination.
 GENETIC POLYMORPHISM

It is the science of understanding the correlation between an

individual patient's genetic make-up (genotype) and their response
to drug treatment. Some drugs work well in some patient
populations and not as well in others.
For example, one in every 2000 Caucasians carries a genetic
alteration in plasma enzyme choline esterase, which metabolizes
the muscle relaxant succinylcholine. This altered form of the
enzyme has an approximately 1000- fold reduced affinity for
succinylcholine, resulting in slowed elimination and prolonged
circulation of the active drug. This leads to the respiratory
paralysis and ultimately death of the patient unless supported with
artificial respiration until the drug is cleared.
 GENETIC POLYMORPHISM
Isoniazid which is used in the treatment of tuberculosis is
metabolized by N-acetyl transferase (NAT2). Due to
polymorphism in NAT2 the percentage of slow acetylators in the
population varies with ethinic origin ranging from 90% in North
Africans to less than 10% in many Asian populations with a
frequence 50% in white. If the dose of Isoniazid is not adjusted in
slow acetylators there will be potential toxic effect due to high
blood concentration of Isoniazid.
 
 
S

tudying the genetic basis of patient response to therapeutics

allows drug developers to more effectively design therapeutic
treatments.