Sources of medicines

Natural
Synthetic
 Natural sources
 1. Plants :
Alkaloids eg.morphine,
atropine,quinine,reserpine, ephedrine
Glycosides eg Digoxin, digitoxin
 2. Animals : eg Insulin, Thyroxine
 3. Minerals : Ferrous sulphate, Mg sulphate
 4 : M/O : Penicillin, Streptomycin,
Griseofulvin
 5. Genetic engg : eg Human insulin, human
growth hormone
Synthetic Source
Recombinant DNA Technology
 Routes of Drug Administration
Important
Info

The route of administration (ROA)

that is chosen may have a profound
effect upon the speed and efficiency
with which the drug acts
 Important
Info

The ROA is determined by :

1. the physical characteristics of
the drug.
2. the speed which the drug is
absorbed and/ or released,
3. the need to bypass hepatic
metabolism and achieve high
conc. at particular sites
Factors governing choice of route
 Physical & chemical properties of the drug(solid/liquid/gas,:
solubility,stability,ph,irritancy).

 Site of desired action-localized &approachable or generalized

& not approachable.

 Rate & extent of absorption of the drug from different routes.

 Effect of digestive juices & first pass metabolism on the drug.

 Rapidity with which the response is desired{routine treatment

or emergency}.

 Accuracy of dosage required{I.v. & inhalational can provide

fine tuning}.
 Condition of the patient{unconscious,vomiting}
Routes of Drug administration

Local Action Systemic Action

Deeper Arterial
Topical Supply
tissues
 Local
 Only be used for localized
lesions.
 Drug is administered where
the desired action is required.
 Used for drugs whose
systemic absorption is
minimal /absent.
 Systemic side effects are
minimal/absent
 High concentration attained
at the desired site without
exposing rest of the body.
Systemic
 Drug intended to be
absorbed into blood
stream and distributed
all over including site of
action.
 Drug is distributed to the
site of action through
circulation.
 Drug produces systemic
effects.
Topical Route
Refers to external application of the drug to
the surface for localised action.
More convenient & encouraging to patient.
Efficiently delivered to localised lesions
on : Skin, Oropharyngeal/nasal mucosa,
eyes, ear canal, anal canal, vagina.
Dosage forms include : lotion, ointment,
cream, powder, rinse, paints, drops, sprays,
lozenges, suppositories, pessaries.
 Types of Bougies

Suppositories

Pessaries of different sizes

Egs of topical route
Non-absorbable drugs given orally for
action on g.i.t. mucosa eg. Sucralfate
(anti-ulcer), Neomycin (for sterilization of
gut before surgery)
Inhalation of drugs for action on bronchi:
eg. Salbutamol, Ipratropium bromide (for
asthma)
Irrigating solutions/jellys on urethra eg.
Lidocaine, Povidone iodine. Bougies are
also available for urethral use
Topical Route

.Skin : Drug is applied as ointment,

cream, lotion, paste, powder,dressing,
spray etc

Mucous membranes;
Mouth & Pharynx: as paints, lozenges,
mouth-washes , gargles.
 Topical Route :
Eye, ear& nose :
as drops, ointments, sprays for infection & allergy
Ointments , drops are applied, instilled onto the
conjunctiva for local effects.
Eg : Gentamicin, Chloramphenicol, Ciprofloxacin,
Sulfacetamide.
Ear drops/ nasal drops

Vaginal : as pessaries, vaginal tablets, cream, inserts,

powders, douches
• Eg : Anti-fungal agents used for local application into
vagina.
Deeper Tissues
Deeper tissues can be reached by using syringe
& needle :

Used with drugs whose systemic absorption is

slow.
Eg : Intra-articular inj. (hydrocortisone acetate)
Infiltration anaesthesia (with local anaesthetics)
Intrathecal injection ( lidocaine)
Retrobulbar injection (hydrocortisone acetate)
Intra-articular route
Injection directly into the joint space.
Ensures higher concentration of the drug
in a localised area.

Disadv;
1. Strict aseptic conditions are needed.
2. Painful procedure
3. Repeated administration ---further
damage the joint.
111````````````

Drugs adm:
Hydrocortisone inj. Or gold chloride inj. for the
treatment of rheumatoid arthritis.

It provides local effects of the drug.

Retrobulbar
Injection
Infiltration
anaesthesia
 Arterial supply/ Intra-arterial
 Drug injected into the lumen of desired artery.
 Route mainly provides local effects.

Adv:
1. Greater conc. Of the drug can be delivered at the site of inj.
Disadv:

1. Great expertise reqd & aseptic conditions needed.

Drugs adm:
 radiopaque contrast media for coronary angiography &
cerebral angiography.
 Anti-cancer drugs can be infused in femoral/brachial artery for
localized effect for limb malignancies like nitrogen mustard
perfused through artery to treat malignancy involving limbs.
Enteral Parenteral Topical

Routes

2nd way of Classification of routes

 Enteral
 Placement of a drug directly into any part of git.
(a) Oral
(b) Sub-lingual
(c) Rectal
 Parenteral
Routes other than enteral (intestine)are called
parenteral route .
 Admin. By injection, by inhalation through lungs &
by any other route that bypasses enteral(intestine) are
parenteral.

Topical :
conjunctival, vaginal, urethral , inunction (rubbing)
etc.
Oral
Drug is taken by mouth ( swallowing of drug through
mouth)
Drug has to pass through git & intestine
Most commonly used
Advantages
◦ Most Convenient - can be self- administered.
◦ Pain free, safer route
◦ easy to take
◦ Economical
◦ Not involving any medical procedure.

◦ Both solid dosage form & liquid dosage form can be taken
Demerits/ Disadvantages of Oral route

 Slower onset of action (absorption being slow) not suitable for

emergency.
 Unpalatable i.e bad taste. Drugs are difficult to administer.
 May cause nausea & vomiting.
 Can’t be used for un-cooperative/unconscious/vomiting patient
 Some highly polar drugs eg Streptomycin cannot be absorbed &
thus can’t given orally.
 Drugs that are destroyed by digestive juices can’t be given .
eg Insulin by proteolytic enzymes , Penicillin G by Hcl.
 Drugs that gets destroyed in liver can’t be given eg. Nitroglycerine ,
Lidocaine.
• Irritant drugs can’t be given by oral route. irritation to gastric
mucosa - nausea and vomiting
• Can’t be used while preparing for anaesthesia/ or who had git
First-pass effect
drugs absorbed orally are transported to the general
circulation via the liver.
Some amount of drug is degraded in the way before
reaching systemic circulation. This is called 1 st pass
effect or Pre-systemic metabolism.
The greater the first-pass effect, the lesser the
drug will reach the systemic circulation when the
drug is administered orally.
1st pass effect/ pre-systemic metabolism
Position of hepatic vein & portal vein
 Oral Preparations
Enteric Coated preparations :
tablets coated with such polymers that
resist the action of fluids & enzymes in the
stomach, but dissolves readily in intestine.
Coating useful for drugs that are acid
unstable Eg : Omeprazole
Useful for drug that are gastric irritants eg.
Aspirin
Retards the absorption of the drug.
Controlled Release
Preparations/spansules

Release the active drug over an extended

period of time.
They have particles of drug covered with
coatings which dissolve at different time
intervals.
Provides uniform medication over a
prolonged time.
Sub-lingual route
S/L & Buccal route
 Thedrug is placed beneath the tongue or crushed in the
mouth & spread over buccal mucosa.
Adv:
1. Quick onset of action: within minutes.
2. Avoids 1st pass effect: Drug passes directly into systemic
circulation , bypassing portal circulation.
3. Drug can be spitted out if side effects seen.

Drugs given s/l: Nitroglycerine ( anti-anginal) ,nifedipine,

iso-sorbide di-nitrate tabs.
Buccal : anti-septic lozenges providing local effect.
S/l disadvantage
Inconvinient
Irritant drugs cannot be given. Only non-
irritating drugs can be given.

Only lipid soluble drugs can be given.

Drugs of high M.W are not well absorbed

by this route.
 Rectal administration
 Site : Through rectum as
suppository/enema.

 Adv:
1. Used for patients having nausea & vomiting
2. Useful for gastric irritant drugs also.
3. First pass effect is largely bypassed as a
major portion of drug is absorbed from
external haemorrhoidal veins.

Note :(Drug absorbed in internal haemorrhoidal

veins do not bypass liver )
Disadvantages
Very inconvenient
Absorption is unreliable & un-predictable
Embarassing to the patient
Chances of rectal inflammation

Drugs given by rectal route:

(a) For local effect : Dulcolax & glycerine
suppositories
(b) For systemic effect:
Indomethacin suppositories (anti-inflammatory ),
:Aminophylline (bronchodilator) etc.
Enema : administration of a medicament
in liquid form into rectum.

Evacuant enema : eg. Soap water enema.

The aim is to remove the foecal matter.
Soap acts as lubricant & water stimulates
rectum by distension.
Qty administered. : 600ml
Used in treating constipation,
Given before surgeries, delivery &
radiological investigation of git.
Retention enema :
The fluid containing drug is retained in
the rectum .
Qty admn. : 100-120ml.
Eg : prednisolone enema for ulcerative
colitis for local action.
May act systemically after absorption
through mucous membrane.
Parenteral Routes
1. Intravenous (I/V)
2. Intramuscular (I/M)
3. Subcutaneous (S/c)
4. Intraperitoneal (I/P)
5. Intrathecal/ Intraspinal (for local &
systemic effects)
6. Intra-medullary
7. Intra-arterial ( for local effects)
8. Intra-articular (for local effects)
 Parenteral
Par : beyond , enteral : intestine
Refers to administration by injection which takes the
drug directly into tissue fluid or blood without crossing
the intestinal mucosa.
Adv:
1. Action is faster & surer. Thus valuable in emergencies.
2. Gastric irritation & vomiting is not provoked.
3. Can be employed in unconscious, uncooperative or
vomiting patients.
4. No chances of interference by food or digestive
juices .
5. Liver is bypassed(avoided)
Disadv. Of Parenteral route
Preparation has to be sterilized & is
costlier.
Technique is invasive & painful.
Assistance of another person is mostly
needed.( except insulin inj. that can be
taken by self)
Chances of local tissue injury .
More risky.
.
Intravenous (I/V)
Drug is injected directly into the vein.
 Drug enters directly into systemic circulation. It
bypasses 1st pass effect.
 intravenous route is the fastest way to deliver fluids
and medications throughout the body.
 Provides systemic effects
 100% bioavailability
 Greater risk of adverse effects
 a. high concentration attained

rapidly
 b. risk of embolism
Adv:

Advantages of I.V
1. Precise, accurate and almost immediate onset of action.
Valuable in emergencies.
2. large quantities can be given.
3. Can be used in un-conscious & un-cooperative patients.
Can be used in those having nausea,vomiting &
diarrhoea.
4. Route avoids destruction of the drug by gastric juices &
intestinal juices.
5. Avoids destruction by liver enzymes.
6. Large volumes of fluids can be infused through this
route.
eg dextrose, normal saline, anti-biotics , barbiturate
anaesthetics , diazepam , heparin etc.
7. Hypertonic solutions & git irritants can also be infused
by this route.
8. Amount of drug can be controlled with an accuracy not
 Disadvantages of I.V Route
1. Strict aseptic conditions are needed.
2. Drugs in suspension or oily drugs cannot be given. No
depot injections available for this route.
3.Patient to depend on someone for an injection
4. Painful
5. Risky as once injected, can’t be retrieved.
6. Introduction of any particulate matter or air may produce
embolism which may be fatal .
7. Intense irritation of vein may lead to thrombophlebitis .
( Thrombophlebitis is a condition in which blood clots form
abnormally in veins, usually the veins of the legs)
8. Necrosis around the site of injection can result if
extravasation occurs.
I.M route
Drug injected into one of the large
skeletal muscles.
Eg gluteus maximus, deltoid, triceps
muscles.
Provides systemic effects
Adv of I.M. route
1.rate of absorption is uniform & onset is
quick as compared to oral route.(muscle is
more vascular)

2.Depot injections can be given for obtaining

sustained effects.

3. Mild irritants ,suspensions, colloids can be

injected by this route. (as muscle are less
richly supplied by nerves)
 Disadv. of I.M. route
1. pain & abscess formation at the site of injection.
2. volume injected should not exceed 10ml
3. Self –administration not possible as deep penetration
required.
4. Perfect aseptic conditions are needed.
5. Care to be taken while injecting the drug to avoid injury
to underlying nerves.
Thus chances of nerve damage weakness of muscle
supplied by that nerve.

Drugs adm.: anti-biotics, antiemetics,

depot inj. Of testosterone,& neuroleptics.
Sub-cutaneous route
Drug is injected into loose sub-cutaneous
tissue.
A small amt of drug (2ml or less ) injected
under the skin.
 Adv of s/c route
1. Route is reliable.
2. Self –administration is possible as deep
penetration not needed.
3. Smooth absorption but slower for a
longer period as compared to IV or IM.
Thus slow and constant absorption
4. Depot injections can also be given.
. Disadv:
Since the s/c tissue is richly supplied by nerves,
irritant drugs can’t be injected.
Tissue being less vascular, absorption is slower than
i/m.
 Absorption is limited by blood flow & it is affected if
circulatory problems exist
Not suitable in the states of shock as decreased
peripheral circulation decreases the rate of
absorption.
concurrent administration of vasoconstrictor will
slow absorption.
Drugs administered by s/c are :
Insulin ( for systemic effects)
Local anaesthetics (for local effects)

 Vaccines are given as the active protein

reaches the lymphoid tissue directly
through lymphatics without getting
destructed elsewhere in the body.
Related routes of S/c are:
Intradermal route (intracutaneous route):
Drug is injected into the outer layers of the
skin.
 Amt of drug given is small.
 Absorption is slow.
 A tuberculin syringe is used to give the
injection.
 A bleb is raised.
eg : BCG inj., diagnostic tests & allergy
sensitivity testing in patients.
Dermojet injection
A s/c needleless injection of a drug.
In this method, a high velocity of drug sol. is
projected from a fine orifice using a gun.
Solution gets deposited in s/c tissue.
Painless procedure used for mass inoculations
Pellet implantation
Drug as a solid pellet is implanted under
the skin to provide a uniform but slow
release of a drug lasting over months.
Drug introduced with trochar
and cannula.

Eg testosterone & Contraceptive implants

( for systemic effects)
Sialistic (non-biodegradable )and biodegradable
implants
Crystallinedrug is packed in tubes
/capsules made of suitable materials &
implanted under the skin.
Provides slow & uniform leaching of
drug.
Non-biodegradable implant has to be
removed.

Eg : NORPLANT (Levonorgestrel)

contraceptive.
Intraperitoneal route
Intraperitoneal route
 Insidethe peritoneal space.
 Provides systemic effects

 Most commonly used procedure for administering drugs

in lab animals.
 Provides rapid absorption due to large surface area.
 Used for giving fluids like glucose & saline to
infants .
 Used for giving anti-rabies injection
 Used for peritoneal dialysis in case of poisoning &
renal failure.
Intra-thecal/intraspinal route
Drug is injected into the sub-arachnoid space of
spinal cord.
Drug acts directly on meninges & CNS.
A specialized procedure.

Demerits
Strict aseptic conditions needed.
Great expertise is needed to give such injections.
Painful & risky procedure.

Drugs adm.: Local anaesthetics for spinal

anaesthesia, certain antibiotics, corticosteroids
Intra-medullary
Injection directly into tibial or sternal
bone marrow.
Rarely used or reqd.
Blood has been given to children into
tibia or femur .
No adv over other routes.
Intra-cardiac injection
Inj. Given by a long needle into the heart
muscle (ventricular chamber)
It is through the 4th intercostal space between
the ribs close to sternum.
Used only if other treatment approaches
become ineffective.

Drugs adm: inj. of adrenaline to restart the

heart beat in case of cardiac arrest. (local
effect)
 Epidural injection
Drug is injected through a vertebral
interspace between the dura of spinal cord &
lining of spinal canal.
Epidural analgesia is used to relieve pain in
labour.
Inhalation
Volatile liquids & gases are given by inhalation.
Eg general anaesthetics, bronchodilators
Absorption takes place from the vast surface of
alveoli of the lungs.
Adv:
 Action is very rapid & controlled.
 When administration is discontinued , drug
diffuses back & is rapidly eliminated in expired
air.
 Self-administration is also possible.
 Faster absorption, thus quick onset of action.
 Disadv of Inhalation
 Irritant
vapours can cause inflammation of resp tract &
increase secretions.

 Reaching/ retaining of the drug in alveoli depends upon

particle size of the drug.
Particles >1um in diam. tend to settle in bronchioles/bronchi
Particles < 0.5um fail to settle & mainly are exhaled.
Inhalation
Used when purpose of adm. is action of
the drug on resp. tract itself.

Drugs adm: Oxygen & general

anaesthetics inhalation (systemic effect)

Metered aerosol prep. Of Salbutamol,

Isoprenaline for treatment of bronchial
asthma .(For local effect)
Cutaneous Route
Used for highly lipid soluble drugs for slow &
prolonged absorption.
Drug is incorporated in an ointment & applied over
specified area of skin.

Transdermal Delivery systems are recent developed

devices in the form of adhesive patches. (Diag )
Contained drug is delivered at a constant rate into
systemic circulation via stratum corneum {outermost
layer of skin }.
Drug gets absorbed through skin into circulation by
diffusion.
Adv of Cutaneous route
 Transdermal - absorption of drug through skin (systemic
action)
 Provides stable blood levels. Provide a smooth plasma
conc. without fluctuation.
 Drug is delivered at a constant & predictable rate
irrespective of site of application-chest abdomen upper
arm, back, buttock.
 Liver is Bypassed. no first pass metabolism
 Better Patient compliance.
 More convenient.
 Transdermal patches have been designed to last 1-7 days
in case of different drugs.
 In case of unwanted effects , it can be easily removed.
 Transdermal Patch
1. Occlusive backing film
2. Drug reservoir (drug as in sol.)
3. rate controlling micropore memb.
4. adhesive (sticky)layer with a loading dose.

Adhesive layer is protected by another film that

is to be peeled off just before application.
Drug held between backing film & membrane.
Drug is delivered at skin surface by diffusion,
absorbed into circulation.
Disadvantages of Cutaneous route
Local irritation& erythema (redness ,
inflammation) can occur in some but
generally mild.
This can be minimised by changing site
of application each time by rotation.

Drugs adm : Nitroglycerine (for angina),

Estradiol, Nicotine , Testosterone.
Scopolamine (for motion sickness)
Nasal Route
 Formulation applied as snuff or spray or nebulized
sol. Through nose.
Adv:
1. Mucous memb. Of nose can readily absorb drugs
2. Large mol. Wt drugs can be administered.
3. Digestive juices & liver is bypassed.
Disadv : A toxic substance should not be administered
as it may reach brain.

Drugs adm: Posterior pituitary powder , desmopressin

(ADH) for diabetes insipidus.
 Route for administration
-Time until effect-

intravenous 30-60 seconds

intramuscular 10-20 minutes
subcutaneous 15-30 minutes

inhalation 2-3 minutes

sublingual 3-5 minutes
rectal 5-30 minutes
ingestion 30-90 minutes
transdermal (topical) variable (minutes to
hours)
 Topical Route :
already dealt in local route
A few definitions related to topical route
Inunction : Rubbing of the drug preparation
on the surface of skin.
 Adv: Safe & Convenient.
 Disadv :
 1. Difficulty in finding out the amt. of drug absorbed.
 2. Systemic absorption may occur :

(a) If the skin has abrasions or (b) if the drug is highly lipid
soluble.
Drugs adm: Various antibiotic-antifungal ointments ,powders & solutions, lotions,
liniments, creams & ointments for their anti-septic, anti-pruritic & analgesic
effects locally.
Iontophoresis
Itis possible to apply a drug to the skin &
then drive it into deeper tissues with the
help of electric current. This is called
iontophoresis.
 r t an t
Im p o
Very fo!
In

No single method of drug

administration is ideal for all
drugs in all circumstances
THANK YOU
 Depot Preparation
 Itis a special preparation of the medication, which is given by
injection .
 usually subcutaneous or intramuscular ,
 The active drug is slowly released into the body
over a number of weeks.
 prolonged by using insoluble salts or suspensions
in non-aqueous vehicles.
 Examples of depot injections include:
 Depo Provera ( long acting reversible
hormonal contraceptive birth control drug that is
injected every 3 months and
 haloperidol decanoate.
FAQ’s
. Difference between local route & systemic route?
 Local route:
 is used for localized lesions at accesible sites. High conc. are
attained at the desired site without exposing rest of the body.
 Used for drugs whose systemic absorption from these sites is
minimal/absent.
 Thus systemic side effects are absent.
 These are topical , intra-articular inj.,intra-arterial inj.

 In Systemic Route : the drug administered is intended to be

absorbed into the blood stream & distributed all over
through the circulation incl. the site of action.