Routes of Drug Administration 2023 PDF

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Routes of drug administration

Dr. Kiran Vakade


Professor and Head
Department of Pharmacology
DVVPF’s Medical College Ahmednagar
Routes of Drug Administration

• Routes of drug administration are the medium


through
which drug is administered into the body to
show its pharmacological action or for diagnosis.

• Most drugs can be administered by a variety of routes.

• The choice of appropriate route in a given


situation depends both on drug as well as patient related
factors.
Choice of route affected by following factors
( Factors governing route of administration)

1. Physical and chemical properties of the drug


(solid/ liquid/gas; solubility, stability, pH,
irritancy).
2. Site of desired action- localized and approachable
or generalized and not approachable.
3. Rate and extent of absorption of the drug from
different routes.
4. Effect of digestive juices and first pass metabolism
on the drug.
Choice of route affected by following factors
( Factors governing route of administration)

5. Rapidity with which the response is desired


(routine treatment or emergency).
6. Accuracy of dosage required (i.v. and inhalational
can provide fine tuning).
7. Condition of the patient (unconscious, vomiting,
diarrhoea etc)
Classification
Local Routes
Disadvantages of local route
• used to produce • Not always possible to apply
localized action a drug locally.
• used only for • Local irritation
localized lesion • Sometimes systemic
at accessible absorption and toxicity can
site occur.

Advantages of local route:


• Better concentration at the site of action.
• Faster onset of action
• Less quantity of drug is required.
• Systemic adverse effects are less or absent.
• Convenient to the patient (mostly)
Types Local Routes

• Topical
• Deeper tissue
• Intraarterial
Topical route

• Drug is applied to the surface (skin or


mucus membrane) for localised action.
• It is often more convenient as well as encouraging to
the patient.
• Examples
1. Ointments, cream, powder, lotion, paste are the
dosage form of the drugs applied on the skin to
produce local action. eg. Clotrimazole cream for
fungal infection, Diclofenac ointment, gel, spray for
joint pain..
Topical route

2. Mouthwash, lozenges, gargles; sprays are the


dosage forms used to produce local action on
mucus membrane of the mouth and throat.
Eg Chlorhexidine mouthwash as antiseptic and disinfectant,
2,4 dichlorobenzyl alcohol and amylmetacresol lozenges for
sore throat, Povidone iodine spray for sore thorat
3. Ointments, isotonic aqueous solution, occuserts are
used to produce local action in the eyes.
Eg. Acyclovir eye ointment for herpes infection,
Ciprofloxacin eye drops for bacterial infection, Pilocarpine
drops/ occusert for glaucoma
Topical route

4. Nasal drops and sprays are used locally in the nose


in allergic rhinitis. Xylometazoline spray for
congestion, Azelastine nasal spray for allergic
rhinitis
5. Ear drops used in the Ear . Clotrimazole ear drop
for fungal infection
6. Non-absorable drugs can be used locally to produce
local action in the git (eg- Sucralfate, neomycin).
Topical route

7. In bronchial asthma salbutamol/


beclomethasone/Na chromoglycate used by
inhalational route to produce local effect on
bronchi.
8. Suppositories are the solid dosage forms used to
produce local action at rectum, vagina, and urethra.
Vaginal suppository  Pessary, Urethral suppositories
Bougie
9. Enemata: Administration of medicament in the
liquid form into the rectum is called as enema.
Topical route

Examples of suppositories
• Vaginal suppositories:
Clotrimazole, Clotrimazole
and clindamycin
combination, progesterone
• Rectal suppositories:
Bisacodyl , Mesalamine
• Urethral suppositories:
Alprostadil
Topical route

Evacuant Enema Retention Enema

For evacuation of large bowel Fluid containing drug is retained in the


rectum to produce local or systemic
action
Amount of fluid used is aprox. 600 ml Amount of drug used aprox. 100-120 ml
Warm water, soap solution, glycerin can Local action : steroids are used in
be given Ulcerative colitis
Systemic action: Diazepam in status
epilepticus

Used for preparation of bowel in case of Use in UC and status epilepticus


abdominal surgery, before radiological
examination, before delivery
Dipper Tissue

• Certain deep areas can be approached by using a


syringe and needle, but the drug should be in such a
form that systemic absorption is slow.
• Examples:
 Intra-articular injection: (hydrocortisone acetate in knee
joint).
 Infiltration around a nerve or intrathecal injection
(lidocaine).
 Retro bulbar injection (hydrocortisone acetate behind the
eyeball).
Intra-arterial route

• It is rarely used route.


• Anticancer drugs can be infused in femoral or
brachial artery to localise the effect for limb
malignancies.
• Close intra-arterial injection is used for
contrast media in angiography.
Systemic Route

The drug administered through systemic routes is absorbed into


the blood stream and distributed all over, including the site of
action, through circulation.
Oral Route

• Oldest and commonest route of administration.


• Site: swallowing of a drug through mouth.
• Advantages of oral route:
1. Safer route (even if overdose/poisoning occur gastric lavage can be
done.)
2. No need of assistance  self administration .
3. Noninvasive
4. Painless
5. Medicament need not be sterile.
6. Cheaper
7. Convenient for repeated and prolonged use
8. Both solid dosage form (tablets, capsules, powders) and liquid dosage
forms (syrup, mixture, and elixir) can be given orally.
Oral Route

• Disadvantages of oral route:


1. Slower onset of action as absorption is slow. Not suitable
for emergencies.
2. Irritant and unpalatable drugs are difficult to administer
(drugs may be filled in capsule to circumvent this.)
3. May cause nausea and vomiting.
4. Cannot be used in uncooperative/unconscious / vomiting
patients.
5. Not suitable for unabsorbable drugs (e.g. streptomycin,
heparin etc.)
6. Some drugs are destroy by digestive juice (Penicillin G,
Insulin) or in liver (GTN, Testosterone)
Oral Route

• Examples of drugs given by oral route:


 oral hypoglycemic drugs like glibenclamide,
metformin
 oral anticoagulants like warfarin
• Precautions for oral route:
 Patient should be in upright position.
 Drugs should be taken with glassful of water
 Avoid certain drugs in recumbent position e.g. iron,
tetracycline, bisphosphonates
Sublingual/ Buccal route:

• Site: Drug is placed under the tongue or crushed in the mouth and spread
over buccal mucosa.
• Advantages:
 Rapid onset of action.
 Quick termination of the effect on spitting the tablet.
 Bypass first pass metabolism.
• Disadvantages:
 Lipid insoluble and high molecular weight drugs are not absorbed well
Ineffective
 Irritating drug cannot be given this route
 Not suitable for infants and children below 5 year
• Examples :
 GTN, Isosorbide dinitrate
Rectal Route

• Rectum has rich blood supply.


• Unionized, lipid soluble drugs rapidly absorbed.
• Advantages:
 Irritant and unpleasant drugs can be given
 Can be used in unconscious and vomiting patient.
• Disadvantages:
 Inconvenient, Embarrassing.
 Absorption is slower, irregular, and often unpredictable.
 Rectal inflammation can result from irritant drug.
• Examples: Diazepam, Indomethacin, Paraldehyde, Ergotamine
Parenteral
Parenteral Route

Advantages:
• Rapid onset of action in case of most parenteral routes
• Can be employed in unconscious or uncooperative patients.
• Can be employed in patients having vomiting and diarrhoea
and in patients who are unable to swallow.
• IV, IM are the preferred routes in emergencies.
• Drugs which are destroyed by gastric juice can be given
parenterally.
• Avoids drug modification by GIT and liver enzymes. (Bypass 1st
pass metabolism)
Parenteral Route

Disadvantages:
• Most parenteral routes are inconvenient for use
• Self-medication is being difficult in some of the parenteral
routes  help of assistance may be required. e.g. IV, IM
• Some parenteral route are less safe and liable to infection if
proper care is not taken. e.g. IV route
• More expensive
• Injuries to important structures such as nerves or arteries may
occur with some parenteral routes
Subcutaneous route

• Site: injection into the subcutaneous tissue under


the skin. Subcutaneous tissue is richly supplied by
nerves but is less vascular.
• Advantages:
 Absorption is smooth and uniform though slower as
compare to iv/im route.
 Depot preparation can be given.
 Self-injection is possible
 In paediatric practice saline injected sometimes
subcutaneously Hypodermoclysis.
Subcutaneous route

• Disadvantages:
 Only small volume can be injected by sc
route.(Maximum 2ml)
 Irritant drugs cannot be administered
• -because sloughing and necrosis can occur.(S.C.
tissues have poor blood supply)
• -Painful (S.C. tissues are richly supplied by nerves).
 Not suitable in shock.
• Examples: Insulin, LMWH
Some special forms of subcutaneous route:

• Dermojet:
 Gunlike instrument is used.
 Through a microfine orifice of it high velocity of drug solution
is projected across skin.
 The solution passes through the superficial layers and gets
deposited in the subcutaneous tissue.
 It is essentially painless and suited for mass inoculations.
• Pellet implantation:
 The drug in the form of a solid pellet is introduced with a
trochar and cannula. This provides sustained release of the
drug over weeks and months, e.g. DOCA, testosterone.
• Sialistic (nonbiodegradable) and biodegradable
implants:
 Crystalline drug is packed in tubes or capsules made
of suitable materials and implanted under the skin.
 Slow and uniform leaching of the drug occurs over
months providing constant blood levels.
 The nonbiodegradable implant has to be removed
later on but not the biodegradable one. This has
been tried for hormones and contraceptives
(Norplant)
Intramuscular route

• Site: Drug is injected in one of the large


skeletal muscles- deltoid, triceps, gluteus
maximus, (In children: Vastus muscle
underlying the lateral surface of thigh
because gluteus muscle is very tiny till child
starts walking)
Intramuscular route

• Advantages:
 Mild irritating drugs can be given by IM routes
because muscles are less richly supplied by nerves as
compared to sc tissue.
 Absorption of the drug in aqueous solution is faster
and more predictable compared to oral and sc route
because of the rich blood supply of muscles.
 Depot injections (oily solutions, aqueous
suspensions) can be given by IM route.
Intramuscular route
• Disadvantages:
 Perfect aseptic precautions needed
 Chance of abscess formation at the site of injection.
 Nerve may damage  paralysis may occur. eg. Sciatic nerve
(in buttock)  Foot Drop.
 Large volume cannot be administered. (Max. volume 10ml)
 Local haematoma when im injection given in anticoagulant
treated patient. Should be avoided.
 Local pain and necrosis
 Self-medication cannot be possible
• Examples: Diclofenac sodium, Benzathine penicillin,
procaine penicillin
Intravenous Route
• Site : through lumen of the vein
• A drug may be injected –
 As bolus: e.g. Furosemide  rapid action
 Over 5-10 min in 10-20 ml of isotonic saline or
glucose. e.g. Aminophylline, Ondansetron.
 In an infusion 50-100 ml or larger in volume.
- to slow the administration of drug.
- to maintain constant plasma concentration.
-to administered large volumes either rapidly or over
prolonged periods
Intravenous Route

• Advantages:
 As the drug enters in the systemic circulation (by passing the
first pass metabolism)
 - there is quick onset of action
 - less dose is required to achieve desired plasma conc.
 Titration of the dose is possible.
 Large volume of fluids can be infused at uniform rate.
 Highly irritant drugs can be given by iv because intima is
insensitive and drug gets diluted with blood.
Intravenous Route
• Disadvantages
 Strict aseptic conditions are needed.
 Very risky route  vital organs get exposed to high
concentration of the drug.
 Once injected  it cannot be recalled
 Depot preparations cannot be injected through iv
route  if given embolism can occur.
 Venous thrombosis and thrombophlebitis can occur
due to extravasation of blood.
Intravenous Route
Self-medication cannot be possible
Thrombophlebitis or necrosis of the adjoining
tissue may occur due to extravasation of the
drug this complication can be minimised by
diluting the drug or injecting it into running iv
line.
• Examples: Ondansetron, Aminophylline, ceftriaxone
etc.
Intradermal
• Site : given into the layer of skin (in-between
skin layer)
• Examples:
• BCG vaccine.
• Hypersensitivity testing.
Intramedullary
• Site: Injection into tibial/ sternal bone marrow
• Advantages:
• Onset of action is very fast as vascular spaces of bone marrow
mainly communicate with main vein.
• Disadvantages:
• Risky chances of infection
• Skill is required.
• Examples:
• Bone marrow transplantation
• Blood transfusion in children mainly when veins are not
getting
Intraperitoneal

• Mainly used in infants for giving fluids like glucose, saline as


peritoneum offers larger surface area for absorption.
• Advantages:
• Faster absorption.
• Disadvantages:
• Painful
• Chances of peritoneal infection and adhesions
• Strict aseptic condition is required.
• Use:
• Mainly used in children
• Also used for peritoneal dialysis in poisoning, ARF,CRF.
Transnasal
• Advantages:
 Liver is bypassed.
• Disadvantages:
 Toxic substances cannot be given by this route as it
may directly entre into the brain through lymphatics.
• Examples:
 GnRH analogues,
 Desmopressin,
 calcitonin
Transcutaneous

 Sites of applications: chest, abdomen, upper arm, lower back, buttock or


mastoid region.
Transcutaneous

adhesive patches of
• These are devices in the form of
various shapes and sizes (5–20 cm2) which deliver
the contained drug at a constant rate into
systemic circulation via the stratum corneum.
• The drug (in solution or bound to a polymer) is held in a
reservoir between an occlusive backing film and a rate
controlling micropore membrane.
• The under surface of this rate controlling micropore
membrane is smeared with an adhesive impregnated with
priming dose of the drug.
Transcutaneous

• The adhesive layer is protected by another film that is to be peeled off just before
application.
• The drug is delivered at the skin surface by diffusion for percutaneous absorption
into circulation.
Transcutaneous

• Advantages:
 More convenient (many patients prefer them over oral drugs).
 Patient compliance is better.
 Provide smooth plasma concentration of the offending drug
without fluctuation.
 Bypass first pass metabolism.
 Can be used in uncooperative and vomiting patient.
 Long duration of action
 Fewer side effects.
Transcutaneous

Disadvantages:
 Lipid insoluble and high molecular weight drugs
cannot be absorbed well by this route.
 Irritating drugs cannot be given by this route.
 Not suitable in emergency
• Examples: Transdermal patches of GTN, Fentanyl,
nicotine and estradiol are available in India, while
those of Isosorbide dinitrate, hyoscine, and clonidine
are marketed elsewhere.
Thank you!!!!!!!

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