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Routes of drug administration
Dr. M. Ahsan (MBBS, MD)
Types
Routes of administration
Local Systemic
Local route
• Site of action is same as site of
administration
• Absorption of drug from this site into
systemic circulation is minimal or absent
• Side effects are minimal
Local routes
• Topical
• Deeper tissues
• Arterial supply
Topical
External application of the drug to surfaces for
localized action
 On skin
 Nasal mucosa
 Oralmucosa
 Eyes
 Ear canal
 Anal canal
 Vagina
 Non-absorbable drugs given orally
 Inhalation of drugs for local action on bronchi
Deeper tissues
• Deep areas can be reached with the help of a
needle…..
• But absorption of drug from this site is
minimal
• Drug acts only locally at the site of
administration
Deeper tissues
Intra-articular injection
Intra-thecal injection
Inra-lesional injection
Intra-cardiac
Retrobulbar injection
Infiltration around a nerve
Arterial supply
• Contrast media in angiography
• Chemotherapy of limbs
Systemic routes
• Oral
• Sublingual
• Rectal
• Transdermal
• Inhalation
• Nasal
• Parenteral
Oral route
• Most commonly employed
• Advantages :
 Most convenient, safe & economical
 Non-invasive
 Painless
 Self administration is possible
 Drugs need not be highly purified
 Adverse effect if any, appears slowly
Oral route
• Disadvantages:
 Slowly absorbed; so slow onset of action
 Not useful in unconscious, uncooperative patients & in
patients with vomiting
 Unpalatable drugs are difficult to administer
 May cause nausea and vomiting
 Drugs which are either inactivated in gastic juice or not
absorbed or metabolised extensively in the gut & liver
(first-pass metabolism) cannot be given
 pH of the gut, presence of food or other drugs and
motility of gut interferes with absorption
Sublingual route
• Drug is placed under the tongue
• It can be crushed and spread over the buccal
mucosa
• Only lipid soluble and non-irritant drugs can
be administered
 The drug is rapidly absorbed through highly vascular
buccal mucosa directly into systemic circulation
Sublingual route
• Advantages:
 Rapid onset of action; so can be used in emergency
 Self-administration possible
 Degradation in the gut and liver, ie first-pass
metabolism is bypassed
 After the desired effect is reached, remaining drug
can be discarded
Sublingual route
• Disadvantages:
Irritant and distatesful drugs cannot be
administered
Glyceryl trinitrate
Nifedipine
Buprenorphine
Rectal route
• Enemas, suppositories and ointments can be
administered by the rectal route
Advantages:
50% of the absorbed drug bypasses first-pass
metabolism
Useful in case of vomiting or unconscious
patients
Rectal route
Disadvantages:
 Rectal absorption is often erratic and
incomplete
 Drugs may irritate the rectal mucosa
 It is embarassing
Diazepam – in case of convulsions
Paracetamol suppository
Transdermal patch
Transdermal route
• Mostly used for sustained delivery of the drug
• Highly lipid-soluble drugs can be absorbed through the
skin to achieve systemic effects
• Absorption can be increased by applying drugs as
ointments, rubbing and occlusive dressing
• Transdermal therapeutic systems (TTS) deliver the drug
at a constant rate
Transdermal patch
Transdermal patch
• These are medicated adhesive patches that deliver the
drug into blood stream at a controlled rate
• Come in various shapes and sizes (5-20 sq.cm)
• The patch is applied over the chest, abdomen, upper
arm, lower back, buttock, mastoid region
• Lasts for 1-3 days
Transdermal patch
• Advantages:
 Convenient and painless
 Bypasses first pass metabolism
 Ideal for drugs that are lipophillic and
require prolonged administration
Transdermal patches
• Disadvantages:
 Some patients are allergic to patches, may cause
irritation – (change the site of application)
 More expensive
 Can be used for only few drugs which are highly lipid-
soluble
Transdermal patches
• GTN patches
• Nicotine patches
• Fentanyl patches
• Scopolamine patches
Inhalation
• Volatile liquids or gases are given by inhalation for
systemic action – eg. General anesthetics
• Absorption takes place from the surface of alveoli –
action is rapid
• When drug is discontinued, it diffuses back from the
blood into the alveoli and is exhaled out
• Thus, controlled administration is possible
• Irritant vapors can cause inflammation of respiratory
tract
Nasal
• Drug is absorbed from the nasal mucosa
• Bypasses gastric juices and first-pass
metabolism
Desmopressin spray – diabetes insipidus
Calcitonin spray - osteoporosis
Parenteral route
• Subcutaneous
• Intra-muscular
• Intra-venous
• Intra-dermal
Parenteral routes
Parenteral routes
• Advantages:
 Drug action is rapid
 Gastric irritation and vomiting is not induced
 Can be used in unconscious, uncooperative and
vomiting patients
 No interference with food or digestive juices
 No first-pass metabolism
Parenteral routes
• Disadvantages :
 Preparation has to sterilized- so expensive
 Technique is invasive
 Painful
 Assistance is required
 Chances of local tissue injury
 Adverse effects are more
Subcutaneous route
• Drug is deposited in loose connective tissue
• This tissue is richly supplied by nerves
• Subcutaneous tissue is less vascular
Thus,
 Irritant drugs cannot be given
 Absorption is slower
 Only small volumes can be injected s.c
 Self-injection is possible
 Depot preparations can be given
Subcutaneous route
Special forms of s.c route:
Dermojet
High velocity jet of drug solution is projected from microfine
orifice using a gun. Solution passes through the superficial
layers and gets deposited in subcutaneous tissue
….painless
...mass innoculations
Pellet implantation
Solid pellet is introduced with trochar and cannula
…sustained release of DOCA, testesterone
Subcutaneous route
Sialistic (nonbiodegradable) and
biodegradable implant
Crystalline drug is packed in tubes and
implanted under the skin
…slow and uniform release of drug over months
…non-biodegradable implant has to be removed while
biodegradable implant is left
…hormonal contraceptive eg. NORPLANT
Intramuscular route
• Drug is injected in large skeletal muscle
…deltoid, gluteus maximus
• Muscle has rich blood supply
• Less nerve supply
Thus,
 Mildly irritant drugs can be given
 Absorption is faster (for aqueous soln)
 Less painful….but self-administration not possible
because of deep penetration
 Depot preparations (oily soln) can be injected
Intramuscular route
• Warning:
Avoided in patients on anticoagulant therapy
….risk of hematoma
Intravenous route
• Drug is injected into one of the large veins
….bolus/slow infusion
• Intima is insensitve
• Drug directly reaches into bloodstream
• Only aqueous soln can be givens…..no depot
preparation
Intravenous route
• Advantages:
• Highly irritant drugs can be given
• Useful in emergencies
• Dose required is small as bioavailablity is 100%
• Large volumes can be infused
• Response can be measured accurately
• Titration of dose can be done fore short acting drugs
Intravenous route
• Disadvantages:
• Risk of thrombophlebitis of the injected vein
• Necrosis of adjoining tissue in case of extravasation
• Most risky route – as vital organs get exposed to high
concentrations of drug
Intradermal route
• Drug is injected in the skin to raise a bleb
• Multiple puncture/scarring of the epidermis
• Used for special pusposes:
 BCG vaccination
 Sensitivity testing
Routes of drug administration

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Routes of drug administration

  • 1. Routes of drug administration Dr. M. Ahsan (MBBS, MD)
  • 3. Local route • Site of action is same as site of administration • Absorption of drug from this site into systemic circulation is minimal or absent • Side effects are minimal
  • 4. Local routes • Topical • Deeper tissues • Arterial supply
  • 5. Topical External application of the drug to surfaces for localized action  On skin  Nasal mucosa  Oralmucosa  Eyes  Ear canal  Anal canal  Vagina  Non-absorbable drugs given orally  Inhalation of drugs for local action on bronchi
  • 6.
  • 7. Deeper tissues • Deep areas can be reached with the help of a needle….. • But absorption of drug from this site is minimal • Drug acts only locally at the site of administration
  • 8. Deeper tissues Intra-articular injection Intra-thecal injection Inra-lesional injection Intra-cardiac Retrobulbar injection Infiltration around a nerve
  • 9.
  • 10. Arterial supply • Contrast media in angiography • Chemotherapy of limbs
  • 11. Systemic routes • Oral • Sublingual • Rectal • Transdermal • Inhalation • Nasal • Parenteral
  • 12. Oral route • Most commonly employed • Advantages :  Most convenient, safe & economical  Non-invasive  Painless  Self administration is possible  Drugs need not be highly purified  Adverse effect if any, appears slowly
  • 13. Oral route • Disadvantages:  Slowly absorbed; so slow onset of action  Not useful in unconscious, uncooperative patients & in patients with vomiting  Unpalatable drugs are difficult to administer  May cause nausea and vomiting  Drugs which are either inactivated in gastic juice or not absorbed or metabolised extensively in the gut & liver (first-pass metabolism) cannot be given  pH of the gut, presence of food or other drugs and motility of gut interferes with absorption
  • 14. Sublingual route • Drug is placed under the tongue • It can be crushed and spread over the buccal mucosa • Only lipid soluble and non-irritant drugs can be administered  The drug is rapidly absorbed through highly vascular buccal mucosa directly into systemic circulation
  • 15.
  • 16. Sublingual route • Advantages:  Rapid onset of action; so can be used in emergency  Self-administration possible  Degradation in the gut and liver, ie first-pass metabolism is bypassed  After the desired effect is reached, remaining drug can be discarded
  • 17. Sublingual route • Disadvantages: Irritant and distatesful drugs cannot be administered Glyceryl trinitrate Nifedipine Buprenorphine
  • 18. Rectal route • Enemas, suppositories and ointments can be administered by the rectal route Advantages: 50% of the absorbed drug bypasses first-pass metabolism Useful in case of vomiting or unconscious patients
  • 19. Rectal route Disadvantages:  Rectal absorption is often erratic and incomplete  Drugs may irritate the rectal mucosa  It is embarassing Diazepam – in case of convulsions Paracetamol suppository
  • 20.
  • 22. Transdermal route • Mostly used for sustained delivery of the drug • Highly lipid-soluble drugs can be absorbed through the skin to achieve systemic effects • Absorption can be increased by applying drugs as ointments, rubbing and occlusive dressing • Transdermal therapeutic systems (TTS) deliver the drug at a constant rate
  • 24. Transdermal patch • These are medicated adhesive patches that deliver the drug into blood stream at a controlled rate • Come in various shapes and sizes (5-20 sq.cm) • The patch is applied over the chest, abdomen, upper arm, lower back, buttock, mastoid region • Lasts for 1-3 days
  • 25. Transdermal patch • Advantages:  Convenient and painless  Bypasses first pass metabolism  Ideal for drugs that are lipophillic and require prolonged administration
  • 26. Transdermal patches • Disadvantages:  Some patients are allergic to patches, may cause irritation – (change the site of application)  More expensive  Can be used for only few drugs which are highly lipid- soluble
  • 27. Transdermal patches • GTN patches • Nicotine patches • Fentanyl patches • Scopolamine patches
  • 28. Inhalation • Volatile liquids or gases are given by inhalation for systemic action – eg. General anesthetics • Absorption takes place from the surface of alveoli – action is rapid • When drug is discontinued, it diffuses back from the blood into the alveoli and is exhaled out • Thus, controlled administration is possible • Irritant vapors can cause inflammation of respiratory tract
  • 29. Nasal • Drug is absorbed from the nasal mucosa • Bypasses gastric juices and first-pass metabolism Desmopressin spray – diabetes insipidus Calcitonin spray - osteoporosis
  • 30. Parenteral route • Subcutaneous • Intra-muscular • Intra-venous • Intra-dermal
  • 32. Parenteral routes • Advantages:  Drug action is rapid  Gastric irritation and vomiting is not induced  Can be used in unconscious, uncooperative and vomiting patients  No interference with food or digestive juices  No first-pass metabolism
  • 33. Parenteral routes • Disadvantages :  Preparation has to sterilized- so expensive  Technique is invasive  Painful  Assistance is required  Chances of local tissue injury  Adverse effects are more
  • 34. Subcutaneous route • Drug is deposited in loose connective tissue • This tissue is richly supplied by nerves • Subcutaneous tissue is less vascular Thus,  Irritant drugs cannot be given  Absorption is slower  Only small volumes can be injected s.c  Self-injection is possible  Depot preparations can be given
  • 35. Subcutaneous route Special forms of s.c route: Dermojet High velocity jet of drug solution is projected from microfine orifice using a gun. Solution passes through the superficial layers and gets deposited in subcutaneous tissue ….painless ...mass innoculations Pellet implantation Solid pellet is introduced with trochar and cannula …sustained release of DOCA, testesterone
  • 36. Subcutaneous route Sialistic (nonbiodegradable) and biodegradable implant Crystalline drug is packed in tubes and implanted under the skin …slow and uniform release of drug over months …non-biodegradable implant has to be removed while biodegradable implant is left …hormonal contraceptive eg. NORPLANT
  • 37. Intramuscular route • Drug is injected in large skeletal muscle …deltoid, gluteus maximus • Muscle has rich blood supply • Less nerve supply Thus,  Mildly irritant drugs can be given  Absorption is faster (for aqueous soln)  Less painful….but self-administration not possible because of deep penetration  Depot preparations (oily soln) can be injected
  • 38. Intramuscular route • Warning: Avoided in patients on anticoagulant therapy ….risk of hematoma
  • 39. Intravenous route • Drug is injected into one of the large veins ….bolus/slow infusion • Intima is insensitve • Drug directly reaches into bloodstream • Only aqueous soln can be givens…..no depot preparation
  • 40. Intravenous route • Advantages: • Highly irritant drugs can be given • Useful in emergencies • Dose required is small as bioavailablity is 100% • Large volumes can be infused • Response can be measured accurately • Titration of dose can be done fore short acting drugs
  • 41. Intravenous route • Disadvantages: • Risk of thrombophlebitis of the injected vein • Necrosis of adjoining tissue in case of extravasation • Most risky route – as vital organs get exposed to high concentrations of drug
  • 42. Intradermal route • Drug is injected in the skin to raise a bleb • Multiple puncture/scarring of the epidermis • Used for special pusposes:  BCG vaccination  Sensitivity testing