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Routes of drug administration

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Kanhiya Singh Jayash

Routes of drug administration pharmacology

Health & Medicine
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ROUTES OF DRUG ADMINISTRATION Dr ST
Routes of Drug Administration A route of administration is the path by which a drug, fluid, poison, or other substance is brought into contact with the body. Route of administration (ROA) that is chosen may have a profound effect upon the speed and efficiency with which the drug acts
Factors governing route of administration • Drug factors • Physical and chemical properties of the drug (solid/liquid/gas; solubility, stability, pH, irritancy). • Nature of the drug • Rate and extent of absorption of the drug from different routes • Bioavailability of drug • Distribution • Extensive first pass metabolism
• Patients factor • Condition of the patient (unconscious, vomiting). • Associated comorbidities • Rapidity with which the response is desired (routine treatment or emergency). • Accuracy of dosage required (i.v. and inhalational can provide fine tuning). • Disease factors • Site of desired action—localized and approachable or generalized and not approachable. • Emergency situation
Classification Enteral routes • Oral • Sublingual • Rectal Topical routes Conjunctival,Nasal, auditory mucosal Vaginal & Urethral Inunction & Dermal
Parenteral routes A. Injections Intravenous Intramascular Intraperitoneal Intrathecal Intramedullary Intra-arterial Intra-articular Subcutaneous Intracardiac Epidural B. Inhalational administration C. Transdermal administration
ORAL ADVANTAGES Safe- no injury to structures. Safe – its possible to remove it from stomach. Convenient Economical No complicatio ns of parenteral therapy Easy to adjust doses.
DISADVANTAGES •Action of drugs is slower and thus not suitable for emergencies. •Unpalatable drugs (chloramphenicol) are difficult to administer; •May cause nausea and vomiting . •Cannot be used for uncooperative/unconscious/ vomiting patient. •Absorption of drugs may be variable and erratic; •certain drugs are not absorbed (streptomycin). •Others are destroyed by digestive juices (penicillin G,Insulin) or in liver (GTN, testosterone, lidocaine).
Precautions Patient should be in upright position To be taken with glass full of water Avoid certain drugs in recumbent position •Iron •Tetracycline •Bisphosphonates
TRANSMUCOSAL ROUTE • SUBLINGUAL ROUTE : Tablet is placed under tongue Crosses buccal mucosa Enters into systemic circulation Example Nitroglyceri ne Buprenorph ine Nifedipine
ADVANTAGES OF SUBLINGUAL ROUTE Rapid onset of action Quick termination on spitting Bypass first pass metabolism No degradation in intestinal wall and liver.
First-pass Effect • The first-pass effect is the term used for the metabolism of a drug during its passage from the site of absorption into systemic circulation. • The greater the first-pass effect, the less the agent will reach the systemic circulation when the agent is administered orally
First-pass Effect
• Disadvantages • Only lipid soluble & • Non-irritating drugs can be administered.
TRANSRECTAL ROUTE Upper rectal mucosa Superior hemorrhoidal vein Portal circulation Lower rectal mucosa Middle and inferior hemorrhoidal vein Systemic circulation
Advantages No GI irritation First pass degradation is relatively less Useful in patients with nausea & vomiting Examples Indomethacin in rheumatoid arthritis Bisacodyl, Glycerine suppositories, enema Diazepam in status epilepticus Disadvantage All patients may not be comfortable/ willing to do it. Chances of rectal inflammation Absorption is unreliable
ENEMA EVACUANT ENEMA • For evacuation of large bowel. • Warm water, soap solutions, glycerin can be given. • Amount ~ 600 ml. • Used for – Constipation – Pre-op preperation – Before radiological examination. RETENTION ENEMA • Local action – Steroids in ulcerative colitis. • Systemic action – Diazepam in status epilepticus – Indomethacin in RA. • Amount ~ 100-120 ml. Causes evacuation Should be retained for action
PARENTERAL ROUTES ADVANTAGES Can be used in unconscious and uncooperative patients Beneficial in vomiting & diarrhoea. Irritating drugs can be given. Avoid drug modification by GI & liver enzymes. Rapid action and accuracy of dose is ensured.
PARENTERAL ROUTE DISADVANATES Technically difficult May cause infection May cause injury to the structures More expensive
INTRAVENOUS IV injection As a rapid IV bolus Over 5-10 minutes in 10-20 ml dilution In an infusion in 50- 100 ml or larger in volume. To slow the administration of the drug To maintain constant plasma levels To administer large volumes either rapidly or over prolonged periods. OBJECTIVES RAPID SLOWER EVEN SLOWER !!!
Disadvantage Once given, action can’t be halted Local irritation Self medication difficult Extravasation, sloughing may occur.
Subcutaneus Non irritant drugs can only be given Not effective in shock Insulin, steroid hormone implant In pediatrics  saline
• Dermojet: In this method needle is not used; a high velocity jet of drug solution is projected from a microfine orifice using a gun like implement. 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
Intradermal In between layers of skin BCG vaccine. Penicillin hypersensitivity test http://www.answers.com/topic/injection
Intramuscular Mild irritants can be given. Depot preparations Local pain / necrosis. Damage to nerve deltoid, triceps, gluteus maximus, rectus femoris Intramuscular injections should be avoided in anticoagulant treated patients,
INTRA-ARTERIAL ROUTE Injection in artery. Along with blood flow it will reach the target tissue. For diagnostic dyes (radiocontrast dyes) Anti-cancer drugs
INTRATHECAL In subarachnoid space. Bypass BBB & Blood-CSF barrier. Antibiotic Anticancer drugs. EPIDURAL Drug is injected between the Dura & the lining of spinal canal Lidocaine http://pain- topics.org/images/img_glossar y2.jpg http://www.dhmc.org/dhmc-internet- upload/file_collection/ESI-translaminal.jpg
INTRAPERITONEAL For peritoneal dialysis. For drug administration in laboratory animals
Intramedullary In the bone marrow Saline/blood can be given in new born Rarely used. Intraarticular Into joint cavity Hydrocortisone in Rheumatoid Arthritis Intralesional Glucocorticoid injection.. Local anaesthetic injection. Given in painful spots.
Intracardiac Directly into heart Adrenaline is given During cardiac resuscitation Retrobulber Dexamethasone can be given
INHALATION INHALATION Drug aerosols given by MDI. Dry powders from inhalers Nebulised solutions Gases Salbutamol in bronchial asthma Compressed air driven solutions e.g. salbutamol in bronchial asthma Salbutamol General anaesthetic
Metered dose inhalers • Contain solution /suspensions / emulsion of drugs in a mixture of inert propellants held under pressure in an aerosol dispenser incorporating a metering device. • Poropellants: liquified hydrocarbon gases • Requires careful storage as peopellant may be volatile and inflammable
Nebulisers • Nebulised aerosols delivered through a mask • Relatively large volumes can be nebulised • Mostly used in hospital setting • Useful in pediatric population
Dry powder inhalers • Rota inhaler, spin inhaler, disk inhaler • Used for inhalation of micronized powders of relatively potent drugs • Powder is supplied in a hard gelatin capsules • These devices often breath actuated- synchronisation with breathing cycle is automatic • No dilution of drug with liquid-higher dose per inspiration can be delivered
LOCAL APPLICATION SKIN • Ointment • Cream • Powder • Lotion • Paste MUCOUS MEMBRANE • Mouthwash • Lozenges • Gargles • Spray CAVITY • Bougie • Pessaries • Suppository REMEMBER IT FROM OUT TO IN  SKIN, MUCOUS MEMBRANE, CAVITY
Local • Used only for localized lesions at accessible sites • Systemic absorption from these sites is minimal or absent. • High concentrations are attained at the desired site without exposing the rest of the body. • Systemic side effects or toxicity are consequently absent or minimal.
Topical • External application of the drug to the surface for localized action. • Convenient • Drugs can be efficiently delivered to the localized lesions on skin, oropharyngeal/ nasal mucosa/ eyes, ear canal, anal canal • Lotion, ointment, cream, powder,rinse, paints, drops, spray, lozenges,suppositories • Nonabsorbable drugs given orally for action on g.i. mucosa
Advantages of local route Fast onset of action Better concentration at site of action Less quantity is required. Less systemic ADR. Disadvantages of local route Not always possible to apply a drug locally Local irritation Sometimes systemic absorption and toxicity can occur
TRANSCUTANEUS ROUTE • IONTOPHORESIS : – Galvanic current drives the drug into deeper tissue. – Force of repulsion drives the drug into deeper tissues. – Salicylates .
• Adhesive units : – Transdermal therapeutic system. – Scopolamine – Estradiol – Nitroglycerine
TRANSNASAL ROUTE • dDAVP-- analogue of vasopressin • GnRH • Calcitonin
• Same drug  different route  different action. • Action of MgSO4. Oral Saline laxative Rectally Reduces Intra cranial tension Injection Anticonvulsant Topical Hygroscopic ,reduces edema
• A 5-year-old child is brought to the hospital with the complaint of fever, cough, breathlessness and chest pain. On examination he is found to be dull, but irritable with fast pulse (116/min), rapid breathing (RR 50/min) and indrawing of lower chest during inspiration, wheezing, crepitations and mild dehydration. Body temperature is 40°C (104°F). The paediatrician makes a provisional diagnosis of acute pneumonia and orders relevant haematological as well as bacteriological investigations. • He decides to institute antibiotic therapy. (a) In case he selects an antibiotic which can be given orally as well as by i.m. or i.v. injection, which route of administration will be most appropriate in this case? (b) Should the paediatrician administer the antibiotic straight away or should he wait for the laboratory reports?
• A 35 year old male patients is suffering with mild viral gastroenteritis. He had 3 loose motions in previous 24 hrs. on examination he had no signs of dehydration. He is conscious & Cooperative • No Nausea & vomiting • T/T : To maintain hydration • Decide route of administration
• A 30 yr old male patients presents with complaints of episodic breathlessness often following exertion. After examination & investigations, Physician make a diagnosis of acute bronchial asthama. • Drug of choice is Salbutamol • Decide route of administration & Explain.
• A 55 yr old man presentedwith complaints of tightness & discomfort over middle part of chest felt episodically particularly after exertion. A diagnosis of exertional angina was made & he was prescribed –Tab glyceryl trinitrate. • Decide & explain advantages & disadvantages of decided route of administration.

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Routes of drug administration

  • 2. Routes of Drug Administration A route of administration is the path by which a drug, fluid, poison, or other substance is brought into contact with the body. Route of administration (ROA) that is chosen may have a profound effect upon the speed and efficiency with which the drug acts
  • 3. Factors governing route of administration • Drug factors • Physical and chemical properties of the drug (solid/liquid/gas; solubility, stability, pH, irritancy). • Nature of the drug • Rate and extent of absorption of the drug from different routes • Bioavailability of drug • Distribution • Extensive first pass metabolism
  • 4. • Patients factor • Condition of the patient (unconscious, vomiting). • Associated comorbidities • Rapidity with which the response is desired (routine treatment or emergency). • Accuracy of dosage required (i.v. and inhalational can provide fine tuning). • Disease factors • Site of desired action—localized and approachable or generalized and not approachable. • Emergency situation
  • 5.
  • 6. Classification Enteral routes • Oral • Sublingual • Rectal Topical routes Conjunctival,Nasal, auditory mucosal Vaginal & Urethral Inunction & Dermal
  • 7. Parenteral routes A. Injections Intravenous Intramascular Intraperitoneal Intrathecal Intramedullary Intra-arterial Intra-articular Subcutaneous Intracardiac Epidural B. Inhalational administration C. Transdermal administration
  • 8.
  • 9. ORAL ADVANTAGES Safe- no injury to structures. Safe – its possible to remove it from stomach. Convenient Economical No complicatio ns of parenteral therapy Easy to adjust doses.
  • 10. DISADVANTAGES •Action of drugs is slower and thus not suitable for emergencies. •Unpalatable drugs (chloramphenicol) are difficult to administer; •May cause nausea and vomiting . •Cannot be used for uncooperative/unconscious/ vomiting patient. •Absorption of drugs may be variable and erratic; •certain drugs are not absorbed (streptomycin). •Others are destroyed by digestive juices (penicillin G,Insulin) or in liver (GTN, testosterone, lidocaine).
  • 11. Precautions Patient should be in upright position To be taken with glass full of water Avoid certain drugs in recumbent position •Iron •Tetracycline •Bisphosphonates
  • 12. TRANSMUCOSAL ROUTE • SUBLINGUAL ROUTE : Tablet is placed under tongue Crosses buccal mucosa Enters into systemic circulation Example Nitroglyceri ne Buprenorph ine Nifedipine
  • 13. ADVANTAGES OF SUBLINGUAL ROUTE Rapid onset of action Quick termination on spitting Bypass first pass metabolism No degradation in intestinal wall and liver.
  • 14. First-pass Effect • The first-pass effect is the term used for the metabolism of a drug during its passage from the site of absorption into systemic circulation. • The greater the first-pass effect, the less the agent will reach the systemic circulation when the agent is administered orally
  • 16. • Disadvantages • Only lipid soluble & • Non-irritating drugs can be administered.
  • 17. TRANSRECTAL ROUTE Upper rectal mucosa Superior hemorrhoidal vein Portal circulation Lower rectal mucosa Middle and inferior hemorrhoidal vein Systemic circulation
  • 18. Advantages No GI irritation First pass degradation is relatively less Useful in patients with nausea & vomiting Examples Indomethacin in rheumatoid arthritis Bisacodyl, Glycerine suppositories, enema Diazepam in status epilepticus Disadvantage All patients may not be comfortable/ willing to do it. Chances of rectal inflammation Absorption is unreliable
  • 19. ENEMA EVACUANT ENEMA • For evacuation of large bowel. • Warm water, soap solutions, glycerin can be given. • Amount ~ 600 ml. • Used for – Constipation – Pre-op preperation – Before radiological examination. RETENTION ENEMA • Local action – Steroids in ulcerative colitis. • Systemic action – Diazepam in status epilepticus – Indomethacin in RA. • Amount ~ 100-120 ml. Causes evacuation Should be retained for action
  • 20. PARENTERAL ROUTES ADVANTAGES Can be used in unconscious and uncooperative patients Beneficial in vomiting & diarrhoea. Irritating drugs can be given. Avoid drug modification by GI & liver enzymes. Rapid action and accuracy of dose is ensured.
  • 22. INTRAVENOUS IV injection As a rapid IV bolus Over 5-10 minutes in 10-20 ml dilution In an infusion in 50- 100 ml or larger in volume. To slow the administration of the drug To maintain constant plasma levels To administer large volumes either rapidly or over prolonged periods. OBJECTIVES RAPID SLOWER EVEN SLOWER !!!
  • 23. Disadvantage Once given, action can’t be halted Local irritation Self medication difficult Extravasation, sloughing may occur.
  • 24. Subcutaneus Non irritant drugs can only be given Not effective in shock Insulin, steroid hormone implant In pediatrics  saline
  • 25. • Dermojet: In this method needle is not used; a high velocity jet of drug solution is projected from a microfine orifice using a gun like implement. 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
  • 26. Intradermal In between layers of skin BCG vaccine. Penicillin hypersensitivity test http://www.answers.com/topic/injection
  • 27. Intramuscular Mild irritants can be given. Depot preparations Local pain / necrosis. Damage to nerve deltoid, triceps, gluteus maximus, rectus femoris Intramuscular injections should be avoided in anticoagulant treated patients,
  • 28. INTRA-ARTERIAL ROUTE Injection in artery. Along with blood flow it will reach the target tissue. For diagnostic dyes (radiocontrast dyes) Anti-cancer drugs
  • 29. INTRATHECAL In subarachnoid space. Bypass BBB & Blood-CSF barrier. Antibiotic Anticancer drugs. EPIDURAL Drug is injected between the Dura & the lining of spinal canal Lidocaine http://pain- topics.org/images/img_glossar y2.jpg http://www.dhmc.org/dhmc-internet- upload/file_collection/ESI-translaminal.jpg
  • 31. Intramedullary In the bone marrow Saline/blood can be given in new born Rarely used. Intraarticular Into joint cavity Hydrocortisone in Rheumatoid Arthritis Intralesional Glucocorticoid injection.. Local anaesthetic injection. Given in painful spots.
  • 32. Intracardiac Directly into heart Adrenaline is given During cardiac resuscitation Retrobulber Dexamethasone can be given
  • 34. Metered dose inhalers • Contain solution /suspensions / emulsion of drugs in a mixture of inert propellants held under pressure in an aerosol dispenser incorporating a metering device. • Poropellants: liquified hydrocarbon gases • Requires careful storage as peopellant may be volatile and inflammable
  • 35. Nebulisers • Nebulised aerosols delivered through a mask • Relatively large volumes can be nebulised • Mostly used in hospital setting • Useful in pediatric population
  • 36. Dry powder inhalers • Rota inhaler, spin inhaler, disk inhaler • Used for inhalation of micronized powders of relatively potent drugs • Powder is supplied in a hard gelatin capsules • These devices often breath actuated- synchronisation with breathing cycle is automatic • No dilution of drug with liquid-higher dose per inspiration can be delivered
  • 37.
  • 38. LOCAL APPLICATION SKIN • Ointment • Cream • Powder • Lotion • Paste MUCOUS MEMBRANE • Mouthwash • Lozenges • Gargles • Spray CAVITY • Bougie • Pessaries • Suppository REMEMBER IT FROM OUT TO IN  SKIN, MUCOUS MEMBRANE, CAVITY
  • 39. Local • Used only for localized lesions at accessible sites • Systemic absorption from these sites is minimal or absent. • High concentrations are attained at the desired site without exposing the rest of the body. • Systemic side effects or toxicity are consequently absent or minimal.
  • 40. Topical • External application of the drug to the surface for localized action. • Convenient • Drugs can be efficiently delivered to the localized lesions on skin, oropharyngeal/ nasal mucosa/ eyes, ear canal, anal canal • Lotion, ointment, cream, powder,rinse, paints, drops, spray, lozenges,suppositories • Nonabsorbable drugs given orally for action on g.i. mucosa
  • 41. Advantages of local route Fast onset of action Better concentration at site of action Less quantity is required. Less systemic ADR. Disadvantages of local route Not always possible to apply a drug locally Local irritation Sometimes systemic absorption and toxicity can occur
  • 42. TRANSCUTANEUS ROUTE • IONTOPHORESIS : – Galvanic current drives the drug into deeper tissue. – Force of repulsion drives the drug into deeper tissues. – Salicylates .
  • 43. • Adhesive units : – Transdermal therapeutic system. – Scopolamine – Estradiol – Nitroglycerine
  • 44. TRANSNASAL ROUTE • dDAVP-- analogue of vasopressin • GnRH • Calcitonin
  • 45. • Same drug  different route  different action. • Action of MgSO4. Oral Saline laxative Rectally Reduces Intra cranial tension Injection Anticonvulsant Topical Hygroscopic ,reduces edema
  • 46. • A 5-year-old child is brought to the hospital with the complaint of fever, cough, breathlessness and chest pain. On examination he is found to be dull, but irritable with fast pulse (116/min), rapid breathing (RR 50/min) and indrawing of lower chest during inspiration, wheezing, crepitations and mild dehydration. Body temperature is 40°C (104°F). The paediatrician makes a provisional diagnosis of acute pneumonia and orders relevant haematological as well as bacteriological investigations. • He decides to institute antibiotic therapy. (a) In case he selects an antibiotic which can be given orally as well as by i.m. or i.v. injection, which route of administration will be most appropriate in this case? (b) Should the paediatrician administer the antibiotic straight away or should he wait for the laboratory reports?
  • 47. • A 35 year old male patients is suffering with mild viral gastroenteritis. He had 3 loose motions in previous 24 hrs. on examination he had no signs of dehydration. He is conscious & Cooperative • No Nausea & vomiting • T/T : To maintain hydration • Decide route of administration
  • 48. • A 30 yr old male patients presents with complaints of episodic breathlessness often following exertion. After examination & investigations, Physician make a diagnosis of acute bronchial asthama. • Drug of choice is Salbutamol • Decide route of administration & Explain.
  • 49. • A 55 yr old man presentedwith complaints of tightness & discomfort over middle part of chest felt episodically particularly after exertion. A diagnosis of exertional angina was made & he was prescribed –Tab glyceryl trinitrate. • Decide & explain advantages & disadvantages of decided route of administration.