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Non narcotic analgesics, antipyretics & anti-inflammatory drugs

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Non narcotic analgesics, antipyretics & anti-inflammatory drugs

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An analgesic or painkiller is any member of the group of drugs used to achieve analgesia, relief from pain. Analgesic drugs act in various ways on the peripheral and central nervous systems.
Non-steroidal anti-inflammatory drugs (NSAIDs) are medicines that are widely used to relieve pain, reduce inflammation, and bring down a high temperature. They're often used to relieve symptoms of headaches, painful periods, sprains and strains, colds and flu, arthritis, and other causes of long-term pain.

An analgesic or painkiller is any member of the group of drugs used to achieve analgesia, relief from pain. Analgesic drugs act in various ways on the peripheral and central nervous systems.
Non-steroidal anti-inflammatory drugs (NSAIDs) are medicines that are widely used to relieve pain, reduce inflammation, and bring down a high temperature. They're often used to relieve symptoms of headaches, painful periods, sprains and strains, colds and flu, arthritis, and other causes of long-term pain.

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Non narcotic analgesics, antipyretics & anti-inflammatory drugs

  1. 1. Non-narcotic Analgesics, Antipyretics & Anti-inflammatory Drugs Prof. Amol B. Deore Department of Pharmacology MVP’s Institute of Pharmaceutical Sciences, Nashik
  2. 2. Pain Pain is an unpleasant feeling, such as a prick, tingle, sting, burn, or ache. Pain may be sharp or dull. It may come and go, or it may be constant. You may feel pain in one area of your body, such as your back, abdomen, chest, pelvis, or you may feel pain all over. (टोचणे, मुंग्या येणे, डुंकणे, जाळणे ककुं वा वेदना होणे)
  3. 3. Pyrexia Pyrexia, also known as fever, is an increase in the body temperature of an individual beyond the normal range. This increase in temperature is usually considered dangerous, but it is a natural defensive mechanism of the body to fight against infections.
  4. 4. What is inflammation? Inflammation happens in everyone, whether you’re aware of it or not. Your immune system creates inflammation to protect the body from infection, injury, or disease. There are many things you wouldn’t be able to heal from without inflammation. 5 SIGNS OF INFLAMMATION
  5. 5. Acute inflammation usually occurs for a short (yet often severe) duration. It often resolves in two weeks or less. Symptoms appear quickly such as Heat, Pain, Redness, Swelling and Loss of function Chronic inflammation is a slower and generally less severe form of inflammation. It typically lasts longer than six weeks. It can occur even when there’s no injury, and it doesn’t always end when the illness or injury is healed. Chronic inflammation has been linked to autoimmune disorders and even prolonged stress.
  6. 6. • These are the drugs which relieve pain by blocking the pain impulse generation and transmission. Analgesics • These are the drugs which reduce the elevated body temperature i.e. hyperpyrexia.Antipyretics • These are the drugs used to treat inflammation, swelling and edema. Anti-inflammatory agents
  7. 7. Classification
  8. 8. Non-Narcotic Analgesic, Antipyretics & Anti-Inflammatory Salicylates • Ex. Aspirin, Methyl Salicylates, Magnesium Salicylic acid, Sodium Salicylates, Salicylic acid, Salfasalazine. Para-amino phenol • Ex. Paracetamol, Phenacetin, Pyrazolones • Ex. Phenyl butazone, oxyphenbutazone, analgin.
  9. 9. Non-Steroidal Anti-inflammatory Drugs (NSAIDS) • Ex. Indomethacin, Sulindic, TolmetinIndole derivatives • Ex. Ibuprofen, Ketoprofen, Fenoprofen, Naproxen, Dexibuprofen, Propionic acid derivatives • Ex. Meclofenamate, Mefenamic acid, Flufenamic acid, Tolfenamic acid Fenamates • Ex. Diclofenac, Ketorolac, Aceclofenac.Phenyl acetic acid derivatives • Ex. Piroxicam, Tenoxicam, Dioxicam, Lornoxicam, Meloxicam. Oxicam acid derivatives • Ex. Nimesulide.Sulfonamide
  10. 10. Miscellaneous • Ex. Hydroxychloroquine, Penicillamine. Gold Compounds • Ex. Aurothioglucose. Selective COX-2 inhibitors • Ex. Celecoxib, Rofecoxib, Valdecoxib, Parecoxib, Firocoxib Anti-gout drugs • Ex. Allopurinol, Colchicine, Probenecid
  11. 11. Salicylates: ASPIRIN
  12. 12. Mechanisms of action Aspirin causes several reduction of inflammation, analgesia (relief of pain), the prevention of clotting, and the reduction of fever. Aspirin's suppress the production of prostaglandins and thromboxane is due to inhibition of the cyclooxygenase (COX) enzyme. Cyclooxygenase is required for prostaglandin and thromboxane synthesis.
  13. 13. Prostaglandin PGI-2 Prostaglandin PGE-2 PG synthatase
  14. 14. Pharmacological actions of Aspirin
  15. 15. Analgesic action Salicylates block pain impulse generation and transmission to the pain receptor due to inhibition of prostaglandin synthesis.
  16. 16. Anti-inflammatory action Salicylates show anti-inflammatory action due to inhibition of enzymes cyclooxygenase (COX). Thus, inhibit prostaglandin synthesis. Prostaglandins are required for edema, pain, fever, itching, inflammation, and swelling.
  17. 17. Anti-Rheumatic action Salicylates reduce pain, swelling and fever in rheumatoid arthritis and rheumatic fever by three actions. • Inhibition of prostaglandin synthesis. • Stimulation of adrenal medulla to secrets steroidal hormones to show anti- inflammatory action • By rising the pain threshold value.
  18. 18. Antipyretic action Salicylates reduce the elevated body temperature by sweating and inhibition of synthesis and release of prostaglandin-E2 in hypothalamic temperature regulating center.
  19. 19. Anti-platelet action: Salicylates reduce thromboxane-A2 alpha synthesis hence, they inhibit platelet aggregation thereby show anti-platelet action.
  20. 20. Uric acid excretion Salicylates increase urinary excretion of uric acid hence, used in acute Gout.
  21. 21. Gastrointestinal action Salicylates can cause acute gastritis and gastric ulceration due to damage of mucus layer that result in gastric hemorrhage [gastric bleeding], bloody stool, iron deficiency anemia etc. The mucus production is take place because of prostaglandins but salicylates inhibit prostaglandin synthesis and affect mucus production in stomach. Because of this gastric acid attacks on the gastric mucosa and results in ulcer, erosion and gastric bleeding.
  22. 22. Therapeutic uses of aspirin Analgesia: • Mild to moderate pain of musculoskeletal origin, headache, myalgia, neuralgia, toothache, dysmenorrhea and backache. Antipyretic: • Lowers elevated body temperature (pyrexia) for symptomatic relief. Anti-inflammatory activity: • Rheumatoid arthritis, osteoarthritis, bursitis, and acute rheumatic fever. Prophylaxis of thromboembolism, cerebral ischemia, and venous emboli. Prevention of re- infarction in patients with previous history of acute myocardial infarction. Dose: 350-650 mg
  23. 23. Adverse drug reaction of aspirin Salicylism • headache, confusion, tinnitus, deafness, sweating, palpitation. Hemorrhage • major gastric bleeding and GIT hemorrhage Hypersensitivity reactions • skin rash, pruritus, bronchospasm, edema, shock Reye’s syndrome • aspirin in children with influenza or small pox has been associated with Reye’s syndrome, a life threatening condition marked by severe vomiting, lethargy, delirium, coma, and death. Permanent brain damage may occur in survivors.
  24. 24. Contraindications Pregnancy, Severe bleeding, Allergy, Impaired renal function, Hemophilia, Ulcer, Influenza, Chickenpox
  25. 25. Aspirin should not be given in peptic ulcer?
  26. 26. • Aspirin is weakly acidic drug causing gastric acidosis leading to gastric discomfort (distress) i.e. hyperacidity, nausea, vomiting and headache. • If aspirin is taken in empty stomach, gastric acidosis causes damage to GIT mucosa and erosion. • That results in gastric ulcer, gastric bleeding and anemia.
  27. 27. COX-I and COX-II (cyclooxygenase) enzymes are required for prostaglandin synthesis and ultimately for inflammatory reactions. But COX-I is an enzyme which is present in stomach mucosa and other sites of inflammation. COX-1 is also required for synthesis of gastric mucus to protect and lubricate the internal mucosa layer of stomach from the gastric acid erosion. The COX-2 is present in variety of tissue as including site of inflammation.
  28. 28. • Common NSAIDs and salicylates inhibit both enzymes COX-I and COX-II thereby inhibiting prostaglandin synthesis and hence show anti- inflammatory action. • But blocking of COX-I enzyme also inhibit gastric mucus secretion hence gastric mucosa expose to gastric acid and shows erosion and damage. • This leads to gastric upset, peptic ulceration, gastric bleeding, intestinal bleeding and bloody stools. • Therefore Aspirin should not be given in peptic ulcer.
  29. 29. Aspirin is generally taken after meal or in association with sodium bicarbonate? OR Aspirin is not taken in empty stomach?
  30. 30. • Aspirin is weakly acidic drug causing gastric acidosis leading to gastric discomfort (distress) i.e. hyperacidity, nausea, vomiting and headache. If aspirin is taken in empty stomach, gastric acidosis shows damage to GIT mucosa and erosion causing peptic ulcer, GI bleeding and anemia.
  31. 31. • If aspirin is given after meal, this secreted gastric acid is utilized for food digestion process and loaded stomach avoids direct contact of acid with GI mucosa. Sod bicarbonate if given along with aspirin, neutralizes gastric acid and avoid peptic ulceration.
  32. 32. Why Aspirin (Salicylate) therapy is always supported with Vitamin K?
  33. 33. • Salicylate causes gastric acidosis, peptic ulcer and GIT bleeding at large doses up to 500mg. At low dose of 150mg, it inhibits platelet aggregation and prolongs bleeding time. • Vitamin K activates blood clotting factor. Hence, initiates blood coagulation and prevents hemorrhages (blood loss). So Salicylate therapy is always supported with Vitamin K.
  34. 34. Acute Salicylates Poisoning
  35. 35. Causes: • Accidental overdose more than 650 mg Symptoms: • Gastrointestinal Symptoms: Nausea, Vomiting, Abdominal pain, Gastric bleeding and bloody stools. • Metabolic symptoms: metabolic acidosis, hypoglycemia • Electrolyte imbalance: dehydration, hypokalemia, • Respiratory symptoms: hyperventilation and respiratory alkalosis • Cardiovascular symptoms: CV collapse • CNS Symptoms: Tinnitus, lethargy, seizures,tremor, Hallucination, Convulsion, Vertigo Coma. • Others: Hyperpyrexia
  36. 36. Treatment is Symptomatic and Includes • Patient should be hospitalized immediately. • Gastric lavage to eliminate unabsorbed drugs from the stomach. • Temperature is brought down by external cooling with cold water sponges. • Activated charcoal 1g/kg may be indicated in massive overdose, ideally within 1 hour of ingestion. It adsorbs the aspirin in the gastrointestinal tract. • Intravenous fluids such as dextrose 5% are recommended to increase a urinary output. The IV fluids should contain Na+, K+,HCO3 and glucose (to treat hypokalaemia and acidosis). Blood pH should be monitored.
  37. 37. In severe cases, forced alkaline diuresis with sodium bicarbonate and a diuretic like frusemide is given along with IV fluids. Sodium bicarbonate ionizes salicylates making them water soluble and increases their excretion through kidneys. Diuretics must be given to increase urinary elimination of salicylates. If hemorrhagic complications are seen, Vitamin K and Protamine must be given to prevent hemorrhage. Hemodialysis can be used to enhance the removal of salicylate from the blood. Hemodialysis is usually used in those who are severely poisoned.
  38. 38. PARACETAMOL
  39. 39. MECHANISM OF ACTION Paracetamol has analgesic and antipyretic actions like aspirin. It has poor anti-inflammatory action in comparison to aspirin because it has weak inhibitory activity on cyclooxygenase enzyme. Paracetamol is thought to relieve pain by reducing the production of prostaglandins in the brain and spinal cord. Paracetamol reduces fever by affecting an area of the brain that regulates our body temperature (the hypothalamic temperature- regulating center).
  40. 40. Dose Paracetamol tablet 500 mg Paracetamol syrup 125 mg/5mL
  41. 41. USES OF PARACETAMOL Fever: • Paracetamol is used to provide temporary relief from fever without treating the underlying cause. Headache: • Paracetamol is used to relieve acute headaches including a migraine. Muscle Pain: • Paracetamol is used to relieve mild to moderate pain in the muscles. Menstrual Cramps: • Paracetamol is used to relieve pain and cramping associated with menstrual cycles in women. Post Immunization Pyrexia: • Paracetamol is used in the treatment of pain and fever that sets in after one has taken vaccinations.
  42. 42. ADVERSE DRUG REACTIONS Liver damage • A paracetamol overdose is dangerous and capable of causing serious damage to the liver and kidneys. Allergic skin reaction • Paracetamol can cause red spots on skin, rashes, hives and itching. Anemia • Paracetamol can cause anemia like symptoms in some patients. Stevens-Johnson Syndrome • Paracetamol can cause this rare but potentially fatal allergic reaction of the skin that requires immediate treatment.
  43. 43. CONTRAINDICATIONS Liver Disease • Paracetamol is metabolized by the liver and is not recommended if you suffer from impaired liver function.
  44. 44. NSAIDS [Non-Steroid Anti-Inflammatory Drugs]
  45. 45. NSAIDs are most popularly used as pain killer and anti-inflammatory agents. They do not contain steroidal ring in their chemical structure. They should not be used for minor headache and fever.
  46. 46. NSAIDs mainly use for relieving the pain like osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, lower back pain, migraine, gouty arthritis, menstrual pain, dysmenorrhea, postoperative pain, muscle stiffness, renal stones pain, dental pain, and tennis elbow and athlete injury.
  47. 47. Mechanisms of NSAIDs NSAIDs inhibit cyclooxygenase and prostaglandin synthesis. This enzyme are responsible for formation of prostaglandin PGF2, PGF2 alpha, thromboxane form the arachidonic acid. Inhibition of Prostaglandin E, Prostaglandin F2 alpha show potent analgesic anti-inflammatory action.
  48. 48. Therapeutic uses NSAIDs mainly use for relieving the pain like osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, lower back pain, migraine, gouty arthritis, menstrual pain, dysmenorrhea, postoperative pain, muscle stiffness, renal stones pain, dental pain, and tennis elbow and athlete injury.
  49. 49. Adverse drug reaction • Nephrotoxicity, • Peptic ulcer, • Abdominal pain, • Gastric bleeding Contraindications • Kidney diseases [nephrotoxicity]. • Peptic ulcer. • Pregnancy.
  50. 50. Summary of nonsteroidal anti-inflammatory agents (NSAIDs).
  51. 51. GOUT Gout is medical condition characterized by abnormally high levels of uric acid in the blood, recurring attacks of joint inflammation (arthritis), and deposits of hard crystals of uric acid in and around the joints, and decreased kidney function and kidney stones.
  52. 52. Gout is a purine metabolism disorder resulting from an excess of uric acid in the blood due to either its overproduction or faulty elimination.
  53. 53. Antigout agents Xanthine oxidase inhibitors • Ex. Allopurinol, Oxypurinol, Tisopurine, Febuxostat Uricosuric agent • Ex. Probenecid, Sulphinpyrazine, Benzbromarone, Isobromindione, Azapropazone Others • Ex. Rasburicase, Pegloticase
  54. 54. Prof. Amol Deore

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