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Autacoids and Related Drugs

13/10/2024 | B MANOGNA REDDY

Autacoids and Related Drugs

A. Histaminergic Drugs:

  1. Nonselective agonists (H1 + H2 + H3): Histamine, Betahistine
  2. Selective H1 agonists: 2-Methyl histamine, 2-Pyridyl ethylamine, 2-Thizolyl ethylamine
  3. Selective H2 agonists: Dimaprit, Impromidine
  4. Selective H3 agonists: (R) α-Methylhistamine, Imetit

B. H1 Antagonists (Conventional antihistamines):

  1. Highly sedative: Diphenhydramine, Dimenhydrinate, Promethazine, Hydroxyzine
  2. Moderately sedative: Pheniramine, Cyproheptadine, Meclozine, Cinnarizine
  3. Mildly sedative: Chlorpheniramine, Dexchlorpheniramine, Triprolidine, Clemastine
  4. Second generation (nonsedating) antihistaminics: Fexofenadine, Loratadine, Desloratadine, Cetirizine, Levocetirizine, Azelastine, Mizolastine, Ebastine

C. 5-Hydroxy Tryptamine (5-HT) Antagonists:

  1. Nonselective antagonists & partial agonists/antagonists: Ergotamine, Lysergic acid diethylamide (LSD), 2-Bromo LSD, Methysergide, Cyproheptadine, Cinnarizine
  2. 5-HT2 Antagonists: Ketanserin, Ritanserin, Clozapine, Risperidone
  3. 5-HT3 Antagonists: Ondansetron, Granisetron, Tropisetron, Palonosetron, Ramosetron

D. Drugs for Migrane:

  1. To treat attacks:
    • Simple analgesics: Paracetamol, Aspirin, Metamizol, Codeine
    • Antiemetics: Metoclopramide, Domperidone, Prochlorperazine, Promethazine
    • Selective 5-HTID/IB agonists Sumatriptan, Rizatriptan, Naratriptan, Zolmitriptan, Frovatriptan
    • NSAIDs Ibuprofen, Naproxen, Diclofenac, Mephenamic acid
    • Ergot alkaloids: Ergotamine, Dihydroergotamine (DHE)
  2. To prevent attacks: Propranolol (other β blockers) Amitriptyline (other TCAs), Flunarizine, Valproic acid, Gabapentin, Topiramate, Cyproheptadine

E. Prostaglandins:

  1. Natural PGs: Dinoprostone (PGE2), Gemeprost, Dinoprost (PGF), Alprostadil (PGE1), Prostacyclin (PGI2) (Epoprostenol)
  2. Prostaglandin analogues: Carboprost (15-methyl PGF ), Misoprostol (methyl PGE1 ester), Latanoprost (PGE2 analogue), Travoprost, Bimatoprost

F. Nonsteroidal Antiinflammatory Drugs / Antipyretic Analgesics:

  1. Nonselective COX inhibitors:
    • Salicylates: Aspirin
    • Propionic acid derivatives: Ibuprofen, Naproxen, Ketoprofen, Flurbiprofen
    • Fenamate: Mephenamic acid
    • Enolic acid derivatives: Piroxicam, Tenoxicam
    • Acetic acid derivatives: Ketorolac, Indomethacin, Nabumetone
    • Pyrazolone derivatives: Phenylbutazone, Oxyphenbutazone
  2. Preferential COX-2 inhibitors: Nimesulide, Diclofenac, Aceclofenac, Meloxicam, Etodolac
  3. Selective COX-2 inhibitors: Celecoxib, Etoricoxib, Parecoxib
  4. Analgesic-antipyretics with poor antiinflammatory action:
    • Para aminophenol derivative: Paracetamol (Acetaminophen)
    • Pyrazolone derivatives: Metamizol (Dipyrone), Propiphenazone
    • Benzoxazocine derivative: Nefopam

G. Antirheumatoid Drugs:

  1. Disease modifying antirheumatoid drugs (DMARDs):
  2. Nonbiological drugs:
    • Immunosuppressants: Methotrexate, Azathioprine, Cyclosporine
    • Sulfasalazine, Chloroquine, Hydroxychloroquine, Leflunomide
  3. Biological agents:
    • TNF α-inhibitors: Etanercept, Infliximab, Adalimumab
    • IL-1 antagonist: Amakinra
  4. Adjuvant drugs: Prednisolone and other glucocorticoides

H. Drugs for Gout:

  1. Acute gout: NSAIDS, Colchicine, Glucocorticoids
  2. Chronic gout / Hyperuricemia:
    • Uricosurics: Probenecid, Sulfinpyrazone
    • Synthesis inhibitors: Allopurinol, Febuxostat

Last modified on: 13/10/2024

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