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Botany 3% exam weight

Topic 6

Part of the INI CET (AIIMS PG) study roadmap. Botany topic pharma-006 of Botany.

Autacoids: Histamine and Antihistamines covers autacoids — histamine and antihistamines for INI CET (AIIMS PG).

Autacoids: Locally produced, short-acting chemical messengers (histamine, serotonin, prostaglandins, leukotrienes, kinins).

Histamine:

  • Synthesis: Histidine (via histidine decarboxylase) → Histamine
  • Storage: Mast cells and basophils (in granules — preformed, released immediately)
  • Release triggers: Type I hypersensitivity (IgE-mediated), complement fragments (C3a, C5a — anaphylatoxins), physical agents (cold, trauma), drugs (morphine, tubocurarine), food allergens
  • Receptors:
    • H₁ receptor (GPCR — Gq): Smooth muscle (bronchoconstriction, GI contraction), vascular endothelium (↑NO → vasodilation, ↑vascular permeability → edema), nasal mucosa (sneezing, rhinorrhea) — ALLERGIC reactions
    • H₂ receptor (GPCR — Gs): Gastric parietal cells (↑HCl secretion) — PEPTIC ULCER disease; heart (↑HR), uterus (relaxation)

Antihistamines (H₁ blockers):

  • First-generation (sedating) — cross BBB:
    • Diphenhydramine: Allergy, motion sickness (antiemetic), insomnia; side effects: sedation, anticholinergic (dry mouth, urinary retention, constipation)
    • Dimenhydrinate: Motion sickness (Dramamine)
    • Promethazine: Allergy, sedation, antiemetic
    • Chlorpheniramine: Common cold (less effective than for true allergy)
  • Second-generation (non-sedating) — do NOT cross BBB significantly:
    • Cetirizine: Active metabolite of hydroxyzine; some anticholinergic effect
    • Loratadine: Non-sedating even at high doses
    • Desloratadine: Active metabolite of loratadine
    • Fexofenadine: Active metabolite of terfenadine (terfenadine withdrawn for QT prolongation)
    • Levocetirizine: Active isomer of cetirizine
    • Azelastine: Nasal spray for allergic rhinitis

Clinical Uses of H₁ Antihistamines:

  • Allergic rhinitis (seasonal/perennial) — nasal congestion, sneezing, rhinorrhea, itching
  • Allergic conjunctivitis
  • Urticaria (hives) and angioedema
  • Anaphylaxis (adjunct to epinephrine — epinephrine is first-line for anaphylaxis)
  • Motion sickness (first-generation — antiemetic effect via vestibular pathways)
  • Insomnia (first-generation — CNS depression)
  • Common cold (limited value — rhinovirus not histamine-mediated)

Exam Tip for INI CET (AIIMS PG): Second-generation antihistamines (cetirizine, loratadine, fexofenadine) are non-sedating because they do NOT cross the blood-brain barrier. First-generation (diphenhydramine) cause sedation because they DO cross the BBB and block H₁ receptors in the CNS.