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    H2 Receptor Blockers

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    Apurba Sarker Apu
    H2 receptor antagonists are competitive antagonists that bind to the H2 receptor more strongly than histamine, preventing acid secretion. The document traces the structural evolution of cimetidine from histamine and its analogs to increasingly potent H2 receptor antagonists with improved oral bioavailability and reduced toxicity, culminating in cimetidine. There was a need to develop more potent and long-acting antisecretory agents to treat conditions like nocturnal acidity and avoid acid rebound.

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    H2 Receptor Blockers

    Uploaded by

    Apurba Sarker Apu
    155 views11 pages
    H2 receptor antagonists are competitive antagonists that bind to the H2 receptor more strongly than histamine, preventing acid secretion. The document traces the structural evolution of cimetidine from histamine and its analogs to increasingly potent H2 receptor antagonists with improved oral bioavailability and reduced toxicity, culminating in cimetidine. There was a need to develop more potent and long-acting antisecretory agents to treat conditions like nocturnal acidity and avoid acid rebound.

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    H2 receptor antagonists are competitive antagonists that bind to the H2 receptor more strongly than histamine, preventing acid secretion. The document traces the structural evolution of cimetidine from histamine and its analogs to increasingly potent H2 receptor antagonists with improved oral bioavailability and reduced toxicity, culminating in cimetidine. There was a need to develop more potent and long-acting antisecretory agents to treat conditions like nocturnal acidity and avoid acid rebound.

    Copyright:

    Attribution Non-Commercial (BY-NC)
    Download as PPT, PDF, TXT or read online from Scribd
    Download as ppt, pdf, or txt
    155 views11 pages

    H2 Receptor Blockers

    Uploaded by

    Apurba Sarker Apu
    H2 receptor antagonists are competitive antagonists that bind to the H2 receptor more strongly than histamine, preventing acid secretion. The document traces the structural evolution of cimetidine from histamine and its analogs to increasingly potent H2 receptor antagonists with improved oral bioavailability and reduced toxicity, culminating in cimetidine. There was a need to develop more potent and long-acting antisecretory agents to treat conditions like nocturnal acidity and avoid acid rebound.

    Copyright:

    Attribution Non-Commercial (BY-NC)
    Download as PPT, PDF, TXT or read online from Scribd
    Download as ppt, pdf, or txt
    of 11

    H2 receptor antagonists

    PHRM 304

    H2 receptor antagonists
    Histamine congeners Be recognized by the receptor Bind more strongly than histamine Not trigger acid secretion Competitive antagonists

    Imidazole

    Furan

    Thiazole

    Thiazole

    Structural evolution of Cimetidine:

    Histamine H1 = H2 agonist

    Structural evolution of Cimetidine:

    5-Methylhistamine A highly selective H2 agonist (H2>H1)

    Structural evolution of Cimetidine:

    N-guanylhistamine Weak antagonist Partial H2 receptor agonist Guanidine: Strongly basic group so remain as charged group

    Structural evolution of Cimetidine:


    2-4

    Methyl thiourea Neutral, non-charged

    Burimamide Full antagonist Low potency Poor oral bioavailability Toxic (Thiourea)

    Structural evolution of Cimetidine:

    Electronegative thioether

    Metiamide

    Full H2 antagonist Higher potency Improved oral bioavailability Toxic: Bone marrow toxicity (Thiourea)

    Structural evolution of Cimetidine:

    Cimetidine

    Full H2 antagonist Higher potency Improved oral bioavailability Low toxicity

    The need to develop more potent antisecretory agents:


    Acetylcholine and gastrin act on parietal cells to secrete gastric acid May develop tolerance or resistance Short acting: cannot be used in case of nocturnal acidity Acid rebound property.

    Downregulation and upregulation


    Downregulation is the process by which a cell decreases the quantity of a cellular component, such as RNA or protein, in response to an external variable. An increase of a cellular component is called upregulation.

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