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    Autocoid Pharmacology

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    Lyadelou Fortu
    Autacoids are biological factors that act on smooth muscle and include eicosanoids, angiotensin, nitric oxide, kinins, histamine, serotonin, and endothelins. Histamine is stored in mast cells in tissues like skin, lungs, and gut and triggers smooth muscle contraction and allergic responses. It signals through H1, H2, H3, and H4 receptors. H1 receptor antagonists are used to treat allergies while H2 receptor antagonists inhibit stomach acid secretion and are used to treat ulcers and reflux. While effective, older H1 antagonists have anticholinergic effects while newer ones have fewer side effects.

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    Autocoid Pharmacology

    Uploaded by

    Lyadelou Fortu
    247 views29 pages
    Autacoids are biological factors that act on smooth muscle and include eicosanoids, angiotensin, nitric oxide, kinins, histamine, serotonin, and endothelins. Histamine is stored in mast cells in tissues like skin, lungs, and gut and triggers smooth muscle contraction and allergic responses. It signals through H1, H2, H3, and H4 receptors. H1 receptor antagonists are used to treat allergies while H2 receptor antagonists inhibit stomach acid secretion and are used to treat ulcers and reflux. While effective, older H1 antagonists have anticholinergic effects while newer ones have fewer side effects.

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    Autacoids are biological factors that act on smooth muscle and include eicosanoids, angiotensin, nitric oxide, kinins, histamine, serotonin, and endothelins. Histamine is stored in mast cells in tissues like skin, lungs, and gut and triggers smooth muscle contraction and allergic responses. It signals through H1, H2, H3, and H4 receptors. H1 receptor antagonists are used to treat allergies while H2 receptor antagonists inhibit stomach acid secretion and are used to treat ulcers and reflux. While effective, older H1 antagonists have anticholinergic effects while newer ones have fewer side effects.

    Copyright:

    © All Rights Reserved
    Download as PPT, PDF, TXT or read online from Scribd
    Download as ppt, pdf, or txt
    247 views29 pages

    Autocoid Pharmacology

    Uploaded by

    Lyadelou Fortu
    Autacoids are biological factors that act on smooth muscle and include eicosanoids, angiotensin, nitric oxide, kinins, histamine, serotonin, and endothelins. Histamine is stored in mast cells in tissues like skin, lungs, and gut and triggers smooth muscle contraction and allergic responses. It signals through H1, H2, H3, and H4 receptors. H1 receptor antagonists are used to treat allergies while H2 receptor antagonists inhibit stomach acid secretion and are used to treat ulcers and reflux. While effective, older H1 antagonists have anticholinergic effects while newer ones have fewer side effects.

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    of 29

    AUTOCOID

    PHARMACOLOGY

    AUTOCOIDS
    biological factors that are primarily
    characterized by the effect they have
    upon smooth muscle
    VASODILATOR AUTOCOIDS can be
    released during periods of exercise
    comes from the GREEK "autos"(self)
    and "acos"(drug)

    SOME NOTABLE AUTOCOIDS:

    eicosanoids
    angiotensin
    neurotensin
    nitric oxide
    kinins
    histamine
    serotonin
    endothelins

    DISTRIBUTION, TURNOVER and


    STORAGE OF HISTAMINES

    tissues- 1 to over 100mg/g


    plasma- normally very low
    CSF- high
    brain, stomach, healing tissues
    and some cells in the skin histamine
    is not stored in granules
    identical to mast cells therefore
    wherever mast cells are, there will
    most likely be histamine present

    MAST CELLS ARE DISTRIBUTED IN:

    skin
    bronchial mucosa
    gut mucosa
    other mucosal surfaces
    high turnover
    low steady state levels

    What triggers the release of


    histamine?

    anaphylactic triggers
    antigen specific, IgE mediated
    anaphylactoid triggers
    organic bases
    morphine
    tubocuravine
    succinylchloride
    dextran
    contrast media used in radiography
    vancomycin
    some neuropeptides
    venom from insects

    Diseases associated with


    increased histamine
    urticaria pigmentosa
    systemic mastocytosis
    myelogenous leukemia
    gastrinoma
    gut ulcers and diarrhea, urticaria,
    pruritus

    EFFECTS OF HISTAMINE IN
    HUMANS
    burning due to sensory nerve
    stimulation
    itching
    warmth
    skin flush vasodilation
    hypotension vasodilation
    headache vasodilation
    skin edema
    GI irritation
    acid hypersecretion
    bronchospasm

    HISTAMINE RECEPTORS

    H1
    H2
    H3
    all are 7 transmembrane spanning
    G coupled receptors

    HISTAMINE IN THE BRAIN

    H1 receptors in the brain


    found in hypothalamus
    affect wakefulness
    appetite suppression
    H1 and H2 receptors are involveed in:

    drinking
    BP regulation
    thermoregulation
    secretion of ADH

    HISTAMINE IN THE HEART


    in atrial and ventricular force via
    H2 receptors
    in HR
    in AV conduction time (H1
    receptors)
    arrhythmias

    HISTAMINE IN SMOOTH MUSCLES


    bronchial smooth muscle
    Gut smooth muscle
    HISTAMINE IN THE VESSELS
    H1- activates endothelial relaxation
    via NO
    H2- activates a slower onset of
    direct relaxation

    AGONIST
    - no therapeutic use
    - only used in specialties such as in
    bronchial hyperactivity testing for
    asthmatics
    - used by dermatologists as a
    +control to test for allergen activity
    ANTAGONIST
    - H1 antagonists are used to treat
    mild allergies
    - H2 antagonists are often used to
    treat peptic ulcers, dyspepsia, gastric
    reflux

    - classic H1 antagonists are


    sedative, short acting, significant
    anti-cholinergic action
    NON SEDATING H1 ANTAGONIST
    - low or zero CNS penetration
    - long acting
    - little anticholinergic effects

    IMPORTANT POINTS ABOUT SOME


    OF NEW GENERATION DRUGS:
    Polymorphic Ventricular
    Tacycardia (PVT) may occur when
    ASTEMIZOLE and TERFENADINE are
    taken in high doses in conjunction
    with erythromycin and
    clarithromycin or ketoconazole and
    itraconazole

    H1 ANTAGONISTS: GENERAL
    PROPERTIES
    both 1st and 2nd generation cmpds
    orally active and more metabolized
    by the liver using cytochrome P450
    duration of action is 4-6 hrs
    MECLIZINE and other 2nd gen drugs
    effects for about 12-24 hrs
    1st gen are relatively more
    sedating
    2nd gen are less sedating

    HISTAMINE PHARMACODYNAMICS
    H1 receptor blockers cannot affect in
    gastric acid secretion
    H1 receptor blockers do not completely
    prevent cardiovascular effects

    NON HISTAMINE RECEPTOR-MEDIATED


    EFFECTS
    1st gen H1 receptor blockers causes
    effects mediated by many other receptor
    systems, these other effects in the
    mediated
    by
    muscarinic
    cholinergic
    receptors,

    adrenergic
    receptors,
    serotonergic
    receptors
    and
    local
    anesthetics receptor sites

    SEDATION
    - common side effect of 1st gen H1
    antagonist
    - used as sleep aids (hypnotics)
    - produce a paradoxical excitement
    in children
    - toxic rxns: stimulation, agitation,
    coma

    ANTI-EMETIC/NAUSEA
    - some 1st gen H1 antagonist
    prevent motion sickness
    - should be taken well in advance
    - DIPHENHYDRAMINE
    - PROMETHAZINE
    - MECLIZINE
    less sedating
    - CYCLIZINE

    ANTI-PARKINSONISM
    - bcoz of their antimuscarinic
    properties, turn out to be effective in
    suppressing Parkinsonian symptom
    ANTI-CHOLINERGIC EFFECTS
    - some 1st gen H1 antagonists have
    strong antimuscarinic actions
    - includes blurred vision and urinary
    retention
    pxs
    w/
    benign
    prostatic
    hypertrophy are contraindicated for
    the usage of these drugs

    ALPHA ADRENERGIC BLOCKING


    EFFECTS
    - blockade of adrenergic receptor
    can cause orthostatic hypotension
    SEROTONERGIC BLOCKADE
    LOCAL ANESTHETIC EFFECTS
    DIPHENHYDRAMINE
    and
    PROMETHAZINE are more potent
    than procaine as a local anesthetic

    H1 BLOCKERS TOXICITY
    excessive excitation and convulsions
    in children
    orthostatis hypotension
    drug allergy
    1st gen overdose is similar to
    atropine overdose
    2nd gen overdose induce cardiac
    arrythmias

    H2 ANTAGONISTS
    inhibit histamine-induced stomach
    acid secretion

    CIMETIDINE
    FAMOTIDINE
    RANITIDINE
    NIZATIDINE

    EFFECTS ON ORGAN SYSTEMS

    acid secretion and gastric motility


    rdxn in gastric acid secretion
    reduced gastric acid volume
    reduced pepsin concentration
    CIMETIDINE
    - inhibits cytochrome P450
    CIMETIDINE and RANITIDINE
    - inhibit renal clearance of basic drugs
    that use renal secretory transport
    sytems

    OTHER USES: H2 RECEPTOR


    ANTAGONISTS
    PEPTIC ULCER DUODENAL DISEASE
    - reducing gastric acidity has
    advanced tx of peptic ulcer disease
    OTHER AGENTS THAT REDUCE
    GASTRIC ACID:
    OMEPRAZOLE
    and
    LANZOPRAZOLE- inhibits enzymepump w/c produces hydrogen ionsin
    the stomach

    SUCRALFATE - promotes healing


    ANTIBIOTICS - prominent in current
    therapy
    GASTRIC ULCER
    - H2 receptor antagonists reduce
    symptoms and promotes healing for
    benign gastric ulcers
    GASTROESOPHAGEAL REFLUX
    -high
    dosage
    of
    H2
    receptor
    antagonists along with proton pump
    blockers

    HYPERSECRETORY DISEASE
    ZOLLINGER ELLISON SYNDROME
    - associated with acid hypersecretion
    w/c is caused by gastrin-secreting
    tumor disorder and is often fatal
    - H2 receptor antagonists control
    symptoms

    TOXICITY: H2 RECEPTOR
    ANTAGONISTS

    diarrhea
    dizziness
    somnolence
    headache
    rash
    CIMETIDINE has the most adverse
    effects
    NIZATIDINE has the fewest side
    effects

    PREGNANCY

    harmful effects on the fetus have not


    been observed
    since these drugs can cross the
    placenta, they should only be
    prescribed when absolutely required
    DRUG-DRUG INTERACTION
    CIMETIDINE is particularly effective in
    inhibiting the cytochrome P450 drug
    metabolizing system therefore
    influencing the metabolism of other
    drugs
    reduces liver blood flow and the
    combination of effects on blood flow
    and metabolism tend to the clearance
    of certain drugs

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