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    Lecture 11 - Drugs That Act On Acetylcholine Receptors

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    The document discusses drugs that act on acetylcholine receptors, including muscarinic agonists like bethanechol and pilocarpine which are used to treat conditions like paralytic ileus and glaucoma. Muscarinic antagonists like atropine and hyoscine are used pre-operatively to inhibit secretions and as mydriatics, while ganglion stimulants like nicotine and blockers like trimetaphan act on autonomic ganglia to affect blood pressure, heart rate, and gastrointestinal motility. The learning objectives cover the clinical uses and effects of muscarinic drugs as well as the consequences of ganglionic blockade

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    Lecture 11 - Drugs That Act On Acetylcholine Receptors

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    api-3703352
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    The document discusses drugs that act on acetylcholine receptors, including muscarinic agonists like bethanechol and pilocarpine which are used to treat conditions like paralytic ileus and glaucoma. Muscarinic antagonists like atropine and hyoscine are used pre-operatively to inhibit secretions and as mydriatics, while ganglion stimulants like nicotine and blockers like trimetaphan act on autonomic ganglia to affect blood pressure, heart rate, and gastrointestinal motility. The learning objectives cover the clinical uses and effects of muscarinic drugs as well as the consequences of ganglionic blockade

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    Lecture 11 - Drugs That Act on Acetylcholine Receptors

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    The document discusses drugs that act on acetylcholine receptors, including muscarinic agonists like bethanechol and pilocarpine which are used to treat conditions like paralytic ileus and glaucoma. Muscarinic antagonists like atropine and hyoscine are used pre-operatively to inhibit secretions and as mydriatics, while ganglion stimulants like nicotine and blockers like trimetaphan act on autonomic ganglia to affect blood pressure, heart rate, and gastrointestinal motility. The learning objectives cover the clinical uses and effects of muscarinic drugs as well as the consequences of ganglionic blockade

    Copyright:

    Attribution Non-Commercial (BY-NC)
    Download as PPT, PDF, TXT or read online from Scribd
    Download as ppt, pdf, or txt
    587 views26 pages

    Lecture 11 - Drugs That Act On Acetylcholine Receptors

    Uploaded by

    api-3703352
    The document discusses drugs that act on acetylcholine receptors, including muscarinic agonists like bethanechol and pilocarpine which are used to treat conditions like paralytic ileus and glaucoma. Muscarinic antagonists like atropine and hyoscine are used pre-operatively to inhibit secretions and as mydriatics, while ganglion stimulants like nicotine and blockers like trimetaphan act on autonomic ganglia to affect blood pressure, heart rate, and gastrointestinal motility. The learning objectives cover the clinical uses and effects of muscarinic drugs as well as the consequences of ganglionic blockade

    Copyright:

    Attribution Non-Commercial (BY-NC)
    Download as PPT, PDF, TXT or read online from Scribd
    Download as ppt, pdf, or txt
    of 26

    DRUGS THAT ACT ON ACETYLCHOLINE RECEPTORS

    Muscarinic agonists
    (parasympathomimetic)
    Direct-acting
    Muscarinic antagonists
    Muscarinic (parasympatholytic)

    Indirect-acting Anticholinesterases

    Nicotinic (nicotine)
    agonists
    Ganglion-acting

    Nicotinic Ganglion blockers


    Neuromuscular
    blockers
    MUSCARINIC AGONISTS
    Agonist Structure Selectivity Hydrolysis
    CH3
    O
    Ach +
    N CH3 Muscarinic, Very rapid
    H3 C O nicotinic
    CH3
    CH3
    O
    Carbachol + Muscarinic, No
    N CH3 nicotinic
    H2 N O
    CH3

    CH3
    O CH3
    Methacholine + Muscarinic rapid
    N CH3
    H3 C O
    CH3
    MUSCARINIC AGONISTS (cont’d)

    Agonist Structure Selectivity Hydrolysis

    CH3
    Bethanechol O CH3 Muscarinic No
    +
    N CH3
    H2 N O
    CH3

    Pilocarpine CH3 Muscarinic No


    H3 C N
    O O N
    CLINICAL USES OF MUSCARINIC
    AGONISTS
     Paralytic ileus (Bethanechol)
     Urinary retention (Bethanechol)
     Miotic in cataract surgery (Ach)
     Testing for bronchial hyperreactivity
    (Methacholine)
     Glaucoma (Pilocarpine, carbachol)
    THE EYE
    The eye

    Canal of Iris
    Schlem

    Lens

    Trabecular Ciliary Muscle


    meshwork
    Side Effects of Muscarinic Agonists

    a. Hypotension (vasodilation, via NO) and


    reflex tachycardia (overrides bradycardia)

    b. Bronchospasm (no significance in normals


    but may precipitate asthma in asthmatics).

    c. Others (nausea & vomiting, GIT cramps and


    diarrhoea).
    Contra-Indications of Muscarinic Agonists

    a. Coronary insufficiency (worsened by


    hypotension).

    b. Hyperthyroidism (may precipitate atrial


    arrhythmias).
    c. Peptic ulcer
    d. Asthma
    MUSCARINIC ANTAGONISTS
    SOME IMPORTANT MUSCARINIC
    ANTAGONISTS
     Atropine, an alkaloid found in
    Deadly Nightshade (Atropa belladonna)

     Hyoscine (scopolamine) -another plant product


     Homatropine - a synthetic analogue of
    atropine with briefer action
     Pirenzepine - a member with selectivity for
    M1 subclass
     Ipratropium - quarternary nitrogen compound
    PHARMACOLOGICAL ACTIONS OF
    MUSCARINIC ANTAGONISTS

    Peripheral
     Blocks secretions (saliva, bronchial, GIT, etc.)
     Dilates pupil (mydriasis)

     Tachycardia (block of vagal influence)

     Blocks GIT motility (constipation)

     Relaxes bronchial smooth muscles


    CNS
     Atropine has no effect at low dose
    (excitation at high dose)

     Hyoscine depressant at therapeutic dose


    (sedation, drowsiness, amnesia)

     Antiemetic (Hyoscine)
    CLINICAL USES OF MUSCARINIC
    ANTAGONISTS

    1. In surgery: as pre-anaesthetic to inhibit


    salivary and bronchial secretions (atropine,
    hyoscine)

    2. As mydriatic to dilate pupil and paralyse


    lens for eye examination and treatment,
    (short lasting homatropine; long-lasting
    atropine).
    3. In the treatment of anticholinesterase
    poisoning (atropine)

    4. Treatment of Motion sickness (hyoscine)

    5. Treatment of peptic ulcer (pirenzepine)

    6. Treatment of GIT cramps (atropine, hyoscine)


    7. Treatment of asthma and chronic bronchitis
    (ipratropium)

    8. Treatment of Parkinson's disease


    (atropine, benzatropine)

    9. Treatment of sinus bradycardia after MI


    (atropine)
    SIDE EFFECTS OF MUSCARINIC
    ANTAGONISTS
     Dry mouth and skin

     Blurring of vision
     Tachycardia
     Skin blush and increased body temperature
    (poisoning)
     Behavioural disturbances (poisoning)
     Glaucoma in pre-disposed
    DRUGS ACTING ON
    AUTONOMIC GANGLIA
    GANGLION STIMULANTS

    NICOTINE

     Major Constituent of tobacco

     In low doses stimulates all ganglia

     In high doses blocks all ganglia


    STIMULANT EFFECTS OF LOW DOSE
    NICOTINE ON AUTONOMIC GANGLIA

    • Rise in blood pressure

    • Tachycardia
    (bradycardia overridden by release of Adrenaline)

    • Increase in GIT motility

    • Release of antidiuretic hormone


    GANGLION BLOCKING DRUGS

     Hexamethonium (now of historical interest)

     Trimetaphan (only clinically used member)


    ACTIONS OF GANGLION BLOCKERS

     Cardiovascular system
    Fall in blood pressure & loss of cardiovascular reflex (sy(mpath

     Gastrointestinal tract:
    Inhibition of motility and secretions (constipation)((parasymp

    Genitourinary system:
    Impairment of micturition, failure of erection (parasymp)
    Failure of ejaculation (sympath)
    Eye:
    Loss of accommodation/blurred vision, loss of pupillar
    reflex/photophobia (parasymp)
    Uses of Ganglion Blockers

    Originally used to treat hypertension-


    but no longer in use
    OnlyTrimethaphan is occassionally used-
    for controlled hypotension during surgery
    LEARNING OBJECTIVES

    Describe the clinical uses of muscarinic agonists and antagonists .1


    pointing out any pharmacodynamic and the pharmacokinetic factors
    .that govern the choice of drugs

    .List the adverse effects and contra-indications of muscarinic agonists .2

    Explain the mechanism of hypotensive action of intravenous .3


    .muscarinic agonists

    Understand glaucoma and how muscarinic agonists work in .4


    .its treatment

    Compare and contrast the actions and clinical uses of atropine and .5
    .hyoscine

    .Know why muscarinic antagonists are contra-indicated in glaucoma .5

    .List the consequences of ganglionic blockade .6


    PHARMACOLOGICAL ACTIONS OF
    MUSCARINIC ANTAGONISTS

     Dilation of pupil (mydriasis)


     Inhibition of secretions
     Increase in heart rate
     Inhibition of GIT motility
     Bronchodilation
    MUSCARINIC ANTAGONISTS
    (PROTOTYPE DRUGS)

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