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    Parasympathomimetic Drugs

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    ChAwais
    This document summarizes parasympathomimetic or cholinergic drugs. These drugs act similarly to stimulation of the parasympathetic nervous system. They can have muscarinic effects through G-protein coupled receptors or nicotinic effects via ion channels. Examples include direct-acting agonists like acetylcholine and indirect-acting anticholinesterases. Specific drugs like pilocarpine, methacholine, and nicotine are discussed along with their mechanisms and uses.

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    Parasympathomimetic Drugs

    Uploaded by

    ChAwais
    803 views29 pages
    This document summarizes parasympathomimetic or cholinergic drugs. These drugs act similarly to stimulation of the parasympathetic nervous system. They can have muscarinic effects through G-protein coupled receptors or nicotinic effects via ion channels. Examples include direct-acting agonists like acetylcholine and indirect-acting anticholinesterases. Specific drugs like pilocarpine, methacholine, and nicotine are discussed along with their mechanisms and uses.

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    This document summarizes parasympathomimetic or cholinergic drugs. These drugs act similarly to stimulation of the parasympathetic nervous system. They can have muscarinic effects through G-protein coupled receptors or nicotinic effects via ion channels. Examples include direct-acting agonists like acetylcholine and indirect-acting anticholinesterases. Specific drugs like pilocarpine, methacholine, and nicotine are discussed along with their mechanisms and uses.

    Copyright:

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

    Parasympathomimetic Drugs

    Uploaded by

    ChAwais
    This document summarizes parasympathomimetic or cholinergic drugs. These drugs act similarly to stimulation of the parasympathetic nervous system. They can have muscarinic effects through G-protein coupled receptors or nicotinic effects via ion channels. Examples include direct-acting agonists like acetylcholine and indirect-acting anticholinesterases. Specific drugs like pilocarpine, methacholine, and nicotine are discussed along with their mechanisms and uses.

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    © All Rights Reserved
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    Download as ppt, pdf, or txt
    of 29

    PARASYMPATHOMIMETIC DRUGS

    OR
    CHOLINERGIC DRUGS
    OR
    CHOLINOMIMETIC DRUGS
    OR
    CHOLINOCEPTOR ACTIVATING DRUGS

    DEFINITION
    These are the group of drugs which produce
    effects resembling those produced by the
    stimulation of parasympathetic autonomic
    nervous system on the target organs

    Neurotransmitter
    Two types of activities
    Muscarinic
    Nicotinic

    SYNTHESIS, STORAGE,

    RELEASE & INACTIVATION

    MECHANISM OF
    ACTION
    G protein linked (Muscarinic)
    Ion channel (Nicotinic)

    PHOSPHO INOSITOL SYSTEM


    BINDING OF DRUG WITH RECEPTOR

    (ALPHA-1 ADRENDERGIC, MUSCARINIC- CHOLINERGIC)


    ACTIVATION OF PHOSPHOLIP
    PHOSPHATIDYL INOSITOL 4-5 BIPHOSPHATE

    DIACYL GLYCEROL
    (CONFINEDTO MEMBRANE)

    ACTIVATION OF PROTEIN KINASEC


    INTRACELLULAR
    ENTRY OF Ca++ THROUGH THE CA++

    INOSITOL 1.4.5 TRIPHOSPHATE


    (DIFFUSES INTO CYTOSOL)

    RELEASE OF Ca++ FROM


    SOURCES

    FORMATION OF Ca++ CALMODULIN


    COMPLEX

    CHANNEL

    ALTERATION IN THE ACTIVITY OF C


    DEPENDENT ENZYMES

    EFFECT

    CHOLINERGIC RECEPTORS
    Muscarinic
    M1 = Nerves, Stomach, Brain
    Antagonist:

    Pirenzepine

    M2 = Heart, Nerves, Smooth Muscle.


    Antagonist:

    Gallamine

    M3 = Glands, Endothelium, Smooth Muscle.

    M4 and M5 newly discovered, role not yet known

    Nicotinic
    Neuromuscular Junction
    Agonist: Phenyl Trimethyl Ammonium
    Antagonist: Tubocurarine
    Autonomic Ganglia, Adrenal Medulla
    Agonist:

    Dimethyl phenyl piperazinium

    Antagonist: Hexamethonium

    CLASSICIFICATION
    A. Directly Acting
    B. Indirectly Acting

    A. Directly Acting Cholinergic


    Drugs :
    I. Choline Esters
    Acetylcholine
    Carbachol
    Methacholine
    Bethanechol

    II. Cholinomimetic Alkaloids


    a. Mainly Muscarinic Agonists
    Natural Alkaloids:
    Muscarine
    Pilocarpine
    Arecholine
    Synthetic Alkaloid:
    Oxotramorine
    b. Mainly Nicotinic Agonists
    Natural Alkaloids:
    Nicotine
    Lobeline
    Synthetic Alkaloids:
    Dimethylphenylpiperazinium(DMPP)

    B. Indirectly Acting Cholinergic Drugs


    (Anticholinesterases)

    I- Reversible
    a. Carbamates
    b. Alcohols
    II- Irreversible

    I- Reversible
    a. Carbamates
    Tertiary amines
    Physostigmine
    Quaternary Ammonium compounds
    Neostigmine
    Pyridostigmine
    Distigmine
    Ambenonium
    Demecarium

    b. Alcohols
    Edrophonium

    c. Miscellaneous
    Tacrine
    Donepezil
    Galantamine
    Rivastigmine

    II. Irreversible Anticholinesterases


    (Organophosphorus Compounds)
    1) Therapeutically useful:
    Ecothiophate

    2)

    War Gases:
    Sarin
    Tuban,
    Soman

    3)

    Insecticides:Parathion
    Malathion
    Diisopropyl Flurophosphate (DFP)
    Tetramethyl Pyrophosphate (TMPP)
    Octamethyl Pyrophosphotetraamide (OMPA)

    ACETYLCHOLINE
    NOT USED AS A DRUG

    CHEMISTRY
    CHEMISTRY

    PHARMACOKINETICS

    Acetylcholine & other Choline esters have a


    permanently charged quaternary ammonium group
    in their structure
    All are hydrolysed in the GIT
    The tertiary natural cholinomimetic alkaloids
    (pilocarpine, nicotine, lobeline) are well absorbed from
    most sites of adm. Muscarine, a quaternary amine is
    less completely absorbed from the GIT and is toxic too.
    Excretion mainly by the kidneys

    Pharmacological Actions/ 0rgan


    system effects:
    Muscarinic Actions
    Nicotinic Actions

    EYE:

    Miosis (constriction of pupil).


    Spasm of accommodation
    Decrease in intraocular pressure.
    Conjunctival hyperaemia
    Lacrimation

    CVS (Heart & B.V)


    Respiratory system
    Gastro intestinal tract
    Urinary bladder
    Exocrine glands
    Central Nervous System
    Peripheral nervous system
    N.M .Junction

    CARBACHOL

    Ester of carbamic acid


    Has both muscarinic and nicotinic actions
    Muscarinic actions are prominent on eye, GIT &
    urinary bladder
    DOA more than 30 min
    Therapeutic uses:
    Glaucoma

    METHACHOLINE

    Has methyl group in its structure


    Has both muscarinic and nicotinic actions
    (very mild nicotinic actions )
    Muscarinic actions are prominent on CVS
    Longer DOA as compared to ACh
    Therapeutic uses: given SC for the relief
    of paroxysmal atrial tachycardia

    BETHANECHOL

    Structure related to Ach, acetate is replaced by


    carbamate & choline is methylated
    Has no nicotinic actions
    Muscarinic actions are prominent on eye, GIT &
    urinary bladder
    Prolonged DOA
    Therapeutic uses:

    Post operative Gastric distension


    Paralytic ileus
    Bladder atonia

    MUSCARINE

    Quaternary amine (Amanita muscaria)


    Less complete absorption from the GIT
    Very toxic & can even enter the brain
    Rx : Atropine

    PILOCARPINE

    Tertiary amine (Pilocarpus jaborandi leaves)


    Has muscarinic actions
    Therapeutic uses:

    Glaucoma
    To reduce the effect of mydriatics
    To break adhesions

    Not used for systemic diseases


    increased
    tracheobronchial secretions leading to
    pulmonary oedema

    NICOTINE & LOBELINE

    Plant derivatives
    Actions are mainly on nicotinic receptors (CNS,
    PNS, NMJ)
    CNS, have important effects on brainstem and
    cortex.
    PNS autonomic ganglia.
    NMJ, immediate depolarization of the end plate
    increase in permeability to Na and K ions.

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