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    Cholinergic Blocking Agents

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    shivanshpande
    This document discusses anticholinergic drugs, which block the actions of acetylcholine at parasympathetic nerve endings. It focuses on atropine, a tertiary amine alkaloid that acts as a competitive antagonist at muscarinic receptor sites throughout the body. The document outlines atropine's pharmacological actions, pharmacokinetics, uses for conditions like peptic ulcer and Parkinson's disease, adverse effects like dry mouth and blurred vision, and treatment of atropine poisoning with a physostigmine antidote.

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    Cholinergic Blocking Agents

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    shivanshpande
    141 views14 pages
    This document discusses anticholinergic drugs, which block the actions of acetylcholine at parasympathetic nerve endings. It focuses on atropine, a tertiary amine alkaloid that acts as a competitive antagonist at muscarinic receptor sites throughout the body. The document outlines atropine's pharmacological actions, pharmacokinetics, uses for conditions like peptic ulcer and Parkinson's disease, adverse effects like dry mouth and blurred vision, and treatment of atropine poisoning with a physostigmine antidote.

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    This document discusses anticholinergic drugs, which block the actions of acetylcholine at parasympathetic nerve endings. It focuses on atropine, a tertiary amine alkaloid that acts as a competitive antagonist at muscarinic receptor sites throughout the body. The document outlines atropine's pharmacological actions, pharmacokinetics, uses for conditions like peptic ulcer and Parkinson's disease, adverse effects like dry mouth and blurred vision, and treatment of atropine poisoning with a physostigmine antidote.

    Copyright:

    Attribution Non-Commercial (BY-NC)
    Download as PPTX, PDF, TXT or read online from Scribd
    Download as pptx, pdf, or txt
    141 views14 pages

    Cholinergic Blocking Agents

    Uploaded by

    shivanshpande
    This document discusses anticholinergic drugs, which block the actions of acetylcholine at parasympathetic nerve endings. It focuses on atropine, a tertiary amine alkaloid that acts as a competitive antagonist at muscarinic receptor sites throughout the body. The document outlines atropine's pharmacological actions, pharmacokinetics, uses for conditions like peptic ulcer and Parkinson's disease, adverse effects like dry mouth and blurred vision, and treatment of atropine poisoning with a physostigmine antidote.

    Copyright:

    Attribution Non-Commercial (BY-NC)
    Download as PPTX, PDF, TXT or read online from Scribd
    Download as pptx, pdf, or txt
    of 14

    4/13/2012

    CHOLINERGIC BLOCKING AGENTS/ PARASYMPATHOLYTICS/ ANTICHOLINERGICS

    By: Shivansh Pande


    Clinical Pharmacist Apollo Health City, Hyderabad
    1

    4/13/2012

    ANTICHOLINERGIC DRUGS

    Anticholinergic drugs block or interfere with the actions of acetylcholine (ACh) at the postganglionic parasympathetic nerve endings.

    Nicotinic receptor blockade neuromuscular blocking agents Muscarinic receptor blockade Anticholinergic agents (atropine and congeners)

    4/13/2012

    CLASSIFICATION

    Natural alkaloids: Atropine, Hyoscine (scopolamine) Semisynthetic derivatives: homatropine, atropine methonitrate, hyoscine butyl bromide, ipratropium bromide, tiotropium bromide Synthetic compounds:

    a) Mydriatics: Cyclopentolate, Tropicamide b) Antisecretory-antispasmodics:


    (i) Quarternary ammonium compounds: Propantheline, oxyphenonium, clidinium, pipenzolate, isopropamide. (ii) Tertiary amines: Dicyclomine, Oxybutynin, flevoxate, pirenzepine

    c) Antiparkinsonian: Trihexyphenidyl, procyclidine, biperiden, benztropine


    3

    4/13/2012

    MECHANISM OF ACTION
    Prolonged occupation of muscarinic cholinergic receptors Competitive antagonism of acetylcholine at muscarinic receptor sites (smooth muscle, cardiac muscle, exocrine glands and CNS)

    4/13/2012

    ATROPINE
    Tertiary amine alkaloid ester of tropic acid From Atropa belladona (deadly nightshade) and Datura stramonium (jimsonweed or Jamestown weed) Scopolamine (hyoscine) from Hyoscyamus niger

    4/13/2012

    PHARMACOLOGICAL ACTIONS (ATROPINE)

    CNS

    In normal dose: Stimulation In toxic dose: Overexcitation, euphoriaCerebral Toxic syndrome (talkative, disorientated)Followed by depression, stupor, coma.

    Respiratory System

    Small Dose: StimulationBronchodilation and reduced bronchial secretion Toxic dose: Respiratory depression
    6

    4/13/2012

    PHARMACOLOGICAL ACTIONS CONTD.

    Cardiovascular System

    HR Small dose: Central vagus stimulation HR. Large dose: Peripheral vagus blockade; HR Very large doses: Postural hypotension due to peripheral vascular pooling.Atropine flush

    GIT

    Tone and movement of the gut (peristalsis) Gastric secretion Relaxes gall bladder and bile duct
    7

    4/13/2012

    PHARMACOLOGICAL ACTIONS CONTD..

    Other Smooth muscles


    tone and contraction of ureter Detrusor muscle relaxed. No significant effect in the uterus secretions from mouth, nose, pharynx. Sweating. Skin becomes hot and dry. Mydriasis (passive)Relaxation of circular muscles Cycloplegia weaken contraction of the ciliary muscleloss of accomodation lacrimal secretion Aqueous drainage, IOT.
    8

    Secretions

    Eye

    4/13/2012

    PHARMACOKINETICS

    Absorption Readily and completely absorbed from the GIT. Distribution Significant plasma protein binding. Atropine is 50% excreted unchanged in the kidneys. Effects decline rapidly in all organs except the eye (>72 hrs)
    9

    4/13/2012

    USES/ INDICATIONS

    CNS disorders:

    Motion sickness (scopolamine): Prevent nausea and vomitting Antiparkinsonism (benzhexol, procyclidine, benztropine): Reduces tremor and rigidity.

    Antispasmodic (dicyclomine, atropine, oxyphenonium): Intestinal, urinary and biliary tract relaxation. Bronchodilation (ipratropium) Antisecretory (Propantheline): Reduce gastric secretion in peptic ulcer. Reduce sweating in night sweats.
    10

    4/13/2012

    USES/ INDICATIONS CONTD.

    Preanaesthetic Medication (atropine): Reduce salivary and bronchial secretions. Ophthalmic (atropine, homatropine, tropicamide):

    As a mydriatic for measurement of refractive errors. Relief of corneal ulcer (LA activity) Alternating with miotics to break ahdseions between cornea and iris.

    Cardiac stimulant in vasovagal syncope. Antidote in anticholinesterase poisoning Urinary incontinence (enuresis)

    11

    4/13/2012

    ADVERSE REACTIONS
    Dryness of mouth and throat (xerostomia) Skin is dry, hot and red (atropine flush) Hyperpyrexia Blurred vision, loss of accommodation, may precipitate glaucoma. Urinary retention Palpitation and tachycardia Constipation

    12

    4/13/2012

    ATROPINE POISONING
    Acute poisoning may result due to dose error. Symptoms

    Severe dryness of mouth and throat. Wide pupillary dilation Dysphagia and thirst Tachycardia Redness of skin, body temperature Uncoordinated muscle movements. Delirium, hallucinations, mania, apathy, stupor Strenous breathing, coma, respiratory collapse

    13

    4/13/2012

    ATROPINE POISONING CONTD.

    Treatment:
    Specific

    antidote (physostigmine salicylate) Ice cap and cold sponging Respiratory stimulants like caffeine with sodium benzoate or oxygen-carbon dioxide mixtures. Artificial respiration if necessary. Diazepam if required for mental symptoms Usual supportive measures.

    14

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