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• Atropine is a prototype anticholinergic/antimuscarinic/parasympatholytic drug.
• It blocks the action of acetylcholine by blocking the muscarinic cholinergic receptors.
• It does not block nicotinic cholinergic receptors.
• It is a naturally occurring tropane alkaloid that is found in Atropa belladonna and Hyocyamus niger.
• Atropine is a racemic mixture of l-hyoscyamine and d-hyoscyamine.
• It occurs as colourless crystals or white crystalline powder. It is odourless and has bitter taste.
• Atropine is official as sulphated salt which contains one molecule of water of crystallization.
• Atropine has low solubility in water but its official salt, atropine sulphate is very soluble in water.
• It is an amino alcohol ester. It is composed of a tropine (an amino alcohol) and a tropic acid (a carboxylic acid), which form an ester bond (see image).
• In acidic or alkaline medium, it is hydrolyzed to give tropine and tropic acid.
• Storage condition: It is required to be kept in well closed containers, protected from light.
Pharmacological Actions of Atropine
• Pharmacological actions of atropine are observed mainly because it competitively antagonizes acetylcholine at the muscarinic receptor.
• Atropine doesn’t affect the nicotinic actions of acetylcholine at autonomic ganglia and skeletal muscles.
• Effect on secretions: Atropine reduces the volume and total acidity of gastric secretions. It also reduces salivary secretion (salivary glands secretion), secretions in nose, pharynx, and bronchi. It also reduces the sweat secretion.
• Effect on smooth muscles: Usually, atropine relaxes all smooth muscles such as that of gastrointestinal tract, urinary tract, bronchi, etc.
• Atropine stops excessive tone and motility of gastrointestinal tract. It does not interfere with normal peristalsis.
• Atropine reduces normal as well as drug induced ureteral peristalsis. It reduces tone of bladder muscles and tends to produce urinary retention.
• Atropine is effective in relieving the bronchospasm produced by cholinergic drugs.
• Effect on eye: On local instillation, atropine produces mydriasis by blocking the cholinergic nerve supply. It causes photophobia and ‘Paralysis of accommodation’ that is known as ‘Cycloplegia’.
• Effect on cardiovascular system: Atropine in therapeutic doses may initially decrease the heart rate because it has partial agonist property with acetylcholine. But it is followed by tachycardia. Toxic doses of atropine produce cutaneous vasodilation resulting in atropine flush and hypotension.
• Effect on CNS: Atropine in therapeutic doses stimulates the medullary vagal nuclei. This causes increase in rate and depth of respiration. At low doses, it causes slight restlessness; and at high or toxic doses it causes restlessness, agitation, hallucination.
Important Dosage, Indications and Contraindications of Atropine
• Bradycardia: 1 mg every 3 to 5 minutes upto a max. total dose of 3 mg I.V. (Adult). Repeat the doses until obtaining the desired effects.
• As preanaesthetic agent: 2 mg oral/0.2 to 1 mg I.V., I.M., or S.C. 30 to 60 min prior to anesthesia.
• Antisialogogue/Antivagal: 0.5 mg to 1 mg every 1 to 2 hours I.V. (Adult)
• Organophosphate/Muscarinic poisoning: 2 to 3 mg every 20 to 30 min I.V. (Adult)
• Irritable bowel syndrome, non-ulcer dyspepsia and diverticular disease: Adult: 0.6 to 1.2 mg as a single dose at bed time.
• Ophthalmic: Uveitis, iritis: 1% solution: Instill 1-2 drop(s) into the eye up to 4 times daily (adults).
• Contraindications: Glaucoma, Benign prostatic hyperplasia, achalasia of esophagus, paralytic ileus, severe ulcerative colitis, intestinal ileus, severe ulcerative colitis, intestinal atony, obstructive uropathy, myasthenia gravis, CHF with tachycardia.
Atropine Brand names: Atro Injection, Atrosulph, Atropine.
Atropine Poisoning/ Belladonna Poisoning
Atropine/ belladonna poisoning may occur due to drug overdose or consumption of seeds and berries of belladonna/datura plant.
Symptoms of poisoning are: Dry mouth, difficulty in swallowing and talking, dry, flushed and hot skin, fever, urinary retention, decreased bowel sounds, a scarlet rash may appear, dilated pupil (mydriasis), photophobia, blurring of near vision, hypotension, weak and rapid pulse.
The central effects include restlessness, confusion, psychotic behaviour, weakness, muscle in-coordination, hallucinations, convulsions, and coma.
Finally cardiovascular collapse with respiratory depression and failure.
Treatment
Treatment should be started in a dark quiet room to relieve photophobia. Treatment includes gastric lavage, universal antidote, anticholinesterase such as physostigmine / neostigmine and other general measures such appropriate.
MCQs
1. Which one of the following is not the therapeutic use of atropine?
(a) As a mydriatic
(b) As an antidote for organophosphate poisoning
(c) As a preanaesthetic medication
(d) As an anti-inflammatory agent
2. Atropine sulphate, a parasympatholytic drug belongs to the class _____.
(a) Amino alcohol esters
(b) Amino alkyl ethers
(c) Amino alcohols
(d) Amino amides
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Blog content and MCQs have been taken from the following:
1) Essential Pharmacy Review for Drugs Inspector Exams by Nirali Prakashan, Pune
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2) Pharmacist Recruitment Exam by Nirali Prakashan, Pune
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To know more about our DPEE book DIPLOMA IN PHARMACY EXIT EXAMINATION (DPEE) – Based on PCI-ER 2020 Syllabus (5000+ MCQs)
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PHARMACOLOGY (Second Year Diploma in Pharmacy PCI – ER 2020)
Authors: Sunil R. Bakliwal , Praneta R. Desale , Pravin P. Jawale
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