Distigmine bromide


Generic Medicine Info
Indications and Dosage
Oral
Myasthenia gravis
Adult: Initially, 5 mg daily preferably 30 minutes before breakfast, increased to 7.5 mg daily on the 2nd week then to 10 mg on the 3rd week. Max: 20 mg daily, as necessary. Individualised dosage depending on the severity and patient’s response.

Oral
Neurogenic bladder disorders
Adult: 5 mg daily 30 minutes before breakfast until the onset of action. Maintenance: 5-10 mg at 2-3 day intervals.

Oral
Chronic hypotonic constipation, Megacolon
Adult: Initially, 2.5 mg daily preferably 30 minutes before breakfast, may increase in increments of 2.5 mg every 3 days interval up to Max 10 mg daily, continue treatment until normal intestinal function has been restored (10-14 days).

Oral
Postoperative gastrointestinal atony, Postoperative urinary retention
Adult: 5 mg daily preferably before breakfast.
Administration
Should be taken on an empty stomach. Take 30 min before breakfast.
Contraindications
Obstructive and/or spastic conditions of the intestinal tract, biliary or urinary tract; iritis, bronchial asthma; severe hypotonia, myotonia, tetany, epilepsy, Parkinson’s syndrome; thyrotoxicosis, decompensated cardiac insufficiency, MI, arrhythmias, especially AV block.
Special Precautions
Patient with gastric ulcer, duodenal ulcer, bradycardia, hypotension, enteritis, organic obstruction of the digestive tract or urinary tract, mild to moderate vagotonia, recent intestinal and bladder surgery, hyperthyroidism. Pregnancy and lactation.
Adverse Reactions
Cardiac disorders: Bradycardia, ventricular tachycardia. Rarely, angina, arrhythmia.
Eye disorders: Miosis, lacrimation, cycloplegia, blurred vision.
Gastrointestinal disorders: Nausea, vomiting, abdominal pain, diarrhoea, increased salivation.
Musculoskeletal and connective tissue disorders: Muscle spasm, weakness, fascination, skeletal muscle paralysis.
Nervous system disorders: Dizziness, drowsiness, headache, dysarthria, grand mal seizures
General disorders and admin site conditions: Sweating.
Respiratory, thoracic and mediastinal disorders: Hypersecretion in respiratory tract.
Vascular disorder: Hypotension.
Patient Counseling Information
This drug may cause visual disturbances and miosis, if affected, do not drive or operate machinery.
Monitoring Parameters
Rule out neurogenic bladder emptying intravesical obstruction prior to treatment.
Overdosage
Symptoms: Cholinergic crisis characterised by excessive sweating, lacrimation, miosis, ciliary spasm, nystagmus, increased peristalsis, involuntary defaecation and urination, bradycardia, hypotension, muscle cramps, fasciculation, weakness, paralysis, tight chest, wheezing, bronchoconstriction, bradycardia, blood pressure drop, bronchospasm, paradoxical tachycardia; ataxia, convulsions, coma, slurred speech, restlessness, agitation and fear. Treatment: Supportive treatment. Assisted respiration and oxygen may be given as required. For severe poisoning, initiate stomach aspiration. Administer atropine 1-2 mg IV or IM for suppression of muscarinic effects, may be repeated until signs of mild atropism (e.g. dry mouth, mydriasis) appear. May antagonise effect with cholinesterase reactivators (e.g. pralidoxime).
Drug Interactions
Anticholinergics (e.g. atropine), TCA, tetracyclic antidepressants, neuroleptics, lithium, nondepolarizing muscle relaxant, and antihistamines may antagonise the effect of distigmine bromide. Decreased effect with aminoglycoside antibiotics (e.g. neomycin, streptomycin, kanamycin), antiarrhythmic agents (e.g. quinidine, procainamide), ß-blockers, glucocorticoids and dipyridamole. Potentiated effect with esterase inhibitors. Prolonged effect with depolarising muscle relaxants (e.g. succinylcholine, decamethonium).
Action
Description: Distigmine bromide, a quaternary ammonium compound, is a reversible cholinesterase inhibitor that enhance the action of acetylcholine thereby increasing the tonicity and peristalsis in the gastrointestinal tract, increasing the wall tension of urinary bladder, sphincter, ureter and of the skeletal muscles and reduces intraocular pressure.
Duration: Approx 24 hours (IM).
Pharmacokinetics:
Absorption: Poorly absorbed from the gastrointestinal tract. Bioavailability: 5%.
Metabolism: Hydrolysed by plasma esterases.
Excretion: Oral: Via faeces (88%), urine (6.5%); IV: Via urine (85%), faeces (4%). Plasma elimination half-life: 70 hours (oral); 60 hours (IV).
Chemical Structure

Chemical Structure Image

Source: National Center for Biotechnology Information. PubChem Database. Distigmine bromide, CID=27522, https://pubchem.ncbi.nlm.nih.gov/compound/Distigmine-bromide (accessed on Jan. 21, 2020)

Storage
Store below 25°C. Protect from light.
ATC Classification
N07AA03 - distigmine ; Belongs to the class of anticholinesterase. Used as parasympathomimetics.
References
Buckingham R (ed). Distigmine Bromide. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 03/06/2019.

Ubretid (Globopharm, Austria). MIMS Singapore. http://www.mims.com/singapore. Accessed 03/06/2019.

Disclaimer: This information is independently developed by MIMS based on Distigmine bromide from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2021 MIMS. All rights reserved. Powered by MIMS.com
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