Atropisole

Uses

Atropisole is used for Non ulcer dyspepsia, Irritable bowel syndrome, Diverticular disease, Bradycardia, Organophosphorus poisoning, Premedication in anesthesia, Poisoning or overdosage with compound having muscarinic actions, Ophthalmic Inflammatory eye disorders, Eye refraction.

Atropisole is also used to associated treatment for these conditions: Amblyopia, Atrioventricular Heart Block, Bradycardia, Bronchospasm, Crying, Detrusor Hyperreflexia, Excessive bronchial secretion, Hypertonic uterine contraction, Hypertonicity of the small intestine, Ocular Inflammation, Parkinsonism, Peptic Ulcer, Poisoning by parasympathomimetics (cholinergics), Poisoning caused by mushrooms, Poisoning caused by organophosphate anticholinesterase nerve agents, Poisoning caused by organophosphorus pesticides, Pylorospasm, Rhinorrhoea, Sinus Bradycardia, Spasms, Toxic effect of organophosphate and carbamate, Hypermobility of the colon, Laughing, Muscarinic side effects

How Atropisole works

Atropisole binds to and inhibit muscarinic acetylcholine receptors, producing a wide range of anticholinergic effects.

Dosage

Atropisole dosage

Adult:

• IV: Bradycardia: 500 mcg every 3-5 mins. Total: 3 mg.
• IV/IM: Organophosphorus poisoning: 2 mg every 10-30 mins until muscarinic effects disappear or atropine toxicity appears.
• IM/SC: Premedication in anesthesia: 300-600 mcg 30-60 mins before anesthesia.
• IV/IM/SC: Poisoning or overdosage with compound having muscarinic actions: 0.6-1 mg, repeat 2 hrly.
• Ophthalmic: Inflammatory eye disorders: As 0.5-1% solution: 1-2 drops 4 times/day.
• Ophthalmic: refraction: 1% solution 1 drop twice daily for 1-2 days before procedure.
• Oral: Non ulcer dyspepsia, Irritable bowel syndrome, Diverticular disease: 0.6-1.2 mg as a single dose at bedtime.

Usual Pediatric Dose for Anesthesia:

• 7 to 16 pounds: 0.1 mg, IV, IM, or subcutaneously
• 17 to 24 pounds: 0.15 mg, IV, IM, or subcutaneously
• 24 to 40 pounds: 0.2 mg, IV, IM, or subcutaneously
• 40 to 65 pounds: 0.3 mg, IV, IM, or subcutaneously
• 65 to 90 pounds: 0.4 mg, IV, IM, or subcutaneously
• Over 90 pounds: 0.4 to 0.6 mg, IV, IM, or subcutaneously

Side Effects

Injection: Dry mouth, dysphagia, constipation, flushing and dryness of skin, tachycardia, palpitations, arrhythmias, mydriasis, photophobia, cycloplegia, raised intraocular pressure. Toxic doses cause tachycardia, hyperpyrexia, restlessness, confusion, excitement, hallucinations, delirium and may progress to circulatory failure and resp depression.

Eye drops or ointment: Systemic toxicity esp in children, on prolonged use may lead to irritation, hyperaemia, oedema and conjunctivitis. Increased intraocular pressure.

Toxicity

Oral, mouse: LD₅₀ = 75 mg/kg. Symptoms of overdose includes widespread paralysis of parasympathetically innervated organs. Dry mucous membranes, widely dilated and nonresponsive pupils, tachycardia, fever and cutaneous flush are especially prominent, as are mental and neurological symptoms. In instances of severe intoxication, respiratory depression, coma, circulatory collapse and death may occur.

Precaution

Reflux oesophagitis; elderly; infants and children; Pregnancy.

Interaction

Additive anticholinergic effects with quinidine, antidepressants and some antihistamines.

Food Interaction

• Avoid alcohol.
• Take with food.

Atropisole Alcohol interaction

[Moderate] GENERALLY AVOID:

Use of anticholinergic agents with alcohol may result in sufficient impairment of attention so as to render driving and operating machinery more hazardous.

In addition, the potential for abuse may be increased with the combination.

The mechanism of interaction is not established but may involve additive depressant effects on the central nervous system.

No effect of oral propantheline or atropine on blood alcohol levels was observed in healthy volunteers when administered before ingestion of a standard ethanol load.

However, one study found impairment of attention in subjects given atropine 0.5 mg or glycopyrrolate 1 mg in combination with alcohol.

Alcohol should generally be avoided during therapy with anticholinergic agents.

Patients should be counseled to avoid activities requiring mental alertness until they know how these agents affect them.

Atropisole Hypertension interaction

[Minor] Cardiovascular effects of anticholinergics may exacerbate hypertension.

Therapy with anticholinergic agents should be administered cautiously in patients with hypertension.

Atropisole Drug Interaction

Moderate: diphenhydramine, diphenhydramineMinor: acetaminophen, acetaminophen, acetaminophen, acetaminophenUnknown: aspirin, aspirin, epinephrine, epinephrine, lorazepam, lorazepam, glucose, glucose, furosemide, furosemide, midazolam, midazolam, ondansetron, ondansetron

Atropisole Disease Interaction

Major: autonomic neuropathy, GI obstruction, glaucoma, obstructive uropathy, reactive airway diseases, myasthenia gravis, infectious diarrheaModerate: cardiac disease, tachycardia, coronary artery disease, gastric ulcer, gastroesophageal reflux, ulcerative colitis, liver disease, renal failureMinor: hypertension, hyperthyroidism, diarrhea, fever

Elimination Route

Atropisole is rapidly and well absorbed after intramuscular administration. Atropisole disappears rapidly from the blood and is distributed throughout the various body tissues and fluids.

Half Life

3.0 ± 0.9 hours in adults. The half-life of atropine is slightly shorter (approximately 20 minutes) in females than males.

Elimination Route

Much of the drug is destroyed by enzymatic hydrolysis, particularly in the liver; from 13 to 50% is excreted unchanged in the urine.

Pregnancy & Breastfeeding use

Pregnancy Category C. Animal reproduction studies have not been conducted with atropine. It also is not known whether atropine can cause fetal harm when given to a pregnant woman or can affect reproduction capacity. Atropisole should be given to a pregnant woman only if clearly needed.

Contraindication

Glaucoma, chronic respiratory disease, sick sinus syndrome, thyrotoxicosis, cardiac failure, pyloric stenosis, prostatic hypertrophy.

Acute Overdose

May cause hyperthermia, hypertension, increased respiratory rate, nausea and vomiting. May also lead to CNS stimulation. Severe intoxication may lead to CNS depression, coma, respiratory failure and death.

Storage Condition

Store atropine at room temperature between 20 to 25° C. Store away from heat, moisture, and light. Keep atropine out of the reach of children.

Innovators Monograph

You find simplified version here Atropisole