Propantheline

Uses

Propantheline is used with other medications to treat peptic ulcers. It works by decreasing the release of acid in the stomach.

Propantheline is also used to associated treatment for these conditions: Peptic Ulcer, Gastrointestinal spasms

How Propantheline works

Action is achieved via a dual mechanism: (1) a specific anticholinergic effect (antimuscarinic) at the acetylcholine-receptor sites and (2) a direct effect upon smooth muscle (musculotropic).

Dosage

Propantheline dosage

Adultdose: The usual initial adult dose of propantheline bromide tablets is 15 mg taken 30 minutes before each meal and 30 mg at bedtime (a total of 75 mg daily). Subsequent dosage adjustment should be made according to the patient’s individual response and tolerance.

Pediatric Use: Safety and effectiveness in children have not been established.

Side Effects

Varying degrees of drying of salivary secretions may occur as well as decreased sweating. Ophthalmic side effects include blurred vision, mydriasis, cycloplegia, and increased ocular tension. Other reported adverse reactions include urinary hesitancy and retention, tachycardia, palpitations, loss of the sense of taste, headache, nervousness, mental confusion, drowsiness, weakness, dizziness, insomnia, nausea, vomiting, constipation, bloated feeling, impotence, suppression of lactation, and allergic reactions or drug idiosyncracies including anaphylaxis, urticaria and other dermal manifestations.

Precaution

Propantheline should be used with caution in the elderly and in all patients with autonomic neuropathy, hepatic or renal disease, hyperthyroidism, coronary heart disease, congestive heart failure, cardiac tachyarrhythmias, hypertension, or hiatal hernia associated with reflux esophagitis, since anticholinergics may aggravate this condition.

In patients with ulcerative colitis, large doses of propantheline may suppress intestinal motility to the point of producing paralytic ileus and, for this reason, may precipitate or aggravate toxic megacolon, a serious complication of the disease.

Interaction

Anticholinergics may delay absorption of other medication given concomitantly. Excessive cholinergic blockade may occur if propantheline is given concomitantly with belladonna alkaloids or synthetic and semisynthetic anticholinergic agents, narcotic analgesics such as meperidine, Type 1 antiarrhythmic drugs (e.g., disopyramide, procainamide, or quinidine), antihistamines, phenothiazines, tricyclic antidepressants, or other psychoactive drugs. Propantheline may also potentiate the sedative effect of phenothiazines. Increased intraocular pressure may result from concurrent administration of anticholinergics and corticosteroids.

Concurrent use of propantheline with slow-dissolving tablets of digoxin may cause increased serum digoxin levels. This interaction can be avoided by using only those digoxin tablets that rapidly dissolve by USP standards.

Food Interaction

• Take before a meal. Take before a meal. Propantheline bromide should be taken 15 to 30 minutes before meals.

Propantheline 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.

Propantheline Hypertension interaction

[Minor] Cardiovascular effects of anticholinergics may exacerbate hypertension.

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

Propantheline Drug Interaction

Moderate: contained in alcoholic beverages , atropine / diphenoxylate, morphine, metoclopramideMinor: acetaminophenUnknown: naproxen, aspirin, celecoxib, tadalafil, alendronate, methenamine, isosorbide mononitrate, furosemide, atorvastatin, gabapentin, polyethylene glycol 3350, omeprazole, desvenlafaxine, cholecalciferol, sertraline

Propantheline Disease Interaction

Major: arrhythmias, autonomic neuropathy, GI obstruction, glaucoma, obstructive uropathy, tardive dyskinesia, infectious diarrheaModerate: psychosesMinor: hypertension, fever

Elimination Route

Approximately 70% of the dose is excreted in the urine, mostly as metabolites.

Pregnancy & Breastfeeding use

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

Nursing Mothers: It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when propantheline is administered to a nursing woman. Suppression of lactation may occur with anticholinergic drugs.

Contraindication

Propantheline is contraindicated in patients with:

• Glaucoma, since mydriasis is to be avoided.
• Obstructive disease of the gastrointestinal tract (pyloroduodenal stenosis, achalasia, paralytic ileus, etc.).
• Obstructive uropathy (e.g., bladder-neck obstruction due to prostatic hypertrophy).
• Intestinal atony of elderly or debilitated patients.
• Severe ulcerative colitis or toxic megacolon complicating ulcerative colitis.
• Unstable cardiovascular adjustment in acute hemorrhage.
• Myasthenia gravis.

Acute Overdose

The symptoms of overdosage with propantheline progress from an intensification of the usual side effects to CNS disturbances (from restlessness and excitement to psychotic behavior), circulatory changes (flushing, fall in blood pressure, circulatory failure), respiratory failure, paralysis, and coma.

Measures to be taken are (1) immediate induction of emesis or lavage of the stomach and (2) injection of physostigmine 0.5 to 2 mg intravenously, and repeated as necessary up to a total of 5 mg, and (3) monitoring of vital signs and managing as necessary.

Fever may be treated symptomatically (cooling blanket or alcohol sponging). Excitement of a degree which demands attention may be managed with thiopental sodium 2% solution given slowly intravenously or diazepam, 5 to 10 mg intravenously or 10 mg intramuscularly. In the event of progression of the curare-like effect to paralysis of the respiratory muscles, mechanical respiration should be instituted and maintained until effective respiratory action returns.

The oral LD50 of propantheline bromide is 780 mg/kg in the mouse and 370 mg/kg in the rat.

Storage Condition

Store below 25° C.

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