PHL-bethanechol

Uses

PHL-bethanechol is a muscarinic agonist used to treat postoperative and postpartum nonobstructive functional urinary retention and neurogenic atony of the bladder with retention.

PHL-bethanechol is indicated for the treatment of acute, functional postpartum and postoperative urinary retention. It is also indicated for the treatment of neurogenic atony of the bladder with retention.

PHL-bethanechol is also used to associated treatment for these conditions: Acute post-operative Urinary retention, Neurogenic atony of the urinary bladder, Non-obstructive postpartum urinary retention

How PHL-bethanechol works

PHL-bethanechol is a direct muscarinic agonist and stimulates the parasympathetic nervous system by binding to postganglionic muscarinic receptors.

Though there are 5 types of muscarinic receptors (M1, M2, M3, M4, M5), binding of bethanechol to M3 is most clinically significant since M3 receptors are present in intestinal smooth muscle and the bladder. The cholinergic effects of bethanechol lead to increased detrusor muscle tone to promote bladder emptying and increased smooth muscle tone which restores gastrointestinal peristalsis and motility.

As a result of selectivity for muscarinic receptors, bethanechol produces minimal to no nicotinic effects.

Toxicity

Symptoms of bethanechol overdose include nausea, vomiting, abdominal discomfort, salivation, sweating, and flushing of the skin.

In case of overdose, atropine sulfate is available as an antidote and although subcutaneous administration is preferred, it may be given intravenously in emergencies. In adults, the recommended dose of atropine is 0.6 mg and may be repeated every 2 hours based on the patient’s response. In infants and children up to 12 years of age, the recommended dose of atropine is 0.01 mg/kg (maximum single dose = 0.04 mg) and may be repeated every 2 hours until the desired response is achieved or until adverse effects of atropine limit usage.

In mice, the oral LD50 of bethanechol is 1510 mg/kg.

Food Interaction

• Take on an empty stomach. Nausea and vomiting may occur if taken after food.

PHL-bethanechol Hypertension interaction

[Major] The use of cholinergic agonists, such as bethanechol and pilocarpine, is contraindicated in patients with pronounced bradycardia, hypotension

PHL-bethanechol Drug Interaction

Unknown: duloxetine, duloxetine, tamsulosin, tamsulosin, pregabalin, pregabalin, polyethylene glycol 3350, polyethylene glycol 3350, esomeprazole, esomeprazole, pantoprazole, pantoprazole, levothyroxine, levothyroxine, acetaminophen, acetaminophen, cyanocobalamin, cyanocobalamin, cholecalciferol, cholecalciferol

PHL-bethanechol Disease Interaction

Major: bronchospasm, cardiac dysfunction, GI/bladder neck obstruction, hyperthyroidism, parkinsonism, seizure disorders

Elimination Route

After oral administration of bethanechol, maximum effectiveness of the drug on the bladder and GI tract typically occur after 60-90 minutes; however, effects may present as early as 30 minutes after administration. The duration of action of a typical oral dose of bethanechol is around 1 hour while higher doses (300-400 mg) may be effective for up to 6 hours.

Subcutaneously administered bethanechol produces effects more rapidly after 5-15 minutes with maximum effectiveness achieved after 15-30 minutes. The effects of subcutaneous bethanechol subside within 2 hours of administration.

Innovators Monograph

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