Bethanechol

Atropine Sulfate is a specific antidote. The recommended dose for adults is 0.6 mg. Repeat doses can be given every two hours, according to clinical response. The recommended dosage in infants and children up to 12 years of age is 0.01 mg/kg (to a maximum single dose of 0.4 mg) repeated every two hours as needed until the desired effect is obtained or adverse effects of atropine preclude further usage. Subcutaneous injection of atropine is preferred except in emergencies when the intravenous route may be employed. (L1712)

Atropine sulfate competes with bethanechol at the muscarinic receptor junction, competitively blocking its binding at the postganglionic arch receptors and preventing parasympathetic cholinergic activation. A 0.6 mg dosage of atropine is recommended for adults and is repeatable every 2 hours as needed, depending on therapeutic responses. Dosages that range from 0.01 to 0.4 mg/kg can be administered in the pediatric population (infant/children) and should be repeated every 2 hours as needed, depending on therapeutic responses. The subcutaneous route via injection is also an option. An emergency indicates the use of the intravenous administration route.

Bethanechol directly stimulates cholinergic receptors in the parasympathetic nervous system while stimulating the ganglia to a lesser extent. Its effects are predominantly muscarinic, inducing little effect on nicotinic receptors and negligible effects on the cardiovascular system.

Benchmark Dataset for the Liver Toxicity Knowledge Base (LTKB)

bethanechol

Urecholine®

Cholinergics

Not Applicable

no-DILI-concern

N07AB02

N - Nervous system

QN - Nervous system

Bethanechol is selective for muscarinic receptors and has little to no impact on nicotinic receptors. The charged quaternary amine in the structure of bethanechol prevents it from crossing the blood-brain barrier which minimizes central nervous system related adverse effects.

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.

004F72P8F4

BETHANECHOL

Established Pharmacologic Class [EPC] - Cholinergic Muscarinic Agonist

Mechanisms of Action [MoA] - Cholinergic Muscarinic Agonists

Bethanechol is a Cholinergic Muscarinic Agonist. The mechanism of action of bethanechol is as a Cholinergic Muscarinic Agonist.

Drugs that mimic the effects of parasympathetic nervous system activity. Included here are drugs that directly stimulate muscarinic receptors and drugs that potentiate cholinergic activity, usually by slowing the breakdown of acetylcholine (CHOLINESTERASE INHIBITORS). Drugs that stimulate both sympathetic and parasympathetic postganglionic neurons (GANGLIONIC STIMULANTS) are not included here.

Drugs that bind to and activate muscarinic cholinergic receptors (RECEPTORS, MUSCARINIC). Muscarinic agonists are most commonly used when it is desirable to increase smooth muscle tone, especially in the GI tract, urinary bladder and the eye. They may also be used to reduce heart rate.

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.

Use (kg; approx.) in Germany (2009): >100

For the treatment of acute postoperative and postpartum nonobstructive (functional) urinary retention and for neurogenic atony of the urinary bladder with retention.