Brand name: Urecholine
Drug class: Parasympathomimetic (Cholinergic) Agents
VA class: AU300
CAS number: 590-63-6

Introduction

Cholinergic agonist.

Uses for Bethanechol

Urinary Retention

Treatment of acute postoperative and postpartum nonobstructive urinary retention and neurogenic atony of the bladder with retention.

Preferred agent to other parasympathomimetic drugs because of its relatively localized effect on the urinary tract and relative lack of adverse cardiovascular effects.

Heartburn

Has been shown to produce symptomatic improvement and decrease antacid use in some patients with chronic refractory heartburn^{† [off-label]} and gastroesophageal reflux disease (GERD), including vagotomized and antrectomized patients. However, use has decreased because of adverse CNS effects; acid suppression therapy with other agents (e.g., proton-pump inhibitors, histamine H₂-receptor antagonists) is principally used.

Bethanechol Dosage and Administration

Administration

Administer orally on an empty stomach (e.g., 1 hour before or 2 hours after a meal) to minimize nausea and vomiting.

Has been administered by sub-Q injection, but an injectable dosage form no longer is commercially available in the US.

Dosage

Available as bethanechol chloride; dosage expressed in terms of the salt.

Individualize dosage according to the type and severity of the condition.

Adults

Urinary Retention

Oral

Determine the minimum effective dosage by administering 5 or 10 mg every hour until a satisfactory response occurs or a maximum of 50 mg has been given.

Usual dosage: 10–50 mg 3–4 times daily.

Heartburn† [off-label]

Oral

25 mg 4 times daily has been given.

Special Populations

No special population dosage recommendations at this time.

Related/similar drugs

neostigmine, Urecholine, pamabrom, Prostigmin, Bloxiverz, Prostigmin Bromide

Cautions for Bethanechol

Contraindications

• Hyperthyroidism.

• Peptic ulcer.

• Latent or active bronchial asthma.

• Coronary artery disease (CAD).

• Epilepsy.

• Parkinsonism.

• Pronounced bradycardia or hypotension.

• Vasomotor instability.

• Condition in which the strength or integrity of the GI or bladder wall is in question or when increased muscular activity of GI tract or urinary bladder might prove harmful (e.g., recent urinary bladder surgery, GI resection and anastomosis) or when there is possible obstruction of GI tract or bladder neck, spastic GI disturbances, acute inflammatory GI tract lesions, peritonitis, or marked vagotonia.

• Known hypersensitivity to the drug or any ingredient in the formulation.

Warnings/Precautions

General Precautions

Urinary Tract Infections

Risk of infection in patients with urinary retention and bacteriuria; if sphincter fails to relax, bethanechol-induced bladder contraction may force urine up ureter into kidney pelvis, causing reflux infection.

Cardiovascular Effects

May produce a slight, transient decrease in diastolic BP with mild reflex tachycardia. Patients with hypertension may react with a precipitous fall in BP.

Periods of atrial fibrillation reported in hyperthyroid patients following administration of cholinergic drugs.

Specific Populations

Pregnancy

Category C.

Lactation

Not known whether bethanechol is distributed into milk. Discontinue nursing or the drug.

Pediatric Use

Safety and efficacy not established.

Common Adverse Effects

Adverse effects rare after oral administration; more common after sub-Q injection (no longer commercially available in the US). Adverse effects are most likely to occur when dosage is increased.

Abdominal cramps , colicky pain, flushing, sweating, salivation, malaise, headache, diarrhea, nausea, vomiting, bronchial constriction, urinary urgency, miosis.

Drug Interactions

Specific Drugs and Laboratory Tests

Bethanechol Pharmacokinetics

Absorption

Bioavailability

Poorly absorbed from the GI tract.

Onset

Effects may be evident within 30 minutes after oral administration; usually, 60–90 minutes required to reach maximum effectiveness.

Administration by sub-Q injection produces a more intense action on bladder muscle than oral administration; however, an injectable dosage form no longer is commercially available in the US.

Duration

Usually, 1 hour following oral administration; however, large doses (300–400 mg) have been reported to produce effects for up to 6 hours.

Distribution

Extent

Does not cross the blood-brain barrier in usual doses. Distribution into other body fluids is largely unknown.

Elimination

Metabolic path and mode of excretion not known.

Stability

Storage

Oral

Tablets

Tight containers at 20–25°C.

Actions

• Synthetic ester structurally and pharmacologically related to acetylcholine.

• Directly stimulates cholinergic receptors; stimulates ganglia to a lesser extent.

• Effects are almost exclusively muscarinic; little, if any, nicotinic activity, and cardiovascular effects are negligible.

• Increases tone and peristaltic activity in the stomach and intestines, increases esophageal peristalsis and the resting pressure of the lower esophageal sphincter, increases pancreatic and GI secretions, contracts detrusor muscle of urinary bladder, decreases bladder capacity, and increases frequency of ureteral peristaltic waves.

Advice to Patients

• Inform patient to take 1 hour before or 2 hours after meals to avoid nausea or vomiting.

• Risk of dizziness, lightheadedness, or fainting. Use caution when rising from a lying or sitting position.

• Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs.

• Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.

• Importance of informing patients of other important precautionary information. (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

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