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    All Other Urological Products

    DEA CLASS

    Rx

    DESCRIPTION

    Synthetic parasympathomimetic; used for urinary retention; is occasionally used to offset some of the bothersome anticholinergic reactions to tricyclic antidepressants

    COMMON BRAND NAMES

    Duvoid, Urecholine

    HOW SUPPLIED

    Bethanechol/Bethanechol Chloride/Duvoid/Urecholine Oral Tab: 5mg, 10mg, 25mg, 50mg

    DOSAGE & INDICATIONS

    For treatment of acute postoperative/postpartum non-obstructive urinary retention and treatment of atonic neurogenic bladder.
    Oral dosage
    Adults

    Determine minimal effective dose initially by giving 5—10 mg and repeating at hourly intervals until therapeutic goals are attained or until maximum of 50 mg PO given. The usual dosage is 10—50 mg PO 3—4 times per day. Drug effects may appear within 30 minutes, and usually occur within 60—90 minutes. Duration of action is about 1 hour.

    Children†

    0.6 mg/kg/day PO in 3—4 divided doses.

    Subcutaneous dosage
    Adults

    The usual dose is 5 mg subcutaneous 3—4 times per day as needed. The minimum effective dose may be determined by administering 2.5 mg and then repeating the same dose every 15—30 minutes until satisfactory results are obtained or until given 4 times (up to total 10 mg). Large single doses (> 5 mg) should only be employed after an adequate trial has established that smaller doses (2.5—5 mg) are ineffective. Rarely, single doses up to 10 mg may be required; although such large doses may cause severe reactions. Bethanechol is usually effective in 5—15 minutes after subcutaneous injection, with maximal effects reached in 15—30 minutes, and duration less than 2 hours. After subcutaneous administration of bethanechol, the patient should be observed for 30 minutes to 1 hour for possible severe reactions, and a syringe containing a dose of atropine should be immediately available to promptly counteract adverse effects.

    For the treatment of gastroesophageal reflux disease (GERD)† by increasing lower esophageal pressure.
    Oral dosage
    Adults

    10—25 mg PO 4 times per day, after meals and at bedtime.

    Children

    0.1—0.2 mg/kg PO 4 times per day (given 0.5—1 hour before each meal), or 3 mg/m2 PO every 8 hours.

    For the treatment of gastric atony† or adynamic ileus†.
    Oral dosage
    Adults

    10—20 mg PO 3—4 times per day before meals in cases of incomplete retention.

    Subcutaneous dosage
    Adults

    10—20 mg subcutaneous 3—4 times per day if retention is complete and nothing enters the duodenum.

    For treating disabling anticholinergic side effects 'anticholinergic syndrome' from medications such as tricyclic antidepressants†.
    Oral dosage
    Adults

    A dosage of 25 mg PO 3 times per day has been used.

    †Indicates off-label use

    MAXIMUM DOSAGE

    Adults

    200 mg/day PO or 40 mg/day SC (single maximum dose: 50 mg PO or 10 mg SC).

    Elderly

    200 mg/day PO or 40 mg/day SC (single maximum dose: 50 mg PO or 10 mg SC).

    Adolescents

    Safety and efficacy have not been established.

    Children

    Safety and efficacy have not been established.

    DOSING CONSIDERATIONS

    Hepatic Impairment

    Specific guidelines for dosage adjustments in hepatic impairment are not available; the metabolic disposition of bethanechol is unknown.

    Renal Impairment

    No dosage adjustment needed.

    ADMINISTRATION

    Oral Administration

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

    Injectable Administration

    Visually inspect parenteral products for particulate matter and discoloration prior to administration whenever solution and container permit.

    Subcutaneous Administration

    Bethanechol injection is for subcutaneous injection only. Do NOT administer intravenously or intramuscularly; serious adverse effects may occur.
    Inject subcutaneously taking care not to inject intradermally.
    No dilution necessary.
    After subcutaneous administration, the patient should be observed for 30 minutes to 1 hour for possible severe reactions, and a syringe containing a dose of atropine should be immediately available during this period.

    STORAGE

    Duvoid :
    - Store between 68 to 77 degrees F, excursions permitted 59 to 86 degrees F
    Urecholine:
    - Store between 68 to 77 degrees F, excursions permitted 59 to 86 degrees F

    CONTRAINDICATIONS / PRECAUTIONS

    Bladder obstruction, GI obstruction, ileus, inflammatory bowel disease, peptic ulcer disease, peritonitis, surgery, urinary tract obstruction

    Bethanechol use is contraindicated when the strength or integrity of the gastrointestinal or bladder wall is questionable. Increased muscular activity of the GI tract or bladder may prove harmful, worsening the underlying condition and risking rupture or perforation. Conditions that contraindicate bethanechol use include: GI obstruction (ileus) and bladder obstruction or urinary tract obstruction. Bethanechol is contraindicated in patients with inflammatory bowel disease, peritonitis, marked vagotonia, or who have undergone recent gastrointestinal or bladder surgery. Increased stimulation of gastric acid also contraindicates bethanechol use in peptic ulcer disease.

    Bradycardia, coronary artery disease, driving or operating machinery, hypertension, hypotension, intramuscular injections, intravenous administration, orthostatic hypotension, syncope

    Bethanechol use is contraindicated in patients with pronounced bradycardia, pronounced hypotension, or coronary artery disease. Bethanechol can cause orthostatic hypotension, specifically after subcutaneous administration, and should be used with caution in patients at risk for syncope. Bethanechol should never be given by intramuscular injections or intravenous administration. Administration by either of these routes can precipitate cholinergic over-stimulation, causing circulatory collapse, sudden hypotension, abdominal cramps, bloody diarrhea, shock, or sudden cardiac arrest. A more precipitous drop in blood pressure can be seen in patients with hypertension. Administration by the oral or subcutaneous route can have a mild negative chronotropic effect. Due to potential for orthostatic hypotension, patients may be warned to avoid driving or operating machinery until the effects of bethanechol are known.

    Asthma, chronic obstructive pulmonary disease (COPD)

    Bethanechol is contraindicated in patients with asthma; Bethanechol should also be avoided in chronic obstructive pulmonary disease (COPD) because cholinergic stimulation constricts the airways.

    Hyperthyroidism, parkinsonism, seizure disorder, seizures

    Bethanechol is also contraindicated in patients with hyperthyroidism, seizures or seizure disorder, and parkinsonism because it can exacerbate these conditions. Cholinergic drugs may precipitate atrial fibrillation in patients with hyperthyroidism.

    Children

    The manufacturer states that the safe and effective use of bethanechol in children has not been established. However, bethanechol has been used off-label to treat children with urinary retention or certain gastrointestinal (GI) conditions.

    Pregnancy

    Bethanechol is classified in FDA pregnancy risk category C. Adequate studies have not been performed to determine whether bethanechol is teratogenic. The drug is best avoided during pregnancy.

    Breast-feeding

    Bethanechol should only be administered during lactation when benefit to the mother outweighs the risk. It is not known if bethanechol is excreted into breast-milk. If bethanechol therapy is essential, breast-feeding should be discontinued because of the potential for severe adverse effects (e.g., cholinergic excess) in nursing infants.

    Geriatric

    The federal Omnibus Budget Reconciliation Act (OBRA) regulates medication use in residents (e.g., geriatric adults) of long-term care facilities (LTCFs). According to the OBRA guidelines, assessment of the underlying causes and identification of the type/category of urinary incontinence needs to be documented prior to or soon after the time of initiating treatment with a urinary incontinence medication. These medications have specific and limited indications based on the cause and categorization of incontinence. Patients should be assessed periodically for medication effects on urinary incontinence as well as lower urinary tract symptoms and treatment tolerability. Adverse consequences of bethanechol include hypotension, increased sweating and salivation, headache, cramps, diarrhea, nausea, vomiting, and worsening of asthma.

    ADVERSE REACTIONS

    Severe

    bronchospasm / Rapid / Incidence not known
    seizures / Delayed / Incidence not known

    Moderate

    wheezing / Rapid / Incidence not known
    sinus tachycardia / Rapid / Incidence not known

    Mild

    diarrhea / Early / Incidence not known
    hypersalivation / Early / Incidence not known
    flatulence / Early / Incidence not known
    borborygmi / Early / Incidence not known
    vomiting / Early / Incidence not known
    abdominal pain / Early / Incidence not known
    nausea / Early / Incidence not known
    flushing / Rapid / Incidence not known
    diaphoresis / Early / Incidence not known
    lacrimation / Early / Incidence not known
    miosis / Early / Incidence not known
    increased urinary frequency / Early / Incidence not known
    urinary urgency / Early / Incidence not known
    headache / Early / Incidence not known
    dizziness / Early / Incidence not known
    syncope / Early / Incidence not known
    malaise / Early / Incidence not known

    DRUG INTERACTIONS

    Acetaminophen; Chlorpheniramine; Dextromethorphan; Phenylephrine: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects.
    Acetaminophen; Chlorpheniramine; Dextromethorphan; Pseudoephedrine: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects.
    Acetaminophen; Chlorpheniramine; Phenylephrine; Phenyltoloxamine: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects.
    Acetaminophen; Dextromethorphan; Guaifenesin; Phenylephrine: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects.
    Acetaminophen; Dextromethorphan; Phenylephrine: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects.
    Acetaminophen; Dextromethorphan; Pseudoephedrine: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects.
    Acetaminophen; Dichloralphenazone; Isometheptene: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects.
    Acetaminophen; Diphenhydramine: (Moderate) Drugs that possess antimuscarinic properties, such as diphenhydramine, are pharmacologic opposites of bethanechol. These agents should not be used with bethanechol except when the specific intent is to counteract excessive actions of one or the other.
    Acetaminophen; Guaifenesin; Phenylephrine: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects.
    Acetaminophen; Pseudoephedrine: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects.
    Acrivastine; Pseudoephedrine: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects.
    Alosetron: (Moderate) Pharmacodynamic interactions between alosetron and drugs that enhance peristalsis are theoretically possible, based on opposing pharmacologic outcomes. It may be wise to avoid use of bethanechol during alosetron treatment. Although these potential interactions have not been studied, bethanechol might negate the effect of alosetron.
    Ambenonium Chloride: (Major) Cholinergic agonists can cause additive pharmacodynamic effects if used concomitantly with cholinesterase inhibitors. Concurrent use is unlikely to be tolerated by the patient and should be avoided.
    Amoxapine: (Major) Amoxapine may antagonize some of the effects of parasympathomimetics. However, bethanechol has occasionally been used therapeutically to offset some of the adverse antimuscarinic effects of cyclic antidepressants. Due to their anticholinergic actions, some cyclic antidepressants, such as amoxapine, may potentially antagonize the therapeutic actions of cholinergic agonists.
    Amphetamine: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects.
    Amphetamine; Dextroamphetamine: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects.
    Anticholinergics: (Major) The muscarinic actions of drugs known as parasympathomimetics, including both direct cholinergic receptor agonists and cholinesterase inhibitors, can antagonize the antimuscarinic actions of anticholinergic drugs, and vice versa.
    Articaine; Epinephrine: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects.
    Atropine: (Major) The muscarinic actions of drugs known as parasympathomimetics, including both direct cholinergic receptor agonists and cholinesterase inhibitors, can antagonize the antimuscarinic actions of anticholinergic drugs, and vice versa.
    Atropine; Benzoic Acid; Hyoscyamine; Methenamine; Methylene Blue; Phenyl Salicylate: (Major) The muscarinic actions of drugs known as parasympathomimetics, including both direct cholinergic receptor agonists and cholinesterase inhibitors, can antagonize the antimuscarinic actions of anticholinergic drugs, and vice versa.
    Atropine; Difenoxin: (Major) The muscarinic actions of drugs known as parasympathomimetics, including both direct cholinergic receptor agonists and cholinesterase inhibitors, can antagonize the antimuscarinic actions of anticholinergic drugs, and vice versa. (Moderate) Pharmacodynamic interactions between antidiarrheals and drugs that enhance peristalsis are theoretically possible. It is wise to avoid use of antidiarrheals in patients who require bethanechol.
    Atropine; Diphenoxylate: (Major) The muscarinic actions of drugs known as parasympathomimetics, including both direct cholinergic receptor agonists and cholinesterase inhibitors, can antagonize the antimuscarinic actions of anticholinergic drugs, and vice versa. (Moderate) Pharmacodynamic interactions between antidiarrheals and drugs that enhance peristalsis are theoretically possible. It is wise to avoid use of antidiarrheals in patients who require bethanechol.
    Atropine; Edrophonium: (Major) Cholinergic agonists can cause additive pharmacodynamic effects if used concomitantly with cholinesterase inhibitors. Concurrent use is unlikely to be tolerated by the patient and should be avoided. (Major) The muscarinic actions of drugs known as parasympathomimetics, including both direct cholinergic receptor agonists and cholinesterase inhibitors, can antagonize the antimuscarinic actions of anticholinergic drugs, and vice versa.
    Atropine; Hyoscyamine; Phenobarbital; Scopolamine: (Major) The muscarinic actions of drugs known as parasympathomimetics, including both direct cholinergic receptor agonists and cholinesterase inhibitors, can antagonize the antimuscarinic actions of anticholinergic drugs, and vice versa.
    Belladonna Alkaloids; Ergotamine; Phenobarbital: (Major) The muscarinic actions of drugs known as parasympathomimetics, including both direct cholinergic receptor agonists and cholinesterase inhibitors, can antagonize the antimuscarinic actions of anticholinergic drugs, and vice versa.
    Belladonna; Opium: (Major) The muscarinic actions of drugs known as parasympathomimetics, including both direct cholinergic receptor agonists and cholinesterase inhibitors, can antagonize the antimuscarinic actions of anticholinergic drugs, and vice versa.
    Benzoic Acid; Hyoscyamine; Methenamine; Methylene Blue; Phenyl Salicylate: (Major) The muscarinic actions of drugs known as parasympathomimetics, including both direct cholinergic receptor agonists and cholinesterase inhibitors, can antagonize the antimuscarinic actions of anticholinergic drugs, and vice versa.
    Benzphetamine: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects.
    Benztropine: (Major) The muscarinic actions of drugs known as parasympathomimetics, including both direct cholinergic receptor agonists and cholinesterase inhibitors, can antagonize the antimuscarinic actions of anticholinergic drugs, and vice versa.
    Bismuth Subsalicylate: (Moderate) Pharmacodynamic interactions between loperamide and drugs that enhance peristalsis are theoretically possible. It is wise to avoid use loperamide in patients who require bethanechol.
    Bismuth Subsalicylate; Metronidazole; Tetracycline: (Moderate) Pharmacodynamic interactions between loperamide and drugs that enhance peristalsis are theoretically possible. It is wise to avoid use loperamide in patients who require bethanechol.
    Brompheniramine; Carbetapentane; Phenylephrine: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects.
    Brompheniramine; Hydrocodone; Pseudoephedrine: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects.
    Brompheniramine; Pseudoephedrine: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects.
    Bupropion: (Moderate) Bupropion exhibits moderate anticholinergic properties. Avoid co-use when possible since the effects of bethanechol, a cholinergic agonist, may be diminished. If co-use is necessary, monitor for the intended clinical response.
    Bupropion; Naltrexone: (Moderate) Bupropion exhibits moderate anticholinergic properties. Avoid co-use when possible since the effects of bethanechol, a cholinergic agonist, may be diminished. If co-use is necessary, monitor for the intended clinical response.
    Carbetapentane; Chlorpheniramine; Phenylephrine: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects.
    Carbetapentane; Diphenhydramine; Phenylephrine: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects. (Moderate) Drugs that possess antimuscarinic properties, such as diphenhydramine, are pharmacologic opposites of bethanechol. These agents should not be used with bethanechol except when the specific intent is to counteract excessive actions of one or the other.
    Carbetapentane; Guaifenesin; Phenylephrine: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects.
    Carbetapentane; Phenylephrine: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects.
    Carbetapentane; Phenylephrine; Pyrilamine: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects.
    Carbetapentane; Pseudoephedrine: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects.
    Carbinoxamine: (Moderate) Drugs that possess antimuscarinic properties, such as carbinoxamine, are pharmacologic opposites of bethanechol. These agents should not be used with bethanechol except when the specific intent is to counteract excessive actions of one or the other.
    Carbinoxamine; Dextromethorphan; Pseudoephedrine: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects. (Moderate) Drugs that possess antimuscarinic properties, such as carbinoxamine, are pharmacologic opposites of bethanechol. These agents should not be used with bethanechol except when the specific intent is to counteract excessive actions of one or the other.
    Carbinoxamine; Hydrocodone; Phenylephrine: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects. (Moderate) Drugs that possess antimuscarinic properties, such as carbinoxamine, are pharmacologic opposites of bethanechol. These agents should not be used with bethanechol except when the specific intent is to counteract excessive actions of one or the other.
    Carbinoxamine; Hydrocodone; Pseudoephedrine: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects. (Moderate) Drugs that possess antimuscarinic properties, such as carbinoxamine, are pharmacologic opposites of bethanechol. These agents should not be used with bethanechol except when the specific intent is to counteract excessive actions of one or the other.
    Carbinoxamine; Phenylephrine: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects. (Moderate) Drugs that possess antimuscarinic properties, such as carbinoxamine, are pharmacologic opposites of bethanechol. These agents should not be used with bethanechol except when the specific intent is to counteract excessive actions of one or the other.
    Carbinoxamine; Pseudoephedrine: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects. (Moderate) Drugs that possess antimuscarinic properties, such as carbinoxamine, are pharmacologic opposites of bethanechol. These agents should not be used with bethanechol except when the specific intent is to counteract excessive actions of one or the other.
    Cetirizine; Pseudoephedrine: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects.
    Cevimeline: (Moderate) Cevimeline and bethanechol are both cholinergic agonists. Coadministration is expected to result in additive parasympathomimetic effects.
    Chlophedianol; Dexchlorpheniramine; Pseudoephedrine: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects.
    Chlophedianol; Guaifenesin; Phenylephrine: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects.
    Chlordiazepoxide; Clidinium: (Major) The muscarinic actions of drugs known as parasympathomimetics, including both direct cholinergic receptor agonists and cholinesterase inhibitors, can antagonize the antimuscarinic actions of anticholinergic drugs, and vice versa.
    Chlorpheniramine; Dextromethorphan; Phenylephrine: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects.
    Chlorpheniramine; Dihydrocodeine; Phenylephrine: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects.
    Chlorpheniramine; Dihydrocodeine; Pseudoephedrine: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects.
    Chlorpheniramine; Guaifenesin; Hydrocodone; Pseudoephedrine: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects.
    Chlorpheniramine; Hydrocodone; Phenylephrine: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects.
    Chlorpheniramine; Hydrocodone; Pseudoephedrine: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects.
    Chlorpheniramine; Phenylephrine: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects.
    Chlorpheniramine; Pseudoephedrine: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects.
    Chlorpromazine: (Moderate) Drugs that possess antimuscarinic properties, such as chlorpromazine, are pharmacologic opposites of bethanechol. These agents should not be used with bethanechol except when the specific intent is to counteract excessive actions of one or the other.
    Cholinesterase inhibitors: (Major) Cholinergic agonists can cause additive pharmacodynamic effects if used concomitantly with cholinesterase inhibitors. Concurrent use is unlikely to be tolerated by the patient and should be avoided.
    Clemastine: (Moderate) Drugs that possess antimuscarinic properties, such as clemastine, are pharmacologic opposites of bethanechol. These agents should not be used with bethanechol except when the specific intent is to counteract excessive actions of one or the other.
    Clozapine: (Moderate) Drugs that possess antimuscarinic properties, such as clozapine, are pharmacologic opposites of bethanechol. These agents should not be used with bethanechol except when the specific intent is to counteract excessive actions of one or the other.
    Codeine; Phenylephrine; Promethazine: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects. (Moderate) Drugs that possess antimuscarinic properties, such as promethazine, are pharmacologic opposites of bethanechol. These agents should not be used with bethanechol except when the specific intent is to counteract excessive actions of one or the other.
    Codeine; Promethazine: (Moderate) Drugs that possess antimuscarinic properties, such as promethazine, are pharmacologic opposites of bethanechol. These agents should not be used with bethanechol except when the specific intent is to counteract excessive actions of one or the other.
    Darifenacin: (Major) The muscarinic actions of drugs known as parasympathomimetics, including both direct cholinergic receptor agonists and cholinesterase inhibitors, can antagonize the antimuscarinic actions of anticholinergic drugs, and vice versa.
    Desloratadine; Pseudoephedrine: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects.
    Dexchlorpheniramine; Dextromethorphan; Pseudoephedrine: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects.
    Dexmethylphenidate: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects.
    Dextroamphetamine: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects.
    Dextromethorphan; Diphenhydramine; Phenylephrine: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects. (Moderate) Drugs that possess antimuscarinic properties, such as diphenhydramine, are pharmacologic opposites of bethanechol. These agents should not be used with bethanechol except when the specific intent is to counteract excessive actions of one or the other.
    Dextromethorphan; Guaifenesin; Phenylephrine: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects.
    Dextromethorphan; Guaifenesin; Pseudoephedrine: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects.
    Dextromethorphan; Promethazine: (Moderate) Drugs that possess antimuscarinic properties, such as promethazine, are pharmacologic opposites of bethanechol. These agents should not be used with bethanechol except when the specific intent is to counteract excessive actions of one or the other.
    Dextromethorphan; Quinidine: (Moderate) Drugs that possess antimuscarinic properties, such as quinidine, are pharmacologic opposites of bethanechol. These agents should not be used with bethanechol except when the specific intent is to counteract excessive actions of one or the other.
    Dicyclomine: (Major) The muscarinic actions of drugs known as parasympathomimetics, including both direct cholinergic receptor agonists and cholinesterase inhibitors, can antagonize the antimuscarinic actions of anticholinergic drugs, and vice versa.
    Diethylpropion: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects.
    Dihydrocodeine; Guaifenesin; Pseudoephedrine: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects.
    Diphenhydramine: (Moderate) Drugs that possess antimuscarinic properties, such as diphenhydramine, are pharmacologic opposites of bethanechol. These agents should not be used with bethanechol except when the specific intent is to counteract excessive actions of one or the other.
    Diphenhydramine; Hydrocodone; Phenylephrine: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects. (Moderate) Drugs that possess antimuscarinic properties, such as diphenhydramine, are pharmacologic opposites of bethanechol. These agents should not be used with bethanechol except when the specific intent is to counteract excessive actions of one or the other.
    Diphenhydramine; Ibuprofen: (Moderate) Drugs that possess antimuscarinic properties, such as diphenhydramine, are pharmacologic opposites of bethanechol. These agents should not be used with bethanechol except when the specific intent is to counteract excessive actions of one or the other.
    Diphenhydramine; Naproxen: (Moderate) Drugs that possess antimuscarinic properties, such as diphenhydramine, are pharmacologic opposites of bethanechol. These agents should not be used with bethanechol except when the specific intent is to counteract excessive actions of one or the other.
    Diphenhydramine; Phenylephrine: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects. (Moderate) Drugs that possess antimuscarinic properties, such as diphenhydramine, are pharmacologic opposites of bethanechol. These agents should not be used with bethanechol except when the specific intent is to counteract excessive actions of one or the other.
    Disopyramide: (Moderate) Disopyramide possesses clinically significant antimuscarinic properties and these appear to be dose-related. It is possible that disopyramide could antagonize the muscarinic actions of cholinergic agonists. Clinicians should be alert to this possibility.
    Dobutamine: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects.
    Donepezil: (Major) Cholinergic agonists can cause additive pharmacodynamic effects if used concomitantly with cholinesterase inhibitors. Concurrent use is unlikely to be tolerated by the patient and should be avoided.
    Donepezil; Memantine: (Major) Cholinergic agonists can cause additive pharmacodynamic effects if used concomitantly with cholinesterase inhibitors. Concurrent use is unlikely to be tolerated by the patient and should be avoided.
    Dopamine: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects.
    Edrophonium: (Major) Cholinergic agonists can cause additive pharmacodynamic effects if used concomitantly with cholinesterase inhibitors. Concurrent use is unlikely to be tolerated by the patient and should be avoided.
    Ephedrine: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects.
    Epinephrine: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects.
    Fesoterodine: (Major) The muscarinic actions of drugs known as parasympathomimetics, including both direct cholinergic receptor agonists and cholinesterase inhibitors, can antagonize the antimuscarinic actions of anticholinergic drugs, and vice versa.
    Fexofenadine; Pseudoephedrine: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects.
    Flavoxate: (Major) The muscarinic actions of drugs known as parasympathomimetics, including both direct cholinergic receptor agonists and cholinesterase inhibitors, can antagonize the antimuscarinic actions of anticholinergic drugs, and vice versa.
    Fluoxetine; Olanzapine: (Moderate) Drugs that possess antimuscarinic properties, such as olanzapine, are pharmacologic opposites of bethanechol (a direct agonist at muscarinic cholinergic receptors). These agents should not be used with bethanechol except when the specific intent is to counteract excessive actions of one or the other.
    Fosfomycin: (Moderate) Bethanechol increases gastrointestinal motility and may decrease the systemic absorption of fosfomycin when the drugs are coadministered.
    Galantamine: (Major) Cholinergic agonists can cause additive pharmacodynamic effects if used concomitantly with cholinesterase inhibitors. Concurrent use is unlikely to be tolerated by the patient and should be avoided.
    Glycopyrrolate: (Major) The muscarinic actions of drugs known as parasympathomimetics, including both direct cholinergic receptor agonists and cholinesterase inhibitors, can antagonize the antimuscarinic actions of anticholinergic drugs, and vice versa.
    Glycopyrrolate; Formoterol: (Major) The muscarinic actions of drugs known as parasympathomimetics, including both direct cholinergic receptor agonists and cholinesterase inhibitors, can antagonize the antimuscarinic actions of anticholinergic drugs, and vice versa.
    Guaifenesin; Hydrocodone; Pseudoephedrine: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects.
    Guaifenesin; Phenylephrine: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects.
    Guaifenesin; Pseudoephedrine: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects.
    Guanidine: (Moderate) Guanidine and bethanechol are both cholinergic agonists. Coadministration is expected to result in additive parasympathomimetic effects.
    Homatropine; Hydrocodone: (Major) The muscarinic actions of drugs known as parasympathomimetics, including both direct cholinergic receptor agonists and cholinesterase inhibitors, can antagonize the antimuscarinic actions of anticholinergic drugs, and vice versa.
    Hydrocodone; Phenylephrine: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects.
    Hydrocodone; Potassium Guaiacolsulfonate; Pseudoephedrine: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects.
    Hydrocodone; Pseudoephedrine: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects.
    Hyoscyamine: (Major) The muscarinic actions of drugs known as parasympathomimetics, including both direct cholinergic receptor agonists and cholinesterase inhibitors, can antagonize the antimuscarinic actions of anticholinergic drugs, and vice versa.
    Hyoscyamine; Methenamine; Methylene Blue; Phenyl Salicylate; Sodium Biphosphate: (Major) The muscarinic actions of drugs known as parasympathomimetics, including both direct cholinergic receptor agonists and cholinesterase inhibitors, can antagonize the antimuscarinic actions of anticholinergic drugs, and vice versa.
    Ibuprofen; Pseudoephedrine: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects.
    Indacaterol; Glycopyrrolate: (Major) The muscarinic actions of drugs known as parasympathomimetics, including both direct cholinergic receptor agonists and cholinesterase inhibitors, can antagonize the antimuscarinic actions of anticholinergic drugs, and vice versa.
    Isoproterenol: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects.
    Lisdexamfetamine: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects.
    Loperamide: (Moderate) Pharmacodynamic interactions between loperamide and drugs that enhance peristalsis are theoretically possible. If possible, avoid use of loperamide in patients who require bethanechol.
    Loperamide; Simethicone: (Moderate) Pharmacodynamic interactions between loperamide and drugs that enhance peristalsis are theoretically possible. If possible, avoid use of loperamide in patients who require bethanechol.
    Loratadine; Pseudoephedrine: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects.
    Maprotiline: (Major) Maprotiline may antagonize some of the effects of parasympathomimetics. However, bethanechol has occasionally been used therapeutically to offset some of the adverse antimuscarinic effects of cyclic antidepressants. Due to their anticholinergic actions, some cyclic antidepressants like maprotiline may potentially antagonize the therapeutic actions of the cholinesterase-inhibitors used for the treatment of dementia.
    Mepenzolate: (Major) The muscarinic actions of drugs known as parasympathomimetics, including both direct cholinergic receptor agonists and cholinesterase inhibitors, can antagonize the antimuscarinic actions of anticholinergic drugs, and vice versa.
    Meperidine; Promethazine: (Moderate) Drugs that possess antimuscarinic properties, such as promethazine, are pharmacologic opposites of bethanechol. These agents should not be used with bethanechol except when the specific intent is to counteract excessive actions of one or the other.
    Mepivacaine; Levonordefrin: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects.
    Mesoridazine: (Moderate) Drugs that possess antimuscarinic properties, such as mesoridazine, are pharmacologic opposites of bethanechol. These agents should not be used with bethanechol except when the specific intent is to counteract excessive actions of one or the other.
    Methamphetamine: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects.
    Methenamine; Sodium Acid Phosphate; Methylene Blue; Hyoscyamine: (Major) The muscarinic actions of drugs known as parasympathomimetics, including both direct cholinergic receptor agonists and cholinesterase inhibitors, can antagonize the antimuscarinic actions of anticholinergic drugs, and vice versa.
    Methscopolamine: (Major) The muscarinic actions of drugs known as parasympathomimetics, including both direct cholinergic receptor agonists and cholinesterase inhibitors, can antagonize the antimuscarinic actions of anticholinergic drugs, and vice versa.
    Methylphenidate: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects.
    Midodrine: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects.
    Naproxen; Pseudoephedrine: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects.
    Neostigmine: (Major) Cholinergic agonists can cause additive pharmacodynamic effects if used concomitantly with cholinesterase inhibitors. Concurrent use is unlikely to be tolerated by the patient and should be avoided.
    Norepinephrine: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects.
    Olanzapine: (Moderate) Drugs that possess antimuscarinic properties, such as olanzapine, are pharmacologic opposites of bethanechol (a direct agonist at muscarinic cholinergic receptors). These agents should not be used with bethanechol except when the specific intent is to counteract excessive actions of one or the other.
    Opiate Agonists: (Moderate) Bethanechol facilitates intestinal and bladder function via parasympathomimetic actions. Opiate agonists impair the peristaltic activity of the intestine. Thus, these drugs can antagonize the beneficial actions of bethanechol on GI motility.
    Oxybutynin: (Major) The muscarinic actions of drugs known as parasympathomimetics, including both direct cholinergic receptor agonists and cholinesterase inhibitors, can antagonize the antimuscarinic actions of anticholinergic drugs, and vice versa.
    Pemoline: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects.
    Phendimetrazine: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects.
    Phentermine: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects.
    Phentermine; Topiramate: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects.
    Phenylephrine: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects.
    Phenylephrine; Promethazine: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects. (Moderate) Drugs that possess antimuscarinic properties, such as promethazine, are pharmacologic opposites of bethanechol. These agents should not be used with bethanechol except when the specific intent is to counteract excessive actions of one or the other.
    Physostigmine: (Major) Cholinergic agonists can cause additive pharmacodynamic effects if used concomitantly with cholinesterase inhibitors. Concurrent use is unlikely to be tolerated by the patient and should be avoided.
    Pilocarpine: (Moderate) Pilocarpine and bethanechol are both cholinergic agonists. Coadministration is expected to result in additive parasympathomimetic effects.
    Pralidoxime: (Moderate) Pralidoxime and bethanechol are both cholinergic agonists. Coadministration is expected to result in additive parasympathomimetic effects.
    Prilocaine; Epinephrine: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects.
    Procainamide: (Moderate) Drugs that possess antimuscarinic properties, such as procainamide, are pharmacologic opposites of bethanechol. These agents should not be used with bethanechol except when the specific intent is to counteract excessive actions of one or the other.
    Promethazine: (Moderate) Drugs that possess antimuscarinic properties, such as promethazine, are pharmacologic opposites of bethanechol. These agents should not be used with bethanechol except when the specific intent is to counteract excessive actions of one or the other.
    Propantheline: (Major) The muscarinic actions of drugs known as parasympathomimetics, including both direct cholinergic receptor agonists and cholinesterase inhibitors, can antagonize the antimuscarinic actions of anticholinergic drugs, and vice versa.
    Pseudoephedrine: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects.
    Pyridostigmine: (Major) Cholinergic agonists can cause additive pharmacodynamic effects if used concomitantly with cholinesterase inhibitors. Concurrent use is unlikely to be tolerated by the patient and should be avoided.
    Quinidine: (Moderate) Drugs that possess antimuscarinic properties, such as quinidine, are pharmacologic opposites of bethanechol. These agents should not be used with bethanechol except when the specific intent is to counteract excessive actions of one or the other.
    Racepinephrine: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects.
    Ritodrine: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects.
    Rivastigmine: (Major) Cholinergic agonists can cause additive pharmacodynamic effects if used concomitantly with cholinesterase inhibitors. Concurrent use is unlikely to be tolerated by the patient and should be avoided.
    Scopolamine: (Major) The muscarinic actions of drugs known as parasympathomimetics, including both direct cholinergic receptor agonists and cholinesterase inhibitors, can antagonize the antimuscarinic actions of anticholinergic drugs, and vice versa.
    Sincalide: (Moderate) Sincalide-induced gallbladder ejection fraction may be affected by bethanechol. False study results are possible in patients with drug-induced hyper- or hypo-responsiveness; thorough patient history is important in the interpretation of results.
    Sympathomimetics: (Moderate) Bethanechol offsets the effects of sympathomimetics at sites where sympathomimetic and cholinergic receptors have opposite effects.
    Tacrine: (Major) Cholinergic agonists can cause additive pharmacodynamic effects if used concomitantly with cholinesterase inhibitors. Concurrent use is unlikely to be tolerated by the patient and should be avoided.
    Thioridazine: (Moderate) Drugs that possess antimuscarinic properties, such as thioridazine, are pharmacologic opposites of bethanechol. These agents should not be used with bethanechol except when the specific intent is to counteract excessive actions of one or the other.
    Tricyclic antidepressants: (Moderate) Tricyclic antidepressants (TCAs) may antagonize some of the effects of parasympathomimetics (e.g., cholinesterase inhibitors) due to their anticholinergic activity. However, parasympathomimetics like bethanechol have occasionally been used historically to offset some of the adverse peripheral antimuscarinic (anticholinergic) effects of TCAs, such as dry mouth, constipation, or urinary retention. For years, physostigmine was used as an adjunct to the treatment of TCA overdose; however, its efficacy was limited to addressing anticholinergic effects. Additionally, case reports suggest that harmful effects such as seizures and bradyarrhythmias progressing to asystole, especially in patients with cardiac conduction abnormalities at baseline, are possible. For these reasons, physostigmine is no longer considered a standard of care in the treatment of TCA overdose.
    Trihexyphenidyl: (Major) The muscarinic actions of drugs known as parasympathomimetics, including both direct cholinergic receptor agonists and cholinesterase inhibitors, can antagonize the antimuscarinic actions of anticholinergic drugs, and vice versa.
    Trospium: (Moderate) Pharmacologically, parasympathomimetic drugs enhance muscarinic/cholinergic function. Because trospium is an antimuscarinic, the muscarinic actions of drugs known as parasympathomimetics, including direct cholinergic agonists, could be antagonized when used concomitantly with trospium.

    PREGNANCY AND LACTATION

    Pregnancy

    Bethanechol is classified in FDA pregnancy risk category C. Adequate studies have not been performed to determine whether bethanechol is teratogenic. The drug is best avoided during pregnancy.

    Bethanechol should only be administered during lactation when benefit to the mother outweighs the risk. It is not known if bethanechol is excreted into breast-milk. If bethanechol therapy is essential, breast-feeding should be discontinued because of the potential for severe adverse effects (e.g., cholinergic excess) in nursing infants.

    MECHANISM OF ACTION

    Bethanechol is a synthetic muscarinic stimulant. It does not inactivate acetylcholinesterase. Bethanechol exerts its parasympathomimetic effects by a direct action on muscarinic (cholinergic) receptors, all of which can be antagonized by atropine. Bethanechol primarily affects the urinary and GI tracts. Its effect on the bladder results from stimulation of muscarinic receptors in the detrusor muscle. The detrusor contracts, decreasing bladder capacity and producing urination. Bethanechol also stimulates ureteral peristalsis and relaxes the trigone and external sphincter. Because bethanechol is a direct-acting agonist, spinal cord injury will not compromise these actions.
     
    Stimulation of muscarinic receptors in the GI tract restores peristalsis, increases motility, and increases the resting lower esophageal sphincter pressure. Bethanechol also stimulates the lower GI tract, producing defecation. Bethanechol produces a much more vigorous response in denervated than in normal smooth muscle. It does not stimulate nicotinic receptors and is not degraded by acetylcholinesterase. Bethanechol is a preferred drug in the treatment of postpartum and postoperative nonobstructive urinary retention, and it also can counteract bladder dysfunction often seen with phenothiazines and tricyclic antidepressants.

    PHARMACOKINETICS

    Bethanechol is administered orally and subcutaneously. After administration, the distribution of bethanechol is not well known. Due to its quaternary (i.e., charged) state, bethanechol does not penetrate the blood-brain barrier at therapeutic doses. Because it is not susceptible to degradation by acetylcholinesterase, bethanechol has a longer duration of action than endogenous acetylcholine. The mechanism of elimination is unknown.

    Oral Route

    Bethanechol poorly absorbed from the gastrointestinal tract. Its oral bioavailability is unknown. Onset of action occurs within 30—90 minutes when taken orally. It is a short-acting drug; effects typically last 1 hour when taken orally.

    Subcutaneous Route

    Parenteral doses of bethanechol are much more potent than equivalent oral doses and should be administered cautiously. Onset of action occurs within 5—15 minutes when given subcutaneously. It is a short-acting drug; effects typically last 2 hours when taken subcutaneously.