Bethanechol chloride, a cholinergic agent, is a synthetic esler which is structurally and pharmacologically related to acetylcholine.

It is designated chemically as Z-[(aminocarbony) oxy]-N, N, (V-trimethyl-1-propanaminium chloride. Its molecular formula is C₇H₁₇CIN₂0₂ and its structural formula is:

It is a white, hygroscopic crystalline powder having a slight amine-like odor, freely soluble in water, and has a molecular weight of 196.68.

Each tablet for oral administration contains 5 mg, 10 mg, 25 mg or 50 mg bethanechol chloride, USP Tablets also contain the following inactive ingredients: colloidal silicon dioxide, lactose monohydrate, magnesium stearate, microcrystalline cellulose, sodium starch glycolate, (25 mg and 50 mg) D&C~ Yellow # 10 Lake and FD&C Yellow # 6 Lake.

Last updated on RxList: 5/28/2008

bethanechol chloride is indicated for the treatment of acute postoperative and postpartum non obstructive (functional) urinary retention and for neurogenic atony of the urinary bladder with retention.

Dosage must be individualized, depending on the type and severity of the condition to be treated.

Preferably give the drug when the stomach is empty. If taken soon after eating, nausea and vomiting may occur.

The usual adult oral dose ranges from 10 to 50 mg three or four times a day. The minimum effective dose is determined by giving 5 to 10 mg initially and repeating the same amount at hourly intervals until satisfactory response occurs, or until a maximum of 50 mg has been given. The effects of the drug sometimes appear within 30 minutes and are usually maximal within 60 to 90 minutes. The drug effects persist for about one hour.

If necessary, the effects of the drug can be abolished promptly by atropine (see OVERDOSAGE).

Bethanechol Chloride Tablets, USP

5 mg - White, 7/16" diameter, round flat faced bevel edge tablets: one side scored and debossed BCL bisect 5, one side debossed 832, in bottles of 100 and 1000, and in unit dose cartons of 100 tablets (10 cards containing 10 tablets each).

10 mg - White, 7/16" diameter, round flat faced bevel edge tablets; one side scored and debossed BCL bisect 10, one side debossed 832, in bottles of 100. 250 and 1000, and in unit dose cartons of 100 tablets (10 cards containing 10 tablets each).

25 mg - Yellow, 7/16" diameter, round flat faced bevel edge tablets; one side scored and debossed BCL bisect 25, one side debossed 832, in bottles of 100, 250, 500 and 1000, and in unit dose cartons of 100 tablets (10 cards containing 10 tablets each).

50 mg - Yellow, 7/16" diameter, round fiat faced bevel edge tablets; one side scored and debossed BCL bisect 50, one side debossed 832, in bottles of 100, 500 and 1000. and in unit dose cartons of 100 tablets (10 cards containing 10 tablets each).

Store at 20-25°C (68-7?°F) and excursions permitted to 15-30"C (59-86°F) [see USP Controlled Room Temperature].

Dispense in a tight container as defined in the USP

Keep out of reach of children.

Rev. 05-05. Manufactured by: UPSHER-SMITH LABORATORIES, INC. Minneapolis, MN 55447. FDA Rev date: 6/1/2005

Last updated on RxList: 5/28/2008

Adverse reactions are rare following oral administration of bethanechol, but are more common following subcutaneous injection. Adverse reactions are more likely to occur when dosage is increased.

The following adverse reactions have been observed: Body as a Whole: malaise; Digestive: abdominal cramps or discomfort, colicky pain, nausea and belching, diarrhea, borborygmi, salivation; Renal: urinary urgency; Nervous System: headache; Cardiovascular: a fall in blood pressure with reflex tachycardia, vasomotor response; Skin: flushing producing a feeling of warmth, sensation of heat about the face, sweating; Respiratory: bronchial constriction, asthmatic attacks; Special Senses: lacrimation, miosis,

Causal Relationship Unknown

The following adverse reactions have been reported, and a causal relationship to therapy with bethanechol has not been established: Body as a Whole: malaise; Nervous System: seizures.

Special care is required if this drug is given to patients receiving ganglion blocking compounds because a critical fail in blood pressure may occur. Usually, severe abdominal symptoms appear before there is such a fail in the blood pressure.

Last updated on RxList: 5/28/2008

No information provided.

General

In urinary retention, if the sphincter fails to relax as bethanechol contracts the bladder, urine may be forced up the ureter into the kidney pelvis. If there is bacteriuria, this may cause reflux infection.

Carcinogenesis, Mutagenesis, Impairment of Fertility

Long-term studies in animals have not been performed to evaluate the effects upon fertility, mutagenic or carcinogenic potential of bethanechol chloride.

Pregnancy

Teratogenic Effects

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

Nursing Mothers

It is not known whether this drug is secreted in human milk. Because many drugs are secreted in human milk and because of the potential for serious adverse reactions from bethanechol chloride in nursing infants, a decision should be made whether to discontinue nursing or to discontinue the drug, taking Into account the importance of the drug to the mother.

Pediatric Use

Safety and effectiveness in pediatric patients have not been established.

Last updated on RxList: 5/28/2008

Early signs of overdosage are abdominal discomfort, salivation, flushing of the skin ("hot feeling"), sweating, nausea, and vomiting.

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.

The oral LD50 of bethanechol chloride is 1510 mg/kg in the mouse.

Hypersensitivity to bethanechol chloride tablets, hyperthyroidism, peptic ulcer, latent or active bronchial asthma, pronounced bradycardia or hypotension, vasomotor Instability, coronary artery disease, epilepsy and parkinsonism.

bethanechol chloride should not be employed when the strength or integrity of the gastrointestinal or bladder wall is in question, or in the presence of mechanical obstruction; when increased muscular activity of the gastrointestinal tract or urinary bladder might prove harmful, as following recent urinary bladder surgery, gastrointestinal resection and anastomosis, or when there Is possible gastrointestinal obstruction; in bladder neck obstruction, spastic gastrointestinal disturbances, acute inflammatory lesions of the gastrointestinal tract, or peritonitis; or in marked vagotonia.

Last updated on RxList: 5/28/2008

Bethanechol chloride acts principally by producing the effects of stimulation of the parasympathetic nervous system. It increases the tone of the detrusor urinae muscle, usually producing a contraction sufficiently strong to initiate micturition and empty the bladder. It stimulates gastric motility, increases gastric tone and often restores impaired rhythmic peristalsis.

Stimulation of the parasympathetic nervous system releases acetylcholine at the nerve endings. When spontaneous stimulation is reduced and therapeutic intervention is required, acetylcholine can be given, but it is rapidly hydrolyzed by cholinesterase and its effects are transient. Bethanechol chloride is not destroyed by cholinesterase and its effects are more prolonged than those of acetylcholine.

Effects on the GI and urinary tracts sometimes appear within 30 minutes after oral administration of bethanechol chloride, but more often SO to 90 minutes are required to reach maximum effectiveness. Following oral administration, the usual duration of action of bethanechol is one hour, although large doses (300 to 400 mg) have been reported to produce effects for up to six hours. Subcutaneous injection produces a more intense action on bladder muscle than does oral administration of the drug.

Because of the selective action of bethanechol, nicotinic symptoms of cholinergic stimulation are usually absent or minimal when orally or subcutaneously administered in therapeutic doses, while muscarinic effects are prominent. Muscarinic effects usually occur within 5 to 15 minutes after subcutaneous injection, reach a maximum in 15 to 30 minutes, and disappear within two hours. Doses that stimulate micturition and defecation and increase peristalsis do not ordinarily stimulate ganglia or voluntary muscles. Therapeutic test doses in normal human subjects have little effect on heart rate, blood pressure or peripheral circulation.

Bethanechol chloride does not cross the blood-brain barrier because of its charged quaternary amine moiety. The metabolic rate and mode of excretion of the drug have not been elucidated.

A clinical study (Diokno, A.C., Lapides, J.; Urol 10 : 23-24, July 1977) was conducted on the relative effectiveness of oral and subcutaneous doses of bethanechol chloride on the stretch response of bladder muscle in patients with urinary retention. Results showed that 5 mg of the drug given subcutaneously stimulated a response that was more rapid in onset and of larger magnitude than an oral dose of 50 mg, 100 mg, or 200 mg. All the oral doses, however, had a longer duration of effect than the subcutaneous dose. Although the 50 mg oral dose caused little change in intravesical pressure in this study, this dose has been found in other studies to be clinically effective in the rehabilitation of patients with decompensated bladders.

Last updated on RxList: 5/28/2008

Bethanechol chloride tablets should preferably be taken one hour before or two hours after meals to avoid nausea or vomiting. Dizziness, lightheadedness or fainting may occur, especially when getting up from a lying or sitting position,

Last updated on RxList: 5/28/2008

IMPORTANT NOTE: This is a summary and does not contain all possible information about this product. For complete information about this product or your specific health needs, ask your health care professional. Always seek the advice of your health care professional if you have any questions about this product or your medical condition. This information is not intended as individual medical advice and does not substitute for the knowledge and judgment of your health care professional. This information does not contain any assurances that this product is safe, effective, or appropriate for you.

BETHANECHOL - ORAL

(beth-AN-eh-coal)

COMMON BRAND NAME(S): Urecholine

USES: This medication is used to treat certain bladder problems such as the inability to urinate or empty the bladder completely due to certain causes (e.g., surgery, bladder muscle problems). It works by helping the bladder muscle to squeeze better, thereby improving your ability to urinate.

OTHER USES: This section contains uses of this drug that are not listed in the approved professional labeling for the drug but that may be prescribed by your health care professional. Use this drug for a condition that is listed in this section only if it has been so prescribed by your health care professional.

This drug may also be used to treat heartburn. It works by helping the stomach muscles move food down out of the stomach faster and by increasing the strength of the muscle between the esophagus and stomach (lower esophageal sphincter). This helps prevent food/acid in the stomach from rising back into the esophagus.

HOW TO USE: Take this medication by mouth on an empty stomach (1 hour before or 2 hours after meals), usually 3 to 4 times daily or as directed by your doctor. Taking this medication on an empty stomach will help reduce nausea/vomiting.

Dosage is based on your medical condition and response to treatment.

Use this medication regularly to get the most benefit from it. To help you remember, take it at the same times each day.

Tell your doctor if your condition persists or worsens.

SIDE EFFECTS: Dizziness, lightheadedness, nausea, vomiting, abdominal cramps/pain, diarrhea, increased saliva/urination, sweating, flushing, watery eyes, or headache may occur. If any of these effects persist or worsen, tell your doctor or pharmacist promptly.

To reduce dizziness and lightheadedness, get up slowly when rising from a sitting or lying position.

Remember that your doctor has prescribed this medication because he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.

Tell your doctor immediately if any of these unlikely but serious side effects occur: fainting, fast heartbeat, severe abdominal pain.

Seek immediate medical attention if any of these rare but very serious side effects occur: trouble breathing.

A very serious allergic reaction to this drug is rare. However, seek immediate medical attention if you notice any symptoms of a serious allergic reaction, including: rash, itching, swelling, severe dizziness, trouble breathing.

This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.

Contact your doctor for medical advice about side effects. The following numbers do not provide medical advice, but in the US you may report side effects to the Food and Drug Administration (FDA) at 1-800-FDA-1088. In Canada, you may call Health Canada at 1-866-234-2345.

PRECAUTIONS: Before taking bethanechol, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies.

This medication should not be used if you have certain medical conditions. Before using this medicine, consult your doctor or pharmacist if you have: recent stomach/intestinal/bladder surgery, stomach/intestinal problems (e.g., ulcers, blockage, spasms), peritonitis, blockage of the bladder, a certain nerve problem (vagotonia), overactive thyroid (hyperthyroidism), lung disease (e.g., asthma, chronic obstructive pulmonary disease-COPD), heart problems (e.g., coronary artery disease, slow heartbeat), seizures, Parkinson's disease, blood pressure problems.

Before using this medication, tell your doctor or pharmacist your medical history.

This drug may make you dizzy. Use caution while driving, using machinery, or doing any activity that requires alertness. Limit alcoholic beverages.

During pregnancy, this medication should be used only when clearly needed. Discuss the risks and benefits with your doctor.

It is not known whether this drug passes into breast milk. Because of the possible risk to the infant, breast-feeding while using this drug is not recommended. Consult your doctor before breast-feeding.

DRUG INTERACTIONS: Your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor or pharmacist first.

Before using this medication, tell your doctor or pharmacist of all prescription and nonprescription/herbal products you may use, especially of: medications for high blood pressure (e.g., mecamylamine).

This medication may interfere with certain laboratory tests (including amylase/lipase levels), possibly causing false test results. Make sure laboratory personnel and all your doctors know you use this drug.

This document does not contain all possible interactions. Therefore, before using this product, tell your doctor or pharmacist of all the products you use. Keep a list of all your medications with you, and share the list with your doctor and pharmacist.

OVERDOSE: If overdose is suspected, contact your local poison control center or emergency room immediately. US residents can call the US National Poison Hotline at 1-800-222-1222. Canada residents can call a provincial poison control center. Symptoms of overdose may include: stomach/abdominal pain, flushing, increased saliva, sweating, nausea, vomiting.

NOTES: Do not share this medication with others.

MISSED DOSE: If you miss a dose, take it as soon as you remember. If it is near the time of the next dose, skip the missed dose and resume your usual dosing schedule. Do not double the dose to catch up.

STORAGE: Store at room temperature between 59-86 degrees F (15-30 degrees C) away from light and moisture. Do not store in the bathroom. Keep all medicines away from children and pets.

Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company for more details about how to safely discard your product.

Information last revised July 2008 Copyright(c) 2008 First DataBank, Inc.