Bentylol (Dicyclomine HCl)

BENTYLOL®

Hoechst Marion Roussel

Dicyclomine HCl

Antispasmodic

Action And Clinical Pharmacology: Dicyclomine relieves smooth muscle spasm of the gastrointestinal tract. Animal studies indicate that this action is achieved via a dual mechanism: 1) a specific anticholinergic effect (antimuscarinic) at the ACh-receptor sites with approximately 1/8 the mg potency of atropine (in vitro guinea pig ileum); 2) a direct effect upon smooth muscle (musculotropic) as evidenced by dicyclomine’s antagonism of bradykinin- and histamine-induced spasms of the isolated guinea pig ileum. Atropine did not affect responses to these 2 agonists. Animal studies showed dicyclomine to be equally potent against ACh- or BaCl2-induced intestinal spasm while atropine was at least 200 times more potent against the effects of ACh than against BaCl2. Tests for mydriatic effects in mice showed that dicyclomine was approximately 1/500 as potent as atropine; antisialagogue tests in rabbits showed dicyclomine to be 1/300 as potent as atropine.

After a single oral 20 mg dose of dicyclomine in volunteers, peak plasma concentration reached a mean value of 58 ng/mL in 1 to 1.5 hours. The principal route of elimination is via the urine.

Indications And Clinical Uses: For the treatment of functional gastrointestinal tract conditions involving smooth muscle spasm such as irritable colon (mucous colitis, spastic colon, irritable bowel syndrome) and spastic constipation. It can also be used as adjunctive therapy in organic gastrointestinal conditions to relieve associated smooth muscle spasm such as in colitis, diverticulitis, regional enteritis, gastritis, and peptic ulcer.

Contra-Indications: Known idiosyncrasy to dicyclomine. Infants less than 6 months of age (see Warnings) and in nursing mothers (see Precautions). Should not be used in patients with obstructive uropathy, obstructive disease of the gastrointestinal tract, paralytic ileus and intestinal atony, severe ulcerative colitis, myasthenia gravis, reflux esophagitis, glaucoma, unstable cardiovascular status in acute hemorrhage.

Manufacturers’ Warnings In Clinical States: Infants: There are reports of infants who, in their first 3 months of life, were given dicyclomine syrup and evidenced respiratory symptoms (breathing difficulty, shortness of breath, breathlessness, respiratory collapse, apnea), as well as seizures, syncope, asphyxia, pulse rate fluctuations, muscular hypotonia, and coma. In some instances, these symptoms occurred within minutes of ingestion and lasted up to 20 to 30 minutes. The symptoms were reported in association with dicyclomine syrup therapy but a proven cause and effect relationship has not been established.

Worldwide, a few deaths have been reported in infants 3 months of age or less who had been given dicyclomine syrup. Two of these were reported to have been associated with excessively high dicyclomine blood levels.

Although no causal relationship between these effects, observed in infants, and dicyclomine administration has been established, dicyclomine is contraindicated in infants 6 months of age or less (see Contraindications).

Other: Diarrhea may be an early symptom of incomplete intestinal obstruction, especially in patients with ileostomy or colostomy. In this instance, treatment with this drug would be inappropriate and possibly harmful.

Occupational Hazards: Dicyclomine may produce drowsiness or blurred vision. The patient should be warned not to engage in activities requiring mental alertness, such as operating a motor vehicle or other machinery or performing hazardous work while taking this drug.

Psychosis has been reported in sensitive individuals given anticholinergic drugs. CNS signs and symptoms include confusion, disorientation, short-term memory loss, hallucinations, dysarthria, ataxia, coma, euphoria, decreased anxiety, fatigue, insomnia, agitation and mannerisms, and inappropriate affect. These CNS signs and symptoms usually resolve within 12 to 24 hours after discontinuation of the drug.

Precautions: General: Dicyclomine should be used with caution in any patient with, or suspected of having: prostatic hypertrophy, hiatal hernia associated with reflux esophagitis because anticholinergic drugs may aggravate the condition, autonomic neuropathy, hepatic or renal disease, hyperthyroidism, hypertension, coronary heart disease, congestive heart failure, cardiac tachyarrhythmia.

Pregnancy: Epidemiologic studies in pregnant women with products containing dicyclomine (at doses up to 40 mg/day) have not shown that dicyclomine increases the risk of fetal abnormalities if administered during the first trimester of pregnancy. There are however no adequate and well-controlled studies in pregnant women at the recommended doses (80 to 160 mg/day). Animal reproduction studies have revealed no evidence of impaired fertility or harm to the fetus due to dicyclomine. Because animal reproduction studies are not always predictive of human response, dicyclomine should be used during pregnancy only if required.

Lactation: Since dicyclomine has been reported to be excreted in human milk, its use is contraindicated in nursing mothers (see Contraindications).

Drug Interactions: The following agents may increase certain actions or side effects of anticholinergic drugs: amantadine, antiarrhythmic agents of class I (e.g., quinidine), antihistamines, antipsychotic agents (e.g., phenothiazines), benzodiazepines, MAO inhibitors, narcotic analgesics (e.g., meperidine), nitrates and nitrites, sympathomimetic agents, tricyclic antidepressants, and other drugs having anticholinergic activity.

Anticholinergics antagonize the effects of antiglaucoma agents. Anticholinergic drugs in the presence of increased intraocular pressure may be hazardous when taken concurently with agents such as corticosteroids.

Anticholinergic agents may affect gastrointestinal absorption of various drugs, such as slowly dissolving dosage forms of digoxin; increased serum digoxin concentrations may result. Anticholinergic drugs may antagonize the effects of drugs that alter gastrointestinal motility such as metoclopramide. Because antacids may interfere with the absorption of anticholinergic agents, simultaneous use of these drugs should be avoided.

The inhibiting effects of anticholinergic drugs on gastric hydrochloric acid secretion are antagonized by agents used to treat achlorhydria and those to test gastric secretion.

Adverse Reactions: Most adverse reactions reported in clinical trials conducted with dicyclomine were typically anticholinergic in nature and included, in decreasing order of frequency: dry mouth, dizziness, blurred vision, nausea, lightheadedness, drowsiness, weakness and nervousness.

Other adverse reactions reported with dicyclomine and pharmacologically similar drugs, e.g., other anticholinergics and antispasmodics, were the following:

Gastrointestinal: vomiting, constipation, bloated feeling, abdominal pain, taste loss, anorexia.

CNS: tingling, headache, numbness, mental confusion and/or excitement (especially in elderly persons), dyskinesia, lethargy, syncope, speech disturbance, insomnia.

Ophthalmologic: diplopia, mydrias, cycloplegia, increased ocular tension.

Dermatologic/Allergic: rash, urticaria, itching, and other dermal manifestations; severe allergic reaction or drug idiosyncrasies including anaphylaxis.

Genitourinary: urinary hesitancy, urinary retention.

Cardiovascular: tachycardia, palpitations.

Respiratory: dyspnea, apnea, asphyxia.

Other: decreased sweating, nasal stuffiness or congestion, sneezing, throat congestion, impotence, suppression of lactation (see Precautions).

Symptoms And Treatment Of Overdose: Symptoms: Signs and symptoms of dicyclomine overdosage are headache; nausea; vomiting; blurred vision; dilated pupils; hot, dry skin; dizziness; dry mouth; difficulty in swallowing; and CNS stimulation. A curare-like action may occur (i.e., neuromuscular blockage leading to muscular weakness and possible paralysis). tag_Treatment

Treatment: Treatment should consist of gastric lavage, emetics and activated charcoal. Sedatives (e.g., short-acting barbiturates, benzodiazepines) may be used for management of overt signs of excitement. If indicated, an appropriate parenteral cholinergic agent may be used as an antidote.

Dialysis: It is not known if dicyclomine is dialyzable.

Dosage And Administration: Dosage should be adjusted to individual patient needs.

Syrup and Tablets: Adults: 10 to 20 mg 3 to 4 times daily. Depending upon the patient’s response during the first week of therapy, the dose should be increased to 160 mg/day unless side effects limit dose escalation. If efficacy is not achieved within 2 weeks or side effects require doses below 80 mg/day, the drug should be discontinued. Documented safety data are not available for doses above 80 mg daily for periods longer than 2 weeks.

Children (2 to 12 years): 10 mg 3 to 4 times daily.

Infants (6 months to 2 years): 5 to 10 mg 3 to 4 times daily, 15 minutes before feeding. Do not exceed 40 mg daily. Syrup should be diluted with equal volume of water.

Availability And Storage: Syrup: Each 5 mL of clear red syrup contains: dicyclomine HCl USP 10 mg. Nonmedicinal ingredients: artificial and natural vanilla flavors, artificial blackcurrant flavor, artificial cherry flavor, artificial raspberry flavor, citric acid, glucose, methylparaben, propylene glycol, propylparaben, purified water, red no. 2, sodium citrate, sodium cyclamate and yellow FD&C #6. Energy: 57.4 kJ (14 kcal)/5 mL. Bottles of 250 mL. Store at room temperature, between 15 and 30°C. Protect from excessive heat.

Tablets: 10 mg: Each white, flat-faced, beveled edge, compressed tablet, with 10 on one side and M on the other with a double circle around it, contains: dicyclomine HCl USP 10 mg. Bottles of 100 and 500. Store at room temperature between 15 and 30°C. Protect from excessive heat and moisture.

20 mg: Each white, flat-faced, beveled edge, compressed tablet, with 20 on one side and M on the other with a double circle around it, contains: dicyclomine HCl USP 20 mg. Bottles of 100 and 500. Store at room temperature between 15 and 30°C. Protect from excessive heat and moisture. (Shown in Product Recognition Section)

BENTYLOL® Hoechst Marion Roussel Dicyclomine HCl Antispasmodic

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