Dicyclomine Hydrochloride

Dicyclomine hydrochloride is an antispasmodic and anticholinergic (antimuscarinic) agent.

Chemically, dicyclomine hydrochloride is [bicyclohexyl]-1-carboxylic acid, 2-(diethylamino) ethyl ester, hydrochloride with the following structural formula, molecular weight, and molecular formula:

Dicyclomine hydrochloride occurs as a fine, white, crystalline, practically odorless powder with a bitter taste. It is soluble in water, freely soluble in alcohol and chloroform, and very slightly soluble in ether.

Dicyclomine hydrochloride tablets, for oral administration, contain 20 mg of dicyclomine hydrochloride, USP. In addition, each tablet contains the following inactive ingredients: anhydrous lactose, colloidal silicon dioxide, FD&C Blue No.1 Lake, magnesium stearate, microcrystalline cellulose, pregelatinized starch, and sodium lauryl sulfate.

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 acetylcholine-receptor sites with approximately 1/8 the milligram potency of atropine (in vitro, guinea pig ileum); and (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 two agonists. In vivo studies in cats and dogs showed dicyclomine to be equally potent against acetylcholine (ACh)- or barium chloride (BaCl₂)-induced intestinal spasm while atropine was at least 200 times more potent against effects of ACh than 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.

In man, dicyclomine is rapidly absorbed after oral administration, reaching peak values within 60 to 90 minutes. The principal route of elimination is via the urine (79.5% of the dose). Excretion also occurs in the feces, but to a lesser extent (8.4%). Mean half-life of plasma elimination in one study was determined to be approximately 1.8 hours when plasma concentrations were measured for 9 hours after a single dose. In subsequent studies, plasma concentrations were followed for up to 24 hours after a single dose, showing a secondary phase of elimination with a somewhat longer half-life. Mean volume of distribution for a 20 mg oral dose is approximately 3.65 L/kg suggesting extensive distribution in tissues.

In controlled clinical trials involving over 100 patients who received drug, 82% of patients treated for functional bowel/irritable bowel syndrome with dicyclomine hydrochloride at initial doses of 160 mg daily (40 mg q.i.d.) demonstrated a favorable clinical response compared with 55% treated with placebo (P < 0.05). In these trials, most of the side effects were typically anticholinergic in nature (see table) and were reported by 61% of the patients.

Nine percent (9%) of patients were discontinued from the drug because of one or more of these side effects (compared with 2% in the placebo group). In 41% of the patients with side effects, side effects disappeared or were tolerated at the 160 mg daily dose without reduction. A dose reduction from 160 mg daily to an average daily dose of 90 mg was required in 46% of the patients with side effects who then continued to experience a favorable clinical response; their side effects either disappeared or were tolerated. (See ADVERSE REACTIONS.)

For the treatment of functional bowel/irritable bowel syndrome.

1. Obstructive uropathy
2. Obstructive disease of the gastrointestinal tract
3. Severe ulcerative colitis (See PRECAUTIONS.)
4. Reflux esophagitis
5. Unstable cardiovascular status in acute hemorrhage
6. Glaucoma
7. Myasthenia gravis
8. Evidence of prior hypersensitivity to dicyclomine hydrochloride or other ingredients of these formulations
9. Infants less than 6 months of age (See WARNINGS and PRECAUTIONS: Information for Patients.)
10. Nursing mothers (See WARNINGS and PRECAUTIONS: Information for Patients.)

In the presence of a high environmental temperature, heat prostration can occur with drug use (fever and heat stroke due to decreased sweating). If symptoms occur, the drug should be discontinued and supportive measures instituted.

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.

Dicyclomine hydrochloride 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.

There are reports that administration of dicyclomine hydrochloride syrup to infants has been followed by serious respiratory symptoms (dyspnea, shortness of breath, breathlessness, respiratory collapse, apnea, asphyxia), seizures, syncope, pulse rate fluctuations, muscular hypotonia, and coma. Death has been reported. No causal relationship between these effects observed in infants and dicyclomine administration has been established. DICYCLOMINE HYDROCHLORIDE IS CONTRAINDICATED IN INFANTS LESS THAN 6 MONTHS OF AGE AND IN NURSING MOTHERS. (See CONTRAINDICATIONS and PRECAUTIONS: Nursing Mothers and Pediatric Use.)

Safety and efficacy of dicyclomine hydrochloride in pediatric patients have not been established.

Controlled clinical trials have provided frequency information for reported adverse effects of dicyclomine hydrochloride listed in a decreasing order of frequency. (See CLINICAL PHARMACOLOGY.)

Not all of the following adverse reactions have been reported with dicyclomine hydrochloride. Adverse reactions are included here that have been reported for pharmacologically similar drugs with anticholinergic/antispasmodic action.

Gastrointestinal: dry mouth, nausea, vomiting, constipation, bloated feeling, abdominal pain, taste loss, anorexia

Central Nervous System: dizziness, light-headedness, tingling, headache, drowsiness, weakness, nervousness, numbness, mental confusion and/or excitement (especially in elderly persons), dyskinesia, lethargy, syncope, speech disturbance, insomnia

Ophthalmologic: blurred vision, diplopia, mydriasis, 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 (See WARNINGS.)

Other: decreased sweating, nasal stuffiness or congestion, sneezing, throat congestion, impotence, suppression of lactation (See PRECAUTIONS: Nursing Mothers.)

Abuse of and/or dependence on dicyclomine for anticholinergic effects have been rarely reported.

DOSAGE MUST BE ADJUSTED TO INDIVIDUAL PATIENT NEEDS. (See CLINICAL PHARMACOLOGY.)

Dicyclomine Hydrochloride Tablets, USP are available containing dicyclomine hydrochloride, USP equivalent to 10 mg of dicyclomine.

The 10 mg tablet is a blue, round, tablet debossed with M over D6 on one side of the tablet and blank on the other side.

They are supplied by State of Florida DOH Central Pharmacy as follows:

Store at 20° to 25°C (68° to 77°F). [See USP for Controlled Room Temperature.]

To prevent fading, avoid exposure to direct sunlight.

Dispense in a tight, light-resistant container as defined in the USP using a child-resistant closure.

Mylan Pharmaceuticals Inc.
Morgantown, WV 26505

This Product was Repackaged By:

State of Florida DOH Central Pharmacy
104-2 Hamilton Park Drive
Tallahassee, FL 32304
United States

PRINCIPAL DISPLAY PANEL - 10 mg

NDC 53808-0352-1

DICYCLOMINE
HYDROCHLORIDE
TABLETS, USP
20 mg

30 TABLETS (Rx only)

Each tablet contains:
Dicyclomine
hydrochloride, USP 10 mg

Dispense in a tight, light-resistant
container as defined in the USP
using a child-resistant closure.

Keep container tightly closed.

Keep this and all medication out
of the reach of children.

Store at 20° to 25°C (68° to 77°F).
[See USP for Controlled Room
Temperature.]

To prevent fading, avoid
exposure to direct sunlight.

Usual Dosage: See accompanying
prescribing information.