imes 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.
12.2 Pharmacodynamics
BENTYL can inhibit the secretion of saliva and sweat, decrease gastrointestinal secretions and motility, cause drowsiness, dilate the pupils, increase heart rate, and depress motor function.
12.3 Pharmacokinetics
Absorption and Distribution
In man, dicyclomine is rapidly absorbed after oral administration, reaching peak values within 60-90 minutes. Mean volume of distribution for a 20 mg oral dose is approximately 3.65 L/kg suggesting exentsive distribution in tissues.
Elimination
The metabolism of dicyclomine was not studied. The principal route of excretion 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.
13 NONCLINICAL TOXICOLOGY
13.1 Carcinogenesis, Mutagenesis, Impairment of Fertility
Long-term animal studies have not been conducted to eva luate the carcinogenic potential of dicyclomine. In studies in rats at doses of up to 100 mg/kg/day, dicyclomine produced no deleterious effects on breeding, conception, or parturition.
14 CLINICAL STUDIES
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 four times daily) demonstrated a favorable clinical response compared with 55% treated with placebo (p<0.05).
16 HOW SUPPLIED/STORAGE AND HANDLING
BENTYL Capsules
10 mg blue capsules, imprinted BENTYL 10, supplied in bottles of 100. Store at room temperature, preferably below 86°F (30°C).
NDC number: 58914-012-10.
BENTYL Tablets
20 mg compressed, light blue, round tablets, debossed BENTYL 20, supplied in bottles of 100. To prevent fading, avoid exposure to direct sunlight. Store at room temperature, preferably below 86°F (30°C).
NDC 58914-013-10.
BENTYL Syrup
10 mg/5 mL pink syrup, supplied in 16 ounce bottles. Store at room temperature, preferably below 86°F (30°C). Protect from excessive heat.
NDC 58914-015-16.
BENTYL Injection
20 mg/2 mL (10 mg/mL) injection supplied in boxes of five 20 mg/2 mL ampoules (10 mg/mL). Store at room temperature, preferably below 86°F (30°C). Protect from freezing.
NDC 58914-080-52.
17 PATIENT COUNSELING INFORMATION
17.1 Inadvertent Intravenous Administration
BENTYL injection is for intramuscular administration only. Do not administer by any other route. Inadvertent administration may result in thrombosis or thrombophlebitis and injection site such as pain, edema, skin colour change and even reflex sympathetic dystrophy syndrome [see Adverse Reactions (6.2)].
17.2 Use in Infants
Inform parents and caregivers not to administer BENTYL in infants less than 6 months of age [see Use in Specific Populations (8.4)] .
17.3 |
