Dicyclomine (Page 4 of 4)

12 CLINICAL PHARMACOLOGY

12.1 Mechanism of Action

Dicyclomine relieves smooth muscle spasm of the gastrointestinal tract. Animal studies indicate that this action is achieved via a dual mechanism:

  • 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

  • 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.

12.2 Pharmacodynamics

Dicyclomine hydrochloride 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

A b s o r p ti o n 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 extensive distribution in tissues.

E li m i n a ti o n

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 evaluate 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

Dicyclomine hydrochloride tablets, USP 20 mg are supplied as Blue, Round, Unscored Tablet; Debossed “WW 27” and are available in:

Bottles of 100 tablets NDC 0143-1227-01

Bottles of 1000 tablets NDC 0143-1227-10

Store at 20° to 25°C (68° to 77°F). [See USP Controlled Room Temperature]. Protect from light and moisture.

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.

17 PATIENT COUNSELING INFORMATION

17.2 Use in Infants

Inform parents and caregivers not to administer dicyclomine hydrochloride in infants less than 6 months of age [see Use in Specific Populations (8.4)].

17.3 Use in Nursing Mothers

Advise lactating women that dicyclomine hydrochloride should not be used while breastfeeding their infants [see Use in Specific Populations (8.3,8.4)].

17.4 Peripheral and Central Nervous System

In the presence of a high environmental temperature, heat prostration can occur with dicyclomine hydrochloride use (fever and heat stroke due to decreased sweating). If symptoms occur, the drug should be discontinued and a physician contacted. 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 to perform hazardous work while taking dicyclomine hydrochloride [see Warnings and Precautions (5.3)].

Distr. by:

West-Ward Pharmaceuticals Corp.

Eatontown, NJ 07724

Revised May 2018

C50000174/01

NDC 0143-1227-01
Dicyclomine Hydrochloride Tablets, USP
20 mg
100 Tablets
Rx Only

NDC 0143-1227-01 Dicyclomine Hydrochloride Tablets, USP 20 mg 100 Tablets Rx Only
(click image for full-size original)
DICYCLOMINE
dicyclomine hydrochloride tablet
Product Information
Product Type HUMAN PRESCRIPTION DRUG Item Code (Source) NDC:0143-1227
Route of Administration ORAL DEA Schedule
Active Ingredient/Active Moiety
Ingredient Name Basis of Strength Strength
DICYCLOMINE HYDROCHLORIDE (DICYCLOMINE) DICYCLOMINE HYDROCHLORIDE 20 mg
Inactive Ingredients
Ingredient Name Strength
ANHYDROUS LACTOSE
FD&C BLUE NO. 1
LACTOSE MONOHYDRATE
MAGNESIUM STEARATE
CELLULOSE, MICROCRYSTALLINE
Product Characteristics
Color BLUE (BLUE) Score no score
Shape ROUND (ROUND) Size 7mm
Flavor Imprint Code WW;27
Contains
Packaging
# Item Code Package Description Multilevel Packaging
1 NDC:0143-1227-01 100 TABLET in 1 BOTTLE, PLASTIC None
2 NDC:0143-1227-10 1000 TABLET in 1 BOTTLE, PLASTIC None
Marketing Information
Marketing Category Application Number or Monograph Citation Marketing Start Date Marketing End Date
ANDA ANDA040161 10/01/1996
Labeler — Hikma Pharmaceuticals USA Inc. (001230762)

Revised: 05/2018 Hikma Pharmaceuticals USA Inc.

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