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Chemical name

Clidinium Bromide: (±) - 3 - Hydroxy - 1 - methylquinuclidinium bromide benzilate.
Chlordiazepoxide: 3H - 1, 4 - Benzodiazepin - 2 - amine, 7 - chloro - N - methyl - 5 - phenyl -, 4 - oxide.

Category

Anticholinergic - sedative.

Mechanism of action

Clidinium bromide inhibits the muscarinic actions of acetylcholine on structures innervated by postganglionic cholinergic nerves as well as on smooth muscles that respond to acetylcholine but lack cholinergic innervation. These postganglionic receptor sites are present in the autonomic effector cells of the smooth muscle, cardiac muscle, sinoartrial and atrioventricular nodes, and exocrine glands.
Chlordiazepoxide stimulates GABA receptors in the ascending reticular activating system. Since GABA is inhibitory, receptor stimulation increases inhibition and blocks both cortical and limbic arousal following stimulation of the brain stem reticular formation.

Indications

- Ulcer, peptic (treatment adjunct). - Bowel syndrome, irritable (treatment).

Precautions to consider

Risk benefit should be considered when the following medical problems exist:
Brain damage, in children; cardiac disease; down's syndrome; esophagitis, reflux; fever; gastrointestinal tract obstructive disease; glucoma, angle - closure; glucoma, open - angle; hemorrhage, acute; renal and hepatic function impairment; hernia, hiatal, associated - with reflux esophagitis; hypertension; hyperthyroidism; intestinal atony; paralytic ileus; lung disease; myasthenia gravis; neuropathy, autonomic; prostatic hypertrophy, nonobstructive; urinary retention; uropathy, obstructive; pyloric obstruction; Sensitivity to any belladonna alkaloids or derivatives; Sensitivity to benzodiazepines; spastic paralysis, tachycardia; porphyria; toxemia of pregnancy; ulcerative colitis; xerostomia; hyperkinesis; epilepsy or seizures; sleep apnea.

Pregnancy

Use is not recommended; chronic use of chlordiazepoxide may cause physical dependence and withdrawal symptoms in the neonate; Chlordiazepoxide increases risk of congenital malformations in first trimester.

Breast - feeding

Chlordiazepoxide distributed into breast milk; Clidinium may cause inhibition of lactation.

Drug interactions

Combinations containing any of the following medications, depending on the amount present, may also interact with this medication.
Only specific interactions between anticholinergics and other oral medications have been identified. However, because of decreased gastrointestinal motility and delayed gastric emptying, absorption of other oral medications may be decreased during concurrent use with anticholinergics.
Alcohol; CNS depressants; Amantadine; Antidiarrheals, adsorbent; Antimyasthenics; Digoxin; Ketoconazole; Metoclopramide; Opioid (narcotic) analgesics; Haloperidol; Antacids, calcium - and / or magnesium - containing; Potassium chloride, especially wax-matrix preparations; Tricyclic antidepressants; Phenothiazines; Erythromycin; Levodopa; Hypotension - producing medications.

Side / Adverse effects

Signs of potentinal side effects, especially agranulocytosis, granulocytopenia, or leukopenia; allergic reaction; CNS depression; increased intraocular pressure; jaundice; and paradoxical reaction.

Administration and dosage

Usual adult dose:
Oral, 1 or 2 tablets 1 to 4 times a day, 30 to 60 minutes before meals or food, the dosage then being adjusted as needed and tolerated.
Usual adult prescribing limits:
Up to a total of 8 tablets daily (40 mg of chlordiazepoxide and 20 mg of clidinium bromide).
Usual pediatric dose:
Dosage has not been established.
Usual geriatric dose:
Oral, initially no more than 1 tablet 2 times a day, the dosage then being adjusted as needed and tolerated.

How supplied

Tablets: Box of 100 tablets. Each tablet contains 2.5 mg clidinium bromide and 5 mg chlordiazepoxide.

Storage

Store below 30° C, protect from light and moisture.

References

1 - USP DI Vol: 1 (1997) - pages: 215-223, 532-540,797-798.
2 - Drug facts and comparisons (1994).
3 - USP 23 pages: 340,387.

   
 

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