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Chemical
nameClidinium Bromide: (±)
- 3 - Hydroxy - 1 - methylquinuclidinium bromide
benzilate. Chlordiazepoxide: 3H - 1, 4 - Benzodiazepin - 2 - amine, 7 -
chloro - N - methyl - 5 - phenyl -, 4 - oxide.
CategoryAnticholinergic - 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 -
feedingChlordiazepoxide
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
suppliedTablets: Box of 100
tablets. Each tablet contains 2.5 mg clidinium bromide and 5 mg
chlordiazepoxide.
StorageStore below 30° C, protect from light and
moisture.
References1 - 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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