Chlorspas

Chlorspas Uses, Dosage, Side Effects, Food Interaction and all others data.

An anxiolytic benzodiazepine derivative with anticonvulsant, sedative, and amnesic properties. It has also been used in the symptomatic treatment of alcohol withdrawal.

Chlordiazepoxide has antianxiety, sedative, appetite-stimulating and weak analgesic actions. The drug seems to block EEG arousal from stimulation in the brain stem reticular formation. The drug has been studied extensively in many species of animals and these studies are suggestive of action on the limbic system of the brain, which recent evidence indicates is involved in emotional responses. Hostile monkeys were made tame by oral drug doses which did not cause sedation. Chlordiazepoxide revealed a "taming" action with the elimination of fear and aggression. The taming effect of chlordiazepoxide was further demonstrated in rats made vicious by lesions in the septal area of the brain. The drug dosage which effectively blocked the vicious reaction was well below the dose which caused sedation in these animals.

Dicycloverine HCl relieves smooth muscle spasm in the GI and urinary tract. This effect is partly due to antimuscarinic action and partly direct action on the smooth muscle.

Dicyclomine is an anticholinergic drug used to relax the smooth muscles of the intestines. It's duration of action is not especially long as it is usually taken 4 times daily with individual doses of 20-40mg orally or 10-20mg by intramuscular injection. Dicyclomine should not be administered intravenously.

Trade Name Chlorspas
Generic Chlordiazepoxide + Clidinium Bromide + Dicyclomine
Type Tablet
Therapeutic Class
Manufacturer Rkg Pharma Pvt Ltd
Available Country India
Last Updated: September 19, 2023 at 7:00 am
Chlorspas
Chlorspas

Uses

Chlordiazepoxide is a benzodiazepine used to treat the withdrawal symptoms of acute alcoholism, to treat preoperative anxiety, and to treat anxiety over a short term period.

For the management of anxiety disorders or for the short-term relief of symptoms of anxiety, withdrawal symptoms of acute alcoholism, and preoperative apprehension and anxiety.

Dicycloverine is used for:

  • Functional bowel/ irritable bowel syndrome
  • Urinary incontinence secondary to unstable detrusor muscle
  • Infantile colic
  • GIT spasm
  • Colicky abdominal pain
  • Diverticulitis
  • Abdominal colic

Chlorspas is also used to associated treatment for these conditions: Alcohol Withdrawal Syndrome, Anxiety, Anxiety Disorders, Depression, Peptic Ulcer Disease, Acute Anxiety, Pyschosomatic diseaseFunctional bowel syndrome, Irritable Bowel Syndrome (IBS), Gastrointestinal cramps caused by Gas

How Chlorspas works

Chlordiazepoxide binds to stereospecific benzodiazepine (BZD) binding sites on GABA (A) receptor complexes at several sites within the central nervous system, including the limbic system and reticular formation. This results in an increased binding of the inhibitory neurotransmitter GABA to the GABA(A) receptor. BZDs, therefore, enhance GABA-mediated chloride influx through GABA receptor channels, causing membrane hyperpolarization. The net neuro-inhibitory effects result in the observed sedative, hypnotic, anxiolytic, and muscle relaxant properties.

Dicyclomine achieves its action partially through direct antimuscarinic activity of the M1, M3, and M2 receptors; and partially through antagonism of bradykinin and histamine. Dicyclomine non-competitively inhibits the action of bradykinin and histamine, resulting in direct action on the smooth muscle, and decreased strength of contractions seen in spasms of the ileum.

Dosage

Chlorspas dosage

Oral dosage forms-

  • Adults:10 to 20 mg three times a day.
  • Children >6 months of age: 5 to 10 mg three times a day.
  • Children <6 months of age: Dose must be determined by the doctor.

Oral dicycloverine Hydrochloride should be started as soon as possible

Intramuscular dosage form

  • Adults:Intramuscular injection. Not for intravenous use. The recommended intramuscular dose is 80 mg daily (in 4 equally divided doses).

Intramuscular dosage form should not be used for periods longer than 1 or 2 days.

Side Effects

Insomnia, mydriasis, cycloplegia, increased ocular tension, urinary hesitancy, palpitations, dyspnea.

Toxicity

LD50=537 mg/kg (Orally in rats). Signs of overdose include respiratory depression, muscle weakness, somnolence (general depressed activity).

Patients experiencing an overdose may present with headache, nausea, vomiting, blurred vision, dilated pupils, dizziness, dry mouth, difficulty swallowing, CNS stimulation, as well as hot, dry skin. Treat patients with gastric lavage, emetics, activated charcoal, sedatives for excitement, and a cholinergic agent if indicated.

The oral LD50 in mice is 625mg/kg.

Precaution

Use with caution in patients with autonomic neuropathy, hepatic or renal disease, ulcerative colitis, coronary heart disease, congestive heart failure, cardiac tachyarrhythmia, known or suspected prostatic hypertrophy.

Interaction

The following agents may increase certain actions or side-effects of Dicycloverine-antiarrhythmic agents, antihistamines, antipsychotic agents, benzodiazepines, MAO inhibitors, narcotic analgesics, nitrates and nitrites, sympathomimetic agents, tricyclic antidepressants and other drugs having anticholinergic activity.

Volume of Distribution

The volume of distribution for a 20mg oral dose is 3.65L/kg.

Elimination Route

The bioavailability of dicyclomine has not been determined, though it is likely well absorbed as the primary route of elimination is in the urine. Dicyclomine has a Tmax of 1-1.5h.

Half Life

24-48 hours

The mean plasma elimination half life is approximately 1.8 hours.

Clearance

Data regarding the clearance of dicyclomine is not readily available.

Elimination Route

Chlordiazepoxide is excreted in the urine, with 1% to 2% unchanged and 3% to 6% as conjugate.

Dicyclomine is 79.5% eliminated in the urine and 8.4% in the feces.

Pregnancy & Breastfeeding use

Pregnancy: Category B. Dicycloverine was neither teratogenic nor embryocidal in animal trial. It, like other drugs should be used during pregnancy only if clearly needed. There are no data on the secretion of this drug into breast milk. Dicycloverine should be used cautiously in case of lactating mother.

Contraindication

Dicycloverine is contraindicated in:

  • Obstructive uropathy
  • Obstructive disease of the gastrointestinal tract
  • Severe ulcerative colitis
  • Reflux esophagitis
  • Unstable cardiovascular status in acute hemorrhage
  • Glaucoma
  • Myasthenia gravis
  • Evidence of prior hypersensitivity to dicycloverine hydrochloride or other ingredients of this formulation
  • Infants less than 6 months of age

Acute Overdose

Toxic reaction seldom occurs with dicycloverine. The signs and symptoms of overdosage are headache; nausea; vomiting; blurred vision; dilated pupils; hot, dry skin; dizziness; dryness of the mouth; difficulty in swallowing; and CNS stimulation.

Storage Condition

Store below 30°C.

Innovators Monograph

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*** Taking medicines without doctor's advice can cause long-term problems.
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