Colispas Forte

Uses

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

Mefenamic acid is used in mild to moderate pain including headache, dental pain, postoperative and postpartum pain, dysmenorrhoea, menorrhagia, in musculoskeletal and joint disorders such as osteoarthritis and rheumatoid arthritis; and in children with fever and juvenile idiopathic arthritis.

Colispas Forte is also used to associated treatment for these conditions: Functional bowel syndrome, Irritable Bowel Syndrome (IBS), Gastrointestinal cramps caused by GasMild pain, Primary Dysmenorrhoea, Gastrointestinal cramps, Moderate Pain

How Colispas Forte works

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.

Mefenamic acid binds the prostaglandin synthetase receptors COX-1 and COX-2, inhibiting the action of prostaglandin synthetase. As these receptors have a role as a major mediator of inflammation and/or a role for prostanoid signaling in activity-dependent plasticity, the symptoms of pain are temporarily reduced.

Dosage

Colispas Forte 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.

As with other NSAIDs, the lowest dose should be sought for each patient. Therefore, after observing the response to initial therapy with Mefenamic acid, the dose and frequency should be adjusted to suit an individual patient's needs.Administration is by the oral route, preferably with food.

• Adult: A 500 mg dose should be given to adults up to three times (1.5 g total) per day.
• Infants over 6 months: 25 mg/kg of body weight daily in divided doses for not longer than 7 days.

Side Effects

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

In patients taking Mefenamic acid or other NSAIDs, the most frequently reported adverse experiences include : abdominal pain, constipation, diarrhoea, dyspepsia, flatulence, gross bleeding/perforation, heartburn, nausea, GI ulcers, vomiting, abnormal renal function, anaemia, dizziness, oedema, elevated liver enzymes, headache, increased bleeding time, pruritus, rash and tinnitus.

Toxicity

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.

Oral, rat LD₅₀: 740 mg/kg. Symptoms of overdose may include severe stomach pain, coffee ground-like vomit, dark stool, ringing in the ears, change in amount of urine, unusually fast or slow heartbeat, muscle weakness, slow or shallow breathing, confusion, severe headache or loss of consciousness.

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.

NSAIDs should be prescribed with extreme caution in those with a prior history of ulcer disease or gastrointestinal bleeding. To minimise the potential risk for an adverse GI event, the lowest effective dose should be used for the shortest possible duration. In cases with pre-existing advanced kidney disease, treatment with Mefenamic acid is not recommended.

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.

Concomitant use with CYP2C9 isoenzyme inhibitors may alter safety and efficacy of mefenamic acid. May enhance methotrexate toxicity. Reduced BP response to ACE inhibitors or angiotensin II receptor antagonists. Increased risk of serious GI events with aspirin. May reduce the natriuretic effects of furosemide or thiazide diuretics. Reduced renal lithium clearance and elevated plasma lithium levels. May enhance anticoagulant effect of warfarin.

Volume of Distribution

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

• 1.06 L/kg [Normal Healthy Adults (18-45 yr)]

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 T_max of 1-1.5h.

Mefenamic acid is rapidly absorbed after oral administration.

Half Life

The mean plasma elimination half life is approximately 1.8 hours.

2 hours

Clearance

Data regarding the clearance of dicyclomine is not readily available.

• Oral cl=21.23 L/hr [Healthy adults (18-45 yrs)]

Elimination Route

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

The fecal route of elimination accounts for up to 20% of the dose, mainly in the form of unconjugated 3-carboxymefenamic acid.3 The elimination half-life of mefenamic acid is approximately two hours. Mefenamic acid, its metabolites and conjugates are primarily excreted by the kidneys. Both renal and hepatic excretion are significant pathways of elimination.

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.

Pregnancy: In late pregnancy, as with other NSAIDs, Mefenamic acid should be avoided because it may cause premature closure of the ductus arteriosus. In general there are no adequate and well controlled studies in pregnant women. Mefenamic acid should be used during pregnancy only if the potential benefit justifies the potential risk to the foetus. Rated as Pregnancy Category C.

Lactation: Trace amounts of Mefenamic acid may be present in breast milk. Taking into account the importance of the drug to the mother , decision should be made whether to discontinue nursing or to discontinue the drug.

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

Mefenamic acid is contraindicated in patients with known hypersensitivity to Me Mefenamic acid acid. Mefenamic acid should not be given to patients who have experienced asthma, urticaria, or allergic type reactions after taking aspirin or other NSAIDs. Rarely fatal, anaphylactic like reactions to NSAIDs have been reported in such patients. Mefenamic acid is contraindicated in patients with active ulceration or chronic inflammation of upper gastrointestinal tract and should not be used in patients with preexisting renal disease.

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.

Symptoms: Headache, nausea, vomiting, epigastric pain, GI bleeding. Rarely, diarrhoea, disorientation, excitation, coma, drowsiness, tinnitus, fainting, and occasionally convulsions.

Management: Symptomatic and supportive treatment. In acute overdosage, empty the stomach immediately by inducing emesis or by gastric lavage followed by admin of activated charcoal.

Storage Condition

Store below 30°C.

Store between 20-25° C.

Innovators Monograph

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