Avospas

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

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.

Nimesulide is a nonsteroidal anti-inflammatory drug (NSAID) with anti-inflammatory, anti-pyretic, and analgesic properties. It inhibits prostaglandin synthetase/cyclooxygenase, which limits prostaglandin production. Its cyclooxygenase inhibiting potency is intermediate, but is relatively selective for the cyclo-oxygenase-2 (COX-2) thus the potential for gastric injury and intolerance is less. It is also a free radical scavenger, and helps protect against the tissue damage that occurs during inflammation.

Food, gender and advanced age have negligible effects on nimesulide pharmacokinetics.

Trade Name Avospas
Generic Dicyclomine + Nimesulide
Type Tablet
Therapeutic Class
Manufacturer Shreeyam Healthcare
Available Country India
Last Updated: September 19, 2023 at 7:00 am
Avospas
Avospas

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

Nimesulide is used for acute pain; extra-articular disorders; osteoarthritis; post-op pain; primary dysmenorrhoea

Avospas is also used to associated treatment for these conditions: Functional bowel syndrome, Irritable Bowel Syndrome (IBS), Gastrointestinal cramps caused by GasMenstrual Distress (Dysmenorrhea), Pain, Pain, Acute, NSAIDs

How Avospas 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.

The therapeutic effects of Nimesulide are the result of its complete mode of action which targets a number of key mediators of the inflammatory process such as: COX-2 mediated prostaglandins, free radicals, proteolytic enzymes and histamine.

Dosage

Avospas 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.

100 mg twice daily.Should be taken with food. Take after meals.

Side Effects

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

Epigastric discomfort, heartburn or abdominal cramps, nausea, vomiting and diarrhoea; skin rash, pruritus, oedema, headache, dizziness, drowsiness; hypersensitivity reactions (e.g. bronchospasm, rhinitis, angioedema urticaria); GI haemorrhage/perforation; bullous/erosive stomatitis, purpura, thrombocytopenia, toxic epidermal necrolysis, haematuria, oliguria, and renal failure; increases in liver enzymes.

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 TDLO (human): 1.429 mg/kg; Oral TDLO (woman): 2 mg/kg; Oral LD50 (rat): 200 mg/kg; Oral LD50 (mouse): 392 mg/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.

History of GI tract disease, infections, oedema, hypertension, elderly, lactation.

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.

Additive hepatotoxic effects with known hepatotoxins: anti-convulsants (e.g. valproic acid), anti-fungals (e.g. ketoconazole), anti-tuberculous drugs (e.g. isoniazid), tacrine, pemoline, amiodarone, methotrexate, methyldopa, amoxicillin/clavulanic acid. May decrease the oral bioavailability of furosemide and the natriuretic and diuretic response to furosemide. Increased risks of GI and hepatic adverse effects with other NSAIDs, including aspirin. May increase anti-coagulant effect of warfarin. Potentiates the action of phenytoin. May be displaced from binding sites with fenofibrate, salicylic acid, and tolbutamide. Interactions between NSAIDs and lithium, probenecid and ciclosporin, have been documented.

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.

Rapidly absorbed following oral administration.

Half Life

The mean plasma elimination half life is approximately 1.8 hours.

1.8–4.7 hours

Clearance

Data regarding the clearance of dicyclomine is not readily available.

Elimination Route

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

Renal (50%), fecal (29%)

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.

Category not classified

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

Hypersensitivity; GI bleeding, active peptic ulcer disease; severe renal and heart failure; hepatic impairment or known liver disease; coagulation disorders; pregnancy; children <12 yr.

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.

Epigastric pain, nausea, vomiting, drowsiness, lethargy, GI haemorrhage, seizures, hypertension, apnoea, coma, anaphylactic reactions and renal failure. Treatment is supportive.

Storage Condition

Store below 30°C.

Protect from heat and humidity; store at <25°C.

Innovators Monograph

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