Openos
Openos Uses, Dosage, Side Effects, Food Interaction and all others data.
Levocetirizine Dihydrochloride is a preparation of Levocetirizine Dihydrochloride. Levocetirizine is the active (levo) isomer of Cetirizine. It is a new highly effective and well-tolerated non-sedating antihistamine with potent antiallergic properties. It has a two-fold higher affinity for H1-receptors than Cetirizine. Levocetirizine has a rapid and long-lasting action, allowing once-a-day administration.
Levocetirizine is a second generation histamine H1 antagonist used to treat various allergic symptoms. It has a long duration of action as it is generally taken once daily, and a wide therapeutic window as animal studies show the maximal nonlethal dose is over 100x a normal dose. Patients are cautioned to avoid tasks that require complete alertness, avoid alertness, and use caution in patients with factors predisposing urinary retention.
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 | Openos |
| Generic | Nimesulide + Levocetirizine |
| Weight | 100mg |
| Type | Tablet |
| Therapeutic Class | |
| Manufacturer | Panacea Biotec Ltd |
| Available Country | India |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Levocetirizine Dihydrochloride is used for the treatment of symptoms associated with allergic conditions such as seasonal allergic rhinitis, perennial allergic rhinitis and chronic idiopathic urticaria.
Nimesulide is used for acute pain; extra-articular disorders; osteoarthritis; post-op pain; primary dysmenorrhoea
Openos is also used to associated treatment for these conditions: Allergic Rhinitis (AR), Chronic Idiopathic Urticaria, Common Cold, Nasal Congestion, Perennial Allergic Rhinitis (PAR), Seasonal Allergic RhinitisMenstrual Distress (Dysmenorrhea), Pain, Pain, Acute, NSAIDs
How Openos works
Levocetirizine selectively inhibits histamine H1 receptors. This action prevents histamine from activating this receptor and causing effects like smooth muscle contraction, increased permeability of vascular endothelium, histidine uptake in basophils, stimulation of cough receptors, and stimulation of flare responses in the nervous system.
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
Openos dosage
Adults and children 12 years of age and older: 5 mg once daily in the evening
Children 6 to 11 years of age: 2.5 mg once daily in the evening
Children 6 months to 5 years of age: 1.25 mg (1/2 teaspoon oral solution) once daily in the evening
Renal Impairment: Adjust the dose in patients 12 years of age and older with decreased renal function
100 mg twice daily.Should be taken with food. Take after meals.
Side Effects
The most common adverse reactions (rate ≥2% and > placebo) were somnolence, nasopharyngitis, fatigue, dry mouth, and pharyngitis in subjects 12 years of age and older, and pyrexia, somnolence, cough, and epistaxis in children 6 to 12 years of age. In subjects 1 to 5 years of age, the most common adverse reactions (rate ≥2% and > placebo) were pyrexia, diarrhea, vomiting, and otitis media. In subjects 6 to 11 months of age, the most common adverse reactions (rate ≥3% and > placebo) were diarrhea and constipation.
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 drowsiness. Children may become agitated and restless before drowsiness. Patients should be treated with supportive measures. Dialysis will not assist in removing the drug from the body.
The maximal nonlethal dose in mice and rats is 240mg/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
Epileptic patients and patients at risk of convulsions. Renal impairment. Pregnancy and lactation.
History of GI tract disease, infections, oedema, hypertension, elderly, lactation.
Interaction
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 of levocetirizine is 0.33±0.02L/kg.
Elimination Route
Following a 5mg oral dose of levocetirizine, a Cmax of 0.27±0.04µg/mL with a Tmax of 0.75±0.50h. The AUC of levocetirizine is 2.31±0.50µg*h/mL. Taking levocetirizine with food does not affect the AUC but delays Tmax by 1.25 hours and lowers Cmax by 36%.
Rapidly absorbed following oral administration.
Half Life
The average half life of levocetirizine is 7.05±1.54 hours.
1.8–4.7 hours
Clearance
The average clearance of levocetirizine is 0.57±0.18mL/min/kg.
Elimination Route
168 hours post dose an average of 85.4% of a radiolabeled dose was recovered with an average of 80.8% in the urine and 9.5% in the feces. In the urine, 77% of the dose was recovered as unchanged drug, 0.5% as the M8 and M9 metabolites, 0.4% as the M10a metabolite, 0.4% as the M10b metabolite, 0.3% as the M3 metabolite, 0.3% as the M4 and M5 metabolite, 0.2% as the M2 metabolite, and 0.1% as the M1 metabolite. In the feces, 9.0% of the dose was recovered as unchanged drug, 1.0% as the M4 and M5 metabolite, and 0.1% as the M1 metabolite.
Renal (50%), fecal (29%)
Pregnancy & Breastfeeding use
Pregnancy: The safety of Levocetirizine in pregnancy has not been established. Therefore, it should be used with caution during pregnancy and only if the potential benefits to the mother outweigh any risks to the foetus.
Lactation: Levocetirizine passes into breast milk. So, it should be used with caution in nursing mothers and only if the expected benefit to the mother is greater than the risk to the nursing infant.
Category not classified
Contraindication
It is contraindicated in patients who are hypersensitive to this medication or to any of its ingredients.
Hypersensitivity; GI bleeding, active peptic ulcer disease; severe renal and heart failure; hepatic impairment or known liver disease; coagulation disorders; pregnancy; children <12 yr.
Special Warning
Paediatric use: Not recommended for use in children less than 6 years of age.
Acute Overdose
Symptoms: Drowsiness, agitation, restlessness, confusion, diarrhoea, dizziness, fatigue, headache, malaise, mydriasis, pruritus, sedation, somnolence, stupor, tachycardia, tremor and urinary retention.
Management: Symptomatic and supportive treatment. Gastric lavage must be considered shortly following ingestion.
Epigastric pain, nausea, vomiting, drowsiness, lethargy, GI haemorrhage, seizures, hypertension, apnoea, coma, anaphylactic reactions and renal failure. Treatment is supportive.
Storage Condition
Store between 20-25°C.
Protect from heat and humidity; store at <25°C.
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