Sodium Oxybate 500mg/ml oral solution

 

Category: Non-steroidal anti-inflammatory drugs.

Composition:

Each hard gelatin capsule contains:

Celecoxib BP.......200mg

Excipients...q.s.

Approved colors used in capsule shell.

Indications:

It is indicated in pain and inflammation in Osteoarthritis, rheumatoid arthritis and ankylosing spondylitis.

Pharmacology:

Pharmacodynamics

Cyclooxygenase is responsible for generation of prostaglandins. Two isoforms, COX-1 and COX-2 have been identified. COX-2 is the isoform of the enzyme that has been shown to be induced by pro-inflammatory stimuli and has been postulated to be primarily responsible of the synthesis of proteinoid mediators of pain, inflammation, and fever. COX-2 is also involved in ovulation, implantation and closure of the ductus arteriosus, regulation of renal function, and central nervous system functions (fever induction, pain perception and cognitive function), It may also play a role in ulcer healing. COX-2 has been identified in tissue around gastric ulcers in man but its relevance to ulcer healing has not been established.

The difference in antiplatelet activity between some COX-1 inhibiting NSAIDs and COX-2 selective inhibitors may be of clinical significance in patients at risk of thrombo-embolic reactions. COX-2 selective inhibitors reduce the formation of systemic (and therefore possibly endothelial) prostacyclin without affecting platelet thromboxane. Celecoxib is a diary-substituted pyrazole, chemically similar to other non-arylamine sulfonamides (e.g. thiazides, furosemide) but differs from aryl amine sulfonamides (e.g. sulfamethoxazole and other sulfonamide antibiotics).

Pharmacokinetics

Absorption: Celecoxib is well absorbed reaching peak plasma concentrations after approximately 2-3 hours. Dosing with food (high fat meal) delays absorption by about 1 hour.

Distribution: Plasma protein binding is about 97 % at therapeutic plasma concentrations and the drug is not preferentially bound to erythrocytes.

Metabolism: Celecoxib metabolism is primarily mediated via cytochrome P450 2C9. Three metabolites, inactive as COX-1 or COX-2 inhibitors, have been identified in human plasma. a primary alcohol, the corresponding carboxylic acid and its glucuronide conjugate.

Elimination: Celecoxib is mainly eliminated by metabolism. Less than 1 % of the dose is excreted unchanged in urine. The inter-subject variability in the exposure of celecoxib is about10-fold. Celecoxib exhibits dose- and time-independent pharmacokinetics in the therapeutic dose range. Elimination half-life is 8-12 hours. Steady state plasma concentrations are reached within5 days of treatment.

Dosage

Osteoarthritis: 200ng daily in 1-2 divided doses, increased if necessary to maximum 200ng twice daily.

Rheumatoid arthritis: 10Omg twice daily, increased if necessary to 200mg twice daily.

Ankylosing spondylitis: 200mg daily in 1-2 divided doses increased if necessary to max.

400mg daily in 1-2 divided doses. It is not recommended for children.

Contraindications

It is contraindicated in patients with hypersensitivity to aspirin or any other NSAID which includes those in whom attacks of asthma, angioedema, urticaria or rhinitis and in coagulation defects. It is also contraindicated in sulphonamide sensitivity, inflammatory bowel disease.

Side effects

It includes Gastro disturbances including discomfort nausea, diarrhea and occasionally Secang laceration, dyspnea, influenzas like symptoms, less commonly stomatitis palpitation, cerebral infraction, fatigue, paresthesia, muscle cramps, rarely taste disturbance alopecia, very rarely seizures, also reported chest pain.

Precautions and Warnings

It should be used in caution in the elderly, in allergic disorders and in cardiac impairment. Blood pressure should be monitored before and after treatment.

Pregnancy and Lactation

It should be avoided during Pregnancy and lactation.

Drug interactions: It may interact with this drug include aliskiren, ACE inhibitors (such as captopril, lisinopril), angiotensin Il receptor blockers (such as valsartan, losartan), cidofovir, lithium, diuretics such as furosemide. This medication may increase the risk of bleeding when taken with other drugs that also may cause bleeding.

Over dosage: Symptoms following acute NSAID overdoses are usually limited to lethargy, drowsiness, nausea, vomiting, and epigastric pain, which are generally reversible with supportive care. Gastrointestinal bleeding can occur. Hypertension, acute renal failure, respiratory depression and coma may occur but are rare. Anaphylactoid reactions have been reported with therapeutic ingestion of NSAIDs and may occur following an overdose. Patients should be managed by symptomatic and supportive care following an NSAID overdose. There are no specific antidotes.

Storage

Store in cool & dry place, below 30°C. Keep out of reach of children.

Presentation

Pack size 3 x 10 capsules Alu-Alu pack.

FDA Reg No.: FDA/GD.213-12229

Imported by

ERNEST CHEMISTS LIMITED

PO.Box 3345 Acora, Ghana.

Manufactured by:

SWISS PHARMA PVT. LTD.

3709, G.I.D.C. Phase IV, Vatva,

Ahmedabad-382445, Gujarat, India.

Eoded by/ exporté par:

LAVIRA PHARMACEUTICALS PVT. LTD.

o No402, 4th Floor, Satra Plaza,

PHorNo19-20, Sector-19D ,Vasa Mavi Mumbai 400703, INDIA