Sunday, January 24, 2016

Nimesulide drug interactions


Nimesulide is a recently developed analgesic, antipyretic and anti-inflammatory agent that differs from conventional nonsteroidal anti-inflammatory drugs both in structure and pharmacological profile.
 Since nimesulide may be prescribed for patients receiving concomitant medication, the propensity for drug interactions exists.
Major interactions involving interference with drug metabolism have not been described with Nimesulide.
A marginal decrease in plasma theophylline levels (without changes in respiratory function tests) has been described after addition of Nimesulide to chronic theophylline therapy.
 Nimesulide is available in the market with the dosage of 100mg.

Nimesulide solubility

Nimesulide NSAID’s tablet is an efficient and safe therapeutic selection for the treatment of assorted painful inflammatory conditions like inflammation, sore throat, stomatitis, arthritis, degenerative joint disease, low back pain etc., with a speedy onset of analgesic activity.

The quick dissolving tablets of Nimesulide contains superdisintegrants, that accelerates the disintegration of tablets by virtue of their ability to soak up great deal of water once exposed to binary compound surroundings.

Nimesulide is soluble in organic solvents like alcohol, DMSO, and dimethyl formamide  (DMF).

Nimesulide is a unique non- steroidal anti-inflammatory drug that acts specifically on cyclo-oxygenase-2 and does not affect cyclo-oxygenase-1. Hence, it exerts its anti-inflammatory action characteristics of non- steroidal anti-inflammatory drug. 

Solubility of Nimesulide Increased on solubilization of drug in semi-polar solvents and non-ionic surfactants.
Solubility of Nimesulide was studied using different cosolvent mixtures and various classes of non-ionic surfactant. Solubility increased drastically (>70 mg/rnl) when polyethylene glycol 300 and polyethylene glycol 400 were used as solvents.

Sunday, January 17, 2016

Nimesulide synthesis


Nimesulide is a non-steroidal anti-inflammatory agent that is generally utilized as a part of the treatment of inflammatory torment which hinders the protein cyclooxygenase-2 (COX-2) and has better gastro-intestinal mediocrity in addition to different NSAIDs in its class.
Its approved signs are the treatment of intense torment, the symptomatic treatment of osteoarthritis and essential dysmenorrhoea, sports wounds and so on.
A variety of new Nimesulide derivatives were synthesized through incorporation of a 5-LOX pharmacophore into nimesulide followed with some structural modifications, which were then characterized for dual enzyme inhibitors for these two types of enzymes (Cyclooxygenase-½ (COX-½) and 5-lipoxygenase (5-LOX) ). Their structure-activity relationships (SARs) were studied, and compound 20f was found to be an excellent dual enzyme inhibitor.
Its binding conformation and interaction mode were studied with molecular docking experiments. Compound 20f could become a lead compound for further development for potential anti-inflammatory drugs.
Clinically it has demonstrated that it supports an especially good profile as far as gastrointestinal tolerability.



Thursday, January 7, 2016

Nimesulide efficacy


The abilities of NSAID’s drug nimesulide to inhibit COX-2 preferentially and to exert other novel anti-inflammatory actions are consistent with good efficacy and safety and is consistently superior to placebo.
The quick dissolving tablets of Nimesulide contains superdisintegrants, that accelerates the disintegration of tablets by virtue of their ability to soak up great deal of water once exposed to binary compound surroundings.
Nimesulide must be prescribed by a licensed physician as second line treatment in the approved indications and in compliance with the recommendations
Daily dose is 100mg twice-a-day. As for other NSAIDs the use of nimesulide is recommended for the shortest duration necessary to control symptoms in patients with acute pain or primary dysmenorrhoea.

Nimesulide gel


Nimesulide transdermal gel is a well tolerated novel hydroalcoholic microcarrier based drug delivery system with penetration enhancer. This is cause of superior efficacy of Nimesulide Transdermal Gel.
Nimesulide gel is indicated for a variety of conditions characterized by pain, inflammation and stiffness, such as osteoarthritis, periarthritis, post-traumatic or acute musculoskeletal disorders including tendinitis, tenosynovitis, sprains, strains and low back pain. It Functions by inhibiting particular nerve impulses sent from the periphery to your central system.
Nimesulide is a non-steroidal anti-inflammatory (NSAID) agent which also possess analgesic properties. The product has been formulated using a novel combination of solvents for solubilization of Nimesulide.
Nimesulide exhibited better efficacy it also demonstrated faster onset of action. Significant concentration of Nimesulide could be detected in the blood within 30 minutes of treatment and persisted for 8 hours post treatmen

Nimesulide tablet dose

Nimesulide is indicated for the treatment of acute pain, Painful osteoarthritis (Swelling in the joints) and primary dysmenorrhoea.

It is considered as the most prescribed tablet for variety of painful inflammatory conditions including those associated with osteoarthritis, postoperative trauma, sports injuries.
Dose: 

The usual dose is 100mg twice a day. 
Children: 5mg/kg of body weight in 2 or 3 divided doses. 

The maximum duration of a treatment course is 15 days and, as for other NSAIDs, treatment should be as short as possible maximum of 15 days. Nimesulide also improves the skin tone and to increase in energy level.

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

NImesulide tablets is also available in the form of Gel which is needed to apply to the affected area, rubbing in a thin layer of the gel 2 to 4 times every day.

Tuesday, January 5, 2016

Nimesulide composition


Nimesulide is a Non steroidal anti inflammatory drug (NSAID) and targets COX-2 an enzyme responsible for inflammation & pain.
The nimesulide is preferably used in the composition in an amount of 0.1-5% by weight, more preferably in an amount of 0.1-3% by weight, most preferably in an amount of around 1 % by weight of the composition.
This medication is for the most part used as an issue of the treatment of inflammatory torment and also used for postoperative trauma, sports injuries, acute musculoskeletal disorders.
Nimesulide have pain relieving and antipyretic properties which, specially restrains the protein cyclooxygenase-2 (COX-2) and has better gastro-intestinal bearableness in addition to different Nsaids in its class.

Nimesulide combination


The generic Nimesulide combination is manufactured by 399 companies and has nearly 522 Brands of Generics of Nimesulide.

Nimesulide is a Non steroidal anti inflammatory drug (NSAID) and targets COX-2 an enzyme responsible for inflammation & pain.

The Nimesulide is preferably used in the composition in an amount of 0.1-5% by weight, more preferably in an amount of 0.1-3% by weight, most preferably in an amount of around 1 % by weight of the composition.

Some of brands of Nimesulide are:
  • Nepar - Nimuselide 100 mg + Paracetamol 500 mg
  • Nimular Plus - Nimesulide, Acetaminophen
  • Nipar (100 mg) - Nimesulide, Paracetamol
  • Abinim-P - Nimesulide 100 mg, paracetamol 500 mg.
Nimesulide is distributed world-wide through a network of selected international partners. 

Nimesulide is mainly used for the treatment of:
  • Back Pain 
  • Dysmenorrhea
  • Osteoarthritis
  • Rheumatoid Arthritis
Nimesulide is always recommended to use under a licensed physician supervision