Morniflumate

Morniflumate is Non- Steroidal Anti inflammatory Drugs belonging to anti-inflammatory agents.

Morniflumate is used for the treatment of inflammatory conditions affecting the airways, ENT system, urogenital tract and bone and joint systems.

Bioavailability and pharmacokinetics studies after oral and intravenous (IV) administration demonstrate that morniflumate is absorbed as from the gastrointestinal tract, followed by rapid hydrolysis in the plasma, releasing the free acidic form, the molecule responsible for its anti-inflammatory effects. The ester displays gastroprotective effect against the ulcerogenic effects of niflumic acid.

The onset of action for Morniflumate for Oral was 0.5 hours

The Tmax of Morniflumate was within 2 hours and Cmax of Morniflumate was found within 1200 mg to 3200 mg

Morniflumate shows common side effects like Oedema, HTN, cardiac failure, nausea, epigastric pain, diarrhea, indigestion, heartburn, flatulence, abdominal pain, constipation, vomiting, ulcerative stomatitis, dyspepsia, hematemesis, melaena, rectal bleeding, exacerbation of colitis, vasculitis, headaches

Morniflumate is available in Oral, tablet, sachet, suspension.

Morniflumate is available in India, Germany, Canada, France, USA

Morniflumate, given at therapeutic dosages to healthy human volunteers, on leukotriene B4 (LTB4) and thromboxane (TXB2) synthesis, both in purified PMNs (polymorphnuclear neutrophils) and in whole blood.

In whole blood experiments, morniflumate reduced blood leukotriene B4 (LTB4) synthesis induced by Ca-ionophore A23187 Bx approximately 50%, both after a single dose and at steady state; the level of inhibition showed a pattern similar to the plasma levels of the bioactive metabolite of morniflumate (M1). The inhibition of serum thromboxane B2 (TXB2) levels was higher than 85%. Hence, morniflumate is demonstrated to reduce arachidonic acid metabolism, by exerting its effects on cyclooxygenase and 5-lipoxygenase. This characteristic might provide a better approach for anti-inflammatory therapy.

In several animal models orally administered morniflumate, the beta-morpholinoethyl ester of niflumic acid, proved almost equal to the parent compound in anti-inflammatory, analgesic and antipyretic activity with the absence of gastric irritating/ulcerogenic effects of its acidic parent compound.

Morniflumate is available in the form of Oral, tablet, sachet, suspension.

Morniflumate is used for the treatment of inflammatory conditions affecting the airways, ENT system, urogenital tract and bone and joint systems.

Morniflumate, given at therapeutic dosages to healthy human volunteers, on leukotriene B4 (LTB4) and thromboxane (TXB2) synthesis, both in purified PMNs (polymorphnuclear neutrophils) and in whole blood .

Morniflumate is approved for use in the following clinical indications

Inflammatory conditions affecting the airways, ENT system, urogenital tract and bone and joint systems.

Morniflumate is available in the dosage strength of 200 mg, 400 mg & 350 mg.

Morniflumate is available in the form of Oral, tablet, sachet, suspension.

• Dosage Adjustment for Pediatric Patients:-

Oral route

The recommended daily dose of morniflumate in pediatric patients is 17.5 milligrams/kilogram on a body weight basis.

• In children 8 to 14 years of age (25 to 45 kilograms of body weight), the recommended dosage of morniflumate is 350 milligrams twice daily.
• In children 4 to 8 years of age (15 to 25 kilograms of body weight), the recommended dosage of morniflumate is 175 milligrams twice daily .
• In children up to 4 years of age (10 to 15 kilograms of body weight), the recommended dosage of morniflumate is 175 milligrams once daily .

Rectal route

In children over 12 months of age, the recommended dose of rectal morniflumate is 285 milligrams (mg) once, twice or three times daily as needed (one 285 mg suppository per 10 kilograms of body weight); in children 6 to 12 months of age, the recommended dose of rectal morniflumate is 285 mg daily .

Morniflumate is contraindicated in patients with:

Hypersensitivity (eg, anaphylactic reaction) to Morniflumate or any component of the formulation.

Common Adverse effects:

• Oedema, HTN, cardiac failure, nausea, epigastric pain, diarrhea, indigestion, heartburn, flatulence, abdominal pain, constipation, vomiting, ulcerative stomatitis, dyspepsia, hematemesis, melaena, rectal bleeding, exacerbation of colitis, vasculitis, headaches

Less Common Adverse effects:

• Dizziness, abnormal vision, pyrexia, drowsiness, tinnitus, rash, pruritus, fatigue, depression, insomnia, confusion, paresthesia, tremor, weakness, dyspnea

Rare Adverse effects

• Hepatic function abnormalities, jaundice, urinary frequency, Crohn's disease, photosensitivity, asthma, nephritis, anaemia.

The common side effects of Morniflumate include the following :

• Oedema, HTN, cardiac failure, nausea, epigastric pain, diarrhoea, indigestion, heartburn, flatulence, abdominal pain, constipation, vomiting, ulcerative stomatitis, dyspepsia, haematemesis, melaena, rectal bleeding, exacerbation of colitis, vasculitis, headaches

• Pharmacodynamic

Morniflumate, given at therapeutic dosages to healthy human volunteers, on leukotriene B4 (LTB4) and thromboxane (TXB2) synthesis, both in purified PMNs (polymorphnuclear neutrophils) and in whole blood .

In whole blood experiments, morniflumate reduced blood leukotriene B4 (LTB4) synthesis induced by Ca-ionophore A23187 Bx approximately 50%, both after a single dose and at steady state; the level of inhibition showed a pattern similar to the plasma levels of the bioactive metabolite of morniflumate (M1). The inhibition of serum thromboxane B2 (TXB2) levels was higher than 85%. Hence, morniflumate is demonstrated to reduce arachidonic acid metabolism, by exerting its effects on cyclooxygenase and 5-lipoxygenase. This characteristic might provide a better approach for anti-inflammatory therapy

• Pharmacokinetics

Metabolism:

The pharmacokinetic availability of niflumic acid in two different pharmaceutical preparations have been studied in 12 subjects after oral administration .

Bioavailability and pharmacokinetics studies after oral and intravenous (IV) administration demonstrate that morniflumate is absorbed as from the gastrointestinal tract, followed by rapid hydrolysis in the plasma, releasing the free acidic form, the molecule responsible for its anti-inflammatory effects. The ester displays gastroprotective effect against the ulcerogenic effects of niflumic acid.

1. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC1364710/
2. https://reference.medscape.com/drug/colestid-Morniflumate -342452
3. https://go.drugbank.com/drugs/DB00375
4. https://www.sciencedirect.com/topics/medicine-and-dentistry/Morniflumate
5. https://europepmc.org/article/med/6988203