Zaltoprofen

Zaltoprofen is a Analgesic and Antipyretic belonging to Non-Steroidal anti-inflammatory Drug

Zaltoprofen is used in the treatment of Osteoarthritis, rheumatoid arthritis, ankylosing spondylitis.

After oral administration, Zaltoprofen is well absorbed (82%) in the GIT. About 98% of the administered drug is bound to plasma proteins. After oral administration, 62% of the dose is excreted as conjugate in the urine and only 3% is excreted as unchanged compound by this route. No systemic accumulation has been reported. Zaltoprofen has biological half-life of 2.8 hr. The Zaltoprofen is predominantly metabolized by CYP2C9 and UGT2B7 in liver. Zaltoprofen is also biotransformed to S-oxide Zaltoprofen (M-2), 10-hydroxy Zaltoprofen (M-3) and S-oxide-10-hydroxy-Zaltoprofen (M-5) in humans, and conjugate of M-2 and M-3 are excreted in urine, although urinary level of each of these metabolites account for less than 10% of the dose.

Zaltoprofen shows common side effects like vomiting, indigestion, flatulence, nausea, abdominal pain, constipation, epigastric pain, diarrhoea, large intestine carcinoma

Zaltoprofen is available in tablets

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

Zaltoprofen is a non-steroidal anti-inflammatory drug (NSAID). It works by blocking the release of certain chemical messengers that cause fever, pain and inflammation (redness and swelling). It works by stopping Prostaglandin E2 selectively that plays an important role in mediating the pain pathway.

Zaltoprofen is available in the form of tablets.

Zaltoprofen is used in the treatment of fever, osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, gout and Pain relief.

Zaltoprofen, a preferential COX-2 inhibitor, selectively inhibits Prostaglandin E2 which enhances the pain pathway. It also stops bradykinin induced pain without adversely affecting the bradykinin receptors.

Zaltoprofen is approved for use in the following clinical indications

fever, osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, gout and Pain relief.

Zaltoprofen is available in the dosage strength of 80 mg.

Zaltoprofen is available in the form of tablets.

Take after eating and with a full glass of water to decrease gastric upset.

• General warnings

Heart diseases

This medicine should be used with caution in patients with heart diseases due to the increased risk of severe adverse effects on the heart. This risk is especially higher if the medicine is used for a prolonged period of time. Appropriate dose adjustments or replacement with a suitable alternative may be required based on the clinical condition of the patient.

Gastro-intestinal bleeding

This medicine may cause severe gastrointestinal bleeding and perforation after a prolonged usage. These adverse events may occur with or without warning symptoms. This risk is especially higher in the elderly population and in patients with a history of gastrointestinal diseases. Appropriate dose adjustments or replacement with a suitable alternative may be required based on the clinical condition of the patient.

Liver diseases

This medicine should be used with caution in patients with mild-to-moderate liver diseases due to the increased risk of severe side effects. Appropriate dose adjustments may be necessary for some patients. If the liver function impairment is severe, use of this medicine is not recommended.

Kidney diseases

This medicine should be used with caution in patients with mild-to-moderate kidney diseases due to the increased risk of severe side effects. Appropriate dose adjustments may be necessary for some patients. If the kidney function impairment is severe, use of this medicine is not recommended.

Other medicines

This medicine may interact with many other medicines and may cause severe adverse effects. Hence, it is recommended that you report all your current medicines, including any herbs and supplements, to the doctor before beginning therapy with this medicine.

Zaltoprofen may cause liver problems, and using it with substantial quantities of ethanol may increase that risk.

Food may decrease the rate but not the extent of absorption. Zaltoprofen peak serum levels may be delayed if taken with food. Management: Administer with food or milk to minimize GI upset.

Common Adverse effects: Vomiting, indigestion, Flatulence, Nausea, Abdominal pain, Constipation, Epigastric pain

Less Common Adverse effects: Pain/tenderness in the pit of stomach, Abdominal pain, Diarrhea accompanies.

Rare Adverse Effects: Sore throat, Fever, Bleeding tendency.

• Quinolone antibacterial- Concomitant use of antibacterial with Zaltoprofen may trigger convulsion. The dose may have to be adjusted in such cases.
• Coumarin anticoagulant agent- dose may have to be adjusted as there may be intensification in the anticoagulant action.
• Sulfonylurea antidiabetic agents- The dose may have to be adjusted as there may be an intensification in the hypoglycemic action.
• Lithium- The dose of lithium may have to be adjusted as there may be intensification in the lithium action.
• Methotrexate- Since there is a report that it will enhance the action of methotrexate, care should be taken to adjust the dose of methotrexate.

The common side effects of Zaltoprofen include the following :

Vomiting, Indigestion, Flatulence, Nausea, Abdominal pain, Constipation, Epigastric pain, Diarrhea, Large intestine carcinoma.

• Pharmacodynamics

Zaltoprofen is (±)-2-(10,11-dihydro-10-oxodibenzo [b, f] thiepin-2-yl) propionic acid, belongs to the therapeutic class of nonsteroidal antiinflammatory drugs (NSAIDs) that exhibits anti-inflammatory, analgesic and antipyretic activities. Zaltoprofen is a COX-2 preferential inhibitor. The main mechanism of Zaltoprofen is prostaglandin biosynthesis inhibitory action due to the COX inhibition in the arachidonic acid metabolism system. Besides this, membrane stabilizing action such as leukocyte migration inhibitory action and lysosomal enzyme inhibitory action are also observed with Zaltoprofen. Experimental studies have shown that Prostaglandin biosynthesis inhibitory action in the stomach tissue is weaker with Zaltoprofen than in case of indomethacin. Zaltoprofen possesses novel anti-nociceptive mechanism by inhibiting B2-type bradykinin (BK) receptor function in nerve endings and selectively inhibiting PGE2 production at inflammatory sites and exhibits a powerful anti-inflammatory effect with a good safety margin and stronger inhibitory effect on BK-nociception than other NSAIDs

• Pharmacokinetics

Absorption: After oral administration, Zaltoprofen is well absorbed (82%) in the GIT.

Distribution: About 98% of the administered drug is bound to plasma proteins.

Metabolism: The Zaltoprofen is predominantly metabolized by CYP2C9 and UGT2B7 in liver.

Elimination: After oral administration, 62% of the dose is excreted as conjugate in the urine and only 3% is excreted as unchanged compound by this route. No systemic accumulation has been reported. Zaltoprofen is also biotransformed to S-oxide Zaltoprofen (M-2), 10-hydroxy Zaltoprofen (M-3) and S-oxide-10-hydroxy-Zaltoprofen (M-5) in humans, and conjugate of M-2 and M-3 are excreted in urine, although urinary level of each of these metabolites account for less than 10% of the dose.

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