Actions of Locet in details
Pharmacology: Locet is a nonsteroidal agent with marked anti-inflammatory and analgesic properties. It has higher anti-inflammatory action than conventional NSAIDs and is a cytokine inhibitor. The mode of action of Locet is largely based on the inhibition of prostaglandin synthesis. Locet is a potent inhibitor of the enzyme cyclooxygenase, inflammatory cytokines interleukin IL1, tumor necrosis factor and prostaglandins E2. Cyclooxygenase is involved in the production of prostaglandins (chemicals in the body) which cause pain, swelling and inflammation.
Pharmacokinetics: After oral administration, Locet is rapidly and completely absorbed as unchanged drug. Peak plasma concentrations are reached approximately 1-3 hrs following ingestion. Locet is highly protein bound (>99%). Locet penetrates into the synovial fluid, where the concentrations reach approximately 57% of those in plasma. The volume of distribution is approximately 25 L. The mean plasma elimination t½ is around 4 hrs. Locet is metabolized to a major metabolite 4'-hydroxyaceclofenac and other metabolites 5 hydroxyaceclofenac, 4'-hydroxydiclofenac, diclofenac and 5 hydroxydiclofenac.
Approximately 2/3 of the administered dose is excreted via the urine, mainly as hydroxymetabolites. No changes in the pharmacokinetics of Locet have been detected in the elderly.
Locet administration
Should be taken with food. Take w/ or immediately after meals.
Locet pharmacology
After intake is absorbed from the gastrointestinal tract. Eating slows down the rate of absorption, extent of absorption is not changed. About 50% of the active substance is metabolized in the "first passage" through the liver. When used rectally absorption is slower. Time to reach Cmax in plasma after oral administration is 2-4 hours depending on the used dosage form, after rectal - 1 h, I.M. administration - 20 min. The concentration of active substance in plasma is a linear function of the applied dose.
Not cumulative. Plasma protein binding is 99.7% (predominantly albumin). Penetrates into synovial fluid, Cmax is achieved in 2-4 hours later than in plasma.
To a large extent metabolized to form several metabolites, among which two pharmacologically active, but to a lesser extent than diclofenac.
Systemic clearance of the active substance is about 263 ml / min. T1/2 from plasma is 1-2 h, from synovial fluid - 3-6 h. Approximately 60% of the dose was excreted as metabolites by the kidneys, less than 1% excreted in the urine as unchanged, while the rest is displayed in the form of metabolites with bile.
References
- DailyMed. "CETIRIZINE HYDROCHLORIDE; PSEUDOEPHEDRINE HYDROCHLORIDE: DailyMed provides trustworthy information about marketed drugs in the United States. DailyMed is the official provider of FDA label information (package inserts).". https://dailymed.nlm.nih.gov/dailyme... (accessed September 17, 2018).
- NCIt. "Cetirizine Hydrochloride: NCI Thesaurus (NCIt) provides reference terminology for many systems. It covers vocabulary for clinical care, translational and basic research, and public information and administrative activities.". https://ncit.nci.nih.gov/ncitbrowser... (accessed September 17, 2018).
- EPA DSStox. "Aceclofenac: DSSTox provides a high quality public chemistry resource for supporting improved predictive toxicology.". https://comptox.epa.gov/dashboard/ds... (accessed September 17, 2018).
Reviews
The results of a survey conducted on ndrugs.com for Locet are given in detail below. The results of the survey conducted are based on the impressions and views of the website users and consumers taking Locet. We implore you to kindly base your medical condition or therapeutic choices on the result or test conducted by a physician or licensed medical practitioners.User reports
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Information checked by Dr. Sachin Kumar, MD Pharmacology
