Brands of Loxoprofen in Kenya
No Brands available
MODE OF ACTION
Like most NSAIDs, loxoprofen is a non-selective cyclooxygenase inhibitor and works by reducing the synthesis of prostaglandins from arachidonic acid.
Loxoprofen is a nonsteroidal anti-inflammatory drug (NSAID) in the propionic acid derivatives group, which also includes ibuprofen and naproxen among others. It is available in some countries for oral administration. A transdermal preparation was approved for sale in Japan in January 2006
INDICATIONS
- For relief of inflammation and pain in the following disorders and symptoms:
Rheumatoid arthritis, osteoarthritis, lower back pain, periarthritis of the shoulder, and shoulder-arm-neck syndrome, toothache - For relief of postoperative, post-traumatic, or post- exodontia pain and inflammation
- For antipyresis and relief of pain in the following disorder:
Acute upper respiratory, tract inflammation, (including acute upper. airway inflammation, accompany- ing acute bronchitis)
DOSAGE AND ADMINISTRATION
For relief of inflammation and relieve of postoperative pain, the usual adult dosage is
60 mg of loxoprofen sodium (as anhydride) orally three times a day.
For p.r.n. use, administer 60-120 mg once orally. The dosage may be adjusted according to the patient’s age and symptoms.
For an indication of antipyresis the usual adult dosage is 60 mg of loxoprofen sodium (as anhydride) p.r.n. once orally. The dosage may be adjusted according to the patient’s age and symptoms. In principle, the recommended maximum daily dose of loxoprofen is twice-daily administration, and the total daily dose should not exceed 180 mg/day.
The use of loxoprofen on an empty stomach should be avoided.
Use in the Elderly
In as much as adverse reactions are likely to occur in elderly patients, loxoprofen should be used with caution, e.g., starting at a low dose, while closely monitoring the patient’s condition (see “Important Precautions”).
Pediatric Use
The safety of loxoprofen in low birth weight infants, newborn infants, Infants and toddlers, children, and adolescents has not been established.
CONTRAINDICATIONS
Loxoprofen is contraindicated in the following patients.
Patients with peptic ulcers [Peptic ulcers may be aggravated due to reduced gastric blood flow resulting from inhibition of prostaglandin biosynthesis.]
Patients with severe blood disorders [Platelet dysfunction may occur and the abnormality may be worsened]
Patients with severe hepatic functions disorders [Hepatic function disorders have been reported with the use of loxoprofen, and the patient’s hepatic function disorder may be aggravated]
Patients with severe renal impairment [Adverse reactions such as acute renal failure, nephrotic syndrome, etc. have been reported with the use of loxoprofen]
Patients with severe cardiac function failure [Cardiac symptoms may be exacerbated because inhibition of prostaglandin biosynthesis in the kidneys may cause edema and an increase in circulating body fluid volume, with a consequent increase in cardiac work.]
Patients with a history of hypersensitivity to any
ingredients of loxoprofen.
Patients with or with a history of aspirin-induced asthma (induction of asthmatic attack with nonsteroidal anti-inflammatory-analgesics, etc.) [May induce an aspirin-induced asthmatic attack.]
Women in the late stages of pregnancy
DRUG INTERACTIONS
Loxoprofen should not be administered at the same time as second-generation quinolone antibiotics such as ciprofloxacin and norfloxacin, as it increases their inhibition of GABA and this may cause seizures. It may also increase the plasma concentration of warfarin, methotrexate, sulfonylurea derivatives, and lithium salts, so care should be taken when loxoprofen is administered to patients taking any of these drugs
Drugs
Coumarin Anticoagulants (e.g., Warfarin)
The anticoagulant effect of these drugs may be enhanced. Therefore, caution should be exercised and the dosage reduced as necessary.
The inhibitory effect of this drug on prostaglandin biosynthesis may lead to inhibition of platelet aggregation and hypo-coagulation, thereby adding to the anticoagulant effects of these drugs.
Sulfonylurea hypoglycemic agents (e.g., Tolbutamide)
The hypoglycemic effect of these drugs may be enhanced. Therefore, caution should be exercised and the dosage reduced as necessary.
It is generally considered that co-administration of this drug, the protein-binding rate of which is as high as 97.0% as loxoprofen or 92.8% as its trans-OH form, results in increased plasma levels of the active form of the concurrently administered hypoglycemic agent with a high protein-binding rate, to enhance the effect of the latter drug.
New quinolone antimicrobial agents (e.g., Enoxacin hydrate)
The convulsant effect of these drugs may be enhanced.
New quinolone antimicrobials inhibit receptor binding of GABA, an inhibitory neurotransmitter in the central nervous system, and hence may produce a convulsant effect. Co-administration with these drugs is thus considered to enhance their inhibitory effects.
Methotrexate
Plasma methotrexate concentration may be increased, leading to enhancement of the effects of methotrexate.
Therefore, the dose should be reduced whenever deemed necessary.
Although the exact mechanism is not known, it is generally thought that excretion of the drug from the kidneys is reduced with a consequent elevation in its plasma concentration due to the drug’s inhibition of prostaglandin biosynthesis in the kidneys.
ADVERSE EFFECTS
Shock and anaphylactoid symptoms:
Shock and anaphylactoid symptoms (decreased blood pressure, urticaria, edema of the larynx, dyspnea,etc.) have been reported with the use of Loxoprofen. Patients should be carefully monitored during treatment. If any abnormal symptoms occur in a patient being treated with Loxoprofen, Loxoprofen should be discontinued and appropriate therapies should be initiated immediately.
Hemolytic anemia, leukopenia, and thrombocytopenia:
Hemolytic anemia, leukopenia, and thrombocytopenia have been reported with the use of Loxoprofen. Patients should be carefully followed by a hematological examination, etc. during treatment. If any abnormal symptoms occur in a patient being treated with Loxoprofen, Loxoprofen should be discontinued and appropriate therapies should be initiated immediately.
Oculomucocutaneous syndrome and toxic epidermal necrolysis:
Oculomucocutaneous syndrome (Stevens-Johnson syndrome) and toxic epidermal necrolysis (Lyell syndrome) have been reported with the use of Loxoprofen. Patients should be carefully monitored during treatment. If any abnormal symptoms occur in a patient being treated with Loxoprofen, Loxoprofen should be discontinued and appropriate therapies should be initiated immediately
Acute renal failure, nephrotic syndrome, and interstitial nephritis:
Acute renal failure, nephrotic syndrome, and interstitial nephritis have been reported with the use of Loxoprofen. Patients should be carefully monitored during treatment. If any abnormal symptoms occur in a patient being treated with Loxoprofen, Loxoprofen should be discontinued and appropriate therapies should be initiated immediately. Loxoprofen should be used with special caution in such patients because hyperkalemia may appear in association with acute renal failure.
Congestive Cardiac failure :
Cardiac failure congestive has been reported with the use of Loxoprofen. Patients should be carefully monitored during treatment. If any abnormal symptoms occur in a patient being treated with Loxoprofen, Loxoprofen should be discontinued and appropriate therapies should be initiated immediately.
Interstitial pneumonia:
Interstitial pneumonia with manifestations of fever, cough, dyspnea, chest X-ray abnormalities, and eosinophilia have been reported with the use of Loxoprofen. If these signs/findings are observed in a patient being treated with Loxoprofen, Loxoprofen should be discontinued and appropriate therapies such as corticosteroid medication should be initiated immediately.
Gastrointestinal bleeding:
Serious peptic ulceration or gastrointestinal bleeding from the small intestine and/or large intestine, e.g., hematemesis, melena, and hematochezia, and consequent shock has been reported with the use of Loxoprofen. Patients should be carefully monitored during treatment. If any abnormal symptoms occur in a patient being treated with Loxoprofen, Loxoprofen should be discontinued and appropriate therapies should be initiated immediately.
Gastrointestinal perforation:
Gastrointestinal perforation has been reported with the use of Loxoprofen. If epigastric pain, abdominal pain, etc. are noted in a patient being treated with Loxoprofen, Loxoprofen should be discontinued and appropriate therapies should be initiated immediately.
Hepatic function disorders, and jaundice:
Hepatic function disorders including jaundice increased serum levels of AST (GOT), ALT (GPT) and ã-GTP, or fulminant hepatitis have been reported with the use of Loxoprofen. Patients should be carefully monitored during treatment. If any abnormal symptoms occur in a patient being treated with Loxoprofen, Loxoprofen should be discontinued and appropriate therapies should be initiated.
Asthmatic attack:
Acute respiratory disorders such as asthmatic attacks have been reported with the use of Loxoprofen. Patients should be carefully monitored during treatment. If any abnormal symptoms occur in a patient being treated with Loxoprofen, Loxoprofen should be discontinued and appropriate therapies should be initiated immediately.
Aseptic meningitis:
Aseptic meningitis including fever, headache, nausea, and vomiting, nuchal rigidity, clouding of consciousness, etc. has been reported with the use of Loxoprofen. Patients should be carefully monitored during treatment. If any abnormal symptoms occur in a patient being treated with Loxoprofen, Loxoprofen should be discontinued and appropriate therapies should be initiated immediately. (in particular, the adverse event is likely to occur in the patients with systemic lupus erythematosus or mixed connective tissue disease).
Reporting of suspected adverse reactions:
The PPB Department of Pharmacovigilance was set up with a vision to develop, implement and continuously upgrade an appropriate system for detecting, reporting, and monitoring adverse drug reactions (ADRs) and other relevant problems with medicines in Kenya. The department strives to ensure the safety and efficacy of pharmaceutical products in Kenya.
Reporting suspected adverse reactions after authorization of the medicinal product are important. It allows continued monitoring of the benefit/risk balance of the medicinal product. Healthcare professionals/ Patients are encouraged to report any suspected adverse reactions via Pharmacovigilance Yellow Form, pv@pharmacyboardkenya.org, or click the below button:
Loxoprofen in Kenya
Loxoprofen in Kenya
Loxoprofen in Kenya
Loxoprofen in Kenya
Loxoprofen in Kenya
Clinical | Pharmacokinetic data
Pregnancy Category:
Routes of Administration:
Bioavailability: Not Available
Protein Binding: 97%
Metabolosim: Hepatic glucuronidation
Onset of Action: N/A
Elimination Half life: 75 minutes
Excretion: Renal
Legal Status | Dosage forms & Strengths
Prescription Category:
Prescription only Medicine (POM) , ℞-only
Narcotic Drugs and Psychotropic Substances (Control ) Act Schedule:
This drug is not a controlled substance under Narcotic Drugs and Psychotropic Substances (Control ) Act
Dosage Forms | Strengths:
Drug Indentifiers:
| CAS Number | |
|---|---|
| PubChem CID | |
| ChemSpider | |
| UNII | |
| KEGG | |
| ChEBI | |
| ChEMBL | |
| CompTox Dashboard (EPA) | |
Drug Images
References/ Citation:
- Sugimoto, Masahiko, et al. “Inhibition of prostaglandin production in the inflammatory tissue by loxoprofen-Na, an anti-inflammatory prodrug.” Biochemical pharmacology 42.12 (1991): 2363-2368.
- Noguchi, Masahiro, et al. “Enzymologic and pharmacologic profile of loxoprofen sodium and its metabolites.” Biological and pharmaceutical bulletin 28.11 (2005): 2075-2079.