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Nabumetone Tablets

Function and Efficacy

This product is a non-acidic non-steroidal anti-inflammatory drug, which is rapidly metabolized to 6-methoxy-2-naphthylacetic acid (6-MNA) in the liver and has antipyretic, analgesic and anti-inflammatory effects. 1 The anti-inflammatory, analgesic and antipyretic effects are related to the fact that the active metabolites of cabutimetone inhibit the synthesis of prostaglandins in inflammatory tissues. 2 Little effect on gastric mucosa: This product is a non-acidic, non-ionic prodrug, which has no obvious local direct effect on the gastric mucosa during the absorption process; at the same time, this product has little inhibitory effect on the physiological cyclooxygenase of the gastric mucosa. Therefore, the incidence of gastrointestinal mucosal erosion and bleeding caused by this product is low. 3 No effect on bleeding and coagulation: This product has no effect on the platelet aggregation induced in vitro in blood samples of healthy volunteers. There were no significant changes in bleeding time and coagulation tests.

Ingredients

The main ingredient of this product is nabumetone, whose chemical name is 4-(6-methoxy-2-naphthyl)butanone-2.

Name Description Content CAS NO. Manufacturer
NabumetoneIngredients

Non-acidic nonsteroidal anti-inflammatory drugs, which exert antipyretic, analgesic and anti-inflammatory effects by being metabolized to 6-methoxy-2-naphthylacetic acid (6-MNA). Its active metabolites inhibit the synthesis of prostaglandins in inflammatory tissues, have little effect on the gastric mucosa, and do not cause significant changes in platelet aggregation, bleeding time and coagulation tests in healthy volunteers.

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42924-53-8 27

Appearance

This product is white tablets.

Usage and Dosage

1Usual dosage for adults is 1.0g (2 tablets) orally, once a day. The maximum daily dosage is 2g, divided into two doses. Adults weighing less than 50kg can start with 0.5g (1 tablet) daily. Gradually increase to the effective dose. 2The dosage for children has not yet been established.

Adverse Reactions

1 Gastrointestinal tract: nausea, vomiting, indigestion, diarrhea, abdominal pain and constipation, about 1% to 3%. Upper gastrointestinal bleeding, about 0.7%. In the cases of this product, the incidence of ulcers in the short-term treatment group (6 weeks to 6 months) and the long-term treatment group (8 years) were 0.1% and 0.95%, respectively. The incidence of diarrhea increased with daily oral administration of 2g of nabumetone. 2 Nervous system: manifestations include headache, dizziness, tinnitus, sweating, insomnia, drowsiness, tension and dreaminess, with an incidence of less than 1.5%. 3 Skin: rash and itching, about 2.1%, edema, about 1.1%. 4 Rare or occasional adverse reactions include jaundice, abnormal liver function, anxiety, depression, paresthesia, tremor, dizziness, bullous rash, urticaria, dyspnea, asthma, allergic pneumonia, proteinuria, hematuria and angioneurotic edema.

Precautions

It is contraindicated for patients with active peptic ulcer or bleeding, severe liver function abnormalities, and allergies to this product and other non-steroidal anti-inflammatory drugs.

Special Population Medication

Precautions for children: There is no clinical data recommending the use of nabumetone in children, and it should be prohibited. Precautions for pregnancy and lactation: Use during pregnancy and lactation: Animal experimental studies have shown no potential teratogenicity. Like other compounds. Maternal toxicity can be seen in animals at high enough doses, and embryonic signs are recorded (the dose in rabbit studies was 300 mg/kg). High-dose studies in rats (320 mg/kg) can delay delivery, which is believed to be due to the inhibition of prostaglandin synthesis. Nabumetone active metabolites can be found in mammalian milk. Nabumetone tablets are not recommended for use by pregnant and lactating women. There is no experience in clinical trials of nabumetone in human pregnancy and lactation. It has not been confirmed whether nabumetone can be secreted through human milk, but 6-MNA can be secreted in the milk of lactating rats. Considering the potential possibility of serious adverse reactions to nabumetone in breastfed infants, the importance of this drug to the mother must be weighed to decide to stop breastfeeding or stop the drug. The use of nabumetone in the first six months of pregnancy should be limited to the following situations, that is, the potential efficacy (benefit) of the drug to the mother clearly outweighs the potential risks to the fetus and the nursing infant. The effects of this class of drugs on the human fetus in late pregnancy are known to include arterial stenosis, as well as lung and heart changes, so nabumetone is not recommended for use in late pregnancy. Precautions for the elderly: Elderly patients usually have higher blood concentrations of many drugs. Elderly people should maintain the lowest effective dose when using this product. The recommended dose in this age group does not exceed 1 gram per day, and some patients will get satisfactory results by taking 0.5 grams.

Drug Interactions

1. The absorption rate of this product is not affected by the combined use of aluminum hydroxide gel, aspirin or acetaminophen. However, it is generally not recommended to use two or more non-steroidal anti-inflammatory drugs at the same time. 2. There is no interaction between this product and the anticoagulant warfarin in healthy volunteers. However, there is no data on the combined use of these two drugs in patients. 3. When this product is used in combination with acetyl anticonvulsants and sulfonylurea hypoglycemic drugs, the dosage should be appropriately reduced.

Storage

Keep away from light and store in a sealed container.

Packaging Specification

0.5 g

Validity Period

24 months

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