Naproxen

Pharmacological properties

Nalgesin is an NSAID that has analgesic, anti-inflammatory and antipyretic effects. the mechanism of action of the drug is due to inhibition of cog, an enzyme that takes part in the synthesis of prostaglandins. as a result, prostaglandin levels in various body fluids and tissues are reduced.

After oral administration, it is rapidly absorbed in the digestive tract. WITH_max in blood plasma is achieved 1–2 hours after administration and increases in proportion to an increase in the dose of the drug. The concentration of naproxen in plasma increases in proportion to the dose increase. About 99.5% of naproxen binds to plasma albumin at a drug concentration of up to 50 μg / ml. Approximately 70% of naproxen is excreted unchanged and approximately 30% is in the form of an inactive metabolite of 6-dimethyl-naproxen. Approximately 95% of the drug is excreted in the urine, about 5% - with feces. T_½ does not depend on the dose and plasma concentration and is 12-15 hours.

Indications

Headache and toothache, migraine, menstrual pain; pain in muscles, joints and pain in the spine (disorders of the musculoskeletal system); muscle and joint pain with colds and flu, rheumatoid diseases (rheumatoid arthritis, osteoarthrosis, ankylosing spondylitis and gout).

Application

In adults and children over the age of 16 years.

The tablets should be swallowed whole with a glass of water.

Treatment should be started with the minimum recommended dose, especially in elderly patients.

Toothache, headache and disorders of the musculoskeletal system. The recommended dose is 2 tablets (550 mg) 2 times a day, not more than 4 tablets (1100 mg) per day. Only in case of severe pain (except for disorders of the musculoskeletal system) up to 5 tablets (1375 mg) per day are possible.

Migraine. The recommended dose is 3 tablets (825 mg) at the first sign of an approaching attack. If necessary, during the day you can take 1 tablet (275 mg) or 2 tablets (550 mg), but not earlier than half an hour after taking the initial dose. Do not exceed the total dose of 5 tablets (1375 mg) per day.

Menstrual pain. The initial recommended dose is 2 tablets (550 mg). Then, if necessary, take 1 tablet (275 mg) every 6-8 hours. The maximum dose on the first day of treatment is 5 tablets (1375 mg) and 4 tablets (1100 mg) on ​​the following days.

In the case of an acute attack of gout, the initial dose is 825 mg (1.5 tablets), then 275 mg (half a tablet) is taken every 8 hours until the attacks stop and until the daily dose exceeds 1375 mg.

The initial dose for rheumatic diseases (rheumatoid arthritis, osteoarthrosis, ankylosing spondylitis) ranges from 550 to 1100 mg and is distributed in the morning and evening. For patients with severe pain at night or with stiff movements in the morning, for patients who replace high doses of other anti-inflammatory drugs with naproxen, and for patients with arthrosis, when pain is the main symptom, the initial daily dose should be 825–1375 mg. Treatment should be continued with daily doses of 550–1100 mg distributed in 2 doses. The dose in the morning and the dose in the evening should not be the same; they should be adjusted in accordance with the prevailing symptoms, namely pain at night or stiffness in the morning. A single daily dose in the morning or evening is sufficient for some patients.

Elderly patients. Patients over the age of 65, if necessary, should take tablets only every 12 hours.

Dosing for patients with impaired renal or hepatic function. Patients with impaired renal or hepatic function should be given lower doses.

Taking the drug is contraindicated in patients with severe impaired renal function (creatinine clearance less than 30 ml / min) or during dialysis due to the accumulation of naproxen metabolites in such patients.

Contraindications

Hypersensitivity to naproxen sodium or any excipient.

Hypersensitivity to salicylates and other NSAIDs, manifested in the form of AD, urticaria and nasal polyps.

An acute period or relapse of a stomach ulcer or duodenal ulcer, hemorrhage in the digestive tract.

Severe impairment of liver and kidney function (creatinine clearance 30 ml / min).

Heart failure.

During pregnancy and breastfeeding.

Age to 16 years.

Side effects

Side effects are most often associated with high doses.

From the hemopoietic system and lymphatic system: eosinophilia, granulocytopenia, leukopenia, thrombocytopenia, aplastic anemia, hemolytic anemia.

From the immune system: hypersensitivity reactions, anaphylactic reactions.

From the nervous system: headache, vertigo, dizziness, drowsiness, depression, sleep disturbance, inability to concentrate, insomnia, weakness, aseptic meningitis, cognitive impairment.

From the psyche: convulsions, abnormal dreams.

On the part of the organ of hearing and the labyrinth: tinnitus, hearing loss, hearing impairment.

From the side of the organ of vision: visual impairment, clouding of the cornea, papillitis, retrobulbar neuritis, swelling of the optic papilla.

From the side of the heart: edema, palpitations, congestive heart failure.

From the vessels: vasculitis.

From the respiratory system, chest and mediastinal organs: shortness of breath, eosinophilic pneumonia, agranulocytosis, asthma, pulmonary edema.

From the side of metabolism and nutrition: hyperglycemia, hypoglycemia.

From the gastrointestinal tract: constipation, abdominal pain, nausea, dyspepsia, diarrhea, stomatitis, ulcerative stomatitis, the formation of gastrointestinal ulcers, gastrointestinal bleeding and / or perforation of the stomach, vomiting, vomiting with blood, melena, esophagitis, pancreatitis, colitis .

From the liver and biliary tract: elevated levels of liver enzymes, jaundice, hepatitis.

On the part of the skin and subcutaneous tissues: itching, rashes, bruises, purpura, alopecia, photosensitive dermatitis, erythema nodosum, lichen planus, pustules, systemic lupus erythematosus, epidermal necrolysis, polymorphic erythema, photosensitivity reactions similar to chronic hematoporphyria and bullous epidermolysis, Stevens-Johnson syndrome, urticaria.

From the side of musculoskeletal and connective tissue: muscle pain and muscle weakness.

From the side of the kidneys and urinary tract: glomerulonephritis, hematuria, interstitial nephritis, nephrotic syndrome, impaired renal function, renal failure, renal papilla necrosis.

From the genitals and mammary glands: infertility in women.

Common disorders: thirst, sweating, menstruation, hyperthermia (chills and fever), angioedema.

Influence on the results of laboratory and instrumental studies: hyperkalemia, increased creatinine.

Edema, hypertension, and heart failure associated with NSAIDs have been reported.

Based on clinical studies and epidemiological data, it is suggested that an increased risk of cases of arterial thrombosis (for example, myocardial infarction or stroke) may be associated with the use of certain NSAIDs (especially in high doses and for a long time).

If severe adverse reactions occur, treatment should be discontinued.

special instructions

In order to reduce the likelihood of side effects, the drug should be used in the minimum effective dose and for the shortest period. in case of prolonged use, constant monitoring is necessary in order to identify adverse reactions. since cases of gastrointestinal bleeding have been noted with naproxen, it should be used with special care in patients with gastrointestinal diseases. serious adverse reactions from the gastrointestinal tract were detected with the use of NSAIDs. the risk of developing these reactions does not depend on the duration of treatment.elderly patients and debilitated patients are more prone to the formation of gastrointestinal ulcers, bleeding and the development of serious adverse reactions. the anti-inflammatory and antipyretic effect of the drug can mask the manifestations of diseases and complicate their diagnosis. in persons with a history of BA, allergic diseases or cases of bronchospasm, the development of bronchospasm is possible. may report abnormalities in laboratory tests of liver function. naproxen reduces platelet aggregation and prolongs bleeding time. this must be taken into account when determining the time of bleeding. with the use of naproxen, slight peripheral edema is possible, the risk of its development is high in patients with impaired heart function. patients with blood clotting disorders, using drugs that affect hemostasis, require more careful monitoring. in case of simultaneous use of anticoagulants, the risk of bleeding increases. in the presence of an infectious disease, the anti-inflammatory and antipyretic effects of naproxen should be considered, since they can mask the signs of these diseases.

Naproxen should be used very carefully in patients with impaired renal function. Patients with renal failure should determine creatinine clearance and monitor it during treatment. Naproxen is not recommended if creatinine clearance is 30 ml / min.

Anaphylactoid (anaphylactic) reactions can occur in individuals with or without a history of hypersensitivity to acetylsalicylic acid, other NSAIDs, or naproxen-containing drugs. Patients with angioedema, bronchospasm, AD, rhinitis and nasal polyps can also develop anaphylactoid reactions. Some of them, such as anaphylactic shock, can be fatal.

If the dose is reduced or NSAIDs are canceled during treatment with naproxen, their dose should be reduced gradually and under the supervision of a doctor to identify any adverse reactions, including adrenal cortex insufficiency and exacerbation of arthritis symptoms.

When using NSAIDs, including naproxen, diseases from the side of the organ of vision, in particular papillitis, retrobulbar neuritis and swelling of the optic papilla, have been occasionally noted, although a causal relationship has not been established. Therefore, patients who develop visual impairment during treatment with naproxen should undergo an ophthalmic examination.

Before starting treatment with naproxen, it is necessary to establish (consultation with a doctor) the presence of hypertension and / or heart failure in the patient’s medical history with fluid retention and edema associated with NSAIDs. Based on clinical studies and epidemiological data, it is suggested that an increased risk of arterial thrombosis may be associated with the use of certain NSAIDs (especially in high doses and for a long time). According to these data, the use of naproxen (1000 mg / day) is associated with lower risks, however, some risks cannot be excluded.

For patients with uncontrolled hypertension, congestive heart failure, coronary heart disease, peripheral arterial disease and / or cerebrovascular accident, the use of naproxen should be carefully weighed. For individuals with risk factors for cardiovascular events (eg, hypertension, hyperlipidemia, diabetes mellitus, smoking), the need for naproxen should also be carefully evaluated before starting long-term therapy.

Naproxen, like other COX synthesis inhibitors, can affect fertility. Women who are planning a pregnancy and / or have trouble conceiving should stop using naproxen.

Use with caution in patients with impaired liver function.In chronic alcoholic cirrhosis of the liver and other forms of cirrhosis, the total concentration of naproxen in the blood plasma decreases, and the concentration of unbound naproxen in the blood plasma increases.

Patients with epilepsy or porphyria who are taking naproxen should be carefully monitored.

Concomitant use with acetylsalicylic acid and other NSAIDs is not recommended due to an increased risk of side effects.

Elderly patients should take naproxen at the lowest effective doses.

Important information on some of the ingredients of nalgesin and nalgesin forte. Nalgesin contains 1.09 mmol (25.097 mg) of sodium in the 1st dose; Nalgesin Forte contains 2.18 mmol (50.16 mg) of sodium in the 1st dose. This should be considered for patients who follow a salt-free diet.

Use during pregnancy and lactation. Do not use during pregnancy and lactation.

The ability to influence the reaction rate when driving vehicles or working with other mechanisms. While using the drug, some patients may experience drowsiness, dizziness, visual disturbances, insomnia, or depression. In the case of the development of the above side effects, patients should refrain from driving and working with mechanisms.

Children. Nalgesin is used in children over the age of 16 years. Nalgesin forte is used only in adults.

Interactions

The simultaneous administration of acetylsalicylic acid and other NSAIDs is not recommended due to the high risk of adverse reactions.

Concomitant use with antacids or colestyramine may slow the absorption of naproxen.

Simultaneous use with cardiac glycosides can lead to exacerbation of heart failure, a decrease in glomerular filtration rate and an increase in the level of cardiac glycosides in the blood.

Do not use naproxen within 8-12 days after the use of mifepristone because of its ability to reduce the severity of the effects of the latter.

Caution is advised to use naproxen with corticosteroids at the same time because of the increased risk of ulcers and bleeding in the digestive tract.

Naproxen sodium can reduce platelet aggregation and prolong bleeding time, this should be considered when determining bleeding time and during concomitant treatment with anticoagulants.

Animal studies show the possibility of seizures caused by quinolone antibiotics. Patients taking quinolones have an increased risk of developing seizures.

Since naproxen is almost completely bound to plasma proteins, it should be used with caution when taken simultaneously with hydantoin derivatives and sulfonylurea derivatives.

Naproxen may reduce the severity of the natriuretic action of furosemide.

Naproxen may reduce the severity of the hypotensive effect of antihypertensive drugs.

With the simultaneous administration of lithium and naproxen sodium, the concentration of lithium in blood plasma increases.

Naproxen, like NSAID drugs, can reduce the severity of the antihypertensive effect of propranolol and other β-adrenoreceptor blockers and may increase the risk of renal failure in patients who take ACE inhibitors in parallel.

Naproxen reduces tubular secretion of methotrexate, therefore, with the parallel administration of methotrexate, its toxicity may increase.

At the same time taking probenecid increases T_½ naproxen and its concentration in blood plasma rises.

Concomitant use of cyclosporine may increase the risk of impaired renal function.

In vitro studies have shown that with the simultaneous administration of naproxen sodium and zidovudine, the concentration of the latter in blood plasma increases.

Overdose

After accidental or deliberate administration of a large amount of the drug, pain in the abdominal cavity, nausea, vomiting, dizziness, tinnitus, irritability may appear, in more severe cases - bloody vomiting, melena, impaired consciousness, respiratory distress, convulsions and renal failure. gastric lavage, intake of activated carbon, antacids, inhibitors of h2 receptors, proton pump inhibitors, misoprostol, etc. are indicated.

Storage conditions

At a temperature not exceeding 25 ° c.