Nalgesin forte, 550 mg 20 pcs

Pharmacotherapeutic group: nonsteroidal anti-inflammatory drug

ATX code: M01AE02

Pharmacological properties

Pharmacodynamics

The drug Nalgesin^® forte is naproxen and has analgesic, antipyretic and anti-inflammatory effects. The mechanism of action is associated with non-selective inhibition of cyclooxygenase-1 and -2 (COX-1, COX-2) activity.

The drug Nalgesin ^® forte, film-coated tablets are well soluble, quickly absorbed from the gastrointestinal tract and provides rapid onset of analgesic effect.

Pharmacokinetics

It is quickly and completely absorbed from the gastrointestinal tract. Bioavailability is 95% (food intake has practically no effect on the completeness or speed of absorption). Time to reach maximum concentration is 1-2 hours. Blood plasma protein binding is 99 %. The elimination half-life is 12-15 hours. Metabolism occurs in the liver to dimethylnaproxen with participation of CYP2C9 isoenzyme. Clearance is 0.13 ml/min/kg. Excreted by the kidneys is 98%, 10% is excreted unchanged, 0.5-2.5% is excreted in the bile. The equilibrium concentration in blood plasma is determined after 4-5 doses of the drug (2-3 days).

In case of renal insufficiency cumulation of metabolites is possible.

Indications

The drug Nalgesin® forte is used for symptomatic therapy (to reduce pain, inflammation and decrease elevated body temperature) and has no effect on the progression of the underlying disease.

Active ingredient

Composition

1 film-coated tablet contains:

The core

The active ingredient:

Naproxen sodium 550.00 mg

The excipients: povidone K30, microcrystalline cellulose, talc, magnesium stearate, purified water

Filmy shell: Opadray 02F2050041

1Opadray 02F205004: hypromellose, titanium dioxide (E171), macrogol, indigo carmine dye (E132).

How to take, the dosage

Intravenously.

Strictly follow the doctor’s instructions. You should not stop treatment or change the dosage without first consulting your doctor. Ask your doctor about the duration of use of the drug.

The recommended therapy regimen

Adults, children 16 years of age and older

The usual daily dose used for pain relief is 1-2 tablets (550-1100 mg).

In very severe pain and no history of gastrointestinal disease, the doctor may increase the daily dose to 3 tablets (1650 mg), but not for more than 2 weeks.

When Nalgesin® forte is used as an antipyretic, the initial dose is 1 tablet (550 mg) and then ½ tablet (275 mg) every 6-8 hours.

To prevent migraine attacks, 1 tablet (550 mg) twice a day is recommended. However, treatment should be stopped if frequency, intensity and duration of migraine attacks do not decrease within 4-6 weeks. At the first signs of a migraine attack, you should take 1½ tablets (825 mg) and, if necessary, another ½-1 tablet (275-550 mg) 30 minutes later.

For relief of menstrual pain and cramps, pain after IUD insertion and other gynecological pain (adnexitis, childbirth as an analgesic and tocolytic agent), we recommend prescribing the drug at an initial dose of 1 tablet (550 mg), then ½ tablet (275 mg) every 6-8 hours.

In an acute attack of gout, the initial dose is 1½ tablets (825 mg), followed by 1 tablet (550 mg) after 8 hours and then ½ tablet (275 mg) every 8 hours until the attack stops.

In rheumatoid diseases (rheumatoid arthritis, osteoarthritis, and ankylosing spondylitis), the initial dose of the drug is usually 1-2 tablets (550-1100 mg) twice daily in the morning and evening. A starting daily dose of 1½-3 tablets (825-1650 mg) is recommended for patients with severe nocturnal pain and/or severe morning stiffness, patients being switched to naproxen treatment from high doses of other NSAIDs, and patients in whom pain is the leading symptom. Usually the daily dose is 1-2 tablets (550-1100 mg) administered in 2 doses.

The morning and evening doses may not be the same. With your doctor’s approval, you can change them depending on the prevalence of symptoms, i.e., nighttime pain and/or morning stiffness.

To reduce the risk of gastrointestinal adverse events, you should use the lowest effective dose for the shortest possible course.

If you get the impression that the effect of the drug is very strong or weak, inform your doctor or pharmacist.

Children

The drug Nalgesin® forte is contraindicated for use in children under 16 years of age.

Interaction

When treating with anticoagulants, it should be borne in mind that naproxen may increase bleeding time. Nalgesin® forte should not be used concomitantly with acetylsalicylic acid, other NSAIDs, including selective cyclooxygenase-2 inhibitors (increased risk of side effects).

According to clinical pharmacodynamic data, concomitant use of naproxen and acetylsalicylic acid for more than one day may inhibit the effect of a low dose of acetylsalicylic acid on platelet activity; the inhibition may persist for several days after stopping naproxen therapy. The clinical significance of this interaction is unknown.

Patients concomitantly receiving guidantoins, anticoagulants or other drugs that bind significantly to plasma proteins should watch for signs of potentiation or overdose of these drugs.

Nalgesin® forte may decrease the antihypertensive effects of propranololol and other beta-adrenoblockers and may increase the risk of renal failure associated with angiotensin-converting enzyme (ACE) inhibitors. NSAIDs may reduce the diuretic effect of diuretics. Naproxen inhibits the natriuretic effect of furosemide. Diuretics may increase the risk of nephrotoxicity of NSAIDs.

Inhibition of renal clearance of lithium leads to an increase in plasma lithium concentration. Probenecid administration increases the plasma concentration of naproxen.

Cyclosporine increases the risk of renal failure.

Naproxen slows down excretion of methotrexate, phenytoin, sulfonamides, increasing the risk of their toxic effects.

The antacids containing magnesium and aluminum decrease the absorption of naproxen.

Myelotoxic drugs increase the manifestation of hematoxicity of the drug.

According to in vitro studies, concomitant use of naproxen and zidovudine increases the concentration of zidovudine in plasma.

The concomitant use of corticosteroids may increase the risk of gastrointestinal ulceration or bleeding.

The use of NSAIDs may increase the effect of anticoagulants, such as warfarin.

The concomitant use of naproxen and antiplatelet drugs, selective serotonin reuptake inhibitors increases the risk of gastrointestinal bleeding.

The concomitant use of NSAIDs for 8-12 days after mifepristone is not recommended.

The concomitant use of NSAIDs and tacrolimus increases the risk of nephrotoxicity.

Special Instructions

Do not exceed the doses indicated in the instructions. To reduce the risk of gastrointestinal adverse events, use the lowest effective dose for the shortest possible course.

If pain and fever persist or get worse, you should see a doctor.

Patients with bronchial asthma, with blood clotting disorders, or with hypersensitivity to other analgesics should consult a physician before taking Nalgesin® forte.

Patients with liver disease and renal impairment should be prescribed with caution. In patients with renal insufficiency, creatinine clearance should be monitored. In CKR below 30 ml/min, it is not recommended to use naproxen. In chronic alcoholic and other forms of liver cirrhosis the concentration of unbound naproxen is increased, therefore lower doses are recommended for such patients. After two weeks of using the drug it is necessary to monitor liver function parameters.

The drug Nalgesin® forte should not be taken with other anti-inflammatory and analgesic drugs unless prescribed by a physician.

Lower doses are also recommended for elderly patients.

Naproxen should be avoided for 48 hours before surgery. If 17-corticosteroid determination is necessary, the drug should be discontinued 48 hours before the study. Similarly, naproxen may affect the determination of 5-hydroxyindoleacetic acid in urine.

The use of naproxen, as well as other drugs that block the synthesis of prostaglandins, may affect fertility, so it is not recommended for women who plan to become pregnant.

Each tablet of Nalgesin® forte contains approximately 50 mg of sodium. This should be considered when restricting salt intake.

Influence on driving, operating machinery

Naproxen slows down reaction time in patients. This should be considered when driving and performing tasks requiring increased attention.

Synopsis

Oval biconvex tablets with a rib on one side, covered with a blue film coating.

Breakage appearance: a rough white mass with a blue film coating.

Contraindications

– Hypersensitivity to naproxen or sodium naproxen.

– Complete or incomplete combination of bronchial asthma, recurrent nasal or paranasal sinus polyposis and intolerance to acetylsalicylic acid and other non-steroidal anti-inflammatory drugs (NSAIDs) (including history).

– Period after coronary artery bypass grafting.

– Erosive ulcerative changes of the mucosa of the stomach or 12 duodenum, active gastrointestinal bleeding.

– Inflammatory bowel disease (non-specific ulcerative colitis, Crohn’s disease) in the acute phase.

– Hemophilia and other disorders of blood clotting.

– Cerebrovascular bleeding or other bleeding disorders.

– Decompensated heart failure.

– Severe liver failure or active liver disease.

– Severe renal insufficiency (creatinine clearance (CK) less than 30 ml/min), progressive renal disease, confirmed hyperkalemia.

– Pregnancy, breastfeeding period.

– Child age under 16 years.

With caution

Coronary heart disease, cerebrovascular disease, congestive heart failure, dyslipidemia/hyperlipidemia, diabetes mellitus, peripheral arterial disease, smoking, renal impairment (CK 30-60 ml/min), anamnestic data about the development of gastrointestinal (GI) ulcers, presence of Helicobacter pylori infection, use in elderly patients, systemic lupus erythematosus or mixed connective tissue diseases (Sharp’s syndrome), long-term use of NSAIDs, frequent alcohol consumption, severe somatic diseases, concomitant therapy with the following drugs: anticoagulants (e.g., warfarin), antiaggregants (e.g., acetylsalicylic acid, clopidogrel), oral glucocorticoids (e.g., prednisolone), selective serotonin reuptake inhibitors (e.g., citalopram, fluoxetine, paroxetine, sertraline).

Side effects

Unwanted effects that may develop during treatment with naproxen are classified according to the following frequency of occurrence: Very common (³ 1/10), common (³ 1/100 to < 1/10), infrequent (³ 1/1,000 to < 1/100), rare (³ 1/10,000 to < 1/1,000), very rare (< 1/10,000), frequency unknown (cannot be determined based on available data).

Gastrointestinal disorders: Gastrointestinal adverse events have been observed most frequently. Possible development of peptic ulcer, perforation or gastrointestinal bleeding, sometimes with fatal outcome, especially in elderly patients (see section “Special indications”).

In each group, the adverse events are listed in descending order of severity.

Disorders of the blood and lymphatic system:

Infrequent: eosinophilia, granulocytopenia, leukopenia, thrombocytopenia.

Nervous system disorders:

often: headache, vertigo, dizziness, drowsiness;

infrequently: depression, sleep disturbances, inability to concentrate, insomnia, malaise.

Visual disorders:

often: visual disturbances.

Hearing organ disorders and labyrinth disorders:

often: tinnitus, hearing impairment;

infrequently: decreased hearing.

Heart disorders:

often: swelling, palpitations;

infrequently: congestive heart failure.

Respiratory system, chest and mediastinum disorders:

often: dyspnea;

infrequently: eosinophilic pneumonia.

Gastrointestinal disorders:

often: constipation, abdominal pain, dyspepsia, nausea, diarrhea, stomatitis, flatulence;

infrequent: gastrointestinal bleeding and/or gastric perforation, bloody vomiting, melena, vomiting;

very rare: recurrence or exacerbation of ulcerative colitis or Crohn’s disease;

frequency unknown: gastritis.

Liver and biliary tract disorders:

infrequent: increased activity of “liver” enzymes, jaundice.

Skin and subcutaneous tissue disorders:

often: skin itching, skin rash, ecchymosis, purpura;

infrequently: alopecia, photodermatosis;

very rare: bullous reactions, including Stevens-Johnson syndrome and toxic epidermal necrolysis.

Musculoskeletal and connective tissue disorders:

infrequently: myalgia and muscle weakness.

Renal and urinary tract disorders:

infrequent: glomerulonephritis, hematuria, interstitial nephritis, nephrotic syndrome, renal failure, renal papillary necrosis.

General disorders and disorders at the site of administration:

often: thirst, increased sweating;

infrequent: hypersensitivity reactions, menstrual irregularities, hyperthermia (chills and fever).

The occurrence of edema and symptoms of heart failure and increased blood pressure have been reported during NSAID therapy.

Clinical studies and epidemiologic data suggest that use of some NSAIDs (especially high doses and long-term therapy) may be associated with a slightly increased risk of arterial thrombosis (e.g., myocardial infarction or stroke).

Unwanted effects with no causal relationship to the use of naproxen

Disorders of the blood and lymphatic system: aplastic anemia, hemolytic anemia.

Nervous system disorders: aseptic meningitis, cognitive dysfunction.

Skin and subcutaneous tissue disorders: erythema multiforme, photosensitivity reactions similar to late cutaneous porphyria and epidermolysis bullosa, urticaria.

Vascular disorders: vasculitis.

General disorders and disorders at the site of administration: angioedema, hyperglycemia, hypoglycemia.

If you notice these changes, stop taking the drug and see your doctor, if possible.

Overdose

Symptoms

A significant overdose of naproxen may be characterized by drowsiness, dyspeptic disorders (heartburn, nausea, vomiting, abdominal pain), weakness, tinnitus, irritability, in severe cases – bloody vomiting, melena, impaired consciousness, seizures and renal failure.

Treatment

A patient who has accidentally or intentionally taken a large amount of the drug Nalgesin® forte should flush the stomach, take activated charcoal and conduct symptomatic therapy: antacids, H2-receptor blockers, proton pump inhibitors. Hemodialysis is ineffective.

Pregnancy use

The drug Nalgesin® forte is not recommended for use in pregnancy and during breastfeeding.

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