Naklofen - a drug with analgesic, antipyretic, antirheumatic and antiaggregatory action.
Release form and composition
Naklofen is available in the following dosage forms:
- Enteric-coated film-coated tablets: slightly biconvex, round, smooth, brownish-yellow (in blisters, 10 pcs., 2 blisters in a carton box);
- Solution for intramuscular injection: slightly yellowish or colorless, transparent, without visible mechanical impurities (3 ml ampoules; 5 ampoules per blister or plastic tray; 1 blister or pallet in a cardboard box);
- Rectal suppositories: conical, yellowish-white or white, with a uniform yellowish-white or white wax mass in a longitudinal section (in strips of 5 pieces; 2 strips in a cardboard box);
- Gel for external use 1%: white, homogeneous (in aluminum tubes 60 g; 1 tube in a carton box).
The composition of 1 tablet includes:
- Active ingredient: Diclofenac sodium - 50 mg;
- Auxiliary components: magnesium stearate, anhydrous colloidal silicon dioxide, povidone, microcrystalline cellulose, corn starch, lactose monohydrate;
- Shell: talc, propylene glycol, methacrylic acid-ethyl acrylate copolymer, titanium dioxide, iron dye yellow oxide (E172), iron dye red oxide (E172), hypromellose.
The composition of 1 ml solution for intramuscular injection includes:
- Active ingredient: Diclofenac sodium - 25 mg;
- Auxiliary components: sodium hydroxide, sodium disulfide, propylene glycol, benzyl alcohol, water for injection.
The structure of 1 suppository rectal includes:
- Active ingredient: Diclofenac sodium - 50 mg;
- Auxiliary component: solid fat.
The composition of 1000 mg of gel for external use includes active ingredients:
- Diclofenac Sodium - 10 mg;
- Diclofenac Diethylamine - 11.6 mg.
Auxiliary components: decyloleate, liquid paraffin, macrogol, cetomacrogol, anhydrous sodium sulfite, propylene glycol, diethanolamine, isopropanol, carbomer, purified water.
Indications for use
- Rheumatoid arthritis;
- Rheumatic lesions of soft tissues (bursitis, tendovaginitis).
Additional indications for the use of tablets, injection and suppositories are:
- Diseases of the musculoskeletal system of the inflammatory and degenerative nature: arthritis in Reiter's disease, gouty arthritis, Bechterew's disease, psoriatic and juvenile chronic arthritis, osteoarthritis of the spine and peripheral joints (including with radicular syndrome), synovitis, myositis, bursitis, periarthritis ;
- Pain syndrome of moderate or mild severity: renal and biliary colic, toothache, proctitis, adnexitis, algomenorrhea, migraine, headache, postoperative pain, post-traumatic pain syndrome, accompanied by inflammation, lumboischialgia, myalgia, neuralgia;
- Febrile syndrome (pills);
- Infectious diseases of the ear, nose and throat with severe pain: otitis, tonsillitis, pharyngitis (tablets, along with other drugs).
Additional indications for the use of the gel are:
- Bruises, tendon, muscle and ligament damage;
- Inflammatory swelling of soft tissues, sore muscles and joints, including those caused by heavy physical exertion.
- III trimester of pregnancy;
- Age up to 15 years or body weight <45 kg for tablets, up to 18 years for injection solution, up to 15 years for suppositories, up to 6 years for gel for topical use;
- Hypersensitivity to the components of the drug or other nonsteroidal anti-inflammatory drugs.
Additional contraindications to the use of tablets, suppositories and injection solutions are:
- The period after coronary artery bypass surgery;
- Decompensated heart failure;
- Erosive and ulcerative changes of the mucous membrane of the stomach or duodenum, active gastrointestinal bleeding;
- Inflammatory bowel disease (with exacerbation): Crohn's disease, ulcerative colitis;
- Severe liver failure or active liver disease;
- Rectal bleeding, hemorrhoids, inflammation or injuries of the rectum (suppositories);
- Severe renal failure (with creatinine clearance <30 ml per minute), including confirmed hyperkalemia and progressive kidney disease;
- Oppression of bone marrow hematopoiesis;
- Hemophilia and other coagulation disorders (suppositories);
- The combination of intolerance to acetylsalicylic acid and other nonsteroidal anti-inflammatory drugs (complete or incomplete) with bronchial asthma and recurrent polyposis of the nose and paranasal sinuses, including instructions in the anamnesis (suppositories);
- Lactation period.
Naklofen in the form of a gel is contraindicated to apply for violations of the integrity of the skin.
The drug in the form of tablets, injectable solution and suppositories should be used with caution in the following conditions / diseases:
- Coronary heart disease;
- Cerebrovascular diseases;
- Hyperlipidemia and / or dyslipidemia;
- Peripheral artery diseases;
- Ulcerative lesions of the gastrointestinal tract (in history);
- Severe somatic diseases;
- Helicobacter pylori infection;
- Long-term therapy with nonsteroidal anti-inflammatory drugs;
- Smoking, frequent use of alcohol;
- Creatinine clearance <60 ml per minute;
- Simultaneous therapy with anticoagulants (warfarin), antiplatelet agents (acetylsalicylic acid, clopidogrel), oral glucocorticoids (prednisone), selective serotonin reuptake inhibitors (sertraline, paroxetine, fluoxetine, citalopram);
- Induced porphyria (tablets and injection solution);
- Epilepsy (pills and injection);
- Diverticulitis (tablets and injection solution);
- Systemic diseases of the connective tissue (pills and injection solution);
- Significant decrease in circulating blood volume, incl. after carrying out massive surgical interventions (tablets and injection solution);
- Old age (including patients receiving diuretics and weakened patients with low body weight).
Naklofen in the form of an external gel should be used under the supervision of a physician in such diseases / conditions as:
- Hepatic porphyria in the acute phase;
- Erosive and ulcerative lesions of the gastrointestinal tract;
- Severe functional disorders of the liver and kidneys;
- Chronic heart failure;
- Bronchial asthma;
- Blood clotting disorders (including hemophilia, prolonged bleeding time, bleeding tendency);
- Elderly age;
- Lactation period.
Injection solution, suppositories and gel in the I-II trimester of pregnancy is prescribed with caution, Naklofen in the form of tablets - only in cases where the expected health benefits of the mother are higher than the potential risk to the fetus.
Dosing and Administration
Naklofen in pill form is taken orally, without chewing, with a small amount of water, preferably during or after a meal.
Single dose for adolescents from 15 years (with a body weight> 45 kg) and adults - 1 tablet 2-3 times a day. The dose is gradually reduced when the optimum therapeutic effect is achieved and transferred to supportive treatment - 2 tablets per day. The maximum daily dose is 3 tablets.
The solution is administered intramuscularly. The single dose for adults is 75 mg (1 ampoule). Not earlier than after 12 hours, repeated administration of the drug is possible (for renal colic, after 30 minutes). The duration of therapy is not more than 2 days, then, if necessary, the patient can be transferred to oral or rectal use of diclofenac.
Naklofen should not be mixed with other drugs in the same syringe.
Suppositories are used rectally. The initial dose for adults is 1 suppository 2-3 times a day, depending on the severity of the disease; for adolescents aged 15 years and older - 1 suppository no more than 2 times a day. Maintenance dose - 1 suppository 2 times a day.
The gel is applied externally, causing the affected area and gently rubbing. Adolescents from 12 years of age and adults are prescribed the drug 2-3 times a day, a single dose - a strip of gel about 5-10 cm long; children 6-12 years old - a strip of gel no more than 3 cm, no more than 2 times a day. If Naklofen is used for more than 10 days, it is recommended to consult a doctor.
It should be borne in mind that when combining several dosage forms of Naklofen (in addition to oral administration), the daily dose should not exceed 150 mg.
The following side effects may occur during the period of application of Naklofen in the form of tablets, injection solution and suppositories:
- Digestive system: often - increased activity of aminotransferases, anorexia, flatulence, dyspepsia, diarrhea, nausea, vomiting, epigastric pain; rarely, liver dysfunction, jaundice, hepatitis, gastrointestinal ulcers (with or without bleeding or perforation), gastrointestinal bleeding (diarrhea with blood, melena, vomiting of blood), proctitis, gastritis; very rarely - fulminant hepatitis, pancreatitis, constipation, diaphragm-like intestinal strictures (non-specific hemorrhagic colitis, exacerbation of Crohn's disease or ulcerative colitis), damage to the esophagus, dry mucous membranes (including the mouth), glossitis, stomatitis; local inflammation and irritation (suppositories);
- Nervous system: often - dizziness, headache; rarely - drowsiness; very rarely - a violation of sensitivity, including mental disorders, irritability, nightmares, insomnia, depression, disorientation, aseptic meningitis, cerebrovascular disorders, anxiety, convulsions, tremor, memory disorders, paresthesias;
- Cardiovascular system: very rarely - myocardial infarction, heart failure, vasculitis, increased blood pressure, chest pain, extrasystole, palpitations;
- Urinary system: very rarely - papillary necrosis, nephrotic syndrome, interstitial nephritis, proteinuria, hematuria, acute renal failure;
- Respiratory system: rarely - cough, bronchial asthma (including shortness of breath); very rarely - laryngeal edema, pneumonitis;
- Organs of blood formation: very rarely - agranulocytosis, hemolytic and aplastic anemia, eosinophilia, leukopenia, thrombocytopenia;
- Sense organs: often - vertigo; very rarely - a violation of taste, tinnitus, hearing loss, impaired vision (diplopia, blurred vision);
- Allergic reactions: anaphylactic / anaphylactoid reactions, including shock and marked reduction in blood pressure; very rarely - angioedema (including faces);
- Skin: often - skin rash; rarely - urticaria; very seldom - purpura, including allergic, photosensitization, hair loss, pruritus, exfoliative dermatitis, Lyell's syndrome, eczema, incl. multiforme and Stevens-Johnson syndrome, bullous eruptions.
With the intramuscular injection of the solution, irritation, swelling, pain and redness of the skin at the injection site may occur.
When using Naklofen in the form of an external gel, side effects such as can occur:
- Skin: eczema, urticaria, erythematous skin rash, burning sensation, contact dermatitis (itching, hyperemia, swelling of the treated skin area, papular-vesicular rash, peeling), photosensitization, redness;
- Systemic reactions: general anaphylactic reactions (including shock), angioedema, bronchial asthma, urticaria.
Due to the fact that with long-term diclofenac therapy, serious hepatotoxic reactions may occur in rare cases, it is necessary to regularly examine the function of the liver. Also, with prolonged treatment, it is recommended to perform a fecal occult blood test and monitor the picture of peripheral blood.
It is not recommended to use Naklofen for women who want to become pregnant, because the drug has a negative effect on fertility. Discontinuation of the drug is necessary in patients with infertility (including women undergoing examination).
Alcohol should not be taken during therapy.
To reduce the risk of side effects from the gastrointestinal tract, it is recommended to use the lowest effective dose of the drug with the lowest possible course.
Diclofenac sodium has anti-inflammatory and antipyretic properties that can mask the symptoms of infectious diseases.
If during the period of use of suppositories there are signs of liver damage, it is recommended to cancel the drug and consult a doctor for advice.
The preparation in the form of a gel should be applied only to intact areas of the skin. It is important to avoid contact with eyes, mucous membranes and open wounds. Gel can not be used under occlusive dressings.
It is recommended to be careful when applying a large amount of gel on large surfaces of sensitive skin for a long time.
During the period of use of the gel, you should avoid prolonged exposure to the sun. Wash hands thoroughly after using the product.
Patients in the application period of Naklofen in the form of tablets, injection solution or suppositories should refrain from performing potentially hazardous types of work requiring increased attention and quick psychomotor reactions.
The effect of diclofenac sodium on drugs / substances with simultaneous use:
- Preparations of lithium, digoxin, cyclosporine, methotrexate: increases their concentration in plasma;
- Diuretics: reduces their effect;
- Methotrexate: increases its toxicity;
- Hypnotic, hypoglycemic and antihypertensive drugs: reduces their effect;
- Glucocorticosteroids and other nonsteroidal anti-inflammatory drugs: increases the likelihood of their side effects;
- Cyclosporine: increases its nephrotoxicity.
The effect of drugs / substances on diclofenac sodium while applying:
- Acetylsalicylic acid: reduces its concentration in the blood;
- Paracetamol: increases the risk of its nephrotoxic effects;
- Drugs that cause photosensitization: increase its sensitizing effect to ultraviolet radiation;
- Drugs that block tubular secretion: increase its concentration in plasma, thereby increasing its toxicity;
- Preparations of gold, cyclosporine: increase its effect on the synthesis of prostaglandins in the kidneys, which is manifested by an increase in nephrotoxicity.
With the simultaneous use of Naklofen with other drugs / substances should consider the possibility of the development of the following disorders:
- Plikamycin, valproic acid, cefotetan, cefoperazone, cefamandol: an increase in the incidence of hypoprothrombinemia;
- Potassium-sparing diuretics: increased risk of hyperkalemia;
- Selective serotonin reuptake inhibitors: an increased risk of bleeding from the gastrointestinal tract;
- Ethanol, colchicine, corticotropin, Hypericum preparations: increased risk of bleeding in the gastrointestinal tract;
- Quinolone antibiotics: increased risk of seizures;
- Anticoagulants, antiplatelet and thrombolytic drugs (alteplase, streptokinase, urokinase): increased risk of bleeding (usually the gastrointestinal tract).
Terms and conditions of storage
Store in a dry place out of reach of children.
- Tablets and injection solution - 5 years at temperatures up to 25 ºС;
- Rectal suppositories - 4 years at temperatures up to 25 ºС;
- Gel for external use - 4 years at temperatures up to 30 ºС.