Naklofen

Naklofen is a drug from the category of NSAIDs, a derivative of α-toluic acid. Among its properties - painkillers, anti-inflammatory and antipyretic.

[1]

Indications Naklofen

Among the indications:

• degenerative pathologies or inflammatory processes in the ODE. These are diseases such as juvenile, rheumatoid and psoriatic forms of arthritis in the chronic stage, and in addition Bechterew's disease, a reactive and gouty form of arthritis. Also, for rheumatism of soft tissues, osteoarthritis of the spine along with peripheral joints (may be accompanied by a Minor symptom), and in addition with bursitis, tendovaginitis, inflammation of skeletal muscles, periarthritis and synovitis;
• weak or moderate pain with myalgia, neuralgia, and also lumbosciatica. Also with post-traumatic pains, with inflammatory processes against their background, with dental and headaches, pain after surgical operations. In addition to migraine, dysmenorrhea, inflammation of the appendages, proctitis, biliary or renal colic;
• as a component of the integrated treatment of ENT diseases of an infectious-inflammatory nature, in which severe pain (such as otitis, pharyngitis, and tonsillitis) is felt;
• fever.

[2], [3], [4]

Release form

It is available in capsules having a modified release. The volume of capsules is 75 mg. There are 10 capsules on one blister, and 2 blister plates in one package.

[5], [6]

Pharmacodynamics

The active component of the drug is diclofenac sodium. It acts on the body in the following way: it unselectively suppresses the activity of the enzymes COX-1 and also COX-2, as a result of which there is a disruption in the metabolism of eicosatetraenoic acid, as well as a decrease in the synthesis of thromboxane and also of PG and prostacyclin. The concentration of various PG within the synovial fluid, urine, and gastric mucosa decreases.

The greatest effectiveness manifests in the elimination of pain, developing as a result of inflammatory processes. In the treatment of rheumatic pathologies, analgesic and anti-inflammatory qualities of diclofenac can reduce the strength of pain, swelling and marked stiffness of the joints in the morning - this increases the functional capacity of the joint. The active substance also helps to reduce inflammation and pain in the post-surgical period, and in addition to injuries.

Like other NSAIDs, diclofenac has antiplatelet properties. In the therapeutic dosage, it almost does not affect the processes of blood flow. In the case of prolonged therapy, the efficacy of the active ingredient is not impaired.

[7], [8], [9], [10]

Pharmacokinetics

The active substance is absorbed completely and quickly. The peak of the plasma concentration reaches 0.5-1 hour after ingestion. This indicator is linearly dependent on the amount of dosage administered to the body.

With repeated use of the drug, there is no change in the pharmacokinetics of the active substance. If you keep the necessary interval between drugs, it does not accumulate in the body. The bioavailability index is 50%, and with plasma proteins binds more than 99% (the main part - with albumins). The substance passes inside the synovial fluid, and the peak concentration in it reaches 2-4 hours later than inside the plasma. The time for diclofenac to be removed from the plasma will also be shorter.

As a result of the first pass in the liver, about 50% of the active ingredient undergoes a metabolic process that develops as a result of a one- or multiple-time hydroxylation process, as well as conjugation with glucuronic acid. A participant of metabolic processes is also the enzyme system P450CYP2C9. Decomposition products have a lower pharmacological activity than the active component of drugs.

The system Cl reading is 260 ml / minute, and the distribution volume is 550 ml / kg. The plasma half-life of the substance is 2 hours. Approximately 70% of the dose used is eliminated through the kidneys in the form of pharmacologically inactive decay products, and even less than 1% of the substance is excreted unchanged. The residue is excreted together with bile in the form of decay products.

[11], [12], [13], [14], [15]

Dosing and administration

Take the medicine by mouth, swallowing the capsule, not chewing, and washing it with water. Do this at the end of the meal or immediately after it (best in the morning). Dosages are determined individually, according to the severity of the pathology. For adults, the dose is usually 1 capsule 1-2 times per day. A day is allowed to take no more than 150 mg of the drug.

[23], [24], [25]

Use Naklofen during pregnancy

Use of the drug during pregnancy is permitted only in cases where the possible benefit exceeds the risk of developing negative consequences for the fetus. But in the 3rd trimester, Naklofen is prohibited in any case.

Contraindications

Among the contraindications:

• individual intolerance to diclofenac;
• a combination (in incomplete or full form) of bronchial asthma, polyposis of the nose with paranasal sinuses (in a relapsing form), and hypersensitivity to aspirin and other NSAIDs (also in the anamnesis);
• Postoperative period after the procedure for aortocoronary bypass;
• presence of ulcers and erosions on mucous membranes of the duodenum gut or stomach, as well as active bleeding in the gastrointestinal tract;
• exacerbated inflammation in the intestine (such as nonspecific form of ulcerative colitis, as well as regional enteritis);
• cerebrovascular or other form of bleeding, as well as disorders of hemostasis;
• severe form of hepatic insufficiency or active hepatic pathology;
• a pronounced form of renal failure (Cl creatinine is less than 30 ml / minute), diagnosed hyperkalemia, and kidney disease in the progressing stage;
• decompensated form of heart failure;
• suppression of hematopoietic processes in the bone marrow;
• children under 18 years of age.

[16], [17], [18], [19]

Side effects Naklofen

Taking medication can lead to the development of such adverse reactions:

• organs of the digestive system: often - vomiting with nausea, pain in the epigastrium, abdominal pain syndrome, dyspeptic manifestations, diarrhea, bloating. In addition, it is also anorexia, and an increase in the activity of transaminases. In rare situations - the gastrointestinal tract develops bleeding (diarrhea or vomiting with blood, as well as melena). In addition, such disorders as gastritis, gastrointestinal processes in the digestive tract (with or without perforation or bleeding), as well as jaundice with hepatitis and a disorder in the liver can develop. Single - dryness of mucous membranes (also in the oral cavity), glossitis and stomatitis, and in addition to esophageal injury, diaphragm-like intestinal strictures (nonspecific form of hemorrhagic colitis, exacerbated ulcerative colitis or regional enteritis), pancreatitis, constipation and hepatitis with fulminant course;
• organs of the National Assembly: often it is dizziness or headaches. Occasionally - a feeling of drowsiness. Individual disorders of sensitivity (for example, paresthesia) develop, seizures, tremors, memory problems, anxious feelings develop. In addition, cerebrovascular disorders, aseptic meningitis, a sense of depression, the development of insomnia, disorientation and the appearance of nightmares. Also a feeling of excitement or irritability and mental disorders;
• senses: Vertigo often develops. Visually observed disorders of vision (diplopia or fogging), taste sensations or hearing, there are noises in the ears;
• organs of the urinary system: hematuria, acute form of renal failure, tubulointerstitial nephritis can be developed individually, in addition to proteinuria and nephrotic syndrome, necrotic papillitis, as well as puffiness;
• organs of the hematopoietic system: there is individual thrombocyto- or leukopenia, aplastic or hemolytic form of anemia, eosinophilia, and in addition agranulocytosis;
• allergy: anaphylactoid and anaphylactic reactions (among them a noticeable decrease in blood pressure, as well as a shock state). Single - the development of edema Quincke (also on the face). Allergic reaction is provoked by the substances contained in the drug methylparahydroxybenzoate, as well as propyl parahydroxybenzoate;
• organs of the cardiovascular system: tachycardia develops individually, problems with the heart rhythm, pain inside the chest, extrasystole, increase in the level of blood pressure. In addition, the development of heart failure, as well as vasculitis or myocardial infarction;
• respiratory organs: in rare situations, the appearance of cough or bronchial asthma (also dyspnea); single - development of laryngeal edema or pneumonitis;
• Skin: mostly develop rashes on the skin. In rare situations, hives can occur. Single violations are observed, such as bullous rash, as well as eczema (including polyform). In addition, malignant exudative erythema, toxic epidermal necrolysis, skin itching, exfoliative dermatitis, alopecia, photophobia, and purpura (possibly in an allergic form).

[20], [21], [22]

Overdose

Manifestations of drug overdose: increased side effects - nausea with vomiting, pain in the abdomen, diarrhea, bleeding inside the gastrointestinal tract, and dizziness with headaches, cramps and tinnitus. In addition, high excitability, the development of hyperventilation of the lungs with increased convulsive readiness. In the case of a significant excess of the dose - the development of hepatotoxic effects and acute form of renal failure.

To eliminate violations, it is necessary to rinse the stomach and drink activated charcoal, and in addition to carry out symptomatic treatment. The effectiveness of procedures for hemodialysis and forced diuresis is very small, since overdose is associated with a significant binding to proteins, as well as an intensive metabolism.

[26]

Interactions with other drugs

The drug increases the plasma concentration of substances such as methotrexate and digoxin, as well as cyclosporine and lithium drugs. Weaken the effectiveness of diuretics. In combination with potassium-sparing diuretics, the risk of hyperkalemia increases. In conjunction with anticoagulants, antiaggregants, as well as fibrinolytic drugs (alteplase and streptokinase with urokinase), the risk of bleeding (in the gastrointestinal tract) increases.

Relieves the effect of sleeping pills and antihypertensive drugs. In conjunction with GCS and other NSAIDs increases the risk of developing their adverse reactions (bleeding inside the gastrointestinal tract), and in addition the toxic properties of methotrexate and nephrotoxic effects of cyclosporine.

Aspirin weakens the blood concentration of diclofenac. And when combined with paracetamol, the risk of developing nephrotoxic properties of the active component of Naclofen increases.

In conjunction with antidiabetic drugs, hypo- or hyperglycemia may develop. In the case of combining Naklofen with these drugs, you need to carefully monitor the level of glucose in the blood.

Due to the combination with cefotetan, cefamandol, plikamycin, as well as cefoperazone and valproic acid, the frequency of hypoprothrombinemia increases.

The effect of diclofenac on the processes of synthesis of PG within the kidneys increases in conjunction with cyclosporine and gold preparations - as a result, its nephrotoxic properties increase.

Selective inhibitors of reverse serotonin capture increase the risk of bleeding in the gastrointestinal tract.

In the case of combination with St. John's wort, as well as substances such as colchicine, ethanol and corticotropin, the risk of bleeding in the gastrointestinal tract increases.

Drugs that promote the development of photosensitivity, enhance the sensitizing effect of diclofenac in relation to UV radiation.

The tubular secretion blockers increase the plasma diclofenac concentration, thereby increasing its toxicity.

Included in the category of quinolone antibacterial agents increase the risk of seizures.

[27], [28], [29], [30]

Storage conditions

You need to keep the medicine in standard conditions for medicines, in a place inaccessible to children. The temperature regime is a maximum of 30 ° C.

[31]

Shelf life

Naklofen is allowed to be used for 3 years from the date of manufacture of the medicine.

[32]