Naclofen

Naklofen is a drug from the NSAID category, a derivative of α-toluic acid. Its properties include pain relief, anti-inflammatory and antipyretic.

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Indications Naclofen

Among the indications:

• degenerative pathologies or inflammatory processes in the musculoskeletal system. These are diseases such as juvenile, rheumatoid and psoriatic forms of arthritis in the chronic stage, as well as Bechterew's disease, reactive and gouty forms of arthritis. Also with rheumatism of soft tissues, osteoarthrosis of the spine together with peripheral joints (may be accompanied by Minor's symptom), as well as with bursitis, tendovaginitis, inflammation of skeletal muscles, periarthritis and synovitis;
• mild or moderate pain in myalgia, neuralgia, and also lumbosciatica. Also in post-traumatic pain, with inflammatory processes on their background, in toothache and headache, pain after surgery. In addition, in migraine, dysmenorrhea, inflammation of the appendages, proctitis, biliary or renal colic;
• as part of a comprehensive treatment for ENT diseases of an infectious and inflammatory nature, in which severe pain is felt (such as otitis, pharyngitis, and tonsillitis);
• fever.

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Release form

Available in the form of capsules with modified release. The volume of capsules is 75 mg. There are 10 capsules on one blister, and 2 blister strips in one package.

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Pharmacodynamics

The active component of the drug is sodium diclofenac. It affects the body as follows - non-selectively suppresses the activity of the enzymes COX-1, as well as COX-2, as a result of which the process of metabolism of eicosatetraenoic acid is disrupted, as well as the processes of synthesis of thromboxane, as well as PG and prostacyclin are reduced. The concentration of various PGs in the synovial fluid, urine, and gastric mucosa decreases.

It is most effective in eliminating pain that develops as a result of inflammatory processes. In the treatment of rheumatic pathologies, the analgesic and anti-inflammatory properties of diclofenac help reduce the intensity of pain, swelling and noticeable stiffness of the joints in the morning - this increases the functional capacity of the joint. The active substance also helps reduce inflammation and pain in the period after surgery, as well as in case of injuries.

Like other NSAIDs, diclofenac has antiplatelet properties. In therapeutic dosages, it has almost no effect on blood flow processes. In case of long-term therapy, the effectiveness of the active component does not weaken.

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Pharmacokinetics

The active substance is absorbed completely and quickly. The peak plasma concentration is reached 0.5-1 hour after use. This indicator is linearly dependent on the amount of the drug dose introduced into the body.

With repeated use of the drug, no changes in the pharmacokinetics of the active substance are noted. If you observe the required interval between doses of the drug, it does not accumulate in the body. The bioavailability index is 50%, and it binds to plasma proteins by more than 99% (the main part - to albumins). The substance passes into the synovial fluid, and reaches its peak concentration in it 2-4 hours later than in the plasma. The time of diclofenac elimination from plasma will also be shorter.

As a result of the 1st passage in the liver, about 50% of the active component undergoes a metabolic process, which develops as a result of single/multiple hydroxylation processes, as well as conjugation with glucuronic acid. The P450CYP2C9 enzyme system is also a participant in metabolic processes. The decay products have lower pharmacological activity than the active component of the drug.

The systemic Cl is 260 ml/min, and the distribution volume is 550 ml/kg. The plasma half-life of the substance is 2 hours. Approximately 70% of the dose taken 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 remainder is excreted in the bile in the form of decay products.

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Dosing and administration

The medicine should be taken orally, swallowing the capsule without chewing and washing it down with water. This should be done at the end of a meal or immediately after it (preferably in the morning). Dosages are determined individually, in accordance with the severity of the pathology. For adults, the dose is usually 1 capsule 1-2 times a day. No more than 150 mg of the medicine can be taken per day.

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Use Naclofen during pregnancy

The 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, the use of Naklofen is prohibited in any case.

Contraindications

Among the contraindications:

• individual intolerance to diclofenac;
• a combination (in partial or complete form) of bronchial asthma, nasal polyposis with paranasal sinuses (in recurrent form), as well as hypersensitivity to aspirin and other NSAIDs (also in the anamnesis);
• postoperative period after coronary artery bypass grafting;
• the presence of ulcers and erosions on the mucous membranes of the duodenum or stomach, as well as active bleeding in the gastrointestinal tract;
• aggravated inflammation in the intestines (such as non-specific ulcerative colitis, as well as regional enteritis);
• cerebrovascular or other form of bleeding, as well as hemostasis disorders;
• severe liver failure or active liver pathology;
• severe renal failure (creatinine Cl is less than 30 ml/minute), diagnosed hyperkalemia, as well as kidney disease in a progressive stage;
• decompensated form of heart failure;
• suppression of hematopoietic processes in the bone marrow;
• children under 18 years of age.

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Side effects Naclofen

Taking the medicine may lead to the development of the following side effects:

• Digestive system organs: often - vomiting with nausea, pain in the epigastrium, abdominal pain syndrome, dyspeptic symptoms, diarrhea, bloating. In addition, also anorexia and increased transaminase activity. In rare situations, bleeding develops in the gastrointestinal tract (diarrhea or vomiting with blood, as well as melena are observed). In addition, such disorders as gastritis, ulcerative processes in the gastrointestinal tract (with / without perforation or bleeding) can develop, as well as jaundice with hepatitis and liver dysfunction. Isolated - dry mucous membranes (also in the oral cavity), glossitis and stomatitis, as well as esophageal injuries, diaphragm-like intestinal strictures (non-specific form of hemorrhagic colitis, exacerbated ulcerative colitis or regional enteritis), pancreatitis, constipation and hepatitis with a fulminant course;
• NS organs: often – dizziness or headaches. Rarely – a feeling of drowsiness. Sensitivity disorders (for example, paresthesia) appear sporadically, convulsions, tremors, memory problems, and anxiety develop. In addition, cerebrovascular disorders, aseptic meningitis, a feeling of depression, development of insomnia, disorientation, and the appearance of nightmares. Also a feeling of excitement or irritability and mental disorders;
• sensory organs: vertigo often develops. Visual disturbances (diplopia or blurring), taste or hearing disturbances are occasionally observed, and tinnitus may appear;
• urinary system organs: hematuria, acute renal failure, tubulointerstitial nephritis, in addition to proteinuria and nephrotic syndrome, necrotic papillitis, and edema may develop occasionally;
• organs of the hematopoietic system: thrombocyto- or leukopenia, aplastic or hemolytic anemia, eosinophilia, and in addition agranulocytosis are observed in isolated cases;
• allergy: anaphylactoid and anaphylactic reactions (including a noticeable decrease in blood pressure, as well as a state of shock). Isolated cases – development of Quincke's edema (also on the face). The allergic reaction is provoked by the substances contained in the drug: methyl parahydroxybenzoate, as well as propyl parahydroxybenzoate;
• cardiovascular system organs: tachycardia, problems with heart rhythm, pain inside the chest, extrasystole, increased blood pressure develop occasionally. In addition, heart failure, as well as vasculitis or myocardial infarction, may develop;
• respiratory organs: in rare situations, the appearance of cough or bronchial asthma (also dyspnea); isolated cases – development of laryngeal edema or pneumonitis;
• Skin: mainly skin rashes develop. In rare situations, urticaria may occur. Isolated disorders such as bullous rash and eczema (including polyform eczema) are observed. In addition, malignant exudative erythema, toxic epidermal necrolysis, skin itching, exfoliative dermatitis, alopecia, photophobia, and purpura (possibly in an allergic form).

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Overdose

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

To eliminate the disorders, it is necessary to wash the stomach and drink activated carbon, and in addition to this, carry out symptomatic treatment. The effectiveness of hemodialysis and forced diuresis procedures is very low, since with an overdose, significant binding to proteins occurs, and an intensive metabolism is also observed.

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Interactions with other drugs

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

Reduces the effect of sleeping pills and antihypertensive drugs. In combination with GCS and other NSAIDs, it increases the risk of developing their side effects (bleeding inside the gastrointestinal tract), as well as the toxic properties of methotrexate and the nephrotoxic effect of cyclosporine.

Aspirin reduces the blood concentration of diclofenac. And when combined with paracetamol, the risk of nephrotoxic properties of the active component of Naklofen increases.

In combination with antidiabetic drugs, hypo- or hyperglycemia may develop. In case of combining Naklofen with these drugs, it is necessary to carefully monitor the blood glucose level.

Due to the combination with cefotetan, cefamandole, plicamycin, as well as cefoperazone and valproic acid, the incidence of hypoprothrombinemia increases.

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

Selective serotonin reuptake inhibitors increase the risk of gastrointestinal bleeding.

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

Medicines that provoke the development of photosensitivity enhance the sensitizing effect of diclofenac in relation to UV radiation.

Tubular secretion blockers increase the plasma concentration of diclofenac, thereby increasing its toxicity.

Antibacterial agents in the quinolone class increase the risk of developing seizures.

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Storage conditions

The medicine should be kept in standard conditions for medicines, in a place inaccessible to children. Temperature conditions – maximum 30°C.

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Shelf life

Naklofen is permitted to be used for 3 years from the date of manufacture of the drug.

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