Naclofen Duo

Naklofen Duo is a medicine from the NSAID category.

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Indications Naclofen Duo

Shown for:

• inflammations of rheumatic origin - such pathologies as rheumatoid arthritis, Bechterew's disease, osteoarthritis, as well as spondyloarthritis, non-articular rheumatism and pain in different places;
• swelling, inflammation and pain syndromes that occur after operations and injuries;
• gynecological inflammations or pains (for example, such as primary dysmenorrhea or inflammation of the appendages).

In addition, Naklofen Duo is a good remedy for relieving migraine attacks.

Release form

Available in capsules, 10 pieces inside one blister. One pack contains 2 blister strips.

Pharmacodynamics

Diclofenac is the active component of the drug - it is a non-steroidal compound with powerful antipyretic, anti-inflammatory, analgesic and antirheumatic properties. Experiments have shown that the main active mechanism of the substance is to slow down the process of binding PG. These elements are important components of the development of inflammatory processes, pain and fever.

In vitro tests have shown that diclofenac sodium in amounts similar to those achieved during treatment does not inhibit proteoglycan biosynthesis within cartilage tissue.

During the treatment of rheumatic pathologies, the pain-relieving and anti-inflammatory properties of the drug significantly reduce the intensity of pain (not only during movement, but also at rest), the feeling of stiffness in the morning, and swelling in the joints. This allows for a significant improvement in the patient's condition.

When eliminating inflammatory processes that have arisen due to surgery or injury, the drug removes spontaneous pain, as well as pain that occurs during movement. It also helps reduce inflammatory swelling inside the tissues, as well as swelling in the areas of surgical sutures. The use of Naklofen Duo allows you to reduce the body's need for opioid drugs, which are used to eliminate pain after surgery.

During clinical trials, it was found that the drug has a powerful analgesic effect in eliminating severe or moderate pain of non-rheumatic origin. Testing also revealed that the drug can relieve pain and reduce blood loss during the treatment of primary dysmenorrhea.

Pharmacokinetics

When taken orally, the drug is absorbed fairly quickly, and its rate exceeds 90%, although due to primary hepatic metabolism, the bioavailability level is only 60%. The peak serum level of the drug is observed after 1-4 hours (the specific time depends on the type of drug).

Since diclofenac is absorbed within the small intestine and duodenum, food slows its absorption, causing peak serum levels of the active ingredient to be reduced and delayed. Although food slows the rate of absorption, it does not affect the extent of this process. Food does not affect plasma levels of diclofenac upon repeated administration.

Synthesis of diclofenac with plasma protein is 99% (mainly binding to albumins).

The active substance easily passes into the synovial fluid, the values in which are equal to 60-70% of the serum values. After 3-6 hours, the level of the substance and its decay products in the synovial fluid begin to exceed the serum values. Excretion of diclofenac from the synovial fluid occurs much slower than a similar process in the serum.

The half-life of the substance is 1-2 hours. A similar indicator is observed in patients with kidney or liver failure.

The drug is almost completely metabolized in the liver (methoxylation and hydroxylation processes are predominant). About 70% of the substance is excreted in the urine in the form of pharmacologically inactive decay products. Only 1% is excreted unchanged. Other decay products are excreted in the feces and bile.

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Dosing and administration

At the initial stage of treatment, it is recommended to take 75-150 mg per day (1-2 capsules of LS). A more precise dose depends on the severity of the manifestations of the pathology. During a long course, it is often enough to take 1 capsule of LS per day. If the signs of the disease are most pronounced at night or in the morning, it is necessary to take the medicine in the evening.

The capsules must be swallowed whole with water. It is recommended to do this with or immediately after meals.

It is recommended to use drugs in the most effective dosages over a short period of time, while taking into account the individual treatment indications of each patient.

Use Naclofen Duo during pregnancy

It is allowed to use Naklofen Duo in the 1st and 2nd trimesters (but only in cases where the probable benefit to the woman outweighs the possible risks of negative consequences for the fetus). In the 3rd trimester, this medicine is completely contraindicated.

Contraindications

Among the contraindications:

• the patient has intolerance to diclofenac or other components of the drug;
• IHD in people with angina pectoris or a history of myocardial infarction;
• cerebrovascular pathologies in people who have had a stroke or in people who experience episodes of microstrokes;
• diseases of the peripheral arteries;
• active forms of gastric ulcers or duodenal ulcers, as well as perforation or bleeding in the gastrointestinal tract;
• congestive heart failure (NYHA II-IV);
• severe forms of renal failure (creatinine clearance level is <30 ml/minute) or liver failure (Child-Pugh category C; presence of ascites or cirrhosis);
• inflammatory intestinal diseases (ulcerative colitis or regional enteritis);
• elimination of perioperative pain that occurs during coronary artery bypass grafting (or in the case of the use of artificial cardiac output);
• lactation period;
• Prescription in childhood – since the capsules contain the active ingredient in high concentrations.

Naklofen Duo, like other NSAIDs, is prohibited for use in people suffering from urticaria, bronchial asthma, acute rhinitis, nasal polyps and other allergic reactions caused by the use of aspirin or other drugs that have the property of being able to slow down prostaglandin synthetase.

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Side effects Naclofen Duo

The use of drugs can cause the following side effects:

• Digestive tract organs: in some cases, diarrhea, nausea, abdominal pain, constipation, and bloating may occur. Occasionally, bleeding in the gastrointestinal tract may develop (melena, vomiting of blood, and diarrhea with blood), gastric or intestinal ulcers, which are accompanied/not accompanied by perforation/bleeding. Gastritis, anorexia, or vomiting may also develop. Colitis may occasionally appear (its ulcerative form becomes aggravated, a hemorrhagic form of the disease or regional enteritis develops), glossitis with stomatitis, as well as pancreatitis, esophageal dysfunction, and stenosis of diaphragmatic intestinal strictures;
• Digestive system organs: acute, active chronic or asymptomatic hepatitis occasionally develops, as well as jaundice, cholestasis and acute toxic hepatitis. Liver failure, liver dysfunction and increased transaminase levels may be observed. Fulminant hepatitis occurs occasionally;
• NS organs: dizziness or headaches occasionally occur. Less frequently, nightmares, paresthesia, disorientation, memory disorders and psychotic disorders occur. In addition, tremors, anxiety, and seizures occur. Taste disorders, aseptic meningitis, insomnia, stroke, fatigue, irritability, anxiety or drowsiness, as well as depression and asthma (including dyspnea) develop;
• kidneys and urinary system: renal failure (or its acute form), hematuria, and fluid retention occasionally develop. Pathologies such as tubulointerstitial nephritis, necrotic papillitis, nephrotic syndrome, and proteinuria are observed sporadically;
• organs of the immune system: in some cases, rashes or exanthema are observed; even more rarely, urticaria or itching may appear. Intolerance reactions, phototoxic or anaphylactic manifestations (including bronchospasm), Quincke's edema (anaphylaxis and facial swelling occur) and anaphylactoid manifestations develop occasionally;
• cardiovascular system: in rare cases, chest pain, palpitations, heart failure, vasculitis and myocardial infarction may occur, and blood pressure may increase; however, edema, heart failure and increased blood pressure were observed in combination with NSAIDs. Epidemiological data and clinical test results have shown that there is a high risk of thrombotic complications (including stroke or myocardial infarction) associated with the use of diclofenac (long-term use and use of high doses – 150 mg per day);
• lymph and hematopoietic system: leukopenia or thrombocytopenia, anemia (in aplastic or hemolytic form), and in addition agranulocytosis develop occasionally;
• visual organs: in rare situations, blurred or impaired vision is observed, diplopia develops;
• auditory organs: vertigo often appears, less often hearing impairment or tinnitus may develop;
• subcutaneous layer, as well as skin: mainly rashes appear; eczema, urticaria, bullous dermatitis, erythema (also of the polyform type) often develop, as well as Lyell's or Stevens-Johnson syndromes, alopecia, photosensitivity, itching and purpura (also in allergic form) and exfoliative dermatitis;
• organs of the sternum and mediastinum, as well as the respiratory tract: pneumonitis occasionally develops.

If severe side effects develop, treatment must be discontinued.

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Overdose

Acute overdose mainly affects the central nervous system and digestive tract, as well as the liver and kidneys. Symptoms include diarrhea and vomiting, nausea and epigastric pain, agitation, dizziness and tinnitus. Sometimes vomiting with blood, loss of consciousness, melena, kidney failure, and breathing problems and seizures may occur. In severe poisoning, liver damage may occur.

There is no specific antidote, so symptomatic and supportive treatment methods should be used to eliminate intoxication. This will help in getting rid of symptoms such as seizures, renal failure, respiratory depression, gastrointestinal disorders and decreased blood pressure. The probability that procedures such as hemodialysis and forced diuresis with hemoperfusion will help remove diclofenac from the body is quite low, because the components of this drug have a high synthesis rate with blood protein and also undergo an intensive metabolism process.

In case of using drugs in potentially toxic doses, it is necessary to drink activated charcoal, and in case of using doses that can be life-threatening, it is necessary to disinfect the stomach (for example, wash it out or induce vomiting).

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Interactions with other drugs

Naklofen Duo can increase plasma levels of digoxin and lithium. In the case of a combination of diclofenac with these drugs, it is necessary to monitor the levels of these substances in the body.

Like other NSAIDs, Naklofen Duo can inhibit the action of diuretics. When combined with potassium-sparing diuretics, serum potassium levels may increase (therefore, these values should be closely monitored). In addition, a combination with potassium drugs can also increase their level in the serum, which is why it is necessary to constantly monitor the patient's health.

Combination with antihypertensive and diuretic drugs (for example, with ACE inhibitors and β-blockers) can be carried out only with reservations, and people (especially the elderly) need to be closely monitored, assessing blood pressure indicators. It will also be necessary to obtain the necessary hydration, as well as monitoring the kidney function (not only during the combined treatment, but also after its completion - this is especially true for ACE inhibitors and diuretics, since they increase the risk of nephrotoxicity).

Although clinical trials have failed to establish the effect of diclofenac on the function of anticoagulants, there is some evidence that patients who combined these substances had an increased risk of bleeding. For this reason, careful monitoring of the patient is recommended with this type of treatment.

The combined use of NSAIDs with selective serotonin reuptake inhibitors may increase the risk of gastrointestinal bleeding.

Clinical trials have shown that diclofenac can be combined with antidiabetic drugs, as it does not change their medicinal effect. But there is information that sometimes hyper- or hypoglycemia developed with such a combination - in such cases, it is necessary to adjust the dosage of antidiabetic drugs. Also, during the treatment period, it is necessary to monitor blood sugar levels.

It is necessary to combine NSAIDs with methotrexate (within 24 hours before or after taking the latter) with caution, because in these cases its levels in the body may increase, as a result of which its toxic effect also increases.

The effect of NSAIDs (including Naklofen Duo) on the process of renal PG synthesis may increase the nephrotoxic properties of cyclosporine. As a result, people who use cyclosporine should take diclofenac in reduced doses.

There are isolated reports of seizures occurring in people who combine NSAIDs with quinoline derivatives.

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Storage conditions

The medicine should be kept in a place protected from moisture and out of reach of small children. The temperature values are a maximum of 30°C.

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Shelf life

Naklofen Duo is permitted to be used for a period of 3 years from the date of release of the drug.