Larfix

Larfix is a drug from the NSAID group.

Indications Larfixa

It is used in the following cases:

• for short-term relief of acute pain of moderate or mild severity;
• to eliminate symptoms of inflammation, as well as pain in rheumatoid arthritis or osteoarthritis.

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Release form

The release occurs in tablets, 10 pieces per blister cell. A separate pack contains 3 or 10 blister plates.

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Pharmacodynamics

The substance lornoxicam is an NSAID with anti-inflammatory and analgesic effects. It belongs to the oxicams group.

The active component inhibits the process of PG binding (slowing down the COX enzyme), resulting in desensitization of peripheral nociceptors, as well as slowing down of the inflammatory process. In addition, lornoxicam has a central effect on nociceptors not associated with the anti-inflammatory effect. At the same time, the drug does not affect vital parameters (such as heart rate, respiratory rate, temperature, ECG, blood pressure and spirometry).

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Pharmacokinetics

Suction.

The drug is rapidly and almost completely absorbed in the gastrointestinal tract. The substance reaches peak values in plasma 1-2 hours after taking the drug. The bioavailability of lornoxicam is 90-100%. There is no first-pass effect. Half-life is about 3-4 hours.

When taken with food, peak drug values are reduced by approximately 30% and the time to reach the peak is extended to 2.3 hours. AUC values may also decrease by up to 20%.

Distribution.

Inside the plasma, the substance remains unchanged, as well as in the form of an inactive hydroxylated decay product. Plasma synthesis of the substance with proteins is 99%. This indicator does not depend on the concentration level of the drug.

Metabolic processes.

Lornoxicam undergoes extensive hepatic metabolism via the process of hydroxylation, being converted first to the inactive moiety 5-hydroxylornoxicam.

The substance also undergoes biotransformation, in which the hemoprotein CYP2C9 is involved. Due to the existing genetic polymorphism, some people may have an intensive or slow metabolism of this enzyme, which is expressed in a significant increase in plasma lornoxicam indicators (if the metabolism is slow). The hydroxylated decay product exhibits medicinal activity. The active component is completely metabolized. About 2/3 is excreted by the liver, and another 1/3 by the kidneys in the form of inactive elements.

The drug did not provoke the induction of liver enzymes during preclinical tests. There is no information on the accumulation of the active substance as a result of repeated administration of standard doses of the drug.

Excretion.

The half-life of the active ingredient is approximately 3-4 hours. Approximately 50% of the drug is excreted with feces, and another 42% is excreted by the kidneys. Excretion occurs mainly in the form of the element 5-hydroxylornoxicam. The half-life of the component 5-hydroxylornoxicam is approximately 9 hours - with parenteral use of the drug 1-2 times a day.

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Dosing and administration

The tablets are taken orally with water. The medicine should be taken before meals. The dose is determined by the doctor.

In case of pain development, it is necessary to take the drug 2-3 times a day in the amount of 4-8 mg. It is allowed to take no more than 16 mg per day.

To eliminate rheumatic pathologies, against the background of which pain and inflammation occur, 4 mg of the drug is required, 2-3 times a day. A maximum of 12 mg of the drug is taken per day.

Taking into account the nature of the disease, as well as the individual indicators of the patient, the dose size may change, but only the attending physician can make adjustments.

Elderly patients (and also those with liver/kidney problems) are required to take a maximum of 12 mg of Larfix per day.

If the patient requires long-term treatment, it is necessary to monitor liver and kidney function, as well as blood values.

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Use Larfixa during pregnancy

The use of the drug in the 1st and 2nd trimesters has not been tested, so its use during these periods is prohibited.

It is also prohibited to use Larfix in the 3rd trimester.

There is no information about the passage of the drug into breast milk, so it is not prescribed to nursing mothers.

Lornoxicam may impair fertility.

Contraindications

Among the contraindications:

• presence of hypersensitivity to the elements of Larfix;
• intolerance to non-narcotic painkillers (the so-called aspirin triad);
• severe heart failure;
• thrombocytopenia;
• bleeding and disorders of the hematological type (this also includes cerebral bleeding);
• the presence of bleeding or perforation within the gastrointestinal tract (also if there is a history of such a disorder) associated with the use of NSAIDs;
• peptic ulcer (current or history);
• severe liver or urinary insufficiency;
• appointment for children;
• presence of chickenpox.

If the drug is prescribed to people who have recently undergone complex surgeries, and in addition to this, to people who have heart failure or are taking diuretics, it is recommended that they regularly monitor their kidney function.

It is necessary to prescribe the medicine with caution to people with problems in the liver or kidneys (to a moderate degree). Also, caution is necessary when using it in people with poor blood clotting (treatment is allowed only with constant monitoring of blood values). The drug is also prescribed to elderly people with caution.

With certain restrictions, the drug can be used in the following conditions in patients:

• tendency to develop swelling;
• smoking, elevated blood pressure, elevated plasma lipid levels and diabetes mellitus;
• bronchial asthma;
• Libman-Sachs disease;
• tendency to bleeding.

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Side effects Larfixa

Most often, the use of drugs results in side effects typical of non-narcotic painkillers - for example, vomiting (sometimes bloody), ulcerative stomatitis, dyspeptic symptoms, melena, bloating, problems with stool, and in addition, exacerbation of regional enteritis and colitis. Some manifestations may be symptoms of perforation inside the gastrointestinal tract - in this case, urgent medical assistance is needed (for example, with acute abdominal pain, melena and bloody vomiting).

In addition, the following disorders were observed when using Larfix:

• infectious processes: development of pharyngitis;
• disorders of the hematopoietic system: the appearance of anemia (sometimes hemolytic type), thrombocytopenia, neutro-, leukopenia or pancytopenia, and in addition to this, agranulocytosis or ecchymosis, as well as coagulation disorders;
• metabolic disorders: occurrence of hyponatremia, problems with appetite and weight changes;
• CNS dysfunction: a feeling of anxiety, drowsiness or excitability, development of insomnia, cognitive impairment, depression, headaches, migraines and tremors. In addition, there are disorders of consciousness and problems with concentration, dizziness and cognitive impairment, as well as hyperkinesia and dysgeusia. Rarely, aseptic meningitis occurs (in people with connective tissue diseases);
• dysfunction of the cardiovascular system: the appearance of tachycardia, swelling, facial hyperemia, hot flashes, vasculitis and hematomas, as well as fluid retention, irregular heartbeat, heart failure and increased blood pressure;
• sensory problems: blurred vision, decreased vision, color vision problems, conjunctivitis, diplopia, scotoma, lazy eye, as well as anterior uveitis, vertigo and tinnitus;
• gastrointestinal disorders: nausea, belching, development of gastric or intestinal ulcers or gastritis, and dryness or ulceration of the oral mucosa, and in addition, bleeding gums. Dysphagia, GERD, esophagitis and glossitis may also appear, as well as hemorrhoids or aphthous stomatitis;
• damage to the hepatobiliary system: liver intoxication, cholestasis and jaundice, as well as liver failure, hepatitis and increased ALT and AST levels;
• Allergy symptoms: rash, urticaria, increased sweating and hyperthermia. Alopecia, chills, erythema, angioedema, anaphylaxis, as well as dyspnea, bronchospasm and rhinitis may occur. Along with this, TEN, Stevens-Johnson syndrome, purpura and bullous rash may occur.

As a result of taking the pills, musculoskeletal diseases may develop (muscle pain and spasms, pain in the back, joints or bones, as well as myasthenia). In addition, there is a risk of developing urinary system diseases (problems with urination, hyperuricemia or nocturia, as well as acute renal failure (if there are pathologies in the urinary system), hypercreatininemia, nephrotic syndrome, necrotic papillitis and nephritis).

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Overdose

As a result of poisoning with Larfix, cerebral manifestations (dizziness and visual disturbances) develop, convulsions, nausea with vomiting, as well as ataxia and a state of coma appear. In addition, due to an overdose, blood clotting may be disrupted and liver function may be impaired.

In case of poisoning, it is necessary to stop taking the drug. Since the drug has a short half-life, it is quickly eliminated from the body. The dialysis procedure does not reduce the serum values of the substance.

There is no information about the existence of a special antidote. If less than 20 minutes have passed since the moment of intoxication, gastric lavage can be performed and the victim can be given sorbents.

Treatment may also be prescribed to reduce the symptoms of poisoning.

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Interactions with other drugs

When the drug is used simultaneously with cimetidine, serum lornoxicam levels increase.

Larfix is able to enhance the properties of anticoagulants, as well as prolong the bleeding time in the case of a combination of these drugs.

The drug weakens the effects of phenprocoumone, diuretics, ACE inhibitors, drugs that block angiotensin II, and in addition, β-blockers.

As a result of epidural or spinal anesthesia, individuals who are also taking heparin may have an increased risk of developing a hematoma.

The combination of Larfix with digoxin reduces the excretion of the latter through the kidneys.

GCS taken together with Larfix increases the risk of bleeding and ulcers inside the gastrointestinal tract.

The combination of the drug with drugs from the quinolone category increases the possibility of developing seizures.

Thrombolytics, serotonin reuptake inhibitors, and non-narcotic painkillers when combined with Larfix increase the likelihood of bleeding within the gastrointestinal tract.

Lornoxicam enhances the toxic properties of cyclosporine with methotrexate, as well as lithium drugs and pemetrexed.

The drug is capable of enhancing the antidiabetic properties of sulfonylurea derivative drugs.

The development of interactions between lornoxicam and inducers or inhibitors of the CYP2 C9 element should be expected.

The drug in combination with tacrolimus can increase nephrotoxicity (by reducing renal production of prostacyclin).

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Storage conditions

Larfix must be kept in standard conditions for medicines. Temperature level – maximum 25°C.

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Special instructions

Reviews

Larfix receives mostly positive reviews, which indicate the fairly high effectiveness of this drug.

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Shelf life

2 years.

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