Larix

Larix is a drug from the NSAID group.

Indications of the larixx

It is used in such cases:

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

[1], [2], [3],

Release form

The release takes place in tablets, 10 pieces inside a blister cell. In a separate pack contains 3 or 10 blister plates.

[4], [5], [6], [7]

Pharmacodynamics

The substance lornoxicam is an NSAID with an anti-inflammatory and analgesic effect. It is part of the group of oxycomas.

The active component inhibits the process of binding of PG (slowing down the enzyme of COX), resulting in desensitization of nociceptors of peripheral type, as well as slowing of the inflammatory process. In addition, lornoxicam has a central effect on nociceptors, not associated with anti-inflammatory effect. In this case, the medicine does not affect important for life indicators (such as heart rate, respiration rate, temperature, ECG, blood pressure level and spirometry).

[8], [9], [10], [11], [12], [13], [14]

Pharmacokinetics

Suction.

The medicine is quickly and almost completely absorbed inside the digestive tract. Peak values within the plasma material reaches after 1-2 hours after the use of drugs. The bioavailability level of lornoxicam is 90-100%. There is no effect of the 1st hepatic transit. Half-life is about 3-4 hours.

During simultaneous consumption with food, the peak values of drugs decrease by approximately 30%, and the peak time is extended to 2.3 hours. Indicators AUC can also fall to 20%.

Distribution.

Inside the plasma, the substance remains unchanged, and also 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 level of drug concentration.

Metabolic processes.

Lornoxicam undergoes active hepatic metabolism by the hydroxylation process, transforming first into an inactive element of 5-hydroxylornoxicam.

Also, the substance undergoes biotransformation, in which the hemoprotein CYP2S9 participates. Due to the existing genetic polymorphism, some people may have an intensive or delayed metabolism of this enzyme, expressed in a significant increase in plasma lornoxicam (if the metabolism is slowed down). The hydroxylated degradation product exhibits a drug activity. The active ingredient is completely metabolized. About 2/3 is excreted by the liver, and another 1/3 - by kidneys in the form of inactive elements.

The drug did not provoke the induction of liver enzymes during preclinical tests. Information on the accumulation of active substance as a result of multiple use of standard dosages of drugs is not available.

Excretion.

The half-life of the active ingredient is about 3-4 hours. Excretion with feces undergoes approximately 50% of the drug, and another 42% is excreted by the kidneys. In general, the excretion takes place in the form of an element of 5-hydroxylornoxicam. The half-life of the component 5-hydroxylornoxicam is approximately 9 hours - for parenteral drug use 1-2 times per day.

[15], [16], [17], [18], [19], [20], [21]

Dosing and administration

Tablets are consumed orally with water. It is necessary to take drugs before eating. The size of the dose is determined by the doctor

In the case of pain, it is required to take the drug 2-3 times / day in the amount of 4-8 mg. A day is allowed to take no more than 16 mg.

To eliminate rheumatic pathologies, against which pain and inflammation occur, 4 mg of the drug are required, 2-3 times per 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 parameters of the patient, the size of the dose may vary, but only the treating doctor can correct it.

Elderly patients (and in addition to those with liver / kidney problems) are required to take a maximum of 12 mg Larix for a day.

If the patient needs long-term treatment, it is necessary to monitor the liver's work with the kidneys, as well as the blood values.

[32], [33],

Use of the larixx during pregnancy

Testing of drug use in the 1 st and 2 nd trimester was not carried out, therefore it is prohibited to use it in these periods.

Apply Larfix at the 3rd trimester is also prohibited.

There is no information about the passage of the medicine into the mother's milk, therefore it is not prescribed to the nursing mothers.

Lornoxicam can weaken fertility.

Contraindications

Among the contraindications:

• Hypersensitivity to Larixx elements;
• intolerance to non-narcotic analgesic drugs (the so-called aspirin triad);
• heart failure in severe form;
• thrombocytopenia;
• bleeding and hematological disorders (this includes also cerebral bleeding);
• the presence of bleeding or perforation inside the gastrointestinal tract (also if such a history is present) associated with the use of NSAIDs;
• a peptic type ulcer (present or present in history);
• hepatic or urinary insufficiency in a marked degree;
• appointment to children;
• presence of chicken pox.

If it is necessary to prescribe drugs to people who have recently undergone complex surgical operations, and in addition to those who have heart failure or who take diuretics, they are recommended to regularly monitor kidney performance.

It is necessary to prescribe cautiously the medicine to people with problems in the work of the liver or kidneys (to a moderate extent). Also, caution is necessary when used in persons with poor blood circulation (treatment is allowed only with constant monitoring of blood values). Elderly medicine is also prescribed with care.

With certain limitations, the drug can be used in this condition in patients:

• propensity to develop edemas;
• smoking, increased blood pressure, increased plasma lipid values, and diabetes mellitus;
• bronchial asthma;
• Libmann-Sachs disease;
• tendency to bleeding.

[22], [23], [24], [25], [26]

Side effects of the larixx

Most often as a result of the use of drugs, there are side reactions that are typical for non-narcotic analgesics - for example, vomiting (sometimes bloody), ulcerative stomatitis, dyspeptic phenomena, melena, bloating, stool problems, and, in addition, exacerbation of regional enteritis and colitis . Individual manifestations may be symptoms of perforation inside the gastrointestinal tract - in this case, urgent medical attention is needed (for example, with acute abdominal pain, melena and bloody vomiting).

In addition, when using Larix, the following violations were observed:

• infectious processes: development of pharyngitis;
• disorders of the hematopoietic system: the appearance of anemia (sometimes hemolytic type), thrombocyto-, neutro-, leuko- or pancytopenia, and in addition to agranulocytosis or ecchymosis, as well as coagulation disorders;
• disorders of metabolic processes: the emergence of hyponatremia, problems with appetite and weight changes;
• lesions of the central nervous system: sensation of anxiety, drowsiness or excitability, development of insomnia, cognitive impairment, depression, headaches, migraine and tremor. In addition, there are disorders of consciousness and problems with concentration of attention, dizziness and cognitive impairment, as well as hyperkinesia and dysgeusia. Occasionally an aseptic form of meningitis occurs (in people with connective tissue diseases);
• disturbances of the function of SSS: the appearance of tachycardia, edemas, facial hyperemia, hot flashes, vasculitis and hematomas, and in addition, fluid retention, irregular heartbeat, heart failure and increased pressure;
• problems with the senses: blurred vision, visual impairment, color perception problems, conjunctivitis, diplopia, scotoma, lazy eye, as well as anterior uveitis, vertigo and ear ringing;
• disorders in the gastrointestinal tract: the appearance of nausea, eructation, the 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 can also occur, and in addition hemorrhoids or stomatitis of aphthous type;
• lesions of the hepatobiliary system: hepatic intoxication, cholestasis and jaundice, and in addition hepatic insufficiency, hepatitis and an increase in ALT and AST;
• allergy symptoms: rashes, urticaria, increased sweating and hyperthermia. Perhaps the appearance of alopecia, chills, erythema, angioedema, anaphylaxis, as well as dyspnea, bronchial spasm and runny nose. Together with this, there may occur TEN, Stevens-Johnson syndrome, purpura and bullous rash.

As a result of taking tablets, diseases of the ODA (muscle pains and spasms, pain in the back, joints or bones, as well as myasthenia gravis) can develop. In addition, there is a possible occurrence of diseases of the urination system (problems with urination, hyperuricemia or nocturia, as well as acute form of renal failure (if there are pathologies in the area of urinary organs), hypercreatininaemia, nephrotic syndrome, necrotic papillitis and nephritis).

[27], [28], [29], [30], [31],

Overdose

As a result of poisoning, Larixx develops cerebral manifestations (dizziness and visual disturbances), seizures, nausea with vomiting, as well as ataxia and coma. In addition, because of an overdose, blood circulation can be disturbed and there may be a breakdown in the liver.

In case of poisoning, you must cancel the drug taking. Since the drug has a short half-life, it is quickly excreted from the body. The dialysis procedure does not reduce the serum values of the substance.

There is no information about the existence of a specific antidote. At the end of intoxication less than 20 minutes, you can perform gastric lavage and give the victim sorbents.

Can also be prescribed treatment, designed to reduce the manifestations of poisoning.

[34], [35], [36]

Interactions with other drugs

With the simultaneous use of the drug with cimetidine, lornoxicam values within the serum are increased.

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

The drug weakens the effects of fenprocoumone, diuretics, ACE inhibitors, drugs blocking angiotensin II, and in addition to β-blockers.

As a result of performing epidural or spinal anesthesia to persons who also take heparin, it is possible to increase the probability of developing a hematoma.

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

GCS, taken with Larix, increases the likelihood of bleeding and ulcers inside the gastrointestinal tract.

Combination of the drug with funds from the category of quinolones increases the possibility of developing seizures.

Thrombolytics, drugs, inhibitors of reverse serotonin capture, as well as non-narcotic pain medication, combined with Larix, cause an increase in the likelihood of bleeding in the gastrointestinal tract.

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

The drug is able to enhance the antidiabetic properties of drug-derivatives of sulfonylurea.

We should expect the development of interaction between lornoxicam, as well as inductors or inhibitors of the CYP2 C9 element.

The drug in combination with tacrolimus can enhance nephrotoxicity (reducing renal excretion of prostacyclin).

[37], [38], [39]

Storage conditions

Larfix is required to be kept in standard for medicines conditions. The temperature level is a maximum of 25 ° C.

[40], [41], [42]

Special instructions

Reviews

Larix receives mostly positive reviews, which speak about the rather high effectiveness of this drug.

[43], [44], [45]

Shelf life

2 years.

[46], [47], [48], [49]