Amelotex tablets belong to the group of non-steroidal anti-inflammatory drugs. Thanks to their anti-inflammatory, analgesic and antipyretic properties and the rapid absorption of the active substance in the gastrointestinal tract, their use can quickly relieve pain in various joint diseases.
Composition of the medicine
In Amelotex biconvex tablets, the instructions indicate this, the main active ingredient is meloxicam. The drug may contain 7.5 or 15 mg. In the production of tablets, various additional substances are used, all of which are indicated in the manufacturer's instructions.
Both types of tablets have a rough surface. Depending on the manufacturer, they may have a pale yellow or slightly greenish tint. Sometimes the appearance of their surface is slightly marbling. The 15 mg tablets have a score on one side.
Main substance
The main active ingredient is meloxicam. It is a representative of the group of non-selective cyclooxygenase inhibitors, that is, it blocks the production of prostaglandins, the number of which increases significantly during the progression of inflammatory processes.
The solution in ampoules may have a greenish tint, although it is mostly transparent. Amelotex does not contain hormones and belongs to the group of non-steroidal (non-hormonal) anti-inflammatory drugs.
Effect of the drug
The main active ingredient can suppress the production of prostaglandins, which are mediators of inflammation. This provides the anti-inflammatory and analgesic properties of the drug.
Meloxicam is characterized by rapid absorption from the gastrointestinal tract. This feature persists regardless of food intake. At the same time, clinical studies of the drug have confirmed that side effects from the digestive system when taking the drug occur much less frequently compared to other NSAIDs. Bioavailability after taking the tablets is 90%. In this case, the maximum concentration in the blood is observed after approximately 2 hours.
Amelotex, 15 mg, tablets, 20 pcs.
Solution for intramuscular administration
Communication with plasma proteins - 99%. Passes through histohematic barriers and penetrates into the synovial fluid. Concentration in synovial fluid reaches 50% of Cmax in plasma.
It is excreted equally through the intestines and kidneys, mainly in the form of metabolites. Less than 5% of the daily dose is excreted unchanged through the intestines; the drug is found unchanged in urine only in trace amounts. T1/2 of meloxicam is 15–20 hours. Plasma clearance averages 8 ml/min. In elderly people, drug clearance is reduced. Vd is low and averages 11 liters. Hepatic or renal failure of moderate severity does not have a significant effect on the pharmacokinetics of meloxicam.
Pills
Well absorbed from the gastrointestinal tract, the absolute bioavailability of meloxicam is 89%. Concomitant food intake does not alter absorption. When using the drug orally in doses of 7.5 and 15 mg, its concentrations are proportional to the doses. Css are reached within 3–5 days. With long-term use of the drug (more than 1 year), concentrations are similar to those observed after the first achievement of Css. The range of differences between Cmax and basal concentrations of the drug after taking it once a day is relatively small and is 0.4–1 mcg/ml when using a dose of 7.5 mg, and 0.8–2 mcg/ml when using a dose of 15 mg. ml (the values of Cmin and Cmax are given, respectively).
Almost completely metabolized in the liver to form four pharmacologically inactive derivatives. The main metabolite, 5′-carboxymeloxicam (60% of the dose), is formed by oxidation of an intermediate metabolite, 5′-hydroxymethylmeloxicam, which is also excreted, but to a lesser extent (9% of the dose). In vitro studies
showed that the CYP2C9 isoenzyme plays an important role in this metabolic transformation; the CYP3A4 isoenzyme is of additional importance. Peroxidase is involved in the formation of the other two metabolites (constituting 16 and 4% of the drug dose, respectively), the activity of which probably varies individually.
It is excreted equally through the intestines and kidneys, mainly in the form of metabolites. Less than 5% of the daily dose is excreted unchanged through the intestines; the drug is found unchanged in urine only in trace amounts. T1/2 of meloxicam is 15–20 hours. Plasma clearance averages 8 ml/min. In elderly people, drug clearance is reduced. Vd is low and averages 11 liters. Hepatic or renal failure of moderate severity does not have a significant effect on the pharmacokinetics of meloxicam.
Gel for external use
Studies on rabbits have shown that meloxicam in the form of a gel when applied cutaneously is characterized by prolonged transdermal absorption, prolonged circulation in the blood and gradual elimination, significantly different in kinetic characteristics from the intramuscular route of administration of the drug. There is no data indicating significant absorption of meloxicam into the systemic circulation.
In the systemic circulation, meloxicam binds tightly to plasma proteins, mainly albumin (99%). It undergoes biotransformation in the liver with the formation of inactive metabolites. It is excreted mainly in the form of metabolites in urine and feces in approximately equal proportions.
Indications for use
Amelotex tablets, the instructions for use indicate this, are used for symptomatic therapy. They can reduce the intensity of pain in various inflammatory and degenerative joint diseases. The medicine has no effect on the progression of the disease.
In particular, the drug is prescribed for:
- Osteoarthritis, which is characterized by the destruction of articular cartilage.
- Rheumatoid arthritis, which is a chronic disease affecting the joints.
- Ankylosing spondylitis, which is manifested by inflammation of the intervertebral joints, which leads to immobility.
Indications for use
For all drugs in the NSAID group, the direction of action comes down to three basic principles:
- reduce fever;
- eliminate pain;
- relieve inflammation.
But each individual drug in this group has a more pronounced effect and is less active in relation to others. Amelotex works well in reducing the severity of pain in arthritis and arthrosis. In addition, this remedy successfully fights inflammatory processes, so the main indications for use are:
- Ankylosing spondylitis or ankylosing spondylitis;
- inflammatory diseases of the joints;
- degenerative changes in joint tissue;
- rheumatoid arthritis;
- osteoarthritis.
Amelotex does not treat the disease that caused pain and inflammation in the joint. It is a means of symptomatic therapy, allowing you to relieve unpleasant pain while the medication is in effect.
Despite the fact that Amelotex is a drug of the NSAID group, it is not prescribed for fever. It cannot be called an effective antipyretic. Meloxicam does not have a pronounced effect on the thermoregulation center, and therefore its antipyretic abilities are extremely ineffective. The main focus of the product is pain in diseases of the joint tissue.
Amelotex: rules of admission
The Amelotex tablet, the instructions for use confirm this, should be taken once a day. It is advisable to do this during meals.
The recommended dosage for adults depends on the type of disease that causes pain. According to instructions:
- For rheumatoid arthritis, take 15 mg per day. If it is possible to achieve the desired result, then the dose is reduced by 2 times.
- For osteoarthritis, 7.5 mg is prescribed. But if the pain intensity persists, the dosage is doubled.
- For ankylosing spondylitis, 15 mg per day is indicated.
To exclude an overdose or the occurrence of adverse negative reactions of the body, you should not take more than one 15 mg tablet per day. In case of severe renal failure, the maximum dose should not exceed 7.5 mg per day. This limitation also applies to patients who are on hemodialysis, as well as in cases where, due to the characteristics of the body, the risks of unpleasant side reactions increase.
For children aged 3-12 years, the permissible daily dose is reduced to ½ tablet of 7.5 mg. In this case, the amount of the drug for treatment up to the age of 14 years is calculated at the rate of 0.25 mg/kg.
Special conditions of admission
If symptomatic treatment cannot be carried out without the participation of non-steroidal anti-inflammatory drugs of the first group, it is necessary to assess the risks of side effects, especially in patients over 65 years of age. Patients with a high risk of adverse reactions from the gastrointestinal tract and older patients should be prescribed a drug that protects the mucous membranes of the gastrointestinal tract from damage as a complex therapy. For example, Nolpaza.
If a patient, while taking Amelotex, notices changes in the skin in the form of irritation, redness, itching or rash, it is necessary to consider options for replacing symptomatic therapy.
Contraindications and possible adverse reactions of the body
An absolute contraindication is individual intolerance to the main active ingredient and hypersensitivity to other components of the drug. The instructions for use indicate that amelotex should not be used to relieve pain during pregnancy and lactation.
The drug is also contraindicated in many other pathologies. Therefore, only a doctor should prescribe it, taking into account the patient’s condition. Increased caution should be observed in case of chronic heart failure, diabetes mellitus, when infection with the bacterium Helicobacter pylori is confirmed, etc.
Negative reactions of the body when taking the drug are most often associated with problems with the functioning of the digestive system. Nausea, diarrhea, and increased gas formation may occur. The instructions also list other dangerous reactions of the body: the development of gastritis, colitis, gastrointestinal bleeding, etc.
There are also warnings about possible negative reactions from other systems and organs of the human body. But, as a rule, the risks of their occurrence increase if medical recommendations are not followed. In any case, if any negative effects occur, you should stop taking the drug and consult a doctor about replacing the drug.
Contraindications
Due to the fact that Amelotex is a non-selective COX-1 inhibitor, its use, along with symptomatic treatment, carries a number of side effects, on the basis of which contraindications are formed:
- patient age over 60 years;
- ulcerative colitis;
- active or history of gastric bleeding;
- erosion of the gastric mucosa;
- kidney failure requiring dialysis;
- gestation period;
- lactation period;
- liver diseases in the active phase;
- patient age under 15 years
- bleeding from the rectum.
Long courses of taking the drug are unacceptable. In case of prolonged inflammation or prolonged pain, it is necessary to consult a specialist to identify the cause and prescribe adequate treatment for joint diseases.
Overdose
An overdose of the drug can lead to the development of conditions that threaten health. When the medication exceeds the permissible limit, it causes abdominal pain, severe nausea and vomiting. Against the background of a deterioration in the general condition, confusion is noted. In severe cases, renal and liver failure develops, and respiratory and cardiac arrest occurs.
To stabilize the condition, it is recommended to perform gastric lavage and take sorbents. An enhanced drinking regime should be ensured. Other symptomatic therapy is also recommended. Cholestyramine allows you to speed up the removal of amelotex from the body. Hemodialysis is considered ineffective due to the high binding of the active substance to blood proteins.
