Composition, form of production and packaging
Capsules with modified release 1 caps.
acetemethacin 90 mg
10 pieces. - blisters from PVC / PVDH / aluminum foil (2) - packs cardboard.
10 pieces. - blisters of PVC / PVDC / aluminum foil (5) - packs of cardboard.
10 pieces. - blisters from PVC / PVDC / aluminum foil (10) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2013.
Acetecacin is a derivative of indolylacetic acid. Its pharmacological effect is partly due to the effect of indomethacin, the metabolite product of acetemethacin.
Acetetacin is an anti-inflammatory, analgesic and antipyretic agent and, like other anti-inflammatory drugs, suppresses platelet aggregation.
The anti-inflammatory effect of acetemethacin has been demonstrated in animal experiments on a large number of models of inflammation. Acemetazin acts at various stages of the inflammatory process. It was found that it inhibits the synthesis of prostaglandins and the release of histamine, and also acts as a bradykinin and serotonin antagonist. It also inhibits the activity of the complement system and the release of hyaluronidase.
The membrane-stabilizing property of acetemethacin prevents the release of proteolytic enzymes, leading to the suppression of exudative and proliferative inflammatory processes.
After ingestion, acetemethacin is absorbed quickly and completely.
Acetetacin accumulates in the area of вЂ‹вЂ‹inflammation.
It was found that after six days of treatment with acetemethacin (2 Г— 90 mg per day) or indometacin (3-50 mg per day) six hours after the last intake, the concentrations of the active substance were significantly higher in the synovial fluid, the synovial membrane, and in the muscles (a also in bone tissue after treatment with acetemethacin), compared to the concentrations found in the blood. In all studied tissues, except for synovial fluid and adipose tissue, after taking acetemethacin concentrations were higher than after taking indomethacin.
After taking one dose and after re-taking the drug, Rantudil Retard, acetemethacin and indomethacin, which is formed by the metabolism of acetylcin, are present in the blood in a ratio of 1: 1. There is no evidence of the induction of enzymes that destroy acetemethacin.
Acetetacin is excreted by the kidneys and with bile. 40% of the ingested drug is excreted through the kidneys, the remainder is excreted by the intestine. Acetecacin is excreted by the kidneys partially in unchanged form, partly as acetomethacin conjugated with glucuronic acid, in the form of metabolite indomethacin (free and conjugated), formed during esterolysis and after cleavage of the ester (in the methoxy group at position 5) and deacylation (decomposition of p-chlorobenzoyl group) in the form of a pharmacologically inactive compound.
Binding to proteins and half-life
Acetetacin binds to plasma proteins. The half-life is approximately 4.5 hours.
Concentrations in the blood
When using the drug with controlled release, the maximum concentration in the blood is reached much later (p <0.05) than when using other forms; concentration in the blood is also significantly lower (p <0.01) two hours after ingestion. However, at 6 and 10 hours, plasma-controlled concentrations of acetemethacin are significantly higher than those of other acetcemetin formulations.
Pain and impaired motor activity resulting from the following diseases:
- chronic rheumatoid arthritis (chronic polyarthritis), rheumatoid arthritis;
- Acute pain syndrome associated with degenerative joint disease, in particular large joints and spine (arthrosis, spondylarthrosis);
- Bechterew's disease (rheumatoid spondylitis);
- Gout attacks;
- inflammation of the joints, muscles and tendons, tendosinovitis, bursitis;
- lumbago, ischialgia;
- Inflammation of superficial veins (thrombophlebitis) and vasculitis;
- psoriatic arthritis;
- inflammation and swelling after surgery and trauma.
Capsules should be swallowed whole, with a sufficient amount of liquid while eating.
Recommended dose - 1 capsule 1-2 times a day.
Dosage regimen for gout attacks
The standard recommended dose for the treatment of acute gout attacks, before relieving symptoms, is 180 mg of acetylcin a day (corresponding to 2 capsules of Rantudil Retard).
The duration of treatment depends on the clinical picture, but therapy in doses exceeding 2 capsules of Rantudil Retard a day should last no more than 7 days.
The incidence of side effects is defined as follows (the number of patients who showed this reaction): very often:> 1/10; often: <1/10> 1/100; infrequently: <1/100> 1/1000; rarely: <1/1000> 1/10000; very rarely: <1/10000.
From the gastrointestinal tract: very often - dyspepsia: nausea, vomiting, flatulence, abdominal pain, loss of appetite; often: ulcerative lesions in the digestive tract, sometimes accompanied by bleeding and perforation; infrequently - the presence of blood in vomit masses, feces or with diarrhea; very rarely - stomatitis, inflammation of the tongue, lesion of the esophagus, exacerbation of Crohn's disease or ulcerative colitis, constipation, pancreatitis.
From the nervous system: often - CNS disorders, including headache, lethargy / fatigue, dizziness, drowsiness; very rarely - muscular asthenia, hyperhidrosis, dysgeusia, memory impairment, sleep disorders, convulsions.
From the cardiovascular system: very rarely - increased heart rate, angina pectoris, heart failure, hypertension.
On the part of the liver and biliary tract: often - increasing the level of liver enzymes; infrequently - liver damage (toxic hepatitis with or without jaundice); very rarely - a lightning course and sometimes without previous symptoms).
From the side of the circulatory system: very rarely - anemia caused by the loss of latent blood from the digestive tract, hemolytic anemia, pancytopenia (anemia, including aplastic anemia, leukopenia, agranulocytosis, thrombocytopenia). Initial symptoms may include fever, sore throat, superficial lesions in the oral cavity, flu-like conditions, severe fatigue, nosebleeds and subcutaneous bleeding. In these cases, you must immediately stop taking the drug and see a doctor. Do not take analgesics and / or antipyretics yourself. In the case of prolonged treatment, a blood test should be performed regularly. Possible effects on platelet aggregation and increased hemorrhagic diathesis.
From the immune system: often - reactions of hypersensitivity (rash and itching); infrequently - hives; very rarely severe hypersensitivity reactions: edema of the face or eyelids, swelling of the tongue, angioneurosis, respiratory distress, which can lead to asthma attack, lowering blood pressure; very rarely - allergic vasculitis and pneumonitis.
On the part of the endocrine system: very rarely - hyperglycemia and glucosuria.
On the part of the organs of vision: infrequently - degeneration of retinal pigment, opacification of the cornea of вЂ‹вЂ‹the eyes with prolonged use of indomethacin, the main metabolite of acetemethacin.
From the organs of hearing: very rarely - noise in the ears and hearing impairment.
From the skin and subcutaneous tissue: infrequently - alopecia; very rarely eczema, enanthema, erythema, photosensitivity, exfoliative dermatitis and bullous rash, which can also have severe course, for example, in the form of Stevens-Johnson syndrome and toxic epidermal necrolysis (Lyell's syndrome).
From the side of the urinary system: infrequently - the development of edema, in particular, in patients with hypertension and / or impaired renal function; very rarely - urination disorders, increased urea levels in the blood, acute renal failure, proteinuria, hematuria, interstitial nephritis, nephrotic syndrome, papillary necrosis. In this regard, the indicators of kidney function of the patient should be regularly monitored.
- hypersensitivity to the active substance - acetemethacin or indomethacin;
- violation of hematopoiesis of unknown etiology;
- complete or incomplete combination of bronchial asthma, recurrent nasal polyposis or paranasal sinuses and intolerance to acetylsalicylic acid and other NSAIDs (including in anamnesis);
- cerebrovascular or other bleeding, inflammatory bowel disease (Crohn's disease, ulcerative colitis) in the phase of exacerbation;
- any active liver disease, marked renal failure (CC less than 30 ml / min);
- confirmed hyperkalemia;
- erosive and ulcerative changes in the gastric mucosa and duodenum;
- Acute or recurrent peptic ulcer in history / bleeding (two or more manifest episodes of ulcerative lesion or bleeding);
- cardiovascular insufficiency of the III class;
- period after aortocoronary shunting;
- In I and II trimesters of pregnancy, as well as women who are trying to become pregnant, acetemethacin should be taken only in case of emergency; the use of acetemethacin in the last trimester of pregnancy and during lactation is contraindicated;
- Children and adolescence (no experience in this category of patients).
- in the presence of Crohn's disease, ulcerative colitis or other diseases of the intestine in the anamnesis;
- with SLE, connective tissue diseases;
- in case of arterial hypertension and / or heart failure;
- in cases of impaired renal or hepatic function;
- reported cases of hypokalemia in the use of indomethacin, this fact should be taken into account when the recommended intake of potassium-sparing diuretics;
- in the presence of epilepsy, Parkinson's disease and psychiatric disorders, including in anamnesis;
- with hemophilia;
- in elderly patients;
- in the case of infections caused by the varicella-zoster virus (chicken pox, shingles) due to the possible increased risk of serious skin complications.
PREGNANCY AND LACTATION
In the first and second trimesters of pregnancy, you should prescribe acetemethacin only in case of emergency. If acecemetine is used in women who are trying to get pregnant, or in the first and second trimesters of pregnancy, the dose should be so low and the duration of treatment as short as possible. In the third trimester of pregnancy, the use of acetemethacin is contraindicated.
The use of the drug is contraindicated, since small amounts of the active substance can enter the breast milk.
APPLICATION FOR FUNCTIONS OF THE LIVER
Contraindicated in severe renal failure (CC less than 30 ml / min). With caution in the violation of kidney function.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Contraindicated in any active liver disease. With caution in the violation of liver function.
APPLICATION FOR CHILDREN
Contraindicated in childhood and adolescence.
APPLICATION IN ELDERLY PATIENTS
Caution should be given to elderly patients.
Rantudil Retard should only be used if there is an opportunity to provide emergency assistance:
- Patients with hypersensitivity reactions (eg, asthma attacks, skin reactions or acute rhinitis) on NSAIDs / analgesics;
- patients suffering from asthma, hay fever, edema of the nasal mucosa or chronic respiratory disease;
Particular caution is needed when Rantudil Retard is taken concomitantly with other drugs acting on the central nervous system, or alcohol.
In some patients who took Rantudil Retard, there was an increase in liver and kidney function.
With a long course of treatment, a hemogram, coagulation monitoring, and ophthalmological examination are recommended.
Impact on the ability to drive vehicles and manage mechanisms
The use of Rantudil Retard may cause side effects, including effects on the central nervous system, so during treatment should refrain from potentially dangerous activity requiring high speed of mental and physical reactions (driving, working with machinery, working at height, etc.) .
Given the mechanism of action of the drug, overdose or misuse can cause central nervous system disorders, including headache, dizziness, confusion, drowsiness, convulsions and loss of consciousness right up to coma. In addition, nausea, vomiting, pain in the epigastric region, sweating, abnormal electrolyte balance, arterial hypertension, ankle edema, oliguria, hematuria, respiratory depression are possible.
With symptoms of overdose or in case of an alleged overdose, it is recommended to carry out symptomatic treatment, including gastric lavage, induction of diuresis while maintaining the water balance, and, if necessary, the use of anti-shock measures.
The specific antidote is unknown.
The following interactions were described with Rantudil Retard in combination with the following preparations:
Digoxin, lithium, phenytoin:
There may be an increase in the concentration of these drugs in the blood plasma.
NSAIDs can enhance the effect of anticoagulants, such as warfarin, so it is recommended that coagulation of the patient's blood be monitored if used simultaneously.
Increased risk of ulcerative lesions of the gastrointestinal tract or bleeding.
Other NSAIDs, including salicylates:
Simultaneous administration of several NSAIDs may increase the risk of gastrointestinal ulceration or bleeding due to a synergistic effect, therefore, simultaneous administration of acetemethacin with other NSAIDs should be avoided.
They can slow the excretion of acetemethacin.
Antibiotics of penicillin series
They can slow the excretion of acetemethacin.
Diuretics and antihypertensive drugs:
The hypotensive effect of drugs can be weakened. Furosemide accelerates the excretion of acetemethacin.
Can increase the level of potassium in the blood (hyperkalemia); it is often necessary to monitor the potassium content.
Antiaggregants and selective serotonin reuptake inhibitors (SSRls):
Increased risk of gastrointestinal bleeding. There have been no reports of interactions between acetemethacin and other active substances that also bind to plasma proteins.
May decrease the absorption rate of acetemethacin.
TERMS OF RELEASE FROM PHARMACY
TERMS AND CONDITIONS OF STORAGE
At a temperature of no higher than 30 В° C. Keep out of the reach of children. Shelf life - 3 years.