Indomethacin rectal suppositories 100mg №6×1

Name:
Indomethacin supp rect 100mg in ct.cell. pack. No. 6×1
Description:
Suppositories of a cylindrical-conical shape, white with a yellowish tinge. On the cut, the presence of an airy, porous rod and a funnel-shaped recess is allowed. The main active ingredient Indomethacin Release form Suppositories Dosage 100 mg Pharmacodynamics Indomethacin has anti-inflammatory, analgesic and antipyretic effects. The mechanism of action is associated with inhibition of the COX enzyme, which leads to inhibition of the synthesis of prostaglandins from arachidonic acid. The anti-inflammatory effect is due to the influence on both the exudative and proliferative phases of inflammation. The anti-inflammatory effect occurs by the end of the first week of treatment. Suppresses platelet aggregation. In diseases of a rheumatic nature, it helps to relieve pain in the joints at rest and during movement, reduce morning stiffness, swelling of the joints and increase range of motion. Contributes to the weakening or disappearance of non-rheumatic pain syndrome, incl. and in inflammatory processes that occur after operations and injuries, it reduces inflammatory edema at the wound site. In primary algomenorrhea, the drug reduces pain and reduces bleeding. With prolonged use, it has a desensitizing effect. Pharmacokinetics When administered rectally, the maximum concentration is reached after 1 hour. The bioavailability of the drug is 80-90%. Plasma protein binding 90-98%. Passes through the blood-brain barrier, placenta, penetrates into breast milk. Metabolized in the liver. The half-life is about 4.5 hours. In the blood, it is determined unchanged and in the form of metabolites. 70% of the drug is excreted in the urine, 30% in the feces as metabolites. Not removed by hemodialysis. Indications for use It is used for short-term symptomatic treatment of acute and chronic pain in inflammatory and degenerative diseases of the musculoskeletal system: rheumatoid arthritis, ankylosing spondylitis, osteoarthritis, inflammation of the periarticular tissues (bursitis and/or tendinitis), acute gouty arthritis. If you need more information about your condition, ask your doctor for advice. Method of administration and doses The use of this medicinal product is possible only after consulting a doctor! Do not stop taking INDOMETACIN without first consulting your doctor! If you have any doubts or questions, please contact your doctor. The dosage regimen is set individually, taking into account the clinical course of the disease. It is recommended to start treatment with small doses, increasing them if necessary. It is recommended to use the smallest effective dose. During treatment it is necessary to avoid taking alcoholic beverages. Adults and children over 14 years of age Recommended dose: 1 suppository 50 mg 1-3 times a day or 1 suppository 100 mg 1-2 times a day. Patients suffering from persistent night pain and / or morning stiffness are recommended to use indomethacin at bedtime at a dose of up to 100 mg. The maximum daily dose should not exceed 200 mg. The use of a daily dose exceeding 200 mg, as a rule, does not increase the effectiveness of the drug, but the risk of developing adverse reactions increases. Duration of treatment The duration of treatment with the drug should not exceed 7 days. Elderly patients Due to the higher risk of adverse reactions, the use of indomethacin in elderly patients requires extreme caution. It is recommended to take the lowest effective dose for the shortest possible time. Children The safety of use in children under 14 years of age has not been established. The use of suppositories in children is contraindicated. Instructions for rectal administration of the drug When using rectal suppositories, abdominal cramps and the urge to defecate often occur, so before the procedure, perform a cleansing enema or empty the intestines naturally. Wash your hands thoroughly with soap. Prepare wet wipes or a handkerchief soaked in water in advance. Lie on your side with your knees pressed to your stomach. For the procedure, this position is the most convenient, as it allows you to minimize discomfort. Remove the candle from the package. The candle is taken with the thumb and middle fingers of the right hand in the middle of the widest part, the index finger rests on the blunt end of the candle. The candle is directed with the free end to the anus and pushed with the index finger into the anal canal until it is completely immersed to a depth of 2-3 cm. Carry out the procedure carefully, without exerting excessive pressure. Despite the fact that the suppository has a streamlined shape, careless use can injure the mucous membrane. Do not get out of bed for about 20 minutes. Wipe your hands with a pre-prepared damp cloth or handkerchief. If within 10 minutes after the introduction of a rectal suppository there is an urge to defecate, empty the intestines and introduce a new suppository. If more than 10 minutes have passed between the introduction of the suppository and a bowel movement, an additional dose of the drug is not required. Use during pregnancy and lactation If you are pregnant or breastfeeding, if you suspect that you are pregnant or do not exclude the possibility of pregnancy, inform your doctor. In the I and II trimester of pregnancy, the drug can be prescribed only when the expected benefit to the mother outweighs the potential risk to the fetus, and only at the minimum effective dose, the duration of treatment should be as short as possible. Indomethacin is not used during the last trimester of pregnancy due to an increased risk of bleeding and birth defects. Due to excretion in breast milk, its use during breastfeeding is contraindicated or requires the cessation of breastfeeding during treatment. Precautions Cardiovascular Disorders Cardiovascular Thrombotic Events Clinical studies of several COX-2 selective and non-selective NSAIDs up to three years have shown an increased risk of severe cardiovascular (CV) thrombotic events, myocardial infarction, and stroke, which may be fatal. All NSAIDs, whether COX-2, selective or non-selective, may mask this risk. Patients with known CV disease or risk factors for CV disease may be at greater risk. To minimize the potential risk of adverse CV complications in patients treated with NSAIDs, the lowest effective dose should be used for the shortest period of time. Physicians and patients should be alert to the occurrence of such events, even in the absence of preexisting CV symptoms. Patients should be informed about the signs and/or symptoms of serious CV events and the steps to take if they occur. There is no convincing evidence that the concomitant use of aspirin reduces the increased risk of serious CV thrombotic events associated with the use of NSAIDs. The combined use of aspirin and NSAIDs increases the risk of serious gastrointestinal (GI) events (see GI side effects). Two large, controlled clinical trials of COX-2 selective NSAIDs for the treatment of pain in the first 10-14 days after CABG surgery revealed an increased incidence of myocardial infarction and stroke. Hypertension NSAIDs, including indomethacin, can lead to the onset of hypertension or worsening of a pre-existing hypertensive disease, and in any case this may contribute to an increase in the incidence of CV events. In patients taking thiazides or loop diuretics, the response to this treatment may worsen when NSAIDs are used together. NSAIDs, including indomethacin, should be used with extreme caution in patients with hypertensive disease. Blood pressure (BP) should be monitored at the start of NSAID treatment and throughout the course of treatment. Congestive heart failure and edema Some patients taking NSAIDs experience fluid retention and edema. Indomethacin should be used with extreme caution in patients with fluid retention or heart failure. In the study of patients with severe heart failure and hyponatremia, indomethacin is associated with a significant deterioration in circulatory hemodynamics, which is probably due to the inhibition of prostaglandin-dependent compensatory mechanisms. Gastrointestinal effects – risk of ulceration, bleeding, and perforation NSAIDs, including indomethacin, can cause serious GI adverse reactions, including inflammation, bleeding, ulceration, and perforation of the esophagus, stomach, small or large intestine, which can be fatal. These serious adverse events can occur at any time in patients treated with NSAIDs, with or without warning symptoms. Only one in five patients who developed a serious upper GI adverse reaction to NSAID treatment experienced symptoms of the disease. Ulcers, severe bleeding or perforation in the upper GI tract caused by NSAIDs occur in approximately 1% of patients treated for 3–6 months, and in 2–4% of patients for 1 year. These trends are observed both with long-term use, and increase the likelihood of developing a serious gastrointestinal complication during the course of treatment, and with short-term therapy. Rarely in patients taking indomethacin, intestinal ulceration is associated with stenosis and obstruction. Appears gastrointestinal bleeding without obvious ulceration and perforation of pre-existing sigmoid lesions (diverticulum, carcinoma, etc.). Rarely, an increase in abdominal pain in patients with ulcerative colitis or the development of ulcerative colitis and regional ileitis has been reported. NSAIDs should be used with extreme caution in patients with a history of peptic ulcer disease or gastrointestinal bleeding. Patients with a history of peptic ulcer disease and/or gastrointestinal bleeding who use NSAIDs are at a 10-fold higher risk of developing GI bleeding compared with patients who do not have these risk factors. Other factors that increase the risk of GI bleeding in patients treated with NSAIDs are concomitant use of oral corticosteroids or anticoagulants, long duration of NSAID treatment, smoking, alcohol use, older age, and poor general health. Most spontaneous reports of fatal GI events involve malnourished or elderly patients, and for this reason special care is required when treating such patients. To minimize the potential risk of adverse gastrointestinal events in patients treated with NSAIDs, the lowest effective dose should be used for the shortest possible period of time. Patients and physicians should be alert to signs and symptoms of GI ulceration and bleeding during NSAID treatment and promptly conduct additional evaluation and treatment if a serious adverse GI event is suspected. This should include discontinuation of NSAID use until a serious adverse GI event has been ruled out. For high-risk patients, treatment that does not include NSAIDs should be considered. Renal reactions Long-term use of NSAIDs has been associated with papillary necrosis and other renal impairment. Renal toxicity has also been observed in patients in whom renal prostaglandins play a compensatory role in maintaining renal perfusion. In such patients, the use of a non-steroidal anti-inflammatory agent can cause, firstly, a dose-dependent decrease in the formation of prostaglandins, and, secondly, a decrease in renal blood flow. Patients at higher risk for this reaction are patients with impaired renal function, heart failure, liver dysfunction, those taking diuretics and ACE inhibitors, patients with volume depletion, and elderly patients. After stopping NSAID treatment, kidney function usually recovers. When using indomethacin, an increase in serum potassium concentration, including hyperkalemia, has been reported, even in patients without kidney damage. In patients with normal renal function, these reactions are explained by the state of hypoenamic hypoaldosteronism. Renal impairment There are no clinical studies on the use of indomethacin in patients with renal insufficiency. For this reason, treatment with indomethacin is not recommended in patients with a decrease in GFR < 60 ml/min/1.73 m2. If it is necessary to start treatment with indomethacin, continuous monitoring of renal function is recommended. Anaphylactic/anaphylactoid reactions As with other NSAIDs, anaphylactic/anaphylactoid reactions may occur in patients without prior use of indomethacin. Indomethacin should not be used in patients with the aspirin triad. Seek emergency care if an anaphylactic/anaphylactoid reaction occurs. Skin reactions NSAIDs, including indomethacin, can cause serious skin side effects such as exfoliative dermatitis, Stevens-Johnson syndrome and toxic epidermal necrolysis, which can be fatal. These serious events may occur suddenly. Patients should be informed of the signs and symptoms of serious skin reactions and the drug should be discontinued at the first appearance of a skin rash or other sign of hypersensitivity. Eye reactions Corneal deposits and retinal disturbances have been observed in some patients on long-term treatment with indomethacin. The prescribing physician should be aware of the possible association between the observed changes and indomethacin. It is recommended to stop treatment if such changes are noticed. Blurred vision can be an important symptom and requires a complete ophthalmological examination. Since these changes may be asymptomatic, periodic ophthalmological examinations are recommended in patients in case of prolonged treatment. Central Nervous System Reactions Indomethacin may worsen depression or other psychiatric disorders, epilepsy and parkinsonism and should be used with extreme caution in patients with these conditions. If a severe CNS adverse reaction occurs, indomethacin should be discontinued. Indomethacin can cause drowsiness and, therefore, patients should be warned about activities that require increased attention and motor coordination, such as driving. Indomethacin can also cause headaches. Headache that persists despite dose reduction requires discontinuation of indomethacin treatment. Excipients The drug contains cetyl alcohol, which can cause local skin reactions (contact dermatitis). Interaction with other drugs If you are currently or have recently taken other drugs, tell your doctor. Aspirin: the simultaneous use of indomethacin with acetylsalicylic acid and other salicylates is not recommended; controlled clinical studies did not reveal an increase in therapeutic effect. Other NSAIDs: The combined use of indomethacin and other NSAIDs is not recommended; increases the risk of side effects from the gastrointestinal tract in the absence or slight increase in the effect. Diflunisal: simultaneous use increases the concentration of indomethacin in plasma and reduces the renal clearance of indomethacin; possible development of fatal gastrointestinal bleeding; combined use is not recommended. Anticoagulants: indomethacin enhances the effect of anticoagulants, as well as antiplatelet agents, fibrinolytics. Probenecid: co-administration potentiates the action of indomethacin by increasing its plasma concentration. Methotrexate: simultaneous use may increase the toxicity of methotrexate by reducing its tubular secretion; recommended to be used with caution. Cyclosporine: simultaneous use can lead to an increase in the toxic effect of cyclosporine, possibly due to a decrease in the synthesis of renal prostacyclin; when used together, strict control is necessary. Lithium: simultaneous use with lithium salts enhances their effect by increasing the concentration of lithium in the blood plasma and reducing renal clearance; regular monitoring of plasma lithium concentrations is recommended. Diuretics: simultaneous use may reduce the diuretic and antihypertensive effect of loop (eg, furosemide), potassium-sparing and thiazide diuretics; strict observation and monitoring of diuresis is recommended; indomethacin reduces plasma renin activity (ARP), can block the increase in plasma renin activity caused by furosemide, this must be taken into account when assessing plasma ARP in patients with arterial hypertension; do not use indomethacin and triamterene at the same time; simultaneous use with potassium-sparing diuretics can lead to an increase in plasma potassium concentration; it is recommended to monitor the concentration of potassium and the functional state of the kidneys. Cardiac glycosides / Digoxin: simultaneous use may increase the concentration of digoxin in the blood plasma and increase the half-life of digoxin; strict monitoring of plasma concentrations of digoxin is recommended. Antihypertensive drugs: single dose use may reduce the antihypertensive effect due to the suppression of prostaglandin synthesis by indamethacin; caution is advised when co-administering indomethacin with ACE inhibitors (eg captopril) and angiotensin II antagonists (eg losartan), alpha and beta-blockers, diuretics, hydralazine. Phenylpropanolamine: simultaneous use increases the risk of developing a hypertensive crisis, possibly due to the suppression of prostaglandin synthesis by indomethacin; caution is advised when used together. Corticosteroids: simultaneous use increases the risk of side effects from the gastrointestinal tract (bleeding, ulcer) Alcohol: simultaneous use increases the risk of side effects from the gastrointestinal tract, accompanied by bleeding; combined use is not recommended. Mifepristone: It is not recommended to use NSAIDs for 8-12 days after stopping mifepristone. Quinolones: Concomitant use may increase the risk of seizures in patients with or without a history of epilepsy or seizures. Contraindications Hypersensitivity to indomethacin and other components of the drug; hypersensitivity to acetylsalicylic acid or other NSAIDs with clinical manifestations of bronchospasm, rhinitis, angioedema and urticaria; history of active gastrointestinal ulcer/bleeding, perforation or recurrent gastrointestinal ulcer/bleeding (two or more separate episodes of established ulcer or bleeding); history of bleeding or perforation of the gastrointestinal tract associated with previous use of NSAIDs; severe heart, liver or kidney failure; nasal polyps; inflammatory diseases of the rectum (proctitis), hemorrhoids in the acute stage, rectal bleeding of various origins, incl. history: III trimester of pregnancy and breastfeeding period; Composition One suppository contains: active substance: indomethacin 50 mg or 100 mg; excipients: cetyl alcohol, semi-synthetic glycerides. Overdose With rectal use of indomethacin, overdose is extremely rare. Symptoms: nausea, vomiting, severe headache, dizziness, memory impairment, disorientation. In severe cases - paresthesia, numbness of the extremities, convulsions. Treatment: symptomatic and supportive therapy of vital signs. Hemodialysis is ineffective. Side effect On the part of the digestive system: gastropathy, abdominal pain, nausea, vomiting, heartburn, loss of appetite, diarrhea, impaired liver function (increased activity of "liver" transaminases, hyperbilirubinemia). From the nervous system: headache, dizziness, insomnia, agitation, irritability, excessive fatigue, drowsiness, depression, peripheral neuropathy, aseptic meningitis. From the senses: taste disturbance, hearing loss, tinnitus, diplopia, blurred vision, corneal clouding, conjunctivitis. From the side of the cardiovascular system: the development (aggravation) of CHF phenomena, tachyarrhythmia, edematous syndrome, increased blood pressure. From the urinary system: impaired renal function, proteinuria, hematuria, interstitial nephritis, nephrotic syndrome, papillary necrosis. On the part of the hematopoietic organs and the hemostasis system: anemia (hemolytic and aplastic), leukopenia, thrombocytopenia, eosinophilia, agranulocytosis, thrombocytopenic purpura, bleeding (gastrointestinal, gingival, uterine, hemorrhoidal). Allergic reactions: skin rash, skin itching, urticaria, angioedema, bronchospasm; in isolated cases - photosensitivity, toxic epidermal necrolysis, erythema nodosum, anaphylactic shock. Laboratory indicators: hyperglycemia, glucosuria, hyperkalemia, etc. Local reactions: burning, itching of the skin, heaviness in the anorectal region, exacerbation of hemorrhoids. Storage conditions Store in a dry, dark place at a temperature of 15 to 25 ° C. Buy Indomethacin rectal suppositories 100mg No. 6x1