Diclofenac retard Akrikhin pills 100mgN20
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Description
Diclofenac Retard-Akrikhin pills have anti-inflammatory, analgesic, antipyretic and antiaggregant effects.
Active ingredients
Diclofenac
Release form
Pills
Composition
1 tab. Contains Diclofenac Sodium 100 mg. Auxiliary substances: ludepress LCE (lactose monohydrate - 94.7-98.3%, povidone - 3-4%), hypromellose (hydroxypropylmethylcellulose), microcrystalline cellulose, magnesium stearate, colloidal silicon dioxide (aerosil 200), stearic acid. The composition of the shell: hypromellose (hydroxypropyl methyl cellulose), macrogol (polyethylene glycol 6000), glycerol (glycerin), talc, titanium dioxide, dye iron oxide red.
Pharmacological effect
Nonsteroidal anti-inflammatory drug (NSAIDs), a derivative of phenylacetic acid. It has anti-inflammatory, analgesic, antipyretic and antiplatelet effect. Indiscriminately inhibiting COX-1 and COX-2, violates the metabolism of arachidonic acid, reduces the number of prostaglandins in the inflammation, suppresses the exudative and proliferative phases of inflammation. In rheumatic diseases, the anti-inflammatory and analgesic effect of diclofenac significantly reduces the severity of pain, morning stiffness, swelling of the joints, which improves the condition of the joint. With injuries in the postoperative period, diclofenac reduces pain and inflammatory edema.
Pharmacokinetics
Suction. Absorption is fast and complete; food slows down the rate of absorption. Plasma concentration is linearly dependent on the magnitude of the dose administered. As a result of the sustained release of the active substance, Cmax in the plasma is lower than that which is formed with the administration of a short-acting drug, but remains high for a long time after administration. Cmax is 0.5-1 mcg / ml, the time to reach Cmax - 5 hours after taking the drug in the form of a tablet of prolonged action in a dose of 100 mg. Bioavailability - 50%. Distribution. Plasma protein binding - more than 99% (most of it is bound to albumin). It penetrates into synovial fluid, Cmax in synovial fluid is observed 2-4 hours later than in plasma. Changes in the pharmacokinetics of diclofenac against the background of repeated administration is not observed.It does not accumulate while observing the recommended interval between doses. Metabolism. 50% of the active substance is subject to the “first pass” effect through the liver. Metabolism occurs as a result of repeated or single hydroxylation and conjugation with glucuronic acid. CYP2C9 isoenzyme is also involved in diclofenac metabolism. Pharmacological activity of metabolites is lower than diclofenac. Inference. Systemic clearance is 260 ml / min. T1 / 2 from plasma - 1-2 hours, from synovial fluid - 3-6 hours (the concentration of the active substance in the synovial fluid 4-6 hours after drug administration is higher than in plasma, and remains higher for another 12 hours). 60% of the administered dose is excreted in the form of metabolites by the kidneys, less than 1% is excreted unchanged, the rest of the dose is excreted in the form of metabolites with bile.
Indications
Inflammatory and degenerative diseases of the musculoskeletal system: rheumatoid arthritis, psoriatic arthritis, juvenile chronic arthritis, ankylosing spondylitis (ankylosing spondylitis), gouty arthritis (with an acute attack of gout, fast-acting dosage forms are preferable), rheumatoid arthritis, ostrotechnology, ostrotechni, ophthalmic arthritis, ophthalmic arthritis; including with radicular syndrome, tendovaginitis, bursitis. The drug is intended for symptomatic therapy, reducing pain and inflammation at the time of use, does not affect the progression of the disease. Pain syndrome of mild or moderate severity: lumbago, sciatica, neuralgia, myalgia, post-traumatic pain syndrome accompanied by inflammation, postoperative pain, headache, migraine, toothache, algomenorrhea, adnexitis, proctitis, As part of complex therapy of infectious and inflammatory diseases with severe pain: pharyngitis, tonsillitis, otitis media.
Contraindications
A complete or incomplete combination of asthma, recurrent polyposis of the nasal mucosa and paranasal sinuses, and intolerance to acetylsalicylic acid or other nonsteroidal anti-inflammatory drugs (including history), erosive and ulcerative lesions of the gastric or duodenal ulcer, or erosive ulcerative lesions of the gastric or duodenal ulcers, or erosive ulcerative lesions of the gastric or duodenal ulcers, or erosive ulcerative lesions of the gastric or duodenal ulcer inflammatory bowel diseases (ulcerative colitis, Crohn's disease) in the acute phase, the period after coronary artery bypass grafting, decompensated cardiac non Residual, hematopoiesis disorders, hemostatic disorders (includinghemophilia), severe hepatic impairment or active liver disease, severe renal insufficiency (CC less than 30 ml / min), progressive kidney disease, confirmed hyperkalemia, III trimester of pregnancy, lactation, childhood and adolescence to 18 years.
Use during pregnancy and lactation
The use of the drug in the III trimester of pregnancy and during lactation is contraindicated. Precautions should be prescribed the drug in the I and II trimesters of pregnancy.
Dosage and administration
The drug is taken orally, during or after a meal. Tablets should be swallowed, not chewed and squeezed with a small amount of water. Adults appoint 100 mg 1 time / day. With algomenorrhea and migraine attacks - up to 200 mg / day for no more than 1-2 days. When taking pills of a prolonged action of 100 mg, if you need to increase the daily dose to 150 mg / day, you can additionally take 1 regular tablet (50 mg). The maximum daily dose is 150 mg.
Side effects
On the part of the digestive system: nausea, vomiting, anorexia, pain and discomfort in the epigastric region, flatulence, constipation, diarrhea, in some cases - erosive and ulcerative lesions, bleeding and perforation of the gastrointestinal tract, rarely - impaired liver function. When administered rectally in isolated cases, there was inflammation of the colon with bleeding, exacerbation of ulcerative colitis. On the part of the central nervous system and peripheral nervous system: dizziness, headache, agitation, insomnia, irritability, fatigue, rarely - paresthesia, visual disturbances (vagueness, diplopia), tinnitus, sleep disorders, convulsions, irritability, tremor, mental disorders, depression.
Overdose
Symptoms: vomiting, bleeding from the gastrointestinal tract, epigastric pain, diarrhea, dizziness, tinnitus, convulsions, increased blood pressure, respiratory depression, with a significant overdose - acute renal failure, hepatotoxic effect. Treatment: gastric lavage, the introduction of activated carbon, conducting symptomatic therapy aimed at eliminating arterial hypertension, renal dysfunction, seizures, gastrointestinal irritation, respiratory depression. Forced diuresis and hemodialysis are ineffective (due to the high degree of protein binding and intensive metabolism).
Interaction with other drugs
Diclofenac increases plasma concentration of digoxin, methotrexate, lithium preparations and cyclosporine.
special instructions
To quickly achieve the desired therapeutic effect of the drug is recommended to take 30 minutes before a meal. In other cases, take before, during or after a meal, without chewing, pouring plenty of water.