Brufen SR sustained release pills 800mg, 14pcs

Composition

Active ingredient:

ibuprofen – 800 mg.

Auxiliary substances:

Xanthan gum-196.8 mg;

povidone-25.9 mg;

stearic acid-10.3 mg;

colloidal silicon dioxide-3.0 mg,

hypromellose-16.0 mg;

Opadry white M-1-7111 B-5.0 mg;

talc – 3.0 mg;

brown ink Opacode S-1 – 9460HV-traces.

Pharmacological action

Nonsteroidal Anti-inflammatory drug (NSAID)ATX: M. 01. A. E. 01 Ibuprofen Pharmacodynamics :

Ibuprofen is a propionic acid derivative, a nonsteroidal anti-inflammatory drug (NSAID) that has analgesic, anti-inflammatory and antipyretic effects. The therapeutic effect of the drug is due to the inhibition of the cyclooxygenase enzyme, which leads to a significant decrease in prostaglandin synthesis. These properties help eliminate the symptoms of inflammation, pain, and fever.

Experimental data suggest that concomitant use of ibuprofen may inhibit the effect of low-dose acetylsalicylic acid on platelet aggregation. In a single study, when a single dose of ibuprofen 400 mg was administered 8 hours before or 30 minutes after the use of immediate-release acetylsalicylic acid (81 mg), a decrease in the effect of acetylsalicylic acid on thromboxane formation or platelet aggregation was observed.

However, due to the limitations of these data and the inaccuracy in extrapolating ex vivo data to the clinical situation, reliable conclusions regarding the continuous use of ibuprofen cannot be made. The development of clinically significant effects is considered unlikely with the occasional use of ibuprofen.

Pharmacokinetics: Ibuprofen is a racemic mixture of [+] S-and [-] R-enantiomers. Studies have shown that food intake has no noticeable effect on overall bioavailability. Absorption Ibuprofen is rapidly absorbed in the gastrointestinal tract, bioavailability is 80-90%, the time to reach the maximum concentration (TMAX) in blood plasma when using the immediate-release dosage form is 1-2 hours. The extended-release dosage form of ibuprofen tablets 800 mg provides a gradual release of the Active ingredient, with a slower release rate compared to immediate-release dosage forms and a decrease in the maximum concentration (Cmax) in blood plasma, which is reached approximately 3 hours after the use of ibuprofen. As a result of the prolonged absorption phase in the systemic circulation, plasma concentrations of ibuprofen are maintained longer. Thus, ibuprofen 800 mg tablets with prolonged action is enough to take only once a day. A comparison of the pharmacokinetic profile of two 800 mg long-release ibuprofen tablets and 400 mg immediate-release ibuprofen tablets taken four times a day showed that the extended-release dosage form reduces the range of differences between Cmax and threshold concentrations of immediate-release tablets and maintains higher average plasma concentrations after 5,10,15 and 24 hours. For immediate – release tablets and long-release tablets, the area under the concentration-time curve (AUC) was similar. Distribution Ibuprofen binds intensively to plasma proteins (99%). The volume of distribution (Vd) of ibuprofen is small and is approximately 0.12 – 0.2 l/kg in adults. Metabolism Ibuprofen is rapidly metabolized in the liver with the participation of cytochrome P 450 isoenzymes, mainly the CYP2C9 isoenzyme, with the formation of two main inactive metabolites-2-hydroxyibuprofen and 3-carboxyibuprofen. When ibuprofen is administered orally, a little less than 90% of the ibuprofen dose taken can be detected in the urine in the form of oxidative metabolites and their glucuronic conjugates. A small amount of ibuprofen is excreted unchanged in the urine. Elimination of ibuprofen through the kidneys is rapid and complete. The half-life (T1/2) of the immediate-release dosage forms is about two hours. Ibuprofen is almost completely eliminated from the body 24 hours after taking the last dose. Special patient groups Elderly patients and elderly patients in the absence of renal insufficiency, only small, clinically insignificant differences in the pharmacokinetic profile and urinary excretion are observed compared with young patients. Renal insufficiency In patients with moderate renal insufficiency, elevated plasma levels of (S)-ibuprofen, increased values of the AUC (S)-ibuprofen index, and increased values of the enantiomeric AUC (S/R) ratio were observed compared with healthy patients in the control group. In patients with end-stage renal failure who were on dialysis, the average free fraction of ibuprofen was about 3%, compared with 1% in healthy volunteers. Severe renal impairment can lead to accumulation of ibuprofen metabolites. The significance of this effect is unknown. Metabolites can be eliminated by hemodialysis. Hepatic insufficiency The presence of alcoholic liver disease in mild or moderate hepatic insufficiency did not significantly affect the pharmacokinetic parameters. In patients with cirrhosis of the liver and moderate hepatic insufficiency (6-10 points on the Child-Pugh scale) treated with racemic ibuprofen, an increase in T 1/2 was observed, on average, by 2 times, and the value of the enantiomeric ratio AUC (S/R) was significantly lower compared to healthy patients in the control group, which indicates a violation of the metabolic transformation of (R)-ibuprofen into the active (S)-enantiomer.

Indications

Inflammatory and degenerative diseases: rheumatoid arthritis, including juvenile rheumatoid arthritis or Still’s syndrome, osteoarthritis, joint syndrome with gout exacerbation, psoriatic arthritis, ankylosing spondylitis, spondylosis.

Diseases of the periarticular tissues, including rheumatic ones: scapular periarthritis (capsulitis), bursitis, tendinitis, tenosynovitis, tendovaginitis, low back pain, sciatica.

Soft tissue damage: traumatic inflammation of the soft tissues and musculoskeletal system, dislocations and sprains, hematomas.

Relief of mild or moderate pain in: headache, toothache, primary dysmenorrhea, postoperative pain, migraine, panniculitis, neuralgia, myalgia.

Inflammatory processes in the small pelvis: adnexitis, algodismenorrhea.

Use during pregnancy and lactation

Reproductive function, pregnancy and delivery In the first and second trimesters of pregnancy, Brufen CP can only be taken if absolutely necessary, if the potential benefit to the mother outweighs the potential risk to the fetus and child. The use of Brufen CP in the third trimester of pregnancy is contraindicated, and, as with all prostaglandin synthesis inhibitors, it carries the following risks for the fetus: – cardiopulmonary toxicity (premature closure of the ductus arteriosus and arterial hypertension);- impaired renal function, with a further possibility of developing renal failure and a decrease in the volume of amniotic fluid. During labor, ibuprofen, like all prostaglandin synthesis inhibitors, exposes the mother and newborn to the following risks: : – increased bleeding time; – inhibition of contractile activity of the uterus, which can lead to a delay or increase in the duration of labor. In this regard, it is not recommended to take ibuprofen during labor. The use of ibuprofen may negatively affect female fertility and is not recommended for women planning pregnancy. If ibuprofen is prescribed to women who are planning pregnancy, as well as in the first or second trimester of pregnancy, the dose should be reduced as much as possible and the duration of ibuprofen therapy should be reduced. In women who are experiencing conception problems or undergoing infertility screening, discontinuation of ibuprofen therapy should be considered. Breast-feedingin view of the limited data available on the penetration of ibuprofen into breast milk in very low concentrations, the use of Brufen CP during breastfeeding is not recommended.

Contraindications

-hypersensitivity to the Active ingredient or to any of the excipients;- complete or incomplete combination of bronchial asthma, recurrent nasal and paranasal sinus polyposis, and intolerance to acetylsalicylic acid (ASA) or other NSAIDs (including in the anamnesis);- severe heart failure;- severe liver failure;- active liver disease;- severe renal insufficiency (creatinine clearance less than 30 ml / min);- progressive kidney diseases; – hemophilia and other blood clotting disorders (including hypocoagulation), hemorrhagic diathesis;- gastrointestinal bleeding or perforation in the anamnesis associated with previous NSAID use;- ulcerative colitis, Crohn’s disease, recurrent peptic ulcer disease, or gastrointestinal bleeding (defined by two or more separate episodes of confirmed ulceration or bleeding), including a history;- condition after coronary artery bypass grafting;- confirmed hyperkalemia; – inflammatory bowel diseases; – intracranial hemorrhage;- pregnancy (third trimester);- breast-feeding period; – children under 12 years of age.With caution:A single episode of erosive and ulcerative diseases of the gastrointestinal tract in the anamnesis (including peptic ulcer of the stomach and duodenum); simultaneous use of oral corticosteroids (including prednisone), anticoagulants (including warfarin), antiplatelet agents (including clopidogrel), selective serotonin reuptake inhibitors (including citalopram, fluoxetine, paroxetine, sertraline); long-term use of NSAIDs; bronchial asthma, chronic rhinitis or allergic diseases (including in the anamnesis); liver failure and/or chronic renal failure (creatinine clearance 30-60 ml/min); heart failure; arterial hypertension; coronary heart disease; cerebrovascular diseases; dyslipidemia/hyperlipidemia; diabetes mellitus; peripheral arterial diseases; smoking; presence of infections H. pylori; frequent alcohol consumption; severe somatic diseases; systemic lupus erythematosus or other autoimmune connective tissue diseases (increased risk of aseptic meningitis); blood diseases of unknown etiology (leukopenia and anemia); cirrhosis of the liver with portal hypertension; nephrotic syndrome; hyperbilirubinemia; gastritis; enteritis; colitis; dehydration; pregnancy (I-II trimester), old age.

Side effects

The side effects observed with ibuprofen are typical for the entire class of NSAIDs. Undesirable effects can be minimized by applying the minimum effective dose for a short period of time necessary to eliminate symptoms.

All adverse reactions considered to have at least a possible association with ibuprofen are reported by organ system and frequency: very common (≥1/10), common (≥ 1/100 to < 1/10), uncommon (≥1/1000 to < 1/100), rare (≥1/10000 to < 1/1000), very rare (

1-when using NSAIDs, cases of exacerbation of inflammation caused by infections (for example, the development of necrotizing fasciitis) have been described. If a patient shows signs of infection or the course of infection worsens while using ibuprofen, you should immediately consult a doctor.

2-in exceptional cases, serious skin infection and soft tissue disorders may occur due to chickenpox infection.

3-data from clinical and epidemiological studies indicate that the use of ibuprofen (at a high dose-2400 mg per day) and with long-term treatment may be associated with a slight increase in the risk of arterial thrombotic complications, including myocardial infarction or stroke.

Interaction

Due to reports of drug interactions in some patients, Brufen CP should be used with caution in patients taking any of the following medications::

How to take, course of use and dosage

Inside, after eating. Tablets should be swallowed whole, without chewing, washed down with plenty of water.

Adults and children aged 12 years and older: The recommended dose is 2 Brufen CP tablets once a day, preferably before bedtime. In severe and acute conditions, the maximum daily dose is 3 tablets taken separately. The maximum daily dose is 2400 mg.

Elderly patients: with normal renal and hepatic function, no dosage adjustment is required in elderly patients. If renal and/or hepatic function is impaired, the dose should be selected individually. In this group of patients, dosage should be carried out with caution.

Overdose

Toxicity: in children and adults, when taking ibuprofen in doses less than 100 mg/kg, signs and symptoms of toxicity are usually absent. However, in some cases, symptomatic therapy may be required. In children, the appearance of toxicity symptoms was observed after taking ibuprofen in doses of 400 mg / kg or more. Most patients with an ibuprofen overdose develop symptoms 4-6 hours after ingestion.

Symptoms: The most frequently reported overdose symptoms were nausea, vomiting, abdominal pain, lethargy, and drowsiness. Central nervous system (CNS) disorders include headache, tinnitus, dizziness, depression, seizures, and loss of consciousness. Nystagmus, metabolic acidosis, hypothermia, impaired renal function, gastrointestinal bleeding, coma, respiratory arrest, and suppression of CNS and respiratory system activity were also rarely reported.

Cases of cardiovascular toxicity, including hypotension, bradycardia, and tachycardia, have been reported. In cases of significant overdose, acute renal failure and liver damage may develop. Overdose with large doses of Brufen CP is usually well tolerated if no other medications were taken at the same time.

Treatment: there is no specific antidote. In case of overdose, gastric lavage (within the first hour after ingestion) and maintenance therapy are recommended. In the presence of symptoms from the gastrointestinal tract-antacids. With the development of arterial hypotension-intravenous infusions and, if necessary, inotropic support. Drinking, forced diuresis, and symptomatic therapy (correction of CBS, electrolyte balance, and blood pressure).

Description

White oblong coated tablets with “BRUFEN RETARD” overprint in red-brown color on one side.

Special instructions

Gastrointestinal bleeding, ulceration and perforation Brufen CP should be used with caution in patients with a history of pentic ulcer and other gastrointestinal diseases, as these conditions may worsen. Gastrointestinal bleeding, ulceration, or perforation have been reported with all NSAIDs during any period of treatment. These adverse events can be life-threatening and occur in the presence/absence of warning symptoms or a history of serious gastrointestinal diseases. The risk of gastrointestinal bleeding, ulceration or perforation increases with increasing doses of Brufen CP in patients with peptic ulcer disease, especially complicated by bleeding or perforation in the anamnesis, and in elderly patients. In these patients, treatment should be started with the lowest dose.In this group of patients, as well as in patients requiring concomitant therapy with low-dose acetylsalicylic acid or other drugs that may increase the risk of gastrointestinal disease, the possibility of combined therapy with gastroprotectors (for example, misoprostol or proton pump inhibitors) should be considered. Concomitant use of Brufen CP and other NSAIDs, including selective cyclooxygenase-2 (COX-2) inhibitors, should be avoided due to the increased risk of ulceration or bleeding. At the initial stage of treatment, patients with a history of gastrointestinal diseases, especially elderly patients, should report any unusual abdominal symptoms (especially gastrointestinal bleeding). Brufen CP should be used with caution in patients receiving concomitant medications that may increase the risk of ulceration or bleeding, such as oral glucocorticosteroids, anticoagulants (including warfarin), selective serotonin reuptake inhibitors, or antiplatelet medications, including acetylsalicylic acid. If gastrointestinal bleeding or ulceration occurs, Brufen CP therapy should be discontinued. Respiratory disorders Caution should be exercised when using Brufen CP in patients with bronchial asthma, chronic rhinitis or allergic diseases, including in the anamnesis, as cases of bronchospasm, urticaria or angioedema have been reported when using Brufen CP in this group of patients. Heart failure, renal and hepatic insufficiency Caution should be exercised when using Brufen CP in patients with renal, hepatic or heart failure, as taking NSAIDs can lead to deterioration of renal function. Simultaneous therapy with several analgesics additionally increases this risk. In patients with renal, hepatic or heart failure, the minimum effective dose should be used for the shortest possible period of time and renal function should be monitored, especially during long-term treatment. Cardiovascular and cerebrovascular disorders Brufen CP should be used with caution in patients with a history of heart failure or hypertension, as cases of edema have been reported with ibuprofen. Data from epidemiological studies indicate that the use of ibuprofen in a high dose (2400 mg per day) and with long-term treatment may be associated with a slight increase in the risk of arterial thrombotic complications, including myocardial infarction or stroke. Epidemiological studies have not shown that the use of low-dose ibuprofen (Brufen CP therapy in patients with uncontrolled hypertension, heart failure, coronary artery disease, peripheral artery disease, and/or cerebrovascular disease should only be performed after a thorough benefit/risk assessment. Such an assessment should also be made before prescribing long-term treatment to patients with risk factors for developing cardiovascular diseases (such as arterial hypertension, hyperlipidemia, diabetes mellitus, smoking). Dermatological disorders Very rare cases of serious skin reactions, including life-threatening ones, including exfoliative dermatitis, Stevens-Johnson syndrome, and toxic epidermal necrolysis, have been reported with NSAIDs. At the initial stage of therapy, patients are most at risk of developing these reactions. In most cases, the reaction develops during the first month of treatment. At the first appearance of skin rash, mucosal lesions or any other signs of hypersensitivity, the use of Brufen CP should be discontinued. Renal impairment Brufen CP therapy should be initiated with caution in patients with significant dehydration. There is a risk of developing kidney failure, especially in children and adolescents with dehydration. Long-term use of ibuprofen, as well as other NSAIDs, has led to the development of medullary necrosis of the kidney and other pathological changes in the kidneys. Renal toxicity has also been observed in patients in whom” renal ” prostaglandins play a compensatory role in maintaining renal perfusion. The use of NSAIDs in this group of patients can lead to a dose-dependent decrease in prostaglandin production and, secondarily, renal blood flow, which can cause renal failure. Patients with impaired renal function, heart failure, impaired liver function, taking diuretics, ACE inhibitors, as well as elderly patients are at an increased risk of this reaction. After discontinuation of NSAIDs, as a rule, the condition is restored before starting treatment. Hematological abnormalities Brufen CP, like other NSAIDs, can inhibit platelet aggregation and increase bleeding time in healthy patients. Aseptic meningitis patients treated with ibuprofen have rarely developed aseptic meningitis. Although the occurrence of aseptic meningitis is most likely in patients with systemic lupus erythematosus and related connective tissue diseases, cases of aseptic meningitis have been reported in patients without this chronic disease. Elderly patients In elderly patients, the use of NSAIDs may be associated with an increased incidence of adverse reactions, especially perforation and gastrointestinal bleeding, which can be life-threatening. Influence on the ability to drive vehicles and mechanisms:It may affect the speed of reaction. During the treatment period, care should be taken when driving vehicles and engaging in other potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions.

Storage conditions

At a temperature not exceeding 25 °C. Keep out of reach of children.

Shelf

life is 3 years. Do not use the drug after the expiration date.

Active ingredient

Ibuprofen

Conditions of release from pharmacies

By prescription

Dosage form

long-acting tablets