Brufen SR, 800 mg 28 pcs

Pharmacokinetics:

Ibuprofen is a racemic mixture of [+]S- and [-]R-enantiomers. Studies have shown that food intake has no significant effect on overall bioavailability.

Absorption

Ibuprofen is rapidly absorbed in the gastrointestinal tract, bioavailability is 80 – 90%, time to maximum concentration (TCmax) in plasma when using the drug form of immediate release – 1-2 hours. Prolonged dosage form of ibuprofen 800 mg tablets provides a gradual release of the active substance, with a slower release rate compared to the dosage form of immediate release and a decrease in the value of 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, plasma concentrations of ibuprofen are maintained longer in the systemic bloodstream.

Thus, ibuprofen 800 mg tablets with prolonged action only once a day. A comparison of the pharmacokinetic profile of two 800 mg sustained-release ibuprofen tablets and 400 mg immediate-release ibuprofen tablets taken four times daily showed that the sustained-release dosage form provided a reduced range of differences between Cmax and threshold concentrations of immediate-release tablets and maintained higher mean plasma concentrations after 5, 10, 15 and 24 hours. The area under the curve “concentration – time” (AUC) was similar for immediate release tablets and prolonged release tablets.

Distribution

Ibuprofen is intensively bound to blood 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 P450 isoenzymes, primarily CYP2C9, to form two major inactive metabolites – 2-hydroxyibuprofen and 3-carboxyibuprofen. When ibuprofen is administered orally, slightly less than 90% of the ingested dose of ibuprofen may be detected in the urine as oxidative metabolites and their glucuron conjugates. A small amount of ibuprofen is excreted unchanged in the urine.

Excretion

Excretion of ibuprofen through the kidneys is fast and complete. The elimination half-life (T1/2) of immediately-released forms is about two hours. Ibuprofen is almost completely eliminated from the body 24 hours after the last dose.

Special patient groups

Patients of the elderly

In elderly patients in the absence of renal failure only small, clinically insignificant differences in the pharmacokinetic profile and urinary excretion compared to younger patients are observed. Renal failure

In patients with moderate renal failure, elevated plasma (S)-ibuprofen levels, elevated AUC (S)-ibuprofen values and elevated enantiomeric AUC (S/R) ratio values were observed compared to healthy control patients. In patients with end-stage renal failure who were on dialysis, the mean free fraction of ibuprofen was about 3% compared to 1% in healthy volunteers. Serious renal dysfunction can lead to accumulation of ibuprofen metabolites. The significance of this effect is unknown. Metabolites may be excreted by hemodialysis.

Liver failure

The presence of alcoholic liver disease in mild to moderate liver failure had no significant effect on pharmacokinetic parameters.

Patients with cirrhosis and moderate liver failure (6-10 Child-Pugh scores) treated with racemic ibuprofen showed a 2-fold increase in T1/2, on average, and the enantiomeric AUC (S/R) value was significantly lower compared to healthy control group patients, indicating impaired metabolic transformation of (R)-ibuprofen to the active (S)-enantiomer.

Indications

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

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

Padded tissue injuries: traumatic inflammation of soft tissues and locomotor system, sprains and strains, bruises.

Mild to moderate pain relief in: headache, toothache, primary dysmenorrhea, post-operative pain, migraine, panniculitis, neuralgia, myalgia.

Inflammatory processes in the pelvis: adnexitis, algodysmenorrhea.

Active ingredient

Ibuprofen

Composition

Active ingredient:

Ibuprofen – 800 mg.

Excipients:

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-1-7111B – 5.0 mg;

Talc – 3.0 mg;

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

How to take, the dosage

Ingestion, after a meal. Tablets should be swallowed whole, without chewing, with plenty of water.

Adults and children 12 years of age and older: The recommended dose is 2 tablets Brufen CP 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, dosage regimen adjustment in elderly patients is not required. In patients with impaired renal and/or hepatic function the dose should be adjusted individually. In this group of patients the dosing should be conducted with caution.

Interaction

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

Special Instructions

Gastrointestinal bleeding, ulcers and perforations

Use Brufen CP with caution in patients with a history of penthic ulcers and other gastrointestinal conditions, as exacerbation of these conditions is possible.

Cases of gastrointestinal bleeding, ulceration or perforation have been reported with all NSAIDs during any treatment period. These adverse events may be life-threatening and may occur in the presence/absence of warning symptoms or a history of serious gastrointestinal disease. The risk of gastrointestinal bleeding, ulceration or perforation increases with increasing doses of Brufen CP in patients with peptic ulcer disease, especially those with a history of bleeding or perforation, and in the elderly. 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, combination therapy with gastroprotectors (such as misoprostol or proton pump inhibitors) should be considered.

Simultaneous use of Brufen CP and other NSAIDs, including selective cyclooxygenase-2 (COX-2) inhibitors, should be avoided due to increased risk of ulceration or bleeding.

Patients with a history of gastrointestinal disease, especially elderly patients, should report any unusual abdominal symptoms (especially gastrointestinal bleeding) during initial treatment.

Caution should be exercised when using Brufen CP in patients concomitantly receiving medications that may increase the risk of ulceration or bleeding, such as oral glucocorticosteroids, anticoagulants (including warfarin), selective serotonin reuptake inhibitors or antiaggregant drugs, including acetylsalicylic acid.

If gastrointestinal bleeding or ulceration occurs, therapy with Brufen CP should be discontinued.

Respiratory disorders

Caution should be exercised when using Brufen CP in patients with bronchial asthma, chronic rhinitis or allergic diseases, including a history of bronchospasm, urticaria or angioedema have been reported in this group of patients.

Heart failure, renal and hepatic impairment

Caution should be exercised when using Brufen CP in patients with renal, hepatic or cardiac impairment, as taking NSAIDs may lead to worsening of renal function. Simultaneous treatment with several analgesics further increases this risk. In patients with renal, hepatic or cardiac insufficiency, 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

Use Brufen CP with caution in patients with a history of heart failure or arterial hypertension, as cases of edema have been reported with ibuprofen.

Data from epidemiologic studies suggest that use of ibuprofen at a high dose (2400 mg daily) and with long-term treatment may be associated with a small increase in the risk of arterial thrombotic complications, including myocardial infarction or stroke. Epidemiological studies have not shown that the use of ibuprofen at a low dose (< 1200 mg per day) is associated with an increased risk of arterial thrombotic complications, in particular myocardial infarction.

Therapy with Brufen CP in patients with uncontrolled arterial hypertension, heart failure, CHD, peripheral artery disease and/or cerebrovascular disease should only be undertaken after a thorough benefit/risk assessment. Similar assessment should also be performed before prescribing long-term treatment for patients with cardiovascular risk factors (such as arterial hypertension, hyperlipidemia, diabetes mellitus, smoking).

Dermatological disorders

Very rare cases of serious skin reactions, including life-threatening, including exfoliative dermatitis, Stevens-Johnson syndrome and toxic epidermal necrolysis have been reported when using NSAIDs. Patients are at greatest risk of developing these reactions during the initial phase of therapy. In most cases, the reaction develops during the first month of treatment. If skin rash, mucosal lesions or any other signs of hypersensitivity first appear, Brufen CP should be discontinued.

Renal disorders

Caution should be exercised when initiating therapy with Brufen CP in patients with significant dehydration. There is a risk of renal failure, especially in children and adolescents with dehydration.

Prolonged use of ibuprofen, as well as other NSAIDs, has resulted in the development of medullary renal necrosis and other pathological changes in the kidneys. Also renal toxicity was observed in patients in whom “renal” prostaglandins play a compensatory role in maintaining renal perfusion. Use of NSAIDs in this group of patients may lead to a dose-dependent decrease in prostaglandin production and, secondarily, in renal blood flow, which may cause renal failure.

Patients with impaired renal function, heart failure, impaired liver function, those taking diuretics, ACE inhibitors, as well as elderly patients are at increased risk of this reaction. After discontinuation of NSAIDs, there is usually a recovery before treatment.

Hematologic disorders

Brufen CP, like other NSAIDs, may inhibit platelet aggregation and increase bleeding time in healthy patients.

Aseptic meningitis

Aseptic meningitis has rarely developed in patients treated with ibuprofen. Although aseptic meningitis is most likely to occur 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 accompanied by an increased incidence of adverse reactions, especially perforation and gastrointestinal bleeding, which may be life-threatening.

.

Synopsis

White oblong, film-coated tablets with “BRUFEN RETARD” printed on one side in red-brown.

Contraindications

.

Side effects

The side effects observed with ibuprofen are common to the entire class of NSAIDs. Unwanted effects can be minimized by using the lowest effective dose for the short period of time needed to relieve symptoms.

All adverse reactions considered to have at least a possible association with ibuprofen use are presented by organ system and frequency of occurrence: Very common (≥1/10), common (≥1/100 to < 1/10), infrequent (≥1/1000 to < 1/100), rare (≥1/10000 to < 1/1000), very rare (< 1/10000) and frequency unknown (cannot estimate frequency based on available data).

Dyspepsia

Diarrhea

Nausea

Vomiting (including bloody)

Pain in the stomach

Meoterism

/p>

Constipation

Melena

Gastrointestinal bleeding

/p>

br>

br>

p>

/p>

/p>

1 – cases of exacerbation of inflammation caused by infections (e.g., development of necrotizing fasciitis) have been described when using NSAIDs. If when using ibuprofen the patient shows signs of infection or the course of infection worsens, the patient should immediately consult a physician.

2 – In exceptional cases, serious skin infection and soft tissue abnormalities may occur with chickenpox infection.

3 – Evidence from clinical and epidemiologic studies suggests that use of ibuprofen (at a high dose of 2400 mg daily) and with long-term treatment may be associated with a small increase in the risk of arterial thrombotic complications, including myocardial infarction or stroke.

Overdose

Toxicity: In children and adults when taking ibuprofen in doses less than 100 mg/kg there are usually no signs and symptoms of toxicity. However, in some cases symptomatic therapy may be required. In children, the appearance of symptoms of toxicity has been observed after administration of ibuprofen in doses of 400 mg/kg or more. Most patients with ibuprofen overdose experience symptoms 4-6 hours after ingestion.

Symptoms: the most frequently reported symptoms of overdose are 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, CNS and respiratory system suppression have also rarely been reported.

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

Treatment: There is no specific antidote. In case of overdose, gastric lavage (within the first hour of ingestion) and supportive therapy are recommended. In the presence of symptoms of the gastrointestinal tract – antacid drugs. If arterial hypotension develops, intravenous infusion and, if required, inotropic support. Drinking, forced diuresis and symptomatic therapy (correction of COS, electrolyte balance, BP).

Pregnancy use

Reproduction, Pregnancy and Childbirth

In the first to second trimesters of pregnancy, Brufen CP should only be taken if strictly necessary and if the potential benefit to the mother outweighs the potential risk to the fetus and child. Use of Brufen CP in the third trimester of pregnancy is contraindicated and, as with the use of all prostaglandin synthesis inhibitors, carries the following risks to the fetus:

– cardiopulmonary toxicity (premature closure of the arterial duct and arterial hypertension);

– impaired renal function, with further possibility of renal failure and reduction of amniotic fluid volume.

During labor, ibuprofen, as well as all inhibitors of prostaglandin synthesis, exposes the mother and the newborn to the following risks:

– increased bleeding time;

– inhibition of uterine contractile activity, which may lead to a delay or increase the duration of labor.

In this regard, it is not recommended to take ibuprofen during labor activity. The use of ibuprofen may adversely affect female fertility and is not recommended for women planning pregnancy.

If ibuprofen is prescribed to women planning pregnancy, as well as in the I or II trimesters of pregnancy, the doses and duration of ibuprofen therapy should be reduced as much as possible. In women who have difficulty conceiving or who are undergoing infertility studies, consideration should be given to withdrawing ibuprofen therapy.

Breastfeeding

Due to the limited data available on the penetration of ibuprofen into breast milk at very low concentrations, use of Brufen CP while breastfeeding is not recommended.

Similarities

Nurofen, Nurofen Express, Ibuprofen, Dolgit, Ibuprofen-Chemopharm, Nurofen Forte, MIG 400, Faspik, Nurofen Express Lady, Nurofen Express Forte, Nurofen Kids, Next Uno Express, Nurofast