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

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:

Concomitant use of ibuprofen with the following medications:

Possible effects

Other NSAIDs, including selective cyclooxygenase-2 inhibitors

Concurrent use with other NSAIDs, including selective cyclooxygenase-2 inhibitors, should be avoided due to possible additive effects.

Heart glycosides

NSAIDs may worsen the course of heart failure, decrease glomerular filtration rate, and increase plasma concentrations of cardiac glycosides.

Glucocorticosteroids

The use of NSAIDs increases the risk of GI ulcers or bleeding.

Anticoagulants

Special Instructions

Synopsis

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).

An organ system

Frequency

Unintended effect

Infectious diseases1

Infrequent

Rhinitis

Rarely

Aseptic meningitis

Disorders of the blood and lymphatic system

Rarely

Anemia (including hemolytic, aplastic)

Thrombocytopenia

Neutropenia

Agranulocytosis

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Leukopenia

Immune system disorders

Rarely

Anaphylactic reaction

Mental disorders

Infrequent

Insomnia

Anxiety

Rarely

Depression

Confusion

Frequency unknown

Hallucinations

Nervous system disorders

Frequent

Headache

Dizziness

Infrequent

Paresthesia

Sleepiness

Rarely

Optic neuritis

Visual disturbances

Infrequent

Visual disturbances

Rarely

Toxic optical neuropathy

Hearing and labyrinth disorders

Infrequent

Hearing impairment

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Ringing or tinnitus

Vertigo

Heart disturbances

Worsening heart failure

Myocardial infarction

Vascular disorders3

Very rare

Increased blood pressure

Constipation

Melena

Gastrointestinal bleeding

Infrequent

Gastritis

Gastric and/or duodenal ulcer

Eraging of oral mucosa

Gastrointestinal mucosal perforation

Very rare

Pancreatitis

Frequency unknown

Aggravation of colitis and Crohn’s disease

Aphthous stomatitis

Disorders of the liver and biliary tract

Infrequent

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Hepatitis

Jaundice

Impaired liver function

Very rarely

Hepatic failure

Skin and subcutaneous tissue disorders2

Often

Skin rash

Infrequent

Urticaria

Cutaneous itching

Hemorrhagic rash Angioneurotic edema Photosensitization

Very rare

Multiform exudative erythema Bullous dermatosis (incl.ч. Stevens-Johnson syndrome)

Toxic epidermal necrolysis (Lyell syndrome)

Renal and urinary tract disorders

Infrequent

Tubulointerstitial nephritis (including.ч. Allergic nephritis)

Nephrotic syndrome

Renal failure

General disorders

Often

Elevated fatigue

Rarely

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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

Similarities