Pelubio^® (Tablets) Instructions for Use

Marketing Authorization Holder

Akrikhin Chemical and Pharmaceutical Plant, JSC (Russia)

Manufactured By

Devon Pharma, Co. Ltd. (Republic of Korea)

Packaging and Quality Control Release

DEVON PHARMA, Co. Ltd. (Republic of Korea)

Or

PHARMSTANDARD-LEKSREDSTVA, JSC (Russia)

ATC Code

M01AX (Other non-steroidal anti-inflammatory drugs)

Active Substance

Pelubiprofen (Rec.INN registered by WHO)

Dosage Form

Pelubio®

Tablets 30 mg: 10, 20, 30, 60 or 100 pcs.

Dosage Form, Packaging, and Composition

Tablets light yellow in color, round, flat-cylindrical, with a bevel; an engraving is applied: on one side – “PE”, on the other side – “P” and 4 wavy lines.

Excipients : lactose monohydrate – 47.9 mg, low-substituted hypromellose – 18 mg, carmellose calcium – 10 mg, hypromellose – 2.1 mg, magnesium stearate – 1.9 mg, yellow iron oxide dye – 0.1 mg.

10 pcs. – blister packs (1) – cardboard packs.
10 pcs. – blister packs (2) – cardboard packs.
10 pcs. – blister packs (3) – cardboard packs.
10 pcs. – blister packs (6) – cardboard packs.
10 pcs. – blister packs (10) – cardboard packs.
30 pcs. – polyethylene jars (1) – cardboard packs.

Clinical-Pharmacological Group

NSAID

Pharmacotherapeutic Group

Anti-inflammatory and antirheumatic drugs; non-steroidal anti-inflammatory and antirheumatic drugs; other non-steroidal anti-inflammatory and antirheumatic drugs

Pharmacological Action

NSAID, a derivative of arylpropionic acid, which is structurally and pharmacologically related to ibuprofen. The mechanism of action is due to non-selective inhibition of the enzymes – COX-1 and COX-2, which leads to inhibition of the synthesis of prostaglandins – mediators of pain, inflammation and hyperthermic reaction.

Pelubiprofen has analgesic, anti-inflammatory and antipyretic effects. The analgesic effect is most pronounced in inflammatory pain.

It is intended for symptomatic therapy, reducing pain and inflammation at the time of use, does not affect the progression of the disease.

Pharmacokinetics

After oral administration, it is rapidly absorbed from the gastrointestinal tract. Food intake has practically no effect on pharmacokinetic parameters. C_max is reached within 2 hours. It is rapidly distributed in the liver and kidneys. The binding of pelubiprofen and its metabolites to plasma proteins is 93.3-98.9%. Most of the active substance is metabolized to form metabolites (trans-OH, cis-OH forms, unsaturated OH form and saturated ketone form). The main active metabolites (trans-OH, and unsaturated OH form) are formed at a high rate. It is excreted by the kidneys and through the intestines. More than 60% is excreted by the kidneys and through the intestines within 24 hours. It is excreted in breast milk, but the concentration of the active substance in it is lower than in blood plasma.

Indications

Osteoarthritis; rheumatoid arthritis; back pain.

ICD codes

Dosage Regimen

Administer orally after meals to reduce gastrointestinal irritation.

The standard adult dosage is 30 mg three times daily.

Do not exceed the maximum daily dose of 90 mg.

Prior to initiation, assess the risk-benefit ratio and consider alternative therapeutic options.

Use the lowest effective dose for the shortest possible duration consistent with individual treatment goals.

For elderly patients and those with mild to moderate renal or hepatic impairment, initiate therapy at the lower end of the dosing range.

Monitor renal function and adjust dosage if necessary in patients with compromised renal function.

Re-evaluate the need for continued therapy periodically.

Discontinue treatment if signs of liver injury (e.g., elevated liver enzymes) or gastrointestinal bleeding occur.

Avoid concomitant use with other NSAIDs, including aspirin, due to increased risk of adverse effects.

Adverse Reactions

Infectious and parasitic diseases common – upper respiratory tract infections; uncommon – viral infections.

Blood and lymphatic system disorders uncommon – leukocytosis, increased blood potassium concentration; frequency unknown – anemia, prolonged bleeding time.

Immune system disorders frequency unknown – anaphylactoid reactions.

Nervous system disorders common – headache, dizziness; uncommon – drowsiness, stupor, insomnia, severe dizziness, paresthesia, pain.

Eye disorders uncommon – dry eyes, floaters before the eyes.

Ear and labyrinth disorders uncommon – tinnitus.

Cardiovascular system disorders uncommon – chest pain, sinus tachycardia, sinus bradycardia, myocardial infarction, myocardial ischemia, arterial hypotension, arterial hypertension; frequency unknown – stroke.

Respiratory system disorders uncommon – respiratory distress syndrome, cough, nosebleed, sore throat.

Endocrine system disorders uncommon – hyperglycemia.

Digestive system disorders common – abdominal pain, heartburn, dyspepsia, nausea, vomiting, diarrhea; uncommon – epigastric discomfort, constipation, loss of appetite, bloating, glossitis, stomatitis, increased appetite; frequency unknown – gastrointestinal bleeding, ulcer formation, stomach or intestinal perforation.

Hepatobiliary disorders uncommon – increased liver enzyme activity; frequency unknown – jaundice, fulminant hepatitis, liver necrosis, liver failure.

Skin and subcutaneous tissue disorders uncommon – skin redness, urticaria, xeroderma, alopecia; frequency unknown – exfoliative dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis.

Musculoskeletal and connective tissue disorders uncommon – muscle pain, back pain, arthrosis, fractures.

Renal and urinary disorders common – fluid retention, edema, including facial edema; uncommon – frequent urination, pain in the urinary tract, renal papillary necrosis, worsening of renal failure.

Reproductive system and breast disorders uncommon – oliguria, vaginitis, vaginal bleeding.

General disorders uncommon – asthenia, weight gain, chills, fever, pallor, weight loss.

Laboratory and instrumental data uncommon – increased plasma urea concentration, aleukemia, hypercholesterolemia.

Contraindications

Hypersensitivity to pelubiprofen; peptic ulcer in the acute phase; severe hemostasis system disorders; severe liver dysfunction; severe renal dysfunction; severe heart failure; arterial hypertension of the 3rd degree and/or 3rd stage; history of bronchial asthma, urticaria or allergic reactions after taking aspirin or other NSAIDs; treatment of perioperative pain in coronary artery bypass surgery; children and adolescents under 18 years of age; pregnancy, breastfeeding period; simultaneous use with aspirin or other NSAIDs.

With caution

Patients with peptic ulcer disease (outside exacerbation); with a history of gastrointestinal bleeding; with disorders of the blood coagulation system, having a risk of bleeding (except for severe hemostasis system disorders); with mild to moderate liver dysfunction; with mild to moderate renal dysfunction; with cardiovascular diseases and risk factors for cardiovascular diseases; with arterial hypertension of the 1st-2nd degree, 1st-2nd stage; with bronchial asthma and other allergic diseases/conditions (except NSAID-associated); systemic lupus erythematosus; with connective tissue diseases; with ulcerative colitis; with Crohn’s disease; elderly patients, debilitated patients; smoking patients; chronic alcoholism; patients taking ACE inhibitors, furosemide, thiazide diuretics, lithium preparations, methotrexate, indirect anticoagulants, oral corticosteroids.

Use in Pregnancy and Lactation

Contraindicated for use during pregnancy and breastfeeding.

Use in Hepatic Impairment

Contraindication: severe liver dysfunction.

Use in Renal Impairment

Contraindication: severe renal dysfunction.

Pediatric Use

Contraindicated for use in children and adolescents under 18 years of age.

Geriatric Use

Use with caution. To reduce the risk of adverse reactions in elderly patients, the lowest effective dose should be used for a short duration. Careful medical monitoring of the patient’s condition should be carried out.

Special Precautions

All patients receiving Pelubiprofen should be monitored for the development of possible adverse reactions. Patients with acute inflammatory processes, pain syndrome, fever, elderly patients, and debilitated patients require particularly careful medical monitoring.

Since Pelubiprofen has anti-inflammatory and antipyretic effects, its use may mask the clinical symptoms of infectious complications of non-infectious diseases and conditions accompanied by pain syndrome.

Patients with inflammation of infectious origin receiving pelubiprofen therapy should be under careful medical supervision.

Patients receiving NSAIDs for a long time should periodically monitor general and biochemical blood test parameters. If clinical signs and symptoms of liver or kidney disease occur, systemic reactions develop (including eosinophilia, rash), abnormalities develop or liver tests worsen, Pelubiprofen should be discontinued and the possibility of prescribing alternative therapy not containing NSAIDs should be considered.

In patients taking 3 or more alcohol units per day, Pelubiprofen increases the risk of gastrointestinal bleeding. Such patients should be advised to abstain from alcohol and consider replacing pelubiprofen with an alternative drug with anti-inflammatory and antipyretic effects.

Pelubiprofen and other NSAIDs can cause or worsen arterial hypertension, which may contribute to an increase in the frequency of adverse reactions from the cardiovascular system. In patients with arterial hypertension (except for arterial hypertension of the 3rd degree and/or 3rd stage), Pelubiprofen should be used with caution. Blood pressure should be monitored from the very beginning and throughout the course of pelubiprofen therapy.

In patients taking thiazide or “loop” diuretics, the effectiveness of therapy when taken together with NSAIDs may be reduced.

Pelubiprofen may increase the risk of myocardial infarction and stroke. The risk is higher with long-term use of pelubiprofen, as well as in patients with cardiovascular diseases or risk factors for such diseases.

Factors that increase the risk of gastrointestinal bleeding during NSAID therapy include: long-term course of NSAID therapy, simultaneous use of NSAIDs with oral corticosteroids or anticoagulants, smoking, alcohol consumption, old age, debilitated body. Particular caution should be exercised when prescribing pelubiprofen to patients with a history of peptic ulcer disease and/or gastrointestinal bleeding, in whom the risk of developing gastrointestinal bleeding is characterized by a 10-fold increase. Most reports of fatal cases are associated with adverse reactions from the gastrointestinal tract in elderly or debilitated patients.

Effect on ability to drive vehicles and operate machinery

Due to the possibility of visual impairment, dizziness, drowsiness and other symptoms from the central nervous system, patients receiving Pelubiprofen should exercise caution when driving vehicles and performing other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Drug Interactions

Pelubiprofen can enhance the effects of other drugs.

Simultaneous use with other NSAIDs should be avoided.

NSAIDs may reduce the antihypertensive effect of ACE inhibitors. This should be taken into account in patients taking Pelubiprofen together with ACE inhibitors.

There is no convincing evidence that the simultaneous use of acetylsalicylic acid and NSAIDs reduces the risk of serious cardiovascular thrombotic events. Simultaneous use of acetylsalicylic acid and NSAIDs increases the risk of serious adverse reactions from the gastrointestinal tract. Such combinations are not recommended.

Clinical studies have shown that NSAIDs can reduce the natriuretic effect of furosemide and thiazide diuretics in some patients. This is due to inhibition of prostaglandin synthesis in the kidneys. When prescribing NSAIDs together with furosemide and thiazide diuretics, careful monitoring of renal function is necessary.

NSAIDs cause an increase in lithium levels in blood plasma and a decrease in renal clearance of lithium. This effect is explained by the suppression of renal prostaglandin synthesis. When prescribing NSAIDs together with lithium, careful monitoring is necessary to identify symptoms of lithium intoxication.

When prescribing NSAIDs together with methotrexate, the toxicity of the latter may increase. Caution is required when used simultaneously.

Warfarin and NSAIDs can have a synergistic effect, provoking gastrointestinal bleeding. In patients taking both groups of drugs simultaneously, the risk of serious gastrointestinal bleeding is higher than when taken separately. If it is necessary to use pelubiprofen together with indirect anticoagulants, caution is required.

Alcohol consumption during treatment with pelubiprofen is associated with an increased risk of gastrointestinal bleeding.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.