Abenol® Neo- injection

INSTRUCTIONS FOR MEDICAL USE

ABENOL NEO

Trade name of the drug: Abenol® Neo

Active substance (INN): Ketoprofen

Pharmaceutical form: Solution for injection.

Contents:

2 ml of the solution (1 ampoule) contains:

active substance: ketoprofen 100 mg;

Excipients: propylene glycol, 96% ethyl alcohol, benzyl alcohol, sodium metabisulfite, sodium hydroxide, sodium hydroxide 1M solution, water for injection.

Description: Clear, colorless or slightly yellowish solution.

Pharmacotherapeutic group: Nonsteroidal anti-inflammatory drug.

ATX code: M01AB15.

Pharmacological properties

Ketoprofen is a non-steroidal anti-inflammatory agent, a derivative of propionic acid. It has analgesic, anti-inflammatory and antipyretic effects. Mechanism of action is related to inhibition of cyclooxygenase-1 and cyclooxygenase-2 activity and decrease in prostaglandin biosynthesis, which play the major role in pathogenesis of inflammation, pain and fever.

Ketoprofen has a pronounced analgesic effect due to two mechanisms: peripheral – mediated by inhibition of prostaglandin synthesis in tissues, and central – due to inhibition of prostaglandin synthesis in central and peripheral nervous system and also due to the effect on biological activity of other neurotropic substances which play a key role in release of pain mediators in the spinal cord. In addition, ketoprofen has anti-bradykinin activity, stabilizes lysosomal membranes, causes significant inhibition of neutrophil activity in patients with rheumatoid arthritis. Inhibits platelet aggregation.

Pharmacokinetics

Bioavailability is 90%. Maximum concentration (Cmax) in blood is reached within 30 minutes. The degree of binding to proteins, mainly to albumin, is 99%. Volume of distribution (Vd) is 0.1 – 0.2 l/kg.

Ketoprofen penetrates rapidly through the blood-brain barrier and into the synovial fluid. Concentration of ketoprofen in synovial fluid is lower than in blood, but it stays there for a longer time, which determines the long-term action of the drug.

After intramuscular (I/m) introduction of 100 mg, after 3 hours the drug concentration in blood plasma is 3 µg/ml, and in synovial fluid – 1.5 µg/ml; after 4 hours the concentration in blood plasma is 0.3 µg/ml, and in synovial fluid – 0.8 µg/ml.

Significant levels of concentrations in synovial fluid are reached 15 min after a single intravenous injection of ketoprofen at a dose of 100 mg.

Ketoprofen is mainly metabolized in the liver via microsomal oxidation reactions to form conjugates.

The elimination half-life (T½ ) of ketoprofen is 2 hours. It is eliminated mainly in the urine (more than 50% as metabolites), 1% is eliminated in the faeces.

INDICATIONS FOR USE

Symptomatic therapy of painful inflammatory processes of different genesis:

  • rheumatoid arthritis;
  • ankylosing spondylitis;
  • psoriatic arthritis;
  • reactive arthritis;
  • gout, pseudopodagra;
  • osteoarthritis;
  • Extra-articular rheumatism (tendinitis, bursitis, shoulder capsulitis).

Pain syndrome (including post-operative and post-traumatic pain, algodysmenorrhea, pain from tumor metastases).

Dosage and administration

The drug is administered parenterally (intramuscular (IV/m) and intravenously (IV)).

For treating acute pain syndrome the drug is administered 2 ml (100 mg) 1 to 2 times a day in a car. The duration of parenteral therapy is usually several days. After achieving the desired effect, the drug is prescribed in the form of capsules, tablets or suppositories.

Infusion of the drug is administered only in hospitals.

For an intermittent IV infusion of 100-200 mg of ketoprofen is diluted in 100 ml of isotonic solution (0.9%) of sodium chloride for injection and given for 0.5-1 hours; after 8 hours the injection is repeated. Maximum daily dose is 300 mg.

For continuous intravenous infusion 100-200 mg of ketoprofen is diluted in 500 ml of infusion solution (0.9% sodium chloride solution for injection, Ringer’s solution with lactate, dextrose (glucose) solution) and infused for 8 hours; after 8 hours the preparation is repeated.

Ketoprofen can be combined with centrally acting analgesics.

Ketoprofen solution must not be mixed with tramadol in the same vial, as this produces a precipitate.

The bottle with infusion solution containing ketoprofen should be wrapped in dark paper or aluminum foil because ketoprofen decomposes in light.

Side effects

Digestive system: dyspepsia, nausea, flatulence, abdominal pain, diarrhea, constipation, anorexia, vomiting, stomatitis. There are separate reports on the development of colitis, intestinal perforation (as a complication of diverticulitis), exacerbation of ulcerative colitis and Crohn’s disease. Less than 0.1% have enteropathy with perforation, adhesions, intestinal ulcers; in enteropathy bleeding is possible; in 1% of patients after 3-6 months of treatment and in 2-4% of patients after 12 months of treatment there were cases of GI ulcers, bleeding, small intestine perforation. There are some reports of hepatitis development, marked liver function abnormalities with jaundice. Changes in liver function tests values were observed in 15% of patients; sometimes (less than 1% of patients) significant increase of ALT or AST is noted.

CNS: 1-3% – depression, nervousness, nightmares, somnolence; 0.1% – disorientation, delirium with visual and auditory hallucinations, speech disorders; asthenia, weakness, dizziness, headache.

Sensory organs: 1-3% – visual impairment, conjunctivitis (after oral administration), tinnitus.

Respiratory system: rarely – hemoptysis, dyspnea, rhinitis, bronchospasm, increased attacks of bronchial asthma.

Cardiovascular system: edema (2%); sometimes (1%) – congestive heart failure, arterial hypertension.

Blood system: less than 1% – agranulocytosis, anemia, hemolysis, purpura, thrombocytopenia. When using the drug in high doses – inhibition of platelet aggregation, prolongation of bleeding time, bruising, hemorrhage. Dermatological reactions: 1-3% – skin rash; less than 1% – alopecia, eczema, exfoliative dermatitis, erythema multiforme, lichenoid dermatitis, photosensitivity reactions. There are reports of the development of Stevens-Johnson syndrome and toxic epidermal necrolysis.

Urinary system: acute renal failure, interstitial nephritis, nephrotic syndrome, acute pyelonephritis.

Allergic reactions: rarely – urticaria, angioedema. Local reactions: at the injection site, a reaction in the form of burning and/or pain.

Contraindications

  • Gastrointestinal erosive and ulcerative lesions in the acute phase;
  • Severe heart failure;
  • Severe liver dysfunction;
  • Severe renal dysfunction;
  • susceptibility to bleeding;
  • Chronic dyspepsia in anamnesis;
  • Bronchial asthma, rhinitis;
  • pregnancy;
  • lactation (breast-feeding);
  • Children under 15 years of age;
  • Hypersensitivity to ketoprofen, acetylsalicylic acid or other NSAIDs.

Drug interactions

When used concomitantly, ketoprofen may reduce the effect of diuretics and antihypertensive drugs.

Concomitant use of ketoprofen and diuretics or ACE inhibitors increases the risk of impaired renal function.

When concomitant use of ketoprofen and cardiac glycosides, lithium drugs, cyclosporine and methotrexate their toxicity increases due to decreased excretion. Ketoprofen can decrease the effect of mifepristone, so there should be at least 8-12 days between mifepristone treatment and initiation of ketoprofen therapy. Acetylsalicylic acid reduces the degree of binding of ketoprofen to plasma proteins. Combined use of ketoprofen with other salicylates should be avoided.

Special indications

Caution should be exercised when prescribing the drug in patients with a history of gastrointestinal diseases due to the risk of gastrointestinal bleeding or gastrointestinal perforation. Caution should be exercised when prescribing to patients with blood clotting disorders, hemophilia, Willebrand’s disease, severe thrombocytopenia, renal and hepatic insufficiency.

Ketoprofen may mask the symptoms of infectious diseases.

Caution should be exercised when prescribing ketoprofen to patients with arterial hypertension and cardiovascular diseases, which are characterized by fluid retention in the body. BP should be monitored regularly (especially in patients with cardiovascular disease).

During long-term treatment with ketoprofen, especially in elderly patients, systematic monitoring of blood count, as well as liver and kidney function, is necessary. If creatinine clearance is less than 0.33 ml/s (20 ml/min), the dose of ketoprofen should be adjusted.

Ketoprofen should be discontinued before surgical intervention.

The solution for injection contains ethanol. Each ampoule (2 ml) contains 200 mg of ethanol, which should be taken into account when prescribing the drug to patients who abuse alcohol, patients with trauma or with brain diseases. Alcohol intake should be avoided during treatment with ketoprofen.

When using the drug, caution should be exercised by persons whose activities require quick psychomotor reactions (driving a car, working with mechanisms), because the drug may cause drowsiness and dizziness.

Overdose

There are few data on overdose of parenteral forms of the drug.

The following symptoms are possible: headache, dizziness, nausea, vomiting, epigastric pain, bloody vomiting, darkened stool, confusion, difficulty in breathing, convulsions, renal failure and renal failure.

Treatment: No specific antidote exists. Symptomatic therapy, histamine H2-receptor blockers, proton pump inhibitors and prostaglandins are used.

Form of production

Solution for injection 100 mg/2 ml in 2 ml ampoules.

Storage conditions

Store in a dark place at temperatures not exceeding 25°C. Keep out of the reach of children!

Shelf life

3 years. Do not use after the expiration date.

Conditions of dispensing from pharmacies

Released by a doctor’s prescription.

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