Abenol ®- film-coated tablets

INSTRUCTIONS FOR MEDICAL USE

ABENOL®

Trade name of the drug: Abenol®

Active substance (INN): Dexetoprofen trometamol

Dosage form: coated tablets

Contents:

1 tablet contains:

Active substance: dexketoprofen trometamol – 36.9 mg (equivalent to 25.0 mg of dexketoprofen)

Excipients of the core: microcrystalline cellulose, corn starch, sodium glycolate starch, glycerin.

Excipients of the shell: hydroxypropyl methylcellulose, polyethylene glycol 4000, titanium dioxide.

Description: Round biconvex white or almost white coated tablets.

Pharmacotherapeutic group: Nonsteroidal anti-inflammatory drugs.

ATX code: M01AE17.

Pharmacological properties

Pharmacodynamics

Dexetoprofen trometamol is the active substance of the drug – NSAID, which has analgesic, anti-inflammatory and antipyretic effects. The mechanism of action is associated with inhibition of GH synthesis at the level of COX-1 and COX-2.

Analgesic effect occurs 30 min after oral administration. The duration of analgesic effect after administration of 50 mg is 4-8 hours.

In combined therapy with analgesics of opioid series dexketoprofen trometamol significantly (up to 30-45%) reduces the need for opioids.

Pharmacokinetics

Absorption. Cmax after dexketoprofen trometamol administration is reached after an average of 30 min (15-60 min). The AUC after a single administration at a dose of 25-50 mg is proportional to the dose as when administered. The corresponding pharmacokinetic parameters are similar after single and repeated administration, indicating that there is no cumulation of the drug.

Distribution. Dexketoprofen trometamol is characterized by high level of binding to plasma proteins (99%). The average value of Vd is less than 0.25 l/kg, the half-distribution time is about 0.35 h.

Excretion. The main way of dexketoprofen excretion is its conjugation with glucuronic acid with following excretion via the kidneys. T1/2 of dexketoprofen trometamol is about 1-2.7 hours. In the elderly there is a prolongation of T1/2 (both after single and repeated administration), on average up to 48%, and a decrease in total clearance of the drug.

Indications for use

  • Control of pain syndrome of different genesis (including postoperative pain, post-traumatic pain, pain due to bone metastases, renal colic, algodysmenorrhea, sciatica, radiculitis, neuralgia, toothache);
  • symptomatic treatment of acute and chronic inflammatory, inflammatory-degenerative and metabolic diseases of the musculoskeletal system (including rheumatoid arthritis, spondyloarthritis, arthrosis, osteochondrosis).

Dosage and administration

Inside, with meals.

Depending on the intensity of the pain syndrome, the recommended dose for adults is 12.5 mg (1/2 tablet) every 4-6 hours or 25 mg (1 tablet) every 8 hours. The maximum daily dose is 75 mg.

In elderly patients and patients with hepatic and/or renal dysfunction, therapy should be started with lower doses. Maximum daily dose is 50 mg.

The drug is not intended for long-term therapy, treatment course should not exceed 3-5 days.

Side effects

Possible side effects when using dexketoprofen trometamol, as well as when using other dexketoprofen preparations, are listed below in descending frequency of occurrence: frequently (1-10% of patients); infrequently (0.1-1% of patients); rarely (0.01-0.1% of patients); very rarely (less than 0.01% of patients), including individual reports.

Blood and lymphatic system disorders: rare – anemia; very rare – neutropenia, thrombocytopenia.

CNS: infrequent – headache, dizziness, insomnia, somnolence, rarely – paresthesia.

Senses: infrequent – blurred vision; rarely – tinnitus.

Cardiovascular system: infrequent – arterial hypotension, fever, skin flushing; rarely – extrasystole, tachycardia, arterial hypertension, peripheral edema, superficial thrombophlebitis.

Respiratory system: rare – bradypnea; very rare – bronchospasm, dyspnea.

Gastrointestinal system: frequently – nausea, vomiting, infrequently – abdominal pain, dyspepsia, diarrhea, constipation, hematemesis, dry mouth, rarely – erosive-ulcerative lesions of the gastrointestinal tract, including bleeding and perforations, anorexia, very rarely – damage to the pancreas.

Liver and gallbladder: rare – increased liver enzymes activity, jaundice; very rare – liver damage.

The urinary system: rare – polyuria, renal colic, very rare – nephritis or nephrotic syndrome.

The reproductive system: rare – menstrual disorders (in women), prostate disorders (in men).

Musculoskeletal system: rare – muscle spasm, difficulty in moving the joints.

Skin: infrequent – dermatitis, rash, sweating, rarely – urticaria, acne, very rare – severe skin reactions (Stevens-Johnson syndrome, Lyell syndrome), angioedema, allergic dermatitis, photosensitization.

Metabolism: rarely – hyperglycemia, hypoglycemia, hypertriglyceridemia.

Laboratory parameters: rarely – ketonuria, proteinuria.

Local and general reactions: infrequent – inflammatory reaction, hematoma, fever, chills, fatigue, rare – back pain, fainting, fever, very rare – anaphylactic shock, facial edema.

Other disorders: aseptic meningitis, occurring mainly in patients with systemic lupus erythematosus or mixed connective tissue diseases, hematologic disorders (purpura, aplastic and hemolytic anemia); rarely – agranulocytosis and bone marrow hypoplasia

Contraindications

  • Hypersensitivity to dexectoprofen or other NSAIDs, or any of the excipients included in the preparation;
  • gastric and duodenal ulcer;
  • gastrointestinal bleeding in the history, other active bleeding (including suspected intracranial bleeding), anticoagulant therapy;
  • gastrointestinal diseases (Crohn’s disease, nonspecific ulcerative colitis);
  • severe liver dysfunction (10-15 points on the Child-Pugh scale);
  • severe renal impairment (creatinine Cl<50 ml/min);
  • bronchial asthma (including anamnesis);
  • severe heart failure;
  • treatment of pain syndrome in case of aortocoronary bypass surgery;
  • hemorrhagic diathesis or other coagulation disorders;
  • childhood.

With caution: history of allergic conditions; hematopoietic disorders; systemic lupus erythematosus or mixed connective tissue diseases; concomitant therapy with other drugs; predisposition to hypovolemia; coronary heart disease; advanced age (over 65 years).

Drug interactions

Undesirable combinations

Concomitant administration of several NSAIDs, including salicylates in high doses (more than 3 g/day) increases the risk of gastrointestinal bleeding and ulcers due to synergistic action.

Concomitant use with oral anticoagulants, heparin in doses higher than prophylactic, and ticlopidine increases the risk of bleeding due to inhibition of platelet aggregation and damage to the gastrointestinal mucosa.

NSAIDs increase the concentration of lithium in blood plasma, up to toxic, in connection with which this indicator should be monitored when prescribing, changing the dose and after withdrawal of NSAIDs.

When used with methotrexate at high doses (15 mg/week or more), hematological toxicity of methotrexate increases due to its decreased renal clearance during NSAID therapy.

When concomitant use with hydantoins and sulfonamides there is a risk of increased toxicity of these drugs.

Combinations requiring caution

If concomitant use with diuretics, ACE inhibitors is necessary, it should be taken into account that NSAID therapy is associated with the risk of acute renal failure in patients with dehydration (decreased glomerular filtration due to inhibition of prostaglandin synthesis). NSAIDs may reduce the hypotensive effect of some drugs. When concomitant use with diuretics, it is necessary to make sure that the patient’s water balance is adequate, and to monitor renal function before prescribing NSAIDs.

When concomitant use with methotrexate at low doses (less than 15 mg/week), hematological toxicity of methotrexate may increase due to its decreased renal clearance during NSAID therapy. It is necessary to monitor the blood cell count weekly during the first weeks of concomitant therapy. In the presence of even mild renal dysfunction, as well as in the elderly, close medical supervision is required.

Simultaneous use with pentoxifylline increases the risk of bleeding. Intensive clinical monitoring and frequent monitoring of bleeding time (clotting time) is necessary.

When concomitant use with zidovudine, there is a risk of increased toxic effects on red blood cells due to the effect on reticulocytes, with the development of severe anemia a week after administration of NSAIDs. All blood cells and reticulocytes should be monitored 1-2 weeks after initiation of NSAID therapy.

Hypoglycemic effect of sulfonylurea derivatives may be increased due to its displacement from binding sites with plasma proteins under the influence of NSAIDs.

When concomitant use with preparations of low molecular weight heparin, the risk of bleeding increases.

Combinations that should be taken into account

NSAIDs may decrease the hypotensive effect of beta-adrenoblockers, which is caused by inhibition of prostaglandin synthesis.

When concomitant use with cyclosporine and tacrolimus, NSAIDs may increase nephrotoxicity, which is mediated by the action of renal prostaglandins. Renal function should be monitored during combination therapy.

When concomitant use with thrombolytics, the risk of bleeding increases.

When concomitant use with probenecid, plasma concentrations of NSAIDs may increase, which may be due to inhibition of renal secretion and/or conjugation with glucuronic acid. This requires adjustment of the NSAID dose.

NSAIDs may cause increased plasma concentrations of cardiac glycosides.

Because of the theoretical risk of prostaglandin inhibitors altering mifepristone’s effectiveness, NSAIDs should not be prescribed any earlier than 8-12 days after mifepristone withdrawal.

Experimental animal data indicate a high risk of convulsions when NSAIDs are prescribed with ciprofloxacin at high doses.

Special indications

In patients with digestive system disorders or gastrointestinal diseases in the anamnesis, constant monitoring is necessary. In case of gastrointestinal bleeding or ulcerous lesions, the drug therapy should be discontinued.

Since all NSAIDs can inhibit platelet aggregation and increase bleeding time due to inhibition of prostaglandin synthesis, simultaneous administration of dexketoprofenatrometamol and low molecular weight heparin drugs in prophylactic doses in the postoperative period has been studied in controlled clinical trials. No effect on coagulation parameters was observed. Nevertheless, when concomitant administration of the drug with other drugs affecting blood clotting, careful medical monitoring is required.

As other NSAIDs, it may increase plasma creatinine and nitrogen levels. Like other inhibitors of prostaglandin synthesis, it may have adverse effects on the urinary system, which may lead to glomerulonephritis, interstitial nephritis, papillary necrosis, nephrotic syndrome and acute renal failure.

During therapy with the drug, as well as other NSAIDs, there may be a slight transient increase in some liver parameters, as well as a significant increase in serum levels of AST and ALT. In this case, monitoring of liver and kidney functions is necessary in elderly patients. In case of significant increase in the corresponding indicators, the drug should be discontinued.

Like other NSAIDs, dexketoprofen tromethamol may mask the symptoms of infectious diseases. In the case of symptoms of bacterial infection or deterioration of well-being during the therapy with the drug, the patient should inform the doctor.

Influence on the ability to drive motor transport and operate machinery

During the drug treatment, due to possible dizziness and somnolence, concentration ability and speed of psychomotor reactions may decrease.

Overdose

Symptoms: nausea, anorexia, abdominal pain, headache, dizziness, disorientation, insomnia.

Treatment: symptomatic therapy; if necessary – gastric lavage, dialysis.

Form of production

25 mg coated tablets, 10 (1×10), 20 (2×10) or 30 (3×10) in a carton pack.

Storage conditions

Store in a dark place at temperatures under 25°C.

Keep out of the reach of children!

Shelf life

3 years. Do not use after the expiration date.

Conditions for dispensing from pharmacies

Released by a doctor’s prescription.

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