Ketonal, 50 mg/ml 2 ml 5 pcs

Pharmacodynamics Ketoprofen is a NSAID with anti-inflammatory, analgesic and antipyretic effects.

By inhibiting COX-1 and -2 and partially lipooxygenase, Ketoprofen inhibits the synthesis of PG and bradykinin and stabilizes lysosomal membranes.

Ketoprofen has no adverse effect on articular cartilage.

Pharmacokinetics

Bioavailability is more than 90%. Binding to plasma proteins – 99%. Cmax of the drug in plasma is reached after 15-30 minutes after parenteral administration. Ketoprofen penetrates into the synovial fluid. Ketoprofen undergoes intensive metabolism through liver microsomal enzymes. It binds to glucuronic acid and is excreted as glucuronide.

Up to 80% of ketoprofen is excreted by the kidneys, mainly (over 90%) in the form of ketoprofen glucuronide, and approximately 10% – through the intestine. Due to the rapid metabolism of ketoprofen its biological T1/2 is less than 2 hours.

Indications

Symptomatic therapy of painful and inflammatory processes of different genesis, including:

Inflammatory and degenerative diseases of the musculoskeletal system:

• rheumatoid arthritis,
• seronegative arthritis (ankylosing spondylitis /bechterew syndrome/, psoriatic arthritis, reactive arthritis /reiter’s syndrome/),<
• podagra, pseudopodagra,
• osteoarthritis.

Pain syndrome:

• headache,
• tendinitis, bursitis, myalgia, neuralgia, sciatica,
• algodysmenorrhea,
• cancer pain syndrome.

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Active ingredient

Ketoprofen

Composition

1 ampoule contains:

active ingredient: ketoprofen – 100 mg;

excipients:

propylene glycol – 800 mg;

ethanol – 200 mg;

benzyl alcohol – 40 mg;

water for injection – up to 2 ml.

How to take, the dosage

For treatment of acute pain syndrome the drug is administered 2 ml 1-2 times per day.

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.

Interaction

Ketoprofen reduces the effect of diuretics, antihypertensive agents.

Enhances the effect of oral hypoglycemic drugs.

Accelerates the effect of some anticonvulsants (e.g., phenytoin).

Concomitant use with other NSAIDs, salicylates, GCS and ethanol increases the risk of gastrointestinal bleeding.

Concomitant use with anticoagulants, thrombolytics, antiaggregants increases the risk of bleeding.

The risk of renal dysfunction increases with concomitant use of diuretics or ACE inhibitors.

Concomitant use increases concentrations of cardiac glycosides, slow calcium channel blockers, lithium preparations, cyclosporine, methotrexate.

Ketoprofen may decrease the effectiveness of mifepristone. NSAIDs should not be started before 8-12 days after withdrawal of mifepristone.

Special Instructions

Ketonal may be washed with milk or taken with antacids in order to reduce the frequency of gastrointestinal disorders (milk and antacids do not affect absorption of ketoprofen).

When prolonged use of NSAIDs, the blood count and hepatic and renal function should be monitored, especially in elderly patients.

Caution should be exercised and BP should be monitored more frequently when using ketoprofen to treat patients with arterial hypertension, cardiovascular disease, which leads to fluid retention.

Like other NSAIDs, ketoprofen can mask the symptoms of infectious diseases.

Influence on driving and operating machinery

There are no data on adverse effects of Ketoprofen in recommended doses on the ability to drive or operate machinery. However, patients who have noted unusual effects while taking Ketonal® should be cautious when driving or operating machinery during potentially dangerous activities requiring increased concentration and rapid psychomotor reaction time.

Contraindications

• bronchial asthma, rhinitis, urticaria in the anamnesis caused by taking acetylsalicylic acid or other NSAIDs,
• gastric and duodenal ulcer in the acute phase,
• NEC, Crohn’s disease,
• hemophilia and other blood clotting disorders,
• severe liver failure,
• severe renal failure,
• uncompensated heart failure,
• a postoperative period after aortocoronary bypass,
• gastrointestinal, cerebrovascular, and other bleeding (or suspected bleeding),
• chronic dyspepsia,
• high sensitivity to ketoprofen or other components of the drug, and salicylates or other NSAIDs.

With caution: the drug should be prescribed in case of a history of peptic ulcer disease, history of bronchial asthma, clinically pronounced cardiovascular, cerebrovascular disease, peripheral artery disease, dyslipidemia, liver failure, hyperbilirubinemia, alcoholic liver cirrhosis, renal failure, chronic heart failure, arterial hypertension, In addition, the following conditions should be adhered to: – blood diseases, dehydration, diabetes, history of peptic ulcer disease, smoking, concomitant therapy with anticoagulants (e.g., warfarin), antiplatelet agents (e.g., acetylsalicylic acid), oral GCS (e.g., prednisolone), selective serotonin reuptake inhibitors (e.g., citalopram, sertraline).

Side effects

Prevalence of adverse reactions:

• Very common ( > 10%).
• Prevalent ( > 1%, but < 10%).
• Uncommon ( > 0.1%, but < 1%).
• Rare ( > 0.01%, but < 0.1%).
• Very rare ( < 0.01%).

Digestive system disorders: widespread – dyspepsia (nausea, flatulence, diarrhea or constipation, vomiting, decreased or increased appetite), abdominal pain, stomatitis, dry mouth; non-spread (with long-term use in high doses – ulceration of the mucous membrane of the GIT, liver function disorders); rare – GIT perforation, worsening Crohn’s disease, melena, GIT bleeding, transient increase in liver enzymes.

CNS and peripheral nervous system disorders: common – headache, dizziness, drowsiness, fatigue, nervousness, nightmares; rare – migraine, peripheral neuropathy; very rare – hallucinations, disorientation, speech disorders.

Sensory organs: rare – tinnitus, change in taste, blurred vision, conjunctivitis.

Cardiovascular system disorders: rare – tachycardia, arterial hypertension, peripheral edema.

Hematopoietic system: decreased platelet aggregation; rare – anemia, thrombocytopenia, agranulocytosis, purpura.

Urinary system disorders: rare – renal dysfunction, interstitial nephritis, nephrotic syndrome, hematuria (with prolonged use of NSAIDs and diuretics).

Allergic reactions: common – itching, urticaria; non-spread – rhinitis, dyspnea, bronchospasm, angioedema, anaphylactoid reactions.

Others: rare – hemoptysis, metrorrhagia.

Overdose

Symptoms: vomiting, melena, seizures, nausea, abdominal pain, vomiting blood, renal failure, impaired consciousness, respiratory depression, impaired renal function.

Treatment: gastric lavage, administration of activated charcoal, symptomatic therapy. Histamine H2-receptor blockers, prostaglandin inhibitors, proton pump inhibitors are indicated. There is no specific antidote.

Similarities

Ketonal, OKI, Bystromgel, Febrofid, Flamax forte, Ketoprofen, Flamax, Fastum, Rocketal Rompharm, Pentalgin extra-gel, Ketonal DUO, Ketoprovel, OKI ACT, Brustel