Ketonal Duo: instructions for using the medicine, structure, Contraindications

Active material: Ketoprofen
When ATH: M01AE03
CCF: NSAIDs
ICD-10 codes (testimony): M02, M02.3, M05, M07, M10, M15, M45, M54.1, M65, M70, M71, M79.1, M79.2, N94.4, N94.5, R51, R52.0, R52.2
When CSF: 05.01.01.06
Manufacturer: LEK d.d. (Slovenia)

Ketonal Duo: dosage form, composition and packaging

Modified release capsule with a transparent body and a blue cap; size №1; contents of capsules – Pellets white and yellow.

Excipients: microcrystalline cellulose, lactose monohydrate, povidone, Croscarmellose sodium, polysorbate 80.

The composition of the shell pellets: eudragit RS 30D (ethyl acrylate copolymer, methyl methacrylate and trimetilammonioetilmetakrilata (1:2:0.1)), éudragit RL 30D (ethyl acrylate copolymer, methyl methacrylate and trimetilammonioetilmetakrilata (1:2:0.2)), triэtiltsitrat, polysorbate 80, talc, gland (III) oxide yellow (E172), colloidal silicon dioxide.
Ingredients of the capsule shell: gelatin, indigokarmin (E132), Titanium dioxide (E171).

10 PC. – blisters (2) – packs cardboard.
10 PC. – blisters (3) – packs cardboard.

Ketonal Duo: pharmachologic effect

NSAIDs. It has analgesic, anti-inflammatory and antipyretic effect.

Due to the inhibition of COX-1 and COX-2, and partially lipoxygenase, Ketoprofen inhibits the synthesis of prostaglandins and bradykinin, stabilizes the lysosomal membrane.

Ketoprofen has no negative effect on the articular cartilage.

Ketonal Duo: pharmacokinetics

Absorption

Capsules Ketonal^® Duo presented in a new dosage form, different from the usual special capsules release the active substance. Capsules contain two types of pellets: white (about 60% of total) and yellow (coated). Ketoprofen is rapidly released from the white pellets and slowly from yellow, which causes a combination of fast and long-acting.

After oral administration, ketoprofen is well absorbed from the gastrointestinal tract.

Bioavailability of ketoprofen in the form of conventional capsules, modified-release capsules is 90%.

When food intake does not affect the overall bioavailability (AUC) ketoprofen, but reduces the rate of absorption. After oral dose of ketoprofen 150 mg in capsules modified release C_max in plasma is 9036.64 ng / ml for 1.76 no.

Distribution

Ketoprofen binding to plasma proteins (mostly to albumin) is 99%. V_d – 0.1-0.2 l / kg. Ketoprofen is well into the synovial fluid, where it reaches the 30% plasma concentrations. Significant concentration of ketoprofen in synovial fluid and maintained until stable 30 no, whereby a long time is reduced pain and stiffness of the joints.

Metabolism and excretion

Ketoprofen is extensively metabolized with the participation of microsomal liver enzymes. It binds to glucuronic acid and excreted as glucuronide. No active metabolites of ketoprofen. T_1/2 – less 2 no.

About 80% Ketoprofen is excreted in the urine, primarily as glucuronide metabolite. 10% displayed through the intestines.

Pharmacokinetics in special clinical situations

In patients with hepatic insufficiency, increased plasma concentration of ketoprofen in 2 times probably due to hypoalbuminemia (and due to the high level of unbound ketoprofen active); such patients should be prescribed the drug in a minimal therapeutic dose.

In patients with renal impairment reduces the clearance of ketoprofen, requiring dose adjustment.

Elderly patients metabolism and excretion of ketoprofen slowed, but it has clinical significance only for patients with reduced renal function.

Ketonal Duo: testimony

Symptomatic treatment of painful and inflammatory processes of various origins.

Inflammatory and degenerative diseases of the musculoskeletal system:

• rheumatoid arthritis;
• seronegative arthritis (ankiloziruyushtiy spondylitis / bolezny spondylitis /, psoriaticheskiy arthritis, reactive arthritis / Reiter's syndrome /);
• gout, pseudogout;
• osteoarthritis.
• Pain syndrome:
• headache;
• Tendinitis, ʙursit, myalgia, neuralgia, radiculitis;
• posttraumatic pain;
• post-operative pain;
• algomenorrhea;
• pain syndrome in cancer.

Ketonal Duo: dosing regimen

The standard dose Ketonal^® Duo for adults and children over 15 years is 150 mg / day. The capsules should be taken during or after a meal, drinking water or milk (fluid volume should be at least 100 ml).

The maximum dose of ketoprofen 200 mg / day.

Ketonal Duo: side effects

The incidence of adverse events characterized as very common (>10%), common (>1% <10%), unextended (>0.1% <1%), few (>0.01% < 0.1%) and very rare (< 0.01%).

From the digestive system: common – dyspepsia (nausea, diarrhea or constipation, flatulence, vomiting, decreased or increased appetite), abdominal pain, stomatitis, dry mouth; unextended (long-term use at high doses) – ulceration of the gastrointestinal mucosa, abnormal liver function; few – perforation of the digestive tract, exacerbation of Crohn's disease, ground, gastrointestinal bleeding, transient increase in liver enzymes.

CNS: common – headache, dizziness, sleep disturbance, fatiguability, nervousness, nightmares; few – migraine, peripheral polyneuropathy; very rare – hallucinations, disorientation and speech disorder.

From the senses: few – noise in ears, change in taste, blurred vision, conjunctivitis.

Cardio-vascular system: unextended – tachycardia, arterial hypertension, peripheral edema.

From the hematopoietic system: decrease platelet aggregation; few – anemia, thrombocytopenia, agranulocytosis, purpura.

From the urinary system: few – impairment of renal function, interstitial nephritis, nephrotic syndrome, hematuria (more likely to develop in people, long-term NSAID users and diuretics).

Allergic reactions: common – skin reactions (itch, hives); unextended – rhinitis, breathlessness, bronchospasm, angioedema, anaphylactoid reactions.

Other: few – hemoptysis, menometrorrhagia.

Ketonal Duo: Contraindications

• bronchial asthma, rhinitis, urticaria history, caused by taking aspirin or other NSAIDs;
• gastric ulcer and duodenal ulcer in the acute phase;
• NYAK, Crohn's disease exacerbation, inflammatory bowel disease in the acute stage;
• hemophilia and other bleeding disorders;
• severe hepatic insufficiency;
• severe renal insufficiency;
• progressive kidney disease;
• decompensated heart failure;
• postoperative period after coronary artery bypass grafting;
• gastrointestinal, and other cerebrovascular bleeding (or suspected bleeding);
• hronicheskaya dyspepsia;
• Children up to age 15 years;
• III trimester of pregnancy;
• lactation (breast-feeding);
• hypersensitivity to ketoprofen or other components of the drug, and salicylates or other nonsteroidal antiinflammatory drugs.

FROM caution should be prescribed the drug for peptic ulcer history, bronchial asthma in history, symptomatic cardiovascular, cerebrovascular disease and peripheral arterial disease, dyslipidaemia, progressive liver disease, giperʙiliruʙinemii, alcoholism, renal failure, chronic heart failure, hypertension, blood diseases, degidratacii, diabetes, anamnestic data on the development of ulcerative lesions GIT, smoking, concomitant anticoagulant therapy (eg, warfarin), antiplatelet (eg, acetylsalicylic acid), oral corticosteroids (eg, prednisolone), selective serotonin reuptake inhibitors (eg, citalopram, sertraline), Long-term use of NSAIDs.

Ketonal Duo: Pregnancy and lactation

The use of ketoprofen in the III trimester of pregnancy is contraindicated. In I and II trimesters of pregnancy, use of the drug is possible only in the case, if the expected benefit to the mother outweighs the potential risk to the fetus.

When taken during lactation should decide the issue of termination of breastfeeding.

Ketonal Duo: Special instructions

With prolonged use of NSAIDs is necessary to control blood condition, as well as renal and hepatic function, especially in elderly patients (senior 65 years).

Care should be taken more frequently monitor blood pressure during the application of ketoprofen to treat patients with hypertension, cardiovascular diseases, which lead to fluid retention.

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

Effects on ability to drive vehicles and management mechanisms

Information about the negative impact Ketonal^® Duo at recommended doses on the ability to drive a car or operate machinery No. At the same time, patients, marking custom effects while taking Ketonal^® Duo, Caution should be exercised when engaging in potentially hazardous activities, require high concentration and speed of psychomotor reactions.

Ketonal Duo: overdose

Symptoms: nausea, vomiting, stomach ache, vomiting blood, ground, disturbance of consciousness, respiratory depression, convulsions, impairment of renal function and renal failure.

Treatment: It is shown in overdose gastric lavage and use of activated carbon. Symptomatic therapy. Impact of ketoprofen on the gastrointestinal tract can be reduced by a histamine H₂-receptors, proton pump inhibitors and prostaglandins.

Ketonal Duo: drug interaction

Ketoprofen may weaken the effect of diuretics and antihypertensive drugs, and increase the effects of oral hypoglycemic and certain anticonvulsants (phenytoin).

The combined use with other NSAIDs, salicylates, GCS, ethanol increases the risk of adverse effects on the gastrointestinal tract.

Co-administration with anticoagulants, thrombolytics, antiplatelet agents increases the risk of bleeding.

At the same time taking NSAIDs with diuretics or ACE inhibitors increases the risk of renal dysfunction.

Increases in plasma concentration of cardiac glycosides, blockers slow calcium channels, lithium preparations, cyclosporine, methotrexate.

NSAIDs may reduce the effectiveness of mifepristone. NSAID should be started no earlier than, than 8-12 days after discontinuation of mifepristone.

Ketonal Duo: terms of dispensing from pharmacies

The drug is released under the prescription.

Ketonal Duo: terms and conditions of storage

The drug should be stored out of reach of children, dark place at a temperature no higher than 25 ° C. Shelf life – 2 year.