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)
Modified release capsule with a transparent body and a blue cap; size №1; содержимое капсул – пеллеты белого и желтого цвета.
| 1 caps. | |
| Ketoprofen | 150 mg |
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. – блистеры (2) – пачки картонные.
10 PC. – блистеры (3) – пачки картонные.
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.
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 Cmax
in plasma is 9036.64 ng / ml for 1.76 no.Distribution
Ketoprofen binding to plasma proteins (mostly to albumin) is 99%. Vd – 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. T1/2 – менее 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.
Symptomatic treatment of painful and inflammatory processes of various origins.
Inflammatory and degenerative diseases of the musculoskeletal system:
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.
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: распространенные – диспепсия (nausea, diarrhea or constipation, flatulence, vomiting, decreased or increased appetite), abdominal pain, stomatitis, dry mouth; unextended (long-term use at high doses) – изъязвление слизистой оболочки ЖКТ, abnormal liver function; редкие – перфорация органов ЖКТ, exacerbation of Crohn's disease, ground, gastrointestinal bleeding, transient increase in liver enzymes.
CNS: распространенные – головная боль, dizziness, sleep disturbance, fatiguability, nervousness, nightmares; редкие – мигрень, peripheral polyneuropathy; очень редкие – галлюцинации, disorientation and speech disorder.
From the senses: редкие – шум в ушах, change in taste, blurred vision, conjunctivitis.
Cardio-vascular system: нераспространенные – тахикардия, arterial hypertension, peripheral edema.
From the hematopoietic system: decrease platelet aggregation; редкие – анемия, thrombocytopenia, agranulocytosis, purpura.
From the urinary system: редкие – нарушение функции почек, interstitial nephritis, nephrotic syndrome, hematuria (more likely to develop in people, long-term NSAID users and diuretics).
Allergic reactions: распространенные – кожные реакции (itch, hives); нераспространенные – ринит, breathlessness, bronchospasm, angioedema, anaphylactoid reactions.
Other: редкие – кровохарканье, menometrorrhagia.
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.
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.
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.
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.
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.
The drug is released under the prescription.
The drug should be stored out of reach of children, dark place at a temperature no higher than 25 ° C. Shelf life - 2 year.
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