Быструмкапс®

General characteristics. Structure:

Active ingredient: 200 mg of ketoprofen.

Excipients: macrogoal 4000, ethyl cellulose, stearic acid, ammonium methacrylate copolymer, talc, neutral granules (sugar and starch corn [3:1]). Capsular cover: gelatin, titanium dioxide.

Pharmacological properties:

Pharmacodynamics. Ketoprofen is non-steroidal anti-inflammatory drug from group of derivatives of propionic acid. Has the following properties:

• has analgeziruyushchy effect
• possesses febrifugal action
• shows antiinflammatory action
• slows down aggregation of thrombocytes

All above-stated properties are a consequence of a reduction of synthesis of prostaglandins, by non-selective inhibition of activity of cyclooxygenases 1 and 2 of type.

Pharmacokinetics. The BYSTRUMKAPS capsules of 200 mg — contain granules with controlled release of active agent which are intended for reception once a day.

Release of ketoprofen comes from granules gradually in an intestinal path.

Absorption. After oral administration, ketoprofen is almost completely absorbed from an intestinal path, has effect of "the first passing" through a liver.

The maximum concentration in a blood plasma is reached in 6 - 8 h after oral administration of a dose of 200 mg. Does not kumulirut in an organism. Food does not influence the general biological availability of ketoprofen.

Distribution. Ketoprofen for 99% contacts proteins of plasma. Ketoprofen gets into synovial fluid where reaches bigger concentration, than in plasma. In insignificant quantity gets through a placental barrier.

Metabolism. Biotransformation of ketoprofen proceeds in two main ways: by a hydroxylation, and also connection with glucuronic acid; the last is the main way of metabolism.

Less than 1% of the received dose of ketoprofen are found in not changed look in urine, other part is metabolites among which 65 - 75% make metabolites of glucuronic acid.

Removal. It is removed by kidneys. The elimination half-life _(T1/2) makes about 8 hours. Within 5 days after reception of 70-90% of a dose also 1-8% with a stake are allocated with urine.

At elderly people the period of elimination of ketoprofen decreases, and _T1/2 increases, and at persons with a renal failure of T1/2 increases depending on degree of a renal failure.

Indications to use:

Diseases kostno - muscular system and a pain syndrome of various genesis:

• symptomatic treatment of inflammatory and degenerative diseases of a musculoskeletal system (bursitis, synovitis, capsulitis, tendinitis, periarthritis);
• the joint syndrome (pseudorheumatism, the osteoarthritis ankylosing a spondylitis), is intended for symptomatic therapy, reduction of pain and an inflammation at the time of use, does not influence progressing of a disease;
• back pain and backbone (neuralgia, mialgiya, sciatica, lumbago);
• posttraumatic pains (uncomplicated injuries, in particular, sports, injuries of ligaments and sinews, bruises);
• postoperative pains;
• pains at a dysmenorrhea.

Route of administration and doses:

Orally. Adults and teenagers are more senior than 15 years: one capsule of 200 mg of 1 times a day during food

Features of use:

During treatment control of a picture of peripheral blood and a functional condition of a liver and kidneys is necessary.

In need of definition 17 — ketosteroids drug should be cancelled for 48 h prior to a research.

Reception of ketoprofen can mask symptoms of an infectious disease.

At a renal failure and a liver the dose decline and careful observation is necessary.

During treatment it is necessary to be careful during the driving of motor transport and occupation other potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions.

For decrease in risk of development of the undesirable phenomena from a GIT it is necessary to use a minimal effective dose perhaps short course.

Side effects:

From the alimentary system — NPVP — a gastropathy, heartburn, nausea, vomiting, a diarrhea, a lock, a meteorism, a loss of appetite, stomatitis, abdominal pains and in the field of an epigastrium, is rare — taste change. At prolonged use in high doses — an ulceration of a mucous membrane of a GIT, gingival, hemorrhoidal bleeding, perforation of intestines.

From an urinary system — it is rare: cystitis, an urethritis, a renal failure, an acute renal failure, intersticial nephrite, a nephrotic syndrome, a hamaturia, hypostases (especially at patients with arterial hypertension).

From a liver: changes of activity of transaminases can be noted, it is rare — hepatitis.

From a nervous system: excitement, nervousness, drowsiness, a depression, an adynamy, a headache, dizziness, a sleep disorder, sleeplessness, a sonitus, is rare — confusion or a loss of consciousness, forgetfulness, migraine, a peripheral neuropathy.

From outside warmly — vascular system: heart failure, increase in arterial pressure, it is rare — tachycardia.

Hypersensitivity reactions: rhinitis, a Quincke's disease, an acute anaphylaxis, rash, an itch, a small tortoiseshell, an asthmatic attack, especially at patients with hypersensitivity to acetylsalicylic acid, and also to other medicines from the NPVP group.

Skin reactions: photosensitization, alopecia, polymorphic erythema, mnogoformny exudative erythema, including, Stephens-Johnson's syndrome, toxic epidermal necrolysis (Lyell's disease).

From bodies of a hemopoiesis: anemia, a leukopenia, thrombocytopenia, an agranulocytosis, a pancytopenia, it is rare — hemolitic anemia.

From sense bodys: a reversible toxic amblyopia, not clear sight or doubling, it is rare — conjunctivitis, dryness of a mucous membrane of an eye, eye pain, a conjunctiva hyperemia, decrease in hearing.

Others: sweating strengthening, is rare — a pneumorrhagia, nasal bleeding, a mialgiya, muscular twitchings, an asthma, thirst, at prolonged use in high doses - vaginal bleeding.

In case of any by-effects it is necessary to stop administration of drug immediately.

Interaction with other medicines:

To avoid simultaneous use with:

• other NPVP (including, salicylates in high doses), peroral anticoagulants, heparin, tiklopidiny — the risk of emergence of bleedings increases. If use of ketoprofen is necessary, it is necessary to carry out careful monitoring of a condition of the patient;
• lithium — risk of increase in toxic level of lithium in plasma. If it is necessary, during simultaneous use of drugs of lithium and ketoprofen, and also after its termination, it is necessary to make careful monitoring of concentration of lithium in plasma;
• methotrexate (in a dose more than 15 mg/week) — the risk of a gematotoksichnost increases. Intervals before reception of a methotrexate have to be not less than 12 hours from ketoprofen reception.

Strengthens effect of anticoagulants, antiagregant, fibrinolitik, ethanol, side effects of GKS and ISS, estrogen.

Increases concentration in plasma of verapamil and nifedipine.

Myelotoxic medicines strengthen manifestations of a gematotoksichnost of drug.

Reduces hypotensive effect of beta-blockers.

Increases risk of nephrotoxic effect of beta-blockers.

Increases risk of nephrotoxic effect of cyclosporine and a takrolimus, especially at elderly patients.

Reduces contraceptive efficiency of intrauterine spirals. Increases risk of bleedings when using trombolitik.

It is necessary to be careful at use with:

• diuretics and inhibitors of an angiotensin-converting enzyme — easing of diuretic and hypotensive effects and risk of development of a renal failure, at patients with deficit of volume of the circulating blood;
• pentoksifilliny — the risk of developing of bleeding increases;
• zidovudine — increases risk of emergence of anemia (influences reticulocytes with development of anemia).

As well as when using other NPVP it is possible:

• decrease in efficiency of uricosuric medicines;
• increase in risk of formation of ulcers and development of gastrointestinal bleedings and development of renal failures at joint reception with GKS, ethanol, corticotropin;
• increase in risk of bleeding at co-administration with tsefoperazony, tsefamandoly and tsefotetany;
• increase in hypoglycemic effect of insulin and peroral hypoglycemic medicines (recalculation of a dose is necessary);
• increase in products of hydroxylated active metabolites inductors of a microsomal oxidation in a liver (Phenytoinum, ethanol, barbiturates, rifampicin, phenylbutazone, tricyclic antidepressants);
• disturbance of aggregation of thrombocytes at joint appointment with sodium Valproatum;
• antacids and Colestyraminum reduce absorption.

Contraindications:

• Hypersensitivity to ketoprofen or to any component of drug (including, to other NPVP);
• the bronchial asthma, rhinitis or small tortoiseshell in the anamnesis called by ketoprofen, acetylsalicylic acid or other NPVP;
• peptic ulcer of a stomach and 12-perstny gut (aggravation);
• ulcer colitis (aggravation);
• disease Krone;
• diverticulitis;
• round ulcer;
• hemophilia and other disturbances of a blood coagulation;
• active gastrointestinal, cerebrovascular and other bleedings (or suspicion of bleeding);
• heavy renal failure (clearance of creatinine less than 30 ml/min.);
• the progressing diseases of kidneys;
• heavy liver failure or active disease of a liver;
• state after performing aortocoronary shunting;
• the confirmed hyperpotassemia;
• inflammatory diseases of intestines;
• children's age up to 15 years;
• pregnancy (III trimester), lactation period.

With care: anemia, bronchial asthma, alcoholism, tobacco smoking, alcoholic cirrhosis, hyperbilirubinemia, liver failure, dehydration, sepsis, chronic heart failure, hypostases, arterial hypertension, blood diseases (including, a leukopenia), stomatitis, coronary heart disease, cerebrovascular diseases, дислипидемия / a lipidemia, a diabetes mellitus, diseases of peripheral arteries, clearance of creatinine less than 60 ml/min., cankers of the digestive tract (DT) in the anamnesis, existence of an infection of Helicobacter pylori, long use NPVP, heavy somatopathies, a concomitant use of peroral glucocorticosteroids (GKS) (including, Prednisolonum), anticoagulants (including, warfarin), antiagregant (including, клопидогреля), selective serotonin reuptake inhibitors (including, a tsitaloprama, fluoxetine, a paroksetin, sertraline), advanced age, pregnancy (I, II trimester).

Overdose:

At overdose of ketoprofen there can be symptoms of acute poisoning, such as: a headache, dizziness, drowsiness, nausea, vomiting, a diarrhea, pains in epigastric area, a lowering of arterial pressure, a bronchospasm, bleeding from a GIT.

In case of suspicion on overdose it is necessary to see a doctor immediately.

Treatment: immediate phase-out of drug. If from overdose of drug there passed no more than 1 hour, with absorbent carbon in a dose of 60 - 100 g adults, 1 - 2 g/kg of body weight have a gastric lavage at children.
Symptomatic treatment.

Storage conditions:

List B. In the dry, protected from light place at a temperature from 15 °C to 25 °C. To store in places, unavailable to children. Not to apply after the expiry date specified on packaging. A period of validity - 3 years.

Issue conditions:

According to the recipe

Packaging:

Capsules of the prolonged action of 200 mg. On 10 capsules in the blister from PVC and aluminum foil. On 2 blisters together with the application instruction in a cardboard pack.