Ketotop

General characteristics. Structure:

Active agent - ketoprofen (in terms of 100% substance) 100.0 mg.

Excipients: propylene glycol, alcohol, benzyl alcohol, sodium metabisulphite, sodium hydroxide, sodium hydroxide of 1 M solution, water for injections.

Pharmacological properties:

Pharmacokinetics. The maximum concentration in a blood plasma at intravenous administration is reached in 5 min., at intramuscular - in 15 — 30 min. A ketoprofen elimination half-life from a blood plasma later in/in introductions - 2 h.

Linkng with proteins of a blood plasma makes 99%. Equilibrium concentration in a blood plasma and cerebrospinal fluid remains from 2 to 18 h.

Ketoprofen well gets into synovial fluid and connecting fabrics. Significant levels of concentration in synovial fluid are reached in 15 minutes after single intramuscular introduction of 100 mg of ketoprofen. Though concentration of ketoprofen in synovial fluid are slightly lower, than in a blood plasma, they are stabler (remain till 30 o'clock) therefore the therapeutic effect of drug for longer time remains. It is removed mainly by kidneys and in much smaller degree through intestines.

Pharmacodynamics. Кетотоп® - the non-steroidal anti-inflammatory drug (NPVS) derivative of propionic acid. Кетотоп® has soothing, antiinflammatory and febrifugal effect.

Influencing a cyclooxygenase and lipooksigenazny link of metabolism of arachidonic acid, drug inhibits synthesis of prostaglandins, leukotrienes and thromboxanes. Also stabilizes membranes of lysosomes, slows down release of lizosomalny enzymes, has antibradikininovy effect, interferes with aggregation of thrombocytes, causes considerable braking of activity of neutrophils in patients with a pseudorheumatism, reduces vascular permeability.

Possesses the expressed analgeziruyushchy action.

At a joint syndrome weakens a joint pain at rest and at the movement, reduces morning constraint and a swelling of joints, promotes increase in volume of movements.

Indications to use:

- inflammatory diseases oporno – the motive device (rhematoid, psoriasis, gouty, juvenile chronic arthritises, an ankylosing spondylitis);

- degenerative diseases of a musculoskeletal system (the deforming osteoarthrosis, osteochondrosis);

- lumbago, sciatica, neuralgia, mialgiya, tendovaginitis, bursitis;

- the posttraumatic pain syndrome which is followed by an inflammation;

- postoperative pain, migraine, renal colic;

- primary альгодисменорея, adnexitis, proctitis.

Route of administration and doses:

Solution for injections is entered deeply intramusculary on 100 mg (2 ml) by 1-2 times a day.
Course of treatment at intramuscular introduction of 5-10 days.
Intravenously. Кетотоп® apply to intravenous injections as follows. The recommended daily dose makes 200-300 mg (should not exceed 300 mg). Infusions of Ketotopa® have to be performed only in a hospital. The average time of infusion makes 0,5-1 hour (not less than 20 minutes). Treatment duration an intravenous form of a ketotop should not exceed 48 hours.
For short-term infusion of Кетотоп® 100-200 mg it is dissolved in 100 ml of normal saline solution and entered during 0,5-1 h each 8 hours.
For long infusion of Кетотоп® 100-200 mg it is dissolved in 500 ml of solution for infusions (normal saline solution, Ringer's solution, glucose solution) and entered within 8 hours at an interval of 8 hours.
Because of a photosensitivity bottles with infusion solution of a ketotop should be stored wrapped in dark paper or a foil.

Features of use:

With extra care apply at patients with diseases of a liver and kidneys, diseases of the zheludochno intestinal path (ZIP) in the anamnesis, dispeptic symptoms, right after serious surgical interventions. Кетотоп® with care apply in combination with diuretics, considering risk of development of an acute renal failure against the background of a hypovolemia. In the course of treatment systematic control of function of a liver and kidneys is necessary.

At a concomitant use of Ketotop® and other NPVS the risk of development of erosive cankers of a GIT and gastrointestinal bleeding increases.

As well as other drugs of this group, can mask symptoms of infectious diseases.

With bronchial asthma or allergic diathesis can cause a bronchospasm in patients.

With care to apply in operating time to drivers of vehicles and people whose profession is connected with the increased concentration of attention.

Side effects:

- nausea, eructation, vomiting, diarrhea, abdominal pains, stomatitises;

- headache, dizziness, drowsiness, change of mood, visual frustration, sonitus;

- itch, erythema, skin rash;

- disturbances of functions of kidneys and liver;

- development of hepatitis, intersticial nephrite;

- hypostases, bronkhospastichesky reactions;

- hemopoiesis disturbances, increase in arterial pressure;

- infiltrates, abscess at intramuscular introduction;

- ulcerogenic action at prolonged use.

Interaction with other medicines:

Forces out medicines from communication with proteins of a blood plasma.

Weakens effect of diuretics. At co-administration a ketotop and loopback diuretics nephrotoxic effect of both drugs amplifies.

Exponentiates effect of anticoagulants. At simultaneous use a ketotop and warfarin or salts of lithium patients have to be under strict observation of the doctor (increase in concentration of lithium in a blood plasma to its renal excretion, toxic at the expense of decrease).

Increases concentration in methotrexate blood (strengthening of its side effect).

In order to avoid a deposit it is not necessary to mix rolled into one a ketotop and трамадол.

Кетотоп® can reduce effect of anti-hypertensive means (beta adrenoblockers, APF inhibitors, diuretics) and to strengthen effect of peroral gipoglikemiziruyushchy drugs - sulphonylurea derivatives.

Contraindications:

- hypersensitivity to ketoprofen and salicylates;

- a peptic ulcer of a stomach and duodenum in an aggravation phase;

- heavy abnormal liver functions and kidneys;

- inflammatory diseases of intestines in an aggravation phase;

- pregnancy and period of a lactation;

- children's age up to 14 years.

Overdose:

Symptoms: strengthening of side effects.

Treatment: symptomatic. The specific antidote does not exist.

Storage conditions:

To store in the dry, protected from light place, at a temperature not above 25 °C.

To store in the place, unavailable to children!

Issue conditions:

According to the recipe

Packaging:

On 2.0 ml in ampoules from light-protective glass.

On 5 ampoules pack into a blister strip packaging from a film of polyvinyl chloride and aluminum foil.

On 2 planimetric packagings together with the approved instruction on a medical use in the state and Russian languages place in a pack from a cardboard. Put the scarificator in each pack ampoule. When packaging ampoules with notches, rings and points scarificators do not invest.