Ketoprofen organic chemistry

General characteristics. Structure:

Active ingredients: 100 mg of ketoprofen

Excipients: a hypro rod (klutset LF), Mannitolum (D-mannitol), sodium of a kroskarmelloz (primelloz), cellulose microcrystallic, silicon dioxide colloid (aerosil), stearate magnesium monohydrate.

Structure of a cover: оподрай the II white (polyvinyl alcohol, titanium dioxide, macrogoal (polyethyleneglycol), talc).

The nonsteroid drug having protivospolitelny, febrifugal and analgesic effect.

Pharmacological properties:

Pharmacodynamics. NPVS derivative of propionic acid. Has analgeziruyushchy, antiinflammatory and febrifugal effect. The mechanism of action is connected with oppression of activity of TsOG - the main enzyme of metabolism of arachidonic acid, being the predecessor of prostaglandins which play a major role in a pathogeny of an inflammation, pain and fever.

The expressed analgeziruyushchy effect of ketoprofen is caused by two mechanisms: peripheral (indirectly, through suppression of synthesis of prostaglandins) and central (the caused inhibition of synthesis of prostaglandins in the central and peripheral nervous system, and also action on biological activity of other neurotropic substances playing a key role in release of mediators of pain in a spinal cord). Besides, ketoprofen has antibradikininovy activity, stabilizes lizosomalny membranes, causes considerable braking of activity of neutrophils in patients with a pseudorheumatism. Suppresses aggregation of thrombocytes.

Pharmacokinetics. At intake and rectal administration ketoprofen is well absorbed from a GIT. Cmax in plasma at intake is reached in 1-5 h (depending on a dosage form), at rectal administration - in 45-60 min., introduction in oil - in 20-30 min., in introduction - in 5 min.

Linkng with proteins of plasma makes 99%. Owing to the expressed lipophilicity quickly gets through GEB. Css in a blood plasma and cerebrospinal fluid remains from 2 to 18 h. Ketoprofen well gets into synovial fluid where its concentration in 4 h after reception exceeds that in plasma.

It is metabolized by linkng with glucuronic acid and to a lesser extent at the expense of a hydroxylation.

It is removed mainly by kidneys and in much smaller degree through intestines. Ketoprofen T1/2 after intake makes 1.5-2 h of plasma, after rectal administration - about 2 h, after introduction in oil - 1.27 h, later in/in introductions - 2 h.

Indications to use:

Joint syndrome (pseudorheumatism, the osteoarthritis ankylosing a spondylitis, gout); a symptomatic treatment of inflammatory and degenerative diseases of a musculoskeletal system (the periarthritis, an arthrosynovitis, a tendinitis, tendosinovit, a bursitis, a lumbago), backbone pains, neuralgia, a mialgiya. Uncomplicated injuries, in particular sports, dislocations, stretching or rupture of sheaves and sinews, bruises, posttraumatic pains. As a part of a combination therapy of inflammatory diseases of veins, absorbent vessels, lymph nodes (phlebitis, a periphlebitis, limfangiit, superficial lymphadenitis).

Route of administration and doses:

Establish individually taking into account weight of a course of a disease. For intake for adults the initial daily dose makes 300 mg in 2-3 receptions. For the supporting treatment - the dose depends on the used dosage form. For treatment of acute states or stopping of an aggravation of chronic process enter 100 mg in the form of a single injection in oil. Further ketoprofen is applied inside or rektalno.

Outwardly - apply on the struck surface of 2 times/days.

Maximum dose: at intake or rektalno - 300 mg/days.

Features of use:

With extra care apply at patients with diseases of a liver and kidneys, gastrointestinal diseases in the anamnesis, dispeptic symptoms, right after serious surgical interventions. In the course of treatment systematic control of function of a liver and kidneys is necessary.

In I and II trimesters of pregnancy use of ketoprofen is possible in cases when the potential advantage for mother exceeds potential risk for a fruit.

In need of use of ketoprofen in the period of a lactation breastfeeding is recommended to be stopped.

With extra care apply at patients with liver diseases. In the course of treatment systematic control of function of a liver is necessary.

With extra care apply at patients with diseases of kidneys. In the course of treatment systematic control of function of kidneys is necessary.

Side effects:

From the alimentary system: pains in epigastric area, nausea, vomiting, a lock or diarrhea, anorexia, gastralgias, abnormal liver functions; seldom - erosive cankers of a GIT, bleeding and perforation of a GIT.

From TsNS: headache, dizziness, sonitus, drowsiness.

From an urinary system: renal failures.

Allergic reactions: skin rash; seldom - a bronchospasm.

Local reactions: at use in the form of candles the irritation of a mucous membrane of a rectum, painful defecation are possible; at use in the form of gel - an itch, skin rash in a site of application.

Interaction with other medicines:

At simultaneous use of ketoprofen with other NPVS the risk of development of erosive cankers of a GIT and bleedings increases; with anti-hypertensive means (including with beta adrenoblockers, APF inhibitors, diuretics) - reduction of their action is possible; from trombolitika - increase in risk of development of bleedings.

At simultaneous use with acetylsalicylic acid reduction of linkng of ketoprofen with proteins of a blood plasma and increase in its plasma clearance is possible; with heparin, tiklopidiny - increase in risk of development of bleedings; with lithium drugs - increase in concentration of lithium in a blood plasma to its renal excretion, toxic at the expense of decrease, is possible.

At simultaneous use with diuretics the risk of development of a renal failure owing to reduction of the renal blood-groove caused by inhibition of synthesis of prostaglandins and against the background of a hypovolemia increases.

At simultaneous use with probenetsidy reduction of clearance of ketoprofen and its linkng with proteins of a blood plasma is possible; with a methotrexate – strengthening of side effect of a methotrexate is possible.

At simultaneous use of warfarin development heavy, sometimes fatal bleedings is possible.

Contraindications:

For intake: GIT erosive cankers in an aggravation phase, "an aspirinovy triad", the expressed abnormal liver functions and/or kidneys; III trimester of pregnancy; age up to 15 years (for tablets ретард); hypersensitivity to ketoprofen and salicylates.

For rectal use: a proctitis and proctorrhagias in the anamnesis.

For external use: the becoming wet dermatosis, the eczema infected grazes, wounds.

It is contraindicated to use in the III trimester of pregnancy.

Overdose:

Cases of overdose of drug are not described. There is no specific antidote. Symptomatic treatment.

Storage conditions:

To store in the place protected from light at a temperature not above 30ºС. To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

20 pieces - banks polymeric (1) - packs cardboard.
30 pieces - banks polymeric (1) - packs cardboard.
50 pieces - banks polymeric (1) - packs cardboard.
20 pieces - banks of dark glass (1) - a pack cardboard.
30 pieces - banks of dark glass (1) - a pack cardboard.
50 pieces - banks of dark glass (1) - a pack cardboard.
10 pieces - planimetric strip packagings (2) - packs cardboard.
10 pieces - planimetric strip packagings (3) - packs cardboard.
10 pieces - planimetric strip packagings (5) - packs cardboard.