Ketoprofen (Capsules)

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, R52.0, R52.2, T14.0, T14.3
At KFU: 05.01.01.06
Manufacturer: LEK d.d. (Slovenia)

Pharmaceutical form, composition and packaging

Capsules opaque, №3, with a white hull and blue lid; contents of capsules – crumbly or pressed powder white with a yellowish Sheen.

Excipients: lactose, magnesium stearate, colloidal silicon dioxide.

Ingredients of the capsule shell: gelatin, Titanium dioxide, patented blue dye “Patent blue V”.

25 PC. – vials of dark glass (1) – packs cardboard.

Pills, Film-coated light blue, round, lenticular.

Excipients: magnesium stearate, colloidal silicon dioxide, corn starch, povidone, talc, lactose.

The composition of the shell: gipromelloza, macrogol 400, indigokarmin (E132), Titanium dioxide, talc, carnauba wax.

20 PC. – vials of dark glass (1) – packs cardboard.

Sustained-release tablets white, round, lenticular.

Excipients: magnesium stearate, colloidal silicon dioxide, povidone, microcrystalline cellulose, gipromelloza.

20 PC. – vials of dark glass (1) – packs cardboard.

Solution for in / and the / m colourless or slightly yellowish, clear.

Excipients: propylene glycol, ethanol, benzyl alcohol, Sodium hydroxide, water d / and.

2 ml – vials of dark glass (5) – blisters (2) – packs cardboard.
2 ml – vials of dark glass (5) – blisters (5) – packs cardboard.

Pharmacological action

NSAIDs, propionic acid. It has analgesic, anti-inflammatory and antipyretic effect. Through inhibition of Cox-1 and Cox-2 and, partially, lipooksigenazy, Ketoprofen inhibits the synthesis of prostaglandins and bradykinin, stabilizes the lysosomal membrane.

Ketoprofen has no negative impact on the status of articular cartilage.

Pharmacokinetics

Absorption

The ingestion of ketoprofen is readily absorbed from the digestive tract. Bioavailability – 90%. Before the drug at a dose of 100 mg C_max plasma levels achieved after 1 no 22 and m is 10.4 ug / ml. Eating does not affect the bioavailability of ketoprofen.

C_max When injecting is 15-30 m.

Distribution

V_d is 0.1-0.2 l / kg. Binding to plasma proteins is 99%. Ketoprofen is well into the synovial fluid.

Metabolism

Subjected to intense metabolism in the liver via microsomal enzymes, kongugiruet with glukuronova acid.

Deduction

T_1/2 ketoprofen – 1.6-1.9 no. Ketoprofen, primarily, metabolised in the liver. About 80% Ketoprofen is excreted in the urine, mostly in the form of conjugate with glukuronova acid (90%). About 10% output unchanged through the intestines.

Pharmacokinetics in special clinical situations

In patients with renal insufficiency ketoprofen appears more slowly, T_1/2 increases by 1 no.

In patients with hepatic insufficiency ketoprofen can accumulate in tissues.

In patients older metabolism and excretion of ketoprofen slower, but this has clinical significance only for patients with decreased renal function.

Testimony

-symptomatic therapy of inflammatory and degenerative diseases of the locomotor system (incl. rheumatoid arthritis, seronegative arthritis/ankylosing spondylitis, psoriaticheskiy arthritis, reactive arthritis/), osteoarthritis, gout, pseudogout);

- Pain (incl. headache, myalgia, neuralgia, radiculitis, post-traumatic and postoperative pain, pain syndrome in cancer, algomenorrhea).

Dosage regimen

Adults the drug is prescribed for 1-2 capsules 2-3 times / day; or 1 tab. 2 times / day; or 1 tab. long-acting 1 time / day. Capsules and tablets should be taken during or immediately after a meal, without chewing, squeezed enough water or milk (liquid volume – no less 100 ml). Oral forms can be combined with the use of rectal suppositories or dosage forms Ketonala^® for outdoor use (cream, gel). The maximum daily dose (incl. in the application of various medicinal forms) is 200 mg.

The solution is injected in/m or/in. V / m are introduced by 100 mg 1-2 times / day. In/in infusion ketoprofen carry out only in a hospital environment.

Short in/in cefuroxim: 100-200 mg, divorced 100 ml 0.9% sodium chloride solution, administered over 0.5-1 no. Possible re-introduction 8 no.

Continuous/cefuroxim: 100-200 mg, divorced 500 ml infusion solution (0.9% sodium chloride solution, laktatsoderžaŝij ringer's solution, 5% Dextrose), administered over 8 no. Possible re-introduction 8 no.

Injecting can be combined with the use of oral forms (capsules, tablets) or rectal suppositories. The maximum daily dose (incl. in the application of various medicinal forms) is 200 mg.

Side effect

Frequency of adverse reactions: very common (>10%), common (>1%, but <10%), unextended (>0.1%, but <1%), few (>0.01%, but <0.1%), very rare (<0.01%).

From the digestive system: common – dyspepsia (nausea, flatulence, diarrhea or constipation, 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, bleeding from the gastrointestinal tract, transient increase in liver enzymes.

From the central and peripheral nervous system: common – headache, dizziness, drowsiness, fatiguability, nervousness, nightmares; few – migraine, perifericheskaya neuropathy; very rare – hallucinations, disorientation, 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 – abnormal liver function, Interstitial nephritis, nephrotic syndrome, hematuria (chronic administration of NSAIDS and diuretics).

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

Local reactions: when using suppositories – burning sensation, irritation of the mucous membrane of the rectum, loose stools.

Other: few – hemoptysis, menometrorrhagia.

Contraindications

- Gastric ulcer and duodenal ulcer in the acute phase;

- NYAK, Crohn's disease;

- Hemophilia and other bleeding disorders;

- Severe hepatic impairment;

- Severe renal insufficiency;

is uncompensated heart failure;

- The postoperative period after coronary artery bypass grafting;

- Gastrointestinal, cerebrovascular bleeding or other bleeding suspected;

- Hronicheskaya dyspepsia;

- III trimester of pregnancy;

- Lactation (breast-feeding);

- Children up to age 15 years;

-inflammatory diseases of the rectum (suppository);

-hypersensitivity to ketoprofenu, aspirin or other NSAIDs;

— specify the disease at bronchial asthma, urticaria and rhinitis, caused by the admission of acetylsalicylic acid or other NSAIDS.

FROM caution should designate product with ulcers in history, symptomatic cardiovascular, cerebrovascular diseases, Peripheral arterial disease, dislipidemiâh, hepatic insufficiency, renal failure, chronic heart failure, hypertension, blood diseases, degidratacii, diabetes, history data on the development of ulcerative shock syndrome, smoking, concomitant anticoagulant therapy (warfarin), antiplatelet (acetylsalicylic acid), oral corticosteroids (prednisolone), selective serotonin reuptake inhibitors (citalopram, sertraline).

Pregnancy and lactation

Use Ketonala^® in the third trimester of pregnancy is contraindicated. Use Ketonala^® in the first and second trimesters of pregnancy is possible only in case, the potential benefit to the mother outweighs the risk to the fetus.

If you must use Ketonala^® lactation should decide the issue of termination of breastfeeding.

Cautions

Ketoprofen^® You can zapiwati milk or take antatsidnami drugs to reduce the frequency of gastrointestinal disorders (milk and antacids did not affect the absorption of ketoprofen).

With long-term use, Ketonala^®, like other NSAIDS, requires regular monitoring of blood indicators, indicators of liver and kidneys, especially in elderly patients.

Ketoprofen should be cautious appoint patients with arterial hypertension and heart disease, accompanied by fluid retention, It is recommended that monitoring of HELL.

Ketoprofen^® may mask the symptoms of infectious diseases.

In connection with a sensitivity of drug vials with infusion solution should be wrapped in dark paper or foil.

Effects on ability to drive vehicles and management mechanisms

Data on negative influence of Ketonala^® in the recommended doses on driving ability and work with no mechanisms. However, when use of the drug should be used with caution to individuals, whose work requires quick emotional reactions (driving, using machinery).

Overdose

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

Treatment: gastric lavage, appointment of activated carbon, symptomatic therapy. Demonstrates the use of blockers gistaminovykh n₂-receptors, proton pump inhibitors, prostaglandin inhibitors. No specific antidote.

Drug Interactions

Ketoprofen reduces the effect of diuretics, antihypertensive agents.

Reinforces the effect gipoglikemicakih oral drugs.

Together with the use of other NSAIDS, salicylates, The SCS and ethanol increases the risk of gastrointestinal bleeding.

While the use of anticoagulants, thrombolytics, antiagregantami increased risk of bleeding.

The risk of renal dysfunction increases together with dioretikami or ACE inhibitors.

In an application increases concentration of cardiac glycosides, blockers slow calcium channels, lithium preparations, cyclosporine, methotrexate.

Ketoprofen may reduce the efficacy of Mifepristone. The reception NPVS should start no earlier, than 8-12 days after discontinuation of mifepristone.

Ketoprofen^® can be combined with analgetikami central action. The solution can be mixed with morphine in one bottle. You can not mix in one bottle with tramadol because precipitation.

Conditions of supply of pharmacies

The drug is released under the prescription.

Conditions and terms

The drug should be stored out of reach of children at or above 25 ° C. Shelf life Tablets, coated, prolonged action tablets, capsules – 5 years, solution for i / m and / in the introduction – 3 year.