Ketoprofen (Suppozitorii)

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

◊Rectal Suppositories white, smooth, Homogeneous.

Excipients: tallow, glyceryl kaprilokaprat (migliol 812).

6 PC. – strips (2) – 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

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 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 appoint 1 suppozitoriû 1-2 times/day rectally.

Rectal suppositories can be used in combination with medicinal forms of ketoprofen for topical use systemic or. The maximum daily dose of ketoprofen (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, giperʙiliruʙinemii, alcoholic liver cirrhosis, 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

Patients with inflammatory diseases of the rectum should not appoint Ketonal^® in the form of rectal suppositories.

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.

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.

At the same time, patients, marks custom effects when applying Ketonala^® Caution should be exercised when engaging in potentially hazardous activities, require high concentration and speed of psychomotor reactions.

Overdose

There is no specific antidote. Displaying symptomatic therapy.

Drug Interactions

Ketoprofen reduces the effect of diuretics, antihypertensive agents.

Reinforces the effect gipoglikemicakih oral drugs and some anticonvulsants (phenytoin).

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^® can be combined with analgetikami central action.

Conditions of supply of pharmacies

The drug is resolved to application as an agent Valium holidays.

Conditions and terms

The drug should be stored out of reach of children at or above 25 ° C. Shelf life – 5 years.