Universal reference book for medicines
Product name: VALUSAL (VALUSAL)

Active substance: ketoprofen

Type: NSAID for external use

Manufacturer: GRINDEX (Latvia) manufactured by TALLINNA FARMAATSIATEHASE (Estonia)
Description of the active substance:
This information is a reference and it is not enough that the drug has been prescribed by a doctor ..

NSAID, a derivative of propionic acid.
Has analgesic, anti-inflammatory and antipyretic effect. The mechanism of action is associated with oppression of the activity of COX, the main enzyme of arachidonic acid metabolism, which is the precursor of prostaglandins, which play a major role in the pathogenesis of inflammation, pain and fever.
The pronounced analgesic effect of ketoprofen is due to two mechanisms: peripheral (indirectly, through suppression of prostaglandin synthesis) and central (due to the inhibition of the synthesis of prostaglandins in the central and peripheral nervous system, and the effect on the biological activity of other neurotropic substances that play a key role in releasing mediators of pain in the spinal cord brain).
In addition, ketoprofen has anti-bradykinin activity, stabilizes lysosomal membranes, causes significant inhibition of neutrophil activity in patients with rheumatoid arthritis. Suppresses the aggregation of platelets.
When ingestion and rectal administration, ketoprofen is well absorbed from the digestive tract.
C max in the plasma when ingested is achieved after 1-5 h (depending on the dosage form), rectal administration - after 45-60 min, in / m introduction - after 20-30 min, in / in the introduction - after 5 min .
Binding to plasma proteins is 99%.
Due to the pronounced lipophilicity it rapidly penetrates through the BBB. C ss in blood plasma and cerebrospinal fluid persists from 2 to 18 hours. Ketoprofen penetrates well into the synovial fluid, where its concentration after 4 hours after intake exceeds that in plasma.
Metabolized by binding to glucuronic acid and to a lesser extent by hydroxylation.

It is excreted mainly by the kidneys and to a much lesser extent through the intestines.
T 1/2 of ketoprofen from the plasma after ingestion is 1.5-2 hours, after rectal administration - about 2 hours, after the / m introduction - 1.27 hours, after iv introduction - 2 hours.
Articular syndrome (rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, gout);
symptomatic treatment of inflammatory-degenerative diseases of the musculoskeletal system (periarthritis, arthrosinovitis, tendonitis, tendosynovitis, bursitis, lumbago), pain in the spine, neuralgia, myalgia. Uncomplicated injuries, in particular sports, dislocations, sprains or rupture of ligaments and tendons, bruises, post-traumatic pains. In the combination therapy of inflammatory diseases of veins, lymphatic vessels, lymph nodes (phlebitis, periphlebitis, lymphangitis, superficial lymphadenitis).
Established individually taking into account the severity of the course of the disease.
For oral administration for adults, the initial daily dose is 300 mg in 2-3 divided doses. For maintenance treatment, the dose depends on the dosage form used. To treat acute conditions or arrest the exacerbation of a chronic process, 100 mg is administered as a single IM injection. Further ketoprofen is used orally or rectally.
Outer - applied to the affected surface 2 times / day.

The maximum dose: when ingesting or rectally - 300 mg / day.

On the part of the digestive system: pain in the epigastric region, nausea, vomiting, constipation or diarrhea, anorexia, gastralgia, impaired liver function;
rarely - erosive and ulcerative lesions of the gastrointestinal tract, bleeding and perforation of the gastrointestinal tract.
From the side of the central nervous system: headache, dizziness, tinnitus, drowsiness.

From the side of the urinary system: renal dysfunction.

Allergic reactions: skin rash;
rarely - bronchospasm.
Local reactions: when applied in the form of candles, irritation of the mucous membrane of the rectum, painful defecation;
when applied in the form of a gel - itching, skin rash at the application site.
For oral administration: erosive and ulcerative lesions of the gastrointestinal tract in the phase of exacerbation, "aspirin triad", expressed violations of the liver and / or kidney function;
III trimester of pregnancy; age to 15 years (for retard tablets); hypersensitivity to ketoprofen and salicylates.
For rectal administration: proctitis and rectal hemorrhage in anamnesis.

For external use: wet dermatoses, eczema, infected abrasions, wounds.

Contraindicated in the third trimester of pregnancy.
In the first and second trimesters of pregnancy, the use of ketoprofen is possible in cases where the potential benefit to the mother exceeds the potential risk to the fetus.
If it is necessary to use ketoprofen during lactation, it is recommended to stop breastfeeding.

Contraindications for oral administration are severe renal dysfunction.

With special care apply in patients with kidney disease.
In the process of treatment, systematic monitoring of kidney function is necessary.
Contraindications for ingestion are marked violations of the liver.

Use with extreme caution in patients with liver disease.
In the process of treatment, systematic monitoring of liver function is necessary.
Contraindicated at the age of 15 years (for retard tablets).

With extreme caution apply in patients with liver and kidney disease, a history of gastrointestinal disease, dyspeptic symptoms, immediately after major surgical interventions.
During the treatment, systematic monitoring of liver and kidney function is necessary.
With the simultaneous use of ketoprofen with other NSAIDs, the risk of erosive and ulcerative gastrointestinal lesions and bleeding increases;
with antihypertensive agents (including with beta-adrenoblockers, ACE inhibitors, diuretics) - possibly reducing their effect; with thrombolytics - increased risk of bleeding.
With simultaneous use with acetylsalicylic acid, it is possible to reduce the binding of ketoprofen to plasma proteins and increase its plasma clearance;
with heparin, ticlopidine - increased risk of bleeding; with lithium preparations - it is possible to increase the concentration of lithium in the blood plasma to toxic by reducing its renal excretion.
With simultaneous use with diuretics, the risk of developing kidney failure increases due to a decrease in renal blood flow due to inhibition of prostaglandin synthesis and against hypovolemia.

With simultaneous application with probenecid, the clearance of ketoprofen and its binding to plasma proteins can be reduced;
with methotrexate - may increase the side effect of methotrexate.
With the simultaneous use of warfarin, it is possible to develop severe, sometimes fatal bleeding.

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