Flamax - instructions for use, dose, side effects, contraindications

Excipients: propylene glycol 800 mg, ethanol (ethyl alcohol 95% in terms of 100% substance) 200 mg, benzyl alcohol 40 mg, sodium hydroxide to pH 6.5-7.5, water for injection 2 ml.

Description:

Colorless or with a yellowish tint transparent solution.

Pharmacotherapeutic group:non-steroidal anti-inflammatory drug (NSAID)

ATX: & nbsp

M.02.A.A.10 Ketoprofen

Pharmacodynamics:

Non-steroidal anti-inflammatory drug, a derivative of propionic acid. It has analgesic, anti-inflammatory and antipyretic effects, suppresses platelet aggregation. By acting on the cyclooxygenase and lipoxygenase unit of arachidonic acid metabolism, ketoprofen inhibits the synthesis of prostaglandins, leukotrienes and thromboxanes. The analgesic effect is due to both central and peripheral mechanisms.

Pharmacokinetics:

Distribution

Up to 99% ketoprofen binds to plasma proteins, mainly with albumin. The maximum concentration of the drug in plasma (C_mOh) is achieved quickly due to low volume distribution (0.1-0.2 l / kg). The equilibrium concentration of ketoprofen is reached 24 hours after the beginning of its regular application. Ketoprofen well penetrates into the synovial fluid and connective tissue. Significant concentration in the synovial fluid is achieved only 15 minutes after a single intramuscular injection of 100 mg of ketoprofen. Although the concentration of ketoprofen in the synovial fluid is somewhat lower than in the plasma, they are more stable (lasting up to 30 hours), resulting in a long-term reduction in pain and joint stiffness. In a significant amount does not penetrate the blood-brain barrier (BBB).

Metabolism

Ketoprofen is mainly metabolized in the liver, where it undergoes glucuronidation to form esters with glucuronic acid, mainly excreted by the kidneys. Has the effect of "first pass" through the liver.

Excretion

It is excreted mainly by the kidneys. Excretion with caloric masses is less than 1%.The half-life of ketoprofen ranges from 1.6 to 1.9 hours. Do not cumulate.

Indications:

For symptomatic treatment of pain and inflammation of various genesis of moderate intensity:

- inflammatory and degenerative diseases of the musculoskeletal system: rheumatoid, psoriatic, juvenile chronic arthritis, ankylosing spondylitis (Bechterew's disease), gouty arthritis, rheumatic soft tissue damage, osteoarthrosis of peripheral joints and spine (including radicular syndrome);

- lumbago, sciatica, neuralgia;

- migraine;

- algodismenorea, inflammatory processes of the pelvic organs, incl. adnexitis;

- Post-traumatic pain syndrome, accompanied by inflammation;

- postoperative pain;

- toothache;

- pain syndrome in cancer.

On the progression of the disease is not affected.

Contraindications:

- Hypersensitivity (including other non-steroidal anti-inflammatory drugs or ancillary components);

- erosive-ulcerative lesions of the gastrointestinal tract (GIT) (in the phase of exacerbation);

- bleeding from the gastrointestinal tract, inflammatory bowel disease in the phase of exacerbation (ulcerative colitis, Crohn's disease);

- severe hepatic insufficiency or liver disease in an acute period;

- severe renal failure (creatinine clearance (CK) less than 30 ml / min);

- progressive kidney disease;

- hyperkalemia;

- complete or incomplete combination of bronchial asthma, recurrent nasal polyposis and paranasal sinuses and intolerance to acetylsalicylic acid or other non-steroidal anti-inflammatory drugs (including in anamnesis);

- violation of hematopoiesis, hemostasis disorders (including hemophilia);

- pregnancy (III trimester);

- lactation period;

- children's age (up to 15 years);

- period after aortocoronary bypass surgery.

Carefully:

Bronchial asthma, the presence of factors that increase toxicity in relation to the gastrointestinal tract: alcoholism and cholecystitis, chronic heart failure, edematous syndrome; arterial hypertension, impaired renal function, cholestasis, sepsis, concurrent use with other NSAIDs, advanced age (over 65 years), pregnancy (I-II trimester).

Ischemic heart disease, cerebrovascular disease, dyslipidemia / hyperlipidemia, diabetes, peripheral arterial disease, smoking, chronic renal failure (creatinine clearance 30-60 ml / min).

Anamnestic data on the development of ulcerative lesions of the gastrointestinal tract, confirmed evidence of infection Helicobacter pylori, long-term use of NSAIDs, severe somatic diseases, concomitant therapy with the following drugs:

- anticoagulants (incl. warfarin);

- antiaggregants (incl. acetylsalicylic acid, clopidogrel);

- selective serotonin reuptake inhibitors (incl. citalopram, fluoxetine, paroxetine, sertraline);

- glucocorticosteroids (incl. prednisolone).

To reduce the risk of developing adverse events on the part of the gastrointestinal tract, a minimum effective dose should be used with the minimum possible short course.

Pregnancy and lactation:

The use of Flamax® in III trimester of pregnancy and when breastfeeding is contraindicated (should be abandoned from feeding for the period of application of the drug).

Application in the I and II trimesters of pregnancy is allowed if the potential benefit to the mother exceeds the potential risk to the fetus.

Dosing and Administration:

Intravenous, intramuscular.

Intramuscular injection: 100 mg (1 ampoule) 1-2 times a day.

Intravenous infusion administration of the drug should be carried out only in a hospital.The average infusion time is 0.5-1 hour, maximum - no more than 48 hours, with the dose of the drug should not exceed 300 mg. Short intravenous infusion: 100-200 mg (1-2 ampoules) of the drug diluted in 100 ml of 0.9% solution of sodium chloride, is introduced within 0.5-1 hour. It is possible to re-enter after 8 hours.

Continuous intravenous infusion: 100-200 mg (1-2 ampoules) of the drug diluted in 500 ml of a solution for infusions (0.9% solution of sodium chloride, Ringer's solution, 5% dextrose solution) for 8 hours.

It is possible to re-enter after 8 hours.

Combined application

Flamax® can be combined with analgesics of central action; it can be mixed with morphine in one bottle. Do not mix in one bottle with tramadol due to precipitation.

Parenteral administration of Flamax® can be combined with the use of oral forms (tablets, capsules) or rectal suppositories, while the total daily dose may be increased to 300 mg or reduced to 100 mg, depending on the nature of the disease and the condition of the patient.

A minimum effective dose should be used with the minimum possible short course (see section "Special instructions").

Side effects:

From the digestive system: abdominal pain, dyspepsia (nausea, vomiting, heartburn, flatulence, decreased appetite, diarrhea), stomatitis, impaired liver function, change in taste. With prolonged use in large doses - ulceration of the mucous membrane of the gastrointestinal tract, gingival, gastrointestinal, hemorrhoidal bleeding.

From the nervous system: headache, dizziness, insomnia, agitation, nervousness, drowsiness, depression, asthenia, confusion or loss of consciousness, memory impairment, migraine, peripheral neuropathy.

From the sense organs: noise or ringing in the ears, blurred vision, conjunctivitis, mucous membranes dry eyes, eye pain, conjunctival hyperemia, hearing loss, vertigo.

From the side of the cardiovascular system: increased blood pressure, tachycardia.

From the hematopoiesis: agranulocytosis, anemia, hemolytic anemia, thrombocytopenia, and leukopenia.

From the urinary system: edematous syndrome, cystitis, urethritis, renal dysfunction, interstitial nephritis, nephrotic syndrome, hematuria.

Allergic reactions: skin rash (incl.erythematous, urticaria), skin itching, rhinitis, angioedema, bronchospasm, exfoliative dermatitis, anaphylactic shock.

Other: increased sweating, hemoptysis, epistaxis, myalgia, muscle twitching, shortness of breath, thirst, photosensitivity, with prolonged use in large doses - vaginal bleeding.

Overdose:Cases of overdose are not described. There may be dizziness, vomiting, headache, dyspnea, abdominal pain, bleeding, liver dysfunction and kidney.

Treatment is symptomatic.

Interaction:

With the simultaneous use of Flamax® and loop diuretics, the nephrotoxic effect of both drugs is enhanced. Reduces the effectiveness of uricosuric drugs, enhances the effect of anticoagulants, antiaggregants, fibrinolytics, ethanol, side effects of glucocorticosteroids and mineralocorticosteroids, estrogens; reduces the effectiveness of antihypertensive drugs and diuretics.

Simultaneous use with other NSAIDs, glucocorticosteroids, ethanol, corticotropin can lead to the formation of ulcers and the development of gastrointestinal bleeding, an increased risk of kidney dysfunction.Simultaneous use with oral anticoagulants, heparin, thrombolytic agents, antiplatelet agents, cefapazone, cefamandole and cefotetan increases the risk of bleeding.

Increases hypoglycemic action of insulin and oral hypoglycemic drugs (dose recalculation is necessary).

Inductors of microsomal oxidation in the liver (phenytoin, ethanol, barbiturates, rifampicin, phenylbutazone, tricyclic antidepressants) increase the production of hydroxylated active metabolites.

Joint use with sodium valproate reduces the aggregation of platelets.

Increases the concentration in the plasma of verapamil and nifedipine, lithium preparations, methotrexate.

Antacids and colestramine reduce absorption.

Increases the hematotoxicity of myelotoxic drugs.

To avoid sediment, do not mix in one Flamax® bottle and tramadol.

Special instructions:

With the simultaneous use of Flamax® and warfarin or lithium preparations, patients should be under strict medical supervision.

Care must be taken when prescribing the drug to patients with peptic ulcer diseases of the gastrointestinal tract in an anamnesis,renal or hepatic insufficiency, and also receiving coumarin anticoagulants. Like the rest of the drugs in this group, it can mask the symptoms of infectious diseases.

During treatment, it is necessary to monitor the picture of peripheral blood and the functional state of the liver and kidneys.

If it is necessary to determine 17-ketosteroids, the drug should be discontinued 48 hours before the test.

If there is a violation of the liver, kidneys need to reduce the dose and careful observation.

To reduce the risk of developing adverse events on the part of the gastrointestinal tract, the minimum effective dose should be used as little as possible with a short course (see section "Method of administration and dose").

Effect on the ability to drive transp. cf. and fur:

During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Form release / dosage:

Solution for intravenous and intramuscular injection 50 mg / ml.

Packaging:

By 2 ml in ampoules of light-protective glass type I with a color fracture ring or with a color dot and a notch.

Ampoules are additionally applied with one, two or three

color rings and / or a two-dimensional barcode, and / or alphanumeric encoding or without additional color rings, a two-dimensional barcode, alphanumeric encoding.

5 ampoules are placed in a contour mesh package.

1 or 2 contour packs with instructions for use in a pack of cardboard.

Storage conditions:

At a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

5 years.

Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LS-000429

Date of registration:06.05.2010

The owner of the registration certificate:FarmSirma Soteks, ZAO FarmSirma Soteks, ZAO Russia

Manufacturer: & nbsp

FarmSirma Soteks, ZAO Russia

Representation: & nbspPharm Company Sotex CJSC Pharm Company Sotex CJSC Russia

Information update date: & nbsp16.04.2012

Illustrated instructions

Instructions

Flamax® (FLAMAX®)