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

Excipients: ethanol (ethyl alcohol 95% in terms of 100% substance) 100 mg, sodium chloride 4.35 mg, sodium hydroxide or hydrochloric acid up to> H 6.9-7.9, water for injection up to 1 ml.

Description:A clear solution of light yellow color.

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

ATX: & nbsp

M.01.A.B.15 Ketorolac

Pharmacodynamics:

Non-steroidal anti-inflammatory drug (NSAID). Has a pronounced analgesic effect, has anti-inflammatory and moderate antipyretic effect. The mechanism of action is associated with a nonselective inhibition of cyclooxygenase-1 and cyclooxygenase-2 activity catalyzing the formation of prostaglandins (Pg) from arachidonic acid, which play an important role in the pathogenesis of pain, inflammation and fever.

By the strength of the analgesic effect comparable to morphine, it significantly exceeds other NSAIDs.

After intramuscular injection, the onset of analgesic actionis observed after 30 minutes, the maximum effect is achieved in 1-2 hours.

Pharmacokinetics:

Maximum accumulation in tissues (Cmah) 30 mg - 1.5-3 μg / ml, 60 mg - 3-5.5 μg / ml. Time to reach the maximum concentration (TCmah) - 15-70 minutes. FROMmah after intravenous infusion 15 mg - 1.5-3 μg / ml, 30 mg 3-5 μg / ml. The connection with plasma proteins is 99%.

Time to reach equilibrium concentration (Css) - 24 hours when administered 4 times a day (above the sub-therapeutic) and is 15 mg to 0.5-1 μg / ml, 30 mg to 1-2.5 μg / ml, with intramuscular 15 mg infusion - 0 , 5-1 μg / ml, 30 mg - 1.5-3 μg / ml. The volume of distribution is 0.15-0.3 l / kg. In patients with renal insufficiency, the volume of ketorolac distribution may increase 2-fold, and the volume of distribution of ketorolac R-enantiomer by 20%. Penetrates into breast milk: when the mother receives 10 mg of ketorolac Cmah in milk is achieved 2 hours after the first dose and is 7 mg / ml, 2 hours after the second dose of ketorolac (with the drug 4 times a day) - 8 mg / ml. More than 50% of the administered dose is metabolized in the liver with the formation of pharmacologically inactive metabolites. The main metabolites are glucuronides, which are excreted by the kidneys, and p-hydroxycetorolac.It is excreted by 90% by the kidneys, 6% by the intestine.

The half-life (T_1/2) in patients with normal renal function - an average of 5 h. T_1/2 increases in elderly patients and is shortened in young people. The liver function does not affect T_1/2. In patients with impaired renal function with a creatinine concentration in the plasma of 20-50 mg / l T_1/2 - 10-11 h, with more severe renal failure - more than 13 hours. It is not excreted by hemodialysis.

Indications:

Pain syndrome of strong and moderate severity under the following conditions:

- injury;

- toothache;

- pain in the postoperative period;

- oncological diseases;

- myalgia;

- arthralgia;

- neuralgia;

- radiculitis;

- dislocations, sprains;

- rheumatic diseases.

It is intended for symptomatic therapy, reducing pain and inflammation at the time of application; on the progression of the disease is not affected.

Contraindications:

- Hypersensitivity to the active substance or ancillary components;

- complete or incomplete combination of bronchial asthma, recurrent nasal polyposis and paranasal sinuses and intolerance to acetylsalicylic acid or other NSAIDs (including in the anamnesis);

- urticaria, rhinitis caused by taking an NSAID (in history);

- intolerance of drugs pyrazolone series;

- Hypovolemia (regardless of the cause that caused it);

- erosive and ulcerative lesions of the gastrointestinal tract (GIT) in the acute stage;

- hypocoagulation (including hemophilia);

- bleeding or a high risk of their development;

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

- severe hepatic impairment or active liver disease;

- condition after aortocoronary bypass surgery;

- confirmed hyperkalemia;

- inflammatory bowel disease;

- pregnancy (III trimester);

- period of delivery, lactation period;

- children under 16 years of age (safety and efficacy not established).

Carefully:

Bronchial asthma, the presence of factors that increase toxicity in relation to the gastrointestinal tract (GIT): 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 mellitus, peripheral arterial disease, smoking, creatinine clearance 30-60 ml / min.

Anamnestic data on the development of gastroesophageal ulcer, confirmed presence 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:

It penetrates into breast milk in small amounts. Application in the III trimester of pregnancy and with breastfeeding is contraindicated (should be abandoned from feeding for the period of application of the drug). In extreme cases, if you need to use the drug during the I and II trimesters of pregnancy, you should compare the benefits to the mother and the risk to the fetus.

Dosing and Administration:

Intramuscularly, intravenously.

When administered intravenously, the dose should be administered at least 15 seconds (for dosage forms containing ethanol).

Patients from 16 to 64 years of age with a body weight exceeding 50 kg, intramuscularly for 1 administration is administered not more than 60 mg (including oral dose); usually 30 mg every 6 hours; intravenously - 30 mg (no more than 15 doses per 5 days).

Intramuscularly, for adults with a body weight of less than 50 kg or with chronic renal failure (CRF), no more than 30 mg (including oral dose) is administered per administration; usually - 15 mg (no more than 20 doses per 5 days); in / in - no more than 15 mg every 6 hours (no more than 20 doses in 5 days).

Maximum daily doses for intramuscular and intravenous administration are for patients from 16 before 64 years old with a body weight exceeding 50 kg - 90 mg / day; adult patients with a body weight of less than 50 kg or with CRF, as well as elderly patients (over 65 years of age) - for intramuscular and intravenous administration of 60 mg. The duration of treatment should not exceed 5 days.

Side effects:

Often - more than 3%, less often -1-3%, rarely - less than 1%.

From the digestive system: often - gastralgia, diarrhea; less often - stomatitis, flatulence, constipation, vomiting, sensation of stomach overflow; rarely - loss of appetite, nausea, erosive and ulcerative lesions of the gastrointestinal tract (including with perforation and / or bleeding - abdominal pain, spasm or burning in the epigastric region, blood in the feces or melena,vomiting with blood or the type of "coffee grounds", nausea, heartburn, etc.), cholestatic jaundice, hepatitis, hepatomegaly, acute pancreatitis.

From the urinary system: Rarely - acute renal failure, back pain, hematuria, azotemia, hemolytic uremic syndrome (hemolytic anemia, renal failure, thrombocytopenia purpura), frequent urination, increased or decreased volume of urine, nephritis, edema, renal origin.

From the sense organs: rarely - hearing loss, ringing in the ears, visual impairment (including blurred vision).

From the respiratory system: rarely - bronchospasm, rhinitis, pulmonary edema, laryngeal edema (shortness of breath, difficulty breathing).

From the central nervous system (CNS): often - headache, dizziness, drowsiness, rarely - aseptic meningitis (fever, severe headache, seizures, neck and / or neck stiffness), hyperactivity (mood changes, anxiety), hallucinations, depression, psychosis, fainting.

From the side of the cardiovascular system: less often - increased blood pressure.

On the part of the organs of hematopoiesis: rarely - anemia, eosinophilia, leukopenia.

From the side of the hemostasis system: rarely - bleeding from a postoperative wound, epistaxis, rectal bleeding.

From the skin: less often - skin rash (including maculopapular rash), purpura; rarely exfoliative dermatitis (fever with chills or without, hyperemia, densification or flaking of the skin, enlargement and / or soreness of the tonsils), urticaria, malignant exudative erythema (Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome).

Local Reactions: less often - burning or pain at the injection site.

Allergic reactions: rarely anaphylaxis or anaphylactoid reactions (skin discoloration, skin rash, hives, skin itch, tachypnea or dyspnea, edema of the eyelids, periorbital edema, shortness of breath, shortness of breath, chest pain, wheezing).

Other: often - swelling (face, legs, ankles, fingers, feet, weight gain); less often - increased sweating, rarely - fever.

Overdose:

Symptoms: abdominal pain, nausea, vomiting, erosive-ulcerative gastrointestinal lesion, impaired renal function, metabolic acidosis.

Treatment: symptomatic (maintenance of vital body functions). Dialysis is ineffective.

Interaction:

Combination with paracetamol increases the nephrotoxicity of ketorolac. Admission with other NSAIDs, glucocorticosteroids, ethanol, corticotropin, calcium preparations increases the risk of ulceration of the gastrointestinal mucosa and the development of gastrointestinal bleeding.

Simultaneous use with anticoagulant drugs (drugs) - derivatives of coumarin and indanedione, heparin, thrombolytics (alteplase, streptokinase, urokinase), antiplatelet drugs, cephalosporins, valproic acid and aminosalicylic acid increases the risk of bleeding. Reduces the effect of hypotensive and diuretics (reduces synthesis Pg in the kidneys). The use together with methotrexate increases hepato- and nephrotoxicity of ketorolac (joint use of them is possible only with the use of low doses of the latter and control of its concentration in the plasma).

When used with other nephrotoxic drugs (including drugs with gold) the risk of developing nephrotoxicity increases.

LS, which block tubular secretion, reduce the clearance of ketorolac and increase its concentration in the plasma.

Increases the effect of narcotic analgesics.

Myelotoxic drugs increase the manifestation of hematotoxicity of the drug.

Special instructions:

Before prescribing the drug, it is necessary to clarify the question of the previous allergy to the drug or NSAIDs. Because of the risk of developing allergic reactions, the first dose is administered under close supervision of the doctor.

Hypovolemia increases the risk of developing nephrotoxic adverse reactions.

If necessary, you can prescribe in combination with narcotic analgesics. It is not recommended to be used as a medicine for premedication, maintenance of anesthesia.

When combined with other NSAIDs, fluid retention, cardiac decompensation, and increased blood pressure may occur. The effect on platelet aggregation stops after 24-48 hours. Do not use simultaneously with paracetamol for more than 5 days.

Patients with blood clotting disorder are appointed only with a constant control of the number of platelets, it is especially important for postoperative patients requiring careful control of hemostasis.

The risk of developing drug complications increases with prolonged treatment (in patients with chronic pain) and an increase in the dose of the drug.

To reduce the risk of developing NSAIDs, gastropathies are prescribed misoprostol, omeprazole.

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 dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Solution for intravenous and intramuscular injection 30 mg / ml.

Packaging:

By 1.0 ml in ampoules of type I light-protective glass with a color fracture ring or with a color dot and a notch and / or with additional color identification rings or other coding.

5 ampoules per contour cell pack.

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

Storage conditions:

In the dark place at a temperature of 15 to 25 ° C.

Keep out of the reach of children.

Shelf life:

4 years.

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

Terms of leave from pharmacies:On prescription

Registration number:LS-000430

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

Information update date: & nbsp17.04.2012

Illustrated instructions

Instructions

Dolomin® (Dolomine®)