Flamadex pills coated 25 mg №10

Mechanism of action

NSAIDs, a derivative of propionic acid. It has an analgesic, anti-inflammatory and antipyretic effect. The mechanism of action is associated with inhibition of prostaglandin synthesis at the COX-1 and COX-2 levels.

Analgesic effect occurs 30 minutes after oral administration or parenteral administration. The duration of analgesic action after oral administration is 4-6 hours, after parenteral administration in a dose of 50 mg - about 4-8 hours.

When combined with opioid analgesics, dexketoprofen significantly (up to 30-45%) reduces the need for opioids.

Pharmacokinetics

Suction

After taking the drug inside C_maxDexketoprofen in human serum is reached on average in 30 minutes (15-60 minutes). Simultaneous ingestion slows down the absorption of the drug. The values ​​of AUC after single and repeated doses are similar, which indicates the absence of drug accumulation.

After i / m administration of dexketoprofen C_maxin serum is reached on average after 20 minutes (10-45 minutes). AUC after a single injection in a dose of 25-50 mg is proportional to the dose, as with the / m, and with a / in the introduction. The corresponding pharmacokinetic parameters are similar after a single and repeated intramuscular or intravenous injection, which indicates the absence of drug accumulation.

Distribution

Dexketoprofena is characterized by a high level of plasma protein binding - 99%. Average v value_dis less than 0.25 l / kg, half-time is about 0.35 h.

Metabolism and excretion

Metabolism of dexketoprofen mainly occurs by conjugation with glucuronic acid, followed by excretion by the kidneys.

T_1/2 Dexketoprofen trometamol is about 1-2.7 hours.

Pharmacokinetics in special clinical situations

In the elderly, there is an increase in the duration of T_1/2 (both after a single dose, and after repeated intramuscular injection or intravenous administration), on average, up to 48% and a decrease in the total clearance of the drug.

Indications

- relief of pain syndrome of various genesis (including postoperative pain, pain in bone metastases, post-traumatic pain, pain in renal colic, algomenorrhea, sciatica, sciatica, neuralgia, toothache);

- symptomatic treatment of acute and chronic inflammatory, inflammatory-degenerative and metabolic diseases of the musculoskeletal system (including rheumatoid arthritis, osteoarthritis, spondyloarthritis: ankylosing spondylitis, reactive arthritis, psoriatic arthritis).

The drug is intended for symptomatic therapy, reducing pain and inflammation at the time of use, does not affect the progression of the disease.

Dosage and administration

For oral administration

Flamadex^® taken orally with food.

Depending on the intensitypain syndrome recommended dose foradults makes 12.5 mg (1/2 tab.) each 4-6 h or 25 mg (1 tab.) each 8 h.

The maximum daily dose is 75 mg.

Forpatients with impaired liver and / or kidney function, elderly patients Flamadex drug therapy^® should start with lower doses. The maximum daily dose is 50 mg / day.

Flamadex^® not intended for long-term therapy, the course of drug treatment should not exceed 3-5 days.

For parenteral administration

Enter v / m (deep, slow), in / in the jet (slowly at least 15 seconds) or drip (10-30 min).

Recommended Dose foradults: 50 mg every 8-12 hours. If necessary, repeated administration of the drug with a 6-hour interval is possible. The daily dose should not exceed 150 mg.

Flamadex^® indicated for short-term use, treatment should be limited to a period of acute symptoms (no more than 2 days).

Havepatients with mild and moderately impaired liver function (5-9 points on the Child-Pugh scale) The total daily dose should be reduced to 50 mg and frequent monitoring of liver function should be performed. Flamadex^®should not be appointedin patients with severely impaired liver function.

Forpatients with mild renal dysfunction (CC - 30-60 ml / min)The daily dose is reduced to 50 mg. Flamadex^® should not be appointedin patients with moderate to severe renal failure (CC less than 30 ml / min).

Dose adjustment forelderly patientsAs a rule, it is not required, however, due to the physiological decline in renal function, it is recommended to reduce the dose of the drug:lung renal dysfunction in elderly patients The total daily dose is 50 mg.

Terms of preparation of the solution for IV infusion

To prepare the solution of Flamadex^® for intravenous infusion, the contents of one ampoule (2 ml) are diluted in 30-100 ml of a 0.9% solution of sodium chloride, glucose solution or Ringer's solution. The solution should be prepared under aseptic conditions, protected from exposure to daylight. The prepared solution should be clear and colorless.

Side effect

The incidence of side effects: often (1-10%), infrequently (0.1-1%), rarely (0.01-0.1%), very rarely (less than 0.01%, including individual messages).

Hemic and lymphatic: rarely - anemia; very rarely - neutropenia, thrombocytopenia.

Nervous system: infrequently - headache, dizziness, insomnia, drowsiness; rarely - paresthesia.

Special senses: infrequently - blurred vision; rarely tinnitus.

Cardiovascular: infrequently - arterial hypotension, feeling of heat, hyperemia of the skin; rarely - extrasystole, tachycardia, arterial hypertension, peripheral edema, superficial thrombophlebitis.

Respiratory: rarely bradypnea; very rarely - bronchospasm, dyspnea.

Gastrointestinal: often - nausea, vomiting; infrequently - abdominal pain, dyspepsia, diarrhea, constipation, hematemesis, dry mouth; rarely - erosive and ulcerative lesions of the gastrointestinal tract, including bleeding and perforation, anorexia, increased activity of liver enzymes, jaundice; very rarely - damage to the pancreas, liver damage.

Urogenital: rarely - polyuria, renal colic; very rarely - nephritis or nephrotic syndrome.

From the reproductive system: rarely, in women, menstrual disorders, in men, dysfunction of the prostate gland.

Musculoskeletal system: seldom - a muscular spasm, difficulty of movements in joints.

From the skin: sometimes - dermatitis, rash, sweating; rarely acne; very rarely - photosensitivity.

Allergic reactions: rarely - urticaria; very rarely - severe skin reactions (Stevens-Johnson syndrome, Lyell's syndrome), angioedema, allergic dermatitis, anaphylactic shock, swelling of the face.

Metabolism: rarely - hyperglycemia, hypoglycemia, hypertriglyceridemia.

From the laboratory indicators: rarely - ketonuria, proteinuria.

Local and general reactions: often - pain at the injection site; infrequently - inflammatory reaction, hematoma, hemorrhages at the injection site, feeling hot, chills, fatigue; rarely - back pain, fainting, fever.

Other: aseptic meningitis that occurs predominantly in patients with systemic lupus erythematosus or mixed connective tissue diseases, hematological disorders (purpura, aplastic and hemolytic anemia, rarely agranulocytosis and bone marrow hypoplasia).

Contraindications

- Hypersensitivity to dexketoprofen or other NSAIDs or to any of the excipients that make up the drug (including sulfites);

- complete or incomplete combination of bronchial asthma, recurrent nasal polyposis and paranasal sinuses and intolerance to Acetylsalicylic acid or other NSAIDs (including a history of);

- erosive and ulcerative lesions of the gastrointestinal tract and duodenum;

- a history of Gastrointestinal bleeding, other active bleeding (including suspected intracranial bleeding);

- anticoagulant therapy;

- inflammatory bowel disease (ulcerative colitis, Crohn's disease) in the acute phase;

- severe liver dysfunction (10-15 points on the Child-Pugh scale);

- progressive kidney disease, severe renal dysfunction (CC less than 30 ml / min);

- confirmed hyperkalemia;

- decompensated heart failure ;

- the period after coronary artery bypass surgery;

- hemophilia and other disorders of blood coagulation;

- pregnancy;

- breastfeeding period;

- children and adolescents up to 18 years of age (there are no clinical data on the efficacy and safety of the use of the drug in pediatric practice).

Flamadex^® solution for in / in and in / m administration is contraindicated for neuroaxial (epidural or intrathecal) administration due to the ethanol contained in the preparation.

Carefully:peptic ulcer and duodenal ulcer, ulcerative colitis, Crohn's disease, history of liver disease, hepatic porphyria, chronic renal failure (CC 30-60 ml / min), chronic heart failure, arterial hypertension, significant decrease in BCC (includingafter surgery), bronchial asthma, ischemic heart disease, cerebrovascular diseases, dyslipidemia / hyperlipidemia, diabetes mellitus, peripheral artery disease, the presence of Helicobacter pylori infection, systemic connective tissue diseases, prolonged use of NSAIDs, tuberculosis, marked osteoporosis, simultaneous administration of GCS, including. including prednisolone), anticoagulants (including warfarin), antiplatelet agents (including acetylsalicylic acid, clopidogrel), selective serotonin reuptake inhibitors (including citalopram, fluok setina, paroxetine, sertraline), severe somatic diseases, elderly patients (including receiving diuretics, weakened patients and with low body weight), alcoholism, smoking.

Use during pregnancy and lactation

Use of the drug Flamadex^® during pregnancy and lactation is contraindicated.

Application for violations of the liver

Havepatients with mild and moderately impaired liver function (5-9 points on the Child-Pugh scale) The total daily dose should be reduced to 50 mg and frequent monitoring of liver function should be performed. Flamadex^®should not be prescribed to patients withsevere liver dysfunction.

Application for violations of kidney function

Forpatients with mild renal dysfunction (CC - 30-60 ml / min)The daily dose is reduced to 50 mg. Flamadex^® should not be prescribed to patients withmoderate to severe renal failure (CC less than 30 ml / min).

Use in elderly patients

Dose adjustment forelderly patientsAs a rule, it is not required, however, due to the physiological decline in renal function, it is recommended to reduce the dose of the drug:lung renal dysfunction in elderly patients The total daily dose is 50 mg.

special instructions

Flamadex^® should be used with caution in patients with a history of allergies.

Care must be taken when prescribing the drug Flamadex^® patients with violations of the gastrointestinal tract or gastrointestinal diseases in history. In case of gastrointestinal bleeding or ulcer treatment with Flamadex^® should cancel.

It has been clinically proven that the simultaneous use of dexketoprofen and preparations of low molecular weight Heparin in prophylactic doses in the postoperative period does not change the clotting parameters. However, with simultaneous use of the drug Flamadex^® With other drugs that affect blood clotting, careful medical monitoring of the blood clotting system is necessary. Dexketoprofen may cause reversible inhibition of platelet aggregation.

Like other NSAIDs, Flamadex^® can lead to increased creatinine concentrations and plasma nitrogen levels. Like other prostaglandin synthesis inhibitors, Flamadex^® can have a side effect on the urinary system, which can lead to the development of glomerulonephritis, intestinal nephritis, papillary necrosis, nephrotic syndrome and acute renal failure .

As with the use of other NSAIDs, there may be a slight transient increase in some indicators of liver function, a significant increase in the activity of AST and ALT in serum. At the same time, the control of liver and kidney functions is necessary in elderly patients. In the case of a significant increase in the relevant indicators Flamadex^® should cancel.

Flamadex^® should be used with caution in patients with chronic heart failure I-II functional class by NYHA.

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