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

Excipients: cellulose microcrystalline 181.89-183.84 mg, pregelatinized starch 26.26 mg, sodium carboxymethyl starch (sodium starch glycolate) 10.40 mg, magnesium stearate 2.60-4.55 mg;

composition of the shell: titanium dioxide 2.5 mg, hypromellose (hypromellose 2910) 2.5 mg, polydextrose 2.5 mg, macrogol 0.5 mg.

Description:

Round, biconvex tablets, covered with a film shell of white color, with a risk on both sides. On the cross section, the nucleus is white or almost white in color.

Pharmacotherapeutic group:NSAIDs

ATX: & nbsp

M.01.A.E Propionic acid derivatives

M.01.A.E.17 Dexketoprofen

Pharmacodynamics:

Non-steroidal anti-inflammatory drug (NSAID).

Has analgesic, anti-inflammatory and antipyretic effects. The mechanism of action is associated with inhibition of the synthesis of prostaglandins at the level of COX-1 and COG-2.

The analgesic effect occurs 30 minutes after oral administration, the duration of action is 4-6 h.

With combined therapy with analgesics of the opioid series of dexketoprofen trometamol significantly (up to 30-45%) reduces the need for opioids.

Pharmacokinetics:

Suction

After taking the drug inside the maximum concentration in the serum (C_max) of dexketoprofen in humans is achieved in an average of 30 min (15-60 min). Simultaneous food intake slows the absorption of the drug. Areas under the concentration-time curve (AUC) after a single and repeated procedures are similar, which indicates the absence of cumulation of the drug.

Distribution

The binding with plasma proteins is 99%, the average volume of distribution is less than 0.25 l / kg, the half-distribution period is about 0.35 h.

Excretion

The main way to excrete dexketoprofen is its conjugation with glucuronic acid, followed by excretion by the kidneys. The half-life (T_1/2) is 1.65 hours.In elderly people there is an increase in T_1/2an average of 48% and a decrease in the overall clearance of the drug.

Indications:

- relief of pain of various genesis (including postoperative, posttraumatic pain, bone metastases, renal colic, tuberculosis, sciatica, sciatica, neuralgia, dental pain, etc....);

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

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

Contraindications:

- Hypersensitivity to dexketoprofen or other HPVP or to any of the excipients included in the formulation;

- erosive-ulcerative lesions of the gastrointestinal tract and duodenum in the phase of exacerbation;

- gastrointestinal hemorrhages in the anamnesis, other active bleeding (incl.suspicion of intracranial hemorrhage), anticoagulant therapy;

- Inflammatory bowel disease (Crohn's disease, ulcerative colitis) in the phase of exacerbation;

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

- moderate or severe renal dysfunction (creatinine clearance less than 30 ml / min);

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

- therapy with anticoagulants;

- Decompensated heart failure;

- period after aortocoronary shunting;

- hemophilia and other disorders of blood clotting;

- progressive kidney disease;

- PConfirmed hyperkalemia;

- Children under 18 years of age (there are no clinical data on the effectiveness and safety of the drug in pediatric practice);

- pregnancy, the period of breastfeeding.

Carefully:

Stomach and duodenal ulcer, ulcerative colitis, Crohn's disease, history of liver disease, hepatic porphyria, chronic renal failure (creatinine clearance 30-60 ml / min), chronic heart failure I-II functional class by classification NYHA, arterial hypertension, a significant decrease in the volume of circulating blood (including after surgery), elderly patients (including receiving diuretics, weakened patients and low body weight), bronchial asthma, simultaneous reception of glucocorticosteroids (including prednisolone) , anticoagulants (including warfarin), antiplatelet agents (including acetylsalicylic acid, clopidogrel), selective serotonin reuptake inhibitors (including citalopram, fluoxetine, paroxetine, sertraline), ischemic I have heart disease, cerebrovascular disease, dyslipidemia / hyperlipidemia, diabetes mellitus, peripheral vascular disease, smoking, presence of infection Helicobacter pylori, systemic connective tissue diseases, long-term use of non-steroidal anti-inflammatory drugs, tuberculosis, severe osteoporosis, alcoholism, severe somatic diseases.

Pregnancy and lactation:

Flamadex ® is contraindicated in pregnancy and during breastfeeding due to the lack of reliable clinical data to confirm the safety of its use.

Dosing and Administration:

Flamadex® is taken orally during meals.

Depending on the intensity of the pain syndrome, the recommended adult dose is 12.5 mg (1/2 tablet) every 4 to 6 hours or 25 mg (1 tablet) every 8 hours.

The maximum daily dose is 75 mg.

For patients with impaired liver and / or kidney function, elderly people Therapy with Flamadex® should be started with lower doses. The maximum daily dose is 50 mg per day.

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

Side effects:

The frequency of side effects noted with the use of dexketoprofen is given in accordance with the classification of the World Health Organization (WHO): very often (more than 10%), often (1-10%), infrequently (0.1-1%), rarely (0 , 01-0.1%), very rarely (less than 0.01%), including individual reports.

FROMabout the side of the blood and lymphatic system: very rarely - neutropenia, thrombocytopenia.

FROMabout the side of the nervous system: infrequently - headache, dizziness, insomnia, drowsiness; rarely - paresthesia.

Co side of the senses: rarely - noise in the ears; very rarely - blurred vision.

Co cardiovascular system: infrequent - a feeling of heat, hyperemia of the skin; rarely - extrasystole, increased blood pressure; very rarely - tachycardia, lowering blood pressure.

From the respiratory system: rarely - bradypnoe; very rarely - bronchospasm, dyspnea.

From the gastrointestinal tract: often - nausea, vomiting, abdominal pain, dyspepsia, diarrhea; infrequent - constipation, dry mouth, flatulence; rarely - erosive-ulcerative lesions of the gastrointestinal tract, bleeding from the ulcer or its perforation, anorexia; very rarely - the defeat of the pancreas.

From the liver and bile ducts: rarely - increased activity of "hepatic" enzymes, including aspartate aminotransferase and alanine aminotransferase (ACT and ALT, jaundice; very rarely - liver damage.

From the side of the kidneys and urinary tract: rarely - polyuria; very rarely - nephritis or nephrotic syndrome.

On the part of the reproductive system: rarely - in women the menstrual cycle, in men - transient dysfunction of the prostate gland with prolonged use.

From the musculoskeletal system: rarely - back pain, muscle spasm, difficulty in joint movements.

From the skin and subcutaneous tissues: infrequently, dermatitis, rash; rarely - hives, acne, sweating; very rarely - severe skin reactions (Stevens-Johnson syndrome, Lyell's syndrome). angioedema, allergic dermatitis, photosensitivity.

From the side of metabolism: rarely - hyperglycemia, hypoglycemia, hypertriglyceridemia.

Laboratory data: rarely - ketonuria, proteinuria.

From the general status: infrequently - fever, fatigue; very rarely - anaphylactic shock, swelling of the face.

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

Overdose:

Symptoms: nausea, anorexia, abdominal pain, headache, dizziness, disorientation, insomnia.

Treatment: symptomatic therapy; if necessary - gastric lavage, hemodialysis.

Interaction:

Belowthe following interactions are characteristic of of all NSAIDs.

Unwanted combinations

With others NSAIDs, including salicylates in high doses (more 3 g / day): simultaneous application of several NSAIDs due to the synergistic effect increases the risk of gastrointestinal bleeding and ulcers.

With oral anticoagulants, heparin in doses exceeding preventive, and ticlopidine: increased risk of bleeding due to inhibition of platelet aggregation and damage to the gastrointestinal mucosa.

With lithium preparations: NSAIDs increase the concentration of lithium in the blood, down to toxic, and therefore this indicator should be monitored when applying, changing the dose and after the abolition of NSAIDs.

With methotrexate in high doses (15 mg / week and more): increase of hematological toxicity of methotrexate in connection with a decrease in its renal clearance against the background of therapy with NSAIDs.

With hydantoins and sulfonamides: risk of intensifying the toxic effects of these drugs.

Combinations that require caution

With diuretics, angiotensin-converting enzyme inhibitors: therapy with NSAIDs is associated with the risk of developing acute renal failure in dehydrated patients (reduced glomerular filtration due to reduced synthesis of prostaglandins). NSAIDs may reduce the antihypertensive effect of certain drugs.

With methotrexate in low doses (less than 15 mg / week): increase of hematological toxicity of methotrexate in connection with a decrease in its renal clearance against the background of therapy with NSAIDs. It is necessary to conduct a weekly count of blood cells in the first weeks of simultaneous therapy. In the presence of a violation of kidney function, even in an easy degree, as well as in the elderly, careful medical supervision is necessary.

With serotonin reuptake inhibitors (citalopram, fluoxetine, sertraline), oral glucocorticosteroids: increased risk of developing gastrointestinal bleeding.

With pentoxifylline: increased risk of bleeding. It requires intensive clinical monitoring and frequent checking of bleeding time (blood clotting time).

With zidovudine: risk of intensifying the toxic effect on erythrocytes due to exposure to reticulocytes, with the development of severe anemia a week after NSAID administration. It is necessary to conduct a general blood test with counting the number of reticulocytes 1-2 weeks after the initiation of therapy with NSAIDs.

With oral hypoglycemic agents: NSAIDs can enhance the hypoglycemic effect of sulfonylurea due to its displacement from the binding sites to plasma proteins.

With preparations of low-molecular heparin: increased risk of bleeding.

Combinations that need to be taken into account

FROM βadrenoblockers: NSAIDs can reduce the hypotensive effect of β-blockers, which is due to inhibition of prostaglandin synthesis.

With cyclosporine and tacrolimus: NSAIDs can increase nephrotoxicity, which is mediated by the action of renal prostaglandins. During the simultaneous therapy, it is necessary to monitor the kidney function.

With thrombolytics: increased risk of bleeding.

With probenecid: the concentration of NSAIDs in the blood plasma may increase, which may be due to the inhibitory effect of probenecid on renal tubular secretion and / or conjugation with glucuronic acid, which requires correction of the NSAID dose.

With cardiac glycosides: NSAIDs can lead to an increase in the concentration of glycosides in the blood plasma.

With mifepristone: in connection with the theoretical risk of changing the effectiveness of mifepristone under the influence of synthesis inhibitorsprostaglandins NSAIDs should not be prescribed earlier than 8-12 days after the withdrawal of mifepristone.

With quinolones: the data obtained in experimental studies on animals indicate a high risk of seizures when using NSAIDs with quinolone therapy in high doses.

Special instructions:

Caution should be exercised in prescribing Flamadex® to patients with gastrointestinal disorders or gastrointestinal illnesses in the history. In case of gastrointestinal bleeding or ulcers, Flamadex® should be discontinued.

It has been clinically proven that the simultaneous use of dexketoprofen and low-molecular-weight heparin preparations in prophylactic doses in the postoperative period does not change the coagulability. However, with the simultaneous use of the preparation Flamadex ® with other drugs that affect blood clotting, careful medical testing of the blood clotting system is necessary. Dexketoprofen can cause reversible inhibition of platelet aggregation.

Like other NSAIDs, Flamadex® can lead to an increase in the concentration of creatinine and nitrogen in the blood plasma.Like other inhibitors of prostaglandin synthesis, Flamadex® can have a side effect on the urinary system, which can lead to the development of glomerulonephritis, interstitial nephritis, papillary necrosis, nephrotic syndrome, and acute renal failure.

As in the case of the use of other NSAIDs, against the background of therapy with the drug Flamadex^®there may be a slight transient increase in some hepatic parameters, as well as a significant increase in activity ACT and ALT in the blood serum. At the same time, control of liver and kidney function is necessary in the elderly. In the case of a significant increase in the corresponding indicators of Flamadex^® should be canceled.

Flamadex^® with caution appoint to patients with chronic heart failure I-II functional class by classification NYHA.

Like other NSAIDs, dexketoprofen can mask the symptoms of infectious diseases. In case of signs of infection or deterioration of well-being against the background of therapy with Flamadex^® the patient should immediately consult a doctor.

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

In connection with the possible occurrence of dizziness and drowsiness during the administration of dexketoprofen, caution should be used in patients engaged in potentially hazardous activities requiring increased attention and speed of psychomotor reactions.

Form release / dosage:

Film-coated tablets, 25 mg.

Packaging:

For 10 tablets in a planar cell packaging made of polyvinylchloride film and aluminum foil.

For 1, 3 or 5 contour squares with instructions for use in a pack of cardboard.

Storage conditions:

In a dry, the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

2 years.

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

Terms of leave from pharmacies:On prescription

Registration number:LP-003279

Date of registration:27.10.2015

Date of cancellation:2020-10-27

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

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

Information update date: & nbsp07.01.2016

Illustrated instructions

Instructions

Flamadex® (FLAMADEX®)