Flamadex, solution 25mg/ml ampoules 2ml 5pcs

Composition

1 amp. (2 ml):

– dexketoprofen trometamol (in terms of dexketoprofen) 50 mg

Auxiliary substances:

ethanol (95% ethyl alcohol in terms of 100% substance) 200 mg,

sodium chloride 8 mg,

sodium disulfite 2 mg,

sodium hydroxide up to pH 6.5-8.5,

water for injection up to 2 ml

Description:

transparent colorless solution.

Pharmacological action

Pharmacology:

A nonsteroidal anti-inflammatory drug (NSAID) derived from propionic acid. It has analgesic, anti-inflammatory and antipyretic effects. The mechanism of action is associated with inhibition of prostaglandin synthesis at the level of cyclooxygenase-1 and cyclooxygenase-2.

The analgesic effect occurs 30 minutes after parenteral use. The duration of the analgesic effect after use at a dose of 50 mg is about 4-8 hours.

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

Pharmacokinetics:  

Absorption After intramuscular (i/m) use of dexketoprofen, the maximum concentration (Cmax) in the blood serum is reached on average in 20 minutes (10-45 minutes). The area under the concentration-time curve (AUC) after a single dose of 25-50 mg is proportional to the dose, both with intramuscular and intravenous (IV) use. The corresponding pharmacokinetic parameters are similar after a single and repeated IV or IV use, which indicates that there is no accumulation of the drug.

Distribution Dexketoprofen is characterized by a high level of binding to plasma proteins (99%). The average Vd is less than 0.25 l / kg, and the half – life is about 0.35 hours.

Dexketoprofen is primarily metabolized by conjugation with glucuronic acid, followed by renal elimination. The half-life (T1/2) of dexketoprofen trometamol is about 1-2.7 h. Pharmacokinetics in special clinical cases In the elderly, there is an increase in the duration of T1 / 2 (both after a single and after repeated IV or IV use) by an average of 48% and a decrease in the total clearance of the drug.

Indications

-relief of pain syndrome of various origins (including postoperative pain, pain with bone metastases, post-traumatic pain, pain with renal colic, algodismenorrhea, 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, and does not affect the progression of the disease.

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 and paranasal sinus polyposis, and intolerance to acetylsalicylic acid or other NSAIDs (including in the anamnesis);- 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 diseases (ulcerative colitis, Crohn’s disease) in the acute stage; – severe liver function disorders (10-15 points on the Child-Pugh scale);- progressive kidney disease, severe renal impairment (creatinine clearance less than 30 ml / min);- confirmed hyperkalemia; – decompensated heart failure; – the period after coronary artery bypass grafting; – hemophilia and other blood clotting disorders;- pregnancy, breast-feeding period; – children and adolescents under 18 years of age. Flamadex® is contraindicated for neuroaxial (epidural or intrathecal) use due to the ethanol contained in the preparation. With caution: Peptic ulcer of the stomach and duodenum, ulcerative colitis, Crohn’s disease, a history of liver disease, hepatic porphyria, chronic renal failure (creatinine clearance 30-60 ml/min), chronic heart failure, arterial hypertension, a significant decrease in the volume of circulating blood (including after surgery), elderly patients (including those receiving diuretics, weakened patients and low body weight), bronchial asthma, concomitant use of the drug. use of glucocorticosteroids (including prednisone), anticoagulants (including warfarin), antiplatelet agents (including acetylsalicylic acid, clopidogrel), selective serotonin reuptake inhibitors (including citalopram, fluoxetine, paroxetine, sertraline), ischemic heart disease, cerebrovascular diseases, dyslipidemia/hyperlipidemia, diabetes mellitus, heart diseases peripheral arteries, smoking, presence of Helicobacter pylori infection, systemic connective tissue diseases, long-term use of nonsteroidal anti-inflammatory drugs, tuberculosis, severe osteoporosis, alcoholism, severe somatic diseases.

Side effects

Frequency of side effects: common (1-10%), infrequent (0.1-1%), rare (0.01-0.1%), very rare (less than 0.01%, including individual reports).

From the hematopoietic system: rarely-anemia; very rarely-neutropenia, thrombocytopenia.

From the central nervous system: infrequently-headache, dizziness, insomnia, drowsiness; rarely – paresthesia.

From the sensory organs: infrequently-blurred vision; rarely-tinnitus.

From the cardiovascular system: infrequently-hypotension, fever, hyperemia of the skin; rarely-extrasystole, tachycardia, hypertension, peripheral edema, superficial thrombophlebitis.

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

From the digestive system: often-nausea, vomiting; infrequently-abdominal pain, dyspepsia, diarrhea, constipation, hematemesis, dry mouth; rarely-erosive and ulcerative lesions of the gastrointestinal tract (GIT), including bleeding and perforation, anorexia, increased activity of liver enzymes, jaundice; very rarely – pancreatic damage, liver damage.

From the urinary system: rarely-polyuria, renal colic; very rarely-nephritis or nephrotic syndrome.

From the side of the reproductive system: rarely – in women-a violation of the menstrual cycle, in men-a violation of the function of the prostate gland.

From the musculoskeletal system: rarely-muscle spasm, difficulty moving in the joints.

Dermatological reactions: sometimes-dermatitis, rash, sweating; rarely-acne; very rarely-photosensitization. Allergic reactions: rarely-urticaria; very rarely-severe skin reactions (Stevens-Johnson syndrome, Lyell’s syndrome), angioedema, allergic dermatitis.

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

From the side of laboratory parameters: 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; very rarely-anaphylactic shock, facial edema

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

Interaction

Common interactions are common to all NSAIDs, including dexketoprofen. Unwanted combinations: – with other NSAIDs, including salicylates in high doses (≥ 3 g / day): simultaneous use of several NSAIDs increases the risk of gastrointestinal bleeding and ulcers; – with oral anticoagulants, heparin in doses exceeding the preventive ones;- with ticlopidine (increased risk of bleeding due to inhibition of platelet aggregation and damage to the mucous membrane of the digestive tract);- with lithium preparations, NSAIDs increase the concentration of lithium in the blood plasma (a decrease in renal excretion of lithium), which can reach toxic levels, so the level of lithium in the blood should be monitored when prescribing, changing the dose or discontinuing dexketoprofen; – with methotrexate in high (at least 15 mg/week) doses – methotrexate toxicity increases due to a decrease in its renal clearance when using NSAIDs; – with glucocorticosteroids: the risk of developing ulcers and gastrointestinal bleeding; – hydantoin derivatives and sulfonamides: the severity of their toxic manifestations may increase. Combinations that require caution: – with diuretics, ACE inhibitors, antibacterial drugs from the group of aminoglycosides and angiotensin II receptor antagonists. Dexketoprofen weakens the effect of diuretics and other antihypertensive agents.Treatment with NSAIDs is associated with the risk of acute renal failure in patients with dehydration (reduced glomerular filtration rate due to reduced prostaglandin synthesis). When combined with dexketoprofen and diuretics, it is necessary to ensure adequate hydration of the patient and monitor renal function before prescribing; – with methotrexate in low (less than 15 mg/week) doses-the hematological toxicity of methotrexate increases due to a decrease in its renal clearance when using NSAIDs. Weekly monitoring of the blood picture should be carried out in the first weeks of combined treatment. In the presence of even minor violations of renal function, as well as in the elderly, careful monitoring is necessary; – with pentoxifylline – the risk of bleeding increases. Active clinical monitoring and frequent monitoring of bleeding time or blood clotting time is required;- with zidovudine – a toxic effect of zidovudine on reticulocytes is possible, which after the first week of NSAID use can lead to the development of severe anemia. It is necessary to count blood cells and reticulocytes 1-2 weeks after the start of combined treatment; – with oral hypoglycemic drugs-due to the possible increase in hypoglycemic effect due to the ability of NSAIDs to displace them from the sites of binding to plasma proteins; Combinations that need to be considered:- with beta-blockers-it is possible to reduce their antihypertensive effect due to the inhibition of prostaglandin synthesis by NSAIDs;- with cyclosporine and tacrolimus: it is possible to increase their nephrotoxicity due to the effect of NSAIDs on renal prostaglandins. When conducting combination therapy, it is necessary to monitor renal function;- with thrombolytic drugs – the risk of bleeding increases;- with probenecid: an increase in the concentration of dexketoprofen in blood plasma is possible, which may be due to an inhibitory effect on tubular secretion and/or conjugation with glucuronic acid and requires dose adjustment of dexketoprofen;- with cardiac glycosides – NSAIDs may lead to an increase in their concentration in blood plasma;- with mifepristone – due to the theoretical risk of changing the effectiveness of mifepristone under the influence of prostaglandin synthesis inhibitors, NSAIDs should be prescribed 8-12 days after taking mifepristone;- quinolone antibiotics: a high risk of seizures when using NSAIDs in combination with high doses of quinolones. Pharmaceutical interaction. Flamadex® should not be mixed in the same syringe with a solution of dopamine, promethazine, pentazocine, pethidine or hydroxyzine (a precipitate forms). Flamadex® can be mixed in a single syringe with a solution of heparin, lidocaine, morphine and theophylline. The prepared solution of the drug Flamadex® for intravenous drip use should not be mixed with promethazine or pentazocine. The prepared solution of Flamadex® is compatible with the following solutions for injection: dopamine, heparin, hydroxyzine, lidocaine, morphine, pethidine and theophylline.

How to take, course of use and dosage

Intramuscular (deep, slow), intravenous jet (slow for at least 15 seconds) or drip (10-30 min). Recommended dose for adults: 50 mg every 8-12 hours. If necessary, repeated use of the drug with a 6-hour interval is possible. The daily dose should not exceed 150 mg. Flamadex® is indicated for short-term use, and treatment with it should be limited to the period of acute symptoms (no more than 2 days).

Impaired liver function.

In patients with mild to moderate hepatic impairment (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 carried out. Flamadex® should not be used in patients with severe hepatic impairment.

Impaired renal function.

For patients with mild renal impairment (creatinine clearance 30-60 ml / min), the daily dose is reduced to 50 mg. Flamadex® should not be used in patients with moderate or severe renal insufficiency (creatinine clearance less than 30 ml / min).

Elderly patients.

Dose adjustment for elderly patients is usually not required, but due to a physiological decrease in renal function, it is recommended to reduce the dose of the drug: a total daily dose of 50 mg for mild renal impairment in elderly patients.

Rules for preparing solutions.

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

Special instructions

Flamadex® should be used with caution in patients with a history of allergies. Patients with symptoms of gastrointestinal disorders or a history of gastrointestinal diseases should be monitored by a doctor, especially for gastrointestinal bleeding. In cases of gastrointestinal bleeding in patients taking dexketoprofen, the drug is immediately discontinued.

Caution should be exercised in patients taking concomitant medications that may increase the risk of ulceration or bleeding: corticosteroids, anticoagulants (such as warfarin), selective serotonin reuptake inhibitors, or antiplatelet agents (including acetylsalicylic acid).

Dexketoprofen may cause reversible inhibition of platelet aggregation and increase bleeding time. Flamadex® should be used with caution in patients with chronic heart failure of NYHA functional class I-II.

Similar to other NSAIDs, Flamadex® can cause an increase in plasma creatinine and nitrogen levels, have a negative effect on the urinary system, leading to the development of glomerulonephritis, interstitial nephritis, papillary necrosis, nephrotic syndrome and acute renal failure.

As with other NSAIDs, there may be a slight transient increase in the values of some liver tests, a significant increase in the activity of AST and ALT in the blood serum. At the same time, monitoring of liver and kidney functions is necessary in elderly patients. In case of a significant increase in the corresponding indicators, Flamadex® should be discontinued. Flamadex® should be used with caution in patients with hematopoietic disorders, patients with systemic lupus erythematosus or other connective tissue diseases.

Like other NSAIDs, Flamadex® may mask the symptoms of infectious diseases. Isolated cases of exacerbation of infectious processes localized in soft tissues have been reported with the use of NSAIDs. Therefore, medical supervision of patients with signs of bacterial infection or worsening of the condition during treatment with dexketoprofen is required. Caution should be exercised when prescribing the drug to patients with impaired liver, kidney, heart function or conditions that may cause fluid retention in the body. In these patients, the use of NSAIDs can lead to deterioration of the condition and fluid retention in the body. Caution should also be exercised when prescribing dexketoprofen to patients using diuretics or predisposed to hypovolemia, as they have an increased risk of developing nephrotoxicity.

Caution is necessary when prescribing the drug to the elderly, since they are more likely to have impaired renal, liver or cardiovascular function, as well as the occurrence of adverse reactions, such as gastrointestinal bleeding or intestinal perforation.

Each ampoule of Flamadex® contains 200 mg of ethanol.

Influence on the ability to drive vehicles and other mechanisms that require increased concentration of attention

Due to possible dizziness and drowsiness during treatment with Flamadex®, the ability to concentrate attention and the speed of psychomotor reactions may decrease.

Form of issue.

Solution for intravenous and intramuscular use of 25 mg / ml.

2 ml in ampoules of light-proof glass with a colored break ring or with a colored dot and notch. The ampoules are additionally marked with one, two or three colored rings and/or a two-dimensional barcode, and/or alphanumeric encoding, or without additional colored rings, a two-dimensional barcode, or alphanumeric encoding.

5 ampoules each in a contour cell package made of polyvinyl chloride film and aluminum foil or polymer film, or without foil and film.

1 or 2 contour cell packages together with instructions for use in a cardboard pack. Storage conditions.

In a dark place at a temperature not exceeding 25 °C. Keep out of reach of children.

Expiration date.

2 years old. Do not use after the expiration date indicated on the package.

Product form

solution for intravenous and intramuscular use

Active ingredient

Dexketoprofen

Conditions of release from pharmacies

By prescription

Dosage form

solution for injection and infusion

Purpose

For adults as directed by your doctor

Indications

Rheumatoid Arthritis, Sciatica, Osteochondrosis, Lumbago, Osteoarthritis, Arthritis, Sciatica, Trigeminal Neuralgia