Flamadex injection solution 25mg ml 2ml N5
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Active ingredients
Dexketoprofen
Release form
Solution
Composition
1 amp dexketoprofen (in the form of dexketoprofen trometamol) 50 mg. Excipients: ethanol (95% ethyl alcohol based on 100% substance) - 200 mg, sodium chloride - 8 mg, sodium disulfite - 2 mg, sodium hydroxide - to pH 6.
Pharmacological effect
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. With combined therapy with opioid analgesics, dexketoprofen significantly (up to 30-45%) reduces the need for opioids.
Pharmacokinetics
Absorption: After taking the drug inside the Cmax of dexketoprofen in human serum, an average of 30 minutes (15-60 minutes) is achieved. Simultaneous ingestion slows down the absorption of the drug. The values of AUC after single and repeated doses are similar, which indicates the lack of cumulation of the drug. After i / m administration of dexketoprofen, Cmax in the 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 administration, which indicates the absence of drug accumulation. Distribution: Dexketoprofen is characterized by a high level of plasma protein binding - 99%. The average value of Vd is less than 0.25 l / kg, the half-time is about 0.35 hours. Metabolism and excretion: Dexketoprofen metabolism mainly occurs by conjugation with glucuronic acid, followed by excretion by the kidneys. T1 / 2 of dexketoprofen trometamol is about 1-2.7 hours. Pharmacokinetics in special clinical situations: In elderly people, an increase in the duration of T1 / 2 is observed (both after a single dose and after repeated intramuscular or intravenous administration) to an average of 48 % and a decrease in the total clearance of the drug.
Indications
- relief of pain syndrome of various origins (includingpostoperative 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 (in t. 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.
Contraindications
- hypersensitivity to dexketoprofen or other NSAIDs or to any of the excipients that make up the drug (including sulfites) - a complete or incomplete combination of bronchial asthma, recurrent nasal polyposis, and acetylsalicylic acid or other NSAIDs ( including history) - erosive and ulcerative lesions of the gastrointestinal tract and duodenum - gastrointestinal bleeding in history, other active bleeding (including suspected intracranial bleeding) - anticoagulant th 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 kidney dysfunction (CC less than 30 ml / min) confirmed hyperkalemia - decompensated heart failure - period after coronary artery bypass surgery - hemophilia and other blood clotting disorders - pregnancy - breastfeeding period - children and adolescents under 18 years of age (no clinical data on the efficacy and safety of the drug in pediatric practice). Flamadex solution for iv administration and intramuscular injection is contraindicated for neuroaxial (epidural or intrathecal) administration due to ethanol contained in the preparation. With caution: gastric 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, a significant decrease in BCC (in tons). . h.after 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, fluo xetine, paroxetine, sertraline), severe somatic diseases, elderly patients (including receiving diuretics, weakened patients and with low body weight), alcoholism, smoking.
Use during pregnancy and lactation
The use of the drug Flamadex during pregnancy and lactation is contraindicated.
Dosage and administration
For ingestion, Flamadex is taken orally during meals. Depending on the intensity of the pain syndrome, the recommended dose for adults is 12.5 mg (1/2 tab.) Every 4-6 hours or 25 mg (1 tab.) Every 8 hours. The maximum daily dose is 75 mg. For patients with impaired liver and / or kidney function, elderly patients, Flamadex therapy should be started with lower doses. The maximum daily dose is 50 mg / day. Flamadex is not intended for long-term therapy, the course of drug treatment should not exceed 3-5 days. For parenteral administration. Introduce intramuscularly (deeply, slowly), intravenously in a jet (slowly for at least 15 seconds) or drip (10-30 minutes). Recommended dose for adults: 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 is indicated for short-term use, treatment should be limited to a period of acute symptoms (no more than 2 days). In patients 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 the functional parameters of the liver should be carried out. Flamadex should not be prescribed to patients with severely impaired liver function. For patients with mild renal dysfunction (CK - 30-60 ml / min), the daily dose is reduced to 50 mg.Flamadex should not be prescribed to patients with moderate to severe renal insufficiency (CC less than 30 ml / min). Dose adjustment for elderly patients, as a rule, is not required, but due to the physiological decline in renal function, it is recommended to reduce the dose of the drug: for mild violations of the kidney function in elderly patients, the total daily dose is 50 mg. Terms of preparation of the solution for intravenous infusion To prepare a solution of Flamadex for intravenous infusion, the contents of one ampoule (2 ml) are diluted in 30-100 ml of a 0.9% sodium chloride solution, 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 effects
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). From the hematopoietic system: rarely - anemia; very rarely - neutropenia, thrombocytopenia. From the nervous system: infrequently - headache, dizziness, insomnia, drowsiness; rarely - paresthesia. From the senses: infrequently - blurred vision; rarely tinnitus. Since the cardiovascular system: infrequently - arterial hypotension, feeling of heat, hyperemia of the skin; rarely - extrasystole, tachycardia, arterial hypertension, peripheral edema, superficial thrombophlebitis. On the part of the respiratory system: rarely - bradypnea; very rarely - bronchospasm, dyspnea. On the part of the digestive system: 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. From the urinary system: rarely - polyuria, renal colic; very rarely - nephritis or nephrotic syndrome. Reproductive system: rarely - in women - menstrual disorders, in men - dysfunction of the prostate gland. On the part of the musculoskeletal system: rarely - muscle spasm, difficulty in movements in the joints.For 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 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. 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).
Overdose
Cases of overdose are not described. Symptoms: nausea, vomiting, anorexia, abdominal pain, dizziness, disorientation, headache, drowsiness are possible. Treatment: symptomatic therapy; if necessary, hemodialysis.
Interaction with other drugs
Common types of interaction characteristic of all NSAIDs, including dexketoprin. Unwanted combinations With other NSAIDs, including salicylates in high doses (3 g / day) - the simultaneous use of several NSAIDs increases the risk of gastrointestinal bleeding and ulcers. With oral anticoagulants, heparin in doses exceeding prophylactic; with ticlopidine - increases the 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 (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 canceling dexketoprin. With methotrexate in high (at least 15 mg / week) doses, the toxicity of methotrexate is increased due to a decrease in its renal clearance with the use of NSAIDs.With GCS - the risk of developing ulcerative lesions and gastrointestinal bleeding increases. With hydantoin derivatives and sulfonamides, it is possible to increase the severity of manifestations of their toxicity. 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 drugs. Treatment of NSAIDs is associated with the risk of acute renal failure in patients with dehydration (reduced glomerular filtration due to reduced prostaglandin synthesis). With the combined use of dexketoprofen and diuretics, one should make sure that the patient is adequately hydrated and check renal function before administration. With simultaneous use with methotrexate in low doses (less than 15 mg / week), hematologic toxicity of methotrexate is increased due to a decrease in its renal clearance with the use of NSAIDs. A weekly monitoring of the blood picture should be performed in the first weeks of the combined treatment. In the presence of even minor violations of renal function, as well as in the elderly, careful monitoring is necessary. With simultaneous use with pentoxifylline increases the risk of bleeding. Active clinical monitoring and frequent monitoring of bleeding time or clotting time is required. With zidovudine, the 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 the blood cells and reticulocytes in 1-2 weeks. from the start of the combined treatment. With oral hypoglycemic drugs - due to the possible increase in hypoglycemic action 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 inhibition of NSAIDs prostaglandin synthesis. With cyclosporine and tacrolimus - it is possible to enhance their nephrotoxicity due to the effect of NSAIDs on renal prostaglandins. When conducting a combination therapy, it is necessary to monitor renal function.With thrombolytic drugs - the risk of bleeding increases. With probenecid, an increase in plasma dexketoprofen concentration is possible, which may be due to the inhibitory effect on tubular secretion and / or conjugation with glucuronic acid and requires dose adjustment of dexketoprene. With cardiac glycosides - NSAIDs can lead to an increase in their plasma concentration. With mifepristone, due to the theoretical risk of changing the effectiveness of mifepristone under the influence of prostaglandin synthesis inhibitors. NSAIDs should be administered 8–12 days after taking mifepristone. With quinolone antibiotics - a high risk of seizures when using NSAIDs in combination with high doses of quinolone. Pharmaceutical interaction Flamadex can not be mixed in the same syringe with a solution of dopamine, promethazine, pentazocine, petidine or hydroxyzine (a precipitate forms). Flamadex can be mixed in one syringe with a solution of heparin, lidocaine, morphine and theophylline. The prepared solution of the drug Flamadex for intravenous drip should not be mixed with promethazine or pentazocine. The prepared solution of Flamadex is compatible with the following solutions for injections: dopamine, heparin, hydroxyzine, lidocaine, morphine, pethidine and theophylline.
special instructions
Flamadex should be used with caution in patients with a history of allergies. Care must be taken when prescribing Flamadex to patients with a GI tract or gastrointestinal history. In case of gastrointestinal bleeding or ulcers, Flamadex therapy should be canceled. 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 the 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 an increase in creatinine concentration and plasma nitrogen content.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 be canceled. Flamadex should be used with caution in patients with chronic heart failure I-II functional class according to NYHA. Like other NSAIDs, Flamadex can mask the symptoms of infectious diseases. Reported single cases of exacerbation of infectious processes localized in soft tissues with the use of NSAIDs. Therefore, medical supervision of patients with signs of bacterial infection or deterioration during dexketoprofen treatment is required. Each ampoule of Flamadex with solution for IV and IM administration contains 200 mg of ethanol. Impact on the ability to drive vehicles and control mechanisms In connection with possible dizziness and drowsiness during treatment with the drug Flamadeks may reduce the ability to concentrate and speed of psychomotor reactions.