Communication to plasma proteins is high (99%) and most of the bound to albumin. Half-life in plasma of 1-2 hours.
No accumulation is observed in compliance with the recommended dosing interval. Well distributed in the tissues and body fluids. Synovial fluid penetrates and reaches a maximum concentration of 3-6 hours after administration.
The drug testosterone enanthate vs cypionate is metabolized in the liver: 50% of the active substance is metabolised during the “first pass” through the liver; area under the curve “concentration-time» (AUC) is less than 2 times after oral dosing than after parenteral administration of the same dose. Metabolism is the result of a single or multiple hydroxylation and conjugation. The metabolism is involved enzyme system P450 CYP2C9. The pharmacological activity of metabolites is lower than diclofenac.
The drug is derived primarily through the kidneys. Systemic clearance is 260 ml / min. The half-life is 1-2 hours. 60% of the administered dose is excreted through the kidneys in the form of metabolites and less than 1% – unchanged. The rest of the drug is excreted as metabolites in the bile.
It is noted that the pharmacokinetics of the drug does not vary depending on the age of the patient.
Against the background of repeated administration of diclofenac does not change the pharmacokinetics.
In patients with severe renal impairment (creatinine clearance less than 10 ml / min) increases the excretion of metabolites in the bile. Thus, an increase in their concentration in the blood is not observed.
In patients with chronic hepatitis or cirrhosis compensated diclofenac pharmacokinetic parameters are the same as in patients without liver disease.
Intramuscular injections at :
• Inflammatory diseases of the musculoskeletal system (rheumatoid arthritis, psoriatic, juvenile chronic arthritis, ankylosing spondylitis, acute gouty arthritis).
• Inflammation of the pelvis, adnexitis, primary algomenorrhea, renal or biliary colic, proctitis.
• Degenerative diseases of the musculoskeletal apparatus (deforming osteoarthritis, low back pain).
• pain (lumbago, sciatica, neuralgia, myalgia, tendonitis, bursitis, rheumatic soft tissue, tooth and headache, migraine and pain of moderate severity others. genesis).
• Post-traumatic pain, accompanied by inflammation.
• Post-operative pain.
• In the combined therapy of infectious and inflammatory diseases of the ear, nose and throat with severe pain (pharyngitis, tonsillitis, otitis media).
• Feverish syndrome.
Intravenous drip infusion
Prevention and treatment of postoperative pain.
• Hypersensitivity to NSAIDs (including acetylsalicylic acid), “Aspirin” asthma,
• erosive and ulcerative lesions GIT (exacerbation), bleeding from the gastrointestinal tract,
• inhibition of bone marrow hematopoiesis,
• various hemostatic disorders (including hemophilia) ,
• for conditions associated with a high risk of bleeding (including history),
• children under 15 years,
Precautions: anemia, asthma, congestive heart failure, arterial hypertension, edema syndrome, liver or kidney failure, alcoholism, diverticulitis, erosive and ulcerative diseases of the gastrointestinal tract without exacerbation, diabetes, postoperative induced acute hepatic porphyria, elderly age.
Dosing and Administration
The drug is administered intramuscularly or intravenously as an infusion. Introduce no more than 2 days. If necessary, extension of treatment for patients administered the drug in the form of tablets or suppositories.
Intramuscular injections :
patients with acute pain administered 75 mg daily intramuscularly. If necessary (biliary or renal colic) the daily dose may be increased to 150 mg (1 ampoule 2 times daily)
Intravenous infusion : The drug is administered as a drip infusion. Immediately before administration the contents of one vial (75 mg) should be diluted in 100-500 ml 0.9% NaCl solution or 5% dextrose solution (pre-infusion solutions adding sodium bicarbonate solution – 0.5 ml of 8.4%). Solution for infusion should be transparent.
In the treatment of postoperative pain of moderate to severe severity drug is administered in a dose of 75 mg for 30 – 120 minutes. If necessary, the drug may be administered repeatedly over several hours.However, dose should not exceed 150 mg per 24 hours.
In order to prevent postoperative pain carried infusion “shock” 25-50 mg drug dose within 15-60 min. In still further infusion rate of 5 mg / hr up to a maximum daily dose of 150 mg.
From the digestive system
• common (> 1 case per 100 prescriptions): NSAID-gastropathy (gastralgia and discomfort in the epigastric region, nausea, vomiting, feeling of fullness, belching, heartburn, diarrhea, abdominal pain, flatulence), erosive and ulcerative lesions of the gastrointestinal tract (including the defeat esophagus, stomach, peptic ulcer disease, multiple shock syndrome); perforation of the bowel wall (intensive cutting pain, a burning sensation in the epigastric region, bloody stools, melena, hematemesis), gastrointestinal (hematemesis, melena) bleeding, non-specific colitis with bleeding, dry mouth, constipation, pancreatitis, toxic hepatitis.
• rarely (<1 case per 100 prescriptions, but not> 1 case per 1000 prescriptions) -rvota, colitis or its exacerbation, decreased appetite or anorexia, dryness, soreness of oral mucosa, spasm, aphthous stomatitis (erosion, ulcers, white patches on the oral mucosa)
From the nervous system
• common (> 1 case per 100 prescriptions): headache, testosterone enanthate vs cypionate dizziness
• rarely (<1 case per 100 prescriptions, but not> 1 case per 1000 prescriptions): convulsions, aseptic meningitis, memory loss, depression, psychotic reactions, peripheral neuropathy (gipostezii, tremor, pain or weakness in the muscles of the arms and legs) , drowsiness, irritability and nervousness, anxiety, insomnia, fatigue.
From the senses:
• common (> 1 case per 100 prescriptions): toxic amblyopia, blurred vision, diplopia, scotoma, hearing loss and other hearing loss, ringing in the ears..
For the skin:
• common (> 1 case per 100 prescriptions): itching, skin rash (primarily erythematous and urticaria), redness of the skin;
• rarely (<1 case per 100 prescriptions, but not> 1 case per 1000 prescriptions): erythema multiforme, including Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell’s syndrome), fotodermatit (severe sunburn, skin rashes, pigmentation disorders);
• rare (<0.001% of the cases): in place of the / m are possible: burning; infiltration, aseptic necrosis, necrosis of adipose tissue. In some cases, the injection site may develop necrosis.
With the genitourinary system:
• common (> 1 case per 100 prescriptions): fluid retention;
• rarely (<1 case per 100 prescriptions, but not> 1 case per 1000 prescriptions): repeated vaginal pain of unknown origin, dysmenorrhea, hematuria, cystitis, pollakiuria, proteinuria, interstitial nephritis, nephrotic syndrome, oliguria or anuria, decreased kidney function or worsening peripheral edema.
From the side of hematopoiesis
• rarely (<1 case per 100 prescriptions, but not> 1 case per 1000 prescriptions): agranulocytosis, hemolytic anemia, aplastic anemia, anemia associated with internal bleeding, ecchymosis, leukopenia, neutropenia, thrombocytopenia with or without purpura her.
The respiratory system
• rarely (<1 case per 100 prescriptions, but not> 1 case per 1000 prescriptions): shortness of breath.
• common (> 1 in 100 destinations): increased blood pressure;
• rarely (<1 case per 100 prescriptions, but not> 1 case per 1000 prescriptions): arrhythmia, false angina, collapse;
• rare (<0.001% of the cases): chest pain, worsening of congestive heart failure.
• rare (<0.001% of the cases): weight loss.
• rare (<0.001% of the cases): anaphylaxis and anaphylactoid reactions (focal hyperemia, urticaria, pruritus, dyspnea, angioneurotic edema of the eyelids or paraorbital tissue, lips, tongue, glottis, oppressive chest pain, wheezing, anaphylactic shock ( usually develops rapidly), bronchospastic allergic reactions.
Symptoms: The symptoms of the gastrointestinal tract, hypotension, renal toxicity (up to acute renal failure), disorders of the central nervous system (from lethargy and drowsiness to seizures and coma).
Treatment: symptomatic and supportive, aimed at addressing the symptoms.
Forced diuresis, hemodialysis ineffective.
Interaction with other drugs
Increasing the concentration of digoxin in plasma of methotrexate, and cyclosporine drugs lithium.
Reduces the effect of diuretics, potassium-sparing diuretics in the background increases the risk of hyperkalemia; amid anticoagulants, thrombolytic agents (alteplase, streptokinase, urokinase) – risk of bleeding (usually from the gastrointestinal tract).
It reduces the effects of antihypertensive and hypnotic drugs.
Increases the likelihood of side effects of other drugs, and nonsteroidal anti-inflammatory glucocorticosteroid means (bleeding in the gastrointestinal tract), the toxicity of methotrexate and cyclosporine nephrotoxicity.
Aspirin reduces the concentration of diclofenac in the blood.
Simultaneous use of testosterone enanthate vs cypionate paracetamol increases the risk of nephrotoxic effects of diclofenac.
It reduces the hypoglycemic effect of hypoglycaemic agents.
Tsefamandol, tsefaperazon, tsefotetan, valproic acid and plikamitsin increase the incidence gipoprotrombinemii.
Cyclosporine and gold preparations increase the influence of diclofenac on the synthesis of prostaglandins in the kidney, which is manifested by increased nephrotoxicity.
Co-administration with ethanol, colchicine, corticotropin, and St. John’s wort preparations increases the risk of bleeding in the gastrointestinal tract.
Drugs that cause photosensitivity, increase the sensitizing effect of diclofenac to ultraviolet radiation.
Drugs that block tubular secretion, increase the diclofenac concentration in plasma, thereby increasing its efficiency and toxicity.
In the period of treatment should be systematic monitoring of peripheral blood, liver, kidney, feces study on the presence of blood.
Patients receiving the drug should refrain from activities requiring increased attention and rapid mental and motor reactions, the use of alcohol.
5 vials of 3 ml was placed in a transparent tray and together with instructions for use in putting a cardboard box.
Shelf life 5 years
Do not use end date.
Storage Used List