Voltaren solution for intramuscular injection of 75mg ampoules 3ml N5
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Active ingredients
Diclofenac
Release form
Solution
Pharmacological effect
NSAIDs. Voltaren contains diclofenac sodium, a nonsteroidal substance that has a pronounced anti-inflammatory, analgesic and antipyretic effect. The main mechanism of diclofenac action, established in the experiment, is the inhibition of prostaglandin biosynthesis. Prostaglandins play an important role in the genesis of inflammation, pain and fever. In vitro, diclofenac sodium in concentrations equivalent to those achieved in treating patients does not suppress the biosynthesis of cartilage proteoglycans. In rheumatic diseases, the anti-inflammatory and analgesic properties of Voltaren provide a distinct effect on character. manifestations of diseases such as pain at rest and with movement, morning stiffness and swelling of the joints, as well as improvement in function Functional state. In post-traumatic and postoperative inflammatory events, Voltaren quickly relieves pain (arising both at rest and when moving), reduces inflammatory swelling and swelling of a postoperative wound.
Pharmacokinetics
Absorption After intramuscular (IM) administration of 75 mg of diclofenac, its absorption begins immediately. Cmax, the average value of which is about 2.5 mcg / ml (8 mcmol / l), is reached in about 20 minutes. The amount of active substance absorbed is linearly dependent on the dose of the drug. The area under the concentration-time curve (AUC) after intramuscular administration of Voltaren; about 2 times more than after its oral or rectal use, since in the latter cases about half the amount of diclofenac is metabolized by the first passage through the liver. In subsequent injections, the pharmacokinetic parameters do not change. Subject to the recommended intervals between injections of the drug, no cumulation is noted. Distribution: Communication with serum proteins is 99.7%, mainly with albumin (99.4%). The apparent volume of distribution is 0.12-0.17 l / kg. Diclofenac penetrates into the synovial fluid, where its maximum concentration is reached 2-4 hours later than in the blood plasma.The apparent half-life of synovial fluid is 3-6 hours. 2 hours after reaching the maximum plasma concentration, the concentration of diclofenac in the synovial fluid is higher than in plasma, and its values remain higher over a period of time up to 12 hours. Diclofenac was detected in low concentration (100 ng / ml) in breast milk of one of the nursing mothers. The estimated amount of the drug entering the baby’s body through breast milk is equivalent to 0.03 mg / kg / day. Metabolism Diclofenac metabolism is carried out in part by glucuronization of the unchanged molecule, but mainly through single and multiple hydroxylation and methoxylation, which leads to the formation of several phenolic metabolites (3 ' -hydroxy-, 4'-hydroxy-, 5'-hydroxy-, 4 ', 5-dihydroxy- and 3'-hydroxy-4'-methoxydicofenac), most of which are converted to glucuronide conjugates. The bottom of the phenolic metabolite is biologically active, but to a much lesser extent than diclofenac. Introduction The total systemic plasma clearance of diclofenac is 263 ± 56 ml / min. The final half-life is 1-2 hours. T1 / 2 4 metabolites, including two pharmacologically active, are also short and 1-3 hours. One of the metabolites, 3'-hydroxy-4'-methoxy-diclofenac, has more than a long half-life, however, this metabolite is completely inactive. About 60% of the drug dose is excreted in the urine as glucuronic conjugates of the unchanged active substance, and also as metabolites, most of which are also glucuronic conjugates. Unchanged, less than 1% of diclofenac. The remaining dose of the drug is excreted in the form of metabolites with bile. The concentration of diclofenac in plasma linearly depends on the size of the dose taken. The pharmacokinetics in certain groups of patients Absorption, metabolism and excretion of the drug does not depend on age. However, in some elderly patients, a 15-minute IV infusion of diclofenac resulted in an increase in plasma concentration of the drug by 50% compared to that expected in adult patients. In patients with impaired renal function, the unchanged active substance is not observed when the recommended dosing regimen is observed.When QA is less than 10 ml / min, the calculated equilibrium concentrations of diclofenac hydroxyl tabolites are about 4 times higher than in healthy volunteers, and the metabolites are derived exclusively with bile. In patients with chronic hepatitis or compensated liver cirrhosis, the pharmacokinetics of diclofenac are similar to those in patients without liver disease .
Indications
Inflammatory and degenerative diseases of the musculoskeletal system: rheumatoid arthritis, juvenile rheumatoid arthritis, ankylosing spondylitis, osteoarthritis, spondyloarthritis, osteoarthritis, spinal diseases accompanied by pain, rheumatoid arthritis, extra-articular soft tissue; shell); post-traumatic and postoperative pain syndromes accompanied by inflammation and edema; gynecological diseases accompanied by pain and inflammation (for example, primary algodysmenorrhea, adnexitis); as an additional remedy for severe infectious and inflammatory diseases of the ear, throat and nose, occurring with severe pain, for example, pharyngitis, tonsillitis, otitis (with the exception of retard pills) . The main treatment of the disease is carried out in accordance with generally accepted principles, incl. with the use of etiotropic therapy. Isolated fever is not an indication for the use of a drug. V / m administration of the drug is particularly preferable at the onset of exacerbations of inflammatory and degenerative diseases with a high inflammatory activity and in painful conditions caused by inflammation of non-rheumatic genesis.
Contraindications
An ulcer of the stomach or intestines; anamnestic information about attacks of asthma, urticaria, acute rhinitis associated with the use of acetylsalicylic acid or other NSAIDs, as well as any drugs that suppress the production of prostaglandins; proctitis (only for suppositories); blood formation disorders; children under 14 years old ; Hypersensitivity to diclofenac and any other ingredients of the drug.
Use during pregnancy and lactation
The use of Voltaren in pregnancy is possible only in cases where the expected benefit to the mother outweighs the potential risk to the fetus. The drug is prescribed in the minimum effective dose.Just as in the case of other prostaglandin synthetase inhibitors, these recommendations are especially important in the third trimester of pregnancy (suppression of uterine contractility is possible and premature closure of the arterial duct in the fetus). The use of Voltaren in the form of a solution for i / m administration during pregnancy is not It is recommended. If necessary, the appointment of Voltaren in the form of a solution for i / m injection during lactation should decide on the termination of breastfeeding.
Side effects
On the part of the digestive system: Sometimes - epigastric pain, nausea, vomiting, diarrhea, abdominal cramps, dyspepsia, flatulence, anorexia, increased serum aminotransferase activity. Rarely - gastrointestinal bleeding (vomiting blood, melena, diarrhea with admixture blood), ulcers of the stomach and intestines, accompanied or not accompanied by bleeding or perforation, hepatitis, accompanied or not accompanied by jaundice. In some cases - aphthous stomatitis, glossitis, damage to the esophagus, the occurrence of diaphragm monoid strictures in the intestines, disorders of the distal colon, such as nonspecific hemorrhagic colitis, exacerbation of ulcerative colitis or Crohn's disease, constipation, pancreatitis, fulminant hepatitis. From the CNS and peripheral nervous system: Sometimes - headache, dizziness Rarely - sleep, sleep. In some cases - sensitivity disorders, including paresthesias, memory disorders, disorientation, insomnia, irritability, convulsions, depression, anxiety, nightmares, tremor, psycho Ecy reactions, aseptic meningitis. From the sense organs: In some cases - visual impairment (blurred vision, diplopia), hearing loss, tinnitus, taste disturbances. From the cardiovascular system: In some cases - feeling of palpitations, pain chest, increased blood pressure, aggravation of congestive heart failure. Dermatological reactions: Sometimes - skin rashes. Rarely - urticaria. In some cases - bullous rashes, eczema, erythema multiforme, Stevens-Johnson syndrome, Lyell's syndrome (acute toxic epidermal necrolysis), erythroderma (exfoliative dermatitis), hair loss, photosensitivity reactions, purpura (includingallergic). From the urinary system: Rarely - edema. In some cases - acute renal failure, hematuria, proteinuria, interstitial nephritis, nephrotic syndrome, papillary necrosis. From the hematopoietic system: In some cases - thrombocytopenia, leukopenia, hemolytic anemia, aplastic anemia, agranulocytosis. Hypersensitivity reactions: Rarely - bronchospasm, systemic anaphylactic / anaphylactoid reactions, including hypotension. In some cases - vasculitis, pneumonitis. Local reactions AI: Seal, bol.V some cases - abscesses, nekrozy.Perechislennye Side effects were observed including with the use of doses of the drug and the duration of treatment, different from the recommended.
Overdose
There is no typical clinical picture characteristic of Voltaren's overdose. Symptoms: decrease in blood pressure, renal failure, convulsions, disorders of the gastrointestinal tract and respiratory depression. Treatment: supportive and symptomatic. It is unlikely that forced diuresis, hemodialysis or hemoperfusion will be useful for removing NSAIDs, because The active substances of these drugs are largely associated with plasma proteins and are extensively metabolized.
Interaction with other drugs
Voltaren can increase the concentration of lithium and digoxin in the plasma while used with these drugs. Voltaren, like other NSAIDs, can reduce the effect of diuretics. Simultaneous use of Voltaren with potassium-sparing diuretics can lead to an increase in potassium levels in the blood (in the case of such a combination of drugs, this indicator should be monitored often). Simultaneous use of Voltaren with other NSAIDs may increase the risk of side effects. the action of anticoagulants, there are separate reports of an increased risk of bleeding in cases of their joint use. It is recommended that careful monitoring of patients receiving these drugs at the same time. Voltaren can be assigned together with oral hypoglycemic drugs and the effectiveness of the latter does not change.However, there are individual reports of the development in such cases of both hypoglycemia and hyperglycemia, which necessitated a change in the dose of hypoglycemic drugs during the use of Voltaren. Care should be taken when using NSAIDs less than 24 hours before the start of treatment or after treatment with methotrexate, t. to. its level in the blood (and therefore toxicity) may increase. The effect of NSAIDs on kidney prostaglandin activity may increase cyclosporine nephrotoxicity. There are isolated reports of seizures in patients who took both NSAIDs and quinolone antibacterial drugs. You should not mix the Voltaren solution contained in ampoules, with solutions of other drugs for injection.
special instructions
During the application of Voltaren, careful medical supervision of those patients who have complaints pointing to gastrointestinal diseases is necessary; having a history of ulcerative lesions of the stomach or intestines; suffering from ulcerative colitis or Crohn's disease, as well as having impaired liver function. Against the background of Voltaren's use, gastrointestinal bleeding may occur (for the first time or again) or develop ulceration / perforation of the gastrointestinal tract, with or without precursor symptoms. More serious consequences of these complications may occur in elderly patients. In those rare cases when these complications develop in patients receiving Voltaren, the drug should be discontinued. With the first use of Voltaren, as well as other NSAIDs, in rare cases allergic reactions may develop, including anaphylactic and anaphylactoid reactions. Voltaren, due to its pharmacodynamic properties, it can mask manifestations of infectious diseases. Voltaren, like other NSAIDs, can temporarily inhibit platelet aggregation. Therefore, in patients with impaired hemostasis, careful monitoring of relevant laboratory parameters is necessary. With prolonged use of Voltaren, like other NSAIDs, systematic monitoring of the peripheral blood pattern is shown. Effect on ability to drive vehicles and control mechanisms: Patients who develop Dizziness while using Voltaren. or other disorders of the central nervous system, including visual impairment, should not drive a car or operate mechanisms during the period of use of the drug.