Pharmacological properties Voltaren SR:
diclofenac sodium – material non-steroidal structure, has a marked anti-inflammatory, analgesic and antipyretic effect. The main mechanism of action is inhibition of the biosynthesis of prostaglandins. Prostaglandins play an important role in the genesis of inflammation, pain and fever.
In rheumatic diseases and anti-inflammatory analgesic properties of diclofenac provide clinical effects, characterized by a significant decrease in the severity of symptoms and complaints such as pain at rest and in motion, morning stiffness and swelling of joints, as well as improve function.
In vitro diclofenac sodium in concentrations equivalent to those achieved in patients, does not suppress the biosynthesis of proteoglycans of cartilage.
Post-traumatic and postoperative inflammatory phenomena quickly relieves pain diclofenac (both spontaneously and arising from the movement), reduces inflammation, edema and swelling of the wound.
The results of clinical studies have shown a significant analgesic effect of the drug in moderate and severely of pain non-rheumatic origin.
Diclofenac sodium is able to eliminate pain and reduce the severity of blood loss during primary dysmenorrhea. In addition, has a beneficial effect on the manifestations of migraine.
Absorption. After i / m administration of 75 mg of diclofenac absorption begins immediately. The maximum concentration in blood plasma, whose mean value is about 2.5 mg / ml (8 mmol / l), is reached after about 20 minutes. Immediately after its achievement mark a rapid decrease in drug concentration in blood plasma. The number gets into the active substance is a linear function of the dose.
The value of AUC after i / m administration voltaren approximately 2 times greater than after the oral or rectal administration, as in the latter cases, about half of diclofenac is metabolised during the first passage through the liver. After repeated use of the drug pharmacokinetic parameters are not changed. Subject to the recommended intervals between doses of the drug accumulation is not observed.
Distribution. Binding to serum proteins is 99.7%, with albumin-bound 99.4% of the drug. Volume of distribution is 0,12-0,17 l / kg body weight.
Diclofenac enters the synovial fluid, where its maximum concentration is achieved in 2-4 hours later than in plasma. The half-life of synovial fluid 3-6 hours 2 hours after reaching the maximum concentration in plasma concentration of diclofenac in synovial fluid than in blood plasma, and its values are higher for 12 hours
Metabolism. Diclofenac is metabolized in part by glucuronidation unmodified molecule, but mainly by single and multiple methoxylation, resulting in the formation of several phenolic metabolites (3-hydroxy-4-hydroxy-5-hydroxy-, 4,5-dihydroxy-and 3-hydroxy- 4 metoksidiklofenaka), most of which are converted into glyukuronidnye conjugates. Two of these phenolic metabolites are biologically active, but much less than diclofenac.
Excretion. Total systemic plasma clearance of diclofenac is 263 ± 56 ml / min. Terminal half-life of 1-2 h. The half-life four metabolites, including two pharmacologically active, and also of short duration is 1-3 h. One of the metabolites, 3-hydroxy-4-methoxy-diclofenac, has a longer half-life, but this completely inactive metabolite.
About 60% of the applied dose is excreted in the urine as glucuronic conjugates of unchanged active ingredient, as well as metabolites, most of which are glucuronic conjugates. In the unchanged output of less than 1% of diclofenac. The rest of the applied dose excreted as metabolites in the bile and feces.
Patients with impaired renal function in the appointment of a conventional single doses of diclofenac accumulation was observed. In that case, if creatinine clearance is less than 10 ml / min, the calculated equilibrium concentrations of diclofenac gidroksimetabolitov about 4 times higher than in healthy subjects. Ultimately, however, metabolites are excreted in the bile.
In patients with chronic hepatitis or compensated cirrhosis rates are similar to those of the pharmacokinetics of diclofenac in patients without liver disease.
INDICATIONS Voltaren SR:
inflammatory and degenerative forms of rheumatic diseases (rheumatoid arthritis, ankylosing spondylitis, osteoarthritis, spondylitis);
pain in the spine;
extra-articular rheumatic diseases of soft tissues;
an acute attack of gout;
Post-traumatic and postoperative pain, accompanied by inflammation and edema;
migraines heavy flow;
renal and biliary colic.
Application Voltaren SR:
used in adults, type in / m by deep injection into the buttock area. You should not use Voltaren injections over 2 days. If necessary, treatment can be continued with Voltaren tablets or rectal suppositories.
In carrying out the i / m injection in order to avoid damage to nerves or other tissues at the injection site, we recommend that you follow these guidelines.
The drug should be administered deeply into the / m in the upper outer quadrant of the gluteal area. The dose is usually 75 mg (contents of 1 mg), 1 per day. In severe cases (such as colic) as an exception can be made two injections of 75 mg with an interval of several hours (the second injection should be carried out in the opposite gluteal region). Alternatively, a single injection of the drug per day (75 mg) can be combined with taking other medicines voltaren (tablet, rectal suppository), the maximum daily dose is 150 mg.
CONTRAINDICATIONS Voltaren SR:
stomach ulcer or intestine;
hypersensitivity to diclofenac and other ingredients of the drug;
patients who receive in response to aspirin or other NSAIDs having bouts of asthma, urticaria or acute rhinitis.
Pp Injection is not indicated for children and adolescents under the age of 18 years, during pregnancy.
SIDE EFFECTS Voltaren SR:
When assessing frequency of occurrence of various adverse reactions used the following grades: common -> 10%, sometimes -> 1-10%, rare -> 0.001-1%, in some cases -
Gastrointestinal disorders: sometimes – epigastric pain, nausea, vomiting, diarrhea, abdominal cramps, indigestion, bloating, anorexia, rarely – gastrointestinal bleeding (hematemesis, melena, bloody diarrhea), stomach or intestines accompanied or unaccompanied bleeding or perforation, in some cases – aphthous stomatitis, glossitis, changes in the esophagus, the occurrence of diafragmopodobnyh strictures in the intestines, disorders of the lower intestine, such as non-specific haemorrhagic colitis, exacerbation of ulcerative colitis or Crohn’s disease, constipation , pancreatitis.
Central nervous system: sometimes – headache, dizziness, and rarely – drowsiness and in some cases – sensory disturbances, including paresthesia, memory disturbances, disorientation, insomnia, irritability, convulsions, depression, anxiety, nightmares, tremor, psychotic reactions, aseptic meningitis.
From the senses: in some cases – visual disturbances (blurred vision, diplopia), impaired hearing, tinnitus, taste disturbances.
Dermatological reactions: sometimes – skin rash, rarely – urticaria, and in some cases – in the form of bubbles rashes, eczema, erythema multiforme, Stevens – Johnson syndrome, Lyell (acute toxic epidermolysis), erythroderma (exfoliative dermatitis), loss of hair, photosensitivity reactions ; purpura, including allergic asthma.
The kidneys: rare – swelling and in some cases – acute renal failure, changes in urine sediment (hematuria and proteinuria), interstitial nephritis, nephrotic syndrome, papillary necrosis.
Of the liver: sometimes – increase in serum aminotransferases, rarely – hepatitis, accompanied or not accompanied by jaundice, and in some cases – fulminant hepatitis.
From the hemopoietic system: in some cases – thrombocytopenia, leukopenia, hemolytic anemia, aplastic anemia, agranulocytosis.
Hypersensitivity reactions: seldom – hypersensitivity reactions such as asthma, systemic anaphylactic / anaphylactoid reactions including hypotension and in some cases – vasculitis, pneumonitis.
Cardio-vascular system: in some cases – palpitations, chest pain, hypertension, congestive heart failure.
Other: sometimes – site reactions / m injection in the form of local pain and seals, in some cases – local abscesses, and necrosis at the site of the i / m injection.
Precautions Voltaren SR:
During treatment Voltaren at any time it may be gastro-intestinal bleeding or ulcers develop gastrointestinal perforation complicating sometimes, and do not always have the symptoms – the forerunners of these complications or the presence of anamnestic information about canker. More serious consequences of these complications may occur in elderly patients. In those rare cases where patients receiving Voltaren, develop these complications, the drug should be discontinued.
The patient has not previously in receipt of Voltaren in the period of drug treatment, as well as during therapy, other NSAIDs, may in rare cases develop allergic reactions, including anaphylactic and anaphylactoid reactions.
Voltaren due to its pharmacodynamic properties can mask the complaints and symptoms of infectious and inflammatory diseases.
May develop hypersensitivity to sodium metabisulfite, a part of the injectable Valium.
During the application of Voltaren requires careful medical supervision of patients with complaints suggestive of gastrointestinal disease or who have information about medical history of ulcerative lesions of the stomach or intestine, patients with ulcerative colitis or Crohn’s disease and patients with impaired liver function.
During the application of Voltaren in the same way as other NSAIDs, may increase the level of one or more liver enzymes. Therefore, prolonged therapy Voltarenom as a precautionary measure shows regular liver function tests. If violations of the functional parameters of liver preserved or enhanced, there are complaints or develop symptoms suggestive of liver disease, as well as in the case, if there are other side effects (eg eosinophilia, rash, etc.), Voltaren should be discontinued. We must bear in mind that hepatitis in patients receiving Voltaren may occur without prodromal phenomena.
The drug can provoke porphyria attacks, so you must be careful in appointing Voltaren in patients with hepatic porphyria.
Because prostaglandins play an important role in maintaining renal blood flow, particular caution is required when treating patients with disorders of the heart or kidney disease, elderly patients, patients receiving diuretics, and patients who have a significant decrease in the volume of circulating blood plasma of any etiology, such as before and after massive surgery. In these cases, while using Voltaren is recommended as a precaution regular monitoring of renal function. Discontinuation of the drug usually leads to recovery of renal function to baseline. With prolonged use Voltaren, like other NSAIDs, shows a systematic monitoring of peripheral blood.
Voltaren, like other NSAIDs, may temporarily inhibit platelet aggregation. Therefore, in patients with disorders of hemostasis requires careful control of the laboratory parameters.
Given the general health status, caution is needed when using Voltaren in patients of advanced age. This is particularly relevant in frail or have underweight elderly patients are advised to prescribe a drug in the lowest effective dose.
Particular caution should be exercised when i / m administration Voltaren in patients with asthma (due to risk of increased severity of symptoms), and patients with allergic rhinitis (including seasonal) and polyps of the nasal mucosa.
Use during pregnancy and lactation. During pregnancy is contraindicated. If necessary, use drugs nursing mother should decide on the termination of breastfeeding.
Effects on ability to drive and use machines. Patients experiencing while using Voltaren dizziness or other discomfort from the central nervous system, including visual impairment, you should not drive vehicles or operate machinery
INTERACTION Voltaren SR:
Lithium, digoxin. Voltaren may increase the concentration of lithium and digoxin in the blood plasma.
Diuretics. Voltaren as well as other NSAIDs, may reduce the severity of diuretic action. Concomitant use of potassium-sparing diuretics may cause the increase in serum potassium (in the case of such a combination of drugs, this figure should be frequently monitored).
NSAIDs. Combined systemic administration of NSAIDs may increase the incidence of adverse events.
Anticoagulants. Although clinical studies have not been found to influence voltaren action of anticoagulants, there are anecdotal reports of an increased risk of bleeding in patients taking both these medicines and Voltaren. Therefore, in case of such a combination recommended careful and regular monitoring of patients.
Antidiabetic drugs. Clinical studies have shown that it is possible the simultaneous use of Voltaren and antidiabetic drugs, and the effectiveness of the latter does not change. However, there are occasional reports of development in cases such as hypoglycemia, hyperglycemia, and, necessitating changes in sugar-reducing drugs dose while using Voltaren.
Methotrexate. Caution must be exercised in the appointment of NSAIDs for less than 24 hours before or after taking methotrexate with the possibility of increasing concentrations of methotrexate in blood and increase its toxicity.
Cyclosporine. Effect of NSAIDs on prostaglandin synthesis in the kidneys may increase the nephrotoxicity of cyclosporine.
Antibacterials – quinolone derivatives. There are anecdotal reports of seizures in patients treated with both NSAIDs and quinolone derivatives.
Pharmaceutical incompatibility. As a rule, should not be confused pp Voltaren, contained in ampoules, with a p-ramie other drugs for injection.
OVERDOSE Voltaren SR:
typical clinical picture, typical of an overdose of Voltaren, no.
Treatment of acute poisoning with NSAIDs (supportive and symptomatic therapy) is shown in complications such as hypotension, renal failure, convulsions, disorders of the gastrointestinal and respiratory depression. It’s unlikely that forced diuresis, hemodialysis, or hemoperfusion would be useful for removing NSAIDs as active ingredients of these drugs is largely bound to plasma proteins and subjected to intensive metabolism.
