Drug used in treating for relief of signs and symptoms of osteoarthritis, of rheumatoid arthritis. For acute or long-term use in the relief of signs and symptoms of ankylosing spondylitis.
Mode of action:
The drug has anti-inflammatory, analgesic and antipyretic effect. Drug belongs to the group of non-steroidal anti-inflammatory drugs, cyclooxygenase inhibitors. Diclofenac (active drug substance ) equally inhibits enzymes tsikloosginenazu -1 and cyclooxygenase -2. The drug leads to disruption of the metabolism of arachidonic acid and a decrease in the synthesis of prostaglandins. Reducing the amount of prostaglandins in the inflammation causes the analgesic effect of the drug, and the reduction of prostaglandins in the hypothalamus - antipyretic effect.
Diclofenac when used for the treatment of primary dysmenorrhea is not only eliminates pain, but also significantly reduces blood loss.
After taking the drug in the form of coated tablets of diclofenac is completely absorbed into the systemic circulation, but the effect does not occur immediately, as enteric-coated tablets. Maximum plasma concentration is achieved within 2 hours after ingestion.
After receiving the drug in the form of sustained release tablets ( Voltaren retard ) of the active substance release is slower (compared to conventional tablets ) and the maximum concentration is achieved within 4 hours after administration. Therapeutically relevant concentrations of diclofenac in plasma after a single use Voltaren retard tablet form is maintained for 24 hours.
In applying the drug in the form of suppositories, rectal absorption of the drug starts substantially faster, however, the absorption rate is less ( as compared to tablets ). The maximum concentration of active substance in plasma is achieved within 1 hour after a single administration of a suppository containing 50 mg of diclofenac.
With repeated applications of the drug Voltaren (regardless of the issue) pharmacokinetic parameters are not changed, and subject to the instructions specified intervals between applications cumulation of diclofenac was observed.
Diclofenac has a high degree of binding to plasma proteins (99% ). Most of diclofenac, about 99 % is bound to albumin. Maximum concentration in synovial fluid than in blood plasma, and maintained for 12 hours. However, the transition to the synovial fluid diclofenac slower and the maximum concentration reached in 2-4 hours after treatment.
Metabolized in the liver by the reactions of methoxylated and glucuronidation. Most of the inactive metabolites diclofenac and those which exhibit pharmacological activity, less effective than diclofenac. The half-life is 2-3 hours. 60 % of diclofenac and its metabolites are excreted in the urine. At the same time constant of diclofenac revealed no more than 2 %. The drug is also displayed through the bile in the faeces. Age and comorbidities, including liver problems or kidney problems do not affect the absorption, metabolism and excretion of the drug Voltaren.
Indications for use:
- Ankylosing spondylitis;
- Rheumatoid arthritis, including juvenile ( used only Voltaren tablets, enteric coated at 25mg, rectal suppositories Voltaren 25mg );
- Back pain;
- Extra-articular soft-tissue disease and rheumatic;
- Gout ( for Voltaren tablets, enteric-coated );
- Pain and swelling and inflammation of soft tissues and joints, resulting from trauma;
- Primary dysmenorrhea and other gynecological diseases accompanied by inflammation and / or pain;
- Migraines (for drug Voltaren rectal suppository form ).
How to use:
The drug is taken by a doctor, who picks up the dose for each patient depending on the severity of the disease.
Tablets, enteric coated:
The drug is taken with or without food, a tablet is swallowed, without chewing, washing it down with plenty of water. It is not recommended to grind or divide the tablet before taking. The initial dose for adults is usually 150 mg (3 tablets Voltaren 50mg ) / day. In cases where long term treatment is necessary or average pain intensity 75-100mg/sutki usually sufficient. The desired daily dose is usually divided into several doses. Patients who are concerned about pain at night and morning stiffness, are used in addition to the drug Voltaren tablets in the form of suppositories once at night. However, it is necessary to adjust the dose of diclofenac obtained in the form of tablets, the total dose should not exceed 150mg/sutki. During menstruation, accompanied by pain, is used by 50 - 150mg per day, depending on the intensity of pain.
Children from 6 to 15 years prescribed the drug only in the form of tablets, enteric-coated, on 25mg. The calculation of doses produced in accordance with the age and weight of the child. Typically, from 0.5 to designate 2mg/kg body weight per day. The resulting dose is divided into several stages.
The drug is taken after meals. Pills do not chew and do not divide, it is recommended to swallow tablets whole with a required amount of water. The tablets are not indicated for children under 16. The dose is usually 100 mg per day, which allows you to take retard tablets once a day. Recommended to take the tablets in the evening.
Voltaren solution for injection is intended for intramuscular use. It is not recommended to use an injection of more than 2 consecutive days. If necessary, the injection may be combined with other forms of pharmaceutical drug Voltaren, but it does not exceed the recommended daily dose - 150 mg. The drug is injected deep into a muscle in the upper outer buttock square. Typically prescribed 75 mg (1 ampoule ) 1 times a day. In the case of strongly expressed pain syndrome can be assigned to two injections with an interval of a few hours, then make a second injection in the opposite buttock.
Used in adults the initial dose of 100 - 150mg. The daily dose is usually divided into 2-3 doses. In combination with other dosage forms of the drug Voltaren suppositories are usually given at night, you need to watch what would the daily dose of diclofenac did not exceed 150 mg.
In painful menstruation dose is from 50 to 150 mg depending on the severity of pain and the individual characteristics of the patient.
A preparation in the form of suppositories for rectal administered pain relief in migraine attacks. For this drug, patients are advised Voltaren suppositories in a daily dose of 100 mg, in case of need to increase the dose. The daily dose of diclofenac should not exceed 150 mg.
The gastro -intestinal tract: stomach pain, nausea, vomiting, stool disorders, flatulence, loss of appetite, gastrointestinal bleeding, ulceration of the stomach and duodenum. Inflammatory diseases of the mouth and throat ( stomatitis, gingivitis, glossitis ). Elevated liver enzymes, hepatitis, including accompanied by jaundice.
For the cardiovascular system: hypertension, tachycardia, chest pain, deterioration of patients with congestive heart failure.
On the part of the central and peripheral nervous systems: dizziness, headache, disorientation in space, paresthesia, impaired memory, impaired sleep and wakefulness, fatigue, irritability, mood swings. Depression, anxiety, nightmares, tremor of the limbs. Very rarely may develop aseptic meningitis.
From the senses: visual impairment, hearing loss, tinnitus, taste alteration.
For the skin: hives, skin rash, eczema, Lyell's syndrome, erythema multiforme, Stevens-Johnson syndrome, erythroderma, photosensitivity, hair loss.
For part of the blood: anemia, leukopenia, thrombocytopenia, agranulocytosis.
Genitourinary: edema, hematuria, proteinuria, interstitial nephritis, papillary necrosis, nephrotic syndrome. Very rarely may develop acute renal failure. Other side effects may rarely develop bronchospasm, anaphylactic reactions up to anaphylactic shock. In addition, in some cases, there pneumonitis and vasculitis.
Using the drug Voltaren in the form of rectal suppositories may be local reactions, including hemorrhoids and irritation of the mucous membrane of the rectum.
Taking the drug does not affect the ability to drive and potentially dangerous machinery. The appearance of side effects, one should inform your doctor.
- Hypersensitivity to the drug, as well as intolerance of dipyrone (reaction to receiving dipyrone as bronchospasm, rhinitis or urticaria );
- Ulceration of the stomach and / or duodenal ulcers, gastritis, erosive including colitis, Crohn's disease;
- Malfunction of the blood, of unknown etiology;
- The third trimester of pregnancy;
- Children under 6 years of age ( for the drug in tablet form retard to 14 years).;
severe liver, kidney, cardiovascular system;
- For the drug in the form of rectal suppositories - hemorrhoids, rectal bleeding, proctitis.
Be wary appoint:
patients who in the past suffered from a stomach ulcer and duodenal ulcer;
elderly patients, especially with low birth weight;
patients with gastrointestinal bleeding in history;
to patients with hemostatic disorders.
With long-term use of the drug Voltaren is necessary to control the function of the liver, kidney and peripheral blood picture.
The drug is contraindicated in the third trimester of pregnancy, as it is believed that it may cause uterine inertia and impaired blood flow. In the first and second trimesters of pregnancy, the drug is prescribed only for health reasons, and the lowest effective dose. Before the appointment of the drug must weigh the potential benefit to the mother and the possible risks to the fetus.
If necessary, use during lactation should decide on the termination of breastfeeding, because diclofenac is excreted in breast milk and may cause unwanted reactions in the child.
Interactions with other drugs:
Simultaneous application of the drug to atsetamfitaminom can lead to the development of renal dysfunction.
Ethyl alcohol, GCS, corticotropin and potassium supplements increase the risk of side effects of diclofenac on the part of the digestive system.
Means reducing platelet aggregation (anticoagulants direct and indirect ) may increase the risk of intestinal bleeding.
Diclofenac reduces the level of glucose in the blood, while the use of oral antidiabetic agents and insulin. In the case of co-administration of a correction dose of drugs that lower blood sugar.
The drug Voltaren can reduce the effectiveness of diuretics and antihypertensive agents. With the simultaneous use of potassium-sparing diuretics increases the risk of hyperkalemia. In addition, the risk of side effects from the urinary system. Simultaneous treatment with a derivative of salicylic acid and other nonsteroidal anti-inflammatory drugs increase the risk of side effects of diclofenac. Colchicine promotes the appearance of side effects from the gastrointestinal tract. Simultaneous with the appointment of cardiac glycosides, in particular with digitalis drugs, increases the risk of developing digitalisovoy intoxication. Diclofenac increases cyclosporine nephrotoxicity. Increasing the concentration of lithium in the blood while taking diclofenac and lithium preparations. Antacids increase the amount of diclofenac in plasma.
The drug does not accumulate in the body, so a chronic overdose is unlikely. In acute overdose marked nausea, vomiting (sometimes with blood, vomit ), epigastric pain, convulsions, coma.
In case of overdose shown gastric lavage, enterosorbents.
Symptomatic therapy. To reduce the severity of symptoms of overdose of gastro -intestinal tract is prescribed alkalizing agents. In some cases, shows the introduction of corticosteroids. With the development of renal failure is shown hemodialysis.
After an overdose the patient should be monitored for several days.
Injection solution for intramuscular injection in 3 ml vial 5 vials per carton.
Tablets, enteric coated, with 25 or 50 mg of the active substance of 10. a blister, 2 or 3 blisters in a carton.
Retard tablets, film-coated, 100 mg of the active substance of 10. a blister, 3 blisters in a carton.
Rectal suppositories of 25 mg or 50 mg of the active substance to 5 pieces per blister, 2 blisters in a carton.
Rectal suppositories 100 mg of active substance 5 pieces in a blister, 1 blister in a cardboard box.
The drug should be stored in a dry place at room temperature.
Shelf life - 2 years.
Diclofenac, Naklofen, Orthophene, Dikloran.
1 tablet Voltaren enteric coated, comprising:
Diclofenac Sodium - 25 or 50 mg;
1 tablet Voltaren retard film coating contains:
Diclofenac sodium - 100 mg;
1 Voltaren rectal suppository contains:
Diclofenac Sodium - 25, 50 or 100 mg;
1 ml of a solution for intramuscular injection Voltaren comprises:
Diclofenac sodium - 25 mg;