Producer: HFZ CJSC NPTs Borshchagovsky Ukraina
Code of automatic telephone exchange: M02AA65
Release form: Soft dosage forms. Gel.
General characteristics. Structure:
Main physical and chemical properties: gel of white color, a homogeneous consistence, with a specific smell;+-structure: 1 g of gel contains 30 mg of diclofenac of sodium and 5 mg of menthol; excipients: alcohol of ethyl 96%, propylene glycol, glycerin, карбопол, ammonia solution of 15%, formaldehyde solution, the water purified.
Pharmacodynamics. Diklofen-gel at topical administration renders expressed antiinflammatory, analgeziruyushchy, antiedematous and antiagregantny effects that is connected with oppression of biosynthesis of prostaglandins, kinin and other mediators of an inflammation. Drug reduces permeability of a vascular wall of capillaries, stabilizes membranes of lysosomes, reduces temperature in the inflammation center.
The menthol which is a part of drug has bystry analgetic effect due to the cooling effect, strengthening analgetic effect of diclofenac.
Diklofen-gel promotes reduction of hypostasis of joints and circumarticular fabrics, reduces expressiveness of a rest pain and at the movement, reduces morning constraint, increases the volume of movements in joints, their functional and motive capacity. Reducing aggregation ability of thrombocytes, drug improves local microcirculation.
Pharmacokinetics. The amount of the diclofenac getting through skin is proportional to time of contact of Diklofen-gelya and the area of skin on which it is applied, and also depends on a dose of drug and extent of hydration of skin. After drawing on the surface of skin of Diklofen-gelya absorption of diclofenac makes about 6%. The occlusive bandage can raise a diclofenac resorption several times. After topical administration diclofenac is defined in a blood plasma, a synovial membrane and synovial fluid of joints. Diclofenac contacts proteins of a blood plasma for 99%. Metabolism of diclofenac happens mainly by a hydroxylation to formation of several derivatives, two of which pharmacological are active, but in much smaller degree, than diclofenac. Diclofenac and its metabolites are removed preferential with urine in the form of glucuronides.
Patients with diseases of kidneys have cumulation of diclofenac and its metabolites it is noted. At patients with chronic hepatitis or the compensated cirrhosis indicators of pharmacokinetics and metabolism of diclofenac do not change.
Indications to use:
• Acute and chronic, inflammatory and degenerative diseases of joints and backbone: rhematoid, gouty, infectious and psoriasis arthritises, polyarthritis, an osteoarthritis, the spondylarthritis ankylosing a spondylitis, arthrosis, an osteoarthrosis, osteochondrosis, radiculitis, a lumbago, a sciatica;
• rheumatic diseases of soft tissues (including a tendovaginitis, a bursitis, a periarthritis, periartropatiya);
• posttraumatic inflammation of soft tissues, musculoskeletal system injuries (sinews, ligaments, muscles and joints): bruises, stretchings, dislocations, hypostases.
Route of administration and doses:
Drug is used outwardly. 1 g of Diklofen-gelya (a strip of gel 2,5 - 3 cm long) apply with a uniform thin layer on skin and slightly rub within 1 – 2 minutes. After putting drug it is necessary to wash up hands (except those cases when application is carried out on area of hands). The procedure is repeated by 2 – 4 times a day. The average daily dose for adults and children is more senior than 15 years makes 4 – 5 g of gel that corresponds to 120 - 150 mg of diclofenac of sodium. Duration of treatment of Diklofen-gelem makes 10 – 14 days. At simultaneous use of Diklofen-gelya with diclofenac tablets the daily dose of the last should not exceed 50 mg.
Features of use:
Drug needs to be applied only on the unimpaired sites of skin. Not to allow hit of drug in eyes and on other mucous membranes, and in case of hit it is necessary to wash out them enough flowing water. It is not necessary to apply gel under air-tight (occlusal) bandages. At prolonged use of Diklofen-gelya, use of the doses exceeding recommended, putting drug on extensive sites of skin, simultaneous use of other drugs of diclofenac emergence of the side effects characteristic of diclofenac is possible. At long use periodic control of function of a liver, composition of peripheral blood, a calla on the occult blood is necessary.
Use during pregnancy or feeding by a breast.
Use of drug during pregnancy is contraindicated. In need of drug use by the women nursing feeding is recommended to be stopped.
Ability to influence speed of response at control of motor transport or other mechanisms.
Diklofen-gel does not exert impact on speed of response at control of motor transport or other mechanisms.
Efficiency and safety of use of drug for children aged up to 15 years were not studied.
In this dosage form of Diklofen-gel it is well transferred. However it is impossible to exclude emergence of local reactions: seldom – allergic or contact dermatitis with papulation, bulls or skin desquamation; isolated cases of a photosensitization, formation of infiltrate, abscess, a necrosis of fatty tissue are possible.
Possibility of system side effects after topical administration of Diklofen-gelya is improbable, however, considering a possibility of prolonged use, uses of the doses exceeding recommended, putting drug on extensive sites of skin, simultaneous use of other drugs of diclofenac can be observed such side reactions:
from a GIT: heartburn, appetite loss, nausea, vomiting, a lock or diarrhea, pain in epigastric area, enterospasms, a meteorism; seldom – ulcerogenic action with or without bleeding or perforation; in isolated cases development of nonspecific hemorrhagic colitis, aphthous stomatitis, a glossitis, damages of a gullet, pancreatitis, an exacerbation of hemorrhoids is possible;
from kidneys: hypostases, in isolated cases – an acute renal failure, a hamaturia, a proteinuria, intersticial nephrite, a nephrotic syndrome, a necrotizing papillitis;
from a liver: increase in activity of serumal aminotransferases is possible;
from TsNS: dizziness, a headache, is extremely rare – increased fatigue, in isolated cases – paresthesia, memory disturbances, a disorientation, sleeplessness, irritability, concern, a depression, dreadful dreams, a tremor, psychotic reactions, spasms, aseptic meningitis, vision disorders (diplopia), a hearing disorder (sonitus), taste disturbances;
allergic reactions: in isolated cases – generalized skin rash, violent rashes, eczema, a polymorphic erythema, a purpura, a small tortoiseshell, an erythrosis, Stephens's syndrome – Johnson, a Lyell's disease (a toxic epidermal necrolysis), a bronchospasm;
changes of laboratory indicators: anemia, a leukopenia, thrombocytopenia, an agranulocytosis, decrease or increase in level of glucose and potassium in blood;
from cardiovascular system: tachycardia, pain in a breast, increase in arterial pressure, the phenomenon of heart failure.
Interaction with other medicines:
When using Diklofen-gelya the possibility of interaction with other medicines is minimum. However, considering a possibility of prolonged use, uses of the doses exceeding recommended, putting drug on extensive sites of skin, simultaneous use of other drugs of diclofenac it is impossible to exclude a possibility of such interactions:
• with anticoagulants, antitrombotichesky means the risk of development of bleedings increases;
• Diklofen-gel can reduce efficiency of anti-hypertensive therapy;
• at use with other NPVP, glucocorticoids, alcohol ulcerogenic action amplifies;
• use of Diklofen-gelya with digoxin, Phenytoinum, drugs of lithium, a hinolonama can lead to increase in concentration of these medicines in a blood plasma;
• Diklofen-gel can reduce efficiency of diuretic drugs, at appointment with kaliysberegayushchy diuretics development of a hyperpotassemia is possible;
• use of Diklofen-gelya during 24 h to or after reception of a methotrexate can lead to increase in concentration of a methotrexate in a blood plasma and, respectively, to manifestation of its toxic effects;
• at a combination to peroral glucose-lowering drugs development both hypo - and a hyperglycemia is possible;
• Diklofen-gel can increase nephrotoxicity of cyclosporine.
• Hypersensitivity to diclofenac, menthol or other components of drug;
• GIT erosive cankers, and also the states which are followed by bleeding from bodies of a GIT (including hemorrhoidal bleeding);
• disturbance of a hemopoiesis of various etiology;
• the bronchial asthma or allergic reactions in the anamnesis caused by reception of acetylsalicylic acid or other non-steroidal anti-inflammatory drugs;
• pregnancy period.
About cases of overdose it was not reported. However, considering a possibility of prolonged use, uses of the doses exceeding recommended, putting drug on extensive sites of skin, simultaneous use of other drugs of diclofenac can be observed the specified side reactions.
Treatment: to remove or wash away the remained gel from skin. If necessary to carry out symptomatic therapy. The artificial diuresis is ineffective in view of high extent of linkng of diclofenac with proteins of plasma. There is no specific antidote.
To store in protected from light and the place, unavailable to children, at a temperature from 15ºС to 25ºС.
Period of validity – 2 years.
According to the recipe
On 25 g of gel in tubas and packs.