VOLTAREN Z
Active substance

diclofenac (diclofenac (in the form of sodium salt))
Pharmacological group

NPVS
Form of production, composition and packaging

Tablets, coated enteric-soluble coating shell yellow, round, convexoconvex, with bevelled edges, marked with "CG" on one side and "BZ" on the other.
1 tab.
diclofenac (in the form of sodium salt) 25 mg
Additional ingredients: colloidal silicon dioxide anhydrous, microcrystalline cellulose, lactose, magnesium stearate, maize starch, povidone K30, sodium carboxymethyl, hypromellose, glyceryl polyethylene glycol oksistearat, yellow iron oxide, talc, titanium dioxide, copolymer of polyacrilic / metacrylic acid and esters, macrogol 8000, silicon defoamer emulsion SE2.
10 pcs. - Blisters (3) - packs cardboard.
Tablets, coated enteric-soluble coating shell light-brown, round, convexoconvex, with bevelled edges, marked with "CG" on one side and "GT" on the other.
1 tab.
diclofenac (in the form of sodium salt) 500 mg
Additional ingredients: colloidal silicon dioxide anhydrous, microcrystalline cellulose, lactose, magnesium stearate, maize starch, povidone K30, sodium carboxymethyl, hypromellose, glyceryl polyethylene glycol oksistearat, yellow iron oxide, talc, titanium dioxide, copolymer of polyacrilic / metacrylic acid and esters, macrogol 8000, silicon defoamer emulsion SE2, red iron oxide.
10 pcs. - Blisters (2) - packs cardboard.
Tablets prolonged action, film-coated 1 tab.
diclofenac sodium 100 mg
Additional ingredients: colloidal silicon dioxide anhydrous, cetyl alcohol, magnesium stearate, povidone K30, sucrose, hypromellose, iron oxide red, polysorbate 80, talc, titanium dioxide, macrogol 8000, sucrose crystal, black ink 8015 (to mark).
10 pcs. - Blisters (1) - packs cardboard.
10 pcs. - Blisters (3) - packs cardboard.
Suppositories rectal a supp.
diclofenac (in the form of sodium salt) 25 mg
- "- 50 mg
Auxiliary substances: solid fats.
5 pcs. - Blisters (2) - packs cardboard.
Suppositories rectal a supp.
diclofenac (in the form of sodium salt) 100 mg
Auxiliary substances: solid fats.
5 pcs. - Blisters (1) - packs cardboard.
The solution for the on / m introduction colorless or light yellow.
1 ml of 1 amp.
diclofenac (in the form of sodium salt) 25 mg, 75 mg
Excipients: mannitol, sodium disulfide, benzyl alcohol, propylene glycol, water h /, and sodium hydroxide.
3 ml ampoule (5) - packs cardboard.
Clinical-pharmacological group

NPVS
Registration No.

tab., cover. enteric-soluble coating shell, 50 mg: 20 pcs. - P # 015266/01, 16.06.06
ATC code

M01AB05
Description of the medicinal product VOLTAREN z is based on officially approved the instructions on the application of the drug VOLTAREN z for specialists and approved by the company-producer for the 2010 edition
Pharmacological action

NPVS. Voltaren z contains diclofenac sodium, a substance non-steroidal structure, providing expressed anti-inflammatory, analgesic and antipyretic action.
The main mechanism of action of diclofenac, established in the conditions of the experiment, is considered to be the inhibition of the biosynthesis of prostaglandins. Prostaglandins play an important role in the genesis of the inflammation, pain and fever.
In vitro diclofenac sodium in concentrations equivalent to that achieved in the treatment of patients, does not suppress the synthesis of proteoglycans of the cartilaginous tissue.
In rheumatic diseases inflammatory and analgesic properties voltaren z provide the clinical effect, characterized by a significant decrease in the severity of such manifestations of the disease as pain at rest and with movement, morning stiffness and swelling of the joints, as well as improved functional status .
In post-traumatic and postoperative inflammatory events Voltaren z quickly eliminates the pain (emerging both in rest and with movement, reduces inflammatory swelling and edema of postoperative wounds.
In the application of Voltaren z tablets and suppositories marked by pronounced analgesic effect of the drug at a moderate and severe pain non-rheumatic of origin. In applying the drug in the form of a solution for the on / m introduction of the product is through 1-15 min. It was also established that Voltaren z able to reduce the pain and reduce blood loss in the primary dismenoree.
In addition, Voltaren z facilitates migraine attacks (when used in suppositories).
The Pharmacokinetics Of

Absorption
After the reception inside tablets, coated enteric-soluble coating shell, diclofenac completely absorbed from the intestine. Although the absorption occurs rapidly, its onset can be delayed because of the availability of the pill enteric-soluble coating shell. After a single dose of 50 mg drug Cmax noted in an average of two hours and is 1.5 mcg / ml (5 mmol / l). The degree of absorption is in direct dependence on the dose.
In case of reception of tablets voltaren z during or after a meal passing it through the stomach slows (compared with the reception of prandial), but the number of gets into diclofenac does not change.
Since about half of the dose of diclofenac is metabolized in the time of the first passage "through the liver (effect of" first pass "), of the AUC in the case of reception of Voltaren z oral or rectal use almost in 2 times is less, than in the case of parenteral introduction of the preparation in the equivalent dose.
After repeated receptions of the product indicators pharmacokinetics do not change. Subject to the recommended dosing regimen of the drug cumulation is not observed.
Judging by the number of output with urine unchanged diclofenac and his gidrauxilirovannah metabolites after taking a tablet prolonged action covered liner out of it is released and absorbed the same amount of active substances, as from the regular tablets, coated enteric-soluble coating shell. However, the systemic bioavailability of diclofenac, the release of tablets prolonged action on average 82% of the value of the same indicator after the reception of tablets, film-coated, in the same dose. This was probably caused by another manifestation of the effect of "first pass" through the liver for medicinal forms with a slow release of the active substance. Because of the active substance is released from the tablets prolonged action slower, the Cmax diclofenac in blood plasma is less, than in case of reception of tablets, coated enteric-soluble coating shell.
After reception of tablets prolonged action-100 mg Cmax diclofenac in the plasma is achieved in an average of four hours, the average value of it is 0.5 g / ml (1.6 mmol / l). Admission food has no clinically significant effect on the absorption of the active substance from the tablets prolonged action and the systemic bioavailability.
Within 24 hours of observation after reception of tablets prolonged action-100 mg diclaufenaka concentration in the plasma is an average of 13 ng / ml (40 nmol / l). The degree of absorption is in direct dependence on the dose of the drug.
As the "first pass" through the liver metabolized about half of the number of diclofenac, the AUC after administration of tablets prolonged action approximately in 2 times is less, than in the case of parenteral introduction of equivalent dose of the drug.
After repeated receptions of the drug pharmacokinetic parameters are not changed. Subject to the recommended dosing regimen of the drug cumulation is not observed. Basal concentrations of diclofenac, which is defined in the morning before receiving the next dose, is about 22 ng / ml (70 nmol / l) during treatment Voltarenom z in the form of tablets prolonged action at a dose of 100 mg 1 time / day .
The absorption of diclofenac suppositories rectal starts quickly, although its rate of absorption is less in comparison with the similar indicator of the ingestion of tablets, coated enteric-soluble coating shell. After the application of rectal suppositories containing 50 mg of active substance, Cmax diclofenac in the plasma is achieved on average within an hour, but the Cmax, calculated per unit of the applied dose is approximately two thirds of the respective indicator registered after the reception inside enteric-soluble coating tablets. The degree of absorption is in direct dependence on the dose of the drug.
With the re-introductions of the product in the form of suppositories pharmacokinetic parameters are not changed. Subject to the recommended dosing regimen of the drug cumulation is not observed.
After the / m of diclofenac in a dose of 75 mg its absorption begins immediately. Cmax diclofenac in plasma is reached in 20 minutes and is 2.5 g / ml (8 mmol / l). The degree of absorption is in direct dependence on the dose. AUC after the / m of approximately in 2 times more, than after its oral or rectal use, because in the latter cases, about half of the number of diclofenac metabolism in "first pass" through the liver. On subsequent introductions of the drug pharmacokinetic parameters are not changed. Subject to the recommended interval between wvedeniami preparation of cumulation is not observed.
The Distribution Of
Binding to serum proteins of the blood - 99.7%, predominantly to albumin (99.4%). The Apparent distribution volume is 0.12-0.17 l / kg.
Diclofenac enters the synovial fluid, where it Cmax is achieved 2 to 4 hours later than in the blood plasma. Seemingly T1 / 2 from the synovial fluid is 3-6 hours. After 2 h after reaching a Cmax in plasma concentration of diclofenac in synovial fluid higher than in plasma and its values ​​remain higher for a period of time up to 12 hours.
Metabolism
Metabolism of diclofenac is carried out partly by glukuronization unchanged molecules, but, mainly, by means of single and multiple gidrauxilirovania and methoxylation, which leads to the formation of several phenolic metabolites (3'-hydroxy-, 4'-hydroxy-, 5 ' -hydroxy-, 4 ',5-dihydroxy-and 3'-hydroxy-4'-metoksidiklofenaka), most of which becomes