ДИКЛОНАТ П

Active material: Diclofenac
When ATH: M01AB05
CCF: NSAIDs
When CSF: 05.01.01.03.01
Manufacturer: PLIVA HRVATSKA d.o.o. (Croatia)

Pharmaceutical form, composition and packaging

Solution for in / and the / m clear, colorless to pale yellow, со слабым запахом бензилового спирта.

Excipients: benzyl alcohol, mannitol, Sodium hydroxide, sodium metabisulfite, propylene glycol, water d / and.

3 ml – ampoule (5) – pallets (1) – packs cardboard.

Rectal Suppositories yellowish-white, формы конуса, со слабым запахом жира; на продольном срезе допускается наличие воздушного стержня или воронкообразного углубления.

Excipients: fat solid.

5 PC. – strips (2) – packs cardboard.

Sustained-release tablets, coated Pink colour, circular shape, с однородной и гладкой поверхностью, with beveled edges; of presentations – White core.

Excipients: sucrose, cetyl alcohol, colloidal silicon dioxide, magnesium stearate, polyvidone.

The composition of the shell: hydroxypropyl, iron oxide red (E172), polysorbate, talc, Titanium dioxide, polyethylene glycol, sucrose.

10 PC. – blisters (2) – cardboard boxes.

DESCRIPTION OF ACTIVE SUBSTANCES.

Pharmacological action

NSAIDs, phenylacetic acid. Has a pronounced anti-inflammatory, mild analgesic and antipyretic effect. The mechanism of action is associated with inhibition of COX – primary enzyme metabolism of arachidonic acid, is a precursor of prostaglandins, which play a major role in the pathogenesis of inflammation, pain and fever. Analgesic effect is caused by two mechanisms: peripheral (indirectly, through inhibition of prostaglandin synthesis) and central (by inhibiting the synthesis of prostaglandins in the central and peripheral nervous system).

It inhibits the synthesis of proteoglycan in cartilage.

In rheumatic diseases reduces joint pain at rest and during movement, as well as morning stiffness and swelling of joints, increases range of motion. It reduces post-traumatic and post-operative pain, and inflammatory edema.

Inhibits platelet aggregation. Prolonged use has a desensitizing effect.

The local application in ophthalmology reduces swelling and pain in inflammatory processes of infectious etiology.

Pharmacokinetics

Once inside absorbed from the gastrointestinal tract. Food intake slows the rate of absorption, the degree of absorption is not changed. About 50% the active substance is metabolized in the “first pass” through the liver. For rectal administration, the absorption is slower. The time to reach C_max in plasma after oral administration is 2-4 h depending on the dosage form, after rectal administration – 1 no, the / m – 20 m. The concentration of active substance in plasma is a linear function of the value of the applied dose.

Not accumulates. Plasma protein binding is 99.7% (mostly to albumin). It penetrates into synovial fluid, C_max achieved at 2-4 hours later, than in plasma.

In largely metabolized to form several metabolites, including two pharmacologically active, but less, Cem diclofenac.

Systemic clearance of the active substance is about 263 ml / min. T_1/2 from plasma is 1-2 no, synovial fluid – 3-6 no. About 60% the dose is excreted as metabolites kidneys, less 1% excreted in the urine as unchanged, the rest is excreted as metabolites in the bile.

Testimony

Articular Syndrome (rheumatoid arthritis, osteoarthritis, ankiloziruyushtiy spondylitis, gout), degenerative and chronic inflammatory diseases of the musculoskeletal system (osteochondrosis, osteoarthritis, periartropatii), Post-traumatic inflammation of soft tissue and musculoskeletal system (stretching, injuries). Pain in the spine, neuralgia, mialgii, artralgii, pain and inflammation after surgery or injury, pain gout, migraine, algomenorrhea, pain in adnexitis, proctitis, gripes (biliary and renal), pain in infectious and inflammatory diseases of upper respiratory tract.

For topical application,: inhibition of miosis during cataract surgery, prevention of cystoid macular edema, associated with the removal and lens implantation, inflammation of the eye infectious nature, post-traumatic inflammation in penetrating and non-penetrating wounds of the eyeball.

Dosage regimen

For intake for adults is a single dose 25-50 mg 2-3 times / day. The frequency of administration depends upon the dosage form, the severity of the disease and is 1-3 times / day, rectally – 1 time / day. For the treatment of acute conditions or edema exacerbation of chronic process used / m at a dose 75 mg.

For children over 6 teenage years and daily dose is 2 mg / kg.

External used at a dose of 2-4 g (depending on the size of painful area) in the affected area 3-4 times / day.

When used in ophthalmology frequency and duration of administration are determined individually.

The maximum dose: ingestion for adults – 150 mg / day.

Side effect

From the digestive system: nausea, vomiting, anorexia, pain and discomfort in the epigastric region, flatulence, constipation, diarrhea; in some cases – erosive and ulcerative lesions, bleeding or perforation of the gastrointestinal tract; rarely – abnormal liver function. When rectally administered in single cases occurred inflammation of the colon with bleeding, exacerbation of ulcerative colitis.

From the central and peripheral nervous system: dizziness, headache, excitation, insomnia, irritability, feeling tired; rarely – paresthesia, visual impairment (fuzziness, diplopia), noise in ears, sleep disorders, convulsions, irritability, tremor, mental disorders, depression.

From the hematopoietic system: rarely – anemia, leukopenia, thrombocytopenia, agranulocytosis.

From the urinary system: rarely – impairment of renal function; in predisposed patients may be edema.

Dermatological reactions: rarely – hair loss.

Allergic reactions: skin rash, itch; when used in the form of eye drops – itch, redness, photosensitivity.

Local reactions: in place of the / m of possible burning, in some cases – Education infiltration, abscess, necrosis of adipose tissue; for rectal administration may be local irritation, the appearance of mucus mixed with blood, painful defecation; when used topically in rare cases – itch, redness, rash, burning; local application in ophthalmology possible transient burning sensation and / or temporary blurred vision immediately after instillation.

With long-term outdoor applications and / or applied to the vast surface of the body may be systemic side effects due to resorptive action of diclofenac.

Contraindications

Erosive and ulcerative lesions of the gastrointestinal tract in the acute phase, “aspirinovaâ triad”, violation of hematopoiesis of unclear etiology, hypersensitivity to diclofenac and the dosage form components, or other NSAIDs.

Pregnancy and lactation

Use in pregnancy and lactation is possible in cases, when the potential benefit to the mother outweighs the potential risk to the fetus or newborn.

Cautions

With caution used in diseases of the liver, kidney, GI history, dyspepsia, asthma, hypertension, Heart Failure, immediately after major surgery, as well as in elderly patients.

When specifying a history of allergic reactions to NSAIDs diclofenac and sulfites are used only in emergency cases. During treatment requires systematic monitoring of liver and kidney function, peripheral blood.

We do not recommend the rectal use in patients with anorectal disease or a history of bleeding anorectal. Outwardly should only be used on intact skin areas.

Avoid contact with eyes diclofenac (except eyedrops) or mucosal. Patients, using contact lenses, You should apply eye drops no earlier than 5 min after lens removal.

Not recommended for use in children under the age of 6 years.

During treatment dosage forms for systemic use is not recommended the use of alcohol.

Effects on ability to drive vehicles and management mechanisms

During treatment may reduce the speed of psychomotor reactions. With the deterioration of visual acuity after using eye drops should not drive and engage in other potentially hazardous activities.

Drug Interactions

In an application with diclofenac antihypertensive drugs may weaken their action.

There are few reports of the occurrence of seizures in patients, taking both NSAIDs and quinolone antibiotics series.

While the use of corticosteroids increases the risk of side effects from the digestive system.

With simultaneous use of diuretics may decrease the diuretic effect. While the use of potassium-sparing diuretics may increase the concentration of potassium in the blood.

When applied simultaneously with other NSAIDs may increase the risk of side effects.

There are reports of hypoglycemia or hyperglycemia in patients with diabetes, diclofenac is applied simultaneously with the hypoglycemic drugs.

In an application with acetylsalicylic acid may decrease the concentration of diclofenac in the blood plasma.

Although clinical studies have not found the influence of diclofenac on the effects of anticoagulants, described isolated cases of bleeding, while the use of diclofenac and warfarin.

With simultaneous use may increase the concentration of digoxin, lithium and phenytoin in blood plasma.

The absorption of diclofenac from the gastrointestinal tract is reduced while the use of kolestiraminom, less – with colestipol.

With simultaneous use may increase the concentration of methotrexate in plasma and increased toxicity.

With simultaneous use of diclofenac may not affect the bioavailability of morphine, However, the concentration of the active metabolite of morphine may be increased in the presence of diclofenac, which increases the risk of side effects of morphine metabolite, incl. respiratory depression.

In an application with pentazocine, a case of grand mal seizure; rifampicin – possible to reduce the concentration of diclofenac in plasma; with ceftriaxone – increased excretion of ceftriaxone in the bile; Cyclosporin – may increase the nephrotoxicity of cyclosporine.