Diclofenac

General characteristics. Structure:

Active agent: diclofenac of sodium of 100 mg.

Pharmacological properties:

NPVS derivative of phenylacetic acid. Renders the expressed antiinflammatory, analgeziruyushchy and moderate febrifugal action. The mechanism of action is connected with oppression of activity of TsOG - the main enzyme of metabolism of arachidonic acid, being the predecessor of prostaglandins which play a major role in a pathogeny of an inflammation, pain and fever. Analgeziruyushchy action is caused by two mechanisms: peripheral (indirectly, through suppression of synthesis of prostaglandins) and central (at the expense of inhibition of synthesis of prostaglandins in the central and peripheral nervous system).
Inhibits synthesis of proteoglycan in cartilages.
At rheumatic diseases reduces joint pains at rest and at the movement, and also morning constraint and a swelling of joints, promotes increase in volume of movements. Reduces posttraumatic and postoperative pains, and also inflammatory hypostasis.
Suppresses aggregation of thrombocytes. At prolonged use has the desensibilizing effect.
At topical administration in ophthalmology reduces hypostasis and pain at inflammatory processes of a noninfectious etiology.

Pharmacokinetics. After intake it is absorbed from a GIT. Meal slows down absorption speed, extent of absorption at the same time does not change. About 50% of active agent are metabolized at "the first passing" through a liver. At rectal administration absorption happens more slowly. Time of achievement of Cmax in plasma after intake makes 2-4 h depending on the applied dosage form, after rectal administration - 1 h, introductions in oil - 20 min. Concentration of active agent in plasma is in linear dependence on size of the applied dose.

Does not kumulirut. Linkng with proteins of plasma makes 99.7% (preferential with albumine). Gets into synovial fluid, Cmax is reached on 2-4 h later, than in plasma.

It is substantially metabolized with formation of several metabolites among which two pharmacological are active, but to a lesser extent, than diclofenac.

The system clearance of active agent makes about 263 ml/min. of T1/2 of plasma makes 1-2 h, of synovial fluid - 3-6 h. About 60% of a dose are removed in the form of metabolites by kidneys, less than 1% are excreted with urine in not changed look, other part is removed in the form of metabolites with bile.

Indications to use:

Joint syndrome (pseudorheumatism, the osteoarthritis ankylosing a spondylitis, gout), degenerative and chronic inflammatory diseases of a musculoskeletal system (osteochondrosis, osteoarthrosis, periartropatiya), posttraumatic inflammation of soft tissues and musculoskeletal system (stretchings, bruises). Backbone pains, neuralgia, a mialgiya, an arthralgia, a pain syndrome and an inflammation after operations and injuries, a pain syndrome at gout, migraine, альгодисменорея, a pain syndrome at an adnexitis, a proctitis, gripes (bilious and renal), a pain syndrome at infectious and inflammatory diseases of ENT organs.

For topical administration: miosis inhibition during operation for a cataract, prevention of the tsistoidny macular hypostasis connected with removal and implantation of a crystalline lens inflammatory processes of an eye of the noninfectious nature, posttraumatic inflammatory process at the getting and not getting eyeglobe wounds.

Route of administration and doses:

For intake for adults the single dose makes 25-50 mg of 2-3 times/days. Frequency of reception depends on the applied dosage form, weight of a course of a disease and makes 1-3 times/days, rektalno - 1 times/days. Apply in oil 75 mg in a dose to treatment of acute states or stopping of an aggravation of chronic process.
For children over 6 years and teenagers the daily dose makes 2 mg/kg.
Outwardly apply in a dose 2-4 g (depending on the area of the painful site) on the struck place of 3-4 times/days.
At use in ophthalmology the frequency and duration of introduction are defined individually.
The maximum daily dose for adults at intake makes 150 mg/days.

Features of use:

With extra care apply at diseases of a liver, kidneys, a GIT in the anamnesis, the dispeptic phenomena, bronchial asthma, an arterial hypertension, heart failure, right after serious surgical interventions, and also at patients of advanced age.

At instructions in the anamnesis on allergic reactions to NPVS and sulfites diclofenac is applied only in urgent cases. In the course of treatment systematic control of function of a liver and kidneys, pictures of peripheral blood is necessary.

Rectal use for patients with diseases of anorectal area or anorectal bleedings in the anamnesis is not recommended. Outwardly it is necessary to apply only on the unimpaired sites of skin.

It is necessary to avoid hit of diclofenac in eyes (except for eye drops) or on mucous membranes. The patients using contact lenses have to apply eye drops not earlier than in 5 min. after removal of lenses.

It is not recommended to apply at children under 6 years.

During treatment dosage forms for system use do not recommend alcohol intake.

Influence on ability to driving of motor transport and to control of mechanisms

During treatment reduction in the rate of psychomotor reactions is possible. At deterioration in clearness of sight after use of eye drops it is not necessary to drive the car and to be engaged in other potentially dangerous types of activity.

Side effects:

From the alimentary system: nausea, vomiting, anorexia, pains and unpleasant feelings in epigastric area, a meteorism, a lock, diarrhea; in some cases - erosive cankers, bleedings and perforation of a GIT; seldom - an abnormal liver function. At rectal administration in isolated cases were noted an inflammation of a large intestine with bleeding, an exacerbation of ulcer colitis.

From TsNS and peripheral nervous system: dizziness, headache, excitement, sleeplessness, irritability, feeling of fatigue; seldom - paresthesias, vision disorders (a vagueness, a diplopia), a sonitus, frustration of a dream, a spasm, irritability, a tremor, mental disturbances, a depression.

From system of a hemopoiesis: seldom - anemia, a leukopenia, thrombocytopenia, an agranulocytosis.

From an urinary system: seldom - a renal failure; at predisposed patients hypostases are possible.

Dermatological reactions: seldom - a hair loss.

Allergic reactions: skin rash, itch; at use in the form of eye drops - an itch, reddening, a photosensitization.

Local reactions: in the place in oil of introduction burning, in some cases - formation of infiltrate, abscess, a necrosis of fatty tissue is possible; at rectal administration the local irritation, emergence of mucous allocations with blood impurity, painful defecation are possible; at external use in rare instances - an itch, reddening, rash, burning; at topical administration in ophthalmology the passing burning sensation and/or a temporary illegibility of sight right after an instillation are possible.

At prolonged external use and/or drawing on extensive body surfaces system side effects owing to resorptive effect of diclofenac are possible.

Interaction with other medicines:

At simultaneous use with diclofenac of anti-hypertensive medicines weakening of their action is possible.

The patients accepting at the same time NPVS and antibacterial drugs of a hinolonovy row have single messages on developing of spasms.

At simultaneous use with GKS the risk of emergence of side effects from the alimentary system increases.

At simultaneous use of diuretics reduction of diuretic effect is possible. At simultaneous use with kaliysberegayushchy diuretics increase in potassium concentration in blood is possible.

At simultaneous use with other NPVS increase in risk of development of side effects is possible.

The patients with a diabetes mellitus applying diclofenac along with hypoglycemic drugs have messages on development of a hypoglycemia or a hyperglycemia.

At simultaneous use with acetylsalicylic acid reduction of concentration of diclofenac in a blood plasma is possible.

Though in clinical trials it is not established influences of diclofenac on effect of anticoagulants, separate cases of developing of bleedings at simultaneous use of diclofenac and warfarin are described.

At simultaneous use increase in concentration of digoxin, lithium and Phenytoinum in a blood plasma is possible.

Absorption of diclofenac from a GIT decreases at simultaneous use with Colestyraminum, to a lesser extent - with kolestipoly.

At simultaneous use increase in concentration of a methotrexate in a blood plasma and strengthening of its toxicity is possible.

At simultaneous use diclofenac can not exert impacts on bioavailability of morphine, however concentration of an active metabolite of morphine can remain raised in the presence of diclofenac that increases risk of development of side effects of a metabolite of morphine, including respiratory depressions.

At simultaneous use with pentazocine the case of development of a big convulsive attack is described; with rifampicin - reduction of concentration of diclofenac in a blood plasma is possible; with tseftriaksony - excretion of a tseftriakson with bile raises; with cyclosporine - increase in nephrotoxicity of cyclosporine is possible.

Contraindications:

GIT erosive cankers in an aggravation phase, "an aspirinovy triad", disturbances of a hemopoiesis of not clear etiology, hypersensitivity to diclofenac and components of the applied dosage form, or other NPVS.

Use at pregnancy and feeding by a breast
Use at pregnancy and in the period of a lactation perhaps in cases when the potential advantage for mother exceeds potential risk for a fruit or the newborn.

Use at abnormal liver functions
With extra care apply at liver diseases in the anamnesis.

Use at renal failures
With extra care apply at diseases of kidneys in the anamnesis.

Use for elderly patients
With extra care apply at patients of advanced age.

Use for children
It is not recommended to apply at children under 6 years.

Overdose:

Symptoms: vomiting, dizziness, a headache, short wind, consciousness opacification, children have myoclonic spasms, nausea, abdominal pain, bleedings, an abnormal liver function and kidneys.

Treatment: gastric lavage, administration of absorbent carbon, symptomatic therapy, artificial diuresis.
The hemodialysis is ineffective.

Storage conditions:

List B. At a temperature from 15 °C to 25 °C, in the place unavailable to children protected from light and moisture.

Issue conditions:

According to the recipe

Packaging:

Tablets пролонгир. actions, покр. film cover, 100 mg: 20 pieces.