Diklofenak-akos

General characteristics. Structure:

Ointment of 1% of white or almost white color, with a slight specific smell.

Active ingredient:     1 g
diclofenac of sodium             of 10 mg

Excipients: Dimexidum, polyethyleneglycol-400, poly(ethylene oxide)-4000, 1,2 propylene glycol, нипагин, нипазол.

Pharmacological properties:

NPVS. Has antiinflammatory, analgeziruyushchy and febrifugal effect. Inhibits TsOG enzyme in the cascade of metabolism of arachidonic acid and breaks biosynthesis of prostaglandins.

At external use has antiinflammatory and analgeziruyushchy effect. Reduces and stops pains in an ointment site of application (including joint pains at rest and at the movement), reduces morning constraint and a swelling of joints. Promotes increase in volume of movements.

 

Pharmacokinetics. Absorption

At introduction in oil Cmax in a blood plasma is reached in 10-20 min.

At external use it is partially soaked up through skin; bioavailability makes 6%.

Distribution

Linkng with blood proteins makes at introduction in oil 99%, at external use - 99.7%.

Diclofenac well gets into fabrics and synovial fluid in which Cmax of active agent is reached in 4 h after introduction in oil.

At patients with polyarthritis who receive drug in the form of ointment (on area of the inflamed joint) concentration in synovial fluid is higher, than concentration in a blood plasma.

Metabolism and removal

T1/2 makes 2 h of plasma, T1/2 from synovial fluid is 4-6 h.

35% of diclofenac are removed in the form of metabolites with a stake, 65% are exposed to metabolism in a liver and are removed in the form of inactive metabolites with urine.

Indications to use:

Solution for introduction in oil:

— acute pain syndrome;

— acute rheumatism;

— pseudorheumatism;

— ankylosing spondylitis (Bekhterev's disease);

— arthrosis;

— spondylarthrosis;

— renal colic;

— hepatic colic.

Ointment:

— inflammatory and degenerative diseases of joints;

— rheumatism of soft tissues;

— traumatic bruises;

— sprains, muscles and sinews;

— inflammatory hypostases of soft tissues;

— the arthralgia and a mialgiya caused by a heavy exercise stress.

Route of administration and doses:

Diklofenak-AKOS enter in initiation of treatment once in oil in a dose 75 mg (1 ampoule) or at most 150 mg (2 ampoules) a day only the adult and only when it is necessary to gain especially bystry therapeutic effect.

Usually injections are appointed within 1-5 days.

In need of continuation of therapy pass to reception of diclofenac in the form of tablets, capsules, use of suppositories.

Injections in oil can be combined using drug inside or rektalno, at the same time the maximum daily dose should not exceed 150 mg.

Ointment in a dose of 2-4 g is applied a thin layer on skin over the center of an inflammation and slightly rubbed, use frequency - 2-3 Maximum daily dose of ointment should not exceed 8 g. A course of treatment - no more than 14 days. Need of more prolonged use of drug is defined by the doctor.

Features of use:

Administration of the drug Diklofenak-AKOS in oil is possible only under strict control of the doctor after careful assessment of a ratio advantage/risk at the following states: the induced porphyria; system lupus erythematosus and other general diseases of connecting fabric.

Especially careful observation is required in need of administration of drug in oil from patients with gastrointestinal diseases, including erosive cankers (ulcer colitis, a disease Krone) in the anamnesis; at patients with the previous diseases of kidneys and/or heavy abnormal liver functions; at heavy arterial hypertension and/or heart failure; at patients of senile age; directly right after surgical intervention.

Carefully and only under direct control of the doctor it is possible to apply Diklofenak-AKOS in oil at patients with bronchial asthma, allergic rhinitis, polyps of a mucous membrane of a nasal cavity, and also at chronic obstructive respiratory diseases and persistent infections of respiratory tracts in connection with danger of emergence of an attack of asthma, a Quincke's edema or a small tortoiseshell.

Use of Diklofenaka-AKOS in the form of ointment perhaps only on doctor's orders in the following cases: a peptic ulcer of a stomach and duodenum in the anamnesis; abnormal liver function and kidneys; the expressed disturbances from system of a hemopoiesis; bronchial asthma, rhinitis, polyps of a mucous membrane of a nose; allergic reactions in the anamnesis.

With care to use drug in the form of ointment along with other NPVS.

Use in pediatrics

In need of use of drug in the form of ointment control of the doctor is required from children under 6 years.

Influence on ability to driving of the car and to control of mechanisms

Because at use of drug in high doses development of such side effects as dizziness and feeling of fatigue is possible, ability to drive the car or other moving objects is in some cases broken. These phenomena amplify at a concomitant use of alcohol.

Side effects:

Side effects depend on individual sensitivity, size of the applied dose and duration of treatment.

At use of solution for introduction in oil

From the alimentary system: nausea, vomiting, pains in epigastriums, anorexia, a meteorism, locks, gastritis up to erosive with bleeding, increase in activity of transaminases, medicinal hepatitis, pancreatitis.

From an urinary system: intersticial nephrite.

From TsNS: headache, dizziness, disorientation, excitement, sleeplessness, irritability, fatigue, aseptic meningitis.

From respiratory system: bronchospasm.

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

Dermatological reactions: dieback, erythema, eczema, hyperemia, erythrosis, photosensitization.

Allergic reactions: a multiformny erythema, a Lyell's disease, Stephens-Johnson's syndrome, anaphylactic reactions, including shock.

Local reactions: in the place of an injection burning, formation of infiltrate, a necrosis of fatty tissue are possible.

Others: a liquid delay in an organism, hypostases, increase in the ABP.

At external use

In a site of application of ointment skin rash, burning, reddening are possible. At prolonged external use of drug development of system side effects from the alimentary system, TsNS, respiratory system, and also allergic reactions is possible.

Interaction with other medicines:

At simultaneous use of the drug Diklofenak-AKOS with digoxin, Phenytoinum or drugs of lithium increase in concentration in plasma of the specified medicines is possible; with diuretics and antihypertensives - reduction of effect of these drugs is possible; with kaliysberegayushchy diuretics - development of a hyperpotassemia is possible; with atsetisalitsilovy acid - decrease in concentration of diclofenac in a blood plasma and increase in risk of development of side effects.

Diclofenac can strengthen toxic effect of cyclosporine on kidneys.

Diklofenk-AKOS can cause hypo - or a hyperglycemia therefore at simultaneous use with hypoglycemic means control of concentration of glucose in blood is required.

At use of a methotrexate during 24 h to or after reception of Diklofenaka-AKOS increase in concentration of a methotrexate and strengthening of its toxic action is possible.

At simultaneous use with anticoagulants regular control of indicators of a blood coagulation is necessary.

Contraindications:

— pathological changes of a picture of blood of not clear genesis (for introduction in oil);

— a peptic ulcer of a stomach and duodenum (for introduction in oil), in an aggravation phase (for external use);

— destructive and inflammatory diseases of intestines in an aggravation phase (for introduction in oil);

— pregnancy;

— the lactation period (it is necessary to refuse breastfeeding);

— children's and teenage age up to 18 years (for introduction in oil);

— children's age till 1 year (for external use);

— hypersensitivity to acetylsalicylic acid or other NPVS (including "an aspirinovy triad");

— hypersensitivity to diclofenac and other components of drug.

 

Use of drug DIKLOFENAK-AKOS at pregnancy and feeding by a breast
Drug is contraindicated to use at pregnancy and in the period of a lactation.

 

Use at abnormal liver functions
Especially careful observation is required in need of administration of drug in oil from patients with heavy abnormal liver functions. Use of Diklofenaka-AKOS in the form of ointment perhaps only on doctor's orders at abnormal liver functions.

 

Use at renal failures
Especially careful observation is required in need of administration of drug in oil from patients with the previous diseases of kidneys.

Use of Diklofenaka-AKOS in the form of ointment perhaps only on doctor's orders at renal failures.

 

Use for children
In need of use of drug in the form of ointment control of the doctor is required from children under 6 years.

Overdose:

Symptoms: the clinical picture is defined by disturbances from TsNS (a headache, dizziness, a hyperexcitability, the hyperventilation phenomena with the increased convulsive readiness, children have myoclonic spasms) and disturbances from the alimentary system (abdominal pains, nausea, vomiting; there can be bleedings from a GIT and/or abnormal liver functions); renal failures are possible.

Treatment: symptomatic therapy, careful observation of a condition of the patient. The specific antidote is not known.

Storage conditions:

List B. Solution for introduction in oil should be stored in the place protected from light. To store in places unavailable to children. A period of validity - 2 years.

Issue conditions:

Without recipe

Packaging:

3 ml - ampoules (5) - packs cardboard.
3 ml - ampoules (10) - packs cardboard.
30 g - aluminum (1) - packs cardboard.