Olfen-75

General characteristics. Structure:

Active ingredient:

diclofenac of sodium         of 37.5 mg 75 mg
lidocaine hydrochloride     of 10 mg 20 mg

Excipients: N-Acetylcysteinum, dinatrium эдетат, propylene glycol, polyethyleneglycol, sodium hydroxide.

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 drug, thanks to antiinflammatory and analgeziruyushchy action, reduces joint pains at rest and at the movement, and also morning constraint and a swelling of joints, promotes increase in volume of movements.

At posttraumatic and postoperative inflammations of Olfen™-75 promotes bystry simplification of spontaneous pains and an oxycinesia, and also reduces inflammatory hypostases.

Drug shows analgeziruyushchy effect at moderate and severe pain of not rheumatic genesis.

At primary dysmenorrhea of Olfen™-75 has analgeziruyushchy effect.

Lidocaine has mestnoanesteziruyushchy effect.

Pharmacokinetics. Absorption

After introduction in oil time of achievement of Cmax in a blood plasma makes about 20 min. the Analgeziruyushchy effect develops in 15-30 min.

Distribution

Linkng with proteins of plasma - 99.7% (it is preferential with albumine).

Gets into synovial fluid where Cmax is reached on 2-4 h later, than in a blood plasma. T1/2 makes 3-6 h of synovial fluid.

Metabolism

Gidroksiglyukuronid and sulphatic metabolites have practically no biological activity.

Removal

T1/2 makes 2 h of a blood plasma. The system clearance of diclofenac makes about 263 ml/min.

Pharmacokinetics in special clinical cases

The pharmacokinetics does not depend on age of the patient. At patients with the expressed renal failures (KK less than 10 ml/min.) the specific weight of removal of metabolites with bile therefore increase in their concentration in plasma is not observed increases.

Indications to use:

— aggravation of a course of rheumatism;

— pseudorheumatism;

— ankylosing spondylitis;

— degenerative spondylarthritis;

— painful vertebralny syndrome;

— gout;

— renal colic;

— bilious colic;

— pains, an inflammation and puffiness after injuries and surgical interventions.

Route of administration and doses:

Drug appoint in oil (deeply) in an upper outside quadrant of a buttock in a dose of 75 mg (1 ampoule) of 1 times /

In hard cases (for example, at renal or bilious colic) it is possible to appoint 2 injections a day at an interval of several hours (the place of an injection should be changed).

The combination of parenteral use of drug with other dosage forms of diclofenac (Olfen™-50 Laktab, Olfen™-100 Rektokaps) to the maximum daily dose of 150 mg is possible.

Drug can be used in oil within 2 days. In case of need it is possible to continue therapy by diclofenac in other dosage forms (Olfen™-50 Laktab, Olfen™-100 Rektokaps).

Features of use:

During treatment of Olfenom-75, as well as other NPVS, it is necessary to control indicators of function of a liver regularly. Treatment should be stopped in case of an abnormal liver function if clinical symptoms of a disease of a liver (for example, hepatitis) or other manifestations appeared (including an eosinophilia, skin rashes).

With care it is necessary to apply Olfen™-75 at patients with a hepatic porphyria.

The patients with dysfunctions of heart, kidneys weakened to patients and elderly people during treatment need observation of the doctor.

For treatment of the weakened patients of advanced age and with small body weight drug is recommended to be used in the smallest effective dose.

At prolonged use of Olfena-75 monitoring of functions of kidneys is recommended, to a liver, and also pictures of peripheral blood.

Олфен™-75, as well as other NPVS, temporary oppression of aggregation of thrombocytes can cause. Therefore patients with disturbance of coagulation need strict control of the doctor.

Before purpose of the drug Olfen™-75 careful medical examination of patients with the instruction in the anamnesis on a round ulcer, patients with gastrointestinal disturbances of not clear genesis, with damages of kidneys or a liver is required, at increase in the ABP, patients of advanced age.

With bronchial asthma, hay fever, a chronic respiratory disease, polyps in a nose or in the presence of allergic reactions to analgetics or antirheumatic means of all types use of Olfena-75 can cause attacks of asthmatic character in patients.

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

Patients with a rotatory vertigo (вертиго) or other frustration of TsNS (including with vision disorders) have to refrain from driving of vehicles and work with mechanisms during treatment of Olfenom-75.

Side effects:

From the alimentary system: pains in epigastric area, nausea, vomiting, diarrhea, spasms in a stomach, dyspepsia, a meteorism, anorexia, gastrointestinal bleedings (a hematemesis, a melena, diarrhea with blood), a round ulcer without bleeding and perforation, nonspecific hemorrhagic colitis and an exacerbation of ulcer colitis or a disease Krone, aphthous stomatitis, a glossitis, an esophagitis, pancreatitis, a lock, an exacerbation of hemorrhoids, increase in activity of aminotransferases in blood serum sometimes to moderate or high degree with/without jaundice; in some cases – fulminant hepatitis.

From TsNS and peripheral nervous system: headache, dizziness, вертиго, fatigue, disturbance of touch, paresthesia, tremor, memory disturbance, disorientation, sleeplessness, irritability, concern, depression, dreadful dreams, psychotic reactions, aseptic meningitis.

From sense bodys: visual disturbances (sight illegibility, diplopia), hearing disorder, sonitus, taste disturbance.

From cardiovascular system: in isolated cases – tachycardia, a stethalgia, arterial hypertension, heart failure.

From an urinary system: acute renal failure, hamaturia, proteinuria, intersticial nephrite, nephrotic syndrome, necrotizing papillitis.

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

Dermatological reactions: skin rash, it is rare – violent rashes, eczema, an erythrosis (exfoliative dermatitis), a hair loss, a photosensitization, a purpura.

Allergic reactions: seldom – urticaria, violent rashes, a mnogoformny erythema, Stephens-Johnson's syndrome, a Lyell's disease (a toxic epidermal necrolysis), an allergic purpura, a bronchospasm, anaphylactic/anaphylactoid reactions (including arterial hypotension).

Local reactions: pain, infiltrate, sometimes - abscess and a local necrosis.

Interaction with other medicines:

At simultaneous use of diclofenac with drugs of lithium or digoxin increase in concentration of lithium and digoxin in a blood plasma is possible.

Олфен™-75 can reduce efficiency of diuretics. At simultaneous use with kaliysberegayushchy diuretics development of a hyperpotassemia is possible (regular control of content of potassium in serum is necessary).

At simultaneous use of other NPVS or GKS for system use increase in risk of gastrointestinal bleedings is possible.

Олфен™-75 does not interact with anticoagulants. However in need of simultaneous use as a precautionary measure it is necessary to carry out control of indicators of a blood coagulation for assessment of development of anticoagulating effect. Sodium diclofenac in a high dose (200 mg) can oppress reversibly aggregation of thrombocytes.

Олфен™-75 it is possible to apply together with peroral hypoglycemic means, at the same time medicinal interaction is not observed. Hypoglycemic and hyper glycemic reactions after drug Olfen-75 use are in some cases possible that demands correction of its dose or a dose of hypoglycemic means.

With care it is necessary to apply NPVS during 24 h to or after treatment by a methotrexate as concentration of a methotrexate in blood and its toxicity can raise.

At simultaneous use with Olfenom-75 increase in nephrotoxicity of cyclosporine is possible.

Contraindications:

— peptic ulcer of a stomach;

— peptic ulcer of a duodenum;

— "an aspirinovy triad" (attacks of bronchial asthma, urticaria, acute rhinitis) after reception of acetylsalicylic acid and other NPVS in the anamnesis;

— pregnancy;

— period of a lactation (breastfeeding);

— children's age up to 12 years;

— hypersensitivity to diclofenac and other components of drug.

Use of the drug OLFEN™-75 at pregnancy and feeding by a breast
Drug is contraindicated at pregnancy and in the period of a lactation (breastfeeding).

Use at abnormal liver functions

During treatment of Olfenom-75 it is necessary to control indicators of function of a liver regularly. Treatment should be stopped in case of an abnormal liver function if clinical symptoms of a disease of a liver appeared (for example, hepatitis). With care it is necessary to apply Olfen-75 at patients with a hepatic porphyria.

Use at renal failures

Patients with renal failures during treatment need observation of the doctor.

Overdose:

Symptoms: arterial hypotension, a renal failure, spasms, symptoms of irritation of a GIT, breath difficulty are possible.

Treatment: after intake of an overdose of drug for prevention of its absorption it is necessary to carry out as soon as possible a gastric lavage and to appoint absorbent carbon. At development of the listed above symptoms carry out a symptomatic and maintenance therapy.

Because of high extent of linkng of diclofenac with proteins of plasma and his intensive metabolism in a liver such measures as an artificial diuresis, dialysis or hemoperfusion, apparently, are ineffective for removal of NPVS from an organism.

Storage conditions:

Drug should be stored in the place, unavailable to children, at a temperature from 0 °C to 25 °C. A period of validity – 5 years.

Issue conditions:

According to the recipe

Packaging:

2 ml - ampoules (5) - planimetric strip packagings (1) - packs cardboard.