Olfen-100 ректокапс

General characteristics. Structure:

Capsules rectal pinkish color, one end of the capsule stupid, another - pointed.

Active ingredient: diclofenac of sodium of 100 mg

Excipients: triglycerides with chains of average size, the triglycerides hydrogenated by C8-C18 lecithin soy, gelatin, глицерол 85%, titanium dioxide, ferrous oxide red (E172), polyethyleneglycol 20 000, polyethyleneglycol 1550, a glitserol monooleate and dioleate, polyvinyl acetate, talc.

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.

At posttraumatic and postoperative inflammations 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™-100 Rektokaps has analgeziruyushchy effect.

Pharmacokinetics. Absorption

After introduction to a rectum of Olfen™-100 Rektokaps resolves within several minutes, absorption happens more slowly, than at use of other forms of Olfen. Cmax in plasma is reached in 1 h after use.

Distribution

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

Metabolism and removal

Gidroksilglyukuronid and sulphatic metabolites have practically no biological activity and only about 1% of these substances are removed by kidneys in not changed look. Biological half-decay in plasma happens during 2 h and does not depend on a renal failure. T1/2 from synovial fluid is 3-6 h. The system clearance of active agent makes about 263 ml/min.

Pharmacokinetics in special clinical cases

The pharmacokinetics does not change depending 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 blood is not observed increases.

Indications to use:

— chronic polyarthritises, arthritises, arthroses;

— degenerative spondylarthrites;

— ankylosing spondylites;

— rheumatic joint and extraarticular inflammations;

— bursitis;

— tendovaginitis;

— tendinites;

— lumbago, sciatica;

— cervical syndrome;

— gout;

— pains and hypostases after injuries and surgeries;

— pains and/or inflammations of female generative organs (including primary dysmenorrhea, adnexitis);

— as supportive application at the treatment of acute infectious and inflammatory diseases of a throat, nose or ears which are followed by pain, for example, of pharyngotonsillites, otitises;

— migraine.

Route of administration and doses:

The initial daily dose makes 100 mg.

At mild and moderate pains and at long therapy the dose of 200 mg / usually is sufficient. To prevent emergence of pain at night and morning constraint, reception of Olfen™-100 Rektokaps before going to bed can be combined with reception of Olfen™-50 Laktab (to the maximum daily dose of 150 mg). The course of treatment proceeds usually 5-6 weeks.

At primary dysmenorrhea the daily dose which is picked up individually makes 200 mg; the initial dose has to be 100 mg and if it is necessary, can be raised during several menstrual cycles to the maximum 200 mg / Therapy it is necessary to begin in case of the first symptoms and to continue some more days, depending on a condition of the patient.

The Olfen™-100 capsules of Rektokaps need to be entered rektalno a blunt end. For introduction simplification they are processed by the greasing substance. In case of need before introduction the capsule can be moistened with water. After administration of drug the patient has to be in a bed within 20-30 min.

Features of use:

During treatment by the drug Olfen™-100 of Rektokaps, 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™-100 Rektokaps at patients with a hepatic porphyria.

Fever is not the indication for use of this drug.

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 the drug Olfen™-100 of Rektokaps monitoring of functions of kidneys is recommended, to a liver, and also pictures of peripheral blood.

Olfen™-100 Rektokaps, as well as other NPVS, can cause temporary oppression of aggregation of thrombocytes. Therefore patients with disturbance of coagulation need strict control of the doctor.

Before purpose of the drug Olfen™-100 of Rektokaps 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 the drug Olfen™-100 of Rektokaps 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 by the drug Olfen™-100 of Rektokaps.

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 – a small tortoiseshell, 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).

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.

Olfen™-100 Rektokaps 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.

Olfen™-100 Rektokaps 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.

Olfen™-100 Rektokaps can be applied together with peroral hypoglycemic means, at the same time medicinal interaction is not observed. Hypoglycemic and hyper glycemic reactions after use of the drug Olfen™-100 of Rektokaps 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 Olfen™-100 Rektokaps increase in nephrotoxicity of cyclosporine is possible.

Contraindications:

— peptic ulcer of a stomach and duodenum;

— attacks of bronchial asthma, urticaria, acute rhinitis after reception of acetylsalicylic acid and other NPVS in the anamnesis;

— proctites;

— pregnancy;

— period of a lactation (breastfeeding);

— children's age up to 12 years (because of the high content of active agent);

— hypersensitivity to drug components.

Use of the drug OLFEN™-100 REKTOKAPS at pregnancy and feeding by a breast
Drug is contraindicated at pregnancy and in the period of a lactation.

Use at abnormal liver functions

Administration of drug at acute disorders of function of a liver is prohibited.

Overdose:

Typical clinical symptoms of overdose of diclofenac of sodium are unknown. Arterial hypotension, a renal failure, spasms, 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:

It is necessary to store drug in the place, unavailable to children, at a temperature from 0 ° to 25 °C. A period of validity – 5 years.

Issue conditions:

According to the recipe

Packaging:

5 - blisters (1) - packagings cardboard.