Naklofen

Naklofen – non-steroidal anti-inflammatory drug (NPVS).

Form of release and structure

Dosage forms:

• The tablets covered with a kishechnorastvorimy film cover: yellowy-brown color, have round slightly biconvex form and a smooth surface (on 10 pieces in blisters, in a cardboard pack 2 blisters);
• Solution for intramuscular introduction (in oil): colourless or yellowish color transparent liquid (on 3 ml in ampoules, on 5 pieces in blisters, in a cardboard pack 1 blister, or on 3 ml in glass ampoules, on 5 pieces in plastic pallets, in a cardboard pack 1 pallet);
• Suppositories rectal: a cone-shaped form with homogeneous wax structure of yellow-white or white color (on 5 pieces in strips, in a cardboard pack 2 strips);
• Gel for external use of 1%: homogeneous mass of white color (on 60 g in aluminum tubas, in a cardboard pack 1 tuba).

Active ingredient of Naklofen – sodium diclofenac:

• 1 tablet – 50 mg;
• 1 ml of solution – 25 mg;
• 1 suppository – 50 mg;
• 1 g of gel – 10 mg that is equivalent to 11,6 mg diethyl amine diclofenac.

Auxiliary components:

• Tablets: starch corn, lactoses monohydrate, cellulose microcrystallic, povidone, magnesium stearate, silicon dioxide colloid anhydrous;
• Solution: propylene glycol, benzyl alcohol, sodium hydroxide, sodium disulphite, water for injections;
• Suppositories: fat firm;
• Gel: diethanol amide, carbomer, isopropanol, a macrogoal, a liquid paraffin, propylene glycol, цетомакрогол, sodium sulfite anhydrous, decyloleate, the water purified.

In addition as a part of a kishechnorastvorimy film cover: titanium dioxide, gipromelloz, propylene glycol, dye ferrous oxide yellow (E172), dye ferrous oxide red (E172), copolymer of ethyl acrylate and methacrylic acid, talc.

Indications to use

Naklofen's appointment is shown for the symptomatic therapy directed to achievement of bystry anesthetic and antiinflammatory effect, drug does not exert impact on progressing of a disease.

Indications to use of tablets, solution and suppositories:

• Degenerative and inflammatory pathologies of a musculoskeletal system: a pseudorheumatism, juvenile chronic arthritis, the psoriasis arthritis ankylosing a spondylarthritis (Bekhterev's disease), arthritis at a disease of Reuters, gouty arthritis, rheumatic defeat of soft tissues, an osteoarthrosis of a backbone and peripheral joints including a tendovaginitis, a bursitis, a periarthritis, a miositis, a synovitis, a radicular syndrome;
• Pain syndrome of weak or moderate degree of manifestation at traumatic defeats (followed by an inflammation), during the postoperative period, at bilious and renal colic, a mialgiya, neuralgia, a lumbar ishialgia, and also at such states as migraine, head and a dentagra, an adnexitis, альгодисменорея.

Besides, Naklofen appoint:

• Tablets: at a proctitis, a feverish syndrome, a strong pain syndrome against the background of infectious and inflammatory pathologies of a throat, ear, nose (tonsillitis, otitis, pharyngitis) as a part of complex therapy;
• Solution: at a proctitis;
• Gel: at a pseudorheumatism, a bursitis, a tendovaginitis and other rheumatic defeats of soft tissues, an osteoarthrosis, injury of muscles, sheaves and sinews, bruises, hypostases of soft tissues of inflammatory genesis, morbidity of joints and muscles, including against the background of heavy exercise stresses.

Contraindications

• III trimester of pregnancy;
• Syndrome of intolerance of acetylsalicylic acid (full or incomplete) – asthma, urticaria, rinosinusit, polyps mucous a nose;
• Hypersensitivity to NPVS, diclofenac and components of drug.

Contraindications to use of tablets, solution and suppositories:

• Oppression of a marrowy hemopoiesis;
• Acute stage of inflammatory diseases of intestines (disease Krone, nonspecific ulcer colitis (NUC));
• Exacerbation of gastrointestinal bleeding, erosive and ulcer pathologies mucous stomach or duodenum;
• The period after performing aortocoronary shunting;
• Dekompensirovanny heart failure;
• Disturbances of a hemostasis, cerebrovascular and other types of bleedings;
• The expressed renal failure (the clearance of creatinine (CC) is less than 30 ml/min.), including the progressing disease of kidneys, the diagnosed hyperpotassemia;
• Active disease of a liver, heavy liver failure;
• Breastfeeding period.

It is recommended to appoint suppositories, tablets and Naklofen's solution with care at coronary heart disease, cerebrovascular diseases, a lipidemia or a dislipidemiya, a diabetes mellitus, diseases of peripheral arteries, smoking, KK is less than 60 ml/min.; given in the anamnesis about development of an ulcer of the digestive tract (DT), existence of an infection of Helicobacter pylori, long use of NPVS, frequent alcohol intake, heavy somatopathies; the accompanying therapy: antiagregant (acetylsalicylic acid, klopidogret), selective serotonin reuptake inhibitors (to tsitalopra, fluoxetine, пароксетин, sertraline), anticoagulants (including warfarin), peroral glucocorticosteroids (Prednisolonum); to the patients of advanced age receiving diuretics including the weakened patients with low body weight.

Besides, tablets and solution should be applied with care at patients with general diseases of connecting fabric, the epilepsy induced by a porphyria, a diverticulitis at considerable decrease in the volume of the circulating blood (VCB), including after extensive surgery.

Use of diclofenac in the I-II trimester of pregnancy is possible only according to vital indications if the expected clinical effect for mother exceeds potential threat for a fruit.

It is impossible to apply suppositories at hemorrhoids, rectal bleedings, an injury or an inflammation of a rectum.

With care appoint suppositories at the accompanying therapy of a fibrinolitikama.

Use of gel at disturbance of integrity of an integument is contraindicated.

With care patients are recommended to use gel at chronic heart failure, an aggravation of a hepatic porphyria, erosive cankers of a GIT, the expressed renal failures and/or a liver, disturbance of coagulability of blood (including hemophilia, tendency to bleedings, lengthening of a bleeding time), bronchial asthma; during breastfeeding and advanced age.

Age restrictions of use of Naklofen:

• Tablets: up to 15 years or with body weight it is lower than 45 kg;
• Solution: up to 18 years;
• Suppositories: up to 15 years;
• Gel: up to 6 years.

Route of administration and dosage

• Tablets: accept inside, swallowing entirely, washing down with enough water, in time or right after food. The recommended dosing: in an initiation of treatment – on 1 tablet 2-3 times a day, but no more than 3 tablets a day. After achievement of the optimum effect sick transfer to a maintenance dose – 2 tablets a day;
• Solution: in oil 1 ampoule (75 mg) in a single dose is entered. Repeated introduction at severe renal colic – in 30 minutes, at other pathologies – only in 12 hours. Duration in oil of administration of solution should not exceed 2 days, then the patient (if necessary) should be transferred to reception of tablets or use of suppositories. Naklofen's solution cannot be mixed in one syringe with other drugs;
• Suppositories: the patient with bad portability of oral administration of diclofenac, drug is used rektalno. The recommended dosing: the adult – on 1 suppository 2-3 times a day, appointment depends on disease severity; to patients at the age of 15-18 years – on 1 suppository no more than 2 times a day. A maintenance dose – on 1 suppository 2 times a day. It is necessary to apply a minimal effective dose during minimum possible period;
• Gel: apply outwardly, applying a certain quantity on an affected area of a body and carefully rubbing in skin. Dosing has age restrictions: patients are more senior than 12 years – the one-time length of a strip of gel makes 5-10 cm, the procedure is carried out by 2-3 times a day; children from 6 to 12 years – no more than 3 cm of gel on 2 times a day. In need of drug use over 10 days it is necessary to get advice of the attending physician.

In case of simultaneous use of other forms of diclofenac, its total daily dose should not exceed 150 mg.

Side effects

Naklofen's use in the form of tablets, solution and suppositories can cause side effects:

• Nervous system: often – dizziness, a headache; seldom – drowsiness; very seldom – dysmnesias, nightmares, sensitivity disturbance (including paresthesias), a tremor, alarm, spasms, cerebrovascular disturbances, sleeplessness, a disorientation, irritability, a depression, mental disturbances, aseptic meningitis;
• Cardiovascular system: very seldom – a stethalgia, heartbeat, increase in the arterial pressure (AP), premature ventricular contraction, a myocardial infarction, a vasculitis, heart failure;
• Alimentary system: often – nausea, pain in epigastric area, increase in activity of aminotransferases, vomiting, dyspepsia, diarrhea, anorexia, a meteorism; seldom – a proctitis, GIT ulcers (with bleeding, perforation or without them), gastritis, bleeding from a GIT (a melena, vomiting and/or diarrhea with blood impurity), an abnormal liver function, jaundice, hepatitis; very seldom – dryness of an oral cavity and other mucous membranes, a glossitis, stomatitis, gullet erosive cankers, a lock, an exacerbation of a disease Krone or ulcer colitis, nonspecific hemorrhagic colitis, fulminant hepatitis, pancreatitis;
• Urinary system: very seldom – a hamaturia, an acute renal failure, a proteinuria, a nephrotic syndrome, a papillary necrosis, intersticial nephrite;
• Sense bodys: often – вертиго; very seldom – a sonitus, a hearing disorder, a vision disorder (a diplopia, sight misting), disturbance of flavoring feelings;
• Hemopoietic bodies: very seldom – a leukopenia, thrombocytopenia, an eosinophilia, an agranulocytosis, aplastic and hemolitic anemia;
• Respiratory system: seldom – short wind and bronchial asthma, cough; very seldom – throat hypostasis, a pneumonitis;
• Allergic reactions: anaphylactoid or anaphylactic reactions, including strong decrease in the ABP and shock; very seldom – a Quincke's disease (including persons);
• Integument: often – skin rash; seldom – a small tortoiseshell; very seldom – an itch, violent rashes, exfoliative dermatitis, eczema (including multiformny eczema and Stephens-Johnson's syndrome), a purpura, a Lyell's disease, a photosensitization, including allergic, a hair loss.

Besides, it is possible:

• Solution: in an injection site – emergence of pain, irritation, reddening and hypostasis of an integument;
• Suppositories: local irritation and inflammation.

Against the background of gel use Naklofen side effects appear seldom:

• Integument: reddening, a small tortoiseshell, burning sensation, a photosensitization, erythematic skin rash, eczema, contact dermatitis in the form of an itch, papular and vesicular rashes, a peeling of skin, a hyperemia, puffiness of the site of skin covered by gel;
• System reactions: Quincke's disease, bronchial asthma, system anaphylactic reactions, shock.

Special instructions

In some cases, when bystry achievement of therapeutic effect a pill is required it is possible to take in 30 min. prior to food and to wash down with enough water.

It is necessary to appoint tablets, solution and suppositories in minimal effective doses and minimum possible short course, it will allow to reduce risk of development of by-effects from a GIT.

Patients with the instruction in the anamnesis on pathology of upper parts of a GIT should be observed carefully during treatment by Naklofen.

With care it is necessary to apply diclofenac at a disease Krone and ulcer colitis not to allow an exacerbation of a disease.

In rare instances long therapy by diclofenac can cause development of strong hepatotoxic reactions therefore it is necessary to control function of a liver regularly.

Besides, at long treatment it is necessary to carry out the analysis a calla on the occult blood, to control a pattern of peripheral blood.

Because of influence of diclofenac on a renal blood stream treatment of the patients of advanced age (accepting diuretics), with renal or heart failure, with reduced OTsK needs to be accompanied with constant control of function of kidneys.

With care it is recommended to apply diclofenac at patients against the background of simultaneous receiving anticoagulants or fibrinolitik, with blood coagulation disturbance, epilepsy, a porphyria.

During treatment it is impossible to take alcoholic beverages.

Diclofenac has negative effect on fertility therefore purpose of drug is not recommended to the women wishing to become pregnant or having infertility.

Sodium diclofenac use at infectious diseases can mask symptoms of diseases.

It is not necessary to apply suppositories in combination with other NPVS.

Suppositories can influence properties of thrombocytes, but do not replace preventive effect of acetylsalicylic acid at cardiovascular pathologies.

Treatment by Naklofen (tablets, solution, suppositories) can reduce the speed of motor and mental reactions in this connection patients are recommended to refuse during use of drug potentially dangerous types of activity which performance demands the high speed of psychomotor reactions and special attention.

Gel cannot be applied on sites with the broken integrity of an integument.

It is not necessary to allow hits of gel on mucous membranes, in eyes or open wounds. Use of occlusive bandages is contraindicated.

It is necessary to be careful in case of need drawings a high dose of gel on the extensive surfaces of sensitive skin during the long period.

At simultaneous use with other forms of diclofenac it is required to observe the maximum total daily dose strictly.

During treatment by gel it is necessary to avoid long influence of direct sunshine.

It is recommended to wash up carefully hands after each rubbing in of gel in skin.

Gel Naklofen does not influence ability of the patient to control of vehicles and mechanisms.

Medicinal interaction

As Naklofen's use is shown only to destination the attending physician, the concomitant use of other medicines needs to be begun after preliminary consultation with the specialist not to allow development of side effects.

Terms and storage conditions

To store in the place, unavailable to children:

• Tablets – in the dry place, at a temperature not above 25 °C;
• Solution and suppositories – at a temperature up to 25 °C;
• Gel – to 30 °C.

Period of validity: tablets and solution – 5 years, suppositories and gel – 4 years.