Indometacin

Indometacin – non-steroidal anti-inflammatory drug with analgeziruyushchy, febrifugal action.

Form of release and structure

Dosage forms:

• The tablets covered with a kishechnorastvorimy cover: a round biconvex form, color of a kernel of a tablet – white or white with a yellowish shade, covers – from white to almost white (on 10 or 30 pieces in blister strip packagings from aluminum or polyvinylchloride, in a cardboard pack of 1, 2, 3, 4, 5, 6, 8 or 10 packagings; on 10, 20, 30, 40, 50, 60 or 100 pieces in polymeric banks, in a cardboard pack of 1 bank);
• Suppositories rectal: have the torpedo-shaped form, color, white with a yellow or cream shade, and a slight specific smell (in a blister strip packaging: on 50 mg – 3 or 5 pieces, in a pack cardboard 2 packagings; 6 pieces, in a cardboard pack 1 packaging; on 100 mg – 5 pieces, in a cardboard pack 2 packagings);
• Ointment for external use of 10%: from color, dark yellow to light yellow with a greenish shade, and specific smell (on 15, 30 or 40 g in aluminum tubas, or on 30 g in a polymeric tuba, in a cardboard pack 1 tuba; on 10, 15, 20, 25, 30 or 40 g in glass jars, in a cardboard pack of 1 bank);
• Gel for external use of 5% or 10%: has homogeneous structure of yellow color and a slight smell of alcohol (on 40 g in aluminum tubas, in a cardboard pack 1 tuba).

Active agent – indometacin:

• 1 tablet – 25 mg;
• 1 suppository – 50 or 100 mg;
• 1 g of ointment – 100 mg;
• 1 g of gel – 50 or 100 mg.

Auxiliary components:

• Tablets: potato starch, lactoses monohydrate, cellulose microcrystallic, magnesium stearate, povidone;
• Ointment: macrogoal 1500, dimethyl sulfoxide, глицерол, macrogoal 400;
• Gel: carbomer, macrogoal 400, propylene glycol, ethanol of 96%, Natrium benzoicum.

In addition as a part of tablets – a film cover: polysorbate-80, целлацефат, titanium dioxide.

Indications to use

• System use: a joint syndrome (including an osteoarthritis, a pseudorheumatism, gout, an ankylosing spondylitis), backbone pains, a mialgiya, neuralgia, inflammatory processes in soft tissues and joints as a result of traumatizing, rheumatism, diffusion diseases of connecting fabric, a dysmenorrhea; as a part of complex therapy at prostatitis, an adnexitis, cystitis, infectious and inflammatory diseases in otorhinolaryngology;
• External use: a joint syndrome at an exacerbation of gout and rheumatism, the pseudorheumatism ankylosing a spondylarthritis, psoriasis arthritis, backbone pains, an osteoarthrosis, osteochondrosis with a radicular syndrome, radiculitis, neuralgia, a mialgiya, inflammatory damage of sinews and sheaves, a sciatica, a bursitis, a lumbago; posttraumatic inflammation of soft tissues and joints; pains in muscles of rheumatic and not rheumatic genesis;
• Topical administration: miosis inhibition at an operative measure, prevention of inflammatory processes after surgeries on a front segment of an eye and concerning a cataract.

Contraindications

Use of all forms of Indometacin is contraindicated:

• Aggravation of erosive cankers of the digestive tract (DT);
• Hypocoagulation and other disturbances of a hemopoiesis;
• Period of pregnancy and breastfeeding;
• Age up to 14 years;
• Hypersensitivity to drug components.

It is forbidden to appoint tablets, suppositories and ointment the patient with the following diseases:

• Aspirinovy triad;
• The expressed abnormal liver functions and/or kidneys;
• Severe form of chronic heart failure;
• Severe form of arterial hypertension;
• Pancreatitis.

Besides, rectal use is contraindicated to patients at a proctitis, with a recent proctorrhagia, outside – at disturbance of integrity of an integument.

With care it is recommended to appoint:

• Indometacin in the form of tablets, suppositories, ointments to patients with gastrointestinal diseases, kidneys, a liver in the anamnesis, epilepsy, heart failure, arterial hypertension, at parkinsonism, directly after serious surgeries, the patient of advanced age;

• Gel along with other non-steroidal anti-inflammatory drugs (NPVS), at bronchial asthma, allergic rhinitis, polyps on the mucous surface of a nose.

Route of administration and dosage

The dosage form, dose and the period of treatment is appointed by the attending physician on the basis of clinical testimonies and a condition of the patient.

Pill is taken inside, after food. An initial dose for adults – on 25 mg 2-3 times a day, within 4 weeks. For achievement of therapeutic effect increase in dosing up to 50 mg 3 times a day is allowed. The maximum daily dose – 200 mg, at prolonged treatment no more than 75 mg.

Suppositories apply rektalno 50-100 mg 2 times a day, at a maintenance therapy of 1 times a day (for the night). The maximum daily dose – 200 mg.

Ointment is applied outwardly by 2 times a day.

Gel is applied with a thin layer on painful body parts, and the easy movements rubbed in skin. The single dose for adults corresponds to a gel strip of 4-5 cm, for teenagers – 2-2,5 cm. Frequency rate of procedures for 5% of gel – 3-4 times, for 10% – 2-3 times a day. It is not necessary to exceed the recommended drug dose.

Side effects

Use of tablets, suppositories, ointments can cause side effects:

• From the alimentary system: unpleasant feelings and abdominal pain, nausea, vomiting, lock or diarrhea, anorexia, bleedings, erosive cankers and perforation of a GIT; seldom – stomatitis, intestines strictures, a meteorism, gastritis, jaundice, bleeding from a diverticulum or a sigmoid gut, hepatitis;
• From cardiovascular system: increase in the arterial pressure (AP), hypostases, tachycardia, arrhythmia, thorax pains, arterial hypotension, palpitation, hamaturia, congestive heart failure;
• From a nervous system: depression, dizziness, feeling of fatigue, headache; seldom – drowsiness, alarm, spasms, a faint, a peripheral neuropathy, muscular weakness, the involuntary movements of muscles, sleep disorders, paresthesias, mental disorders (psychotic episodes, depersonalization), parkinsonism, a dysarthtia;
• From system of a hemopoiesis: seldom – petechias or ecchymomas, a leukopenia, a purpura, thrombocytopenia, hemolitic and aplastic anemia, the IDCS;
• Allergic reactions: seldom – urticaria, skin rash and an itch, an angiitis, a knotty erythema, Stephens-Johnson's syndrome, exfoliative dermatitis, a hair loss, a mnogoformny erythema, an acute respiratory distress, a toxic epidermal necrolysis, sharp decrease in the ABP, bronchial asthma, anaphylactic reactions, диспноэ, a Quincke's disease, a fluid lungs;
• From sense bodys: seldom – the diplopia, orbital and periorbital eye pains, disturbance of visual perception, a hearing disorder, tinnit, deafness;
• From an urinary system: seldom – a nephrotic syndrome, a proteinuria, renal failures, intersticial nephrite, a renal failure;
• From a metabolism: seldom – a glucosuria, a hyperglycemia, a hyperpotassemia;
• Others: seldom – inflows, vaginal bleeding, tension and increase in mammary glands, the increased sweating, nasal bleeding, a gynecomastia;
• Local reactions: at rectal use tenesmus, irritation of a mucous membrane of a rectum, an exacerbation of chronic colitis are possible; at outside – reddening, an itch, rash in a site of application.

At long use of gel emergence of local collateral manifestations in the form of burning, reddenings, an itch and rash, a dermahemia, development of allergic reactions is possible.

At emergence of signs of undesirable effects it is necessary to see the attending physician.

Special instructions

Drug should be used with care if the patient has dispeptic symptoms.

Simultaneous use with acetylsalicylic acid and other NPVS, with diflunizaly is not recommended.

Only in case of emergency apply Indometacin in the presence in the anamnesis of data on allergic reactions to NPVS.

Use of drug needs to be accompanied with systematic control of a peripheral picture of blood, function of a liver and kidneys.

Ointment and gel apply only on sites with undisturbed integrity of an integument, it is not necessary to allow their hit on mucous membranes, including in eyes.

During drug use by the patient it is recommended to refrain from all types of activity which performance depends on the high speed of psychomotor reactions and concentration of attention.

Medicinal interaction

Drug reduces action uricosuric, hypotensive and diuretics (saluretics); increases effect of antiagregant, indirect anticoagulants, fibrinolitik; increases development of side effects of estrogen, mineralokortikosteroid, other NPVS; promotes growth of toxic action of a zidovudine.

The concomitant use of a probenetsid can increase concentration of indometacin in blood.

At simultaneous use of Indometacin:

• Glucocorticosteroids, colchicine, diflunizat, ethanol – is raised by probability of gastrointestinal complications and developing of bleedings;
• Gold drugs, paracetamol, cyclosporine – increase nephrotoxic effect of indometacin;
• Tsefoperazon, цефамандол, valproic acid – promote development of a prothrombinopenia, increase risk of bleedings;
• Sulphonylurea derivatives – strengthen hypoglycemic effect.

At a combination to penicillin, lithium drugs, digoxin, a methotrexate, there is an increase in level of their concentration in a blood plasma.

Terms and storage conditions

To protect from children. To store:

• Tablets and gel: in the place protected from light, at a temperature up to 25 °C;
• Suppositories: in the dry place, at a temperature up to 25 °C;
• Ointment: in the place protected from light, at a temperature from 5 to 30 °C.

Period of validity: tablets – 3 years; suppositories, ointment, gel – 2 years.