Indometacin

Indomethacin has analgesic, anti-inflammatory, anti-aggregation and antipyretic effect.

[1], [2], [3], [4], [5],

Indications Indometacin

It is used to treat the following disorders:

• articular syndrome (this includes painful symptoms of osteoarthritis, gout, as well as rheumatoid arthritis and Bekhterev's disease);
• dysmenorrhoea;
• a variety of neuralgic conditions;
• rheumatism ;
• pain syndrome in the spine;
• myalgia ;
• Pathological conditions affecting connective tissues, and having a diffuse form;
• inflammation in the soft tissue or joints, having a traumatic origin;
• inflammation or infection, developing against a background of cystitis, adnexitis, prostatitis, or diseases affecting the ENT organs (as an additional treatment).

Release form

Release of the medication occurs in the form of suppositories, tablets for ingestion, as well as ointments (tube volume 10-40 g) or gel (the tube volume is 40 g).

[6], [7]

Pharmacodynamics

The drug is an indoleacetic acid derivative and is included in the category of NSAID medicines.

The effect of the drug is carried out by suppressing the activity of the enzyme COX, resulting in the suppression of metabolic transformations of eicosatetraenoic acid, as well as weakening of the binding of PG. In addition, the drug slows the process of platelet aggregation.

Parenteral, as well as oral use of drugs, reduces the intensity of pain, especially joint pain (both during movement and at rest), weakens the symptoms of joint stiffness and swelling in the mornings, and at the same time increases their motor volume. The anti-inflammatory effect occurs after 5-7 days of therapy.

When external treatment with gel or ointment, weakening of edemas and erythema, elimination of pain, and in addition, a reduction in joint stiffness that occurs in the morning, and an increase in the activity of their movements.

[8], [9], [10], [11],

Pharmacokinetics

Drugs taken inside the tablet are absorbed at high speed from the digestive tract. The C max level inside the serum is recorded after 2 hours.

After the processes of recycling substances inside the intestine and the liver, subsequent metabolic transformations are carried out inside the liver. Inside the plasma, an unchanged active element and unbound metabolic products - dezbenzoyl, as well as desmethyl with desmethyl-de-benzoyl ones - are detected.

Mean values of the half-life is about 4.5 hours. 60% of the drug is excreted through the kidneys (in the unchanged state and in the form of metabolic products), and another 33% (as decay products) is excreted through the intestine.

Suppositories are quickly absorbed through the rectum. The bioavailability index in this case is about 80-90%. The connection with proteins inside the serum is about 90% of the active ingredient.

The half-life is in the range of 4-9 hours. Inside the liver, metabolic transformations are carried out.

Through the kidneys, about 70% of the medicine is excreted, and another 30% is excreted through the intestine.

[12], [13],

Dosing and administration

Scheme of the use of tablets.

The size of dosage portions in tablets is selected separately for each patient, taking into account the intensity of the negative manifestations of the diagnosed disease.

Use the medication inside, immediately after eating or during this. Usually the starting dose is 25 mg; take them should be 2-3 times a day. If this dosage does not work, you can double it (2-3 times taking 50 mg of LS per day). For a day, a maximum of 0.2 g of medicament is allowed.

After receiving the desired result, you need to continue treatment during another 1 month, in the established or reduced portion. With prolonged therapy, a maximum of 75 mg Indomethacin is allowed per day.

At the initial stage of therapy in case of relief of severe or acute conditions, it is required to apply injections of the drug, and then transfer the patient to the use of suppositories or tablets. With the development of pain in the eyes, it is allowed to prescribe eye drops containing a similar active ingredient (eg Indocollir).

Mode of application of suppositories.

To introduce suppositories is necessary rectally - inside the rectum. This procedure is performed in the evening, before bedtime; you must first cleanse the intestines. You need to inject the medicine as deeply as possible to ensure a more intensive absorption.

Often, the suppository is administered in a dose of 50 mg with a 3-fold application per day, or a scheme with a 1-fold administration of a suppository with a volume of 0.1 g is administered. People with severe pain (for example, in case of a gout attack) can be administered per day to 0 , 2 g of substance in suppositories (thus supplementing the oral use of tablets).

Methods of using ointment or gel.

This form of the drug is used in the form of applications and rubbed into the epidermis in the area where the pain is felt. The medicine is applied in a thin layer. The epidermis needs to be cleared before the procedure. Do not treat places where there are any damages to the skin.

5% external medicines are applied at a frequency of 3-4 times per day. But the application of 10% medicines should be performed 2-3 times per day. Single and maximum servings of indomethacin are selected by calculating the amount (in cm) of the ointment or gel taken from the tube.

For an adult, 4-5 cm of medication is sufficient; while a maximum of 15-20 cm of substance is allowed per day. The child should use dosages, the size of which is reduced by half.

[23], [24], [25], [26], [27]

Use Indometacin during pregnancy

Suppositories with tablets can not be used during lactation or pregnancy.

Ointment and gel should not be used on the 3rd trimester (if the medicine is required to be applied over large areas of the body). Doctors believe that the external forms of indomethacin can be used with caution and in small doses when lactating and on the 1st and 2nd trimester of pregnancy.

Contraindications

The main contraindications (suppositories and tablets):

• regional enteritis;
• failure of hepatic function or active hepatic disease;
• the presence of intolerance;
• Ulcerative form of colitis;
• AND;
• a common cold with a sharp form, or urticaria, which developed due to the use of previously NSAID preparations;
• diagnosed hyperkalemia;
• ulcers that appear in the gastrointestinal tract;
• CRF (CC level is below 30 ml / minute) or progressive kidney disease;
• the presence of bleeding;
• a recent coronary artery bypass graft;
• disorders of blood-spinning processes;
• heart defects of an innate nature;
• problems with hematopoietic function (among them leukopenia or anemia).

Suppositories are also not used for signs of proctitis, symptoms of hemorrhoids, or bleeding in the rectal area.

Caution is necessary in case of use in such violations:

• Parkinsonism;
• somatic forms of diseases with a severe degree of severity, as well as CHD and cerebrovascular disorders;
• state of depression, epilepsy, CHF;
• hyper- or dyslipidemia;
• mental disorders, as well as alcoholism or nicotine dependence;
• diseases in the field of peripheral arteries;
• increased values of blood pressure, thrombocytopenia;
• diabetes mellitus, history of gastrointestinal ulcers;
• Hyperbilirubinemia, as well as CRF (level of CK - within 30-60 ml / min);
• prolonged use of other NSAIDs;
• presence of H. Pylori;
• hepatic cirrhosis, against which there is a portal form of hypertension;
• Combination with oral GCS (for example, prednisolone), anticoagulants (such as warfarin), SSRIs (among them citalopram, fluoxetine and sertraline with paroxetine) and antiaggregants (such as aspirin or clopidogrel);
• appointment to the elderly.

Ointments and gels are forbidden to apply in such cases:

• violation of the integrity of the epidermis at the processing sites;
• the presence of hypersensitivity.

External types of medication should be used with caution in such disorders:

• any combination, when the patient has polyposis in the nose or paranasal sinuses, asthma and hypersensitivity to NSAIDs;
• ulcer in the GIT area at the stage of exacerbation;
• problems with the processes of blood-spinning;
• children under 6 years of age.

[14], [15], [16], [17]

Side effects Indometacin

The use of suppositories and tablets can lead to the appearance of side effects:

• digestive function disorders: vomiting, jaundice, bloating, anorexia, nausea, bleeding within the gastrointestinal tract, gastritis, diarrhea or constipation and stomatitis. In addition, there is pain or discomfort in the abdominal area, ulcers, erosions or perforations inside the gastrointestinal tract, intestinal strictures, hepatitis and bleeding from the intestine of the sigmoid type or diverticulum;
• problems with the work of the National Assembly: fainting, dysarthria, weakness in the muscles, headaches, paresthesia, depression and dizziness. In addition, there is a feeling of fatigue, anxiety or drowsiness, Parkinsonism, sleep disorder, polyneuropathy, as well as mental disorders (depersonalization and psychotic manifestations), involuntary muscle contractions and cramps;
• disorders of SSS: puffiness, palpitation, hematuria, increase or decrease in blood pressure, cardiac failure (in stagnant form), arrhythmia, tachycardia and pain in the sternum;
• damage to the hematopoietic function: purpura, thrombocyto- or leukopenia, petechiae, hemolytic or aplastic form of anemia, and in addition coagulopathy of consumption and ecchymosis;
• disorders of urinary excretion: problems with kidney function, proteinuria, nephrotic syndrome, renal function deficiency and tubulointerstitial nephritis;
• problems with the work of the senses: visual or hearing impairment, deafness, tinnitus, diplopia, and periorbital pain sensations;
• disorders of metabolic processes: glucosuria and hyperkalemia or -glycemia;
• signs of allergy: rashes, hives, itching, alopecia, anaphylactic symptoms, angiitis and asthma. In addition, a sudden decline in blood pressure, nodular type of erythema, pulmonary edema and exfoliative form of dermatitis. Dyspnoea, Quincke edema, Stevens-Johnson syndrome, RDSS, erythema multiforme and TEN are also being developed;
• others: bleeding from the vagina or nose, hot flashes, gynecomastia, hyperhidrosis, as well as an increase in the size of the mammary glands or their tension.

Suppositories can also cause tenesmus, irritation of the mucous membranes inside the rectum and exacerbation of colitis or hemorrhoids.

The use of ointment or gel can lead to such negative symptoms: allergy, skin hyperemia or dryness, rashes or itching in the application area and burning sensation. With prolonged use, there are common symptoms. There is an exacerbation of existing psoriasis.

[18], [19], [20], [21], [22]

Overdose

The development of signs of drug poisoning is usually noted when using its rectal or oral forms: a sense of disorientation, memory disorder, nausea, dizziness, vomiting and severe headaches. With severe intoxication, convulsions with paresthesias or numbness in the limbs region appear.

Therapy is selected, taking into account the registered negative symptoms.

[28], [29], [30], [31], [32]

Interactions with other drugs

Combination with lithium agents, methotrexate and digoxin increases their indices inside the serum, which can increase their toxic properties.

Combined use with GCS, drugs containing ethyl alcohol, corticotropins and colchicine may increase the likelihood of bleeding in the gastrointestinal tract.

Combination with medications containing paracetamol increases the likelihood of developing nephrotoxic effects.

Simultaneous use with insulin and other antidiabetic drugs potentiates their properties.

Use together with thrombolytics, anticoagulants, as well as antiaggregants with indirect type of activity potentiates their effect, resulting in increased probability of bleeding.

Combination with cyclosporine or gold medications leads to increased nephrotoxicity (most likely, this is due to suppression of the processes of binding of PG within the kidneys).

The combination with diuretic potassium-sparing nature leads to a weakening of their effectiveness, which increases the likelihood of hyperkalemia.

Treatment in which indolemacin is used with plicamycin, cefamandol, valproic acid, as well as cefaperazone and cefotetan, increases the risk of bleeding and increases the frequency of hypoprothrombinemia.

Combination with uricosuric or antihypertensive drugs causes a weakening of their drug activity.

Combined use with GCS, estrogens and other NSAIDs leads to an increase in the characteristic negative reactions.

Antacids, and in addition colestramine weaken the absorption of the drug.

Use together with zidovudine may provoke an increase in its toxic properties (due to suppression of metabolic processes).

Combination with myelotoxic substances enhances their hematotoxic effect.

[33], [34], [35], [36], [37], [38]

Storage conditions

Indomethacin should be kept at temperatures not exceeding 25 ° C.

[39], [40], [41], [42], [43]

Shelf life

Indomethacin can be used within 3-5 years from the date of manufacture of the therapeutic drug.

[44], [45], [46], [47]

Application for children

The tablet form of drugs and suppositories is forbidden to use in children under the age of 14, and a gel or ointment is allowed to use from the first year.

[48], [49], [50], [51], [52]

Analogues

The analogues of the drug are medicines Adolor, Diclouran and Bioran with Diclofenac and Voltaren, and besides, Aerelt, Ortophen, Rapten with Diklak, Naklofen with Ketalgin and Ketorol with Piroxicam and Naise. Also in the list of Ketanov, Ibuprofen and so on.

[53], [54], [55], [56], [57], [58], [59]

Reviews

Indomethacin (suppositories and tablets) often receives positive feedback regarding its anti-inflammatory and analgesic effect. Most people note that it helped to eliminate the swelling and pain that arose in the back, muscles and joints due to various diseases of the ODA, without leading to the development of negative symptoms. But there are also comments of those to whom the medicine did not help, on the contrary provoking the appearance of characteristic negative manifestations. From all of the above, we can conclude that the drug is not suitable for everyone, so the selection of a drug from the category of NSAIDs must be done individually for each patient.

The degree of effectiveness of ointment or gel application is also determined by the individual characteristics of the human body, but in such cases, even if therapy does not work, the appearance of negative symptoms is unlikely.