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Indocin is prescribed for articular syndrome, back pain, neuralgia, myalgia, traumatic inflammation of soft tissues and joints, rheumatism, diffuse connective tissue diseases, dysmenorrhea. As an adjuvant for infectious and inflammatory diseases of the ENT organs, adnexitis, prostatitis, cystitis.

Brand: Indomethacin

Availability: In Stock
Average Delivery Time: 9 Days
Exp. Date: June 2024
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Product description

Pharmacology of the drug Indocin

Buy Indocin in Canada

Pharmacological action - anti-inflammatory, analgesic.

It inhibits cyclooxygenase (COX-1 and COX-2), reduces the synthesis of GHGs, which cause the development of pain in the inflammation focus, an increase in temperature and an increase in tissue permeability. It has an antiplatelet effect.

It causes a weakening or disappearance of pain syndrome of a rheumatic and non-rheumatic nature (including with pain in the joints at rest and during movement, reduces morning stiffness and swelling of the joints, increases the range of motion; in inflammatory processes that occur after operations and injuries, quickly relieves both spontaneous pain and pain on movement, reduces inflammatory edema at the site of the wound).

After oral administration of a single dose of 25 or 50 mg is rapidly absorbed, Tmax - about 2 hours; with rectal use, the absorption rate is higher. When taken orally, bioavailability is 90–98%, with rectal administration, it is slightly less - 80–90%, which is probably due to the insufficient retention time of the suppository (less than 1 hour) to ensure complete absorption. Plasma protein binding - 90–98%. T1/2 - 4-9 hours. With a daily intake of 25 or 50 mg of indomethacin three times a day, the equilibrium concentration is on average 1.4 times higher than the concentration after a single dose. Biotransformed mainly in the liver. In the blood plasma is in the form of an unchanged substance and desmethyl-, desbenzoyl- and desmethyl-desbenzoylmetabolites, which are present in unconjugated form. It is excreted mainly by the kidneys - 70% (30% - unchanged) and the gastrointestinal tract - 30%. Passes through the BBB, placenta, and enters breast milk. Not removed by hemodialysis.

When instilling eye drops, it penetrates into the anterior chamber of the eye. After a single instillation, it is determined in the moisture of the anterior chamber for several hours.

Carcinogenicity, mutagenicity, effects on fertility

In an 81-week study of chronic toxicity in rats when administered orally at doses up to 1 mg / kg / day, no carcinogenic effect was found. In carcinogenicity studies in rats (study period - 73–110 weeks) and in mice (study period - 62–88 weeks) at doses up to 1.5 mg / kg / day, indomethacin caused neoplastic or hyperplastic changes.

Indomethacin mutagenicity was not detected in a number of bacterial tests in vitro (Ames test, test with E. Coli with / without metabolic activation) and in a series oftests in vivo, including the test for sex-linked recessive flying Drosophyla, a micronucleus test in mice.

In reproduction studies, incl. in two generations, at a dose level of up to 0.5 mg / kg / day, indomethacin did not affect fertility in mice and rats.

Application of the substance Indomethacin

Arthritis treatment with Indocin

For systemic use (orally, intramuscularly, rectally)

Inflammatory and degenerative diseases of the musculoskeletal system: rheumatoid, psoriatic, juvenile chronic arthritis, arthritis in Paget's and Reiter's disease, neuralgic amyotrophy (Personage-Turner disease), ankylosing spondylitis (ankylosing spondylitis), gouty arthritis, rheumatism. Pain syndrome: headache (including with menstrual syndrome) and toothache, lumbago, sciatica, neuralgia, myalgia, after injuries and surgical interventions accompanied by inflammation, bursitis and tendonitis (most effective when localized in the shoulder and forearm). Algodismenorrhea, to preserve pregnancy, Barter's syndrome (secondary hyperaldosteronism), pericarditis (symptomatic treatment), childbirth (as an analgesic and tocolytic agent in preterm labor), inflammatory processes in the small pelvis, incl. adnexitis, non-closure of the botalle duct. Infectious and inflammatory diseases of ENT organs with severe pain syndrome (as part of complex therapy): pharyngitis, tonsillitis, otitis media. Feverish syndrome (including with lymphogranulomatosis, other lymphomas and hepatic metastases of solid tumors) - in case of ineffectiveness of acetylsalicylic acid and paracetamol.

Interaction of the Indocin

Indocin drug appearance

Reduces the diuretic effect of potassium-sparing, thiazide and loop diuretics. Increases (mutually) the risk of side effects (primarily gastrointestinal lesions) of other NSAIDs. Increases plasma concentration of digoxin, methotrexate and Lipreparations+, which can lead to increased toxicity. Concomitant use with paracetamol increases the risk of nephrotoxicity. Ethanol, colchicine, glucocorticoids, and corticotropin increase the risk of gastrointestinal bleeding. Enhances the hypoglycemic effect of insulin and oral hypoglycemic drugs; enhances the effect of indirect anticoagulants, antiplatelet agents, fibrinolytics (alteplase, streptokinase and urokinase) and increases the risk of bleeding. With the use of potassium-sparing diuretics, the risk of hyperkalemia increases; reduces the effectiveness of uricosuric and antihypertensive drugs (including beta-blockers); enhances the side effects of mineral and glucocorticoids, estrogens. Cyclosporine and gold preparations increase nephrotoxicity (by suppressing the synthesis of PG in the kidneys). Cefamandol, cefoperazone, cefotetan, valproic acid - increase the incidence of hypoprothrombinemia and the risk of bleeding. Antacids and cholestyramine reduce the absorption of indomethacin. Increases the toxicity of zidovudine (by inhibiting metabolism), in newborns it increases the risk of developing the toxic effects of aminoglycosides (because it reduces renal clearance and increases blood concentration). Myelotoxic drugs increase the manifestations of hematotoxicity.


Symptoms: nausea, vomiting, severe headache, dizziness, memory impairment, disorientation; in severe cases - paresthesia, numbness of the limbs and convulsions.

Treatment: symptomatic therapy. Hemodialysis is ineffective.

Precautions for the substance Indomethacin

Especially careful medical supervision is required when a history of allergic reactions to drugs of the "aspirin" series, "aspirin" triad, gastric ulcer and duodenal ulcer, as well as in violation of blood coagulation, hyperbilirubinemia, thrombocytopenia, parkinson's epilepsy , in childhood and old age.

The risk of cardiovascular complications. NSAIDs, incl. and indomethacin, may increase the risk of serious cardiovascular complications, incl. myocardial infarction and stroke, which can be fatal, especially with prolonged use. Patients with cardiovascular disease or cardiovascular risk factors are particularly at risk.

Risk of gastrointestinal complications. NSAIDs, incl. and indomethacin, increase the risk of serious gastrointestinal side effects, including bleeding, ulceration, and perforation of the stomach or intestines, which can be fatal, especially with prolonged use. These complications can occur at any time of use without predictive symptoms. Elderly patients are at higher risk of serious gastrointestinal complications.

When indicated in the history of allergic reactions to NSAIDs, they are used only in urgent cases.

During treatment, it is necessary to monitor the picture of peripheral blood and the functional state of the liver and kidneys. If it is necessary to determine 17-ketosteroids, the drug should be discontinued 48 hours before the study.

For eye drops: after removing contact lenses, instillation is performed after 5 minutes. In the presence of an infection or the threat of its development, local antibacterial treatment is simultaneously prescribed.

Avoid contact with the eyes, mucous membranes and open wounds of the cutaneous application forms.

During the period of treatment, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require an increased concentration of attention and speed of psychomotor reactions.



For systemic use: "aspirin" triad (combination of bronchial asthma, recurrent polyposis of the nose and paranasal sinuses, as well as intolerance to acetylsalicylic acid and drugs of the pyrazolone series), peptic ulcer of the stomach and duodenum, ulcerative colitis, bleeding (including intracranial or intracranial) from the gastrointestinal tract), congenital heart defects, in which the patent ductus arteriosus is necessary to maintain the pulmonary or systemic circulation, incl. severe coarctation of the aorta, pulmonary atresia, tetrad of Fallot; violation of color vision, diseases of the optic nerve, bronchial asthma, cirrhosis of the liver with portal hypertension, chronic heart failure, edema, arterial hypertension, blood clotting disorders (including hemophilia, prolonged bleeding time, tendency to bleeding), liver failure, chronic renal failure, hearing loss, pathology of the vestibular apparatus, deficiency of glucose-6-phosphate dehydrogenase; hematopoietic disorders (leukopenia and anemia), pregnancy, lactation, childhood (up to 14 years); for rectal use (optional): rectal bleeding, proctitis, hemorrhoids; for cutaneous use: pregnancy (III trimester - for application to large surfaces), violation of the integrity of the skin, children under 1 year of age.

Restrictions on use

For cutaneous use: pregnancy (I and II trimesters), lactation, children under 6 years of age.

In ophthalmology (eye drops): epithelial herpetic keratitis (including a history), pregnancy, lactation, childhood.

Application during pregnancy and lactation

Teratogenic effects. Teratogenicity studies conducted in rats and mice using doses of 0.5; 1.0; 2.0 and 4.0 mg / kg / day showed that at a dose of 4 mg / kg / day there was no increase in the incidence of malformations compared to the control group, with the exception of delayed ossification in fetuses (considered as secondary to a decrease in average fruit weight). In other studies in mice, using higher doses (5-15 mg / kg / day), toxicity and mortality in females, increased resorption and fetal malformations were found. A comparative study in rodents using high doses of acetylsalicylic acid showed similar effects in females and their fetuses. However, reproductive studies in animals do not always predict effects in humans. There are no adequate and strictly controlled studies in pregnant women.

Non-teratogenic effects. Since the adverse effect of NSAIDs on the cardiovascular system of the fetus (premature closure of the ductus arteriosus) is known, use should be avoided during pregnancy (especially in later stages).

The effects of indomethacin and other drugs of this class on a human fetus in the third trimester of pregnancy include: intrauterine closure of the ductus arteriosus, tricuspid valve insufficiency, and pulmonary hypertension; non-closure of the ductus arteriosus in the postnatal period, resistant to drug correction; degenerative changes in the myocardium, platelet disorders leading to bleeding, intracranial bleeding, renal dysfunction or failure, kidney damage / malformation, which can lead to renal failure, oligohydramnios, gastrointestinal bleeding or perforation, increased risk of necrotizing enterocolitis.

In studies in rats and mice treated with indomethacin at doses of 4 mg / kg / day in the last 3 days of pregnancy, there was a decrease in body weight in females and a small number of deaths in females and fetuses. An increase in the frequency of neuronal necrosis in the diencephalon in live fetuses has been noted. At a dose of 2.0 mg / kg / day, there was no increase in the frequency of neuronal necrosis compared with the control group. Administration of 0.5 or 4.0 mg / kg / day in the first 3 days of life did not increase the frequency of neuronal necrosis.

Childbirth and delivery. Studies in rats have shown that NSAIDs, like other agents that inhibit GHG synthesis, increase the number of obstructed labor, delay the onset of labor and delivery, and reduce the number of surviving pups.

The FDA category of action on the fetus is C.

Indomethacin passes into breast milk, therefore, breastfeeding should be discontinued during treatment or the use of indomethacin should be avoided during breastfeeding.

Side effects of the substance Indomethacin

From the nervous system and sensory organs: headache, dizziness, vertigo, agitation, irritability, excessive fatigue, drowsiness, depression, peripheral neuropathy, taste disturbance, hearing loss, tinnitus, diplopia, blurred vision perception, corneal opacity, conjunctivitis.

On the part of the cardiovascular system and blood (hematopoiesis, hemostasis): the development (aggravation) of chronic heart failure, tachyarrhythmia, edema syndrome, increased blood pressure, bleeding (from the gastrointestinal tract, gingival, uterine, hemorrhoidal), anemia (including autoimmune hemolytic and aplastic), leukopenia, thrombocytopenia, eosinophilia, agranulocytosis, thrombocytopenic purpura.

From the digestive tract: NSAIDs-gastropathy, nausea, vomiting, abdominal pain, heartburn, loss of appetite, diarrhea, liver dysfunction (increased activity of hepatic transaminases, hyperbilirubinemia); with prolonged use in high doses - erosive and ulcerative lesions of the gastrointestinal tract.

From the genitourinary system: impaired renal function, proteinuria, hematuria, interstitial nephritis, nephrotic syndrome, papillary necrosis.

Allergic reactions: pruritus, rash, urticaria, exfoliative dermatitis, erythema nodosum, anaphylactic shock, bronchospasm, angioedema, toxic epidermal necrolysis (Lyell's syndrome).

Others: hyperglycemia, glucosuria, hyperkalemia, photosensitivity; aseptic meningitis (more often in patients with autoimmune diseases), increased sweating; local reactions with rectal application: burning, itching of the skin, heaviness in the anorectal region, exacerbation of hemorrhoids.

When applied to the skin: allergic reactions; itching and flushing of the skin, rash at the site of application, dry skin, burning; in isolated cases - exacerbation of psoriasis; with prolonged use - systemic manifestations.

When instilled in the eye: allergic reactions; with prolonged use - corneal opacity, conjunctivitis, systemic side effects.