• Code CAS
Most popular brand: Indocin
Active ingredient: Indomethacin
Available dosage forms: 25, 50, 75 mg
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Indomethacin general information
Breast-feedingProbenecid hasn’t been reported to cause issues in nursing babies. So, one ought to offer detailed information about their health care history to a physician prior to taking indomethacin. Doctors continue to be unable to get the cause of myositis ossificans. Make it quite strong in order to ensure it is high in Tannic acid.
As with the remainder of the muscles within your body, it is quite simple to sprain your chest muscles too, causing a painful sensation in the territory. This results within the person sitting in a single spot with the legs in a stationary position, thus resulting in swelling. Topical NSAIDs are frequently utilized to ease musculoskeletal pain caused by sports-related injuries. Swollen ankles might occur as an immediate effect of the surgery, or it might occur because you’ve become inactive after it.
Often, pain relief becomes the principal concern for the patient instead of disease control. Pain is likewise the primary symptom of several other illnesses and hence pain relief is the fundamental and among the most essential elements of treatment. The pain in the aforementioned condition is unbearable, still, it can be medicated with medications. Most lung infections normally have similar symptoms.
The details presented above reveal that gabapentin is really a multi-purpose drug that’s useful in the therapy for different varieties of diseases and health conditions. Although NSAIDs are generally taken orally, they could be administered intravenously, transdermally, and even rectally within the form of the suppository to ease pain. Indomethacin is beneficial as it is helpful to decrease the pain. Since the utilization of gabapentin contributes to accumulation of toxins, taking the vital precautions mentioned above becomes extremely important.
There is a single theory about the way that it works in treating seizure. Ergo, taking selective NSAIDs doesn’t alter the stomach lining, however at the identical time, they provide pain relief. Several research have pointed out that people using non-steroidal anti-inflammatory drugs for a prolonged time period, can get a greater risk of strokes as well as heart attacks. Follow the healing techniques we’ve explained within the aforementioned content religiously to knock out sinus infection fast.
Costochondritis symptoms are typical for children and men too. The symptoms differ from person to person. As previously mentioned, urine color too can indicate health conditions. Cholecystitis is distinguished by pain within the perfect upper quadrant of the abdomen.
Sterilized paraffin wax can assist you in relieving a number of the pain and safeguard the sunburned region of the skin. To prevent such unwanted side effects, it is best to consult the physician before giving any suppositories. Other side effects might occur that usually don’t need medical attention. Regardless, it is optimum to ask your doctor.
Bacterial infections are typically cured by taking the total course of prescribed antibiotics in accordance with the instructions of the physician. High doses of the drug are primarily responsible for the side-effects. Either way, augmenting the dosage raises the chance of side consequences.
Indometacin (Indomethacin): instruction, and the use of a formula
Feature substance Indomethacin
NSAIDs. indole acetic acid derivative.
A white or slightly yellow powder, odorless or almost odorless. Practically insoluble in water. Sparingly soluble in ethanol, chloroform, ether. It is soluble in alkaline solutions.
Mode of action – anti-inflammatory, antipyretic, analgesic.
inhibits cyclooxygenase (COX – 1 and COX – 2), reduces the synthesis of GHGs. causing the outbreak of inflammation in the development of pain, fever and an increase in tissue permeability. Has antiplatelet effect.
It is the weakening or disappearance of pain rheumatic and rheumatic character (including pain in the joints at rest and during movement, reduces morning stiffness and swelling of joints, increases range of motion; in inflammatory processes that occur after surgery and injuries quickly facilitates both spontaneous pain and pain on movement and reduces inflammatory swelling at the wound site).
After oral administration of a single dose of 25 mg or 50 mg is rapidly absorbed, T max ; about 2 hours; when using rectal absorption rate is higher. When ingestion bioavailability of 90 – 98% for rectal application somewhat less ; 80 – 90%, which is probably due to insufficient to ensure complete absorption of the retention time of the suppository (less than 1 hour). Binding to plasma proteins ; 90 – 98%. T 1/2 ; 4 –. If nine hours daily intake of 25 or 50 mg of Indomethacin three times daily average equilibrium concentration 1.4 times higher than the concentration after a single dose. Biotransformiroetsa mainly in the liver. The plasma is in the form of unchanged substance and desmethyl -, desbenzoyl – and desmethyl – dezbenzoilmetabolitov present in an unconjugated form. Excreted mainly kidneys ; 70% (30% ; in unchanged form) and GI ; thirty%. It passes through the BBB. placenta, enters the breast milk. Not removed by hemodialysis.
When the instillation of eye drops enters the anterior chamber of the eye. After a single instillation is determined by the moisture front of the camera within a few hours.
carcinogenicity, mutagenicity, effects on fertility
The 81 – when applied weekly chronic toxicity study in rats orally at doses of up to 1 mg / kg / day revealed no carcinogenic effect. In carcinogenicity studies in rats (study period ; 73 – 110 weeks) and mice (study period ; 62 – 88 weeks) at doses up to 1.5 mg / kg / day indomethacin induced neoplastic or hyperplastic changes.
There were no mutagennocti indomethacin in some bacterial tests in vitro (Ames test, the test with E.Coli with / without metabolic activation) and in a series of tests in vivo . including a test for sex-linked recessive flew Drosophyla, micronucleus test in mice.
In the reproduction studies, including two generations, at dose levels up to 0.5 mg / kg / day indomethacin had no effect on fertility in rats and mice.
Application of the substance Indomethacin
for systemic use (inside, in / m. Rectally)
Inflammatory and degenerative diseases of the musculoskeletal – musculoskeletal system: rheumatoid, psoriatic, juvenile chronic arthritis, arthritis, Paget’s disease, and Reiter, neuralgic amyotrophy (disease Personeydzha – Turner), ankylosing spondylitis (ankylosing spondylitis), gouty arthritis, rheumatism. Pain: headache (including the menstrual syndrome), and toothache, lumbago, sciatica, neuralgia, myalgia, after injuries and surgical interventions, accompanied by inflammation, bursitis and tendonitis (the most effective in the localization of the shoulder and forearm). Algomenorrhea, to maintain pregnancy, Bartter syndrome (secondary hyperaldosteronism), pericarditis (symptomatic treatment), childbirth (as analgesic and tocolytic agent in preterm labor), inflammation of the pelvis, including adnexitis, cleft arterial duct. Infectious – inflammatory diseases of ENT – organs with marked pain syndrome (in the complex therapy): pharyngitis, tonsillitis, otitis media. Feverish syndrome (including with chlamydia, other lymphomas and liver metastases with & oacute; solid tumors) ; in case of failure of aspirin and paracetamol.
For topical use (for application to the skin)
due to traumatic inflammation of the tendons, ligaments, muscles and joints (due to strains, sprains, and bruises after the load). Localized forms of inflammation of soft tissues, including tenosynovitis, tendinitis, a syndrome of “shoulder – hand”, bursitis, myalgia; radiculitis (sciatica, lumbago). Inflammatory and degenerative diseases of the musculo – skeletal system (deforming osteoarthritis, rheumatoid arthritis, psoriatic arthritis, rheumatoid arthritis, frozen shoulder, ankylosing spondylitis, low back pain with radicular syndrome) except for degenerative disease of the hip joints.
In ophthalmology (eye drops): inhibition of miosis during cataract surgery; inflammation caused by surgery; prevention and treatment of cystoid macular edema after cataract surgery; treatment and prevention of inflammation of the eyeball; non-infectious conjunctivitis.
In dentistry (systemic and cutaneous application): arthritis and arthrosis of the temporo – mandibular joint, inflammatory diseases of the oral tissues, myalgia, neuralgia, postoperative period.
for systemic use: «Aspirin” triad (a combination of asthma, recurrent nasal polyposis, and paranasal sinuses and intolerance of aspirin and drugs pirazolonovogo series), gastric ulcer and duodenal ulcer, ulcerative colitis bleeding (including intracranial or gastrointestinal tract), congenital heart disease, in which the ductus arteriosus is necessary for maintaining the pulmonary or systemic circulation, including severe coarctation of the aorta, pulmonary artery atresia, tetralogy of Fallot; violation of color vision, optic nerve disease, asthma, liver cirrhosis with portal hypertension, chronic heart failure, edema, hypertension, clotting disorders (including hemophilia, prolonged bleeding, bleeding tendency), hepatic failure, chronic kidney failure, hearing loss, vestibular pathology, deficiency of glucose – 6 – phosphate dehydrogenase; disorders of blood (leukopenia and anemia), pregnancy, lactation, children’s age (14 years); for rectal use (optional): rectal bleeding, proctitis, hemorrhoids; for cutaneous application : pregnancy (III trimester ; for use on large surfaces), violation of the integrity of skin, children under 1 year.
Restrictions on the use
For cutaneous application . pregnancy (I and II trimester), lactation, children under 6 years of age.
In ophthalmology (eye drops) . epithelial herpetic keratitis (including history), pregnancy, lactation, children’s age.
Application of pregnancy and breastfeeding
Teratogenic effects of teratogenicity studies conducted in rats and mice at doses of 0.5.; 1.0; 2.0 and 4.0 mg / kg / day. We showed that at a dose of 4 mg / kg / day there was no increase in the frequency of malformations as compared to the control group, except for delayed ossification in fetuses (seen as secondary in relation to the average weight loss of fruits). In other studies in mice when using higher doses (5 – 15 mg / kg / day) was found to toxicity and lethality of females, increased resorption and fetal malformations. Comparative study in rodents using high doses of aspirin showed similar effects in females and their fetuses. However, reproductive studies in animals do not always predict effects in humans. Adequate and well-controlled studies in pregnant women have not done.
Nonteratogenic effects Since it is known adverse effects of NSAIDs on the cardio -. Vascular system of the fetus (premature closure of the ductus arteriosus), the use should be avoided during pregnancy (especially in the later stages).
Effects of indomethacin and other drugs in this class on the human fetus in III trimester of pregnancy include intrauterine closure of the ductus arteriosus, tricuspid valve and pulmonary hypertension; unclosed ductus arteriosus in the postnatal period, resistance to drug correction; degenerative changes in the myocardium, platelet disorders, leading to bleeding, intracranial bleeding, renal dysfunction or failure, failure / defect of kidney development, which can lead to renal failure, oligohydramnios, gastro – intestinal bleeding or perforation, increased risk of necrotising enterocolitis
The studies in rats and mice given indomethacin at a dose of 4 mg / kg / day in the last 3 days of pregnancy, there was a reduction in body weight of females and a small number of deaths and female fetuses. It was observed increase in the incidence of neuronal necrosis in the diencephalon in live births fruit. At a dose of 2.0 mg / kg / day increased frequency of neuronal necrosis was not compared with the control group. Introduction 0.5 or 4.0 mg / kg / day in the first 3 days of life did not cause any increase in the frequency of neuronal necrosis.
labor and delivery. In studies in rats showed that the NSAIDs. as well as other means of inhibiting the synthesis of GHGs. increase the number of cases of obstructed labor, causing delay in the onset of labor and delivery, reducing the number of surviving pups.
Category effects on the fetus by FDA ; C.
Indomethacin passes into breast milk, so breast-feeding should be discontinued during treatment and avoid the use of indomethacin during breastfeeding.
Side effects of substance Indomethacin
Systemic side effects
From the nervous system and sensory organs: headache, dizziness, vertigo, agitation, irritability, excessive tiredness, drowsiness, depression, peripheral neuropathy, taste disturbance, hearing loss, tinnitus, diplopia , blurred vision, corneal opacity, conjunctivitis.
From the cardio – vascular system and blood (blood, hemostasis): development (worsening) of chronic heart failure, tachyarrhythmia, edema syndrome, increased blood pressure. bleeding (from the gastrointestinal tract. gingival, uterine, hemorrhoids), anemia (including autoimmune hemolytic and aplastic), leukopenia, thrombocytopenia, eosinophilia, agranulocytosis, thrombocytopenic purpura.
From the digestive tract: NSAID – gastropathy, nausea, vomiting, abdominal pain, heartburn, loss of appetite, diarrhea, abnormal liver function (elevated liver transaminases, hyperbilirubinemia); long-term use at high doses ; erosive – ulcerative lesions gastrointestinal.
With the genitourinary system: renal failure, proteinuria, hematuria, interstitial nephritis, nephrotic syndrome, necrosis papillae.
Allergic reactions: pruritus, rash, urticaria, exfoliative dermatitis, erythema nodosum, anaphylactic shock, bronchospasm, angioedema, toxic epidermal necrolysis (Lyell’s syndrome).
Other: hyperglycemia, glycosuria, hyperkalemia, photosensitivity; aseptic meningitis (usually in patients with autoimmune diseases), increased sweating; local reactions at the rectal: burning, itching, heaviness in the anorectal region, exacerbation of hemorrhoids.
When applied to the skin: allergic reactions; itching and skin flushing, rash at the site of application, dry skin, burning sensation; in a few cases ; exacerbation of psoriasis; long-term use ; systemic manifestations.
With instillation of the eye: allergic reactions; long-term use ; corneal opacities, conjunctivitis, systemic side effects.
Reduces the diuretic effect of potassium-sparing, thiazide and loop diuretics. Increases (mutually) the risk of side effects (primarily gastrointestinal lesions) to other NSAIDs. Increasing the concentration of digoxin in plasma methotrexate and drugs Li +. which may lead to increased toxicity. Sharing with paracetamol increases the risk of nephrotoxicity manifestations. Ethanol, colchicine, corticosteroids and corticotropin increase the risk of bleeding in the gastrointestinal tract. Enhances hypoglycemic effect of insulin and oral hypoglycemic drugs; It enhances the effect of anticoagulants, antiplatelet agents, fibrinolytic agents (alteplase, streptokinase and urokinase), and increases the risk of bleeding. Against the background of the use of potassium-sparing diuretics increase the risk of hyperkalemia; reduces the effectiveness of uricosuric and antihypertensive drugs (including beta – blockers); It increases the side effects of mineral – and glucocorticoid, estrogen. Cyclosporine and gold preparations increase the nephrotoxicity (due to suppression of PG synthesis in the kidneys). Cefamandole, ceftazidime, tsefotetan, valproic acid ; gipoprotrombinemii increase the incidence of, and risk of bleeding. Antacids and cholestyramine reduce the absorption of indomethacin. Enhances AZT toxicity (due to inhibition of metabolism), in newborns an increased risk of toxic effects of aminoglycosides (as reduced renal clearance and increases in blood concentration). Myelotoxic drugs increase the expression gematotoksichnosti.
ACE inhibitors and angiotensin II
NSAIDs may reduce the antihypertensive effect of ACE inhibitors and angiotensin II receptor antagonists. Indomethacin may reduce the antihypertensive effect of captopril and losartan. These interactions should be considered in patients taking NSAIDs concurrently with ACE inhibitors or angiotensin II. In some patients with compromised renal function concomitant use of NSAIDs and ACE inhibitors or angiotensin II antagonists may result in further deterioration of renal function, including possible acute renal failure, which is usually reversible.
Symptoms: nausea, vomiting, severe headache, dizziness, memory impairment, disorientation; in severe cases ; paresthesia, numbness and cramps.
Treatment: symptomatic therapy. Hemodialysis is ineffective.
Dosing and Administration
Inside, in / m. rectally . on skin, conjunctival. The mode set individually, depending on the indication, the severity of the disease and other factors.
Inside: adults administered in an initial dose of 25 mg of 2 – 3 times a day, in case of insufficient magnitude of the effect ; 50 mg three times a day, retard tablets (75 mg) ; 1 – 2 times a day with a maximum daily dose of ; 200 mg. With prolonged use of the maximum daily dose should not exceed 75 mg. Upon reaching the effect of treatment should be continued for 4 weeks in the same or a reduced dose.
For the treatment of acute exacerbation of chronic or cupping process is introduced into / m to 60 mg of 1 – 2 times a day for 7 – 14 days and then move on ingestion or rectal administration. Rectal: after intestinal release, 50 mg of 1 – 3 times daily or 100 mg at bedtime; the maximum daily dose of ; 200 mg. Children over the age of 14 ; for 1,5 – 2,5 mg / kg / day.
Cutaneous: rub a thin layer of the skin over the painful parts of the body (applied only to undamaged areas) 3 – 4 times per day.
Kongungualno: inhibiting intraoperative miosis 1 drop was instilled into the conjunctival sac for 2 hours at intervals of 30 minutes (4 times) before surgery. In other testimony ; 1 drop of 3 – 4 times a day.
In dentistry, inside, adult ; 25 – 50 mg 3 – 4 times a day; locally ; 10% ointment is rubbed into the skin (applied only to undamaged portions) 3 – 4 times a day.
Precautions substance Indomethacin
Particularly close medical supervision is required when specifying a history of allergic reactions to drugs, “aspirin” series, “aspirin” triad, stomach ulcer and duodenal ulcers, as well as problems with blood clotting, hyperbilirubinemia, thrombocytopenia, epilepsy, Parkinson’s disease, depression, in childhood and old age.
The risk of cardio – vascular complications NSAIDs.. including and indomethacin, may cause an increased risk of serious cardio – vascular complications, including myocardial infarction and stroke, which can lead to death, especially after prolonged use. In patients with cardio – vascular disease or risk factors for heart development -. Vascular disease risk is particularly high
The risk of gastro – intestinal complications NSAIDs.. including and indomethacin, cause an increased risk of serious side effects from the gastrointestinal tract. including bleeding, ulceration and perforation of the stomach or intestines, which can be fatal, especially in long-term use.
During the period of treatment must be careful when driving and occupation of other potentially hazardous activities that require high concentration and psychomotor speed reactions.