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Indometacin

Indometacin

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PRODUCT NAME: Indometacin
CAS NUMBER: 53-86-1
Indometacin or indomethacin is a non-steroidal anti-inflammatory drug (NSAID) commonly used as a prescription medication to reduce fever, pain, stiffness, and swelling. It works by inhibiting the production of prostaglandins, molecules known to cause these symptoms. It is marketed under more than seventy different trade names.

MP 155-162 °C
storage temp.
Store at RT
solubility ethanol: 50 mg/mL, clear, yellow-green
Stability Stable. Incompatible with strong oxidizing agents.
anti-inflammatory analgesic Indomethacin is a kind of stronger corticoid anti-inflammatory and antipyretic and analgesic, by inhibiting cyclooxygenase reducing the synthesis of prostaglandin (PG), to prevent the formation of the nere impulses, inflammation tissue inhibiting inflammatory reaction, including inhibition of leukocyte chemotaxis and lysosomal enzyme release, etc., and produce antipyretic, analgesic and anti-inflammatory effects. Indomethacin anti-inflammatory, antipyretic effect is very strong, its anti-inflammatory effect is better than bute, 84 times better than hydrocortisone, and sugar cortical hormone, used in combination with aspirin, bute, can reduce their dosage, toxic and side effects, improve curative effect; Second is antipyretic effect, 10 times than amidopyrine ;its analgesic action is weak , only to the inflammatory pain has obvious analgesic effect, but the effect is good for inflammatory pain than Baotai loose, analgin and salicylic acid. Clinical is mainly used for the salicylic acid, drugs are less tolerance or curative effect is not obvious in the acute and chronic rheumatic or rheumatoid arthritis, ankylosing spondylitis, slippery bursa phlogistic, tenosynovitis, articular capsulitis, osteoarthritis and acute gout and cancerous pain, etc.In recent years, the researchers try to use indomethacin biliary colic, dysmenorrhea, migraine, glomerulonephritis, polyuria, salmonella gastroenteritis, orthostatic hypotension, bart syndrome and so on, all have good curative effect.It can also be used to treat eye pigment meningitis, keratitis, scleritis, glaucoma and fever caused by cancer or other difficult to control the fever. Dermatologist for lupus erythematosus (sle), white plug syndrome, scleroderma, nodular erythema, herpes zoster, joint type of psoriasis, etc. photosensitive dermatitis induced by topical treatment of eczema, allergic dermatitis, and local pain.
Pharmacokinetics Oral medicine absorbed quickly and completely, can absorb more than 90% of the dosage of food with in 4 h, take medicine of acid containing aluminum and magnesium can be slightly slowed absorption, plasma protein conjugation rate is about 99%. After oral 25 mg, tmax is 1 ~ 4 h, the blood medicine peak concentration (Cmax) is 1.4 mu g/ml, when 50 mg, Cmax is 2.8 mu g/ml; Half-life (t1/2) of an average is 4.5 h, premature extended obviously. A small amount of indomethacin can through the blood-brain barrier. And through the placenta.This article in the liver metabolism go methyl chloride and chlorobenzene formyl chloride, and can be hydrolyzed into recycle indomethacin to absorb. Renal excretion from 60%, 10% ~ 20% in prototype discharge; Part with droppings.33% from the bile excretion, 1.5% were prototype;In the breast milk also has a discharge (up to 0.5 ~ 2.0 mg daily).This product can not be dialysis to remove.
Adverse reactions Adverse reactions of Indomethacin are high incidence , common adverse reactions are as follows:
1. nausea, vomiting, abdominal pain, diarrhea, anorexia, serious ulcers can occur and cause bleeding and perforation. After dinner, that can reduce the incidence.
2. common headache, dizziness, fatigue, occasional seizures, mental derangement, syncope, etc. Should be paid attention to in due course.
3.the skin pruritus, erythema, urticaria, and one of the few of asthma, breathing problems and even breathing, circulation inhibition.
4.Inhibition of hematopoietic system such as granulocytopenia, aplastic anemia, thrombocytopenia, and so on. Although rare, but more severe consequences.There are also some other similar to aspirin reaction, notes are also the same.
matters need attention 1.indomethacin and aspirin have cross allergic. Caused by aspirin allergic asthmatic patients, the application of this product can be induced bronchospasm. Other non steroidal anti-inflammatory drugs to which are allergic may also be allergic to this product.
2.This product is contraindicated with active ulcer disease, ulcerative colitis and history, epilepsy, Parkinson’s disease, mental disease, liver and kidney function, the goods or aspirin or other nonsteroidal anti-inflammatory drug allergic person, angioedema or bronchial asthma. This product for the last 3 months of pregnancy can make fetal ductus arteriosus closure and result in persistent pulmonary hypertension, so pregnant women, disabled. This product can be discharged from the milk, breast-feeding women also disable.
3.This product is used for patients with cardiac insufficiency, and hypertension (because this product sodium can lead to water retention, hemophilia and other patients with hemorrhagic disease (because this product can make the bleeding time prolonged, aggravate bleeding tendency), aplastic anemia, granulocytopenia disease patients (this product is inhibition of hematopoietic system).Age < 14 years old children should not be commonly used drug, When it is applied,it should be closely observed.Easily occur in elderly patients with renal toxicity, which should also be careful.
4.Because indomethacin has inhibition to the platelet aggregation, which can make the bleeding time prolonged, the role after the drug was stopped sustainable. During the blood urea nitrogen and serum creatinine,levels are also often higher. During the medication,it should be regularly check routine blood and liver and kidney function. Case reports referred to in this article that the product can lead to corneal composure and retinal change (including macular degeneration), if it comes to the blurred vision eye exams should be done immediately.
5.Drug overdose (especially when dose > 150 mg a day) is easy to cause toxic reactions such as nausea, vomiting, tension headaches, sleepiness, spirit, behavior disorders, etc., with vomiting or gastric lavage, symptomatic and supportive treatment.
chemical property White or slightly yellow crystalline powder. Melting point is 158-162℃, soluble in acetone, slightly soluble in ethanol, chloroform, ether, almost insoluble in water.
methods of production Para aminophenylmethylether is through diazotization, reduction, cyclization, hydrolysis, acidification to get indomethacin.
classification of toxicity Highly toxic.
acute toxicity Oral administration: LD50 2.42 mg / kg in rats; oral administration of 11.84 mg / kg of LD50: in mice.
Combustible hazard characteristics Open flame fuel; high heat decomposition of toxic chloride and nitrogen oxide gas.
Storage and transportation characteristics Low temperature and dry air ventilation; and oxidant, food additives separately.
Extinguisher Foam, fog water, sand, carbon dioxide.
Air & Water Reactions Practically insoluble in water. Decomposes in alkali.
Reactivity Profile A weak organic acid.
Fire Hazard Non-combustible, substance itself does not burn but may decompose upon heating to produce corrosive and/or toxic fumes. Some are oxidizers and may ignite combustibles (wood, paper, oil, clothing, etc.). Contact with metals may evolve flammable hydrogen gas. Containers may explode when heated.
Biological Activity Cyclooxgenase (COX) inhibitor; displays selectivity for COX-1 (IC 50 values are 230 and 630 nM for human COX-1 and COX-2 respectively). Widely used anti-inflammatory agent.
usage and dosage 1.Anti-rheumatism: adult dosage: oral: early quantity from 25 to 50 mg each time, 2 ~ 4 times a day, immediately take at food service or after a meal. Such as good tolerance, the daily dosage can be increased from 25 to 50 mg per week, the most mount should not be more than 200 mg a day. Arthritis patients such as persistent pain at night or morning stiffness, can give quantity of 100 mg in bed all day.
2. Resistance to gout: oral: At the beginning quantity is 100 mg once, then 50 mg, three times a day, until the pain relief, and then gradually reduced as soon as possible, until the drug withdrawal.
3. Antifebrile: adult dosage: oral: 25 ~ 50 mg each time, 3 ~ 4 times daily.Rectal drug delivery: every time 50 mg, 50 to 100 mg per day. Pediatric dosage: oral: 0.5 ~ 1 mg/kg each time, 3 times a day.
Application 1.The product is anti-inflammatory, and antipyretic effect is obvious, mainly is used for salicylates to tolerance or the effect is not significant rheumatism and arthritis, ankylosing light spondylitis, osteoarthritis.
2.Non steroid anti-inflammatory analgesic
Usage Inhibits cyclooxygenase (IC50=0.1uM) selectively over liposygenases (IC50=100uM for 5-,12- and 15-LO). A clinically useful NAISD
Usage antiinflammatory, antipyretic, analgesic
Item Requirement Result
Description White crystalline powder White crystalline powder
Melting point 289-294°C 291-293°C
Identification IR Identical
Assay ≥ 98.5% 99.2%
Heavy metal ≤ 10ppm ≤ 10ppm
Loss on drying ≤ 1.0% ≤ 1.0%
Ask ≤ 0.1% ≤ 0.1%

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