Ketorolac tromethamine

Ketorolac tromethamine 속성

Ketorolac tromethamine C화학적 특성, 용도, 생산

개요

Ketorolac tromethamine is a nonsteroidal antiinflammatory agent that exhibits analgesic and antipyretic activity. The compound is effective in the management of moderate to severe postoperative pain. It is, however, the first of this type of agent to be administered parenterally as an analgesic and is specifically indicated for intramuscular injection. Ketorolac represents a useful alternative to the narcotic analgesics due to its lack of abuse potential.

화학적 성질

A carboxylic acid derivative nonsteroidal antiinflammatory agent, ketorolac tromethamine occurs as an off-white crystalline powder with a pKa of 3.54 (in water). More than 500 mg are soluble in one mL of water at room temperature. The commercially available injection is a clear, slightly yellow solution with a pH of 6.9 – 7.9. Sodium chloride is added to make the solution isotonic. Ketorolac tromethamine may also be known as RS-37619-00- 31-3; many trade names are available.

용도

Cyclo-oxygenase inhibitor; analgesic; anti-inflammatory.

정의

ChEBI: An organoammonium salt resulting from the mixture of equimolar amounts of ketorolac and tromethamine (tris). It has potent non-sedating analgesic and moderate anti-inflammatory effects. It is used in the short-term management of post-operative pain, and in eye drops to relieve the ocular itching associated with seasonal allergic conjunctivitis.

Indications

Ketorolac tromethamine is a pyrrolol-pyrrole nonsteroidal anti- inflammatory agent that inhibits prostaglandin formation. Prostaglandins mediate inflammation within the eye by disrupting the blood-aqueous barrier, inducing vasodilation and increasing intraocular pressure. Prostaglandins may also cause iris sphincter constriction (miosis) independent of cholinergic mechanisms. Ketorolac tromethamine is marketed for use before cataract extraction in human patients (to prevent miosis during surgery) and for control of post surgical inflammation, especially following cataract surgery. It is also approved for management of conjunctivitis associated with seasonal allergy in people. In veterinary medicine, ketorolac tromethamine is primarily used to control surgical or nonsurgical uveitis particularly in cases with concurrent corneal bacterial infection or ulceration when topical corticosteroids are contraindicated. It is also used in diabetic patients, especially smaller patients, adversely affected by systemic uptake of topically applied corticosteroids. Nonsteroidal agents like ketorolac tromethamine can be combined with topical steroids in patients with severe uveal inflammation.

일반 설명

Pharmaceutical secondary standards for application in quality control, provide pharma laboratories and manufacturers with a convenient and cost-effective alternative to the preparation of in-house working standards. Ketorolac Tromethamine belongs to the class of non-steroidal anti-inflammatory drugs, and its mode of action involves the inhibition of the bodily synthesis of prostagladins. It exhibits anti-inflammatory, antipyretic and analgesic effects.

Pharmacokinetics

After oral administration, ketorolac is rapidly absorbed; in dogs peak levels occur in about 50 minutes and oral bioavailability is about 50 – 75%.
Ketorolac is distributed marginally through the body. It does not appear to cross the blood-brain barrier and is highly bound to plasma proteins (99%). The volume of distribution in dogs is reported to be about 0.33 – 0.42 L/kg (similar in humans). The drug does cross the placenta.
Ketorolac is primarily metabolized via glucuronidation and hydroxylation. Both unchanged drug and metabolites are excreted mainly in the urine. Patients with diminished renal function will have longer elimination times than normal. In normal dogs, the elimination half-life is between 4 – 8 hours.

Pharmacology

Like other NSAIDs, ketorolac exhibits analgesic, antiinflammatory, and antipyretic activity probably through its inhibition of cyclooxygenase with resultant impediment of prostaglandin synthesis. Ketorolac may exhibit a more potent analgesic effect than some other NSAIDs. It inhibits both COX-1 and COX-2 receptors.

부작용

The manufacturer indicates that ketorolac tromethamine does not enhance the spread of preexisting corneal fungal, viral or bacterial infections in animal models. Ketorolac tromethamine does not in and of itself induce postoperative pressure elevation other then that which frequently follows cataract extraction in people and animals.

Safety Profile

Ketorolac does cross the placenta. In humans, the FDA categorizes this drug as category C for use during the first two trimesters of pregnancy (Animal studies have shown an adverse effect on the fetus, but there are no adequate studies in humans; or there are no animal reproduction studies and no adequate studies in humans.) In humans, all NSAIDs are assigned to category D for use during pregnancy during the third trimester or near delivery (There is evidence of human fetal risk, but the potential benefits from the use of the drug in pregnant women may be acceptable despite its potential risks.) Most NSAIDs are excreted in milk. Ketorolac was detected in human breast milk at a maximum milk:plasma ratio of 0.037. It is unlikely to pose great risk to nursing offspring.

Overdosage

Limited information is available. The oral LD50 is 200 mg/kg in mice. GI effects, including GI ulceration are likely in overdoses in small animals. Metabolic acidosis was reported in one human patient. Consider GI emptying in large overdoses; patients should be monitored for GI bleeding. Treat ulcers with sucralfate; consider giving misoprostol early.

주의 사항

Ketorolac is relatively contraindicated in patients with a history of, or preexisting, hematologic, renal or hepatic disease. It is contraindicated in patients with active GI ulcers or with a history of hypersensitivity to the drug. It should be used cautiously in patients with a history of GI ulcers, or heart failure (may cause fluid retention), and in geriatric patients. Animals suffering from inflammation secondary to concomitant infection, should receive appropriate antimicrobial therapy. Because ketorolac has a tendency to cause gastric erosion and ulcers in dogs, long-term use (>3 days) is not recommended in this species.

Ketorolac tromethamine 준비 용품 및 원자재

원자재

준비 용품

Ketorolac tromethamine 공급 업체

공급자	전화	이메일	국가	제품 수	이점
airuikechemical co., ltd.	+undefined86-15315557071	sales05@airuikechemical.com	China	994	58
Capot Chemical Co.,Ltd.	571-85586718 +8613336195806	sales@capotchem.com	China	29797	60
Henan Tianfu Chemical Co.,Ltd.	+86-0371-55170693 +86-19937530512	info@tianfuchem.com	China	21689	55
Hangzhou FandaChem Co.,Ltd.	008657128800458; +8615858145714	fandachem@gmail.com	China	9341	55
Nanjing ChemLin Chemical Industry Co., Ltd.	025-83697070	product@chemlin.com.cn	CHINA	3012	60
career henan chemical co	+86-0371-86658258	sales@coreychem.com	China	29914	58
Jinan Shengqi pharmaceutical Co,Ltd	86+18663751872	christine@shengqipharm.com	CHINA	491	58
Xiamen AmoyChem Co., Ltd	+86-592-6051114 +8618959220845	sales@amoychem.com	China	6387	58
Hubei xin bonus chemical co. LTD	86-13657291602	linda@hubeijusheng.com	CHINA	22968	58
Chongqing Chemdad Co., Ltd	+86-023-61398051 +8613650506873	sales@chemdad.com	China	39916	58

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