【药物名称】 中文通用名称:酮洛酸氨丁三醇 英文通用名称:Ketorolac Tromethamine 其它名称:安贺拉、酮酪酸氨丁三醇、酮洛来克、酮洛酸、酮洛酸氨基丁三醇、痛力克、痛立消、Acula、Acular、Droal、Ketanov、Ketorol、Ketorolac、Ketorolac Trometamol、Ketorolac Tromethamin、Ketorolacum、Ketorolacum Tromethaminum、Tonum、Toradol、Torolac 【功效】 1.用于中、重度疼痛(如术后、骨折、扭伤疼痛、牙痛及癌性疼痛等)的止痛。 2.本药滴眼液用于治疗眼科手术后的炎症、季节变应性结膜炎等(国外资料)。 【药理】 1.药效学 本药为吡咯酸的衍生物,属非甾体类抗炎药,其结构与托美丁(Tolmtin)和吲哚美辛等药物类似。通过抑制前列腺素环氧酶(不与脑中的阿片受体μ、δ、κ等作用)而抑制前列腺素的生物合成,从而产生镇痛、解热和抗炎作用。镇痛作用与阿司匹林近似,肌内注射后镇痛作用与中等量吗啡近似。本药还可抑制由花生四烯酸和胶原诱导的血小板聚集作用,但不抑制二磷酸腺苷(ADP)的诱导作用。 2.药动学 本药肌内注射吸收迅速完全,注射30mg在50分钟后平均血药浓度峰值为2.2μg/ml;口服吸收完全,给药后24小时可达稳态血药浓度。关节腔内药物浓度为血中浓度50%以上。口服给药或肌内注射时镇痛作用可持续6-8小时。药物可通过胎盘。口服生物利用度为80%-100%。本药血浆蛋白结合率达99%。原形药及其代谢产物主要经肾脏排泄,少量随粪便排出。青壮年的半衰期为5.3小时;老年人(平均72岁)的半衰期延长至7小时;肾功能不全者的半衰期延长至9.62-9.91小时。 【注意事项】 1.禁忌症 (1)对本药、阿司匹林或其它非甾体类抗炎药过敏者。(2)鼻息肉综合征患者(国外资料)。(3)血管性水肿患者(国外资料)。(4)有高危出血倾向者(国外资料)。(5)活动性消化性溃疡患者。(6)肝肾疾病、心脏病、高血压患者。(7)孕妇。(8)儿童。 2.慎用 尚不明确。 3.药物对妊娠的影响 本药不宜用于分娩镇痛。美国药品和食品管理局(FDA)对本药的妊娠安全性分级为C级。 4.药物对哺乳的影响 尚不明确。 【不良反应】 1.常见精神神经系统不良反应(如嗜睡、头晕、头痛、思维异常、抑郁、欣快、失眠)及消化道不良反应(如恶心、呕吐、腹痛、消化不良)。 2.偶见注射部位疼痛、出汗增多、皮肤瘙痒、皮下出血及紫绀。 3.其它不良反应有口干、肌肉痛、心悸、血管扩张等。 4.长期使用可引起皮疹、支气管痉挛、休克等过敏反应和肾功能不全。 5.现已有因消化道出血、术后出血、急性肾功能不全和过敏反应而致死的报道。 【国外不良反应参考】 1.血液 有一例接受本药治疗关节痛复发时,引起溶血性尿毒症的报道。 2.心血管系统 临床试验中,有受试者出现水肿和高血压。尚有发生心悸、晕厥、低血压和皮肤潮红的报道。 3.中枢神经系统 临床试验中,有引起头痛、头晕、嗜睡、神经过敏和感觉异常的报道。但因许多患者的用药时间为大手术后的恢复期,故这些反应与本药的关系尚不明确。 4.代谢/内分泌系统 有使用本药后引起高血钾和体重增加的报道。 5.消化系统 本药可能引起溃疡形成、出血和穿孔,老年人大剂量使用时更易出现。也可引起恶心、消化不良、腹痛、腹泻、肝功能检测值升高等。很少引起胰腺炎。 6.泌尿生殖系统 临床试验中,本药引起血尿、蛋白尿、少尿、尿潴留、多尿和尿频的发生率大于1%。肾炎、急性肾衰竭和溶血性尿毒症也有报道。 7.眼 使用本药眼用制剂后,可引起一过性刺痛和烧灼感。其它眼部不良反应还有过敏反应、浅表性角膜炎、眼部刺激、角膜水肿或虹膜炎等。 8.呼吸系统 本药在临床试验中有引起支气管痉挛和过敏反应的报道,出现这些症状的很多患者曾有阿司匹林过敏、哮喘和鼻息肉三联征病史。 9.其它 有用药后出现听力丧失、耳鸣、头痛及引起血管性水肿的报道。还可出现注射部位疼痛。肌注后有皮肤瘙痒、烧灼感、出汗和寒战的报道,但少见。 【药物相互作用】 ·药物-药物相互作用 1.本药与其它非甾体类抗炎药合用,不良反应增加,应避免合用。 2.合用利尿药可使本药不良反应增加。 3.本药与吗啡或盐酸哌替啶合用治疗术后疼痛,无明显不良相互作用。 4.与某些抗感染药如β-内酰胺类的青霉素、头孢菌素及氨基糖苷类抗生素、止吐药、泻药、支气管扩张药等合用,无药物相互作用。 ·药物-食物相互作用 食物可降低本药的吸收速度,但不影响吸收率。 【给药说明】 1.本药可延长出血时间,故不作为预防性镇痛药用于大手术前和术中。 2.本药若与吗啡或哌替啶合用,可减少后两者用量。 3.本药不宜长期口服用于治疗慢性疼痛。 【用法与用量】 成人: ·常规剂量 ·口服给药 一次10mg,一日2次。剧痛时可增至一次20mg。用药时间不宜超过2日。 ·肌内注射 一次30-60mg,一日极量为90mg。首次注射后,可每6小时注射20-30mg。用药不宜超过3日。 ·静脉注射 用于重度疼痛,一次10-30mg。 ·经眼给药 一次1-2滴,一日3次。 ·肾功能不全时剂量:推荐用低剂量。 ·老年人剂量:65岁以上老人推荐用低剂量。 【国外用法用量参考】 成人: ·常规剂量 ·口服给药 在英国,推荐一次10mg,每4-6小时1次,一日极量为40mg;在美国,建议给药持续时间不超过5日。 ·肌内注射 术后疼痛:初量为一次10mg,每2小时1次。必要时可将剂量调整为一次10-30mg,每4-6小时1次。一日极量为90mg;体重小于50kg者,一日极量为60mg。建议给药持续时间不超过2日,且应尽早改为口服给药。 ·静脉注射 术后疼痛:一次给药时间不应小于15秒,其余同肌内注射项。 ·经眼给药 季节变应性结膜炎所致的眼瘙痒、囊斑样水肿的局部治疗和眼科手术引起炎症的防治:使用0.5%的本药溶液。 ·肾功能不全时剂量:轻度肾功能不全时,肌内注射或静脉给药的极量为一日60mg。 ·老年人剂量:肌注或静脉给药的极量为一日60mg。 【制剂与规格】 酮洛酸氨丁三醇片 10mg。 酮洛酸氨丁三醇注射液 (1)1ml:10mg。(2)1ml:30mg。 酮洛酸氨丁三醇滴眼液 8ml:8mg。 【禁忌】 (1)对本药、阿司匹林或其它非甾体类抗炎药过敏者。(2)鼻息肉综合征患者(国外资料)。(3)血管性水肿患者(国外资料)。(4)有高危出血倾向者(国外资料)。(5)活动性消化性溃疡患者。(6)肝肾疾病、心脏病、高血压患者。(7)孕妇。(8)儿童。
规格: 10毫克/片 100片/瓶 【英文商品名】KETOROLAC(Generic TORADOL) 10mg/tab 100tabs/bottle 【原产地英文药品名】KETOROLAC TROMETHAMINE 【中文参考商品译名】 酮洛酸(TORADOL仿制药) 10毫克/片 100片/瓶 【中文参考药品译名】 酮洛酸氨丁三醇
How does this medication work? What will it do for me? Ketorolac belongs to the class of medications called nonsteroidal anti-inflammatory drugs (NSAIDs). It is used for the short-term treatment (five to seven days) of moderate to moderately severe acute pain associated with muscle sprains and strains, dental pain, and pain after surgery or giving birth. It works by reducing pain, swelling, and inflammation.
Your doctor may have suggested this medication for conditions other than the ones listed in these drug information articles. If you have not discussed this with your doctor or are not sure why you are taking this medication, speak to your doctor. Do not stop taking this medication without consulting your doctor.
Do not give this medication to anyone else, even if they have the same symptoms as you do. It can be harmful for people to take this medication if their doctor has not prescribed it.
How should I use this medication? The usual adult dose of ketorolac when taken by mouth is 10 mg every four to six hours as required for pain. Doses exceeding 40 mg daily are not recommended. The medication should be used for a maximum of 5 days for treatment of pain after surgery and for a maximum of 7 days when treating muscular aches and pains. The lowest dose required to control the pain should be used.
Ketorolac is also available for use in the hospital as an injectable medication. It is injected into the muscle and should not be used for more than two days.
Many things can affect the dose of medication that a person needs, such as body weight, other medical conditions, and other medications. If your doctor has recommended a dose different from the ones given here, do not change the way that you are taking the medication without consulting your doctor.
It is very important that this medication be taken exactly as prescribed by your doctor. If you miss a dose of medication that has been scheduled, take it as soon as you remember. If it is almost time for your next dose, skip the missed dose and carry on with your regular schedule. Do not double-up on doses.
Do not dispose of medications in wastewater (e.g. down the sink or in the toilet) or in household garbage. Ask your pharmacist how to dispose of medications that are no longer needed or have expired.
What form(s) does this medication come in? Toradol Each white, round, film-coated tablet, with one side printed in black ink with on one side, contains ketorolac tromethamine 10 mg. Nonmedicinal ingredients: hydroxypropyl methylcellulose, lactose, magnesium stearate, microcrystalline cellulose, polyethylene glycol and titanium dioxide.
Toradol IM 10 mg/mL Each mL of clear, slightly yellow, sterile solution contains ketorolac tromethamine 10 mg. Nonmedicinal ingredients: alcohol 10% w/v and sodium chloride in sterile water. The pH is adjusted with sodium hydroxide or hydrochloric acid.
30 mg/mL Each mL of clear, slightly yellow, sterile solution contains ketorolac tromethamine 30 mg. Nonmedicinal ingredients: alcohol 10% w/v and sodium chloride in sterile water. The pH is adjusted with sodium hydroxide or hydrochloric acid.
Some medications may have other generic brands available. Always ask your doctor or pharmacist about the safety of switching between brands of the same medication.
Who should NOT take this medication? This medication should not be taken by anyone who: currently has or has recently had an inflammatory disease of the stomach and intestines such as stomach or intestinal ulcer, or ulcerative colitis is currently taking other NSAIDs is or may be allergic to ketorolac or any of the ingredients of the medication has had an allergic reaction to ASA or other anti-inflammatory medications has complete or partial syndrome of nasal polyps has a history of significant liver disease or kidney disease is scheduled for surgery in the immediate future is in labour and delivery is taking probenecid or oxpentifylline
What side effects are possible with this medication? The side effects listed below are not experienced by everyone who takes this medication. If you are concerned about side effects, discuss the risks and benefits of this medication with your doctor. Your health professional may be able to help you to deal with some of the effects.
The following side effects may go away as your body becomes used to the medicine; check with your doctor if the following side effects continue or become bothersome. A common side effect of nonsteroidal anti-inflammatory drugs (NSAIDs) is stomach upset. This can be minimized by taking the medication immediately after a meal, or with food or milk.
More common abdominal or stomach pain (mild or moderate) bruising at place of injection diarrhea dizziness drowsiness headache indigestion nausea
Less common or rare bloating or gas burning or pain at place of injection constipation feeling of fullness in abdominal or stomach area increased sweating vomiting
Check with your doctor as soon as possible if any of the following side effects occur: More common swelling of face, fingers, lower legs, ankles, or feet weight gain (unusual) Less common bruising (not at place of injection) high blood pressure skin rash or itching small, red spots on skin sores, ulcers, or white spots on lips or in mouth Rare abdominal or stomach pain, cramping, or burning (severe) bloody or cloudy urine blurred vision of other vision change burning, red, tender, thick, scaly, or peeling skin cough or hoarseness dark urine decrease in amount of urine (sudden) fever with severe headache, drowsiness, confusion, and stiff neck or back fever with or without chills or sore throat general feeling of illness hallucinations (seeing, hearing, or feeling things that are not there) hearing loss hives increase in amount of urine or urinating often light-coloured stools loss of appetite low blood pressure mood changes or unusual behaviour muscle cramps or pain nausea, heartburn, or indigestion (severe and continuing) nosebleeds pain in lower back or side pain, tenderness, or swelling in the upper abdominal area painful or difficult urination pale skin puffiness or swelling of the eyelids or around the eyes ringing or buzzing in ears runny nose severe restlessness swollen or painful glands swollen tongue thirst (continuing) unusual tiredness or weakness yellow eyes or skin Stop taking this medication and contact your doctor immediately if any of the following side effects occur: Rare bleeding from the rectum or bloody or black, tarry stools bleeding or crusting sores on lips blue lips and fingernails chest pain convulsions fainting shortness of breath; fast, irregular, noisy, or troubled breathing;, tightness in chest; or wheezing vomiting of blood or material that looks like coffee grounds
Some people may experience side effects other than those listed. Check with your doctor if you notice any symptom that worries you while you are taking this medication.
Are there any other precautions or warnings for this medication? Drowsiness/reduced altertness: Headaches, sometimes accompanied by dizziness or lightheadedness, may occur during treatment with ketorolac. (These headaches usually occur early in the treatment.) Although the severity of these effects rarely requires the treatment to be stopped, ketorolac should be discontinued if the headaches persist despite dose reduction. Avoid operating motor vehicles and doing other potentially hazardous activities until you determine the effect this medication has on you.
Fertility: This medication may decrease fertility. It is not recommended for women who are trying to become pregnant.
Fluid and electrolyte balance: Fluid retention and edema have been reported with the use of this medication. Ketorolac should be used with caution by anyone who: has certain heart conditions (e.g., congestive heart failure) has high blood pressure has kidney disease or reduced kidney function is recovering from a surgical operation under general anesthesia has any other condition that might lead to fluid retention
There is a risk of high blood potassium with NSAID treatment. People most at risk are seniors; those having conditions such as diabetes or kidney failure; and those who take beta-blockers, angiotensin converting enzyme (ACE) inhibitors, or some diuretics (water pills).
Gastrointestinal: Stomach ulcers, perforation, and bleeding from the stomach have been known to occur during treatment with ketorolac. These complications can occur at any time, and are sometimes severe enough to require immediate medical attention. The risk of ulcers and bleeding are increased for people taking higher doses of NSAIDs for longer periods of time.
Ketorolac should be taken under close medical supervision by people prone to irritation of the stomach and intestines, particularly those who have had a stomach ulcer, bloody stools, or diverticulosis or other inflammatory disease of the stomach or intestines (such as ulcerative colitis or Crohn's disease). In these cases, your doctor must weigh the benefits of treatment against the possible risks.
Stop taking the medication and contact your doctor immediately if you experience symptoms or signs suggestive of stomach ulcers or bleeding in the stomach (black, tarry stools). These reactions can occur at any time during treatment without warning.
Infection: This medication may mask the usual signs of infection.
Kidney function: Use of ketorolac may lead to a higher risk of reduced kidney function. This is most common for people who already have kidney disease, liver disease, or heart failure; for people who are taking diuretics (water pills); and seniors.
Long-term use: Long-term use of ketorolac (beyond 5 to 7 days for the tablets, or 2 days for the injection) is not recommended as the risk of side effects increases with the length of treatment.
Pregnancy: This medication is not recommended for use during pregnancy as its safety has not been established.
Breast-feeding: This medication should not be used by nursing women.
Children and adolescents: Ketorolac is not recommended for children and adolescents under the age of 16 years. The safety, effectiveness, and dosages of this medication for this age group have not been established.
Seniors: Seniors appear to have a higher risk of side effects with this medication. They should use the lowest effective dosage under close medical supervision.
What other drugs could interact with this medication? The following medications may affect the way that ketorolac works or increase the risk of side effects: ASA angiotensin converting enzyme (ACE) inhibitors (e.g., ramipril) beta-adrenergic blockers (e.g.,metoprolol, atenolol) corticosteroids (e.g., prednisone) diuretics (water pills; e.g., spironolactone, triamterene) heparin other NSAIDs (e.g., naproxen, diclofenac) oxpentifylline potassium supplements probenecid warfarin
Ketorolac may affect the way that the following medications work: aminoglycosides (e.g., amikacin, gentamycin, tobramycin) cyclosporine diuretics (water pills; e.g., furosemide, hydrochlorothiazide) heparin lithium methotrexate warfarin
If you are taking any of these medications, speak with your doctor or pharmacist. Depending on your specific circumstances, your doctor may want you to: stop taking one of the medications, change one of the medications to another, change how you are taking one or both of the medications, or leave everything as is.
An interaction between two medications does not always mean that you must stop taking one of them. In many cases, interactions are intended or are managed by close monitoring. Speak to your doctor about how any drug interactions are being managed or should be managed.
Medications other than those listed above may interact with this medication. Tell your doctor or prescriber about all prescription, over-the-counter (non-prescription), and herbal medications that you are taking. Also tell them about any supplements you take. Since caffeine, alcohol, the nicotine from cigarettes, or street drugs can affect the action of many medications, you should let your prescriber know if you use them. |