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Cycloset^TM单一疗法或作为磺酰脲类（sulfonylurea）、二甲双胍联用磺酰脲类以及单次或2次口服低血糖药物治疗的辅助疗法可改善广泛患者群体的血糖控制情况。
2009年5月5日，美国食品药品管理局(FDA)批准Cycloset(甲磺酸溴隐亭) 0.8mg用于治疗2型糖尿病患者。该药可用于辅助饮食和运动疗法，进一步改善血糖控制。该药制造商VeroScience公司表示，Cycloset是作用于中枢神经系统的多巴胺受体激动剂溴隐亭的速释制剂，可作用于中枢神经系统，使调节餐后胰岛素介导的葡萄糖水平和脂质代谢的下丘脑中枢复位，从而降低餐后高血糖和高血脂状态。
该产品是多巴胺D2受体激动剂溴隐亭的速释剂型。当清晨给药时，溴隐亭被认为可作用于下丘脑内神经元的节律以“重新设定”异常升高的下丘脑驱力，其会导致患者空腹和餐后血糖、甘油三酯和游离脂肪酸水平升高。
2型糖尿病的新药——甲磺酸溴隐亭片（Cycloset）。这种药物与以往的降糖药不同的是，它通过调节中枢神经系统来起到控糖的作用。
多巴胺是大脑中分泌的一种化学物质，能调节人们的行为、情绪、能力和睡眠。科学家认为，糖耐量受损和胰岛素抵抗与多巴胺异常分泌有关，因此提高多巴胺的活性就能解决上述问题。而甲磺酸溴隐亭就有这种作用。研究显示：与安慰剂相比，服用甲磺酸溴隐亭片能够使糖尿病人的糖化血红蛋白值下降0.6%—0.9%。研究者指出，医务工作者可以给那些通过饮食调节，体育锻炼，服用二甲双胍、磺酰脲类药物和胰岛素增敏剂等效果仍然不理想的病人使用此药。大规模试验显示，此药物不会增加心血管疾病的风险。不过，这种药物不适合1型糖尿病人和酮症酸中毒的患者服用。
溴隐亭速释片:是一种不会增加心血管危险的糖尿病新药
近日美国FDA批准溴隐亭速释片用于治疗2型糖尿病，研究证实溴隐亭速释片单一治疗或辅助磺酰脲、二甲双胍加磺酰脲治疗，均可改善对广大糖尿病患者的血糖控制，且不增加心血管疾病危险，为糖尿病患者提供了一条崭新的治疗途径。
美国FDA批准VeroScience公司与S2治疗公司合作开发的溴隐亭速释片（bromocriptine，Cycloset）治疗2型糖尿病，这是此类药物获准上市的第一个。溴隐亭速释片单一治疗或辅助磺酰脲、二甲双胍加磺酰脲治疗，均可改善对广大糖尿病患者的血糖控制。
临床前研究表明，增加多巴胺活性可改善糖尿病症状，白日增加多巴胺能活性也是重要的。对糖尿病动物研究显示，在白日特定的时间增加多巴胺能活性在生理学上是改善糖尿病代谢障碍最有效“重新设定”生物时钟神经化学。溴隐亭速释片一日1次早上用药，口服后不久可产生单一简短脉冲式多巴胺激动活性。溴隐亭上午改善膳食后的血糖而不增加血浆胰岛素浓度，在药物已基本从血液循环中清除后的许多小时还显示对2型糖尿病餐后（如午餐和晚餐）血糖控制的有效作用。
溴隐亭速释片代表了治疗2型糖尿病的新途径。对糖尿病患者来说是首个靶向人体多巴胺（神经系统内神经元或神经细胞的化学递质）活性的药物。多巴胺激动剂溴隐亭增加多巴胺活性。然而，溴隐亭速释片在人体内改善血糖控制的特异机制尚未清晰，溴隐亭治疗糖尿病的研发是基于临床前研究显示在代谢疾病状态时大脑多巴胺活性低，在2型糖尿病患者体内发现这些因素主要是诸如胰岛素抵抗性（人体丧失胰岛素降血糖作用的能力）等多种代谢功能障碍。而且，临床前以多巴胺激动剂溴隐亭治疗糖尿病动物显示，溴隐亭速释片作用于中枢神经系统启动重新设定和改善对外周代谢的控制。
溴隐亭速释片是美国FDA颁布“糖尿病治疗药需研究结果显示不增加心血管疾病危险”新准则后首个获准上市的药品。溴隐亭速释片纳入3000例患者的52周双盲安全性研究显示，其与安慰剂相比不加重下述心血管疾病：心肌梗塞、休克、因不稳定心绞痛住院、充血性心力衰竭和再次血管手术。
对新诊断的2型糖尿病或不能以目前已上市药物控制血糖的患者，溴隐亭速释片提供了治疗糖尿病的一条崭新途径。此外，2型糖尿病是心血管疾病高危人群，故溴隐亭速释片显示不增加诸如心脏病发作等心血管疾病危险的特点尤为引人注目。溴隐亭速释片纳入3000例患者为期一年的安全性研究显示，治疗2型糖尿病每日剂量高达4.8mg的安全性与安慰剂相媲美。
【原产地英文商品名】CYCLOSET 0.8mg/tab 200tabs/bottle
【原产地英文药品名】BROMOCRIPTINE MESYLATE
【中文参考商品译名】CYCLOSET 0.8毫克/片 200片/瓶
【中文参考药品译名】甲磺酸溴隐亭
【生产厂家中文参考译名】VEROSCIENCE
【生产厂家英文名】VEROSCIENCE
CYCLOSET (bromocriptine mesylate) is a first-in-class antidiabetic treatment that may lower your blood sugar, without increasing insulin.
Important Safety Information
CYCLOSET is a prescription medicine used with diet and exercise to lower blood sugar in adults with type 2 diabetes. CYCLOSET may be taken alone or in combination with other medications that also help control blood sugar.
CYCLOSET should not be taken by patients who take ergot medicines. A healthcare provider or pharmacist can provide a list of these medications. CYCLOSET should not be taken by anyone who is allergic to bromocriptine or any other ingredient of CYCLOSET. Patients with syncopal (fainting) migraine headaches should not take CYCLOSET, because it may cause very low blood pressure. Women who are breastfeeding should not take CYCLOSET. It may prevent them from producing milk. Some breastfeeding women taking bromocriptine, the active ingredient in CYCLOSET, have had strokes. CYCLOSET is a prescription medicine used with diet and exercise to lower blood sugar in adults with type 2 diabetes. CYCLOSET may be taken alone or in combination with other medications that also help control blood sugar.
Warnings for patients taking CYCLOSET. CYCLOSET can cause very low blood pressure (hypotension) and fainting, especially when patients are starting treatment or have increased the dose of CYCLOSET. Patients taking medicines for high blood pressure (hypertension) should be careful when taking CYCLOSET because they may cause blood pressure to drop too much. CYCLOSET may worsen psychotic disorders or reduce the effectiveness of medicines that treat psychosis. CYCLOSET may cause sleepiness. Patients taking CYCLOSET who feel sleepy should not drive a car or operate other heavy machinery until they feel alert. Patients who are taking dopamine antagonist medications should talk to their healthcare provider before taking CYCLOSET. The combined use of these medicines is not recommended.
Safety of CYCLOSET. No antidiabetic drug, including CYCLOSET, has ever been proven to reduce the risk of having a heart attack or other cardiovascular problem such as stroke. However, a 52-week study showed that CYCLOSET did not increase the risk of major cardiovascular events. In clinical studies, the most common side effects that seemed to be caused by CYCLOSET were nausea, fatigue, dizziness, vomiting and headache. Safety and effectiveness have not been established in pediatric patients.
For Full Prescribing Information, please see CYCLOSET Prescribing Information (Consumers or patients, please refer to section 17.2 on pages 12-13). Please consult with your healthcare professional to see if CYCLOSET is right for you.
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Chemical formula:
Bromocriptine Mesylate Oral tablet
What is this medicine?
BROMOCRIPTINE (broe moe KRIP teen) comes from a group of medicines called ergot alkaloids. This medicine is useful in treating menstrual and fertility problems and symptoms caused by certain cancers. It is also used to treat Parkinson's disease and people who have too much growth hormone.
This medicine may be used for other purposes; ask your health care provider or pharmacist if you have questions.
What should I tell my health care provider before I take this medicine?
They need to know if you have any of these conditions:
•drowsiness
•heart or vessel disease
•high or low blood pressure
•history of heart attack
•kidney disease
•liver disease
•mental illness
•seizures
•an unusual or allergic reaction to bromocriptine, ergot alkaloids, sulfites, other medicines, foods, dyes, or preservatives
•pregnant or trying to get pregnant
•breast-feeding
How should I use this medicine?
Take this medicine by mouth with a glass of water. Follow the directions on the prescription label. Take with food to prevent stomach upset. Take your doses at regular intervals. Do not take your medicine more often than directed. Do not stop taking except on the advice of your doctor or health care professional.
Talk to your pediatrician regarding the use of this medicine in children. While this medicine may be prescribed for children as young as 11 years of age for selected conditions, precautions do apply.
Overdosage: If you think you have taken too much of this medicine contact a poison control center or emergency room at once.
NOTE: This medicine is only for you. Do not share this medicine with others.
What if I miss a dose? Try not to miss a dose. If it is almost time for your next dose, take only that dose. Do not take double or extra doses.
What may interact with this medicine?
Do not take this medicine with any of the following medications:
•cocaine
•dihydroergotamine, ergotamine, ergoloid mesylates, methysergide, or ergot-type medication
•imatinib
•medicines for fungal infections like ketoconazole and itraconazole
•medicines for HIV infection like amprenavir, delavirdine, efavirenz, indinavir, nelfinavir, ritonavir and saquinavir
•medicines for migraine headache like almotriptan, eletriptan, frovatriptan, naratriptan, rizatriptan, sumatriptan, zolmitriptan
This medicine may also interact with the following medications:
•aspirin and aspirin-like medicines
•chloramphenicol
•isometheptene
•levodopa
•medicines for high blood pressure
•medicines for mental problems and psychotic disturbances
•metoclopramide
•phenylpropanolamine
•probenecid
•stimulant medicines for attention disorders, weight loss, or to stay awake
•sulfa medicines
This list may not describe all possible interactions. Give your health care provider a list of all the medicines, herbs, non-prescription drugs, or dietary supplements you use. Also tell them if you smoke, drink alcohol, or use illegal drugs. Some items may interact with your medicine.
What should I watch for while using this medicine?
Visit your doctor or health care professional for regular checks on your progress. Ask your doctor or health care professional if you should check your blood pressure regularly, especially if you get severe headaches. Report changes in blood pressure if they occur. Contact your doctor or health care professional promptly if you develop an unusual or severe headache or have changes in your vision.
If you stop taking this medicine when it is being used for tumor treatment, the tumor may regrow quickly, and your original symptoms may return. Do not stop taking this medicine unless your doctor tells you to.
You may get dizzy or drowsy. Do not drive, use machinery, or do anything that requires mental alertness until you know how this medicine affects you. To reduce the risk of dizzy or fainting spells, do not stand or sit up quickly, especially if you are an older patient. Alcohol can make you more dizzy, and increase flushing and rapid heartbeats. Avoid alcoholic drinks. Dizziness is more common after the first dose. Take it before bedtime if possible and be careful getting out of bed.
If you find that you have sudden feelings of wanting to sleep during normal activities, like cooking, watching television, or while driving or riding in a car, you should contact your health care professional.
Your mouth may get dry. Chewing sugarless gum or sucking hard candy, and drinking plenty of water may help. Contact your doctor if the problem does not go away or is severe.
What side effects may I notice from receiving this medicine?
Side effects that you should report to your doctor or health care professional as soon as possible:
•allergic reactions like skin rash, itching or hives, swelling of the face, lips, or tongue
•breathing problems
•changes in vision
•confusion
•dizziness
•falling asleep during normal activities like driving
•fast, irregular heartbeat
•feeling anxious
•feeling faint or lightheaded, falls
•hallucination, loss of contact with reality
•increased hunger
•low blood pressure
•numbness, tingling, or burning in hands or feet
•runny nose
•seizures
•shakiness
•spasm in fingers or toes, or unusual muscle movements
•stomach pain
•sweating
•unusual bleeding or bruising
•unusual or severe headache
•unusually weak or tired
•vomiting
Side effects that usually do not require medical attention (report to your doctor or health care professional if they continue or are bothersome):
•diarrhea or constipation
•loss of appetite
•mild stomach cramps
•nausea
This list may not describe all possible side effects. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.
Where should I keep my medicine?
Keep out of the reach of children.
Store below 25 degrees C (77 degrees F). Protect from light. Keep container tightly closed. Throw away any unused medicine after the expiration date.
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