英文药名: Relpax(Eletriptan HBr Tablets)

中文药名: 依立曲坦,曲普坦氢溴酸片

生产厂家: Pfizer

分类名称
一级分类：神经系统药物 二级分类：抗偏头痛药物 三级分类： 
 
药品英文名
Eletriptan
 
药品别名
依立曲坦、曲普坦氢溴酸片、EletriptanHydrobromide、Relpax
 
药物剂型
依立曲坦薄膜包衣片剂：20mg/片，40mg/片，80mg/片。
 
药理作用
本品是有效的血管选择性5-HT1B和神经元5-HT1D受体激动剂。对5-HT1F受体有高度亲和力，对人体5-HT1A、5-HT2B、5-HT1E和5-HT7受体有中度亲和力，对其他多种受体(β受体，腺苷A1，多巴胺D1、D2，毒蕈碱和阿片受体)及钙通道二氢吡啶结合位点无亲和力或药理活性。人体5-HT1B受体介导颅内血管收缩，5-HT1D受体主要位于三叉神经末梢突触前，5-HT1B和5-HT1F受体位于人体三叉神经中枢。本品可能通过激活上述受体来抑制神经肽的释放，通过收缩颅内血管并抑制神经性炎症来发挥抗偏头痛效应。本品的亲脂性强，能透过血-脑屏障。动物试验显示，本品对颈动脉、冠状动脉和股动脉血管床的选择性高，可抑制动物硬脑膜中的神经性炎症。
 
药动学
本品口服后经胃肠道迅速吸收，达峰时间约为1.5h，生物利用度约为50%，与高脂食物合用时药时曲线下面积(AUC)和峰浓度(Cmax)增加20%～30%。静注后分布体积约为138L，与血浆蛋白结合率约为85%。主要由细胞色素P450酶系CYP3A4酶代谢，目前唯一可知的活性代谢物为N-脱甲基依来曲普坦，消除t1/2约为4h，口服后非肾清除约占总清除的90%。
 
适应证
适用于成人有或无先兆的偏头痛急性发作的治疗。
 
禁忌证
1.对本品及制剂成分过敏者禁用。
2.严重肝、肾受损者禁用。
3.高血压未控制者禁用。
4.冠心病、周围血管病、有脑血管意外(CVA)或短暂性局部缺血发作(TIA)史的患者禁用。
5.偏瘫性或基底性头痛患者禁用。
 
注意事项
1.本品只用于明确诊断为偏头痛患者，不作为偏头痛的预防药物使用。
2.除非能进行全程心脏监测，一般不用于易发生心脏疾病因素者(如高血压、高胆固醇血症、吸烟、肥胖、糖尿病、冠心病家族史等)。
3.首次剂量最好在专业人士监督下使用。
4.过量后无特殊解毒剂，只能采取保持通风、充足吸氧等治疗措施，同时严密监测心脏功能。
5.本品不可与麦角胺、麦角胺衍生物(包括美西麦角)或其他5-HT1受体激动剂同时使用。
6.轻中度肾脏受损者慎用。
7.怀孕、哺乳期妇女慎用。
8.不推荐用于65岁以上、18岁以下人群。
 
不良反应
本品通常耐受性好，多数不良反应比较轻微，且为一过性。
1.最常见的不良反应有虚弱、恶心、眩晕、嗜睡，均与剂量相关。
2.其他还有感觉异常、潮红、胸痛、腹部不适、口干、消化不良和咽痛等。
3.严重的不良反应为心脏疾病，对有易发心脏病因素者甚至可引起致命危险，但发生率很低，如冠状动脉血管痉挛、一过性心肌局部缺血、心肌梗死、室性心动过速、室性纤颤等。
 
用法用量
成人偏头痛发作后应尽早给予本品，推荐初始剂量为40mg，用水吞服。如果在24h内头痛复发，可重复给药一次，但两种剂量之间至少间隔2h，最大日剂量为80mg。对于正在服用红霉素和其他CYP3A4抑制剂如酮康唑、伊曲康唑、克拉霉素的患者，推荐剂量为20mg，最大日剂量为40mg。
 
药物相应作用
1.本品主要由CYP3A4酶代谢，因此与CYP3A4酶抑制剂(如酮康唑、伊曲康唑、奈法唑酮、克拉霉素、利托纳韦、奈法纳韦)之间有相互作用，可增强本品的药理作用，与这类药物合用时至少间隔72h。
2.普萘洛尔也可增强本品的药理作用。
3.本品与其他含麦角类化合物以及其他5HT1受体拮抗剂合用时应至少间隔24h。

Drug Name: ELETRIPTAN - ORAL
Other Brand Names: Relpax
Uses: Eletriptan is used to treat migraines when they occur. It helps to relieve headaches, pain, and other symptoms of migraines, including nausea, vomiting, and sensitivity to light/sound. Prompt treatment allows you to get back to your normal routine and may decrease your need for other pain medications. Eletriptan does not prevent future migraines or reduce how often you may get a migraine. Eletriptan belongs to a group of drugs called "triptans." Migraines are thought to occur when certain blood vessels in the brain become swollen (dilated). This drug works by helping blood vessels in the brain to return to normal size. It may also block pain signals in the brain.
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Relpax
Generic Name: eletriptan (EL e TRIP tan)
Brand Names: Relpax
What is Relpax?
Relpax (eletriptan) is a headache medicine that narrows blood vessels around the brain. Eletriptan also reduces substances in the body that can trigger headache pain, nausea, sensitivity to light and sound, and other migraine symptoms.
Relpax is used to treat migraine headaches. Relpax will only treat a headache that has already begun. It will not prevent headaches or reduce the number of attacks.
Relpax should not be used to treat a common tension headache, a headache that causes loss of movement on one side of your body, or any headache that seems to be different from your usual migraine headaches. Use this medication only if your condition has been confirmed by a doctor as migraine headaches.
Relpax may also be used for purposes not listed in this medication guide.
Important information about Relpax
You should not take Relpax if you are allergic to eletriptan, if you have any history of heart disease, or if you have coronary heart disease, angina, blood circulation problems, lack of blood supply to the heart, uncontrolled high blood pressure, severe liver disease, ischemic bowel disease, a history of a heart attack or stroke, or if your headache seems to be different from your usual migraine headaches.
Do not take Relpax within 24 hours before or after using another migraine headache medicine, including almotriptan (Axert), frovatriptan (Frova), naratriptan (Amerge), rizatriptan (Maxalt), sumatriptan (Imitrex, Treximet), zolmitriptan (Zomig), or ergot medicine such as ergotamine (Ergomar, Cafergot, Migergot), dihydroergotamine (D.H.E. 45, Migranal), or methylergonovine (Methergine). Do not use Relpax within 72 hours before or after taking ketoconazole (Extina, Ketozole, Nizoral, Xolegal), itraconazole (Sporanox), nefazodone, clarithromycin (Biaxin), ritonavir (Norvir, Kaletra), or nelfinavir (Viracept).
Before taking Relpax, tell your doctor if you have liver or kidney disease, high blood pressure, a heart rhythm disorder, or coronary heart disease (or risk factors such as diabetes, menopause, smoking, being overweight, having high cholesterol, having a family history of coronary artery disease, being older than 40 and a man, or being a woman who has had a hysterectomy).
Also tell your doctor if you are also taking an antidepressant such as citalopram (Celexa), desvenlafaxine (Pristiq), duloxetine (Cymbalta), escitalopram (Lexapro), fluoxetine (Prozac, Sarafem), fluvoxamine (Luvox), paroxetine (Paxil), sertraline (Zoloft), or venlafaxine (Effexor).
Relpax will only treat a headache that has already begun. It will not prevent headaches or reduce the number of attacks.
After taking an Relpax tablet, you must wait two (2) hours before taking a second tablet. Do not take more than 80 mg of Relpax in 24 hours.
Before using Relpax
You should not use Relpax if you are allergic to eletriptan, or if you have:
•coronary heart disease, angina (chest pain), blood circulation problems, lack of blood supply to the heart;
•a history of heart disease, heart attack, or stroke, including "mini-stroke";
•severe or uncontrolled high blood pressure;
•severe liver disease;
•ischemic bowel disease; or
•a headache that seems different from your usual migraine headaches.
To make sure you can safely take Relpax, tell your doctor if you have any of these other conditions:
•liver disease;
•kidney disease;
•high blood pressure, a heart rhythm disorder; or
•coronary heart disease (or risk factors such as diabetes, menopause, smoking, being overweight, having high cholesterol, having a family history of coronary artery disease, being older than 40 and a man, or being a woman who has had a hysterectomy).
FDA pregnancy category C. It is not known whether Relpax will harm an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant while using Relpax. Eletriptan can pass into breast milk and may harm a nursing baby. Do not use this medication without telling your doctor if you are breast-feeding a baby. Do not give this medicine to anyone under 18 years old.
See also: Relpax pregnancy and breastfeeding warnings (in more detail)
How should I use Relpax?
Take Relpax exactly as prescribed by your doctor. Do not take in larger or smaller amounts or for longer than recommended. Follow the directions on your prescription label. Overuse of migraine headache medicine can actually make your headaches worse.
Take Relpax as soon as you notice headache symptoms, or after an attack has already begun.
Your doctor may want to give your first dose of this medicine in a hospital or clinic setting to see if you have any serious side effects.
Take one Relpax tablet whole with a full glass of water.
After taking a tablet: If your headache does not completely go away, or goes away and comes back, take a second tablet two (2) hours after the first. Do not take more than 80 mg of Relpax in 24 hours. If your symptoms have not improved, contact your doctor before taking any more tablets.
Contact your doctor if you have more than three headaches in one month (30 days).
If you use Relpax long-term, your doctor may want to check your heart function using an electrocardiograph or ECG (sometimes called an EKG), a machine that measures electrical activity of the heart. This will help your doctor determine if it is still safe for you to use this medication. Visit your doctor regularly.
Store Relpax at room temperature away from moisture and heat.
What happens if I miss a dose?
Since Relpax is used as needed, it does not have a daily dosing schedule. Call your doctor promptly if your symptoms do not improve after using Relpax.
After taking an Relpax tablet, you must wait two (2) hours before taking a second tablet. Do not take more than 80 mg of Relpax in 24 hours.
What happens if I overdose?
Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.
Overdose could cause high blood pressure (severe headache, blurred vision, buzzing in your ears, anxiety, confusion, chest pain, shortness of breath, uneven heartbeats, or seizure).
What should I avoid while using Relpax?
Do not take Relpax within 24 hours before or after using another migraine headache medicine, including:
•almotriptan (Axert), frovatriptan (Frova), naratriptan (Amerge), rizatriptan (Maxalt, Maxalt-MLT), sumatriptan (Imitrex, Treximet), or zolmitriptan (Zomig); or
•ergot medicine such as ergotamine (Ergomar, Cafergot, Migergot), dihydroergotamine (D.H.E. 45, Migranal), or methylergonovine (Methergine).
Do not use Relpax within 72 hours before or after taking any of the following medicines:
•ketoconazole (Extina, Ketozole, Nizoral, Xolegal), itraconazole (Sporanox);
•nefazodone;
•clarithromycin (Biaxin); or
•ritonavir (Norvir, Kaletra), nelfinavir (Viracept).
Relpax may impair your thinking or reactions. Be careful if you drive or do anything that requires you to be alert.
Relpax side effects
Get emergency medical help if you have any of these signs of an allergic reaction to Relpax: hives; difficulty breathing; swelling of your face, lips, tongue, or throat. Stop using Relpax and call your doctor at once if you have a serious side effect such as:
•feeling of pain or tightness in your jaw, neck, or throat;
•chest pain or heavy feeling, pain spreading to the arm or shoulder, nausea, sweating, general ill feeling;
•sudden numbness or weakness, especially on one side of the body;
•sudden severe headache, confusion, problems with vision, speech, or balance;
•sudden and severe stomach pain and bloody diarrhea;
•numbness or tingling and a pale or blue-colored appearance in your fingers or toes; or
•(if you are also taking an antidepressant) - agitation, high fever, sweating, fast or pounding heartbeats, nausea, vomiting, diarrhea, loss of balance or coordination, overactive reflexes, hallucinations, fainting.
Less serious Relpax side effects may include:
•mild headache (not a migraine);
•pressure or heavy feeling in any part of your body;
•dry mouth, upset stomach, stomach pain or cramps;
•dizziness, drowsiness, weakness; or
•warmth, redness, or mild tingling under your skin.
This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

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