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【通用名称】阿托伐醌
【英文名称】Atovaquone
【中文别名】美普龙；阿托喹酮；2-(反式-4-(4-氯苯基)环己基)-3-羟基-1,4-萘二酮
【英文名】 Atovaquone
分子式 C22H19ClO3
分子量 366.84 CAS号 95233-18-4
【药理】
本品为羟基 1,4-萘喹啉，是辅酶Q的同系物，具有抗几种原虫的活性。对疟原虫属，其作用部位为细胞色素bcl结合点(结合点Ⅲ)。本品能可逆性地与多肽上的11500Da分子集团结合。二氢乳清醒脱氢酶是吡啶生物合成中重要的酶，通过辅酶Q连接线粒体作电子传递，因此本品通过抑制电子传递阻止吡啶的合成。一些代谢酶通过辅酶Q参与线粒体的电子传递，因此，本品抑制电子传递作用实际上是抑制了这些酶的活性。 100mg／kg·d剂量的本品可100％的防止和治疗小鼠P.carinii。其抑制的IC50范围为0.1～3.0μg/ml。
【药动学】
本品为高亲脂性，低溶于水的物质，在剂量750mg以上时其生物利用度减少很多且变化也大，给饮食正常的健康志愿者服用本品，其血浆浓度时间曲线表现为双峰，第一峰出现在服药后1至8小时，第二峰出现在服药后24至96小时。双峰说明了该药存在着肠肝循环。与肉类特别是脂肪同服，可增加吸收约30％。 本品有较长的半衰期，正常人半衰期为2.9±0.8天。AIDS病人半衰期为2.2±0.6天。其原因主要为不经肾排泄，肠肝循环也延迟了其从粪便排泄的速度。 在一多剂量试验中，给4名HIV血清阳性的志愿者服用本品，同时给予食物。生物利用度降低。每天最大剂量为300mg，其平均稳态血浓为40.0±19.0μg/ml。而每天服用750mg，稳态血浓为26.9±10μg/ml。 给10名免疫受损的儿童用本品，其平均半衰期为2.7±1.6天。这些儿童的平均年龄为5个月到13岁，体重在3.5kg到85.5kg。10mg/kg每天一次的给药方案可达到平均稳态血浓度值7.5±4.6μg/ml，其中3名儿童每日给药达40mg/kg，其稳态血浓度平均值为14.0±2.2kg/ml。本品血浆蛋白结合率达到99.9％。
【适应症】
适用于不能耐受SMZ-TMP的患轻度至中度卡氏肺炎的AIDS病人的口服治疗,卡氏肺囊虫感染
。
【用法用量】
一日三次750mg，与食物同服，共21天。儿童剂量(14个月以上)为40mg／kg·d。体重超过40kg的儿童剂量按成人剂量。
[制剂与规格]250mg片剂
【给药说明】
由于本品与血浆蛋白结合率高，所以在与其他高血浆蛋白结合率的药物同用时应注意其替代作用。
【不良反应】
红斑23％，呕吐14％，恶心21％，头昏19％，头痛16％，发热14％，失眠10％，肝药酶活性增加。
Wellvone®
atovaquone
Wellvone® (atovaquone)
Domaine thérapeutique
Infection par le VIH
Mentions légales
Wellvone 750 mg/5 ml suspension buvable
Notices
Wellvone 750 mg/5 ml suspension buvable
Avis de transparence
Wellvone 750 mg/5 ml suspension buvable
You are viewing: Wellvone 750mg/5ml oral suspension
Wellvone (Well-vone) is a medicine which is used in Pneumocystis carinii infection. Wellvone contains atovaquone. It is supplied by GlaxoSmithKline UK.
The information in this Medicine Guide for Wellvone varies according to the condition being treated and the particular preparation used.
.Wellvone 750mg/5ml oral suspension
Information specific to Wellvone 750mg/5ml oral suspension when used in Pneumocystis carinii infection
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How to use your medicine – includes taking, storing and stopping your medicine, what to do if you take too much, plus the ingredients of your medicine.
Warnings – covers the suitability of the medicine for you and side effects and interactions with other medicines.
Your medicine and everyday activities – includes alcohol, your diet, complementary medicines and vitamins as well as driving.
Family planning – provides advice about whether this medicine is suitable for you in pregnancy and breast feeding.
Your medicine
Wellvone is used to treat Pneumocystis carinii pneumonia. This is a type of fungal infection which occurs mainly in people who have a weakened immune system.
Do not share your medicine with other people. It may not be suitable for them and may harm them.
The pharmacy label on your medicine tells you how much medicine you should take. It also tells you how often you should take your medicine. This is the dose that you and your prescriber have agreed you should take. You should not change the dose of your medicine unless you are told to do so by your prescriber.
If you feel that the medicine is making you unwell or you do not think it is working, then talk to your prescriber.
Back to top.When to take your medicine
Some medicines work best if they are taken at a specific time of day. Getting the most from your medicine can also be affected by what you eat, when you eat and the times at which you take other medicines. Make sure you follow any specific instructions given to you by your prescriber or that are in the Patient Information Leaflet that comes with this medicine.
Back to top.How to take your medicine
Some medicines have specific instructions about how to take them. This is because they work better when taken correctly. These instructions can include getting the right dose and special instructions for preparing the medicine. Make sure you follow any specific instructions given to you by your prescriber or that are in the Patient Information Leaflet that comes with this medicine.
In the case of Wellvone:
take this medicine with food. It is best to take Wellvone with food that has a high fat content
do not dilute this medicine
this medicine comes with a 5ml medicine measure which should be used to measure the correct dose
If you are having problems taking this form of Wellvone, you should talk to your prescriber or pharmacist. They may be able to give you advice on other ways to take your medicine or other preparations that are easier for you to take.
Back to top.Taking too much of your medicine
Taking extra doses of some medicines can be harmful. In some cases even one extra dose can cause you problems. If you take extra doses of your medicine, you must get medical advice immediately. You may need a test to assess the effect of taking extra doses. This is because the effects of taking too much medicine are very complex so it is very important that you seek medical advice.
Contact your prescriber, pharmacist, specialist clinic or NHS Direct on 0845 46 47 for advice.
Make sure you take all of your medicine containers with you if you are advised to go to hospital.
Back to top.Stopping your medicine
If you are not having any problems with this medicine, do not stop taking it, even if you feel better, unless you have completed the course or you are advised to stop taking it by your prescriber.
If you are in any doubt, contact your prescriber, pharmacist, specialist clinic or NHS Direct on 0845 46 47.
Back to top.Looking after your medicine
The instructions on how you should keep your medicine are on the pharmacy label. It is a good idea to keep your medicine in the original container. This will help to keep your medicine in the best condition and also allow you to check the instructions. Do not take the medicine if the packaging appears to have been tampered with or if the medicine shows any signs of damage. Make sure that the medicine is out of the sight and reach of children.
In the case of Wellvone:
do not store in temperatures above 25°C
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