药品英文名
Allopurinol
药品别名
痛风平、别嘌呤、赛洛力、痛风宁、全嘌呤、别嘌令醇、维洛林、Milurit、Zyloric、Isopurionl、Zyloprim、Adenock、Anzief
药物剂型
片剂:100mg。
药理作用
别嘌醇与体内的次黄嘌呤为同分异构体,它及其代谢产物可抑制次黄嘌呤氧化酶,从而使尿酸生成减少降低血中尿酸浓度,减少尿酸盐在骨、关节及肾脏的沉着,有助于痛风结节及尿酸结晶的重新溶解,促使痛风结节的消散。与其他排尿酸药不同的是,本品能减少尿中尿酸的排泄量,其作用不被水杨酸盐所对抗。
药动学
本品口服易吸收,自胃肠道可吸收80%~90%。口服后2~6h血药浓度达峰值,约70%在肝内代谢为具有活性的氧嘌呤醇。别嘌醇半衰期为2~8h,生物利用度约80%,肾功能损害者大大延长。由肾脏排泄,约10%以原形、70%以代谢产物随尿排出。
适应证
1.慢性原发性及继发性痛风的治疗,而对急性痛风无效。
2.用于治疗伴有或不伴有痛风症状的尿酸性肾病。
3.用于反复发作性尿酸结石患者,以预防结石的形成。
4.用于预防白血病、淋巴瘤或其他肿瘤在化疗或放疗后继发的组织内尿酸盐沉积、肾结石等。对已经形成的尿酸结石,也有助于结石的重新溶解。
5.本品还可用于非尿酸性结石如复发性钙结石尤其是草酸钙结石,它可显著降低新石的形成。
禁忌证
除对本品不能耐受外,无绝对禁忌证。
注意事项
1.本品属妊娠C类药品,孕妇、哺乳期妇女、特发性血液病及肾功能不全者慎用。治疗初期可诱发痛风,应与小剂量秋水仙碱或吲哚美辛合用加以预防。服药期间应大量饮水,并维持尿液呈中性或偏碱性,以促进尿酸排出。
2.本品不能控制痛风性关节炎的急性炎症症状,不能作为抗炎药使用。因为本品促使尿酸结晶重新溶解时可再次诱发并加重关节炎急性期症状。
3.本品必须在痛风性关节炎的急性炎症症状消失后(一般在发作后两周左右)方开始应用。
4.本品必须由小剂量开始,逐渐递增至有效量维持正常血尿酸和尿酸水平,以后逐渐减量,用最小有效量维持较长时间。
5.有肾、肝功能损害者及老年人应谨慎用药,并应减少一日用量。
6.用药期间应定期检查血象及肝肾功能。为调整用量,应定期检测血清尿酸含量。
7.老年人应谨慎用药,并应减少一日用量。
8.每次口服量不要超过300mg,每天量超过300mg时须分次服用。
不良反应
1.过敏反应:皮疹、皮肤瘙痒或荨麻疹等较常见,发生率3%~9%。严重者可有其他过敏反应,如剥脱性和紫癜性病变、多形性红斑等。一旦出现皮肤病变,应立即停药。
2.恶心、呕吐、腹痛、腹泻等消化道反应,发生率1%~3%,重症或持续存在者应对症处理。
3.末梢神经炎症状:如手脚麻木感、刺痛或疼痛、乏力等;血液学毒性,包括粒细胞减少、骨髓抑制等。发生率小于1%。
4.全身过敏性血管炎,能导致不可逆的肝脏中毒,应及早发现,及时停药。
用法用量
1.治疗痛风:口服,每天1~3次,每天100mg逐渐增加剂量,严重者可增至每天700~900mg,直到血清尿酸水平正常或接近正常,肝、肾功能不良患者剂量。维持量,每天100~200mg。儿童每天8mg/kg。
2.治疗肾结石:每次100~200mg,每天1~4次;或每次300mg,每天1次。
3.用于恶性肿瘤的继发性高尿酸血症:成人每次100~200mg,每天1~4次,儿童6岁以内每次50mg,每天3次;6~12岁每次100mg,每天3次,或300mg,每天1次,给药48h后,根据患者反应调整剂量。饭后服,并需大量饮水,每天尿量应保持2L以上。
药物相应作用
本品可使硫唑嘌呤。6-巯基嘌呤等嘌呤类药物在体内的代谢受抑制,提高其作用2~4倍,并增加毒性,因此如与这些药伍用时,应将这两种药减至常用量的1/4。本品不可与氯化钙、维生素C、磷酸钾(或钠)同服,因可增加肾脏中黄嘌呤结石的形成。应避免与布美他尼、美卡拉明及吡嗪酰胺合用,因可增加血中尿酸浓度。本品可增加烷化剂类药物的毒性,故在治疗恶性肿瘤引起的继发性高尿酸血症时,应在化疗(若用烷化剂)前接受本品治疗。本品可延长丙磺舒的血浆半衰期,丙磺舒则可增加本品的代谢产物别嘌呤的排泄,当两药合用于慢性痛风的治疗时,应减少丙磺舒的剂量,并增加别嘌醇的剂量。本品可抑制肝药酶活性,减慢口服抗凝剂等药的代谢,在合用时应减少后者的用量,并需随时监测凝血酶原的活性。对高血压或肾功能差的患者,本品与噻嗪类利尿剂同用时,有发生肾衰竭及出现过敏的报道。与环磷酰胺合用时,对骨髓抑制可更明显。与尿酸化药同用时,可增加肾结石形成的可能。
专家点评
国外报道,别嘌醇用于12例痛风及高尿酸血症患者,每天3次,每次100mg,在1~2周内血清尿酸盐水平除1例外均有下降,平均血尿酸浓度由8.3mg/100ml,下降至6.2mg/100ml,部分病例降至正常。每天服200~600mg可维持血尿酸小于5mg/100ml,尿酸小于每天500mg。长期用药不仅可抑制痛风石的形成或增大,并使已形成的痛风石逐渐缩小和溶解。由于本品的作用是抑制尿酸合成,与促进尿酸排泄的丙磺舒比较,其优点是,可以用于痛风性肾病患者,用药后不仅症状减轻,而且可以防止肾脏尿酸盐结石的形成。本品主要用于预防白血病、淋巴瘤,在化疗或放疗后继发的尿酸盐和尿结石形成,对于已形成的尿结石,本品也有助于重新溶解。
产地:watson(沃森)
Do not use allopurinol
If you are allergic (hypersensitive) to the active substance or any of the other ingredients of the medicinal product is prescribed for you . If you think you may be allergic, ask your doctor.
Allergy symptoms may include
- Crisis of asthma, shortness of breath, wheezing or rapid breathing audible.
- more or less sudden swelling of face, lips, tongue or other part of the body. This is especially critical if affects the vocal cords.
- Urticaria, itching, rash
- Anaphylactic shock (loss of consciousness, paleness, sweating, etc.).
Take special care with allopurinol
- If you have an acute attack of gout.
- if you are you pregnant, might be pregnant or are breast-feeding her child.
- if you have or have had kidney disease or liver disease.
- if you are taking or will begin taking any medication for heart disease or high blood pressure.
- If you notice that you bruise more easily than before, or if you get a sore throat or other signs of infection.
- if a rash , peeling skin, blisters or sores on the lips or mouth, wheezing (wheezing), palpitations or chest tightness, loss of consciousness: These symptoms may mean that you are allergic to allopurinol. Discontinue treatment and contact your doctor immediately.
If in doubt consult your doctor.
Should discontinue treatment and contact their doctor as soon as possible if, while you are taking allopurinol submit any of the following symptoms:
- High fever.
- Joint pain or painful swelling of the English, armpit or neck.
- jaundice (yellowing of the skin and eyes.)
- Nausea or vomiting (which may be bloody).
- General feeling of discomfort.
- Weakness, numbness or loss of consciousness.
- Headache, drowsiness, dizziness, impaired vision.
- chest pain, high blood pressure or pulse slowing.
- Swelling (edema) of the ankles.
- Feeling thirst, fatigue and weight loss.
- Appearance of boils.
- Appearance of blood in urine.
It is possible that at the start of treatment with allopurinol to precipitate an acute attack of gout. Your doctor will recommend the use of certain medications to avoid.
In the event of an attack by gout, it is necessary to stop treatment with allopurinol together whenever using a suitable anti-inflammatory medicine.
Taking other medicines
Tell your doctor or pharmacist if you are taking or have recently taken any other medicines, including herbal products obtained without a prescription.
Especially the following:
6-mercaptopurine, azathioprine, adenine arabinoside (Vidarabine), salicylates (aspirin, ..) uricosuric agents (probenecid, …), chlorpropamide, theophylline, phenytoin, ampicillin, amoxicillin, cyclophosphamide, doxorubicin, bleomycin, procarbazine, mechlorethamine, cyclosporine, coumarin anticoagulants and didanosine.
Special physiological situations
Pregnancy and lactation
Always consult your doctor or pharmacist before taking any medicine during pregnancy or breastfeeding.
Allopurinol is not recommended if you are pregnant or breast feeding.
Elderly:
The doctor will prescribe the lowest dose that produces a satisfactory answer. Caution should be used in cases of impaired renal function.
Driving and using machines
Due to its side effects (drowsiness, dizziness and impaired coordination), allopurinol may impair your ability to drive.
Do not drive, operate any tools or machines until you are reasonably certain that the drug does not limit its capabilities.
Consult your doctor or pharmacist before taking any medicine.
Recommendations for use of allopurinol
Follow instructions exactly allopurinol administration provided by your doctor. Consult your doctor or pharmacist if you have questions. Follow the instructions in preference to those given in this website which may be different. Ask your doctor to explain any question you do not understand, contained in the instruction booklet that comes with the medicine.
It is given orally exclusively.
Swallow the tablet whole with the help of a little water. It is usually taken once a day, usually after lunch.
The usual dose is:
Adults:
The usual dose of allopurinol to start treatment is 100 to 300 mg. The dose may be increased to 900 mg per day, depending on the case. In this case and if apareciesen upset stomach, you should divide the dose into several doses per day and accompany food.
Children under 15 years:
The usual dose of this medicine in children is 100 to 400 mg daily.
Elderly:
Your doctor will prescribe the lowest possible dose of allopurinol to get reduce uric acid levels and control their symptoms.
Use in patients with impaired hepatic or renal function:
If you have liver or kidney problems, your doctor will prescribe the lowest possible dose of allopurinol that successfully reduces uric acid levels and control their symptoms.
In case of kidney failure, your doctor may advise you to take less than 100 mg per day or tell you to take a single dose of 100 mg at intervals longer than one day.
If you are on dialysis 2 or 3 times a week, your doctor may prescribe a dose of 300-400 mg immediately after each dialysis session.
If you think the effect of the medicine is too strong or too weak, talk to your doctor.
If you have any further questions on the use of this product, ask your doctor or pharmacist.
Please note while taking allopurinol
If you become pregnant , consult your doctor.
If a doctor prescrib
es another medication , let them know you received allopurinol.
Check with your doctor regularly the course of the condition giving rise to the administration of allopurinol. Perhaps there is some reason that has prevented properly receive the indicated doses and induce misleading your doctor about treatment.
Do not restart on its own initiative allopurinol therapy without first talking to your doctor, or recommend their decision to another person, even if have the same symptoms you have. Nor is it advisable to discontinue or reduce the dose without considering the opinion of your doctor.
If during treatment with allopurinol is wrong, immediately consult your doctor.
If you use more than you should allopurinol
In this case, consult your local poison control center in your country or consult your physician.
In case of accidental ingestion of too much medication seek medical attention without delay or to the emergency room of the nearest hospital. Keep this leaflet with you.
If you forget to take allopurinol
If you forget a dose, retake the next dose as soon as you remember. Then continue the way they usually did.
Do not take a double dose to make up for forgotten doses.
If you miss several doses, it is best to contact your doctor for him to decide that you should do from that point.
If treatment interrrumpe
Your doctor will indicate the duration of treatment with allopurinol. Do not stop treatment early, even if you feel better.
If you have any further questions on the use of this product, ask your doctor or pharmacist.
Side effects of allopurinol
Like all medicines, Allopurinol can cause side effects, although not everybody gets them.
The probability of occurrence is higher when there are renal and / or liver.
The frequency of side effects is classified into:
Very common (more than 1 in 10 patients)
Common (more than 1 in 100 patients)
Uncommon (at least 1 in 1,000)
rare (less than 1 in 10,000)
Very rare (less than 1 per 10,000)
Infections and infestations
Very rare
Follicle infection
Blood and lymphatic system
Very rare
Decreased number of white blood cells (increased risk of infection), red blood cells (may make you tired, fatigue), platelets (cells involved in clotting blood, bruising or bleeding more easily than usual)
Immune System Disorders
Uncommon
Hypersensitivity reactions (allergy: possible appearance of skin rash, peeling skin, blisters or sores on the lips or in the mouth)
Rare
Serious hypersensitivity reactions associated with exfoliation, fever, joint pain or painful swelling of the English, armpit or neck, jaundice (yellowing of the skin and eyes), and other disorders of the skin and subcutaneous tissues (see below).
Very Rare
Angioimmunoblastic lymphadenopathy (swollen armpits, neck, English).
Very rarely can cause seizures, wheezing (wheezing), palpitations, chest tightness or blackouts.
Metabolism and nutrition
Very rare
Diabetes mellitus (high blood sugar levels in the blood), increased levels of lipids (fats) in the blood, increased blood uric acid.
Psychiatric Disorders
Very rare
Depression
Nervous System Disorders
Very rare
Weakness, numbness or loss of consciousness, paralysis, uncoordinated movements, impairment of normal sensation (neuropathy), drowsiness, headache, altered taste
Eye Disorders
Very rare
Niagara, visual disturbances
Ear and labyrinth
Very rare
Vertigo
Cardiac disorders
Very rare
Chest pain or slowing of the pulse
Vascular disorders
Very rare
High blood pressure
Gastrointestinal Disorders
Uncommon
Nausea, vomiting
Very rare
Appearance of blood in vomiting, excess fat in the stool, mouth infections, changes in bowel habits
Hepatobiliary disorders
Uncommon
Asymptomatic increases in liver function tests
Rare
Hepatitis
Skin and subcutaneous tissue
Frequently
Rash
Very rare
Hives, rash drug type, hair loss or discoloration
Renal and urinary disorders
Very rare
Appearance of blood in urine
Reproductive system and breast
Very rare
Male infertility, impotence, breast enlargement
General disorders at the site of Administració n
Very rare
Swelling (edema) of the ankles, malaise, fatigue, fever
There have been reports of fever with or without obvious signs or symptoms of a generalized hypersensitivity to allopurinol.
Do not be alarmed by this list of side effects and that it may not appear if any of them.
If you notice any side effects not listed in this website or in the leaflet accompanying the package, ask your doctor or pharmacist.
If any of the side effects gets serious, tell your doctor or pharmacist.