盐酸伐地那非片(艾力达)说明书如下:

【艾力达药品名称】
 通用名：盐酸伐地那非片
英文名：Vardenafil Hydrochloride Tablets

【艾力达主要成分】
艾力达主要成份为盐酸伐地那非。

【艾力达性状】
艾力达为浅橙色至暗橙色的薄膜衣片，除去薄膜衣后显白色。

【艾力达药理作用】
药理作用
阴茎勃起是涉及阴茎海绵体及其相关小动脉血管平滑肌的松弛的血流动力学过程。在性刺激过程中。阴茎海绵体内的神经元末梢释放一氧化氮(NO)，NO激活平滑肌细胞的鸟苷酸环化酶，使细胞内环鸟苷酸(cGMP)水平增加，终导致平滑肌松弛，增加阴茎内的血流量。伐地那非通过抑制人体阴茎海绵体内降解cGMP的磷酸二酯酶5型(PDE5)，增加性刺激作用下海绵体局部内源性的一氧化氮的释放，从而增强性刺激的自然反应。
毒理研究
急性毒性：大鼠的LD50是190mg/kg，光镜、电镜及视觉等检查均未发现药物对视觉悟的影响。
长期毒性：大鼠和和犬的无毒剂量（NOEL）均为3mg/kg。此外，动物均表现出与PDE5有关的心血管毒性，大鼠还表现出与PDE有关的胰腺、外分泌腺和甲状腺毒性。遗传毒性：离体鼠伤寒沙门氏菌回复突变试验、哺乳动物细胞HPRT突变试验、染色体畸变试验、以及在体小鼠微核试验，未发现伐地那非具有基因毒性和致突变性。
生殖毒性：大鼠和家兔经口给予伐地那非，未见伐地那非对动物生育力和胚胎发育产生影响。
致癌性：大鼠和小鼠分别连续24个月经口给予伐地那非，给药剂量按体表面积折算分别为临床推荐用药剂量20mg的225倍和450倍，按药时曲线下面积（AUC）折算分别为临床推荐用药剂量20mg的360倍和25倍，此时未见伐地那非具有致癌性。

【艾力达药代动力学】
吸收：伐地那非口服给药迅速吸收，禁食状态下快15分钟达到血药浓度(Cmax)，达峰时间(Tmax)90％为30-120分钟（平均为60分钟）。由于显著的首过效应，口服伐地那非的平均生物利用度大约是15％。在推荐剂量5-20mg范围内，口服伐地那非后，AUC（药物浓度-时间曲线下面积）和Cmax的增加几科与剂量增加成正比。伐地那非与高脂饮食（脂含量57％）同时摄入时，伐地那非的吸收率降低，Tmax延长60分钟，Cmax值平均降低20％，但AUC不受影响。伐地那非与普通饮食（脂含量30％）同时摄入时，其药代动学参数（Cmax,Tmax,和AUC）不受影响。因此，伐地那非和食物同服或单独服用均可。分布：伐地那非达到稳态时平均分布容积为208L。伐地那非及其主要活性代谢物M1与人血浆蛋白高度结合（约为95％），这种结合和药物总浓度无关且可逆。健康志愿者服用伐地那非90分钟后精液中药物浓度不超过服用剂量的0.00012％。
代谢：伐地那非主要通过肝脏酶系CYP3A4型代谢，小部分通过CYP3A5和CYP2C9同工酶代谢。伐地那非血浆消除半衰期大约为4-5小时。体内伐地那非主要的循环代谢（M1）来自哌嗪枸橼酸盐脱乙基，然后M1继续代谢。M1的血浆消除半衰期与原形药相似，约为4小时。体循环中，部分M1为结合型葡萄糖醛酸苷。血浆中非葡萄糖醛苷的M1约占原形成分的26％。代谢物M1具有与伐地那非相似的磷酸二酯酶选择性，在体外试验中，M1抑制PDE5的作用约为伐地那非的28％，占药效的7％。
排泄：伐地那非在体内的总清除率56升/小时，其终末半衰期为4-5小时。口服用药后，伐地那非以代谢物的形式排泄，大部分通过粪便排泄（91-95％），小部分通过尿液排泄（2-6％）。

【艾力达适应症】
治疗男性阴茎勃起功能障碍。

【艾力达用法用量】
用法：口服。推荐剂量：推荐开始剂量为10mg，在性交之前大约25-60分钟服用。在临床试验中草药，性交前4-5小时服用，仍显示药效。推荐剂量使用频率为一日一次。伐地那非和食物同服或单独服用均可。需要性刺激作为本能的反应进行治疗。剂量范围：根据药效和耐受性，剂量可以增加到20mg或减少到5mg。推荐剂量是每日20mg。肝损害：轻度肝损害的患者（Child-PughA）不需调整剂量；中度肝损害患者(Child-PughB)，由于伐地那非的清除率减少，建议起始剂量为5mg，随后根据耐受性和药效逐渐增加到10mg，重度肝损害患者（Child-PughC）的伐地那非的药代动力学研究尚未进行。肾损害：轻度、中度或重度肾损害的患者均无需进行剂量调整。透析患者的伐地那非药代动力学研究尚未进行。

【艾力达不良反应】
全球临床试验中，超过7800位患者服用了伐地那非，耐受性良好。发生的不良事件通常是一过性、轻度到中度的。发生率≥10％（很常见）：系统不良反应，整个机体头痛，心血管系统面色潮红，1％≤发生率＜10％（常见）：系统不良反应，消化系统消化不良，恶心，神经系统眩晕，呼吸系统鼻炎，0.1％≤发生率＜1％(少见)：系统不良反应，整个机体面部水肿，光过敏反应，背痛，心血管系统高血压，消化系统肝功能异常，GGTP升高代谢营养肌酸激酶升高，肌肉骨骼肌痛，神经系统嗜睡，呼吸系统呼吸困难，特殊感觉泌尿生殖系统，视觉异常、多泪阴茎异常勃起症（包括勃起延长或疼痛）0.01％≤发生率＜0.1％(罕见)：整个机体过敏反应（包括喉部水肿），心血管系统心绞痛、低血压、心肌缺血、体位性低血压、昏劂，神精系统紧张，呼吸系统鼻衄特殊感觉青光眼上市后：服用伐地那非进行性活动时，曾报道心肌梗死（MI）的发生，但无法确定心肌梗死与伐地那非，或与性活动，或与患乾潜在的心血管疾病，或与这些因素综合作用直接相关。

【艾力达禁忌】
1．对药物的的任何成分（活性成分或非活性成分）有过敏症状的患者禁用。
2．与PDE抑制剂在NO/cE、GMP通路的作用机制相同，PDE5抑制剂可能增强硝酸盐类药物的降压效果。因此，服用硝酸盐类或一氧化氮供体治疗的患者避免同时使用伐地那非。
3．避免HIV蛋白激酶抑制剂印地那韦或利托那韦和伐地那非同时使用，因为它们是强效CYP3A4抑制剂。

【艾力达孕妇及哺乳期妇女用药】
不适用。

【艾力达儿童用药】
儿童（出生至16岁）：伐地那非不适用于儿童。

【艾力达老人用药】
老年患者（≥65岁）伐地那非的清除率减少，起始剂量考虑为5mg。

【艾力达贮藏】
低于25℃密封保存。

【艾力达生产企业】
BayerPharmaAG

Vivanza

Active Substance: vardenafil 
Common Name: vardenafil 
ATC Code: G04BE09
Marketing Authorisation Holder: Bayer Pharma AG  
Active Substance: vardenafil 
Status: Authorised
Authorisation Date: 2003-03-04
Therapeutic Area: Erectile Dysfunction
Pharmacotherapeutic Group: Urologicals

Therapeutic Indication

Treatment of erectile dysfunction in adult men. Erectile dysfunction is the inability to achieve or maintain a penile erection sufficient for satisfactory sexual performance.

In order for Vivanza to be effective, sexual stimulation is required.

Vivanza is not indicated for use by women.

What is Vivanza?

Vivanza is a medicine that contains the active substance vardenafil. It is available as film-coated tablets (5, 10 and 20 mg) and as orodispersible tablets (10 mg). Orodispersible tablets are tablets that dissolve in the mouth.

What is Vivanza used for?

Vivanza is used to treat adult men with erectile dysfunction (sometimes called impotence), when they cannot get, or keep, a hard penis (erection) sufficient for satisfactory sexual activity. For Vivanza to be effective, sexual stimulation is required.

The medicine can only be obtained with a prescription.

How is Vivanza used?

The recommended dose of Vivanza is 10 mg, taken by mouth with or without food, about 25 to 60 minutes before sexual activity; patients should not take more than one dose a day. The orodispersible tablets must be taken without liquid. If Vivanza is taken with a high-fat meal, the onset of activity may be delayed. The dose may be increased to a maximum of 20 mg or decreased to 5 mg depending on the effectiveness and side effects. Patients with liver problems or severe kidney problems should start treatment on the 5 mg dose.

The dose may need to be adjusted in patients taking other medicines that block enzymes that break down Vivanza. For full details, see the package leaflet.

How does Vivanza work?

The active ingredient of Vivanza, vardenafil, belongs to a group of medicines called phosphodiesterase-type-5 (PDE5) inhibitors. It works by blocking the phosphodiesterase enzyme which normally breaks down a substance known as cyclic guanosine monophosphate (cGMP). During normal sexual stimulation, cGMP is produced in the penis, where it causes the muscle in the spongy tissue of the penis (the corpora cavernosa) to relax. This allows blood to flow into the corpora, producing the erection. By blocking the breakdown of cGMP, Vivanza restores erectile function. Sexual stimulation is still needed to produce an erection.

How has Vivanza been studied?

Vivanza film-coated tablets have been compared with placebo (a dummy treatment) in four main studies including 2,431 men aged 20 to 83 years. One study was carried out in diabetic men and another in men who had had their prostate gland removed. Two additional main studies compared orodispersible tablets with placebo in 701 men aged 21 to 84 years.

The main measure of effectiveness was the ability to get and maintain an erection. This was recorded in two questionnaires completed at home.

What benefit has Vivanza shown during the studies?

Vivanza was significantly more effective than placebo for all measures in all studies.

What is the risk associated with Vivanza?

The most common side effect with Vivanza (seen in more than 1 patient in 10) is headache. For the full list of all side effects reported with Vivanza, see the package leaflet.

Vivanza must not be used in people who are hypersensitive (allergic) to vardenafil or any of the other ingredients. It must not be used when sexual activity is inadvisable, such as in men with severe heart disease. It must also not be taken by patients who have ever had loss of vision because of a problem with blood flow to the nerve in the eye (non arteritic anterior ischemic optic neuropathy or NAION). Vivanza must not be taken with nitrates (medicines used to treat angina).

Because Vivanza has not been studied in the following groups of patients, they must not use the medicine:

· patients with severe liver disease or end-stage kidney disease requiring dialysis;

· patients who have hypotension (low blood pressure);

· patients who have had a stroke or a heart attack within the last six months;

· patients with unstable angina or hereditary eye problems known as ‘retinal degenerative disorders’.

Vivanza must not be taken with some medicines, such as ketoconazole and itraconazole (to treat fungal infections) in men over 75 years, or medicines called ‘HIV protease inhibitors’ such as ritonavir or indinavir (to treat HIV infection).

In addition, Vivanza must not be taken with medicines known as guanylate cyclase stimulators, including riociguat (used to treat pulmonary hypertension [high blood pressure in the lungs]).

Why has Vivanza been approved?

The CHMP decided that Vivanza’s benefits are greater than its risks and recommended that it be given marketing authorisation.

What measures are being taken to ensure the safe and effective use of Vivanza?

A risk management plan has been developed to ensure that Vivanza is used as safely as possible. Based on this plan, safety information has been included in the summary of product characteristics and the package leaflet for Vivanza, including the appropriate precautions to be followed by healthcare professionals and patients.

Other information about Vivanza

The European Commission granted a marketing authorisation valid throughout the European Union for Vivanza on 4 March 2003.

For more information about treatment with Vivanza, read the package leaflet (also part of the EPAR) or contact your doctor or pharmacist.