英文药名: Levitra (Vardenafil Tablets)

中文药名: 艾力达（伐地那非片）

生产厂家: Bayer Corporation

药品名称

盐酸伐地那非片.艾力达.
适应症

治疗男性阴茎勃起功能障碍。
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。最大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。最大推荐剂量是每日20mg。
肝损害： 轻度肝损害的患者（Child-Pugh A）不需调整剂量；中度肝损害患者(Child-Pugh B),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-Pugh C）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。
如果您有任何疑问，请遵医嘱。
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 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。"
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。
孕妇及哺乳期妇女用药

不适用
儿童用药

儿童（出生至16岁）：伐地那非不适用于儿童。
老年患者用药

老年患者（≥65岁）伐地那非的清除率减少，起始剂量考虑为5mg。
药物过量

单剂量受、试者研究中，最高试验剂量达到每日80mg 。最高试验剂量（每日80m，）耐受性良好而未发生任何严重药物不良反应。同样持结果在另一项应用40mg 伐地那非以40mg伐地那非（每日一次），连续服药4周的临床试验中得到证实。当伐地那非以40mg每日两次的剂量服用时，观察到儿例较严重的背痛，然而并未证实有肌肉或神精毒性作用。服药过量时，应根据需要给予一般的剂量服用时，观察到儿例较严得的背痛，然而并未证实有肌肉或神经毒性作用。服医药费过量时，应根据需要给予一般的对症治疗措施。由于伐地那非与血浆蛋白结合率很高，且不主要由尿液清除，因此肾透析不会提搞其体内的清除率。

包装规格：

10mg *4片
   
20mg *4片
   
5mg *4片

10mg *10片
   
20mg *10片

Levitra
Generic Name: vardenafil hydrochloride
Dosage Form: tablet, film coated
FULL PRESCRIBING INFORMATION
Indications and Usage for Levitra
Levitra® is indicated for the treatment of
Levitra Dosage and Administration
------------------------------------------------------------------------------------------
Active substance: Vardenafil (Vardenafil)
Structure and Composition Levitra (Levitra): Film-coated tablets.
1 table. – Vardenafil 5 mg, 10 mg, 20 mg (equivalent to 5.926, 11.852, 23.705 mg of vardenafil hydrochloride trihydrate, respectively). Inactive ingredients: crospovidone, magnesium stearate, MCC, silica colloidal anhydrous, macrogol 400, hypromellose, titanium dioxide, iron oxide yellow, iron oxide red in blisters 1, 2, 3 or 4 pieces.; A stack of cardboard 1, 2 or 3 boxes.
Description of the dosage form Levitra (Levitra): Round, biconvex, slightly rough tablets from light orange to grayish-orange color, coated, embossed:
Tablets 5 mg: on one side – “5″, on the other – corporate Bayer cross.
Tablets 10 mg: on one side – “10″, on the other – corporate Bayer cross.
Tablets 20 mg: on one side – “20″, on the other – corporate Bayer cross.
Pharmacological action of Levitra (Levitra): improving erectile function (increases potency).
Pharmacokinetics Levitra (Levitra): Absorption. After ingestion it’s rapidly absorbed. When you receive an empty stomach early peak Cmax can be reached in 15 minutes, but 90% of the average Cmax achieved within 60 min (30 to 120 min). The absolute bioavailability of approximately 15%. At the recommended dose range (5-20 mg), the parameter “area under the curve of the concentration-time» (AUC) and Cmax increased in proportion to the dose.
When receiving vardenafil simultaneously with food containing high fat (57%), the rate of absorption decreases with time to reach Cmax (Tmax) to 60 min, and the value of the average Cmax decreased by 20% without a significant change in the AUC. When receiving a normal diet containing no more than 30% fat, the pharmacokinetic parameters of vardenafil (Cmax, Tmax, AUC) are not changed.
Distribution. The average volume of distribution at steady state vardenafil is 208 liters, which demonstrates its good tissue distribution. Vardenafil and its major metabolite (M1) is well bound to plasma proteins (95%), and this property is reversible and does not depend on the total concentration of the drug.
Based on the results of measurements of vardenafil in semen of healthy men after 90 minutes after ingestion, it can be assumed that no more than 0.00012% of the administered dose may be determined in the semen of patients.
Metabolism. Vardenafil is metabolized predominantly liver enzymes involving izoformyCYP3A4, as well as CYP3A5 and CYP2C9 cytochrome P450. The average T1 / 2 of vardenafil is 4-5 h, and the major metabolite M1 – about 4 hours in the blood contained glucuronide metabolite M1. The concentration of the rest of the metabolite M1 is 26% of the concentration of active ingredient. Profile selectivity for phosphodiesterase in M1 is similar to that of vardenafil; in vitro ability to inhibit PDE-5 is 28% compared to vardenafil, which corresponds to 7% efficacy.
Excretion. The total clearance of vardenafil is 56 L / h, the final T1 / 2 – about 4-5 hours after oral vardenafil in the form of metabolites derived primarily through the gastrointestinal tract (91-95% dose), to a lesser extent – by the kidneys (2-6% of the dose ).
Elderly patients. In healthy older men (? 65 years) compared with younger individuals (? 45 years) hepatic clearance of vardenafil was reduced. The average AUC in the elderly increased by 52%. However, differences in efficacy and safety in elderly patients and young adults are not marked.
Renal failure. Patients with mild (Cl creatinine> 55-80 ml / min) and moderate (Cl creatinine> 30-50 ml / min), degree of renal dysfunction vardenafil pharmacokinetic parameters are comparable with those in healthy subjects. With severe renal impairment (Cl creatinine <30 ml / min), the mean AUC value of the index rises by 21% and Cmax decreased by 23%. Significant correlation between creatinine clearance and vardenafil plasma concentrations (AUC and Cmax) are not marked.
In patients on hem dialysis, pharmacokinetics of vardenafil has not been studied.
Abnormal liver function. Patients with minor or moderate hepatic dysfunction Vardenafil clearance is reduced in proportion to the degree of liver function abnormalities. Mild hepatic failure (stage A to Child-Pugh) marked rises in AUC and Cmax of 1,2 times (AUC – 17%, C max – 22%), while for moderate (stage B according to Child-Pugh) – 2,6 (160%) and 2.3 (130%) times, respectively, compared with healthy volunteers.
Patients with severe hepatic dysfunction (Stage B of Child-Pugh), the pharmacokinetics of vardenafil has not been studied.
Pharmacodynamics Levitra (Levitra): penile erection is a homodynamic process, based on the relaxation of smooth muscles of cavernous bodies and placed them in the arterioles. During sexual stimulation of the nerve endings of the corpus cavernous released nitric oxide (NO), activates the enzyme granulate cycles, which leads to an increase in content in the cavernous bodies of cyclic guanidine monophosphate (cGMP). The result is relaxation of smooth muscles of cavernous bodies, which increases blood flow to the penis.
By blocking specific phosphodiesterase fifth type (PDE-5), which participates in the cleavage of cGMP, vardenafil enhances local action of endogenous nitric oxide (NO) in cavernous bodies during sexual stimulation.
This effect accounts for the ability to Levitra enhance response to sexual stimulation.
Indications Levitra (Levitra): Erectile dysfunction (inability to achieve and maintain an erection necessary for sexual intercourse).
Contraindications Levitra (Levitra): hypersensitivity to any component of the drug;
simultaneous application of nitrate or drugs, which are nitric oxide donators;
combination with HIV protease inhibitors like endeavor or ritonavir.
Precautions:
congenital prolongation QT;
anatomical deformity of the penis (curvature, cavernous fibrosis, Peyronie’s disease);
diseases predisposing to priapism (sickle cell anemia, multiple myeloma, leukemia);
severe hepatic dysfunction;
kidney disease in the terminal stage;
hypotension (SBP alone – less than 90 mm Hg. Art.)
recent stroke and myocardial infarction;
unstable angina;
hereditary degenerative diseases of the retina (eg retinitis pigmentosa);
tendency to bleeding and exacerbation of peptic ulcer disease;
aortic stenosis and idiopathic hypertrophic subaortalny stenosis.
Side effects: Levitra, generally well tolerated, side effects, usually slightly or moderately expressed and are transient in nature.
These placebo-controlled clinical trials
The frequency of – 1%
Nervous system: dizziness, headache.
Cardiovascular system: hot flashes (hot flashes, redness of facial skin, “hot flashes”).
Respiratory System: congestive hyperemia of the nasal mucosa (mucosal edema, rhinitis, rhino rhea).
Digestive system: dyspepsia, nausea.
Data from all clinical trials
The most common -> 10%
Nervous system: headache.
Cardiovascular system: hot flashes (hot flashes, redness of facial skin, “hot flashes”).
Typical -> 1 – <10%
Nervous System: dizziness.
Respiratory System: congestive hyperemia of the nasal mucosa (mucosal edema, rhinitis, rhino rhea).
Digestive system: dyspepsia, nausea.
Atypical -> 0.1 – <1%
Nervous System: somnolence.
Organs of vision: increased tearing blurred vision (luminance of view).
Cardiovascular system: hypertension, hypotension, orthostatic hypotension.
Respiratory System: dyspnea, epistaxis.
Skin: facial swelling, photosensitivity reaction.
Rare -> 0,01 – <0,1%
Immune System: hypersensitivity reaction.
Psychiatric disorders: anxiety.
Nervous system: syncope.
Organs of vision: increased intraocular pressure.
Cardiovascular System: angina pectoris, myocardial ischemia.
Respiratory system: laryngeal edema.
Musculoskeletal system: increased muscle tone.
Reproductive system: Extension of an erection or painful erections.
There are rare post marketing reports of cases of anterior ischemic optic neuropathy (PINZN), which leads to impaired vision (including the permanent loss of vision), related in time with taking PDE-5 inhibitors, including and Levitra, patients, many of which have the associated risk factors for this condition as an anatomical defect of the optic disc, age over 50 years, diabetes mellitus, hypertension, coronary artery disease, hyperlipidemia and smoking. Not established whether the development is related directly PINZN using PDE-5 inhibitors, or with the existing patient concomitant vascular risk factors, and anatomic defects, or with a combination of these factors, or other reasons.
Cases of visual impairment, including temporary or permanent loss of vision, which are associated in time with the inhibitors of PDE-5, including and Levitra. Not established whether these cases are directly taking PDE-5 inhibitors, or with concomitant vascular risk factors, or other reasons.