Generic Name and Formulations:
Riociguat 0.5mg, 1mg, 1.5mg, 2mg, 2.5mg; tabs.
Company:
Bayer Healthcare Pharmaceuticals Inc.
Indications for ADEMPAS:
Treatment of persistent/recurrent chronic thromboembolic pulmonary hypertension (CTEPH), (WHO Group 4) after surgical treatment, or inoperable CTEPH, to improve exercise capacity and WHO functional class. Pulmonary arterial hypertension (PAH), (WHO Group 1) to improve exercise capacity, WHO functional class, and to delay clinical worsening.
Adult:
Initially 1mg three times daily; if intolerant, consider starting at 0.5mg three times daily. Increase dose by 0.5mg (three times daily) at intervals of ≥2 weeks as tolerated (SBP >95mmHg and no hypotension); max 2.5mg three times daily. If intolerant at any time, decrease dose by 0.5mg three times daily. Smokers: consider titrating to doses >2.5mg three times daily; may require dose reduction after smoking cessation. Concomitant strong CYP450 and P-gp/BCRP inhibitors: initiate at 0.5mg three times daily.
Children:
Not established.
Pharmacological Class:
Soluble guanylate cyclase (sGC) stimulator.
Contraindications:
Pregnancy (Cat. X). Concomitant nitrates or nitric oxide donors in any form, specific or non-specific phosphodiesterase (PDE) inhibitors (eg, sildenafil, tadalafil, vardenafil, dipyridamole, theophylline).
Warnings/Precautions:
In females of reproductive potential, exclude pregnancy prior to starting, monthly during, and for 1 month after treatment discontinuation; must use acceptable methods of contraception. Risk of hypotension or ischemia in hypovolemia, severe left ventricular outflow obstruction, resting hypotension, autonomic dysfunction; consider dose reduction if signs/symptoms occur. Bleeding risk. Pulmonary veno-occlusive disease: not recommended; discontinue if confirmed. Severe hepatic (Child Pugh C) or renal impairment (CrCl<15mL/min), or on dialysis: not recommended. Nursing mothers: not recommended.
Interactions:
See Contraindications. Potentiated by strong CYP450 and P-gp/BCRP inhibitors (eg, ketoconazole, itraconazole, ritonavir), antihypertensives; monitor for hypotension. Antagonized by smoking. May be antagonized by strong CYP3A inducers (eg, rifampin, phenytoin, carbamazepine, phenobarbital, St. John’s Wort). Separate dosing of antacids by ≥1hr of riociguat.
Adverse Reactions:
Headache, dizziness, dyspepsia/gastritis, nausea, diarrhea, hypotension, vomiting, anemia, gastroesophageal reflux, constipation.
REMS:
YES
Note:
For all female patients: available only through the Adempas REMS program. To enroll call (855) 4ADEMPAS or www.AdempasREMS.com.
How Supplied:
Tabs—42, 90
Adempas治疗肺动脉高压适应证获FDA批准
日前，美国食品药品管理局（FDA）批准拜耳研发的Adempas(Riociguat)用于治疗成人两种形式的肺动脉高压。
Adempas属于一类叫做可溶性鸟苷酸环化酶激活剂的药物，这类药物有助于动脉松弛，从而使血流增加、血压降低。这款药物用于术后慢性血栓栓塞性肺动脉高压(CTEPH)患者或无法接受手术患者的治疗，以改善他们的运动能力。Adempas也用于治疗不明原因引起的、遗传性的或与结缔组织病有关的肺动脉高压(PAH)，以改善患者的运动能力并推迟其疾病的临床恶化进度。
“Adempas是可溶性鸟苷酸环化酶激活剂中首款获批用于治疗肺动脉高压的药物，也是首款被证明对CTEPH患者有效的药物。”FDA药物评价与研究中心心血管与肾病药物产品部门主任Norman Stockbridge说。
Adempas治疗CTEPH的安全性和有效性结果基于一项由261名受试者参与的临床试验，试验中受试者被随机配给Adempas，用药剂量逐渐增加到2.5mg，每天用药三次，或配给安慰剂每天使用三次。研究的目的是检测受试者6分钟之内所能行走距离的变化。经过16周的治疗后，Adempas用药患者6分钟行走距离平均增加46米，远超过安慰剂组患者。
Adempas治疗中患者常见的副作用包括头痛、头晕、消化不良、组织肿胀(外围性水肿)、恶心、腹泻和呕吐。
