——0.4％硝酸甘油软膏获美国FDA批准治疗慢性肛裂疼痛
协和发酵麒麟有限公司子公司ProStrakan于 6月22日宣布，它的硝酸甘油（nitroglycerin）0.4％软膏获美国FDA批准，用于治疗与慢性肛裂有关的中度至重度疼痛。 它将是唯一被FDA批准用于此症的处方产品。
与肛裂相关疼痛相当难受。Rectiv的获准使此症患者能够恢复正常的起居生活。“现在我们有一个有效的和易于使用的外用药膏，让患者感激恢复他们的日常生活。”
肛裂相当普遍，在美国每年诊断和治疗肛裂者约有70万人。大便粗硬、排便用劲不当或腹泻后会导致肛门产生小块皮肤撕裂线，即肛裂。肛裂时通常会导致严重的排便疼痛和出血。慢性肛裂会显著影响患者生活质量。每次肛裂发作需6至8周方能愈合，如果久不愈合就需作手术治疗。
之前本品已在欧盟国家获准上市，商品名Rectiv
Manufacturer:
Aptalis Pharmaceutical Technologies
Pharmacological Class:
Nitrate.
Active Ingredient(s):
Nitroglycerin 0.4% (1.5mg/inch); oint; contains lanolin.
Indication(s):
Treatment of moderate-to-severe pain associated with chronic anal fissure.
Pharmacology:
Nitroglycerin is an organic nitrate that forms free radical nitric oxide (NO), which activates guanylate cyclase, resulting in an increase of guanosine 3’,5’-monophosphate (cyclic GMP) in smooth muscle and other tissues. This process leads to dephosphorylation of myosin light chains, which regulates the contractile state in smooth muscle and results in vasodilatation.
Clinical Trials:
Rectiv ointment was evaluated in a 3-week double-blind, randomized, multi-center, placebo-controlled study. Patients with a painful chronic anal fissure for at least 6 weeks and moderate or severe pain prior to treatment (≥50mm on the 100mm visual analog scale [VAS]) were randomized to receive 0.4% (1.5mg) nitroglycerin or placebo ointment applied to the anal canal every 12 hours. Pain as assessed by the change in VAS from baseline to Days 14–18 was lower in patients receiving 0.4% ointment compared to placebo. The mean change from baseline was 44mm for Rectiv and 37mm for placebo. The difference in the mean change in pain between Rectiv and placebo was –7.0mm (95% Confidence Interval: –13.6 to –0.4mm).
Legal Classification:
Rx
Adults:
Apply using finger covering (eg, plastic-wrap, disposable surgical glove, finger cot). ≥18 years: 1 inch of ointment intra-anally every 12 hours for up to 3 weeks. Not for oral, ophthalmic, or intravaginal use.
Children:
<18 years: not recommended.
Contraindication(s):
Concomitant PDE5 inhibitors (eg, sildenafil, vardenafil, tadalafil). Severe anemia. Increased intracranial pressure.
Warnings/Precautions:
Volume depleted. Hypotension. Cardiomyopathy. CHF. Acute MI. Poor cardiac function. Elderly. Pregnancy (Cat.C). Nursing mothers.
Interaction(s):
See Contraindications. Hypotension with PDE5 inhibitors, antihypertensive drugs (eg, calcium channel blockers, beta-adrenergic blockers, other nitrates). Potentiated by aspirin. Antagonizes tissue-type plasminogen activator (t-PA); caution. Anticoagulant effect of heparin may be reduced; monitor APTT. Potentiates ergotamine; possible ergotism. Additive vasodilating effects with alcohol; avoid use.
Adverse Reaction(s):
Headache, dizziness, hypotension (including orthostatic hypotension); rare: flushing, allergic reactions, application site reactions (eg, drug rash, exfoliative dermatitis), methemoglobinemia.
How Supplied:
Oint—30g
Last Updated:
2/13/2012
