New Drugs and Devices From 2011 – 2012 That Might Change Your Practice

Joe Lex, MD


Western J Emerg Med. 2013;14(6):619-628. 

In This Article

Rectiv® (Nitroglycerin Ointment 0.4%)

Most anal fissures are caused by stretching of the anal mucosa beyond its capability; in adults, this includes constipation, the passing of large, hard stools, prolonged diarrhea, or anal sex. Sometimes they cause bright red blood on the toilet paper, occasionally in the toilet. When acute they cause pain after defecation; chronic fissures cause pain less frequently. Anal fissures typically extend from the anal opening and are usually posteriorly in the midline, probably because of the relatively unsupported nature and poor perfusion of the anal wall in that location. Fissures can be superficial or extend down to the underlying sphincter muscle. The incidence of anal fissures is around 1 in 350 adults, equally common in men and women, and most frequent in young adults aged 15 to 40.

First-line management of anal fissure generally includes increasing fluid and fiber intake, stool softeners, topical analgesics (e.g., 1% lidocaine) or anti-inflammatories (e.g., 1% hydrocortisone), and sitz baths.

Nitroglycerin is a vasodilator and causes smooth muscle relaxation. It was first used by William Murrell to treat anginal attacks in 1878. As a topical agent, it is applied as a 0.2% to 0.4% ointment. When applied topically to the anus, it increases local blood flow, relaxes anal sphincter tone, and reduces anal pressure. The literature is mixed, but according to pooled data, topical nitroglycerin appears to be associated with healing in at least 50% of treated chronic fissures and is associated with a significant decrease in pain.

The recommended dosage is 1 inch of ointment (375 mg of ointment equivalent to 1.5 mg of nitroglycerin) applied intra-anally every 12 hours for up to 3 weeks. As with all nitrates, Rectiv® is contraindicated within a few days of using PDE5 inhibitors such as sildenafil, tadalafil, and vardenafil due to potentiating hypotensive effects. After treatment with topical nitroglycerin, recurrence of anal fissures occurs in about one-third of the patients over the following 18 months.

Topical calcium channel blockers such as diltiazem and nifedipine inhibit calcium ion entry through voltage-sensitive areas of vascular smooth muscle and also cause muscle relaxation and vascular dilatation. By relaxing the internal anal sphincter, calcium channel blockers also lower the resting anal pressure. In fact there is evidence that topical calcium channel blockers may be as effective as topical nitroglycerin, but with fewer side effects, such as headache. Diltiazem and nifedipine are not available in topical ointment or gel form and must be compounded by a pharmacist. The typical strengths used for anal fissure are diltiazem 2% and nifedipine 0.2% to 0.5%. The usual dosing is a pea-sized amount applied rectally 2 to 4 times daily.

Considering the ubiquity of nitroglycerin, the cost for a 30-gram tube is staggeringly expensive: US$386.