What Is Lidocaine / Nifedipine Rectal Gel?
It is a compounded mucoadhesive gel that combines nifedipine — a calcium channel blocker — with lidocaine, a local anesthetic, for anorectal application. It is most often prescribed for chronic anal fissure and anorectal pain, and is prepared by prescription for an individual patient.
How Does It Work?
Nifedipine — Calcium Channel Blocker
Chronic anal fissures are linked to internal anal sphincter spasm and reduced blood flow. Nifedipine inhibits calcium inflow into the internal anal sphincter, reducing anal resting pressure, and appears to also modulate anal microcirculation — a non-surgical "chemical sphincterotomy." nih
Lidocaine — Local Anesthetic
Lidocaine blocks nerve sodium channels at the application site to ease the pain that makes fissures and anorectal procedures so uncomfortable.
MucoLox™ Mucoadhesive Base
The MucoLox™ component forms a mucoadhesive film that helps the gel stay in contact with the anorectal mucosa for sustained local delivery, while VersaBase® provides a smooth gel vehicle.
What Does the Evidence Show?
- The American Society of Colon and Rectal Surgeons recommends topical calcium channel blockers as a first-line medical therapy for chronic anal fissure, citing a better side-effect profile than nitrates.
- In a prospective, randomized, double-blind trial of 110 patients, a topical nifedipine-with-lidocaine ointment healed chronic anal fissures in 94.5% of treated patients at 6 weeks versus 16.4% of controls, while lowering mean anal resting pressure. American Urological Association
- In a randomized, double-blind, multicenter study of 283 patients with acute anal fissures, topical nifedipine achieved remission in about 95% of patients versus 50% of controls. nih
- A 2012 Cochrane review found calcium channel blockers as effective as glyceryl trinitrate for fissure healing, with fewer side effects.
These findings come from the cited studies and are not a promise of any individual outcome.
Why Is It Compounded?
There is no commercially available topical or rectal nifedipine product in the United States; oral nifedipine is approved for blood pressure and angina, not for anal fissure. When a prescriber wants this combination, a compounding pharmacy prepares it to the specified strengths.
How Is It Typically Used?
In the published protocol, a gel containing about 0.3% nifedipine and 1.5% lidocaine was applied twice daily for roughly six weeks, alongside conservative measures such as a high-fiber diet, fluids, and sitz baths. Dosing and duration are the prescriber's clinical decision. clinicaltrials
Safety Information
The combination is generally well tolerated, with mostly local effects, and topical calcium channel blockers cause fewer systemic effects (such as headache) than topical nitrates. Because lidocaine is absorbed across mucosa, prescribers consider the total dose to avoid systemic anesthetic effects; nifedipine is a calcium channel blocker, so cardiovascular history and interacting medications are also considered. Patient selection, dosing, and monitoring are the prescriber's responsibility.
Quality and Compliance
Mixwell Compounding Pharmacy prepares this gel in our purpose-built lab to the prescriber's exact strengths, dispensed only with a valid prescription. Mixwell follows USP <795> standards for non-sterile compounding, and our facility also meets USP <800> standards for hazardous-drug compounding. Mixwell is a non-sterile pharmacy and does not prepare sterile products or injectables. Compounded medications are not reviewed or approved by the FDA. Nothing here promises a specific result, and compounded preparations are not presented as superior to commercially available products.
References
- The American Society of Colon and Rectal Surgeons Clinical Practice Guidelines for the Management of Anal Fissures. Dis Colon Rectum. 2023.
- Perrotti P, Bove A, Antropoli C, et al. Topical nifedipine with lidocaine ointment vs. active control for treatment of chronic anal fissure: a prospective, randomized, double-blind study. Dis Colon Rectum. 2002;45(11):1468–1475. doi:10.1007/s10350-004-6452-1.
- Antropoli C, Perrotti P, Rubino M, et al. Nifedipine for local use in conservative treatment of anal fissures: preliminary results of a multicenter study. Dis Colon Rectum. 1999;42(8):1011–1015.
- Perrotti P, Dominici P, Grossi E, Cerutti R, Antropoli C. Topical nifedipine with lidocaine ointment versus active control for pain after hemorrhoidectomy: a multicentre, prospective, randomized, double-blind study. Can J Surg. 2010;53(1):17–24.
- Nelson RL, Thomas K, Morgan J, Jones A. Non-surgical therapy for anal fissure. Cochrane Database Syst Rev. 2012;(2):CD003431.
