Lidocaine/Nitroglycerin

• Local pain support — Lidocaine works quickly to numb sensitive anal tissue, providing comfort for patients with fissures or post-procedural soreness.¹
• Anal sphincter spasm management— Nitroglycerin helps relax the internal anal sphincter, comforting the painful muscle tightening that is a hallmark of ongoing anal fissures.²
• Blood flow modulation to support tissue recovery — By dilating local blood vessels, nitroglycerin may contribute to oxygen and nutrient delivery to injured tissue, supporting tissue recovery.³
• Non-surgical option — Topical nitroglycerin is characterized in the clinical literature as a non-surgical route of administration. Whether a surgical or non-surgical approach is appropriate is determined by your prescriber. Individual outcomes may vary.⁴
• Targeted delivery — Because the ointment is applied directly to the affected area, systemic (whole-body) absorption is limited compared to oral medications.¹
• May support long-term maintenance — Some studies referenced in the literature indicate that using nitroglycerin may support the long-term maintenance of fissure recurrence when used consistently as directed.⁵
• Well-established drug profile — Both lidocaine and nitroglycerin have decades of documented use in clinical settings, supporting a well-studied tolerability profile when used topically.⁶

Potential Side Effects

• Headache — The most commonly reported side effect of nitroglycerin, even with topical use; usually mild and temporary. Taking the ointment in a lower amount or less frequently may help.²
• Dizziness or lightheadedness — Some patients experience a drop in blood pressure after application, especially when standing up quickly.
• Local skin irritation — Redness, burning, or itching at the application site may occur, particularly with more frequent use.
• Numbness beyond the target area — Lidocaine may occasionally numb surrounding tissue; avoid touching eyes or sensitive areas after application.¹
• Flushing — Warmth or redness of the face may occur due to nitrate-related blood vessel dilation.
• Methemoglobinemia (rare) — A rare but serious condition associated with high doses of lidocaine. Contact your provider immediately if you notice pale or bluish skin, shortness of breath, or unusual fatigue.⁷

Warnings and Precautions

• Use only as directed — apply the smallest amount as prescribed by your provider.
• Avoid contact with eyes, mouth, and open wounds not being addressed.
• Do not use more frequently or in higher quantities than prescribed, as excess nitroglycerin can cause significant drops in blood pressure.
• If you experience severe headache, feel faint, or have chest discomfort after application, lie down and contact your provider.
• Store the ointment out of reach of children and pets.
• Inform your provider of all other medications you are taking before starting this compounded medication.

Contraindications

• Known allergy or hypersensitivity to lidocaine, other local anesthetics, or nitroglycerin
• Concurrent use of phosphodiesterase-5 (PDE-5) inhibitors such as sildenafil (Viagra), tadalafil (Cialis), or vardenafil — combining with nitroglycerin can cause a severe, life-threatening drop in blood pressure⁸
• Severe low blood pressure (hypotension) or recent history of shock
• Pregnancy or breastfeeding — consult your provider before using; safety data for topical nitroglycerin in pregnancy is limited
• Severe liver disease — may affect lidocaine metabolism
• Children under 18 — use only under provider guidance

Drug Interactions

This medication may interact with several other drugs. Always share your full medication list with your prescriber and pharmacist before starting the regimen.⁸

• PDE-5 inhibitors (sildenafil, tadalafil, vardenafil): Combining these with nitroglycerin — even topically — can cause a dangerous, rapid fall in blood pressure. Do not use these together.
• Other nitrate medications: Using additional nitrate-based drugs alongside nitroglycerin ointment can compound blood-pressure-lowering effects.
• Antihypertensive medications (blood pressure drugs): May have an additive effect on lowering blood pressure when combined with nitroglycerin.
• Antiarrhythmic drugs (e.g., amiodarone): May increase the risk of lidocaine-related side effects if significant systemic absorption occurs.
• Alcohol: Can promote blood vessel dilation from nitroglycerin, increasing the risk of dizziness or fainting.

Lidocaine works by temporarily blocking the nerve signals in the tissue where it is applied. This effect sets in within a few minutes of application and typically lasts long enough to provide meaningful comfort during and after bowel movements or daily activity.¹

Nitroglycerin acts differently. It belongs to a class of medications called nitrates that release nitric oxide in the body. Nitric oxide is a natural signaling molecule that tells smooth muscle to relax. The internal anal sphincter is a smooth muscle — when it tightens abnormally, it restricts blood flow to the lining of the anal canal and slows recovery of existing fissures. Nitroglycerin tells that muscle to let go, relieving the spasm and allowing blood flow to resume.²³

Because both agents are applied directly to the affected area rather than taken by mouth or by injection, very little medication enters the bloodstream. This targeted approach is one of the reasons the combination is well-tolerated in most patients. The small amount of nitroglycerin that does absorb through the skin can occasionally cause a mild headache.⁶

Together, lidocaine and nitroglycerin help with both sides of the concern at once: lidocaine manages the immediate pain while nitroglycerin works to remove the underlying barrier to tissue recovery. Early studies and clinical experience suggest that this dual approach may provide accelerated clinical response and comprehensive support compared to either agent alone.⁵

IMPORTANT INFORMATION ABOUT COMPOUNDED MEDICATIONS

This medication has been compounded (custom-prepared) by a pharmacy. Compounded medications are specially prepared for individual patient needs based on a valid prescription from a prescribing healthcare practitioner and, as such, are not reviewed or approved by the U.S. Food and Drug Administration (FDA) for safety or efficacy. Compounded drugs are intended for patients whose prescriber has determined their medical needs are not met by an available FDA-approved drug. These statements have not been evaluated by the FDA.

This compounded preparation:

• Has not been approved by the FDA
• Has not undergone FDA review for safety, effectiveness, or quality
• Is prepared specifically for you based on your prescriber's order
• Individual outcomes may vary

Dosing is determined by the prescribing provider based on patient-specific factors. Always follow your healthcare provider's instructions. Compounded medications are not subject to FDA approval and lack the same safety and efficacy data as FDA-approved commercial medications. This medication should be prescribed and monitored by a licensed healthcare professional familiar with the condition being addressed and the specific applications of the medication.

1. Butterworth JF, Mackey DC, Wasnick JD. Morgan & Mikhail's Clinical Anesthesiology, 6th ed. McGraw-Hill Education; 2018. [Lidocaine mechanism of action, pp. 263–278]
2. Lund JN, Scholefield JH. A randomised, prospective, double-blind, placebo-controlled trial of glyceryl trinitrate ointment in treatment of anal fissure. Lancet. 1997;349(9044):11–14. doi:10.1016/S0140-6736(96)06090-4
3. Carapeti EA, Kamm MA, Phillips RK. Topical diltiazem and bethanechol decrease anal sphincter pressure and heal anal fissures without side effects. Dis Colon Rectum. 2000;43(10):1359–1362. doi:10.1007/BF02236630 [Discusses vasodilator mechanisms relevant to nitrates]
4. Brisinda G, Maria G, Bentivoglio AR, et al. A comparison of injections of botulinum toxin and topical nitroglycerin ointment for the treatment of chronic anal fissure. N Engl J Med. 1999;341(2):65–69. doi:10.1056/NEJM199907083410201
5. Nelson RL, Thomas K, Morgan J, Jones A. Non-surgical therapy for anal fissure. Cochrane Database Syst Rev. 2012;2:CD003431. doi:10.1002/14651858.CD003431.pub3
6. Perrotti P, Bove A, Antropoli C, et al. Topical nifedipine with lidocaine ointment versus active control for treatment of chronic anal fissure: results of a prospective, randomized, double-blind study. Dis Colon Rectum. 2002;45(11):1468–1475. doi:10.1007/s10350-004-6456-9
7. Guay J. Methemoglobinemia related to local anesthetics: a summary of 242 episodes. Anesth Analg. 2009;108(3):837–845. doi:10.1213/ane.0b013e318187c4b7
8. Münzel T, Daiber A, Mülsch A. Explaining the phenomenon of nitrate tolerance. Circ Res. 2005;97(7):618–628. doi:10.1161/01.RES.0000184694.03262.6d [Covers nitrate pharmacology including drug interactions]

Q: What does this ointment actually do?

A: This ointment does two things at once. The lidocaine portion numbs the tissue at the application site, which may help manage discomfort — especially during and after bowel movements. The nitroglycerin portion relaxes the muscle inside the anal canal, which may support blood flow and creates a better environment for the tissue to heal. Together, they address both the pain you feel today and the underlying cause that's making healing difficult.

Q: Why do I have an anal fissure, and why won't it heal on its own?

A: Anal fissures — small tears in the lining of the anal canal — are often caused by hard stools, straining, or trauma to the area. The tricky part is that the internal anal sphincter muscle can go into spasm after a fissure forms, cutting off some of the blood flow the tissue needs to repair itself. This is why fissures can become a frustrating cycle: pain causes spasm, spasm reduces healing, and the cycle repeats. This ointment is formulated to address both components of that cycle. Individual outcomes may vary and are determined by your prescriber.

Q: How soon will I start to feel better?

A: Onset of local numbing from lidocaine is reported in the clinical literature to occur within minutes of application. Individual responses vary. The tissue-recovery effects from nitroglycerin take longer to show potential benefits — research suggests that consistent daily use over several weeks is typically needed to see favorable changes in fissure recovery. ⁴ Give the medication time, and follow your provider's instructions for the full course.

Q: Can I use this ointment if I take medication for erectile dysfunction?

A: This is very important: if you take medications like sildenafil (Viagra), tadalafil (Cialis), or vardenafil (Levitra), you must tell your provider before using this ointment. Combining these drugs with nitroglycerin — even topical  — can cause a severe and potentially dangerous drop in blood pressure. Your provider will guide you on the appropriate options.

Q: Do I need to use a glove or finger cot for internal application?

A: It is good practice to protect your finger, and your provider or pharmacist may supply you with a finger cot for this purpose. Whether you use a glove, a finger cot, or a clean bare finger, the most important things are to wash your hands thoroughly before and after application and to apply only a thin layer of ointment.