Compounded Creams for Anal Fissures and Hemorrhoids: Clinical Insights and Formulation Guide

Introduction

Anal fissures and hemorrhoids are among the most common anorectal disorders, affecting up to 50% of adults by age 50 and causing significant discomfort, pain, and bleeding.¹ Tailored topical therapies delivered via compounded creams can optimize drug concentrations, combine synergistic agents, and improve patient adherence. This blog provides high-level clinical insights into the most commonly compounded formulations for anal fissures and hemorrhoids, along with practical guidance on vehicle selection, stability, and eNavvi’s streamlined compounding services.

Pathophysiology & Therapeutic Targets

• Anal fissures are linear tears in the anoderm caused by trauma (e.g., hard stools), leading to internal sphincter hypertonia, local ischemia, and pain.
• Hemorrhoids arise from dilated vascular cushions in the anal canal due to increased venous pressure, resulting in pruritus, pain, and bleeding.

Topical treatments aim to:

Reduce sphincter pressure (improve blood flow and pain control).

Promote mucosal healing (protective agents and growth factors).

Alleviate inflammation and pruritus.

Compounded Formulations for Anal Fissures

1. Glyceryl Trinitrate (Nitroglycerin) 0.2–0.4% Cream

• Mechanism: Nitric oxide donor that relaxes internal anal sphincter, enhancing perfusion.
• Dosing: Apply a pea-sized amount twice daily.
• Evidence: A randomized dose-finding study demonstrated improved healing rates in chronic fissures with 0.2–0.4% NTG versus placebo

2. Topical Calcium Channel Blockers

• Nifedipine 0.5% Cream
  • Superior to 0.2% NTG for pain relief, healing rate, and fewer side effects
• Diltiazem 2% Ointment
  • Effective in reducing sphincter tone and promoting fissure healing, often used when nifedipine is contraindicated.

3. Sucralfate 7% (± Metronidazole 1%) Cream

• Mechanism: Forms a protective polyanion gel that enhances mucus production and growth factor activity, promoting epithelial repair.
• Combination Therapy: Adding metronidazole 1% may offer antimicrobial support without compromising healing; studies show efficacy comparable to diltiazem 2%

Compounded Formulations for Hemorrhoids

1. Lidocaine 2–5% & Hydrocortisone 2% Cream

• Lidocaine (2–5%) provides rapid analgesia via sodium channel blockade; 5% formulations (e.g., RectiCare®) can be applied up to six times daily.
• Hydrocortisone 2% reduces inflammation, pruritus, and edema.
• Dosing: Apply a thin film 2–3 times daily to the perianal area; rectal cream versions may be inserted twice daily.

2. Phenylephrine 0.25–1% Cream

• Mechanism: α-adrenergic agonist that vasoconstricts hemorrhoidal vessels, reducing edema and discomfort.
• Use: Typically compounded for precise titration when OTC strengths are insufficient.

Vehicle Selection & Stability

• Bases: Nonaqueous vehicles (e.g., white petrolatum, pluronic lecithin organogel) enhance adhesion and residence time, reducing leakage.
• Stability: Studies recommend petrolatum bases to maintain potency of NTG, nifedipine, and hydrocortisone preparations.

Compounding Best Practices

Quality Control: Use USP-grade active ingredients; conduct batch testing.

pH Adjustment: Maintain pH 4.5–7.0 for skin compatibility.

Preservatives: Incorporate as needed for water-containing formulations.

Packaging: Utilize airless dispensers or light-protective tubes for photolabile agents.

eNavvi’s Online Compounding Platform

• Digital Prescription Pad: Select from clinician-vetted templates or customize formulations.
• Transparent Pricing: Cash prices displayed upfront, with no hidden fees.
• Fulfillment: Partner pharmacies accredited for compounding deliver nationwide in two days to all 50 states