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Rectal Rocket Hydrocortisone 2% | Lidocaine 3% | Nifedipine 0.2%

Rectal Rocket Hydrocortisone 2% | Lidocaine 3% | Nifedipine 0.2% is a gastrointestinal or oral/rectal preparation selected when the prescriber needs a customized route, strength, texture, flavor, or combination for a patient-specific need.

SuppositoryRectalRx Only503A Compounded

Rectal Rocket is a compounded anorectal suppository (torpedo-shaped) or ointment combining hydrocortisone 2%, lidocaine 3%, and nifedipine 0.2%—three pharmacologically distinct active ingredients that address the pain, inflammation, and vascular/sphincter dysfunction underlying hemorrhoids and anal fissures. Nifedipine relaxes the internal anal sphincter to promote fissure healing, lidocaine provides rapid local anesthesia, and hydrocortisone reduces inflammatory edema and pruritus. Genesis Compounding prepares this as a prescription-only 503A compounded preparation that is not FDA-approved as a combined formulation.

Active IngredientPharmacologic Role
Hydrocortisone 2%Topical corticosteroid that suppresses local inflammatory mediators (prostaglandins, cytokines) to reduce anorectal edema, pruritus, and mucosal inflammation associated with hemorrhoids and anal fissures.
Lidocaine 3%Amide local anesthetic that blocks sodium channels in anorectal sensory nerve fibers, producing rapid-onset local analgesia and reducing pain during and after bowel movements.
Nifedipine 0.2%Dihydropyridine calcium channel blocker that, when applied topically to the anus, relaxes internal anal sphincter smooth muscle, reduces resting anal canal pressure, and increases local blood flow to promote fissure healing.

Route: Anorectal (rectal and perianal) application.

  • Suppository (Rectal Rocket): The unique torpedo shape allows the suppository to span both internal (rectal) and external (perianal) anorectal structures simultaneously. Moisten the tip with water and gently insert the narrow end into the rectum so that the broader end remains partially external, allowing the medication to deliver to both internal and external hemorrhoidal tissue.
  • Ointment: Apply a small amount (pea-sized) to the perianal area and gently insert applicator tip (if provided) just inside the anal canal 2–3 times daily, or as directed by the prescriber—particularly 20–30 minutes before a bowel movement.
  • Wash hands thoroughly before and after application.
  • Avoid using for more than 2 weeks with hydrocortisone (corticosteroid-related tissue thinning/atrophy).

All dosing is prescriber-directed. Typical regimens in clinical practice for anal fissure:

  • Apply 2–3 times daily and/or before anticipated bowel movements for 4–6 weeks.
  • Nifedipine-lidocaine combinations demonstrated fissure healing in 94.5% of patients at 6 weeks in randomized clinical trials.
  • Hydrocortisone use should be limited to 2 weeks to avoid skin atrophy; reassess continued need at follow-up.
  • Do not use more frequently than prescribed; excessive topical nifedipine may cause systemic vasodilation effects (headache, hypotension).
  • Hydrocortisone: Binds glucocorticoid receptors in anorectal mucosa and perianal skin, suppressing phospholipase A2 and downstream prostaglandin/leukotriene synthesis; reduces histamine release from mast cells; inhibits inflammatory cytokine transcription (IL-1β, TNF-α), resulting in decreased mucosal edema, erythema, and pruritus.
  • Lidocaine: Blocks voltage-gated sodium channels (Nav1.7, Nav1.8) in perianal sensory neurons (C-fibers and Aδ-fibers), preventing action potential propagation and providing fast-onset analgesia within minutes. Duration of action is approximately 30–60 minutes per application.
  • Nifedipine: Antagonizes L-type voltage-dependent calcium channels in internal anal sphincter smooth muscle, reducing calcium-dependent myosin phosphorylation, causing muscle relaxation, lowering resting anal canal pressure, and improving ischemic blood flow to the fissure bed—the primary mechanism impeding chronic anal fissure healing.

Indication context: This combination is prescribed for acute and chronic anal fissures, symptomatic internal and external hemorrhoids, chronic proctalgia associated with internal sphincter hypertonia, and post-anorectal surgical pain management. The nifedipine-lidocaine combination has Level I evidence for chronic anal fissure with a 94.5% healing rate at 6 weeks vs. 16.4% for lidocaine-hydrocortisone control in a pivotal randomized trial. Hydrocortisone augments anti-inflammatory benefit for hemorrhoidal disease.

Monitoring considerations:

  • Limit hydrocortisone use to 2 weeks to prevent anoderm atrophy; reassess indication for continued use.
  • Monitor blood pressure if systemic absorption of nifedipine is a concern (more relevant with higher concentrations or inflamed mucosa).
  • Re-examine fissure healing at 4–6 weeks; persistent fissures may require surgical sphincterotomy or botulinum toxin injection.
  • Rule out secondary causes of anal pain (abscess, Crohn's disease, malignancy) before initiating treatment.

Contraindications:

  • Known hypersensitivity to hydrocortisone, lidocaine (or other amide anesthetics), nifedipine, or any formulation excipient.
  • Active anorectal infection (viral, bacterial, fungal) in the absence of concurrent antimicrobial treatment.
  • Pregnancy: use only if clearly needed and risk-benefit has been assessed by the prescriber (topical nifedipine systemic absorption is low but not zero).

Warnings & Precautions:

  • Prolonged hydrocortisone use (beyond 2 weeks): risk of anoderm atrophy, skin thinning, and increased susceptibility to trauma.
  • Topical nifedipine may cause systemic vasodilation at higher doses or with inflamed mucosa: monitor for headache, dizziness, facial flushing, or palpitations; advise patients with cardiovascular disease or on antihypertensives.
  • Topical lidocaine: systemic toxicity is rare at anorectal doses but can occur if applied to large raw mucosal surfaces; monitor for CNS signs (ringing in ears, metallic taste, perioral numbness).
  • Avoid contact with eyes; wash hands after application.

Drug Interactions:

  • Nifedipine may potentiate hypotensive effects of systemic antihypertensives if significant systemic absorption occurs.
  • CYP3A4 inhibitors (grapefruit juice, azole antifungals): may increase systemic nifedipine exposure from topical application with inflamed mucosa.

Common Side Effects: Local erythema or burning at application (transient); headache or mild hypotension (nifedipine, typically transient); skin thinning with prolonged hydrocortisone use.

Store at room temperature (15–25°C). Suppositories should not be exposed to temperatures above 25°C as they may soften—store in the refrigerator (2–8°C) if ambient temperatures exceed this. Protect from light. Keep in the original packaging. Use within the beyond-use date assigned by Genesis Compounding per USP <795> standards. Keep out of reach of children.

What conditions is Rectal Rocket used for?

This combination is prescribed for anal fissures (tears in the anal lining), hemorrhoids (internal and external), and chronic anorectal pain associated with tight sphincter tone (proctalgia). Each ingredient targets a distinct cause of anorectal pain and impaired healing.

How does the shape of the suppository work?

The torpedo (rocket) shape is designed so the narrow end is inserted into the rectum while the wider base remains outside. This allows medication to be released into both the internal canal (for internal hemorrhoids and fissures) and the perianal skin (for external hemorrhoids), providing more comprehensive coverage than a conventional round suppository.

How long should I use this medication?

Use as directed by your prescriber—typically 4–6 weeks for anal fissure healing. The hydrocortisone component should not be used for more than 2 weeks continuously without reassessment, as prolonged corticosteroid use on skin and mucosa can cause tissue thinning. Nifedipine and lidocaine can be used for the full treatment course.

Will nifedipine lower my blood pressure?

At the low topical concentrations in this preparation (0.2%), systemic absorption is generally minimal. Clinical studies have not shown significant blood pressure changes. However, patients with cardiovascular disease, very inflamed mucosa, or concurrent antihypertensive therapy should discuss this with their prescriber, as some systemic absorption is possible.

Is this FDA-approved?

No single FDA-approved product contains this three-ingredient combination. Nifedipine-lidocaine is marketed in some EU countries for anal fissure, and hydrocortisone-lidocaine combination products exist OTC/Rx in the US. This three-ingredient preparation is a patient-specific 503A compounded product from Genesis Compounding.

Clinical References

Authoritative sources reviewed in preparing this clinical summary. Provided for prescriber reference; not a substitute for the prescriber’s clinical judgment.

Topical Nifedipine with Lidocaine Ointment vs. Active Control for Chronic Anal Fissure
PMC / Canadian Journal of Surgery
Source →
Nifedipine–Lidocaine for Treating Chronic Anal Fissure (NIHR Health Technology Briefing)
NIHR / io.nihr.ac.uk, 2024
Source →
Aggressive Treatment of Acute Anal Fissure with Nifedipine
PMC / World Journal of Gastroenterology, 2006
Source →