Description

(Compounded Rectal Suppository – Multi-Drug Analgesic and Neuromodulatory Formula)

Advanced Multimodal Pain Relief for Chronic Pelvic, Neuropathic, and Muscle-Spasm–Related Pain Syndromes

This custom-compounded 60-gram suppository formulation combines three synergistic active ingredients—Amitriptyline 2%, Baclofen 2%, and Gabapentin 2%—to provide powerful, localized relief for complex pain conditions including neuropathic pelvic pain, vulvodynia, chronic prostatitis, interstitial cystitis, and pudendal neuralgia. Designed for rectal administration, this formulation enables targeted drug delivery near affected pelvic and lumbosacral nerves while reducing systemic side effects.

By addressing multiple mechanisms of pain signaling—including nerve excitability, central sensitization, and pelvic muscle tension—this combination provides a comprehensive approach to otherwise difficult-to-manage conditions.

Key Features

• 3-in-1 multimodal pain therapy: tricyclic antidepressant, GABA agonist, and calcium channel modulator

• Localized delivery via rectal suppository for regional effect

• 60 grams total, dispensed in custom unit-dosed suppositories

• Bypasses first-pass metabolism for enhanced therapeutic effect

• Ideal for neuropathic pain syndromes and patients intolerant to oral regimens

• Compounded in compliance with USP <795> standards for patient-specific prescriptions

Active Ingredients and Mechanism of Action

Each gram contains:

• Amitriptyline 2% – A tricyclic antidepressant that modulates norepinephrine and serotonin pathways in the spinal cord and peripheral nerves, reducing pain hypersensitivity.

• Baclofen 2% – A muscle relaxant and GABA-B receptor agonist that inhibits excitatory neurotransmission and reduces neurogenic muscle spasm.

• Gabapentin 2% – A voltage-gated calcium channel modulator that reduces the release of glutamate and substance P, key drivers of chronic nerve pain.

By combining these agents into one suppository, the formulation targets peripheral, spinal, and central mechanisms of pain simultaneously.

Indications

This compounded suppository formulation is often prescribed for:

• Chronic Pelvic Pain Syndrome (CPPS)

• Pudendal Neuralgia

• Vulvodynia / Vestibulodynia

• Interstitial Cystitis / Bladder Pain Syndrome (IC/BPS)

• Prostatodynia or Chronic Prostatitis

• Levator Ani Syndrome / Pelvic Floor Dysfunction

• Post-surgical pelvic or lower spine nerve pain

• Radiation-induced pelvic neuropathy

It is particularly useful in patients who are unable to tolerate oral medications due to GI distress, sedation, or drug interaction concerns.

Dosage and Administration

• Route: Rectal

• Dosage: As directed by the prescribing provider (commonly once or twice daily)

• Suppository base: Typically polyethylene glycol or cocoa butter, based on formulation preference

• Total volume: 60 grams (divided into custom-sized, unit-dose suppositories as prescribed)

• Insert rectally using clean hands or gloves, preferably while lying down

• Patients should remain reclined for 15–30 minutes post-insertion for optimal absorption

• Do not use orally or vaginally

Suppositories are dispensed in labeled, patient-specific packaging with dosing instructions.

Advantages of Rectal Delivery

• Localized drug effect for the pelvic region and lower spine

• Avoids gastrointestinal irritation or nausea common with oral baclofen or amitriptyline

• Reduced sedation and systemic drug load

• Improved adherence for patients unable to take oral capsules

• Direct absorption into pelvic venous plexus allows faster onset of relief

Safety and Precautions

Possible side effects (typically mild and dose-related):

• Mild rectal irritation or discomfort

• Sedation, dizziness, or dry mouth

• Rarely: constipation, urinary retention, or mood changes

Contraindications:

• Hypersensitivity to any of the active ingredients

• Severe hepatic or renal impairment (requires caution and monitoring)

• Use in pediatric patients or during pregnancy, unless specifically directed by a physician

Drug interactions may occur with CNS depressants or anticholinergic agents; a thorough medication review is advised prior to prescribing.

Storage and Handling

• Store at 2°C to 8°C (36°F to 46°F) in a refrigerator unless otherwise directed

• Keep away from heat and moisture

• Do not freeze

• Keep out of reach of children

• Handle with clean hands or gloves to maintain hygiene

Custom Compounding and Personalization

This formulation is prepared by a licensed compounding pharmacy and is available by prescription only. The total 60g compound is typically divided into 15–30 unit doses, depending on prescribed strength and patient requirements. All ingredients meet USP monograph specifications, and the compounding process is validated for potency, uniformity, and safety.

Comprehensive Relief for Complex Pain Syndromes

For patients suffering from chronic pelvic pain, neuropathic irritation, or muscle-related discomfort, the Amitriptyline/Baclofen/Gabapentin 2%/2%/2% compounded suppository provides a uniquely effective, regionally targeted solution. With multimodal action and local delivery, it addresses both the physical and neurological aspects of pain—making it a valuable tool in the long-term management of refractory pelvic and neuralgic pain conditions.