Cyclobenzaprine 2% | Diclofenac 3% | Gabapentin 6% | Lidocaine 5%

Route: Topical application to the painful area.

• Apply a small amount (typically a pea- to dime-sized quantity) to the skin directly over the painful joint, muscle group, or nerve territory.
• Gently massage or rub in until absorbed; wash hands after application unless the hands are the treated area.
• Do not apply to open wounds, abraded skin, mucous membranes, or the eyes.
• Do not occlude with airtight dressings (increases lidocaine and diclofenac systemic absorption).
• Apply 3–4 times daily or per prescriber instruction.

Dosing is prescriber-determined and individualized for the patient's pain condition. General considerations:

• Typically applied 2–4 times daily to the affected area.
• Use the minimum effective amount to minimize systemic absorption, particularly of lidocaine.
• Duration of use should be guided by clinical response and prescriber reassessment.
• These agents are used to treat localized chronic pain conditions including musculoskeletal pain, neuropathic pain, and post-surgical pain syndromes.

• Cyclobenzaprine: Centrally, cyclobenzaprine acts on brainstem noradrenergic pathways (similar to TCAs) to reduce muscle hyperactivity. Peripherally in topical application, some evidence suggests direct effects on muscle spindle afferents and local nerve terminals that may reduce spasm and hypertonicity at the application site.
• Diclofenac: Reversible, non-selective COX-1/COX-2 inhibitor; reduces conversion of arachidonic acid to prostaglandins (PGE2, PGI2) and thromboxane A2. Topically, diclofenac achieves tissue concentrations in joint synovium, cartilage, tendon, and muscle sufficient for anti-inflammatory effect with substantially lower plasma levels than equivalent oral doses.
• Gabapentin: Binds the α2δ-1 subunit of voltage-dependent calcium channels in presynaptic dorsal root ganglion neurons and peripheral nociceptors; reduces calcium influx and attenuates release of excitatory neurotransmitters (glutamate, norepinephrine, substance P). May also modulate central sensitization via peripheral afferent downregulation. Topical delivery targets peripheral sensitization with reduced CNS side effects.
• Lidocaine: Binds the intracellular face of voltage-gated sodium channels in Na(v)1.7/Na(v)1.8-expressing peripheral nociceptors, stabilizing the inactivated channel state and blocking action potential generation and conduction. Provides reversible analgesia confined to the area of application with minimal systemic absorption at topical concentrations.

This multi-mechanism topical formulation is used for localized chronic pain conditions where multiple pain pathways contribute simultaneously—including musculoskeletal pain (osteoarthritis, myofascial pain, post-surgical pain), neuropathic pain (diabetic peripheral neuropathy, post-herpetic neuralgia, complex regional pain syndrome), and mixed pain syndromes. The topical route reduces GI, renal, cardiac, and CNS systemic effects that accompany oral analgesic use.

Prescriber monitoring:

• Assess effectiveness at 4–6 weeks; modify components if inadequate response.
• Screen for contact sensitization with prolonged use.
• Lidocaine: systemic toxicity is rare at topical concentrations but possible with extensive application or broken skin; CNS (tinnitus, circumoral paresthesia) and CV symptoms warrant discontinuation.
• Diclofenac: topical NSAID with low systemic exposure, but caution in patients with severe renal impairment or NSAID hypersensitivity.
• Monitor for methemoglobinemia risk with lidocaine in patients on other oxidizing agents.

Contraindications:

• Hypersensitivity to any of the four ingredients or related compounds (amide local anesthetics, NSAIDs, tricyclics, gabapentinoids)
• Application to open wounds, mucous membranes, or eyes
• Diclofenac: NSAID hypersensitivity (aspirin-exacerbated respiratory disease)
• Lidocaine: known severe hypersensitivity to amide anesthetics

Warnings & Precautions:

• Lidocaine systemic toxicity with excessive application or application to abraded skin: CNS (tinnitus, seizures) and cardiovascular (arrhythmia) toxicity can occur.
• Diclofenac: avoid use in patients with severe renal or hepatic impairment; topical NSAID use near perioperative period of CABG surgery is contraindicated for systemic NSAIDs (topical risk is much lower but monitor accordingly).
• Cyclobenzaprine: systemic sedation is unlikely at topical concentrations but not fully characterized.
• Gabapentin: limited topical systemic absorption data; sedation/dizziness unlikely but uncharacterized.

Drug Interactions:

• Topical lidocaine: additive effect with other sodium channel blockers if applied to large areas; methemoglobinemia risk with sulfonamides, nitrates, dapsone.
• Topical diclofenac: systemic NSAID effects minimal, but avoid duplication with oral NSAIDs.
• Cyclobenzaprine: systemic MAO inhibitors are a contraindication for oral cyclobenzaprine; topical absorption is very low but note history.

Common Side Effects: Application site erythema, pruritus, burning, and dryness (most common); contact dermatitis; rare—lidocaine systemic toxicity with large-area application; diclofenac photosensitivity.

Store at controlled room temperature (20–25°C / 68–77°F). Protect from heat and direct light. Do not freeze. Keep tightly sealed. Use before the beyond-use date assigned by Genesis Compounding. Keep out of reach of children and pets.

Why use four ingredients in one cream instead of separate medications?

Chronic pain—especially neuropathic or musculoskeletal pain—often involves multiple simultaneous pathways: inflammation, nerve sensitization, muscle spasm, and sodium-channel-mediated nociception. This multi-target approach addresses all four pathways simultaneously with a single application and allows lower individual concentrations of each agent than would be needed if used alone. The topical route also minimizes systemic side effects compared to oral versions of these same medications.

Is this as effective as oral pain medications?

For localized pain, topical analgesic combinations can achieve therapeutically meaningful local tissue concentrations with substantially lower systemic drug levels, reducing systemic side effects. The analgesic effect is concentrated at the application site rather than distributed throughout the body. Evidence for topical compounded multi-drug preparations is emerging; your prescriber has determined this approach is appropriate for your condition.

Can I apply this to any area that hurts?

Apply only to intact, non-abraded skin at the specific painful area directed by your prescriber. Do not apply near the eyes, on mucous membranes, or over large body surface areas. Do not apply under airtight wrapping or bandages unless specifically instructed.

Is this product FDA-approved?

No. Individual components (diclofenac topical, lidocaine topical) have FDA-approved forms, but this specific multi-ingredient compounded combination is a 503A prescription preparation from Genesis Compounding for a named patient. Compounded topical pain creams have been studied in randomized clinical trials (Ann Intern Med. 2019;170:309-318) but are not FDA-approved products.

What side effects should prompt me to contact my prescriber?

Contact your prescriber promptly for: ringing in the ears, numbness around the mouth, or a metallic taste (signs of lidocaine systemic absorption); persistent severe skin rash or allergic reaction; severe diarrhea or GI bleeding (NSAID-related, rare with topical); unusual muscle weakness or severe dizziness.