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Menthol is a cooling counterirritant and topical analgesic that compounding pharmacies include in creams, gels, sprays and mouth rinses by prescription.
Menthol is a cyclic monoterpene alcohol found in peppermint and other mint plants. It produces a cooling sensation by activating TRPM8, the cold-sensing receptor on sensory nerves, and at higher concentrations it desensitizes that receptor and blocks sodium channels in a way that resembles a local anesthetic. It is sold without a prescription as the active ingredient in many over-the-counter external analgesic creams, gels and patches, which carry Drug Facts labeling for temporary relief of minor muscle and joint aches and pains, and it appears in cough drops, mouth rinses and anti-itch lotions. A prescriber might order compounded menthol combined with other topical pain agents in one preparation, at a concentration or in a vehicle not sold over the counter, or in a mouth rinse or scalp preparation. Compounded preparations are not FDA-approved and require a prescription.
Over-the-counter menthol products have no boxed warning. Their Drug Facts labels say: for external use only; avoid the eyes; do not apply to wounds or damaged skin; do not bandage tightly; do not use with heating pads; and stop and ask a doctor if the condition worsens, symptoms last more than 7 days, or they clear and return. A mild cold or burning sensation is common and fades; redness is more likely at high concentrations, and some people develop paradoxical cold sensitivity. Keep it away from children; swallowing pure menthol can cause vomiting and seizures. No drug interactions are listed in the sources. Ask your prescriber before use if you are pregnant or breastfeeding; LactMed notes menthol passes into breast milk in small amounts and that peppermint gels on the nipples should be wiped off before feeding. If a side effect bothers you, talk to your prescriber or pharmacist.
Menthol activates TRPM8 on dorsal root and trigeminal ganglion neurons at low to moderate concentrations, producing cooling and analgesia that a 2022 review in Frontiers in Molecular Neuroscience attributes almost entirely to TRPM8, with central kappa-opioid and group II/III metabotropic glutamate signaling mediating the effect downstream. It also blocks Nav1.8, Nav1.9 and TTX-sensitive sodium channels independent of TRPM8, modulates TRPA1 and TRPV1, and cross-desensitizes irritation from capsaicin and other agents, the basis of its counterirritant use. High concentrations sensitize TRPM8 and can cause cold allodynia. No pharmacokinetic data for topical menthol are given in the sources. There is no FDA-approved prescription menthol product; OTC external analgesics are marketed under Drug Facts labeling for temporary relief of minor muscle and joint pain. Prescribers have ordered compounded menthol in combination topical preparations for musculoskeletal pain, chemotherapy-induced peripheral neuropathy, postherpetic neuralgia and pruritus, uses the Frontiers review describes as supported by small or pilot studies with mixed results in osteoarthritis and ankle sprain. Concentration and vehicle are per prescriber. Monitoring is clinical: irritation, contact dermatitis and cold hypersensitivity at the application site; inhaled menthol may aggravate asthma. Menthol is not a controlled substance.
Compounded at Bayview
Patient guides for the preparations we make most often. Each one is compounded to order and requires a prescription.
For prescribers
Every preparation in our formulary that contains this ingredient. Strength, base and dose form are set by the prescription.
Other salt forms of this molecule, and ingredients commonly compounded alongside it.
This page describes an active pharmaceutical ingredient, not a finished drug product. Bayview Pharmacy compounds preparations containing it only on a prescriber's order for an individual patient.
Compounded preparations are not FDA-approved, and the FDA has not evaluated them for safety, effectiveness, or manufacturing quality. Nothing on this page is a claim that any preparation is effective for any condition.
A valid prescription is required. Availability depends on Bayview's licensure in your state. This page is general information, not medical advice. Discuss your situation with a licensed healthcare provider.
Our pharmacists work with prescribers to build preparations around a patient's dose, form and tolerances. Ask us what is possible with this ingredient.
