Chemical formula: C₁₇H₂₃N₃O Molecular mass: 285.384 g/mol PubChem compound: 4992
Mepyramine is a first generation antihistamine, targeting the H1 receptor. However, it rapidly permeates the brain and so often causes drowsiness as a side effect. Mepyramine is a histamine H1 receptor inverse agonist. It binds to a G protein-coupled form of the receptor and promotes a G protein-coupled inactive state of the H1 receptor that interferes with the Gq/11-mediated signaling. Mepyramine competes with histamine for binding at H1-receptor sites on the effector cell surface, resulting in suppression of histaminic edema, flare, and pruritus. The sedative properties of mepyramine occur at the subcortical level of the CNS. It has mild hypnotic properties and some local anesthetic action and is used for allergies (including skin eruptions) both parenterally and locally. It is a common ingredient of cold remedies.
This medicinal substance has been classified in the anatomical therapeutic chemical (ATC) classification according to its main therapeutic use as follows:
| ATC code | Group title | Classification |
|---|---|---|
| D04AA02 | Mepyramine | D Dermatologicals → D04 Antipruritics, incl. antihistamines, anesthetics, etc. → D04A Antipruritics, incl. antihistamines, anesthetics, etc. → D04AA Antihistamines for topical use |
| R06AC01 | Mepyramine | R Respiratory system → R06 Antihistamines for systemic use → R06A Antihistamines for systemic use → R06AC Substituted ethylene diamines |
Competent medicine agencies globally have authorized commercialization of this active ingredient according to these medication package inserts (MPIs):
| Title | Information Source | Document Type | |
|---|---|---|---|
| ANTHISAN BITE AND STING Cream | Medicines & Healthcare Products Regulatory Agency (GB) | MPI, EU: SmPC |
Mepyramine is an active ingredient of these brands:
Ecuador (EC)
Hong Kong (HK)
Israel (IL)
Malta (MT)Mexico (MX)
New Zealand (NZ)Poland (PL)
South Africa (ZA)
Spain (ES)
Turkey (TR)United Kingdom (UK)Note the following: The list of brand names is continuously updated, and thus does not include the total of products circulating worldwide. |
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