Drug intelligence / Profile preview

phenyltoloxamine

Development stage
Unknown
Modality
Small Molecules
Administration
Oral, Ophthalmic
01

Overview

Phenyltoloxamine is a first-generation antihistamine of the ethanolamine class with sedative and mild analgesic effects. It acts as an H1 receptor antagonist and is primarily used to treat symptoms of the common cold (such as sneezing, cough, runny nose, watery eyes), allergies (allergic rhinitis and conjunctivitis), and as a short-acting sedative. Due to its central nervous system penetration and tranquilizing properties, it is also used in combination with other agents like acetaminophen or codeine for enhanced analgesia or antitussive effect. Phenyltoloxamine stabilizes mast cells by lowering intracellular calcium levels and reduces inflammatory responses by inhibiting NF-kB signaling pathways[1][2][5][6]. It is most commonly found in over-the-counter combination products for relief of minor aches/pains associated with colds or allergies.

Brand names
DologesicRelagesicPercogesicMajor-gesicPhenylgesic
Other names
phenyltoloxamine hydrochloridephenyltoloxamine citrate
02

Targets

SIGMAR1 (Sigma non-opioid intracellular receptor 1)HRH1 (Histamine H1 Receptor)

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