Drug intelligence / Profile preview

Cefalium

Development stage
Phase 3
Lead developer
Ache Pharmaceutical
Modality
Small Molecules
Administration
Oral
01

Overview

Cefalium is a fixed-dose combination medication developed by Aché Laboratórios Farmacêuticos for the acute treatment of moderate to severe migraine attacks. It utilizes a multi-modal pharmacological approach by combining four active ingredients: paracetamol (acetaminophen), dihydroergotamine mesylate, caffeine, and metoclopramide hydrochloride. Dihydroergotamine acts as a non-selective agonist at 5-HT1 receptors, particularly 5-HT1B and 5-HT1D, leading to the vasoconstriction of dilated intracranial blood vessels and the inhibition of pro-inflammatory neuropeptide release. Caffeine serves as an adjuvant that enhances the absorption of ergot alkaloids and provides additional cranial vasoconstriction via adenosine receptor antagonism. Paracetamol provides analgesic and antipyretic effects through the inhibition of prostaglandin synthesis in the central nervous system. Metoclopramide is included as a prokinetic and antiemetic agent, acting primarily as a dopamine D2 receptor antagonist to alleviate migraine-associated nausea and vomiting while improving the gastric absorption of the other components during an attack.

Brand names
Cefalium
Other names
paracetamol + caffeine + dihydroergotamine + metoclopramideparacetamol + cafeína + di-hidroergotamina + metoclopramida
02

Targets

ADORA1 (Adenosine receptor A1 subtype)HTR2A (Serotonin receptor 5-HT2A)PGHS-1 (Prostaglandin G/H Synthase 1)HTR3A (5-hydroxytryptamine receptor 3A)DRD2 (Dopamine D2 Receptor)HTR1B (5-Hydroxytryptamine Receptor 1B)ADORA2A (Adenosine A₂A Receptor)HTR1D (5-hydroxytryptamine receptor 1D)ADRA1A (α1A)HTR4 (5-Hydroxytryptamine receptor 4)

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