Drug intelligence / Profile preview

dihydroergotamine + paracetamol + caffeine

Development stage
Unknown
Modality
Small Molecules
Administration
Oral
01

Overview

This is a fixed-dose combination of three active pharmaceutical ingredients: **dihydroergotamine**, **paracetamol** (also known as acetaminophen), and **caffeine**. - **Dihydroergotamine** is an ergot alkaloid used as an acute treatment for migraine attacks. It exerts its effect primarily via vasoconstriction of intracranial blood vessels and by acting as a partial agonist or antagonist at various serotonin (5-HT) and adrenergic receptors, inhibiting neurogenic inflammation associated with migraine. - **Paracetamol** is an analgesic and antipyretic agent that acts centrally by inhibiting prostaglandin synthesis, likely via inhibition of cyclooxygenase (COX) enzymes in the brain, thus reducing pain and fever. - **Caffeine** is a central nervous system stimulant and an adenosine receptor antagonist. In combination, it both enhances the analgesic effect of paracetamol and dihydroergotamine and contributes to vasoconstriction, amplifying the anti-migraine effect. This combination may be used for the **acute treatment of moderate to severe migraine attacks**, especially in patients with inadequate response to paracetamol or NSAIDs alone. Studies show the combination’s efficacy is higher than either component alone for migraine relief[5].

02

Targets

ADOR (Adenosine receptors)COXHTR1B (5-Hydroxytryptamine Receptor 1B)ADRA2A (α2A)HTR1D (5-hydroxytryptamine receptor 1D)

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