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Dihydroergotamine mesylate

Cat. No. M13868
Dihydroergotamine mesylate Structure
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Biological Activity

Dihydroergotamine mesylate is an ergot alkaloid used to treat migraines. Target: 5-HT Receptors Dihydroergotamine is not as effective as sumatriptan or phenothiazines as a single agent for treatment of acute migraine headache; however, when administered with an antiemetic, dihydroergotamine appears to be as effective as opiates, ketorolac, or valproate. Given its nonnarcotic properties, parenteral dihydroergotamine combined with an antiemetic should be considered as effective initial therapy in clinical practice. The introduction of the intranasal formulation of DHE provides both pharmacologic and patient-convenience advantages for use in migraine therapy [2, 3].

Chemical Information
Molecular Weight 679.78
CAS Number 6190-39-2
Solubility (25°C) DMSO 50 mg/mL
Storage 2-8°C, protect from light, dry, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Rasha Srouji, et al. Headache. Dihydroergotamine infusion for pediatric refractory headache: A retrospective chart review

[2] Stephen Silberstein. Expert Opin Pharmacother. MAP0004: dihydroergotamine mesylate inhalation aerosol for acute treatment of migraine

[3] John A Morren, et al. Expert Opin Pharmacother. Where is dihydroergotamine mesylate in the changing landscape of migraine therapy?

[4] R B Lipton. Headache. Ergotamine tartrate and dihydroergotamine mesylate: safety profiles

[5] J A Barone, et al. Pharmacotherapy. Combination dihydroergotamine mesylate and heparin sodium with lidocaine HCl. Pharmacokinetics, mechanism of action, clinical efficacy, and adverse effects

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