Dihydro α-Ergocryptine

Absorption

Alpha-dihydroergocryptine is rapidly absorbed but it presents a very low bioavailability as it is part of a first-pass hepatic metabolism and thus less of 5% of the administered dose reaches blood circulation. The peak plasma concentration is attained after 30-120 minutes. The absorption of alpha-dihydroergocryptine is not affected by the co-administration with food. When administered in repeated oral doses the Cmax after 1 hour was registered to be 2157 pg/ml. To know more about the ergoloid mesylate mixture please visit Ergoloid mesylate.

Toxicity

Alpha-dihydroergocryptine does not have effect in fertility and it does not present mutagenic potential. To know more about the ergoloid mesylate mixture please visit Ergoloid mesylate.

The Uses of Dihydro α-Ergocryptine

Dihydro α-Ergocryptine is a hydrogenated ergot alkaloids, specifically an equiproportional mixture of dihydroergocornine methanesulfonate, dihydroergocristine methanesulfonate, α and β-dihydroergocrytine methanesulfonate in the ratio of 1.5-2.5:1. Dihydro α-Ergocryptine is an α-adrenergic blocker used for the treatment of impaired mental function in the elderly.

The Uses of Dihydro α-Ergocryptine

Dihydro α-Ergocryptine is a hydrogenated ergot alkaloids, specifically an equiproportional mixture of dihydroergocornine methanesulfonate, dihydroergocristine methanesulfonate, α and β-dihydroergocrytine methanesulfonate in the ratio of 1.5-2.5:1. Dihydro α-Ergocryptine is an α-adrenergic blocker used for the treatment of impaired mental function in the elderly.

Background

Alpha-dihydroergocryptine is usually referred to the mixture of the alpha and beta dihydroergocryptine. These two compounds are differentiated in the position of a methyl group. This structural difference is due to a proteinogenic amino acid replacement from leucine to isoleucine. Both compounds are hydrogenated ergot derivatives. Alpha-dihydroergocryptine approved drug product is as a part of an ergoloid mixture. To know more about this mixture, please visit Ergoloid mesylate

Indications

Alpha-dihydroergocryptine has been studied for the early treatment of Parkinson disease as well as for its use in migraine prophylaxis, treatment of low blood pressure and peripheral vascular disorder. To know more about the ergoloid mesylate mixture and its uses please visit Ergoloid mesylate.

Definition

ChEBI: alpha-Ergocryptine in which a single bond replaces the double bond between positions 9 and 10.

Pharmacokinetics

The effect of alpha-dihydroergocryptine in dopamine receptors was tested in PD patients and seem to generate a significant clinical improvement in the tested patients as well as to reduce motor complications and side effects. In long-term clinical trials with Parkinson disease patients, the administration of alpha-dihydroergocryptine and levodopa, the symptoms were reposted to improve or completely vanish in 80% of the tested individuals. All the registered effects of alpha-dihydroergocryptine suggest a potential neuroprotective effect of this drug and some reports have indicated that this activity may be related to the activation of NF-kB. The effect of alpha-dihydroergocryptine in the dopamine D2 receptor also reduces prolactin plasma levels and induce hypotension. To know more about the ergoloid mesylate mixture please visit Ergoloid mesylate.

Metabolism

Alpha-dihydroergocryptine presents a linear metabolism with the formation of active metabolites and the metabolism kinetics of this compound has no interference with L-dopa. It is highly metabolized with a rate of 2.4 ng/min/mg protein in the microsomal system and a formation of eight different metabolites. the metabolism of alpha-dihydroergocryptine seems to be highly marked by the action of CYP 3A4. To know more about the ergoloid mesylate mixture please visit Ergoloid mesylate.