Introduction
Pergolide mesylate salt , also known as 8-beta-((methylthio)methyl)-D-6-propylergoline methanesulfonate, is a dopamine receptor (D receptor) agonist acting like bromocriptine, which is responsible for the treatment of hyperprolactinemia and Parkinson's disease. The drug has the characteristics of quick onset, strong action, long duration of action, and small dosage.
Pharmacologic action
Pergolide mesylate salt is a D receptor agonist. It has the neuropharmacological effects of typical D 2receptor agonist and the effect of lowering serum prolactin level. After subcutaneous injection of peperilate mesylate salt, the ability of the mice to move autonomously can be quickly increased, allowing the mice to climb for a long time. This effect could be blocked by the D receptor antagonist, fluoroacetidine. After intraperitoneal injection or oral administration, the rats have obvious stereotyped movement. It can prolong the metabolic transformation in rat brain and reduce the content of 3,4-dihydroxyphenylacetic acid. Intravenous injection has obvious inhibitory effect on spontaneous discharge activity of the A neurons projecting into the striatum of rat mesencephalic dense area, and the discharge effect can be reversed by the receptor blocker hysteropiperidine. Subcutaneous injection can significantly reduce serum prolactin content. Intraperitoneal injection of reserpine can significantly inhibit the level of serum prolactin in rats, and the release of prolactin from anterior pituitary.
Function
This product is a synthetic ergoalkaloid drug, a new dopaminergic agonist. Compared with other dopaminergic agonists, the drug has a strong effect, small dose, quick effect and long maintenance time. The dopamine content in the striatum of Parkinson's disease is low. The D receptor agonist can stimulate the D receptor in the striatum and alleviate some dyskinesia, so it can be used in the treatment of Parkinson's disease. Dopamine is the most important inhibitor of prolactin secretion. So D receptor agonist is also an effective drug for the treatment of hyperprolactinemia.
Pharmacokinetics and metabolism
The drug is well absorbed after oral administration. The drug concentration in blood reached peak value after 1 ~ 1.5h, and the plasma protein binding rate was 91% in all tissues. The drug is mainly metabolized by sulfoxide, sulfone and phenolics in the body. After oral administration of pepeoride mesylate, 5% radioactivity was detected in the CO 2 exhaled after 24h, the fecal radioactivity was 45% after 96 hours, and the radioactivity of urine was 58% after 48 hours, and the total recovery rate was 106%.
References:
Jacobson, G. A., Pirie, A., Edwards, S., Hughes, K. J., Rendle, D. I., & Davies, N. W. (2014). Determination of pergolide in horse plasma by UPLC–MS/MS for pharmacokinetic applications. Journal of pharmaceutical and biomedical analysis, 94, 54-57.
Pohanka, M., Kaňovský, P., Bareš, M., Pulkrábek, J., & Rektor, I. (2005). The long-lasting improvement of sexual dysfunction in patients with advanced, fluctuating Parkinson's disease induced by pergolide: evidence from the results of an open, prospective, one-year trial. Parkinsonism & related disorders, 11 (8), 509-512.
