API raw material cabergoline Powder

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cabergoline Usage and Synthesis.

First, when combined with levodopa to treat Parkinson's disease, it can enhance the efficacy, so it should be appropriately reduced.

Second, when combined with macrolides, it can increase blood drug concentration and may show signs of dopamine overdose.

Third, when combined with antihypertensive drugs, can strengthen the antihypertensive effect, the amount of antihypertensive drugs should be reduced.

Fourth, oral hormonal contraceptives can cause amenorrhea or galactorrhea, interfering effect, not suitable for use.

5. Haloperidol, methyldopa, monoamine oxidase inhibitors, metoclopramide, phenothiazines, seropine and thathacanthracene can increase the concentration of serum prolactin and interfere with the effect, and the dose should be adjusted appropriately when it must be combined.

6. When combined with other ergot derivatives, it can occasionally aggravate hypertension, but it is rare.

When combined with alcohol, it may reduce the tolerance of the drug, so alcohol is prohibited during the medication.

The combination of butoxybenzoic antipsychotics or H2-receptor blockers can increase the concentration of prolactin and decrease the efficacy.

Uses of cabergoline.

Carergoline is an ergot alkaloid derivative that acts as a dopamine receptor agonist similar to bromocriptine. It is characterized by strong, long-acting and selective, and has a high affinity for the D2 dopamine receptor. And has a strong and lasting inhibition of mammary gland secretion. The product is easy to absorb, the peak time of blood concentration is 1 ~ 3 hours, the plasma protein binding rate is 40%, and the half-life is 63 ~ 100 hours. It is widely metabolized by hydrolysis and is excreted mainly through bile and feces. It is mainly used for Parkinson's disease, Parkinson's syndrome and hyperprolactinemia. This product can reduce the severity of the "switching phenomenon" caused by long-term use of levodopa, the time of being "on" is significantly increased, and the need for levodopa is reduced by 18%.

Product method of cabergoline.

The reaction of 6-(2-propenyl) ergolin-8β-carboxylic acid (I) and carbonized diimide in tetrahydrofuran gives carbergoline.

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