Extensive ultrastructural changes in rat mammotrophs following administration of the dopamine agonist ergocristine-reflecting inhibition of prolactin release
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저자는 유즙분비 억제를 목적으로 Bromocriptine을 투여한 15예와 Estrogen을 투여한 10예에서 임상적 효과와 혈청 prolactin치의 변화를 수유군과 비교 관찰하여 다음과 같은 결론을 얻었다. 1. 분만직후 2시간 이내의 혈청 prolactin치는 분만전의 혈청 prolactin치보다 상승하였다.(p<0.01). 2. 수유군에서 혈청 prolactin치는 분만후 제 3 주경에 비임신시의 혈청 prolactin 치로 감소되었다. 3. Estrogen 투여시 유즙분비 억제효과는 부분적이었고 약 40%에서 rebound lactation이 나타났다. 4. Bromocriptine 투여시 유즙분비 억제효과는 우수하였고 7∼13%에서 유즙분비와 유방팽창이 나타 났으나 그 정도는 매우 경미하였다. 5. Bromocriptine 투여시 혈청 prolactin치의 감소는 수유군보다 현저한 차이를 나타내었다. (P<0.01). 6. Bromocriptine과 Estrogen 투여시 약물에 의한 부작용은 관찰할 수 없었다.
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Journal Article THE DOPAMINE AGONIST BROMOCRIPTINE: Theoretical and Clinical Aspects Get access Acta Endocrinologica (Norway), Volume 89, Issue 1_Supplement, Aug 1978, Pages 3–230, https://doi.org/10.1530/acta.0.0880003 Published: 01 August 1978
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Ovarian hyperstimulation syndrome
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Bromocriptine treatment of lactating rats, or removal of the litter, led to a decrease in the number of insulin receptors in the mammary gland and an increase in the concentration of insulin in the serum. Bromocriptine also induced a decrease in the concentration of both prolactin and progesterone in the serum, whilst concurrent treatment with the former but not the latter prevented all the effects of bromocriptine for 48 h. Removal of the litter produced a similar decrease in the concentration in the serum of prolactin but not of progesterone. Treatment with prolactin prevented all of the effects of removal of the litter for 24 but not 48 h. This suggests that these effects of prolactin may require a mammary gland actually synthesizing milk since the gland rapidly fills with milk after removing the litter whereas milk removal continues to take place in bromocriptine-treated rats allowed to continue nursing their litters.
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The effect of bromocriptine withdrawal after long-term treatment on prolactin levels has been investigated in thirty-seven patients with prolactinomas. In ten patients with macroprolactinomas and post-operatively excessively high prolactin levels persisting suppression of prolactin secretion after bromocriptine withdrawal has been observed. This effect was not observed in patients with microprolactinomas or macroprolactinomas with only moderately elevated prolactin levels. The degree of persisting suppression correlated to the height of prolactin levels before treatment and to the duration of bromocriptine therapy. No correlation was found between the rise of prolactin levels after bromocriptine withdrawal and withdrawal time. It is suggested that the persisting suppression of prolactin levels is a sequence of reduction in tumour size. This anti-proliferative action of bromocriptine seems to be specific for the prolactin secreting cells in macroprolactinomas with high proliferation rate and high prolactin turn-over. These findings offer new possibilities in the management of patients with macroprolactinomas.
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Patients with prolactinoma are commonly treated with the D2 dopamine agonist bromocriptine, which in most cases, normalizes prolactin (PRL) levels. However, resistance to bromocriptine has been observed in 5 to 18% of tested prolactinomas and is associated to a decrease in both D2 receptor density and mRNA levels. In this study, we used quantitative RT‐PCR to investigate whether expression of G α proteins could be also modified in bromocriptine resistant prolactinomas. No difference in G α o mRNA levels or in the relative expression of G α s between bromocriptine sensitive and bromocriptine resistant prolactinomas was observed. In contrast, the relative expression of G α i 2 was found to be decreased in bromocriptine resistant prolactinomas when compared to that of bromocriptine sensitive prolactinomas. Interestingly, the relative G α i 2 expression was correlated to both bromocriptine inhibition of in vitro PRL secretion and D2 receptor mRNA levels. Bromocriptine resistance could thus result from a decrease in D2 dopamine receptors associated with a decrease in G α i 2 expression.
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パーキンソン病の最も基本的かつ有効な治療薬であるL-DOPAとドーバミンアゴニストbromocriptineの利点と欠点をまとめた.パーキンソン病の進行にフリーラジカルが重要な役割を果たしているとの最近の考えからすると,脳内でフリーラジカルの発生源となるL-DOPAの投与量をできるだけ少なくして,フリーラジカル消去作用を持つドーパミソアゴニストbromocriptineと併用するのが現時点では最も有効かつ好ましい薬物療法であると考えられる.
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