Cabergoline: A Superior Prolactin Inhibitor

LakeMountD

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Prolactinoma- A prolactinoma is a benign tumor (adenoma) of the pituitary gland that produces a hormone called prolactin.

Most studies are conducted on people with these tumors since their bodies produce excess Prolactin sometimes 40+ times higher than a normal person makign them the perfect test subjects.



Treatment of prolactin-secreting macroadenomas with the once-weekly dopamine agonist cabergoline
BM Biller, ME Molitch, ML Vance, KB Cannistraro, KR Davis, JA Simons, JR Schoenfelder and A Klibanski
Neuroendocrine Unit, Massachusetts General Hospital, Boston 02114, USA.
-------->Dopamine agonist administration is the primary therapy for macroprolactinomas, but bromocriptine is the only agent approved in the United States. Its use is limited by a high incidence of side effects, a short duration of action, and a lack of effectiveness in some patients. Cabergoline is a long-acting dopamine agonist specific for the D2 receptor that is more effective and better tolerated than bromocriptine in women with microadenomas or idiopathic hyperprolactinemia. However, experience with cabergoline in the treatment of patients with macroadenomas is limited. We report the first study of chronic administration of cabergoline conducted exclusively in patients with macroprolactinomas. Fifteen patients (8 women, 7 men) ages 18-76 yr were studied in an open-label 48-week dose escalation trial of cabergoline administered once per week. Eleven patients had received prior therapy with other dopamine agonists. Mean prolactin (PRL) levels decreased by 93.6%, and normal levels were attained in 73% of patients at doses of 0.5-3.0 mg per week. Three of five patients who had failed to normalize PRL on prior dopamine agonists achieved normal levels. Gonadal function was restored in all hypogonadal men and in 75% of premenopausal women with amenorrhea. Tumor size decreased in 11 of the 15 patients. Side effects were minimal. Of the 5 patients who had experienced side effects in prior dopamine agonists, 4 had none on cabergoline, and the fifth had milder symptoms. During two further years of follow up, the improvement in PRL levels, gonadal function, and tumor size has persisted during cabergoline administration, and three patients have experienced a further decline in PRL and/or tumor size. This study demonstrates the effectiveness and minimal side effects of once-weekly cabergoline for treatment of macroprolactinomas.





Successful Treatment of a Large Macroprolactinoma with Cabergoline During Pregnancy

Chienying Liu1 and J. Blake Tyrrell1
(1) Division of Endocrinology and Metabolism, Department of Medicine, University of California, San Francisco, San Francisco, California
-------->We report a pregnant woman with a large macroprolactinoma successfully treated with cabergoline after a suboptimal response to bromocriptine. A 7 week pregnant woman with a history of a prolactinoma presented to the endocrine clinic with the complaints of headaches and nausea. She had a prolactin level of 65 µg/L 1/2 weeks following her last menstrual period. Bromocriptine was discontinued at 6 weeks gestation when pregnancy was confirmed. A PRL concentration was 1899 µg/L (non-pregnant normal range 1.39–24.20 µg/L, the mean peak levels during pregnancy reported from the literature are 200–210 µg/L) at 7 weeks gestation, and a repeat was 2197 µg/L. An MRI showed a 3 × 2.2 × 2.5 cm seller mass abutting the optic chiasm and displacing the optic nerves superiorly; the visual field testing was normal. Bromocriptine was reinitiated and the patient responded initially with decreasing headaches and declining PRL concentrations to 1488 µg/L at 15 weeks gestation. However, PRL increased to 1836 µg/L at 16 weeks and remained elevated despite bromocriptine 2.5 mg three times a day; in addition, she complained of severe nausea, vomiting, and persistent headaches. Cabergoline was added at 18 weeks gestation. PRL decreased dramatically from 1710 to 859 µg/L in 1 week, and to 488 µg/L within 4 weeks. A repeat MRI showed more than 30% reduction in tumor size. Bromocriptine was discontinued at 24 weeks gestation; she was maintained on cabergoline 0.5 mg twice a week without complaints. PRL levels ranged from 190 to 278 µg/L during the last 10 weeks of pregnancy. She had a C-section electively at 37 weeks gestation and delivered a healthy baby. Management options in this patient and during pregnancy are discussed.
 
Syr

Syr

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Yes, cabergoline is much better than bromo :)
 

SHADOW2492

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I am having a prolactin problem now and have cabergoline on the way, I ahve searched quite a bit on the boards and havent found how long I should be running it for. does anyone have any idea? thanks in advance/ Also if anyone wants I will post here my results if any.
 

NevrEnuf

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i'm also interested in cabergoline and have similar questions on how long to use it, the dose, and can it be used in combo with nolva or is that unnecessary?
 
CNorris

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I take .5mg twice a week. Im not sure of the duration, but I would like to know cause I've been on it for 2 weeks now.
 

NevrEnuf

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I take .5mg twice a week. Im not sure of the duration, but I would like to know cause I've been on it for 2 weeks now.

Hows it working for you? are you on cycle right now, if so whats ur cycle look like?

also does anyone know if this is a more effective treatment than say letrosole or dosenex or other AI's?
 
LakeMountD

LakeMountD

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Hows it working for you? are you on cycle right now, if so whats ur cycle look like?

also does anyone know if this is a more effective treatment than say letrosole or dosenex or other AI's?
Two different beasts here. You don't even need the letro unless you are running some test along with it. If you aren't taking any aromatising compounds then you can just go with the cabergoline.
 

NevrEnuf

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Two different beasts here. You don't even need the letro unless you are running some test along with it. If you aren't taking any aromatising compounds then you can just go with the cabergoline.
I'm finishing week 2 of my second cycle shown below, my first cycle was bunk gear unfortunately but what can you do...


1-14 test E 600mg/wk
1-13 deca 400mg/wk
4-7 igf 40mcg/day post wo
14-17 igf 40mcg/day post wo
PCT 16-19 nolva, tribex, cee, blah blah

I started getting sensative in the nips area so i've been takin tamaxofin citrite @40mg for the last 4 days or so, so i'm assuming this time around its real (even tho i've never heard of the brand name before)
 

olb

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Ok, so in plain english...This could help with gyno?

If yes, I am very interested. Will try anything.
 

CHAPS

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Using igf-1 on your second cycle, a little premature don't ya think?
 

shct

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Quoted from mesomorphsis site:

From the reading I’ve done, you only need about half a milligram (1/2mg) a week to experience all of the anti-prolactin, prosexual, antidepressant, and cognitive effects of Dostinex, but that’s on the very low end of the effectiveness scale. This stuff has an extremely long active life in the body, so once a week dosing is fine…but if it were me, and I were taking this stuff, I’d probably be using about .25mgs-.5mgs twice a week.

It should be taken before bed-time, because it may actually help you sleep a bit better, (9), Can be taken with or without food and not alter the pharmacokinetics (how it functions in your body) (10), and (incidentally) according to the literature is a much more efficient drug than Bromocriptine (11).

shct
 

djsdjs

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cabergoline has been shown to cause potentially fatal heart valve disease
http:/ /neurology.jwatch.org/cgi/content/full/2007/130/2

I would recommend low and sporadic dosing rather than trying to maintain 24/7 libido.
 
JackSteel

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Hows it working for you? are you on cycle right now, if so whats ur cycle look like?

also does anyone know if this is a more effective treatment than say letrosole or dosenex or other AI's?
caber isn't an AI
 

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