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Quantity: 100 tabs
Packaging: Capsulated and in Mylar Bags
Label: 7.5cm x 2.8cm
Cabergoline, an ergot derivative, is a potent dopamine receptor agonist on D2 receptors. Rat studies show cabergoline has a direct inhibitory effect on pituitary lactotroph (prolactin) cells. It is frequently used as a first-line agent in the management of prolactinomas due to its higher affinity for D2 receptor sites, less severe side effects, and more convenient dosing schedule than the older bromocriptine, though in pregnancy bromocriptine is often still chosen since there is less data on safety in pregnancy for cabergoline.
- Lactation suppression
- adjunctive therapy of prolactin-producing pituitary gland tumors (prolactinomas);
- monotherapy of Parkinson’s disease in the early phase;
- combination therapy, together with levodopa and a decarboxylase inhibitor such as carbidopa, in progressive-phase Parkinson’s disease;
- in some countries also: ablactation and dysfunctions associated with hyperprolactinemia (amenorrhea, oligomenorrhea, anovulation, nonpuerperal mastitis, and galactorrhea);
- treatment of uterine fibroids.
- adjunctive therapy of acromegaly, cabergoline has low efficacy in suppressing growth hormone levels and is highly efficient in suppressing hyperprolactinemia that is present in 20-30% of acromegaly cases; growth hormone and prolactin are similar structurally and have similar effects in many target tissues, therefore targeting prolactin may help symptoms when growth hormone secretion cannot be sufficiently controlled by other methods.
Pregnancy and Lactation
Relatively little is known about the effects of this medication during pregnancy and lactation. In some cases, the related bromocriptine may be an alternative when pregnancy is expected.
- Pregnancy: available preliminary data indicates a somewhat increased rate of congenital abnormalities in patients who became pregnant while treated with cabergoline.. However, one study concluded that “fetal exposure to cabergoline through early pregnancy does not induce any increase in the risk of miscarriage or fetal malformation.”
- Lactation: In rats, cabergoline was found in the maternal milk. Since it is not known if this effect also occurs in humans, breastfeeding is usually not recommended if/when treatment with cabergoline is necessary.
- Lactation suppression: In some countries, cabergoline (Dostinex) is sometimes used as a lactation suppressant. It is also used in veterinary medicine to treat false pregnancy in dogs.
- Hypersensitivity to ergot derivatives
- Pediatric patients (no clinical experience)
- Severely impaired liver function or cholestasis
- Co-medication with drugs metabolized mainly by CYP P450 such as erythromycin and ketoconazole, because increased plasma levels of cabergoline may result (although cabergoline undergoes minimal CYP450 metabolism).
- Cautions: severe cardiovascular disease, Raynaud’s disease, gastroduodenal ulcers, active gastrointestinal bleeding, hypotension.
Side effects are mostly dose-dependent. Much more severe side effects are reported for treatment of Parkinson’s disease and (off-label treatment) for restless leg syndrome which both typically require very high doses. The side effects are considered mild when used for the treatment of hyperprolactinemia and other endocrine disorders or gynecologic indications where the typical dose is one hundredth to one-tenth that for Parkinson’s disease.
Cabergoline requires slow dose titration (2–4 weeks for hyperprolactinemia, often much longer for other conditions) to minimize side effects. The extremely long bioavailability of the medication may complicate dosing regimens during titration and require particular precautions.
Cabergoline is considered the best tolerable option for hyperprolactinemia treatment although the newer and less tested quinagolide may offer similarly favorable side effect profile with quicker titration times.
No interactions were noted with levodopa or selegiline. The drug should not be combined with other ergot derivatives. Dopamine antagonists such as antipsychotics and metoclopramide counteract some effects of cabergoline. The use of antihypertensive drugs should be intensively monitored because excessive hypotension may result from the combination.
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Also known as: 1-((6-allylergolin-8beta-yl)carbonyl)-1-(3-(dimethylamino)propyl)-3-ethylurea, 1-ethyl-2-(3′-dimethylaminopropyl)-3-(6′-allylergoline-8′-beta-carbonyl)urea diphosphate, Cabaser, Cabaseril, cabergoline, cabergoline diphosphate, Dostinex, FCE 21336, Galastop