Cabergoline (Generic Dostinex) - Uses, Dosage and Side Effects

Cabergoline (Generic Dostinex), an ergot derivative, is a potent dopamine receptor agonist on D2 receptors. Cabergoline is used for the treatment of hyperprolactinemic disorders, either idiopathic or due to pituitary adenomas. It is frequently used as a first-line agent in the management of prolactinomas due to higher affinity for D2 receptor sites, less severe side effects, and more convenient dosing schedule than the older bromocriptine.
Following a single oral dose, resorption of cabergoline from the gastrointestinal (GI) tract is highly variable, typically occurring within 0.5 to 4 hours. Ingestion with food does not alter its absorption rate. The therapeutic effect in treatment of hyperprolactinemia will typically persist for at least 4 weeks after cessation of treatment.

Cabergoline (Generic Dostinex) - Availability And Packaging

Cabergoline is available as Generic Dostinex Tablets which is packaged in 0.5 mg tablets. It is also available under brand names Dostinex and Cabaser

Generic Dostinex - Dosage

The dosage of Generic Dostinex (Cabergoline) *Parkinson's disease: Monotherapy: Initial dose should be 0.5 mg daily. The usual maintenance dose is 2 to 4 mg daily. Combination therapy: Usually 2 to 6 mg daily.
*Tumors of the pituitary gland and other hyperprolactinemic conditions: Initially 0.5 mg per week, slowly titrated to 4.5 mg per week, if necessary.
*Ablactation: As per specific treatment scheme.

Contraindications And Precautions

Listed below are the Contraindications And Precautions to be observed before undergoing Cabergoline therapy

  • 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).
  • Precautions: severe cardiovascular disease, Raynaud's disease, gastroduodenal ulcers, active gastrointestinal bleeding, hypotension.

 

Side Effects of Cabergoline (Generic Dostinex)

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 treatment of hyperprolactinemia and other endocrine disorders or gynecologic indications where the typical dose is 10-100 times smaller than for Parkinson's disease.
Cabergoline requires slow dose titration (2–4 weeks for hyperprolactinemia, often much longer for other conditions) to minimise 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 favourable side effect profile with quicker titration times.
GI tract: Side effects were extremely frequent. Fifty-three percent of patients reported side effects. Very frequent: Nausea (30%), constipation (22%), and dry mouth (10%). Frequent: Gastric irritation (7%), vomiting (5%), and dyspepsia (2%).
Psychiatric disturbances and central nervous system (CNS): Altogether 51 percent of patients were affected. Very frequent: Sleep disturbances (somnolence 18%, insomnia 11%), vertigo (27%), and depression (13%). Frequent: dyskinesia (4%) and hallucinations (4%).
Cardiovascular: Approximately 30 percent of patients experienced side effects. Most frequent were hypotension (10%), peripheral edema (14%) and non-specific edema (2%). Arrhythmias were encountered in 4.8%, palpitations in 4.3%, and angina pectoris in 1.4%.

Effects of Cabergoline (Generic Dostinex) During Pregnancy And Lactation

The effects of Generic Dostinex during pregnancy and lactation is described below.In certain 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.
  • 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 treatment 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.

 

Additional Information

Additional Info: Prescribing Information



Considerable portions of the text here is from http://en.wikipedia.org/wiki/Cabergoline and is reproduced here under the Creative Commons Attribution-ShareAlike License