DOSTINEX, Cabergoline

DOSTINEX DOSTINEX [cabergoline], marketed by Pharmacia & Upjohn is a dopamine receptor agonist which works by stimulating a part of the brain that can decrease the production of the hormone prolactin that causes milk production. DOSTINEX is primarily indicated for the treatment of hyperprolactinemia, either idiopathic or due to pituitary adenomas. With regards to hyperprolactinemia, it is way beyond drugs like Parlodel (Bromocriptine). It induces a complete biochemical response and shows much better clinical efficacy and at the same time was better tolerated than bromocriptine in the majority of patients. Hyperprolactinemia It is a condition seen in females in which there is an increased level of the hormone PROLACTIN in blood. Normal levels are less than 580 mIU/L for women, and less than 450 mIU/L for men Increased prolactin levels are usually associated during pregnancy, lactation, stress and sleep. Pathologically, the most common cause is a pituitary gland tumor called an adenoma also called as a prolactinoma. The levels are usually around 1000 mIU/L though levels of more than 5000 mIU/L are also seen. The regulation of prolactin is under the control of dopamine and estrogen. Prolactin secretion in the pituitary is normally suppressed by dopamine hence drugs which inhibit or deplete dopamine stores are commonly associated with increased levels of prolactin. These include tranquilizers, trifluoperazine and haloperidol some antipsychotic medications; metoclopramide, which is used to treat gastro esophageal reflux and the nausea caused by certain cancer drugs; and, less often, alpha-methyldopa and reserpine, used to control hypertension; and estrogens and TRH. Other causes include Cushing’s syndrome, chronic renal failure, hypothyroidism and sarcoidosis. It is also seen in patients with polycystic ovarian disease. Signs and Symptoms: In females a high blood level of prolactin often causes hypoestrogenism with anovulatory infertility and a decrease in menstruation. In some women may experience amenorrhea while some may experience irregular flow. Non gravid or non lactating females may experience breast milk secretion. Some might encounter a loss of libido (interest in sex). Coitus may become painful because of vaginal dryness. In men, the most common symptoms of hyperprolactinemia are decreased libido, erectile dysfunction, and infertility. In men excess prolactin may also cause Gynecomastia. Since men do not have any indicators like menstrual abnormalities in females, the diagnosis of hyperprolactinemia is usually delayed. They present late with symptoms like headache, ocular disturbances due to compression of the optic nerve by the tumor. Hyperprolactinemia can lead to osteoporosis, due to low estrogen levels. Uses of DOSTINEX: • prolactin-producing pituitary gland tumors and hyperprolactinemia • Monotherapy of Parkinson's disease in the early phase since it is a dopamine receptor agonist whereas Parkinson’s disease is associated with depletion of dopamine levels • Combination therapy, together with levodopa and a decarboxylase inhibitor such as carbidopa, in progressive-phase Parkinson's disease. • When the patient is unresponsive to bromocriptine Off Label uses: - used as an adjunct to SSRI antidepressants as there is evidence that it counteracts certain side effects of those drugs, like decreased libido. - Used by Bodybuilders who use anabolic steroids which can cause gynecomastia due to elevated levels of serum prolactin hormone. Side effects: The most notable side effect of DOSTINEX is Nausea Body As a Whole: facial edema, influenza-like symptoms, malaise Cardiovascular System: hypotension, syncope, palpitations Digestive System: dry mouth, flatulence, diarrhea, anorexia Metabolic and Nutritional System: weight loss, weight gain Nervous System: somnolence, nervousness, paresthesia, insomnia, anxiety Respiratory System: nasal stuffiness, epistaxis Skin and Appendages: acne, pruritis Special Senses: abnormal vision Urogenital System: dysmenorrhea, increased libido. With regards to increased libido, it is also at times used as a substitute for VIAGRA. Contraindications and Precautions: • Hypersensitivity to cabergoline or to ergot derivatives • Children due to lack of any trial on them • 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, however cabergoline undergoes minimal CYP450 metabolism. • Precautions: Raynaud's disease severe cardiovascular disease, gastro duodenal ulcers, active gastrointestinal bleeding, hypotension. Dosage: 500 mcg once a week, increased by 500 mcg increments, up to a maximum of 2 mg Samir is the author of Dostinex, Cabergoline information located at Genericsmed.com site References: - http://en.wikipedia.org/wiki/Cabergoline - http://www.webmd.com/drugs/drug-14605-Dostinex.aspx?drugid=14605&drugname=Dostinex - http://en.wikipedia.org/wiki/Hyperprolactinemia - Pharmacology and Pharmacotherapeutics Revised 17th Edition, R.S.Satoskar, S.D.Bhandarkar, and S.S.Ainapure. pg 943

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