Drug: Dostinex

DOSTINEX Tablets contain cabergoline, a dopamine receptor agonist. The chemical name for cabergoline is 1-[(6-allylergolin-8ß-yl)-carbonyl]-1-[3-(dimethylamino) propyl]-3-ethylurea. Its empirical formula is C26H37N5O2, and its molecular weight is 451.62. The structural formula is as follows: Cabergoline is a white powder soluble in ethyl alcohol, chloroform, and N, Ndimethylformamide (DMF); slightly soluble in 0.1N hydrochloric acid; very slightly soluble in n-hexane; and insoluble in water. DOSTINEX Tablets, for oral administration, contain 0.5 mg of cabergoline. Inactive ingredients consist of leucine, USP, and lactose, NF.

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The safety of DOSTINEX Tablets has been evaluated in more than 900 patients with hyperprolactinemic disorders. Most adverse events were mild or moderate in severity. In a 4-week, double-blind, placebo-controlled study, treatment consisted of placebo or cabergoline at fixed doses of 0.125, 0.5, 0.75, or 1.0 mg twice weekly. Doses were halved during the first week. Since a possible dose-related effect was observed for nausea only, the four cabergoline treatment groups have been combined. The incidence of the most common adverse events during the placebo-controlled study is presented in the following table. Incidence of Reported Adverse Events During the 4-Week, Double-Blind, Placebo-Controlled Trial
Adverse Event* Cabergoline
(n=168)
0.125 to 1 mg two times a week Placebo
(n=20) Number (percent) Gastrointestinal   Nausea 45 (27) 4 (20)   Constipation 16 (10) 0   Abdominal pain 9 (5) 1 (5)   Dyspepsia 4 (2) 0   Vomiting 4 (2) 0 Central and Peripheral Nervous System   Headache 43 (26) 5 (25)   Dizziness 25 (15) 1 (5)   Paresthesia 2 (1) 0   Vertigo 2 (1) 0 Body As a Whole   Asthenia 15 (9) 2 (10)   Fatigue 12 (7) 0   Hot flashes 2 (1) 1 (5) Psychiatric   Somnolence 9 (5) 1 (5)   Depression 5 (3) 1 (5)   Nervousness 4 (2) 0 Autonomic Nervous System   Postural hypotension 6 (4) 0 Reproductive – Female   Breast pain 2 (1) 0   Dysmenorrhea 2 (1) 0 Vision   Abnormal vision 2 (1) 0 *Reported at ≥ 1% for cabergoline In the 8-week, double-blind period of the comparative trial with bromocriptine, DOSTINEX (at a dose of 0.5 mg twice weekly) was discontinued because of an adverse event in 4 of 221 patients (2%) while bromocriptine (at a dose of 2.5 mg two times a day) was discontinued in 14 of 231 patients (6%). The most common reasons for discontinuation from DOSTINEX were headache, nausea and vomiting (3, 2 and 2 patients respectively); the most common reasons for discontinuation from bromocriptine were nausea, vomiting, headache, and dizziness or vertigo (10, 3, 3, and 3 patients respectively). The incidence of the most common adverse events during the double-blind portion of the comparative trial with bromocriptine is presented in the following table. Incidence of Reported Adverse Events During the 8-Week, Double-Blind Period of the Comparative Trial With Bromocriptine
Adverse Event* Cabergoline
(n=221) Bromocriptine
(n=231) Number (percent) Gastrointestinal   Nausea 63 (29) 100 (43)   Constipation 15 (7) 21 (9)   Abdominal pain 12 (5) 19 (8)   Dyspepsia 11 (5) 16 (7)   Vomiting 9 (4) 16 (7)   Dry mouth 5 (2) 2 (1)   Diarrhea 4 (2) 7 (3)   Flatulence 4 (2) 3 (1)   Throat irritation 2 (1) 0   Toothache 2 (1) 0 Central and Peripheral Nervous System   Headache 58 (26) 62 (27)   Dizziness 38 (17) 42 (18)   Vertigo 9 (4) 10 (4)   Paresthesia 5 (2) 6 (3) Body As a Whole   Asthenia 13 (6) 15 (6)   Fatigue 10 (5) 18 (8)   Syncope 3 (1) 3 (1)   Influenza-like symptoms 2 (1) 0   Malaise 2 (1) 0   Periorbital edema 2 (1) 2 (1)   Peripheral edema 2 (1) 1 Psychiatric   Depression 7 (3) 5 (2)   Somnolence 5 (2) 5 (2)   Anorexia 3 (1) 3 (1)   Anxiety 3 (1) 3 (1)   Insomnia 3 (1) 2 (1)   Impaired concentration 2 (1) 1   Nervousness 2 (1) 5 (2) Cardiovascular   Hot flashes 6 (3) 3 (1)   Hypotension 3 (1) 4 (2)   Dependent edema 2 (1) 1   Palpitation 2 (1) 5 (2) Reproductive – Female   Breast pain 5 (2) 8 (3)   Dysmenorrhea 2 (1) 1 Skin and Appendages   Acne 3 (1) 0   Pruritus 2 (1) 1 Musculoskeletal   Pain 4 (2) 6 (3)   Arthralgia 2 (1) 0 Respiratory   Rhinitis 2 (1) 9 (4) Vision   Abnormal vision 2 (1) 2 (1) *Reported at ≥ 1% for cabergoline Other adverse events that were reported at an incidence of < 1.0% in the overall clinical studies follow. 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, pruritus Special Senses: abnormal vision Urogenital System: dysmenorrhea, increased libido The safety of cabergoline has been evaluated in approximately 1,200 patients with Parkinson's disease in controlled and uncontrolled studies at dosages of up to 11.5 mg/day which greatly exceeds the maximum recommended dosage of cabergoline for hyperprolactinemic disorders. In addition to the adverse events that occurred in the patients with hyperprolactinemic disorders, the most common adverse events in patients with Parkinson's disease were dyskinesia, hallucinations, confusion, and peripheral edema. Heart failure, pleural effusion, pulmonary fibrosis, and gastric or duodenal ulcer occurred rarely. One case of constrictive pericarditis has been reported. Postmarketing Surveillance data The following events have been reported in association with DOSTINEX: cardiac valvulopathy and extracardiac fibrotic reactions, (See WARNINGS, Cardiac Valvulopathy and Extracardiac Fibrotic Reactions). Others events have been reported in association with cabergoline: hypersexuality, increased libido, pathological gambling (See PRECAUTIONS, Psychiatric). In addition, cases of alopecia, aggression and psychotic disorder have been reported in patients taking DOSTINEX. Some of these reports have been in patients who have had prior adverse reactions to dopamine agonist products. Read the Dostinex (cabergoline) Side Effects Center for a complete guide to possible side effectsLearn More »

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The recommended dosage of DOSTINEX Tablets for initiation of therapy is 0.25 mg twice a week. Dosage may be increased by 0.25 mg twice weekly up to a dosage of 1 mg twice a week according to the patient's serum prolactin level. Before initiating treatment, cardiovascular evaluation should be performed and echocardiography should be considered to assess for valvular disease. Dosage increases should not occur more rapidly than every 4 weeks, so that the physician can assess the patient's response to each dosage level. If the patient does not respond adequately, and no additional benefit is observed with higher doses, the lowest dose that achieved maximal response should be used and other therapeutic approaches considered. Patients receiving long term treatment with DOSTINEX should undergo periodic assessment of their cardiac status and echocardiography should be considered. After a normal serum prolactin level has been maintained for 6 months, DOSTINEX may be discontinued, with periodic monitoring of the serum prolactin level to determine whether or when treatment with DOSTINEX should be reinstituted. The durability of efficacy beyond 24 months of therapy with DOSTINEX has not been established.

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DOSTINEX should not be administered concurrently with D2antagonists, such as phenothiazines, butyrophenones, thioxanthenes, or metoclopramide.Read the Dostinex Drug Interactions Center for a complete guide to possible interactions Learn More »

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DOSTINEX Tablets are indicated for the treatment of hyperprolactinemic disorders, either idiopathic or due to pituitary adenomas.

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DOSTINEX Tablets are contraindicated in patients with:
  • Uncontrolled hypertension or known hypersensitivity to ergot derivatives.
  • History of cardiac valvular disorders, as suggested by anatomical evidence of valvulopathy of any valve, determined by pre-treatment evaluation including echocardiographic demonstration of valve leaflet thickening, valve restriction, or mixed valve restriction-stenosis. (See WARNINGS)
  • History of pulmonary, pericardial, or retroperitoneal fibrotic disorders. (See WARNINGS)
Last reviewed on RxList: 7/28/2011
This monograph has been modified to include the generic and brand name in many instances.

Source: http://www.rxlist.com

Overdosage might be expected to produce nasal congestion, syncope, or hallucinations. Measures to support blood pressure should be taken if necessary.

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DOSTINEX Tablets are white, scored, capsule-shaped tablets containing 0.5 mg cabergoline. Each tablet is scored on one side and has the letter P and the letter U on either side of the breakline. The other side of the tablet is engraved with the number 700. DOSTINEX is available as follows: Bottles of 8 tablets NDC 0013-7001-12 Storage Store at controlled room temperature 20°to 25°C (68°to 77°F) [see USP]. Distributed by : Pharmacia & Upjohn Company, Division of Pfizer Inc, NY, NY 10017. Revised July 2011 Last reviewed on RxList: 7/28/2011
This monograph has been modified to include the generic and brand name in many instances.

Source: http://www.rxlist.com

General Initial doses higher than 1.0 mg may produce orthostatic hypotension. Care should be exercised when administering DOSTINEX with other medications known to lower blood pressure. Postpartum Lactation Inhibition or Suppression DOSTINEX is not indicated for the inhibition or suppression of physiologic lactation. Use of bromocriptine, another dopamine agonist for this purpose, has been associated with cases of hypertension, stroke, and seizures. Hepatic Impairment Since cabergoline is extensively metabolized by the liver, caution should be used, and careful monitoring exercised, when administering DOSTINEX to patients with hepatic impairment. Psychiatric Pathological gambling, increased libido, and hypersexuality have been reported in patients treated with dopamine agonists including cabergoline. This has been generally reversible upon reduction of the dose or treatment discontinuation (See Postmarketing Surveillance data). Carcinogenesis, Mutagenesis, Impairment of Fertility Carcinogenicity studies were conducted in mice and rats with cabergoline given by gavage at doses up to 0.98 mg/kg/day and 0.32 mg/kg/day, respectively. These doses are 7 times and 4 times the maximum recommended human dose calculated on a body surface area basis using total mg/m²/week in rodents and mg/m²/week for a 50 kg human. There was a slight increase in the incidence of cervical and uterine leiomyomas and uterine leiomyosarcomas in mice. In rats, there was a slight increase in malignant tumors of the cervix and uterus and interstitial cell adenomas. The occurrence of tumors in female rodents may be related to the prolonged suppression of prolactin secretion because prolactin is needed in rodents for the maintenance of the corpus luteum. In the absence of prolactin, the estrogen/progesterone ratio is increased, thereby increasing the risk for uterine tumors. In male rodents, the decrease in serum prolactin levels was associated with an increase in serum luteinizing hormone, which is thought to be a compensatory effect to maintain testicular steroid synthesis. Since these hormonal mechanisms are thought to be species-specific, the relevance of these tumors to humans is not known. The mutagenic potential of cabergoline was evaluated and found to be negative in a battery of in vitro tests. These tests included the bacterial mutation (Ames) test with Salmonella typhimurium, the gene mutation assay with Schizosaccharomyces pombe P1 and V79 Chinese hamster cells, DNA damage and repair in Saccharomyces cerevisiae D4, and chromosomal aberrations in human lymphocytes. Cabergoline was also negative in the bone marrow micronucleus test in the mouse. In female rats, a daily dose of 0.003 mg/kg for 2 weeks prior to mating and throughout the mating period inhibited conception. This dose represents approximately 1/28 the maximum recommended human dose calculated on a body surface area basis using total mg/m²/week in rats and mg/m²/week for a 50 kg human. Pregnancy Teratogenic Effects - Category B Reproduction studies have been performed with cabergoline in mice, rats, and rabbits administered by gavage. (Multiples of the maximum recommended human dose in this section are calculated on a body surface area basis using total mg/m²/week for animals and mg/m²/week for a 50 kg human.) There were maternotoxic effects but no teratogenic effects in mice given cabergoline at doses up to 8 mg/kg/day (approximately 55 times the maximum recommended human dose) during the period of organogenesis. A dose of 0.012 mg/kg/day (approximately 1/7 the maximum recommended human dose) during the period of organogenesis in rats caused an increase in post-implantation embryofetal losses. These losses could be due to the prolactin inhibitory properties of cabergoline in rats. At daily doses of 0.5 mg/kg/day (approximately 19 times the maximum recommended human dose) during the period of organogenesis in the rabbit, cabergoline caused maternotoxicity characterized by a loss of body weight and decreased food consumption. Doses of 4 mg/kg/day (approximately 150 times the maximum recommended human dose) during the period of organogenesis in the rabbit caused an increased occurrence of various malformations. However, in another study in rabbits, no treatment-related malformations or embryofetotoxicity were observed at doses up to 8 mg/kg/day (approximately 300 times the maximum recommended human dose). In rats, doses higher than 0.003 mg/kg/day (approximately 1/28 the maximum recommended human dose) from 6 days before parturition and throughout the lactation period inhibited growth and caused death of offspring due to decreased milk secretion. There are, however, no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, this drug should be used during pregnancy only if clearly needed. Nursing Mothers It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk and because of the potential for serious adverse reactions in nursing infants from cabergoline, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother. Use of DOSTINEX for the inhibition or suppression of physiologic lactation is not recommended (see PRECAUTIONS section). The prolactin-lowering action of cabergoline suggests that it will interfere with lactation. Due to this interference with lactation, DOSTINEX should not be given to women postpartum who are breastfeeding or who are planning to breastfeed. Pediatric Use Safety and effectiveness of DOSTINEX in pediatric patients have not been established. Geriatric Use Clinical studies of DOSTINEX did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger patients. Other reported clinical experience has not identified differences in responses between the elderly and younger patients. In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.Last reviewed on RxList: 7/28/2011
This monograph has been modified to include the generic and brand name in many instances.

Source: http://www.rxlist.com

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