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DOSTINEX Tablets contain cabergoline, a dopamine receptor agonist. The chemical name for cabergoline is 1-[(6-allylergolin-8β-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, N-dimethylformamide (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.
DOSTINEX is an ergot derivative indicated for the treatment of hyperprolactinemic disorders, either idiopathic or due to pituitary adenomas in adults.
Avoid use of DOSTINEX for the inhibition or suppression of postpartum physiologic lactation because of the risk of serious adverse reactions [see WARNINGS AND PRECAUTIONS].
Before initiating DOSTINEX evaluate for valvular heart disease, including with an echocardiogram. If valvular disease is detected, do not administer DOSTINEX [see CONTRAINDICATIONS and WARNINGS AND PRECAUTIONS].
The recommended starting dosage of DOSTINEX is 0.25 mg orally twice weekly. Titrate DOSTINEX to achieve normal serum prolactin levels by increasing DOSTINEX by 0.25 mg orally twice weekly at intervals of no less than 4 weeks. The maximum recommended dosage is 1 mg orally, twice weekly [see WARNINGS AND PRECAUTIONS]. Administer DOSTINEX with or without food [see CLINICAL PHARMACOLOGY].
If DOSTINEX is discontinued, monitor the serum prolactin level periodically to determine whether DOSTINEX should be reinstituted.
Tablets: 0.5 mg, white, with functional score, capsule-shaped, scored on one side with the letter P and the letter U on either side of the breakline, engraved with the number 700 on the opposite side.
DOSTINEX (cabergoline) tablets are white, capsule-shaped, with functional score on one side with the letter P and the letter U on either side of the breakline, engraved with the number 700 on the opposite side and they are available in the following configuration: 0.5 mg strength, 8-count bottle, and NDC number 0013-7001-12.
Store at controlled room temperature 20°C to 25°C (68°F to 77°F) [see USP]. Store the tablets in the original container.
Distributed by: Pharmacia & Upjohn Company LLC, A subsidiary of Pfizer Inc. New York, NY 10001. Revised: Apr 2025.
The following clinically significant adverse reactions are described elsewhere in the labeling:
Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.
The safety of DOSTINEX has been evaluated in more than 900 patients with hyperprolactinemic disorders. In a 4-week, double-blind, placebo-controlled trial (DOSTINEX vs. placebo) [see Clinical Studies], the incidence of the most common adverse reactions during the placebo-controlled trial in patients with hyperprolactinemic disorders is presented in Table 1.
Table 1. Adverse Reactions (n (%))* During the 4-Week, Double-Blind, Placebo-Controlled Trial in Hyperprolactinemic Females
| DOSTINEX (n=168) |
Placebo (n=20) |
|
| Nausea | 45 (27%) | 4 (20%) |
| Headache | 43 (26%) | 5 (25%) |
| Dizziness | 25 (15%) | 1 (5%) |
| Constipation | 16 (10%) | 0% |
| Fatigue | 12 (7%) | 0% |
| Postural hypotension | 6 (4%) | 0% |
| Dyspepsia | 4 (2%) | 0% |
| Vomiting | 4 (2%) | 0% |
| Nervousness | 4 (2%) | 0% |
| Vertigo | 2 (1%) | 0% |
| Paresthesia | 2 (1%) | 0% |
| Breast pain | 2 (1%) | 0% |
| Dysmenorrhea | 2 (1%) | 0% |
| Abnormal vision | 2 (1%) | 0% |
| * Adverse reactions that occurred ≥1% in the DOSTINEX group and frequency more than that reported in the placebo group. | ||
In the 8-week, double-blind period of the comparative trial with bromocriptine, 2% (4/221) of DOSTINEXtreated patients (0.5 mg twice weekly) discontinued treatment because of an adverse event and 6% (14/231) of bromocriptine-treated patients (at a dose of 2.5 mg twice daily) discontinued treatment because of an adverse event. The most common reasons for DOSTINEX discontinuation were headache, nausea, and vomiting (3, 2, and 2 patients, respectively). The incidence of the most common adverse events during the double-blind period of the comparative trial with bromocriptine is presented in Table 2.
Table 2. Adverse Events* During the 8-Week, Double-Blind Period of the Comparative Trial in Hyperprolactinemic Females
| DOSTINEX (n=221) |
Bromocriptine (n=231) |
|
| Nausea | 63 (29%) | 100 (43%) |
| Headache | 58 (26%) | 62 (27%) |
| Dizziness | 38 (17%) | 42 (18%) |
| Constipation | 15 (7%) | 21 (9%) |
| Asthenia | 13 (6%) | 15 (6%) |
| Abdominal pain | 12 (5%) | 19 (8%) |
| Dyspepsia | 11 (5%) | 16 (7%) |
| Fatigue | 10 (5%) | 18 (8%) |
| Vertigo | 9 (4%) | 10 (4%) |
| Vomiting | 9 (4%) | 16 (7%) |
| Depression | 7 (3%) | 5 (2%) |
| Hot flashes | 6 (3%) | 3 (1%) |
| Breast pain | 5 (2%) | 8 (3%) |
| Dry mouth | 5 (2%) | 2 (1%) |
| Paresthesia | 5 (2%) | 6 (3%) |
| Somnolence | 5 (2%) | 5 (2%) |
| Diarrhea | 4 (2%) | 7 (3%) |
| Flatulence | 4 (2%) | 3 (1%) |
| Pain | 4 (2%) | 6 (3%) |
| Acne | 3 (1%) | 0% |
| Anorexia | 3 (1%) | 3 (1%) |
| Anxiety | 3 (1%) | 3 (1%) |
| Hypotension | 3 (1%) | 4 (2%) |
| Insomnia | 3 (1%) | 2 (1%) |
| Syncope | 3 (1%) | 3 (1%) |
| Abnormal vision | 2 (1%) | 2 (1%) |
| Arthralgia | 2 (1%) | 0% |
| Dependent edema | 2 (1%) | 1 (<1%) |
| Dysmenorrhea | 2 (1%) | 1 (<1%) |
| Impaired concentration | 2 (1%) | 1 (<1%) |
| Influenza-like symptoms | 2 (1%) | 0% |
| Malaise | 2 (1%) | 0% |
| Nervousness | 2 (1%) | 5 (2%) |
| Palpitation | 2 (1%) | 5 (2%) |
| Periorbital edema | 2 (1%) | 2 (1%) |
| Peripheral edema | 2 (1%) | 1 (<1%) |
| Pruritus | 2 (1%) | 1 (<1%) |
| Rhinitis | 2 (1%) | 9 (4%) |
| Throat irritation | 2 (1%) | 0% |
| Toothache | 2 (1%) | 0% |
| * Adverse events reported ≥1% in the DOSTINEX group. Abbreviation: n=number of patients. | ||
Events that were reported at an incidence of <1% in the clinical studies follow:
The following adverse reactions have been identified during post-approval use of DOSTINEX. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure.
DOSTINEX, a dopamine receptor agonist, is not recommended for concomitant use with D2-antagonists, such as phenothiazines, butyrophenones, thioxanthenes, or metoclopramide.
Included as part of the "PRECAUTIONS" Section
Before initiating DOSTINEX, perform a cardiovascular evaluation, including with an echocardiogram, to evaluate for valvular disease. DOSTINEX is contraindicated in the presence of valvular disease or pericardial fibrosis [see CONTRAINDICATIONS].
Cases of valvular and pericardial fibrosis have often manifested as heart failure. Following DOSTINEX treatment initiation, monitor for the development of valvulopathy with a cardiac echocardiogram at intervals of 6 to 12 months or as clinically indicated with new onset edema, cardiac murmur, dyspnea, or heart failure. During DOSTINEX treatment, monitor for chest pain and signs and symptoms of heart failure and if heart failure occurs, valvular fibrosis and pericarditis should be excluded. Consider clinical and diagnostic monitoring such as erythrocyte sedimentation rate, serum creatinine measurements, chest-x- ray, and other investigations and cardiac imaging at baseline and as necessary while patients are treated with during DOSTINEX treatment. Use DOSTINEX in patients treated with other drugs associated with valvulopathy only if the potential benefit of DOSTINEX outweighs the risk.
Discontinue DOSTINEX if the patient has a new diagnosis of valvular regurgitation, valvular restriction, valve leaflet thickening, or pericarditis.
Postmarketing cases of cardiac valvulopathy have been reported in patients who received DOSTINEX. These cases have generally occurred during administration of high doses of DOSTINEX (>2 mg/day) for the treatment of Parkinson’s disease (PD) (DOSTINEX is not approved for the treatment of PD). Cases of cardiac valvulopathy have also been reported in patients who received lower dosages of DOSTINEX for the treatment of hyperprolactinemic disorders. In a 12-year, multi-country retrospective cohort study, the use of DOSTINEX for PD was associated with an increased risk of cardiac valvular regurgitation (CVR). Compared to non-ergotderived dopamine agonists and levodopa, CVR with DOSTINEX use had an incidence rate per 10,000 person years of 68 (95% CI: 37, 115) versus 10 (95% CI: 5, 19) for non-ergot dopamine agonists and 11 (95% CI: 7, 17) for levodopa.
DOSTINEX is contraindicated in patients with a history of pleural, pulmonary, or retroperitoneal fibrosis. During DOSTINEX treatment monitor for signs and symptoms of progressive fibrosis, including:
Consider clinical and diagnostic monitoring for pleural, pulmonary, and retroperitoneal fibrosis such as with erythrocyte sedimentation rate, serum creatinine measurements, chest-x-ray, and other investigations at baseline and as necessary during DOSTINEX treatment. If pleural, pericardial, retroperitoneal, or pulmonary fibrosis occur, discontinue DOSTINEX.
Postmarketing cases of pleural, pulmonary, and retroperitoneal fibrosis have been reported following DOSTINEX administration. Some reports were in patients previously treated with other ergotinic dopamine agonists. DOSTINEX-treated patients who developed a pleural effusion or pulmonary fibrosis and subsequently discontinued DOSTINEX had improvement of their pulmonary symptoms.
Check blood pressure at baseline and during treatment with DOSTINEX and monitor for orthostatic hypotension. Warn patients about the risk of orthostatic hypotension and precautions to take when rising from a supine or sitting position. Instruct patients to report dizziness or lightheadedness with changes in position to their healthcare provider.
DOSTINEX can cause orthostatic hypotension [see ADVERSE REACTIONS]. In a 4-week, placebo-controlled trial in patients with hyperprolactinemic disorders, the percentage of DOSTINEX-treated patients and placebo-treated patients who developed orthostatic hypotension was 4% and 0%, respectively [see ADVERSE REACTIONS]. The risk of orthostatic hypotension is greater in DOSTINEX-treated patients when taking concomitant drugs that lower blood pressure.
Avoid use of DOSTINEX for the inhibition or suppression of postpartum physiologic lactation because of the risk of serious adverse reactions. Use of bromocriptine, another dopamine agonist for this unapproved use has been associated with cases of hypertension, stroke, myocardial infarction seizures, and death.
Because patients may not recognize impulse control and compulsive behaviors as abnormal, it is important for health care providers to specifically ask patients about the development of new or increased gambling urges, sexual urges, uncontrolled spending, or other urges while being treated with DOSTINEX. Consider dosage reduction or stopping DOSTINEX if a patient develops such urges while taking DOSTINEX.
Patients can experience intense urges to gamble or to spend money, increased sexual urges, binge eating, and/or other intense urges, and the inability to control these urges while taking one or more drugs that increase central dopaminergic tone, including DOSTINEX. In some cases, these urges were reported to have stopped when the dosage was reduced, or the drug was stopped.
Advise the patient to read the FDA-approved patient labeling (PATEINT INFORMATION).
There is a risk of cardiac valvulopathy, and pericardial, pleural, pulmonary, and retroperitoneal fibrosis with DOSTINEX treatment Advise patients to notify their healthcare provider if they develop shortness of breath, chest pain, persistent cough, difficulty with breathing when lying down, or swelling in their extremities [see WARNINGS AND PRECAUTIONS].
Warn patients about the risk of orthostatic hypotension and instruct patients to rise slowly from a supine or sitting position. Advise patients to notify their healthcare provider if they develop dizziness or lightheadedness [see WARNINGS AND PRECAUTIONS].
Patients should be alerted to the possibility that patients may experience intense urges to spend money uncontrollably, intense urges to gamble, increased sexual urges, and other intense urges and the inability to control these urges while taking DOSTINEX. Advise patients to inform their health care provider if they develop new or increased uncontrolled spending, gambling urges, sexual urges, or other urges while being treated with DOSTINEX [see WARNINGS AND PRECAUTIONS].
Advise patients to notify their health care provider if they suspect they are pregnant, become pregnant, or intend to become pregnant during therapy. A pregnancy test should be done if there is any suspicion of pregnancy and continuation of DOSTINEX treatment should be discussed with their health care provider [see Use In Specific Populations].
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 cabergoline dose of 0.003 mg/kg for 2 weeks prior to mating and throughout the mating period inhibited conception. This dose represents approximately 0.04 times 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.
This finding is likely due to the role of prolactin in implantation in rats and is not thought to be relevant to humans.
If conception occurs during DOSTINEX therapy, discontinue DOSTINEX if the risks to the mother or fetus outweigh the benefits to the mother. There are risks to the mother associated with the use of DOSTINEX (see Clinical Considerations).
The estimated background risk of major birth defects and miscarriage in patients with hyperprolactinemic disorders, either idiopathic or due to pituitary adenomas is unknown. All pregnancies have a risk of birth defect, loss, or other adverse outcomes. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively.
Maternal Adverse Reactions
In general, avoid use of dopamine agonists, including DOSTINEX, during pregnancy and the postpartum period. The risks of DOSTINEX use increase in pregnant females with pregnancy-induced hypertension, preeclampsia, and eclampsia.
Human Data
Published case reports have not reported a clear association with DOSTINEX and major birth defects, miscarriage, or adverse fetal outcomes when DOSTINEX was used during early pregnancy. However, these case reports cannot definitely establish the absence of DOSTINEX-associated risk.
Animal Data
Embryo-fetal development studies have been performed with cabergoline administered by oral gavage in mice, rats, and rabbits:
DOSTINEX is not recommended in postpartum women who are breastfeeding or who are planning to breastfeed. Avoid use of DOSTINEX for the inhibition or suppression of physiologic lactation [see INDICATIONS and WARNINGS AND PRECAUTIONS].
Safety and effectiveness of DOSTINEX in pediatric patients have not been established.
Clinical studies of DOSTINEX did not include sufficient numbers of patients 65 years of age and older to determine whether they respond differently from younger adult patients.
The use of DOSTINEX in patients with severe hepatic impairment (HI) (Child-Pugh C) is not recommended. When using DOSTINEX in patients with moderate HI (Child-Pugh B) increase monitoring of DOSTINEXassociated adverse reactions. The recommendations for use of DOSTINEX in patients with mild HI (Child Pugh A) is the same as those with normal hepatic function.
Patients with moderate or severe HI had increased cabergoline exposure [see CLINICAL PHARMACOLOGY], which may increase the risk of DOSTINEX-associated adverse reactions.
Take measures to support blood pressure, if necessary. Consider contacting the Poison Help line (1-800-222-1222) or a medical toxicologist for additional overdose management recommendations.
DOSTINEX is contraindicated in patients with:
Cabergoline is an ergot derivative and dopamine receptor agonist with a high affinity for D2 receptors. Results of in vitro studies demonstrate that cabergoline exerts a direct inhibitory effect on the secretion of prolactin by rat pituitary lactotrophs. Cabergoline decreased serum prolactin levels in reserpinized rats. Receptor-binding studies indicate that cabergoline has low affinity for dopamine D1, α1- and α2-adrenergic, and 5-HT1- and 5- HT2-serotonin receptors.
The exposure-response relationship and time course of pharmacodynamic response for the safety and effectiveness of DOSTINEX have not been fully characterized.
The time to reach maximum cabergoline plasma concentration was 2 to 3 hours after single oral doses of 0.5 mg to 1.5 mg (1.5 times the maximum recommended dose) of DOSTINEX in healthy subjects. Following dosing of DOSTINEX between 0.5 mg to 7 mg (7 times the maximum recommended dose), cabergoline plasma levels appeared to be dose-proportional. The absolute bioavailability of cabergoline is unknown. A significant fraction of the administered dose undergoes a first-pass effect.
Effect of Food
High-fat food did not alter the pharmacokinetics of cabergoline [see DOSAGE AND ADMINISTRATION].
Protein binding of cabergoline was 40% to 42%.
The elimination half-life of cabergoline estimated from urinary data of 12 healthy subjects ranged between 63 to 69 hours.
Metabolism
Cabergoline is extensively metabolized, predominately via hydrolysis of the acylurea bond or the urea moiety. Hydrolysis of the acylurea or urea moiety abolishes the prolactin-lowering effect of cabergoline, and major metabolites identified thus far do not contribute to the therapeutic effect.
Excretion
After oral dosing of radioactive cabergoline to 5 healthy volunteers, approximately 22% and 60% of the dose was excreted within 20 days in the urine and feces, respectively. Less than 4% of the dose was excreted unchanged in the urine. Nonrenal and renal clearances for cabergoline are about 3.2 L/min and 0.08 L/min, respectively. Urinary excretion in hyperprolactinemic patients was similar.
In a pharmacokinetic hepatic impairment (HI) study [see Use In Specific Populations]:
Male and Female Patients
Males aged 20 to 34 years were shown to have had higher Cmax than females aged 20 to 27 years) while males aged 66 to 75 years had lower Cmax compared to females aged 66 to 74 years. The clinical significance of the findings is unknown.
Patients with Renal Impairment
The pharmacokinetics of cabergoline were not altered in 12 patients with moderate-to-severe renal impairment as assessed by creatinine clearance.
The prolactin-lowering efficacy of DOSTINEX was demonstrated in 647 females with hyperprolactinemic disorders (including 55% microprolactinomas, 7% macroprolactinomas, 3% empty sella syndromes, and 3% idiopathic) in two randomized, double-blind, studies: one 4-week placebo-controlled dose-response study with an 12-month open-label extension (Study 1) and one 8-week active comparator study comparing DOSTINEX and bromocriptine with 16-week open extension (Study 2).
Study 1 enrolled 188 non-pregnant, hyperprolactinemic females (these patients had a prolactin level >20 ng/ml (the upper normal reference limit)) with the following hyperprolactinemic etiologies: macroprolactinoma (60%, n=113), idiopathic (36%, n=67) and another etiology (4%, n= 8). Patients had a mean age of 32 years (range, 16-46 years of age), 99% were White (n=186), 0.5% were Asian (n=1) and 0.5% were another race (n=1). Patients were randomized one of the following five oral treatments given twice weekly for four weeks (for the DOSTINEX groups, the first week the DOSTINEX dosage was lower to reduce the risk of hypotensive reactions):
In Study 1, the endpoint was the percentage of patients who achieved a normal serum prolactin level (<20 ng/dL) at the end of the 4-week treatment period. At 4-weeks, 0%, 76%, 74% and 95% of patients in the placebo group (group 1), group 3, group 4, and group 5, achieved normal serum prolactin levels, respectively (p <0.0001 across all the DOSTINEX groups vs. placebo).
Study 2 was an 8-week, randomized, double-blind active-control study that compared DOSTINEX (n=223) with bromocriptine (n=236) for the treatment of hyperprolactinemic amenorrhea. In this study, patients had a mean age of 31 years (range 16 – 46 years of age). Patients were randomized to oral DOSTINEX 0.5 mg twice weekly or oral bromocriptine 2.5 mg twice daily for eight weeks (there was an attrition rate respectively of 46% and 43%, in the DOSTINEX and bromocriptine groups, respectively). Endpoints included percentage of patients who achieved the following at 8 weeks:
In Study 2, at 8 weeks, DOSTINEX-treated and bromocriptine-treated patients had a normal serum prolactin level (77% and 59%, respectively), restoration of menses (77% and 70% respectively), and disappearance of galactorrhea, 73% and 56%, respectively).
The durability of the efficacy of DOSTINEX beyond 24 months of therapy has not been established.
DOSTINEX
(dos-tin-nex)
(cabergoline) tablets for oral use
What is DOSTINEX?
DOSTINEX is a prescription medicine used to treat a condition called hyperprolactinemia (increased levels of prolactin) in adults.
DOSTINEX is not for use to prevent or suppress breastfeeding after having given birth (postpartum lactation).
It is not known if DOSTINEX is safe and effective in children.
Who should not take DOSTINEX?
Do not take DOSTINEX if you:
Before taking DOSTINEX, tell your health care provider about all of your medical conditions, including if you:
How should I take DOSTINEX?
If you take too much DOSTINEX, call your Poison Help line at 1-800-222-1222 or go to the nearest hospital emergency room right away.
What are the possible side effects of DOSTINEX?
DOSTINEX can cause serious side effects, including:
The most common side effects of DOSTINEX include:
These are not all the possible side effects of DOSTINEX. For more information, ask your health care provider including your pharmacist. Call your health care provider for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.
How should I store DOSTINEX?
Keep DOSTINEX and all medicines out of the reach of children.
General Information about the safe and effective use of DOSTINEX.
Medicines are sometimes prescribed for purposes other than those listed in a Patient Information Leaflet. Do not use DOSTINEX for a condition for which it was not prescribed. Do not give DOSTINEX to other people, even if they have the same symptoms you have. It may harm them. You can ask your health care provider, including your pharmacist, for information that is written for health care providers.
What are the ingredients in DOSTINEX?
Active ingredient: cabergoline.
Inactive ingredients: leucine, USP and lactose, NF.
This product’s labeling may have been updated. For the current labeling, please visit www.pfizer.com.
This Patient Information has been approved by the U.S. Food and Drug Administration.
