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Drug overview for CABERGOLINE (cabergoline):
Generic name: cabergoline (ka-BER-goe-leen)
Drug class: Antiparkinsonian Dopamine Agonists
Therapeutic class: Endocrine
Cabergoline is an ergot-derivative dopamine receptor agonist and prolactin inhibitor.
No enhanced Uses information available for this drug.
Generic name: cabergoline (ka-BER-goe-leen)
Drug class: Antiparkinsonian Dopamine Agonists
Therapeutic class: Endocrine
Cabergoline is an ergot-derivative dopamine receptor agonist and prolactin inhibitor.
No enhanced Uses information available for this drug.
DRUG IMAGES
CABERGOLINE 0.5 MG TABLET
The following indications for CABERGOLINE (cabergoline) have been approved by the FDA:
Indications:
Hyperprolactinemia
Professional Synonyms:
None.
Indications:
Hyperprolactinemia
Professional Synonyms:
None.
The following dosing information is available for CABERGOLINE (cabergoline):
Cabergoline therapy should be initiated with a low dosage and increased slowly (at intervals of at least 4 weeks) until therapeutic response is achieved.
An initial adult cabergoline dosage of 0.25 mg twice weekly is recommended for the treatment of hyperprolactinemic disorders; dosage may be increased in increments of 0.25 mg twice weekly up to 1 mg twice weekly based on the patient's serum prolactin concentrations; the lowest effective dosage should be used.
Patients receiving long-term treatment with the drug should be periodically evaluated to determine continued need for therapy. Some patients (e.g., those with normal prolactin concentrations for 6 months) may be able to discontinue the drug with periodic monitoring of serum prolactin concentrations to determine whether or when cabergoline therapy should be reinstituted; discontinuance of therapy in those with macroadenomas should be undertaken with extreme caution. The manufacturer states that efficacy of cabergoline beyond 24 months has not been established.
An initial adult cabergoline dosage of 0.25 mg twice weekly is recommended for the treatment of hyperprolactinemic disorders; dosage may be increased in increments of 0.25 mg twice weekly up to 1 mg twice weekly based on the patient's serum prolactin concentrations; the lowest effective dosage should be used.
Patients receiving long-term treatment with the drug should be periodically evaluated to determine continued need for therapy. Some patients (e.g., those with normal prolactin concentrations for 6 months) may be able to discontinue the drug with periodic monitoring of serum prolactin concentrations to determine whether or when cabergoline therapy should be reinstituted; discontinuance of therapy in those with macroadenomas should be undertaken with extreme caution. The manufacturer states that efficacy of cabergoline beyond 24 months has not been established.
Cabergoline is administered orally without regard to meals.
| DRUG LABEL | DOSING TYPE | DOSING INSTRUCTIONS |
|---|---|---|
| CABERGOLINE 0.5 MG TABLET | Maintenance | Adults take 1 tablet (0.5 mg) by oral route twice weekly |
| DRUG LABEL | DOSING TYPE | DOSING INSTRUCTIONS |
|---|---|---|
| CABERGOLINE 0.5 MG TABLET | Maintenance | Adults take 1 tablet (0.5 mg) by oral route twice weekly |
The following drug interaction information is available for CABERGOLINE (cabergoline):
There are 1 contraindications.
These drug combinations generally should not be dispensed or administered to the same patient. A manufacturer label warning that indicates the contraindication warrants inclusion of a drug combination in this category, regardless of clinical evidence or lack of clinical evidence to support the contraindication.
| Drug Interaction | Drug Names |
|---|---|
| Cabergoline; Pergolide/Metoclopramide SEVERITY LEVEL: 1-Contraindicated Drug Combination: This drug combination is contraindicated and generally should not be dispensed or administered to the same patient. MECHANISM OF ACTION: Dopamine antagonists such as metoclopramide may block the effects of cabergoline(1) and pergolide(2,3), dopamine agonists. CLINICAL EFFECTS: Concurrent administration of cabergoline or pergolide with metoclopramide may decrease the effectiveness of cabergoline(1) and pergolide.(2,3) PREDISPOSING FACTORS: None determined. PATIENT MANAGEMENT: The manufacturers of cabergoline and pergolide state that cabergoline(1) and pergolide(2) should not be administered concurrently with dopamine antagonists such as metoclopramide. DISCUSSION: The manufacturers of cabergoline and pergolide state that these agents should not be administered concurrently with dopamine antagonists such as metoclopramide.(1-3) |
GIMOTI, METOCLOPRAMIDE HCL, REGLAN |
There are 3 severe interactions.
These drug interactions can produce serious consequences in most patients. Actions required for severe interactions include, but are not limited to, discontinuing one or both agents, adjusting dosage, altering administration scheduling, and providing additional patient monitoring. Review the full interaction monograph for more information.
| Drug Interaction | Drug Names |
|---|---|
| Cabergoline/Selected Dopamine Blockers SEVERITY LEVEL: 2-Severe Interaction: Action is required to reduce the risk of severe adverse interaction. MECHANISM OF ACTION: Dopamine (D2) blockers such as the phenothiazines, butyrophenones, thioxanthenes and atypical antipsychotics may decrease the effects of cabergoline, a dopamine agonist.(1) CLINICAL EFFECTS: Concurrent administration of cabergoline with dopamine blockers (e.g. phenothiazines, butyrophenones, or thio xanthines) may decrease the effectiveness of cabergoline.(1) Cabergoline may decrease the effectiveness of antipsychotic treatment. PREDISPOSING FACTORS: None determined. PATIENT MANAGEMENT: The manufacturer of cabergoline states cabergoline(1) should not be administered concurrently with dopamine antagonists. Avoid concurrent use when possible. If cabergoline is started in a patient receiving long term antipsychotic treatment, monitor closely for loss of antipsychotic efficacy. If an antipsychotic is required for a patient on long term cabergoline therapy, consider use of a shorter half-life, less potent dopamine (D2) blocking atypical antipsychotic (e.g. clozapine, quetiapine) and monitor closely. DISCUSSION: The manufacturer of cabergoline state that it should not be administered concurrently with dopamine antagonists. |
ABILIFY, ABILIFY ASIMTUFII, ABILIFY MAINTENA, ADASUVE, ARIPIPRAZOLE, ARIPIPRAZOLE ODT, ARISTADA, ARISTADA INITIO, ASENAPINE MALEATE, BARHEMSYS, CHLORPROMAZINE HCL, COMPAZINE, COMPRO, DROPERIDOL, ERZOFRI, FANAPT, FLUPHENAZINE DECANOATE, FLUPHENAZINE HCL, GEODON, HALDOL DECANOATE 100, HALOPERIDOL, HALOPERIDOL DECANOATE, HALOPERIDOL DECANOATE 100, HALOPERIDOL LACTATE, INVEGA, INVEGA HAFYERA, INVEGA SUSTENNA, INVEGA TRINZA, LATUDA, LOXAPINE, LURASIDONE HCL, LYBALVI, MOLINDONE HCL, OLANZAPINE, OLANZAPINE ODT, OLANZAPINE-FLUOXETINE HCL, OPIPZA, PALIPERIDONE ER, PERPHENAZINE, PERPHENAZINE-AMITRIPTYLINE, PERSERIS, PIMOZIDE, PROCHLORPERAZINE, PROCHLORPERAZINE EDISYLATE, PROCHLORPERAZINE MALEATE, QUETIAPINE FUMARATE, QUETIAPINE FUMARATE ER, REXULTI, RISPERDAL, RISPERDAL CONSTA, RISPERIDONE, RISPERIDONE ER, RISPERIDONE ODT, RYKINDO, SAPHRIS, SECUADO, SEROQUEL, SEROQUEL XR, THIORIDAZINE HCL, THIORIDAZINE HYDROCHLORIDE, THIOTHIXENE, TRIFLUOPERAZINE HCL, UZEDY, VRAYLAR, ZIPRASIDONE HCL, ZIPRASIDONE MESYLATE, ZYPREXA |
| Selected CYP3A4 Substrates/Lonafarnib SEVERITY LEVEL: 2-Severe Interaction: Action is required to reduce the risk of severe adverse interaction. MECHANISM OF ACTION: Lonafarnib is a strong inhibitor of CYP3A4 and may decrease the metabolism of drugs metabolized by the CYP3A4 enzyme. Lonafarnib is also an inhibitor of P-glycoprotein (P-gp) and may increase the absorption of sirolimus. CLINICAL EFFECTS: Concurrent use of lonafarnib may lead to increased serum levels and adverse effects of drugs sensitive to inhibition of the CYP3A4 pathway or P-gp.(1) PREDISPOSING FACTORS: None determined. PATIENT MANAGEMENT: The manufacturer of lonafarnib states that coadministration of CYP3A4 substrates should be avoided. If concomitant use is unavoidable, monitor for adverse effects and consider dose reduction of the CYP3A4 substrate according to its prescribing information.(1) The manufacturer of lonafarnib states that the dose of P-gp substrates may need to be reduced with coadministration with lonafarnib.(1) DISCUSSION: In a study of healthy volunteers, lonafarnib (100 mg twice daily for 5 days) increased the area-under-the-curve (AUC) and maximum concentration (Cmax) of a single dose of midazolam (3 mg) by 639% and 180%, respectively.(1) In a study of healthy volunteers, lonafarnib (100 mg twice daily for 5 days) increased the AUC and Cmax of single-dose fexofenadine (180 mg) by 24% and 21%, respectively.(1) CYP3A4 substrates with a narrow therapeutic index linked to this monograph include: bromocriptine, cabergoline, cannabidiol-tetrahydrocannabinol, clonazepam, darolutamide, felodipine, mefloquine, nisoldipine, oliceridine, pomalidomide, regorafenib, sirolimus, and zanubrutinib.(1-3) |
ZOKINVY |
| Bromocriptine; Cabergoline/Selected Macrolide Antibiotics SEVERITY LEVEL: 2-Severe Interaction: Action is required to reduce the risk of severe adverse interaction. MECHANISM OF ACTION: Selected macrolide antibiotics that are strong CYP3A4 inhibitors may inhibit the metabolism of bromocriptine and cabergoline.(1-3) CLINICAL EFFECTS: Concurrent use of selected macrolide antibiotics may result in increased levels of bromocriptine and cabergoline, which may result in increased side effects of these agents.(1-3) PREDISPOSING FACTORS: None determined. PATIENT MANAGEMENT: Use caution with concurrent therapy with bromocriptine and cabergoline with selected macrolide antibiotics.(1-3) The US manufacturer of bromocriptine states use caution when co-administering drugs that are inhibitors of CYP3A4. Concomitant use of strong CYP3A4 inhibitors should be avoided. Ensure adequate washout of strong CYP3A4 inhibitor drug before initiating bromocriptine.(2) DISCUSSION: Concurrent administration of selected macrolide antibiotics with bromocriptine or cabergoline may increase the side effects of these agents. Clarithromycin, josamycin, telithromycin and troleandomycin are strong CYP3A4 inhibitors.(4) Itraconazole has been shown to increase cabergoline concentrations with concurrent use. A case report including 2 patients with concurrent therapy of cabergoline and itraconazole noted plasma levels of cabergoline to be increased by 300% in one of the patients. This increase in cabergoline concentrations was noted to increase clinical improvement.(6) A study compared ten healthy male volunteers taking cabergoline (1 mg/day) alone for 6 days or a single oral dose of cabergoline plus clarithromycin (400 mg/day) for 6 days. Mean plasma cabergoline concentrations increased 2.6-fold with clarithromycin coadministration. The study also compared seven patients with Parkinson's disease receiving stable doses of cabergoline alone and with the addition of clarithromycin (400 mg/day for 6 days). Cabergoline plasma concentrations increased 1.7-fold during clarithromycin coadministration.(7) A study in five healthy subjects found that concurrent administration of erythromycin, a moderate CYP3A4 inhibitor, and bromocriptine resulted in a 268% increase in area-under-curve (AUC) for bromocriptine and a 4.6-fold increase in bromocriptine maximum concentration (Cmax).(8) |
CLARITHROMYCIN, CLARITHROMYCIN ER, LANSOPRAZOL-AMOXICIL-CLARITHRO, OMECLAMOX-PAK, VOQUEZNA TRIPLE PAK |
There are 2 moderate interactions.
The clinician should assess the patient’s characteristics and take action as needed. Actions required for moderate interactions include, but are not limited to, discontinuing one or both agents, adjusting dosage, altering administration.
| Drug Interaction | Drug Names |
|---|---|
| Bromocriptine; Cabergoline/Selected CYP3A4 Inhibitors SEVERITY LEVEL: 3-Moderate Interaction: Assess the risk to the patient and take action as needed. MECHANISM OF ACTION: Certain azole antifungals (itraconazole(1,6), ketoconazole(2), posaconazole(3,4), and voriconazole(5)), protease inhibitors (amprenavir(7), atazanavir(8), boceprevir(9), darunavir(10), fosamprenavir(11), indinavir(12), lopinavir(13), nelfinavir(14), nirmatrelvir/ritonavir,(15) ritonavir(16), saquinavir(17), telaprevir(18), and tipranavir(19)), and other strong CYP3A4 inhibitors (cobicistat, idelalisib, levoketoconazole, mibefradil, nefazodone, and ribociclib(20)) may inhibit the metabolism of bromocriptine and cabergoline by CYP3A4. CLINICAL EFFECTS: Concurrent use of bromocriptine or cabergoline with azole antifungals, protease inhibitors, or other strong CYP3A4 inhibitors may result in increased levels of bromocriptine and cabergoline, which may result in increased side effects of these agents. PREDISPOSING FACTORS: None determined. PATIENT MANAGEMENT: Use caution with concurrent therapy with bromocriptine and cabergoline with azole antifungals, protease inhibitors, or other strong CYP3A4 inhibitors. DISCUSSION: Itraconazole has been shown to increase cabergoline concentrations with concurrent use. A case report including 2 patients with concurrent therapy of cabergoline and itraconazole noted plasma levels of cabergoline to be increased by 300% in one of the patients. This increase in cabergoline concentrations was noted to increase clinical improvement.(6) Posaconazole has been shown to inhibit the CYP3A4 mediated metabolism of midazolam by 83%.(3) Voriconazole (400 mg every 12 hours for one day, then 200 mg every 12 hours for 8 days) increased the maximum concentration (Cmax) and area-under-curve (AUC) of a single dose of sirolimus (2 mg) by 7-fold and 11-fold, respectively. Ergot alkaloids are metabolized by the same isoenzyme system.(5) |
APTIVUS, ATAZANAVIR SULFATE, DARUNAVIR, FOSAMPRENAVIR CALCIUM, GENVOYA, ITRACONAZOLE, ITRACONAZOLE MICRONIZED, KALETRA, KETOCONAZOLE, KISQALI, LOPINAVIR-RITONAVIR, NEFAZODONE HCL, NORVIR, NOXAFIL, PAXLOVID, POSACONAZOLE, PREZISTA, RECORLEV, REYATAZ, RITONAVIR, SPORANOX, STRIBILD, TOLSURA, TYBOST, VFEND, VFEND IV, VIRACEPT, VORICONAZOLE, ZYDELIG |
| Bromocriptine; Cabergoline/Selected Macrolide Antibiotics SEVERITY LEVEL: 3-Moderate Interaction: Assess the risk to the patient and take action as needed. MECHANISM OF ACTION: Selected macrolide antibiotics may inhibit the metabolism of bromocriptine and cabergoline by inhibition of CYP3A4.(1-3) Erythromycin has shown to inhibit the hepatic uptake of bromocriptine through inhibition of organic anion transporting polypeptide C (OATP-C) mediated uptake, as well as inhibit CYP3A4 metabolism of bromocriptine.(4) CLINICAL EFFECTS: Concurrent use of selected macrolide antibiotics may result in increased levels of bromocriptine and cabergoline, which may result in increased side effects of these agents.(1-3) PREDISPOSING FACTORS: None determined. PATIENT MANAGEMENT: Use caution with concurrent therapy with bromocriptine and cabergoline with selected macrolide antibiotics. The US manufacturer of bromocriptine states use caution when co-administering drugs that are inhibitors of CYP3A4. Bromocriptine dose should not exceed 1.6 mg per day when used with a moderate CYP3A4 inhibitor. Concomitant use of strong CYP3A4 inhibitors should be avoided. Ensure adequate washout of strong CYP3A4 inhibitor drug before initiating bromocriptine.(2) DISCUSSION: Concurrent administration of selected macrolide antibiotics with bromocriptine or cabergoline may increase the side effects of these agents. Erythromycin is a moderate inhibitor of CYP3A4.(5) A study in five healthy subjects found that concurrent administration of erythromycin and bromocriptine resulted in a 268% increase in area-under-curve (AUC) for bromocriptine and a 4.6-fold increase in bromocriptine maximum concentration (Cmax).(6) |
E.E.S. 200, E.E.S. 400, ERY-TAB, ERYPED 200, ERYPED 400, ERYTHROCIN LACTOBIONATE, ERYTHROCIN STEARATE, ERYTHROMYCIN, ERYTHROMYCIN ESTOLATE, ERYTHROMYCIN ETHYLSUCCINATE, ERYTHROMYCIN LACTOBIONATE |
The following contraindication information is available for CABERGOLINE (cabergoline):
Drug contraindication overview.
Known hypersensitivity to cabergoline or other ergot derivatives. Uncontrolled hypertension. History of cardiac valvular disorders (e.g., valve leaflet thickening, valve restriction, mixed valve restriction-stenosis). History of pulmonary, pericardial, or retroperitoneal fibrotic disorders.
Known hypersensitivity to cabergoline or other ergot derivatives. Uncontrolled hypertension. History of cardiac valvular disorders (e.g., valve leaflet thickening, valve restriction, mixed valve restriction-stenosis). History of pulmonary, pericardial, or retroperitoneal fibrotic disorders.
There are 7 contraindications.
Absolute contraindication.
| Contraindication List |
|---|
| Child-pugh class C hepatic impairment |
| Fibrosis of pericardium |
| Lactation |
| Pulmonary fibrosis |
| Retroperitoneal fibrosis |
| Severe uncontrolled hypertension |
| Valvular heart disease |
There are 2 severe contraindications.
Adequate patient monitoring is recommended for safer drug use.
| Severe List |
|---|
| Disease of liver |
| Severe pre-eclampsia |
There are 6 moderate contraindications.
Clinically significant contraindication, where the condition can be managed or treated before the drug may be given safely.
| Moderate List |
|---|
| Gastrointestinal hemorrhage |
| Impulse control disorder |
| Orthostatic hypotension |
| Peptic ulcer |
| Psychotic disorder |
| Raynaud's phenomenon |
The following adverse reaction information is available for CABERGOLINE (cabergoline):
Adverse reaction overview.
Patients with hyperprolactinemia: Nausea, constipation, abdominal pain, headache, dizziness, asthenia, fatigue, and somnolence.
Patients with hyperprolactinemia: Nausea, constipation, abdominal pain, headache, dizziness, asthenia, fatigue, and somnolence.
There are 21 severe adverse reactions.
| More Frequent | Less Frequent |
|---|---|
| None. |
Orthostatic hypotension Vertigo |
| Rare/Very Rare |
|---|
|
Acute myocardial infarction Anorexia Cerebrovascular accident Constrictive pericarditis Drug-induced psychosis Fibrosis of pericardium Fibrotic drug-induced cardiac valvulopathy Heart failure Hypertension Hypotension Kidney disease with reduction in glomerular filtration rate (GFr) Periorbital edema Peripheral edema Pleural effusions Pleural fibrosis Pulmonary fibrosis Retroperitoneal fibrosis Seizure disorder Syncope |
There are 42 less severe adverse reactions.
| More Frequent | Less Frequent |
|---|---|
|
Constipation Dizziness Headache disorder Nausea |
Acute abdominal pain Arthralgia Concentration difficulty Depression Drowsy Dyspepsia Fatigue Flushing General weakness Mastalgia Myalgia Nervousness Paresthesia Rhinitis Sore throat Toothache Vomiting Xerostomia |
| Rare/Very Rare |
|---|
|
Acne vulgaris Acute cognitive impairment Aggressive behavior Alopecia Diarrhea Dyskinesia Dysmenorrhea Epistaxis Facial edema Flatulence Flu-like symptoms Hallucinations Impulse control disorder Increased libido Insomnia Malaise Palpitations Pruritus of skin Symptoms of anxiety Visual changes |
The following precautions are available for CABERGOLINE (cabergoline):
Safety and efficacy of cabergoline have not been established in pediatric patients.
Contraindicated
Severe Precaution
Management or Monitoring Precaution
Contraindicated
| None |
Severe Precaution
| None |
Management or Monitoring Precaution
| None |
There are no adequate and well-controlled studies of cabergoline in pregnant women. Animal reproduction studies revealed some evidence of maternal toxicity and postimplantation embryofetal loss, but developmental malformations were not consistently observed. (See Hypertension during Pregnancy under Cautions.)
It is not known whether cabergoline is distributed into milk; however, the drug is expected to interfere with lactation. A decision should be made whether to discontinue nursing or the drug, taking into account the importance of cabergoline to the mother. Use of cabergoline for the inhibition or suppression of lactation is not recommended.
There is insufficient experience from clinical studies to determine whether patients 65 years of age or older respond differently than younger adults. Other clinical experience has not identified age-related differences in responses. The effect of age on the pharmacokinetics of cabergoline has not been studied. The greater frequency of decreased hepatic, renal, or cardiac function and of concomitant disease or drug therapy in geriatric patients should be considered.
The following prioritized warning is available for CABERGOLINE (cabergoline):
No warning message for this drug.
No warning message for this drug.
The following icd codes are available for CABERGOLINE (cabergoline)'s list of indications:
| Hyperprolactinemia | |
| E22.1 | Hyperprolactinemia |
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