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Pharmacologic Category
Hyperprolactinemia Agent, Dopamine (D2) Agonist
Dosing: Adult
Hyperprolactinemia: Oral:
Initial: 0.025 mg once daily for 3 days followed by 0.05 mg once daily for 3 days (starter pack)
Maintenance (beginning on day 7): 0.075 mg once daily; if needed, a further stepwise titration may occur at intervals of ≥1 week; usual maintenance range: 0.075 to 0.15 mg/day; if higher doses are needed, titrate in increments of 0.075 to 0.15 mg/day at intervals ≥4 weeks up to a maximum of 0.9 mg/day
Dosing: Geriatric
Refer to adult dosing.
Dosing: Renal Impairment: Adult
Use in contraindicated.
Dosing: Hepatic Impairment: Adult
Use in contraindicated.
Use: Labeled Indications
Note: Not approved in the US
Hyperprolactinemia: Treatment of hyperprolactinemia (idiopathic or due to a prolactin-secreting pituitary microadenoma or macroadenoma)
Administration: Oral
Administer once daily with snack at bedtime. Nausea and vomiting may be alleviated by premedicating with a peripheral dopamine antagonist.
Storage/Stability
Store at 15°C to 30°C (59°F to 86°F). Protect from light and humidity.
Medication Safety Issues
Sound-alike/look-alike issues:
Contraindications
Hypersensitivity to quinagolide or any component of the formulation; hepatic or renal impairment
Warnings/Precautions
Concerns related to adverse effects:
• CNS depression: May cause CNS depression (eg, sudden sleep onset and somnolence) particularly in patients with Parkinson disease which may impair physical or mental abilities; patients must be cautioned about performing tasks that require mental alertness (eg, operating machinery, driving). Use with other agents known to induce somnolence or sleep may be expected to potentiate these risks. Dose reduction or therapy discontinuation may be needed if sudden onset of sleep develops.
• Fertility changes: Use caution in women of childbearing age; restoration of fertility may occur; patients not wanting to conceive should implement a reliable method of birth control.
• Gastrointestinal distress: Use may be associated with frequent (but transient) nausea and vomiting early in therapy; during initial therapy, premedication with a peripheral dopamine antagonist may alleviate these effects and improve tolerance.
• Hypotension: Hypotensive episodes along with syncope may occur with the onset of therapy; monitor blood pressure early in therapy.
• Impulse control disorders: Monitor for development of impulse control disorders (eg, pathological gambling, increased libido, hypersexuality, compulsive spending, or binge and compulsive eating). Consider dose reduction or tapered discontinuation if symptoms develop.
Disease-related concerns:
• Psychosis: Use with caution in patients with prior psychotic disorders; the onset of acute psychosis has rarely been observed with use of quinagolide (reversible upon discontinuation).
Concurrent drug therapy issues:
• Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.
Other warnings/precautions:
• Radiotherapy/Surgery: Treatment with quinagolide may not exclude the need for radiation and/or surgical intervention if appropriate.
Pregnancy Considerations
Discontinue use with confirmed pregnancy unless medically necessary to continue. No increase in the incidence of abortion has been seen upon discontinuation of the drug during pregnancy. The reinstitution of therapy may be necessary in patients who display symptoms of tumor enlargement (headaches, visual field changes).
Fertility may be restored with treatment; contraception should be used by females of reproductive potential who do not wish to conceive.
Breast-Feeding Considerations
By inhibiting prolactin secretion, quinagolide suppresses lactation.
Adverse Reactions
>10%:
Central nervous system: Dizziness, fatigue, headache
Gastrointestinal: Nausea, vomiting
1% to 10%:
Cardiovascular: Edema (2%), flushing (1%), hypotension (1%), palpitations (1%), syncope (1%)
Central nervous system: Sedation (3%), insomnia (2%), emotional lability (1%), lack of concentration (1%), malaise (1%)
Gastrointestinal: Constipation (3%), abdominal pain (≤3%), abdominal distress (≤3%), anorexia (2%), dyspepsia (2%), diarrhea (1%)
Endocrine & metabolic: Weight gain (1%)
Genitourinary: Mastalgia (1%)
Neuromuscular & skeletal: Weakness (3%), limb pain (1%)
Respiratory: Nasal congestion (2%)
<1%, postmarketing, and/or case reports: Acute psychosis, decreased hematocrit, decreased hemoglobin, drowsiness, increased creatine phosphokinase, increased serum bilirubin, increased serum potassium, increased serum transaminases, increased serum triglycerides, neutropenia
Metabolism/Transport Effects
None known.
Drug Interactions Open Interactions
Alcohol (Ethyl): May enhance the adverse/toxic effect of Quinagolide. Risk C: Monitor therapy
Amisulpride: May diminish the therapeutic effect of Quinagolide. Quinagolide may diminish the therapeutic effect of Amisulpride. Risk X: Avoid combination
Antipsychotic Agents: May diminish the therapeutic effect of Quinagolide. Risk C: Monitor therapy
Blood Pressure Lowering Agents: Quinagolide may enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Bromopride: May diminish the therapeutic effect of Quinagolide. Risk C: Monitor therapy
Metoclopramide: May diminish the therapeutic effect of Quinagolide. Risk C: Monitor therapy
Pipamperone [INT]: May diminish the therapeutic effect of Quinagolide. Quinagolide may diminish the therapeutic effect of Pipamperone [INT]. Risk X: Avoid combination
Sulpiride: Quinagolide may diminish the therapeutic effect of Sulpiride. Sulpiride may diminish the therapeutic effect of Quinagolide. Risk X: Avoid combination
Monitoring Parameters
Prolactin levels; blood pressure; sedation, mental changes
Product Availability
Not available in the US
Dosage Forms: Canada
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet, Oral:
Norprolac: 0.025 mg, 0.05 mg, 0.075 mg, 0.15 mg
Anatomic Therapeutic Chemical (ATC) Classification
- G02CB04
Generic Available (US)
Yes
Mechanism of Action
Selective dopamine D2 receptor agonist that exerts a direct inhibitory effect on cells (lactotrophs) in the anterior pituitary gland which synthesize and secrete prolactin; not an ergot alkaloid
Pharmacodynamics/Kinetics
Onset of action: 2 hours; maximum effect: 4 to 6 hours
Duration: >24 hours
Absorption: Rapid
Distribution: Vd: 100 L
Protein binding: ~90%
Metabolism: Hepatic; via conjugation (glucuronide and sulfate)
Bioavailability: 4%
Half-life elimination: 11.5 hours; steady state: 17 hours
Time to peak, serum: 30 to 60 minutes
Excretion: Urine (50%); feces (40%); >95% as metabolites
Local Anesthetic/Vasoconstrictor Precautions
No information available to require special precautions
Effects on Dental Treatment
No significant effects or complications reported
Effects on Bleeding
No information available to require special precautions
Index Terms
Quinagolide Hydrochloride
References
Barlier A and Jacquet P, “Quinagolide − A Valuable Treatment Option for Hyperprolactinaemia,” Eur J Endocrinol, 2006, 154(2):187-95.[PubMed 16452531]
Bronstein M, “Prolactinomas and Pregnancy”, Pituitary, 2005, 8(1):31-8.[PubMed 16411066]
DiSarno A, Landi ML, Marzullo P, et al, “The Effect of Quinagolide and Cabergoline, Two Selective Dopamine Receptor Type 2 Agonists, in the Treatment of Prolactinomas,” Clin Endocrinol (Oxf), 2000, 53(1):53-60.[PubMed 10931080]
Norprolac (quinagolide) [product monograph]. Toronto, Ontario, Canada: Ferring, Inc; October 2013.
Schultz PN, Ginsberg L, McCutcheon IE, et al, “Quinagolide in the Management of Prolactinoma,” Pituitary, 2000, 3(4):239-49.[PubMed 11788012]
Brand Names: International
Norprolac (AE, AT, AU, BE, BG, BH, CH, CR, CY, CZ, DE, DK, DO, EG, ES, FI, FR, GB, GR, GT, HK, HN, HR, HU, IL, JO, KW, LB, LU, MX, NI, NL, NO, PA, PL, PT, QA, RU, SA, SE, SG, SI, SK, SV, TR, UA, ZA)
Last Updated 1/15/20
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