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Quinagolide (United States: Not available): Drug information

Quinagolide (United States: Not available): Drug information
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For additional information see "Quinagolide (United States: Not available): Patient drug information"

For abbreviations, symbols, and age group definitions show table
Brand Names: Canada
  • Norprolac [DSC]
Pharmacologic Category
  • Hyperprolactinemia Agent, Dopamine (D2) Agonist
Dosing: Adult
Hyperprolactinemia

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.

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Kidney Impairment: Adult

Use in contraindicated.

Dosing: Hepatic Impairment: Adult

Use in contraindicated.

Dosing: Older Adult

Refer to adult dosing.

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.

>10%:

Gastrointestinal: Nausea, vomiting

Nervous system: Dizziness, fatigue, headache

1% to 10%:

Cardiovascular: Edema (2%), hypotension (1%)

Gastrointestinal: Abdominal distress (3%), abdominal pain (3%), anorexia (2%), constipation (3%), dyspepsia (2%)

Nervous system: Insomnia (2%), malaise (1%), sedated state (3%)

Neuromuscular & skeletal: Asthenia(3%)

Respiratory: Nasal congestion (2%)

Ophthalmic: Eye disease (2%)

<1%:

Cardiovascular: Flushing, palpitations, syncope

Endocrine & metabolic: Weight gain

Gastrointestinal: Diarrhea

Genitourinary: Mastalgia

Nervous system: Acute psychosis, drowsiness, emotional lability, lack of concentration

Neuromuscular & skeletal: Limb pain

Frequency not defined:

Endocrine & metabolic: Increased creatinine phosphokinase in blood specimen, increased serum potassium, increased serum triglycerides

Hematologic & oncologic: Decreased hematocrit, decreased hemoglobin, neutropenia

Hepatic: Increased serum bilirubin, increased serum transaminases

Postmarketing: Nervous system: Withdrawal syndrome (dopamine agonist withdrawal syndrome [DAWS]) (Health Canada 2021)

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.

• 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).

Other warnings/precautions:

• Radiotherapy/Surgery: Treatment with quinagolide may not exclude the need for radiation and/or surgical intervention if appropriate.

Product Availability

Not available in the US

Generic Equivalent Available: US

May be product dependent

Dosage Forms: Canada

Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product

Tablet, Oral:

Norprolac: 0.025 mg [DSC], 0.05 mg [DSC], 0.075 mg [DSC], 0.15 mg [DSC]

Administration: Adult

Oral: Administer once daily with snack at bedtime. Nausea and vomiting may be alleviated by premedicating with a peripheral dopamine antagonist.

Use: Labeled Indications

Note: Not approved in the US

Hyperprolactinemia: Treatment of hyperprolactinemia (idiopathic or due to a prolactin-secreting pituitary microadenoma or macroadenoma)

Medication Safety Issues
Sound-alike/look-alike issues:

Quinagolide may be confused with quinapril

Metabolism/Transport Effects

None known.

Drug Interactions

Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the drug interactions program by clicking on the “Launch drug interactions program” link above.

Alcohol (Ethyl): May enhance the adverse/toxic effect of Quinagolide. Risk C: Monitor therapy

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]: Quinagolide may diminish the therapeutic effect of Pipamperone [INT]. Pipamperone [INT] may diminish the therapeutic effect of Quinagolide. 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

Reproductive Considerations

Quinagolide is approved for the treatment of hyperprolactinemia. Increased prolactin concentrations due to a prolactinoma may cause galactorrhea, amenorrhea, oligomenorrhea, or luteal phase insufficiency (ES [Melmed 2011]; ESE [Luger 2021]). Fertility may be restored with treatment; contraception should be used by patients of reproductive potential who do not wish to conceive.

Treatment with a dopamine agonist is recommended for patients with a prolactinoma who are trying to conceive. However, quinagolide is not preferred if treatment is needed during pregnancy (ES [Melmed 2011]; ESE [Luger 2021]).

Normalizing prolactin concentrations during dopamine agonist treatment for a micro- or macroadenoma also improves fertility by restoring nocturnal penile tumescence, sperm count, and sperm motility (ES [Melmed 2011]).

Pregnancy Considerations

Quinagolide is approved for the treatment of hyperprolactinemia. Information related to the use of quinagolide during pregnancy is limited (ESE [Luger 2021]).

Based on known safety data, if treatment of a prolactinoma during pregnancy is required, a dopamine agonist other than quinagolide may be preferred (ES [Melmed 2011]; ESE [Luger 2021]). Discontinue use with confirmed pregnancy unless medically necessary to continue. The reinstitution of therapy may be necessary in patients who display symptoms of tumor enlargement (headaches, visual field changes).

Serum prolactin concentrations are increased during pregnancy; monitoring prolactin levels may not be reliable for tumor progression (ES [Melmed 2011]; ESE [Luger 2021]).

Breastfeeding Considerations

Quinagolide suppresses lactation.

Monitoring Parameters

Prolactin levels; blood pressure; sedation, mental changes

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

Pharmacokinetics (Adult Data Unless Noted)

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

Brand Names: International
International Brand Names by Country
For country code abbreviations (show table)

  • (AE) United Arab Emirates: Norprolac;
  • (AT) Austria: Norprolac;
  • (BE) Belgium: Norprolac;
  • (BG) Bulgaria: Norprolac;
  • (CH) Switzerland: Norprolac;
  • (CN) China: Norprolac;
  • (CO) Colombia: Norprolac;
  • (CZ) Czech Republic: Norprolac;
  • (DE) Germany: Norprolac;
  • (DO) Dominican Republic: Norprolac;
  • (EC) Ecuador: Norprolac;
  • (EG) Egypt: Norprolac;
  • (ES) Spain: Norprolac;
  • (FI) Finland: Norprolac;
  • (FR) France: Norprolac;
  • (GB) United Kingdom: Norprolac | Quinagolide;
  • (GR) Greece: Norprolac;
  • (HK) Hong Kong: Norprolac;
  • (HU) Hungary: Norprolac;
  • (IL) Israel: Norprolac;
  • (JO) Jordan: Norprolac;
  • (KW) Kuwait: Norprolac;
  • (LB) Lebanon: Norprolac;
  • (LU) Luxembourg: Norprolac;
  • (MA) Morocco: Norprolac;
  • (MX) Mexico: Norprolac;
  • (NL) Netherlands: Norprolac;
  • (NO) Norway: Norprolac;
  • (NZ) New Zealand: Norprolac;
  • (PE) Peru: Norprolac;
  • (PL) Poland: Norprolac;
  • (PT) Portugal: Norprolac;
  • (QA) Qatar: Norprolac | Norprolac Starter Pack;
  • (RU) Russian Federation: Norprolac;
  • (SA) Saudi Arabia: Norprolac;
  • (SE) Sweden: Norprolac;
  • (SI) Slovenia: Norprolac;
  • (SK) Slovakia: Norprolac;
  • (TR) Turkey: Norprolac;
  • (UA) Ukraine: Norprolac;
  • (ZA) South Africa: Norprolac
  1. Barlier A and Jacquet P, “Quinagolide − A Valuable Treatment Option for Hyperprolactinaemia,” Eur J Endocrinol, 2006, 154(2):187-95. [PubMed 16452531]
  2. Bronstein M, “Prolactinomas and Pregnancy”, Pituitary, 2005, 8(1):31-8. [PubMed 16411066]
  3. 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]
  4. Health Canada. Summary safety review - dopamine agonists - assessing the potential risk of dopamine agonist withdrawal syndrome. https://hpr-rps.hres.ca/reg-content/summary-safety-review-detail.php?lang=en&linkID=SSR00269. Updated June 8, 2021. Accessed June 10, 2021.
  5. Luger A, Broersen LHA, Biermasz NR, et al. ESE clinical practice guideline on functioning and nonfunctioning pituitary adenomas in pregnancy. Eur J Endocrinol. 2021;185(3):G1-G33. doi:10.1530/EJE-21-0462 [PubMed 34425558]
  6. Melmed S, Casanueva FF, Hoffman AR, et al; Endocrine Society. Diagnosis and treatment of hyperprolactinemia: an Endocrine Society clinical practice guideline. J Clin Endocrinol Metab. 2011;96(2):273-288. doi:10.1210/jc.2010-1692 [PubMed 21296991]
  7. Norprolac (quinagolide) [product monograph]. Toronto, Ontario, Canada: Ferring, Inc; October 2013.
  8. Schultz PN, Ginsberg L, McCutcheon IE, et al, “Quinagolide in the Management of Prolactinoma,” Pituitary, 2000, 3(4):239-49. [PubMed 11788012]
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