Quinagolide (Norprolac) is a centrally acting dopamine D-2 receptor agonist. It is used for the treatment of prolactin-secreting pituitary adenoma.

Quinagolide Uses:

• Hyperprolactinemia:

  • It is used for the treatment of hyperprolactinemia due to prolactin-secreting pituitary adenoma (microadenoma or macroadenoma). It can also be used to treat idiopathic hyperprolactinemia.

Other drugs to treat hyperprolactinemia or prolactinomas include:

• Cabergoline
• Bromocriptine

Quinagolide (Norprolac) dose in Adults

Quinagolide (Norprolac) dose in the treatment of Hyperprolactinemia: 

• Initial: 0.025 mg (25 micrograms) orally once a day for three days followed by 0.05 mg (50 micrograms) once a day for three days (starter pack).

• The maintenance dose (beginning on day 7):

  • 75 micrograms once a day.
  • The dose may be titrated gradually at weekly intervals to the usual maintenance dose of 150 micrograms per day. The usual dosage range is 75 micrograms to 150 micrograms per day.
  • If higher doses are required, the dose may be titrated at intervals of 4 weeks or more to a maximum dose of 0.9 mg (900 micrograms) per day.

Use in Children:

Not indicated.

Quinagolide (Norprolac) Pregnancy Risk Category: N

• Animal reproduction studies have shown adverse outcomes for fetal health, but data on its use in pregnancy are limited.
• The treatment may lead to the restoration of fertility. The treatment should be stopped if pregnancy is confirmed.
• Miscarriages have not been linked to treatment discontinuation. 
• The patient should not be treated if they experience headaches, visual impairments, diplopia, visual field effects, or any other symptoms of tumor enlargment.

Use of Quinagolide during breastfeeding

• Quinagolide reduces lactation because it inhibits prolactin production, which has direct effects on breastmilk production.

Dose in Kidney Disease:

Use is contraindicated.

Dose in Liver disease:

Use is contraindicated.

Common Side Effects of Quinagolide (Norprolac):

• Central Nervous System:

  • Dizziness
  • Fatigue
  • Headache

• Gastrointestinal:

  • Nausea
  • Vomiting

Less Common Side Effects of Quinagolide (Norprolac):

• Cardiovascular:

  • Hypotension
  • Palpitations
  • Syncope
  • Edema
  • Flushing

• Gastrointestinal:

  • Constipation
  • Abdominal Pain
  • Abdominal Distress
  • Anorexia
  • Dyspepsia
  • Diarrhea

• Central Nervous System:

  • Sedation
  • Insomnia
  • Emotional Lability
  • Lack Of Concentration
  • Malaise

• Neuromuscular & Skeletal:

  • Weakness
  • Limb Pain

• Endocrine & Metabolic:

  • Weight Gain

• Genitourinary:

  • Mastalgia

• Respiratory:

  • Nasal Congestion

Contraindication to Quinagolide (Norprolac):

• adverse fetal outcomes have been observed in animal reproduction studies, however, data regarding its use in pregnancy is limited.
• Treatment may result in the restoration of fertility. If pregnancy is confirmed, the treatment should be discontinued unless medically necessary.
• Treatment discontinuation has not been associated with miscarriages. 
• If the patient develops a headache, visual impairment, diplopia, visual field changes, or other signs of tumor enlargement after treatment discontinuation, the treatment should be reinstituted.

Quinagolide use during breastfeeding:

• Quinagolide suppresses lactation as it inhibits the production of prolactin which has direct effects on the production of breastmilk.

Quinagolide (United States: Not available): Drug Interaction

Monitoring parameters:

• Prolactin levels;
• blood pressure;
• mental status changes including drowsiness and sedation.

How to administer Quinagolide?

• It is administered orally with a snack at bedtime.
• Patients may develop nausea or vomiting that may be alleviated by premedication with a peripherally acting dopamine antagonist.

Mechanism of action of Quinagolide (Norprolac):

• It acts as a selective D-2 receptor antagonist and acts on the anterior pituitary lactotrophs. It is not an alkaloid of ergot.

The onset of action:

• It has an onset of action within 2 hours.
• The maximum effect is seen in 4 to 6 hours

Absorption:

• It is rapidly absorbed.

Duration:

• More than 24 hours

Protein binding:

• About 90%

Bioavailability:

• 4%

Metabolism:

• It is metabolized in the liver via conjugation (glucuronide and sulfate)

Half-life elimination:

• 11.5 hours;
• A steady state is achieved within 17 hours

Time to peak serum concentration:

• 30 to 60 minutes

Excretion:

• 50% is excreted in the urine
• 40% is excreted in feces ( more than 95% of the drug is excreted as metabolites)

International Brand Names of Quinagolide:

• Norprolac

Quinagolide Brand Names in Pakistan:

No Brands Available in Pakistan.