Adult: In cases of idiopathic or due to a prolactin-secreting pituitary microadenoma or macroadenoma: Initially, 25 mcg once daily for 3 days, followed by 50 mcg once daily for the next 3 days. From Day 7 onwards, give 75 mcg once daily; may increase the daily dose gradually until achieving an optimal response. Usual maintenance dose: 75-150 mcg daily. May further increase the dose in increments of 75-150 mcg daily at intervals of at least 4 weeks, if higher doses are needed. All doses should be given at bedtime. Dosage is individualised according to prolactin-lowering effect and tolerability.
Renal Impairment
Contraindicated.
Hepatic Impairment
Contraindicated.
Administration
Should be taken with food.
Contraindications
Renal and hepatic impairment.
Special Precautions
Patient with history of psychotic disorders; Parkinson's disease. Avoid abrupt withdrawal. Pregnancy and lactation.
Adverse Reactions
Significant: CNS depression (e.g. sudden sleep onset, somnolence), gastrointestinal distress (e.g. frequent but transient nausea and vomiting); hypotension (along with syncope); impulse control disorders (e.g. pathological gambling, compulsive spending or buying, increased libido, hypersexuality, binge eating and compulsive eating). Rarely, acute psychosis. Gastrointestinal disorders: Abdominal pain, constipation, diarrhoea. General disorders and administration site conditions: Fatigue, asthenia, oedema. Metabolism and nutrition disorders: Anorexia. Nervous system disorders: Headache, dizziness. Psychiatric disorders: Insomnia. Respiratory, thoracic and mediastinal disorders: Nasal congestion. Vascular disorders: Flushing.
Patient Counseling Information
This drug may cause sudden sleep onset or somnolence, if affected, do not drive or operate machinery. Women of childbearing potential who do not wish to conceive must use proven birth control methods during therapy.
Monitoring Parameters
Monitor prolactin levels and blood pressure (both lying and standing position). Assess for mental changes.
Overdosage
Symptoms: Severe nausea, vomiting, headache, dizziness, drowsiness, hypotension, collapse and hallucinations. Management: Symptomatic treatment.
Drug Interactions
Concomitant use with agents having strong dopamine antagonistic properties (e.g. neuroleptic agents) may result in a reduced prolactin-lowering effect. May enhance the hypotensive effect of blood pressure lowering agents.
Food Interaction
Enhanced adverse effects with alcohol.
Action
Description: Mechanism of Action: Quinagolide is a non-ergot, selective dopamine D2 receptor agonist. It exerts a direct and strong inhibitory effect on lactotroph cells located in the anterior pituitary gland, which are responsible for the synthesis and secretion of prolactin. Onset: 2 hours. Duration: >24 hours. Pharmacokinetics: Absorption: Rapidly absorbed from the gastrointestinal tract. Bioavailability: 4%. Time to peak plasma concentration: 30-60 minutes. Distribution: Volume of distribution: 100 L. Plasma protein binding: Approx 90%. Metabolism: Undergoes extensive first-pass metabolism in the liver to form N-desethyl (active metabolite) and N,N-didesethyl analogue. Excretion: Via urine (50%); faeces (40%); >95% as metabolites. Elimination half-life: 11.5 hours.
Chemical Structure
Quinagolide Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 3086401, Quinagolide. https://pubchem.ncbi.nlm.nih.gov/compound/Quinagolide. Accessed June 25, 2024.
Storage
Store below 25°C. Protect from light and humidity.
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