quinagolide

Action and Spectrum

Actions and Spectrum: 

Action: quinagolide stimulates specific dopamine receptors in the brain, specifically the D2-like dopamine receptors. Dopamine is a neurotransmitter that regulates various physiological processes, including prolactin secretion from the pituitary gland. In cases of hyperprolactinemia, there is an overproduction of prolactin, which can lead to symptoms and complications, such as menstrual irregularities, infertility, and galactorrhea (abnormal breast milk production). 

Spectrum:  

Prolactinomas: These are benign tumors of the pituitary gland that can cause excess prolactin production, leading to various hormonal disturbances. quinagolide can help shrink these tumors and normalize prolactin levels. 

Infertility: Hyperprolactinemia can interfere with ovulation and fertility in women. By reducing prolactin levels, quinagolide can improve fertility and increase the chances of successful conception. 

Drug Interaction

Adverse Reaction

Frequency not defined  

Somnolence 

Psychotic episodes 

Pathological gambling 

Nausea 

Nasal congestion 

Insomnia 

Increased libido 

Hypotension 

Hypersexuality 

Headache 

Flushing 

Fluid retention 

Fatigue 

Faintness 

Dizziness 

Diarrhoea 

Constipation 

Anorexia 

Abdominal pain
 

Black Box Warning

Black Box Warning:  

None

Contraindication / Caution

Contraindication/Caution:  

Hypersensitivity: quinagolide is contraindicated for individuals with a known hypersensitivity or allergic response to quinagolide or any of its constituent elements. 

Uncontrolled Hypertension: The use of quinagolide is contraindicated in patients with uncontrolled high blood pressure (hypertension). It can potentially exacerbate hypertension and lead to serious cardiovascular complications. 

Cardiovascular Disorders: quinagolide is contraindicated in individuals with a history of certain cardiovascular disorders, such as heart valve disorders or fibrotic disorders of the heart, due to the potential risk of worsening these conditions. 

Severe Hepatic Impairment: Patients with severe liver impairment should avoid quinagolide, Since the liver is responsible for metabolizing the drug, any disruption in its function can impact the drug’s elimination from the body. 

Psychiatric Disorders: quinagolide should be used with caution in patients with a history of psychiatric disorders, such as severe depression or psychosis, as the drug’s dopamine-modulating effects could potentially worsen these conditions. 

Concurrent Use of Dopamine Antagonists: quinagolide should not be used concurrently with other medications that are dopamine antagonists, as this can interfere with the therapeutic effects of quinagolide. 

Pregnancy and Breastfeeding: quinagolide is typically not advisable for use during pregnancy or breastfeeding because of possible dangers to the growing baby or the nursing child.  

Pregnancy / Lactation

Pregnancy warnings:     

Pregnancy category: contraindicated in pregnancy 

Lactation: contraindicated in Breastfeeding 

Pregnancy Categories:         

Category A: Studies that were well-controlled and met expectations revealed no risk to the fetus in either the first or second trimester. 

Category B: There were a lack of studies on pregnant women and no evidence of risk to the fetus in animal experiments.   

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    

Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.   

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    

Category N: There is no data available for the drug under this category

Pharmacology

Pharmacology:  

quinagolide is a dopamine agonist medication used primarily for the treatment of hyperprolactinemia. 

Pharmacodynamics:  

quinagolide is a selective D2 dopamine receptor agonist. It binds to and activates dopamine D2 receptors, primarily in the pituitary gland. This activation inhibits the release of prolactin, thereby reducing elevated prolactin levels in conditions such as hyperprolactinemia.   

Pharmacokinetics: 

Absorption 

quinagolide is well-absorbed after oral administration and reaches peak plasma concentrations within a few hours. 

Distribution It has a moderate distribution throughout the body and crosses the blood-brain barrier, allowing it to exert its effects in the central nervous system. 

Metabolism 

quinagolide undergoes extensive hepatic metabolism primarily via the CYP3A4 enzyme system. 

Excretion and Elimination 

The elimination half-life of quinagolide is relatively long, which allows for once-daily dosing. It is excreted primarily through the liver and feces. 

Adminstartion

Administration:  

quinagolide is typically available in tablet form and is taken orally. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: quinagolide 

Why do we use quinagolide?  

Hyperprolactinemia: quinagolide is commonly utilized in the medical field to address hyperprolactinemia, a medical condition distinguished by elevated concentrations of prolactin hormone within the bloodstream. Its mechanism of action involves the activation of dopamine receptors situated in the brain, thereby initiating a suppression of prolactin synthesis and secretion originating from the pituitary gland. Elevated levels of prolactin are linked to an array of complications, including disruptions in menstrual patterns, fertility challenges, and the occurrence of abnormal milk production known as galactorrhea. 

Prolactinoma: quinagolide can help manage the symptoms associated with these tumors and reduce prolactin levels, thereby alleviating symptoms like irregular menstrual cycles, infertility, and galactorrhea. 

Parkinson’s Disease: quinagolide has also been investigated for its potential use in Parkinson’s disease. It functions as a dopamine agonist, activating dopamine receptors within the brain. This activation has the potential to enhance motor symptoms linked to the condition, like tremors, rigidity, and bradykinesia (reduced movement speed). 

Restless Legs Syndrome (RLS): quinagolide has shown promise in the treatment of restless legs syndrome.The exact mechanism of its effectiveness in RLS is not fully understood, but it may be related to its dopamine agonist properties.