Parlodel

Parlodel (bromocriptine mesylate) represents a sophisticated therapeutic approach in neuroendocrine medicine, offering targeted dopamine receptor agonism with established clinical efficacy. This ergot-derived alkaloid functions as a potent D2-dopamine receptor agonist, providing a mechanism-based solution for hyperprolactinemic disorders and Parkinson’s disease management. With over four decades of clinical application, Parlodel maintains its position as a cornerstone therapy in endocrine and neurological practice, demonstrating consistent pharmacokinetic profiles and predictable therapeutic outcomes across diverse patient populations. Its ability to directly modulate prolactin secretion through pituitary dopamine receptors makes it particularly valuable for addressing both functional and organic hyperprolactinemia.

Features

• Contains bromocriptine mesylate as active pharmaceutical ingredient
• Available in 2.5mg scored tablets and 5mg capsules
• Exhibits selective D2-dopamine receptor agonist activity
• Demonstrates high oral bioavailability with peak plasma concentrations within 1-3 hours
• Shows extensive hepatic metabolism via cytochrome P450 system (primarily CYP3A4)
• Features elimination half-life of approximately 15 hours
• Maintains stable shelf life of 36 months when stored properly

Benefits

• Effectively normalizes elevated prolactin levels through direct pituitary action
• Restores gonadal function and fertility in hyperprolactinemic patients
• Reduces prolactinoma size in approximately 60-70% of microadenomas
• Provides symptomatic relief in Parkinson’s disease through dopaminergic activation
• Offers flexible dosing regimens adaptable to individual patient response
• Demonstrates established safety profile with extensive clinical documentation

Common use

Parlodel is primarily indicated for the treatment of hyperprolactinemia-associated conditions, including amenorrhea, galactorrhea, infertility, and hypogonadism. It serves as first-line therapy for prolactin-secreting adenomas (prolactinomas), effectively reducing tumor size and normalizing hormonal parameters. In neurological practice, it finds application as adjunctive therapy in Parkinson’s disease, particularly in early-stage management. Off-label uses include acromegaly management (though superseded by newer agents) and neuroleptic malignant syndrome treatment. The medication demonstrates particular efficacy in functional hyperprolactinemia where dopamine tone restoration provides rapid symptomatic improvement.

Dosage and direction

Initiate therapy with 1.25-2.5mg once daily, preferably with evening meal to minimize gastrointestinal discomfort. Titrate gradually by 2.5mg increments every 3-7 days based on prolactin level response and tolerability. Maintenance doses typically range from 2.5mg to 15mg daily, divided into 2-3 administrations. For Parkinson’s disease, initiate with 1.25mg twice daily, increasing gradually to therapeutic range of 10-40mg daily. Always administer with food to enhance bioavailability and reduce nausea. Regular monitoring of prolactin levels should guide dosage adjustments, with most patients achieving normalization within 4-8 weeks of appropriate dosing.

Precautions

Exercise caution in patients with cardiovascular disease due to potential hypotensive effects. Monitor hepatic function regularly as impaired metabolism may necessitate dose adjustment. Use cautiously in psychiatric patients as dopamine agonism may exacerbate underlying conditions. Pregnancy requires careful risk-benefit assessment—discontinue once pregnancy confirmed unless treating macroprolactinoma. Elderly patients require slower titration and closer monitoring for orthostatic hypotension. Regular ophthalmologic examinations recommended during long-term therapy due to rare reports of retinal changes. Patients should avoid sudden position changes to minimize orthostatic effects.

Contraindications

Absolute contraindications include hypersensitivity to ergot alkaloids, uncontrolled hypertension, toxemia of pregnancy, and coronary artery disease. Avoid use in patients with peripheral vascular disorders such as Raynaud’s syndrome. Contraindicated in patients with history of psychotic disorders unless compelling clinical indication exists. Not recommended for patients with hepatic impairment (Child-Pugh Class C) due to altered metabolism. Avoid concomitant use with other dopamine antagonists as they may diminish therapeutic efficacy.

Possible side effect

Common adverse effects (≥5%) include nausea (40-50%), headache (15-20%), dizziness (10-15%), and fatigue (8-12%). Gastrointestinal disturbances typically diminish with continued therapy. Less frequent effects include orthostatic hypotension (5-8%), nasal congestion (3-5%), and constipation (2-4%). Rare but serious effects include psychiatric manifestations (hallucinations, confusion), pulmonary fibrosis, and cardiac valvulopathy (particularly with long-term high-dose use). Sudden somnolence has been reported, warranting caution when operating machinery.

Drug interaction

Significant interactions occur with CYP3A4 inhibitors (macrolide antibiotics, azole antifungals, protease inhibitors) which may increase bromocriptine levels. Avoid concomitant use with dopamine antagonists (phenothiazines, butyrophenones, metoclopramide) as they antagonize therapeutic effects. Hypotensive agents may potentiate orthostatic effects. Ergot alkaloids may increase vasoconstrictive potential. Serotonin agonists may theoretically increase risk of serotonin syndrome, though clinical evidence limited. Always review concomitant medications for potential interactions before initiation.

Missed dose

If a dose is missed within 4 hours of scheduled time, administer immediately. If beyond 4 hours, skip the missed dose and resume regular schedule. Do not double subsequent doses to compensate. Maintain consistent timing to ensure stable dopaminergic tone. For patients on multiple daily doses, adjust subsequent doses to maintain total daily amount if feasible. Document missed doses when assessing therapeutic response or side effects.

Overdose

Symptoms may include severe nausea, vomiting, hypotension, hallucinations, and syncope. Management involves immediate gastric lavage if presented early, followed by activated charcoal. Support blood pressure with intravenous fluids and vasopressors if needed. Control nausea with antiemetics that don’t antagonize dopamine receptors. Monitor cardiac function and provide symptomatic treatment. No specific antidote exists—hemodialysis not effective due to high protein binding. Contact poison control center for latest management recommendations.

Storage

Store at controlled room temperature (20-25°C/68-77°F) in original container. Protect from light and moisture. Keep blister strips intact until administration. Do not transfer to alternative containers as humidity protection may be compromised. Discard any tablets showing discoloration or physical degradation. Keep out of reach of children and pets. Do not use beyond expiration date printed on packaging.

Disclaimer

This information provides educational content regarding Parlodel therapy but does not replace professional medical advice. Treatment decisions must be made by qualified healthcare providers considering individual patient circumstances. Full prescribing information should be consulted before initiation. Dosage adjustments and monitoring requirements may vary based on clinical context. Report adverse events to appropriate regulatory authorities.

Reviews

Clinical studies demonstrate prolactin normalization in 80-90% of microprolactinoma patients within 4-12 weeks of therapy. Long-term data shows maintained efficacy with continuous treatment over years. Patient satisfaction surveys indicate improved quality of life measures particularly regarding restoration of fertility and sexual function. Neurological studies show moderate efficacy in Parkinson’s disease, though newer agents often preferred due to side effect profile. Systematic reviews confirm position as first-line therapy for hyperprolactinemia with decades of clinical validation supporting its risk-benefit profile.