Parlodel (bromocriptine mesylate) represents a cornerstone in the management of hyperprolactinemic disorders, offering targeted dopamine receptor agonism to restore endocrine balance. As a first-generation ergot derivative, it demonstrates high specificity for D2 dopamine receptors, making it particularly effective for suppressing pathological prolactin secretion. This medication has established clinical efficacy across multiple indications, supported by decades of real-world use and extensive research documentation. The following comprehensive overview provides healthcare professionals with essential information for appropriate prescribing and patient management.

Features

• Active ingredient: Bromocriptine mesylate
• Pharmacological class: Dopamine D2 receptor agonist
• Available formulations: 2.5mg tablets and 5mg capsules
• Half-life: Approximately 15 hours
• Metabolism: Hepatic, primarily via CYP3A4
• Excretion: Primarily biliary (85-98%)
• Bioavailability: 28% when taken with food
• Protein binding: 90-96%

Benefits

• Effectively normalizes elevated prolactin levels through targeted dopamine receptor activation
• Restores ovulatory cycles and fertility in women with hyperprolactinemic amenorrhea
• Reduces prolactinoma size in approximately 50-60% of macroprolactinomas
• Alleviates galactorrhea and associated breast discomfort
• Improves testosterone levels and sexual function in male hypogonadism secondary to hyperprolactinemia
• Provides flexible dosing options with both immediate and long-acting formulations available

Common use

Parlodel is primarily indicated for the treatment of hyperprolactinemia-associated conditions, including amenorrhea, galactorrhea, infertility, and hypogonadism. It is also approved for the management of prolactin-secreting adenomas, both microprolactinomas and macroprolactinomas. Additionally, it finds application in acromegaly as adjunctive therapy to somatostatin analogs and in Parkinson’s disease for its dopaminergic effects. Off-label uses include neuroleptic malignant syndrome management and cyclical mastalgia treatment.

Dosage and direction

For hyperprolactinemia: Initiate therapy with 1.25-2.5mg daily, preferably with food to minimize gastrointestinal side effects. Gradually titrate upward by 2.5mg increments at 3-7 day intervals until optimal therapeutic response is achieved. Most patients require 2.5-15mg daily divided into 2-3 doses. Maximum recommended dose is 30mg daily. For prolactinomas, maintenance doses typically range from 2.5-20mg daily. Regular monitoring of prolactin levels is essential during dose titration and maintenance therapy.

Precautions

Cardiovascular evaluation is recommended before initiation, particularly in patients over 60 years old. Monitor blood pressure regularly during initial treatment phase. Use caution in patients with hepatic impairment due to extensive hepatic metabolism. Psychiatric history should be thoroughly assessed as dopamine agonists may exacerbate or precipitate psychotic disorders. Regular ophthalmologic examinations are advised during long-term therapy due to potential fibrotic reactions. Pregnancy should be excluded before treatment initiation in women of childbearing potential.

Contraindications

Hypersensitivity to ergot derivatives or any component of the formulation. Uncontrolled hypertension, coronary artery disease, or other severe cardiovascular conditions. History of psychotic disorders unless benefits outweigh risks. Concurrent use with other dopamine antagonists. Severe hepatic impairment. Pre-eclampsia or pregnancy-induced hypertension. Peripheral vascular disorders including Raynaud’s syndrome.

Possible side effect

Common adverse reactions (>10%): nausea, headache, dizziness, fatigue, vomiting. Less frequent (1-10%): nasal congestion, orthostatic hypotension, abdominal cramps, constipation. Rare but serious: cardiac valvulopathy, pleural fibrosis, retroperitoneal fibrosis, psychotic symptoms, impulse control disorders. Dose-dependent side effects typically diminish with continued therapy. Sudden onset sleep attacks have been reported, particularly in Parkinson’s disease patients.

Drug interaction

Strong CYP3A4 inhibitors (ketoconazole, ritonavir) may significantly increase bromocriptine levels. Dopamine antagonists (neuroleptics, metoclopramide) may diminish therapeutic effect. Antihypertensive agents may potentiate hypotensive effects. Ergot alkaloids may increase risk of ergotism. Serotonin agonists may theoretically increase risk of serotonin syndrome. Macrolide antibiotics may elevate bromocriptine concentrations.

Missed dose

If a dose is missed, take it as soon as remembered unless it is nearly time for the next scheduled dose. Do not double the dose to make up for a missed administration. Maintain regular dosing schedule to ensure stable prolactin suppression. Consult healthcare provider if multiple doses are missed, as retitration may be necessary.

Overdose

Symptoms may include severe nausea, vomiting, hypotension, confusion, hallucinations, and syncope. Management involves immediate gastric lavage if ingestion recent, followed by activated charcoal. Supportive care including IV fluids for hypotension and antiemetics for nausea. Dopamine antagonists should be avoided as they may worsen hyperprolactinemia. Hemodialysis is not effective due to high protein binding.

Storage

Store at controlled room temperature (20-25°C/68-77°F) in original container. Protect from light and moisture. Keep tightly closed. Do not store in bathroom or near kitchen sink. Keep out of reach of children and pets. Do not use after expiration date printed on packaging.

Disclaimer

This information is intended for healthcare professionals and should not replace professional medical advice. Treatment decisions must be based on individual patient characteristics and thorough clinical assessment. Prescribers should consult full prescribing information before initiating therapy. Patients should be thoroughly educated about potential benefits and risks before treatment initiation.

Reviews

Clinical studies demonstrate 70-90% normalization of prolactin levels in microprolactinomas with Parlodel therapy. Macroprolactinomas show 50-60% reduction in tumor size with long-term treatment. Patient satisfaction surveys indicate significant improvement in quality of life measures, particularly regarding restoration of fertility and resolution of galactorrhea. Long-term safety data support generally favorable risk-benefit profile when used appropriately under medical supervision.