Parlodel

Parlodel

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Product dosage: 1.25mg
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Product dosage: 2.5mg
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Synonyms

Parlodel: Effective Dopamine Agonist Therapy for Hyperprolactinemia

Parlodel (bromocriptine mesylate) is a dopamine receptor agonist medication specifically formulated to address hyperprolactinemic disorders. This first-generation ergot derivative demonstrates significant efficacy in normalizing prolactin levels, restoring gonadal function, and managing symptoms associated with elevated prolactin. Its well-established pharmacokinetic profile and decades of clinical use make it a cornerstone therapy in endocrine management, particularly for patients requiring long-term dopaminergic suppression.

Features

  • Contains bromocriptine mesylate as active pharmaceutical ingredient
  • Available in 2.5mg scored tablets and 5mg capsules
  • Rapid absorption with peak plasma concentrations within 1-3 hours
  • Extensive hepatic metabolism via cytochrome P450 system (primarily CYP3A4)
  • Elimination half-life of approximately 12-15 hours
  • High protein binding capacity (>90%)
  • Ergot alkaloid derivative with selective D2 dopamine receptor agonism

Benefits

  • Effectively suppresses pathological prolactin secretion within therapeutic doses
  • Restores ovulation and fertility in women with hyperprolactinemic amenorrhea
  • Reduces galactorrhea in both male and female patients
  • Normalizes testosterone levels in hypogonadal men with hyperprolactinemia
  • Provides symptomatic relief from headaches associated with prolactinomas
  • May reduce tumor size in patients with prolactin-secreting pituitary adenomas

Common use

Parlodel is primarily indicated for the treatment of hyperprolactinemia-associated conditions, including amenorrhea, galactorrhea, infertility, and hypogonadism. It is also prescribed for prolactin-secreting adenomas, both microadenomas and macroadenomas. Off-label uses include management of acromegaly (as adjunctive therapy), neuroleptic malignant syndrome, and Parkinson’s disease, though its use in movement disorders has largely been supplanted by newer dopamine agonists with improved side effect profiles.

Dosage and direction

Initial dosage typically begins with 1.25-2.5mg once daily, preferably with food to minimize gastrointestinal adverse effects. Dosage should be titrated gradually, increasing by 1.25-2.5mg every 3-7 days based on prolactin level response and tolerance. Maintenance doses generally range from 2.5mg to 15mg daily, divided into two or three administrations. For large prolactinomas, higher doses up to 30mg daily may be required. Patients should be advised to take Parlodel at the same time(s) each day to maintain stable plasma concentrations. Therapy duration is typically long-term, with regular monitoring of prolactin levels and potential dose adjustments based on biochemical response.

Precautions

Patients should be monitored for development of fibrotic reactions, including pleural effusion, pleural fibrosis, and retroperitoneal fibrosis. Regular assessment of erythrocyte sedimentation rate and chest radiography should be considered during long-term therapy. Caution is advised in patients with hepatic impairment due to extensive hepatic metabolism. Cardiovascular evaluation is recommended prior to initiation in patients with history of myocardial infarction or coronary artery disease. Patients should be warned about the potential for hypotension, particularly during the initial dose titration phase. Psychiatric monitoring is advised, especially in patients with history of psychotic disorders.

Contraindications

Parlodel is contraindicated in patients with hypersensitivity to ergot alkaloids or any component of the formulation. It should not be used in patients with uncontrolled hypertension, toxemia of pregnancy, or coronary artery disease. Contraindicated in patients with a history of cardiac valvular disorders due to increased risk of fibrotic reactions. Not recommended for use in patients with severe hepatic impairment. Avoid concomitant use with other dopamine antagonists, as they may diminish therapeutic effect.

Possible side effect

Common adverse reactions include nausea (40-50%), headache (15-25%), dizziness (15-20%), and fatigue (10-15%). Orthostatic hypotension occurs in approximately 15% of patients, particularly during initial therapy. Less frequent side effects include nasal congestion (8-10%), abdominal cramps (5-8%), and vomiting (5-7%). Serious but rare adverse effects include psychiatric disturbances (hallucinations, confusion), digital vasospasm, and pleural effusion. Approximately 3-5% of patients may experience augmentation of pre-existing psychotic symptoms.

Drug interaction

Parlodel demonstrates significant interactions with CYP3A4 inhibitors such as macrolide antibiotics, azole antifungals, and protease inhibitors, which may increase bromocriptine levels and toxicity. Concomitant use with antihypertensive agents may potentiate hypotensive effects. Dopamine antagonists (phenothiazines, butyrophenones, metoclopramide) may diminish therapeutic efficacy. Ergot alkaloids and other serotonin agonists may increase risk of serotonin syndrome. Caution advised with alcohol consumption due to enhanced hypotensive and sedative effects.

Missed dose

If a dose is missed, patients should take it as soon as remembered unless it is nearly time for the next scheduled dose. In that case, the missed dose should be skipped and the regular dosing schedule resumed. Doubling of doses is not recommended due to increased risk of adverse effects. Patients should contact their healthcare provider if multiple doses are missed, as retitration may be necessary to minimize side effects upon reinitiation.

Overdose

Symptoms of overdose may include severe nausea, vomiting, hypotension, confusion, hallucinations, and syncope. Management involves immediate gastric lavage if ingestion occurred within recent hours and administration of activated charcoal. Cardiovascular monitoring is essential, with supportive measures including IV fluids for hypotension. Dopamine antagonists may be considered for severe neurological symptoms, though this may exacerbate hyperprolactinemia. There is no specific antidote for bromocriptine overdose.

Storage

Store at controlled room temperature (20-25Β°C or 68-77Β°F) in original container. Protect from light and moisture. Keep tightly closed and out of reach of children. Do not use if tablets show signs of discoloration or deterioration. Dispense in original container with child-resistant closure. Do not transfer to other containers, as this may affect stability.

Disclaimer

This information is provided for educational purposes only and does not constitute medical advice. Treatment decisions should be made in consultation with a qualified healthcare professional. Individual response to therapy may vary, and not all side effects are listed here. Patients should report any unusual symptoms to their physician promptly. Parlodel should only be used under appropriate medical supervision with regular monitoring.

Reviews

Clinical studies demonstrate Parlodel’s efficacy in normalizing prolactin levels in 80-90% of patients with microprolactinomas and 60-70% of those with macroprolactinomas. Long-term follow-up studies show maintenance of normoprolactinemia in approximately 70% of patients after 5 years of therapy. Patient satisfaction surveys indicate significant improvement in quality of life measures related to restoration of fertility and reduction of galactorrhea. However, approximately 15-20% of patients discontinue therapy due to side effects, primarily gastrointestinal intolerance.