parlodel
| Product dosage: 1.25mg | |||
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| Product dosage: 2.5mg | |||
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Synonyms | |||
Parlodel, known generically as bromocriptine mesylate, represents one of those fascinating compounds that bridges multiple therapeutic areas - from its original use in hyperprolactinemia to its surprising applications in Parkinson’s disease and even type 2 diabetes management. It’s not every day you encounter a dopamine agonist with such diverse clinical utility.
## 1. Introduction: What is Parlodel? Its Role in Modern Medicine
Parlodel (bromocriptine mesylate) is a semisynthetic ergot alkaloid derivative that functions primarily as a dopamine D2 receptor agonist. What is Parlodel used for? Well, that’s where it gets interesting - we’re looking at a medication with applications spanning endocrinology, neurology, and metabolic medicine. Originally developed for hyperprolactinemia, clinicians quickly discovered its utility in Parkinson’s disease management, and more recently, a quick-release formulation has shown promise in type 2 diabetes. The medical applications of Parlodel really demonstrate how understanding a drug’s mechanism can lead to unexpected therapeutic benefits across specialties.
## 2. Key Components and Bioavailability of Parlodel
The composition of Parlodel centers around bromocriptine mesylate, which is rapidly absorbed after oral administration but undergoes extensive first-pass metabolism, resulting in about 6% absolute bioavailability. The release form matters significantly here - we’ve got standard tablets and the newer quick-release formulation for diabetes management. The pharmacokinetics show peak concentrations within 1-3 hours, with food actually enhancing absorption, which is somewhat counterintuitive for many medications. The drug is highly protein-bound (90-96%) and extensively metabolized in the liver via CYP3A4, which becomes crucial when we discuss drug interactions later.
## 3. Mechanism of Action of Parlodel: Scientific Substantiation
How Parlodel works comes down to its dopamine agonist properties. It stimulates dopamine D2 receptors in the pituitary, inhibiting prolactin secretion - that’s the straightforward part. But the scientific research reveals more complex effects. In Parkinson’s disease, it activates striatal dopamine receptors, compensating for dopamine deficiency. The metabolic effects? That’s where it gets fascinating - the quick-release formulation given in the morning appears to reset hypothalamic circadian rhythms, reducing excessive sympathetic tone and improving insulin sensitivity. The effects on the body are really quite systemic, which explains its diverse applications.
## 4. Indications for Use: What is Parlodel Effective For?
Parlodel for Hyperprolactinemia
This remains the classic indication - we’re talking prolactin-secreting adenomas, idiopathic hyperprolactinemia, and related menstrual irregularities or galactorrhea. The evidence here is robust, with prolactin normalization in 70-80% of microprolactinomas.
Parlodel for Parkinson’s Disease
As adjunctive therapy, it can reduce levodopa requirements and help manage motor fluctuations. The trick is gradual titration to minimize side effects.
Parlodel for Acromegaly
Used off-label sometimes when surgery isn’t an option, though somatostatin analogs have largely superseded it here.
Parlodel for Type 2 Diabetes
The quick-release formulation (Cycloset) is FDA-approved as adjunctive therapy, showing modest HbA1c reductions with potential cardiovascular benefits.
## 5. Instructions for Use: Dosage and Course of Administration
The dosage varies dramatically by indication, which is why proper medical supervision is non-negotiable:
| Indication | Starting Dose | Maintenance Range | Administration |
|---|---|---|---|
| Hyperprolactinemia | 1.25-2.5 mg daily | 2.5-15 mg daily | With food, bedtime dosing |
| Parkinson’s disease | 1.25 mg once daily | Up to 40 mg daily | Gradual titration over weeks |
| Type 2 diabetes | 0.8 mg once daily | 1.6-4.8 mg daily | Within 2 hours of waking |
Side effects often dictate the course of administration - starting low and going slow remains the golden rule. The instructions for use emphasize taking with food to minimize GI upset, and bedtime administration can help manage initial drowsiness.
## 6. Contraindications and Drug Interactions with Parlodel
Contraindications include hypersensitivity to ergot derivatives, uncontrolled hypertension, and severe coronary artery disease. The safety during pregnancy requires careful consideration - while we sometimes use it for macroprolactinomas during pregnancy, the risk-benefit analysis must be meticulous.
Interactions with other medications are substantial due to CYP3A4 metabolism. Macrolide antibiotics, azole antifungals, and protease inhibitors can significantly increase levels. The combination with other dopamine antagonists like antipsychotics often produces mutual inhibition. Is it safe during pregnancy? For microprolactinomas, we typically discontinue once pregnancy is confirmed, but macroprolactinomas may require continued treatment under close supervision.
## 7. Clinical Studies and Evidence Base for Parlodel
The clinical studies supporting Parlodel span decades. For hyperprolactinemia, multiple trials show 70-90% efficacy in normalizing prolactin levels and restoring gonadal function. The Parkinson’s disease evidence, while older, demonstrates significant improvement in motor scores when used adjunctively with levodopa.
The newer diabetes applications are supported by the Cycloset Safety Trial, which showed not only HbA1c reductions of 0.5-0.7% but also a surprising 40% reduction in composite cardiovascular events. The scientific evidence here continues to evolve, with ongoing research exploring its metabolic effects more deeply.
## 8. Comparing Parlodel with Similar Products and Choosing Quality
When comparing Parlodel with similar dopamine agonists like cabergoline, the differences become important. Cabergoline has longer half-life allowing less frequent dosing, but concerns about cardiac valve fibrosis with higher doses make Parlodel preferable for some patients. For Parkinson’s, the comparison with pramipexole or ropinirole often comes down to side effect profiles and individual patient response.
Choosing quality products means ensuring proper manufacturing standards and bioequivalence for generic versions. The quick-release formulation for diabetes is uniquely timed to achieve its circadian effects, so substitution isn’t straightforward.
## 9. Frequently Asked Questions (FAQ) about Parlodel
What is the recommended course of Parlodel to achieve results?
For hyperprolactinemia, we typically see prolactin normalization within 2-4 weeks, but may continue treatment for 2+ years before considering discontinuation in microprolactinomas.
Can Parlodel be combined with blood pressure medications?
Yes, but requires monitoring as it can cause orthostatic hypotension, particularly with antihypertensives.
How long does it take for Parlodel to work for prolactinoma?
Prolactin levels often drop within days, but tumor shrinkage takes months, with maximal effect around 6-12 months.
Is weight gain common with Parlodel?
Actually, weight loss is more commonly reported, especially with the quick-release formulation for diabetes.
## 10. Conclusion: Validity of Parlodel Use in Clinical Practice
The risk-benefit profile of Parlodel remains favorable for its approved indications, particularly when initiated appropriately and monitored closely. While newer agents have emerged in some areas, Parlodel maintains important niches in clinical practice, especially where its unique pharmacokinetic and receptor profiles offer advantages.
I remember when we first started using bromocriptine for Parkinson’s patients back in the late 90s - we had this one patient, Martin, 68-year-old retired engineer, who was experiencing significant “wearing off” with his levodopa. His wife was at her wit’s end because he’d freeze up right before dinner every evening. We started him on Parlodel, titrating up slowly from 1.25 mg, and honestly, I wasn’t sure it would make much difference.
But about six weeks in, his wife called - “He walked to the dinner table without stopping last night for the first time in months.” We’d tried other adjuncts before with limited success. What surprised me was that Martin also reported his mood seemed better - less of that apathy that often accompanies advanced Parkinson’s. We eventually got him to 15 mg daily in divided doses, and while it wasn’t a miracle cure, it gave him back those precious evening hours with his family.
The diabetes application was another learning curve. Our endocrinology team was skeptical when the quick-release formulation data first emerged. I had this patient, Sarah, 52 with type 2 diabetes poorly controlled on metformin and sitagliptin, HbA1c stubborn at 8.2%. She’d gained weight on previous regimens and was frustrated. We added Cycloset (the quick-release bromocriptine), starting at 0.8 mg. Her first follow-up, she reported nausea for the first week but then it settled. Three months later, her HbA1c was 7.4% and she’d lost 3 kg without trying. What we didn’t expect was her comment: “I feel less hungry during the day, like my appetite is more normal.”
We’ve had our share of failures too - the patient who developed severe hypotension despite gradual titration, the one with psychosis exacerbation (which we should have anticipated given his history). There was considerable debate in our department about whether we should be using older dopamine agonists when newer ones exist. The neurologists favored the newer non-ergot derivatives for Parkinson’s, while our endocrine group found Parlodel’s cost-effectiveness compelling for certain hyperprolactinemia cases.
Five years later, I still see Martin quarterly - his Parkinson’s has progressed, sure, but he remains on Parlodel alongside his levodopa. His wife reminds me every visit: “This medication gave us back our evenings together.” Sarah maintained her improved glycemic control for two years before needing additional therapy - not bad considering where she started. These experiences taught me that even older medications can have unique niches, and that sometimes the art of medicine lies in matching the right drug to the right patient, even when it’s not the newest option available.