Description

Cabergoline Teva 1 mg Tablets

Composition

• Active ingredient: Cabergoline 1 mg per tablet.
• Excipients: lactose, leucine, magnesium stearate, plus standard non‑active fillers.

Description

Cabergoline Teva is a long‑acting dopamine D₂ receptor agonist belonging to the ergot alkaloid class. Available as scored white tablets (1 mg strength), typically supplied in blister packs of 2, 8, 30, or 90 tablets. Designed for once‑ or twice‑weekly dosing due to its prolonged half‑life (~63‑69 hours), it is indicated primarily for treating hyperprolactinemia, prolactinomas, and related hormonal disorders.

Pharmacological Properties

Cabergoline exerts its therapeutic effect by high‑affinity partial agonism at dopamine D₂ receptors in the pituitary lactotrophs, suppressing prolactin secretion. It also exhibits activity at D₃, 5‑HT₁A, and 5‑HT₂ receptors, and α₂‑adrenergic receptors, but clinical effects are mediated mainly via D₂ agonism. Minimal central sedative action makes it preferable over older dopamine agonists.

Indications

• Hyperprolactinemia (idiopathic or due to pituitary adenomas/prolactinomas)
• Galactorrhea and menstrual irregularities caused by excess prolactin
• Infertility linked to prolactin excess, especially in PCOS or prolactinoma
• Off‑label use: adjunct in reducing risk of ovarian hyperstimulation syndrome during IVF

Dosage and Administration

• Initial adult dose: 0.5 mg once or twice weekly.
• Titration: increase by 0.5 mg increments every 4 weeks as needed to achieve normoprolactinemia (max ~1 mg/week in most patients).
• Maintenance: often ≤1 mg/week in divided doses.
• Monitor prolactin levels periodically; consider MRI for tumor size evaluation.

Side Effects

• Mild and transient: nausea, headache, dizziness, abdominal discomfort.
• Less common: hypotension, peripheral edema, depression, fatigue.
• Rare but serious (at high/duration doses): valvular fibrosis, pulmonary/peritoneal fibrosis, arrhythmias.

Side effects are dose-dependent and often attenuate with gradual titration. Rains & Molitch, 1995 reported rapid prolactin suppression with few discontinuations (<4 %).

Contraindications

• Allergy to ergoline-derived agents
• Uncontrolled hypertension or known valvular heart disease
• History of pulmonary, pleural, or retroperitoneal fibrosis
• Severe hepatic impairment

Precautions

• Baseline echocardiography recommended before long-term therapy to rule out valvulopathy.
• Slow dose escalation reduces early adverse effects.
• Discontinue temporarily prior to pregnancy; use bromocriptine instead if conception is planned.
• Monitor mood changes and impulse-control behaviors, especially with long-term use.

Interactions

• Concomitant ergot alkaloids should be avoided.
• Metabolism is minimally CYP450‑dependent, but caution advised when co-administered with CYP3A4 inhibitors (e.g., ketoconazole, erythromycin).
• Antipsychotics and metoclopramide may antagonize effects.
• Antihypertensives may exacerbate hypotension risk.

Overdose

Overdose may manifest as severe hypotension, nausea, syncope, hallucinations, or arrhythmia. Management includes immediate discontinuation, symptomatic support, fluid resuscitation, and monitoring.

Storage

• Store tablets at room temperature (15–25 °C).
• Protect from moisture, light, and heat.
• Keep out of reach of children.

Mechanism of Action

Cabergoline acts as a potent agonist at dopamine D₂ receptors, inhibiting adenylate cyclase and reducing intracellular cAMP in lactotrophs, thereby suppressing prolactin gene transcription and secretion. Its long half-life supports intermittent dosing schedules.

Clinical Studies and Evidence

A landmark retrospective review of 455 hyperprolactinemic patients showed normalization of prolactin in ~84% of bromocriptine-intolerant and ~70% of resistant cases using cabergoline (median 1.0 mg/week) with only ~3.9% discontinuation due to side effects. Verhelst et al., 1999

In a prospective study, high-dose cabergoline normalized prolactin and hypogonadism in nearly all subjects with macroadenomas, demonstrating efficacy regardless of baseline tumor size. Ono et al., 2008

Use in Special Populations

In reproductive-aged women, cabergoline supports restoration of ovulation and improves fertility outcomes. Systematic reviews confirm its tolerability and superior dosing convenience vs bromocriptine.

For athletes and physically active professionals, cabergoline does not exhibit performance‐enhancing properties and is allowed under WADA; however, due to hypotensive effects, caution is advised prior to competition.

Comparison with Other Therapies

Compared to bromocriptine, cabergoline offers higher efficacy, less frequent dosing, and fewer gastrointestinal side effects. Quinagolide is an alternative D₂ agonist but lacks long-term safety data outside Europe. Cabergoline remains the first-line agent in international endocrine guidelines.

Summary

Cabergoline Teva 1 mg is a high-affinity dopamine agonist indicated for hyperprolactinemia and related hormonal disorders. It is highly effective, tolerable, and convenient for long-term use. Use requires baseline and follow-up echocardiography, gradual titration, and monitoring of prolactin levels. The risk of valvulopathy is minimal at doses used for endocrine indications. Therapeutic use should be supervised by an endocrinologist.