Microrelin® 3.75 mg

Description

Microrelin® is a synthetic gonadotropin-releasing hormone (GnRH) agonist with greater potency than the natural hormone. GnRH, released from the hypothalamus, stimulates the anterior pituitary to secrete follicle-stimulating hormone (FSH) and luteinizing hormone (LH).

Microrelin® is a sustained-release formulation that provides continuous release of the drug over 28 days. Natural GnRH secretion is pulsatile, stimulating sex hormone production. Continuous administration of Microrelin® in therapeutic doses initially causes a transient increase in circulating levels of LH, FSH, and sex hormones (testosterone in men or estradiol in women). Prolonged administration then leads to downregulation of pituitary GnRH receptors, resulting in suppression of gonadotropin secretion and a marked reduction (up to 95%) in sex hormone levels.

The active pharmaceutical ingredient (API) is manufactured by Bachem Co. (Switzerland) and Corbion Co. (Netherlands). Microsphere development and quality control testing are performed by Primm Co. (Italy). The final product is produced by Homa Pharmed Co.

Microrelin® is supplied as a sterile lyophilized powder in a 5 mL glass vial containing 3.75 mg of triptorelin (as acetate) incorporated in microspheres with excipients. The kit includes an ampule with 2 mL of solvent for reconstitution into a suspension for intramuscular (IM) injection.

Indications

– Treatment of advanced prostate cancer

– Treatment of pediatric patients with central precocious puberty

– Management of endometriosis (for pain relief and reduction of endometriotic lesions)

– Management of uterine fibroids (including preoperative hematologic improvement in anemic patients when hormonal suppression is required, and reduction of fibroid size)

– Adjuvant treatment in combination with tamoxifen or an aromatase inhibitor in endocrine-responsive early breast cancer in premenopausal women at high risk of recurrence

Administration

Microrelin® should be administered by a trained healthcare provider. It is essential to closely follow the mixing instructions included in the packaging.

Microrelin® should be administered by deep intramuscular injection in the gluteal region at 4-week intervals (28 days). Do not exceed 4-week intervals between injections.

Injection sites should be alternated to avoid irritation.

Side Effects

All medications can cause side effects, although not everybody experiences them. Many patients have no side effects or only minor ones. Contact your doctor if any side effects bother you, persist, or if you experience any other effects.

During the first few weeks of treatment, Microrelin® may cause a transient increase in sex hormone levels (known as a “flare-up”). This can temporarily worsen symptoms (e.g., bone pain or urinary issues in prostate cancer patients, or signs of puberty in children). This effect typically resolves within 1–4 weeks with continued treatment. Maintain the prescribed dosing schedule.

The most common side effects are related to reduced sex hormone levels and include:

– Hot flushes

– Decreased libido

– Erectile dysfunction (in men)

– Fatigue/weakness

– Weight gain

– Hypertension

– Mood changes

Other possible effects include visual disturbances or fever.

Warnings

– Hypersensitivity to triptorelin or any component of the formulation.

– Contraindicated in pregnancy (may cause fetal harm or pregnancy loss).

Consult a healthcare professional for additional warnings and precautions.

Pregnancy and Lactation

Microrelin® is contraindicated during pregnancy, as expected hormonal changes increase the risk of pregnancy loss and may cause fetal harm.

It is unknown whether triptorelin is excreted in human breast milk. Due to the potential for serious adverse reactions in a breastfed infant, a decision must be made whether to discontinue breastfeeding or discontinue the drug, taking into account the importance of the treatment to the mother. This decision should be made in consultation with a physician.

Storage

– Store Microrelin® at room temperature (15–25°C).

– Protect from light and moisture.

– Keep out of the reach of children.