Apulset
Generic Name
Leuprolide Acetate
Manufacturer
Hypothetical Pharma Co.
Country
Bangladesh
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Price Details
Current market pricing information
| Variant | Unit Price | Strip Price |
|---|---|---|
| apulset 8 mg injection | ৳ 30.00 | N/A |
Description
Overview of the medicine
Apulset 8 mg Injection is a synthetic analogue of gonadotropin-releasing hormone (GnRH). It acts as a potent inhibitor of gonadotropin secretion when administered continuously, leading to a decrease in sex hormone levels. This depot formulation is designed for sustained release over several months.
Uses & Indications
Dosage
Adults
The usual dosage for prostate cancer, endometriosis, or uterine fibroids with an 8 mg depot injection is once every 3-6 months, depending on the specific formulation and indication. Physician discretion is paramount.
Elderly
No specific dose adjustment is generally required for elderly patients with normal renal and hepatic function.
Renal_impairment
No dose adjustment is typically required in patients with renal impairment.
How to Take
Apulset 8 mg injection is for intramuscular (IM) or subcutaneous (SC) administration. It should be administered by a healthcare professional. The powder should be reconstituted with the supplied diluent immediately before use, and the suspension should be injected slowly.
Mechanism of Action
Leuprolide initially stimulates pituitary GnRH receptors, leading to an increase in gonadotropin (LH and FSH) release. However, continuous administration desensitizes these receptors, leading to a down-regulation of GnRH receptors and a subsequent profound decrease in gonadotropin secretion and ovarian/testicular steroidogenesis. This results in a 'medical castration' effect.
Pharmacokinetics
Onset
Initial transient increase in hormone levels (flare-up) within the first week, followed by therapeutic suppression within 2-4 weeks.
Excretion
Excreted primarily by the kidneys.
Half life
Plasma half-life of leuprolide is approximately 3 hours, but the depot formulation provides sustained release for several months.
Absorption
After intramuscular or subcutaneous administration of the depot formulation, leuprolide is slowly absorbed, providing sustained plasma concentrations over months.
Metabolism
Metabolized by peptidases into inactive metabolites.
Side Effects
Contraindications
- •Hypersensitivity to leuprolide acetate, GnRH, or GnRH agonist analogues
- •Undiagnosed abnormal vaginal bleeding
- •Pregnancy and lactation
Drug Interactions
Androgen deprivation therapies
May exacerbate cardiovascular risks when used with other drugs affecting the cardiovascular system.
Drugs affecting pituitary-gonadal axis
Concurrent use may alter the effectiveness of Apulset. Caution is advised.
Storage
Store at room temperature (20°C to 25°C), away from light and moisture. Do not freeze.
Overdose
There is no clinical experience with overdose of Apulset 8 mg. In case of an overdose, symptomatic and supportive treatment should be given. Due to the depot nature, the effect will be prolonged.
Pregnancy & Lactation
Contraindicated during pregnancy due to the risk of fetal harm and during lactation as it may suppress milk production and harm the infant.
Frequently Asked Questions
Common questions about this medicine
Pack Sizes
Shelf Life
Typically 2-3 years from manufacturing date, when stored properly.
Availability
Hospitals, specialty pharmacies
Approval Status
Approved (e.g., FDA/DGDA)
Patent Status
Generic available
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