FOLISURGE 1200

Indications

• Hypertension
• Benign prostatic hyperplasia
• Urinary retention related to prostate enlargement

Dosage

Children: Refer to the BNF for Children for appropriate dosing guidelines in the paediatric population.

Adults: Refer to the BNF for specific dosing recommendations based on individual clinical scenarios.

Mechanism of action

Alpha acts by selectively blocking alpha-1 adrenergic receptors, which are responsible for mediating vasoconstriction in blood vessels. By inhibiting these receptors, alpha promotes vasodilation, leading to a decrease in peripheral vascular resistance and subsequently lowering blood pressure. Additionally, this action can help alleviate urinary symptoms associated with an enlarged prostate.

Pharmacodynamics

The pharmacodynamics of alpha involve its competitive antagonism at alpha-1 adrenergic receptors, resulting in decreased vasoconstriction and increased blood flow. This mechanism is beneficial in conditions characterized by high blood pressure and urinary retention due to prostatic enlargement. The onset of action typically occurs within hours, with peak effects observed within a few days of consistent dosing.

Pharmacokinetics

Alpha is absorbed well from the gastrointestinal tract, with peak plasma concentrations achieved within 1-3 hours post-administration. The drug undergoes hepatic metabolism, primarily via cytochrome P450 enzymes, resulting in active and inactive metabolites. The elimination half-life varies, but it generally is around 6-12 hours, allowing for once-daily dosing in many cases. Renal excretion is a significant route for its metabolites, necessitating caution in patients with renal impairment.

Interactions

• maois, irreversible + alpha blockers: Severe (increases effects)
• ribociclib + alpha blockers: Severe (increases exposure)
• cobicistat + alpha blockers: Moderate (increases exposure)
• idelalisib + alpha blockers: Moderate (increases exposure)
• dronedarone + alpha blockers: Unknown (increases exposure)
• antifungals, azoles + alpha blockers: Unknown (increases exposure)
• crizotinib + alpha blockers: Unknown (increases exposure)
• imatinib + alpha blockers: Unknown (increases exposure)
• letermovir + alpha blockers: Unknown (increases exposure)
• clarithromycin + alpha blockers: Unknown (increases exposure)

Indications

• Infertility due to hypogonadotropic hypogonadism
• Assisted reproductive technologies, such as in vitro fertilization (IVF)
• Ovarian stimulation in women undergoing fertility treatments
• Male infertility due to insufficient spermatogenesis

Dosage

Children: Refer to the BNF for Children for appropriate dosing guidelines in paediatric populations.

Adults: Refer to specific clinical guidelines and the BNF for dosing recommendations based on individual patient factors and treatment protocols.

Mechanism of action

Follitropin acts by binding to and activating the follicle-stimulating hormone receptor (FSHR) on the surface of ovarian granulosa cells and testicular Sertoli cells. This activation leads to a cascade of intracellular signaling pathways that promote the growth and maturation of ovarian follicles in women and stimulate spermatogenesis in men, thus facilitating fertility.

Pharmacodynamics

Follitropin enhances the ovarian response to gonadotropin stimulation, leading to increased estradiol production and follicular growth. In males, it stimulates Sertoli cells to support spermatogenesis. The pharmacodynamic effects of follitropin are dose-dependent, with higher doses generally resulting in a greater biological response, although individual responses may vary based on receptor sensitivity and other factors.

Pharmacokinetics

Follitropin is administered via subcutaneous injection, with peak plasma concentrations occurring approximately 12 to 24 hours post-injection. The half-life of follitropin is approximately 2 to 4 hours, but its biological effects last longer due to the continuous stimulation of the FSH receptor. It is primarily eliminated through renal pathways, and its pharmacokinetic profile can be influenced by factors such as patient age, body weight, and renal function.

Contra-indications

• Hypersensitivity to follitropin or any of its excipients
• Primary ovarian failure
• Pituitary or hypothalamic tumors
• Ovarian cysts or enlarged ovaries not due to polycystic ovary syndrome
• Pregnancy

Adverse effects

• Ovarian hyperstimulation syndrome (OHSS)
• Headache
• Abdominal pain
• Nausea
• Injection site reactions
• Multiple pregnancies
• Breast tenderness

Interactions

• Other gonadotropins may have additive effects
• Hormonal contraceptives may reduce the efficacy of follitropin
• Corticosteroids may affect ovarian response

Precautions

• Use with caution in patients with a history of thromboembolic events
• Monitor for signs of OHSS
• Assess ovarian response carefully during treatment
• Consider patient’s psychological state when undergoing fertility treatment

Pregnancy

Follitropin is contraindicated in pregnancy due to potential risks to the fetus.

Breast-feeding

Limited data available; caution is advised when administering to breastfeeding women.

Storage

Store in a refrigerator (2-8 degrees Celsius), do not freeze. Protect from light.

Formulations

• Follitropin alfa (recombinant)
• Follitropin beta (recombinant)