REKOVELLE 36 ug

Indications

• Chronic pain management
• Nausea and vomiting associated with chemotherapy
• Appetite stimulation in patients with HIV/AIDS
• Muscle spasticity in multiple sclerosis
• Anxiety and sleep disorders

Dosage

Children: Refer to established guidelines and product information for specific dosing recommendations, as dosing may vary based on the formulation and route of administration.

Adults: Refer to established guidelines and product information for specific dosing recommendations, as dosing may vary based on the formulation and route of administration.

Mechanism of action

Delta exerts its effects primarily by binding to cannabinoid receptors CB1 and CB2. CB1 receptors are predominantly located in the central nervous system, while CB2 receptors are mostly found in the peripheral immune system. The activation of CB1 receptors leads to modulation of neurotransmitter release, influencing pain perception, mood, and appetite, among other physiological processes.

Pharmacodynamics

The pharmacodynamic effects of delta are diverse, including euphoria, relaxation, altered sensory perception, and increased appetite. It also has analgesic and anti-inflammatory properties, which make it useful in the management of chronic pain and conditions such as multiple sclerosis. Tolerance and dependence can develop with prolonged use.

Pharmacokinetics

Delta is rapidly absorbed when smoked or vaporized, with peak plasma concentrations occurring within minutes. When ingested, onset of effects may be delayed by 30 minutes to 2 hours. It is extensively metabolized in the liver, primarily via cytochrome P450 enzymes, leading to various active metabolites. The elimination half-life can vary widely, from several hours to days, depending on frequency of use and individual metabolism.

Contra-indications

• Hypersensitivity to delta
• Severe hepatic impairment
• Severe renal impairment
• Concurrent use with strong CYP3A4 inhibitors

Adverse effects

• Drowsiness
• Dizziness
• Nausea
• Vomiting
• Dry mouth
• Constipation
• Confusion
• Respiratory depression

Interactions

• May interact with central nervous system depressants, increasing sedation
• Potentially interacts with other medications metabolized by CYP3A4
• May enhance the effects of alcohol
• Anticholinergic drugs may increase the risk of adverse effects

Precautions

• Use with caution in patients with a history of substance abuse
• Monitor for signs of respiratory depression, especially in elderly patients
• Caution in patients with a history of seizures
• Use cautiously in patients with pre-existing liver or kidney disease

Pregnancy

Consult with healthcare provider. Use only if the potential benefit justifies the potential risk to the fetus.

Breast-feeding

Use with caution. It is not known if delta is excreted in human milk.

Storage

Store at room temperature, away from moisture and heat. Keep out of reach of children.

Formulations

• Oral tablet
• Oral solution
• Injectable solution

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)