Adult Dosing

Endometriosis

• 3.75 mg IM qmonth leuprolide in combination with norethindrone acetate 5 mg PO Daily
• Initial treatment course is limited to 6 months and use is not recommended longer than a total of 12 months due to concerns about adverse impact on bone mineral density.

Note:

• Refer package insert for rconstitution procedure

Pediatric Dosing

• Safety and effectiveness in pediatric patients have not been established

[Outline]

• Adult Dosing
• Pediatric Dosing

• Used for initial management of the painful symptoms of endometriosis and for management of recurrence of symptoms

• Hypersensitivity to any of the ingredients of the product
• Hypersensitivity to gonadotropin-releasing hormone (GnRH), GnRH agonist analogs
• Undiagnosed abnormal uterine bleeding
• Known, suspected or planned pregnancy during the course of therapy
• Lactating women
• Known, suspected or history of breast cancer or other hormone-sensitive cancer
• Current or history of thrombotic or thromboembolic disorder
• Liver tumors or liver disease

• N/A

Renal Dose Adjustment

• Renal impairment: Dose adjustments not defined

Hepatic Dose Adjustment

• Hepatic impairment: Dose adjustments not defined

• Assess bone density prior to initiation.
• Therapy induces a hypoestrogenic state that may lead to loss of bone mineral density (BMD), which may be reduced with the concurrent use of norethindrone acetate. Duration of use of therapy is limited to two six-month courses of treatment
• Exclude pregnancy before starting treatment and discontinue use if pregnancy occurs. Patients should use nonhormonal methods of contraception
• Discontinue treatment in case of sudden loss of vision or onset of proptosis, diplopia or migraine
• Depression may occur or worsen during treatment. Carefully observe patients with a history of clinical depression and discontinue if the depression recurs to a serious degree
• Assess and manage risk factors for cardiovascular disease before initiating treatment
• Increase in symptoms associated with endometriosis may be observed during the initial days of therapy, but these should dissipate with continued therapy

Pregnancy Category:X

Breastfeeding: According to the manufacturer’s data, small amounts of progestins are excreted into the breast milk of nursing mothers

• CNS: Headache, dizziness, paresthesia
• NEURO: Asthenia, vertigo
• PSYCHIATRY: Depression, nervousness, anxiety, insomnia
• GI: Constipation, diarrhea, changes in appetite, dyspepsia, flatulence, nausea, vomiting
• GU: Breast changes/tenderness, vaginitis
• METABOLIC: Edema, weight gain
• DERM: Acne, alopecia
• REPRODUCTIVE: Decreased libido
• MUSC: Leg cramps
• MISC: Hot flashes, sweats
• LOCAL: Injection site reaction

Leuprolide

• GnRH agonist; suppresses ovarian and testicular steroidogenesis by inhibiting gonadotropin release
• Unknown metabolism; CYP450: Unknown; active metabolite: pentapeptide (M-1)
• Renally excreted: <5%
• Half-life: 3 hrs

Norethindrone

• Progestin; induces secretory changes in an estrogen-primed endometrium
• Extensively metabolized in the liver; CYP450: 3A4 substrate
• Excreted in urine and feces
• Half-life: Approximately 9 hrs

US Trade Name(s)

• Lupaneta Pack

US Availability

Lupaneta Pack (leuprolide/norethindrone)

• leuprolide
• INJ: 11.25 mg

• norethindrone
• TABS: 5 mg

Canadian Trade Name(s)

• N/A

Canadian Availability

• N/A

UK Trade Name(s)

• N/A

UK Availability

• N/A

Australian Trade Name(s)

• N/A

Australian Availability

• N/A

[Outline]

Obstetrics/Gynecology

Miscellaneous Gynecologic Agents