Lupaneta Pack (leuprolide acetate/norethindrone acetate)

Lupaneta Pack contains 2 different prescription medicines:

• leuprolide acetate for depot suspension is a medicine injected into your muscle and used to treat pain due to endometriosis.
• norethindrone acetate tablets is a medicine taken by mouth and used to help lower the side effect of bone thinning that is caused by leuprolide acetate for depot suspension.

Lupaneta Pack may cause serious side effects, including:

• bone thinning (decreased bone mineral density)
• harm to your unborn baby
• vision problems. Call your doctor right away if you have sudden loss of vision, double vision, bulging eyes, or migraine headaches.
• depression or worsening depression
• allergic reactions. Get medical help right away if you have any of these symptoms of a serious allergic reaction:
  • swelling of your face, lips, mouth, or tongue
  • trouble breathing
  • wheezing
  • severe itching
  • skin rash, redness, or swelling
  • dizziness or fainting
  • fast heartbeat or pounding in your chest (tachycardia)
  • sweating
• worsening endometriosis symptoms when you start taking Lupaneta Pack
• swelling (fluid retention)

The most common side effects of Lupaneta Pack include:

• hot flashes and sweats
• headaches or migraine headaches
• depression and mood swings
• nausea and vomiting
• problems sleeping
• nervousness or feeling anxious
• pain
• acne
• weakness
• vaginal infection or inflammation
• weight gain
• constipation or diarrhea

Tell your doctor if you have any side effect that bothers you or that does not go away.

These are not all the possible side effects of Lupaneta Pack. For more information, ask your doctor or pharmacist.

Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Dosing Information

Lupaneta Pack is a co-packaging of leuprolide acetate for depot suspension for intramuscular use and norethindrone acetate tablets for oral use. Administer as follows:

• 3.75 mg of leuprolide acetate by intramuscular injection once a month for up to six injections (6 months of therapy); to be administered by a healthcare provider
• 5 mg of norethindrone acetate orally once daily for up to 6 months of therapy

The initial course of treatment with leuprolide acetate for depot suspension 3.75 mg in combination with norethindrone acetate 5 mg daily is not to exceed six months.

If the symptoms of endometriosis recur after the initial course of therapy, consider retreatment with Lupaneta Pack for up to another six months. It is recommended that bone density be assessed before retreatment begins.

Treatment beyond two six-month courses has not been studied and is not recommended due to concerns about adverse impact on bone mineral density.

Different Formulations Of Leuprolide Acetate

Due to the specific release characteristics of the 1-month depot formulation, HCPs should not administer 3 doses of the 3.75 mg 1-month formulation simultaneously to mimic the pharmacological profile of the 11.25 mg 3-month formulation.

Drug-Drug Interactions

Leuprolide Acetate For Depot Suspension

• No pharmacokinetic-based drug-drug interaction studies have been conducted with leuprolide acetate for depot suspension.
• However, drug interactions associated with cytochrome P-450 enzymes or protein binding would not be expected to occur.

Norethindrone Acetate

• No pharmacokinetic drug interaction studies investigating any drug-drug interactions with norethindrone acetate have been conducted.
• Drugs or herbal products that induce or inhibit certain enzymes, including CYP3A4, may decrease or increase the serum concentrations of norethindrone.

Drug/Laboratory Test Interactions

Leuprolide Acetate For Depot Suspension

• Administration of leuprolide acetate for depot suspension in therapeutic doses results in suppression of the pituitary-gonadal system.
• Normal function is usually restored within three months after treatment is discontinued.
• Therefore, diagnostic tests of pituitary gonadotropic and gonadal functions conducted during treatment and for up to three months after discontinuation of leuprolide acetate for depot suspension may be affected.

• Lupaneta Pack is contraindicated in women who are or may become pregnant while receiving the drug.
• Before starting and during treatment with leuprolide acetate for depot suspension, establish whether the patient is pregnant.
• Leuprolide acetate for depot suspension is not a contraceptive. In reproductively capable women, a non-hormonal method of contraception should be used.
• Do not use Lupaneta Pack in nursing mothers because the effects of leuprolide acetate for depot suspension on lactation and/or the breast-fed child have not been determined.
• It is not known whether leuprolide acetate for depot suspension is excreted in human milk.
• Detectable amounts of progestins have been identified in the milk of mothers receiving them.