(nelfinavir mesylate)

Prescribing Information
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8 USE IN SPECIFIC POPULATIONS

8 USE IN SPECIFIC POPULATIONS

8.1 Pregnancy

Pregnancy Exposure Registry

There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to VIRACEPT during pregnancy. Healthcare providers are encouraged to register patients by calling the Antiretroviral Pregnancy Registry (APR) at 1-800-258-4263.

Risk Summary

Published reports of hepatic adverse events ranging from elevated liver enzymes to hepatic failure in pregnant patients exposed to nelfinavir have been reported (see Clinical Considerations). Due to VIRACEPT's overall adverse event profile, including hepatic adverse events, and literature reports of decreased exposures in second and third trimesters, consider alternative antiretroviral drugs during pregnancy.

Available data from the APR suggests a statistically significant increase in overall risks of major birth defects with first trimester exposure with nelfinavir (3.9%) when compared with the background rate of 2.7% in one U.S. reference population (the Metropolitan Atlanta Congenital Defects Program [MACDP]), but the risk is similar to the background rate of 4.2% reported in another U.S. reference population (the Texas Birth Defects Registry [TBDR]). No pattern of defects was identified by the APR. The clinical relevance of this statistical finding is uncertain (see Data).

The estimated background risk of major birth defects and miscarriage for the indicated populations is unknown. In the U.S. general population, the estimated background risk of major birth defects and miscarriages in clinically recognized pregnancies is 2 to 4% and 15 to 20% respectively.

In animal reproductive studies, no effects on embryo-fetal development were observed when nelfinavir was administered orally to pregnant rats and rabbits during organogenesis at systemic exposures similar to or less than human exposure (based on AUC) at the maximum recommended human dose (MRHD), respectively (see Data).

Clinical Considerations

Maternal Adverse Reactions

There have been reports of hepatic adverse events ranging from elevated liver enzymes to hepatic failure in pregnant patients receiving nelfinavir as part of combination treatment of HIV-1 infection. Consider alternative antiretroviral drugs during pregnancy. If VIRACEPT is used during pregnancy, clinical monitoring is recommended [see Warnings and Precautions (5.2) and Use in Specific Populations (8.6)].

Data

Human Data

Based on prospective reports to the APR of over 1,200 live births following first trimester and over 2,700 live births following second and third trimester exposure to nelfinavir-containing regimens, there was an increase in overall rates of major birth defects (n=47) with nelfinavir when compared with the background birth defect rate of 2.7% in the U.S. reference population of the MACDP. The prevalence of birth defects in live births was 3.9% (95% CI: 2.9% to 5.1%) with first trimester exposure to nelfinavir-containing regimens and 3.1% (95% CI: 2.5% to 3.9%) with the second/third trimester exposure to nelfinavir-containing regimens. The rate for nelfinavir-containing regimens is greater than the overall rates of defects in the MACDP (2.7%) but less than rates of defects in the TBDR (4.2%). Methodological limitations of the APR include the use of MACDP as the external comparator group. Limitations of using an external comparator include differences in methodology and populations, as well as confounding due to the underlying disease; these limitations preclude an accurate comparison of outcomes. The MACDP population is not disease specific, evaluates women and infants from a limited geographic area, and does not include outcomes for births that occurred at <20 weeks gestation.

Animal Data

Nelfinavir was administered orally to pregnant rats and rabbits during organogenesis, from gestation day 6 to 17 (rats) and 7 to 20 (rabbits). There were no effects on fetal development or maternal toxicity when nelfinavir was administered to pregnant rats at systemic exposures (AUC) similar to human exposure. Administration of nelfinavir to pregnant rabbits resulted in no fetal development effects up to a dose at which a slight decrease in maternal body weight was observed; however, even at the highest dose evaluated, systemic exposure in rabbits was significantly lower than human exposure. Additional studies in rats indicated that exposure to nelfinavir in females from mid-pregnancy through lactation (gestation day 6 to lactation day 20) had no effect on the survival, growth, and development of the offspring. Subsequent reproductive performance of these offspring was also not affected by maternal exposure to nelfinavir.

8.2 Lactation

Risk Summary

The Centers for Disease Control and Prevention recommend that HIV-1 infected patients in the United States not breastfeed their infants to avoid risking potential transmission of HIV-1 infection. Based on limited published data, nelfinavir is present in low levels in human milk, and adverse effects in infants exposed to nelfinavir have been reported. Because of the potential for (1) HIV-1 transmission (in HIV-negative infants), (2) developing viral resistance (in HIV-positive infants), and (3) the potential for serious adverse reactions in breastfed infants similar to those seen in adults, instruct mothers not to breastfeed if they are receiving VIRACEPT.

8.3 Females and Males of Reproductive Potential

Contraception

Use of VIRACEPT may reduce the efficacy of estrogen-based oral contraceptives. Advise patients to use alternative or additional contraceptive measures when oral contraceptives containing ethinyl estradiol or norethindrone and VIRACEPT are coadministered [see Drug Interactions (7.3)].

8.4 Pediatric Use

The safety, tolerability, pharmacokinetic profile and efficacy of VIRACEPT were evaluated in HIV infected pediatric patients from 2 to 13 years of age in multicenter clinical trials, Study 556 and PACTG 337 [see Clinical Pharmacology (12.3) and Clinical Studies (14.3)]. In patients less than 2 years of age, VIRACEPT was found to be safe at the doses studied, but a reliably effective dose could not be established [see Dosage and Administration (2.2), Adverse Reactions (6.2), and Clinical Pharmacology (12.3)]. The pharmacokinetic profile, safety and antiviral activity of VIRACEPT in adolescent patients 13 years and older is supported by data from the adult clinical trials where some trials allowed enrolment of subjects 13 years and older. Thus, the data for adolescents and adults were analyzed collectively [see Adverse Reactions (6.1)].

8.5 Geriatric Use

Clinical studies of VIRACEPT did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects.

8.6 Hepatic Impairment

VIRACEPT should not be used in patients with either moderate or severe hepatic impairment (Child-Pugh B or C, score greater than or equal to 7) [see Warnings and Precautions (5.2) and Clinical Pharmacology (12.3)]. No dose adjustment of VIRACEPT is necessary for patients with mild hepatic impairment (Child-Pugh A, score 5–6).

8.7 Renal Impairment

The safety and efficacy of VIRACEPT have not been established in patients with renal impairment.

Medication Guide
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MEDICATION GUIDE

PATIENT INFORMATION

VIRACEPT (VI-ra-cept)
(nelfinavir mesylate)
Tablets

VIRACEPT (VI-ra-cept)
(nelfinavir mesylate)
Oral Powder

Important: VIRACEPT can interact with other medicines and cause serious side effects. It is important to know the medicines that should not be taken with VIRACEPT. See the section "Do not take VIRACEPT if you:"

What is VIRACEPT?

VIRACEPT is a prescription HIV-1 medicine used with other HIV-1 medicines to treat human immunodeficiency virus (HIV-1) infection. HIV-1 is the virus that causes Acquired Immune Deficiency Syndrome (AIDS).

It is not known if VIRACEPT is safe and effective in children less than 2 years of age.

Do not take VIRACEPT if you:

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are taking any of the following medicines. VIRACEPT may cause serious life-threatening side effects or death when used with these medicines:
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alfuzosin
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amiodarone
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cisapride
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ergot-containing medicines:
▪
dihydroergotamine
▪
ergotamine
▪
methylergonovine
o
lovastatin
o
lurasidone
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midazolam, when taken by mouth for sedation
o
pimozide
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quinidine
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rifampin
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sildenafil (Revatio®), when used for the treatment of pulmonary arterial hypertension (PAH)
o
simvastatin
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St. John's wort (Hypericum perforatum)
o
triazolam

Before taking VIRACEPT, tell your healthcare provider about all of your medical conditions, including if you:

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have liver problems
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have kidney problems
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have phenylketonuria. VIRACEPT Oral Powder contains aspartame.
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have high blood sugar (diabetes)
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have hemophilia
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are pregnant or plan to become pregnant. VIRACEPT may harm your unborn baby.
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Tell your healthcare provider right away if you become pregnant during treatment with VIRACEPT.
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Hormonal forms of birth control, such as injections, vaginal rings or implants, contraceptive patches, and some birth control pills may not work during treatment with VIRACEPT. Talk to your healthcare provider about forms of birth control that may be used during treatment with VIRACEPT.
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Pregnancy Registry. There is a pregnancy registry for women who take VIRACEPT during pregnancy. The purpose of the registry is to collect information about the health of you and your baby. Talk to your healthcare provider about how you can take part in this registry.
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are breastfeeding or plan to breastfeed. Do not breastfeed if you take VIRACEPT.
o
You should not breastfeed if you have HIV-1 because of the risk of passing HIV-1 to your baby.
o
VIRACEPT can pass into your breast milk.
o
Talk to your healthcare provider about the best way to feed your baby.

Tell your healthcare provider about all the medicines you take, including prescription and over-the-counter medicines, vitamins and herbal supplements. Some medicines interact with VIRACEPT. Keep a list of your medicines to show your healthcare provider and pharmacist.

•
You can ask your healthcare provider or pharmacist for a list of medicines that interact with VIRACEPT.
•
Do not start taking a new medicine without telling your healthcare provider. Your healthcare provider can tell you if it is safe to take VIRACEPT with other medicines.
o
Especially tell your healthcare provider if you take medicines that contain didanosine. Take VIRACEPT with food one hour after or more than two hours before you take didanosine.

How should I take VIRACEPT?

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You should stay under a healthcare provider's care during treatment with VIRACEPT.
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Take VIRACEPT every day exactly as prescribed by your healthcare provider.
•
Do not change your dose of VIRACEPT or stop treatment without talking to your healthcare provider first.
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Take VIRACEPT with a meal.
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VIRACEPT is usually taken 2 or 3 times each day. Your healthcare provider will tell you how much VIRACEPT to take and when to take it.
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If your child is taking VIRACEPT, your child's healthcare provider will decide the right dose based on your child's weight.
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VIRACEPT Tablets are film-coated to help make the tablets easier to swallow.
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If you or your child are unable to swallow the tablets:
o
You may dissolve the tablets in a small amount of water. Once the tablets are dissolved, the liquid will be cloudy.
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Mix the cloudy liquid well, and then drink it right away.
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Rinse the glass with water and drink the water to ensure that you take the full dose of VIRACEPT.
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If you miss a dose of VIRACEPT, take it as soon as possible. If you skip a dose, do not double the next dose.
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If you take too much VIRACEPT, call your healthcare provider or go to the nearest hospital emergency room right away.
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Do not run out of VIRACEPT. Get your VIRACEPT refilled from your healthcare provider or pharmacy before you run out.

How should VIRACEPT Oral Powder be prepared?

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Your healthcare provider should tell you how much VIRACEPT Oral Powder to use.
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VIRACEPT Oral Powder comes with a scoop for measuring. Ask your healthcare provider or pharmacist for help measuring the correct amount of VIRACEPT Oral Powder.
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Do not mix VIRACEPT Oral Powder in the container that it comes in. Measure the correct amount of VIRACEPT Oral Powder into a cup.
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You may mix VIRACEPT Oral Powder with a small amount of water, milk, formula, soy formula, soy milk, or liquid dietary supplements.
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You should not mix VIRACEPT Oral Powder with acidic food or juice, such as orange juice, apple juice, or applesauce because the mixture may taste bitter.
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Your child should drink all of the mixture to be sure that the entire dose of VIRACEPT is taken.
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If your child does not take the dose right away, store in the refrigerator until you are ready to use it. Do not store a mixed dose of VIRACEPT Oral Powder for more than 6 hours.

What are the possible side effects of VIRACEPT?

VIRACEPT can cause serious side effects, including:

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Diabetes and high blood sugar (hyperglycemia). Some people who take protease inhibitors including VIRACEPT can get high blood sugar, develop diabetes, or your diabetes can get worse. Some people have had to start taking medicine to treat diabetes or have had to change their diabetes medicine. Tell your healthcare provider if you notice an increase in thirst or urinate often while taking VIRACEPT.
•
Increased bleeding in people with hemophilia. Some people with hemophilia have increased bleeding with protease inhibitors including VIRACEPT.
•
Changes in body fat. These changes can happen in people taking HIV-1 medicines. The changes may include an increased amount of fat in the upper back and neck ("buffalo hump"), breast, and around the middle of your body (trunk). Loss of fat from the legs, arms, and face may also happen. The exact cause and long-term health effects of these conditions are not known.
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Changes in your immune system (Immune Reconstitution Syndrome) can happen when you start taking HIV-1 medicines. Your immune system may get stronger and begin to fight infections that have been hidden in your body for a long time. Call your healthcare provider right away if you start having new symptoms after starting your HIV-1 medicine.

The most common side effects of VIRACEPT in adults and adolescents (13 years of age and older) include:

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diarrhea
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nausea
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rash
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gas

The most common side effects of VIRACEPT in children (2 years of age to less than 13 years of age) include:

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diarrhea
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low white blood cell count (leukopenia and neutropenia)
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rash
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loss of appetite
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stomach-area (abdominal) pain

These are not all the possible side effects of VIRACEPT.

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

How should I store VIRACEPT?

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Store VIRACEPT Tablets and Oral Powder at room temperature, between 59ºF to 86ºF (15ºC to 30ºC).
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Store VIRACEPT in the original container.
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Keep the container closed tightly.

Keep VIRACEPT and all medicines out of the reach of children.

General information about the safe and effective use of VIRACEPT.

Medicines are sometimes prescribed for purposes other than those listed in a Patient Information leaflet. Do not use VIRACEPT for a condition for which it was not prescribed. Do not give VIRACEPT to other people, even if they have the same symptoms that you have. It may harm them. You can ask your pharmacist or healthcare provider for information about VIRACEPT that is written for health professionals.

What are the ingredients in VIRACEPT?

Active ingredient: nelfinavir mesylate

Tablet inactive ingredients: calcium silicate, crospovidone, magnesium stearate, hypromellose, and triacetin. In addition, the 250 mg tablet contains FD&C blue #2 powder and the 625 mg tablet contains colloidal silicon dioxide.

Oral powder inactive ingredients: microcrystalline cellulose, maltodextrin, dibasic potassium phosphate, crospovidone, hypromellose, aspartame, sucrose palmitate, and natural and artificial flavor.

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VIRACEPT is a registered trademark of Agouron Pharmaceuticals, LLC

For more information, call 1-800-438-1985.

Trademarks are the property of their respective owners.

LAB-0346-15.0

This Patient Information has been approved by the U.S. Food and Drug Administration.     Revised: 10/2023

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