Viracept Information
Viracept (Nelfinavir) Description
Viracept (Nelfinavir) (nelfinavir mesylate) is an inhibitor of the human immunodeficiency virus (HIV) protease. Viracept (Nelfinavir) Tablets are available for oral administration as a light blue, capsule-shaped tablet with a clear film coating in 250 mg strength (as nelfinavir free base) and as a white oval tablet with a clear film coating in 625 mg strength (as nelfinavir free base). Each tablet contains the following common 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. Viracept (Nelfinavir) Oral Powder is available for oral administration in a 50 mg/g strength (as nelfinavir free base) in bottles. The oral powder also contains the following inactive ingredients: microcrystalline cellulose, maltodextrin, dibasic potassium phosphate, crospovidone, hypromellose, aspartame, sucrose palmitate, and natural and artificial flavor. The chemical name for nelfinavir mesylate is [3-[2(2, 3), 3α,4aβ,8aβ]]--(1,1-dimethylethyl)decahydro-2-[2-hydroxy-3-[(3-hydroxy-2-methylbenzoyl)amino]-4-(phenylthio)butyl]-3-isoquinoline carboxamide mono-methanesulfonate (salt) and the molecular weight is 663.90 (567.79 as the free base). Nelfinavir mesylate has the following structural formula:
Nelfinavir mesylate is a white to off-white amorphous powder, slightly soluble in water at pH ≤4 and freely soluble in methanol, ethanol, 2-propanol and propylene glycol.
Viracept (Nelfinavir) Clinical Pharmacology
(also see , , )
CYP3A and CYP2C19 appear to be the predominant enzymes that metabolize nelfinavir in humans. The potential ability of nelfinavir to inhibit the major human cytochrome P450 enzymes (CYP3A, CYP2C19, CYP2D6, CYP2C9, CYP1A2 and CYP2E1) has been investigated . Only CYP3A was inhibited at concentrations in the therapeutic range. Specific drug interaction studies were performed with nelfinavir and a number of drugs. Table 6 summarizes the effects of nelfinavir on the geometric mean AUC, C and C of coadministered drugs. Table 7 shows the effects of coadministered drugs on the geometric mean AUC, C and C of nelfinavir.
For information regarding clinical recommendations see , , .
Viracept (Nelfinavir) Indications And Usage
Viracept (Nelfinavir) in combination with other antiretroviral agents is indicated for the treatment of HIV infection.
Viracept (Nelfinavir) Contraindications
Viracept (Nelfinavir) is contraindicated in patients with clinically significant hypersensitivity to any of its components.
Coadministration of Viracept (Nelfinavir) is contraindicated with drugs that are highly dependent on CYP3A for clearance and for which elevated plasma concentrations are associated with serious and/or life-threatening events. These drugs are listed in Table 9.
Viracept (Nelfinavir) Warnings
ALERT: Find out about medicines that should not be taken with Viracept (Nelfinavir)
(also see )
Nelfinavir is an inhibitor of the CYP3A enzyme. Coadministration of Viracept (Nelfinavir) and drugs primarily metabolized by CYP3A may result in increased plasma concentrations of the other drug that could increase or prolong its therapeutic and adverse effects. Caution should be exercised when inhibitors of CYP3A, including Viracept (Nelfinavir) , are coadministered with drugs that are metabolized by CYP3A and that prolong the QT interval. (See .) Nelfinavir is metabolized by CYP3A and CYP2C19. Coadministration of Viracept (Nelfinavir) and drugs that induce CYP3A or CYP2C19 may decrease nelfinavir plasma concentrations and reduce its therapeutic effect. Coadministration of Viracept (Nelfinavir) and drugs that inhibit CYP3A or CYP2C19 may increase nelfinavir plasma concentrations. (Also see .)
Concomitant use of Viracept (Nelfinavir) with lovastatin or simvastatin is not recommended. Caution should be exercised if HIV protease inhibitors, including Viracept (Nelfinavir) , are used concurrently with other HMG-CoA reductase inhibitors that are also metabolized by the CYP3A pathway (e.g., atorvastatin). (Also see and ). The risk of myopathy including rhabdomyolysis may be increased when protease inhibitors, including Viracept (Nelfinavir) , are used in combination with these drugs.
Particular caution should be used when prescribing sildenafil, or other PDE5 inhibitors, in patients receiving protease inhibitors, including Viracept (Nelfinavir) . Coadministration of these drugs is expected to substantially increase PDE5 inhibitor concentrations and may result in an increase in PDE5 inhibitor-associated adverse events, including hypotension, visual changes, and priapism. (See and , and the complete prescribing information for sildenafil and other PDE5 inhibitors.)
Concomitant use of St. John's wort (hypericum perforatum) or St. John's wort-containing products and Viracept (Nelfinavir) is not recommended. Coadministration of St. John's wort with protease inhibitors, including Viracept (Nelfinavir) , is expected to substantially decrease protease inhibitor concentrations and may result in sub-optimal levels of Viracept (Nelfinavir) and lead to loss of virologic response and possible resistance to Viracept (Nelfinavir) or to the class of protease inhibitors.
Viracept (Nelfinavir) Precautions
A statement to patients and healthcare providers is included on the product's bottle label:. A Patient Package Insert (PPI) for Viracept (Nelfinavir) is available for patient information.
For optimal absorption, patients should be advised to take Viracept (Nelfinavir) with food (see and ).
Patients should be informed that Viracept (Nelfinavir) is not a cure for HIV infection and that they may continue to acquire illnesses associated with advanced HIV infection, including opportunistic infections.
Patients should be told that there is currently no data demonstrating that Viracept (Nelfinavir) therapy can reduce the risk of transmitting HIV to others through sexual contact or blood contamination.
Patients should be told that sustained decreases in plasma HIV RNA have been associated with a reduced risk of progression to AIDS and death. Patients should be advised to take Viracept (Nelfinavir) and other concomitant antiretroviral therapy every day as prescribed. Patients should not alter the dose or discontinue therapy without consulting with their doctor. If a dose of Viracept (Nelfinavir) is missed, patients should take the dose as soon as possible and then return to their normal schedule. However, if a dose is skipped, the patient should not double the next dose.
Patients should be informed that Viracept (Nelfinavir) Tablets are film-coated and that this film-coating is intended to make the tablets easier to swallow.
The most frequent adverse event associated with Viracept (Nelfinavir) is diarrhea, which can usually be controlled with non-prescription drugs, such as loperamide, which slow gastrointestinal motility.
Patients should be informed that redistribution or accumulation of body fat may occur in patients receiving antiretroviral therapy and that the cause and long-term health effects of these conditions are not known at this time.
Viracept (Nelfinavir) may interact with some drugs; therefore, patients should be advised to report to their doctor the use of any other prescription, non-prescription medication or herbal products, particularly St. John's wort.
Patients receiving oral contraceptives should be instructed that alternate or additional contraceptive measures should be used during therapy with Viracept (Nelfinavir) .
Patients receiving sildenafil, or other PDE5 inhibitors, and nelfinavir should be advised that they may be at an increased risk of PDE5 inhibitor-associated adverse events including hypotension, visual changes, and prolonged penile erection, and should promptly report any symptoms to their doctor.
(Also see , , )
Nelfinavir is an inhibitor of CYP3A. Coadministration of Viracept (Nelfinavir) and drugs primarily metabolized by CYP3A (e.g., dihydropyridine calcium channel blockers, HMG-CoA reductase inhibitors, immunosuppressants and PDE5 inhibitors) may result in increased plasma concentrations of the other drug that could increase or prolong both its therapeutic and adverse effects. (See and ). Nelfinavir is metabolized by CYP3A and CYP2C19. Coadministration of Viracept (Nelfinavir) and drugs that induce CYP3A or CYP2C19, such as rifampin, may decrease nelfinavir plasma concentrations and reduce its therapeutic effect. Coadministration of Viracept (Nelfinavir) and drugs that inhibit CYP3A or CYP2C19 may increase nelfinavir plasma concentrations.
Drug interaction studies reveal no clinically significant drug interactions between nelfinavir and didanosine, lamivudine, stavudine, zidovudine, efavirenz, nevirapine, or ketoconazole and no dose adjustments are needed. In the case of didanosine, it is recommended that didanosine be administered on an empty stomach; therefore, nelfinavir should be administered with food one hour after or more than 2 hours before didanosine.
Based on known metabolic profiles, clinically significant drug interactions are not expected between Viracept (Nelfinavir) and dapsone, trimethoprim/sulfamethoxazole, or itraconazole.
Carcinogenicity studies in mice and rats were conducted with nelfinavir at oral doses up to 1000 mg/kg/day. No evidence of a tumorigenic effect was noted in mice at systemic exposures (C) up to 9-fold those measured in humans at the recommended therapeutic dose (750 mg TID or 1250 mg BID). In rats, thyroid follicular cell adenomas and carcinomas were increased in males at 300 mg/kg/day and higher and in females at 1000 mg/kg/day. Systemic exposures (C) at 300 and 1000 mg/kg/day were 1- to 3-fold, respectively, those measured in humans at the recommended therapeutic dose. Repeated administration of nelfinavir to rats produced effects consistent with hepatic microsomal enzyme induction and increased thyroid hormone deposition; these effects predispose rats, but not humans, to thyroid follicular cell neoplasms. Nelfinavir showed no evidence of mutagenic or clastogenic activity in a battery of and genetic toxicology assays. These studies included bacterial mutation assays in and a mouse lymphoma tyrosine kinase assay, a chromosomal aberration assay in human lymphocytes, and an mouse bone marrow micronucleus assay.
Nelfinavir produced no effects on either male or female mating and fertility or embryo survival in rats at systemic exposures comparable to the human therapeutic exposure.
The Centers for Disease Control and Prevention recommends that HIV-infected mothers not breast-feed their infants to avoid risking postnatal transmission of HIV.
mothers should be instructed not to breast-feed if they are receiving Viracept (Nelfinavir)
The safety and effectiveness of Viracept (Nelfinavir) have been established in patients from 2 to 13 years of age. The use of Viracept (Nelfinavir) in these age groups is supported by evidence from adequate and well-controlled studies of Viracept (Nelfinavir) in adults and pharmacokinetic studies and studies supporting activity in pediatric patients. In patients less than 2 years of age, Viracept (Nelfinavir) was found to be safe at the doses studied, but a reliably effective dose could not be established (see , , and ).
The following issues should be considered when initiating Viracept (Nelfinavir) in pediatric patients:
Study 556 was a randomized, double-blind, placebo-controlled trial with Viracept (Nelfinavir) or placebo coadministered with ZDV and ddI in 141 HIV-positive children who had received minimal antiretroviral therapy. The mean age of the children was 3.9 years. Ninety four (67%) children were between 2–12 years, and 47 (33%) were
PACTG 377 was an open-label study that randomized 181 HIV treatment-experienced pediatric patients to receive: d4T+NVP+RTV, d4T+3TC+NFV, or d4T+3TC+NVP+NFV with NFV given on a TID schedule. The median age was 5.9 years and 46% were male. At baseline the median HIV RNA was 4.4 log and median CD4 cell count was 690 cells/mm. Substudy PACTG 725 evaluated d4T+3TC+NFV with NFV given on a BID schedule. The proportion of patients with detectable viral load at baseline achieving HIV RNA
Viracept (Nelfinavir) has been evaluated in 2 studies of young infants. The PENTA 7 study was an open-label study to evaluate the toxicity, tolerability, pharmacokinetics, and activity of NFV+d4T+ddI in 20 HIV-infected infants less than 12 weeks of age. PACTG 353 evaluated the pharmacokinetics and safety of Viracept (Nelfinavir) in infants born to HIV-infected women receiving NFV as part of combination therapy during pregnancy.
Viracept (Nelfinavir) Adverse Reactions
The safety of Viracept (Nelfinavir) was studied in over 5000 patients who received drug either alone or in combination with nucleoside analogues. The majority of adverse events were of mild intensity. The most frequently reported adverse event among patients receiving Viracept (Nelfinavir) was diarrhea, which was generally of mild to moderate intensity.
Drug-related clinical adverse experiences of moderate or severe intensity in ≥ 2% of patients treated with Viracept (Nelfinavir) coadministered with d4T and 3TC (Study 542) for up to 48 weeks or with ZDV plus 3TC (Study 511) for up to 24 weeks are presented in Table 12.
Adverse events occurring in less than 2% of patients receiving Viracept (Nelfinavir) in all phase II/III clinical trials and considered at least possibly related or of unknown relationship to treatment and of at least moderate severity are listed below.
Viracept (Nelfinavir) Overdosage
Human experience of acute overdose with Viracept (Nelfinavir) is limited. There is no specific antidote for overdose with Viracept (Nelfinavir) . If indicated, elimination of unabsorbed drug should be achieved by emesis or gastric lavage. Administration of activated charcoal may also be used to aid removal of unabsorbed drug. Since nelfinavir is highly protein bound, dialysis is unlikely to significantly remove drug from blood.
Viracept (Nelfinavir) Dosage And Administration
In children 2 years of age and older, the recommended oral dose of Viracept (Nelfinavir) Oral Powder or 250 mg tablets is 45 to 55 mg/kg twice daily or 25 to 35 mg/kg three times daily. All doses should be taken . Doses higher than the adult maximum dose of 2500 mg per day have not been studied in children. For children unable to take tablets, Viracept (Nelfinavir) Oral Powder may be administered. The oral powder may be mixed with a small amount of water, milk, formula, soy formula, soy milk, or dietary supplements; once mixed, the entire contents must be consumed in order to obtain the full dose. If the mixture is not consumed immediately, it must be stored under refrigeration, but storage must not exceed 6 hours. Acidic food or juice (e.g., orange juice, apple juice, or apple sauce) are not recommended to be used in combination with Viracept (Nelfinavir) , because the combination may result in a bitter taste. Viracept (Nelfinavir) Oral Powder should not be reconstituted with water in its original container.
The healthcare provider should assess appropriate formulation and dosage for each patient. Crushed 250 mg tablets can be used in lieu of powder. Tables 14 and 15 provide dosing guidelines for Viracept (Nelfinavir) tablets and powder based on age and body weight.
Viracept (Nelfinavir) How Supplied
Viracept (Nelfinavir) (nelfinavir mesylate) 250 mg: Light blue, capsule-shaped tablets with a clear film coating engraved with "Viracept (Nelfinavir) " on one side and "250 mg" on the other.
Bottles of 300, 250 mg tablets………………………………...NDC 63010-010-30
Viracept (Nelfinavir) (nelfinavir mesylate) 625 mg: White oval tablet with a clear film coating engraved with "V" on one side and "625" on the other.
Bottles of 120, 625 mg tablets………………………………...NDC 63010-027-70
Viracept (Nelfinavir) (nelfinavir mesylate) Oral Powder is available as a 50 mg/g off-white powder containing 50 mg (as nelfinavir free base) in each level scoopful (1 gram).
Multiple use bottles of 144 grams of powder with scoop …….NDC 63010-011-90
Viracept (Nelfinavir)
Viracept (Nelfinavir) Viracept (nelfinavir Mesylate) Tablets And Oral Powder
Generic Name: nelfinavir (nel-FIN-na-veer) mesylate
Please read this information carefully before taking Viracept (Nelfinavir) . Also, please read this leaflet each time you renew the prescription, in case anything has changed. This is a summary and not a replacement for a careful discussion with your healthcare provider. You and your healthcare provider should discuss Viracept (Nelfinavir) when you start taking this medication and at regular checkups. You should remain under a healthcare provider's care when taking Viracept (Nelfinavir) and should not change or stop treatment without first talking with your healthcare provider.
Viracept (Nelfinavir) is a type of medicine called an HIV (human immunodeficiency virus) protease (PRO-tee-ase) inhibitor. Viracept (Nelfinavir) is always used in combination with other antiretroviral drugs in the treatment of people with HIV infection. Viracept (Nelfinavir) is for adults and for children 2 years of age and older.
Infection with HIV leads to the destruction of CD4 (T) cells, which are important to the immune system. After a large number of CD4 (T) cells have been destroyed, the infected person develops acquired immune deficiency syndrome (AIDS).
Viracept (Nelfinavir) works by blocking HIV protease (a protein-cutting enzyme), which is required for HIV to multiply. Viracept (Nelfinavir) has been shown to significantly reduce the amount of HIV in the blood. Although Viracept (Nelfinavir) is not a cure for HIV or AIDS, Viracept (Nelfinavir) can help reduce your risk for death and illness associated with HIV. Patients who took Viracept (Nelfinavir) also had significant increases in the number of CD4 (T) cells.
Viracept (Nelfinavir) is not a cure for HIV infection or AIDS. People taking Viracept (Nelfinavir) may still develop opportunistic infections or other conditions associated with HIV infection. Some of these conditions are pneumonia, herpes virus infections, complex (MAC) infections, and Kaposi's sarcoma.
Viracept (Nelfinavir) does not reduce the risk of transmitting HIV to others through sexual contact or blood contamination. Continue to practice safe sex and do not use or share dirty needles.
If you forget to take a dose of Viracept (Nelfinavir) , take it as soon as possible. However, if you skip the dose entirely, do not double the next dose. If you forget a lot of doses, talk to your healthcare provider about how you should continue taking your medicine.
If you suspect that you took more than the prescribed dose of this medicine, contact your local poison control center or emergency room immediately.
Together with your healthcare provider, you need to decide whether Viracept (Nelfinavir) is appropriate for you.
For more information about medicines you should not take with Viracept (Nelfinavir) , please read the section titled "."
Viracept (Nelfinavir) may interact with other drugs, including those you take without a prescription. You must tell your healthcare provider about all medicines you are taking or planning to take before you take Viracept (Nelfinavir) . It is a good idea to keep a complete list of all the medicines that you take, including non-prescription medicines, herbal remedies and supplements and street drugs. Update this list when medicines are added or stopped. Give copies of this list to all of your healthcare providers time you visit or fill a prescription.
Do not take the following medicines when you take Viracept (Nelfinavir) . They may reduce the levels of Viracept (Nelfinavir) in the blood and make it less effective. Talk with your healthcare provider if you are currently taking these medicines because other medicines may have to be given to take their place:
Do not take Viracept (Nelfinavir) with St. John's wort (hypericum perforatum), an herbal product sold as a dietary supplement, or products containing St. John's wort. Talk with your healthcare provider if you are taking or planning to take St. John's wort. Taking St. John's wort may decrease Viracept (Nelfinavir) levels and lead to increased viral load and possible resistance to Viracept (Nelfinavir) .
Do not take Viracept (Nelfinavir) with cholesterol-lowering medicines Mevacor (lovastatin) or Zocor (simvastatin) because of possible serious reactions.
Do not take Viracept (Nelfinavir) with Serevent (salmeterol) because of possible serious reactions.
Talk to your healthcare provider before you start taking any new prescription or non-prescription medicines or herbal supplements with Viracept (Nelfinavir) .
It is possible that your healthcare provider may need to increase or decrease the dose of other medicines when you are also taking Viracept (Nelfinavir) .
There is also an increased risk of drug interactions between Viracept (Nelfinavir) and Lipitor (atorvastatin), Crestor (rosuvastatin), Pravachol (pravastatin) and Lescol (fluvastatin); talk to your healthcare provider before you take any of these cholesterol-reducing medicines with Viracept (Nelfinavir) .
Before you take PDE5 Inhibitors, such as Viagra (sildenafil), Levitra (vardenafil) or Cialis (tadalafil) with Viracept (Nelfinavir) , talk to your healthcare provider about possible drug interactions and side effects. If you take these types of drugs and Viracept (Nelfinavir) together, you may be at increased risk of side effects of these drugs such as low blood pressure, visual changes, and penile erection lasting more than 4 hours. If an erection lasts longer than 4 hours, you should seek immediate medical assistance to avoid permanent damage to your penis. Your healthcare provider can explain these symptoms to you.
Before you take Adcirca™ (tadalafil) with Viracept (Nelfinavir) , talk to your healthcare provider since Viracept (Nelfinavir) may increase the amount of tadalafil in your blood.
Before you take Tracleer (bosentan) with Viracept (Nelfinavir) , talk to your healthcare provider since Viracept (Nelfinavir) may increase the amount of bosentan in your blood.
Before you take colchicine with Viracept (Nelfinavir) , talk to your healthcare provider since Viracept (Nelfinavir) may increase the amount of colchicine in your blood.
Before you take warfarin (Coumadin) with Viracept (Nelfinavir) , talk to your healthcare provider since Viracept (Nelfinavir) may affect the amount of warfarin in your blood.
Discuss all questions about your health with your healthcare provider. If you have questions about Viracept (Nelfinavir) or any other medication you are taking, ask your doctor, nurse, pharmacist, or other healthcare provider. You can also call 800-438-1985 toll free.
Viracept (Nelfinavir) and Agouron are registered trademarks of Agouron Pharmaceuticals, Inc.
Trademarks are the property of their respective owners.
AGOURON PHARMACEUTICALS, INC.La Jolla, CA 92037, USA
LAB-0346-8.0
February 2011
Viracept (Nelfinavir) Principal Display Panel - Mg Bottle Label
Note to Pharmacist: Do notcover ALERT box withpharmacy label.
Viracept (Nelfinavir) Principal Display Panel - Mg Bottle Label
ALERT: Find out about medicines thatshould NOT be taken with Viracept (Nelfinavir) .
Viracept (Nelfinavir) Principal Display Panel - G Bottle Label
Each level measuring scoop (one gram)contains nelfinavir mesylate equivalentto 50 mg of nelfinavir (free base).
Note to Pharmacist: Do not coverALERT box with pharmacy label.
