Viracept

Generic Name: Nelfinavir Mesylate
Class: HIV Protease Inhibitors
VA Class: AM800
Chemical Name: [3S-[2(2S*,3S*),3α,4aβ,8aβ]] -N-(1,1-dimethylethyl)decahydro-2-[2-hydroxy-3-[(3-hydroxy-2 -methylbenzoyl)amino]-4-(phenylthio)butyl]-3-isoquinolinecarboxamide monomethanesulfonate (salt)
Molecular Formula: C₃₂H₄₅N₃O₄S•CH₄O₃S
CAS Number: 159989-65-8

Introduction

Antiretroviral; HIV protease inhibitor (PI).^{1 2 3 4 6 7 8}

Uses for Viracept

Treatment of HIV Infection

Treatment of HIV infection in conjunction with other antiretrovirals.¹

Because of inferior virologic efficacy, nelfinavir is not recommended for initial therapy.⁹⁵

Postexposure Prophylaxis of HIV

Postexposure prophylaxis of HIV infection† in health-care workers and others exposed occupationally via percutaneous injury or mucous membrane or nonintact skin contact with blood, tissues, or other body fluids associated with risk for transmission of the virus.¹⁴⁶ Used in conjunction with other antiretrovirals.¹⁴⁶

Postexposure prophylaxis of HIV infection† in individuals who have had nonoccupational exposure to blood, genital secretions, or other potentially infectious body fluids of a person known to be infected with HIV when that exposure represents a substantial risk for HIV transmission.¹⁷⁴ Used in conjunction with other antiretrovirals.¹⁷⁴

Viracept Dosage and Administration

Administration

Oral Administration

Administer orally with a meal or light snack.^{1 95 119}

Children who are able to swallow tablets may receive the appropriate number of tablets.¹ Smaller children and children unable to swallow tablets may receive nelfinavir powder for oral suspension.¹

Reconstitution

When the powder for oral suspension is used, the appropriate dose of powder should be added to a small amount of water, milk, soy milk, milk- or soy-based formula or liquid dietary supplement, pudding, or ice cream.^{1 80 119} Each level scoop (provided with the powder by the manufacturer) provides 50 mg of nelfinavir; if a teaspoon measure is used, each level teaspoon provides 200 mg of nelfinavir.^{1 80} After mixing, the entire mixture must be consumed to provide the full dose of nelfinavir; the dose should be consumed within 6 hours of preparation.¹

For individuals unable to swallow tablets, the appropriate dose of nelfinavir tablets (whole or crushed) may be placed in a small amount of water and allowed to disperse and then this dispersion swallowed or mixed with milk or chocolate milk.^{1 80 119 124} Alternatively, the tablets may be crushed and mixed in a small amount of food (e.g., pudding).^{1 119} After being dispersed in water or mixed in food, the entire contents must be consumed within 6 hours to provide the full dose of nelfinavir.¹

Nelfinavir oral powder or tablets should not be mixed with acidic food or juice (e.g., apple juice, applesauce, orange juice) since the resultant mixture may have a bitter taste.^{1 80 119}

Dosage

Available as nelfinavir mesylate; dosage expressed as nelfinavir.¹

Must be given in conjunction with other antiretrovirals.¹ If used with didanosine, lopinavir, or indinavir, adjustment in the treatment regimen may be necessary.^{1 80 95} (See Specific Drugs under Interactions.)

Pediatric Patients

Treatment of HIV Infection

Oral

Neonates and children <2 years of age†: Reliably effective dosage not established.¹ High interindividual variability in drug concentrations observed when 40 mg/kg every 12 hours was evaluated in neonates and infants up to 6 weeks of age; higher dosages are being investigated.¹¹⁹

Children 2–13 years of age: 45–55 mg/kg twice daily or 25–35 mg/kg 3 times daily.^{1 119}

Children >13 years of age: 1.25 g (five 250-mg tablets or two 625-mg tablets) twice daily or 750 mg (three 250-mg tablets) 3 times daily.^{1 95 119}

Table 1. Pediatric Patients ≥2 Years of Age (Tablets)

Weight (kg)	No. of 250-mg Tablets 2 times daily (45–55 mg/kg 2 times daily)	No. of 250-mg Tablets 3 times daily (25–35 mg/kg 3 times daily)
10–12	2	1
13–18	3	2
19–20	4	2
≥21	4–5	3

Table 2. Pediatric Patients ≥2 years of Age (Oral Powder)

Weight (kg)	No. of Level 50-mg Scoops 2 times daily (45–55 mg/kg 2 times daily)	No. of Level 200-mg Teaspoons 2 times daily (45–55 mg/kg 2 times daily)	No. of Level 50-mg Scoops 3 times daily (25–35 mg/kg 3 times daily)	No. of Level 200-mg Teaspoons 3 times daily (25–35 mg/kg 3 times daily)
9 to <10.5	10	2½	6	1½
10.5 to <12	11	2¾	7	1¾
12 to <14	13	3¼	8	2
14 to <16	15	3¾	9	2¼
16 to <18	Use tablets	Use tablets	10	2½
18 to <23	Use tablets	Use tablets	12	3
≥23	Use tablets	Use tablets	15	3¾

Adults

Treatment of HIV Infection

Oral

1.25 g (five 250-mg tablets or two 625-mg tablets) twice daily or 750 mg (three 250-mg tablets) 3 times daily.^{1 95}

Postexposure Prophylaxis of HIV†

Occupational Exposure†

Oral

1.25 g twice daily.¹⁴⁶

Initiate postexposure prophylaxis as soon as possible following exposure (within hours rather than days) and continue for 4 weeks, if tolerated.¹⁴⁶

Nonoccupational Exposure†

Oral

1.25 g twice daily or 750 mg 3 times daily in conjunction with other antiretrovirals.¹⁷⁴

Initiate postexposure prophylaxis as soon as possible following exposure (preferably ≤72 hours after exposure) and continue for 28 days.¹⁷⁴

Prescribing Limits

Pediatric Patients

Treatment of HIV

Oral

>2.5 g daily not studied in children.¹

Special Populations

Hepatic Impairment

Treatment of HIV Infection

Oral

Dosage adjustment not needed in patients with mild hepatic impairment (Child-Pugh class A).¹ Not recommended in patients with moderate or severe hepatic impairment.¹

Renal Impairment

Treatment of HIV Infection

Oral

Dosage adjustments not necessary.⁹⁵

Cautions for Viracept

Contraindications

• 
  

  Known hypersensitivity to nelfinavir or any ingredient in the formulation.¹

  
  


• 
  

  Concomitant use with drugs highly dependent on CYP3A for metabolism and for which elevated plasma concentrations are associated with serious and/or life-threatening events (e.g., amiodarone, cisapride, ergot alkaloids, midazolam, pimozide, quinidine, triazolam).^{1 95} (See Specific Drugs under Interactions.)

  
  

Warnings/Precautions

Warnings

Interactions

Concomitant use with certain drugs not recommended (e.g., lovastatin, simvastatin, St. John’s wort, fluticasone) or requires particular caution (e.g., sildenafil, tadalafil, vardenafil).^{1 95 119} (See Specific Drugs under Interactions.)

Phenylketonuria

Nelfinavir powder for oral suspension contains aspartame (NutraSweet), which is metabolized in the GI tract to provide 11.2 mg of phenylalanine for each 50-mg dose of nelfinavir.¹

Ethyl Methanesulfonate (EMS)

In September 2007, the manufacturer of nelfinavir informed prescribers that commercially available preparations contained EMS, an impurity from the manufacturing process.¹⁷⁸ EMS is a potential human carcinogen.¹⁷⁸ Recommendations that limited use of nelfinavir in children and pregnant women were issued at that time.^{168 178 179} The manufacturer and FDA have agreed on a final limit for EMS in nelfinavir preparations; all nelfinavir preparations manufactured and released after March 31, 2008 meet the final limit established by FDA for all patient populations, including children and pregnant women.¹⁸⁴ Recommendations concerning use in pregnant women and children issued in 2007 no longer apply.^{1 184} Nelfinavir may be used in pregnant women and for initial therapy in pediatric patients.¹⁸⁵

Hyperglycemic Effects

Hyperglycemia, new-onset diabetes mellitus, or exacerbation of preexisting diabetes mellitus reported with use of HIV protease inhibitors (PIs); diabetic ketoacidosis has occurred.^{1 82 130 131 132 148}

Monitor blood glucose and initiate or adjust dosage of oral hypoglycemic agent or insulin as needed.¹

General Precautions

HIV Resistance

Possibility of HIV resistance to nelfinavir and possible cross-resistance to other PIs.^{1 95} Effect of nelfinavir therapy on subsequent therapy with other PIs under investigation.^{1 95}

Hemophilia A and B

Spontaneous bleeding noted with PIs; causal relationship not established.^{1 75 77 124 148}

Caution in patients with a history of hemophilia type A or B.^{1 75} Increased hemostatic (e.g., antihemophilic factor) therapy may be needed.¹

Immune Reconstitution Syndrome

During initial treatment, patients who respond to antiretroviral therapy may develop an inflammatory response to indolent or residual opportunistic infections (e.g., Mycobacterium avium complex [MAC], M. tuberculosis, cytomegalovirus [CMV], Pneumocystis jiroveci [formerly P. carinii]); this may necessitate further evaluation and treatment.¹

Adipogenic Effects

Possible redistribution or accumulation of body fat, including central obesity, dorsocervical fat enlargement (“buffalo hump”), peripheral wasting, breast enlargement, and general cushingoid appearance.^{1 137 138 139 140 141 142 143 144}

Specific Populations

Pregnancy

Category B.¹ Antiretroviral Pregnancy Registry at 800-258-4263.¹

Some experts state that nelfinavir is an alternative PI when the regimen is given solely for perinatal prophylaxis.¹⁶⁸

Lactation

Distributed into milk in rats.¹

Instruct HIV-infected women not to breast-feed because of risk of HIV transmission and risk of adverse effects in the infant.^{1 79 168}

Pediatric Use

Safety and efficacy not established in children <2 years of age.¹ Some data collected in this age group, but reliably effective dosage not established.¹ Some evidence that those <2 years of age have a lower response rate than older children.¹

Use of nelfinavir in children 2–13 years of age supported by evidence from adequate and well-controlled studies in adults and pharmacokinetic and clinical studies supporting activity in pediatric patients.^{1 80 119 124 126 127 147 152 153 154 161} Diarrhea reported less frequently in children than in adults.^{80 124}

Geriatric Use

Insufficient experience in those ≥65 years of age to determine whether they respond differently than younger adults.¹

Hepatic Impairment

Use in patients with moderate or severe hepatic impairment not recommended.¹

Common Adverse Effects

Diarrhea, nausea.^{1 4 80}

Interactions for Viracept

Metabolized by CYP3A and CYP2C19.^{1 80 83}

Inhibits CYP3A; does not inhibit CYP2D6, CYP2C9, CYP2C19, CYP2C8, CYP1A2, or CYP2E1.^{1 80 83}

Drugs Affecting or Metabolized by Hepatic Microsomal Enzymes

Pharmacokinetic interactions likely with drugs that are inhibitors, inducers, or substrates of CYP3A or CYP2C19 with possible alteration in metabolism of nelfinavir and/or other drug.¹

Specific Drugs

Drug	Interaction	Comments
Abacavir	In vitro evidence of synergistic antiretroviral effects1
Antiarrhythmic agents (amiodarone, quinidine)	Possible increased antiarrhythmic agent concentrations; potential for serious or life-threatening effects (e.g., cardiac arrhythmias)1	Concomitant use with amiodarone or quinidine contraindicated1
Anticonvulsants (carbamazepine, phenobarbital, phenytoin)	Decreased phenytoin concentrations and AUC; no change in nelfinavir plasma concentrations1 Possible decreased nelfinavir concentrations with carbamazepine or phenobarbital1 90	Monitor phenytoin concentrations; adjustment of phenytoin dosage may be needed 1 Monitor anticonvulsant concentrations and virologic response; consider use of alternative anticonvulsant or monitoring nelfinavir concentrations95
Antifungals, azoles (itraconazole, ketoconazole, voriconazole)	Itraconazole: Manufacturer states pharmacokinetic interactions unlikely;1 some experts state possible pharmacokinetic interactions affecting both drugs95 Ketoconazole: Increased nelfinavir concentrations and AUC1 Voriconazole: Possible pharmacokinetic interactions; may affect both drugs95	Itraconazole: Dosage adjustment not needed;80 monitor itraconazole concentrations95 Ketoconazole: Dosage adjustments not necessary1 95 Voriconazole: Monitor for toxicities95
Antimycobacterials (rifabutin, rifampin, rifapentine)	Rifabutin: Increased rifabutin concentrations; decreased nelfinavir concentrations1 95 Rifampin: Decreased nelfinavir concentrations1 84 95	Rifabutin: Reduce rifabutin dosage to 150 mg once daily or 300 mg 3 times weekly;95 nelfinavir 1.25 g twice daily is preferred regimen when concomitant therapy is necessary1 Rifampin: Concomitant use not recommended1 85 95 145 Rifapentine: Concomitant use not recommended95
Benzodiazepines	Pharmacokinetic interaction with midazolam or triazolam; potential for prolonged or increased sedation or respiratory depression1	Manufacturer of nelfinavir states that concomitant use with midazolam or triazolam contraindicated;1 95 however, some experts state a single parenteral dose of midazolam can be used with caution in a monitored situation for procedural sedation95
Cisapride	Pharmacokinetic interaction; potential for serious or life-threatening reactions (e.g., cardiac arrhythmias)95	Concomitant use not recommended95
Corticosteroids (fluticasone)	Fluticasone nasal spray/oral inhalation: Possible increased plasma fluticasone concentrations1	Fluticasone nasal spray/oral inhalation: Consider alternatives in patients receiving nelfinavir, especially when long-term corticosteroid therapy is anticipated1
Co-trimoxazole	Interaction unlikely1
Dapsone	Interaction unlikely1
Darunavir		Concomitant use with ritonavir-boosted darunavir not recommended pending further accumulation of data177
Delavirdine	Decreased plasma delavirdine concentrations; increased plasma nelfinavir concentrations1 80 95 133 176 Increased toxicity (i.e., neutropenia) observed1 80 133 In vitro evidence of synergistic antiretroviral effects1	Appropriate dosages for concomitant use with respect to safety and efficacy not established 1 176
Didanosine	No change in nelfinavir concentrations when didanosine administered 1 hour before nelfinavir1 80 In vitro evidence of additive antiretroviral effects1	Administer nelfinavir (with food) 1 hour after or 2 hours before didanosine (without food)1 80
Efavirenz	Increased peak plasma concentrations and AUC of nelfinavir; decreased peak plasma concentrations and AUC of nelfinavir metabolite (M8); no change in the pharmacokinetics of efavirenz1 95 122 147 In vitro evidence of synergistic antiretroviral effects1	Dosage adjustment not needed1 93 95 122 147
Emtricitabine	In vitro evidence of additive or synergistic antiretroviral effects182
Ergot alkaloids (dihydroergotamine, ergonovine, ergotamine, methylergonovine)	Possibility of pharmacokinetic interaction; potential for serious or life-threatening reactions (e.g., acute ergot toxicity)1	Concomitant use contraindicated1 95 If treatment of uterine atony and excessive postpartum bleeding is indicated in a woman receiving nelfinavir, use methylergonovine maleate (Methergine) only if alternative treatments cannot be used and if potential benefits outweigh risks; use methylergonovine at lowest dosage and shortest duration possible168
Estrogens/Progestins	Hormonal contraceptives: Decreased concentrations of ethinyl estradiol and norethindrone with oral contraceptive preparations95	Use alternative or concomitant nonhormonal contraceptive measures1 95
Etravirine	Increased nelfinavir concentrations183	Concomitant use not recommended95 183
Fosamprenavir	Studies using amprenavir indicate possible alterations in amprenavir pharmacokinetics;181 concomitant use of ritonavir-boosted fosamprenavir with nelfinavir not evaluated181 In vitro evidence of additive antiretroviral effects181	Appropriate dosages for concomitant use with respect to safety and efficacy not established95 181
HMG-CoA reductase inhibitors	Decreased clearance and increased concentrations of some HMG-CoA reductase inhibitors with potential for increased risk of myopathy (including rhabdomyolysis)1	Concomitant use with lovastatin or simvastatin not recommended;1 95 caution if used with other HMG-CoA reductase inhibitors metabolized by the CYP3A4 pathway1 95 If used with atorvastatin or rosuvastatin, use lowest possible dosage of the HMG-CoA reductase inhibitor1 Consider using HMG-CoA reductase inhibitors with low potential for interaction (e.g., fluvastatin, pravastatin)1
Immunosuppressive agents	Potential for increased concentrations of cyclosporine, sirolimus, or tacrolimus1
Indinavir	Increased AUC of both drugs1 80 87 95	Appropriate dosages for concomitant use with respect to safety and efficacy not established 1 Limited data supports use of nelfinavir 1.25 g twice daily with indinavir 1.2 g twice daily95
Lamivudine	Increased lamivudine peak plasma concentrations and AUC1 In vitro evidence of synergistic antiretroviral effects1	Dosage adjustment not needed1 80 124
Lopinavir	Decreased lopinavir concentrations and increased nelfinavir concentrations95 171	Once-daily lopinavir regimen not recommended with nelfinavir171 Some experts state that appropriate dosages for concomitant use of lopinavir and nelfinavir not established95 For adults, manufacturer of lopinavir recommends 500 mg of lopinavir and 125 mg of ritonavir (as tablets) twice daily171 Manufacturer of lopinavir recommends that adults receive 533 mg of lopinavir and 133 mg of ritonavir (6.7 mL of the oral solution) twice daily171 For pediatric patients 6 months to 18 years of age, manufacturer of lopinavir recommends 300 mg/m2 of lopinavir and 75 mg/m2 of ritonavir twice daily (do not exceed the adult dosage)171
Macrolides (azithromycin)	Increased azithromycin peak plasma concentrations and AUC; no clinically important changes in nelfinavir pharmacokinetic values1	Dosage adjustment not needed; monitor for azithromycin adverse effects (e.g., hepatic enzyme abnormalities, hearing impairment)1 173
Maraviroc	Possible increased concentrations of maraviroc95	Recommended dosage of maraviroc is 150 mg twice daily95 186
Methadone	Decreased methadone plasma concentrations and AUC1	Monitor and titrate methadone dose if needed; consider need to increase methadone dosage1 30 95
Nevirapine	Clinically important pharmacokinetic interactions unlikely1 80 95 In vitro evidence of synergistic antiretroviral effects1	Dosage adjustment not needed1 95
Pimozide	Pharmacokinetic interaction; potential for serious or life-threatening reactions (e.g., cardiac arrhythmias)1	Concomitant use contraindicated1 95
Proton-pump inhibitors	Omeprazole: Decreased nelfinavir concentrations and possible loss of therapeutic effect1	Concomitant use with proton pump inhibitors not recommended1
Ritonavir	Increased nelfinavir concentrations;1 80 87 95 no change in ritonavir concentrations95	Appropriate dosages for concomitant use with respect to safety and efficacy not established 1
Saquinavir	Increased saquinavir concentrations and increased nelfinavir concentrations1 80 95 Ritonavir-boosted saquinavir not studied158	Manufacturer of nelfinavir states appropriate dosages for concomitant use with respect to safety and efficacy not established1 Saquinavir 1.2 g twice daily with nelfinavir 1.25 g twice daily results in adequate plasma concentrations of both PIs158
St. John’s wort (Hypericum perforatum)	Decreased nelfinavir concentrations; possible loss of virologic response and increased risk of nelfinavir resistance 95 164 165	Concomitant use not recommended1 95
Sildenafil	Increased sildenafil concentrations1 95 148 157	Use caution and reduced sildenafil dosage (25 mg repeated no more frequently than every 48 hours);1 95 closely monitor for adverse effects (e.g., hypotension, syncope, visual changes, prolonged erection)1 95 148 157
Stavudine	Pharmacokinetic interactions unlikely1 In vitro evidence of additive antiretroviral effects1	Dosage adjustments not needed1
Tadalafil	Increased tadalafil concentrations1 95	Use caution and reduced tadalafil dosage (10 mg repeated no more frequently than every 72 hours); closely monitor for adverse effects (e.g., hypotension, syncope, visual changes, prolonged erection);1 some experts recommend initial dose of 5 mg and not maximum dosage of 10 mg once every 72 hours95
Tenofovir	Pharmacokinetic interaction unlikely176 In vitro evidence of synergistic antiretroviral effects1
Tipranavir	Data not available to date95	Concomitant use not recommended; appropriate dosage not established95
Trazodone	Possible increased trazodone concentrations1	Use with caution; consider using decreased trazodone dosage1
Vardenafil	Possible increased vardenafil concentrations1 95	Use caution and reduced vardenafil dosage (2.5 mg repeated no more frequently than every 72 hours); closely monitor for adverse effects (e.g., hypotension, syncope, visual changes, prolonged erection)1 95
Zidovudine	Decreased zidovudine peak plasma concentrations and AUC1 In vitro evidence of synergistic antiretroviral effects1	Dosage adjustment not needed1

Viracept Pharmacokinetics

Absorption

Bioavailability

Well absorbed from GI tract; peak plasma concentrations attained within 2–4 hours when administered with food.^{4 8 20 21 80}

Nelfinavir 625-mg tablets are not bioequivalent to the 250-mg tablets; AUC 24% higher with the 625-mg tablets (given with food) compared with the 250-mg tablets (given with food).¹

Food

Presence of food in the GI tract substantially increases extent of absorption and decreases pharmacokinetic variability of the drug relative to the fasting state.^{1 20 80} Peak plasma concentration and AUC reportedly are 2–5 times greater when administered with a meal (125–1000 kcal with 20–50% fat) rather than under fasting conditions.^{1 80}

Special Populations

Use in children associated with highly variable drug concentrations;¹ may be related to inconsistent food intake.¹

Plasma concentrations of nelfinavir not altered in individuals with mild hepatic impairment (Child-Pugh class A).¹ AUC increased 62% in individuals with moderate hepatic impairment (Child-Pugh class B).¹ Pharmacokinetics not investigated in individuals with severe hepatic impairment.¹

Distribution

Extent

Not fully characterized.¹

Not detected in CSF in adults.¹⁵⁰

Not known whether crosses the placenta or is distributed into human milk.¹

Plasma Protein Binding

98%.¹

Elimination

Metabolism

Metabolized by CYP3A and CYP2C19.^{1 80}

The major metabolite (M8) has in vitro antiviral activity similar to that of nelfinavir.¹

Elimination Route

Excreted principally in feces as unchanged drug and metabolites.¹

Removed by hemodialysis;⁵¹ does not appear to be removed by peritoneal dialysis.¹⁶⁰

Half-life

3.5–5 hours.^{1 80}

Special Populations

Nelfinavir clearance is 2–3 times greater in children 2–13 years of age than in adults (weight-adjusted basis).^{80 124}

Stability

Storage

Oral

Tablets

15–30°C.¹

Powder for Oral Suspension

15–30°C.¹

Actions and SpectrumActions

• 
  

  Pharmacologically related to other PIs (e.g., amprenavir, atazanavir, fosamprenavir, indinavir, lopinavir, ritonavir, saquinavir); differs structurally from these drugs and also differs pharmacologically and structurally from other currently available antiretrovirals.^{1 80}

  
  


• 
  

  Active against HIV-1 and HIV-2.^{1 7 8} The major metabolite (M8) has antiviral activity similar to that of nelfinavir.¹

  
  


• 
  

  Inhibits replication of HIV-1 and HIV-2 by interfering with HIV protease.^{1 2 3 4 7 92 120}

  
  


• 
  

  HIV-1 with reduced susceptibility to nelfinavir have been selected in vitro and have emerged during therapy with the drug.^{1 7 9 80}

  
  


• 
  

  Varying degrees of cross-resistance occur among PIs; only limited data available to date regarding cross-resistance between nelfinavir and other PIs.^{1 4 11 13 14 15 19 93 94}

  
  


• 
  

  Cross-resistance between nelfinavir and nucleoside reverse transcriptase inhibitors (NRTIs) or nonnucleoside reverse transcriptase inhibitors (NNRTIs) unlikely since the drugs have different target enzymes and mechanisms of action.¹

  
  

Advice to Patients

• 
  

  Critical nature of compliance with HIV therapy.¹ Importance of using nelfinavir in conjunction with other antiretrovirals—not for monotherapy.¹

  
  


• 
  

  Antiretroviral therapy is not a cure for HIV infection, and opportunistic infections still may occur.¹ HIV transmission via sexual contact or sharing needles is not prevented by antiretrovirals.¹

  
  


• 
  

  Importance of taking with food.¹

  
  


• 
  

  Importance of reading patient package insert from manufacturer.¹

  
  


• 
  

  Redistribution/accumulation of body fat may occur, with as yet unknown long-term health effects.¹

  
  


• 
  

  Diarrhea, a frequent adverse effect, can be controlled with OTC drugs such as loperamide.¹

  
  


• 
  

  If using oral contraceptives, need for alternative or concomitant nonhormonal contraceptive measures^{1 95}

  
  


• 
  

  Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs and dietary or herbal products.¹

  
  


• 
  

  Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.¹

  
  


• 
  

  Importance of advising patients of other important precautionary information.¹ (See Cautions.)

  
  

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Nelfinavir Mesylate

Routes	Dosage Forms	Strengths	Brand Names	Manufacturer
Oral	For suspension	50 mg (of nelfinavir) per g	Viracept Oral Powder	Agouron
	Tablets, film-coated	250 mg (of nelfinavir)	Viracept	Agouron
		625 mg (of nelfinavir)	Viracept	Agouron

Comparative Pricing

This pricing information is subject to change at the sole discretion of DS Pharmacy. This pricing information was updated 03/2011. Actual costs to patients will vary depending on the use of specific retail or mail-order locations and health insurance copays.

Viracept 250MG Tablets (VIIV HEALTHCARE): 300/$716.02 or 900/$2110.06

Viracept 50MG/GM Powder (VIIV HEALTHCARE): 144/$72.99 or 432/$195.97

Disclaimer

This report on medications is for your information only, and is not considered individual patient advice. Because of the changing nature of drug information, please consult your physician or pharmacist about specific clinical use.

The American Society of Health-System Pharmacists, Inc. and Drugs.com represent that the information provided hereunder was formulated with a reasonable standard of care, and in conformity with professional standards in the field. The American Society of Health-System Pharmacists, Inc. and Drugs.com make no representations or warranties, express or implied, including, but not limited to, any implied warranty of merchantability and/or fitness for a particular purpose, with respect to such information and specifically disclaims all such warranties. Users are advised that decisions regarding drug therapy are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and the information is provided for informational purposes only. The entire monograph for a drug should be reviewed for a thorough understanding of the drug's actions, uses and side effects. The American Society of Health-System Pharmacists, Inc. and Drugs.com do not endorse or recommend the use of any drug. The information is not a substitute for medical care.

AHFS Drug Information. © Copyright, 1959-2011, Selected Revisions November 2009. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

† Use is not currently included in the labeling approved by the US Food and Drug Administration.

References

1. Agouron Pharmaceuticals. Viracept (nelfinavir mesylate) tablets and oral powder prescribing information. La Jolla, CA; 2008 Sep.

2. Longer M, Shetty B, Zamansky I et al. Preformulation studies of a novel HIV protease inhibitor, AG1343. J Pharm Sci. 1995; 84:1090-3. [PubMed 8537887]

3. Kaldor SW, Kalish VJ, davies JF et al. Viracept (nelfinavir mesylate, AG13430: a potent orally bioavailable inhibitor of HIV-1 protease. J Med Chem. 1997; 40:3979-85. [PubMed 9397180]

4. Moyle G, Gazzard B. Current knowledge and future prospects for the use of HIV protease inhibitors. Drugs. 1996; 51:701-12. [PubMed 8861542]

5. Vella S. Rationale and experience with reverse transcriptase inhibitors and protease inhibitors. J Acquir Immune Defic Syndr Hum Retrovirol. 1995; 10(Suppl 1):S58-61.

6. .

7. Patick AK, Mo H, Markowitz M et al. Antiviral and resistance studies of AG1343, an orally bioavailable inhibitor of human immunodeficiency virus protease. Antimicrob Agents Chemother. 1996; 40:292-7. [PubMed 8834868]

8. Shetty BV, Kosa MB, Khalil DA et al. Preclinical pharmacokinetics and distribution to tissue of AG1343, an inhibitor of human immunodeficiency virus type 1 protease. Antimicrob Agents Chemother. 1996; 40:110-4. [PubMed 8787890]

9. Patick AK, Duran M, Cao Y et al. Genotypic and phenotypic characterization of human immunodeficiency virus type 1 variants isolated from patients treated with the protease inhibitor nelfinavir. Antimicrob Agents Chemother. 1998; 42:2637-44. [PubMed 9756769]

10. Lech WJ, Wang G, Yang YL et al. In vivo sequence diversity of the protease of human immunodeficiency virus type 1: presence of protease inhibitor-resistant variants in untreated subjects. J Virol. 1996; 70:2038-43. [PubMed 8627733]

11. Ridky T, Leis J. Development of drug resistance to HIV-1 protease inhibitors. J Biol Chem. 1995; 270:29621-3. [PubMed 8530341]

12. Montaner JSG, Hogg RS, O’Shaughnessy MV. Emerging international consensus for use of antiretroviral therapy. Lancet. 1997; 349:1042. [IDIS 383566] [PubMed 9107240]

13. Deeks SG, Smith M, Holodniy M