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
Brands: Viracept
Introduction
Antiretroviral; HIV protease inhibitor (PI).1 2 3 4 6 7 8
Uses for Nelfinavir Mesylate
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
Nelfinavir Mesylate 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
|
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 |
|
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†
Oral1.25 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†
Oral1.25 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 Nelfinavir Mesylate
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
Interactions for Nelfinavir Mesylate
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 |
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 |
|
|
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 |
|
|
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 |
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 |
|
|
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 |
|
|
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 |
|
|
Pimozide |
Pharmacokinetic interaction; potential for serious or life-threatening reactions (e.g., cardiac arrhythmias)1 |
|
|
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 |
|
|
Sildenafil |
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 |
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 |
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 |
Nelfinavir Mesylate 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
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 measures1 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.
|
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
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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]
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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]
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14. Izzedine H, Diquet B, Launay-Vacher V et al. Pharmacokinetics of nelfinavir in an HIV patient with renal insufficiency. AIDS. 1999; 13:1989. [PubMed 10513666]
15. Emini EA, Condra JH, Schleif WA et al. Maintenance of long-term virus suppression in patients treated with the HIV-1 protease inhibitor Crixivan (indinavir). In: XI International Conference on AIDS, 1996: Abstracts-on-disk. Vancouver, BC, 1996 Jul 7–12. Abstract No. Mo.B.170.
16. Moyle GJ. Resistance to antiretroviral compounds: implications for the clinical management of HIV infection. Immunol Infect Dis. 1995; 5:170-82.
17. Pollard RB. Use of proteinase inhibitors in clinical practice. Pharmacotherapy. 1994; 14:21-9S.
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