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Indinavir Sulfate

Class: HIV Protease Inhibitors
VA Class: AM800
Chemical Name: [1S-[1α(R*),2α]]-2,3,5-trideoxy-N-(2,3-dihydro -2-hydroxy-1H-inden-1-yl)-5-[2-[[(1,1-dimethylethyl)amino]carbonyl]-4 -(3-pyridinylmethyl)-1-piperazinyl]-2-(phenylmethyl)-d-erythro-pentonamide sulfate (1:1) (salt)
Molecular Formula: C36H47N5O4
CAS Number: 157810-81-6
Brands: Crixivan

Introduction

Antiretroviral; HIV protease inhibitor (PI).1 2 3 6 7

Uses for Indinavir Sulfate

Treatment of HIV Infection

Treatment of HIV infection in conjunction with other antiretrovirals.1

Because of the inconvenient dosing regimen and fluid requirements, indinavir is not recommended for initial therapy.108 Because of the high incidence of nephrolithiasis, ritonavir-boosted indinavir is not recommended for initial therapy.108

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 increased risk for transmission of the virus.94 95 97 Used in conjunction with other antiretrovirals.95

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.184 Used in conjunction with other antiretrovirals.184

Indinavir Sulfate Dosage and Administration

Administration

Oral Administration

Administer orally.1

If used without low-dose ritonavir, administer with water at least 1 hour before or 2 hours after a meal.1 108 Alternatively, administer with some other liquid (e.g., skim milk, juice, coffee, tea) or with a light meal (e.g., dry toast with jelly, apple juice, coffee with skim milk and sugar; corn flakes with skim milk and sugar).1 Do not administer with a meal high in calories, fat, and protein.1

Some clinicians suggest the drug may be taken without regard to meals if used with low-dose ritonavir (ritonavir-boosted indinavir).108

To ensure adequate hydration, patients should drink at least 1.5 L (approximately 48 ounces) of liquids daily (i.e., every 24 hours).1 4 108 If ritonavir-boosted indinavir is used, some experts suggest patients drink 1.5–2 L of noncaffeinated liquids daily.108

Dosage

Available as indinavir sulfate; dosage expressed as indinavir.1

Must be given in conjunction with other antiretrovirals.1 If used with delavirdine, certain didanosine preparations, efavirenz, lopinavir/ritonavir, nelfinavir, nevirapine, or ritonavir, adjustment in the treatment regimen recommended.1 100 105 108 180 (See Specific Drugs and Food under Interactions.)

Pediatric Patients

Treatment of HIV Infection
Oral

Children 4–15 years of age†: 500 mg/m2 every 8 hours under investigation.147

Adults

Treatment of HIV Infection
Oral

800 mg every 8 hours.1 108 If ritonavir-boosted indinavir is used, 800 mg twice daily with low-dose ritonavir (100 or 200 mg twice daily).108

Postexposure Prophylaxis of HIV†
Occupational Exposure†
Oral

800 mg twice daily boosted with low-dose ritonavir (100 mg twice daily).95 Alternatively, 800 mg every 8 hours (without low-dose ritonavir).95

Initiate postexposure prophylaxis as soon as possible following exposure (within hours rather than days) and continue for 4 weeks, if tolerated.95

Nonoccupational Exposure†
Oral

800 mg twice daily boosted with low-dose ritonavir (100 or 200 mg every 12 hours).184 Alternatively, 800 mg every 8 hours (without low-dose ritonavir).184

Initiate postexposure prophylaxis as soon as possible following exposure (preferably ≤72 hours after exposure) and continue for 28 days.184

Special Populations

Hepatic Impairment

Treatment of HIV Infection
Oral

Adults with mild to moderate hepatic impairment due to cirrhosis: 600 mg every 8 hours.1 108

Renal Impairment

Treatment of HIV Infection
Oral

Dosage adjustment not needed.108

Geriatric Patients

Select dosage with caution.1

Cautions for Indinavir Sulfate

Contraindications

  • Known hypersensitivity to indinavir 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., alprazolam, amiodarone, cisapride, ergot alkaloids, oral midazolam, pimozide, triazolam).1 (See Specific Drugs and Food under Interactions.)

Warnings/Precautions

Warnings

Interactions

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

Renal and GU Effects

Nephrolithiasis/urolithiasis,1 4 26 68 73 sometimes associated with substantial renal impairment, acute renal failure, or pyelonephritis with or without bacteremia, reported.1

Adequate hydration recommended for all patients receiving indinavir.1 108 Risk of nephrolithiasis/urolithiasis may be greater with ritonavir-boosted indinavir compared with indinavir (without low-dose ritonavir).1 108

If signs and symptoms of nephrolithiasis/urolithiasis (flank pain, with or without hematuria or microscopic hematuria) occur, temporary interruption (e.g., for 1–3 days) or discontinuance of therapy may be considered.1

Interstitial nephritis with medullary calcification and cortical atrophy reported in patients with asymptomatic severe leukocyturia (≥100 cells per high power field).1 Monitor patients who have asymptomatic severe leukocyturia (i.e., perform frequent urinalysis); further diagnostic evaluation may be needed.1 Consider discontinuing indinavir in patients with severe leukocyturia.1

Hemolytic Anemia

Acute hemolytic anemia, including cases resulting in death, reported.1

If acute hemolytic anemia occurs, take appropriate measures to treat the condition (including discontinuance of indinavir).1

Hepatic Effects

Acute hepatitis sometimes resulting in hepatic failure and death reported; causal relationship not established.1 116 Generally has occurred in patients with confounding medical conditions and/or receiving concomitant drugs.1

Elevated indirect bilirubin, infrequently associated with increased serum AST (SGOT) or ALT (SGPT) concentrations, reported.1 4 17 23 73

Hyperglycemic Effects

Hyperglycemia, new-onset diabetes mellitus, or exacerbation of preexisting diabetes mellitus reported with use of PIs; diabetic ketoacidosis has occurred.1 88 120 121 122 123

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 indinavir and possible cross-resistance to other PIs.1 147 Effect of indinavir therapy on subsequent therapy with other PIs under investigation.1 147

Hemophilia A and B

Spontaneous bleeding noted with PIs; causal relationship not established.1 40 119

Caution in patients with a history of hemophilia type A or B.1 40 119 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]);1 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

Specific Populations

Pregnancy

Category C.1

Antiretroviral Pregnancy Registry at 800-258-4263.1

Hyperbilirubinemia, generally reported as an increase in indirect bilirubin, has occurred in patients receiving indinavir; it is not known whether administration of the drug to a pregnant woman during the perinatal period can exacerbate physiologic hyperbilirubinemia in the neonate.1

Substantially decreased plasma indinavir concentrations reported during pregnancy.1 172 (See Special Populations under Pharmacokinetics.)

Some experts state use of ritonavir-boosted indinavir is an alternative HIV protease inhibitor (not a preferred PI) for use in pregnant women;172 however optimal dosage of ritonavir-boosted indinavir for use during pregnancy not known.1

Lactation

Distributed into milk in rats; not known whether distributed into human milk.1

Instruct HIV-infected women not to breast-feed because of risk of HIV transmission and risk of adverse effects in the infant.1 57 172

Pediatric Use

Safety and efficacy not established in pediatric patients.1

Has been used in a limited number of HIV-infected children ≥3 months of age†.1 39 72 124 125 147 151 152 166 173 Nephrolithiasis/urolithiasis reported more frequently in pediatric patients than in adults.1

Because hyperbilirubinemia has been reported in patients receiving indinavir,1 4 17 23 73 147 the drug should not be used in neonates until further information is available.147

Geriatric Use

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

Use with caution because of age-related decreases in hepatic, renal, and/or cardiac function and concomitant disease and drug therapy.1

Hepatic Impairment

Dosage adjustment recommended in patients with hepatic impairment due to cirrhosis.1 (See Hepatic Impairment under Dosage and Administration.)

Common Adverse Effects

Nausea, abdominal pain, headache, nephrolithiasis/urolithiasis, asymptomatic hyperbilirubinemia.1

Interactions for Indinavir Sulfate

Metabolized by CYP3A.1

Inhibits CYP3A and, to a lesser extent, CYP2D6.1

Does not inhibit CYP1A2, 2C9, 2E1, or 2B6.1

Drugs Affecting or Metabolized by Hepatic Microsomal Enzymes

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

Specific Drugs and Food

Drug or Food

Interaction

Comments

Antiarrhythmic agents (amiodarone, systemic lidocaine, quinidine)

Potential increased antiarrhythmic concentrations1

Potential for serious or life-threatening effects (e.g., cardiac arrhythmias) if indinavir used with amiodarone1

Concomitant use with amiodarone contraindicated1

Caution if indinavir used concomitantly with systemic lidocaine or quinidine; monitoring plasma antiarrhythmic concentrations recommended1

Anticonvulsants (carbamazepine, phenobarbital, phenytoin)

Possible decreased plasma concentrations of indinavir; possible decreased antiretroviral effectiveness1

No change in plasma concentrations of carbamazepine167

Use concomitantly with caution;1 consider using alternative anticonvulsants, using ritonavir-boosted indinavir, and/or monitoring indinavir concentrations108

Antifungals, azole (itraconazole, ketoconazole, voriconazole)

Increased concentrations of indinavir when administered with itraconazole, ketoconazole, or fluconazole; no change in AUC of indinavir with fluconazole1 74 108 145

Voriconazole: Pharmacokinetic interactions unlikely with indinavir;108 decreased voriconazole concentrations reported with low-dose ritonavir108

Fluconazole: Dosage adjustment not needed145

Itraconazole: When given with itraconazole 200 mg twice daily, reduce indinavir dosage to 600 mg every 8 hours;1 108 do not use itraconazole dosage >200 mg twice daily108

Ketoconazole: When given with ketoconazole, reduce indinavir dosage to 600 mg every 8 hours1 108

Voriconazole: Dosage adjustment not needed with indinavir1 108

Voriconazole: Concomitant use with ritonavir-boosted indinavir not recommended unless potential benefits outweigh risk108

Antimycobacterials

Isoniazid: No change in AUC of indinavir and clinically unimportant increases in AUC of isoniazid1 74

Rifabutin: Decreased indinavir concentrations and increased rifabutin concentrations1 108

Rifampin: Decreased indinavir concentrations; possible decreased antiretroviral efficacy and increased risk of antiretroviral resistance1

Isoniazid: Dosage adjustment not needed1

Rifabutin: Reduce rifabutin dosage to 150 mg once daily or 300 mg 3 times weekly; increase indinavir dosage to 1 g every 8 hours1 108

Rifampin: Concomitant use not recommended1 108 148

Rifapentine: Concomitant use not recommended108

Atazanavir

Potential for additive hyperbilirubinemia;108 e concomitant use has not been studiede

In vitro evidence of additive antiretroviral effectse

Concomitant use not recommended108 e

Benzodiazepines

Pharmacokinetic interaction with alprazolam, midazolam, or triazolam; potential for prolonged or increased sedation or respiratory depression1

Concomitant use with alprazolam, oral midazolam, or triazolam contraindicated;1 108 some experts state that a single parenteral dose of midazolam can be used with caution in a monitored situation for procedural sedation108

Calcium-channel blocking agents, dihydropyridine (amlodipine, felodipine, isradipine, nicardipine, nifedipine, nimodipine, nisoldipine)

Possible increased concentrations of calcium-channel blocking agent; potential for increased or prolonged therapeutic or adverse effects of the cardiac drug1

Use concomitantly with caution; clinical monitoring recommended1

Cisapride

Pharmacokinetic interaction; potential for serious or life-threatening reactions (e.g., cardiac arrhythmias)1

Concomitant use contraindicated1 108

Corticosteroids (fluticasone)

Fluticasone nasal spray/oral inhalation: Increased plasma fluticasone concentrations with indinavir (with or without low-dose ritonavir) resulting in decreased cortisol concentrations1

Fluticasone nasal spray/oral inhalation: Consider alternative in patients receiving indinavir (without ritonavir), especially when long-term corticosteroid therapy is anticipated; concomitant use with ritonavir-boosted indinavir not recommended unless potential benefits outweigh risk of systemic corticosteroid adverse effects1

Co-trimoxazole

Interaction unlikely1

Dosage adjustment not needed1

Darunavir

Increased concentrations of darunavir and indinavir185

Appropriate dosage for concomitant use of ritonavir-boosted darunavir and indinavir not established185

Delavirdine

Increased peak plasma concentrations and AUC of indinavir; no change in pharmacokinetics of delavirdine1 108 129 144

When given with delavirdine 400 mg 3 times daily (usual delavirdine dosage), reduce indinavir dosage to 600 mg every 8 hours1 108 129

Didanosine

When buffered didanosine preparations administered at the same time as indinavir, decreased AUC of indinavir155

In vitro evidence of synergistic antiretroviral effects1

Administer indinavir and buffered didanosine (pediatric oral solution admixed with antacid) ≥1 hour apart1 4

Efavirenz

Decreased peak plasma concentrations and AUC of indinavir; no change in pharmacokinetics of efavirenz1 149

In vitro evidence of synergistic antiretroviral effects149

Adjustment of efavirenz dosage not needed; increase indinavir dosage to 1 g every 8 hours or consider ritonavir-boosted indinavir108

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 108

If treatment of uterine atony and excessive postpartum bleeding is indicated in a woman receiving indinavir, 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 possible147

Estrogens/Progestins

Hormonal contraceptives: Increased AUC of ethinyl estradiol and norethindrone reported with oral contraceptive preparations1

Hormonal contraceptives: Dosage adjustment not needed1 108

Etravirine

Decreased indinavir concentrationsg

Concomitant use not recommended108 g

Fosamprenavir

Studies using amprenavir indicate possible increased plasma amprenavir concentrations and AUC;f concomitant use of ritonavir-boosted fosamprenavir with indinavir not evaluatedf

In vitro evidence of additive antiretroviral effectsf

Appropriate dosages for concomitant use with respect to safety and efficacy not establishedf

Grapefruit juice

Decreased AUC and concentrations of indinavir1 108

Monitor virologic response108

Histamine H2-receptor antagonists (cimetidine)

Pharmacokinetic interaction unlikely with cimetidine1

Dosage adjustment not needed1

HMG-CoA reductase inhibitors (statins)

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, rosuvastatin, or simvastatin not recommended1

If used with atorvastatin, use lowest possible dosage of atorvastatin1

Consider using HMG-CoA reductase inhibitors with low potential for interaction (e.g., fluvastatin, pravastatin)1

Immunosuppressive agents (cyclosporine, sirolimus, tacrolimus)

Potential for increased concentrations of cyclosporine, sirolimus, or tacrolimus1

Lopinavir

Pharmacokinetic interaction; increased indinavir AUC and concentrations108 177

Consider indinavir 600 mg twice daily with 400 mg of lopinavir and 100 mg of ritonavir twice daily108 177

Macrolides (clarithromycin)

Increased AUC of indinavir and clarithromycin; decreased AUC of 14-hydroxyclarithromycin1 74 108 171

Indinavir manufacturer states appropriate dosages for concomitant use with respect to safety and efficacy not established;1 some experts state that modification of usual clarithromycin dosage not necessary in patients with normal renal function; reduce clarithromycin dosage by 50% if Clcr 30–60 mL/minute and reduce by 75% if Clcr <30 mL/minute 108

Maraviroc

Possible increased concentrations of maraviroc108

Recommended dosage of maraviroc is 150 mg twice daily108

Methadone

Pharmacokinetic interactions unlikely1 108

Nelfinavir

Increased AUC of both drugs105 126 127

Appropriate dosages for concomitant use with respect to safety and efficacy not established1 105

Limited data supports use of indinavir 1.2 g twice daily with nelfinavir 1.25 g twice daily108

Nevirapine

Decreased peak and trough plasma concentration and AUC of indinavir; no clinically important change in the pharmacokinetics of nevirapine100 108

In vitro evidence of additive or synergistic antiretroviral effects60

Manufacturers state appropriate dosages for concomitant use with respect to safety and efficacy not established1

Some experts state adjustment of nevirapine dosage not needed; consider increasing indinavir dosage to 1 g every 8 hours or using ritonavir-boosted indinavir100 108

Pimozide

Pharmacokinetic interaction; potential for serious or life-threatening reactions (e.g., cardiac arrhythmias)1

Concomitant use contraindicated1 108

Quinupristin and dalfopristin

Possible increased indinavir plasma concentrations169

Ritonavir

Increased indinavir concentrations and increased ritonavir concentrations;1 5 44 108 concomitant low-dose ritonavir used to therapeutic advantage (ritonavir-boosted indinavir)108

Incidence of renal effects (nephrolithiasis) may be higher when ritonavir and indinavir used concomitantly compared with usual dosage of indinavir alone1

Limited data supports use of indinavir 400 mg twice daily with ritonavir 400 mg twice daily 108 174 180 or indinavir 800 mg twice daily with ritonavir 100 or 200 mg twice daily108 180

Saquinavir

Increased saquinavir concentrations;1 30 no effect on indinavir concentrations108

Data not available on concomitant use with ritonavir-boosted saquinavir30

Appropriate dosages for concomitant use with respect to safety and efficacy not established 1 30

St. John’s wort (Hypericum perforatum)

Decreased indinavir concentrations; possible loss of virologic response and increased risk of lopinavir resistance1

Concomitant use not recommended1 108

Sildenafil

Increased sildenafil concentrations and increased risk of sildenafil-associated adverse effects (e.g., hypotension, visual changes, prolonged erection)1 108 154 170

Use caution and reduced sildenafil dosage (25 mg repeated no more frequently than every 48 hours);1 108 closely monitor for adverse effects (e.g., hypotension, syncope, visual changes, prolonged erection)1 108

Stavudine

Clinically important pharmacokinetic interaction unlikely1 74 108

Tadalafil

Increased tadalafil concentrations and increased risk of tadalafil-associated adverse effects (e.g., hypotension, visual changes, prolonged erection)1 108

Use an initial tadalafil dose of 5 mg and do not exceed a single tadalafil dose of 10 mg in 72 hours108

Tenofovir

Slight alterations in indinavir and tenofovir concentrations;108 d not clinically important108

In vitro evidence of additive or synergistic antiretroviral effectsd

No dosage adjustment needed108

Theophylline

Pharmacokinetic interactions unlikely1

Tipranavir

Data not available to date108

Concomitant use not recommended; appropriate dosage not established108

Trazodone

Possible increased trazodone concentrations; increased risk of trazodone-associated adverse effects1 182

Caution; consider decreased trazodone dosage1 182

Vardenafil

Increased vardenafil concentrations and AUC and increased risk of vardenafil-associated adverse effects (e.g., hypotension, visual changes, prolonged erection); decreased indinavir concentrations108 183

When using indinavir (without ritonavir), do not exceed a single vardenafil dosage of 2.5 mg in 24 hours;1 183 some experts recommend an initial vardenafil dosage of 2.5 mg in 72 hours108

Venlafaxine

Decreased indinavir concentrations; no change in venlafaxine concentrations1

Clinical importance unknown1

Vitamin C

Decreased indinavir concentrations with vitamin C dosage ≥1 g daily108

Monitor virologic response108

Zidovudine

Clinically important pharmacokinetic interactions unlikely1 108

In vitro evidence of synergistic antiretroviral effects1

Indinavir Sulfate Pharmacokinetics

Absorption

Bioavailability

Well absorbed from GI tract; peak plasma concentrations attained within 1 hour.1 37 38

Food

Presence of food in the GI tract can substantially decrease the extent of absorption of oral indinavir.1 38

Administration with a substantial meal (48.6 g fat, 31.3 g protein; 784 kcal) decreases AUC and peak plasma concentrations by 77 and 84%, respectively; administration with a light meal (e.g., dry toast with jelly, apple juice, coffee with skim milk and sugar; corn flakes with skim milk and sugar) is not associated with clinically important changes in AUC or peak or trough plasma concentrations.1 135

Special Populations

Hepatic impairment: AUC 60% higher in adults with cirrhosis and mild to moderate hepatic impairment compared with adults with normal hepatic function.1

Pregnant women: AUC 74% lower in pregnant women receiving indinavir (without low-dose ritonavir) compared with nonpregnant patients.1

Distribution

Extent

Not fully characterized.65

Distributed into CSF in low concentration in adults21 132 or children.125 134

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

Plasma Protein Binding

60%.1

Elimination

Metabolism

Metabolized by CYP3A4.1

Elimination Route

Excreted principally in the feces (83%) as unabsorbed drug or metabolites.1

Half-life

1.8 hours.1 37 38

Special Populations

Pharmacokinetics not studied in patients with severe hepatic impairment.1 AUC may be increased and half-life prolonged in patients with hepatic impairment.1 Half-life of 2.8 hours reported in adults with cirrhosis and mild to moderate hepatic impairment.1

Pharmacokinetics not studied in renal impairment.1

Stability

Storage

Oral

Capsules

15–30°C in tightly closed containers.1 Protect from moisture.1 Dispense and store in original container; the desiccant should remain in the original bottle.1

Actions and SpectrumActions

  • Pharmacologically related to other PIs (e.g., atazanavir, fosamprenavir, lopinavir, nelfinavir, ritonavir, saquinavir); differs structurally from these drugs and also differs pharmacologically and structurally from other currently available antiretrovirals.2 3

  • Active against HIV-1 and HIV-2.1 2 3 6 7

  • Inhibits replication of HIV-1 and HIV-2 by interfering with HIV protease.1 2 3 6 7

  • HIV-1 with reduced susceptibility to indinavir have been selected in vitro and have emerged during therapy with the drug.1 3 8 9 10 12 13 14 15 16 51

  • Varying degrees of cross-resistance occur among PIs; only limited data available to date regarding cross-resistance between indinavir and other PIs.1 4 5 7 9 10 11 13 39 168

  • Cross-resistance between indinavir 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 indinavir 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 46 HIV transmission via sexual contact or sharing needles is not prevented by antiretrovirals.1

  • Importance of taking on an empty stomach or with a light meal.1

  • Importance of drinking 1.5 L of liquids daily.1

  • Importance of storing indinavir in the original container; the desiccant should remain in the bottle.1

  • Importance of reading the patient package insert from the manufacturer.1

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

  • 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.

Indinavir Sulfate

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Oral

Capsules

100 mg (of indinavir)

Crixivan

Merck

200 mg (of indinavir)

Crixivan

Merck

333 mg (of indinavir)

Crixivan

Merck

400 mg (of indinavir)

Crixivan

Merck

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.

Crixivan 200MG Capsules (MERCK SHARP &amp; DOHME): 360/$475.98 or 1080/$1414.95

Crixivan 400MG Capsules (MERCK SHARP &amp; DOHME): 90/$239.99 or 270/$719.98

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 October 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. Merck & Company Inc. Crixivan (indinavir sulfate) capsules prescribing information. Whitehouse Station, NJ; 2008 Oct.

2. Dorsey BD, Levin RB, McDaniel SL et al. L-735,524: the design of a potent and orally bioavailable HIV protease inhibitor. J Med Chem. 1994; 37:3443-51. [PubMed 7932573]

3. Vacca JP, Dorsey BD, Schleif WA et al. L-735,524: an orally bioavailable human immunodeficiency virus type 1 protease inhibitor. Proc Natl Acad Sci USA. 1994; 91:4096-100. [PubMed 8171040]

4. Anon. New drugs for HIV infection. Med Lett Drugs Ther. 1996; 38:35-8. [PubMed 8606677]

5. Abbott Laboratories. Norvir (ritonavir) soft gelatin capsules and oral solution prescribing information. North Chicago, IL; 2001 Sept.

6. 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.

7. Chen Z, Li Y, Schock HB et al. Three-dimensional structure of a mutant HIV-1 protease displaying cross-resistance to all protease inhibitors in clinical trials. J Biol Chem. 1995; 270:21433-6. [PubMed 7665551]

8. Condra JH, Holder DJ, Schleif WA et al. Genetic correlates of in vivo viral resistance to indinavir, a human immunodeficiency virus type 1 protease inhibitor. J Virol. 1996; 70:8270-6. [PubMed 8970946]

9. Tisdale M, Myers RE, Maschera B et al. Cross-resistance analysis of human immunodeficiency virus type 1 variants individually selected for resistance to five different protease inhibitors. Antimicrob Agents Chemother. 1995; 39:1704-10. [PubMed 7486905]

10. Condra JH, Schleif WA, Blahy OM et al. In vivo emergence of HIV-1 variants resistant to multiple protease inhibitors. Nature. 1995; 374:569-71. [PubMed 7700387]

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

12. Mellors JW, McMahon DK, Chodakewitz JA et al. Correlation between genotypic evidence of HIV-1 resistance to the protease inhibitor MK-639 and loss of anti-retroviral effect in treated patients. J Acquir Immune Defic Syndr Hum Retrovirol. 1995; 10(Suppl 3):S35.

13. Gulnik SV, Suvorov LI, Liu B et al. Kinetic characterization and cross-resistance patterns of HIV-1 protease mutants selected under drug pressure. Biochemistry. 1995; 34:9282-7. [PubMed 7626598]

14. Goebel FD. Combination therapy from a clinician’s perspective. J Acquir Immune Defic Syndr Hum Retrovirol. 1995; 10(Suppl 1):S62-8. [PubMed 8595513]

15. Condra JH, Schleif WA, Blahy OM et al. Dynamics of acquired HIV-1 clinical resistance to the protease inhibitor MK-639. J Acquir Immune Defic Syndr Hum Retrovirol. 1995; 10(Suppl 3):S35-6.

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183. GlaxoSmithKline. Levitra (vardenafil HCL) tablets prescribing information. Research Triangle Park, NC; 2003 Aug.

184. Centers for Disease Control and Prevention. Antiretroviral postexposure prophylaxis after sexual, injection-drug use, or other nonoccupational exposure to HIV in the United States: Recommendations from the U.S. Department of Health and Human Services. MMWR Recomm Rep. 2005; 54 (No. RR-2):1-19.

185. Tibotec. Prezista (darunavir) prescribing information. Raritan, NJ; 2006 Jun.

b. GlaxoSmithKline. Agenerase (amprenavir) capsules prescribing information. Research Triangle Park, NC; 2005 May.

d. Gilead Sciences Inc. Viread (tenofovir disoproxil fumarate) tablets prescribing information. Foster City, CA; 2004 Jun.

e. Bristol-Myers Squibb. Reyataz (atazanavir sulfate) prescribing information. Princeton, NJ; 2004 Oct.

f. GlaxoSmithKline. Lexiva (fosamprenavir calcium) tablets prescribing information. Research Triangle Park, NC; 2005 Nov.

g. Tibotec Therapeutics. Intelence (etravirine) tablets prescribing information. Raritan, NJ; 2008 Jan.

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