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Concomitant use of CRIXIVAN with [[lovastatin]] or [[simvastatin]] is contraindicated due to an increased risk of [[myopathy]] including [[rhabdomyolysis]]. Caution should be exercised if CRIXIVAN is used concurrently with [[atorvastatin]] or [[rosuvastatin]]. Titrate the [[atorvastatin]] and [[rosuvastatin]] doses carefully and use the lowest necessary dose with CRIXIVAN.  
Concomitant use of CRIXIVAN with [[lovastatin]] or [[simvastatin]] is contraindicated due to an increased risk of [[myopathy]] including [[rhabdomyolysis]]. Caution should be exercised if CRIXIVAN is used concurrently with [[atorvastatin]] or [[rosuvastatin]]. Titrate the [[atorvastatin]] and [[rosuvastatin]] doses carefully and use the lowest necessary dose with CRIXIVAN.  


[[Midazolam]] is extensively metabolized by [[CYP3A4]]. Co-administration with CRIXIVAN with or without ritonavir may cause a large increase in the concentration of this benzodiazepine. No drug interaction study has been performed for the co-administration of CRIXIVAN with benzodiazepines. Based on data from other CYP3A4 inhibitors, plasma concentrations of midazolam are expected to be significantly higher when midazolam is given orally. Therefore CRIXIVAN should not be co-administered with orally administered midazolam (see CONTRAINDICATIONS), whereas caution should be used with co-administration of CRIXIVAN and parenteral midazolam. Data from concomitant use of parenteral midazolam with other protease inhibitors suggest a possible 3-4 fold increase in midazolam plasma levels. If CRIXIVAN with or without ritonavir is co-administered with parenteral midazolam, it should be done in a setting which ensures close clinical monitoring and appropriate medical management in case of respiratory depression and/or prolonged sedation. Dosage reduction for midazolam should be considered, especially if more than a single dose of midazolam is administered.
[[Midazolam]] is extensively metabolized by [[CYP3A4]]. Co-administration with CRIXIVAN with or without [[ritonavir]] may cause a large increase in the concentration of this [[benzodiazepine]]. No drug interaction study has been performed for the co-administration of CRIXIVAN with [[benzodiazepines]]. Based on data from other [[CYP3A4]] inhibitors, plasma concentrations of [[midazolam]] are expected to be significantly higher when midazolam is given orally. Therefore CRIXIVAN should not be co-administered with orally administered [[midazolam]], whereas caution should be used with co-administration of CRIXIVAN and parenteral [[midazolam]]. Data from concomitant use of parenteral [[midazolam]] with other [[protease inhibitors]] suggest a possible 3-4 fold increase in midazolam plasma levels. If CRIXIVAN with or without [[ritonavir]] is co-administered with parenteral [[midazolam]], it should be done in a setting which ensures close clinical monitoring and appropriate medical management in case of respiratory depression and/or prolonged sedation. Dosage reduction for midazolam should be considered, especially if more than a single dose of [[midazolam]] is administered.


Particular caution should be used when prescribing sildenafil, tadalafil, or vardenafil in patients receiving indinavir. Coadministration of CRIXIVAN with these medications is expected to substantially increase plasma concentrations of sildenafil, tadalafil, and vardenafil and may result in an increase in adverse events, including hypotension, visual changes, and priapism, which have been associated with sildenafil, tadalafil, and vardenafil (see CONTRAINDICATIONS and PRECAUTIONS, DRUG INTERACTIONS and INFORMATION FOR PATIENTS, and the manufacturer's complete prescribing information for sildenafil, tadalafil, or vardenafil).
Particular caution should be used when prescribing [[sildenafil]], [[tadalafil]], or [[vardenafil]] in patients receiving indinavir. Coadministration of CRIXIVAN with these medications is expected to substantially increase plasma concentrations of [[sildenafil]], [[tadalafil]], and [[vardenafil]] and may result in an increase in adverse events, including [[hypotension]], visual changes, and [[priapism]], which have been associated with [[sildenafil]], [[tadalafil]], and [[vardenafil]].


Concomitant use of CRIXIVAN and St. John's wort (Hypericum perforatum) or products containing St. John's wort is not recommended. Coadministration of CRIXIVAN and St. John's wort has been shown to substantially decrease indinavir concentrations (see CLINICAL PHARMACOLOGY, DRUG INTERACTIONS) and may lead to loss of virologic response and possible resistance to CRIXIVAN or to the class of protease inhibitors.
Concomitant use of CRIXIVAN and [[St. John's wort]] ([[Hypericum perforatum]]) or products containing [[St. John's wort]] is not recommended. Coadministration of CRIXIVAN and [[St. John's wort]] has been shown to substantially decrease indinavir concentrations and may lead to loss of virologic response and possible resistance to CRIXIVAN or to the class of [[protease inhibitors]].
|alcohol=Alcohol-Indinavir interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.
|alcohol=Alcohol-Indinavir interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.
}}
}}

Revision as of 15:36, 2 February 2015

Indinavir
Adult Indications & Dosage
Pediatric Indications & Dosage
Contraindications
Warnings & Precautions
Adverse Reactions
Drug Interactions
Use in Specific Populations
Administration & Monitoring
Overdosage
Pharmacology
Clinical Studies
How Supplied
Images
Patient Counseling Information
Precautions with Alcohol
Brand Names
Look-Alike Names

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Alberto Plate [2]

Disclaimer

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Overview

Indinavir is an antiretroviral agent and protease inhibitor that is FDA approved for the treatment of HIV infection in combination with other antiretroviral agents. Common adverse reactions include abdominal pain, heartburn, loss of appetite, nausea, taste sense altered, vomiting, neutrophil count abnormal, hyperbilirubinemia and headache.

Adult Indications and Dosage

FDA-Labeled Indications and Dosage (Adult)

There is limited information regarding Indinavir FDA-Labeled Indications and Dosage (Adult) in the drug label.

Off-Label Use and Dosage (Adult)

Guideline-Supported Use

There is limited information regarding Off-Label Guideline-Supported Use of Indinavir in adult patients.

Non–Guideline-Supported Use

There is limited information regarding Off-Label Non–Guideline-Supported Use of Indinavir in adult patients.

Pediatric Indications and Dosage

FDA-Labeled Indications and Dosage (Pediatric)

There is limited information regarding Indinavir FDA-Labeled Indications and Dosage (Pediatric) in the drug label.

Off-Label Use and Dosage (Pediatric)

Guideline-Supported Use

There is limited information regarding Off-Label Guideline-Supported Use of Indinavir in pediatric patients.

Non–Guideline-Supported Use

There is limited information regarding Off-Label Non–Guideline-Supported Use of Indinavir in pediatric patients.

Contraindications

CRIXIVAN is contraindicated in patients with clinically significant hypersensitivity to any of its components.

Inhibition of CYP3A4 by CRIXIVAN can result in elevated plasma concentrations of the following drugs, potentially causing serious or life-threatening reactions:

Warnings

ALERT: Find out about medicines that should NOT be taken with CRIXIVAN. This statement is included on the product's bottle label.

Nephrolithiasis/Urolithiasis

Nephrolithiasis/urolithiasis has occurred with CRIXIVAN therapy. The cumulative frequency of nephrolithiasis is substantially higher in pediatric patients (29%) than in adult patients (12.4%; range across individual trials: 4.7% to 34.4%). The cumulative frequency of nephrolithiasis events increases with increasing exposure to CRIXIVAN; however, the risk over time remains relatively constant. In some cases, nephrolithiasis/urolithiasis has been associated with renal insufficiency or acute renal failure, pyelonephritis with or without bacteremia. If signs or symptoms of nephrolithiasis/urolithiasis occur, (including flank pain, with or without hematuria or microscopic hematuria), temporary interruption (e.g., 1-3 days) or discontinuation of therapy may be considered. Adequate hydration is recommended in all patients treated with CRIXIVAN.

Hemolytic Anemia

Acute hemolytic anemia, including cases resulting in death, has been reported in patients treated with CRIXIVAN. Once a diagnosis is apparent, appropriate measures for the treatment of hemolytic anemia should be instituted, including discontinuation of CRIXIVAN.

Hepatitis

Hepatitis including cases resulting in hepatic failure and death has been reported in patients treated with CRIXIVAN. Because the majority of these patients had confounding medical conditions and/or were receiving concomitant therapy(ies), a causal relationship between CRIXIVAN and these events has not been established.

Hyperglycemia

New onset diabetes mellitus, exacerbation of pre-existing diabetes mellitus and hyperglycemia have been reported during post-marketing surveillance in HIV-infected patients receiving protease inhibitor therapy. Some patients required either initiation or dose adjustments of insulin or oral hypoglycemic agents for treatment of these events. In some cases, diabetic ketoacidosis has occurred. In those patients who discontinued protease inhibitor therapy, hyperglycemia persisted in some cases. Because these events have been reported voluntarily during clinical practice, estimates of frequency cannot be made and a causal relationship between protease inhibitor therapy and these events has not been established.

Drug Interactions

Concomitant use of CRIXIVAN with lovastatin or simvastatin is contraindicated due to an increased risk of myopathy including rhabdomyolysis. Caution should be exercised if CRIXIVAN is used concurrently with atorvastatin or rosuvastatin. Titrate the atorvastatin and rosuvastatin doses carefully and use the lowest necessary dose with CRIXIVAN.

Midazolam is extensively metabolized by CYP3A4. Co-administration with CRIXIVAN with or without ritonavir may cause a large increase in the concentration of this benzodiazepine. No drug interaction study has been performed for the co-administration of CRIXIVAN with benzodiazepines. Based on data from other CYP3A4 inhibitors, plasma concentrations of midazolam are expected to be significantly higher when midazolam is given orally. Therefore CRIXIVAN should not be co-administered with orally administered midazolam, whereas caution should be used with co-administration of CRIXIVAN and parenteral midazolam. Data from concomitant use of parenteral midazolam with other protease inhibitors suggest a possible 3-4 fold increase in midazolam plasma levels. If CRIXIVAN with or without ritonavir is co-administered with parenteral midazolam, it should be done in a setting which ensures close clinical monitoring and appropriate medical management in case of respiratory depression and/or prolonged sedation. Dosage reduction for midazolam should be considered, especially if more than a single dose of midazolam is administered.

Particular caution should be used when prescribing sildenafil, tadalafil, or vardenafil in patients receiving indinavir. Coadministration of CRIXIVAN with these medications is expected to substantially increase plasma concentrations of sildenafil, tadalafil, and vardenafil and may result in an increase in adverse events, including hypotension, visual changes, and priapism, which have been associated with sildenafil, tadalafil, and vardenafil.

Concomitant use of CRIXIVAN and St. John's wort (Hypericum perforatum) or products containing St. John's wort is not recommended. Coadministration of CRIXIVAN and St. John's wort has been shown to substantially decrease indinavir concentrations and may lead to loss of virologic response and possible resistance to CRIXIVAN or to the class of protease inhibitors.

Adverse Reactions

Clinical Trials Experience

There is limited information regarding Indinavir Clinical Trials Experience in the drug label.

Postmarketing Experience

There is limited information regarding Indinavir Postmarketing Experience in the drug label.

Drug Interactions

There is limited information regarding Indinavir Drug Interactions in the drug label.

Use in Specific Populations

Pregnancy

Pregnancy Category (FDA): There is no FDA guidance on usage of Indinavir in women who are pregnant.
Pregnancy Category (AUS): There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Indinavir in women who are pregnant.

Labor and Delivery

There is no FDA guidance on use of Indinavir during labor and delivery.

Nursing Mothers

There is no FDA guidance on the use of Indinavir in women who are nursing.

Pediatric Use

There is no FDA guidance on the use of Indinavir in pediatric settings.

Geriatic Use

There is no FDA guidance on the use of Indinavir in geriatric settings.

Gender

There is no FDA guidance on the use of Indinavir with respect to specific gender populations.

Race

There is no FDA guidance on the use of Indinavir with respect to specific racial populations.

Renal Impairment

There is no FDA guidance on the use of Indinavir in patients with renal impairment.

Hepatic Impairment

There is no FDA guidance on the use of Indinavir in patients with hepatic impairment.

Females of Reproductive Potential and Males

There is no FDA guidance on the use of Indinavir in women of reproductive potentials and males.

Immunocompromised Patients

There is no FDA guidance one the use of Indinavir in patients who are immunocompromised.

Administration and Monitoring

Administration

There is limited information regarding Indinavir Administration in the drug label.

Monitoring

There is limited information regarding Indinavir Monitoring in the drug label.

IV Compatibility

There is limited information regarding the compatibility of Indinavir and IV administrations.

Overdosage

There is limited information regarding Indinavir overdosage. If you suspect drug poisoning or overdose, please contact the National Poison Help hotline (1-800-222-1222) immediately.

Pharmacology

There is limited information regarding Indinavir Pharmacology in the drug label.

Mechanism of Action

There is limited information regarding Indinavir Mechanism of Action in the drug label.

Structure

There is limited information regarding Indinavir Structure in the drug label.

Pharmacodynamics

There is limited information regarding Indinavir Pharmacodynamics in the drug label.

Pharmacokinetics

There is limited information regarding Indinavir Pharmacokinetics in the drug label.

Nonclinical Toxicology

There is limited information regarding Indinavir Nonclinical Toxicology in the drug label.

Clinical Studies

There is limited information regarding Indinavir Clinical Studies in the drug label.

How Supplied

There is limited information regarding Indinavir How Supplied in the drug label.

Storage

There is limited information regarding Indinavir Storage in the drug label.

Images

Drug Images

{{#ask: Page Name::Indinavir |?Pill Name |?Drug Name |?Pill Ingred |?Pill Imprint |?Pill Dosage |?Pill Color |?Pill Shape |?Pill Size (mm) |?Pill Scoring |?NDC |?Drug Author |format=template |template=DrugPageImages |mainlabel=- |sort=Pill Name }}

Package and Label Display Panel

{{#ask: Label Page::Indinavir |?Label Name |format=template |template=DrugLabelImages |mainlabel=- |sort=Label Page }}

Patient Counseling Information

There is limited information regarding Indinavir Patient Counseling Information in the drug label.

Precautions with Alcohol

Alcohol-Indinavir interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.

Brand Names

There is limited information regarding Indinavir Brand Names in the drug label.

Look-Alike Drug Names

There is limited information regarding Indinavir Look-Alike Drug Names in the drug label.

Drug Shortage Status

Price

References

The contents of this FDA label are provided by the National Library of Medicine.


Indinavir
CRIXIVAN® FDA Package Insert
Description
Clinical Pharmacology
Microbiology
Indications and Usage
Contraindications
Warnings and Precautions
Adverse Reactions
Overdosage
Dosage and Administration
How Supplied
Labels and Packages

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [3]; Associate Editor(s)-in-Chief: Mohamed Moubarak, M.D. [4]

Overview

Indinavir (IDV; trade name Crixivan, manufactured by Merck) is a protease inhibitor used as a component of highly active antiretroviral therapy (HAART) to treat HIV infection and AIDS.

Category

Protease inhibitor

US Brand Names

CRIXIVAN®

FDA Package Insert

Description | Clinical Pharmacology | Microbiology | Indications and Usage | Contraindications | Warnings and Precautions | Adverse Reactions | Overdosage | Dosage and Administration | How Supplied

Mechanism of Action

HIV-1 protease is an enzyme required for the proteolytic cleavage of the viral polyprotein precursors into the individual functional proteins found in infectious HIV-1. Indinavir binds to the protease active site and inhibits the activity of the enzyme. This inhibition prevents cleavage of the viral polyproteins resulting in the formation of immature non-infectious viral particles.[1]

References

  1. "CRIXIVAN (INDINAVIR SULFATE) CAPSULE [MERCK SHARP & DOHME CORP.]". Text " accessdate" ignored (help)