Drug/Small Molecule:
indinavir

PharmGKB contains no dosing guidelines for this drug/small molecule. To report known genotype-based dosing guidelines, or if you are interested in developing guidelines, click here.

PharmGKB gathers information regarding PGx on FDA drug labels from the FDA's "Table of Pharmacogenomic Biomarkers in Drug Labels", and from FDA-approved FDA and EMA-approved (European Medicines Agency) EMA labels brought to our attention. Excerpts from the label and downloadable highlighted label PDFs are manually curated by PharmGKB.

Please note that some drugs may have been removed from or added to the FDA's "Table of Pharmacogenomic Biomarkers in Drug Labels" without our knowledge. We periodically check the table for additions to this table and update PharmGKB accordingly.

There is currently no such list for European drug labels - we are working with the EMA to establish a list of European Public Assessment Reports (EPAR)s that contain PGx information. We are constructing this list by initially searching for drugs for which we have PGx-containing FDA drug labels - of these 44 EMA EPARs were identified and are being curated for pgx information.

We welcome any information regarding drug labels containing PGx information approved by the FDA, EMA or other Medicine Agencies around the world - please contact feedback.


last updated 09/16/2014

European Medicines Agency (EMA) Label for indinavir and CYP3A4

Informative PGx

Summary

The EMA European Public Assessment Report (EPAR) for indinavir (Crixivan) does not contain pharmacogenetic information. It contains information regarding metabolism by CYP3A4 and contraindicates concomitant use of drugs that are CYP3A4 substrates.

Annotation

The EMA-approved drug indinavir is tagged with CYP3A4 in [Article:24433361].

For the complete drug label text with sections containing pharmacogenetic information highlighted, see the indinavir EMA drug label.

*Disclaimer: The contents of this page have not been endorsed by the EMA and are the sole responsibility of PharmGKB.

Genes and/or phenotypes found in this label

  • CYP3A4
    • Contraindications section, Drug interactions section, Pharmacokinetics section, Warnings and precautions section, toxicity, metabolism/PK
    • source: European Medicines Agency (EMA) Label

Links to Unannotated Labels

These links are to labels associated with indinavir that have not been annotated by PharmGKB.

  1. DailyMed - DrugLabel PA166105162

PharmGKB contains no Clinical Variants that meet the highest level of criteria.

To see more Clinical Variants with lower levels of criteria, click the button at the bottom of the page.

Disclaimer: The PharmGKB's clinical annotations reflect expert consensus based on clinical evidence and peer-reviewed literature available at the time they are written and are intended only to assist clinicians in decision-making and to identify questions for further research. New evidence may have emerged since the time an annotation was submitted to the PharmGKB. The annotations are limited in scope and are not applicable to interventions or diseases that are not specifically identified.

The annotations do not account for individual variations among patients, and cannot be considered inclusive of all proper methods of care or exclusive of other treatments. It remains the responsibility of the health-care provider to determine the best course of treatment for a patient. Adherence to any guideline is voluntary, with the ultimate determination regarding its application to be made solely by the clinician and the patient. PharmGKB assumes no responsibility for any injury or damage to persons or property arising out of or related to any use of the PharmGKB clinical annotations, or for any errors or omissions.

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This is a non-comprehensive list of genetic tests with pharmacogenetics relevance, typically submitted by the manufacturer and manually curated by PharmGKB. The information listed is provided for educational purposes only and does not constitute an endorsement of any listed test or manufacturer.

A more complete listing of genetic tests is found at the Genetic Testing Registry (GTR).

PGx Test Variants Assayed Gene?

The table below contains information about pharmacogenomic variants on PharmGKB. Please follow the link in the "Variant" column for more information about a particular variant. Each link in the "Variant" column leads to the corresponding PharmGKB Variant Page. The Variant Page contains summary data, including PharmGKB manually curated information about variant-drug pairs based on individual PubMed publications. The PMIDs for these PubMed publications can be found on the Variant Page.

The tags in the first column of the table indicate what type of information can be found on the corresponding Variant Page.

Links in the "Gene" column lead to PharmGKB Gene Pages.

Gene ? Variant?
(138)
Alternate Names / Tag SNPs ? Drugs ? Alleles ?
(+ chr strand)
Function ? Amino Acid?
Translation
No VIP available No Clinical Annotations available VA
rs11568695 3609G>A, 8786216C>T, 95696540C>T, Ala1203=
C > T
Synonymous
Ala1203Ala
No VIP available CA VA
rs2740574 -392G>A, 37414939C>T, 4713G>A, 5'-flanking region -392A>G, 99382096C>T, CYP3A4*1B, CYP3A4-V, CYP3A4:-392A>G
C > T
5' Flanking
rs4148323 175755G>A, 211G>A, 234669144G>A, 61-6536G>A, 615403G>A, 856-6536G>A, 862-6536G>A, 868-6536G>A, Gly71Arg, UGT1A1*6, UGT1A1: G71R, UGT1A1:211G>A, UGT1A1:G211A, UGT1A1:Gly71Arg
G > A
Intronic
Gly71Arg
VIP No Clinical Annotations available No Variant Annotations available
rs776746 12083G>A, 219-237G>A, 321-1G>A, 37303382C>T, 581-237G>A, 689-1G>A, 99270539C>T, CYP3A5*1, CYP3A5*3, CYP3A5*3C, CYP3A5:6986A>G, g.6986A>G, intron 3 splicing defect, rs776746 A>G
C > T
Acceptor
rs8175347 233760235_233760236TA[5][6][7][8], 5-TA insertion in promoter, 7-TA insertion in promoter, 8-TA insertion in promoter, UGT1A1*28, UGT1A1*36, UGT1A1*37, microsatellite, short tandem repeat
(TA)6 > (TA)8
(TA)6 > (TA)5
(TA)6 > (TA)7
Not Available
Alleles, Functions, and Amino Acid Translations are all sourced from dbSNP 138
2D structure from PubChem
provided by PubChem

Overview

Generic Names
  • Compound J
  • Indinavir sulfate
Trade Names
  • Crixivan
Brand Mixture Names

PharmGKB Accession Id:
PA449977

Description

A potent and specific HIV protease inhibitor that appears to have good oral bioavailability.

Source: Drug Bank

Indication

Indinavir is an antiretroviral drug for the treatment of HIV infection.

Source: Drug Bank

Other Vocabularies

Information pulled from DrugBank has not been reviewed by PharmGKB.

Pharmacology, Interactions, and Contraindications

Mechanism of Action

Indinavir inhibits the HIV viral protease enzyme which prevents cleavage of the gag-pol polyprotein, resulting in noninfectious, immature viral particles.

Source: Drug Bank

Pharmacology

Indinavir is a protease inhibitor with activity against Human Immunodeficiency Virus Type 1 (HIV-1). Protease inhibitors block the part of HIV called protease. 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. Protease inhibitors are almost always used in combination with at least two other anti-HIV drugs.

Source: Drug Bank

Food Interaction

Avoid taking with grapefruit juice|Avoid excessive or chronic alcohol use.|Take on empty stomach: 1 hour before or 2 hours after meals.|Take with a full glass of water.

Source: Drug Bank

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Hepatic. Seven metabolites have been identified, one glucuronide conjugate and six oxidative metabolites. In vitro studies indicate that cytochrome P-450 3A4 (CYP3A4) is the major enzyme responsible for formation of the oxidative metabolites.

Source: Drug Bank

Protein Binding

60%

Source: Drug Bank

Absorption

Rapidly absorbed

Source: Drug Bank

Half-Life

1.8 (+/- 0.4) hours

Source: Drug Bank

Toxicity

Symptoms of overdose include myocardial infarction and angina pectoris.

Source: Drug Bank

Route of Elimination

Less than 20% of indinavir is excreted unchanged in the urine.

Source: Drug Bank

Chemical Properties

Chemical Formula

C36H47N5O4

Source: Drug Bank

Isomeric SMILES

CC(C)(C)NC(=O)[C@@H]1CN(CCN1C[C@H](C[C@@H](Cc2ccccc2)C(=O)N[C@H]3c4ccccc4C[C@H]3O)O)Cc5cccnc5

Source: OpenEye

Canonical SMILES

CC(C)(C)NC(=O)[C@@H]1CN(CC2=CN=CC=C2)CCN1C[C@@H]

Source: Drug Bank

Average Molecular Weight

613.7895

Source: Drug Bank

Monoisotopic Molecular Weight

613.362805017

Source: Drug Bank

Genes that are associated with this drug in PharmGKB's database based on (1) variant annotations, (2) literature review, (3) pathways or (4) information automatically retrieved from DrugBank, depending on the "evidence" and "source" listed below.

Curated Information ?

Drug Interactions

Drug Description
indinavir The serum concentration of Abacavir may be decreased by protease inhibitors such as Indinavir. The antiviral response should be closely monitored. (source: Drug Bank)
indinavir The serum concentration of Abacavir may be decreased by protease inhibitors such as Indinavir. The antiviral response should be closely monitored. (source: Drug Bank)
indinavir The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
indinavir The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
indinavir Indinavir increases the effect and toxicity of amiodarone (source: Drug Bank)
indinavir Indinavir increases the effect and toxicity of amiodarone (source: Drug Bank)
indinavir Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
indinavir Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
indinavir Increased risk of hyperbilirubinemia with this association (source: Drug Bank)
indinavir Increased risk of hyperbilirubinemia with this association (source: Drug Bank)
indinavir Indinavir increases the effect and toxicity of atorvastatin (source: Drug Bank)
indinavir Indinavir increases the effect and toxicity of atorvastatin (source: Drug Bank)
indinavir Indinavir, a strong CYP3A4 inhibitor, may increase the serum concentration of bromazepam by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of bromazepam if indinavir is initiated, discontinued or dose changed. Dosage adjustments may be required. (source: Drug Bank)
indinavir The antiacid decreases the absorption of indinavir (source: Drug Bank)
indinavir The antiacid decreases the absorption of indinavir (source: Drug Bank)
indinavir Indinavir increases the effect and toxicity of carbamazepine (source: Drug Bank)
indinavir Indinavir increases the effect and toxicity of carbamazepine (source: Drug Bank)
indinavir The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
indinavir The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
indinavir Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
indinavir Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
indinavir Increases the effect and toxicity of indinavir (source: Drug Bank)
indinavir Increases the effect and toxicity of indinavir (source: Drug Bank)
indinavir The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
indinavir The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
indinavir The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
indinavir The protease inhibitor increases the effect of cyclosporine (source: Drug Bank)
indinavir The protease inhibitor, indinavir, may increase the effect of cyclosporine. (source: Drug Bank)
indinavir Indinavir may increase the serum concentration of dantrolene by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of dantrolene if indinavir is initiated, discontinued or dose changed. (source: Drug Bank)
indinavir Increases the effect of indinavir (source: Drug Bank)
indinavir Increases the effect of indinavir (source: Drug Bank)
indinavir The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
indinavir The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
indinavir Indinavir increases the effect and toxicity of ergot derivative (source: Drug Bank)
indinavir Indinavir increases the effect and toxicity of ergot derivative (source: Drug Bank)
indinavir Efavirenz decreases the effect of indinavir (source: Drug Bank)
indinavir Efavirenz decreases the effect of indinavir (source: Drug Bank)
indinavir Indinavir increases the effect and toxicity of ergot derivative (source: Drug Bank)
indinavir Indinavir increases the effect and toxicity of ergot derivative (source: Drug Bank)
indinavir This CYP3A4 inhibitor increases levels/toxicity of erlotinib (source: Drug Bank)
indinavir This CYP3A4 inhibitor increases levels/toxicity of erlotinib (source: Drug Bank)
indinavir Omeprazole decreases the absorption of indinavir (source: Drug Bank)
indinavir Omeprazole decreases the absorption of indinavir (source: Drug Bank)
indinavir The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
indinavir The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
indinavir The protease inhibitor increases the effect and toxicity of fentanyl (source: Drug Bank)
indinavir The protease inhibitor, indinavir, may increase the effect and toxicity of fentanyl. (source: Drug Bank)
indinavir The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
indinavir The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
indinavir Indinavir increases the effect and toxicity of fusidic acid (source: Drug Bank)
acenocoumarol The protease inhibitor increases the anticoagulant effect (source: Drug Bank)
acenocoumarol The protease inhibitor, indinavir, may increase the anticoagulant effect of acenocoumarol. (source: Drug Bank)
alprazolam The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
alprazolam The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
aluminium The antacid decreases the absorption of indinavir (source: Drug Bank)
amiodarone Indinavir increases the effect and toxicity of amiodarone (source: Drug Bank)
amiodarone Indinavir increases the effect and toxicity of amiodarone (source: Drug Bank)
anisindione The protease inhibitor, indinavir, may increase the anticoagulant effect of anisindione. (source: Drug Bank)
astemizole Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
astemizole Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
atazanavir Increased risk of hyperbilirubinemia with this association (source: Drug Bank)
atazanavir Increased risk of hyperbilirubinemia with this association (source: Drug Bank)
atorvastatin Increases the effect and toxicity of atorvastatin (source: Drug Bank)
atorvastatin Increases the effect and toxicity of atorvastatin (source: Drug Bank)
Calcium The antacid decreases the absorption of indinavir (source: Drug Bank)
Calcium The antacid decreases the absorption of indinavir (source: Drug Bank)
carbamazepine Indinavir increases the effect and toxicity of carbamazepine (source: Drug Bank)
carbamazepine Indinavir increases the effect and toxicity of carbamazepine (source: Drug Bank)
chlordiazepoxide The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
chlordiazepoxide The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
cisapride Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
cisapride Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
clarithromycin Clarithromycin increases the effect and toxicity of indinavir (source: Drug Bank)
clarithromycin Clarithromycin increases the effect and toxicity of indinavir (source: Drug Bank)
clonazepam The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
clonazepam The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
clorazepate The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
cyclosporine The protease inhibitor increases the effect of cyclosporine (source: Drug Bank)
cyclosporine The protease inhibitor, indinavir, may increase the effect of cyclosporine. (source: Drug Bank)
delavirdine Delavirdine increases the effect of indinavir (source: Drug Bank)
delavirdine Delavirdine increases the effect of indinavir (source: Drug Bank)
diazepam The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
diazepam The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
dicumarol The protease inhibitor increases the anticoagulant effect (source: Drug Bank)
dicumarol The protease inhibitor, indinavir, may increase the anticoagulant effect of dicumarol. (source: Drug Bank)
dihydroergotamine Increases the effect and toxicity of the ergot derivative (source: Drug Bank)
efavirenz Efavirenz decreases the effect of indinavir (source: Drug Bank)
efavirenz Efavirenz decreases the effect of indinavir (source: Drug Bank)
ergotamine Increases the effect and toxicity of the ergot derivative (source: Drug Bank)
erlotinib This CYP3A4 inhibitor increases levels/toxicity of erlotinib (source: Drug Bank)
erlotinib This CYP3A4 inhibitor increases levels/toxicity of erlotinib (source: Drug Bank)
esomeprazole Omeprazole decreases the absorption of indinavir (source: Drug Bank)
esomeprazole Omeprazole decreases the absorption of indinavir (source: Drug Bank)
estazolam The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
estazolam The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
fentanyl The protease inhibitor increases the effect and toxicity of fentanyl (source: Drug Bank)
fentanyl The protease inhibitor, indinavir, may increase the effect and toxicity of fentanyl. (source: Drug Bank)
flurazepam The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
flurazepam The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
halazepam The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
ketoconazole Ketoconazole increases the efefct of indinavir (source: Drug Bank)
ketoconazole Ketoconazole increases the efefct of indinavir (source: Drug Bank)
lansoprazole Omeprazole decreases the absorption of indinavir (source: Drug Bank)
lansoprazole Omeprazole decreases the absorption of indinavir (source: Drug Bank)
Magnesium The antacid decreases the absorption of indinavir (source: Drug Bank)
Magnesium The antacid decreases the absorption of indinavir (source: Drug Bank)
magnesium oxide The antacid decreases the absorption of indinavir (source: Drug Bank)
midazolam The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
midazolam The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
omeprazole Omeprazole decreases the absorption of indinavir (source: Drug Bank)
omeprazole Omeprazole decreases the absorption of indinavir (source: Drug Bank)
pantoprazole Omeprazole decreases the absorption of indinavir (source: Drug Bank)
pantoprazole Omeprazole decreases the absorption of indinavir (source: Drug Bank)
pimozide The protease inhibitor increases the effect and toxicity of pimozide (source: Drug Bank)
pimozide The protease inhibitor, indinavir, may increase the effect and toxicity of pimozide. (source: Drug Bank)
prazepam The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
quazepam The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
quinupristin This combination presents an increased risk of toxicity (source: Drug Bank)
rabeprazole Omeprazole decreases the absorption of indinavir (source: Drug Bank)
rabeprazole Omeprazole decreases the absorption of indinavir (source: Drug Bank)
ranolazine Increased levels of ranolazine - risk of toxicity (source: Drug Bank)
rifabutin Rifabutin decreases the effect of indinavir (source: Drug Bank)
rifabutin Rifabutin decreases the effect of indinavir (source: Drug Bank)
rifampin Rifampin decreases the effect of indinavir (source: Drug Bank)
rifampin Rifampin decreases the effect of indinavir (source: Drug Bank)
risperidone Increased risk of extrapyramidal symptoms (source: Drug Bank)
risperidone Increased risk of extrapyramidal symptoms (source: Drug Bank)
saquinavir Possible antagonism of action (source: Drug Bank)
saquinavir Possible antagonism of action (source: Drug Bank)
sildenafil The protease inhibitor increases the effect and toxicity of sildenafil (source: Drug Bank)
sildenafil The protease inhibitor, indinavir, may increase the effect and toxicity of sildenafil. (source: Drug Bank)
sunitinib Possible increase in sunitinib levels (source: Drug Bank)
sunitinib Possible increase in sunitinib levels (source: Drug Bank)
tacrolimus Increases the effect and toxicity of tacrolimus (source: Drug Bank)
tacrolimus Increases the effect and toxicity of tacrolimus (source: Drug Bank)
terfenadine Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
terfenadine Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
trazodone This strong CYP3A4 inhibitor increases the effect and toxicity of trazodone (source: Drug Bank)
trazodone This strong CYP3A4 inhibitor increases the effect and toxicity of trazodone (source: Drug Bank)
triazolam The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
triazolam The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
vardenafil The protease inhibitor increases the effect and toxicity of vardenafil (source: Drug Bank)
vardenafil The protease inhibitor, indinavir, may increase the effect and toxicity of vardenafil. (source: Drug Bank)
vitamin c Vitamin C decreases indinavir levels (source: Drug Bank)
warfarin The protease inhibitor increases the anticoagulant effect (source: Drug Bank)
warfarin The protease inhibitor, indinavir, may increase the anticoagulant effect of warfarin. (source: Drug Bank)
indinavir Ketoconazole increases the effect of indinavir (source: Drug Bank)
indinavir Ketoconazole increases the effect of indinavir (source: Drug Bank)
indinavir Omeprazole decreases the absorption of indinavir (source: Drug Bank)
indinavir Omeprazole decreases the absorption of indinavir (source: Drug Bank)
indinavir Indinavir may increase the effect and toxicity of lovastatin. Concomitant therapy is contraindicated. (source: Drug Bank)
indinavir The antiacid decreases the absorption of indinavir (source: Drug Bank)
indinavir The antiacid decreases the absorption of indinavir (source: Drug Bank)
indinavir The protease inhibitor increases the effect of benzodiazepine (source: Drug Bank)
indinavir The protease inhibitor increases the effect of benzodiazepine (source: Drug Bank)
indinavir Omeprazole decreases the absorption of indinavir (source: Drug Bank)
indinavir Omeprazole decreases the absorption of indinavir (source: Drug Bank)
indinavir Omeprazole decreases the absorption of indinavir (source: Drug Bank)
indinavir Omeprazole decreases the absorption of indinavir (source: Drug Bank)
indinavir The protease inhibitor increases the effect and toxicity of pimozide (source: Drug Bank)
indinavir The protease inhibitor, indinavir, may increase the effect and toxicity of pimozide. (source: Drug Bank)
indinavir This combination presents an increased risk of toxicity (source: Drug Bank)
indinavir Omeprazole decreases the absorption of indinavir (source: Drug Bank)
indinavir Omeprazole decreases the absorption of indinavir (source: Drug Bank)
indinavir Increased levels of ranolazine - risk of toxicity (source: Drug Bank)
indinavir Rifabutin decreases the effect of indinavir (source: Drug Bank)
indinavir Rifabutin decreases the effect of indinavir (source: Drug Bank)
indinavir Rifampin decreases the effect of indinavir (source: Drug Bank)
indinavir Rifampin decreases the effect of indinavir (source: Drug Bank)
indinavir The protease inhibitor, Indinavir, may increase the blood concentration of Tacrolimus. Monitor for changes in the therapeutic/toxic effects of Tacrolimus if Indinavir therapy is initiated, discontinued or altered. (source: Drug Bank)
indinavir Indinavir may reduce the metabolism of Tadalafil. Concomitant therapy should be avoided if possible due to high risk of Tadalafil toxicity. (source: Drug Bank)
indinavir Indinavir may increase the serum concentration of Tamoxifen by decreasing its metabolism. Monitor for increased adverse/toxic effects of Tamoxifen. (source: Drug Bank)
indinavir Indinavir may increase the serum concentration of Tamoxifen by decreasing its metabolism. Monitor for increased adverse/toxic effects of Tamoxifen. (source: Drug Bank)
indinavir Indinavir, a CYP3A4 inhibitor, may decrease the metabolism and clearance of Tamsulosin, a CYP3A4 substrate. Monitor for changes in therapeutic/adverse effects of Tamsulosin if Indinavir is initiated, discontinued, or dose changed. (source: Drug Bank)
indinavir Indinavir, a CYP3A4 inhibitor, may decrease the metabolism and clearance of Tamsulosin, a CYP3A4 substrate. Monitor for changes in therapeutic/adverse effects of Tamsulosin if Indinavir is initiated, discontinued, or dose changed. (source: Drug Bank)
indinavir Indinavir may increase the plasma concentration of Telithromycin. Consider alternate therapy or monitor therapeutic/adverse effects. (source: Drug Bank)
indinavir Indinavir may inhibit the metabolism and clearance of Temsirolimus. Concomitant therapy should be avoided. (source: Drug Bank)
indinavir The strong CYP3A4 inhibitor, Indinavir, may decrease the metabolism and clearance of Teniposide, a CYP3A4 substrate. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Teniposide if Indinavir is initiated, discontinued or dose changed. (source: Drug Bank)
indinavir Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
indinavir Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
indinavir The strong CYP3A4 inhibitor, Indinavir, may decrease the metabolism and clearance of Tiagabine, a CYP3A4 substrate. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Tiagabine if Indinavir is initiated, discontinued or dose changed. (source: Drug Bank)
indinavir Indinavir may decrease the metabolism and clearance of Tolterodine. Adjust Tolterodine dose and monitor for efficacy and toxicity. (source: Drug Bank)
indinavir Indinavir may decrease the metabolism and clearance of Tolterodine. Adjust Tolterodine dose and monitor for efficacy and toxicity. (source: Drug Bank)
indinavir Indinavir may increase Tramadol toxicity by decreasing Tramadol metabolism and clearance. (source: Drug Bank)
indinavir The protease inhibitor, Indinavir, may increase the efficacy/toxicity of Trazodone by inhibiting Trazodone metabolism and clearance. Monitor for changes in Trazodone efficacy/toxicity if Indinavir is initiated, discontinued or dose changed. (source: Drug Bank)
indinavir This strong CYP3A4 inhibitor increases the effect and toxicity of trazodone (source: Drug Bank)
indinavir The protease inhibitor, Indinavir, may increase the efficacy/toxicity of Trazodone by inhibiting Trazodone metabolism and clearance. Monitor for changes in Trazodone efficacy/toxicity if Indinavir is initiated, discontinued or dose changed. (source: Drug Bank)
indinavir The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
indinavir The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
indinavir The strong CYP3A4 inhibitor, Indinavir, may decrease the metabolism and clearance of Trimipramine, a CYP3A4 substrate. Consider alternate therapy or monitor for changes in therapeutic and adverse effects of Trimipramine if Indinavir is initiated, discontinued or dose changed. (source: Drug Bank)
indinavir Indinavir, a potent CYP3A4 inhibitor, may decrease the metabolism and clearance of Vardenafil. Concomitant therapy is contraindicated. (source: Drug Bank)
indinavir Indinavir, a CYP3A4 inhibitor, may decrease the metabolism and clearance of Venlafaxine, a CYP3A4 substrate. Monitor for changes in therapeutic/adverse effects of Venlafaxine if Indinavir is initiated, discontinued, or dose changed. (source: Drug Bank)
indinavir Indinavir, a strong CYP3A4 inhibitor, may increase the serum concentration of Veramapil, a CYP3A4 substrate, by decreasing its metabolism and clearance. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Verapamil if Indinavir is initiated, discontinued or dose changed. (source: Drug Bank)
indinavir Indinavir, a strong CYP3A4 inhibitor, may decrease the metabolism of Vinblastine. Consider alternate therapy to avoid Vinblastine toxicity. Monitor for changes in the therapeutic/adverse effects of Vinblastine if Indinavir is initiated, discontinued or dose changed. (source: Drug Bank)
indinavir Indinavir, a strong CYP3A4 inhibitor, may increase the serum concentration of Vincristine by decreasing its metabolism. Consider alternate therapy to avoid Vincristine toxicity. Monitor for changes in the therapeutic and adverse effects of Vincristine if Indinavir is initiated, discontinued or dose changed. (source: Drug Bank)
indinavir Indinavir, a strong CYP3A4 inhibitor, may increase the serum concentration of Vinorelbine by decreasing its metabolism. Consider alternate therapy to avoid Vinorelbine toxicity. Monitor for changes in the therapeutic and adverse effects of Vinorelbine if Indinavir is initiated, discontinued or dose changed. (source: Drug Bank)
indinavir Voriconazole may increase the serum concentration of indinavir by decreasing its metabolism. Indinavir may increase the serum concentration of voriconazole. Monitor for changes in the therapeutic and adverse effects of both agents if concomitant therapy is initiated, discontinued or if doses are changed. (source: Drug Bank)
indinavir Indinavir, a strong CYP3A4 inhibitor, may increase the serum concentration of zolpidem by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of zolpidem if indinavir is initiated, discontinued or dose changed. (source: Drug Bank)
indinavir Indinavir, a strong CYP3A4 inhibitor, may increase the serum concentration of zonisamide by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of zonisamide if indinavir is initiated, discontinued or dose changed. (source: Drug Bank)
indinavir Indinavir, a strong CYP3A4 inhibitor, may increase the serum concentration of zopiclone by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of zopiclone if indinavir is initiated, discontinued or dose changed. (source: Drug Bank)

Curated Information ?

Relationships from National Drug File - Reference Terminology (NDF-RT)

May Treat
Contraindicated With

Publications related to indinavir: 38

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PharmGKB summary: very important pharmacogene information for UGT1A1. Pharmacogenetics and genomics. 2014. Barbarino Julia M, et al. PubMed
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PharmGKB summary: very important pharmacogene information for CYP3A5. Pharmacogenetics and genomics. 2012. Lamba Jatinder, et al. PubMed
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The Dual Role of Pharmacogenetics in HIV Treatment: Mutations and Polymorphisms Regulating Antiretroviral Drug Resistance and Disposition. Pharmacological reviews. 2012. Michaud Veronique, et al. PubMed
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HIV-1 antiretroviral drug therapy. Cold Spring Harbor perspectives in medicine. 2012. Arts Eric J, et al. PubMed
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Very important pharmacogene summary: ABCB1 (MDR1, P-glycoprotein). Pharmacogenetics and genomics. 2011. Hodges Laura M, et al. PubMed
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Nuclear receptor-mediated induction of CYP450 by antiretrovirals: functional consequences of NR1I2 (PXR) polymorphisms and differential prevalence in whites and sub-Saharan Africans. Journal of acquired immune deficiency syndromes (1999). 2010. Svärd Jenny, et al. PubMed
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Coprescription of tamoxifen and medications that inhibit CYP2D6. Journal of clinical oncology : official journal of the American Society of Clinical Oncology. 2010. Sideras Kostandinos, et al. PubMed
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Influence of pharmacogenetics on indinavir disposition and short-term response in HIV patients initiating HAART. European journal of clinical pharmacology. 2009. Bertrand Julie, et al. PubMed
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Histone deacetylase inhibitors induce a very broad, pleiotropic anticancer drug resistance phenotype in acute myeloid leukemia cells by modulation of multiple ABC transporter genes. Clinical cancer research : an official journal of the American Association for Cancer Research. 2009. Hauswald Stefanie, et al. PubMed
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Genetic determinants of response to clopidogrel and cardiovascular events. The New England journal of medicine. 2009. Simon Tabassome, et al. PubMed
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Redox regulation of multidrug resistance in cancer chemotherapy: molecular mechanisms and therapeutic opportunities. Antioxidants & redox signaling. 2009. Kuo Macus Tien. PubMed
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Several major antiepileptic drugs are substrates for human P-glycoprotein. Neuropharmacology. 2008. Luna-Tortós Carlos, et al. PubMed
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Structure, function and regulation of P-glycoprotein and its clinical relevance in drug disposition. Xenobiotica; the fate of foreign compounds in biological systems. 2008. Zhou S-F. PubMed
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Polymorphisms in the drug transporter gene ABCB1 predict antidepressant treatment response in depression. Neuron. 2008. Uhr Manfred, et al. PubMed
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Citalopram enantiomers in plasma and cerebrospinal fluid of ABCB1 genotyped depressive patients and clinical response: a pilot study. Pharmacological research : the official journal of the Italian Pharmacological Society. 2008. Nikisch Georg, et al. PubMed
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Cobalamin potentiates vinblastine cytotoxicity through downregulation of mdr-1 gene expression in HepG2 cells. Cellular physiology and biochemistry : international journal of experimental cellular physiology, biochemistry, and pharmacology. 2007. Marguerite Véronique, et al. PubMed
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Mechanism of inhibition of P-glycoprotein mediated efflux by vitamin E TPGS: influence on ATPase activity and membrane fluidity. Molecular pharmaceutics. 2007. Collnot Eva-Maria, et al. PubMed
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Orosomucoid (alpha1-acid glycoprotein) plasma concentration and genetic variants: effects on human immunodeficiency virus protease inhibitor clearance and cellular accumulation. Clinical pharmacology and therapeutics. 2006. Colombo Sara, et al. PubMed
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Pharmacogenetic characteristics of indinavir, zidovudine, and lamivudine therapy in HIV-infected adults: a pilot study. Journal of acquired immune deficiency syndromes (1999). 2006. Anderson Peter L, et al. PubMed
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Gefitinib modulates the function of multiple ATP-binding cassette transporters in vivo. Cancer research. 2006. Leggas Markos, et al. PubMed
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Impact of P-glycoprotein on clopidogrel absorption. Clinical pharmacology and therapeutics. 2006. Taubert Dirk, et al. PubMed
Relationship between hyperbilirubinaemia and UDP-glucuronosyltransferase 1A1 (UGT1A1) polymorphism in adult HIV-infected Thai patients treated with indinavir. Pharmacogenetics and genomics. 2006. Boyd Mark A, et al. PubMed
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Single nucleotide polymorphisms in human P-glycoprotein: its impact on drug delivery and disposition. Expert opinion on drug delivery. 2006. Dey Surajit. PubMed
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Overview of the pharmacogenetics of HIV therapy. The pharmacogenomics journal. 2006. Rodríguez-Nóvoa S, et al. PubMed
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In vitro inhibition of UDP glucuronosyltransferases by atazanavir and other HIV protease inhibitors and the relationship of this property to in vivo bilirubin glucuronidation. Drug metabolism and disposition: the biological fate of chemicals. 2005. Zhang Donglu, et al. PubMed
Gilbert syndrome and the development of antiretroviral therapy-associated hyperbilirubinemia. The Journal of infectious diseases. 2005. Rotger Margalida, et al. PubMed
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Effects of ketoconazole on glucuronidation by UDP-glucuronosyltransferase enzymes. Clinical cancer research : an official journal of the American Association for Cancer Research. 2005. Yong Wei Peng, et al. PubMed
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Influence of lipid lowering fibrates on P-glycoprotein activity in vitro. Biochemical pharmacology. 2004. Ehrhardt Manuela, et al. PubMed
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Interactions of human P-glycoprotein with simvastatin, simvastatin acid, and atorvastatin. Pharmaceutical research. 2004. Hochman Jerome H, et al. PubMed
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Polymorphisms in human MDR1 (P-glycoprotein): recent advances and clinical relevance. Clinical pharmacology and therapeutics. 2004. Marzolini Catia, et al. PubMed
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Genetic polymorphisms of the human MDR1 drug transporter. Annual review of pharmacology and toxicology. 2003. Schwab Matthias, et al. PubMed
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Mechanism of indinavir-induced hyperbilirubinemia. Proceedings of the National Academy of Sciences of the United States of America. 2001. Zucker S D, et al. PubMed
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Interaction of omeprazole, lansoprazole and pantoprazole with P-glycoprotein. Naunyn-Schmiedeberg's archives of pharmacology. 2001. Pauli-Magnus C, et al. PubMed
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The role of intestinal P-glycoprotein in the interaction of digoxin and rifampin. The Journal of clinical investigation. 1999. Greiner B, et al. PubMed
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Biochemical, cellular, and pharmacological aspects of the multidrug transporter. Annual review of pharmacology and toxicology. 1999. Ambudkar S V, et al. PubMed
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Efavirenz. Drugs. 1998. Adkins J C, et al. PubMed
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Competitive, non-competitive and cooperative interactions between substrates of P-glycoprotein as measured by its ATPase activity. Biochimica et biophysica acta. 1997. Litman T, et al. PubMed
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P-glycoprotein structure and evolutionary homologies. Cytotechnology. 1993. Croop J M. PubMed

LinkOuts

Web Resource:
Wikipedia
National Drug Code Directory:
0006-0570-62
DrugBank:
DB00224
ChEBI:
5898
KEGG Compound:
C07051
PubChem Compound:
5362440
PubChem Substance:
197165
46506442
Drugs Product Database (DPD):
2229161
BindingDB:
517
ChemSpider:
4515036
Therapeutic Targets Database:
DAP000168
FDA Drug Label at DailyMed:
e19405d9-d9a1-4072-5b9e-40cd3ae4bf1f

Clinical Trials

These are trials that mention indinavir and are related to either pharmacogenetics or pharmacogenomics.

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Sources for PharmGKB drug information: DrugBank, Open Eye Scientific Software.