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INDINAVIR SULFATE
DIR Classification
Classification:Moderate-DIR concern
Severity Score:3
Description in Drug Labeling: View Full Labeling: SPL in DailyMed | PDF
- WARNINGS
- Risk of Serious Adverse Reactions Due to Drug Interactions
- Initiation of CRIXIVAN, a CYP3A inhibitor, in patients receiving medications metabolized by CYP3A or initiation of medications metabolized by CYP3A in patients already receiving CRIXIVAN, may increase plasma concentrations of medications metabolized by CYP3A. Initiation of medications that inhibit or induce CYP3A may increase or decrease concentrations of CRIXIVAN, respectively. These interactions may lead to:
- - Clinically significant adverse reactions, potentially leading to severe, life-threatening, or fatal events from greater exposures of concomitant medications.
- - Clinically significant adverse reactions from greater exposures of CRIXIVAN.
- - Loss of therapeutic effect of CRIXIVAN and possible development of resistance.
- See TABLE 9 for steps to prevent or manage these possible and known significant drug interactions, including dosing recommendations. Consider the potential for drug interactions prior to and during CRIXIVAN therapy; review concomitant medications during CRIXIVAN therapy; and monitor for the adverse reactions associated with the concomitant medications.
- 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. (See PRECAUTIONS, DRUG INTERACTIONS.)
- 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.
- 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).
- 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.
- PRECAUTIONS
- Drug Interactions
- Indinavir is an inhibitor of the cytochrome P450 isoform CYP3A4. Coadministration of CRIXIVAN and drugs primarily metabolized by CYP3A4 may result in increased plasma concentrations of the other drug, which could increase or prolong its therapeutic and adverse effects (see CONTRAINDICATIONS and WARNINGS).
- Indinavir is metabolized by CYP3A4. Drugs that induce CYP3A4 activity would be expected to increase the clearance of indinavir, resulting in lowered plasma concentrations of indinavir. Coadministration of CRIXIVAN and other drugs that inhibit CYP3A4 may decrease the clearance of indinavir and may result in increased plasma concentrations of indinavir.
Postmarketing Surveillance
Contingency Table:
Current Drug
Other Drugs
Rhabdomyolysis
31
42881
Other ADRs
4209
14113070
Odds Ratio = 2.425
Drug Property Information
ATC Code(s):
- J05AE02 - indinavir sulfate
- J05AE - Protease inhibitors
- J05A - DIRECT ACTING ANTIVIRALS
- J05 - ANTIVIRALS FOR SYSTEMIC USE
- J - ANTIINFECTIVES FOR SYSTEMIC USE
Active Ingredient:indinavir sulfate
Active Ingredient UNII:771H53976Q
Drugbank ID:DB00224
PubChem Compound:5362440
CAS Number:150378-17-9
Dosage Form(s):capsule
Route(s) Of Administrator:oral
Daily Dose:
- 2400.0 mg/day J05AE02
Chemical Structure: 
SMILE Code:
CC(C)(C)NC(=O)[C@@H]1CN(CCN1C[C@H](C[C@@H](CC2=CC=CC=C2)C(=O)N[C@@H]3[C@@H](CC4=CC=CC=C34)O)O)CC5=CN=CC=C5
CC(C)(C)NC(=O)[C@@H]1CN(CCN1C[C@H](C[C@@H](CC2=CC=CC=C2)C(=O)N[C@@H]3[C@@H](CC4=CC=CC=C34)O)O)CC5=CN=CC=C5
Reference
COHORT STUDY:
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