"Entry Inhibitors (including Fusion Inhibitors) and CCR5 Co-receptor Antagonist
Entry inhibitors block HIV entry into CD4+ cells.
The only drug in this class "...
Human experience of acute overdose with REYATAZ is limited. Single doses up to 1200 mg (three times the 400 mg maximum recommended dose) have been taken by healthy volunteers without symptomatic untoward effects. A single self-administered overdose of 29.2 g of REYATAZ in an HIV-infected patient (73 times the 400-mg recommended dose) was associated with asymptomatic bifascicular block and PR interval prolongation. These events resolved spontaneously. At REYATAZ doses resulting in high atazanavir exposures, jaundice due to indirect (unconjugated) hyperbilirubinemia (without associated liver function test changes) or PR interval prolongation may be observed. [See WARNINGS AND PRECAUTIONS and CLINICAL PHARMACOLOGY]
Treatment of overdosage with REYATAZ should consist of general supportive measures, including monitoring of vital signs and ECG, and observations of the patient's clinical status. If indicated, elimination of unabsorbed atazanavir should be achieved by emesis or gastric lavage. Administration of activated charcoal may also be used to aid removal of unabsorbed drug. There is no specific antidote for overdose with REYATAZ. Since atazanavir is extensively metabolized by the liver and is highly protein bound, dialysis is unlikely to be beneficial in significant removal of this medicine.
REYATAZ is contraindicated
- in patients with previously demonstrated clinically significant hypersensitivity (eg, Stevens-Johnson syndrome, erythema multiforme, or toxic skin eruptions) to any of the components of REYATAZ capsules or REYATAZ oral powder [see WARNINGS AND PRECAUTIONS].
- when coadministered with drugs that are highly dependent on CYP3A or UGT1A1 for clearance, and for which elevated plasma concentrations of the interacting drugs are associated with serious and/or life-threatening events (see Table 6).
- when coadministered with drugs that strongly induce CYP3A and may lead to lower exposure and loss of efficacy of REYATAZ (see Table 6).
Table 6 displays drugs that are contraindicated with REYATAZ.
Table 6: Drugs that are Contraindicated with REYATAZ
(Information in the table applies to REYATAZ with or without ritonavir, unless
|Drug Class||Drugs within class that are contraindicated with REYATAZ||Clinical Comment|
|Alpha 1- Adrenoreceptor Antagonist||Alfuzosin||Potential for increased alfuzosin concentrations, which can result in hypotension.|
|Antimycobacterials||Rifampin||Rifampin substantially decreases plasma concentrations of atazanavir, which may result in loss of therapeutic effect and development of resistance.|
|Antineoplastics||Irinotecan||Atazanavir inhibits UGT1A1 and may interfere with the metabolism of irinotecan,resulting in increased irinotecan toxicities.|
|Benzodiazepines||Triazolam,orally administered midazolama||Triazolam andorally administered midazolam are extensively metabolized by CYP3A4. Coadministration of triazolam or orally administered midazolam with REYATAZ may cause large increases in the concentration of these benzodiazepines. Potential for serious and/or life-threatening events such as prolonged or increased sedation or respiratory depression.|
|Ergot Derivatives||Dihydroergotamine,ergotamine, ergonovine, methylergonovine||Potential for serious and/or life-threatening events such as acute ergot toxicity characterized by peripheral vasospasm and ischemia of the extremities andother tissues.|
|GI Motility Agent||Cisapride||Potential for serious and/or life-threatening reactions such as cardiac arrhythmias.|
|Herbal Products||St. John’s wort (Hypericum perforatum)||Coadministration of St. John’s wort and REYATAZ may result in loss of therapeutic effect anddevelopment of resistance.|
|HMG-CoA Reductase Inhibitors||Lovastatin, simvastatin||Potential for serious reactions such as myopathy, including rhabdomyolysis.|
|Neuroleptic||Pimozide||Potential for serious and/or life-threatening reactions such as cardiac arrhythmias.|
|PDE5 Inhibitor||Sildenafilb when dosed as REVATIO® for the treatment of pulmonary arterial hypertension||Potential for sildenafil-associated adverse events (which include visual disturbances, hypotension, priapism, and syncope).|
|Protease Inhibitors||Indinavir||Both REYATAZ and indinavir are associated with indirect (unconjugated) hyperbilirubinemia.|
|Non-nucleoside Reverse Transcriptase Inhibitors||Nevirapine||Nevirapine sustantially decreases atazanavir exposure which may result in loss of therapeutic effect and develoment of resistance. Potential risk for nevirapine-associated adverse reactions due to increased nevirapine exposures.|
|a See DRUG INTERACTIONS, Table 16 for
parenterally administered midazolam.
b See DRUG INTERACTIONS, Table 16 for sildenafil when dosed as VIAGRA® for erectile dysfunction.
Last reviewed on RxList: 6/16/2014
This monograph has been modified to include the generic and brand name in many instances.
Additional Reyataz Information
Reyataz - User Reviews
Reyataz User Reviews
Now you can gain knowledge and insight about a drug treatment with Patient Discussions.
Report Problems to the Food and Drug Administration
You are encouraged to report negative side effects of prescription drugs to the FDA. Visit the FDA MedWatch website or call 1-800-FDA-1088.
Get breaking medical news.