"Entry Inhibitors (including Fusion Inhibitors) and CCR5 Co-receptor Antagonist
Entry inhibitors block HIV entry into CD4+ cells.
The only drug in this class "...
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Details with Side Effects
There is no known antidote for APTIVUS overdose. Treatment of overdose should consist of general supportive measures, including monitoring of vital signs and observation of the patient's clinical status. If indicated, elimination of unabsorbed tipranavir should be achieved by emesis or gastric lavage. Administration of activated charcoal may also be used to aid in removal of unabsorbed drug. Since tipranavir is highly protein bound, dialysis is unlikely to provide significant removal of the drug.
APTIVUS is contraindicated in patients with moderate or severe (Child-Pugh Class B or C, respectively) hepatic impairment [see WARNINGS AND PRECAUTIONS].
Co-administration of APTIVUS/ritonavir with drugs that are highly dependent on CYP 3A for clearance or are potent CYP 3A inducers are contraindicated (see Table 1). These recommendations are based on either drug interaction studies or they are predicted interactions due to the expected magnitude of interaction and potential for serious events or loss of efficacy. For information regarding clinical recommendations [see DRUG INTERACTIONS].
Table 1 : Drugs that are Contraindicated with APTIVUS
Co-Administered with Ritonavir
|Drug Class||Drugs within Class that are Contraindicated with APTIVUS Co-administered with Ritonavir||Clinical Comments:|
|Alpha 1-adrenoreceptor antagonist||Alfuzosin||Potentially increased alfuzosin concentrations can result in hypotension.|
|Antiarrhythmics||Amiodarone, bepridil, flecainide, propafenone, quinidine||Potential for serious and/or life-threatening reactions such as cardiac arrhythmias secondary to increases in plasma concentrations of antiarrhythmics.|
|Antimycobacterials||Rifampin||May lead to loss of virologic response and possible resistance to APTIVUS or to the class of protease inhibitors or other coadministered antiretroviral agents.|
|Ergot derivatives||Dihydroergotamine, ergonovine, ergotamine, methylergonovine||Potential for acute ergot toxicity characterized by peripheral vasospasm and ischemia of the extremities and other tissues.|
|GI motility agent||Cisapride||Potential for cardiac arrhythmias.|
|Herbal products||St. John's wort (hypericum perforatum)||May lead to loss of virologic response and possible resistance to APTIVUS or to the class of protease inhibitors.|
|HMG CoA reductase inhibitors||Lovastatin, simvastatin||Potential for myopathy including rhabdomyolysis.|
|Neuroleptic||Pimozide||Potential for cardiac arrhythmias.|
|PDE-5 inhibitors||Sildenafil (Revatio) [for treatment of pulmonary arterial hypertension]||A safe and effective dose has not been established when used with APTIVUS/ritonavir. There is increased potential for sildenafil-associated adverse events (which include visual disturbances, hypotension, prolonged erection, and syncope).|
|Sedatives/hypnotics||Oral midazolam, triazolam||Prolonged or increased sedation or respiratory depression.|
Due to the need for co-administration of APTIVUS with ritonavir, please refer to the ritonavir prescribing information for a description of ritonavir contraindications.
Last reviewed on RxList: 3/1/2012
This monograph has been modified to include the generic and brand name in many instances.
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