Invirase (Saquinavir Mesylate) Drug Information: Overdosage and Contraindications

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May 27, 2012

Invirase

HIV and AIDS: Antiretroviral Drugs, Treatments and Medications »

Entry Inhibitors (including Fusion Inhibitors) and CCR5 Co-receptor Antagonist

Entry Inhibitors
Entry inhibitors block HIV entry into CD4+ cells.

Fusion inhibitors
The only drug in this class is T-20, which is administered as a twice daily subcutaneous injection. The most common side effect is redness and pain at the site of injection. Rarely, infection can occur at the injection site. There also are reports of generalized allergic reactions.

CCR5 antagonist
Although there were some early concerns of liver inflammation for drugs in this class, MVC appeared to be well tolerated in clinical trials without any specific toxicities attributable to the drug. However, it is a new drug in a new class and the first to actually target the cell. For these reasons, longer follow-up from clinical trials and those followed in the clinic will be very important for assessing the overall safety of the...

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Invirase

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OVERDOSE

There is limited experience of overdose with saquinavir.

No acute toxicities or sequelae were noted in 1 patient who ingested 8 grams of INVIRASE as a single dose. The patient was treated with induction of emesis within 2 to 4 hours after ingestion. A second patient ingested 2.4 grams of INVIRASE in combination with 600 mg of ritonavir and experienced pain in the throat that lasted for 6 hours and then resolved. In an exploratory Phase II study of oral dosing with INVIRASE at 7200 mg/day (1200 mg q4h), there were no serious toxicities reported through the first 25 weeks of treatment.

Treatment of overdose with saquinavir should consist of general supportive measures including monitoring of vital signs and ECG and observations of the patient's clinical status. Since saquinavir is highly protein bound, dialysis is unlikely to be beneficial in significant removal of the active substance.

CONTRAINDICATIONS

QT interval prolongation and torsades de pointes have been reported rarely with INVIRASE/ritonavir use. Do not use in patients with congenital long QT syndrome, those with refractory hypokalemia or hypomagnesemia, and in combination with drugs that both increase saquinavir plasma concentrations and prolong the QT interval [see WARNINGS AND PRECAUTIONS and CLINICAL PHARMACOLOGY].

INVIRASE is contraindicated in patients with complete atrioventricular (AV) block without implanted pacemakers, or patients who are at high risk of complete AV block [see WARNINGS AND PRECAUTIONS].

INVIRASE is contraindicated in patients with clinically significant hypersensitivity (e.g., anaphylactic reaction, Stevens-Johnson syndrome) to saquinavir, saquinavir mesylate, or any of its ingredients including ritonavir.

INVIRASE when administered with ritonavir is contraindicated in patients with severe hepatic impairment.

Coadministration of INVIRASE/ritonavir is contraindicated with drugs that are CYP3A substrates for which increased plasma levels may result in serious or life-threatening reactions. These drugs and potentially related adverse events are listed in Table 1.

Table 1 : Drugs That Are Contraindicated With INVIRASE/Ritonavir

Drug Class	Drugs Within Class That Are Contraindicated With INVIRASE	Clinical Comment
Alpha 1-adrenoreceptor antagonist	Alfuzosin	Potentially increased alfuzosin concentrations can result in hypotension.
Antiarrhythmics	Amiodarone, bepridil, dofetilide, flecainide, lidocaine (systemic), propafenone, quinidine	Potential for serious and/or life-threatening cardiac arrhythmia.
Antidepressant	Trazodone	Increased trazodone concentrations can result in potentially life threatening cardiac arrhythmia.
Antimycobacterial Agents	Rifampin	Rifampin should not be administered in patients taking ritonavir-boosted INVIRASE part of an ART regimen due to the risk of severe hepatocellular toxicity.
Ergot Derivatives	Dihydroergotamine, ergonovine, ergotamine, methylergonovine	Potential for serious and life threatening reactions such as ergot toxicity characterized by peripheral vasospasm and ischemia of the extremities and other tissues.
GI Motility Agent	Cisapride	Potential for serious and/or life threatening reactions such as cardiac arrhythmias.
HMG-CoA Reductase Inhibitors	Lovastatin, Simvastatin	Potential for myopathy including rhabdomyolysis.
Neuroleptics	Pimozide	Potential for serious and/or life threatening reactions such as cardiac arrhythmias.
PDE5 Inhibitors	Sildenafil (Revatio®) [for treatment of pulmonary arterial hypertension]	Increased potential for sildenafil-associated adverse events (which include visual disturbances, hypotension, prolonged erection, and syncope). A safe and effective dose has not been established when used with INVIRASE/ritonavir.
Sedative/Hypnotics	Triazolam, orally administered midazolam	Potential for serious and/or life threatening reactions such as prolonged or increased sedation or respiratory depression. Triazolam and orally administered midazolam are extensively metabolized by CYP3A4. Coadministration of triazolam and orally administered midazolam with INVIRASE/ritonavir may cause large increases in the concentration of these benzodiazepines.