Drug Index

Saquinavir

 
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Mechanism :

It is a protease inhibitor (antiviral drug) used in the treatment of HIV infection.


Indication :

• For the treatment of HIV-1 with advanced immunodeficiency together with antiretroviral nucleoside analogues.


Contraindications :

Hypersensitivity (e.g., anaphylactic reaction, Stevens-Johnson syndrome)

QT and PR interval prolongation and torsades de pointes have been reported rarely; do not use saquinavir/ritonavir with congenital or documented acquired QT prolongation (>450 msec), refractory hypokalemia or magnesemia, and in combination with drugs that prolong QT interval.

Complete atrioventricular (AV) block without implanted pacemakers or high risk of complete AV block.

Severe hepatic impairment.

Coadministration of saquinavir/ritonavir with rifampin due to the risk of severe hepatotoxicity.

Drugs that are contraindicated with saquinavir (when coadministered ‘boosted’ with ritonavir) include CYP3A inhibitors that may result in increased saquinavir plasma levels and cause serious or life-threatening reactions (e.g., prolonged QT interval).

Drug contraindicated with saquinavir/ritonavir include alfuzosin, antiarrhythmics (amiodarone, bepridil, flecainide, propafenone, quinidine), trazodone, rifampin, voriconazole, ergot derivatives (dihydroergotamine, ergonovine, ergotamine, methylergonovine), cisapride, St. John’s wort, HMG-CoA reductase inhibitors (lovastatin, simvastatin), pimozide, sildenafil (when used for PAH), midazolam, and triazolam.


Dosing :

HIV Infection:

<16 years: Safety and efficacy not established.

>16 years: 1000 mg (plus ritonavir 100 mg) PO every 12 hours.

In treatment-experienced children:

<2 years: Not recommended.

≥2 years:

5 to <15 kg: 50 mg/kg (plus ritonavir 3 mg/kg) PO every 12 hours.

15-40 kg: 50 mg/kg (plus ritonavir 2.5 mg/kg) PO every 12 hours.

≥40 kg: 50 mg/kg (plus ritonavir 100 mg) PO every 12 hours.


Adverse Effect :

Rash, hyperglycemia, diarrhea, abdominal discomfort, nausea, abdominal pain, buccal mucosa ulceration, paresthesia, weakness.


Interaction :

Albuterol: Increase the toxicity by pharmacodynamic.
Alfuzosin: Increases the levels of alfuzosin by hepatic/intestinal metabolism.
Rifampin: Decreases the levels of saquinavir.


08/11/2019 20:43:58 Saquinavir
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