Saquinavir Dosage
This dosage information may not include all the information needed to use Saquinavir safely and effectively. See additional information for Saquinavir.
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Usual Adult Dose for:
Usual Pediatric Dose for:
Additional dosage information:
Usual Adult Dose for HIV Infection
1000 mg saquinavir plus 100 mg ritonavir orally twice a day
Concurrent treatment with lopinavir 400 mg-ritonavir 100 mg twice a day: 1000 mg orally twice a day (with no additional ritonavir)
Unboosted saquinavir is not recommended by the manufacturer or the DHHS Panel on Clinical Practices for Treatment of HIV Infection due to low bioavailability.
Usual Adult Dose for Nonoccupational Exposure
1000 mg saquinavir plus 100 mg ritonavir orally twice a day
400 mg saquinavir plus 400 mg ritonavir orally twice a day
Duration: Prophylaxis should be initiated as soon as possible, within 72 hours of exposure, and continued for 28 days.
Saquinavir plus ritonavir plus 2 NRTIs is one of the alternative regimens recommended for nonoccupational postexposure HIV prophylaxis.
Usual Pediatric Dose for HIV Infection
16 years or older:
1000 mg saquinavir plus 100 mg ritonavir orally twice a day
Concurrent treatment with lopinavir 400 mg-ritonavir 100 mg twice a day: 1000 mg orally twice a day (with no additional ritonavir)
Unboosted saquinavir is not recommended by the manufacturer or the DHHS Panel on Clinical Practices for Treatment of HIV Infection due to low bioavailability.
Renal Dose Adjustments
No adjustment recommended.
The manufacturer recommends caution when administering this drug to patients with severe renal dysfunction or end-stage renal disease.
Liver Dose Adjustments
Mild or moderate hepatic impairment: No adjustment recommended.
Saquinavir plus ritonavir:
Severe hepatic dysfunction: Contraindicated
Dose Adjustments
Patients receiving combination therapy with saquinavir plus ritonavir may require dose adjustments. These adjustments should be based on the known toxicity profile of the individual agent and the pharmacokinetic interaction between saquinavir and the coadministered drug. The product information for these drugs should be consulted for dose adjustment recommendations.
Dosages less than 1000 mg saquinavir plus 100 mg ritonavir are not recommended.
Precautions
Saquinavir must be administered in combination with ritonavir.
Saquinavir should be interrupted if a serious or severe toxicity occurs during treatment until the etiology can be identified or the toxicity resolves. At that time, treatment resumption with full-dose saquinavir may be considered; lower dosages have not shown antiretroviral activity.
The combination of saquinavir plus ritonavir is a potent CYP450 3A inhibitor and may potentially interact with many drugs. These interactions may be serious and/or life threatening. Drugs contraindicated for coadministration with saquinavir/ritonavir include alfuzosin, amiodarone, bepridil, dofetilide, flecainide, systemic lidocaine, propafenone, quinidine, trazodone, dihydroergotamine, ergonovine, ergotamine, methylergonovine, rifampin, cisapride, pimozide, oral midazolam, triazolam, lovastatin, simvastatin, and sildenafil for treatment of pulmonary arterial hypertension. Saquinavir interacts with several antiretroviral agents and appropriate dosage adjustments should be made when these drugs are used together. Patients should be advised to report all concurrent medications they are taking.
Saquinavir plus ritonavir causes dose-dependent QT interval prolongation. Torsades de pointes has been reported rarely during postmarketing experience. Saquinavir plus ritonavir is contraindicated in patients with congenital long QT syndrome, in patients with refractory hypokalemia or hypomagnesemia, and in combination with drugs that both increase saquinavir plasma levels and prolong the QT interval. Electrocardiogram (ECG) monitoring is recommended if therapy is initiated in patients with congestive heart failure, bradyarrhythmias, hepatic impairment, and electrolyte abnormalities. Hypokalemia or hypomagnesemia should be corrected before saquinavir plus ritonavir is started and these electrolytes should be monitored periodically during treatment.
An ECG is recommended before starting saquinavir plus ritonavir. Patients with a QT interval greater than 450 msec should not receive ritonavir-boosted saquinavir. For patients with a QT interval less than 450 msec, an on-treatment ECG is recommended after about 3 to 4 days of therapy; patients with a QT interval greater than 480 msec or prolongation over pretreatment by greater than 20 msec should discontinue ritonavir-boosted saquinavir. If drug discontinuation or interruption is considered due to ECG assessment, a cardiology consult is recommended.
For patients requiring drugs that may increase the QT interval and concomitant ritonavir-boosted saquinavir, an ECG is recommended before the concomitant therapy is started. Such combinations are only recommended when no alternative therapy is available and the benefits outweigh the risks. Patients with a QT interval greater than 450 msec should not start the concomitant therapy. If baseline QT interval less than 450 msec, an on-treatment ECG is recommended after 3 to 4 days of therapy; patients with an increase in QT interval to greater than 480 msec or increase by greater than 20 msec after starting concomitant therapy should discontinue either ritonavir-boosted saquinavir or the concomitant therapy or both. If drug discontinuation or interruption is considered due to ECG assessment, a cardiology consult is recommended.
Saquinavir is contraindicated in patients with complete atrioventricular (AV) block without implanted pacemakers, or patients who are at high risk of complete AV block.
The combination of saquinavir plus ritonavir prolongs the PR intervals in a dose-dependent manner. Patients with preexisting conduction system abnormalities, ischemic heart disease, cardiomyopathies, or underlying structural heart disease may be at greater risk for developing cardiac conduction abnormalities. ECG monitoring is recommended in such patients.
The effect on the PR interval of saquinavir plus ritonavir coadministered with other drugs that prolong the PR interval has not been established. Concomitant use of saquinavir plus ritonavir with these drugs should be done with caution (especially with those metabolized by CYP450 3A) and clinical monitoring is recommended.
Spontaneous bleeding episodes have been reported in hemophiliac patients while receiving protease inhibitors. No causal relationship has been established, however, the FDA and the manufacturers of protease inhibitors recommend that hemophiliacs be monitored closely for bleeding during therapy.
Episodes of hyperglycemia, new onset diabetes mellitus, and exacerbation of preexisting diabetes mellitus have been reported in patients receiving protease inhibitors during postmarketing surveillance. In some cases, diabetic ketoacidosis has occurred. No causal relationship has been established. Careful monitoring of blood glucose levels should be done and either initiation or dose adjustments of insulin or oral hypoglycemic agents may be needed.
Triglyceride and cholesterol testing are recommended before starting and periodically during therapy with saquinavir plus ritonavir. Lipid disorders should be managed as clinically appropriate.
Immune reconstitution syndrome has occurred during combination treatment with saquinavir and other antiretrovirals. Patients responding to therapy may develop an inflammatory response to indolent or residual opportunistic infections and require evaluation and treatment.
Saquinavir should always be used in combination with other antiretroviral agents. Saquinavir should generally not be added as a single agent when antiretroviral regimens are changed due to the development of drug resistance and loss of virological response.
The potential for HIV cross-resistance among protease inhibitors exists but has not been fully explored. It is unknown what effect saquinavir therapy will have on the activity of subsequently administered protease inhibitors. Selection of antiretroviral agents for a patient's medication regimen should be done carefully.
Saquinavir is not approved for use in children. Safety and efficacy have not been established in pediatric patients less than 16 years of age. Clinical trials in children have shown that doses of 50 mg/kg every 8 hours do not achieve adequate serum saquinavir concentrations. Clinical trials are ongoing to evaluate saquinavir combined with a second protease inhibitor (such as ritonavir, nelfinavir, or lopinavir-ritonavir). Saquinavir should not be used as the only protease inhibitor in children.
Dialysis
Data not available
Other Comments
Saquinavir and ritonavir should be taken at the same time and within 2 hours following a full meal.
Saquinavir mesylate tablets and hard gelatin capsules may be stored at room temperature.
Saquinavir is used in conjunction with nucleoside analogs. If possible, protease inhibitors should be used in combination with 2 nucleoside analogs since triple therapy appears to be the most potent antiretroviral combination available. However, one nucleoside plus a protease inhibitor may be effective if drug intolerance prevents the use of triple therapy.
