saquinavir (Rx)

Brand and Other Names:Invirase
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 500mg

HIV Infection

1000 mg (with ritonavir 100 mg) PO q12hr, or in combination with ritonavir-enhanced lopinavir

Treatment-naïve patients

  • Initial dose: 500 mg PO BID plus ritonavir 100 mg BID x 7 days, THEN increase to 1000mg/100mg PO BID
  • This gradual increase is due to potential for increased risk of PR and QT interval prolongation with standard 1000/100-mg BID dose
  • Patients with a baseline QT interval <450 msec, an on-treatment ECG is recommended after ~10 days of therapy
  • Patients with a QT interval prolongation over pretreatment by >20 msec should discontinue saquinavir/ritonavir therapy

Dosage Forms & Strengths

tablet

  • 500mg

HIV Infection

Indicated in combination with ritonavir and other antiretrovirals (ARTs) for treatment of HIV-1 infection

<16 years: Safety and efficacy not established

≥16 years: 1000 mg (plus ritonavir 100 mg) PO q12hr

For patients already taking ritonavir 100 mg BID as part of their ART regimen, no additional ritonavir is needed

Treatment-naïve patients

  • Initial dose: 500 mg PO BID plus ritonavir 100 mg BID x 7 days, THEN increase to 1000mg/100mg PO BID
  • This gradual increase is due to potential for increased risk of PR and QT interval prolongation with standard 1000/100-mg BID dose
  • Patients with a baseline QT interval <450 msec, an on-treatment ECG is recommended after ~10 days of therapy
  • Patients with a QT interval prolongation over pretreatment by >20 msec should discontinue saquinavir/ritonavir therapy

Investigational in treatment-experienced children

  • <2 years: Safety and efficacy not established
  • ≥2 years, 5 to <15 kg: 50 mg/kg (plus ritonavir 3 mg/kg) PO q12hr  
  • ≥2 years, 15-40 kg: 50 mg/kg (plus ritonavir 2.5 mg/kg) PO q12hr
  • ≥2 years, ≥40 kg: 50 mg/kg (plus ritonavir 100mg) PO q12hr
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Interactions

Interaction Checker

and saquinavir

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    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

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            Adverse Effects

            1-10%

            Rash

            Hyperglycemia

            Diarrhea

            Abdominal discomfort

            Nausea

            Abdominal pain

            Buccal mucosa ulceration

            Paresthesia

            Weakness

            Increased CPK

            <1%

            Headache

            Confusion

            Seizures

            Ataxia

            Pain

            Stevens-Johnson syndrome

            Hypoglycemia

            Hyper- & hypokalemia

            Low serum amylase

            AML

            Hemolytic anemia

            Thrombocytopenia

            Jaundice

            Ascites

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            Warnings

            Black Box Warnings

            Saquinavir mesylate (Invirase) capsules and tablets, and saquinavir (Fortovase) soft gelatin capsules, are not bioequivalent and cannot be used interchangeably

            Fortovase is no longer available in the United States

            Use saquinavir mesylate (Invirase) only if it is combined with ritonavir, which significantly inhibits saquinavir's metabolism to provide plasma saquinavir levels at least equal to those achieved with saquinavir (Fortovase)

            Contraindications

            Hypersensitivity (eg, anaphylactic reaction, Stevens-Johnson syndrome)

            An ECG should be performed prior to initiation of treatment; patients with a QT interval = 450 msec should not initiate therapy

            Treatment-naïve patients initiating therapy should receive a reduced starting dose of saquinavir 500-mg twice daily with ritonavir 100-mg twice daily for the first 7 days of treatment followed by saquinavir/ritonavir 1000/100 mg twice daily due to potential for an increased risk of PR and QT interval prolongation with the standard 1000/100-mg twice daily dose

            QT and PR interval prolonation 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 (eg, prolonged QT interval)

            Drug contraindicated with saquinavir/ritonavir include alfuzosin, antiarrhythmics (amiodarone, bepridil, flecainide, propafenone, quinidine, lidocaine), trazodone, rifampin, voriconazole, ergot derivatives (dihydroergotamine, ergonovine, ergotamine, methylergonovine), cisapride, St. John’s wort, HMG-CoA reductase inhibitors (lovastatin, simvastatin), lurasidone, pimozide, clarithromycin, erythromycin, halofantrine, pentamidine, clozapine, haloperidol, sertindole, ziprasidone, atazanavir, tacrolimus, rilpivirine, dasatinib, sunitinib, disopyramide, quinine, phenothiazines (e.g. chlorpromazine, mesoridazine, thioridazine), sildenafil (when used for PAH), midazolam, and triazolam

            Cautions

            Hyperlipidemia may occur

            Take within 2 hr after meal; absorption increased with high-fat meal

            Must be used in combination with ritonavir (ie, boosted therapy) to achieve necessary levels for effectiveness

            Autoimmune disorders (eg, Graves disease, polymyositis, Guillain-Barré syndrome) reported in the setting of immune reconstitution; however, time to onset is variable, and can occur many months after treatment initiation

            Risk of QT and PR prolongation that might lead to Torsades de Pointes (particularly if used with ritonavir); discontinue therapy if significant arrhythmias, QT or PR prolongation occurs; perform ECG prior to initiation of treatment; patients with a baseline QT interval < 450 msec, an on-treatment ECG is recommended after approximately 10 days of therapy; patients with a QT interval prolongation over pre-treatment by > 20 msec should discontinue saquinavir/ritonavir therapy

            May develop new onset or exacerbations of diabetes mellitus, hyperglycemia, elevated cholesterol and/or triglyceride concentrations, redistribution/accumulation of body fat, and immune reconstitution syndrome; monitor cholesterol and triglycerides prior to therapy and periodically thereafter

            In patients with underlying hepatitis B or C, cirrhosis, chronic alcoholism or other underlying liver abnormalities, worsening of underlying liver disease and development of portal hypertension reported after initiating therapy; jaundice and exacerbation of chronic liver disease with grade 4 elevated liver function tests also observed; no dosage adjustment necessary for patients with mild or moderate hepatic impairment based on limited data; saquinavir/ritonavir contraindicated in patients with severe hepatic impairment; if a serious or severe toxicity occurs during treatment, discontinue therapy

            Spontaneous bleeding may occur and additional factor VII may be required

            Various degrees of cross-resistance have been observed

            Not recommended for use in combination with cobicistat

            Tablets and capsules contain lactose; not recommended in patients with rare hereditary problems of galactose intolerance, lapp lactase deficiency or glucose-galactose or malabsorption

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            Pregnancy & Lactation

            Pregnancy Category: B

            Lactation: unknown whether present in breast milk, do not breast feed; HIV+ women may cause postnatal vertical transmission to infant with ingestion of HIV in the breast milk

            Pregnancy Categories

            A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA: Information not available.

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            Pharmacology

            Mechanism of Action

            Protease Inhibitor; inhibits cleavage of Gag-Pol polyprotein precursors, which in turn causes the formation of immature, noninfectious viral particles.

            Combination (boosted therapy) use recommended

            Absorption

            Poor absorption; increased with high fat meal

            Protein Bound: ~98%

            Distribution

            Does not distribute into CSF

            Vd: 700 L

            Metabolism

            Extensively metabolized via hepatic CYP3A4; extensive first-pass effect

            Elimination

            Excretion: Fece: 81-88%; urine: 1-3%

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            Administration

            Oral Administration

            Saquinavir plus ritonavir should be taken with 2 hr after a meal

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            Formulary

            FormularyPatient Discounts

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            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
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            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
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            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.