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Saquinavir

Class: HIV Protease Inhibitors
- Protease Inhibitors
VA Class: AM800
Chemical Name: [3S-[2[1R*(R*),2S*],3α,4aβ,8aα]]-N1-[3-[3-[[(1,1-dimethylethyl)amino]carbonyl]octahydro-2(1H)-isoquinolinyl]-2-hydroxy- 1-(phenylmethyl)propyl]-2-[(2-quinolinylcarbonyl)amino]-butanediamide
CAS Number: 127779-20-8
Brands: Invirase

Medically reviewed by Drugs.com on April 28, 2021. Written by ASHP.

Introduction

Antiretroviral; HIV protease inhibitor (PI).

Uses for Saquinavir

Treatment of HIV Infection

Treatment of HIV type 1 (HIV-1) infection in adults and adolescents >16 years of age; used in conjunction with low-dose ritonavir (ritonavir-boosted saquinavir) and other antiretrovirals.

Do not use saquinavir without a pharmacokinetic enhancer (i.e., low-dose ritonavir). Pharmacokinetic enhancer (pharmacokinetic booster) necessary to improve saquinavir pharmacokinetic profile. Do not use with the pharmacokinetic enhancer cobicistat. (See Interactions under Cautions.)

Ritonavir-boosted saquinavir usually used in PI-based regimens that include a PI and 2 HIV nucleoside reverse transcriptase inhibitors (dual NRTIs).

Experts state ritonavir-boosted saquinavir not recommended for initial treatment regimens in antiretroviral-naive adults and adolescents because of higher pill burden and more severe adverse cardiac effects (prolonged PR and QT intervals requiring ECG monitoring) compared with other available ritonavir-boosted PIs. (See Cardiovascular Effects under Cautions.) Experts also state not recommended for initial treatment regimens in antiretroviral-naive pediatric patients because of limited data.

Use of saquinavir without low-dose ritonavir (unboosted saquinavir) not recommended at any time because of inadequate bioavailability and inferior virologic efficacy.

Postexposure Prophylaxis following Occupational Exposure to HIV (PEP)

Postexposure prophylaxis of HIV infection following occupational exposure (PEP) in health-care personnel and others exposed via percutaneous injury (e.g., needlestick, cut with sharp object) or mucous membrane or nonintact skin (e.g., chapped, abraded, dermatitis) contact with blood, tissue, or other body fluids that might contain HIV.

USPHS recommends a 3-drug regimen of raltegravir in conjunction with emtricitabine and tenofovir disoproxil fumarate (tenofovir DF) as the preferred regimen for PEP following occupational exposures to HIV. Ritonavir-boosted saquinavir and 2 NRTIs can be considered an alternative regimen, but use for PEP only with expert consultation. Preferred dual NRTI option for PEP regimens is emtricitabine and tenofovir DF; alternatives are tenofovir DF and lamivudine, zidovudine and lamivudine, or zidovudine and emtricitabine.

Management of occupational exposures to HIV is complex and evolving; consult infectious disease specialist, clinician with expertise in administration of antiretroviral agents, and/or National Clinicians’ Postexposure Prophylaxis Hotline (PEPline at 888-448-4911) whenever possible. Do not delay initiation of PEP while waiting for expert consultation.

Postexposure Prophylaxis following Nonoccupational Exposure to HIV (nPEP)

Postexposure prophylaxis of HIV infection following nonoccupational exposure (nPEP) in individuals exposed to blood, genital secretions, or other potentially infectious body fluids that might contain HIV when the exposure represents a substantial risk for HIV transmission. Used in conjunction with other antiretrovirals.

When nPEP indicated in adults and adolescents ≥13 years of age with normal renal function, CDC states preferred regimen is either raltegravir or dolutegravir used in conjunction with emtricitabine and tenofovir DF (given as emtricitabine/tenofovir DF; Truvada); recommended alternative in these patients is ritonavir-boosted darunavir used in conjunction with emtricitabine/tenofovir DF.

CDC states saquinavir is an alternative antiretroviral that can be used in nPEP regimens, but use in such regimens only with expert consultation.

Consult infectious disease specialist, clinician with expertise in administration of antiretroviral agents, and/or the National Clinicians’ Postexposure Prophylaxis Hotline (PEPline at 888-448-4911) if nPEP indicated in certain exposed individuals (e.g., pregnant women, children, those with medical conditions such as renal impairment) or if considering a regimen not included in CDC guidelines, source virus is known or likely to be resistant to antiretrovirals, or healthcare provider is inexperienced in prescribing antiretrovirals. Do not delay initiation of nPEP while waiting for expert consultation.

Saquinavir Dosage and Administration

Administration

Oral Administration

Administer orally with low-dose ritonavir (ritonavir-boosted saquinavir) within 2 hours of a meal.

Do not administer without low-dose ritonavir.

Administer saquinavir dose at same time as ritonavir dose. In patients already receiving ritonavir as part of an antiretroviral regimen, no additional ritonavir is needed.

For patients unable to swallow capsules, empty contents of appropriate number of saquinavir capsules into container and mix with 15 mL of sugar syrup, 15 mL of sorbitol syrup, or 3 teaspoons of jam. Stir mixture for 30–60 seconds. Allow mixture to reach room temperature and administer entire dose to the patient.

Dosage

Available as saquinavir mesylate; dosage expressed as saquinavir.

Saquinavir mesylate hard gelatin capsules and film-coated tablets are bioequivalent when given with low-dose ritonavir under fed conditions.

Pediatric Patients

Treatment of HIV Infection
Oral

Adolescents >16 years of age: 1 g twice daily with low-dose ritonavir (100 mg twice daily).

Treatment-naive adolescents >16 years of age: Use low initial dosage of 500 mg twice daily with low-dose ritonavir (100 mg twice daily) for 7 days, then 1 g twice daily with low-dose ritonavir (100 mg twice daily) thereafter.

Previously treated adolescents >16 years of age receiving delavirdine or rilpivirine and switching to ritonavir-boosted saquinavir: 500 mg twice daily with low-dose ritonavir (100 mg twice daily) for 7 days, then 1 g twice daily with low-dose ritonavir (100 mg twice daily) thereafter.

Previously treated adolescents >16 years of age receiving a different ritonavir-boosted PI or an NNRTI (except delavirdine or rilpivirine) and switching to ritonavir-boosted saquinavir: 1 g twice daily with low-dose ritonavir (100 mg twice daily).

Adults

Treatment of HIV Infection
Oral

1 g twice daily with low-dose ritonavir (100 mg twice daily).

Treatment-naive adults: Use low initial dosage of 500 mg twice daily with low-dose ritonavir (100 mg twice daily) for 7 days, then 1 g twice daily with low-dose ritonavir (100 mg twice daily) thereafter.

Previously treated adults receiving delavirdine or rilpivirine and switching to ritonavir-boosted saquinavir: 500 mg twice daily with low-dose ritonavir (100 mg twice daily) for 7 days, then 1 g twice daily with low-dose ritonavir (100 mg twice daily) thereafter.

Previously treated adults receiving a different ritonavir-boosted PI or an NNRTI (except delavirdine or rilpivirine) and switching to ritonavir-boosted saquinavir: 1 g twice daily with low-dose ritonavir (100 mg twice daily).

Postexposure Prophylaxis of HIV†
Occupational Exposure†
Oral

1 g twice daily with low-dose ritonavir (100 mg twice daily). Use in conjunction with 2 NRTIs (see Postexposure Prophylaxis following Occupational Exposure to HIV under Uses).

Initiate PEP as soon as possible following occupational exposure to HIV (preferably within hours); continue for 4 weeks, if tolerated.

Special Populations

Hepatic Impairment

Treatment of HIV Infection

Dosage adjustments not necessary in mild to moderate hepatic impairment; some experts recommend caution. Contraindicated in severe hepatic impairment. (See Hepatic Impairment under Cautions.)

Renal Impairment

Treatment of HIV Infection

No initial dosage adjustments needed. Use with caution in severe renal impairment or end-stage renal disease.

Geriatric Patients

Select dosage with caution because of age-related decreases in hepatic, renal, and/or cardiac function and concomitant disease and drug therapy.

Cautions for Saquinavir

Contraindications

  • Hypersensitivity (anaphylactic reaction, Stevens-Johnson syndrome) to saquinavir, or any ingredient in the formulation.

  • Complete AV block without implanted pacemakers and patients at high risk of complete AV block.

  • Congenital long QT syndrome. (See Cardiovascular Effects under Cautions.)

  • Refractory hypokalemia or hypomagnesemia. (See Cardiovascular Effects under Cautions.)

  • Concomitant use with drugs that increase saquinavir plasma concentrations and prolong the QT interval. (See Cardiovascular Effects under Cautions.)

  • Severe hepatic impairment.

  • Concomitant use with drugs highly dependent on CYP3A for metabolism and for which elevated plasma concentrations are associated with serious and/or life-threatening events, including alfuzosin, certain antiarrhythmic agents (amiodarone, bepridil [not commercially available in US], dofetilide, flecainide, systemic lidocaine, propafenone, quinidine), certain anti-infectives (atazanavir, clarithromycin, dapsone, erythromycin, halofantrine [not commercially available in US], pentamidine, quinine, rifampin), certain antipsychotics (clozapine, haloperidol, lurasidone, phenothiazines, pimozide, sertindole [not commercially available in US], ziprasidone), cisapride, disopyramide, ergot alkaloids, lovastatin and simvastatin, oral midazolam, sildenafil used for treatment of pulmonary arterial hypertension [PAH], tacrolimus, trazodone, and triazolam. (See Specific Drugs and Foods under Interactions.)

Warnings/Precautions

Cardiovascular Effects

Ritonavir-boosted saquinavir causes dose-dependent prolongation of PR interval; second- or third-degree AV block reported rarely. Patients with underlying structural heart disease, preexisting conduction system abnormalities, cardiomyopathies, and ischemic heart disease may be at increased risk for developing cardiac conduction abnormalities; ECG monitoring recommended in such patients. Concomitant use of ritonavir-boosted saquinavir and other drugs that prolong the PR interval (e.g., calcium-channel blocking agents, β-adrenergic blockers, digoxin, atazanavir) not evaluated. Use ritonavir-boosted saquinavir with caution in patients receiving other drugs that prolong the PR interval, particularly drugs metabolized by CYP3A; clinical monitoring recommended. (See Specific Drugs and Foods under Interactions.)

Ritonavir-boosted saquinavir causes dose-dependent prolongation of QT interval; torsades de pointes reported rarely. Perform ECG prior to initiation of ritonavir-boosted saquinavir. Do not use in patients with QT interval ≥450 msec. Ritonavir-boosted saquinavir may be initiated in those with baseline QT interval <450 msec; however, repeat ECG after approximately 10 days of ritonavir-boosted saquinavir and discontinue the antiretroviral if QT interval is prolonged >20 msec over baseline. ECG monitoring recommended if ritonavir-boosted saquinavir is initiated in patients with CHF, bradyarrhythmias, hepatic impairment, and electrolyte abnormalities. Correct hypokalemia or hypomagnesemia prior to initiating ritonavir-boosted saquinavir; monitor these electrolytes periodically during therapy.

Do not use ritonavir-boosted saquinavir concomitantly with drugs that increase saquinavir plasma concentrations and prolong QT interval. Manufacturer states that concomitant use of ritonavir-boosted saquinavir and drugs with the potential to increase QT interval should be considered only when no alternative therapy is available and potential benefits outweigh risks. Perform ECG prior to initiation of the drugs. Do not use such concomitant therapy in patients with QT interval >450 msec. If baseline QT interval is <450 msec, repeat ECG after 3–4 days of concomitant therapy. If QT interval is prolonged >20 msec over baseline, clinician should use best clinical judgement regarding discontinuing ritonavir-boosted saquinavir and/or the other drug. Cardiology consult recommended if drug discontinuation or interruption is being considered on the basis of ECG assessment.

Interactions

Saquinavir must be used with a pharmacokinetic enhancer (i.e., low-dose ritonavir). Failure to administer saquinavir with recommended dosage of low-dose ritonavir may result in inadequate antiretroviral effects. When ritonavir-boosted saquinavir is used, consider cautions, precautions, contraindications, and drug interactions associated with both saquinavir and low-dose ritonavir.

Do not use saquinavir with the pharmacokinetic enhancer cobicistat. Cobicistat is not interchangeable with low-dose ritonavir and dosage recommendations for concomitant use of saquinavir and cobicistat not established.

Concomitant use of ritonavir-boosted saquinavir with certain drugs is not recommended or requires particular caution. (See Specific Drugs and Foods under Interactions.)

Consider potential drug interactions prior to and during use of ritonavir-boosted saquinavir; monitor for adverse effects associated with each drug.

Hyperglycemic Effects

Hyperglycemia, new-onset diabetes mellitus, or exacerbation of preexisting diabetes mellitus reported with use of HIV PIs; diabetic ketoacidosis has occurred.

Monitor blood glucose and initiate or adjust dosage of oral hypoglycemic agent or insulin as needed.

Hepatic Effects

Exacerbation of chronic liver dysfunction reported in patients with HBV or HCV, cirrhosis, or other underlying liver abnormalities. (See Hepatic Impairment under Cautions.)

Hemophilia A and B

Spontaneous bleeding noted with HIV PIs; causal relationship not established.

Caution in patients with history of hemophilia type A or B. Increased hemostatic (e.g., antihemophilic factor) therapy may be needed.

Hyperlipidemia

Elevated cholesterol and/or triglycerides reported. Markedly elevated triglycerides are a risk factor for developing pancreatitis.

Monitor cholesterol and triglycerides prior to and periodically during ritonavir-boosted saquinavir therapy. Manage lipid disorders as clinically appropriate. (See HMG-CoA Reductase Inhibitors under Interactions.)

Lactose Intolerance

Each 200-mg capsule contains 63.3 mg of anhydrous lactose; this quantity should not induce specific symptoms of lactose intolerance.

Adipogenic Effects

Possible redistribution or accumulation of body fat, including central obesity, dorsocervical fat enlargement (“buffalo hump”), peripheral wasting, breast enlargement, and general cushingoid appearance. Mechanisms and long-term consequences unknown; causal relationship not established.

Immune Reconstitution Syndrome

During initial treatment, patients who respond to antiretroviral therapy may develop an inflammatory response to indolent or residual opportunistic infections (e.g., Mycobacterium avium complex [MAC], M. tuberculosis, cytomegalovirus [CMV], Pneumocystis jirovecii [formerly P. carinii]); this may necessitate further evaluation and treatment.

Autoimmune disorders (e.g., Graves' disease, polymyositis, Guillain-Barré syndrome) also reported in the setting of immune reconstitution; time to onset is variable and can occur many months after initiation of antiretroviral therapy.

HIV Resistance

Possibility of HIV-1 resistant to saquinavir and possible cross-resistance to other HIV PIs. Continued saquinavir therapy following loss of viral suppression may increase likelihood of cross-resistance to other HIV PIs.

Specific Populations

Pregnancy

Category B.

Antiretroviral Pregnancy Registry at 800-258-4263 or [Web].

Experts state ritonavir-boosted saquinavir not recommended for initial treatment in antiretroviral-naive pregnant women because of limited data, potential toxicities (e.g., prolonged PR and QT intervals requiring ECG monitoring), high pill burden, and need for twice-daily dosing.

Lactation

Distributed into milk in rats; not known whether distributed into human milk.

Instruct HIV-infected women not to breast-feed because of risk of HIV transmission and risk of adverse effects in the infant.

Pediatric Use

Dosages of ritonavir-boosted saquinavir that are effective for treatment of HIV-1 infection in children <16 years of age and below threshold for corrected QT (QTc) and PR interval prolongation not identified to date.

Geriatric Use

Insufficient experience in those ≥65 years of age to determine whether they respond differently than younger adults.

Use caution because of age-related decreases in hepatic, renal, and/or cardiac function and concomitant disease and drug therapy.

Hepatic Impairment

Contraindicated in severe hepatic impairment. Although usual dosage can be used in mild or moderate hepatic impairment, some experts recommend caution.

Renal Impairment

Use caution in severe renal impairment.

Common Adverse Effects

Diarrhea, abdominal discomfort, nausea, vomiting, fatigue.

Interactions for Saquinavir

Metabolized by CYP3A.

Inhibits CYP3A.

Substrate for P-glycoprotein (P-gp).

Drugs Affecting or Metabolized by Hepatic Microsomal Enzymes

Pharmacokinetic interactions likely with drugs that are inhibitors, inducers, or substrates of CYP3A with possible alteration in metabolism of saquinavir and/or other drug.

Drugs Affecting or Affected by P-gp Transport

Potential pharmacokinetic interaction with drugs that are inhibitors, inducers, or substrates of P-gp with possible alteration in pharmacokinetics of saquinavir and/or other drug.

Drugs that Prolong the QT or PR Interval

Dose-dependent prolongation of QT and PR intervals has been reported in individuals receiving ritonavir-boosted saquinavir; additive effects on QT and/or PR interval prolongation may occur if ritonavir-boosted saquinavir is used concomitantly with other drugs known to have similar effects. Concomitant use with other drugs known to prolong QT and/or PR intervals (e.g., class IA and class III antiarrhythmic agents, neuroleptics, phosphodiesterase type 5 inhibitors if used for PAH, some antidepressants, some anti-infectives, some antihistamines) not recommended. (See Cardiovascular Effects under Cautions.)

Specific Drugs and Foods

Drug or Food

Interaction

Comments

Alfentanil, fentanyl

Alfentanil, fentanyl: Possible increased opiate concentrations and accentuated alfentanil- or fentanyl-associated adverse effects (e.g., respiratory depression, apnea, bradycardia)

Fentanyl: Monitor clinically, especially for potentially fatal respiratory depression

Alfuzosin

Possible increased alfuzosin concentrations; may result in hypotension

Concomitant use contraindicated

Antiarrhythmic agents (amiodarone, disopyramide, dofetilide, dronedarone, flecainide, ibutilide, systemic lidocaine, propafenone, quinidine, sotalol)

Amiodarone, disopyramide, dofetilide, dronedarone, flecainide, systemic lidocaine, propafenone, quinidine: Possible increased antiarrhythmic agent concentrations; potential for serious or life-threatening effects (e.g., cardiac arrhythmias)

Ibutilide, sotalol: Possible additive QT and/or PR interval prolongation

Amiodarone, disopyramide, dofetilide, flecainide, systemic lidocaine, propafenone, quinidine: Concomitant use contraindicated

Dronedarone: Experts state concomitant use with ritonavir-boosted saquinavir contraindicated

Ibutilide, sotalol: Concomitant use not recommended

Anticoagulants, oral

Apixaban: Increased apixaban concentrations expected

Dabigatran: Possible increased dabigatran concentrations

Edoxaban, rivaroxaban: Increased anticoagulant concentrations

Warfarin: Possible altered warfarin concentrations

Apixaban, edoxaban, rivaroxaban: Avoid concomitant use

Dabigatran: Dosage adjustments not needed in patients with Clcr >50 mL/minute; avoid concomitant use in those with Clcr <50 mL/minute

Warfarin: Monitor INR, especially when initiating or discontinuing ritonavir-boosted saquinavir; adjust warfarin dosage as needed

Anticonvulsants (carbamazepine, ethosuximide, lamotrigine, phenobarbital, phenytoin)

Carbamazepine: Possible decreased saquinavir concentrations and increased carbamazepine concentrations

Ethosuximide: Possible increased ethosuximide concentrations

Lamotrigine: Possible decreased lamotrigine concentrations

Phenobarbital: Possible decreased saquinavir concentrations

Phenytoin: Possible decreased saquinavir concentrations and decreased phenytoin concentrations

Carbamazepine, phenobarbital, phenytoin: Concomitant use not recommended; experts state consider alternative anticonvulsant; if used concomitantly, monitor anticonvulsant and saquinavir concentrations and assess virologic response

Ethosuximide: Monitor for ethosuximide-associated adverse effects

Lamotrigine: Increased lamotrigine dosage may be needed; consider monitoring lamotrigine concentrations; consider alternative anticonvulsant

Antidepressants, SSRIs

Citalopram, escitalopram, fluoxetine, paroxetine, sertraline: Data not available regarding concomitant use with ritonavir-boosted saquinavir

Fluvoxamine: Possible altered saquinavir and ritonavir concentrations

Citalopram, escitalopram, fluoxetine, paroxetine, sertraline: Titrate SSRI dosage based on clinical response

Fluvoxamine: Consider alternative therapy

Antidepressants, tricyclic or tetracyclic

Amitriptyline, clomipramine, desipramine, imipramine, maprotiline, nortriptyline: Increased antidepressant concentrations expected

In patients receiving ritonavir-boosted saquinavir, titrate antidepressant dosage based on clinical assessment and/or plasma concentrations; use lowest possible antidepressant dosage

Antifungals, azoles

Fluconazole: Data not available regarding concomitant use with ritonavir-boosted saquinavir

Isavuconazonium (prodrug of isavuconazole): Possible increased isavuconazole concentrations and altered saquinavir concentrations

Itraconazole: Possible pharmacokinetic interaction may affect both drugs

Ketoconazole: Increased ketoconazole concentrations and AUC; saquinavir pharmacokinetics not affected

Posaconazole: Possible increased posaconazole and saquinavir concentrations

Voriconazole: Possible decreased voriconazole concentrations

Fluconazole: Some experts state dosage adjustments not needed

Isavuconazonium: Consider monitoring isavuconazole concentrations; monitor for saquinavir-associated adverse effects and virologic efficacy

Itraconazole: Manufacturer states itraconazole dosage >200 mg daily not recommended with ritonavir-boosted saquinavir; experts state consider monitoring itraconazole concentrations to guide dosage adjustments; do not exceed itraconazole dosage of 200 mg daily unless plasma concentrations used to guide dosage

Ketoconazole: Ketoconazole dosage >200 mg daily not recommended with ritonavir-boosted saquinavir

Posaconazole: Consider monitoring posaconazole concentrations; monitor for saquinavir-associated adverse effects

Voriconazole: Concomitant use not recommended unless potential benefits outweigh risks; if used concomitantly, consider monitoring voriconazole concentrations and adjust dosage accordingly

Antimycobacterials (bedaquiline, rifabutin, rifampin, rifapentine)

Bedaquiline: Possible increased bedaquiline concentrations; clinical importance unknown

Rifabutin: If used with ritonavir-boosted saquinavir, increased concentrations of rifabutin and its active metabolite; slightly decreased saquinavir concentrations; no change in ritonavir concentrations

Rifampin: If used with ritonavir-boosted saquinavir, markedly decreased saquinavir AUC (80%) and increased incidence of hepatotoxicity (markedly increased serum transaminases)

Rifapentine: Possible decreased saquinavir concentrations

Bedaquiline: Use concomitantly with ritonavir-boosted saquinavir with caution and only if potential benefits outweigh risks; monitor for QTc interval prolongation and liver dysfunction

Rifabutin: If used concomitantly with ritonavir-boosted saquinavir, saquinavir manufacturer states use usual dosage of ritonavir-boosted saquinavir and decrease rifabutin dosage by at least 75% (i.e., maximum rifabutin dosage of 150 mg every other day or 150 mg 3 times weekly); some experts recommend rifabutin dosage of 150 mg once daily or 300 mg 3 times weekly; increase monitoring for antimycobacterial effects and adverse events and consider monitoring plasma rifabutin concentrations

Rifampin: Concomitant use contraindicated

Rifapentine: Concomitant use not recommended

Antipsychotics (clozapine, haloperidol, lurasidone, phenothiazines, pimozide, quetiapine, sertindole, ziprasidone)

Clozapine, haloperidol, lurasidone, pimozide, risperidone, sertindole, ziprasidone: Potential for serious and/or life-threatening adverse effects (e.g., cardiac arrhythmias)

Phenothiazines (chlorpromazine, fluphenazine, mesoridazine, perphenazine, prochlorperazine, thioridazine): Potential for serious and/or life-threatening adverse effects (e.g., cardiac arrhythmias)

Quetiapine: Increased quetiapine concentrations expected

Clozapine, haloperidol, lurasidone, pimozide, risperidone, sertindole, ziprasidone: Concomitant use contraindicated

Phenothiazines (chlorpromazine, fluphenazine, mesoridazine, perphenazine, prochlorperazine, thioridazine): Concomitant use contraindicated

Quetiapine: Consider alternative antiretroviral; if ritonavir-boosted saquinavir necessary in patient receiving stable quetiapine dosage, reduce quetiapine dosage to one-sixth of original dosage and monitor for quetiapine efficacy and adverse effects; if quetiapine necessary in patient receiving ritonavir-boosted saquinavir, experts state initiate using lowest quetiapine dosage and titrate as needed

Atazanavir

Increased saquinavir concentrations and AUC; no change in atazanavir concentrations

Potential for serious and/or life-threatening cardiac arrhythmias

Concomitant use contraindicated

Avanafil

Possible increased avanafil concentrations and AUC

Do not use concomitantly

β-adrenergic blocking agents (atenolol, labetalol, metoprolol, nadolol, sotalol, timolol)

Metoprolol, timolol: Possible increased concentrations of the β-blocker

Decreased β-blocker dosage may be needed; adjust based on clinical response; consider use of certain β-blockers not metabolized by CYP isoenzymes (e.g., atenolol, labetalol, nadolol, sotalol)

Benzodiazepines

Alprazolam, clonazepam, clorazepate, diazepam, flurazepam: Increased benzodiazepine concentrations

Midazolam or triazolam: Increased benzodiazepine concentrations; potential for serious and/or life-threatening effects (e.g., prolonged or increased sedation or respiratory depression)

Lorazepam, oxazepam, temazepam: No data, but may have less potential for pharmacokinetic interaction with HIV PIs compared with other benzodiazepines

Alprazolam, clonazepam, clorazepate, diazepam, flurazepam: Clinical importance of interaction unknown; decreased benzodiazepine dosage may be needed; monitor for benzodiazepine-associated adverse effects

Alprazolam or diazepam: Consider using a benzodiazepine with less potential for pharmacokinetic interaction (lorazepam, oxazepam, temazepam)

Oral midazolam or triazolam: Concomitant use contraindicated

Parenteral midazolam: Experts state that a single parenteral midazolam dose can be given with caution in a monitored situation for procedural sedation in patients receiving ritonavir-boosted saquinavir; manufacturer states patient should be monitored closely for respiratory depression and/or prolonged sedation and dosage adjustment considered

Bosentan

Potential for substantially increased bosentan concentrations

In patients already receiving ritonavir-boosted saquinavir for ≥10 days, initiate bosentan using a dosage of 62.5 mg once daily or every other day based on individual tolerability

In patients receiving bosentan, discontinue bosentan for at least 36 hours prior to initiating ritonavir-boosted saquinavir; after ≥10 days of ritonavir-boosted saquinavir, resume bosentan using a dosage of 62.5 mg once daily or every other day based on individual tolerability

Buspirone

Increased buspirone concentrations expected

Use concomitantly with caution; use low buspirone dosage and titrate based on clinical response

Calcium-channel blocking agents

Possible increased concentrations of the calcium-channel blocking agent (e.g., amlodipine, diltiazem, felodipine, isradipine, nicardipine, nifedipine, nimodipine, nisoldipine, verapamil)

Use concomitantly with caution; monitor closely and adjust dosage of calcium-channel blocking agent based on clinical response and toxicities

Cisapride

Pharmacokinetic interaction; potential for serious or life-threatening reactions (e.g., cardiac arrhythmias)

Concomitant use contraindicated

Cobicistat

Concomitant use of saquinavir with cobicistat not recommended; dosage recommendations not established

Concomitant use of ritonavir-boosted saquinavir and cobicistat not recommended due to similar effects of cobicistat and ritonavir on CYP3A

Colchicine

Possible increased colchicine concentrations and AUC

Patients with renal or hepatic impairment: Avoid concomitant use of colchicine and ritonavir-boosted saquinavir

Colchicine for treatment of gout flares: In those receiving ritonavir-boosted saquinavir, use initial colchicine dose of 0.6 mg followed by 0.3 mg 1 hour later and repeat dose no earlier than 3 days later

Colchicine for prophylaxis of gout flares: In those receiving ritonavir-boosted saquinavir, decrease colchicine dosage to 0.3 mg once daily in those originally receiving 0.6 mg twice daily or decrease dosage to 0.3 mg once every other day in those originally receiving 0.6 mg once daily

Colchicine for treatment of familial Mediterranean fever (FMF): In those receiving ritonavir-boosted saquinavir, use maximum colchicine dosage of 0.6 mg daily (may be given as 0.3 mg twice daily)

Corticosteroids (beclomethasone, budesonide, dexamethasone, fluticasone, methylprednisolone, prednisolone, prednisone, triamcinolone)

Beclomethasone (orally inhaled, intranasal): Clinically important pharmacokinetic interactions not expected

Budesonide or fluticasone (orally inhaled, intranasal): Increased corticosteroid concentrations; may result in adrenal insufficiency or Cushing's syndrome

Methylprednisolone, prednisolone, triamcinolone (intra-articular or other local injections): Increased corticosteroid concentrations; may result in adrenal insufficiency or Cushing's syndrome

Budesonide, prednisone (systemic): Increased corticosteroid concentrations; may result in adrenal insufficiency or Cushing's syndrome; budesonide (systemic) may decrease saquinavir concentrations and virologic efficacy

Dexamethasone (systemic): Possible decreased saquinavir concentrations

Budesonide or fluticasone (orally inhaled, intranasal): Do not use concomitantly unless potential benefits of intranasal or inhaled corticosteroid outweigh risks of systemic corticosteroid adverse effects; consider alternative (e.g., beclomethasone); if concomitant use with fluticasone necessary, reduce fluticasone dosage and monitor for local and systemic effects

Methylprednisolone, prednisolone, triamcinolone (intra-articular or other local injections): Do not use concomitantly; consider alternative nonsteroidal therapies; if intra-articular corticosteroid required, use alternative antiretroviral that does not alter CYP3A activity (e.g., dolutegravir, raltegravir)

Budesonide, prednisone (systemic): Use concomitantly with caution only when potential benefits outweigh risks of systemic corticosteroid adverse effects

Dexamethasone (systemic): Concomitant use not recommended; consider alternative corticosteroid for long-term therapy

Daclatasvir

Possible increased daclatasvir concentrations

If used concomitantly, use daclatasvir dosage of 30 mg once daily

Dapsone

Possible serious and/or life-threatening cardiac arrhythmias

Concomitant use contraindicated

Darunavir

Decreased darunavir concentrations and AUC and no effect on saquinavir concentrations and AUC with darunavir 400 mg, ritonavir 100 mg, and saquinavir 1 g twice daily

No in vitro evidence of antagonistic antiretroviral effects

Appropriate dosages for concomitant use with respect to safety and efficacy not established; concomitant use of ritonavir-boosted darunavir and saquinavir not recommended

Delavirdine

Possible increased saquinavir concentrations and AUC; no clinically important effect on delavirdine pharmacokinetics

Concomitant use with ritonavir-boosted saquinavir not evaluated

Concomitant use not recommended; if concomitant use required, frequently monitor liver function

Didanosine

In vitro evidence of additive or synergistic antiretroviral effects

Digoxin

Ritonavir-boosted saquinavir: Increased digoxin concentrations

Use concomitantly with caution; monitor digoxin concentrations; may need to reduce digoxin dose

Dolutegravir

Specific data regarding concomitant use not available

Some experts state dosage adjustments not needed

Efavirenz

Decreased saquinavir plasma concentrations and AUC; decreased efavirenz concentrations

In vitro evidence of additive antiretroviral effects

Manufacturer of saquinavir states concomitant use not recommended; appropriate dosages for concomitant use with respect to safety and efficacy not established

Some experts recommend using usual dosage of ritonavir-boosted saquinavir (saquinavir 1 g and ritonavir 100 mg twice daily) with efavirenz

Elbasvir and grazoprevir

Fixed combination of elbasvir and grazoprevir (elbasvir/grazoprevir): Possible increased risk of elevated ALT concentrations due to substantially increased grazoprevir concentrations

Elbasvir/grazoprevir: Concomitant use contraindicated

Elvitegravir

Cobicistat-boosted elvitegravir: Possible altered elvitegravir, cobicistat, and/or saquinavir concentrations if used with ritonavir-boosted saquinavir

Cobicistat-boosted elvitegravir: Do not use concomitantly with ritonavir-boosted saquinavir

Emtricitabine

In vitro evidence of additive or synergistic antiretroviral effects

Enfuvirtide

No clinically important interactions reported

Eplerenone

Increased eplerenone concentrations expected

Experts state concomitant use contraindicated

Ergot alkaloids (dihydroergotamine, ergotamine, methylergonovine)

Possibility of pharmacokinetic interaction; potential for serious or life-threatening reactions (e.g., acute ergot toxicity)

Concomitant use contraindicated

If treatment of uterine atony and excessive postpartum bleeding is indicated in a woman receiving saquinavir, use methylergonovine maleate (Methergine) only if alternative treatments cannot be used and if potential benefits outweigh risks; use methylergonovine at lowest dosage and shortest duration possible

Estrogens/progestins

Hormonal contraceptives: Possible decreased ethinyl estradiol concentrations

Etonogestrel-releasing subdermal implants, transdermal ethinyl estradiol and norelgestromin: Data not available

Alternative or additional contraceptive measures should be used when estrogen-based oral contraceptive is used concomitantly with ritonavir-boosted saquinavir

Etonogestrel-releasing subdermal implants, transdermal ethinyl estradiol and norelgestromin: Consider alternative or additional method of contraception or alternative antiretroviral

Etravirine

Ritonavir-boosted saquinavir: Decreased etravirine concentrations and AUC; no change in saquinavir concentrations and AUC

No in vitro evidence of antagonistic antiretroviral effects

Dosage adjustments not needed

Decrease in systemic exposure to etravirine similar to that in patients receiving etravirine in conjunction with ritonavir-boosted darunavir (a combination found to be safe and effective)

Flibanserin

Increased flibanserin concentrations expected

Experts state concomitant use contraindicated

Fosamprenavir

No clinically important pharmacokinetic interactions with ritonavir-boosted saquinavir

In vitro evidence of synergistic antiretroviral effects

Appropriate dosages for concomitant use with respect to safety and efficacy not established

Fusidic Acid

Possible increased saquinavir, ritonavir, and fusidic acid concentrations; possible increased risk of saquinavir- and fusidic acid-associated adverse effects

Concomitant use not recommended

Garlic

Garlic supplements: Decreased saquinavir plasma concentrations and AUC

Data not available on concomitant use with ritonavir-boosted saquinavir

Garlic supplements: Do not use in patients receiving ritonavir-boosted saquinavir

Grapefruit juice

Oral bioavailability of saquinavir increased

Halofantrine

Potential for serious and/or life-threatening cardiac arrhythmias

Concomitant use contraindicated

HMG-CoA reductase inhibitors (statins)

Atorvastatin, lovastatin, simvastatin: Decreased clearance and increased concentrations of statins with potential for increased risk of myopathy and/or rhabdomyolysis

Pravastatin: If used with ritonavir-boosted saquinavir, decreased pravastatin AUC

Atorvastatin: Carefully titrate atorvastatin dosage using lowest necessary dosage; do not exceed atorvastatin dosage of 20 mg daily

Lovastatin: Concomitant use contraindicated

Pitavastatin: Experts state dosage adjustments not needed

Pravastatin: Experts state dosage adjustments not needed

Rosuvastatin: Carefully titrate rosuvastatin dosage using lowest necessary dosage; monitor for toxicities

Simvastatin: Concomitant use contraindicated

Immunosuppressive agents (cyclosporine, everolimus, sirolimus, tacrolimus)

Cyclosporine, everolimus, sirolimus: Increased immunosuppressive agent concentrations expected

Cyclosporine, everolimus, sirolimus: Monitor immunosuppressive agent concentrations; some experts state initiate immunosuppressive agent with adjusted dosage to account for potential increased concentrations, monitor for toxicities, consult specialist if needed

Tacrolimus: Concomitant use contraindicated

Indinavir

Increased saquinavir concentrations; may result in nephrolithiasis

Data not available on concomitant use with ritonavir-boosted saquinavir

Concomitant use not recommended; appropriate dosages for concomitant use with respect to safety and efficacy not established

Ivabradine

Increased ivabradine concentrations expected

Experts state concomitant use contraindicated

Lamivudine

In vitro evidence of additive or synergistic antiretroviral effects

Ledipasvir and sofosbuvir

Fixed combination of ledipasvir and sofosbuvir (ledipasvir/sofosbuvir): Clinically important pharmacokinetic interactions not expected

Concomitant use of ledipasvir/sofosbuvir and HIV antiretroviral regimen that includes ritonavir-boosted saquinavir and tenofovir DF: Possible increased tenofovir concentrations

Ledipasvir/sofosbuvir: Dosage adjustments not needed

Concomitant use of ledipasvir/sofosbuvir and HIV antiretroviral regimen that includes ritonavir-boosted saquinavir and tenofovir DF: Experts state consider alternative HCV treatment or an alternative antiretroviral regimen; if concomitant use necessary, monitor for tenofovir-associated adverse effects

Lopinavir

Fixed combination of lopinavir and ritonavir (lopinavir/ritonavir): Increased saquinavir concentrations; potential additive effects on QT and/or PR interval prolongation

Saquinavir concentrations achieved with a regimen of saquinavir 1 g twice daily with lopinavir 400 mg/ritonavir 100 mg twice daily are similar to those with ritonavir-boosted saquinavir (saquinavir 1 g and ritonavir 100 mg twice daily)

In vitro evidence of additive to synergistic antiretroviral effects

Use concomitantly with caution

If used concomitantly, recommended dosage is saquinavir 1 g twice daily with lopinavir 400 mg/ritonavir 100 mg twice daily

Once-daily regimen of lopinavir/ritonavir not studied in conjunction with saquinavir

Macrolides (clarithromycin, erythromycin)

Clarithromycin: Increased saquinavir and clarithromycin AUC; decreased 14-hydroxyclarithromycin AUC; potential serious and/or life-threatening cardiac arrhythmias

Erythromycin: Potential serious and/or life-threatening cardiac arrhythmias

Clarithromycin: Concomitant use contraindicated; consider alternative macrolide (e.g., azithromycin);

Erythromycin: Concomitant use contraindicated

Maraviroc

Ritonavir-boosted saquinavir: Increased maraviroc concentrations and AUC

No in vitro evidence of antagonistic antiretroviral effects

Ritonavir-boosted saquinavir: Recommended dosage of maraviroc is 150 mg twice daily

Mefloquine

Low-dose ritonavir: Decreased ritonavir concentrations and AUC; no effect on mefloquine concentrations

Ritonavir-boosted saquinavir: Data not available

Ritonavir-boosted saquinavir: Use concomitantly with caution

Methadone

Decreased methadone concentrations with ritonavir-boosted saquinavir

Potential for additive QT and/or PR interval prolongation

Use concomitantly with caution; monitor closely for opiate withdrawal and increase methadone dosage as clinically indicated

Nefazodone

Possible increased saquinavir concentrations

Monitor for saquinavir-associated adverse effects

Nelfinavir

Increased saquinavir concentrations and increased nelfinavir concentrations

In vitro evidence of additive antiretroviral effects

Concomitant use not recommended

Nevirapine

Decreased saquinavir concentrations and AUC; nevirapine concentrations not affected

Concomitant use with ritonavir-boosted saquinavir not evaluated

In vitro evidence of additive or synergistic antiretroviral effects

Concomitant use not recommended; appropriate dosages for concomitant use with respect to safety and efficacy not established

Ombitasvir, paritaprevir, and ritonavir

Fixed combination of ombitasvir, paritaprevir, and ritonavir with or without dasabuvir: Concomitant use contraindicated

Pentamidine

Possible serious and/or life-threatening cardiac arrhythmias

Concomitant use contraindicated

Proton-pump inhibitors

Omeprazole with ritonavir-boosted saquinavir: Increased saquinavir concentrations

Caution advised if ritonavir-boosted saquinavir used with a proton-pump inhibitor; monitor for saquinavir toxicities (GI symptoms, increased triglycerides, deep-vein thrombosis, QT-interval prolongation)

Quinine

Possible serious and/or life-threatening cardiac arrhythmias

Concomitant use contraindicated

Quinupristin and dalfopristin

Fixed combination of quinupristin and dalfopristin (quinupristin/dalfopristin): Possible increased saquinavir concentrations

Quinupristin/dalfopristin: Use concomitantly with caution; monitor for saquinavir-associated adverse effects

Raltegravir

Specific data regarding concomitant use not available

In vitro evidence of additive to synergistic antiretroviral effects

Experts state dosage adjustments not needed if raltegravir used concomitantly with ritonavir-boosted saquinavir

Ranolazine

Experts state concomitant use contraindicated

Rilpivirine

Ritonavir-boosted saquinavir: Possible increased rilpivirine concentrations; not expected to affect saquinavir concentrations

No in vitro evidence of antagonistic antiretroviral effects

Ritonavir-boosted saquinavir: Dosage adjustments not needed

Ritonavir

Substantially increased saquinavir concentrations when saquinavir 1 g twice daily used with low-dose ritonavir (100 mg twice daily)

Concomitant low-dose ritonavir used as a pharmacokinetic enhancer (pharmacokinetic booster) for therapeutic advantage (ritonavir-boosted saquinavir)

Ritonavir-boosted saquinavir causes dose-dependent prolongation of QT and PR intervals; torsades de pointes and complete heart block reported

Recommended dosage is saquinavir 1 g twice daily with ritonavir 100 mg twice daily

Monitor ECG and electrolytes prior to and during therapy with ritonavir-boosted saquinavir (see Cardiovascular Effects under Cautions)

St. John’s wort (Hypericum perforatum)

Possible decreased saquinavir concentrations; potential loss of virologic response and development of resistance

Do not use concomitantly

Salmeterol

Possible increased salmeterol concentrations and increased risk of QT interval prolongation, palpitations, or sinus tachycardia

Concomitant use not recommended

Sildenafil

Increased sildenafil concentrations and increased risk of sildenafil-associated adverse effects (e.g., hypotension, visual disturbances, prolonged erection)

Sildenafil for treatment of erectile dysfunction: Use caution and reduce sildenafil dosage (do not exceed 25 mg every 48 hours); closely monitor for adverse effects

Sildenafil for treatment of PAH: Concomitant use contraindicated; safe and effective dosage for concomitant use not established

Simeprevir

Possible altered (increased or decreased) simeprevir concentrations

Concomitant use not recommended

Stavudine

In vitro evidence of additive or synergistic antiretroviral effects

Suvorexant

Increased suvorexant concentrations expected

Experts state concomitant use not recommended

Tadalafil

Possible increased tadalafil concentrations and increased risk of tadalafil-associated adverse effects (e.g., hypotension, visual disturbances, prolonged erection)

Tadalafil for treatment of erectile dysfunction: Use initial tadalafil dosage of 5 mg; do not exceed a single dose of 10 mg in 72 hours; monitor closely for adverse effects

Tadalafil for treatment of benign prostatic hyperplasia: Do not exceed tadalafil dosage of 2.5 mg once daily

Tadalafil (Adcirca) for treatment of PAH: In patients already receiving ritonavir-boosted saquinavir for ≥1 week, use initial tadalafil dosage of 20 mg once daily and increase dosage to 40 mg once daily based on individual tolerability

Avoid use of tadalafil (Adcirca) for treatment of PAH during initiation of ritonavir-boosted saquinavir therapy; in patients receiving tadalafil for treatment of PAH, discontinue tadalafil for at least 24 hours before starting ritonavir-boosted saquinavir; tadalafil can be restarted after ≥1 week of ritonavir-boosted saquinavir therapy using initial tadalafil dosage of 20 mg once daily and increasing dosage to 40 mg once daily based on individual tolerability

If tadalafil is used for treatment of benign prostatic hyperplasia, do not exceed tadalafil dosage of 2.5 mg once daily

Tenofovir

No clinically important change in saquinavir or tenofovir concentrations or AUC with saquinavir 1 g twice daily and ritonavir 100 mg twice daily with tenofovir 300 mg once daily

In vitro evidence of additive or synergistic antiretroviral effects against HIV-1

Dosage adjustments not needed with ritonavir-boosted saquinavir

Ticagrelor

Increased ticagrelor concentrations expected

Avoid concomitant use

Tipranavir

Decreased saquinavir concentrations and AUC

Concomitant use not recommended

Trazodone

Increased trazodone concentrations expected; increased risk of potentially life-threatening cardiac arrhythmias

Concomitant use contraindicated

Vardenafil

Possible increased vardenafil concentrations and increased risk of vardenafil-associated adverse effects (e.g., hypotension, visual disturbances, prolonged erection)

Vardenafil for treatment of erectile dysfunction: Use caution; do not exceed vardenafil dosage of 2.5 mg in 72 hours; monitor closely for adverse effects

Vincamine (not available in US)

Possible increased vincamine concentrations; possible increased risk for cardiac arrhythmias

Use concomitantly with caution; monitor for vincamine-associated adverse effects

Vorapaxar

Increased vorapaxar concentrations expected

Avoid concomitant use

Zidovudine

In vitro evidence of additive or synergistic antiretroviral effects

Zolpidem

Possible increased zolpidem concentrations

Experts state initiate zolpidem at low dosage; dosage reduction may be needed

Saquinavir Pharmacokinetics

Absorption

Bioavailability

Saquinavir mesylate incompletely absorbed from GI tract; oral bioavailability is low (calculated bioavailability 4%).

When used with low-dose ritonavir (ritonavir-boosted saquinavir), there is a 5-fold increase in mean saquinavir AUC, increases of a similar magnitude in trough and peak plasma concentrations, and less interindividual variability in saquinavir pharmacokinetics compared with saquinavir without ritonavir.

When low initial dosage of ritonavir-boosted saquinavir (saquinavir 500 mg twice daily with ritonavir 100 mg twice daily) for the first 7 days of therapy used in treatment-naive HIV-infected patients, saquinavir systemic exposures on day 3 are approximately 70% lower compared with exposures on day 3 in healthy adults receiving the usually recommended dosage (saquinavir 1 g twice daily with ritonavir 100 mg twice daily).

Food

Presence of food in GI tract substantially increases absorption of saquinavir.

Effect of food on ritonavir-boosted saquinavir not evaluated.

Special Populations

In HIV-infected patients with moderate liver impairment (Child-Pugh score 7-9), AUC and peak plasma concentrations are approximately 30% lower compared with HIV-infected patients with normal hepatic function.

Limited data from pediatric patients 4 months to <16 years of age who received saquinavir 50 mg/kg twice daily (up to 1 g twice daily) in conjunction with low-dose ritonavir or lopinavir/ritonavir indicate saquinavir plasma concentrations may be substantially higher in this age group than those reported in adults receiving usual saquinavir dosage; in some cases, steady-state exposures were substantially higher than those historically associated with QTc and PR interval prolongation in adults.

Distribution

Extent

Not fully characterized.

Only minimal amounts cross human placenta.

Distributed into milk in rats; not known whether distributed into human milk.

Negligible concentrations detected in CSF.

Plasma Protein Binding

98%.

Elimination

Metabolism

Metabolized by CYP3A.

Elimination Route

Excreted principally in feces as unabsorbed drug and metabolites.

Half-life

3–6.8 hours.

Stability

Storage

Oral

Capsules

25°C (may be exposed to 15–30°C).

Tablets

25°C (may be exposed to 15–30°C).

Actions and Spectrum

  • Saquinavir in an HIV PI.

  • Active against HIV-1 and HIV-2.

  • Inhibits replication of HIV-1 and HIV-2 by interfering with HIV protease.

  • HIV-1 with reduced susceptibility to saquinavir have been selected in vitro and have emerged during therapy with the drug.

  • Varying degrees of cross-resistance occur among HIV PIs.

Advice to Patients

  • Saquinavir medication guide must be provided to the patient each time the drug is dispensed; importance of patient reading the medication guide prior to initiating saquinavir therapy and each time prescription is refilled.

  • Critical nature of compliance with HIV therapy and importance of remaining under the care of a clinician. Importance of taking as prescribed; do not alter or discontinue antiretroviral regimen without consulting clinician.

  • Importance of using in conjunction with other antiretrovirals—not for monotherapy.

  • Antiretroviral therapy is not a cure for HIV infection; opportunistic infections and other complications associated with HIV disease may still occur.

  • Advise patients that sustained decreases in plasma HIV RNA have been associated with reduced risk of progression to acquired immunodeficiency syndrome (AIDS) and death.

  • Advise patients that effective antiretroviral regimens can decrease HIV concentrations in blood and genital secretions and strict adherence to such regimens in conjunction with risk-reduction measures may decrease, but cannot absolutely eliminate, the risk of secondary transmission of HIV to others. Importance of continuing to practice safer sex (e.g., using latex or polyurethane condoms to minimize sexual contact with body fluids), never sharing personal items that can have blood or body fluids on them (e.g., toothbrushes, razor blades), and never reusing or sharing needles.

  • Importance of taking within 2 hours of a meal, not on an empty stomach.

  • Advise patients that ECG changes (PR and/or QT interval prolongation) have occurred; importance of consulting clinician if symptoms such as dizziness, lightheadedness, fainting, or sensation of abnormal heartbeats occur.

  • Redistribution/accumulation of body fat may occur, with as yet unknown long-term health effects.

  • Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs and dietary or herbal supplements (e.g., St. John’s wort), and any concomitant illnesses.

  • Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed. Advise HIV-infected women not to breast-feed.

  • Importance of advising patients of other important precautionary information. (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

Saquinavir Mesylate

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Oral

Capsules

200 mg (of saquinavir)

Invirase

Genentech

Tablets, film-coated

500 mg (of saquinavir)

Invirase

Genentech

AHFS DI Essentials™. © Copyright 2021, Selected Revisions May 8, 2017. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.

† Use is not currently included in the labeling approved by the US Food and Drug Administration.

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