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Saquinavir Dosage

Applies to the following strength(s): mesylate 500 mg ; mesylate 200 mg ; 200 mg

The information at Drugs.com is not a substitute for medical advice. Always consult your doctor or pharmacist.

Usual Adult Dose for:

Usual Pediatric Dose for:

Additional dosage information:

Usual Adult Dose for HIV Infection

Standard dose: Saquinavir 1000 mg plus ritonavir 100 mg orally twice a day

Therapy-naive patients (starting therapy with saquinavir/ritonavir):
-The first 7 days: Saquinavir 500 mg plus ritonavir 100 mg orally twice a day
-After 7 days: Saquinavir 1000 mg plus ritonavir 100 mg orally twice a day

Patients switching immediately (no washout period) from another ritonavir-containing regimen or from a NNRTI-based regimen (excluding delavirdine, rilpivirine): Saquinavir 1000 mg plus ritonavir 100 mg orally twice a day

Patients switching from a regimen containing delavirdine or rilpivirine:
-The first 7 days: Saquinavir 500 mg plus ritonavir 100 mg orally twice a day
-After 7 days: Saquinavir 1000 mg plus ritonavir 100 mg orally twice a day

Use: In combination with ritonavir and other antiretrovirals, for the treatment of HIV-1 infection

Usual Adult Dose for Nonoccupational Exposure

US CDC recommendations: Saquinavir 1000 mg plus ritonavir 100 mg (or saquinavir 400 mg plus ritonavir 400 mg) orally twice a day
Duration of therapy: 28 days

Comments:
-Recommended as part of an alternative regimen for nonoccupational postexposure prophylaxis of HIV infection
-This drug (plus ritonavir) should be used with (lamivudine or emtricitabine) plus (zidovudine or stavudine or abacavir or tenofovir or didanosine).
-Prophylaxis should be started as soon as possible, within 72 hours of exposure.
-Current guidelines should be consulted for additional information.

Usual Adult Dose for Occupational Exposure

US Public Health Service working group recommendations: Saquinavir 1000 mg plus ritonavir 100 mg orally twice a day
Duration of therapy: 28 days, if tolerated

Comments:
-Only with expert consultation, as part of an alternative regimen for use as HIV postexposure prophylaxis
-Prophylaxis should be started as soon as possible, preferably within hours after exposure.
-The optimal duration of prophylaxis is unknown and may differ based on institution protocol.
-Current guidelines should be consulted for additional information.

Usual Pediatric Dose for HIV Infection

16 years or older:
Standard dose: Saquinavir 1000 mg plus ritonavir 100 mg orally twice a day

Therapy-naive patients (starting therapy with saquinavir/ritonavir):
-The first 7 days: Saquinavir 500 mg plus ritonavir 100 mg orally twice a day
-After 7 days: Saquinavir 1000 mg plus ritonavir 100 mg orally twice a day

Patients switching immediately (no washout period) from another ritonavir-containing regimen or from a NNRTI-based regimen (excluding delavirdine, rilpivirine): Saquinavir 1000 mg plus ritonavir 100 mg orally twice a day

Patients switching from a regimen containing delavirdine or rilpivirine:
-The first 7 days: Saquinavir 500 mg plus ritonavir 100 mg orally twice a day
-After 7 days: Saquinavir 1000 mg plus ritonavir 100 mg orally twice a day

Comments:
-Doses that are both reliably effective and safe (i.e., below levels of concern for QT and PR interval prolongation) could not be established for pediatric patients younger than 16 years.

Use: In combination with ritonavir and other antiretrovirals, for the treatment of HIV-1 infection

Renal Dose Adjustments

Mild or moderate renal dysfunction: No adjustment recommended.
Severe renal dysfunction or end-stage renal disease: No adjustment recommended; caution recommended.

Liver Dose Adjustments

Mild or moderate liver dysfunction: No adjustment recommended.

When used with ritonavir:
-Severe liver dysfunction: Contraindicated

Dose Adjustments

If serious or severe toxicity occurs during therapy, this drug should be interrupted until cause is determined or toxicity resolves; at that time, resumption of this drug at the full dose may be considered.

Precautions

Consult WARNINGS section for additional precautions.

Dialysis

Data not available

Comments:
-Significant removal via dialysis is not likely (highly protein bound).

Other Comments

Administration advice:
-Must use in combination with ritonavir and other antiretrovirals.
-Administer this drug at the same time as ritonavir and within 2 hours after a full meal.
-Do not administer additional ritonavir in patients already using ritonavir (100 mg twice a day) as part of their antiretroviral regimen.
-Patients unable to swallow capsules: (1) Open capsules and place contents into empty container; (2) Add 15 mL of either sugar syrup or sorbitol syrup (for patients with type 1 diabetes or glucose intolerance) OR 3 teaspoons of jam to the capsule contents in the container; (3) Stir with spoon for 30 to 60 seconds; (4) Administer the full amount prepared for each dose; suspensions should be at room temperature before use.

Storage requirements:
-Store at 25C (77F); excursion permitted to 15C to 30C (59F to 86F); close bottle tightly.

General:
-The following should be considered when starting this drug: Twice-daily use of this drug (plus ritonavir) is supported by safety and pharmacokinetic data; efficacy of this drug (plus ritonavir) has not been compared against efficacy of antiretroviral regimens currently considered standard of care; the number of baseline primary protease inhibitor mutations affects virologic response to this drug (plus ritonavir).
-Ritonavir significantly inhibits metabolism of this drug, increasing plasma saquinavir levels; the manufacturer product information for ritonavir should be consulted.
-Cobicistat is not interchangeable with ritonavir to increase systemic exposure of this drug.

Monitoring:
-Cardiovascular: ECG (before starting and during therapy); PR interval (if used with other agents that prolong PR interval)
-Metabolic: Potassium and magnesium (periodically during therapy); cholesterol and triglyceride levels (prior to therapy and periodically thereafter)

Patient advice:
-Read the US FDA-approved patient labeling (Medication Guide).
-Consult healthcare provider if dizziness, lightheadedness, or palpitations occur.

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