II. Indications
- HIV Infection (as part of combination therapy)
III. Contraindications
- Age <16 years
-
QTc Prolongation (or risk)
- See below
IV. Mechanism
V. Dosing
-
General
- Used in combination with Ritonavir, in addition to other Antiretrovirals
- Tablets contain lactose
- If taken without food, may have no Antiviral activity
- Take within 2 hours after a full meal
- Meals increase absorption and decrease GI upset
- Adult and age >16 years (all regimens should include Ritonavir)
VI. Adverse Effects
- Rash
- Hyperprolactinemia (rare)
-
Electrocardiogram changes
- Obtain EKG at baseline and 3-4 days after starting medication
- QTc Prolongation (rare Torsades de Pointes)
- Avoid if QTc Prolongation at baseline, congenital Long QT, Hypokalemia, Hypomagnesemia
- Stop if QTc increases >20 msec over baseline
- PR Prolongation (first degree AV Block)
- Second and third degree AV Block is rare
- Avoid if risk of complete Heart Block
- Caution with agents that prolong PR (e.g. Beta Blockers, Calcium Channel Blockers)
VII. Safety
- Avoid in Lactation
- Avoid in pregnancy (despite pregnancy category B status)
VIII. Drug Interactions
- Multiple Drug Interactions
- See Protease Inhibitor
- As with other Protease Inhibitors, check a formal Drug Interaction application before prescribing
-
Rilpivirine
- Stop Rilpivirine at least 2 weeks before starting Saquinavir
- Medication Causes of QTc Prolongation
-
Garlic supplements (do not use with Saquinavir)
- Reduces Saquinavir concentrations by 50%
- Levels may remain reduced even after stopiing Garlic
- Piscitelli (2002) Clin Infect Dis 34:234-8 [PubMed]
-
Statins
- Atorvastatin dose limited to 20 mg
- Rosuvastatin dose limited to lowest effective dose
-
Opioids
- Methadone dose may need to be increased
-
Clarithromycin
- Decrease Clarithromycin dose if Creatinine Clearance <60 ml/min
-
Digoxin
- Monitor levels
IX. Efficacy
- Weak effect and may worsen resistance for better Protease Inhibitors
- Requires high doses that may not be tolerated (lower doses may be ineffective)