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 Zambia HIV National Guidelines
 


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 Guide Editors
 Editor In Chief
    Joel E. Gallant, MD, MPH

Pharmacology Editor
    Paul Pham, PharmD, BCPS

Zambia Guideline Team
   Peter Mwaba MMed PhD FRCP
   Alywn Mwinga MMed
   Isaac Zulu MMed MPH
   Velepie Mtonga MMed
   Albert Mwango MBChB
   Jabbin Mulwanda MMed FCS
 

 

 

Drugs>Antiretrovirals>
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Saquinavir

Paul A. Pham, Pharm.D. and John G. Bartlett, M.D.
10-29-2010

Zambia Specific Information

  • Available formulation in Zambia: Capsule: 200 mg.
  • Not first-line protease inhibitor. Inferior to LPV/r in PI-experienced patients, but non-inferior in treatment-naive patients.
  • Inferior to to EFV in ARV-naïve patients(possibly due to higher rates of GI intolerance in SQV/r-treated patients).
  • High pill burden compared to LPV/r.
  • Less effect on triglycerides than LPV/r.
Zambia Information Author: Paul A. Pham, Pharm.D.

INDICATIONS

FDA

  • Treatment of HIV-infection in combination with other ARV agents.

FORMS

brand 
name
 
generic 
Mfg 
brand 
forms
 
cost* 
Invirase Saquinavir (SQV). Previously referred to as SQVhgc (hard-gel cap) to distinguish from SQVsgc (Fortovase), which is no longer manufactured. Rocheoral
hard gel capsule (hgc)
200 mg
$3.72
      oral
tablet
500 mg
$8.55

*Prices represent cost per unit specified and are representative of "Average Wholesale Price" (AWP). AWP Prices were obtained and gathered by Lakshmi Vasist Pharm D using the Red Book, manufacturer's information, and the McKesson database.

^Dosage is indicated in mg unless otherwise noted.

USUAL ADULT DOSING

Pill burden: minimum 6/d (based on 2 SQV 500 mg tabs twice-daily + 1 RTV 100 mg cap twice-daily). Storage: SQV cap and tab can be stored at room temperature.

  • FDA approved dose: SQV 1000 mg twice-daily + RTV 100 mg twice-daily with or without food (500 mg tab preferred: lower pill burden)
  • Not recommended without RTV boosting
  • SQV 2000 mg once-daily + RTV 100 mg once-daily. Unapproved dose with limited clinical data.
  • SQV 400 mg twice-daily + RTV 400 mg twice-daily (rarely used due to poor tolerability)
  • With LPV/r: SQV1000 mg twice-daily + LPV/r 400/100 mg (2 tabs) twice-daily
  • With NFV: SQV 1200 mg twice-daily + NFV 1250 mg twice-daily (large pill burden; rarely used)
  • With ATV: Use with caution. May increase risk of PR interval prolongation. Consider ATV 300 mg + RTV 100 mg +SQV 1500-2000 mg once-daily (limited clinical data). SQV 1200 mg once-daily + ATV 400 mg once-daily (poor clinical outcome) OR SQV 2000 mg once-daily +ATV 400 mg once-daily (based on PK data)
  • With NVP: SQV 1000 mg twice-daily + RTV 100 mg twice-daily + NVP 200 mg twice-daily OR SQV 400 mg twice-daily + RTV 400 mg twice-daily (rarely used) + NVP 200 mg twice-daily .
  • With EFV: Consider SQV 1000 mg twice-daily + RTV 100 mg twice-daily + EFV 600 mg once-daily.
  • With TPV: SQV AUC decreased by 76%. Co-administration not recommended.
  • With IDV: insufficient data.
  • With FPV: Consider SQV1000 mg twice-daily + RTV 100mg twice-daily + FPV 700 mg twice-daily
  • With DRV: Avoid co-administration.
  • With MVC: SQV 1000 mg twice-daily + RTV 100 mg twice-daily + MVC 150 mg twice-daily.
  • With ETR: SQV 1000 mg twice-daily + RTV 100 mg twice-daily + ETR usual dose, but avoid rifabutin co-administration.
  • With RAL: usual doses likely.

RENAL DOSING

DOSING FOR GLOMERULAR FILTRATION OF 50-80

Usual dose likely

DOSING FOR GLOMERULAR FILTRATION OF 10-50

Usual dose likely

DOSING FOR GLOMERULAR FILTRATION OF <10 ML/MIN

Usual dose likely

DOSING IN HEMODIALYSIS

Usual dose (not removed in HD)

DOSING IN PERITONEAL DIALYSIS

No data: Usual dose likely (Unlikely to be removed in dialysis due to high protein binding and large volume of distribution.)

DOSING IN HEMOFILTRATION

No data

ADVERSE DRUG REACTIONS

COMMON

  • GI intolerance: nausea, diarrhea, abdominal pain
OCCASIONAL

RARE

  • QTc prolongation. Avoid in patients at risk for QTc prolongation (e.g structural heart disease, hypokalemia, and other drugs that prolong QTc).
  • PR interval prolongation may occur. 2nd- and 3rd-degree AV block reported. Use with caution in pts with underlying structural heart disease, preexisting conduction system abnormalities, ischemic heart disease or cardiomyopathies.

DRUG INTERACTIONS

Substrate and weak inhibitor of CYP3A4. May modestly increase serum level of other CYP3A4 substrates. Drugs that are inducers of CYP3A4 may decrease SQV levels.

Drug-to-Drug Interactions

Drug-to-Drug Interaction

DrugEffect of InteractionRecommendations/Comments
Clarithromycin Clarithromycin increases SQV AUC 177% and SQV increases clarithromycin AUC 45%Use standard doses.
Fluconazole No significant interactionUsual dose recommended.

Indinavir (IDV) SQV AUC increased 4-7- fold; no effect on IDVIn vitro antagonism. Clinical significance unknown. Avoid co-administration.
Lopinavir/ritonavir (LPV/rtv) Saquinavir AUC: increased 836%; Cmin: increased 1700%Dose: SQV 800-1000 mg twice daily + LPV/r 400/100 mg twice daily.
Nelfinavir (NFV) SQVsgc AUC increased by 3 to 5-fold. NFV AUC increased by 20%Consider: SQV 1200 mg twice daily + NFV 1250 mg bid (limited clinical experience and rarely used)
Rifampin Rifampin: SQV AUC: decreased by 84%Coadministration of rifampin with SQV (as sole PI) is not recommended due to significant decrease in SQV PK parameters. Boosting SQV with RTV is not recommended due to high incidence (39.3%) of hepatotoxicity.
Ritonavir ( RTV ) SQV AUC increased by 20-fold.Recommended doses: RTV 100 mg twice daily + SQV 1000 mg twice daily. RTV 400 mg twice daily + SQV 400 mg twice daily (higher rate of GI intolerance and hepatoxicity). RTV 100 mg + SQV 2000 mg every day (clinical studies in progress).
Etravirine Etravirine AUC decreased 33%. Clinical significance unknown. SQV/r 1000/100 mg twice daily plus standard dose ETR likely.
Maraviroc Maraviroc AUC increased 732% Recommended dose: SQV 1000 mg twice daily + RTV 100 mg twice daily+ MVC 150 mg twice daily.
Darunavir (DRV) DRV AUC decreased 26%. Avoid co-administration.
Fosamprenavir (FPV) SQV AUC decreased 14% (NS). Consider SQV/r 1000/100-200 mg twice daily + FPV 700 mg twice daily
Alfuzosin May increase alfuzosin serum concentrations. Avoid co-administration. Consider doxazosin and terazosin for BPH (with close monitoring).
Alprazolam May increase serum level of alprazolamAvoid co-administration. Consider an alternative benzodiazepine (i.e lorazepam, oxazepam, or temazepam)
AmiodaroneMay significantly increase amiodarone serum levelAvoid co-administration. Data limited to case report of increased amiodarone concentrations with IDV co-administration. RTV, FPV, SQV and ATV manufacturer recommends against use of amiodarone, but all PIs have the same potential of significantly increasing amiodarone serum concentrations and increasing QTc interval. If coadministration can not be avoided, monitor for amiodarone ADRs (PFTs, TSH). Consider monitoring serum concentrations of amiodarone, but its long half-life may make titration difficult.
AmlodipineMay increase serum level of amlodipineApplies to all PIs: Data limited to an interaction study conducted with ATV and diltiazem which resulted in doubling of diltiazem serum level (this led to PR interval prolongation). All PIs and have the potential of prolonging PR interval with calcium channel blocker coadministration. Ca channel blockers should be started with 50% of the recommended dose and slowly titrated with close monitoring of BP and pulse.
Amprenavir (APV) SQV level decreased by 18%. APV intrinsic clearance was not affected.Data based on PK modeling with many confounding variables (i.e EFV in the background regimen). Consider SQV 800 mg three times a day + APV 800 mg three times a day (but APV essentially replaced by FPV).
Artemether (artemisinin)May increase serum level of artemetherApplies to all PIs: Close monitoring for artemether toxicity (bone marrow suppression, bradycardia and seizure)
AstemizoleMay significantly increase astemizole serum level.Contraindicated due to the potential for cardiac arrhythmias. Recommended alternative antihistamine: loratadine, fexofenadine, desloratidine, or cetirizine.
Atorvastatin Atorvastatin increased by 450% (studied with RTV/SQV)Use with caution. Use lowest possible dose of atrovastatin (10mg). Consider pravastatin or rosuvastatin.
AzathioprineInteraction unlikelyApplies to all PIs and NNRTIs: Use standard dose
BepridilMay significantly increase bepridil serum levelApplies to all PIs: No data. The manufacturer of ATV, RTV, and APV does not recommend bepridil coadministration. This contraindication should be extend to all PIs since a significant increase in bepridil serum level can result in pro-arrhythmic events such as VT, PVC, and VFib.
Beta-blockers May increase risk of PR interval prolongation. Use with close monitoring.
CarbamazepineMay decrease serum levels of SQVConsider alternative anticonvulsants (i.e valproic acid, lamotrigine, levetiracetam, or topiramate). Monitor anticonvulsant levels and SQV Cmin with co-administration.
ChlordiazepoxideMay increase serum level of chlordiazepoxideApplies to all PIs: Consider an alternative benzodiazepine (i.e lorazepam, temazepam, or oxazepam)
CisaprideMay significantly increase cisapride serum level.Contraindicated due to potential for cardiac arrhythmias. Recommended alternative: metoclopramide.
Clorazepate May increase serum level of clorazepateApplies to all PIs: Consider an alternative benzodiazepine (i.e lorazepam, temazepam, or oxazepam)
CyclophosphamideMay increase serum level of cyclophosphamideApplies to all PIs: Data limited to an interaction study conducted with IDV resulting in a 50% increase in cyclophosphamide serum level. Since all PIs have the potential of increasing cyclophosphamide levels, close monitoring of cyclophosphamide-induced toxicity is recommended.
CyclosporineCyclosporine Cmin: increased 300%Case report of significant increase of cyclosporine levels. Monitor serum level of cyclosporine closely with co-administration. Cyclosporine dose may need to be decreased.
DexamethasoneMay decrease SQV serum levelsClinical significance unknown
Digoxin Digoxin AUC and Cmax increased by 49% and 27%, respectively. Reduce digoxin dose with SQV/r co-administration. Magnitude of interaction higher in females (AUC increased 74% in females vs. 33% in males). Use with close monitoring. Significant increased in PR prolongation observed.
Digoxin Digoxin AUC increased 49%. Monitor digoxin serum concentrations closely with SQV/r co-administration. The dose of digoxin may need to be reduced.
DiltiazemMay increase serum level of diltiazemApplies to all PIs: Data limited to an interaction study conducted with ATV which resulted in doubling of diltiazem serum level (this led to PR interval prolongation). All PIs have the potential of prolonging PR interval with diltiazem coadministration. Diltiazem should be started with 50% of the recommended dose and slowly titrated with close monitoring of BP and pulse.
DisopyramideMay increase disopyramide serum levelsApplies to all PIs: No data. Monitor disopyramide serum level (target: 2-7.5 mcg/mL).
DocetaxelMay increase serum level of docetaxelApplies to all PIs: No data. Close monitoring of chemotherapy-induced toxicity recommended.
DofetilideMay significantly increase serum level of dofetilide and increase QTc.Applies to all PIs: No data, but co-administration should be avoided.. Monitor QTc closely and adjust dofetilide dosing based on QTc prolongation and renal function. Consider an alternative class III antiarrhythmic such as bretylium or ibutilide.
Echinacea May decrease SQV serum level. Echinacea decreased (400 mg 4x/d) CYP3A4 substrate (midazolam) by 23%.Clinical significance unknown but should avoided with PIs and NNRTIs until the safety of this combination is further evaluated.
Ergot AlkaloidMay significantly increase serum level of ergotamine resulting in acute ergot toxicityContraindicated. Consider alternative agent for migraine such as sumatriptan (but not eletriptan since it is a CYP3A4 substrate and significant drug-drug interaction occurred with CYP3A4 inhibitor).
Estazolam May increase serum level of estazolamApplies to all PIs: Consider an alternative benzodiazepine (i.e lorazepam, oxazepam, or temazepam)
EthosuximideMay increase serum levels of ethosuximideApplies to all PIs: Consider switching to valproic acid for the treatment of absence seizure.
EtoposideMay increase serum level of etoposideApplies to all PIs: No data. Close monitoring of chemotherapy induced toxicity recommended.
Fatty FoodSQV AUC increased 18-foldSQV should be taken with food.
FelodipineMay increase serum level of felodipineApplies to all PIs: Data limited to an interaction study conducted with ATV and diltiazem which resulted in doubling of diltiazem serum level (this led PR interval prolongation). All PIs has the potential of prolonging PR interval with calcium channel blockers coadministration. Calcium channel blockers should be started with 50% of the dose and slowly titrated with close monitoring of BP and pulse.
Fentanyl May increase fentanyl serum levelUse with caution. Consider morphine.
FlecainideMay increase antiarrhythmic serum levelsApplies to all PIs: Avoid coadministration; if necessary, monitor flecainide trough level with coadministration. Target: 200-1000ng/ml. Toxicity is frequent with trough serum levels above 1000 ng/mL.
Flurazepam May increase serum level of flurazepamApplies to all PIs: Consider an alternative benzodiazepine (i.e lorazepam, oxazepam, or temazepam).
Fluticasone Fluticasone AUC increased 350-fold (studied with RTV 100 mg q12h) Avoid long-term co-administration. Consider beclomethasone.
Garlic supplement SQV Cmin decreased by 49%; AUC: decreased 51%; after 10 d washout period, pharmacokinetic values returned to only 60-70% of baseline.Co-administration not recommended.
GranisetronMay increase serum level of granisetronApplies to all PIs: Due to the large therapeutic index of granisetron, potential interaction is unlikely to be clinically significant.
Grapefruit juice SQV AUC: increased 50% (grapefruit juice 200 mL from concentrate)May be a beneficial interaction.
Heroin (Diamorphine)Drug interactions unlikelyApplies to PIs and NNRTIs: Interaction unlikely but illicit drug use should be avoided for obvious reasons.
IfosphamideMay increase serum level of ifosphamideApplies to all PIs: No data. Close monitoring of chemotherapy-induced toxicity recommended.
IrinoteacanMay increase irinoteacan serum levelNot recommended. All PIs also have the potential for significant interaction with Irinotecan, therefore the coadministration should be done with extreme caution.
Itraconazole SQV: no significant change. Itraconazole level:no significant change.No significant change. Use standard dose of both drugs
Ketoconazole SQV AUC increased 30%Use standard dose. If SQV coadministered with RTV, do not exceed ketoconazole 200 mg/d.
LidocaineMay increase antiarrhythmic serum levelsApplies to all PIs: No data, but co-administration should be avoided.
Lovastatin May increase lovastatin serum levelContraindicated. Recommended alternatives include pravastatin (but pravastatin AUC decreased by 50% with SQV/r), fluvastatin, and rosuvastatin (and possibly atorvastatin). Monitor for adverse effects due to limited clinical data with these agents.
Mefloquine May increase serum levels of mefloquineApplies to all PIs: If available consider mefloquine serum level monitoring. Monitor for mefloquine toxicity (i.e dizziness, LFTs, and periodic ophthalmic examination).
Methadone S-methadone AUC: decreased 25%; R-methadone (active) AUC: decreased 20% (studied with SQV/RTV)Monitor for withdrawal symptoms but unlikely to be significant. Methadone dose may need to be increased if pt experiences withdrawal Sx.
MexiletineMay increase antiarrhythmic serum levelsApplies to all PIs: No data. Use with caution. Monitor EKG and serum level. Serum levels exceeding 1.5-2 mcg/mL have been associated with an increased risk of toxicity.
Midazolam May increase midazolam serum level.Concurrent administration contraindicated due to potential for prolonged sedation. Use alternative: lorazepam, oxazepam, or temazepam. Single dose midazolam may be used (chronic use not recommended).
Milk thistleUnknownData limited to an interaction study with milk thistle and IDV. IDV AUC unchanged and IDV Cmin decreased by 47%. Avoid co-administration. No data available for other PIs and NNRTIs.
MirtazapineMay increase serum level of mirtazapineApplies to all PIs: Use with caution. Consider an alternative antidepressant (i.e SSRI: escitalopram, citalopram, sertraline, or fluoxetine).
MycophenolateInteraction unlikely. No significant interaction observed with NVP.Applies to all PIs and NNRTIs: No significant interaction observed with NVP. Use standard dose.
NefazodoneMay increase serum level of nefazodoneApplies to all PIs: Use with caution. Consider an alternative antidepressant (i.e SSRI: escitalopram, citalopram, sertraline, or fluoxetine).
NifedipineMay increase serum level of nifedipineApplies to all PIs: Data limited to an interaction study conducted with ATV and diltiazem which resulted in doubling of diltiazem serum level (this led PR interval prolongation). All PIs have the potential of prolonging PR interval with calcium channel blocker co-administration. Calcium channel blockers should be started with 50% of the dose and slowly titrated with close monitoring of BP and pulse.
NisoldipineMay increase serum level of nisoldipineApplies to all PIs: Data limited to an interaction study conducted with ATV and diltiazem which resulted in doubling of diltiazem serum level (this led PR interval prolongation). All PIs have the potential of prolonging PR interval with calcium channel blocker coadministration. Calcium channel blockers should be started with 50% of the recommended dose and slowly titrated with close monitoring of BP and pulse.
Oral ContraceptivesNo data for NFV. Ethinyl estradiol AUC decreased by 47%, Norethindrone decreased by 18%.Recommend an alternative form of contraception.
Paclitaxel May increase paclitaxel serum levelApplies to all PIs: Since all PIs have the potential of significantly increasing paclitaxel serum level, close monitoring of paclitaxel-induced toxicity is recommended.
PCPMay significantly increase serum level of PCPApplies to all PIs: Avoid all illicit drug use with PIs.
PhenobarbitalMay decrease serum levels of SQVConsider alternative anticonvulsants (i.e valproic acid, lamotrigine, levetiracetam, or topiramate). Monitor anticonvulsant levels and SQV Cmin with coadministration.
PhenytoinMay decrease serum levels of SQVConsider alternative anticonvulsants (i.e valproic acid, lamotrigine, levetiracetam, or topiramate). Monitor anticonvulsant levels and SQV Cmin with coadministration.
PimozideMay significantly increase pimozide serum level resulting in QTc prolongation.Contraindicated. Consider alternative: olanzapine.
Pravastatin Pravastatin AUC decreased by 50% (studied with SQV/RTV)Clinical significance unknown. May need to increase dose of pravastatin.
Prednisone Prednisolone serum concentration may be increased with SQV/r co-administration. Dose adjustment may be needed with long-term co-administration.
PropafenoneMay increase antiarrhythmic serum levelsApplies to all PIs: No data. Co-administration should be avoided. Serum levels are not routinely recommended due to the poor correlation with efficacy and toxicity.
Proton pump inhibitor (e.g omeprazole) SQV AUC increased 82%. Usual dose recommended.
Quinidine May increase antiarrhythmic serum concentrations and increase QTc prolongation. Avoid co-administration. May increase risk of QTc prolongation. Contraindicated with RTV. With all PIs and NNRTIs co-administration, monitor EKG (QTc) and serum concentrations: Target: 2-5 mcg/mL.
Raltegravir Interaction unlikely Data with RTV (100 mg bid) did not affect RAL PK parameters. SQV/r 1000/100 mg twice daily plus standard dose RAL likely.
RanitidineNo significant interactionUse standard dose
Ranolazine May significantly increase ranolazine serum concentrations. Contraindicated. May increase risk of QTc prolongation.
Rifabutin SQV AUC decreased by 43%.Do not co-administer SQV with rifabutin as a sole PI. Consider RTV 400 mg twice daily + SQV 400 mg twice daily with rifabutin 150 mg 3x/wk OR SQV1000 mg + RTV100 mg twice daily with rifabutin 150 mg every other day (No data, but likely to attain good PK).
Rifapentine SQV serum levels may be significantly decreased.Avoid coadministration. Consider using rifabutin.
Rosuvastatin Other CYP3A4 inhibitor (i.e erythromycin) did not affect rosuvastatin serum level.Applies to PIs and NNRTIs: Interaction unlikely, but close monitoring recommended due to limited clinical data.
Salmeterol May increase salmeterol concentrations. Avoid co-administration. Consider formoterol
SildenafilSildenafil AUC increased by 210% (with SQV1200mg tid).Use with caution. Do not exceed 25 mg of sildenafil in 48-hr period.
Simvastatin Simvastatin AUC: increased 3059% (studied with SQV/RTV)Contraindicated. Recommended alternatives include atorvastatin, pravastatin (but pravastatin AUC decreased by 50% with SQV/r), fluvastatin, and rosuvastatin. Monitor for adverse effects due to limited clinical data with these agents.
SirolimusMay significantly increase serum level of sirolimusApplies to All PIs: Dose sirolimus based on serum level. A significantly reduction of sirolimus dose with all PIs coadministration is highly likely.
St. John's wortMay decrease SQV serum levelContraindicated. Use an alternative (more effective) antidepressant.
TacrolimusMay significantly increase serum level of tacrolimusApplies to all PIs: Dose tacrolimus based on serum level. A significantly reduction of tacrolimus dose with all PIs co-administration is recommended.
TadalafilMay increase serum level of tadalafilApplies to All PIs: Start with 5 mg. Do not exceed 10 mg in 72 hrs. Consider sildenafil due to more clinical data and shorter half-life allowing for easier titration.
TamoxifenMay increase serum level of tamoxifenApplies to all PIs: No data. Close monitoring of tamoxifen-induced toxicity recommended.
TeniposideMay increase serum level of teniposideApplies to all PIs: No data. Close monitoring of teniposide-induced toxicity recommended.
TerfenadineTerfenadine AUC: increased by 368%; Cmax: increased by 253%Contraindicated due to the potential for cardiac arrhythmias. Recommended alternative antihistamine: loratadine, fexofenadine, desloratidine, or cetirizine.
THCBased on data with NFV and IDV interactions are unlikelyApplies to PIs and NNRTIs: Interactions are unlikely but illicit drug use should be avoided for obvious reasons.
TrazadoneMay increase serum level of trazadone and increase risk for QTc prolongation.Applies to All PIs: Use with caution. Consider an alternative antidepressant (i.e SSRI:escitalopram, citalopram, sertraline, or fluoxetine)
Triazolam May significantly increase triazolam serum levelContraindicated. Alternative benzodiazepine that may be used(temazepam, oxazepam, or lorazepam).
VardenafilMay significantly increase serum level of vardenafil.Applies to all PIs: Do not exceed vardenafil 2.5 mg in 72 hrs (with RTV) or 2.5 mg in 24 hrs (with other PIs). Consider sildenafil due to more clinical data and less pronounced interaction. Avoid coadministration with IDV.
VerapamilMay increase serum level of verapamilApplies to all PIs: Data limited to an interaction study conducted with ATV and diltiazem which resulted in doubling of diltiazem serum level (this led PR interval prolongation). All PIs have the potential of prolonging PR interval with calcium channel blocker coadministration. Calcium channel blockers should be started with 50% of the dose and slowly titrated with close monitoring of BP and pulse.
VinblastineMay increase serum level of vinblastineApplies to all PIs: No data. Close monitoring of vinblastine- induced toxicity recommended.
VincristineMay increase serum level of vincristineApplies to all PIs: No data. Close monitoring of vincristine- induced toxicity recommended.
Voriconazole May decrease voriconazole AUC with SQV/r. Voriconazole may increase co-administered SQV.Significant interaction with EFV and RTV (400 mg bid); contraindicated. Voriconazole AUC decreased 39% with RTV 100 mg bid co-administration; avoid co-administration with boosted PI. Consider another antifungal for aspergillosis (i.e ambisome or caspofungin) or use with TDM. Higher dose of voriconazole may be needed.

RESISTANCE

  • L90M: Selected by SQV, resulting in intermediate SQV and NFV resistance, and partial cross-resistance to other PIs.
  • G48V: Selected by SQV, resulting in intermediate SQV resistance and low-level cross-resistance to other PIs.
  • 54V/L, 71VT, 73S, 77I, 82A, 84V, others: Multiple mutations increase resistance.

PHARMACOLOGY

Pharmacology

COMMENTS

.

  • Pros: Less effect on lipids and non-inferior efficacy compared to LPV/r.
  • Cons: Inferior to LPV/r in PI-experienced pts; higher pill burden than the preferred or alternative PIs.  Potential for QTc and PR interval prolongation.

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