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INVIRASE and PPIs
HIV Doesn’t Stop Them. Their Meds Shouldn’t.
Boosted INVIRASE has maintained therapeutic levels with
proton pump inhibitors (omeprazole) 1
In a pharmacokinetic (PK) study of healthy volunteers to investigate the interactions of boosted INVIRASE 500 mg tablet (1000/100 mg twice daily) in combination with a proton pump inhibitor:
- Concomitant use with 40 mg of omeprazole results in steady-state saquinavir AUC and Cmax values 82% and 75% higher than those seen with INVIRASE/r alone 1
- During the PK study no specific adverse events or unusual short-term toxicities were observed 1
- If omeprazole or proton pump inhibitor is taken concomitantly with INVIRASE/r, monitoring for saquinavir toxicity is recommended 1
Previously reported dosing studies with high saquinavir exposures (comparable to exposure levels seen in this PK study) provide detailed safety data; during a 24-week trial, there were no adverse events of Grade 3 or 4 severity recorded, and no patients permanently withdrew from the trial due to adverse events. 2
- The combined evidence from clinical trials and published literature and data do not suggest a safety concern which may result from the concomitant use of saquinavir and a PPI 2,3
Based on this data, no dose adjustments are necessary and patients do not need to space prescription or over-the-counter (OTC) medications and boosted INVIRASE and/or change their medication regimen to treat symptoms of acid reflux or heartburn.
There is a significant drug-drug interaction between some commonly used ARVs and GI treatments, resulting in subtherapeutic levels that can lead to resistance and loss of treatment options. 4
- Gastrointestinal (GI) problems—treatment-related or not—are common among people living with HIV/AIDS 4
- Over-the-counter and prescription agents that affect GI acidity are commonly used by patients for immediate relief of symptoms and to resolve causes of heartburn, gastroesophogeal reflux disease (GERD), ulcers, etc. 4
- Proton pump inhibitors (like omeprazole) substantially decrease plasma concentrations of certain ARVs that require an acidic environment for absorption; concomitant use of PPIs and these ARVs may result in loss of therapeutic effect and development of resistance 5,6
Are your HIV+ patients managing both HIV and gastrointestinal problems?
Results from an online survey of 200 participants show that among patients taking antiretroviral therapy (93% for >1 year) : 4
|
|
Any GI Med |
R x PPI |
OTC PPI/H2B |
ANTACID |
Overall |
Taken since starting HIV therapy? |
88% |
39% |
51% |
77% |
(n=200) |
Within last month? |
53% |
23% |
14% |
32% |
PI Users Only |
Taken since starting HIV therapy? |
86% |
42% |
46% |
73% |
(n=110) |
Within last month? |
52% |
25% |
13% |
28% |
- 62% report heartburn
- 30% report GERD
- 13% report new ulcers
- 56% use over-the-counter drugs to treat stomach problems
- 39% use both over-the-counter and prescription drugs
Boosted INVIRASE has maintained therapeutic levels with proton pump inhibitors (like omeprazole) and levels of unboosted saquinavir did not drop with H2 antagonists (like Zantac®).
INVIRASE 500
More Than 10 Years of Study and Clinical Experience With Saquinavir
OTC Zantac is a registered trademark of Pfizer.
Prescription Zantac is a registered trademark of GlaxoSmithKline.
Ritonavir is manufactured by Abbott Laboratories.
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