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The Protease Inhibitors (PIs)

Detailed Prescribing Information

October 2005

 

Ritonavir = Norvir
Dosing Forms 100 mg capsules (refrigerate) and suspension 125 mg/cc (nonrefrigerated)
Storage Optimally store ritonavir soft gel caps in the refrigerator.  If necessary ritonavir soft gel caps may be stored outside of a refrigerator for up to 30 days if the ambient temperature is < 77 deg Fahrenheit.
Dosing In boosting strategy: 100-200 mg once or twice a day depending on the regimen (see PI Boosting chart for further info)
Used as active protease inhibitor: over 1-2 weeks, gradually increase dose from 3x100 mg twice a day to 6x100 mg twice a day with food (see usage suggestions below)
Adverse Effects High incidence of GI intolerance (abdominal pain and diarrhea) severely limits the ability to use this drug as an active PI especially in patients who are already ill with concomitant GI disease.
Also perioral paresthesia, hyperlipidemia, fat redistribution, Type II diabetes
Interactions Probably more interactions than any other drug.

Favorable interaction with most other PIs makes this drug the ideal PI booster.  It is usually not an active PI when used this way.

Voriconazole levels are reduced to subtherapeutic levels.
Increases trazodone levels: consider decreasing trazodone dosage.

Levels of all erectile dysfunction drugs are increased: the lowest dose of these drugs must be used as a maximum and at intervals not be be decreased beyond every 48-72 hours.

Drugs of abuse/addiction: MDMA levels are increased and severe reactions/deaths have been reported.
Suggested laboratory evaluations Liver profile and glucose monthly x 3 months, then every 3-4 months
Lipid profile q3-4 months
Contraindications
Antiarrhythmics: amiodarone, bepridil, flecainide, propafenone, quinidine
Ergot Derivatives: dihydroergotamine, ergonovine, ergotamine, methylergonivine
GI Motility Agent: cisapride
Herbal Products: St. John's wort (hypericum perforatum)
HMG-CoA Reductase Inhibitors: lovastatin, simvastatin
Neuroleptic: pimozide
Sedative/hypnotics: midazolam, triazolam

Antifungal: voriconazole

Warnings Examine patient's concomitant medications carefully before prescribing.
Ritonavir is generally regarded as too toxic to be used as an active single protease inhibitor.
Usage Suggestions Ritonavir is used nearly exclusively as an inhibitor of the metabolism of other protease inhibitors i.e. as a "boosting" agent.
High dose ritonavir is usually too toxic and other agents such as indinavir and lopinavir/ritonavir have comparable potency as well as the ability to overcome some degree of protease inhibitor resistance.
Full Prescribing Information http://www.norvir.com

 

 

Links to Antiretroviral Sections (click on anything)
Nucleoside & Nucleotide Reverse Transcriptase Inhibitors (NRTI)
AZT  |  ddC  |  ddI  |  d4T  |  3TC  |  ABC  |  FTC  |  TDF  |  Combivir  |  Trizivir  |  Epzicom  |  Truvada
Nonnucleoside Reverse Transcriptase Inhibitors (NNRTI)
efavirenz  |  nevirapine  |  delavirdine
Protease Inhibitors (PI)  Boosted Protease Inhibitors
saquinavir  indinavir  |  ritonavir  |  nelfinavir  |  amprenavir  |  lopinavir + ritonavir  |  atazanavir  |  fosamprenavir  | tipranavir
Fusion Inhibitors
enfuvirtide

 

Quick Menu / Table of Contents
Introduction Principles Management NRTI Info NNRTI Info
PI Info Fusion Inhibitors Drug Summary Investigational Adherence
Lab Evaluation Resistance Tests PEP Antiretroviral Tables OI Prevention
Vaccinations TB Therapy Hepatitis Therapy OI Diagnosis OI Therapy
Bibliography Links Palliative Therapy

 

Updated 10.25.2005