Drug Index

Ritonavir

 
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Mechanism :

Ritonavir inhibits the HIV viral proteinase enzyme which prevents cleavage of the gag-pol polyprotein, resulting in non-infectious, immature viral particles.


Indication :

• Treatment of HIV infection as part of combination boosted protease inhibitor (PI).


Contraindications :

Hypersensitivity; Caution if hepatic impairment, HBV or HCV co-infection, structural heart disease, cardiac conduction disturbance, ischemic heart disease, cardiomyopathy, diabetes mellitus, hemophilia.


Dosing :

>1 month:

Use in children along with other PIs.

Initial dose: 250 mg/sqm orally twice a day. Maintenance dose: Increase by 50 mg/m² twice daily every 2 to 3 days to the full dose of 350 to 400 mg/m² orally twice a day. Maximum dose: 600 mg/dose. Use of ritonavir as the sole protease inhibitor is not recommended.

Adults:

Amprenavir 600 mg twice daily with ritonavir 100 mg twice daily PO.

Atazanavir 300 mg OD with ritonavir 100 mg once daily PO.

Fosamprenavir 700 mg twice daily with ritonavir 100 mg twice daily PO.

Lopinavir co-formulated with ritonavir (lopinavir/ritonavir) 400 mg/100 mg or 800 mg/200 mg PO.

Saquinavir 1000 mg twice daily with ritonavir 100 mg twice daily in ART experienced patients PO.

Tipranavir 500 mg twice daily with ritonavir 200 mg twice daily PO.

Darunavir 600 mg twice daily with ritonavir 100 mg twice daily in ART experienced patients PO.

Darunavir 800 mg once daily with ritonavir 100 mg once daily in ART-naive patients PO.


Adverse Effect :

PR prolongation, AV block, hyperglycemia, hypercholesterolemia, hypertriglyceridemia, pancreatitis, hepatotoxicity, hypersensitivity reactions, anaphylaxis, toxic epidermal necrolysis, exfoliative dermatitis, Stevens-Johnson syndrome, erythema multiforme, thrombocytopenia, neutropenia, immune reconstitution syndrome, autoimmune disorders, nausea/vomiting, diarrhea, asthenia, taste changes, paraesthesia, dizziness, vasodilation, anorexia, abdominal pain, headache, dyspepsia, myalgia, rash, insomnia, lipodystrophy,

elevated ALT/AST/amylase/CPK/uric acid.


Interaction :

Interaction Characteristics:
CYP1A2 inducer, major
CYP2B6 inducer, major
CYP2C9 inducer, major
CYP2D6 inhibitor, weak
CYP3A4 inhibitor, strong
CYP3A4 substrate
GI absorption enhanced by GLP-2 receptor agonist
OATP1B3 inhibitor, strong
P-gp (MDR1) inhibitor, weak
UGT1A1 inhibitor
UGT2B4 inducer
Hyperglycemia
Prolongs PR interval
Contraindicated:
Alfuzosin, Alprazolam, Amiodarone, Cabazitaxel, Chlorpropamide, Cisapride, Cobicistat, Conivaptan, Dihydroergotamine, Disopyramide, Disulfiram, Dronedarone, Eletriptan, Enzalutamide, Eplerenone, Ergotamine, Etravirine, Flecainide, Ifosfamide, Lomitapide, Lovastatin, Lurasidone, Mefloquine, Methylergonovine, Metronidazole, Midazolam, Pimozide, Quinidine (Antiarrhythmic), Ranolazine, Rifampin, Sildenafil, Silodosin, Simvastatin, St. John's Wort, Tamsulosin, Thioridazine, Tinidazole, Tolvaptan, Triazolam, Voriconazole.


08/11/2019 20:57:35 Ritonavir
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