II. Indications
-
HIV Infection (as part of combination therapy)
- Has been replaced by newer Protease Inhibitors with fewer adverse effects
- Among the first Protease Inhibitors for HIV (FDA approved in 1996)
III. Mechanism
IV. Efficacy
- When originally studied in the 1990s, Indinavir was very effective in combination with Zidovudine (AZT)
- Newer Protease Inhibitors are combined with boosters (e.g. Ritonavir, Cobicistat) and are used with other Antiretrovirals
V. Medications
- Capsules: 100, 200, 400 mg
VI. Dosing
- Adults (as part of combination therapy with other Antiretrovirals)
- Indinavir 800 mg orally three times daily
- Indications to reduce dose to 600 mg orally three times daily
- Delavirdine
- Itraconazole or Ketoconazole
- Hepatic insufficiency
- Take on empty Stomach
- One hour before or 2 hours after a meal
- Concurrent food reduces concentration up to 80%
- Drink at least 1.5 Liters (50 oz) liquid per day
- Drink 150 ml water per hour for 3 hours after dose
- Avoids Nephrolithiasis and Interstitial Nephritis
VII. Adverse Effects
- See Protease Inhibitor for adverse effects attributed to the class
- Well tolerated
- Indirect Bilirubin (elevation in 10% of patients)
- Nephrolithiasis in 2-3% of patients
- Hyperglycemia
- Renal Insufficiency
- Alopecia
- Dry Skin
- Xerostomia
- Paronychia
- Gallstones
VIII. Drug Interactions
- See Protease Inhibitor
-
Drug Interactions are common with Protease Inhibitors
- Protease Inhibitors cause the most Drug Interactions of all Antiretrovirals
- Use formal Drug Interaction applications when prescribing
-
St. John's Wort
- May reduce Indinavir concentrations by 80%
- Piscitelli (2000) Lancet 355:547-8 [PubMed]
-
Rifabutin
- Decrease Rifabutin dose to 50% AND
- Increase Indinavir 1000 mg orally three times daily
- Medications contraindicated with Indinavir (a strong CYP3A4 Inhibitor)
- Alfuzosin
- Amiodarone
- Ergot alkaloids (e.g. Ergonovine, Ergotamine)
- Pimozide
- High dose Sildenafil (Revatio)
- Sedative Hypnotics (oral Midazolam, Triazolam, Alprazolam)
IX. Safety
- Avoid in Lactation (as with other Protease Inhibitors)
- Pregnancy Category C
- Risk of perinatal Hyperbilirubinemia
X. Resources
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Related Studies
Definition (NCI) | A synthetic hydroxyaminopentane amide agent that selectively inhibits the protease of both human immunodeficiency virus 1 and 2. The incorporation of a basic amine into the hydroxyethylene backbone improves its aqueous solubility and its oral bioavailability. |
Definition (NCI_NCI-GLOSS) | A drug that interferes with the ability of a virus to make copies of itself. |
Definition (MSH) | A potent and specific HIV protease inhibitor that appears to have good oral bioavailability. |
Definition (CSP) | potent and specific HIV protease inhibitor that appears to have good oral bioavailability. |
Concepts | Pharmacologic Substance (T121) , Organic Chemical (T109) |
MSH | D019469 |
SnomedCT | 108695003, 372529006 |
LNC | LP21311-3, MTHU013846 |
English | Indinavir, indinavir, IDV, Indinavir [Chemical/Ingredient], Compound J, (1(1S,2R),5(S))-2,3,5-Trideoxy-N-(2,3-dihydro-2-hydroxy-1H-inden-1-yl)-5-(2-(((1,1-dimethylethyl)amino)carbonyl)-4-(3-pyridinylmethyl)-1-piperazinyl)-2-(phenylmethyl)-D-erythro-Pentonamide, INDINAVIR, Indinavir (product), Indinavir (substance) |
Swedish | Indinavir |
Czech | indinavir |
Finnish | Indinaviiri |
Russian | INDINAVIR, ИНДИНАВИР |
Polish | Indynawir |
Japanese | インジナァビル, インジナビル |
Spanish | indinavir (producto), indinavir (sustancia), indinavir, Indinavir |
French | Indinavir |
German | Indinavir |
Italian | Indinavir |
Portuguese | Indinavir |
Ontology: Crixivan (C0701105)
Concepts | Pharmacologic Substance (T121) , Organic Chemical (T109) |
MSH | D019469 |
English | indinavir sulfate (Crixivan), crixivan, Crixivan |