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Protease inhibitors
HIV-Related Drug Classes - Navigation |
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amprenavir (Agenerase ® )
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Oral: Note: Capsule and oral solution are not interchangeable on a
mg-per-mg basis. Capsule: Dosing (Adult): Children >13 years (>50 kg) and Adults: 1200 mg twice daily Note: Dosage adjustments for amprenavir when administered in combination therapy: Efavirenz: Adjustments necessary for both agents: Amprenavir 1200 mg 3 times/day (single protease inhibitor) or Amprenavir 1200 mg twice daily plus ritonavir 200 mg twice daily Ritonavir: Adjustments necessary for both agents: Amprenavir 1200 mg plus ritonavir 200 mg once daily or Amprenavir 600 mg plus ritonavir 100 mg twice daily Dosage adjustment in renal impairment: Oral solution is contraindicated in renal failure. Dosage adjustment in hepatic impairment: Child-Pugh score between 5-8: Capsule: 450 mg twice daily Solution: 513 mg twice daily; contraindicated in hepatic failure Child-Pugh score between 9-12: Capsule: 300 mg twice daily Solution: 342 mg twice daily; contraindicated in hepatic failure Supplied: [50, 150 mg caps. 15mg/ml oral solution.] ( large pill burden. Must warn of gastrointestinal (GI) intolerance and rash.) |
atazanavir (Reyataz ® )
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Protease Inhibitor.
Dosing (Adult): Antiretroviral-naive patients: 400 mg once daily with food. Antiretroviral-experienced patients: 300 mg once daily plus ritonavir 100 mg once daily with food. Coadministration with efavirenz: Antiretroviral-naive patients: It is recommended that atazanavir 300 mg plus ritonavir 100 mg be given with efavirenz 600 mg (all as a single daily dose). Administer with food. Antiretroviral-experienced patients: Recommendations have not been established. Coadministration with didanosine buffered formulations: Administer atazanavir 2 hours before or 1 hour after didanosine buffered formulations. Coadministration with tenofovir: The manufacturer recommends that atazanavir 300 mg plus ritonavir 100 mg be given with tenofovir 300 mg (all as a single daily dose). Administer with food. Supplied: Capsule: 100 mg, 150 mg, 200 mg. |
Darunavir (Prezista™)
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Dosing (Adult): Treatment of HIV infection: Oral: 600 mg twice daily with meals. Note: Co-administration with ritonavir (100 mg twice daily) is required. Administer with food (bioavailability is increased). Coadministration with ritonavir is required. Indications: Treatment of HIV-1 infections in combination with ritonavir and other antiretroviral agents; limited to highly treatment-experienced or multiprotease inhibitor-resistant patients Supplied: Tablet: 300 mg |
fosamprenavir (Lexiva ® )
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Protease Inhibitor.
Dosing (Adult): Antiretroviral therapy-naive patients: Unboosted regimen: 1400 mg twice daily (without ritonavir). Ritonavir-boosted regimens: Once-daily regimen: Fosamprenavir 1400 mg plus ritonavir 200 mg once daily. Twice-daily regimen: Fosamprenavir 700 mg plus ritonavir 100 mg twice daily. Note: Also used in protease inhibitor-experienced patients. Protease inhibitor-experienced patients: Fosamprenavir 700 mg plus ritonavir 100 mg twice daily. Note: Once-daily administration is not recommended in protease inhibitor-experienced patients. Combination therapy with efavirenz (ritonavir-boosted regimen): Once-daily regimen: Fosamprenavir 1400 mg daily plus ritonavir 300 mg once daily. Twice-daily regimen: No dosage adjustment recommended for twice-daily regimen. Supplied: 700 mg tablet. |
indinavir (Crixivan ® )
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Dosing (Adult): Oral: 800 mg
every 8 hours Note: Dosage adjustments for indinavir when administered in combination therapy: Delavirdine, itraconazole, or ketoconazole: Reduce indinavir dose to 600 mg every 8 hours. Efavirenz: Increase indinavir dose to 1000 mg every 8 hours Lopinavir and ritonavir (Kaletra™): Indinavir 600 mg twice daily Nevirapine: Increase indinavir dose to 1000 mg every 8 hours Rifabutin: Reduce rifabutin to 1/2 the standard dose plus increase indinavir to 1000 mg every 8 hours Ritonavir: Adjustments necessary for both agents: Ritonavir 100-200 mg twice daily plus indinavir 800 mg twice daily or Ritonavir 400 mg twice daily plus indinavir 400 mg twice daily Dosage adjustment in hepatic impairment: Mild-moderate impairment due to cirrhosis: 600 mg every 8 hours or with ketoconazole coadministration Administration Drink at least 48 oz of water daily. Administer with water, 1 hour before or 2 hours after a meal. Administer around-the-clock to avoid significant fluctuation in serum levels. Supplied: Capsule: 100 mg, 200 mg, 333 mg, 400 mg |
Kaletra ® (Lopinavir 133 mg + Ritonavir 33.3 mg
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Protease Inhibitor.
Dosing (Adult): (take with food): Therapy-naive: Lopinavir 800 mg/ritonavir 200 mg once daily or lopinavir 400 mg/ritonavir 100 mg twice daily. Therapy-experienced: Lopinavir 400 mg/ritonavir 100 mg twice daily. Note: Once-daily dosing regimen has not been evaluated with concurrent indinavir or saquinavir and should not be used with concomitant phenytoin, carbamazepine, or phenobarbital therapy. Dosage adjustment when taken with amprenavir, efavirenz. nelfinavir, or nevirapine: Lopinavir 533 mg/ritonavir 133 mg twice daily. Note: Once-daily dosing regimen should not be used when concomitantly taking amprenavir, efavirenz, nelfinavir, or nevirapine therapy. Supplied: Capsule: Lopinavir 133.3 mg and ritonavir 33.3 mg. oral soln: Lopinavir 80 mg and ritonavir 20 mg/ml. |
nelfinavir (Viracept ®)
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Dosing (Adult):
750 mg orally three times a day or 1250mg orally twice daily. Take with
high fat meal and warn of diarrhea that usually responds to loperamide
or calcium. Note: Dosage adjustments for nelfinavir when administered in combination with ritonavir: Nelfinavir 500-750 mg twice daily plus ritonavir 400 mg twice daily ----------------- Dosing adjustment in renal impairment: No adjustment needed Dosing adjustment in hepatic impairment: Use caution ----------------- Supplied: Powder, oral: 50 mg/g (144 g) Tablet [film coated]: 250 mg, 625 mg |
ritonavir (Norvir ®)
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Protease Inhibitor.
Dosing (Adult): (Day 1): 300mg orally twice daily (Days 2-4): 400 mg orally twice daily. (Day 5): 500mg orally twice daily; (Day 6 or longer): 600mg orally twice a day. Take with food. --- 600 mg twice daily; dose escalation tends to avoid nausea that many patients experience upon initiation of full dosing. Escalate the dose as follows: 300 mg twice daily for 1 day, 400 mg twice daily for 2 days, 500 mg twice daily for 1 day, then 600 mg twice daily. Ritonavir may be better tolerated when used in combination with other antiretrovirals by initiating the drug alone and subsequently adding the second agent within 2 weeks. --- Note: Dosage adjustments for ritonavir when administered in combination therapy: Amprenavir: Adjustments necessary for each agent: Amprenavir 1200 mg with ritonavir 200 mg once daily or Amprenavir 600 mg with ritonavir 100 mg twice daily Amprenavir plus efavirenz (3-drug regimen): Amprenavir 1200 mg twice daily plus ritonavir 200 mg twice daily plus efavirenz at standard dose Indinavir: Adjustments necessary for both agents: Indinavir 800 mg twice daily plus ritonavir 100-200 mg twice daily or Indinavir 400 mg twice daily plus ritonavir 400 mg twice daily Nelfinavir or saquinavir: Ritonavir 400 mg twice daily Rifabutin: Decrease rifabutin dose to 150 mg every other day Dosing adjustment in hepatic impairment: No adjustment required in mild or moderate impairment; however, careful monitoring is required in moderate hepatic impairment (levels may be decreased); caution advised with severe impairment (no data available) Administration Administer with food. Liquid formulations usually have an unpleasant taste. Consider mixing it with chocolate milk or a liquid nutritional supplement. GI intolerance is a major problem and is dose-related. Supplied: 100mg capsule; 80mg/ml -240ml solution. |
saquinavir (Fortovase ® ,
Invirase ®)
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Dosing (Adult): Note: Fortovase® and Invirase® are not bioequivalent and should not be used interchangeably; only Fortovase® should be used to initiate therapy: Fortovase®: 1200 mg (six 200 mg capsules) 3 times/day within 2 hours after a meal in combination with a nucleoside analog or 1000 mg (five 200 mg capsules) twice daily in combination with ritonavir 100 mg twice daily Invirase®: 1000 mg (five 200 mg capsules or two 500 mg tablets) twice daily given in combination with ritonavir 100 mg twice daily; this combination should be given together and within 2 hours after a full meal in combination with a nucleoside analog Note: Dosage adjustments of Fortovase® when administered in combination therapy: Delavirdine: Fortovase® 800 mg 3 times/day Lopinavir and ritonavir (Kaletra™): Fortovase® 800 mg twice daily Nelfinavir: Fortovase® 1200 mg twice daily Elderly: Clinical studies did not include sufficient numbers of patients >/= 65 years of age; use caution due to increased frequency of organ dysfunction Supplied: Capsule, as mesylate (Invirase®): 200 mg Capsule, soft gelatin, as base (Fortovase®): 200 mg Tablet, as base (Invirase®): 500 mg |
tipranavir (Aptivus ® )
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Protease Inhibitor.
Dosing (Adult): 500 mg twice daily with a high-fat meal. Note: Coadministration with ritonavir (200 mg twice daily) is required. Supplied: 250 mg capsule. |
Disclaimer
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Listed dosages are for - Adult patients ONLY. PLEASE READ THE
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GlobalRPH does not directly or indirectly practice medicine or provide
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kind for the information and data accessed through the Service or for
any diagnosis or treatment made in reliance thereon. David F. McAuley, Pharm.D., R.Ph. GlobalRPh Inc. |
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