Prezista

Generic Name: Darunavir
Class: HIV Protease Inhibitors
VA Class: AM800
Chemical Name: [(1S,2R) - 3 - [[(4 - Aminophenyl)sulfonyl](2 - methylpropyl)amino] - 2 - hydroxy - 1 - (phenylmethyl)propyl] - carbamic acid (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl ester
Molecular Formula: C₂₇H₃₇N₃O₇SC₂₇H₃₇N₃O₇S•C₂H₅OH
CAS Number: 206361-99-1

Introduction

Antiretroviral; HIV protease inhibitor (PI).^{1 2 3}

Uses for Prezista

Treatment of HIV Infection

Treatment of HIV infection.¹ Used in conjunction with low-dose ritonavir (ritonavir-boosted darunavir) and other antiretroviral agents.¹

Ritonavir-boosted darunavir is a preferred PI for initial treatment regimens in adults.⁴

Treatment-experienced patients: Use of ritonavir-boosted darunavir should be guided by genotypic and phenotypic viral resistance testing and the individual’s prior antiretroviral treatment.¹

Prezista Dosage and Administration

Administration

Oral Administration

Administer orally in conjunction with low-dose ritonavir (ritonavir-boosted darunavir).^{1 4} Do not use without low-dose ritonavir.¹

Take darunavir and low-dose ritonavir at same time and with food.¹

Administered once daily in treatment-naive adults.¹

Administered twice daily in pediatric patients and treatment-experienced adults.¹

Ensure that pediatric patients can swallow tablets; those unable to swallow tablets are not candidates for ritonavir-boosted darunavir therapy.¹

Dosage

Available as darunavir ethanolate; dosage expressed in terms of darunavir.¹

Pediatric Patients

Treatment of HIV Infection

To avoid medication errors, use extra care in calculating the dose, transcribing the medication order, dispensing the prescription, and providing dosing instructions.¹

Dosage of ritonavir-boosted darunavir in children 6–<18 years of age weighing at least 20 kg is based on weight.¹

Table 1: Dosage for Ritonavir-boosted Darunavir for Pediatric Patients 6–<18 Years of Age1

Body weight	Darunavir dosage	Ritonavir dosage
20 to < 30 kg	375 mg twice daily	50 mg twice daily
30 to < 40 kg	450 mg twice daily	60 mg twice daily
≥ 40 kg	600 mg twice daily	100 mg twice daily

Adults

Treatment of HIV Infection

Treatment-naive Adults

Oral

800 mg once daily boosted with low-dose ritonavir (100 mg once daily).¹

Treatment-experienced Adults

Oral

600 mg twice daily boosted with low-dose ritonavir (100 mg twice daily).¹

Prescribing Limits

Pediatric Patients

Treatment of HIV Infection

Oral

Do not exceed dosage for treatment-experienced adults.¹

Special Populations

Hepatic Impairment

Dosage adjustment not needed in patients with mild to moderate hepatic impairment (Child-Pugh class A or B).^{1 4} Do not use in those with severe hepatic impairment (Child-Pugh class C).^{1 4}

Renal Impairment

Some experts state that dosage adjustments are not necessary.⁴

Geriatric Patients

Select dosage with caution because of age-related decreases in hepatic, renal, and/or cardiac function and concomitant disease and drug therapy.¹

Cautions for Prezista

Contraindications

• 
  

  Concomitant use with drugs highly dependent on CYP3A for metabolism and for which elevated plasma concentrations are associated with serious and/or life-threatening events and other drugs that may lead to loss of virologic response (e.g., cisapride, ergot alkaloids, lovastatin, oral midazolam, pimozide, rifampin, simvastatin, St. John’s wort [Hypericum perforatum], triazolam).¹ (See Specific Drugs under Interactions.)

  
  

Warnings/Precautions

Warnings

Hepatic Effects

Acute hepatitis reported in clinical studies.¹ Liver injury (in some cases fatal) reported during postmarketing surveillance; liver injury generally occurred in patients with advanced HIV infection who were receiving multiple concomitant drugs, who were coinfected with hepatitis B virus (HBV) or hepatitis C virus (HCV), and/or were developing immune reconstitution syndrome.¹

Conduct appropriate laboratory tests before starting darunavir; monitor periodically thereafter.¹ Consider increased AST/ALT monitoring in patients with hepatitis, cirrhosis, or elevated transaminase values prior to therapy, especially during the first several months of therapy.¹

Consider interrupting or discontinuing darunavir in patients who develop manifestations suggestive of hepatic impairment (e.g., fatigue, anorexia, nausea, jaundice, dark urine, liver tenderness, hepatomegaly, clinically important increases in hepatic enzyme concentrations).¹

Interactions

Darunavir is administered concomitantly with low-dose ritonavir (ritonavir-boosted darunavir).¹ Failure to administer with recommended low-dose ritonavir will result in subtherapeutic darunavir concentrations and inadequate antiviral response.¹ The usual cautions, precautions, and contraindications associated with ritonavir should be considered.¹

Concomitant use with certain drugs is not recommended or requires particular caution (e.g., sildenafil, tadalafil, vardenafil).^{1 4} (See Specific Drugs under Interactions.)

Hyperglycemic and Diabetogenic Effects

Hyperglycemia (potentially persistent), new-onset diabetes mellitus, or exacerbation of preexisting diabetes mellitus reported with use of PIs; diabetic ketoacidosis has occurred.¹

Initiate or adjust antidiabetic therapy (e.g., insulin, oral hypoglycemic agents) as needed.¹

Sensitivity Reactions

Sulfonamide Sensitivity

Darunavir contains a sulfonamide moiety; use with caution in patients with known sulfonamide allergy.¹

Dermatologic Reactions

Severe skin reactions, including Stevens-Johnson syndrome reported;¹ fever and increased serum transaminase concentrations also may occur.¹

Discontinue darunavir if severe rash occurs.¹

General Precautions

Hemophilia A and B

Spontaneous bleeding reported with PIs;¹ causal relationship not established.¹

Use with caution in patients with history of hemophilia A or B.¹ Increased hemostatic therapy (e.g., antihemophilic factor) may be needed.¹

Adipogenic Effects

Possible redistribution or accumulation of body fat, including central obesity, dorsocervical fat enlargement (buffalo hump), peripheral wasting, facial wasting, breast enlargement, and general cushingoid appearance.¹

Immune Reconstitution Syndrome

During initial treatment, patients who respond to antiretroviral therapy may develop an inflammatory response to indolent or residual opportunistic infections (e.g., Mycobacterium avium complex [MAC], M. tuberculosis, cytomegalovirus [CMV], Pneumocystis jiroveci [formerly P. carinii]; this may necessitate further evaluation and treatment.¹

HIV Resistance

Possibility of cross-resistance to other PIs not evaluated.¹ Effect of ritonavir-boosted darunavir therapy on subsequent therapy with other PIs unknown.¹

Specific Populations

Pregnancy

Category C.¹

Antiretroviral Pregnancy Registry at 800-258-4263.¹

Some experts state safety and pharmacokinetic data insufficient to recommend ritonavir-boosted darunavir in pregnant women.⁷

Lactation

Distributed into milk in rats;¹ not known whether distributed into human milk.¹

Instruct HIV-infected women not to breast-feed because of risk of HIV transmission and risk of adverse effects in the infant.¹

Pediatric Use

Adverse effects in children 6–<18 years of age similar to those reported in adults.¹

Safety, efficacy, and pharmacokinetic profile not established in children 3 to <6 years of age.¹

Should not be used in children <3 years of age because of toxicity and mortality in juvenile rats.¹

Geriatric Use

Insufficient experience in patients ≥65 years of age to determine whether geriatric patients respond differently than younger adults.¹

Use with caution and monitor because of age-related decreases in hepatic, renal, and/or cardiac function and concomitant disease and drug therapy.¹

Hepatic Impairment

Risk for liver function abnormalities, including severe adverse hepatic effects, in patients with preexisting hepatic impairment, including those with HBV or HCV infection.¹

Pharmacokinetics not altered in individuals with mild (Child-Pugh class A) or moderate (Child-Pugh class B) hepatic impairment.¹

Use not recommended in patients with severe hepatic impairment.¹

Renal Impairment

Pharmacokinetics not altered in patients with Cl_cr≥30 mL/minute.¹ Not studied in patients with severe renal impairment or end-stage renal disease.¹

Common Adverse Effects

Diarrhea,^{1 9} nausea,^{1 9} headache,^{1 9} abdominal pain.¹

Interactions for Prezista

Darunavir metabolized principally by CYP3A.¹

Darunavir and ritonavir inhibit CYP3A4 and CYP2D6.¹

Drugs Affecting or Metabolized by Hepatic Microsomal Enzymes

Pharmacokinetic interactions likely with drugs that are inhibitors or inducers of CYP3A4 with possible alteration in metabolism of darunavir or ritonavir.¹

Potential pharmacokinetic interaction with drugs metabolized by CYP3A or CYP2D6 with possible altered metabolism of drug metabolized by CYP3A or CYP2D6.¹

Specific Drugs

Drug	Interaction	Comments
Abacavir	Pharmacokinetic interaction not expected1 No in vitro evidence of antagonistic antiretroviral effects 1
Antiarrhythmic agents (amiodarone, flecainide, systemic lidocaine, propafenone, quinidine)	Possible increased plasma concentrations of antiarrhythmic agents1	Monitor antiarrhythmic concentrations1
Anticoagulants	Decreased warfarin concentrations1	Monitor INR 1
Anticonvulsants (carbamazepine, phenobarbital, phenytoin)	Carbamazepine: Increased carbamazepine concentrations1 Phenobarbital, phenytoin: Decreased concentrations of the anticonvulsant1	Carbamazepine: Dosage adjustment not needed; monitor carbamazepine concentrations and adjust dose to achieve appropriate clinical effect1 Phenobarbital, phenytoin: Monitor anticonvulsant concentrations1
Antifungals (itraconazole, ketoconazole, voriconazole)	Itraconazole: Increased darunavir and itraconazole concentrations1 Ketoconazole: Increased darunavir and ketoconazole concentrations1 Voriconazole: Decreased voriconazole concentrations1	Itraconazole: Dosage >200 mg daily not recommended1 4 Ketoconazole: Dosage >200 mg daily not recommended 1 4 Voriconazole: Concomitant use not recommended unless benefits outweigh risks1 4
Antimycobacterials, rifamycins (rifabutin, rifampin, rifapentine)	Rifabutin: Increased rifabutin and darunavir concentrations1 Rifampin: Decreased darunavir concentrations; possible decreased antiretroviral activity1	Rifabutin: Reduce rifabutin dosage to 150 mg once every other day (further reduction may be needed); monitor for adverse effects1 4 Rifampin: Concomitant use contraindicated 1 4 Rifapentine: Concomitant use not recommended4
Atazanavir	Plasma concentration of atazanavir with ritonavir-boosted darunavir similar to ritonavir-boosted atazanavir; no change in darunavir concentrations1 No in vitro evidence of antagonistic antiretroviral effects1	Manufacturer and some experts state atazanavir 300 mg once daily can be used with ritonavir-boosted darunavir1 4
β-Adrenergic blocking agents (metoprolol, timolol)	Metoprolol, timolol: Possible increased concentrations of the β-adrenergic blocking agent1	Metoprolol, timolol: Caution; dose reduction of the β-adrenergic blocking agent may be needed1
Benzodiazepines (e.g., midazolam, triazolam)	Possible increased concentrations of midazolam or triazolam; potential for serious and/or life-threatening effects (e.g., prolonged or increased sedation or respiratory depression)1	Concomitant use with oral midazolam or triazolam contraindicated;1 some experts state a single parenteral dose of midazolam can be used with caution in a monitored situation for procedural sedation4
Calcium-channel blocking agents (e.g., felodipine, nicardipine, nifedipine)	Increased concentrations of calcium-channel blocking agents 1	Use concomitantly with caution; clinical monitoring recommended1
Cisapride	Potential for serious and/or life-threatening effects such as cardiac arrhythmias 1	Concomitant use contraindicated1
Clarithromycin	Increased clarithromycin concentrations1	Modification of usual clarithromycin dosage not necessary in patients with normal renal function; reduce clarithromycin dosage by 50% if Clcr 30–60 mL/minute and reduce by 75% if Clcr <30 mL/minute 1
Corticosteroids (dexamethasone, fluticasone)	Fluticasone nasal spray/oral inhalation: Increased fluticasone concentrations with ritonavir-boosted darunavir resulting in decreased cortisol concentrations1 4 Dexamethasone: Decreased darunavir concentration; possible decreased antiretroviral efficacy1	Fluticasone nasal spray/oral inhalation: Consider alternatives to fluticasone, especially when long-term corticosteroid use anticipated1 4
Delavirdine	No in vitro evidence of antagonistic antiretroviral effects 1
Didanosine	Didanosine delayed-release capsules: No change in didanosine or darunavir concentrations1 Conflicting administration instructions with didanosine and food1 No in vitro evidence of antagonistic antiretroviral effects 1	Administer darunavir with low-dose ritonavir (with food) 1 hour after or 2 hours before didanosine (without food)1
Digoxin	Increased digoxin concentrations1	Use lowest possible initial dose of digoxin; monitor digoxin concentrations and adjust dose as clinically indicated1
Dextromethorphan	Increased dextromethorphan concentrations1
Efavirenz	Decreased darunavir AUC; increased efavirenz AUC1 4 No in vitro evidence of antagonistic antiretroviral effects 1	Clinical importance unknown4 Some experts suggest usual dosages can be used with close monitoring; consider monitoring plasma darunavir and efavirenz concentrations4
Emtricitabine	Pharmacokinetic interaction not expected1 No in vitro evidence of antagonistic antiretroviral effects 1
Etravirine	Decrease in AUC of etravirine; no change in darunavir concentrations; safety and efficacy of ritonavir-boosted darunavir and etravirine established in clinical studies1 4	Dosage adjustment not needed1 4
Enfuvirtide	No in vitro evidence of antagonistic antiretroviral effects1
Ergot alkaloids (dihydroergotamine, ergonovine, ergotamine, methylergonovine)	Potential for serious or life-threatening adverse effects (e.g., peripheral vasospasm, ischemia of extremities)1	Concomitant use contraindicated 1 If treatment of uterine atony and excessive postpartum bleeding is indicated in a woman receiving darunavir, use methylergonovine maleate (Methergine) only if alternative treatments cannot be used and if potential benefits outweigh risks; use methylergonovine at lowest dosage and shortest duration possible7
Fosamprenavir	Data not available regarding pharmacokinetic interaction1	Concomitant use not recommended pending further data1
Histamine H2- receptor antagonists (e.g., ranitidine)	Ranitidine: Pharmacokinetic interaction not expected1 4	Dosage adjustment not necessary1
HMG-CoA reductase inhibitors	Lovastatin, simvastatin: Increased risk of serious adverse reactions (e.g., myopathy, rhabdomyolysis)1 Increased concentrations of certain HMG-CoA reductase inhibitors (i.e., atorvastatin, pravastatin, rosuvastatin)1 4	Concomitant use with lovastatin or simvastatin contraindicated1 If used with atorvastatin, pravastatin, or rosuvastatin, use lowest possible dosage of the HMG-CoA reductase inhibitor and monitor carefully; consider using fluvastatin1
Hormonal contraceptives (estrogens or progestins)	Decreased ethinyl estradiol and norethindrone concentrations with oral contraceptive preparations1	Use alternative nonhormonal contraception methods1
Immunosuppressive agents (cyclosporine, sirolimus, tacrolimus)	Potential for increased immunosuppressive agent concentrations1	Monitor plasma concentrations of immunosuppressive agent if used concomitantly1
Indinavir	Increased darunavir and indinavir concentrations1 No in vitro evidence of antagonistic antiretroviral effects1	Appropriate dosages for concomitant use not established1
Lamivudine	Pharmacokinetic interaction unlikely1 No in vitro evidence of antagonistic antiretroviral effects1
Lopinavir	No change in lopinavir concentrations; decreased darunavir concentrations1 No in vitro evidence of antagonistic antiretroviral effects1	Concomitant use not recommended1 4
Maraviroc	Increased maraviroc concentrations4	Recommended dosage of maraviroc is 150 mg twice daily when used with ritonavir-boosted darunavir4
Methadone	Decreased methadone concentrations1	Adjustment in the methadone dosage not needed; closely monitor for signs of opiate withdrawal and adjust methadone dosage if needed1
Nelfinavir	Data not available regarding pharmacokinetic interaction1 No in vitro evidence of antagonistic antiretroviral effects1	Concomitant use not recommended pending further data1
Nevirapine	Increased plasma nevirapine concentrations; unchanged plasma darunavir concentrations1 4 No in vitro evidence of antagonistic antiretroviral effects1	Dosage adjustment not necessary1 4
Proton pump inhibitors	Omeprazole: Decreased omeprazole concentrations1	Dosage adjustment not necessary1
Psychotherapeutic agents (e.g., desipramine, pimozide, risperidone, thioridazine, trazodone, SSRIs)	Pimozide: Potential for serious and/or life-threatening adverse effects (e.g., cardiac arrhythmias)1 Desipramine, trazodone: Potential for increased concentrations of the antidepressant; 1 increased risk of nausea, dizziness, hypotension, syncope1 SSRIs: Decreased concentrations of paroxetine and sertraline; unchanged darunavir concentrations1 4 Risperidone, thioridazine: Potential for increased concentrations of the psychotherapeutic agent1	Pimozide: Concomitant use contraindicated1 Desipramine, trazodone: Caution; reduced dosage of the antidepressant may be needed1 SSRIs: Titrate dosage of paroxetine or sertraline and monitor for clinical response1 4 Risperidone, thioridazine: Reduced dosage of the psychotherapeutic agent may be needed1
Ritonavir	Increased plasma darunavir concentrations and AUC;1 2 4 concomitant low-dose ritonavir used to therapeutic advantage (ritonavir-boosted darunavir)1 2 4 No in vitro evidence of antagonistic antiretroviral effects1
St. John’s wort (Hypericum perforatum)	Potential decreased darunavir concentration; possible decreased antiretroviral efficacy1	Concomitant use contraindicated1
Saquinavir	Decreased darunavir concentrations; unchanged saquinavir concentrations1 No in vitro evidence of antagonistic antiretroviral effects1	Concomitant use not recommended1 4
Sildenafil	Possible increased sildenafil concentrations and increased risk of sildenafil-associated adverse effects (e.g., hypotension, visual changes, prolonged erection)1	Do not exceed sildenafil dosage of 25 mg once every 48 hours; closely monitor for adverse effects (e.g., hypotension, syncope, visual changes, prolonged erection)1 4
Stavudine	Pharmacokinetic interaction unlikely1 No in vitro evidence of antagonistic antiretroviral effects1
Tadalafil	Possible increased tadalafil concentrations and increased risk of tadalafil-associated adverse effects (e.g., hypotension, visual changes, prolonged erection)1	Use with caution and with reduced tadalafil dosage (initial dosage of 5 mg and do not exceed a single dose of 10 mg in 72 hours);4 closely monitor for adverse effects1 4
Tenofovir	Increased plasma tenofovir concentrations; unchanged plasma darunavir concentrations1 4 No in vitro evidence of antagonistic antiretroviral effects1	Manufacturer of darunavir recommends usual dosage of tenofovir with ritonavir-boosted darunavir 1 Some experts state clinical importance unknown; monitor for tenofovir toxicity4
Tipranavir	No in vitro evidence of antagonistic antiretroviral effects 1	Concomitant use not recommended1
Vardenafil	Possible increased vardenafil concentrations and increased risk of vardenafil-associated adverse effects (e.g., hypotension, visual changes, prolonged erection)1	Do not exceed vardenafil dosage of 2.5 mg once every 72 hours; closely monitor for adverse effects (e.g., hypotension, syncope, visual changes, prolonged erection)1 4
Zidovudine	Pharmacokinetic interaction unlikely1 No in vitro evidence of antagonistic antiretroviral effects1

Prezista Pharmacokinetics

Absorption

Bioavailability

Darunavir administered concomitantly with low-dose ritonavir (ritonavir-boosted darunavir).¹ Ritonavir decreases metabolism of darunavir, resulting in increased plasma darunavir concentrations.¹

Peak plasma darunavir concentrations attained approximately 2.5–4 hours after a dose.¹

Food

Compared with administration in the fasting state, administration of ritonavir-boosted darunavir with food increases peak darunavir concentrations and AUC approximately 30%.¹

Distribution

Extent

Not known whether distributed into human milk;¹ distributed into milk in rats.¹

Plasma Protein Binding

95%.¹

Binds principally to α₁-acid-glycoprotein.¹

Elimination

Metabolism

Darunavir extensively metabolized by CYP3A.¹

Elimination Route

Following administration of ritonavir-boosted darunavir, eliminated principally in feces as unchanged darunavir.¹ Approximately 80% of darunavir dose excreted in feces and 14% excreted in urine.¹

Half-life

15 hours.¹

Special Populations

Moderate renal impairment (Cl_cr 30–60 mL/minute): Pharmacokinetics not affected.¹

Severe renal impairment or end-stage renal disease: No pharmacokinetic data.¹

Unlikely to be removed by hemodialysis or peritoneal dialysis.¹

Hepatic impairment: Pharmacokinetics in individuals with mild hepatic impairment (Child-Pugh class A) or moderate hepatic impairment (Child-Pugh class B) similar to values in individuals with normal hepatic function.¹ Pharmacokinetics not evaluated in those with severe hepatic impairment.¹

HBV or HCV coinfection: No effect on darunavir exposure.¹

Higher darunavir concentrations reported in females compared with males; dosage adjustments not required.¹

Stability

Storage

Oral

Tablets

25°C (may be exposed to 15–30°C).¹

Actions and SpectrumActions

• 
  

  Darunavir is administered in conjunction with low-dose ritonavir (ritonavir-boosted darunavir).¹

  
  


• 
  

  Darunavir is extensively metabolized by CYP3A; ritonavir is a potent inhibitor of CYP3A.¹ Concomitant use of these drugs results in decreased metabolism and increased plasma concentrations of darunavir.¹

  
  


• 
  

  Antiretroviral activity is due to darunavir.¹

  
  


• 
  

  Active against HIV-1.¹

  
  


• 
  

  Darunavir inhibits replication of HIV-1 by interfering with HIV proteases.¹

  
  


• 
  

  Darunavir-resistant HIV-1, including strains with decreased susceptibility to other PIs, has been reported.^{1 3}

  
  

Advice to Patients

• 
  

  Critical nature of compliance with HIV therapy.¹ Importance of using darunavir with low-dose ritonavir; importance of using these 2 drugs in conjunction with other antiretrovirals.¹

  
  


• 
  

  Antiretroviral therapy is not a cure for HIV infection, and opportunistic infections still may occur.¹ HIV transmission via sexual contact or sharing needles is not prevented by antiretrovirals.¹

  
  


• 
  

  Importance of reading patient information provided by the manufacturer.¹

  
  


• 
  

  Importance of taking darunavir with food and at the same time as ritonavir.¹ Importance of swallowing the darunavir tablets whole with a drink (e.g., water, milk); the tablets should not be chewed.¹ If also taking didanosine, administer didanosine dose 1 hour before or 2 hours after ritonavir-boosted darunavir.¹

  
  


• 
  

  If a dose of darunavir or ritonavir is missed by <6 hours, administer the dose as soon as it is remembered and the next dose at the regularly scheduled time.¹ If a dose of darunavir or ritonavir is missed by >6 hours, omit the dose and administer the next dose at the regularly scheduled time.¹ Do not administer a double dose to make up for a missed dose.¹

  
  


• 
  

  Importance of patient informing their clinician if they are allergic to sulfonamides.¹

  
  


• 
  

  Redistribution/accumulation of body fat may occur with antiretroviral therapy, with as yet unknown long-term health effects.¹

  
  


• 
  

  Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs and herbal products (e.g., St. John’s wort), and any concomitant illnesses.¹

  
  


• 
  

  Advise patients receiving selective phosphodiesterase (PDE) inhibitors (e.g., sildenafil, tadalafil, vardenafil) that they may be at increased risk of PDE inhibitor-associated adverse effects (e.g., hypotension, visual changes, priapism) and that any symptoms should be promptly reported to their clinician.¹

  
  


• 
  

  Importance of women using a reliable nonhormonal (e.g., barrier) method of contraception because of the potential interaction with hormonal contraceptives.¹

  
  


• 
  

  Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.¹

  
  


• 
  

  Importance of advising patients of other important precautionary information.¹ (See Cautions.)

  
  

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Darunavir (Ethanolate)

Routes	Dosage Forms	Strengths	Brand Names	Manufacturer
Oral	Tablets, film-coated	75 mg (of darunavir)	Prezista	Tibotec
		150 mg (of darunavir)	Prezista	Tibotec
		400 mg (of darunavir)	Prezista	Tibotec
		600 mg (of darunavir)	Prezista	Tibotec

Comparative Pricing

This pricing information is subject to change at the sole discretion of DS Pharmacy. This pricing information was updated 03/2011. Actual costs to patients will vary depending on the use of specific retail or mail-order locations and health insurance copays.

Prezista 400MG Tablets (CENTOCOR ORTHO BIOTECH PRODUCT): 60/$1060.01 or 120/$2120.03

Prezista 600MG Tablets (CENTOCOR ORTHO BIOTECH PRODUCT): 60/$1100.02 or 180/$3109.97

Disclaimer

This report on medications is for your information only, and is not considered individual patient advice. Because of the changing nature of drug information, please consult your physician or pharmacist about specific clinical use.

The American Society of Health-System Pharmacists, Inc. and Drugs.com represent that the information provided hereunder was formulated with a reasonable standard of care, and in conformity with professional standards in the field. The American Society of Health-System Pharmacists, Inc. and Drugs.com make no representations or warranties, express or implied, including, but not limited to, any implied warranty of merchantability and/or fitness for a particular purpose, with respect to such information and specifically disclaims all such warranties. Users are advised that decisions regarding drug therapy are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and the information is provided for informational purposes only. The entire monograph for a drug should be reviewed for a thorough understanding of the drug's actions, uses and side effects. The American Society of Health-System Pharmacists, Inc. and Drugs.com do not endorse or recommend the use of any drug. The information is not a substitute for medical care.

AHFS Drug Information. © Copyright, 1959-2011, Selected Revisions November 2009. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

References

1. Tibotec. Prezista (darunavir) prescribing information. Raritan, NJ; 2008 Dec.

2. Koh Y, Nakata H, Maeda K et al. Novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI) UIC-94017 (TMC114) with potent activity against multi-PI-resistant human immunodeficiency virus in vitro. Antimicrob Agents Chemother. 2003; 47:3123-9. [PubMed 14506019]

3. De Meyer S, Azijn H, Surleraux D et al. TMC114, a novel human immunodeficiency virus type 1 protease inhibitor active against protease inhibitor-resistant viruses, including a broad range of clinical isolates. Antimicrob Agents Chemother. 2005; 49:2314-21. [PubMed 15917527]

4. Panel on Antiretroviral Guidelines for Adults and Adolescents. Guidelines for the use of antiretroviral agents in HIV-1-infected adults and adolescents (November 3, 2008). From the US Department of Health and Human Services HIV/AIDS Information Services (AIDSinfo) website ().

5. Hammer SM, Saag MS, Schechter M, et al. Treatment of adult HIV infection: 2006 recommendations of the International AIDS Society–USA panel. JAMA. 2006; 296:827-43. [PubMed 16905788]

6. Banhegyi D, Esser S, Opravil M, Lefebvre E. TMC114/r outperforms investigator-selected PI(s) in treatment-experienced patients: 24-week primary efficacy and safety analysis of POWER 1. 1st European and Central Asian AIDS conference , Moscow, Russia, 2006 May 15–17. Poster. From Tibotec website ().

7. Perinatal HIV Guidelines Working Group. Public Health Service task force recommendations for use of antiretroviral drugs in pregnant HIV-1-infected women for maternal health and interventions to reduce perinatal HIV-1 transmission in the United States (April 29, 2009). From the US Department of Health and Human Services HIV/AIDS Information Services (AIDSinfo) website ().

8. Working Group on Antiretroviral Therapy and Medical Management of HIV-infected Children of the National Resource Center at the François-Xavier Bagnoud Center, Health Resources and Services Administration (HRSA), and National Institutes of Health (NIH). Guidelines for the use of antiretroviral agents in pediatric HIV infection (February 23, 2009). From the US Department of Health and Human Services HIV/AIDS Information Services (AIDSinfo) website ().

9. Madruga JV, Berger D, McMurchie M et al. Efficacy and safety of darunavir-ritonavir compared with that of lopinavir-ritonavir at 48 weeks in treatment-experienced, HIV-infected patients in TITAN: a randomised controlled phase III trial. Lancet. 2007; 370:49-58. [PubMed 17617272]

10. Ortiz R, DeJesus E, Khanlou H et al. Efficacy and safety of once-daily darunavir/ritonavir versus lopinavir/ritonavir in treatment-naive HIV-1 infected patients at week 48. AIDS. 2008; 22:1389-97. [PubMed 18614861]

11. Tibotec Therapeutics. Intelence (etravirine) tablets prescribing information. Raritan, NJ; 2008 Jan.

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• Prezista Prescribing Information (FDA)


• Prezista Advanced Consumer (Micromedex) - Includes Dosage Information


• Prezista MedFacts Consumer Leaflet (Wolters Kluwer)


• Prezista Consumer Overview

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