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Prezista

Last reviewed on RxList: 9/11/2020
Prezista Side Effects Center

What Is Prezista?

Prezista (darunavir) is a type of antiviral medication called a protease inhibitor used to treat HIV, which causes acquired immunodeficiency syndrome (AIDS).

What Are Side Effects of Prezista?

Prezista is not a cure for HIV or AIDS. Common side effects of Prezista include:

  • diarrhea,
  • nausea,
  • vomiting,
  • heartburn,
  • stomach pain,
  • weakness,
  • headache,
  • skin rash, or
  • changes in the shape or location of body fat (especially in your arms, legs, face, neck, breasts, and waist)

Since Prezista is always taken with other HIV medications, it may be difficult to tell whether it is causing certain side effects.

Dosage for Prezista?

The recommended oral dose of Prezista is 800 mg (two 400 mg tablets or 8 mL of the oral suspension) taken with ritonavir 100 mg (one 100 mg tablet/capsule or 1.25 mL of a 80 mg/mL ritonavir oral solution) once daily and with food.

What Drugs, Substances, or Supplements Interact with Prezista?

Prezista may interact with buprenorphine, naloxone, methadone, risperidone, thioridazine, antibiotics, antifungals, antidepressants, beta-blockers, blood thinners, calcium channel blockers, cholesterol-lowering medicines, drugs that weaken the immune system, heart rhythm medications, insulin or oral diabetes medications, medicines to treat erectile dysfunction, other HIV/AIDS medicines, seizure medications, or steroids. Many other medicines can interact with Prezista. Tell your doctor all medications and supplements you use. During pregnancy, Prezista should be used only when prescribed.

Prezista During Pregnancy and Breastfeeding

It is normal to prescribe certain HIV medicines for pregnant women with HIV. This has been shown to decrease the risk of giving HIV to the baby. Consult your doctor. It is unknown if this medication passes into breast milk. Because breast milk can transmit HIV, do not breastfeed.

Additional Information

Our Prezista (darunavir) Side Effects Drug Center provides a comprehensive view of available drug information on the potential side effects when taking this medication.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

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Prezista Consumer Information

Get emergency medical help if you have signs of an allergic reaction (hives, difficult breathing, swelling in your face or throat) or a severe skin reaction (fever, sore throat, burning eyes, skin pain, red or purple skin rash with blistering and peeling).

Call your doctor at once if you have:

  • the first sign of any skin rash, no matter how mild;
  • high blood sugar--increased thirst, increased urination, dry mouth, fruity breath odor; or
  • signs of liver or pancreas problems--loss of appetite, upper stomach pain (that may spread to your back), nausea or vomiting, fast heart rate, dark urine, jaundice (yellowing of the skin or eyes).

Darunavir affects your immune system, which may cause certain side effects (even weeks or months after you've taken this medicine). Tell your doctor if you have:

  • signs of a new infection--fever, night sweats, swollen glands, cold sores, cough, wheezing, diarrhea, weight loss;
  • trouble speaking or swallowing, problems with balance or eye movement, weakness or prickly feeling; or
  • swelling in your neck or throat (enlarged thyroid), menstrual changes, impotence.

Common side effects may include:

  • nausea, vomiting, diarrhea, stomach pain;
  • headache;
  • rash; or
  • changes in the shape or location of body fat (especially in your arms, legs, face, neck, breasts, and waist).

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Read the entire detailed patient monograph for Prezista (Darunavir)

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Prezista Professional Information

SIDE EFFECTS

The following adverse reactions are discussed in other sections of labeling:

Due to the need for co-administration of PREZISTA with ritonavir, please refer to ritonavir prescribing information for ritonavir-associated adverse reactions.

Clinical Trials Experience

Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in clinical practice.

Treatment Naïve-Adults

TMC114-C211

The safety assessment is based on all safety data from the Phase 3 trial TMC114-C211 comparing PREZISTA/ritonavir 800/100 mg once daily versus lopinavir/ritonavir 800/200 mg per day in 689 antiretroviral treatment-naïve HIV-1-infected adult subjects. The total mean exposure for subjects in the PREZISTA/ritonavir 800/100 mg once daily arm and in the lopinavir/ritonavir 800/200 mg per day arm was 162.5 and 153.5 weeks, respectively.

The majority of the adverse drug reactions (ADRs) reported during treatment with PREZISTA/ritonavir 800/100 mg once daily were mild in severity. The most common clinical ADRs to PREZISTA/ritonavir 800/100 mg once daily (greater than or equal to 5%) of at least moderate intensity (greater than or equal to Grade 2) were diarrhea, headache, abdominal pain and rash. 2.3% of subjects in the PREZISTA/ritonavir arm discontinued treatment due to ADRs.

ADRs to PREZISTA/ritonavir 800/100 mg once daily of at least moderate intensity (greater than or equal to Grade 2) in antiretroviral treatment-naïve HIV-1-infected adult subjects are presented in Table 6 and subsequent text below the table.

Table 6: Selected Clinical Adverse Drug Reactions to PREZISTA/ritonavir 800/100 mg Once Daily* of at Least Moderate Intensity (≥Grade 2) Occurring in ≥2% of Antiretroviral Treatment-Naïve HIV-1-Infected Adult Subjects (Trial TMC114-C211)

System organ class, preferred term, % PREZISTA/ritonavir 800/100 mg once daily + TDF/FTC
N=343
lopinavir/ritonavir 800/200 mg per day + TDF/FTC
N=346
Gastrointestinal Disorders
  Abdominal pain 6% 6%
  Diarrhea 9% 16%
  Nausea 4% 4%
  Vomiting 2% 4%
General Disorders and Administration Site Conditions
  Fatigue <1% 3%
Metabolism and Nutrition Disorders
  Anorexia 2% <1%
Nervous System Disorders
  Headache 7% 6%
Skin and Subcutaneous Tissue Disorders
  Rash 6% 7%
N=total number of subjects per treatment group; FTC=emtricitabine; TDF=tenofovir disoproxil fumarate
* Excluding laboratory abnormalities reported as ADRs.

Less Common Adverse Reactions

Treatment-emergent ADRs of at least moderate intensity (greater than or equal to Grade 2) occurring in less than 2% of antiretroviral treatment-naïve subjects receiving PREZISTA/ritonavir 800/100 mg once daily are listed below by body system:

Gastrointestinal Disorders: acute pancreatitis, dyspepsia, flatulence

General Disorders and Administration Site Conditions: asthenia

Hepatobiliary Disorders: acute hepatitis (e.g., acute hepatitis, cytolytic hepatitis, hepatotoxicity)

Immune System Disorders: (drug) hypersensitivity, immune reconstitution syndrome

Metabolism and Nutrition Disorders: diabetes mellitus

Musculoskeletal and Connective Tissue Disorders: myalgia, osteonecrosis

Psychiatric Disorders: abnormal dreams

Skin and Subcutaneous Tissue Disorders: angioedema, pruritus, Stevens-Johnson Syndrome, urticaria

Laboratory Abnormalities

Selected Grade 2 to 4 laboratory abnormalities that represent a worsening from baseline observed in antiretroviral treatment-naïve adult subjects treated with PREZISTA/ritonavir 800/100 mg once daily are presented in Table 7.

Table 7: Grade 2 to 4 Laboratory Abnormalities Observed in Antiretroviral Treatment-Naïve HIV-1Infected Adult Subjects* (Trial TMC114-C211)

Laboratory parameter % Limit PREZISTA/ ritonavir 800/100 mg once daily + TDF/FTC lopinavir/ ritonavir 800/200 mg per day + TDF/FTC
Biochemistry
Alanine Aminotransferase
  Grade 2 >2.5 to ≤5.0 X ULN 9% 9%
  Grade 3 >5.0 to ≤10.0 X ULN 3% 3%
  Grade 4 >10.0 X ULN <1% 3%
Aspartate Aminotransferase
  Grade 2 >2.5 to ≤5.0 X ULN 7% 10%
  Grade 3 >5.0 to ≤10.0 X ULN 4% 2%
  Grade 4 >10.0 X ULN 1% 3%
Alkaline Phosphatase
  Grade 2 >2.5 to ≤5.0 X ULN 1% 1%
  Grade 3 >5.0 to ≤10.0 X ULN 0% <1%
  Grade 4 >10.0 X ULN 0% 0%
Hyperbilirubinemia
  Grade 2 >1.5 to ≤2.5 X ULN <1% 5%
  Grade 3 >2.5 to ≤5.0 X ULN <1% <1%
  Grade 4 >5.0 X ULN 0% 0%
Triglycerides
  Grade 2 5.65-8.48 mmol/L 500-750 mg/dL 3% 10%
  Grade 3 8.49-13.56 mmol/L 751-1200 mg/dL 2% 5%
  Grade 4 >13.56 mmol/L >1200 mg/dL 1% 1%
Total Cholesterol
  Grade 2 6.20-7.77 mmol/L 240-300 mg/dL 23% 27%
  Grade 3 >7.77 mmol/L >300 mg/dL 1% 5%
Low-Density Lipoprotein Cholesterol
  Grade 2 4.13-4.90 mmol/L 160-190 mg/dL 14% 12%
  Grade 3 ≥4.91 mmol/L ≥191 mg/dL 9% 6%
Elevated Glucose Levels
  Grade 2 6.95-13.88 mmol/L 126-250 mg/dL 11% 10%
  Grade 3 13.89-27.75 mmol/L 251-500 mg/dL 1% <1%
  Grade 4 >27.75 mmol/L >500 mg/dL 0% 0%
Pancreatic Lipase
  Grade 2 >1.5 to ≤3.0 X ULN 3% 2%
  Grade 3 >3.0 to ≤5.0 X ULN <1% 1%
  Grade 4 >5.0 X ULN 0% <1%
Pancreatic Amylase
  Grade 2 >1.5 to ≤2.0 X ULN 5% 2%
  Grade 3 >2.0 to ≤5.0 X ULN 5% 4%
  Grade 4 >5.0 X ULN 0% <1%
N=total number of subjects per treatment group; FTC=emtricitabine; TDF=tenofovir disoproxil fumarate
* Grade 4 data not applicable in Division of AIDS grading scale.

Treatment-Experienced Adults

TMC114-C214

The safety assessment is based on all safety data from the Phase 3 trial TMC114-C214 comparing PREZISTA/ritonavir 600/100 mg twice daily versus lopinavir/ritonavir 400/100 mg twice daily in 595 antiretroviral treatment-experienced HIV-1-infected adult subjects. The total mean exposure for subjects in the PREZISTA/ritonavir 600/100 mg twice daily arm and in the lopinavir/ritonavir 400/100 mg twice daily arm was 80.7 and 76.4 weeks, respectively.

The majority of the ADRs reported during treatment with PREZISTA/ritonavir 600/100 mg twice daily were mild in severity. The most common clinical ADRs to PREZISTA/ritonavir 600/100 mg twice daily (greater than or equal to 5%) of at least moderate intensity (greater than or equal to Grade 2) were diarrhea, nausea, rash, abdominal pain and vomiting. 4.7% of subjects in the PREZISTA/ritonavir arm discontinued treatment due to ADRs.

ADRs to PREZISTA/ritonavir 600/100 mg twice daily of at least moderate intensity (greater than or equal to Grade 2) in antiretroviral treatment-experienced HIV-1-infected adult subjects are presented in Table 8 and subsequent text below the table.

Table 8: Selected Clinical Adverse Drug Reactions to PREZISTA/ritonavir 600/100 mg Twice Daily* of at Least Moderate Intensity (≥Grade 2) Occurring in ≥2% of Antiretroviral Treatment- Experienced HIV-1-Infected Adult Subjects (Trial TMC114-C214)

System organ class, preferred term, % PREZISTA/ritonavir 600/100 mg twice daily + OBR
N=298
lopinavir/ritonavir 400/100 mg twice daily + OBR
N=297
Gastrointestinal Disorders
  Abdominal distension 2% <1%
  Abdominal pain 6% 3%
  Diarrhea 14% 20%
  Dyspepsia 2% 1%
  Nausea 7% 6%
  Vomiting 5% 3%
General Disorders and Administration Site Conditions
  Asthenia 3% 1%
  Fatigue` 2% 1%
Metabolism and Nutrition Disorders
  Anorexia 2% 2%
  Diabetes mellitus 2% <1%
Nervous System Disorders
  Headache 3% 3%
Skin and Subcutaneous Tissue Disorders
  Rash 7% 3%
N=total number of subjects per treatment group; OBR=optimized background regimen
* Excluding laboratory abnormalities reported as ADRs

Less Common Adverse Reactions

Treatment-emergent ADRs of at least moderate intensity (greater than or equal to Grade 2) occurring in less than 2% of antiretroviral treatment-experienced subjects receiving PREZISTA/ritonavir 600/100 mg twice daily are listed below by body system:

Gastrointestinal Disorders: acute pancreatitis, flatulence

Musculoskeletal and Connective Tissue Disorders: myalgia

Psychiatric Disorders: abnormal dreams

Skin and Subcutaneous Tissue Disorders: pruritus, urticaria

Laboratory Abnormalities

Selected Grade 2 to 4 laboratory abnormalities that represent a worsening from baseline observed in antiretroviral treatment-experienced adult subjects treated with PREZISTA/ritonavir 600/100 mg twice daily are presented in Table 9.

Table 9: Grade 2 to 4 Laboratory Abnormalities Observed in Antiretroviral Treatment-Experienced HIV-1-Infected Adult Subjects* (Trial TMC114-C214)

Laboratory parameter, % Limit PREZISTA/ ritonavir 600/100 mg twice daily + OBR lopinavir/ ritonavir 400/100 mg twice daily + OBR
Biochemistry
Alanine Aminotransferase
  Grade 2 >2.5 to ≤5.0 X ULN 7% 5%
  Grade 3 >5.0 to ≤10.0 X ULN 2% 2%
  Grade 4 >10.0 X ULN 1% 2%
Aspartate Aminotransferase
  Grade 2 >2.5 to ≤5.0 X ULN 6% 6%
  Grade 3 >5.0 to ≤10.0 X ULN 2% 2%
  Grade 4 >10.0 X ULN <1% 2%
Alkaline Phosphatase
  Grade 2 >2.5 to ≤5.0 X ULN <1% 0%
  Grade 3 >5.0 to ≤10.0 X ULN <1% <1%
  Grade 4 >10.0 X ULN 0% 0%
Hyperbilirubinemia
  Grade 2 >1.5 to ≤2.5 X ULN <1% 2%
  Grade 3 >2.5 to ≤5.0 X ULN <1% <1%
  Grade 4 >5.0 X ULN <1% 0%
Triglycerides
  Grade 2 5.65-8.48 mmol/L 500-750 mg/dL 10% 11%
  Grade 3 8.49-13.56 mmol/L 751-1200 mg/dL 7% 10%
  Grade 4 >13.56 mmol/L >1200 mg/dL 3% 6%
Total Cholesterol
  Grade 2 6.20-7.77 mmol/L 240-300 mg/dL 25% 23%
  Grade 3 >7.77 mmol/L >300 mg/dL 10% 14%
Low-Density Lipoprotein Cholesterol
  Grade 2 4.13-4.90 mmol/L 160-190 mg/dL 14% 14%
  Grade 3 ≥4.91 mmol/L ≥191 mg/dL 8% 9%
Elevated Glucose Levels
  Grade 2 6.95-13.88 mmol/L 126-250 mg/dL 10% 11%
  Grade 3 13.89-27.75 mmol/L 251-500 mg/dL 1% <1%
  Grade 4 >27.75 mmol/L >500 mg/dL <1% 0%
Pancreatic Lipase
  Grade 2 >1.5 to ≤3.0 X ULN 3% 4%
  Grade 3 >3.0 to ≤5.0 X ULN 2% <1%
  Grade 4 >5.0 X ULN <1% 0%
Pancreatic Amylase
  Grade 2 >1.5 to ≤2.0 X ULN 6% 7%
  Grade 3 >2.0 to ≤5.0 X ULN 7% 3%
  Grade 4 >5.0 X ULN 0% 0%
N=total number of subjects per treatment group; OBR=optimized background regimen
* Grade 4 data not applicable in Division of AIDS grading scale

Serious ADRs

The following serious ADRs of at least moderate intensity (greater than or equal to Grade 2) occurred in the Phase 2b and Phase 3 trials with PREZISTA/ritonavir: abdominal pain, acute hepatitis, acute pancreatitis, anorexia, asthenia, diabetes mellitus, diarrhea, fatigue, headache, hepatic enzyme increased, hypercholesterolemia, hyperglycemia, hypertriglyceridemia, immune reconstitution syndrome, low density lipoprotein increased, nausea, pancreatic enzyme increased, rash, Stevens-Johnson Syndrome, and vomiting.

Patients Co-Infected With Hepatitis B And/Or Hepatitis C Virus

In subjects co-infected with hepatitis B or C virus receiving PREZISTA/ritonavir, the incidence of adverse events and clinical chemistry abnormalities was not higher than in subjects receiving PREZISTA/ritonavir who were not co-infected, except for increased hepatic enzymes [see WARNINGS AND PRECAUTIONS]. The pharmacokinetic exposure in co-infected subjects was comparable to that in subjects without co-infection.

Clinical Trials Experience

Pediatric Patients

PREZISTA/ritonavir has been studied in combination with other antiretroviral agents in 3 Phase 2 trials. TMC114-C212, in which 80 antiretroviral treatment-experienced HIV-1infected pediatric subjects 6 to less than 18 years of age and weighing at least 20 kg were included, TMC114-C228, in which 21 antiretroviral treatment-experienced HIV-1-infected pediatric subjects 3 to less than 6 years of age and weighing at least 10 kg were included, and TMC114-C230 in which 12 antiretroviral treatment-naïve HIV-1 infected pediatric patients aged from 12 to less than 18 years and weighing at least 40 kg were included. The TMC114-C212 and C228 trials evaluated PREZISTA/ritonavir twice daily dosing and the TMC114-C230 trial evaluated PREZISTA/ritonavir once daily dosing [see Use In Specific Populations and Clinical Studies].

Frequency, type, and severity of ADRs in pediatric subjects were comparable to those observed in adults.

TMC114-C212

Clinical ADRs to PREZISTA/ritonavir (all grades, greater than or equal to 3%), were vomiting (13%), diarrhea (11%), abdominal pain (10%), headache (9%), rash (5%), nausea (4%), and fatigue (3%).

Grade 3 or 4 laboratory abnormalities were ALT increased (Grade 3: 3%; Grade 4: 1%), AST increased (Grade 3: 1%), pancreatic amylase increased (Grade 3: 4%, Grade 4: 1%), pancreatic lipase increased (Grade 3: 1%), total cholesterol increased (Grade 3: 1%), and LDL increased (Grade 3: 3%).

TMC114-C228

Clinical ADRs to PREZISTA/ritonavir (all grades, greater than or equal to 5%), were diarrhea (24%), vomiting (19%), rash (19%), abdominal pain (5%), and anorexia (5%).

There were no Grade 3 or 4 laboratory abnormalities considered as ADRs in this trial.

TMC114-C230

Clinical ADRs to PREZISTA/ritonavir (all grades, greater than or equal to 3%), were vomiting (33%), nausea (25%), diarrhea (16.7%), abdominal pain (8.3%), decreased appetite (8.3%), pruritus (8.3%), and rash (8.3%).

There were no Grade 3 or 4 laboratory abnormalities considered as ADRs in this trial.

Postmarketing Experience

The following events have been identified during post approval use of PREZISTA. Because these events are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure.

Redistribution of body fat has been reported.

Rarely, rhabdomyolysis (associated with co-administration with HMG-CoA reductase inhibitors and PREZISTA/ritonavir) has been reported.

In addition, toxic epidermal necrolysis, acute generalized exanthematous pustulosis and drug rash with eosinophilia and systemic symptoms have been reported rarely [see WARNINGS AND PRECAUTIONS].

Read the entire FDA prescribing information for Prezista (Darunavir)

Related Resources for Prezista

Read the Prezista User Reviews »

© Prezista Patient Information is supplied by Cerner Multum, Inc. and Prezista Consumer information is supplied by First Databank, Inc., used under license and subject to their respective copyrights.

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