The pharmacokinetic profile, safety and antiviral activity of PREZISTA/ritonavir were evaluated in 3 randomized, open-label, multicenter studies.
Treatment-experienced pediatric subjects between the ages of 6 and less than 18 years and weighing at least 20 kg were stratified according to their weight (greater than or equal to 20 kg to less than 30 kg, greater than or equal to 30 kg to less than 40 kg, greater than or equal to 40 kg) and received PREZISTA tablets with either ritonavir capsules or oral solution plus background therapy consisting of at least two non-protease inhibitor antiretroviral drugs. Eighty patients were randomized and received at least one dose of PREZISTA/ritonavir. Pediatric subjects who were at risk of discontinuing therapy due to intolerance of ritonavir oral solution (e.g., taste aversion) were allowed to switch to the capsule formulation. Of the 44 pediatric subjects taking ritonavir oral solution, 23 subjects switched to the 100 mg capsule formulation and exceeded the weight-based ritonavir dose without changes in observed safety.
The 80 randomized pediatric subjects had a median age of 14 (range 6 to less than 18 years), and were 71% male, 54% Caucasian, 30% Black, 9% Hispanic and 8% other. The mean baseline plasma HIV-1 RNA was 4.64 log10 copies/mL, and the median baseline CD4+ cell count was 330 cells/mm3 (range: 6 to 1505 cells/mm3). Overall, 38% of pediatric subjects had baseline plasma HIV-1 RNA ≥100,000 copies/mL. Most pediatric subjects (79%) had previous use of at least one NNRTI and 96% of pediatric subjects had previously used at least one PI.
Seventy-seven pediatric subjects (96%) completed the 24-week period. Of the patients who discontinued, one patient discontinued treatment due to an adverse event. An additional 2 patients discontinued for other reasons, one patient due to compliance and another patient due to relocation.
The proportion of pediatric subjects with HIV-1 RNA less than 400 copies/mL and less than 50 copies/mL was 64% and 50%, respectively. The mean increase in CD4+ cell count from baseline was 117 cells/mm3.
Treatment-experienced pediatric subjects between the ages of 3 and less than 6 years and weighing greater than or equal to 10 kg to less than 20 kg received PREZISTA oral suspension with ritonavir oral solution plus background therapy consisting of at least two active non-protease inhibitor antiretroviral drugs. Twenty-one subjects received at least one dose of PREZISTA/ritonavir.
The 21 subjects had a median age of 4.4 years (range 3 to less than 6 years), and were 48% male, 57% Black, 29%, Caucasian and 14% other. The mean baseline plasma HIV-1 was 4.34 log10 copies/mL, the median baseline CD4+ cell count was 927 × 106 cells/L (range: 209 to 2,429 × 106 cells/L) and the median baseline CD4+ percentage was 27.7% (range: 15.6% to 51.1%). Overall, 24% of subjects had a baseline plasma HIV-1 RNA greater than or equal to 100,000 copies/mL. All subjects had used greater than or equal to 2 NRTIs, 62% of subjects had used greater than or equal to 1 NNRTI and 76% had previously used at least one HIV PI.
Twenty subjects (95%) completed the 48 week period. One subject prematurely discontinued treatment due to vomiting assessed as related to ritonavir.
The proportion of subjects with HIV-1 RNA less than 50 copies/mL at Week 48 was 71%. The mean increase in CD4+ percentage from baseline was 4%. The mean change in CD4+ cell count from baseline was 187 × 106 cells/L.
Treatment-naïve pediatric subjects between the ages of 12 and less than 18 years and weighing at least 40 kg received the adult recommended dose of PREZISTA/ritonavir 800/100 mg once daily plus background therapy consisting of at least two non-protease inhibitor antiretroviral drugs.
The 12 randomized pediatric subjects had a median age of 14.4 years (range 12.6 to 17.3 years), and were 33.3% male, 58.3% Caucasian and 41.7% Black. The mean baseline plasma HIV-1 RNA was 4.72 log10 copies/mL, and the median baseline CD4+ cell count was 282 cells/mm3 (range: 204 to 515 cells/mm3). Overall, 41.7% of pediatric subjects had baseline plasma HIV-1 RNA ≥100,000 copies/mL.
All subjects completed the 48 week treatment period.
The proportion of subjects with HIV-1 RNA less than 50 copies/mL and less than 400 copies/mL was 83.3% and 91.7%, respectively. The mean increase in CD4+ cell count from baseline was 221 × 106 cells/L.
PREZISTA® (darunavir) 100 mg per mL oral suspension is a white to off-white opaque liquid supplied in amber-colored multiple-dose bottles containing 100 mg of darunavir per mL packaged with a 6 mL oral dosing syringe with 0.2 mL gradations.
PREZISTA® (darunavir) 75 mg tablets are supplied as white, caplet-shaped, film-coated tablets debossed with “75” on one side and “TMC” on the other side.
PREZISTA® (darunavir) 150 mg tablets are supplied as white, oval-shaped, film-coated tablets debossed with “150” on one side and “TMC” on the other side.
PREZISTA® (darunavir) 600 mg tablets are supplied as orange, oval-shaped, film-coated tablets debossed with “600MG” on one side and “TMC” on the other side.
PREZISTA® (darunavir) 800 mg tablets are supplied as dark red, oval-shaped, film-coated tablets debossed with “800” on one side and “T” on the other side.
PREZISTA is packaged in bottles in the following configuration:
- 100 mg/mL oral suspension – 200 mL bottles (NDC 59676-565-01)
- 75 mg tablets — bottles of 480 (NDC 59676-563-01)
- 150 mg tablets — bottles of 240 (NDC 59676-564-01)
- 600 mg tablets — bottles of 60 (NDC 59676-562-01)
- 800 mg tablets — bottles of 30 (NDC 59676-566-30)
PREZISTA Oral Suspension
- Store at 25°C (77°F); with excursions permitted to 15°–30°C (59°–86°F).
- Do not refrigerate or freeze. Avoid exposure to excessive heat.
- Store in the original container.
- Shake well before each usage.
- Store at 25°C (77°F); with excursions permitted to 15°–30°C (59°–86°F).
Keep PREZISTA out of reach of children.
Advise the patient to read the FDA-approved patient labeling (Patient Information and Instruction for Use).
Instructions for Use
Advise patients to take PREZISTA and ritonavir with food every day on a regular dosing schedule, as missed doses can result in development of resistance. PREZISTA must always be used with ritonavir in combination with other antiretroviral drugs. Advise patients not to alter the dose of either PREZISTA or ritonavir, discontinue ritonavir, or discontinue therapy with PREZISTA without consulting their physician [see Dosage and Administration (2)].
Inform patients that drug-induced hepatitis (e.g., acute hepatitis, cytolytic hepatitis) has been reported with PREZISTA co-administered with 100 mg of ritonavir. Advise patients about the signs and symptoms of liver problems [see Warnings and Precautions (5.2)].
Severe Skin Reactions
Inform patients that skin reactions ranging from mild to severe, including Stevens-Johnson Syndrome, drug rash with eosinophilia and systemic symptoms, and toxic epidermal necrolysis, have been reported with PREZISTA co-administered with 100 mg of ritonavir. Advise patients to discontinue PREZISTA/ritonavir immediately if signs or symptoms of severe skin reactions develop. These can include but are not limited to severe rash or rash accompanied with fever, general malaise, fatigue, muscle or joint aches, blisters, oral lesions, conjunctivitis, hepatitis and/or eosinophilia [see Warnings and Precautions (5.3)].
PREZISTA/ritonavir may interact with many drugs; therefore, advise patients to report to their healthcare provider the use of any other prescription or nonprescription medication or herbal products, including St. John’s wort [see Contraindications (4), Warnings and Precautions (5.4, 5.5) and Drug Interactions (7)].
Instruct patients receiving combined hormonal contraception or the progestin only pill to use an effective alternative (non-hormonal) contraceptive method or add a barrier method during therapy with PREZISTA/ritonavir because hormonal levels may decrease [see Drug Interactions (7.3) and Use in Specific Populations (8.3)].
Inform patients that redistribution or accumulation of body fat may occur in patients receiving antiretroviral therapy, including PREZISTA/ritonavir, and that the cause and long-term health effects of these conditions are not known at this time [see Warnings and Precautions (5.7)].
Immune Reconstitution Syndrome
Advise patients to inform their healthcare provider immediately of any symptoms of infection, as in some patients with advanced HIV infection (AIDS), signs and symptoms of inflammation from previous infections may occur soon after anti-HIV treatment is started [see Warnings and Precautions (5.8)].
Inform patients that there is an antiretroviral pregnancy registry to monitor fetal outcomes of pregnant women exposed to PREZISTA [see Use in Specific Populations (8.1)].
Instruct women with HIV-1 infection not to breastfeed because HIV-1 can be passed to the baby in breast milk [see Use in Specific Populations (8.2)].
Product of Ireland
PREZISTA oral suspension
Janssen Pharmaceutica, NV
Janssen Ortho LLC
Janssen Cilag SpA
Division of Janssen Products, LPTitusville NJ 08560
PREZISTA® is a registered trademark of Janssen Pharmaceuticals.
© 2006 Janssen Pharmaceutical Companies
|This Patient Information has been approved by the U.S. Food and Drug Administration.||Revised: 05/2019|
|PREZISTA ® (pre-ZIS-ta) (darunavir)oral suspension||PREZISTA ® (pre-ZIS-ta) (darunavir)tablet|
|Read this Patient Information before you start taking PREZISTA and each time you get a refill. There may be new information. This information does not take the place of talking to your healthcare provider about your medical condition or your treatment.Also read the Patient Information leaflet for ritonavir.|
| What is the most important information I should know about PREZISTA? |
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|Rash occurred more often in people taking PREZISTA and raltegravir together than with either drug separately, but was generally mild.See “What are the possible side effects of PREZISTA?“ for more information about side effects.|
|What is PREZISTA? PREZISTA is a prescription HIV-1 (Human Immunodeficiency Virus-type 1) medicine used with ritonavir and other antiretroviral medicines to treat HIV-1 infection in adults and children 3 years of age and older. HIV is the virus that causes AIDS (Acquired Immune Deficiency Syndrome).PREZISTA should not be used in children under 3 years of age.When used with other antiretroviral medicines to treat HIV-1 infection, PREZISTA may help: |
Reducing the amount of HIV-1 and increasing the CD4+ (T) cells in your blood may improve your immune system. This may reduce your risk of death or getting infections that can happen when your immune system is weak (opportunistic infections).PREZISTA does not cure HIV-1 infection or AIDS. You must keep taking HIV-1 medicines to control HIV-1 infection and decrease HIV-related illnesses.Avoid doing things that can spread HIV-1 infection to others:
Ask your healthcare provider if you have any questions on how to prevent passing HIV to other people.
|Who should not take PREZISTA?Do not take PREZISTA with any medicine that contains: |
Serious problems can happen if you or your child take any of these medicines with PREZISTA.
| What should I tell my healthcare provider before taking PREZISTA?Before taking PREZISTA, tell your healthcare provider if you: |
Tell your healthcare provider about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements. Some medicines interact with PREZISTA. Keep a list of your medicines to show your healthcare provider and pharmacist.
| How should I take PREZISTA? |
|What are the possible side effects of PREZISTA?PREZISTA may cause serious side effects, including: |
The most common side effects of PREZISTA include:
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|Tell your healthcare provider if you have any side effect that bothers you or that does not go away.These are not all of the possible side effects of PREZISTA.Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.|
| How should I store PREZISTA? |
Keep PREZISTA and all medicines out of the reach of children.
|General information about the safe and effective use of PREZISTA. Medicines are sometimes prescribed for purposes other than those listed in a Patient Information leaflet. Do not use PREZISTA for a condition for which it was not prescribed. Do not give PREZISTA to other people even if they have the same condition you have. It may harm them.This leaflet summarizes the most important information about PREZISTA. If you would like more information, talk to your healthcare provider. You can ask your healthcare provider or pharmacist for information about PREZISTA that is written for health professionals. For more information, call 1-800-526-7736.|
|What are the ingredients in PREZISTA? Active ingredient: darunavirInactive ingredients:PREZISTA oral suspension: citric acid monohydrate, hydrochloric acid (for pH adjustment), hydroxypropyl cellulose, masking flavor, methylparaben sodium, microcrystalline cellulose, purified water, sodium carboxymethylcellulose, strawberry cream flavor, and sucralose.PREZISTA 75 mg and 150 mg tablets: colloidal silicon dioxide, crospovidone, magnesium stearate, microcrystalline cellulose. The film coating contains: OPADRY® White (polyethylene glycol 3350, polyvinyl alcohol-partially hydrolyzed, talc, titanium dioxide).PREZISTA 600 mg tablets: colloidal silicon dioxide, crospovidone, magnesium stearate, microcrystalline cellulose. The film coating contains: OPADRY® Orange (FD&C Yellow No. 6, polyethylene glycol 3350, polyvinyl alcohol-partially hydrolyzed, talc, titanium dioxide).PREZISTA 800 mg tablets: colloidal silicon dioxide, crospovidone, magnesium stearate, microcrystalline cellulose, hypromellose. The film coating contains: OPADRY® Dark Red (iron oxide red, polyethylene glycol 3350, polyvinyl alcohol-partially hydrolyzed, talc, titanium dioxide).Product of IrelandManufactured by: PREZISTA oral suspension, Janssen Pharmaceutica NV, Beerse, Belgium PREZISTA tablets, Janssen Ortho LLC, Gurabo, PR 00778 or Janssen Cilag SpA, Latina, ITManufactured for: Janssen Therapeutics, Division of Janssen Products, LP, Titusville NJ 08560PREZISTA® is a registered trademark of Janssen Pharmaceuticals© 2006 Janssen Pharmaceutical Companies|
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