Prezista Tablets / Film-coated
Darunavir
400mg
JANSSEN-CILAG S.p.A.
| Pack size | 60's HDPE Bottle |
|---|---|
| Dispensing mode | POM |
| Source | ITALY |
| Agent | Modern Pharmaceutical Co. |
| Retail Price | 2284.50 AED |
Available as:
Indications
Prezista Tablets / Film-coated is used for:
HIV Infection
Adult Dose
HIV Infection
Coadministered with ritonavir and in combination with other antiretroviral agents for HIV infection
Treatment-naive or antiretroviral treatment-experienced (with no darunavir resistance associated substitutions): 800 mg + ritonavir 100 mg PO qDay with food
Treatment-experienced (with at least 1 DRV mutation) or genotyping not obtained: 600 mg + ritonavir 100 mg PO q12hr with food
Pregnant females
Recommended: 600 mg + ritonavir 100 mg PO q12hr with food
800 mg + ritonavir 100 mg PO qDay should only be considered in certain pregnant patients who are already on a stable darunavir 800 mg + ritonavir 100 mg qDay regimen prior to pregnancy, are virologically suppressed (ie, HIV-1 RNA <50 copies/mL), and in whom a change to the twice daily regimen may compromise tolerability or compliance
Child Dose
HIV Infection
Coadministered with ritonavir and in combination with other antiretroviral agents for HIV infection
<3 years or <10 kg: Safety and efficacy not established
Treatment-naive or antiretroviral treatment-experienced (with no darunavir resistance associated substitutions)
NOTE: The HIV treatment guidelines differ from the prescribing information and recommend that once-daily darunavir dosing should NOT be used as initial therapy in children <12 yr; a switch to once-daily therapy may be considered in patients who have undetectable viral loads on twice-daily therapy to enhance ease of use and support compliance
Weight 10 kg to <15 kg
Use oral suspension
>10 kg to <11 kg: 350 mg (3.6 mL)* + ritonavir 64 mg (0.8 mL) PO qDay
>11 kg to <12 kg: 385 mg (4 mL)* + ritonavir 64 mg (0.8 mL) PO qDay
>12 kg to <13 kg: 420 mg (4.2 mL) + ritonavir 80 mg (1 mL) PO qDay
>13 kg to <14 kg: 455 mg (4.6 mL)* + ritonavir 80 mg (1 mL) PO qDay
>14 kg to <15 kg: 490 mg (5 mL)* + ritonavir 96 mg (1.2 ml) PO qDay
*NOTE: Doses that were rounded up to nearest measurable suspension dose
Weight >15 kg
>15 kg to <30 kg: 600 mg + ritonavir 100 mg PO qDay
>30 kg to <40 kg: 675 mg + ritonavir 100 mg PO qDay
>40 kg: 800 mg + ritonavir 100 mg PO qDay
Antiretroviral treatment-experienced with at least 1 darunavir resistance associated substitution
Weight 10 kg to <15 kg
Use oral suspension
>10 kg to <11 kg: 200 mg (2 mL) + ritonavir 32 mg (0.4 mL) PO BID
>11 kg to <12 kg: 220 mg (2.2 mL) + ritonavir 40 mg (0.4 mL) PO BID
>12 kg to <13 kg: 240 mg (2.4 mL) + ritonavir 32 mg (0.5 mL) PO BID
>13 kg to <14 kg: 260 mg (2.6 mL) + ritonavir 40 mg (0.5 mL) PO BID
>14 kg to <15 kg: 280 mg (2.8 mL) + ritonavir 48 mg (0.6 mL) PO BID
Weight >15 kg
>15 kg to <30 kg: 375 mg + ritonavir 48 mg PO BID
>30 kg to <40 kg: 450 mg + ritonavir 60 mg PO BID
>40 kg: 600 mg + ritonavir 100 mg PO BID
Renal Dose
Renal impairment
Mild-to-moderate (> 30 mL/min): No dosage adjustment required
Severe (< 30 mL/min): Data not available, but renal clearance is limited and decreased total body clearance not expected
Administration
Swallow tablet whole; do not chew, crush, or split
Must take with food; food increases the area under the curve (AUC) and maximum plasma concentration (Cmax) by 30%
Assess ability to swallow; use oral suspension for adults or children who cannot swallow the tablet whole
Contra Indications
Hypersensitivity
Precautions
Must be taken with ritonavir and food, since dose is based on the fact that darunavir is metabolized by CYP3A4 and ritonavir is a potent CYP3A4 inhibitor
Severe skin reactions, accompanied by fever and/or elevations of transaminases reported (0.4%); Stevens-Johnson Syndrome (<0.1%), toxic epidermal necrolysis, drug rash with eosinophilia and systemic symptoms, and acute generalized exanthematous pustulosis also reported
Caution with elderly patients
Caution with hepatic impairment (not recommended if severe)
Contains a sulfa moiety; monitor patients with a known sulfonamide allergy
Increase in total cholesterol and triglycerides reported; screen before therapy and throughout treatment
Pancreatitis reported; use caution in patients at risk for pancreatitis (those with elevated triglycerids, history of pancreatitis, or advanced HIV disease
Risk of immune reconstitution syndrome
Redistribution/accumulation of body fat, including central obesity, dorsocervical fat enlargement (buffalo hump), peripheral wasting, facial wasting, breast enlargement, and “cushingoid appearance” have been observed in patients receiving antiretroviral therapy
Patients may develop new onset diabetes mellitus or hyperglycemia; initiation or dose adjustments of insulin or oral hypoglycemic agents may be required
Patients with hemophilia may develop increased bleeding events
Not for use in patients < 3 years of age; toxicity may occur
Hepatoxicity
Risk of hepatotoxicity including drug induced hepatitis: acute hepatitis, cytolytic hepatitis
Especially with preexisting liver dysfunction (chronic hepatitis B or C)
Interrupt or discontinue treatment if new/worsening liver dysfunction develops
Pregnancy-Lactation
Pregnancy: The recommended dosage in pregnant patients is 600 mg taken with ritonavir 100 mg twice daily with food; darunavir 800 mg taken with ritonavir 100 mg once daily should only be considered in certain pregnant patients who are already on a stable darunavir 800 mg with ritonavir 100 mg once daily regimen prior to pregnancy, are virologically suppressed (HIV-1 RNA less than 50 copies per mL), and in whom a change to twice daily darunavir 600 mg with ritonavir 100 mg may compromise tolerability or compliance
Use of darunavir may reduce the efficacy of combined hormonal contraceptives and the progestin only pill; advise patients using combined hormonal contraceptives or the progestin only pill to use an effective alternative contraceptive method or add a barrier method of contraception; for co-administration with drospirenone, clinical monitoring recommended due to potential for hyperkalemia
Lactation: The Centers for Disease Control and Prevention recommend that HIV-infected mothers not breastfeed their infants to avoid risking postnatal transmission of HIV
There are no data on the presence of darunavir in human milk, the effects on the breastfed infant, or the effects on milk production; because of the potential for (1) HIV transmission (in HIV-negative infants), (2) developing viral resistance (in HIV-positive infants) and (3) serious adverse reactions in a breastfed infant, instruct mothers not to breastfeed if they are receiving darunavir
Interactions
Adverse Effects
Side effects of Darunavir :
>10%
Increased total cholesterol (10-25%)
Increased triglycerides (3-10%)
1-10%
Diarrhea (9%)
Headache (7%)
Rash (6%)
Abdominal pain (6%)
Nausea (4%)
Vomiting (2%)
Anorexia (2%)
<1%
Fatigue
Frequency Not Defined
Gastrointestinal disorders: Acute pancreatitis, dyspepsia, flatulence
General disorders and administration site Conditions: Asthenia
Hepatobiliary disorders: Acute hepatitis (eg, cytolytic hepatitis, hepatotoxicity)
Immune dystem disorders: Hypersensitivity, immune reconstitution syndrome
Metabolism and nutrition disorders: Diabetes mellitus/hyperglycemia, fat distribution
Musculoskeletal and connective tissue disorders: Myalgia, osteonecrosis
Psychiatric disorders: Abnormal dreams
Skin and subcutaneous tissue disorders: Angioedema, pruritus, Stevens-Johnson Syndrome, urticaria
Mechanism of Action
Protease Inhibitor; inhibits cleavage of Gag-Pol polyprotein precursors, which in turn causes the formation of immature, noninfectious viral particles.
Note
Prezista 400mg Tablets / Film-coated manufactured by JANSSEN-CILAG S.p.A.. Its generic name is Darunavir. Prezista is availble in United Arab Emirates.
Farmaco UAE drug index information on Prezista Tablets / Film-coated is not intended for diagnosis, medical advice or treatment; neither intended to be a substitute for the exercise of professional judgment.