Darunavir

What is Darunavir?

• Darunavir (PREZISTA) is a human immunodeficiency virus (HIV-1) protease inhibitor used for the treatment of HIV infection.
• PREZISTA must be co-administered with ritonavir (PREZISTA/ritonavir) and with other antiretroviral agents.

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Darunavir

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What are the uses of this medicine?

• PREZISTA is an oral tablet used for the treatment of HIV (Human Immunodeficiency Virus) infection in adults and children 6 years of age and older.
• HIV is the virus that causes AIDS (Acquired Immune Deficiency Syndrome).
• PREZISTA is a type of anti-HIV medicine called a protease (PRO-tee-ase) inhibitor.

How does this medicine work?

• Darunavir (dar ue' na vir) is a proteinomimetic, azapeptide that blocks the catalytic site of the HIV protease preventing cleavage of viral polyprotein precursors into mature, functional proteins that are necessary for viral replication.
• PREZISTA blocks HIV protease, an enzyme which is needed for HIV to multiply.
• When used with other anti-HIV medicines, PREZISTA can help to reduce the amount of HIV in your blood (called "viral load") and increase your CD4 (T) cell count. HIV infection destroys CD4 (T) cells, which are important to the immune system.
• The immune system helps fight infection.
• Reducing the amount of HIV and increasing the CD4 (T) cell count may improve your immune system and, thus, reduce the risk of death or infections that can happen when your immune system is weak (opportunistic infections).
• When given in combination with other antiretroviral agents, darunavir has been shown to lower HIV RNA levels and delay onset of AIDS related complications.

Who Should Not Use this medicine ?

This medicine cannot be used in:

• children younger than 6 years of age
• if you are or your child is allergic to darunavir or any of the other ingredients in PREZISTA
• if you are or your child is allergic to ritonavir (NORVIR®)
• if you take or your child takes any of the following types of medicines because you could experience serious side effects:
• alfuzosin, dihydroergotamine, ergonovine, ergotamine, methylergonovine, cisapride, pimozide, oral midazolam, triazolam, St. Johns Wort, lovastatin, simvastatin, rifampin and sildenafil (for treatment of pulmonary arterial hypertension).

What drug interactions can this medicine cause?

• Co-administration of PREZISTA and ritonavir with drugs that are primarily metabolized by CYP3A and CYP2D6 may result in increased plasma concentrations of such drugs, which could increase or prolong their therapeutic effect and adverse events.
• Co-administration of darunavir and ritonavir and other drugs that inhibit CYP3A may decrease the clearance of darunavir and ritonavir and may result in increased plasma concentrations of darunavir and ritonavir.
• The appropriate dose of indinavir in combination with PREZISTA/ritonavir has not been established.
• It is not recommended to co-administer lopinavir/ritonavir and PREZISTA, with or without ritonavir.
• It is not recommended to co-administer saquinavir and PREZISTA, with or without ritonavir.
• The co-administration of PREZISTA/ritonavir and PIs other than lopinavir/ritonavir, saquinavir, atazanavir, and indinavir has not been studied. Therefore, such co-administration is not recommended.

Is this medicine FDA approved?

• It was approved by the Food and Drug Administration (FDA) on June 23, 2006.

How should this medicine be used?

Recommended dosage: Treatment-naïve adult patients:

• 800 mg (two 400 mg tablets) taken with ritonavir 100 mg once daily and with food.

Treatment-experienced adult patients:

• 600 mg (one 600 mg tablet or two 300 mg tablets) taken with ritonavir 100 mg twice daily and with food.

Pediatric patients (6 to < 18 years of age and weighing at least 44 lbs (20 kg)):

• Dosage of PREZISTA and ritonavir is based on body weight and should not exceed the treatment-experienced adult dose. Do not use once daily dosing in pediatric patients. PREZISTA tablets should be taken with ritonavir twice daily and with food.

• PREZISTA/ritonavir is not recommended for use in patients with severe hepatic impairment.

Administration:

• For adults who have never taken anti-HIV medicines, the usual dose is 800 mg (two 400 mg tablets) of PREZISTA, together with 100 mg (one 100 mg capsule) of ritonavir (NORVIR®), once daily every day.
• For adults who have taken anti-HIV medicines in the past, the usual dose is 600 mg (one 600 mg tablet or two 300 mg tablets) of PREZISTA, together with 100 mg (one 100 mg capsule) of ritonavir (NORVIR®), twice daily every day. Do not take PREZISTA once daily if you have taken anti-HIV medicines in the past.
• For children at least 6 years of age weighing at least 44 lbs (20 kg), your child's doctor will decide the right dose based on your child's weight. Your child's doctor will inform you exactly on how many PREZISTA tablets and how much ritonavir (NORVIR®) (capsules or solution) your child should take. In case your child does not tolerate ritonavir oral solution, ask your child's doctor for advice. Do not give PREZISTA once daily to your child.
• PREZISTA and ritonavir (NORVIR®) should be taken together at the same time every day. If you have questions about when to take PREZISTA and ritonavir (NORVIR®), your doctor can help you decide which schedule works for you.
• Take PREZISTA and ritonavir (NORVIR®) with food.
• Swallow the whole tablets with a drink such as water or milk.
• Do not chew the tablets.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As 75 mg tablets, 150 mg tablets, 300 mg tablets, 400 mg tablets, and 600 mg tablets

This medicine is available in fallowing brand namesː

• PREZISTA

What side effects can this medication cause?

The most common side effects of this medicine include:

• diarrhea
• nausea
• rash
• headache
• abdominal pain
• vomiting

What special precautions should I follow?

• PREZISTA must be co-administered with ritonavir and food to achieve the desired antiviral effect. Failure to administer PREZISTA with ritonavir and food may result in a loss of efficacy of darunavir.
• Drug-induced hepatitis (e.g., acute hepatitis, cytolytic hepatitis) has been reported with PREZISTA/ritonavir. Monitor liver function before and during therapy, especially in patients with underlying chronic hepatitis, cirrhosis, or in patients who have pre-treatment elevations of transaminases.
• Skin reactions ranging from mild to severe, including Stevens-Johnson Syndrome and toxic epidermal necrolysis, have been reported. Discontinue treatment if severe reaction develops.
• Darunavir contains a sulfonamide moiety. PREZISTA should be used with caution in patients with a known sulfonamide allergy.
• Patients may develop new onset diabetes mellitus or hyperglycemia. Initiation or dose adjustments of insulin or oral hypoglycemic agents may be required.
• 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.
• There have been reports of increased bleeding, including spontaneous skin hematomas and hemarthrosis in patients with hemophilia type A and B treated with PIs.
• Do not administer PREZISTA/ritonavir in pediatric patients below 3 years of age.
• Patients with hemophilia may develop increased bleeding events.

What to do in case of emergency/overdose?

Symptoms of overdosage may include:

• Human experience of acute overdose with PREZISTA/ritonavir is limited.

Treatment of overdosage:

• No specific antidote is available for overdose with PREZISTA.
• Treatment of overdose with PREZISTA consists of general supportive measures including monitoring of vital signs and observation of the clinical status of the patient.
• If indicated, elimination of unabsorbed active substance is to be achieved by emesis or gastric lavage.
• Administration of activated charcoal may also be used to aid in removal of unabsorbed active substance.
• Since PREZISTA is highly protein bound, dialysis is unlikely to be beneficial in significant removal of the active substance.

Can this medicine be used in pregnancy?

• Pregnancy Category C: PREZISTA should be used during pregnancy only if the potential benefit justifies the potential risk.
• No adequate and well-controlled studies have been conducted in pregnant women.

Can this medicine be used in children?

• Do not administer PREZISTA/ritonavir in pediatric patients below 3 years of age.
• The efficacy of PREZISTA/ritonavir in pediatric patients 3 to < 6 years of age have not been established.

What are the active and inactive ingredients in this medicine?

Active ingredient:

• DARUNAVIR ETHANOLATE

Inactive ingredients:

• SILICON DIOXIDE
• CROSPOVIDONE
• MAGNESIUM STEARATE
• CELLULOSE, MICROCRYSTALLINE
• FD&C YELLOW NO. 6
• POLYETHYLENE GLYCOL 3350
• POLYVINYL ALCOHOL
• TALC
• TITANIUM DIOXIDE

Who manufactures and distributes this medicine?

Manufactured for Tibotec, Inc. by:

• JOLLC, Gurabo, Puerto Rico
• Distributed by:
• Tibotec Therapeutics, Division of Centocor Ortho Biotech Products, L.P., Raritan NJ

What should I know about storage and disposal of this medication?

• Store PREZISTA tablets at room temperature (77°F (25°C)).
• Short-term exposure to higher or lower temperatures [from 59°F (15°C) to 86°F (30°C)] is acceptable.

Antiviral agents

Drugs for HIV Infection, in the Subclass Antiretroviral Agents

• Fusion Inhibitors (HIV)
  • Enfuvirtide, Maraviroc

• Integrase Inhibitors (HIV)
  • Dolutegravir, Elvitegravir, Raltegravir

• Monoclonal Antibodies
  • Ibalizumab

• Nonnucleoside Reverse Transcriptase Inhibitors (HIV)
  • Delavirdine, Efavirenz, Etravirine, Nevirapine, Rilpivirine

• Nucleoside Analogues (HIV)
  • Abacavir, Didanosine, Emtricitabine, Lamivudine, Stavudine, Tenofovir, Zidovudine

• Protease Inhibitors (HIV)
  • Amprenavir, Atazanavir, Darunavir, Fosamprenavir, Indinavir, Lopinavir, Nelfinavir,Ritonavir, Saquinavir, Tipranavir

Drugs for Hepatitis B

• • Alpha Interferon, Adefovir, Emtricitabine, Entecavir, Lamivudine, Telbivudine, Tenofovir

Drugs for Hepatitis C

• Interferon Based Therapies
  • Alpha Interferon and Peginterferon, Ribavirin

HCV NS5A Inhibitors

• Daclatasvir, Elbasvir, Ledipasvir, Ombitasvir, Pibrentasvir, Velpatasvir

HCV NS5B (Polymerase) Inhibitors

• Dasabuvir, Sofosbuvir

HCV Protease Inhibitors

• Asunaprevir, Boceprevir, Glecaprevir, Grazoprevir, Paritaprevir, Simeprevir, Telaprevir, Voxilaprevir

Combination Therapies

• Epclusa, Harvoni, Mavyret, Technive, Viekira Pak, Vosevi, Zepatier

Drugs for Herpes Virus Infections (HSV, CMV, others)

• Acyclovir, Cidofovir, Famciclovir, Foscarnet, Ganciclovir, Valacyclovir, Valganciclovir

Drugs for Influenza

• Amantadine, Oseltamivir, Peramivir, Rimantadine, Zanamivir

• Dailymed label info on Darunavir
• FDA Darunavir

Darunavir Resources
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