Prezista
Prezista - General Information
Prezista is a protease inhibitor used to treat HIV. It acts on the HIV aspartyl protease which the virus needs to cleave the HIV polyprotein into its functional fragments.
Pharmacology of Prezista
Prezista is an inhibitor of the human immunodeficiency virus (HIV) protease. In studies, the drug, co-administered with ritonavir in combination therapy, significantly reduced viral load and increased CD4 cell counts in this treatment-experienced patient population (Tibotec, 2006, Product Monograph, Prezista 2006).
Prezista for patients
Patient Information about
PREZISTA (pre-ZIS-ta)
for HIV (Human Immunodeficiency Virus) Infection
Generic name: darunavir (da-ROO-nuh-veer)
ALERT: Find out about medicines that should NOT be taken with PREZISTA. Please also read the section "Who should not take PREZISTA?".
Please read this information before you start taking PREZISTA. Also, read the leaflet each time you renew your prescription, just in case anything has changed. Remember, this leaflet does not take the place of careful discussions with your doctor. You and your doctor should discuss your treatment with PREZISTA the first time you take your medicine and at regular checkups. You should remain under a doctors care when using PREZISTA and should not change or stop treatment without first talking with a doctor.
WHAT IS PREZISTA?
PREZISTA is an oral tablet used for the treatment of HIV (Human Immunodeficiency Virus) infection in adults. HIV is the virus that causes AIDS (Acquired Immune Deficiency Syndrome). PREZISTA is a type of anti-HIV drug called a protease (PRO-tee-ase) inhibitor.
HOW DOES PREZISTA WORK?
PREZISTA blocks HIV protease, an enzyme which is needed for HIV to multiply. When used with other anti-HIV medicines, PREZISTA may 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).
PREZISTA is always taken with and at the same time as 100 mg of ritonavir (NORVIR™), in combination with other anti-HIV medicines. PREZISTA should also be taken with food.
DOES PREZISTA CURE HIV OR AIDS?
PREZISTA does not cure HIV infection or AIDS. At present, there is no cure for HIV infection. People taking PREZISTA may still develop infections or other conditions associated with HIV infection. Because of this, it is very important for you to remain under the care of a doctor. Although PREZISTA is not a cure for HIV or AIDS, PREZISTA can help reduce your risks of getting illnesses associated with HIV infection (AIDS and opportunistic infection) and eventually dying from these conditions.
DOES PREZISTA REDUCE THE RISK OF PASSING HIV TO OTHERS?
PREZISTA does not reduce the risk of passing HIV to others through sexual contact, sharing needles, or being exposed to your blood. For your health and the health of others, it is important to always practice safer sex by using a latex or polyurethane condom or other barrier method to lower the chance of sexual contact with any body fluids such as semen, vaginal secretions, or blood. Never re-use or share needles.
Ask your doctor if you have any questions on how to prevent passing HIV to other people.
WHAT SHOULD I TELL MY DOCTOR BEFORE I TAKE PREZISTA?
Tell your doctor about all of your medical conditions, including if you:
· are allergic to sulfa medicines.
· have diabetes. In general, anti-HIV medicines, such as PREZISTA, might increase sugar levels in the blood.
· have liver problems.
· have hemophilia. Anti-HIV medicines, such as PREZISTA, might increase the risk of bleeding.
· are pregnant or planning to become pregnant. The effects of PREZISTA on pregnant women or their unborn babies are not known. You and your doctor will need to decide if taking PREZISTA is right for you. If you take PREZISTA while you are pregnant, talk to your doctor about how you can be included in the Antiretroviral Pregnancy Registry.
· are breastfeeding. Do not breastfeed if you are taking PREZISTA. You should not breastfeed if you have HIV because of the chance of passing HIV to your baby. Talk with your doctor about the best way to feed your baby.
WHO SHOULD NOT TAKE PREZISTA**?
Together with your doctor, you need to decide whether taking PREZISTA is right for you.
Do not take PREZISTA if you:
· are allergic to darunavir or any of the other ingredients in PREZISTA
· are allergic to ritonavir (NORVIR™)
· take any of the following types of medicines because you could experience serious side effects:
| Type of Drug | Examples of Generic Names (Brand Names) |
| Antihistamines (to treat allergy symptoms) |
astemizole (Hismanal™) terfenadine (Seldane™) |
| Ergot Derivatives (to treat migraine and headaches) |
dihydroergotamine (D.H.E. 45™, Migranal™) ergonovine ergotamine (Wigraine™, Ergostat™, Cafergot™, Ergomar™) methylergonovine |
| Gastrointestinal Motility Agent (to treat some digestive conditions) |
cisapride (Propulsid™) |
| Neuroleptic (to treat psychiatric conditions) |
pimozide (Orap™) |
| Sedative/hypnotics (to treat trouble with sleeping and/or anxiety) |
midazolam (Versed™) triazolam (Halcion™) |
CAN PREZISTA BE TAKEN WITH OTHER MEDICATIONS?
Tell your doctor about all the medicines you take including prescription and nonprescription medicines, vitamins, and herbal supplements, including St. Johns wort (Hypericum perforatum). PREZISTA and many other medicines can interact. Sometimes serious side effects will happen if PREZISTA is taken with certain other medicines.
Tell your doctor if you are taking estrogen-based contraceptives. PREZISTA might reduce the effectiveness of estrogen-based contraceptives. You must take additional precautions for birth control such as a condom.
Tell your doctor if you take other anti-HIV medicines. PREZISTA can be combined with some other anti-HIV medicines while other combinations are not recommended.
Tell your doctor if you are taking any of the following medicines:
| Type of Drug | Examples of Generic Names (Brand Names) |
| Antiarrhythmics (to treat abnormal heart rhythms) |
bepridil (Vascor™) lidocaine (Lidoderm™) quinidine amiodarone (Cordarone™) |
| Anticoagulants (to prevent the clotting of red blood cells called platelets) |
warfarin (Coumadin™) |
| Anticonvulsants (to treat epilepsy and prevent seizures) |
carbamazepine (Tegretol™, Carbatrol™) phenobarbital phenytoin (Dilantin™, Phenytek™) |
| Antidepressants | trazodone (Desyrel™) |
| Anti-infectives (to treat bacterial infections) |
clarithromycin (Biaxin™) |
| Antifungals (to treat fungal infections) |
ketoconazole (Nizoral™) itraconazole (Sporanox™) voriconazole (Vfend™) |
| Antimycobacterials (to treat bacterial infections) |
rifabutin (Mycobutin™) rifampin (Rifadin™, Rifater™, Rifamate™) |
| Calcium Channel Blockers (to treat heart disease) |
felodipine (Plendil™) nifedipine (Adalat™) nicardipine (Cardene™) |
| Corticosteroids (to treat inflammation or asthma) |
dexamethasone (Decadron™) fluticasone propionate (Advair Diskus™, Cutivate™, Flonase™, Flovent Diskus™) |
| HMG-CoA Reductase Inhibitors (to lower cholesterol levels) |
atorvastatin (Lipitor™) lovastatin (Mevacor™) pravastatin (Pravachol™) simvastatin (Zocor™) |
| Immunosuppressants (to prevent organ transplant rejection) |
cyclosporine (Sandimmune™, Neoral™) tacrolimus (Prograf™) sirolimus (Rapamune™) |
| Narcotic Analgesics | methadone |
| PDE-5 Inhibitors (to treat erectile dysfunction) |
sildenafil (Viagra™) vardenafil (Levitra™) tadalafil (Cialis™) |
| Selective Serotonin Reuptake Inhibitors (SSRIs) (to treat depression, anxiety, or panic disorder) |
paroxetine (Paxil™) sertraline (Zoloft™) |
Tell your doctor if you are taking any medicines that you obtained without a prescription.
This is not a complete list of medicines that you should tell your doctor that you are taking. Know and keep track of all the medicines you take and have a list of them with you. Show this list to all of your doctors and pharmacists any time you get a new medicine. Both your doctor and your pharmacist can tell you if you can take these other medicines with PREZISTA. Do not start any new medicines while you are taking PREZISTA without first talking with your doctor or pharmacist. You can ask your doctor or pharmacist for a list of medicines that can interact with PREZISTA.
HOW SHOULD I TAKE PREZISTA?
Take PREZISTA tablets every day exactly as prescribed by your doctor. You must take ritonavir (NORVIR™) at the same time as PREZISTA. The usual dose is 600 mg (two 300 mg tablets) of PREZISTA, together with 100 mg (one 100 mg capsule) of ritonavir (NORVIR™), twice daily every day. It may be easier to remember to take PREZISTA and ritonavir (NORVIR™) if you take them 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. The type of food is not important. Swallow the whole tablets with a drink such as water or milk. Do not chew the tablets.
Continue taking PREZISTA and ritonavir (NORVIR™) unless your doctor tells you to stop. Take the exact amount of PREZISTA and ritonavir (NORVIR™) that your doctor tells you to take, right from the very start. To help make sure you will benefit from PREZISTA and ritonavir (NORVIR™), you must not skip doses or interrupt therapy. If you dont take PREZISTA and ritonavir (NORVIR™) as prescribed, the beneficial effects of PREZISTA and ritonavir (NORVIR™) may be reduced or even lost.
If you miss a dose of PREZISTA or ritonavir (NORVIR™) by more than 6 hours, wait and then take the next dose of PREZISTA and ritonavir (NORVIR™) at the regularly scheduled time. If you miss a dose of PREZISTA or ritonavir (NORVIR™) by less than 6 hours, take your missed dose of PREZISTA and ritonavir (NORVIR™) immediately. Then take your next dose of PREZISTA and ritonavir (NORVIR™) at the regularly scheduled time.
You should always take PREZISTA and ritonavir (NORVIR™) together with food.
If a dose of PREZISTA or ritonavir (NORVIR™) is skipped, do not double the next dose. Do not take more or less than your prescribed dose of PREZISTA or ritonavir (NORVIR™) at any one time.
WHAT ARE THE POSSIBLE SIDE EFFECTS OF PREZISTA?
Like all prescription drugs, PREZISTA can cause side effects. The following is not a complete list of side effects reported with PREZISTA when taken either alone or with other anti-HIV medicines. Do not rely on this leaflet alone for information about side effects. Your doctor can discuss with you a more complete list of side effects.
Mild to moderate rash has been reported in 7% of subjects receiving PREZISTA. In some patients, PREZISTA has been reported to cause a severe or life-threatening rash. Contact your healthcare provider if you develop a rash. Your healthcare provider will advise you whether your symptoms can be managed on therapy or whether PREZISTA should be stopped.
As with other protease inhibitors, PREZISTA may cause side effects, including:
· high blood sugar (hyperglycemia) and diabetes. This can happen in patients taking PREZISTA or other protease inhibitor medicines. Some patients have diabetes before starting treatment with PREZISTA which gets worse. Some patients get diabetes during treatment with PREZISTA. Some patients will need changes in their diabetes medicine. Some patients may need new diabetes medicine.
· increased bleeding in patients with hemophilia. This may happen in patients taking PREZISTA as it has been reported with other protease inhibitor medicines.
· changes in body fat. These changes can happen in patients taking anti-HIV medicines. The changes may include an increased amount of fat in the upper back and neck, breast, and around the back, chest, and stomach area. Loss of fat from the legs, arms, and face may also happen. The exact cause and long-term health effects of these conditions are not known.
· immune reconstitution syndrome. In some patients with advanced HIV infection (AIDS) and a history of opportunistic infection, signs and symptoms of inflammation from previous infections may occur soon after anti-HIV treatment is started. It is believed that these symptoms are due to an improvement in the bodys immune response, enabling the body to fight infections that may have been present with no obvious symptoms.
The most common side effects include diarrhea, nausea, headache, and common cold.
Tell your doctor promptly about these or any other unusual symptoms. If the condition persists or worsens, seek medical attention.
HOW SHOULD I STORE PREZISTA TABLETS?
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. Ask your doctor or pharmacist if you have any questions about storing your tablets.
This medication is prescribed for your particular condition. Do not use it for any other condition or give it to anybody else. Keep PREZISTA and all of your medicines out of the reach of children. If you suspect that more than the prescribed dose of this medicine has been taken, contact your local poison control center or emergency room immediately.
This leaflet provides a summary of information about PREZISTA. If you have any questions or concerns about either PREZISTA or HIV, talk to your doctor.
For additional information, you may also call Tibotec Therapeutics at 1-800-325-7504.
* Trademark of Tibotec, Inc.,COPYRIGHT ©2006 Tibotec, Inc.,All rights reserved
** The brands listed are the registered trademarks of their respective owners and are not trademarks of Tibotec, Inc.
Prezista Interactions
PREZISTA and ritonavir are both inhibitors of CYP3A. Co-administration of PREZISTA and ritonavir with drugs that are primarily metabolized by CYP3A may result in increased plasma concentrations of such drugs, which could increase or prolong their therapeutic effect and adverse events.
Drugs that are contraindicated and not recommended for co-administration with PREZISTA/rtv are included in Table 10. These recommendations are based on either drug interaction studies or predicted interactions due to the expected magnitude of interaction and potential for serious events or loss of efficacy.
|
Table 10: Drugs That Should Not Be Co-administered With PREZISTA/rtv |
|
| Drug Class: Drug Name | Clinical Comment |
| Anticonvulsants: carbamazepine, phenobarbital, phenytoin |
Carbamazepine, phenobarbital and phenytoin are inducers of CYP450 enzymes. PREZISTA/rtv should not be used in combination with phenobarbital, phenytoin, or carbamazepine as co-administration may cause significant decreases in darunavir plasma concentrations. This may result in loss of therapeutic effect to PREZISTA. |
| Antihistamines: astemizole, terfenadine |
CONTRAINDICATED due to potential for serious and/or life-threatening reactions such as cardiac arrhythmias. |
| Antimycobacterial: rifampin |
Rifampin is a potent inducer of CYP450 metabolism. PREZISTA/rtv should not be used in combination with rifampin, as this may cause significant decreases in darunavir plasma concentrations. This may result in loss ofmtherapeutic effect to PREZISTA. |
| Ergot Derivatives: dihydroergotamine, ergonovine, ergotamine, methylergonovine |
CONTRAINDICATED due to potential for serious and/or life-threatening reactions such as acute ergot toxicity characterized by peripheral vasospasm and ischemia of the extremities and other tissues. |
| Gastrointestinal Motility Agent: cisapride |
CONTRAINDICATED due to potential for serious and/or life-threatening reactions such as cardiac arrhythmias. |
| Herbal Products: St. John's wort (Hypericum perforatum) |
PREZISTA/rtv should not be used concomitantly with products containing St. Johns wort (Hypericum perforatum) because co-administration may cause significant decreases in darunavir plasma concentrations. This may result in loss of therapeutic effect to PREZISTA. |
| HMG-CoA Reductase Inhibitors: lovastatin, simvastatin |
Potential for serious reactions such as risk of myopathy including rhabdomyolysis. |
| For dosing recommendation regarding atorvastatin and pravastatin, see Table 11: Established and Other Potentially Significant Drug Interactions: Alterations in Dose or Regimen May Be Recommended Based on Drug Interaction Studies or Predicted Interaction. | |
| Neuroleptic: pimozide |
CONTRAINDICATED due to the potential for serious and/or life-threatening reactions such as cardiac arrhythmias. |
| Sedative/Hypnotics: midazolam, triazolam |
CONTRAINDICATED due to potential for serious and/or life-threatening reactions such as prolonged or increased sedation or respiratory depression. |
| Table 11: Established and Other Potentially Significant Drug Interactions: Alterations in Dose or Regimen May Be Recommended Based on Drug Interaction Studies or Predicted Interaction | ||
| Concomitant Drug Class: Drug Name | Effect on Concentration of Darunavir or Concomitant Drug | Clinical Comment |
| HIV-Antiviral Agents: Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs) | ||
| Efavirenz | ¯darunavir efavirenz |
Co-administration of darunavir/rtv and efavirenz decreased darunavir AUC by 13% and Cmin by 31%. The AUC of efavirenz increased by 21% and Cmin increased by 17%. The clinical significance has not been established. The combination of PREZISTA/rtv and efavirenz should be used with caution. |
| Nevirapine | «darunavir nevirapine |
PREZISTA/rtv and nevirapine can be co-administered without any dose adjustments. |
| HIV-Antiviral Agents: Nucleoside Reverse Transcriptase Inhibitors (NRTIs) | ||
| Didanosine | It is recommended that didanosine be administered on an empty stomach. Therefore, didanosine should be administered one hour before or two hours after PREZISTA/rtv (which are administered with food). | |
| Tenofovir Disoproxil Fumarate | «darunavir tenofovir |
PREZISTA/rtv andmtenofovir disoproxil fumarate can be co-administered without any dose adjustments. |
| HIV-Antiviral Agents: HIV-Protease Inhibitors (PIs) | ||
| Atazanavir(The reference regimen for atazanavir was atazanavir/ritonavir 300/100 mg q.d.) | «darunavir «atazanavir |
PREZISTA/rtv and atazanavir (300 mg q.d.) can be co-administered. |
| Indinavir (The reference regimen for indinavir was indinavir/ritonavir 800/100 mg b.i.d.) | darunavir indinavir |
The appropriate dose of indinavir in combination with PREZISTA/rtv has not been established. |
| Lopinavir/ritonavir | ¯darunavir lopinavir |
Due to decrease in the exposure (AUC) of darunavir by 53%, appropriate doses of the combination have not been established. Hence, it is not recommended to co-administer lopinavir/ritonavir and PREZISTA, with or without an additional low-dose of ritonavir. |
| Saquinavir | ¯darunavir «saquinavir |
Due to a decrease in the exposure (AUC) of darunavir by 26%, appropriate doses of the combination have not been established. Hence, it is not recommended to co-administer saquinavir and PREZISTA, with or without low-dose ritonavir. |
| Other Agents | ||
| Antiarrhythmics: bepridil, lidocaine (systemic), quinidine, amiodarone |
antiarrhythmics | Concentrations of bepridil, lidocaine, quinidine and amiodarone may be increased when co-administered with PREZISTA/rtv. Caution is warranted and therapeutic concentration monitoring, if available, is recommended for antiarrhythmics when co-administered with PREZISTA/rtv. |
| Anticoagulant: warfarin |
¯warfarin «darunavir |
Warfarin concentrations may be affected when co-administered with PREZISTA/rtv. It is recommended that the international normalized ratio (INR) be monitored when warfarin is combined with PREZISTA/rtv. |
| Antidepressant: trazodone | trazodone | Concomitant use of trazodone and PREZISTA/rtv may increase plasma concentrations of trazodone. Adverse events of nausea, dizziness, hypotension and syncope have been observed following co-administration of trazodone and ritonavir. If trazodone is used with a CYP3A inhibitor such as PREZISTA/rtv, the combination should be used with caution and a lower dose of trazodone should be considered. |
| Anti-infective: clarithromycin | clarithromycin |
No dose adjustment of darunavir or clarithromycin is required for patients with normal renal function. For patients with renal impairment, the following dose adjustments should be considered:
· For subjects with CLcr of 30-60 mL/min, the dose of clarithromycin should be reduced by 50%. |
| Antifungals: ketoconazole, itraconazole, voriconazole |
ketoconazole darunavir itraconazole (not studied) ¯ voriconazole (not studied) |
Ketoconazole and itraconazole are potent inhibitors as well as substrates of CYP3A. Concomitant systemic use of ketoconazole, itraconazole, and darunavir/ritonavir may increase plasma concentration of darunavir. Plasma concentrations of ketoconazole or itraconazole may be increased in the presence of darunavir/ritonavir. When co-administration is required, the daily dose of ketoconazole or itraconazole should not exceed 200 mg. Co-administration of voriconazole with darunavir/ritonavir has not been studied. Administration ofvoriconazole with ritonavir (100 mg twice daily) decreased the AUC of voriconazole by an average of 39%. Voriconazole should not be administered to patients receiving darunavir/ritonavir unless an assessment of the benefit/risk ratio justifies the use of voriconazole. |
| Antimycobacterial: rifabutin | rifabutin ¯darunavir | Rifabutin is an inducer and substrate of CYP450 enzymes. Concomitant use of rifabutin and darunavir in the presence of ritonavir is expected to increase rifabutin plasma concentrations and decrease darunavir plasma concentrations. When indicated, it is recommended to administer rifabutin at a dosage of 150 mg once every other day when co-administered with PREZISTA/rtv. |
| Calcium Channel Blockers: felodipine, nifedipine, nicardipine | calcium channel blockers | Plasma concentrations of calcium channel blockers (e.g. felodipine, nifedipine, nicardipine) may increase when PREZISTA/rtv are co-administered. Caution is warranted and clinical monitoring of patients is recommended. |
| Corticosteroid: dexamethasone fluticasone propionate | ¯darunavir fluticasone propionate |
Use with caution. Systemic dexamethasone induces CYP3A and can thereby decrease darunavir plasma concentrations. This may result in loss of therapeutic effect to PREZISTA. Concomitant use of inhaled fluticasone propionate and PREZISTA/rtv may increase plasma concentrations of fluticasone propionate. Alternatives should be considered, particularly for long term use. |
| HMG-CoA Reductase Inhibitors: atorvastatin, pravastatin |
atorvastatin pravastatin |
When atorvastatin and PREZISTA/rtv is co-administered, it is recommended to start with the lowest possible dose of atorvastatin with careful monitoring. A gradual dose increase of atorvastatin may be considered based on the clinical response. When PREZISTA/rtv was administered with pravastatin, the mean increase in pravastatin AUC was 81%. However, pravastatin AUC increased by up to 5-fold in some subjects. The mechanism of the interaction is not known. |
| H2-Receptor Antagonists and Proton Pump Inhibitors: omeprazole, ranitidine | « darunavir | PREZISTA/rtv can be co-administered with H2-receptor antagonists and proton pump inhibitors without any dose adjustments. |
| Immunosuppressants: cyclosporine, tacrolimus, sirolimus | immunosuppressants | Plasma concentrations of cyclosporine, tacrolimus or sirolimus may be increased when co-administered with PREZISTA/rtv. Therapeutic concentration monitoring of the immunosuppressive agent is recommended for immunosuppressant agents when co-administered with PREZISTA/rtv. |
| Narcotic Analgesic: methadone | ¯methadone | When methadone is co-administered with PREZISTA/rtv, patients should be monitored for opiate abstinence syndrome, as ritonavir is known to induce the metabolism of methadone, leading to a decrease in its plasma concentrations. An increase in methadone dosage may be considered based on the clinical response. |
| Oral Contraceptives/estrogen: ethinyl estradiol norethindrone |
¯ethinyl estradiol ¯norethindrone |
Plasma concentrations of ethinyl estradiol may be decreased due to induction of its metabolism by ritonavir. Alternative or additional contraceptive measures should be used when estrogen-based contraceptives are co-administered with PREZISTA/rtv. |
| PDE-5 inhibitors: sildenafil, vardenafil, tadalafil | PDE-5 inhibitors | Concomitant use of PDE-5 inhibitors with PREZISTA/rtv should be done with caution. If concomitant use of PREZISTA/rtv with sildenafil, vardenafil, or tadalafil is required, sildenafil at a single dose not exceeding 25 mg in 48 hours, vardenafil at a single dose not exceeding 2.5 mg dose in 72 hours, or tadalafil at a single dose not exceeding 10 mg dose in 72 hours, is recommended. |
| Selective Serotonin Reuptake Inhibitors (SSRIs): sertraline, paroxetine | «darunavir ¯sertraline ¯paroxetine |
If sertraline or paroxetine is co-administered with PREZISTA/rtv, the recommended approach is a careful dose titration of the SSRI based on a clinical assessment of antidepressant response. In addition, patients on a stable dose of sertraline or paroxetine who start treatment with PREZISTA/rtv should be monitored for antidepressant response. |
Other NRTIs:
Based on the different elimination pathways of the other NRTIs (zidovudine, zalcitabine, emtricitabine, stavudine, lamivudine and abacavir) that are primarily renally excreted, no drug interactions are expected for these drugs and PREZISTA/rtv.
Other protease inhibitors:
The co-administration of PREZISTA/rtv and PIs other than lopinavir/ritonavir, saquinavir, atazanavir, and indinavir has not been studied. Therefore, such co-administration is not recommended.
Prezista Contraindications
PREZISTA is contraindicated in patients with known hypersensitivity to any of the ingredients of the product.
Co-administration of PREZISTA/rtv is contraindicated with drugs that are highly dependent on CYP3A for clearance and for which elevated plasma concentrations are associated with serious and/or life-threatening events (narrow therapeutic index). These drugs are listed in the table below.
|
Drugs That Are Contraindicated With PREZISTA/rtv |
|
| Drug Class | Drugs Within Class That Are Contraindicated With PREZISTA/rtv |
| Antihistamines | Astemizole, Terfenadine |
| Ergot Derivatives | Dihydroergotamine, Ergonovine, Ergotamine, Methylergonovine |
| GI Motility Agent | Cisapride |
| Neuroleptic | Pimozide |
| Sedative/hypnotics | Midazolam, Triazolam |
Due to the need for co-administration of PREZISTA with 100 mg of ritonavir, please refer to ritonavir prescribing information for a description of ritonavir contraindications.
Additional information about Prezista
Prezista Indication: Prezista, co-administered with 100 mg ritonavir, and with other antiretroviral agents, is indicated for the treatment of human immunodeficiency virus (HIV) infection in antiretroviral treatment-experienced adult patients, such as those with HIV-1 strains resistant to more than one protease inhibitor.
Mechanism Of Action: Prezista is an inhibitor of the HIV-1 protease. It selectively inhibits the cleavage of HIV encoded Gag-Pol polyproteins in infected cells, thereby preventing the formation of mature virus particles.
Drug Interactions: Clarithromycin Increased levels of clarithromycin
Lidocaine Possible increase in lidocaine levels
Saquinavir Decreased levels of darunavir
Lopinavir Decreased levels of darunavir
Food Interactions: Take with food - better absorption (+30%).
Generic Name: Darunavir
Synonyms: Darunavirum [INN-latin]; TMC-114; UIC-94017; AIDS073035
Drug Category: Antiviral Agents; HIV Protease Inhibitors
Drug Type: Small Molecule; Approved
Other Brand Names containing Darunavir: Prezista;
Absorption: The absolute oral bioavailability of a single 600 mg dose of darunavir alone and after co-administration with 100 mg ritonavir twice daily was 37% and 82%, respectively.
Toxicity (Overdose): Not Available
Protein Binding: Darunavir is approximately 95% bound to plasma proteins. Darunavir binds primarily to plasma alpha 1-acid glycoprotein (AAG).
Biotransformation: Hepatic. Darunavir is extensively metabolized by CYP enzymes, primarily by CYP3A.
Half Life: The terminal elimination half-life of darunavir was approximately 15 hours when combined with ritonavir.
Dosage Forms of Prezista: Tablet Oral
Chemical IUPAC Name: [(3R,3aS,6aR)-2,3,3a,4,5,6a-hexahydrofuro[5,4-b]furan-3-yl] N-[(2S,3R)-4-[(4-aminophenyl)sulfonyl-(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]carbamate
Chemical Formula: C27H37N3O7S
Darunavir on Wikipedia: https://en.wikipedia.org/wiki/Darunavir
Organisms Affected: Human Immunodeficiency Virus