Aptivus
Aptivus Uses, Dosage, Side Effects, Food Interaction and all others data.
Aptivus is a sulfonamide-containing dyhydropyrone and a nonpeptidic protease inhibitor that targets the HIV protease. Aptivus and ritonavir are coadministered to treat HIV.
Aptivus is a non-peptidic protease inhibitor (PI) of HIV. Protease inhibitors block the part of HIV called protease. HIV-1 protease is an enzyme required for the proteolytic cleavage of the viral polyprotein precursors into the individual functional proteins found in infectious HIV-1. Nelfinavir binds to the protease active site and inhibits the activity of the enzyme. This inhibition prevents cleavage of the viral polyproteins resulting in the formation of immature non-infectious viral particles. Protease inhibitors are almost always used in combination with at least two other anti-HIV drugs.
| Trade Name | Aptivus |
| Availability | Prescription only |
| Generic | Tipranavir |
| Tipranavir Other Names | Tipranavir |
| Related Drugs | Biktarvy, Truvada, tenofovir, ritonavir, Complera, Atripla, Stribild |
| Weight | 250mg, 100mg/ml, |
| Type | Solution, Oral Capsule, Oral Solution |
| Formula | C31H33F3N2O5S |
| Weight | Average: 602.664 Monoisotopic: 602.206227481 |
| Protein binding | Extensive (> 99.9%), to both human serum albumin and α-1-acid glycoprotein. |
| Groups | Approved, Investigational |
| Therapeutic Class | |
| Manufacturer | Boehringer Ingelheim Limited |
| Available Country | Australia, Canada, United Kingdom, United States, France, Italy, Netherlands, Portugal, Spain, Switzerland, |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Aptivus is a protease inhibitor used to treat HIV-1 resistant to more than 1 protease inhibitor.
For combination antiretroviral treatment of HIV-1 infected adult patients with evidence of viral replication, who are highly treatment-experienced or have HIV-1 strains resistant to multiple protease inhibitors.
Aptivus is also used to associated treatment for these conditions: Human Immunodeficiency Virus Type 1 (HIV-1) Infection
How Aptivus works
Aptivus (TPV) is a non-peptidic HIV-1 protease inhibitor that inhibits the processing of the viral Gag and Gag-Pol polyproteins in HIV-1 infected cells, thus preventing formation of mature virions. Two mechanisms are suggested in regards to the potency of tipranavir: 1. Tipravanir may bind to the active site of the protease enzyme with fewer hydrogen bonds than peptidic protease inhibitors, which results in increased flexibility, allowing it to fit into the active site of the enzyme in viruses that have become resistance to other protease inhibitors. This also enables tipranavir to adjust to amino acid substitutions at the active site. 2. Aptivus's strong hydrogen bonding interaction with the amide backbone of the protease active site Asp30 may lead to its activity against resistant viruses.
Toxicity
Oral LD50 in rat is over 5,000 mg/kg. Side effects include thirst and hunger, unexplained weight loss, increased urination, fatigue, and dry, itchy skin.
Food Interaction
- Take with or without food. However, if taken with ritonavir tablets, tipranavir should be taken with food.
[Moderate] ADJUST DOSING INTERVAL: Food does not appear to substantially alter the pharmacokinetics of tipranavir.
When tipranavir capsules or oral solution was coadministered with ritonavir capsules at steady-state, no clinically significant changes in tipranavir peak plasma concentration (Cmax) and systemic exposure (AUC) were observed under fed conditions (500 to 682 kcal, 23% to 25% calories from fat) relative to fasted conditions.
The effect of food on tipranavir exposure during coadministration with ritonavir tablets has not been evaluated.
High-fat foods may enhance the gastrointestinal absorption of tipranavir.
In a multiple-dose study, administration of tipranavir capsules with a high-fat meal (868 kcal, 53% from fat, 31% from carbohydrates) increased the oral bioavailability of tipranavir by 31% compared to administration with toast and skimmed milk, but did not significantly affect tipranavir Cmax.
Thus, tipranavir may be safely taken with standard or high-fat meals.
MANAGEMENT: Aptivus coadministered with low-dose ritonavir should be taken with food to improve the gastrointestinal tolerability of ritonavir.
According to the product labeling, tipranavir coadministered with ritonavir capsules or solution can be taken with or without meals, whereas tipranavir coadministered with ritonavir tablets must be taken with meals.
Aptivus Cholesterol interaction
[Moderate] Hyperlipidemia has been observed in 10% of patients receiving ritonavir during clinical trials.
Increases of 30% to 40% from baseline have been reported for total cholesterol and 200% to 300% or more for triglycerides.
These effects have also been reported during postmarketing experience with other protease inhibitors (PIs) but may be the most dramatic with ritonavir.
The clinical significance of these elevations is unclear.
Severe hyperlipidemia is known to sometimes cause pancreatitis.
In addition, some patients have reportedly developed symptomatic atherosclerosis and coronary artery disease after initiating PI treatment.
Patients with preexisting hyperlipidemia may require closer monitoring during PI therapy, and adjustments made accordingly in their lipid-lowering regimen.
PI therapy should be administered cautiously in patients with coronary artery disease or a history of ischemic heart disease.
Aptivus Drug Interaction
Major: aspirin, heparinModerate: omeprazoleUnknown: azithromycin, loratadine / pseudoephedrine, sulfamethoxazole / trimethoprim, ubiquinone, copper gluconate, ethanol, glycerin, ibuprofen, arginine, levocarnitine, cysteine, lithium, bioflavonoids, vitamin a topical, oxycodone, bioflavonoids, tramadol
Aptivus Disease Interaction
Major: hemophilia, hepatotoxicityModerate: hyperglycemia, hyperlipidemia
Elimination Route
Absorption is limited, although no absolute quantification of absorption is available.
Half Life
5-6 hours
Innovators Monograph
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