What is Atazanavir:
Atazanavir sulfate is an azapeptide inhibitor of HIV-1 protease. The compound selectively inhibits the virus specific processing of viral gag-pol proteins in HIV-1 infected cells, thus preventing formation of mature virions and infection of other cells.
Atazanavir 100mg & Atazanavir 300mg capsules are proposed for inclusion on the WHO Model List of essential medicines for the treatment of HIV infection.
Atazanavir has a low pill burden and there is evidence of beneficial effects on lipid levels which offers advantages for adherence and longer-term treatment. In this way, the inclusion of this medication (atazanavir) on the WHO Model Lists of Essential Medicines is sought.
Side effects of Atazanavir:
The following list of side effects is not complete. In case of any new or continuing signs and symptoms immediately contact your healthcare provider or click here. If you are wondering and have questions about side effects, talk to your healthcare team.
Your doctor/healthcare provider team may be able to help you in order to manage these side effects. Common side effects include:
- Rash
- Fever
- Nausea
- Vomiting
- Insomnia
- Dizziness
- Diarrhea
- Jaundice
- Headache
- Depression
- Muscle pain
- Abdominal pain
- Peripheral Neurologic Symptoms
- Raised Bilirubin Levels in the blood with atazanavir, but can sometimes lead to jaundice.
Atazanavir Dosage:
Atazanavir capsules must be taken with food. The recommended oral dosage of Atazanavir depends on the treatment history of the patient and the use of other coadministered drugs. When atazanavir coadministered with any H2-receptor antagonists or proton-pump inhibitors, dose separation may be required.
Atazanavir without ritonavir is not recommended for treatment-experienced adult or pediatric patients with prior virologic failure.
How Atazanavir is best medication for HIV:
- This medication binds to the active site HIV protease and prevents it from cleaving the pro-form of viral proteins into the working machinery of the virus.
- In the case of not working of HIV protease enzyme, the virus is not infectious, and no mature virions are made.
- The azapeptide drug was developed and designed as an analog of the (PCS) peptide chain substrate that human immunodeficiency virus syndrome (HIV) protease would cleave normally into active viral proteins.
- Specifically, the atazanavir is a structural analog of the transition state during which the bond between a proline and phenylalanine is broken.
- In humans there are no any sort of enzymes that break bonds between phenylalanine and proline, so this drug will not target human enzymes.
- No harm of Atazanavir has been found among pregnant women who were taking this medication. It is the most recommended and best HIV medication to use in pregnant women who have not taken an HIV medication before.
- Atazanavir was not associated and also not responsible with any sort of birth defects among over 2,400 live births observed. Atazanavir is known for the better cholesterol profile and specified that it is a safe option during pregnancy.
Mechanism of Action: Atazanavir mainly forms an inhibitor-enzyme complex with HIV protease preventing the normal maturation process of Human Immunodeficiency Virus (HIV) and formation of mature infectious virions.
Mechanism of Resistance: Higher levels of protease inhibitor resistance result from the accumulation of multiple protease inhibitor-resistance mutations. The many mechanisms of resistance include reduced binding affinity between the inhibitor and the protease enzyme, alterations in enzyme catalysis, effects on dimer stability, alterations in inhibitor binding kinetics, and re-shaping of the active site.
Active & inactive Pharmaceutical Ingredients:
Capsules, for oral administration in strengths containing the equivalent of 100 mg, or
300 mg of atazanavir as atazanavir sulfate and the following inactive ingredients: crospovidone, lactose monohydrate, and magnesium stearate.
Dosage Forms and Strengths:
The medication comes in the form of capsules and the existing strengths are as follows:
- Atazanavir 100mg Capsule
- Atazanavir 150mg Capsule
- Atazanavir 200mg Capsule
- Atazanavir 300mg Capsule
Contraindications/Warnings/ Precautions: Atazanavir is basically contraindicated with: midazolam, triazolam, dihydroergotamine, ergotamine, ergonovine, methylergonovine, cisapride (no longer marketed in the United States) and pimozide.
Drug Interactions: Atazanavir is a known substrate and inhibitor of CYP3A4 in vitro. Therefore, medications that are also metabolized by CYP3A4 may interact with atazanavir.
