HIV Protease Inhibitors.
Name: Farah nidal alashikID: 201610691
Acquired Immunodeficiency Syndrome (HIV) is a chronic condition that can lead to death due to HIV. HIV destroys your immune system and affects your body’s ability to resist pathogenic bacteria.
HIV is a sexually transmitted infection (STI). It can also be spread by contact with contaminated blood or from mother to son during pregnancy, delivery or breastfeeding. Without treatment, HIV may take years to weaken your immune system to the point of being infected with AIDS.
There is no cure for HIV / AIDS, but there are treatments that can significantly slow the development of the disease. These drugs have reduced AIDS deaths in many developed countries.
Non-nucleoside reverse transcriptase inhibitors (NNRTI): inhibiting the protein action needed for HIV to replicate itself. Examples include:
Molecular formula: C14H9ClF3NO3
low solubility and high permeability
plasma concentration tmax = 3-5 hrs
increase Cmax and AUC
By cytochrome C450 system
Molecular formula: C20H15BrN6O
low solubility and permeability ( lipid soluble)
plasma concentration tmax: 4 hrs
Steven Johnson syndrome
Molecular formula: C22H18N6
High oral bioavailability
Low soluble and high permeability
Decrease Cmax and AUC
Nucleoside reverse transcriptase inhibitors (NRTI):
They are defective copies of the basic building blocks that HIV needs to make copies of itself, used to prevent the HIV from replicating. Examples include:
Molecular formula: C14H18N6O
AUC = 0-12 hrs
Protein binding moderate approximately 50%
Molecular formula: C9H14N5O4P
Weakness and headache
Increase cholesterol in the blood
Molecular formula: C21H29N6O5P
Tmax= 1 hr post oral administration
Metabolism to tenofovir by cathepsin A in PBMCs and macrophages
And by carboxylesterase1 in hepatocytes