Lopinavir Research Paper

2.2 DRUG PROFILE

2.2.1 Drug profile of Lopinavir:

Lopinavir is an antiretroviral drug and it is in the class of the protease inhibitor. It is a second generation HIV-1 protease inhibitor. For HIV infections, Lopinavir is used as a fixed-dose combination with another protease inhibitor. US Food and Drug Administration (FDA) first approved Lopinavir on 15 September 2000. Lopinavir inhibits the HIV viral protease enzyme, thereby preventing cleavage of the gag-pol polyproteins. Therefore, this results in immature, noninfectious viral particles. Kaletra was developed in a combination of lopinavir and ritonavir for clinical use and recommended dosage is 400/100mg taken twice daily with food.

a) Structure of Lopinavir b) Chemical Name / IUPAC Name:

(2S)-N-[(2S,4S,5S)-5-[2-(2,6-dimethylphenoxy)acetamido]-4-hydroxy-1,6-diphenylhexan-2-yl]-3-methyl-2-(2-oxo-1,3-diazinan-1-yl)butanamide

c) Molecular Formula: C37H48N4O5.

d) Molecular Weight: 628.814 g/mol.

e) Description: white to light tan powder

f) Melting point: 124 °C-127 °C

g) Solubility: Practically insoluble in water, freely soluble in methanol and ethanol; soluble in isopropanol. h) Route of administration: Oral

i) Excretion: Mostly fecal

j)

It is used for the treatment of HIV infection by reducing the amount of HIV in the body. Food and Drug Administration approved Emtricitabine on 2 July 2003. It is an analogue of cytidine. Emtricitabine inhibits reverse transcriptase enzyme, that copies HIV RNA into viral DNA. Nucleoside reverse transcriptase inhibitors block this reverse transcription. Thus, interrupting reverse transcription stops HIV replication and prevents HIV from infecting human cells. Market availability of Emtricitabine in the name of Emtriva. It is also available in the name of Truvada with the combination of Tenofovir. Emtricitabine recommended dosage is 200 mg taken once