RESCRIPTOR delavirdine mesylate tablet

Ország: Egyesült Államok

Nyelv: angol

Forrás: NLM (National Library of Medicine)

Aktív összetevők:

DELAVIRDINE MESYLATE (UNII: 421105KRQE) (DELAVIRDINE - UNII:DOL5F9JD3E)

Beszerezhető a:

KAISER FOUNDATION HOSPITALS

INN (nemzetközi neve):

DELAVIRDINE MESYLATE

Összetétel:

DELAVIRDINE MESYLATE 200 mg

Recept típusa:

PRESCRIPTION DRUG

Engedélyezési státusz:

New Drug Application

Termékjellemzők

RESCRIPTOR- DELAVIRDINE MESYLATE TABLET
KAISER FOUNDATION HOSPITALS
----------
RESCRIPTOR
(DELAVIRDINE MESYLATE) TABLETS
DESCRIPTION
RESCRIPTOR Tablets contain delavirdine mesylate, a synthetic
non-nucleoside reverse transcriptase
inhibitor (NNRTI) of the human immunodeficiency virus type 1 (HIV-1).
The chemical name of
delavirdine mesylate is piperazine, 1-[3-[(1-methyl-ethyl)amino]-2-
pyridinyl]-4-[[5-
[(methylsulfonyl)amino]-1H-indol-2-yl]carbonyl]-,
monomethanesulfonate. Its molecular formula is
C
H N O S•CH O S, and its molecular weight is 552.68. The structural
formula is:
Delavirdine mesylate is an odorless white-to-tan crystalline powder.
The aqueous solubility of
delavirdine free base at 23°C is 2,942 mcg/mL at pH 1.0, 295 mcg/mL
at pH 2.0, and 0.81 mcg/mL at pH
7.4.
Each RESCRIPTOR Tablet, for oral administration, contains 200 mg of
delavirdine mesylate
(henceforth referred to as delavirdine). Inactive ingredients consist
of carnauba wax, colloidal silicon
dioxide, croscarmellose sodium, lactose, magnesium stearate, and
microcrystalline cellulose. In
addition, the 200-mg tablet contains hypromellose, Opadry White
YS-1-18202-A, and Pharmaceutical
Ink Black.
MICROBIOLOGY
MECHANISM OF ACTION
Delavirdine is an NNRTI of HIV-1. Delavirdine binds directly to
reverse transcriptase (RT) and blocks
RNA-dependent and DNA-dependent DNA polymerase activities. Delavirdine
does not compete with
template:primer or deoxynucleoside triphosphates. HIV-2 RT and human
cellular DNA polymerases α,
γ, or δ are not inhibited by delavirdine. In addition, HIV-1 group
O, a group of highly divergent strains
that are uncommon in North America, may not be inhibited by
delavirdine.
_IN VITRO HIV-1 SUSCEPTIBILITY: _In vitro anti-HIV-1 activity of
delavirdine was assessed by infecting cell
lines of lymphoblastic and monocytic origin and peripheral blood
lymphocytes with laboratory and
clinical isolates of HIV-1. IC
and IC
values (50% and 90% inhibitory concentrations) for laboratory
isolates (n = 5) ranged from 0.005 to 0.030 μM