MYCOBUTIN- rifabutin capsule

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

RIFABUTIN (UNII: 1W306TDA6S) (RIFABUTIN - UNII:1W306TDA6S)

Available from:

Physicians Total Care, Inc.

INN (International Name):

RIFABUTIN

Composition:

RIFABUTIN 150 mg

Administration route:

ORAL

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

MYCOBUTIN Capsules are indicated for the prevention of disseminated Mycobacterium avium complex (MAC) disease in patients with advanced HIV infection. MYCOBUTIN Capsules are contraindicated in patients who have had clinically significant hypersensitivity to rifabutin or to any other rifamycins.

Product summary:

MYCOBUTIN Capsules (rifabutin capsules, USP) are supplied as hard gelatin capsules having an opaque red-brown cap and body, imprinted with MYCOBUTIN/PHARMACIA & UPJOHN in white ink, each containing 150 mg of rifabutin, USP. MYCOBUTIN is available as follows: Keep tightly closed and dispense in a tight container as defined in the USP. Store at 25°C (77°F); excursions permitted to 15°–30°C (59°–86°F) [see USP Controlled Room Temperature].

Authorization status:

New Drug Application

Summary of Product characteristics

MYCOBUTIN - RIFABUTIN CAPSULE
PHYSICIANS TOTAL CARE, INC.
----------
MYCOBUTIN
RIFABUTIN CAPSULES, USP
DESCRIPTION
MYCOBUTIN Capsules contain the antimycobacterial agent rifabutin,
which is a semisynthetic
ansamycin antibiotic derived from rifamycin S. MYCOBUTIN Capsules for
oral administration contain
150 mg of rifabutin, USP, per capsule, along with the inactive
ingredients microcrystalline cellulose,
magnesium stearate, red iron oxide, silica gel, sodium lauryl sulfate,
titanium dioxide, and edible white
ink.
The chemical name for rifabutin is
1',4-didehydro-1-deoxy-1,4-dihydro-5'-(2-methylpropyl)-1-
oxorifamycin XIV (Chemical Abstracts Service, 9th Collective Index) or
(9_S_, 12_E_, 14_S_, 15_R_, 16_S_, 17_R_,
18_R_, 19_R_, 20_S_, 21_S_, 22_E_,
24_Z_)-6,16,18,20-tetrahydroxy-1'-isobutyl-14-methoxy-7,9,15,17,19,21,25-
heptamethyl-spiro
[9,4-(epoxypentadeca[1,11,13]trienimino)-2_H_-furo[2',3':7,8]naphth[1,2-d]
imidazole-
2,4'-piperidine]-5,10,26-(3_H_,9_H_)-trione-16-acetate. Rifabutin has
a molecular formula of
C
H N O , a molecular weight of 847.02 and the following structure:
Rifabutin is a red-violet powder soluble in chloroform and methanol,
sparingly soluble in ethanol, and
very slightly soluble in water (0.19 mg/mL). Its log P value (the base
10 logarithm of the partition
coefficient between n-octanol and water) is 3.2 (n-octanol/water).
CLINICAL PHARMACOLOGY
PHARMACOKINETICS
Absorption
Following a single oral dose of 300 mg to nine healthy adult
volunteers, rifabutin was readily absorbed
from the gastrointestinal tract with mean (±SD) peak plasma levels (C
) of 375 (±267) ng/mL (range:
®
46
62
4
11
max
141 to 1033 ng/mL) attained in 3.3 (±0.9) hours (T
range: 2 to 4 hours). Absolute bioavailability
assessed in five HIV-positive patients, who received both oral and
intravenous doses, averaged 20%.
Total recovery of radioactivity in the urine indicates that at least
53% of the orally administered
rifabutin dose is absorbed from the gastrointestinal tract. The
bioavailability of rifabutin from the
caps