MYCOBUTIN- rifabutin capsule

Land: USA

Sprog: engelsk

Kilde: NLM (National Library of Medicine)

Aktiv bestanddel:

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

Tilgængelig fra:

Department of State Health Services, Pharmacy Branch

INN (International Name):

RIFABUTIN

Sammensætning:

RIFABUTIN 150 mg

Indgivelsesvej:

ORAL

Recept type:

PRESCRIPTION DRUG

Terapeutiske indikationer:

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.

Produkt oversigt:

MYCOBUTIN (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: NDC 0013-5301-17 Bottles of 100 capsules 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].

Autorisation status:

New Drug Application

Produktets egenskaber

MYCOBUTIN- RIFABUTIN CAPSULE
DEPARTMENT OF STATE HEALTH SERVICES, PHARMACY BRANCH
----------
MYCOBUTIN
(RIFABUTIN) CAPSULES, USP
DESCRIPTION
MYCOBUTIN Capsules for oral administration contain 150 mg of the
rifamycin antimycobacterial agent
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:
141 to 1033 ng/mL) attained in 3.3 (±0.9) hours (T
range: 2 to 4 hours). Absolute bioavailability
®
46
62
4
11
max
max
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
capsule dosage form, relative to an oral solution, was 85% in 12
hea