PENTAM 300- pentamidine isethionate injection, powder, lyophilized, for solution

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

PENTAMIDINE ISETHIONATE (UNII: V2P3K60DA2) (PENTAMIDINE - UNII:673LC5J4LQ)

Available from:

Fresenius Kabi USA, LLC

INN (International Name):

PENTAMIDINE ISETHIONATE

Composition:

PENTAMIDINE ISETHIONATE 300 mg in 3 mL

Administration route:

INTRAMUSCULAR

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

Pentam 300 (pentamidine isethionate for injection) is indicated for the treatment of pneumonia due to Pneumocystis carinii . Contraindicated in patients with a history of hypersensitivity to pentamidine isethionate.

Product summary:

PENTAM® 300 (pentamidine isethionate for injection) Store dry product at 20° to 25°C (68° to 77°F) [see USP Controlled Room Temperature]. Protect from light. Preservative Free.  Discard unused portion.

Authorization status:

New Drug Application

Summary of Product characteristics

PENTAM 300- PENTAMIDINE ISETHIONATE INJECTION, POWDER, LYOPHILIZED,
FOR
SOLUTION
FRESENIUS KABI USA, LLC
----------
PENTAM® 300 (PENTAMIDINE ISETHIONATE FOR INJECTION)
_FOR INJECTION ONLY_
DESCRIPTION
Pentam 300 (pentamidine isethionate for injection), an anti-protozoal
agent, is a sterile,
nonpyrogenic, lyophilized product. After reconstitution, it should be
administered by
intramuscular (IM) or intravenous (IV) routes (see DOSAGE AND
ADMINISTRATION).
Pentamidine isethionate is a white crystalline powder soluble in water
and glycerin,
slightly soluble in alcohol and insoluble in ether, acetone, and
chloroform. It is chemically
designated as 4,4-[1,5-pentanediylbis(oxy)]bis-benzenecarboximidamid
with the
following structural formula:
EACH VIAL CONTAINS:
Pentamidine isethionate . . . . . . . . . . . . . 300 mg
CLINICAL PHARMACOLOGY
Pentamidine isethionate, an aromatic diamidine, is known to have
activity against
_Pneumocystis carinii_. The mode of action of pentamidine is not fully
understood. _In vitro_
studies indicate that the drug interferes with protozoal nuclear
metabolism by inhibition
of DNA, RNA, phospholipid and protein synthesis.
PHARMACOKINETICS
Pharmacokinetic parameters following the administration of 4 mg/kg
pentamidine
isethionate as a single two-hour intravenous infusion or after a
single intramuscular
injection to 12 patients with AIDS are presented in the following
table:
Mean ±
SD
Cmax
ng/mL
Clearance
L/h
Half-life
hours
Vdss
L
Concentration
ng/mL
8 hour
24 hour
2 hour I.V. infusion
4 mg/kg (N=6)
612 ± 371 248 ± 91 6.4 ± 1.3 821 ± 535 19.3 ± 16.92.9 ± 1.4
I.M.
4 mg/kg (N=6)
209 ± 48 305 ± 81 9.4 ± 2.02724 ± 1066 22.9 ± 8.0 6.6 ± 3.5
In seven patients treated with daily IM doses of pentamidine at 4
mg/kg for 10 to 12
days, plasma concentrations were between 300 to 500 ng/mL. The
concentrations did
not appreciably change with time after injection or from day to day.
Higher plasma
concentrations were encountered in patients with an elevated blood
urea nitrogen. The
patients continued