A1,
A2,
B,
C1,
C2,
D,
E,
F,
G-H,
I-K,
L,
M,
N,
O,
P1,
P2,
Q-R,
S,
T,
U-V,
W-Z
Nebupent Pharmacology, Pharmacokinetics, Studies, Metabolism - Pentamidine Isethionate
Nebupent Pharmacology, Pharmacokinetics, Studies, Metabolism - Pentamidine Isethionate
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 with mammalian tissues
and the protozoan
Crithidia oncopelti indicate that the drug
interferes with nuclear
metabolism producing
inhibition of the synthesis
of DNA, RNA, phospholipids and proteins.
Little is known about the drug's pharmacokinetics. Preliminary
studies have shown that in seven patients treated with daily I.M.
doses of pentamidine at 4 mg/kg for 10 to 12 days, plasma
concentrations were between 0.3 and 0.5 mcg/mL.
The levels did not appreciably change with time
after injection or
from day to day. Higher plasma
levels were encountered in patients with an elevated BUN. The patients
continued to excrete decreasing amounts of pentamidine
in urine up to six to
eight weeks after cessation of the treatment.
Tissue distribution
has been studied in mice given a single intraperitoneal injection
of pentamidine at
10 mg/kg. The concentration
in the kidneys was the highest followed by that in the liver. In
mice, pentamidine
was excreted unchanged, primarily via
the kidneys with some elimination
in the feces. The ratio
of amounts excreted in the urine
and feces (4: 1) was constant
over the period of study.
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