Monograph: |
Nitrendipine
A yellow crystalline powder. Practically insoluble in water,
sparingly soluble in absolute alcohol and in methyl alcohol:
freely soluble in ethyl acetate. It exhibits polymorphism. Ex-
posure to ultraviolet light leads to formation of a nitrophe-
nylpyridine derivative. Solutions should be prepared in the
dark or under light of wavelength greater than 420 nm, imme-
diately before use.
Protect from light.
Adverse Effects, Treatment, and Precautions
As for dihydropyridine calcium-channel blockers (see Nifed-
ipine).
Interactions
As for dihydropyridine calcium-channel blockers (see Nifed-
ipine.)
Pharmacokinetics
Nitrendipine. is reported to be well absorbed following oral
administration but undergoes extensive first-pass metabo-
lism; the absolute oral bioavailability is reported to range
from about 10 to 20%, depending in part on the dosage form.
Nitrendipine is extensively metabolised in the liver and is ex-
creted as metabolites, mainly in urine, with small amounts in
the faeces. Although early studies reported a terminal elimi-
nation half-life of about 2 to 4 hours, later studies, using more
sensitive assay procedures, have recorded values between
about 10 and 22 hours. Nitrendipine is about 98% bound to
plasma proteins.
Uses and Administration
Nitrendipine is a dihydropyridine calcium-channel blocker
with actions similar to those of nifedipine . it is used
in the treatment of hypertension .
The usual dose is 20 mg daily as a single dose by mouth or as
2 divided doses. The dose may be increased to 20 mg twice
daily if necessary for the control of resistant hypertension. In
the elderly, and in patients with liver disease, an initial dose
of 10 mg daily has been recommended.
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