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
Optipranolol Pharmacology, Pharmacokinetics, Studies, Metabolism - Metipranolol
Optipranolol Pharmacology, Pharmacokinetics, Studies, Metabolism - Metipranolol
CLINICAL PHARMACOLOGY
Metipranolol blocks beta1 and beta2 (non-selective) adrenergic
receptors. It does not have significant
intrinsic sympathomimetic
activity, and has only weak
local anesthetic
(membrane-stabilizing) and myocardial
depressant activity. Orally administered beta-adrenergic blocking
agents reduce cardiac
output in both healthy
subjects and patients with heart
disease. In patients with
severe impairment
of myocardial function,
beta-adrenergic receptor antagonists may inhibit the sympathetic
stimulatory effect necessary
to maintain adequate cardiac
output.
Beta-adrenergic receptor
blockade in the bronchi
and bronchioles may result in significantly increased airway
resistance from unopposed
para-sympathetic activity. Such an effect
is potentially dangerous in patients with asthma or other bronchospastic
conditions (see CONTRAINDICATIONS
and WARNINGS).
OptiPranolol Ophthalmic Solution, when applied topically in the
eye, has the action of
reducing elevated as well as normal
intraocular pressure
(IOP), whether or not accompanied by glaucoma. Elevated intraocular
pressure is a major risk
factor in the pathogenesis
of glaucomatous
visual field loss. The
higher the level of intraocular
pressure, the greater
the likelihood of glaucomatous
visual field
loss and optic
nerve damage.
The primary mechanism
of the ocular hypotensive
action of metipranolol
is most likely due to a reduction
in aqueous humor
production. A slight increase in outflow
may be an additional mechanism. OptiPranolol Ophthalmic Solution
reduces IOP with little
or no effect
on pupil size or accommodation.
Animal PHARMACOLOGY
In rabbits administered metipranolol in one eye
at 2 to 4 fold increased
concentrations, multi-focal interstitial
nephritis was observed
in male animals, and lympho-hystiocytic and heterophilic
interstitial pneumonia
was observed in female
animals. The clinical
relevance of these findings is unknown.
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