ARISTOMOL
0.25% & 0.50%
Sterile
Eye Drops
Composition:
Each ml of solution contains
0.25%
0.50%
Active
substance:
Timolol Maleate
3.41 mg
6.82 mg
Quantity equivalent to Timolol
base
2.50 mg
5.00 mg
Preservative: Benzalkonium Chloride
0.01%
Vehicle: Hydroxypropyl Methylcellulose
0.50%
Inactives and
purified water.
Pharmacological
data:
The action of Aristomol is usually rapid
occurring approx. 20 minutes following ocular instillation. The
maximum effect occurs in one to two hours and significant lowering
of intraocular pressure has been maintained for periods as long as
24 hours with Aristomol
0.25% or 0.50%. Aristomol has the action of
reducing elevated intraocular pressure, whether or not accompanied
by glaucoma. Pharmacological characteristics of Timolol Maleate, the
active ingredient of Aristomol Eye Drops,
are:
-
Non-selective beta blocking
agent.
-
No intrinsic sympathomimetic activity
(I.S.A.).
-
Non significant local anaesthetic effect (membrane
stabilizer).
Unlike miotics, Aristomol has practically
no effect on pupil size or accommodation. No accommodative spasm or
change in visual acuity are observed.
As with other antiglaucoma drugs, a diminished responsiveness
to Aristomol has been
reported in some patients after prolonged
therapy.
Pharmacokinetics
data:
Systemic absorption: Plasma
levels following ocular instillation have not been
specified.
Indications:
-
Ocular
hypertension
-
Chronic open-angle
glaucoma
-
Aphakic
glaucoma
Contraindications:
Absolute
-
Bronchial asthma, bronchospasm,
history of bronchial asthma or severe chronic obstructive pulmonary
disease.
-
Uncontrolled congestive cardiac
insufficiency, cardiogenic
shock
-
High atrioventricular block (without
apparatus)
-
Raynaud
phenomena
-
High bradycardia (pulse rate <
45 to 50 pulses/min.)
-
Hypersensitivity to any
component
Relative
-
combination with
amiodarone
Warnings:
Sports person should take care
that this specialty contains an active product, which can induce in
a positive way the tests made during antidoping
controls.
Precautions:
As with other
topically applied ophthalmic drugs, this drug may be absorbed
systemically and lead to systemic effects of b-blockers.
Cardiac insufficiency should be
adequately controlled before starting therapy with Aristomol. In patients with
a history of severe cardiac disease and in elderly patients, signs
of cardiac insufficiency should be watched for and pulse rates
should be checked.
Following administration of
Timolol Maleate, severe respiratory reactions and cardiac reactions
have been reported, including death due to bronchospasm in patients
with asthma, and rarely death in association with cardiac failure.
Patients already receiving a beta-blocker orally and who are given
Aristomol should be
observed for a potential additive effect either on the intraocular
pressure or on the known systemic effects of
beta-blockers.
Although Aristomol is well tolerated
in glaucomatous patients wearing contact lenses as well as in aphakic patients, the wear of contact lenses
should be avoided due to the risk of:
-
Decarease of lacrimal secretion due to
beta-blockers.
-
Absorption on the lens of some
components of the drug (Benzalkonium
chloride).
-
Keratitis while
wearing soft contact lenses due to Benzalkonium
chloride.
Diabetes melititus:
Beta-blockers should be
administered with caution in patients subject to spontaneous
hypo-glycemia or to diabetic patients
(especially those with labile diabetes) who are receiving insulin or
oral hypoglycemic agents. Beta-blockers may mask the signs and
symptoms of acute hypoglycemia.
Use in
children:
Clinical studies in children have
not been conducted.
Aristomol is not recommended in premature
baby and newborn.
Use in pregnant
women:
Aristomol has not been studied in human
pregnancy.
Nursing
mothers:
Beta-blockers are excreted in the
milk. The risk of hypoglycemia and bradycardia in nursing infants
has not been evaluated. Breast-feeding is not recommended during
treatment.
Interaction:
Those of beta-blocking agents.
Calcium inhibitors, catecholamine depending drugs, beta-blocking
agents may lead to hypotension and/or severe bradycardia, and when
combined with Aristomol
may produce additive effects. Ophthalmic supervision is required in
case of concomitant therapy with eye drops containing adrenaline
(mydriasis may
occur).
Adverse
reactions:
Aristomol ophthalmic solution is generally
well tolerated. In clinical studies of Timolol Maleate the adverse
reactions reported were-mainly:
Ocular: Symptoms of ocular irritation,
including conjunctivitis, blepharitis,
keratitis, corneal hypoesthesis, visual disturbances including
refractive changes (due to withdrawal of miotics therapy in some cases), diplopia and ptosis.
Cardiovascular: bradycardia, arrhythmia,
hypotension, syncope, heart block, cerebro-vascular accident, cerebral ischemia,
congestive heart failure, palpitation, cardiac
arrest.
Respiratory: bronchospasm (predominantly in
patients with pre-existing bronchospastic
disease), respiratory failure, dyspnea.
Systemic: headache, asthenia, nausea,
dizziness, depression, fatigue.
Integumentary: hypersensitivity reactions,
including localized and generalized rash and urticaria have been
reported.
Dosage &
Administration:
The usual starting dose is one
drop of 0.25% Aristomol
in the affected eye twice a day. If the clinical response is not
adequate, the dosage may be changed to one drop of 0.50% Aristomol in the affected
eye twice a day.
If necessary the physician may
institute a concomitant therapy:
-
either a sympathomimetic or parasympathomimetic antiglaucoma ophthalmic solution,
-
or systemically administered
carbonic anhydrase inhibitors, in order to
obtain a better response.
Since in some patients the
pressure-lowering response to Aristomol may require a few
weeks to stabilize, evaluation should include a determination of
intraocular pressure after approximately 4 weeks of treatment with
Aristomol. If the
intraocular pressure is maintained at satisfactory levels, the
dosage schedule may be changed to one drop once a
day.
Substitution to prior a
treatment:
When Aristomol should be
administered in substitution to another beta-blocking ophthalmic
solution, discontinue this drug at the end of a full-day treatment.
On the following day, one drop of Aristomol 0.25% should be
administered in the affected eye twice a day. If a higher dosage of
Aristomol is required
substitute one drop of Aristomol 0.50%, in the
affected eye twice a day.
When Aristomol should be
administered in substitution to a previously used non beta-blocking
antiglaucoma ophthalmic solution, continue
the agent already being used for one day and add one drop of Aristomol 0.25% twice a
day. On the following day, discontinue the previously used antiglaucoma agent and continue Aristomol 0.25%. If a
higher dosage a Aristomol is required,
substitute one drop of Aristomol
0.50%.
When Aristomol should be
substituted to several concomitantly administered antiglaucoma agents, individualization is
required.
The physician will decide to
discontinue one or all the previously used antiglaucoma agents. When a patient is
transferred from miotics to Aristomol, a refractive
examination may be required when moitics
have no longer effects. The patient should follow strictly the
directions for treatment and intraocular pressure should be
controlled particularly at the beginning of the
treatment.
Shelf
life:
If the pack is unopened, Aristomol eye drops can be
used until the expiry date indicated with “EXP” on the
pack.
Special Storage
Condition:
Supply:
Aristomol 0.25%
Eye drops: Plastic dropper bottle
of 5 ml.
Aristomol 0.5%
Eye drops: Plastic dropper bottle
of 5 ml.
