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Aplaket®
Ticlopidine hydrochloride
COMPOSITION:
Each coated tablet contains:
Active ingredient:
Ticlopidine hydrochloride 250 mg
Excipients:
Lactose monohydrate, sodium starch glycolate, polyethylene glycol, povidone,
magnesium stearate, hydroxypropylcellulose. ethylcellulose. diethyl
phthalate, acacia gum, titanium dioxide, talc, sucrose, carnauba wax, white
beeswax, hard paraffin.
MODE OF ACTIONS:
Ticlopidine is an inhibitor of platelet aggregation. It causes
dose-dependent inhibition of platelet aggregation and release of platelet
factors, as well as a prolongation of bleeding time.
PHARMACOLOGY:
Ticlopidine is a thienopyridine with antithrombotic activity. It decreases
platelet adhesivity, inhibits platelet aggregation (induced by ADP,
collagen, thrombin and endoperoxides). stimulates platelet disaggregation.
decreases the hyperaggregability of erythrocytes (induced by protamine
sulfate). improves erythrocytes ability to modify their shape (filtration
capacity).
Pharmacokinetics properties:
After oral administration of a single 250 mg or 500 mg dose, the peak of the
active ingredient occurs at approximately 2 hours after dosing, and the drug
is almost totally eliminated from blood 8 hours after administration. The
dose is absorbed by 80-90% in rats and man. After a single oral dose of 1000
mg, the plasmatic peak is 2.1 mg/l. The half-life is 24 hours. At the
therapeutic doses. the inhibition of platelet aggregation induced by
ticlopidine becomes significant after 24-48 hours from the beginning of
treatment: the greatest effect is reached during the 5th or 6th day of
treatment and disappears 5 to 6 days after treatment withdrawal.
Oral administration of 14C-ticlopidine (25 mg/Kg) to rats has
shown that the product is eliminated by 70% in the bile and by 30% at renal
level. After a single oral administration of 500 mg ticlopidine, its
concentration decreases rapidly to 0.7 mg/12 hours after dosing.
INDICATIONS:
Ticlopidine is indicated in the secondary prevention of cerebral and
cardiovascular occlusive ischemia in patients with thrombotic risk
(peripheral occlusive arterial disease, previous myocardial infarction,
previous recurrent and transient ischemic attacks, cerebro-ischemic stroke,
unstable angina). In patients who have experienced previous myocardial
infarction and previous recurrent and transient ischemic attacks,
ticlopidine should be used in the case that intolerance to acetylsalicylic
acid (ASA) has been ascertained or when ASA resulted ineffective.
Ticlopidine is also indicated in the prevention of aorta-coronary bypass
graft occlusion, in extra-corporal circulation and in haemodialysis.
CONTRAINDICATIONS:
Assessed individual hypersensitivity to ticlopidine.
The product is contraindicated in patients affected or who have
experienced leucopenia, thrombocytopenia or agranulocytosis.
Bleeding diatheses and haemostatic disorders inducing a prolongation of
bleeding time.
Active pathological bleeding (such as bleeding gastrointestinal ulcer,
bleeding esophageal varices, etc.).
Acute haemorragic cerebrovascular strokes.
Severe hepatopathy.
Use in Pregnancy and Lactation: Ticlopidine should not be prescribed
to a pregnant or nursing mother.
SIDE EFFECTS:
The following undesirable effects have been shown in course of treatment
with ticlopidine:
- bleeding complications (haemorrhages);
- leucopenia, thrombocytopenia, agranulocytosis, medullary aplasia
(particularly severe in the elderly);
- gastrointestinal discomforts (nausea, gastralgia, diarrhoea);
- increase of transaminases and, rarely, cholestatic jaundice (it is
therefore adviced to monitor the hepatic function periodically);
- skin rash, which is reversible by withdrawing the treatment;
- vertigo;
- thrombotic, thrombocytopenic purpura.
PRECAUTIONS:
The physician should prescribe the product only in the pathologies reported
in the section INDICATIONS, monitoring the patients by scheduled blood tests and
observing carefully the contraindications.
Before starting therapy and,
then, every 15 days for the first 3 months of treatment, it is necessary to
perform blood cell counting, particularly leucocyte and platelet counts.
Before a surgical intervention, the treatment must be withdrawn for one.
week (except for those cases who cannot interrupt it) due to the hemorragic
risk induced by the product; after treatment withdrawal and before the
intervention, it is advised to evaluate if the effect on haemostasis still
persists (by determination of the bleeding time).
If a dental extraction is
needed, inform the dentist of the treatment in course.
In the case that pharyngitis, ulcers of the buccal mucosa, angina, fever,
bleeding or hematomas occur, the treatment should be immediately withdrawn
and the physician should be informed; the eventual resumption of therapy
depends from the results of the blood tests and clinical evaluation.
Patients with impaired liver function: Ticlopidine should be used with
caution and treatment should be discontinued if hepatitis or jaundice
develops. Safety and efficacy in children below 18 years old have not been
established.
Drug interactions: As ticlopidine induces a prolongation of bleeding time,
its association with NSAIDs (ASA, etc.), with anticoagulants (eparine,
antivitamin K), should be avoided. The association with potentially
myelotoxic drugs should be avoided.
WARNINGS:
Some cases on ticlopidine treatment evidenced, sometimes irreversibly,
leucopenia and agranulocytosis; therefore the product should be administered
only in the case that is effectively needed. The use of ticlopidine is
absolutely avoided in the primary prevention of clinically healthy subjects.
DOSAGE:
The recommended dose is, for a long-term treatment, 1-2 coated tablets daily
at meals.
OVERDOSAGE:
Symptoms of overdosage: hemorrhage, convulsions, hypothermia, dyspnea, loss
of equilibrium and abnormal gait. Other anormalities reported include
increased bleeding time and increased SGPT.
Following overdosage, induced vomiting, gastric lavage and other general
supportive are recommended.
PRESENTATION:
Aplaket is a white, round shiny sugar coated tablet.
The tablets are packed in blisters of 10's. Each box contains 20 or 30
coated tablets.
Store at cool, dry place at room temperature not exceeding 25°C.
Keep the medicine out of reach of children.
Expiry date is 3 years from the date of manufacturing. |
