Ticlopidine: Uses, Presentation, Dosage, Side Effects, Interactions, Contraindications and Precautions

It is a platelet aggregation inhibitor medication used to prevent blood clots after a recent heart attack or stroke.

It is also used in people with particular heart or blood vessel disorders.

Generic name: ticlopidine hydrochloride.

Uses of Ticlopidine

Ticlopidine is used to prevent blood platelets from coagulating or to prevent unwanted blood clots that can occur with particular heart or vascular conditions.

Presentation

Tablets of this medicine for oral administration are provided in white, oval, film-coated, blue tablets containing 250 mg of ticlopidine hydrochloride.

Each tablet contains citric acid, magnesium stearate, microcrystalline cellulose, povidone, starch, and stearic acid as inactive ingredients.

The white film coating contains hydroxypropylmethylcellulose, polyethylene glycol, and titanium dioxide.

 

Dosage

The recommended dose of Ticlopidine after stroke is 250 mg twice a day and should be taken with food.

After coronary artery stent placement, the recommended dose is 250 mg twice daily with food and antiplatelet doses of Aspirin for up to 30 days of therapy after successful stent implantation.

Side effects

If you experience any side effects, you should immediately consult your treating doctor and discontinue the use of Ticlopidine.

Less serious side effects may include:

  • Stomach ache.
  • Sickness.
  • Vomiting
  • Ringing in the ears.
  • Diarrhea.
  • Dizziness.
  • Itch.
  • Rochas

Serious side effects

Such as:

  • Difficulty breathing.
  • Swelling of your face, lips, tongue, or throat.
  • Nasal hemorrhage or another bleeding that does not stop.
  • Black stools with blood or tarry.
  • Cough up blood or vomit similar to ground coffee.
  • Chest pain.
  • Heaviness sensation
  • Pain that extends to the arm or shoulder.
  • Sudden numbness or weakness, especially on one side of the body.
  • Sudden headache, confusion, vision problems, speech, or balance.
  • Bruises
  • Weakness.
  • Urinate more or less than usual.
  • Signs of infection like fever and chills.
  • Symptoms of flu and sores in the mouth.
  • Nausea, stomach pain, and loss of appetite.
  • Dark or bloody urine.
  • Jaundice (yellowing of the skin or eyes).
  • Convulsions

What to do in case of overdose?

Seek emergency medical attention if you think you have used too much and are out of this medication.

Symptoms of overdose may include feeling cold, unusual bleeding, difficulty breathing, loss of balance or coordination, and seizures.

Interactions

Ticlopidine may interact with Aspirin, warfarin, heparin, dalteparin, enoxaparin, Clopidogrel, dipyridamole, NSAIDs (non-steroidal anti-inflammatory drugs), antacids or cimetidine, digoxintheophylline, or phenytoin.

Ticlopidine should be used only when prescribed during pregnancy. It is not known if this medication passes into breast milk, but it may negatively affect the infant.

It is important to note that this list is much longer and that there are other drug interactions. So it is essential to do a thorough review of these.

Contraindications and precautions

The following are cases in which Ticlopidine is contraindicated or should be administered with caution:

Any condition that may lead to uncontrolled bleeding contraindicates the use of Ticlopidine, such as gastrointestinal bleeding, hemophilia, intracranial hemorrhage, retinal hemorrhage, or coagulopathy.

Ticlopidine should be used with caution in patients at risk of increased bleeding from trauma, peptic ulcer, or other pathological conditions. In addition, medications that can cause gastric or duodenal ulcers, such as Aspirin, should be administered with great caution.

Ticlopidine is contraindicated in patients with a history of hematological disease related to hematopoiesis, such as neutropenia and thrombocytopenia, or a history of agranulocytosis or aplastic anemia, suppression of the bone marrow.

Other diseases are leukemia, neutropenia, pancytopenia, thrombocytopenia, or thrombotic thrombocytopenic purpura (TTP).

Likewise, Ticlopidine should not be used in bone marrow suppression or leukemia patients. A reduction in hematopoietic precursors in the bone marrow has been associated with therapy with Ticlopidine, which results in severe hematologic reactions.

All patients should undergo regular blood tests during therapy. A complete blood count (CBC) should be obtained every two weeks during the first three months of treatment with Ticlopidine.

If there are laboratory signs of TTP or the neutrophil count below 1200 / mm3, then the Ticlopidine should be stopped immediately.

If patients discontinue Ticlopidine during the first three months, patients should have a complete blood count two weeks after stopping treatment due to the prolonged effects of Ticlopidine.

The most frequent monitoring after the first three months of treatment is only necessary in patients with clinical signs; for example, signs and symptoms of an infection; or laboratory (as in the case of neutrophil count <70% of the initial count, anemia, decreased platelet count) of the hematological effects.

Ticlopidine is occasionally associated with thrombocytopenia unrelated to aplastic anemia or TTP.

Any manifestation, such as an event of unusual bleeding, infection in the presence of white blood cells or low platelets, fever, paleness, petechiae or purpura, dark urine, jaundice, or neurological changes, may indicate an adverse hematological reaction.

A simultaneous decrease in platelet count and white blood cell count should prompt further investigation for a diagnosis of aplastic anemia. Because platelet transfusions can accelerate thrombosis in patients with PTT, they should be avoided.

Dental work, surgery

Ticlopidine irreversibly inhibits platelet aggregation, which does not return to normal until 1-2 weeks after cessation of therapy.

Continued Ticlopidine during surgery or dental work can cause uncontrolled bleeding; The medication should be discontinued 10-14 days before an invasive procedure is recommended.

The prolonged bleeding time is normalized within 2 hours after the administration of methylprednisolone 20 mg IV. Platelet transfusions can also be used to reverse the effect of Ticlopidine on bleeding.

Because platelet transfusions can accelerate thrombosis in patients with thrombotic thrombocytopenic purpura, they should, if possible, be avoided.

Liver disease

Ticlopidine is contraindicated in patients with severe liver disease who may have hemorrhagic diathesis. In patients with advanced cirrhosis, the average plasma concentration of Ticlopidine is slightly higher than that observed in older subjects.

Rarely some people may experience marked elevations of liver enzymes during therapy with Ticlopidine. Liver function tests, including ALT, AST, and GGT, should be considered whenever liver dysfunction is suspected, particularly during the first four months of treatment.

Intramuscular injections

Intramuscular injections should be administered with caution to patients receiving Ticlopidine. IM injections can cause excessive bleeding, bruising, or bruising due to abnormal platelet function and, possibly, thrombocytopenia secondary to ticlopidine therapy.

Dental disease

Patients, especially those with dental diseases, should receive instructions on proper oral hygiene, including caution in using ordinary toothbrushes, dental floss, and toothpicks.

Hypercholesterolemia

Serum cholesterol increases approximately between 8% and 10% during the first month of therapy with Ticlopidine. Hypercholesterolemia persists throughout the treatment. Ticlopidine should be used with caution in patients with preexisting hypercholesterolemia.

Geriatric patient

Ticlopidine should be used with caution in geriatric patients due to a possible increase in toxicity compared to Aspirin without an increase in efficacy.

While ticlopidine and related medications (e.g., Clopidogrel) have been used in elderly patients intolerant or allergic to Aspirin, Ticlopidine is considered a potentially inappropriate medication in geriatric patients.

The Omnibus Budget Reconciliation Act (AORP) regulates the use of medications in residents of long-term care centers.

According to the AORP guidelines, Ticlopidine is associated with more severe side effects and toxicity than other platelet inhibitors.

The use should be avoided in older adults; however, Ticlopidine may be appropriate for people who have had a previous stroke or have evidence of stroke precursors (i.e., transient ischemic attacks) and can not tolerate Aspirin or other conditions platelet inhibitors.

Common side effects of platelet inhibitors include headache, dizziness, and vomiting. Ticlopidine can also cause side effects such as nausea and diarrhea.

Platelet inhibitors can cause thrombocytopenia and increase the risk of bleeding.

Serious side effects of Ticlopidine include life-threatening neutropenia. Concurrent use of platelet inhibitors with warfarin or NSAIDs may increase the risk of bleeding.

Labor, obstetric delivery, pregnancy

Ticlopidine is classified in category B of risk of pregnancy by the FDA. There are no adequate and well-controlled studies on pregnant women. Teratology studies have been conducted in mice (doses up to 200 mg / kg / day), rats (doses up to 400 mg / kg / day) and rabbits (doses up to 200 mg / kg / day).

Doses of 400 mg/kg in rats, 200 mg/kg/day in mice, and 100 mg / kg in rabbits produced maternal toxicity and fetal toxicity. Still, there was no evidence of the teratogenic potential of Ticlopidine.

Because animal reproduction studies are not always predictive of human response, this medication should be used during pregnancy only if necessary. Because Ticlopidine inhibits platelet aggregation, there is an increased risk of bleeding during obstetric deliveries.

Renal disease

There are limited data on Ticlopidine in patients with renal insufficiency. No unexpected adverse effects were observed in clinical trials in patients with mild renal impairment.

However, it may be necessary to adjust the dose or discontinue treatment with Ticlopidine in patients with significant renal impairment (e.g., renal disease, renal failure) if hemorrhagic or hematopoietic problems are detected.

Lactation

According to the manufacturer, studies in rats have shown that Ticlopidine is excreted in milk. It is not known if Ticlopidine is excreted in human milk.

Because many drugs are excreted in human milk, and due to the possibility of drug reactions in infants, the decision should be made to discontinue breastfeeding or discontinue the medication, taking into account the importance of the medicine to the mother.

Consult your doctor before breastfeeding.