Ticlopidine
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| Trade names | Ticlid |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a695036 |
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| Routes of administration |
By mouth |
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| Pharmacokinetic data | |
| Bioavailability | >80% |
| Protein binding | 98% |
| Metabolism | Hepatic |
| Biological half-life | 12 hours (single dose) 4–5 days (repeated dosing) |
| Excretion | Renal and fecal |
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| ECHA InfoCard | 100.054.071 |
| Chemical and physical data | |
| Formula | C14H14ClNS |
| Molar mass | 263.786 g/mol |
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Ticlopidine (trade name Ticlid) is an antiplatelet drug in the thienopyridine family which is an adenosine diphosphate (ADP) receptor inhibitor. Research initially showed that it was useful for preventing strokes and coronary stent occlusions. However, because of its rare but serious side effects of neutropenia and thrombotic thrombocytopenic purpura it was primarily used in patients in whom aspirin was not tolerated, or in whom dual antiplatelet therapy was desirable. With the advent of newer and safer antiplatelet drugs such as clopidogrel and ticagrelor, its use remained limited.
Ticlopidine was discovered incidentally in the 1970s while trying to develop a new anti-inflammatory medication. Pharmacology developers noted that this new compound had strong anti-platelet properties. In 1978 it began to be marketed in France for patients at high risk for thrombotic events: postoperative cardiac patients, patients undergoing hemodialysis, peripheral vascular disease, and the prevention of strokes and ischemic heart disease.
Ticlopidine was introduced to the United States under the trade name Ticlid by Roche after it was FDA approved in 1991. The first generic ticlopidine hydrochloride was FDA approved in 1999. As of April 2015, Roche, Caraco, Sandoz, Par, Major, Apotex, and Teva had discontinued generic ticlopidine and no ticlopidine preparations were available in the US.
Ticlopidine is FDA approved for the prevention of strokes and, when combined with aspirin, for patients with a new coronary stent to prevent closure. There are also several off-label uses, including acute treatment of myocardial infarction and unstable angina, peripheral vascular disease, prevention of myocardial infarctions, diabetic retinopathy, and sickle cell disease.
Ticlopidine is considered a second-line option for the prevention of thrombotic strokes among patients who have previously had a stroke or TIA. Studies have shown that it is superior to aspirin in the prevention of death or future strokes. However, it also has more frequent and serious side effects compared to aspirin, so it is reserved for those patients that cannot take aspirin.
When a patient needs to have a stent placed in one of the vessels around their heart, it is important that that stent stay open to keep blood flowing to the heart. Therefore, patients with stents must take medications after the procedure to help maintain that blood flow. Ticlopidine, taken together with aspirin, is FDA approved for this purpose, and in studies it has been shown to work better than aspirin alone or aspirin with an anticoagulant. However, ticlopidine’s serious side effects make it less useful than its cousin, clopidogrel. Current recommendations no longer recommend ticlopidine’s use.
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