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| __NOTOC__
| | #REDIRECT [[Tenecteplase#Pharmacology]] |
| {{Tenecteplase}}
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| {{CMG}}; {{AE}} {{SS}}
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| ==Clinical Pharmacology==
| | [[Category: Cardiovascular Drugs]] |
| | | [[Category: Drug]] |
| ===General===
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| Tenecteplase is a modified form of human [[tissue plasminogen activator]] ([[tPA]]) that binds to fibrin and converts plasminogen to plasmin. In the presence of fibrin, in vitrostudies demonstrate that Tenecteplase conversion of plasminogen to plasmin is increased relative to its conversion in the absence of fibrin. This fibrin specificity decreases systemic activation of [[plasminogen]] and the resulting degradation of circulating fibrinogen as compared to a molecule lacking this property. Following administration of 30, 40, or 50 mg of TNKase, there are decreases in circulating fibrinogen (4%–15%) and plasminogen (11%–24%). The clinical significance of fibrin-specificity on safety (e.g., bleeding) or efficacy has not been established. Biological potency is determined by an in vitro clot lysis assay and is expressed in Tenecteplase-specific units. The specific activity of Tenecteplase has been defined as 200 units/mg.
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| ===Pharmacokinetics===
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| In patients with [[acute myocardial infarction]] ([[AMI]]), TNKase administered as a single bolus exhibits a biphasic disposition from the plasma. Tenecteplase was cleared from the plasma with an initial half-life of 20 to 24 minutes. The terminal phase half-life of Tenecteplase was 90 to 130 minutes. In 99 of 104 patients treated with Tenecteplase, mean plasma clearance ranged from 99 to 119 mL/min.
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| The initial volume of distribution is weight related and approximates plasma volume. Liver metabolism is the major clearance mechanism for Tenecteplase.<ref name="dailymed.nlm.nih.gov">{{Cite web | last = | first = | title = TNKASE (TENECTEPLASE) KIT [GENENTECH, INC.] | url = http://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=69e391bf-1250-4083-aa60-6aa41c33657f | publisher = | date = | accessdate = 6 February 2014 }}</ref>
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| ==References==
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| {{Reflist|2}}
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| [[Category:Thrombolytic drugs]]
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| [[Category:Cardiovascular Drugs]] | |
| [[Category:Drugs]] | |
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