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Once in the body, tPA has can cause the desired thrombolytic activity (see figure), or be inactivated and removed. In the bloodstream tPA has a half-life of 4 to 6 minutes. [39] tPA can be bound by a plasminogen activator inhibitor, resulting in inactivation of its activity. The protein is then removed from the bloodstream by the liver.
5340 18815 Ensembl ENSG00000122194 ENSMUSG00000059481 UniProt P00747 P20918 RefSeq (mRNA) NM_001168338 NM_000301 NM_008877 RefSeq (protein) NP_000292 NP_001161810 NP_032903 Location (UCSC) Chr 6: 160.7 – 160.75 Mb Chr 17: 12.6 – 12.64 Mb PubMed search Wikidata View/Edit Human View/Edit Mouse Plasminogen activator inhibitor-1 not only functions as an inhibitor, but other roles of PAI-1 ...
For example, gentamicin is an antibiotic that can be nephrotoxic (kidney damaging) and ototoxic (hearing damaging); measurement of gentamicin through concentrations in a patient's plasma and calculation of the AUC is used to guide the dosage of this drug. [3] AUC becomes useful for knowing the average concentration over a time interval, AUC/t.
Tenecteplase is a 527 amino acid glycoprotein developed by introducing the following modifications to the complementary DNA for natural human tPA: a substitution of threonine 103 with asparagine, and a substitution of asparagine 117 with glutamine, both within the kringle 1 domain, and a tetra-alanine substitution at amino acids 296–299 in ...
In pharmacokinetics, a loading dose is an initial higher dose of a drug that may be given at the beginning of a course of treatment before dropping down to a lower maintenance dose. [ 1 ] A loading dose is most useful for drugs that are eliminated from the body relatively slowly, i.e. have a long systemic half-life .
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There are various competing calculation methods for the drug accumulation ratio, yielding somewhat different results. A commonly used formula defines R ac as the ratio of the area under the curve (AUC) during a single dosing interval under steady state conditions to the AUC during a dosing interval after one single dose: [1]
Threshold dose is the minimum dose of drug that triggers minimal detectable biological effect in an animal. [1] At extremely low doses, biological responses are absent for some of the drugs. The increase in dose above threshold dose induces an increase in the percentage of biological responses. [ 2 ]