Post-marketing events have been the occurrence of intracranial bleeding, retroperitoneal bleeding, pulmonary hemorrhage and spinal-epidural hematoma. Fatal bleeding have been reported rarely. Sometimes, thrombocytopenia was associated with chills, low-grade fever or bleeding complications (see above). Cases of hypersensitivity including anaphylaxis have occurred. Interactions
The concomitant application of warfarin or other oral anticoagulants may increase the risk of serious bleeding events. The decision whether maintenance therapy with these drugs should be discontinued during tirofiban treatment has to be made by the responsible clinician. Pharmacology
Tirofiban has a rapid onset and short duration of action after proper IV administration. Coagulation parameters turn to normal 4 to 8 hours after the drug is withdrawn. Chemistry
Tirofiban is a synthetic, non-peptide inhibitor of the interaction of fibrinogen with the integrin glycoprotein IIb/IIIa on human platelets. The Merck chemistry team of George Hartman, Melissa Egbertson and Wasyl Halczenko developed tirofiban from a lead compound discovered in focused screening of small molecule replacements of the key arginine-glycine-aspartic acid (Arg-Gly-Asp) subunit of fibrinogen. Computation of the distance between the charged Arg and Asp sites in fibrinogen provided guidance leading to directed screening success. Tirofiban constitutes an antithrombotic, specifically an inhibitor of platelet aggregation. Tirofiban is a modified version of a molecule found in the venom of the saw-scaled viper Echis carinatus. History
The drug is marketed under the brand name Aggrastat in the US by Medicure Pharma, in China by Eddingpharm, and in the rest of the world by Correvio International Sàrl.
Lefamulin, sold under the brand name Xenleta, is an antibiotic medication used it to treat adults with community-acquired bacterial pneumonia. It is taken by mouth or by injection into a vein.Relatively common side effects include diarrhea, nausea, pain at the site of injection, and liver inflammation. It is a pleuromutilin antibiotic that inhibits the large subunit of bacterial ribosomes.Lefamulin was approved for medical use in the United States in August 2019, and in the European Union in July 2020. Medical uses
Lefamulin is used to treat adults with community-acquired bacterial pneumonia. It was also investigated for treatment of acute bacterial skin and skin-structure infections (ABSSSI). Spectrum of activity
Lefamulin has in vitro activity against Streptococcus viridans, Moraxella catarrhalis, Enterococcus faecium, methicillin-resistant Staphylococcus aureus (MRSA), among other bacteria. History
It was developed by Nabriva Therapeutics and approved in the United States in 2019. It was granted fast track status by the US Food and Drug Administration (FDA) in 2014. Although pleuromutilin antibiotics were first developed in the 1950s, lefamulin is the first to be used for systemic treatment of bacterial infections in humans. Society and culture
Legal status
Lefamulin was approved for medical use in the United States in August 2019, and in the European Union in July 2020. References
External links
"Lefamulin". Drug Information Portal. U.S. National Library of Medicine.