Posted in Pharmaceutical materials, Pharmaceutical Raw Materials 04. Jan, 2012 · Edit
Tigecycline [trade name TYGACILTM (U.S. pharmaceutical company Wyeth developed)] is a new broad-spectrum activity of intravenous antibiotics for methicillin-resistant Staphylococcus aureus is also active, the Gly acid in the first tetracycline class drugs, the U.S. Food and Drug Administration (FDA) approved in June 2005 a new drug.
Tigecycline is the first approved new glycyl intravenous antibiotics tetracycline, a broad-spectrum antimicrobial activity, for the treatment of Gram-negative or-positive pathogens, anaerobic organisms and methicillin-resistant Staphylococcus bacteria (MRSA) and methicillin-sensitive strains will Pu (MSSA) caused clA1, DSSSI, tigecycline to doctors to provide a new, early in treatment when the cause is unknown when the wide choice of antibiotics, and impaired renal function do not need to adjust the dose, easy to use, can be taken once every 12 hours. The most common adverse events were nausea (29.5%) and vomiting (9.7%). The antibacterial mechanism is by blocking aminoacyl tRNA into the ribosomal A-site and inhibit bacterial protein synthesis.
Feature
Broad spectrum antimicrobial
Clinical studies have shown that tigecycline can be used for Escherichia coli, Enterococcus faecalis (vancomycin-susceptible strains only), Staphylococcus aureus (methicillin sensitive and resistant strains), Streptococcus agalactiae, angina Streptococcus (including angina, angina, and constellations intermediate Streptococcus Streptococcus), Streptococcus and Bacteroides fragilis purulent, Fernandez Citrobacter, Enterobacter cloacae, Escherichia coli, acid Klebsiella, Klebsiella pneumoniae, Enterococcus faecalis (vancomycin-susceptible strains only), Staphylococcus aureus (methicillin-susceptible strains only), Streptococcus angina (includes angina streptococci, Streptococcus clusters of intermediate and Streptococcus), Bacteroides fragilis, Bacteroides pleomorphic, monomorphic Bacteroides, Bacteroides general, Clostridium perfringens, Peptostreptococcus small intra-abdominal infections caused by adult (cIAI) and complicated skin and soft tissue infections (cSSSI).
Difficult to generate resistance
Studies have shown that tigecycline can overcome the limitations of many antibiotics used two main resistance mechanisms: efflux pumps and ribosomal protection. Thus, tigecycline will be a wider scope.
Long half-life
Single drug half-life of about 27 hours, multiple dose half-life of about 42 hours. Therefore, the medication once every 12 hours, more convenient to use.
Small amount
Reference Wyeth clinical trial data, given tigecycline (initial dose of 100mg, a maintenance dose of 50mg, every 12h), the control group were injected with vancomycin combined aztreonam (1g/2g, every 12h) or imipenem / statin West Division (“imipenem” 200 ~ 500 mg/200 ~ 500mg [according to body weight and creatinine clearance], maintenance dose given every 6h), similar treatment, the two groups, efficacy equivalent to or even better tigecycline However, no significant difference. Tigecycline dosage is very low.
Note
G on two concurrent intra-abdominal infections, bowel perforation occurs clinically in patients, the FDA should be particularly cautious with other drugs, like antibiotics, can cause excessive growth of non-sensitive organisms such as fungi, in the course of treatment should always pay attention to monitoring , in the event of a double infection, must take appropriate measures.
Has not yet been diagnosed before, do not blindly use tigecycline. This product can only treat bacterial infections, not viral infections.
Intermittent irregular medication, or do not complete the entire course of treatment are likely to reduce the effects of treatment, increased drug resistance, even in the future not the FDA or other antibiotics to treat. If you use this product and Wu warfarin, prothrombin time should be monitored and other appropriate anti-coagulation tests.
Pregnant women if the application Tigecycline may cause fetal damage. In the process of tooth development (including late pregnancy, infancy and early childhood before the age of applications tigecycline allows infants discoloration of the teeth (yellow or gray-brown).
Tigecycline is a new class of glycyl tetracycline antibiotics with extended spectrum of antibacterial activity including Gram-positive and gram-negative aerobic bacteria and anaerobic bacteria and other pathogens in clinical isolates of important.
Tigecycline is used to overcome or limit the bacterial efflux pumps and ribosomal protection mechanisms of resistance have two kinds of effect, difficult to generate resistance. Its broad tissue distribution and elimination half-life longer pharmacokinetic properties of cause for optimism.
For patients with renal dysfunction and the need for hemodialysis patients, the need for adjustment of dose and time. Tigecycline has been formally approved by the U.S. FDA for the treatment of complicated intra-abdominal infections and complicated skin of adult and soft tissue infections, including complicated appendicitis, infected burns, intra-abdominal abscesses, deep soft tissue infections and ulcers.
Clinically well tolerated, common side effects are nausea, vomiting and diarrhea, other toxicities were mild. Therefore, the appropriate indications for delivery, which can achieve better therapeutic effect, and its adverse reactions are relatively mild.
Read more: Buy A Tigecycline