HomeTIGECYCLINE: A new broad spectrum antibiotic
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TIGECYCLINE: A new broad spectrum antibiotic
by Admin Mon Jun 18, 2012 4:34 pm
Tigecycline is a glycylcycline antibiotic, got FDA approval on approved on June 17, 2005.
Structure
This antibiotic is the first clinically-available drug in a new class of antibiotics called the glycylcyclines. It is structurally similar to the tetracyclines in that it contains a central four-ring carbocyclic skeleton and is actually a derivative of minocycline. Tigecycline has a substitution at the D-9 position which is believed to confer broad spectrum activity.
Mechanism of action
Tigecycline is bacteriostatic and is a protein synthesis inhibitor by binding to the 30S ribosomal subunit of bacteria and thereby blocking entry of Aminoacyl-tRNA into the A site of the ribosome during prokaryotic translation.
Indications
Tigecycline is given intravenously and has activity against a variety of gram-positive and gram-negative bacterial pathogens, many of which are resistant to existing antibiotics. Tigecycline successfully completed phase III trials in which it was at least equal to intravenous vancomycin and aztreonam to treat complicated skin and skin structure infections (cSSSI), and to intravenous imipenem and cilastatin to treat complicated intra-abdominal infections (cIAI).Tigecycline is active against many Gram-positive bacteria, Gram-negative bacteria and anaerobes – including activity against methicillin-resistant Staphylococcus aureus (MRSA), Stenotrophomonas maltophilia, Haemophilus influenzae, and Neisseria gonorrhoeae (with MIC values reported at 2mcg/mL) and multi-drug resistant strains of Acinetobacter baumannii. It has no activity against Pseudomonas spp. or Proteus spp. The drug is licenced for the treatment of skin and soft tissue infections as well as intra-abdominal infections.
Dosing
Tigecycline is given by slow intravenous infusion (30 to 60 minutes). A single dose of 100 mg is given first, followed by 50 mg every twelve hours after that. Patients with impaired liver function need to be given a lower dose. No adjustment is needed for patients with impaired kidney function. It is not licensed for use in children. There is no oral form available.
Side effects
Tigecycline has similar side effects to the tetracyclines. The most common side effects of tigecycline are diarrhea, nausea and vomiting. Nausea and vomiting is mild or moderate and usually occurs during the first two days of therapy. Other side effects include pain at the injection site, swelling and irritation; increased or decreased heart rate and infections. Also avoid use in children and pregnancy, due to its effects on teeth and bone. As with other antibiotics, overgrowth of organisms that are not susceptible to tigecycline can occur.
Tigecycline showed an increased mortality in patients treated for hospital-acquired pneumonia, especially ventilator-associated pneumonia, but also in patients with complicated skin and skin structure infections, complicated intra-abdominal infections and diabetic foot infection.
Contraindication
Hypersensitivity to Tigecycline or tetracycline class of antibiotics.
Special Precaution
Pregnancy (use may cause fetal harm), lactation, children <18 yr (safety and efficacies not established). Hepatic dysfunctions, liver failure and pancreatitis (including fatalities) have been reported. Not to be use during tooth development (last half of pregnancy, infancy, and childhood up to 8 yr) as it may cause permanent teeth discolouration. Treatment may cause superinfection and Clostridium difficile associate diarrhoea. An increase in all-cause mortality has been observed in Tigecycline-treated patients versus comparator-treated patients (cause of increase has not been established). Not recommended for treatment of hospital-acquired pneumonia and ventilator-associated pneumonia. Caution in patients with complicated intra-abdominal infections secondary to clinically apparent intestinal perforation.
Role of Tigecycline in AML
Scientists have highlighted mitochondrial translation inhibition as a potential therapeutic strategy for treating acute myeloid leukemia (AML). Results showed that the broad-spectrum antibiotic tigecycline selectively killed leukemia stem and progenitor cells without affecting normal hematopoietic cells. Tigecycline in addition showed antileukemic activity in mouse models of human leukemia. The effects of the drug were subsequently found to relate to inhibition of mitochondrial protein translation.
Brand names available in India
Tevran (Ranbaxy)
Tigebax (Glenmark)
Tigez (Lupin)
Tygacil (Wyeth)
Posted by:
Dr. Rituparna Maiti
Associate Professor, Pharmacology
Structure
This antibiotic is the first clinically-available drug in a new class of antibiotics called the glycylcyclines. It is structurally similar to the tetracyclines in that it contains a central four-ring carbocyclic skeleton and is actually a derivative of minocycline. Tigecycline has a substitution at the D-9 position which is believed to confer broad spectrum activity.
Mechanism of action
Tigecycline is bacteriostatic and is a protein synthesis inhibitor by binding to the 30S ribosomal subunit of bacteria and thereby blocking entry of Aminoacyl-tRNA into the A site of the ribosome during prokaryotic translation.
Indications
Tigecycline is given intravenously and has activity against a variety of gram-positive and gram-negative bacterial pathogens, many of which are resistant to existing antibiotics. Tigecycline successfully completed phase III trials in which it was at least equal to intravenous vancomycin and aztreonam to treat complicated skin and skin structure infections (cSSSI), and to intravenous imipenem and cilastatin to treat complicated intra-abdominal infections (cIAI).Tigecycline is active against many Gram-positive bacteria, Gram-negative bacteria and anaerobes – including activity against methicillin-resistant Staphylococcus aureus (MRSA), Stenotrophomonas maltophilia, Haemophilus influenzae, and Neisseria gonorrhoeae (with MIC values reported at 2mcg/mL) and multi-drug resistant strains of Acinetobacter baumannii. It has no activity against Pseudomonas spp. or Proteus spp. The drug is licenced for the treatment of skin and soft tissue infections as well as intra-abdominal infections.
Dosing
Tigecycline is given by slow intravenous infusion (30 to 60 minutes). A single dose of 100 mg is given first, followed by 50 mg every twelve hours after that. Patients with impaired liver function need to be given a lower dose. No adjustment is needed for patients with impaired kidney function. It is not licensed for use in children. There is no oral form available.
Side effects
Tigecycline has similar side effects to the tetracyclines. The most common side effects of tigecycline are diarrhea, nausea and vomiting. Nausea and vomiting is mild or moderate and usually occurs during the first two days of therapy. Other side effects include pain at the injection site, swelling and irritation; increased or decreased heart rate and infections. Also avoid use in children and pregnancy, due to its effects on teeth and bone. As with other antibiotics, overgrowth of organisms that are not susceptible to tigecycline can occur.
Tigecycline showed an increased mortality in patients treated for hospital-acquired pneumonia, especially ventilator-associated pneumonia, but also in patients with complicated skin and skin structure infections, complicated intra-abdominal infections and diabetic foot infection.
Contraindication
Hypersensitivity to Tigecycline or tetracycline class of antibiotics.
Special Precaution
Pregnancy (use may cause fetal harm), lactation, children <18 yr (safety and efficacies not established). Hepatic dysfunctions, liver failure and pancreatitis (including fatalities) have been reported. Not to be use during tooth development (last half of pregnancy, infancy, and childhood up to 8 yr) as it may cause permanent teeth discolouration. Treatment may cause superinfection and Clostridium difficile associate diarrhoea. An increase in all-cause mortality has been observed in Tigecycline-treated patients versus comparator-treated patients (cause of increase has not been established). Not recommended for treatment of hospital-acquired pneumonia and ventilator-associated pneumonia. Caution in patients with complicated intra-abdominal infections secondary to clinically apparent intestinal perforation.
Role of Tigecycline in AML
Scientists have highlighted mitochondrial translation inhibition as a potential therapeutic strategy for treating acute myeloid leukemia (AML). Results showed that the broad-spectrum antibiotic tigecycline selectively killed leukemia stem and progenitor cells without affecting normal hematopoietic cells. Tigecycline in addition showed antileukemic activity in mouse models of human leukemia. The effects of the drug were subsequently found to relate to inhibition of mitochondrial protein translation.
Brand names available in India
Tevran (Ranbaxy)
Tigebax (Glenmark)
Tigez (Lupin)
Tygacil (Wyeth)
Posted by:
Dr. Rituparna Maiti
Associate Professor, Pharmacology
Admin- Administrator
- Posts : 14
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Re: TIGECYCLINE: A new broad spectrum antibiotic
by r.venukumar Tue Jun 19, 2012 3:24 pm
sir,
Can we use it as empirical broad spectrum antibiotic??
Can we use it as empirical broad spectrum antibiotic??
r.venukumar- Newbie
- I am : House Surgeon Batch : 2007 Posts : 5
Points : 7
Reputation : 0
Location : Hyderabad
To R Venukumar
by rituparnamaiti Tue Jun 19, 2012 4:11 pm
No. Not as empirical...we cant use it in hospital acquired and ventilator associated pneumonia. And moreover it is better to restrict its use for resistant strain only.
rituparnamaiti- Newbie
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Location : Karimnagar
Re: TIGECYCLINE: A new broad spectrum antibiotic
by r.venukumar Tue Jun 19, 2012 4:18 pm
ok sir!rituparnamaiti wrote:No. Not as empirical...we cant use it in hospital acquired and ventilator associated pneumonia. And moreover it is better to restrict its use for resistant strain only.
Thank you
r.venukumar- Newbie
- I am : House Surgeon Batch : 2007 Posts : 5
Points : 7
Reputation : 0
Location : Hyderabad
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