Tigestat

Tigestat Uses, Dosage, Side Effects, Food Interaction and all others data.

Tigestat, a glycylcycline, inhibits protein translation in bacteria by binding to the 30S ribosomal subunit and blocking entry of amino-acyl tRNA molecules into the A site of the ribosome. This prevents incorporation of amino acid residues into elongating peptide chains. Tigestat carries a glycylamido moiety attached to the 9-position of minocycline. The substitution pattern is not present in any naturally occurring or semisynthetic tetracycline and imparts certain microbiologic properties to tigecycline. Tigestat is not affected by the two major tetracycline resistance mechanisms, ribosomal protection and efflux. Accordingly, tigecycline has demonstrated in vitro and in vivo activity against a broad spectrum of bacterial pathogens. There has been no cross resistance observed between tigecycline and other antibiotics. Tigestat is not affected by resistance mechanisms such as beta-lactamases (including extended spectrum beta-lactamases), target site modifications, macrolide efflux pumps or enzyme target changes (e.g. gyrase/topoisomerase). In vitro studies have not demonstrated antagonism between tigecycline and other commonly used antibacterial drugs. In general, tigecycline is considered bacteriostatic.

Tigestat is the first clinically-available drug in a new class of antibiotics called the glycylcyclines. Glycylcyclines are a new class of antibiotics derived from tetracycline. These tetracycline analogues are specifically designed to overcome two common mechanisms of tetracycline resistance, namely resistance mediated by acquired efflux pumps and/or ribosomal protection. Glycylcycline antibiotics have a similar mechanism of action as tetracycline antibiotics. Both classes of antibiotics bind to the 30S ribosomal subunit to prevent the amino-acyl tRNA from binding to the A site of the ribosome. However, the glycylcyclines appear to bind more effectively than the tetracyclines.

Trade Name Tigestat
Availability Prescription only
Generic Tigecycline
Tigecycline Other Names Tigeciclina, Tigecycline, Tigecyclinum
Related Drugs amoxicillin, doxycycline, ciprofloxacin, cephalexin, metronidazole, azithromycin, clindamycin, ceftriaxone, Augmentin, amoxicillin / clavulanate
Type Injection
Formula C29H39N5O8
Weight Average: 585.6487
Monoisotopic: 585.279863249
Protein binding

71% to 89%

Groups Approved
Therapeutic Class Tetracycline Group of drugs
Manufacturer
Available Country India
Last Updated: September 19, 2023 at 7:00 am
Tigestat
Tigestat

Uses

Tigestat is used for the treatment of infections caused by susceptible strains of the designated microorganisms in the conditions listed below:

Complicated Skin and Skin structure Infections: Complicated skin and skin structure infections caused by Escherichia coli, Enterococcus faecalis (vancomycin-susceptible isolates only), Staphylococcus aureus (methicillin-susceptible and -resistant isolates), Streptococcus agalactiae, Streptococcus anginosus grp. (includes S. anginosus, S. intermedius, and S. constellatus), Streptococcus pyogenes, Enterobacter cloacae, Klebsiella pneumoniae and Bacteroides fragilis.

Complicated Intra-Abdominal Infections: Complicated intra-abdominal infections caused by Citrobacter freundii, Enterobacter cloacae, Escherichia coli, Klebsiella oxytoca, Klebsiella pneumoniae, Enterococcus faecalis (vancomycin-susceptible isolates only), Staphylococcus aureus (methicillin-susceptible and -resistant isolates), Streptococcus anginosus grp. (includes S. anginosus, S. intermedius, and S. constellatus), Bacteroides fragilis, Bacteroides thetaiotaomicron, Bacteroides uniformis, Bacteroides vulgatus, Clostridium perfringens, and Peptostreptococcus micros.

Community-Acquired Bacterial Pneumonia: Community-acquired bacterial pneumonia caused by Streptococcus pneumoniae (penicillin-susceptible isolates), including cases with concurrent bacteremia, Haemophilus influenzae (beta-lactamase negative isolates), and Legionella pneumophila.

Tigestat is also used to associated treatment for these conditions: Bacterial Infections, Community Acquired Pneumonia (CAP), Complicated Intra-Abdominal Infections, Complicated Skin and Skin Structure Infection

How Tigestat works

Tigestat, a glycylcycline, inhibits protein translation in bacteria by binding to the 30S ribosomal subunit and blocking entry of amino-acyl tRNA molecules into the A site of the ribosome. This prevents incorporation of amino acid residues into elongating peptide chains. Tigestat carries a glycylamido moiety attached to the 9-position of minocycline. The substitution pattern is not present in any naturally occurring or semisynthetic tetracycline and imparts certain microbiologic properties to tigecycline. Tigestat is not affected by the two major tetracycline resistance mechanisms, ribosomal protection and efflux. Accordingly, tigecycline has demonstrated in vitro and in vivo activity against a broad spectrum of bacterial pathogens. There has been no cross resistance observed between tigecycline and other antibiotics. Tigestat is not affected by resistance mechanisms such as beta-lactamases (including extended spectrum beta-lactamases), target site modifications, macrolide efflux pumps or enzyme target changes (e.g. gyrase/topoisomerase). In vitro studies have not demonstrated antagonism between tigecycline and other commonly used antibacterial drugs. In general, tigecycline is considered bacteriostatic.

Dosage

Tigestat dosage

The duration of therapy should be guided by the severity and site of the infection and the patient's clinical and bacteriological progress. The recommended duration of treatment with Tigestat for complicated skin and skin structure infections or for complicated intra-abdominal infections is 5 to 14 days and for community-acquired bacterial pneumonia is 7 to 14 days. The recommended daily dose is as follows:

Adults: The recommended dosage regimen for Tigestat is an initial dose of 100 mg, followed by 50 mg every 12 hours. Intravenous (IV) infusions of Tigestat should be administered over approximately 30 to 60 minutes every 12 hours.

Pediatric use: Safety and effectiveness in pediatric patients below the age of 18 years have not been established.

Geriatric use: No unexpected overall differences in safety or effectiveness were observed between these subjects and younger subjects.

Each vial of Tigestat should be reconstituted with 5.3 ml of 0.9% Sodium Chloride Injection to achieve a concentration of 10 mg/ml of Tigestat. The vial should be gently swirled until the drug dissolves. Withdraw 5 ml of the reconstituted solution from the vial and add to a 100 ml intravenous bag of 0.9% Sodium Chloride or 5% Dextrose for infusion (for a 100 mg dose, reconstitute two vials; for a 50 mg dose, reconstitute one vial). The maximum concentration of IV solution should be 1 mg/ml. If the same intravenous line is used for sequential infusion of several drugs, the line should be flushed before and after infusion of Tigestat with either 0.9% Sodium Chloride Injection or 5% Dextrose Injection. Tigestat is compatible with the following IV fluid: 0.9% Sodium Chloride Injection, 5% Dextrose Injection, Lactated Ringer’s Injection.

Side Effects

The most common treatment-emergent adverse events are nausea and vomiting which generally occurre during the first 1-2 days of therapy.

The following drug-related adverse events are reported infrequently in patients receiving Tigestat: Injection site inflammation & pain, septic shock, allergic reaction, chills, thrombophlebitis, bradycardia, tachycardia, vasodilatation, anorexia, dry mouth, hypoglycemia, hyponatremia, prolonged prothrombin time, eosinophilia, thrombocytopenia, vaginal moniliasis, vaginitis, leukorrhea.

Toxicity

Since glycylcyclines are similar to tetracyclines, they share many of the same side effects and contraindications as tetracyclines. These side effects may include nausea/vomiting, headache, photosensitivity, discoloration of growing teeth, and fetal damage.

Precaution

Tigestat is structurally similar to Tetracycline-class antibiotics and should be administered with caution in patients with known hypersensitivity to Tetracycline-class antibiotics

Interaction

Drug interaction of Tigestat with Digoxin and Warfarin is observed.

Food Interaction

No interactions found.

Tigestat Disease Interaction

Major: colitisModerate: liver disease

Half Life

27-43 hours

Pregnancy & Breastfeeding use

Pregnancy: Tigestat should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Lactation: Caution should be exercised when Tigestat is administered to a nursing woman.

Contraindication

Tigestat is contraindicated for use in patients who have known hypersensitivity to Tigestat.

Acute Overdose

No specific information is available on the treatment of overdosage with Tigestat. Intravenous administration of Tigestat at a single dose of 300 mg over 60 minutes in healthy volunteers resulted in an increased incidence of nausea and vomiting.

Storage Condition

Prior to reconstitution, Tigestat should be stored at 20°C to 25°C. Once reconstituted, Tigestat may be stored at room temperature for up to 24 hours (up to 6 hours in the vial and the remaining time in the intravenous bag). Reconstituted solution may be stored refrigerated at 2°C to 8°C for up to 48 hours following immediate transfer of reconstituted solution into the intravenous bag.

Innovators Monograph

You find simplified version here Tigestat

Tigestat contains Tigecycline see full prescribing information from innovator Tigestat Monograph, Tigestat MSDS, Tigestat FDA label

FAQ

What is Tigestat used for?

Tigestat is used to treat many different bacterial infections of the skin or the digestive system, as well as pneumonia.Tigestat should be used only for infections that cannot be treated with other medicines.

How safe is Tigestat?

Increased risk of death with Tigestat compared to other antibiotics used to treat similar infections.

What are the common side effect of Tigestat?

Nausea, vomiting, headache, dizziness, or pain/swelling at the injection site may occur. If any of these effects last or get worse, tell your doctor or pharmacist promptly.

What is Tigestat indication?

Tigestat for injection is indicated in patients 18 years of age and older for the treatment of complicated skin and skin structure infections caused by susceptible isolates of Escherichia coli.

Is Tigestat safe during pregnancy?

You should not become pregnant while using Tigestat. Tigestat may harm an unborn baby. If you become pregnant, talk to your doctor right away about the risks and benefits of this medication.

Is Tigestat safe during breastfeeding?

Short-term use of Tigestat is acceptable in nursing mothers. As a theoretical precaution, avoid prolonged or repeat courses during nursing. Monitor the infant for rash and for possible effects on the gastrointestinal flora, such as diarrhea or candidiasis.

Can I drink alcohol with Tigestat?

Drinking alcohol while on these medications can increase feelings of nausea.

Can I drive after taking Tigestat?

Do not drive, use machinery, or do anything that needs alertness until you can do it safely. 

How do I take take?

Tigestat injection comes as a powder to be mixed with fluid and injected into a vein. It is usually infused intravenously (into a vein) over a period of 30 to 60 minutes, once every 12 hours.

What is Tigestat indication?

Tigestat for injection is indicated in patients 18 years of age and older for the treatment of community-acquired bacterial pneumonia caused by susceptible isolates of Streptococcus pneumoniae.

Can I take Tigestat long time?

The recommended duration of treatment with Tigestat for complicated skin and skin structure infections or for complicated intra-abdominal infections is 5 to 14 days.

How do I administer Tigestat?

Tigestat is administered only by intravenous infusion over 30 to 60 minutes.Tigestat should be preferably administered over a 60-minute length of infusion in paediatric patients .

Does Tigestat cause fever?

Tigestat may cause fever with other side effects are stomach pain, chills, constipation, nausea, vomiting, fever, or lightheadedness.

When is the best time to take Tigestat?

Tigestat comes as a capsule to take by mouth. It is usually taken two or four times daily.Tigestat should be taken on an empty stomach, at least 1 hour before or 2 hours after meals or snacks. Drink a full glass of water with each dose of Tigestat.

What happens if I stop taking Tigestat?

It usually goes away after Tigestat is stopped; however, there is a chance of permanent vision loss or blindness.

Can Tigestat cause liver damage?

High doses of intravenous tetracycline can induce fatty liver disease and may result in severe hepatic dysfunction, acute liver failure and death. This syndrome is more common among pregnant women, largely during the last trimester or early postpartum period.

Is Tigestat toxic?

The breakdown products of Tigestat are toxic and can cause Fanconi syndrome, a potentially fatal disease affecting proximal tubular function in the nephrons of the kidney.

How does Tigestat affect teeth?

To put it plainly, tooth discoloration occurs when Tigestat binds with the calcium needed for tooth development.

Does Tigestat turn my teeth yellow?

The bound Tigestat will cause the teeth to come out with an initial fluorescent yellow discoloration.

*** Taking medicines without doctor's advice can cause long-term problems.
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