Telavancinum
Telavancinum Uses, Dosage, Side Effects, Food Interaction and all others data.
Telavancinum is a semi-synthetic derivative of vanocymycin that has bactericidal activity against Methicillin-resistant Staphylococcus aureus (MRSA) and other gram-positive bacteria. MRSA is an important pathogen capable of causing hospital-acquired pneumonia (HAP), ventilator-associated pneumonia (VAP), and skin and subcutaneous tissue infections among others.
Telavancinum is a semi-synthetic derivative of vancomycin, therefore the mode of bactericidal action is similar to vancomycin in which both antibiotics inhibit cell wall synthesis. Not only that, it displays concentration-dependent bactericidal action. Furthermore, telavancin is a more potent inhibitor (10-fold) of peptidoglycan synthesis and, unlike vancomycin, disrupts cell membrane integrity via its interaction with lipid II. AUC/MIC ratio best predicts the extent of in-vivo response in which the higher the ratio, the greater the bactericidal activity. The smallest ratio in which one would be able to observe no bacterial growth at 24 hours is 50. Maximal bactericidal activity is observed at a AUC/MIC ratio of 404.
| Trade Name | Telavancinum |
| Availability | Prescription only |
| Generic | Telavancin |
| Telavancin Other Names | Telavancin, Telavancina, Télavancine, Telavancinum |
| Related Drugs | amoxicillin, doxycycline, ciprofloxacin, metronidazole, azithromycin, clindamycin, ceftriaxone, levofloxacin, Augmentin, amoxicillin / clavulanate |
| Type | |
| Formula | C80H106Cl2N11O27P |
| Weight | Average: 1755.65 Monoisotopic: 1753.6374296 |
| Protein binding | >90% to serum albumin in a concentration independent manner (despite being highly protein bound, antimicrobial activity of telavancin is not affected) |
| Groups | Approved |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Telavancinum is an antibacterial agent used in the treatment of complicated skin and skin structure infections and types of hospital-acquired bacterial pneumonia.
For the treatment of complicated skin and skin structure infections (cSSSI) caused by gram-positive bacteria like methicillin-susceptible or -resistant Staphylococcus aureus, vancomycin-susceptible Enterococcus faecalis, and Streptococcus pyogenes, Streptococcus agalactiae, or Streptococcus anginosus group. Also for the treatment of adult patients with hospital-acquired bacterial pneumonia (HAP) and ventilator-associated bacterial pneumonia (VAP), known or suspected to be caused by susceptible isolates of Staphylococcus aureus (including methicillin-susceptible and methicillin-resistant S. aureus).
Telavancinum is also used to associated treatment for these conditions: Bacterial Infections, Nosocomial Pneumonia, Ventilator-associated Bacterial Pneumonia, Complicated Skin and subcutaneous tissue bacterial infection
How Telavancinum works
Telavancinum is a bactericidal lipoglycopeptide that is active against a broad range of gram-positive bacteria. Telavancinum prevents polymerization of N-acetylmuramic acid (NAM) and N-acetylglucosamine (NAG) and cross-linking of peptidoglycan by binding to D-Ala-D-Ala. As a result, inhibition of bacterial cell wall synthesis occurs. Furthermore, telavancin disrupts membrane potential and cell permeability as a result of the lipophillic side chain moiety. This additional bactericidal mechanism is what sets telavancin apart from vancomycin.
Food Interaction
No interactions found.Telavancinum Hypertension interaction
[Moderate] Telavancinum may increase the risk of nephrotoxicity in patients predisposed to kidney dysfunction (preexisting renal disease, diabetes mellitus, congestive heart failure, or hypertension) and in those taking medications known to affect kidney function.
It is recommended to monitor renal function (i.e., serum creatinine, creatinine clearance) prior to initiation of therapy, during treatment, and at the end of treatment in all patients receiving telavancin; and if renal function decreases, the benefit of continuing therapy versus discontinuing and initiating therapy with an alternative agent should be assessed.
Telavancinum Drug Interaction
Major: moxifloxacin, moxifloxacinModerate: amphotericin b liposomal, ciprofloxacin, fluconazoleUnknown: 5-hydroxytryptophan, acetaminophen, acetaminophen / diphenhydramine, lactobacillus acidophilus, retapamulin topical, zolpidem, zolpidem, amoxicillin / clavulanate, aztreonam, diphenhydramine, omega-3 polyunsaturated fatty acids, ertapenem, guaifenesin, omeprazole, ascorbic acid
Telavancinum Disease Interaction
Major: colitis, QT prolongationModerate: coagulation test interference, hepatic impairment, nephrotoxicity, renal impairment
Volume of Distribution
Vss, healthy subjects, 10 mg/kg = 0.14 L/kg
Elimination Route
Telavancinum demonstrates linear pharmacokinetics at doses between 1 and 12.5 mg/kg. Furthermore, 24 hours post-infusion of a dose of 7.5 to 15 mg/kg, activity against MRSA and penicillin-resistant Streptococcus pneumonia can still be observed. The trough concentration at this point of time is approximately 10 μg/mL. Telavancinum also has poor bioavailability and must be administered over 30-120 minutes IV. Cmax, healthy subjects, 10 mg/kg = 93.6 ± 14.2 μg/mL; AUC (0- ∞), healthy subjects, 10 mg/kg = 747 ± 129 μg · h/mL; AUC (0-24h), healthy subjects, 10 mg/kg = 666± 107 μg · h/mL; Time to steady state = 3 days;
Half Life
Terminal elimination half-life = 8 ± 1.5 hours (with normal renal function)
Clearance
Cl, healthy subjects, 10 mg/kg = 13.9 ± 2.9 mL/h/kg
Elimination Route
Urine with >80% as unchanged drug and <20% as hydroxylated metabolites (with dose of 10mg/kg); Feces (<1%)
Innovators Monograph
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