dalbavancin

Action and Spectrum

Mechanism of action 

It is a lipoglycopeptide antibiotic with a mechanism of action similar to other glycopeptide antibiotics, such as vancomycin. It binds to the terminal D-alanine residues of bacterial cell wall peptidoglycan, disrupting cell wall synthesis and leading to bacterial cell death 

Spectrum 

Its spectrum of activity includes gram-positive bacteria, including methicillin-resistant Staphylococcus aureus (MRSA) and Streptococcus pneumoniae. 

Drug Interaction

Adverse Reaction

Frequency defined:  

1-10% 

Adults 

Headache 

Vomiting 

Pruritis 

Nausea 

Diarrhea 

Rash 

<2% 

Anemia 

Leukopenia 

Abdominal pain 

Hepatotoxicity 

Hypoglycemia 

Bronchospasm 

Dizziness 

Anaphylactoid reaction 

Rash 

Urticaria 

Thrombocytopenia 

Oral candidiasis 

Pruritis 

Phlebitis 

Hematoma 

Flushing 

Pediatrics 

Pyrexia 

<1%(Adults) 

Elevated ALT 

Pediatrics 

Dizziness 

Diarrhea 

Pruritis 

Black Box Warning

Contraindication / Caution

Contraindications 

Hypersensitivity 

Caution 

• It should be used with caution in patients with a history of anaphylaxis or other allergic reactions to glycopeptide antibiotics.  
• It should also be used with caution in patients with renal impairment, as the drug is eliminated primarily by the kidneys. Patients should also be closely monitored for signs of superinfection, as antibiotics can lead to the overgrowth of non-susceptible organisms. 
• Additionally, dalbavancin should be used with caution in patients with known or suspected bacteremia, as it has not been studied in these patients. It should also be used cautiously in pregnant or breastfeeding women as these populations have limited safety data. 

Pregnancy / Lactation

Pregnancy consideration: Insufficient data available 

Lactation: Excretion of the drug in human breast milk is unknown 

Pregnancy category: 

Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester.   

Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    

Category D: adequate data available with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.    

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    

Category N: There is no data available for the drug under this category. 

Pharmacology

Pharmacology 

It is a lipoglycopeptide antibiotic that targets the D-alanyl-D-alanine terminus of the stem pentapeptide in nascent cell wall peptidoglycan, preventing cross-linking and disrupting cell wall synthesis. This leads to bacterial cell death. The drug is bactericidal in vitro against several gram-positive bacteria, including Staphylococcus aureus and Streptococcus pyogenes, at concentrations observed in humans at recommended doses. It is also active against other gram-positive bacteria, such as MRSA and Streptococcus pneumoniae. 

Pharmacodynamics 

It has a prolonged half-life, which allows for once-weekly dosing and enables the accumulation of the drug in the serum and at the site of infection. The high serum concentrations achieved with dalbavancin are also responsible for its post-antibiotic effect (PAE). The drug inhibits bacterial growth even after the antibiotic is no longer present. The PAE is prolonged and can last for several days, which can help prevent antibiotic resistance development. Additionally, dalbavancin has a high binding affinity to bacterial cell wall peptidoglycan, which results in a low minimum inhibitory concentration (MIC) and high bactericidal activity against a wide range of gram-positive bacteria.  

Pharmacokinetics 

Absorption: 

The absorption of dalbavancin is high, with a peak plasma concentration of 4287 mg/L for a single 1000 mg dose and an AUC 0-24 of 3185 mg.hr/L 

Distribution:  

The drug is highly protein bound, reversible, and primarily bound to albumin. 

Metabolism:  

It is not a substrate, inhibitor, or inducer of CYP450 isoenzymes. A minor metabolite (hydroxy-dalbavancin) is observed in urine. 

Excretion: 

The elimination half-life of dalbavancin is 346 hours, and it is primarily excreted in the urine and feces, with 33% unchanged in the urine, 12% metabolite in urine, and 20% in fece 

Adminstartion

Administration 

It is typically administered as an intravenous (IV) injection or infusion. The usual recommended dosage is a single dose of 1000 mg, followed by a second dose of 500 mg, given one week later. 

It is typically administered in a hospital or clinic setting, requiring a healthcare professional to administer the injection or infusion. The drug is usually given over 30 minutes to 1 hour. 

It is important to note that dalbavancin should be used with caution in patients with a history of anaphylaxis or other severe allergic reactions to glycopeptide antibiotics and patients with renal impairment. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: dalbavancin 

Pronounced: [ DAL-ba-VAN-sin] 

Why do we use dalbavancin? 

It is an antibiotic used to treat acute bacterial skin and skin structure infections (ABSSSI) caused by sensitive strains of Gram-positive bacteria.