vaborbactam

Action and Spectrum

Actions and spectrum: 

Vaborbactam is a non-beta-lactam beta-lactamase inhibitor. It works by inhibiting certain types of beta-lactamases, enzymes produced by some bacteria that can inactivate beta-lactam antibiotics. This allows vaborbactam to restore the activity of beta-lactam antibiotics, such as meropenem, against resistant bacteria.

Vaborbactam’s spectrum of activity is against beta-lactamase-producing bacteria, helping to enhance the effectiveness of beta-lactam antibiotics against these resistant strains. It is often used in combination with antibiotics like meropenem to treat various infections caused by multidrug-resistant bacteria. 

Drug Interaction

Adverse Reaction

Frequency defined 

1-10% 

Phlebitis (4.4%) 

Hypersensitivity (1.8%) 

Increased ALT (1.8%) 

Pyrexia (1.5%) 

Headache (8.8%) 

Diarrhea (3.3%) 

Nausea (1.8%) 

Increased AST (1.5%) 

Hypokalemia (1.1%)  

>1% 

Leukopenia 

Pharyngitis 

Oral candidiasis 

Decreased appetite 

Hyperglycemia 

Dizziness 

Paresthesia 

Hallucination 

Azotemia 

Deep vein thrombosis 

Vascular pain 

Hypotension 

Renal impairment 

Insomnia 

Lethargy 

Tremor 

Hypoglycemia 

Hyperkalemia 

Vulvovaginal candidiasis 

Chest discomfort 

Black Box Warning

Black Box Warning: 

There were no specific black box warnings associated with vaborbactam. 

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

• Allergy/Hypersensitivity: Contraindicated in individuals with a known hypersensitivity or allergy to vaborbactam or any of its components. 
• Renal Impairment: Use with caution or avoid in patients with severe renal impairment, as dosing adjustments may be necessary. 
• Pregnancy and Lactation: The use of vaborbactam during pregnancy or while breastfeeding should be carefully considered and discussed with a healthcare provider. 
• Drug Interactions: Contraindications can also be influenced by potential drug interactions. Avoid concomitant use with drugs that may interact adversely with vaborbactam. 
• Age Restrictions: There may be age-related contraindications, such as restrictions on use in pediatric or elderly populations, depending on the specific formulation and indication.

Caution: 

• Hepatic Function: Vaborbactam is primarily excreted in the urine, and hepatic metabolism is minimal. However, monitoring hepatic function may still be important, especially in patients with compromised liver function. 
• Pediatric and Geriatric Patients: Special caution may be required when using vaborbactam in pediatric or geriatric populations. Dosing adjustments, if necessary, should be made with consideration of age-related differences. 
• Central Nervous System Effects: Some patients may experience central nervous system (CNS) side effects while taking medications. These effects might include dizziness or confusion. Caution is advised when driving or operating heavy machinery until the patient’s response to the medication is known. 
• Coagulation Abnormalities: In rare cases, antibiotics may impact blood coagulation. If a patient has a history of bleeding disorders or is taking anticoagulant medications, use vaborbactam cautiously.

Comorbidities: 

• Diabetes: Patients with uncontrolled diabetes may be more susceptible to the types of bacterial infections, particularly skin and soft tissue infections. Vaborbactam may be used in these cases, and glycemic control is important for optimal recovery. 
• Immunosuppression: Individuals with conditions that weaken their immune system, such as HIV/AIDS, organ transplantation, or cancer, may be more vulnerable to severe bacterial infections. Vaborbactam, in combination with other antibiotics, may be used in this population. 
• Respiratory Conditions: Patients with chronic respiratory conditions like chronic obstructive pulmonary disease (COPD) or bronchiectasis may be at risk of bacterial lung infections. Vaborbactam may be part of the treatment regimen in these cases. 
• Cardiovascular Disease: Patients with heart conditions, particularly prosthetic heart valves or congenital heart defects, may be at risk for bacterial endocarditis. Vaborbactam and other antibiotics might be used for prophylaxis or treatment. 

Pregnancy / Lactation

Pregnancy consideration: pregnancy category: not assigned 

Lactation: excreted into human milk: 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 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: 

Vaborbactam is a non-beta-lactam beta-lactamase inhibitor, often used in combination with antibiotics to treat serious bacterial infections. Its pharmacology revolves around its ability to inhibit the activity of certain bacterial enzymes known as beta-lactamases, which are responsible for antibiotic resistance in many bacteria.

By blocking these enzymes, vaborbactam restores the effectiveness of beta-lactam antibiotics like piperacillin. This combination allows for the treatment of a broader spectrum of bacteria, including those that would otherwise be resistant to treatment. Vaborbactam’s role in therapy enhances the antibiotic’s potency and extends its utility in the fight against multidrug-resistant bacterial infections.  

Pharmacodynamics: 

The pharmacodynamics of vaborbactam primarily involves its mechanism of action as a beta-lactamase inhibitor. Beta-lactamases are enzymes produced by many bacteria to break down and inactivate beta-lactam antibiotics, rendering them ineffective. Vaborbactam acts as a competitive inhibitor of these enzymes, meaning it competes with the antibiotic for binding to the beta-lactamase.

This inhibition effectively neutralizes the beta-lactamase’s activity, allowing the beta-lactam antibiotic, such as piperacillin, to exert its bactericidal effects. By doing so, vaborbactam broadens the spectrum of antibiotic coverage and enhances the antibacterial activity of the combined antibiotics. This pharmacodynamic synergy is especially valuable in treating infections caused by multidrug-resistant bacteria and those involving extended-spectrum beta-lactamase (ESBL) or AmpC beta-lactamase-producing organisms.  

Pharmacokinetics: 

Absorption 

Vaborbactam is administered intravenously, and it is rapidly distributed throughout the bloodstream. 

Distribution 

Vaborbactam is distributed into various body tissues and fluids, including the plasma. It has a small volume of distribution (Vd), indicating that it remains primarily within the vascular compartment. 

Metabolism 

Vaborbactam itself is not significantly metabolized. It acts primarily as a beta-lactamase inhibitor and does not undergo substantial metabolic transformations in the body. 

Elimination and excretion 

Vaborbactam is primarily eliminated via renal excretion. It is excreted in the urine, and its elimination half-life is short, typically around 2 to 3 hours. Renal function is crucial for the efficient removal of vaborbactam from the body. 

Adminstartion

Administration: 

vaborbactam is available as a lyophilized powder, it must be reconstituted with a compatible IV diluent according to the manufacturer’s instructions. After reconstitution, the vaborbactam solution is often further diluted to a specific concentration to ensure safe and effective administration.

The appropriate dilution instructions can be found in the product labelling. The diluted vaborbactam solution is administered as a slow intravenous infusion. The infusion rate and duration will depend on the product and the clinical condition it is used to treat. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: vaborbactam 

Pronounced: (vah-BOR-bak-tam)  

Why do we use vaborbactam? 

Vaborbactam, when combined with piperacillin, is used to treat complicated intra-abdominal infections. These infections can involve various structures within the abdominal cavity, including the appendix, colon, and peritoneum. Vaborbactam in combination with piperacillin is used for the treatment of complicated urinary tract infections, including pyelonephritis, which is a severe kidney infection. In some cases, vaborbactam is used to treat hospital-acquired or ventilator-associated pneumonia in patients who may have infections caused by multidrug-resistant bacteria.