sulopenem (Pending FDA Approval)

Action and Spectrum

Actions and Spectrum:

It works by inhibiting bacterial cell wall synthesis, leading to the death of susceptible bacteria. This mechanism of action is similar to that of other beta-lactam antibiotics, such as penicillins and cephalosporins. The spectrum of activity of sulopenem includes both Gram-positive and Gram-negative bacteria.

It is active against many common Gram-positive organisms, such as Streptococcus pneumoniae and Staphylococcus aureus (including methicillin-resistant strains), as well as many Gram-negative organisms, such as Escherichia coli, Klebsiella pneumoniae, and Pseudomonas aeruginosa.

sulopenem has also shown promising activity against some antibiotic-resistant bacteria, including carbapenem-resistant Enterobacteriaceae (CRE), which are often difficult to treat due to their resistance to many antibiotics. However, the exact spectrum of activity of sulopenem may vary depending on the specific bacterial strain and local resistance patterns.

Drug Interaction

Adverse Reaction

Frequency not defined

• Fever
• Abdominal pain
• Headache
• Diarrhea
• Nausea and vomiting
• Dizziness
• Skin rash or itching
• Clostridioides difficile infection
• Elevated liver enzyme
• Allergic reactions, such as swelling of the face, lips, tongue or throat, difficulty breathing, or hives.

Black Box Warning

Contraindication / Caution

Contraindication/Caution:

• Hypersensitivity: sulopenem is contraindicated in patients with a known hypersensitivity to sulopenem or any other carbapenem antibiotics. Hypersensitivity reactions can be severe, including anaphylaxis, which can be life-threatening.
• Seizures: sulopenem can lower the seizure threshold and cause seizures, especially in patients with a history of seizures or those who are taking other drugs that can lower the seizure threshold.
• Pregnancy and breastfeeding: The safety of sulopenem in pregnancy and breastfeeding has not been established. Therefore, it is not recommended to use sulopenem during pregnancy or breastfeeding unless the potential benefits outweigh the risks.
• Clostridium difficile-associated diarrhea (CDAD): sulopenem can cause CDAD, a severe and sometimes fatal condition, especially in elderly patients or those who are taking multiple antibiotics.
• Central nervous system disorders: sulopenem can cause central nervous system disorders such as confusion, hallucinations, and delirium, especially in elderly patients with underlying neurological conditions.
• Renal impairment: sulopenem is eliminated mainly by the kidneys, and its dosage should be adjusted in patients with renal impairment.

Pregnancy / Lactation

Pregnancy consideration:

Pregnancy category: N/A

Lactation: Excreted into human milk is unknown

Pregnancy category:

• Category A: well-controlled and Satisfactory studies do not show risk to the fetus in the first/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:

sulopenem administered intravenously (IV) is a thiopenem that exhibits extensive antibacterial properties against a wide range of gram-positive and gram-negative bacteria.

Pharmacodynamics:

Pharmacokinetics:

Absorption

sulopenem is administered intravenously, which means that it bypasses the absorption step in the ADME process. Upon intravenous administration, sulopenem achieves a peak plasma concentration within 30 minutes.

Distribution

sulopenem has a moderate volume of distribution, indicating that it distributes well throughout the body. It has a protein binding of approximately 20%, which is relatively low.

Metabolism

sulopenem undergoes minimal metabolism in the body. It is primarily eliminated unchanged in the urine.

Elimination and Excretion

sulopenem is primarily eliminated via renal excretion, with approximately 88% of the dose excreted unchanged in the urine within 24 hours of dosing. The half-life of sulopenem is approximately 2-3 hours in patients with normal renal function.

Adminstartion

Administration:

sulopenem is typically administered intravenously (IV) over a period of 30 minutes to 1 hour. The recommended dose for adults is 1 gram three times a day. The dose may be adjusted based on the severity of the infection, renal function, and other factors.

For patients with renal impairment, the dose of sulopenem may need to be adjusted. In patients with creatinine clearance (CrCl) of 30 to 50 mL/min, the dose should be reduced to 500 mg three times a day. For patients with CrCl below 30 mL/min or who require hemodialysis, the dose should be reduced to 250 mg three times a day.

sulopenem can be administered with or without food.Even if symptoms improve before completing the course, it is crucial to finish the full treatment regimen as prescribed by the healthcare provider.

It is also important to note that sulopenem is a prescription medication, and the administration of sulopenem should only be performed under the supervision of a licensed healthcare provider.

Patient Information Leaflet

Patient information leaflet

Generic Name: sulopenem (Pending FDA Approval)

Why do we use sulopenem?

sulopenem is a novel β-lactam antibiotic belonging to the penem class of antibiotics. It is being developed for the treatment of various bacterial infections, including complicated urinary tract infections, complicated intra-abdominal infections, and hospital-acquired pneumonia.