RECARBRIO Powder for solution for injection Ref.[90474] Active ingredients: Cilastatin Imipemide Imipenem, Cilastatin and Relebactam

RECARBRIO (imipenem, cilastatin, and relebactam) for injection is an antibacterial combination product consisting of imipenem, a carbapenem antibacterial drug, cilastatin, a renal dehydropeptidase inhibitor, and relebactam, a diazabicyclooctane beta-lactamase inhibitor, for intravenous administration.

Imipenem

Imipenem is a beta lactam antibacterial drug. Imipenem (N-formimidoylthienamycin monohydrate) is a crystalline derivative of thienamycin, which is produced by Streptomyces cattleya. The chemical name is (5R,6S)3[[2-(formimidoylamino)ethyl]thio]6[(R)-1-hydroxyethyl]-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid monohydrate. It is an off-white, non-hygroscopic crystalline compound, sparingly soluble in water. The empirical formula is C₁₂H₁₇N₃O₄S∙H₂O and the molecular weight is 317.37.

Figure 1. Chemical structure of imipenem:

Cilastatin

Cilastatin sodium is the sodium salt of a derivatized heptenoic acid. The chemical name is sodium (Z)7[[(R)-2-amino-2-carboxyethyl]thio]2[(S)-2,2-dimethylcyclopropanecarboxamido]-2-heptenoate. It is an off-white to white, hygroscopic, amorphous compound, very soluble in water. The empirical formula is C₁₆H₂₅N₂NaO₅S and the molecular weight is 380.44.

Figure 2. Chemical structure of cilastatin sodium:

Relebactam

Relebactam is a beta-lactamase inhibitor. It is a crystalline monohydrate. The chemical name is (1R,2S,5R)-7-oxo-2-(piperidin-1-ium-4-ylcarbamoyl)-1,6-diazabicyclo[3.2.1]octan-6-yl sulfate hydrate. It is a white to off-white powder, soluble in water. The empirical formula is C₁₂H₂₀N₄O₆S∙H₂O and the molecular weight is 366.39.

Figure 3. Chemical structure of relebactam:

RECARBRIO is supplied as a white to light yellow sterile powder for constitution in a single-dose vial containing 500 mg imipenem (equivalent to 530 mg imipenem monohydrate), 500 mg cilastatin (equivalent to 531 mg cilastatin sodium), and 250 mg relebactam (equivalent to 263 mg relebactam monohydrate). Each vial of RECARBRIO is buffered with 20 mg sodium bicarbonate to provide solutions in the pH range of 6.5 to 7.6. The total sodium content of the mixture in the vial is 37.5 mg (1.6 mEq). Solutions of RECARBRIO range from colorless to yellow. Variations of color within this range do not affect the potency of the product.