High Quality Rifampicin CAS 13292-46-1 Bright-red crystalline powder with best price and fast delivery

Rifampicin More Info

Rifampicin, also known as rifampin, is a broad-spectrum antibiotic belonging to the rifamycin class. It is primarily used in the treatment of tuberculosis and other bacterial infections due to its potent bactericidal properties.

Mechanism of Action

Rifampicin exerts its antimicrobial effects by inhibiting bacterial DNA-dependent RNA polymerase (RNAP). It binds specifically to the beta-subunit of RNAP, which prevents the enzyme from synthesizing RNA by blocking the elongation process. This action occurs through a "steric-occlusion" mechanism, where rifampicin obstructs the path of the elongating RNA at its 5' end, effectively halting RNA synthesis at an early stage. Importantly, rifampicin selectively targets microbial RNAP and does not affect mammalian RNA polymerase, minimizing potential side effects in human cells

Applications

Tuberculosis: It is a cornerstone in the treatment regimen for both active and latent TB.
Leprosy: Used as part of combination therapy for this chronic infectious disease.
Staphylococcal infections: Effective against methicillin-resistant Staphylococcus aureus (MRSA) when used in combination with other antibiotics.
Meningococcal disease: It can be used to eradicate Neisseria meningitidis from carriers.
Legionnaires’ disease: Sometimes included in treatment protocols for this severe pneumonia caused by Legionella bacteria.

Routes of Administration

Rifampicin is administered orally and is available in capsule and tablet forms. It is recommended to take rifampicin on an empty stomach to enhance absorption; food can significantly reduce its bioavailability

Safety and Side Effects

While generally well-tolerated, rifampicin can cause several side effects, which may include:
Common Side Effects:
Orange or reddish discoloration of bodily fluids (tears, sweat, urine).
Gastrointestinal disturbances (nausea, vomiting, diarrhea).
Rash and itching.
Serious Side Effects:
Allergic reactions (hives, difficulty breathing).
Liver toxicity, which may manifest as jaundice or dark urine.
Severe gastrointestinal issues such as pseudomembranous colitis.
Monitoring liver function is recommended during prolonged therapy due to potential hepatotoxicity.

Pharmacokinetics

Absorption: Rapidly absorbed after oral administration; bioavailability can reach approximately 90% when taken on an empty stomach.
Distribution: Widely distributed throughout body tissues and fluids, including cerebrospinal fluid. Approximately 80% of rifampicin binds to plasma proteins.
Metabolism: Primarily metabolized in the liver to 25-desacetyl rifampicin, which retains some antibacterial activity. The drug induces its own metabolism via cytochrome P450 enzymes, leading to increased clearance with repeated dosing.
Half-life: The elimination half-life is about 4 hours.
Excretion: Most of the drug is excreted via bile into feces; only a small fraction (15-25%) is eliminated unchanged in urine.

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