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Cefalotin | CAS No: 153-61-7 | GMP-certified suppliers
A medication that prevents surgical infections and treats blood, bone, joint, respiratory, skin, and urinary tract infections with broad-spectrum antibacterial activity.
Therapeutic categories
Primary indications
- Used to prevent infection during surgery and to treat many kinds of infections of the blood, bone or joints, respiratory tract, skin, and urinary tract
Product Snapshot
- Cefalotin is a parenteral injectable small molecule antibiotic available as powder for solution and liquid solution formulations
- It is primarily used for prophylaxis in surgery and treatment of infections including blood, bone or joints, respiratory tract, skin, and urinary tract infections
- Cefalotin is approved for use in the Canadian market with both human and veterinary designations
Clinical Overview
The pharmacological activity of cefalotin derives from its inhibition of bacterial cell wall synthesis. It exerts this effect by binding with high affinity to penicillin-binding proteins (PBPs), which are transpeptidases essential for the cross-linking of peptidoglycan layers in the bacterial cell wall. This inhibition disrupts cell wall construction, leading to bacterial lysis and death.
Pharmacokinetically, cefalotin is typically administered via intravenous or intramuscular routes. It undergoes limited metabolism and is primarily eliminated renally through glomerular filtration and tubular secretion. Key absorption, distribution, metabolism, and excretion (ADME) parameters include rapid distribution to most body tissues and fluids. The half-life is generally short, necessitating frequent dosing to maintain therapeutic levels. Cefalotin is known to inhibit organic anion transporters OAT1 (SLC22A6) and OAT3 (SLC22A8), which may influence its renal clearance and interactions with other compounds.
Safety considerations include potential nephrotoxicity, hypersensitivity reactions typical of beta-lactam antibiotics, and the risk of lowering the seizure threshold. Caution is advised in patients with renal impairment or a history of penicillin allergy. The presence of an ester group at the 3'-position distinguishes cefalotin structurally and functionally within the cephalosporin class.
Cefalotin has been approved for human use worldwide and retains roles in veterinary medicine. Notable brand names and product formulations vary regionally.
When sourcing cefalotin active pharmaceutical ingredient (API), attention should be given to compliance with pharmacopeial standards, such as the United States Pharmacopeia (USP) or European Pharmacopeia (EP). API quality must ensure appropriate purity, sterility for parenteral use, and controlled levels of residual solvents and impurities. Reliable suppliers typically provide stability data supporting the formulation and shelf-life requirements of sterile injectable products.
Identification & chemistry
| Generic name | Cefalotin |
|---|---|
| Molecule type | Small molecule |
| CAS | 153-61-7 |
| UNII | R72LW146E6 |
| DrugBank ID | DB00456 |
Pharmacology
| Summary | Cefalotin is a first-generation cephalosporin antibiotic that exerts bactericidal effects by inhibiting penicillin-binding proteins (PBPs), key enzymes involved in bacterial cell wall synthesis. This inhibition disrupts peptidoglycan cross-linking, leading to impaired cell wall formation and bacterial cell death. Cefalotin demonstrates broad-spectrum activity against various bacterial pathogens and is administered parenterally for the treatment and prevention of diverse infections. |
|---|---|
| Mechanism of action | The bactericidal activity of cefalotin results from the inhibition of cell wall synthesis via affinity for penicillin-binding proteins (PBPs). The PBPs are transpeptidases which are vital in peptidoglycan biosynthesis. Therefore, their inhibition prevents this vital cell wall compenent from being properly synthesized. |
| Pharmacodynamics | Cefalotin (INN) or cephalothin (USAN) is a semisynthetic first generation cephalosporin having a broad spectrum of antibiotic activity that is administered parenterally. |
Targets
| Target | Organism | Actions |
|---|---|---|
| D-alanyl-D-alanine carboxypeptidase | Streptomyces sp. (strain R61) | inhibitor |
| Penicillin-binding protein 1A | Streptococcus pneumoniae (strain ATCC BAA-255 / R6) | inhibitor |
| Penicillin-binding protein 1b | Streptococcus pneumoniae (strain ATCC BAA-255 / R6) | inhibitor |
ADME / PK
| Half-life | 30 minutes |
|---|---|
| Protein binding | 65-80% |
| Metabolism | Metabolized to a less active desacetyl metabolite, although 50-75% of the drug is eliminated unchanged in the urine. |
Formulation & handling
- Cefalotin is formulated exclusively for parenteral administration, including intramuscular and intravenous routes.
- As a small molecule cephalosporin ester, it requires reconstitution from powder or lyophilized forms prior to injection.
- Low water solubility necessitates careful dissolution and handling to ensure complete solubilization before administration.
Regulatory status
| Lifecycle | The API patent has expired, allowing for generic competition in the Canadian market. The product is in a mature stage with multiple approved generics available. |
|---|
| Markets | Canada |
|---|
Supply Chain
| Supply chain summary | Cefalotin is manufactured by multiple originator companies, reflecting a diversified supplier base. Branded products are primarily present in the Canadian market, with various formulations available. Patent expiration has led to established generic competition, indicating widespread availability of non-branded alternatives. |
|---|
Safety
| Toxicity | Rat intravenous LD<sub>50</sub> is 4000 mg/kg. |
|---|
- Handle with appropriate personal protective equipment to prevent dermal and respiratory exposure
- Avoid release to the environment due to potential aquatic toxicity
- Store under recommended conditions to maintain chemical stability and minimize degradation
Cefalotin is a type of Cephalosporins
Cephalosporins are a class of pharmaceutical active ingredients (APIs) widely used in the field of antibiotics. They belong to the beta-lactam family, which also includes penicillins. Cephalosporins are derived from a fungus called Acremonium cephalosporium and are known for their potent antimicrobial properties.
These APIs are commonly used to treat a wide range of bacterial infections, including respiratory tract infections, skin and soft tissue infections, urinary tract infections, and even meningitis. Cephalosporins work by inhibiting the synthesis of bacterial cell walls, leading to the disruption of bacterial growth and ultimately their destruction.
Cephalosporins are classified into generations based on their antimicrobial spectrum and activity against specific bacteria. The first-generation cephalosporins are effective against Gram-positive bacteria, while subsequent generations show broader activity against both Gram-positive and Gram-negative bacteria.
Pharmaceutical companies manufacture cephalosporins in various formulations, including tablets, capsules, injectable solutions, and suspensions. They are often prescribed by healthcare professionals and are available under different brand names in the market.
It is important to note that like other antibiotics, cephalosporins should be used judiciously to prevent the development of antibiotic resistance. Proper dosage and adherence to treatment guidelines are crucial to maximize their effectiveness and minimize the risk of resistance.
In conclusion, cephalosporins are a vital category of APIs widely used in the treatment of bacterial infections. Their broad spectrum of activity and effectiveness make them an essential tool in modern medicine.
Cefalotin API manufacturers & distributors
Compare qualified Cefalotin API suppliers worldwide. We currently have 1 companies offering Cefalotin API, with manufacturing taking place in 1 different countries. Use the table below to review supplier type, countries of origin, certifications, product portfolio and GMP audit availability.
| Supplier | Type | Country | Product origin | Certifications | Portfolio |
|---|---|---|---|---|---|
| Antibióticos do Brasila | Producer | Brazil | Brazil | CoA, JDMF | 3 products |
When sending a request, specify which Cefalotin API quality you need: for example EP (Ph. Eur.), USP, JP, BP, or another pharmacopoeial standard, as well as the required grade (base, salt, micronised, specific purity, etc.).
Use the list above to find high-quality Cefalotin API suppliers. For example, you can select GMP, FDA or ISO certified suppliers. Visit our help page to learn more about sourcing APIs via Pharmaoffer.
