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Nafcillin | CAS No: 147-52-4 | GMP-certified suppliers
A medication that treats systemic infections caused by penicillinase-producing Staphylococcus, providing targeted antibacterial therapy against methicillin-sensitive strains.
Therapeutic categories
Primary indications
- Indicated in the treatment of infections caused by penicillinase-producing staphylococci which have demonstrated susceptibility to the drug
Product Snapshot
- Nafcillin is available as injectable formulations including powder for solution, lyophilized powder, and ready-to-use solutions for intravenous and intramuscular administration
- It is primarily used for the treatment of infections caused by penicillinase-producing staphylococci with demonstrated drug susceptibility
- Nafcillin holds approved status in the US and Canada, with additional investigational uses under review
Clinical Overview
Pharmacodynamically, nafcillin is derived from 6-aminopenicillanic acid and retains activity against both penicillinase-producing and non-penicillinase-producing staphylococci. Its mechanism of action involves the inhibition of bacterial cell wall synthesis during active bacterial multiplication. Nafcillin binds covalently to penicillin-binding proteins (PBPs) which are essential for the transpeptidation step in peptidoglycan crosslinking. This binding inhibits the enzymatic functions of transpeptidase and carboxypeptidase, thereby preventing crosslink formation critical for bacterial cell wall integrity and resulting in bactericidal effects.
Key absorption, distribution, metabolism, and excretion (ADME) characteristics include metabolism predominantly by the liver and elimination via biliary and renal pathways. Nafcillin is also noted for its induction of multiple cytochrome P450 isoenzymes, including CYP1A2, CYP3A, and CYP3A4, which may impact the metabolism of concomitant drugs.
Safety considerations include hypersensitivity reactions typical of beta-lactam antibiotics, potential nephrotoxicity, and risk of superinfection with prolonged use. Monitoring for adverse effects and drug interactions is advised in clinical use.
Notable pharmaceutical preparations of nafcillin are indicated predominantly for systemic infections due to susceptible staphylococci. It is recognized as a first-line option for MSSA bacteremia and related infections in various international treatment guidelines.
For API procurement, quality attributes such as consistent potency, absence of impurities, and compliance with pharmacopeial standards are critical. Given nafcillin’s potential for enzymatic induction and sensitivity to degradation, sourcing from manufacturers with robust process controls and validated analytical methods is recommended to ensure suitability for pharmaceutical formulation.
Identification & chemistry
| Generic name | Nafcillin |
|---|---|
| Molecule type | Small molecule |
| CAS | 147-52-4 |
| UNII | 4CNZ27M7RV |
| DrugBank ID | DB00607 |
Pharmacology
| Summary | Nafcillin is a semisynthetic penicillin antibiotic targeting penicillin-binding proteins (PBPs) involved in bacterial cell wall synthesis. It exerts bactericidal activity by inhibiting transpeptidase and carboxypeptidase enzymes, preventing cell wall crosslinking in actively dividing bacteria. Nafcillin is effective against penicillinase-producing and non-penicillinase-producing Staphylococcus species. |
|---|---|
| Mechanism of action | Like other penicillins, nafcillin exerts a bactericidal action against penicillin-susceptible microorganisms during the state of active multiplication in the bacterial cell wall synthesis. It inhibits the biosynthesis of the bacterial cell wall by forming covalent bonds with penicillin-binding proteins that play a critical role in the final transpeptidation process. Binding to penicillin-binding proteins inhibits the transpeptidase and carboxypeptidase activities conferred by these proteins and prevents the formation of the crosslinks . |
| Pharmacodynamics | Nafcillin is a semisynthetic antibiotic substance derived from 6-amino-penicillanic acid. The drugs in this class are highly resistant to inactivation by staphylococcal penicillinase and are active against penicillinase-producing and non penicillinase-producing strains of Staphylococcus species. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Penicillin-binding protein 1b | Streptococcus pneumoniae (strain ATCC BAA-255 / R6) | inhibitor |
| Penicillin-binding protein 2B | Streptococcus pneumoniae (strain ATCC BAA-255 / R6) | inhibitor |
| Penicillin-binding protein 2a | Streptococcus pneumoniae (strain ATCC BAA-255 / R6) | inhibitor |
ADME / PK
| Absorption | Following intravenous administration of 500mg nafcillin, the mean plasma concentration was approximately 30 µg/mL. This value was reached after 5 minutes of injection. |
|---|---|
| Half-life | The serum half-life of nafcillin administered by the intravenous route ranged from 33 to 61 minutes as measured in three separate studies. |
| Protein binding | The degree of nafcillin binding to serum proteins is 89.9 ± 1.5%, where it is mainly bound to albumin. |
| Metabolism | Hepatic metabolism accounts for less than 30% of the biotransformation of most penicillins. |
| Route of elimination | Nafcillin is primarily eliminated by non-renal routes, namely hepatic inactivation and excretion in the bile. |
| Volume of distribution | Nafcillin is reported to be widely distributed in various body fluids, including bile, pleural, amniotic and synovial fluids. |
Formulation & handling
- Nafcillin is a small molecule primarily formulated for intravenous and intramuscular injection, not for oral use.
- Although classified as a dipeptide derivative, it is chemically stable in solid form and used as powder or solution for injection.
- Oral absorption is variable and should be administered on an empty stomach to avoid interaction with food.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient (API) has patents expiring in the US and Canada within the next 12 months, indicating an approaching transition to generic competition. As a result, the market is expected to mature with increased availability of generic alternatives. |
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| Markets | US, Canada |
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Supply Chain
| Supply chain summary | Nafcillin is produced by multiple manufacturers, including originator and generic companies, indicating a competitive supply environment. Its branded products are primarily available in the US and Canada markets. The presence of several manufacturers and generic packagers suggests that patent expirations have allowed for existing generic competition. |
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Safety
| Toxicity | Serious toxicity is unlikely following large doses of nafcillin. Acute ingestion of large doses of nafcillin may cause nausea, vomiting, diarrhea and abdominal pain. Acute oliguric renal failure and hematuria may occur following large doses. The oral LD50 in rats is >5000mg/kg and the intravenous LD50 in rats is >1000mg/kg [MSDS]. |
|---|
- 1
- Nafcillin exhibits low acute toxicity with oral LD50 ›5000 mg/kg and intravenous LD50 ›1000 mg/kg in rats
- 2
Nafcillin is a type of Penicillins
Penicillins belong to the subcategory of pharmaceutical active pharmaceutical ingredients (APIs) and play a crucial role in the treatment of various bacterial infections. They are a class of antibiotics derived from the fungus Penicillium, and are widely used in the pharmaceutical industry.
Penicillins exert their antibacterial effect by inhibiting the formation of bacterial cell walls. They target a specific enzyme, called transpeptidase, which is responsible for cross-linking the peptidoglycan chains in the bacterial cell wall. By blocking this process, penicillins weaken the cell wall, leading to its rupture and subsequent bacterial death.
These APIs are classified into several subclasses, such as penicillin G, penicillin V, and extended-spectrum penicillins. Each subclass has unique characteristics and mechanisms of action. Penicillin G, for example, is effective against a broad range of Gram-positive bacteria, while penicillin V is primarily used for oral administration.
The pharmaceutical industry produces penicillins through a fermentation process using Penicillium strains. The obtained penicillin products are then isolated, purified, and formulated into different dosage forms, including tablets, capsules, and injectables.
Penicillins have been instrumental in the treatment of various infections, including respiratory, skin, urinary tract, and sexually transmitted infections. However, it's essential to note that some bacteria have developed resistance to penicillins through different mechanisms, such as the production of beta-lactamases. As a result, pharmaceutical companies have developed combination therapies and modified penicillins to combat antibiotic resistance effectively.
In summary, penicillins are a vital subcategory of pharmaceutical APIs that provide effective treatment options for bacterial infections. Their diverse subclasses, mechanisms of action, and formulations contribute to their widespread use in the medical field.
Nafcillin (Penicillins), classified under Antibacterials
Antibacterials, a category of pharmaceutical active pharmaceutical ingredients (APIs), play a crucial role in combating bacterial infections. These APIs are chemical compounds that target and inhibit the growth or kill bacteria, helping to eliminate harmful bacterial pathogens from the body.
Antibacterials are essential for the treatment of various bacterial infections, including respiratory tract infections, urinary tract infections, skin and soft tissue infections, and more. They are commonly prescribed by healthcare professionals to combat both mild and severe bacterial infections.
Within the category of antibacterials, there are different classes and subclasses of APIs, each with distinct mechanisms of action and target bacteria. Some commonly used antibacterials include penicillins, cephalosporins, tetracyclines, macrolides, and fluoroquinolones. These APIs work by interfering with various aspects of bacterial cellular processes, such as cell wall synthesis, protein synthesis, DNA replication, or enzyme activity.
The development and production of antibacterial APIs require stringent quality control measures to ensure their safety, efficacy, and purity. Pharmaceutical manufacturers must adhere to Good Manufacturing Practices (GMP) and follow rigorous testing protocols to guarantee the quality and consistency of these APIs.
As bacterial resistance to antibiotics continues to be a significant concern, ongoing research and development efforts aim to discover and develop new antibacterial APIs. The evolution of antibacterials plays a crucial role in combating emerging bacterial strains and ensuring effective treatment options for infectious diseases.
In summary, antibacterials are a vital category of pharmaceutical APIs used to treat bacterial infections. They are designed to inhibit or kill bacteria, and their development requires strict adherence to quality control standards. By continually advancing research in this field, scientists and pharmaceutical companies can contribute to the ongoing battle against bacterial infections.
Nafcillin API manufacturers & distributors
Compare qualified Nafcillin API suppliers worldwide. We currently have 2 companies offering Nafcillin 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 |
|---|---|---|---|---|---|
| ACS Dobfar | Producer | Italy | Italy | CoA, USDMF | 36 products |
| Corden Pharma | Producer | Germany | Italy | CoA, GMP, USDMF | 45 products |
When sending a request, specify which Nafcillin 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.).
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