Every day, humans encounter a multitude of pathogens, increasing the risk of infectious diseases. It is crucial for healthcare providers to accurately identify the responsible organisms during an infection.
This ensures that the appropriate medications can be prescribed promptly and effectively. Fortunately, in cases of bacterial infections, there are several antibiotic options available.
The healthcare provider will select the most suitable antibiotic based on the specific type of bacteria or infection being treated.
In 2017, within the European Union/European Economic Area, cephalosporins accounted for 11.6% of antibiotic usage in the community.
Among these, first generation cephalosporins are frequently prescribed, especially for simple skin infections or common bacterial organisms.
While they have been in use the longest among the cephalosporin groups, they remain highly effective.
What are cephalosporins?
Cephalosporins are a class of antibiotics falling under the category of beta-lactams, effectively combating various bacterial infections.
They work by disrupting bacterial cell wall construction, resulting in direct bacterial elimination.
Cephalosporin generations are categorized into five generations, distinguished by their bacterial coverage and development period.
First-generation, like Keflex (cephalaxin), targets easily treatable infections. In contrast, later generations are reserved for more severe cases.
Administration can be oral or via intravenous injection, depending on the nature of the infection.
Since the discovery of the first cephalosporin classification in 1945, structural enhancements have broadened their spectrum against bacteria, leading to five distinct generations.
Most bear names starting with cef, ceph, or kef, though note that this classification may vary by country.
What are first generation cephalosporins?
First generation cephalosporins belong to the initial class of cephalosporin antibiotics, a type falling under the beta-lactam category.
Currently, five generations of cephalosporins have been developed, all originating from the mold Acremonium.
These cephalosporins typically come in two forms: oral and parenteral preparations.
Orally administered ones are generally reserved for milder, uncomplicated infections, while the parenteral forms are employed for more severe cases, ensuring a swifter resolution of the infection.
Being classified as bactericidal and broad-spectrum antibiotics, first-generation cephalosporins possess the capability to effectively combat a wide array of susceptible bacteria.
These antibacterial agents, pioneers in their class, remain highly favoured choices, even with the availability of newer generations on the market.
They are particularly valuable in treating uncomplicated gram-positive bacterial infections and are often the top choice for surgical prophylaxis.
Other Cephalosporin Generations
There are four other cephalosporin generations, these include:
Second-Generation Cephalosporins
These antibiotics were created to tackle a wider range of bacteria, particularly those that are gram-negative.
They work against bugs like H. influenza, Bacteroides species, and more. Examples include cefuroxime, cefprozil, and others.
Third-Generation Cephalosporins
These are versatile antibiotics effective against various organisms like H. influenza and Streptococcus pneumoniae.
They're crucial in treating conditions like meningitis. Examples include cefotaxime, cefdinir, and others.
Fourth-Generation Cephalosporin (Cefepime)
This is a potent antibiotic reserved for serious cases involving both gram-positive and gram-negative bacteria.
It's the only fourth-generation cephalosporin approved by the FDA.
Fifth-Generation Cephalosporin (Ceftaroline)
This is the most powerful type, offering broad coverage against bacteria, including MRSA and Listeria monocytogenes. It's a strong choice for treating a wide range of infections.
How Do First Generation Cephalosporins Work?
First-generation cephalosporins, a broad category of antibiotics, function through their beta-lactam rings.
These rings bind to the penicillin-binding protein present in various bacteria, hindering crucial activities like cell wall synthesis.
Targeting Peptidoglycan: Cephalosporin Mode of Action
Cephalosporins also impede an enzyme called peptidoglycan within the bacterial cell wall, further disrupting cell wall synthesis and leading to bacterial demise.
While effective in most bodily fluids, they are less potent in cerebrospinal fluid, where higher generations are preferred. Intracellular fluid and vitreous-humor are less receptive to cephalosporins.
Risk of Resistance with First-Generation Cephalosporins
Due to their widespread use, first-generation cephalosporins face a higher risk of bacterial resistance.
Staphylococcus aureus, notorious for such resistance, often adapts by modifying genes in the penicillin-binding protein.
This alteration prevents the antibiotic's beta-lactam rings from inactivating the protein, allowing the bacteria's cell wall to remain intact.
Beta-Lactamase and MRSA
Staphylococcus aureus can also produce an enzyme known as beta-lactamase.
This enzyme hinders the attachment of cephalosporin's beta-lactam ring to penicillin-binding proteins, resulting in resistance, termed methicillin-resistant Staphylococcus aureus (MRSA).
Currently, only fifth-generation cephalosporins remain effective against MRSA.
Enhancing Activity Against Resistant Bacteria
To expand their efficacy against resistant strains, cephalosporins incorporate beta-lactamase inhibitors into their formulations.
Examples include ceftazidime-avibactam and ceftolozane-tazobactam.
Uses of First Generation Cephalosporins
First generation cephalosporins are effective against a range of conditions, including:
- Bacterial endocarditis prevention
- Bladder infection
- Bone infection
- Gallstone inflammation
- Endocarditis
- Impetigo
- Joint infection
- Kidney infections
- Ear infection (otitis media)
- Abdominal wall inflammation
- Pharyngitis
- Pneumonia
- Prevention of birth infections associated with Group B Streptococcal disease
- Prostatitis
- Sepsis
- Skin infection
- Soft tissue infection
- Post-surgical infection prevention
- Tonsillitis
- Upper respiratory tract infection
- Urinary tract infection
Target Bacteria
First generation cephalosporins are most effective against gram-positive bacteria, specifically staphylococci or streptococci.
They have limited efficacy against gram-negative bacteria, which are typically addressed by higher generations.
Notably, the gram-negative organisms susceptible to first-generation cephalosporins are Escherichia coli (E. coli), Proteus mirabilis, and Klebsiella pneumoniae.
While first-generation cephalosporins are valuable, they do have certain limitations. They are not effective against enterococci and methicillin-resistant staphylococci.
Therefore, in cases involving these bacteria, alternative treatments are required.
Allergy Considerations
For individuals with a penicillin allergy, first-generation cephalosporins serve as a suitable alternative.
However, it is important to exercise caution if there has been a severe anaphylactic reaction to previous penicillin use, as these antibiotics may not be the best option.
First generation cephalosporins cost in Pakistan
Affordability and Accessibility
Due to their long-standing presence in the pharmaceutical market, first-generation cephalosporins are readily available and relatively inexpensive.
This accessibility makes them a viable initial choice for treatment.
Price Range
The cost of first-generation cephalosporins can vary, accommodating different budgets.
Prices start at approximately Rs.80 for a prescription and may go up to Rs.500.
Considerations
When considering treatment options, the affordability of first-generation cephalosporins makes them a practical choice for addressing certain bacterial infections effectively.
It is recommended to consult a healthcare professional for personalized advice on medication selection.
Frequently Encountered Side Effects of First Generation Cephalosporins
It's important to be mindful of potential side effects when taking any medication. Here are some commonly observed side effects associated with first-generation cephalosporins:
- Diarrhea
- Dizziness
- Vomiting
- Nausea
- Abdominal pain
- Reduced appetite
- Thrombophlebitis
- Elevated liver enzyme levels
- Hives
- Headache
- Oral thrush
- Elevated eosinophil counts
- Rash
- Pruritus (itchy skin)
Limitations for First Generation Cephalosporins:
- Allergic Reactions: If you've had an allergic reaction to any medication, it's best to avoid first-generation cephalosporins to prevent potential adverse effects.
- Penicillin Anaphylaxis: If you've had a severe reaction to penicillin before, it's advisable to avoid first-generation cephalosporins to ensure your well-being.
- Kidney Disease: Individuals with kidney disease should refrain from using first-generation cephalosporins, as it may worsen the condition or lead to unwanted side effects.
- History of Antibiotic-Associated Colitis: If you've experienced antibiotic-associated colitis in the past, it's recommended to steer clear of first-generation cephalosporins to reduce the risk of recurrence.
- Gastrointestinal Disorders: Those with a history of gastrointestinal disorders should use first-generation cephalosporins with caution, as there may be potential interactions leading to complications.
- Seizure Disorder History: Individuals with a history of seizure disorders should avoid using first-generation cephalosporins, as it may worsen the condition or lead to undesirable side effects.
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FAQs
What are first generation antibiotics?
First generation antibiotics, also known as natural penicillins, are bactericidal substances originally extracted from Penicillium chrysogenum mold. They possess a fundamental structure comprising a thiazolidine ring linked to a beta-lactam ring, along with a variable side chain.
What is cephalosporins mechanism of action?
Cephalosporin's mode of action closely resembles that of penicillins.
It functions by binding to penicillin-binding proteins, disrupting cell wall enzymes.
The primary adverse reactions associated with cephalosporins mirror those observed with penicillin.
What are the differences between first generation cephalosporins?
First-generation cephalosporins, such as cefadroxil (Duricef) and cephalexin (Keflex), can be taken orally.
On the other hand, cefazolin (Ancef) is administered through injection (IV/IM).
Additionally, these cephalosporins vary in their dosing frequency. Please note that cephadrine has been discontinued.
Are first-generation cephalosporins safe to use?
Yes, first-generation cephalosporins are considered a safe choice for antimicrobial treatment. They have low toxicity levels, typically causing only mild gastrointestinal side effects.
Due to their favorable risk-benefit profile, both patients and healthcare providers often prefer these antibiotics.
Are first-generation cephalosporins controlled substances?
First-generation cephalosporin antibiotics are not classified as controlled substances.
They are non-addictive and do not carry a risk of dependency when used for bacterial infections.
Are first-generation cephalosporin antibiotics safe to use while pregnant or breastfeeding?
During pregnancy, first-generation cephalosporin antibiotics are considered safe and do not pose harm to the fetus.
However, research suggests that these antibiotics can be transmitted through breast milk to infants, potentially causing gastrointestinal discomfort.
Therefore, it's advisable to avoid them while breastfeeding.