1 The importance of the pharmaceutical industry in our country is increasing, and the Turkish pharmaceutical sector is changing both in parallel with global developments and within the framework of the health transformation plan.
2 Within the framework of Good Manufacturing Practices (GMP) determined by the World Health Organization and in force since 1984, Akyurt Pharma has made the necessary investments, strengthened its technological infrastructure, and reached a technological level comparable to EU countries.
3 International norms and standards are applied at Akyurt Pharma, and pharmaceutical manufacturing facilities are strictly inspected by the Ministry of Health.
AKYURT PHARMA was established to manufacture sterile injectable cephalosporins and solvent ampoules. As a strong player in the pharmaceutical industry, we manufacture ceftriaxone vials and solvent ampoules, which are among the most widely used products in both Turkey and worldwide.
Cephalosporins are a widely used group of antibiotics today. While first- and second-generation cephalosporins have stronger activity against gram-positive organisms, third-generation cephalosporins predominantly have activity against gram-negative organisms. Cephalosporins are also suitable for outpatient parenteral treatment principles.
They are effective in respiratory tract infections, urinary system infections, soft tissue infections, bone and musculoskeletal system infections, central nervous system infections, bacteremia, and gonorrhea. Cephalosporins are bactericidal, resistant to beta-lactamase, have good distribution into body tissues, and can be used both orally and parenterally.
PHARMACOKINETIC PROPERTIES OF CEPHALOSPORINS
First-generation cephalosporins are not resistant to acid and their absorption is insufficient. They cannot be taken orally. In general, 2nd, 3rd, and 4th generation cephalosporins can be used orally.
Compared to penicillins, they penetrate most tissues better.
Third- and fourth-generation cephalosporins can enter the CSF in inflamed conditions at concentrations sufficient to create therapeutic levels and can be used in the treatment of meningitis.
Most are excreted by the kidneys without being metabolized, via glomerular filtration or tubular secretion.
The antibacterial activity of their desacetyl metabolites is the same as the parent compounds.
They bind to plasma proteins at varying rates.
Highest binding (75–96%): Cefoperazone, Cefazolin, Ceftriaxone
Lowest binding (20% or less): Cefadroxil, Cephalexin
THE GENERAL IMPORTANCE OF CEPHALOSPORINS COMPARED TO OTHER ANTIBIOTICS
Except for broad-spectrum third-generation cephalosporins, the most important feature of cephalosporins is that they are BACTERICIDAL drugs that can replace penicillins in some patients with penicillin allergy or in Staphylococcus aureus infections that produce penicillinase. However, the existence of cheaper drugs such as erythromycin, co-trimoxazole (trimethoprim + sulfamethoxazole), and tetracyclines— which can replace penicillins—reduces the value of cephalosporins as an alternative to penicillin.
Also, as with penicillins, there are very few cephalosporin derivatives that are the most preferred antibiotic for a specific type of infection.
ANTIBACTERIAL SPECTRUM OF CEPHALOSPORINS
Generally effective against gram (+) cocci and gram (–) bacilli.
First-generation cephalosporins have a more limited spectrum compared to others; they are effective against gram (+) bacteria.
They are resistant to penicillinase secreted by Staphylococcus aureus.
Second- and third-generation cephalosporins are less active against gram (+) bacteria.
Second-generation cephalosporins are effective against Haemophilus influenzae.
First- and second-generation cephalosporins have no antipseudomonal effect.
Among the gram (–) bacilli in the Enterobacteriaceae group—E. coli, Proteus mirabilis, and Klebsiella— all three are susceptible to cephalosporins across all generations.
Third-generation cephalosporins are also effective against Pseudomonas aeruginosa.
Fourth-generation cephalosporins are compounds effective against gram (+) microorganisms in a broader spectrum like first-generation cephalosporins; they have greater resistance to beta-lactamases than third-generation cephalosporins, can cross the blood–brain barrier, and are effective in meningitis.
OBTAINING CEPHALOSPORINS
Starting from Cephalosporium culture, it is possible to prepare cephalosporins by applying the methods and processes generally used to obtain other naturally derived antibiotics (penicillins). Synthetic derivatives are obtained starting from 7-ACA.
Classification based on chronological order and antibacterial spectrum:
First-generation cephalosporins (First discovered = Basic cephalosporins)
Second-generation cephalosporins (Transition cephalosporins)
Third-generation cephalosporins (Broad-spectrum cephalosporins)
Fourth-generation cephalosporins
Fifth-generation cephalosporins