Cephalosporins; Types, Uses, Contraindications, Side Effects, Interactions,

Cephalosporins are a large group of B-lactam antibiotics that are closely related to the penicillins. Cephalosporins penetrate well into most body fluids and the ECF of most tissues, especially when inflammation (which enhances diffusion) is present. Cephalosporins are bactericidal and have the same mode of action as other β-lactam antibiotics (such as penicillins), but are less susceptible to β-lactamases. Mechanistically, they inhibit cell-wall synthesis and kill bacteria in a manner similar to the penicillins.

Types / Classification of Cephalosporins

Mechanism of Action of Cephalosporins

Cephalosporins are bactericidal and have the same mode of action as other β-lactam antibiotics (such as penicillins), but are less susceptible to β-lactamases. Cephalosporins disrupt the synthesis of the peptidoglycan layer forming the bacterial cell wall. The peptidoglycan layer is important for cell wall structural integrity. The final transpeptidation step in the synthesis of the peptidoglycan is facilitated by penicillin-binding proteins (PBPs). PBPs bind to the D-Ala-D-Ala at the end of muropeptides (peptidoglycan precursors) to crosslink the peptidoglycan. Beta-lactam antibiotics mimic the D-Ala-D-Ala site, thereby irreversibly inhibiting PBP crosslinking of peptidoglycan.

Indications of Cephalosporins

• Urinary Tract Infection – e.g. cystitis, cystourethritis, uncomplicated pyelonephritis.
• Otitis Media – Otitis caused by Haemophilus influenzae, Moraxella catarrhalis and Streptococcus pyogenes.
• Tonsillitis
• Bronchitis
• Sinusitis.
• Pharyngitis caused by Streptococcus pyogenes.
• Pneumonia caused by Streptococcus pneumoniae and Haemophilus influenzae.
• Typhoid fever.
• Enteric fever
• Gonorrhea
• Osteomyelitis
• Prevention of Chronic Kidney Disease (CKD) / Renal Hypodysplasia, Nonsyndromic
• Cervicitis, Vaginitis
• Acute bronchitis and acute exacerbations of chronic bronchitis caused by Streptococcus pneumoniae and Haemophilus influenzae
• Gonococcal Infection – Uncomplicated or Disseminated
• STD Prophylaxis
• Acute Bacterial Exacerbation of Chronic Bronchitis (ABECB)
• Bacterial Infections
• Bloodstream Infections
• Bone and Joint Infections
• Gonorrhea
• Impetigo
• Infected animal bite
• Lower Respiratory Tract Infection (LRTI)

Contraindications of Cephalosporins

• Clostridium difficile infection
• The decrease in the Blood-Clotting Protein Prothrombin
• Increased risk of bleeding due to the clotting disorder
• Liver problems
• Kidney disease with the reduction in kidney function
• Allergies to cephalosporins & beta-lactams
• Hypersensitivity to the active substance or to any of the excipients
• Patients with known hypersensitivity to cephalosporin antibiotics.
• History of severe hypersensitivity (e.g. anaphylactic reaction) to any other type of beta-lactam antibacterial agent (penicillins, monobactams, and carbapenems).

Side Effects Cephalosporins

The most common

• Constipation
• Diarrhea
• chest pain
• a headache
• joint painPain
• dizziness
• nausea and vomiting
• Severe stomach ache
• anorexia,
• flatulence,
• a headache,
• dizziness,
•  fainting, fast or pounding heartbeats.
• Jarisch/Herxheimer reaction. This is a short-term reaction seen after antibiotic treatment for certain diseases. Symptoms can include fever, chills, or muscle pain.

More common

• diarrhea
• fever
• the general feeling of illness or discomfort
• a headache
• itching of the vagina or genital area
• pain during sexual intercourse
• rigidity
• sweating
• thick, white vaginal discharge with no odor or with a mild odor

Less common

• Black, tarry stools
• chest pain
• a cough
• loose stools
• painful or difficult urination
• shortness of breath
• a sore throat
• sores, ulcers, or white spots on the lips or in the mouth
• swollen glands
• unusual bleeding or bruising
• unusual tiredness or weakness

Rare

• Back, leg, or stomach pains
• bladder pain
• bleeding gums
• bloody or cloudy urine
• body aches or pain
• burning while urinating
• difficulty with breathing
• ear congestion
• fast, pounding, or irregular heartbeat or pulse
• frequent urge to urinate
• loss of appetite
• lower back or side pain
• nasal congestion
• nausea or vomiting
• pain or tenderness around the eyes and cheekbones
• swelling of the joints
• the tightness of chest or wheezing
• white or brownish vaginal discharge
• white patches in the mouth or throat or on the tongue
• white patches with diaper rash
• yellowing of the eyes or skin
• Blistering, peeling, or loosening of the skin
• bloody, black, or tarry stools
• a cough or hoarseness
• fever with or without chills
• the general feeling of tiredness or weakness

Drug Interactions of Cephalosporins

Cephalosporins may interact with the following drugs, supplements & may change the efficacy of the drug

• aminoglycoside antibiotics (e.g., amikacin, gentamicin, tobramycin)
• antacids (e.g., aluminum hydroxide, calcium carbonate, magnesium hydroxide)
• H2 antagonists (e.g., famotidine, ranitidine)
• BCG
• BCG vaccine
• birth control pills
• probenecid
• sodium picosulfate
• typhoid vaccine
• warfarin

References

1. ClinicalTrials.gov
   https://clinicaltrials.gov/
2. https://en.wikipedia.org/wiki/Cephalosporin
3. https://www.drugs.com/drug-class/cephalosporins.html
4. PDB
   http://www.rcsb.org/ligand/REC
5. Wikipedia
   https://www.wikidata.org/wiki/Q27465008

   https://pubchem.ncbi.nlm.nih.gov

6. DrugBank
   http://www.drugbank.ca/drugs/DB03313#targets
   http://www.drugbank.ca/drugs/DB03313
7. FDA/SPL Indexing Data
   https://www.fda.gov/ForIndustry/DataStandards/SubstanceRegistrationSystem-UniqueIngredientIdentifierUNII/
8. https://www.webmd.com/drugs/2/drug-11757/cephalexin-oral/details
9. Human Metabolome Database (HMDB)
   http://www.hmdb.ca/metabolites/HMDB0060450
10. Wikipedia
    https://en.wikipedia.org/wiki/Cephalosporin_C
11. PubChem
    https://pubchem.ncbi.nlm.nih.gov
12. MeSH
    https://www.ncbi.nlm.nih.gov/mesh/67025163
    http://www.nlm.nih.gov/mesh/meshhome.html

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