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What-are-cephalosporins

What are cephalosporins antibiotics used for?

Posted on  March 19, 2021, Edited by Jason, Category  

What are cephalosporins?

1. Definition

Cephalosporins are the general term for cephalosporin antibiotics. Cephalosporins are a class of antibiotics obtained by semi-synthetic modification of the side chain of natural cephalosporin C obtained by culturing Cephalosporins.

There are about 30 commonly used types, which are divided into one, two, three, four, and five generations according to the time of their invention and the difference in antibacterial properties.

In the antibiotic market, cephalosporin antibiotics occupies a large share, and their related intermediates also show considerable market potential. The most popular varieties of cephalosporin antibiotics include ceftriaxone sodium, cefazolin sodium, cefotaxime, ceftriaxone, cefoperazone and cefuroxime (ester), etc. The corresponding intermediates include 7-ACA, 7- ADCA, GCLE, Axamic acid, AE-active ester, triazine ring, tetrazolium acetic acid, thiotetrazole, HO-EPCP, methoxyamine hydrochloride, furan amine salt (SIMA) and chlorosulfonic acid isocyanate, etc.

2. History

The cephalosporin compound was first extracted in 1948 by the Italian scientist Giuseppe Brotzu from the cephalosporin in the drainage ditch of Sardinia. He discovered that these acremonium secreted some substances, which can effectively resist the typhoid bacillus that causes typhoid fever. The University of Oxford has successfully extracted cephalosporin C, which is stable to beta lactamase, but it is not effective enough for clinical use. Clavulanic acid is a new oxygen-containing nucleus beta lactam antibiotic produced by Streptomyces.

The core of cephalosporin is 7-aminocephalosporin (7-ACA for short), which is derived from cephalosporin C and has been confirmed to be similar to the core of penicillin (ie. 6-aminopenicillanic acid, 6-APA). The side chain of 7-ACA was modified and some very useful antibiotics were obtained. The first cephalothin was issued by Eli Lilly in 1964.

3. Uses

Cephalosporins can be applied in various parts of the body. Therefore, if various tissues and organs are infected, as long as the pathogenic bacteria are sensitive to cephalosporins, they can be used. It is a kind of bactericide, which means if the concentration is enough, it can kill the bacteria, unlike those bacteriostatic agents like tetracycline, erythromycin, and chloramphenicol. Therefore, cephalosporins can be used for more serious infections.

  • Cephalosporins have a relatively broader antibacterial spectrum. Cephalosporins have a good antibacterial effect on some Gram-positive bacteria or Gram-negative bacteria. (Stain bacteria with gram staining solution. The bacteria stained purple blue are positive bacteria, and the red are negative bacteria.) That is to say, cephalosporins have certain antibacterial activity for bacteria in various clinical departments such as internal medicine, surgery, obstetrics, gynecology and dermatology department.
  • If bacteria produce some enzymes that destroy certain antibacterial drugs, they can become resistant to certain antibacterial drugs. For example, bacteria are resistant to penicillin, while cephalosporins are stable to most of the enzymes produced by bacteria. So it can replace penicillin to kill bacteria.
    There are more varieties of cephalosporins taken orally. This is because there are many of them taken orally into the stomach are hard to be destroyed by stomach acid. So the drug effect is relatively stable.
  • Compared with penicillin, the incidence of penicillin allergy is higher, especially for penicillin can cause anaphylactic shock and that can be fatal. The molecular structure of cephalosporin is similar to penicillin and can also cause allergic reactions, but the rate of allergic reactions is lower than that of penicillin, and the incidence of anaphylactic shock is even lower.

Because of the above characteristics, cephalosporins have higher practical value in clinical practice.

Principles of using cephalosporins

Principles-of-using-cephalosporins
Principles-of-using-cephalosporins

1. No abuse

As cephalosporin has so many advantages, patients and doctors all favor it. When a patient has an infection or fever, no matter what kind of infection it is, they use cephalosporin first, especially the third-generation cephalosporin produced in large quantities in China with a low price. Therefore, abuse was common in the past.

In the past five years, many negative bacteria such as Escherichia coli and pneumoniae bacteria that are difficult to be treated with third-generation cephalosporium have emerged in China.

The extended-spectrum beta lactamase produced by these bacteria can destroy cephalosporins and produce drug resistance. In Shanghai, the proportion of bacteria resistant to third-generation cephalosporin, such as Escherichia coli and pneumoniae bacteria, has accounted for 10%-40%. Many cephalosporins are used. As a result, the good antibacterial effects of these drugs have been greatly weakened, and infections caused by these drug-resistant bacteria are clinically difficult to deal with.

2. Take it orally if you can, and intravenously by drip

Many patients will ask their doctors to give them intravenous cephalosporins in order to pursue an early recovery. This is not appropriate. Whether to use cephalosporin, or use it intravenously or orally depends on the doctor's decision.

When applying cephalosporins, there must be a trade-off. If the infection is relatively mild, oral administration should be chosen. There are oral preparations for cephalosporins of each generation. If the infection is serious, intravenous administration can be considered.

And intravenous drip is better than bolus injection. Why is this? This is because cephalosporin can also produce adverse reactions. If the patient has a severe allergic reaction or other critical adverse reactions to it, and a bolus injection is used, then the drug will quickly enter the blood and the doctor cannot stop the administration. But if you choose drip infusion, even if the drip is fast, once the patient has an adverse reaction, the infusion speed can be immediately slowed down, and the tube can even be clamped immediately to terminate the administration.

3. It cannot be mixed with other drugs

In principle, antibacterial drugs and any other drugs should not be mixed together, even if they are both antibacterial drugs. For example, if a patient receives an intravenous drip of two antibiotics, cephalosporin and gentamicin, it is not allowed to put the two drugs into the same bottle for infusion at the same time. Because the physical and chemical characteristics of various antibacterial drugs are different.

If they are added together, maybe the color remains unchanged, and there is no precipitation, but in fact they may have interacted, reducing their antibacterial effects, or even producing new compounds harmful to the human body. Therefore, the application of antibacterial drugs must be administered separately, and two drugs must not be placed in one container at the same time.

4. Alcohol or medicine

Do not take medication before or after drinking, or shock and fainting occur easily. The elderly may even be life-threatening.

Side effects of cephalosporins taken with alcohol

Side-effects-of-cephalosporins-taken-with-alcohol
Side-effects-of-cephalosporins-taken-with-alcohol

1. Disulfiram reaction

Cephalosporin and alcohol may have a disulfiram-like reaction. Disulfiram is a drug for abstinence from alcohol. After taking this medicine, even if you drink a small amount of alcohol, your body will experience severe discomfort.

The metabolic process of ethanol in the body can be simply described as: first oxidized to acetaldehyde in the body, and then converted into carbon dioxide and water with the assistance of related enzymes. Disulfiram and other similar drugs can inhibit aldehyde-related enzymes when taken with alcohol, accumulated acetaldehyde in the body producing a series of physiological reactions. Its severity is directly proportional to the dosage of the drug and the amount of alcohol consumed. This reaction is more serious in the elderly, children, patients with cardiovascular and cerebrovascular diseases, and those who are sensitive to ethanol, and generally occurs 15-30 minutes after medication and drinking.

The symptoms of disulfiram-like reactions are very significant, such as facial flushing, conjunctival hyperemia, blurred vision, dizziness, nausea, vomiting, sweating, chest pain, myocardial infarction, acute heart failure, dyspnea, acute liver injury, convulsions and death, etc.

2. Drugs that cause disulfiram reactions

So, what common drugs taken with alcohol can cause disulfiram-like reactions?

A. Cephalosporin drugs

Cefoperazone, Cefoperazone and Sulbactam, Ceftriaxone, Cefazolin (Pioneer Ⅴ), Cefradine (Pioneer Ⅵ), Cefmetazole, Cefminol, Laoxycephalosporin, Cefmenoxime, Cefazolin Meng Duo, Cefamine (Pioneer IV), Cefaclor, etc. Among them, cefoperazone and sulbactam are the most sensitive and can cause the most disulfiram-like reactions. If a patient eats liqueur chocolate, Huoxiang Zhengqi water, or even treats injured skin with alcohol alone after taking this drug, a disulfiram-like reaction will occur. In addition, there are related reports of disulfiram-like reactions caused by ceftazidime.

B. Nimidazole drugs such as metronidazole, tinidazole, ornidazole, secnidazole.

C. Other antibacterial drugs: furazolidone, chloramphenicol, ketoconazole, griseofulvin, etc.

In addition to alcohol, people who take cephalosporins also need to pay special attention to the Huoxiang Zhengqi Water. Huoxiangzhengqi water has high content of active ingredients and good curative effect, and works quickly, which is related to the 40%-50% alcohol in it. Therefore, special attention should be paid to "Huoxiangzhengqi water".

3. The interval between alcohol and cephalosporin

Some people may wonder, shouldn’t drink alcohol only during medication? The answer is "no." After taking the drug, the specific duration of alcohol prohibition needs to be weighted according to his own situation.

According to related literature reports, disulfiram-like reactions caused by cephalosporin antibiotics are highly correlated with alcohol consumption, but there are individual differences as the metabolism rates of alcohol and drugs is different, but the longer the interval between drinking and medication, the lower the incidence of those adverse reactions.

Comprehensive analysis showed that the disulfiram-like reaction may occur 5 days before medication, during medication, or within 7 days after medication, and the highest proportion of disulfiram-like reaction occurred during medication. It is worth noting that there are also reports of this reaction occurring after drinking one week after stopping the drug. In order to prevent disulfiram-like reactions, you should consult your doctor if you apply these drugs within seven days after drinking, and you should refrain from alcohol within seven days after stopping the drug. The period of abstinence should be 14 days to obviate worry. Once the disulfiram-like reaction occurs, the drug should be stopped immediately and corresponding treatment measures should be actively taken.

What should we do if friends around us meet the similar situation? Advise him to stop medication and alcohol-containing products in time, ask the patient to adopt a horizontal posture to keep his breathing smooth. The mild ones can relieve soon, and the more severe ones should be sent to the nearest medical institution immediately.

Conclusion

Cephalosporin is widely used in our daily lives, but it is important to note that the combination of cephalosporin and alcohol is often harmful and sometimes fatal. So, just like no drinking while driving, there should be no drinking during medication.

BALLYA provides a betalactam cephalexin combo test kit to tell you if there are beta lactams residues and cephalosporin residues in dairy products you eat every day.

References

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