Talk about cephalosporin shock

Remember these conclusions about the third generation cephalosporins and gallop around the rivers and lakes!

1, cefoperazone and ceftriaxone can cause sulfur-like reactions in alcohol withdrawal.

Ceftazidime and cefotaxime have no sulfur-like reaction to alcohol withdrawal.

2. Ceftazidime and cefoperazone have antibacterial effects on Pseudomonas aeruginosa.

3. Cefoperazone has the risk of bleeding, so vitamin K is recommended.

4. Ceftazidime and aztreonam are cross-resistant.

5. Ceftriaxone can cause false gallstones.

6. Ceftriaxone, cefotaxime and ceftazidime can penetrate the blood-brain barrier and be used for intracranial infection.

7. Cefoperazone can hardly penetrate the blood-brain barrier and is not used for intracranial infection.

8. Cefotaxime has the best effect on positive bacteria among the third generation cephalosporins.

9. Ceftazidime has the best effect on Pseudomonas aeruginosa among the third generation cephalosporins, and it exceeds aminoglycosides.

10, ceftriaxone is the only cephalosporin that can be administered once a day.

1 1. Ceftriaxone and ceftazidime are the first choice for lactating women.

12, using cefoperazone, the risk groups of bleeding are malnutrition, malabsorption, alcoholism and long-term intravenous or nasal feeding tube hypernutrition patients; Vitamin K should be given to the risk population at the same time, daily 10 mg, and the prothrombin time should be monitored.

13, cefotaxime dripping speed should not be too fast, if it is less than 60 seconds, fatal arrhythmia will occur.

I. β -lactam

(1) Penicillins

1, penicillin (PG): acid-resistant and enzyme-resistant. It is mainly used for diseases infected by positive bacteria such as group A hemolytic streptococcus and streptococcus pneumoniae.

Benzathine penicillin can be used to treat syphilis and chronic rheumatic heart disease.

2. Enzyme-resistant penicillin (anti-staphylococcal penicillin): it is mainly suitable for staphylococcal infections that are sensitive to methicillin and produce penicillin, mainly including oxacillin and nafcillin.

3, broad-spectrum penicillin: acid-resistant, oral.

There are mainly ampicillin and amoxicillin.

4, anti-Pseudomonas aeruginosa penicillin: often combined with aminoglycosides, used to treat Pseudomonas aeruginosa infection.

Piperacillin is unstable to a large number of β -lactamases and is often used with competitive β -lactam acid inhibitors (sulbactam and tazobactam), but it is ineffective against MRSA. Mainly piperacillin, mezlocillin and so on.

(2) Cephalosporin

The first generation cephalosporins: cefazolin and cefathiamidine.

The second generation cephalosporins: cefuroxime, cefprozil and cefaclor.

The third generation cephalosporins: cefixime, ceftriaxone, cefoperazone, ceftazidime, ceftizoxime.

The fourth generation cephalosporins: cefepime and cefpirome.

①G+: the first generation > the second and fourth generations > the third generation.

G-: 4th generation > 3rd generation > 2nd generation > 1st generation.

Nephrotoxicity: first generation > second generation > third generation > fourth generation.

The stability of β -lactamase is the fourth generation > the third generation > the second generation > the first generation.

② Anti-Pseudomonas aeruginosa: ceftazidime, cefoperazone and the fourth generation cephalosporin.

It is mainly excreted by kidney, but cefoperazone and ceftriaxone are mainly excreted by bile. It is forbidden for patients with any history of cephalosporin allergy and allergic shock to penicillin. Cefoperazone can cause thrombocytopenia. Cephalosporins can also cause sulfur-like reactions to alcohol withdrawal.

(III) Other atypical β -lactams

1, cephamycin: such as cefoxitin, cefminox and cefmetazole. Its antibacterial effect is similar to that of the second generation cephalosporins, but its antibacterial effect on anaerobic bacteria such as Bacteroides fragilis is stronger than cephalosporins. Its efficacy in treating infections caused by esbls-producing bacteria has not been proved.

2. Oxycephalosporins: such as levofloxacin and ofloxacin. It has similar antibacterial effect to the third generation cephalosporins, but it has good antibacterial effect on anaerobic bacteria such as Bacteroides fragilis.

3. Carbapenems: such as meropenem, imipenem, ertapenem, etc. , has strong antibacterial activity against various gram-positive cocci, gram-negative bacilli (including Pseudomonas aeruginosa and Acinetobacter) and most anaerobic bacteria. The antibacterial effect on MRSA and stenotrophomonas maltophilia is poor. Ertapenem has a long half-life in blood and can be administered once a day. It has poor antibacterial effect on non-fermentative bacteria such as Pseudomonas aeruginosa and Acinetobacter.

4. Aztreonam: It has good antibacterial activity against aerobic gram-negative bacteria such as Enterobacteriaceae and Pseudomonas aeruginosa, characterized by low nephrotoxicity and less cross-allergy.

5. β -lactamase inhibitors: clavulanic acid, sulbactam and tazobactam.

Second, macrocyclic lipids.

The common drugs are erythromycin, roxithromycin, clarithromycin and azithromycin.

Features: It has strong antibacterial effect on G+ bacteria (such as streptococcus) and some G- bacteria (Haemophilus influenzae and Moraxella catarrhalis), mycoplasma, chlamydia and Legionella. It is not easy to pass through the blood-brain barrier; It is mainly excreted by bile, and its concentration is high in bile.

Adverse reactions:

① Gastrointestinal reaction.

② Hepatotoxicity: Esterified erythromycin has certain hepatotoxicity and should be used in a small amount in a short time.

③ Erythromycin can cause abnormal increase of theophylline and digoxin concentration, leading to poisoning.

Three. Aminoglycosides

The common drugs are streptomycin, gentamicin, amikacin, etimicin, Isepamicin and tobramycin.

Mainly used for G-, it has good antibacterial effect on Enterobacteriaceae and Staphylococcus, and some of it is effective on Pseudomonas aeruginosa. Ineffective to anaerobic bacteria and insensitive to streptococcus.

Drug resistance: formed by the production of passivating enzymes through plasmid conduction.

Pharmacokinetics: it is not easy to pass through the blood-brain barrier and the bile concentration is very low.

Adverse reactions:

Otototoxicity: (drug concentration in lymph of inner ear increases)

Nephrotoxicity: Renal excretion (proximal convoluted tubule injury)

N- muscle block (calcium or neuraminic acid can counteract this effect)

Fourth, quinolones.

The common drugs are norfloxacin, ciprofloxacin, levofloxacin and moxifloxacin.

Main effects: broad spectrum, among which levofloxacin and moxifloxacin have strong effects on anaerobic bacteria such as chlamydia, mycoplasma and Legionella.

Adverse reactions:

1. Gastrointestinal reaction

2. Central nervous system response

3. Photosensitive reaction

4. It may affect cartilage development, so pregnant women, lactating women and patients under 18 are prohibited.

5. Alkaline urine is prone to crystallization (drink more water after taking medicine)

6, tendinitis, tendon rupture, QT interval extension, blood sugar fluctuation.

5. Glycopeptides

Such as vancomycin and teicoplanin.

Can be used for treating infections caused by methicillin-resistant Staphylococcus aureus (MRSA) and ampicillin-resistant Enterococcus.

Oral vancomycin can be used to treat pseudomembranous enteritis caused by Clostridium difficile.

Vancomycin → effective for central infection; Teicolanin → ineffective for central infection.

These drugs are time-dependent fungicides, but their PK/PD evaluation parameters are AUC/MIC.

Adverse reactions of vancomycin:

1. ototoxicity.

2. Nephrotoxicity: damage renal tubules, which can cause renal failure in severe cases.

3. Allergic reaction: occasional patchy rash and anaphylactic shock.

4. Rapid intravenous injection of vancomycin can cause "red man syndrome".

Six, tetracyclines

Such as tetracycline, doxycycline and minocycline.

As a broad-spectrum antibacterial drug, it is mainly used for rickettsia, chlamydia, mycoplasma, spirochete, brucellosis, and respiratory tract, biliary tract, urinary tract, skin and soft tissue infections caused by sensitive bacteria.

Minocycline can be used as one of the combined drugs to treat multidrug-resistant Acinetobacter baumannii infection. It can also be used to treat acne with obvious inflammatory reaction.

Adverse reactions: affecting the development of teeth and bones, flora imbalance, digestive tract reaction, liver and kidney damage, etc.

Seven, nitroimidazoles

Such as metronidazole, tinidazole and ornidazole.

Metronidazole, anti-anaerobic bacteria, anti-trichomonad, anti-amoeba. It is worth noting that metronidazole is a concentration-dependent antibacterial drug, but because the dose is related to the incidence of adverse reactions, it should not be too large at one time, and it still needs to be administered at Q 12h or Q8h.

Tinidazole has stronger effect on Bacteroides fragilis and Clostridium than metronidazole, but weaker effect on Clostridium. The ability of tinidazole to penetrate the blood-brain barrier is higher than that of metronidazole, which is related to the high fat solubility of tinidazole.

The teratogenic effect of ornidazole is lower than that of metronidazole and tinidazole. Although the drug instructions indicate that ornidazole has no inhibitory effect on acetaldehyde dehydrogenase, there are still reports that ornidazole causes disulfiram reaction.

These drugs may cause granulocytopenia and peripheral neuritis. Use with caution in patients with basic diseases of nervous system and hematological diseases.

Eight, anti-mycobacterium tuberculosis drugs

First-line anti-tuberculosis drugs: isoniazid, rifampicin, pyrazinamide, ethambutol and streptomycin.

Second-line anti-tuberculosis drugs: kanamycin, p-aminosalicylic acid, thiosemicarbazone, capreomycin, levofloxacin, linezolid.

Pay attention to the adverse reactions of liver damage caused by isoniazid, rifampicin and pyrazinamide.

Peripheral neuritis caused by isoniazid.

The main adverse reaction of ethambutol is retrobulbar optic neuritis.

Sun exposure should be avoided during taking pyrazinamide, because it will cause photosensitive reaction.

Nine, antifungal drugs

Triazoles: Fluconazole (Dafukang), Voriconazole (Fan Wei), Itraconazole (Spirillum, Yiqikang) and Posaconazole. Broad-spectrum antifungal agents; Pay attention to drug interactions.

Polyolefins: Amphotericin B (extremely toxic invasive fungal infection, especially kidney damage) and nystatin (candidiasis of skin mucosa or intestine).

Imidazole (external use): econazole, bifonazole, ketoconazole, clotrimazole.

Carposine: invasive aspergillosis that is ineffective or intolerant to other drugs. It has high antifungal activity against Candida albicans, but its effect on Candida parasmooth is relatively weak. Cryptococcus neoformans has natural resistance to caspofungin.

Others: such as fluorocytosine (easy to produce drug resistance when used alone), terbinafine (dermatophyte), Amo Lu Fen (dermatophyte) and griseofulvin (dermatophyte).

X. Other categories

1, chloramphenicol: broad spectrum, mainly used in clinical bacterial meningitis, typhoid fever and paratyphoid fever.

2. Clindamycin: It is mainly used for G+ bacteria infection and abdominal and gynecological infections caused by anaerobic bacteria. At present, Streptococcus pneumoniae and other bacteria have high drug resistance to it. This product is the first choice for Staphylococcus aureus osteomyelitis.

3, compound sulfamethoxazole: broad spectrum, suitable for urinary tract infection, lung infection, typhoid and so on.

4. Fusidic acid: used for G+ bacteria infection, mainly used for dermatology infection.

5. Fosfomycin: It acts on bacterial cell walls and has a broad antibacterial spectrum. It is mainly excreted by the kidneys and is mainly used to treat urinary tract infections.

6, polymyxin: obvious nephrotoxicity, used for infections caused by multidrug-resistant Acinetobacter and Pseudomonas aeruginosa.

7. Linezolid: It can be used for methicillin-resistant Staphylococcus aureus (MSRA), vancomycin-resistant enterococci and Mycobacterium tuberculosis.

8. Tigecycline: It has good antibacterial activity against carbapenem-resistant Enterobacteriaceae and Acinetobacter. It has a good effect on most anaerobic bacteria and has natural resistance to Pseudomonas aeruginosa.

9. daptomycin: It has good antibacterial activity against Gram-positive bacteria including masa, but no antibacterial activity against Gram-negative bacteria. Pay attention to the detection of phosphokinase level during use, and consider stopping statins.

(The content is taken from the network platform, only for professionals to learn)