What Is Cefpodoxime?

Cefpodoxime is a chemical substance with a molecular formula of C15H17N5O6S2. Its chemical name is (6R, 7R) -7- [2- (2-amino-4-thiazolyl)-(Z) -2- (methoxyimino) acetylamino] -3-methoxymethyl-8 -Oxo-5-thia-1-azabicyclo [4.2.0] oct-2-ene-2-carboxylic acid, clinically applicable to bronchitis, pneumonia and urinary system, skin and soft tissue caused by sensitive bacteria, Infections in the middle ear and tonsils.

Chinese name: Cefpodoxime
English name: Cefpodoxime

Molecular formula: C15H17N5O6S2
Molecular weight: 427.46

Cefpodoxime compounds

Cefpodoxime Basic Information

Chinese name cephalosporin

Chinese alias: (6R, 7R) -7- [2- (2-amino-4-thiazolyl)-(Z) -2- (methoxyimino) acetylamino] -3-methoxymethyl-8- Oxo-5-thia-1-azabicyclo [4.2.0] oct-2-ene-2-carboxylic acid

English name: cefpodoxime

English alias: Cefpodoxime; Cefpodoxime Acid;

CAS number: 80210-62-4

Molecular formula: C ₁₅ H ₁₇ N ₅ O ₆ S ₂

Structural formula:

Molecular weight: 427.45500

Exact mass: 427.06200

PSA: 209.98000

LogP: 0.37080

Physical and chemical properties of cefpodoxime

Appearance and properties: white to light yellow powder

Density: 1.78 g / cm ³

Melting point: 200-202ºC

Refractive index: 1.78

Storage conditions: -20ºC Freezer ^[1]

Cefpodoxime pharmacology and toxicology:

Cefpodoxime pharmacological effects

Cefpodoxime ester is an oral broad-spectrum third-generation cephalosporin. After entering the body, it is hydrolyzed by non-specific esterase to cefpodoxime to exert antibacterial effects. It is effective against both Gram-positive and negative bacteria. The mechanism of action of this product is The bactericidal effect is achieved by inhibiting the biosynthesis of microbial cell walls. This product is stable to -lactamase, so many -lactamase producing microorganisms resistant to penicillin and cephalosporins are still sensitive to this product. This product is ineffective against some extended-spectrum -lactamase.

In vitro and clinical infection studies have confirmed that this product is active against most of the following microorganisms:

1. Aerobic gram-positive microorganisms: Staphylococcus aureus (including penicillin-producing strains, but not effective against methicillin-resistant staphylococci), saprophytic staphylococcus, pneumococcus (except penicillin-resistant strains), and purulent Streptococcus.

2. Aerobic gram-negative microorganisms: E. coli, Klebsiella pneumoniae, E. coli, Proteus mirabilis, Pseudomonas aeruginosa, Haemophilus influenzae (including -lactamase producing strains), Moraxella catarrhalis Neisseria gonorrhoeae (including penicillin-producing strains).

This product is active against most of the following microorganisms in vitro, but its clinical significance is unclear:

1. Aerobic Gram-positive microorganisms-Streptococcus agalactiae and Streptococcus (groups C, F, G). But this product is not effective on enterococci.

2. Aerobic gram-negative microorganisms-heterocitric citrate, Klebsiella oxytoca, Proteus ordinary, Providence lei, Haemophilus parainfluenzae. However, this product is inactive against most Pseudomonas and Enterobacter species.

3, Anaerobic Gram-positive microorganisms-Streptococcus gigas.

Toxicological Study of Cefpodoxime

Genotoxicity: In vivo and in vitro studies (including Ames test, chromosomal aberration test, non-scheduled DNA synthesis test, mitotic recombination test, gene recovery, forward gene mutation test and in vivo micronucleus test) have not found this product to be genotoxic.

Reproductive toxicity: When the oral dose of this product is about 100mg / kg / day (based on the body surface area, it is twice the human dose), there is no effect on the fertility and reproductive function of the animal. No teratogenic and embryo toxicity. When the rabbit dose reached 30mg / kg / day (in terms of body surface area, 1-2 times the human dose), no teratogenicity and embryo toxicity were seen. At present, there is no sufficient and rigorous research data on pregnant women. Because animal tests cannot fully predict the condition of humans, pregnant women should only use it when they really need it. This product has not been used in childbirth, so it can only be used when it is really needed.

Cefpodoxime may be secreted in human milk. Because this product has a potentially serious response to lactating infants, the pros and cons of mothers and infants should be weighed before determining whether to interrupt breastfeeding or discontinue the drug.

Carcinogenicity: No long-term carcinogenicity research data of this product is available. ^[2]

Cefpodoxime pharmacokinetics

1. Serum concentration: When a healthy adult takes 100mg or 200mg of this product after a single oral administration, the highest serum concentration of cefpodoxime ester appears 3 to 4 hours after administration, and the values are 1.5-1.8 g / ml and 3.0 -3.6 g / ml, showing correlation with dose. The half-life of the drug in the serum is about 2 hours. It is better absorbed after meals than when fasted.

2. Distribution: It is distributed in sputum, tonsil tissue and skin tissue.

3. Metabolism and excretion: When absorbed, it is hydrolyzed by intestinal wall esterase to cefpodoxime, distributed in circulating blood, and excreted by the kidneys. The urine recovery within 2 hours after a meal is about 40% -50%. This product was continuously given 200 mg × 2 times / day for 14 days without accumulation.

4. Serum drug concentration and urinary excretion when renal function is impaired delays urinary excretion as renal function decreases, which increases drug concentration in serum and prolongs half-life.

Cefpodoxime indications:

Used for the following mild to moderate infections caused by sensitive bacteria:

1. Pneumonia, acute bronchitis, chronic bronchitis, sore throat (throat abscess), tonsillitis (peritonsilitis, peritonsillar abscess), secondary infection of bronchiectasis, secondary infection of chronic respiratory diseases.

2. Pyelonephritis, cystitis, gonococcal urethritis.

3. Mastitis.

4. Folliculitis (including pustular acne), carbuncle, edema, dysentery, erysipelas, peak fossa tissue inflammation, lymphangiitis (nodule) inflammation, suppurative paronychia, subcutaneous abscess, sweat glanditis, clustered acne, Infectious powder tumor, abscess around the anus.

5. Vestibular glandular inflammation and vestibular gland abscess.

6, otitis media, paranasal sinusitis. ^[2]

Cefpodoxime Specifications:

0.1g (based on C15H17N5O6S2) ^[2]

Cefpodoxime usage and dosage:

Orally after meals. Adults 0.1 to 0.2 g each time, twice a day, depending on the disease and condition. Generally, for upper respiratory tract infection and simple urinary tract infection, each time is 0.1g, twice a day; in severe cases, it can be increased to 0.2g, twice a day, and the course of treatment is 5 to 7 days. For lower respiratory tract infections, complex urinary tract infections, skin and soft tissue infections, ear, nose and throat infections, 0.2 g each time, 2 times a day for 7 to 14 days. ^[2]

Cefpodoxime adverse reactions:

(1) Serious adverse reactions of this product:

1) Shock: occasionally cause symptoms of shock, should pay attention to observation, if there is discomfort, abnormal mouth feeling, wheezing, dizziness, constipation, tinnitus, sweating, etc., the drug should be discontinued.

2) Skin-mucosa-eye syndrome, toxic epidermal necrosis: occasional skin-mucosa-eye syndrome (Stevens-Johnson syndrome), toxic epidermal necrosis (Lyell syndrome) should be observed carefully, if there is an abnormality, the drug should be discontinued And dispose appropriately.

3) Pseudo-membrane colitis: Severe colitis with bloody stools, such as pseudo-membrane enteritis. If abdominal pain and frequent diarrhea occur, the drug should be stopped quickly and treated appropriately.

(2) Serious adverse reactions caused by similar drugs:

1) Pancytopenia, agranulocytosis, hemolytic anemia; other cephalosporin antibiotics have been reported to cause pancytopenia, agranulocytosis, and hemolytic anemia.

2) Acute renal failure: other cephalosporin antibiotics occasionally cause severe renal damage such as acute renal failure, which should be checked regularly and discontinued if abnormalities occur.

3) Interstitial pneumonia, PIE syndrome; other cephalosporin antibiotics, occasionally interstitial pneumonia, PIE syndrome, etc. accompanied by fever, cough, dyspnea, chest X-ray abnormalities, eosinophilia, etc. If such symptoms occur, the drug should be discontinued and treated with corticosteroid preparations.

4) Spasticity: In patients with renal insufficiency, a large amount of other cephalosporin antibiotics may cause neurological symptoms such as spasm.

(3) Other side effects:

1) Allergies: When rash, urticaria, erythema, pruritus, fever, lymphadenopathy, joint pain, etc. occur, the drug should be discontinued.

2) Blood: Sometimes eosinophilia, thrombocytopenia, and occasionally neutropenia occur.

3) Liver: Sometimes ALT, AST, ALP, LDH rise.

4) Kidney: Sometimes blood BUN and blood creatinine increase.

5) Digestive tract: Sometimes nausea, vomiting, diarrhea, soft stools, stomach pain, abdominal pain, loss of appetite, stomach discomfort and occasional constipation.

6) Alternate flora: occasional intraoral inflammation and candidiasis.

7) Vitamin deficiency: occasional symptoms of vitamin K deficiency (hypothrombinemia, bleeding tendency, etc.), vitamin B group deficiency symptoms (glossitis, stomatitis, loss of appetite, neuritis, etc.).

8) Others: occasional dizziness, headache, and swelling. ^[2]

Cefpodoxime contraindications:

Patients with a history of allergies to this product or cephalosporin antibiotics are contraindicated.

Cefpodoxime precautions:

1. General Note: There is a possibility of causing shock, so you should consult carefully.

2. Prudent use of drugs (careful use of drugs by the following patients):

(1) Patients with a history of allergies to penicillin antibiotics.

(2) I, my parents, or my brothers have physical constitutions that may cause allergic symptoms such as bronchial asthma, rash, urticaria.

(3) Patients with severe renal impairment (this strain is a renal excretion antibiotic, which will cause delayed excretion).

(4) Patients with inadequate oral feeding or non-oral nutritional maintenance, and patients with poor systemic status (symptoms of vitamin K deficiency will appear, so attention should be paid to observation).

3. Impact on clinical test values:

(1) Urine glucose tests performed by Benedet's reagents, Fehling's reagents, and clinical test strips other than the test strip reaction may be false positives, so it should be noted.

(2) Direct Combs test is sometimes positive, so attention should be paid.

Cefpodoxime medication for pregnant and lactating women:

The safety of medications during pregnancy has not been established, so pregnant women or women who may become pregnant should only use them when the benefits of treatment outweigh the risks.

Cefpodoxime medication for children:

The safety of pediatric medications has not been established (less experience).

Cefpodoxime for the elderly:

Elderly people should pay attention to the following content and dosage and dosing interval and observe the state of the patient, and carefully dosing.

(1) Elderly people are more likely to have reduced physiological functions and are prone to side effects.

(2) Elderly people will have bleeding tendency caused by vitamin K deficiency. ^[2]

Cefpodoxime drug interactions:

1. Combination of antacids (sodium bicarbonate or sodium hydroxide) and H2 receptor antagonists with this product can reduce the absorption and blood concentration of this product.
Anticholinergic drugs can reduce peak concentrations without affecting the degree of absorption (AUC).

2. Similar to other -lactam antibiotics, taking probenecid at the same time will inhibit excretion of this product from the kidneys, leading to increased AUC and Cmax.

3. Although this product has little nephrotoxicity when used alone, it should still pay close attention to the simultaneous use with other known nephrotoxic drugs. ^[2]

Cefpodoxime overdose:

There are no data on human overdose. In some rodent acute toxicity studies, a single oral dose of 58 mg / kg did not produce adverse effects. In cases of severe toxicity caused by drug overdose, hemodialysis or peritoneal dialysis can help to remove cefpodoxime from the body. Toxic symptoms of -lactam antibiotic overdose include: nausea, vomiting, epigastric pain, and diarrhea. . ^[2]