What Is an External Cephalic Version?

Cefradine (Cephradine, Velosef) Alias: Pioneerin , Cephalosporin , etc. This product is the first generation of semi-synthetic cephalosporins, with antibacterial effect similar to cephalexin. This product is acid-resistant, can be taken orally, is well absorbed, and has a high blood concentration. It is resistant to -lactamase and has a rapid and reliable bactericidal effect on drug-resistant Staphylococcus aureus and many other bacteria resistant to broad-spectrum antibiotics. , Mainly excreted in the urine in the original form, the higher the concentration in urine. Clinically it is mainly used for infections of the respiratory tract, urinary tract, skin and soft tissues, such as bronchitis, pneumonia, pyelonephritis, cystitis, otolaryngology, enteritis and dysentery.

Cefradine (Cephradine, Velosef) Alias: Pioneerin , Cephalosporin , etc. This product is the first generation of semi-synthetic cephalosporins, with antibacterial effect similar to cephalexin. This product is acid-resistant, can be taken orally, is well absorbed, and has a high blood concentration. It is resistant to -lactamase and has a rapid and reliable bactericidal effect on drug-resistant Staphylococcus aureus and many other bacteria resistant to broad-spectrum antibiotics. , Mainly excreted in the urine in the original form, the higher the concentration in urine. Clinically it is mainly used for infections of the respiratory tract, urinary tract, skin and soft tissues, such as bronchitis, pneumonia, pyelonephritis, cystitis, otolaryngology, enteritis and dysentery.

Drug Name

Cefradine

Foreign name

Cefradine

Whether prescription drugs

prescription

Athletes use with caution

Use with caution

Molecular formula

C16H19N3O4S

Molecular weight

349.40

cas

38821-53-3

Brief introduction of cefradine compounds

Cefraditin Basic Information

Chinese name cefradine

Chinese aliases: Pioneer Redding, Cefatin, Cefraditin, Cefraditin, Hexamectin, Cephacycline, Cyclohexene Cephalosporin, Cyclosporin

English name: cephradine

English alias: CEPHRADINE COMPACTED; CEPHRADINE MICRONISED POWDER; Cephradine; Anspor; Velosef; (6r- (6alpha, 7))-((amino-1,4-cyclohexadien-1-ylacetyl) amino) -3-methyl-8-oxo -5-thia-1-azabicyclo (4.2.0) oct-2-ene-2-carboxylic acid; (6R, 7R) -7-{[((2R) -2-amino-2- (cyclohexa-1,4 -dien-1-yl) acetyl] amino} -3-methyl-8-oxo-5-thia-1-azabicyclo [4.2.0] oct-2-ene-2-carboxylic acid; (7R) -7- { [(2R) -2-amino-2-cyclohexa-1,4-dien-1-ylacetyl] amino} -3-methyl-8-oxo-5-thia-1-azabicyclo [4.2.0] oct-2- ene-2-carboxylic acid

CAS number: 38621-53-3

Molecular formula: C ₁₆ H ₁₉ N ₃ O ₄ S

Molecular weight: 349.40500

Exact mass: 349.11000

PSA: 138.03000

LogP: 1.37770

Physical and chemical properties of cefradine

Appearance and properties: solid

Density: 1.47g / cm ³

Melting point: 140-142ºC

Boiling point: 693.1ºC at 760mmHg

Flash point: 373ºC

Refractive index: 1.684

Storage conditions: Store at 0-5ºC

Cefraditin Safety Information

Customs Code: 2941905400

Danger category code: R36 / 37/38; R42 / 43

Safety instructions: S26-S36

Dangerous Goods Sign: Xi

Cefradine uses

It is a semi-synthetic broad-spectrum cephalosporin.

Cefraditin Customs Data

China Customs Code: 2941905400 ^[1]

Cefraditin Safety Terms

S26In case of contact with eyes, rinse immediately with plenty of water and seek medical advice.

After accidental contact with eyes, rinse immediately with plenty of water and seek medical advice.

S36Wear suitable protective clothing.

Wear appropriate protective clothing.

Cefradine risk terminology

R36 / 37 / 38Irritating to eyes, respiratory system and skin.

Irritation of eyes, respiratory system and skin.

R42 / 43May cause sensitization by inhalation and skin contact.

May cause sensitization by inhalation and skin contact.

Cefradine Pharmacopoeia Standard

Cefradine source (name), content (potency)

This product is (6R, 7R) -7-[(R) -2-amino-2- (1,4-cyclohexenyl) acetylamino] -3-methyl-8-oxo-5-thia 1-Azabicyclo [4.2.0] oct-2-ene-2-carboxylic acid. Calculated as anhydrous content, containing C16H19N3O4S shall not be less than 90.0%.

Cephalosporin traits

This product is white or off-white crystalline powder; slightly odor.

This product is slightly soluble in water and almost insoluble in ethanol, chloroform or ether.

Cefraditin specific rotation

Take this product, weigh it accurately, add acetate buffer solution (take 1.36g of sodium acetate, dissolve in about 50ml with water, adjust the pH to 4.6 with glacial acetic acid, and dilute to 100ml with water) and dissolve and quantitatively dilute to about Contains a 10mg solution. Determined according to law (Appendix VIE of Part Two of the 2010 Pharmacopoeia), the specific rotation is + 80 ° to + 90 °.

Cefraditin identification

(1) Take an appropriate amount of this product and cefradine reference substance, dissolve and dilute with water to make a solution containing about 6mg per 1ml, as the test solution and the reference solution. According to the thin layer chromatography (2010 edition Pharmacopoeia Part II Appendix VB) test, draw 5 l each of the two solutions, and point them on the same silica gel G thin-layer plate [after activation at 105 ° C, place 5% (ml / ml) plus ten In tetra-n-hexane solution, unfold to the top of the thin-layer plate and air dry], take 0.1mol / L citric acid solution-0.2mol / L disodium hydrogen phosphate solution-acetone (60: 40: 1.5) as The developing agent was developed, taken out, and heated at 105 ° C. for 5 minutes, and immediately sprayed with a 0.1% ninhydrin solution made of the developing agent, and heated at 105 ° C. for 15 minutes, and then inspected. The position and color of the main spots displayed by the test solution should be the same as the position and color of the main spots displayed by the reference solution.

(2) In the chromatogram recorded under the content determination item, the retention time of the main peak of the test solution should be consistent with the retention time of the main peak of the reference solution.

(3) Take an appropriate amount of this product, dissolve it in methanol, evaporate to dryness at room temperature, and take the residue for determination by infrared spectrophotometry (Appendix IVC of the second edition of the Pharmacopoeia, 2010 Edition). The infrared light absorption spectrum of this product should be compared with the control spectrum (" Drug Infrared Spectral Collection "722").

The above two items (1) and (2) are optional.

Cefraditin examination

Crystallinity

Take a little of this product and check it according to law (Appendix D of Part II of the Pharmacopoeia 2010), and it should meet the requirements.

acidity

Take this product, add water to make a solution containing 10mg per 1ml, and measure it according to law (Appendix VI H of the Pharmacopoeia Part II of the 2010 edition). The pH value should be 3.5 6.0.

Clarity and color of the solution

Take 5 parts of this product, each 0.55g, and add 0.15g of sodium carbonate and 5ml of water to dissolve. The solution should be clear and colorless; if it is turbid, compare with No. 1 turbidity standard solution (Appendix B of Part Two of the 2010 Pharmacopoeia) , Must not be more concentrated; if the color is developed, it must not be deeper (for injection) compared with the yellow or yellow-green standard colorimetric solution No. 5 (Appendix A of the 2010 edition of the Pharmacopoeia).

Cefalexin

Prepare the test solution according to the method of content determination; take another 20mg of cephalexin reference substance, accurately weigh it, place it in a 50ml volumetric flask, add about 30ml of mobile phase to ultrasonically dissolve, then dilute to the mark with mobile phase, shake well Take 5ml precisely, place it in a 50ml measuring bottle, dilute to the mark with mobile phase, shake well, and use it as a reference solution. According to the chromatographic conditions under the content determination item, take 10 l of the reference solution into the liquid chromatograph, adjust the detection sensitivity, so that the peak height of the main component chromatographic peak of the reference solution is about 25% of full scale. Precisely measure 10 l each of the test solution and the reference solution, and inject them into the liquid chromatograph, record the chromatogram, and calculate the peak area according to the external standard method. The cephalexin-containing solution should be no more than 5.0% as an anhydrous.

relative substance

Accurately weigh the appropriate amount of the product, add the mobile phase to dissolve and quantitatively dilute it to make a solution containing 1mg per 1ml as the test solution; take an appropriate amount, and use the mobile phase to quantitatively dilute it to make a solution containing 5g per 1ml. As a control solution; also separately weigh appropriate amounts of cephalexin, dihydrophenylglycine and 7-aminodesacetoxycefanoic acid reference substance, put in the same volume bottle, add 4ml of 7.3% hydrochloric acid solution, dissolve by ultrasound, and then dissolve The reference solution was quantitatively diluted with the reference solution to prepare a mixed solution containing 10 g of each of the three impurity reference materials in each 1 ml as the impurity reference solution. According to the chromatographic conditions under the content determination item, take 20 l of the impurity reference solution, inject it into the liquid chromatograph, and use 220nm as the detection wavelength. The elution order is: 7-aminodeacetoxycephalosporanic acid, dihydrophenylglycoside ammonia. Acid, cephalexin and cefradine, the resolution between the peaks should meet the requirements. 20 l of the control solution was accurately measured and injected into the liquid chromatograph, and the detection sensitivity was adjusted at 254 nm so that the peak height of the main component chromatographic peak was about 25% of full scale. Then accurately measure 20l each of the test solution, the impurity reference solution and the control solution, and inject them into the liquid chromatograph respectively, and then re-inject with 254nm as the detection wavelength, and then re-inject with 220nm as the detection wavelength. Record the chromatograms to The peak retention time of the main component is 2.5 times. If there is an impurity peak in the chromatogram of the test solution, in addition to cephalexin, dihydrophenylglycine (detected at 220nm) and 7-aminodeacetoxycephalosporanic acid (detected at 254nm) The external standard method is calculated based on the peak area and must not exceed 1.0%; the peak area of other single impurities (detected at 254nm) must not be greater than 4 times (2.0%) the main peak area of the control solution, and the sum of the peak areas of other impurities (detected at 254nm) must not be greater than the control Five times the area of the main peak of the solution (2.5%).

Cefradine polymer

It was determined by molecular exclusion chromatography (Appendix V H, Part Two of the Pharmacopoeia, 2010 Edition).

1 Chromatographic conditions and system suitability tests

Dextran gel G-10 (40-120 m) was used as a filler, the inner diameter of the glass column was 1.0-1.4 cm, and the column length was 30-45 cm. Using 0.2 mol / L phosphate buffer [0.2 mol / L disodium hydrogen phosphate solution-0.2 mol / L sodium dihydrogen phosphate solution (95: 5)] at pH 8.0 as mobile phase A, and water as mobile phase B, The flow rate is 1.0 to 1.5 ml per minute, and the detection wavelength is 254 nm. Measure 100-200 l of a 0.2 mg / ml blue dextran 2000 solution, inject it into a liquid chromatograph, measure with mobile phases A and B, and record the chromatogram. According to the blue glucan 2000 peak calculation, the theoretical plate number is not less than 400, and the tailing factor should be less than 2.0. The retention time ratio of the blue glucan 2000 peak in the two mobile phase systems should be between 0.93 and 1.07. The main peak of the control solution and the polymer peak in the test solution and the blue glucan 2000 peak in the corresponding chromatography system. The ratio of retention time should be between 0.93 and 1.07. Weigh about 0.2g of cefradine, put it in a 10ml measuring bottle, add 4ml of 2% anhydrous sodium carbonate solution to dissolve, add 5ml of 0.6mg / ml blue glucan 2000 solution, dilute to the mark with water, and shake well. Measure 100-200 l into the liquid chromatograph, measure with mobile phase A, and record the chromatogram. The ratio of the peak height of the high polymer to the valley height between the monomer and the high polymer should be greater than 2.0. In addition, with mobile phase B as the mobile phase, 100-200 l of the control solution was accurately measured, and five consecutive injections were performed. The relative standard deviation of the peak area should not be greater than 5.0%. (Before the measurement of the control solution, first rinse the gel column with 200-400ml of a mixed solution containing 0.2mol / L sodium hydroxide and 0.5mol / L sodium chloride, and then rinse with water to neutrality.)

2 Preparation of control solution

Take an appropriate amount of cefradine reference substance, accurately weigh, add water to dissolve and quantitatively dilute to make a solution containing about 10 g of cefradine per 1ml.

3 Assay

Take about 0.2g of this product, weigh it accurately, put it in a 10ml measuring bottle, add 4ml of 2% anhydrous sodium carbonate solution, after dissolving, dilute to the mark with water and shake well. Immediately and accurately measure 100 to 200 l and inject it into the liquid chromatograph, measure with mobile phase A as the mobile phase, and record the chromatogram. In addition, 100-200 l of the reference solution was accurately measured and injected into the liquid chromatograph. The mobile phase B was used as the mobile phase for measurement, and the chromatogram was recorded. Based on the peak area calculated by the external standard method, the polymer containing cefradine must not exceed 0.05% by cefradine.

2-naphthol

Determination according to high performance liquid chromatography (Annex VD of Pharmacopoeia Part II of the 2010 edition).

1 Chromatographic conditions and system suitability tests

Octadecylsilane-bonded silica gel was used as the filler; methanol monowater (55:45) was used as the mobile phase, the flow rate was 1 ml per minute, and the detection wavelength was 225 nm. Take 20ul of the reference solution into the liquid chromatograph, adjust the methanol ratio in the mobile phase so that the retention time of the 2-naphthol peak is about 7 minutes, and the number of theoretical plates is not less than 3000 based on the 2-naphthol peak, and the 2-naphthol The resolution of the peak from adjacent peaks should not be less than 1.5.

2 Assay

Take an appropriate amount of this product, accurately weigh it, add mobile phase to dissolve and quantitatively dilute to make a solution containing about 10mg of cefraditin per 1ml, shake it thoroughly, filter, and take the filtrate as the test solution; take another 2 naphthol Appropriate amount, accurately weighed, dissolved with mobile phase and quantitatively diluted to make a solution containing about 0.5ug of 2-naphthol per 1ml. As a reference solution, accurately measure 20ul each of the two solutions and inject them into liquid chromatography. Instrument, record the chromatogram. According to the external standard method in terms of peak area, the amount of 2-monophenol should not be discussed as 0.05% (for oral preparations) or 0.0025% (for injection).

Moisture

Take this product and measure it according to the Moisture Determination Method (Appendix M, First Method A of Part Two of the Pharmacopoeia, 2010 Edition). The moisture content must not exceed 6.0%.

Residue on ignition

Take 1.0g of this product and check it according to law (Appendix N of Part Two of the 2010 Pharmacopoeia). The residual residue shall not exceed 0.2%.

Heavy metal

Take the residue left under the item of burning residue and check it according to law (Appendix H of the second edition of the Pharmacopoeia of 2010 Edition, the second method H), the content of heavy metals must not exceed 20 parts per million.

Visible foreign body

Take 5 parts of this product, each 2.0g, add 3.0% arginine solution (filtered through 0.45m filter membrane) to dissolve, and check according to law (Appendix H of Part Two of the 2010 Pharmacopoeia), which should meet the regulations use).

Insoluble particles

Take 3 parts of this product, each 2.0g, add 3.0% arginine solution (filtered through 0.45m filter) to make a solution containing 50mg per 1ml, and check according to law (Appendix C of Part Two of the 2010 Pharmacopoeia), each 1g sample should not exceed 6000 particles containing more than 10m particles, and not more than 600 particles containing 25m or more (for injection).

Bacterial endotoxin

Take this product, 2.6% endotoxin-free sodium carbonate solution to dissolve, check according to law (Appendix E of the second edition of the Pharmacopoeia, 2010 edition), and the amount of endotoxin in 1mg of cefraditin should be less than 0.20EU (for injection).

Aseptic

Take this product, dissolve it with 2.6% sterile sodium carbonate solution, transfer it to not less than 500ml of 0.9% sterile sodium chloride solution, treat it with membrane filtration method, and check according to law (Appendix H of Pharmacopoeia Part II of the 2010 edition). ), Should meet the requirements (for injection).

Determination of cefradine

It was determined by high performance liquid chromatography (Appendix D, Part Two of the Pharmacopoeia, 2010 Edition).

Chromatographic conditions and system suitability tests

Octadecylsilane-bonded silica gel is used as the filler; water-methanol-3.86% sodium acetate solution-4% acetic acid solution (1564: 400: 30: 6) is the mobile phase; the flow rate is 0.7-0.9ml per minute; detection The wavelength is 254nm. Take 10 parts of cefradine reference solution and 1 part of cephalexin reference stock solution (0.4mg / ml), mix well, take 10l into the liquid chromatograph, record the chromatogram, and the resolution of the cefradine peak and the cephalexin peak should meet the requirements .

Assay

Take about 70mg of this product, weigh it accurately, place it in a 100ml measuring bottle, add about 70ml of mobile phase to dissolve it, and then dilute to the mark with mobile phase, shake well, and accurately measure 10l into the liquid chromatograph and record the chromatogram; Take cefradine reference solution and measure in the same way. Calculate the peak area according to the external standard method.

Cefraditin Category

-lactam antibiotics, cephalosporins.

Cefradine storage

Shaded, nitrogen-filled, sealed, and stored below 10 ° C.

Cefala custom

(1) Cefradine dry suspension (2) Cefradine tablets (3) Cefradine capsules (4) Cefradine particles (5) Cefradine for injection ^[2]

Cefraditin Drug Description

Cefradine pharmacology and toxicology

Cefraditin is a broad-spectrum antibiotic with the same mechanism of action as other cephalosporins. It inhibits the synthesis of bacterial cell walls. It has bactericidal effect on gram-positive and negative bacteria, is stable under acidic conditions, and can be absorbed quickly on an empty stomach without being affected by penicillinase. It also has significant effects on most of Staphylococcus aureus and Escherichia coli that produce penicillinase. Antibacterial activity.

Cefraditin has good antibacterial effect on some strains of Gram-positive cocci that do not produce penicillinase and penicillinase-producing Staphylococcus aureus, coagulase-negative staphylococcus, group A hemolytic streptococcus, pneumococcus, and Streptococcus grass green.

Anaerobic gram-positive bacteria are more sensitive to this product, and B. fragile is resistant to this product.

Methicillin-resistant Staphylococcus and Enterococcus are resistant to this product.

This product has similar effects on gram-positive and gram-negative bacteria as cephalexin.

This product has a certain effect on Neisseria gonorrhoeae, and it is active against Neisseria gonorrhoeae producing enzymes; its activity against Haemophilus influenzae is poor.

Antibacterial effect against Gram-positive bacteria including penicillin-sensitive and resistant Staphylococcus aureus (except methicillin-resistant Staphylococcus aureus) is stronger than that of second- and third-generation cephalosporins; against Gram-negative bacteria The effect is less than that of the second-generation cephalosporins, and even less than that of the third-generation cephalosporins;

It is unstable to -lactamase produced by Gram-negative bacilli, but it is more stable to -lactamase produced by Staphylococcus aureus than the second and third generation cephalosporins.

Cefraditin pharmacokinetics

Cefradine is rapidly absorbed after oral administration, and reaches a peak plasma concentration (Cmax) of 11 to 18 mg / L within 1 hour after oral administration of 0.5 g on an empty stomach, and the blood elimination half-life (t1 / 2) is 1 hour. After intravenous injection of 0.5 g, the blood drug concentration was 46 g / ml after 5 min; when intramuscular injection of 0.5 g, the blood drug concentration reached a peak value of 6 g / ml after 1 to 2 hours.

Cefraditin is well distributed in tissue and body fluids, and the concentration in liver tissue is equal to the serum concentration, and effective concentrations can be obtained in cardiac muscle, uterus, lung, prostate and bone tissue.

The concentration of the drug in the brain tissue is only 5% to 10% of the blood concentration in the same period, and the concentration in the cerebrospinal fluid is lower. (Intravenous infusion of 2 to 4 g, the concentration in the cerebrospinal fluid is only 1.2 to 1.5 g / ml).

Cefraditin can enter the fetal blood circulation through the blood-placental barrier, and a small amount is excreted through milk. 500 mg orally, the concentration in amniotic fluid was about 1.3 g / ml.

Cefraditin serum protein binding rate is 6% to 10%. The half-life is about 1h.

Over 6 hours, more than 90% of the total dose is excreted, and a small amount can be excreted from the bile. The concentration of the latter can be 4 times that of the serum. After oral administration of 0.5g, the urine output in 24 hours exceeded 99% of the administered dose; 6 hours after intravenous injection, the urine output exceeded 90% of the administered dose; 6 hours after intramuscular injection, the urine output was approximately 66% of the administered dose. %; Another small amount of drugs can be excreted with bile.

Cefraditin is rarely metabolized in the body and can be cleared for hemodialysis and peritoneal dialysis.

Cefradine dosage and usage

Oral, adults, 0.25g to 0.5g / time, 6 hours times / day, up to 4g (16 capsules) per day. Pediatric weight once 6.25 ~ 12.5mg / kg, once every 6 hours. Intramuscular or intravenous injection, adults, 0.25g ~ 0.5g / time, 3 ~ 4 times / day. For severe infections can increase to 4g per day.

Oral administration

(1) Adults:

Mild infection, 0.25 ~ 0.5g once, 3 ~ 4 times a day.

Moderate infection: 0.5 1g once, 3 4 times a day.

The total amount per day does not exceed 4g.

(2) Children: 6.25 to 12.5 mg / kg once, once every 6 to 8 hours.

Intravenous

Adult: 0.5 1g each time, once every 6 hours, intravenous drip or intravenous injection. The maximum daily amount is 8g;

Pediatrics (over 1 year old): 12.5 25mg / kg each time, once every 6 hours, intravenous drip or intravenous injection.

Renal insufficiency dose

Patients with impaired renal function must reduce the dose or extend the interval between administrations. When creatinine clearance is greater than 20ml per minute, the recommended dose is 0.5g every 6 hours; when creatinine clearance is 5-20ml per minute, the dose is 0.25g every 6 hours; when creatinine clearance is less than 5ml per minute, the dose It is 0.25g every 12 hours.

Cefradine indications

It is suitable for acute pharyngitis, tonsillitis, otitis media, bronchitis, and pneumonia caused by sensitive bacteria, respiratory infections, urogenital infections, and skin and soft tissue infections. It is an oral preparation and should not be used for severe infections.

It is also commonly used to prevent infections after surgery. Arginine salt injection is used for patients with heart and kidney insufficiency. This dosage form does not easily cause sodium retention.

Cefraditin precautions

(1) Use with caution in pregnant and lactating women.

Cefraditin can pass through the placental barrier and should be used with caution during pregnancy.

Cefraditin can temporarily change the baby's intestinal flora balance and cause diarrhea. It should be used with caution in breastfeeding women.

(2) Use with caution in patients with liver and kidney dysfunction and those with a history of gastrointestinal diseases.

(3) Use with caution in patients with gastrointestinal diseases, especially antibiotic-associated enteritis.

(4) Cefraditin is mainly excreted through the kidneys. Those with impaired renal function must reduce the dose or extend the interval between administrations.

(5) Long-term medication can also cause secondary infection.

(6) People who are allergic to one cephalosporin may be allergic to other cephalosporins. People who are allergic to penicillins and penicillin derivatives may also be allergic to cephalosporins.

(7) The influence of the drug on the test value or diagnosis: (1) the direct anti-human globulin (Coombs) test can be positive; (2) the copper sulfate method can be false positive.

(8) Liver, kidney function and blood image should be checked when long-term use.

Cefraditin Drug Interactions

(1) Combined with gentamicin or amikacin, it has a synergistic antibacterial effect on some sensitive strains, but it can increase renal toxicity.

(2) Cephalosporin can delay the excretion of phenytoin sodium in the renal tubules, probenecid can reduce the renal excretion of cefradine.

(3) Combined with nephrotoxic drugs (such as potent diuretics, aminoglycosides and antitumor drugs, etc.), it can increase nephrotoxicity.

(4) Combined with mecillin, it has a synergistic effect on Gram-negative bacteria such as Escherichia coli and Salmonella.

Cefraditin adverse reactions

Cefraditin has mild adverse reactions with an incidence of about 6%. Nausea, vomiting, diarrhea, and upper abdominal discomfort are common. The incidence of drug eruption is 1% to 3%. Pseudomeningitis, increased eosinophils, decreased peripheral leukocytes and neutrophils are seen in individual patients. A small number of patients may have transient elevated blood urea nitrogen, and transient increases in serum aminotransferase and serum alkaline phosphatase.

1. Mainly rash, drug fever, etc., occasionally anaphylactic shock.

2. Digestive system: Nausea, vomiting, diarrhea, and abdominal discomfort are more common, and occasionally pseudomembranous enteritis.

3. Blood system: A small number of patients may have eosinophilia, total white blood cells, or neutrophils after treatment.

4. Renal toxicity: A small number of patients may have temporary elevated urea nitrogen after administration, but no serious renal toxicity has been reported.

5. Hepatotoxicity: A few patients may have transient elevations in alkaline phosphatase, serum alanine aminotransferase and aspartate aminotransferase after administration.

6. Others: Cefradine is more pronounced at the site of intramuscular injection, and phlebitis has been reported after intravenous injection.

Cefradine poisoning

Cefraditin (ceftazidime, pioneer ) belongs to the first generation of cephalosporins and has an antibacterial effect similar to that of cephalexin. Oral absorption is good, poor absorption after intramuscular injection, plasma protein binding rate is 6% to 10% lower, and half-life is 16.3h. It is used to treat respiratory infections, genitourinary tract infections and soft tissue infections caused by sensitive bacteria. Can be administered orally and intravenously. The maximum oral dose is 4g / d. It can be injected intravenously in severe infections, and occasionally thrombophlebitis occurs. People who are allergic to penicillin should use this medicine with caution. Allergies and severe renal insufficiency should be used with caution.

For treatment points, please refer to the related content of cephalexin:

1. Taking this medicine for people with impaired renal function can cause the half-life of this medicine to be prolonged in the body and aggravate kidney damage. Long-term and large-scale administration should be avoided.

2. When an allergic reaction occurs, the drug should be stopped immediately and anti-allergic treatment should be given.

3. When a double infection occurs, treat it according to the pathogenic microorganism.

4. Hemodialysis and hemoperfusion can effectively remove the drug from the body ^[3] .

Cefradine injection

Pharmacological action

This product is a broad-spectrum, high-efficiency, low-toxic antibiotic, which has a bactericidal effect on Gram-positive and negative bacteria. This product is not affected by penicillinase and has significant activity against most Staphylococcus aureus and E. coli producing penicillinase. Properties: This product is a white or off-white powder mixed with cefradine and arginine, easily soluble in water.

dynamics

Indications apply to staphylococcus, hemolytic streptococcus, pneumococcus, E. coli, Proteus mirabilis and other indole-negative Proteus, Haemophilus influenzae, Shigella, Salmonella, and Neisseria , Including: urinary tract infections: cystitis, pyelonephritis. Respiratory infections: pharyngitis, otitis media, tonsillitis, bronchitis, lobar pneumonia, bronchial pneumonia. Gastrointestinal infections: dysentery, enteritis, peritonitis. Infectious diseases of the skin, soft tissues, bones and joints are also effective for sepsis and endocarditis.

Dosage

The product can be used for intravenous injection, intramuscular injection, intravenous drip, intraperitoneal injection. In severe cases, intravenous injection is appropriate when starting treatment. Immediately before use, add 2ml of diluted solution to dissolve for intramuscular injection and intravenous injection. At room temperature, the solution should be used within 2 hours. Store the solution at 5 for 12 hours. Intravenous infusion can be added to 5% or 10% glucose injection or sodium chloride, Ringer's and other injections. Patients with peritonitis can be injected intraperitoneally.

Commonly used amount: Adults 2-4g a day, divided into 4 injections, severely infected patients can increase to 8g a day. Children are calculated at 50-100 mg per kg of body weight per day and divided into 4 injections, and severe cases can be increased to 200-300 mg per kg of body weight per day. Patients need to continue treatment for 48-72 hours after the symptoms have disappeared or the bacteria have been killed. For infections caused by hemolytic streptococcus, in order to prevent concurrent rheumatic diseases or glomerulonephritis, it needs to be treated for at least 10 days. Long-term infectious diseases may Needs treatment for weeks.

Adverse reactions

The side effects of this product are similar to other cephalosporins. Occasionally, gastrointestinal dysfunction, glossitis, heartburn, nausea, vomiting, diarrhea, urticaria, arthralgia, and mild eosinophilia, and lactic acid degeneration in some patients Catalase, serum transchlorinase are temporarily elevated.

Taboo

Precautions 1. Cephalosporin and penicillin have partial cross-sensitivity. Use with caution in patients who are allergic to penicillin. Those who are allergic to cephalosporin antibiotics are prohibited. 2. Patients with renal insufficiency should be reduced as appropriate. 3. This product may appear false positive in urine glucose test.

Formulation specifications

(1) 0.5g (calculated based on C16H19N3O4S) (2) 1.0g (calculated based on C16H19N3O4S)

Cefraditin capsule products

Pharmacological action

The structure of this product is closely related to cephalexin. Its antibacterial spectrum and antibacterial effect are similar to those of cephalexin. It is relatively stable to -lactamase, resistant to Staphylococcus aureus and many other bacteria resistant to broad-spectrum antibiotics. Reliable bactericidal effect. It has antibacterial effect on Staphylococcus aureus, hemolytic streptococcus, Streptococcus pneumoniae, E. coli, Proteus mirabilis, Klebsiella pneumoniae, Haemophilus influenzae, etc.

dynamics

This product is acid-resistant, good oral absorption, peak blood drug concentration reached about 1h, high blood drug concentration, although food can delay absorption but does not affect the total absorption. The product is also injected intramuscularly or intravenously. The peak concentration of the blood drug reaches 1 to 2 hours during the intramuscular injection, and the peak value is also lower than that when taken orally, but the total absorption is equal. The study found that after injection of the gluteus maximus, women's absorption is slower than men's and the peak plasma concentration is lower. The protein binding rate is about 10% -20% lower. Although the product can be distributed in most tissues, the concentration in the cerebrospinal fluid is difficult to reach the therapeutic level. The product is mainly secreted by the renal tubules and floats out in its original shape. Higher concentrations in urine. The product can penetrate the placenta. The product has a half-life of about 50 minutes, prolonged when renal insufficiency, and the dose is adjusted accordingly. The renal toxicity of this product is slight.

Indication

It is mainly used for respiratory, urinary tract, skin and soft tissue infections such as bronchitis, pneumonia, pyelonephritis, cystitis, otolaryngology, enteritis, and dysentery. treatment. Injections are also used for sepsis and bone infections.

Dosage

Adults take 1 to 2 g orally daily, divided into 3 to 4 doses. Children 25 to 50 mg / kg daily, divided into 3 to 4 times. Intramuscular, intravenous or instillation, 2 to 4 g per day for adults, divided into 4 injections; 50 to 100 mg / kg per day for children, divided into 4 injections. Patients with renal insufficiency formulate a dosing plan according to the creatinine clearance rate of patients: those whose muscle and liver clearance rate is> 20ml / min, take 500mg every 6 hours; those who are 15-20ml / min, take 25Omg every 6 hours; those who are <15ml / min, each Take 250mg for 12 hours.

Adverse reactions

(1) Adverse reactions mainly include gastrointestinal dysfunction, such as nausea, vomiting, diarrhea, and rash. This product has some cross-allergic reactions with penicillin. This product is mildly toxic to kidneys and has almost no effect on renal function.

(2) Food does not affect total absorption, but it should be taken on an empty stomach to achieve the desired effect.

(3) The injections include those containing arginine and sodium carbonate. Those who have arginine are not likely to cause sodium retention for those with heart and kidney insufficiency. They should be selected appropriately in the application.

Precautions

(1) People with allergies to penicillin or allergies and those with renal insufficiency should be used with caution. Those who are allergic to cephalosporin antibiotics are prohibited.

(2) The injection is less irritating and suitable for intramuscular injection.

(3) Can cause side effects such as dysbiosis, vitamin deficiency, and double infection. Store medicines in a dry, cool place to avoid heat.

preparation

Capsules: 0.25g per capsule; 0.5g. Dry suspension: 0.125g; 0.25g. Cefradine for injection (sodium carbonate added): 0.5g per bottle; 1g. Cefradine A for injection (with arginine added): 0.5g per bottle; 1g.

Cefradine Granules

dynamics

The product is quickly absorbed after oral administration. The fasting oral concentration of 0.5 g, the peak plasma concentration (Cmax) of 11 to 18 mg / L is reached 1 hour after administration, and the blood elimination half-life (t1 / 2) is 1 hour. The product is well distributed in tissue fluids. The concentration in liver tissue is equal to the serum concentration. Effective concentrations can be obtained in myocardium, uterus, lung, prostate and bone tissue. The concentration of the drug in the brain tissue is only 5% to 10% of the blood concentration in the same period, and the concentration in the cerebrospinal fluid is lower. The product can enter the fetal blood circulation through the blood-placental barrier, and a small amount is excreted through milk. The serum protein binding rate was 6% to 10%. Over 90% of the cumulative dose was administered 6 hours after oral administration of 0.5 g. A small amount of this product can be excreted from the bile, the latter concentration can be 4 times the serum concentration. The product is rarely metabolized in the body and can be cleared for hemodialysis and peritoneal dialysis. Probenecid reduces renal excretion of this product

Indication

It is suitable for acute pharyngitis, tonsillitis, otitis media, bronchitis and pneumonia caused by sensitive bacteria, respiratory infections, urogenital infections and skin and soft tissue infections.

Dosage

Oral adult dose: 0.25-0.5g once, once every 6 hours, the severe infection can increase to 1g once, but the total amount in a day does not exceed 4g. Commonly used amount for children: 6.25 12.5mg / kg by weight, once every 6 hours.

Adverse reactions

The product has mild adverse reactions and a low incidence, about 6%. Nausea, vomiting, diarrhea, and upper abdominal discomfort are common. The incidence of drug eruption is about 1% to 3%. Pseudomembranous colitis, eosinophilia, positive direct Coombs test response, decreased peripheral blood leukocytes and neutrophils, dizziness, chest tightness, candida vaginitis, and allergic reactions are seen in Individual patients. A small number of patients may have transient elevated blood urea nitrogen, and transient increases in serum aminotransferase and serum alkaline phosphatase.

Taboo

This product and other cephalosporins are banned.

Precautions

1. Before applying this product, the patient must be asked in detail about the history of allergies to cephalosporins, penicillins and other drugs. People with a history of penicillin-type anaphylactic shock should not use this product. Other patients should use it with caution. Care must be taken when applying this product The chance of cross-allergic reactions between cephalosporins and penicillins is about 5% to 10%, and it should be used with caution under close observation. In the event of an allergic reaction, the drug is discontinued immediately. If anaphylactic shock occurs, rescue must be carried out immediately, including keeping the airway open, inhaling oxygen and using adrenaline and glucocorticoids.

2. This product is mainly excreted by the kidney. Those with impaired renal function must reduce the dose or prolong the administration interval. 3. Patients who use this product may have a false positive reaction when measuring urine glucose by copper sulfate method. Because the product can enter the fetal blood circulation through the blood-placental barrier, pregnant women need accurate indications for medication. This product can also enter a small amount of milk. Although there have been no reports of problems with cephalosporins in lactating women, it is still necessary to weigh the advantages and disadvantages before applying. Elderly patients are often accompanied by impaired renal function. The dose should be appropriately reduced or the interval between administrations should be extended.

Overdose

The drug should be discontinued in time, and symptomatic and supportive treatment should be given. Cefradine can be removed by hemodialysis and peritoneal dialysis.

interaction

1. Cephalosporins can delay the excretion of phenytoin in the renal tubules.

2. Combination of Baotaisong and cephalosporin antibiotics can increase renal toxicity.

3. Combined with strong diuretics, can increase renal toxicity.

4. Combined with mecillin, it has a synergistic effect on Gram-negative bacteria such as Escherichia coli and Salmonella.

5. Probenecid can delay renal excretion of this product.

preparation

(1) 0.125g

(2) 0.25g

News related to cefradine adverse reactions

Warning: About Hematuria

China Food and Drug Administration: Watch out for adverse reactions to acyclovir and cefradine

China News Service, January 12th. According to the website information of the State Administration of Drug Administration, the State Food and Drug Administration recently reminded medical workers, drug manufacturers and the general public to be vigilant about Acyclovir according to the report of the National Drug Adverse Reaction Monitoring Center. Wei and cefradine adverse reactions.

Data from the National Adverse Drug Reaction Monitoring Center Case Report Database show that acyclovir-induced acute renal impairment and cefraditin-induced hematuria are still prominent.

In order to make medical workers, drug manufacturers and the public aware of this situation, the State Food and Drug Administration reminds clinicians that when choosing medicines, they should conduct a full benefit / risk analysis and pay close attention to acyclovir during the medication process. Severe adverse reactions of weiwei and cefradine; related manufacturers should conduct in-depth research on the acute renal impairment caused by acyclovir and the mechanism of hematuria caused by cefradine, comprehensively evaluate the benefits / risks of these two varieties, and take effective measures in a timely manner to minimize them The repeated occurrence of adverse reactions of similar drugs to ensure the safety of public medication.

The State Food and Drug Administration will continue to pay attention to the safety issues of the above-mentioned varieties, timely feedback related information, and ensure the public's drug safety to play its due role.