Alias: ampicillin, ampicillin, ampicillin, Savicillin, Simicillin, ampicillin, Pampatine, AB-PC.
References & gt
Ampicillin (Penbritin, BRL 134 1)
Function and use
This product is a broad-spectrum semi-synthetic penicillin with extremely low toxicity. The antibacterial spectrum is similar to that of penicillin, and the curative effect of bacteria sensitive to penicillin is low, and the antibacterial effect on Streptococcus viridis is similar to or slightly stronger than that of penicillin. Its curative effect on diphtheria, tetanus and actinomycetes is basically the same as that of penicillin. It has better effect on enterococcus and Listeria than penicillin. It has no antibacterial effect on drug-resistant staphylococcus and other bacteria that can produce penicillinase. It is effective for gram-negative bacteria, but it is easy to produce drug resistance.
This product is mainly used for urinary system, respiratory system, biliary tract and intestinal infection, meningitis and endocarditis caused by sensitive bacteria.
Mainly used for treating typhoid and paratyphoid; It is also used for urinary tract and respiratory tract infections.
Dosage and usage
Oral, 2g ~ 6g/ day, divided into 3 ~ 4 times, and taken on an empty stomach. Children, daily 100mg/kg, divided into 3 ~ 4 times, taken on an empty stomach. Intramuscular injection or intravenous injection, 2g ~ 4g/ day for adults; Children, 50 mg ~ 100 mg/kg daily, generally every 4 ~ 6 hours 1 time. Intravenous administration can be divided into slow intravenous injection or intravenous drip; Intravenous drip, 1 time 1 g ~ 2 g, dissolved in 100ml infusion, drip 1/2 ~ 1 hour, 2 ~ 4 times/day. Children, daily100 mg/kg ~150 mg/kg, given in batches.
side effect
1 This product can cause anaphylactic shock, and the incidence of rash is higher than that of penicillin. Sometimes there will be drug fever.
Skin test must be done before injection of this product, and only those who are negative can use it. People with a history of penicillin allergy are prohibited.
Common name: ampicillin
English name: ampicillin
Chinese aliases: ampicillin, ampicillin sodium, ampicillin, ampicillin.
English aliases: Alpen, Amperil, Ampicillin, Ampicillin, Omnipen, Penbritin, Penbriton, Polycillin, Principen, Servicillin, Ampicillin Sodium.
Pharmacology and pharmacodynamics
See penicillin. The antibacterial effect of ampicillin on gram-positive cocci and bacilli (including anaerobic bacteria) is basically the same as that of penicillin, but the effect on fecal cocci is weaker than that of penicillin. Gram-negative bacteria such as meningococcus, Neisseria gonorrhoeae, Influenza Bacillus, Bordetella pertussis, Brucella, Proteus and Salmonella are all sensitive to this product. Most Escherichia coli and some Shigella are also sensitive to this product, but the latter can quickly develop drug resistance. Ampicillin has antibacterial effect on Legionella and Campylobacter fetus. Except Bacteroides fragilis, most other anaerobic Gram bacilli are sensitive to this product.
pharmacokinetics
After intramuscular injection of 0.5g ampicillin, the plasma concentration reached the peak within 0.5 ~ l hours, and the peak concentration was 12 (7 ~ 14) μ g/ml. The blood concentration for 6 hours was 0.5 μ g/ml. The plasma concentrations of 15 minutes and 4 hours after intravenous injection of 0.5g were 17 and 0.6μg/ml, respectively. This product is quite stable to gastric acid, so it is well absorbed after oral administration, but it is affected by food. After oral administration of lg on an empty stomach, the plasma concentration reached a peak of 7.6μg/ml within 2 hours and 65438 0.65438 0 μ g/ml within 6 hours. T 1/2 is 1.5 hours. After intramuscular injection of 10mg/kg and 25mg/kg 1 hour according to body weight, the plasma concentration reached the peak, which were 20 and 60μg/ml respectively, and the T 1/2 was 1.7 ~ 4 hours. The serum concentration of ampicillin in pregnant women was significantly lower than that in non-pregnant women. Ampicillin is evenly distributed in the body. Patients with bacterial meningitis are given intravenous injection of 150mg/kg according to their body weight every day, and the concentration in cerebrospinal fluid can reach 2.9μg/ml in the first three days, and then it will decrease with the reduction of inflammation. Normal cerebrospinal fluid contains only a small amount of ampicillin. This product can reach the fetal circulation through the placenta and has a continuous concentration in amniotic fluid. The concentration in bronchial secretions of patients with pulmonary infection is 1/50 of the blood concentration in the same period. Pleural and abdominal water, joint cavity effusion, aqueous humor and milk all contain a considerable amount of this product. The average bile concentration in B duct of typhoid fever carriers is more than 3 times of the blood drug concentration, and the highest can reach 17.8 times. The delivery volume of this product is 0.28L/kg. Protein binding rate is 20 ~ 25%. 12 ~ 50% of this product is metabolized in the liver. The renal clearance rate of ampicillin is slightly lower than that of penicillin, some of which are filtered through glomeruli and some are secreted through renal tubules. 24 hours after oral administration, 20 ~ 60% of ampicillin was excreted in urine, 50% by intramuscular injection and 70% by intravenous injection. A small amount (0. 1%) is excreted from bile. Probenecid can slow down the clearance of this product in the kidney. Ampicillin can be removed by hemodialysis, but peritoneal dialysis has no effect on this product.
indicate
Can be used for treating respiratory tract infection, gastrointestinal tract infection, urinary tract infection, soft tissue infection, meningitis, septicemia, endocarditis, etc. Caused by sensitive bacteria.
dosage
1. Adult intramuscular injection dose is 2 ~ 4g per day, given in four times; The dosage of intravenous injection is 4 ~ 12g daily, divided into 2 ~ 4 times, and the maximum dosage per day is 16g.
2. The dosage of intramuscular injection for children is 50 ~ 100 mg/kg every day, divided into 4 times; The dosage of intravenous administration is 100 ~ 200mg/kg, divided into 2 ~ 4 times, and the maximum daily dosage is 300mg/kg.
3. Full-term newborns are given intramuscular injection or slow intravenous injection every time according to their weight 12.5 ~ 50mg/kg; Every 12 hours within 48 hours after birth; Every 8 hours from the third day to the second week, and every 6 hours thereafter. Premature infants in the first week, 1 ~ 4 weeks and above are 12.5 ~ 50mg/kg each time, 12 hours once, once every 8 hours and once every 6 hours.
4. The half-life of ampicillin in patients with renal failure and advanced renal failure can be extended from 1.5 hours to 7-20 hours in normal people, so when the GFR is 10- 15 ml/min and less than 10ml/min, the administration interval of ampicillin should be extended to 6.
5. Adults should take 2 ~ 4g orally every day, divided into 4 times; Children take 50 ~ 100 mg/kg daily, four times.
[Preparation and specifications] Based on ampicillin. Ampicillin sodium capsules (1) 0.25g (2) 0.5g.
Ampicillin sodium for injection (1) 0.5g(2) 1g
Oral administration: 0.25- 1g once, 4 times a day; Intramuscular injection: 4-6g daily, divided into 4 times; Intravenous drip: 4- 12g daily, divided into 2-4 times, children daily 100- 150mg/kg.
Don't be careful
People who are allergic to penicillin should not use it.
Management description
See penicillin sodium. The application of ampicillin to pregnant women in the third trimester of pregnancy can reduce the concentration of conjugated estrogen in plasma, but it has no effect on unbound estrogen and progesterone.
counteraction
The adverse reactions of this product are similar to those of penicillin sodium, and allergic reactions are more common. Rash is the most common reaction, which usually occurs 5 days after taking medicine. It is urticaria or maculopapular rash. The former is a typical allergic reaction rash of penicillin, while the latter is specific to ampicillin. The incidence of rash after injection is higher than that after oral administration. Infectious mononucleosis, cytomegalovirus infection, lymphocytic leukemia, lymphoma and other patients. Rash is easy to occur when using this product, so this product cannot be used for these patients. Granulopenia and thrombocytopenia are rare in patients who use ampicillin, and ampicillin-related enteritis is also extremely rare. A few patients have elevated serum alanine aminotransferase. High-dose intravenous injection of ampicillin can cause nervous system toxic symptoms such as convulsion, and infants can have increased intracranial pressure after injection of ampicillin, showing chimney uplift. A very large amount of ampicillin may cause hearing damage, but the ototoxicity of ampicillin has not been finally determined. Interstitial nephritis caused by ampicillin has also been reported.
Prevention and treatment of adverse reactions of ampicillin are the same as penicillin sodium.
Can cause rash, drug fever, chills, facial flushing pallor, wheezing, dyspnea, palpitation, chest tightness, cyanosis, abdominal pain, anaphylactic shock, etc. After oral administration, nausea, vomiting and diarrhea may occur in 1 case. A few patients may have leukopenia, temporary increase of serum transaminase, acute parotid swelling and abnormal renal function.
The incidence of ampicillin rash is 3. 1 ~ 18%, which often occurs 7 ~ 12 days after the start of treatment, and is caused by allergic reaction. The maculopapular rash accounts for 2/3 of the whole rash. The incidence of maculopapular rash and purpura rash in patients with mononucleosis is 42 ~ 100%, and the incidence of rash in patients with renal insufficiency is also high.
The onset of drug eruption has nothing to do with the duration and dose of medication, but with the infected disease, age and sex. The incidence of drug eruption in typhoid patients and patients with gram-negative bacilli septicemia is the highest. Connective tissue disease, leukemia and tumor complicated with infection are the second, and drug eruption in patients with hepatobiliary and urinary tract infections is higher than that in patients with gastrointestinal and respiratory tract infections. The incidence of drug eruption in patients with viral diseases, epidemic hemorrhagic fever, encephalitis and infectious mononucleosis is obviously higher. The incidence of drug eruption in people under 50 years old was significantly higher than that in people over 50 years old (17.5% vs. 5.4%) (P < 0.0 1), and the incidence in women was significantly higher than that in men (16.8% and 7.3% respectively, P < 0.0 1).
A few patients may develop nephropathy, which is an immune response. Immune complex and complement components can be deposited in glomeruli and blood vessels, leading to glomerulonephritis. It has been reported that intravenous injection of ampicillin sodium has promoted the rapid deterioration of hypertension. The analysis shows that ampicillin is easy to cause allergic interstitial nephritis and increase renin, which leads to secondary hypertension. After oral administration of this product 1 week, about 1 1% patients developed diarrhea. Patients with elevated transaminase have 1/4. Chen Fengyun reported that eight patients were injected with ampicillin intravenously for other infectious diseases. After taking the medicine, skin itching and rashes of different shapes appeared, and liver damage occurred to varying degrees. Among them, 2 patients with hepatitis B died due to the aggravation of their illness. Japanese scholars pointed out that drug-induced allergic liver injury is due to the direct damage of drugs to the liver, which changes some cell membrane components of hepatocytes, and the free carrier protein combines with drugs to obtain antigenicity, thus causing allergic liver injury. Patients with urinary tract infection may have double infections of Proteus, Aeromonas and Candida albicans during treatment.
Interaction See Synonyms at penicillin sodium.
(1) The combined application of ampicillin and chloramphenicol has different antibacterial effects on influenza Bacillus in vitro. At high concentration (5 ~ 10μ g/ml), chloramphenicol has no antagonistic effect on this product, and at low concentration (1 ~ 2μ g/ml), it can weaken the bactericidal effect of ampicillin, but it has no antibacterial effect on chloramphenicol. The effects of ampicillin combined with chloramphenicol on the antibacterial activity of meningococcal strain 2 1 in vitro are as follows: antagonistic strain 13, cumulative strain 5 and synergistic strain 3. Only 1 strain showed antagonistic effect on 2 1 strain of pneumococcus, 14 strain showed cumulative effect, and 6 strains showed synergistic effect. Lincomycin can inhibit the antibacterial effect of ampicillin on Staphylococcus aureus in vitro. Kanamycin can enhance the antibacterial effect of ampicillin on Escherichia coli, Proteus and Enterobacter in vitro. Gentamycin can accelerate the bactericidal effect of ampicillin on group B streptococcus in vitro. The minimum inhibitory concentration of ampicillin or amoxicillin on Neisseria gonorrhoeae producing β -lactamases was 64μg/ml, and the minimum inhibitory concentration of these two penicillins could be reduced to 4μg/ml by combined application of clavulanic acid.
(2) This product is not compatible with the following drugs: amikacin sulfate, kanamycin, gentamicin, streptomycin, clindamycin phosphate, lincomycin hydrochloride, sodium colistin methanesulfonate, polymyxin B, chloramphenicol succinate, erythromycin ethylsuccinate, lactobionic acid, tetracycline injection, neomycin, adrenaline, m-hydroxylamine, dopamine, atropine, hydrazine hydrochloride, hydrolyzed protein, calcium chloride. Vitamin C, nutritional injections containing amino acids, polysaccharides (such as dextran 40) and hydrocortisone sodium succinate can inactivate ampicillin.
(3) Allopurinol can increase the incidence of ampicillin rash reaction, especially in hyperuricemia. The incidence of long-term sequelae is higher when chloramphenicol and ampicillin are used together than when they are used alone.
(4) ampicillin can stimulate estrogen metabolism or reduce its intestinal and hepatic circulation, thus reducing the effect of oral contraceptives.
Drugs for children and drugs for elderly patients
Elderly patients should adjust the dosage or interval of medication according to renal function.
Matters needing attention
1. Every time before starting to use this product, patients must have a penicillin skin test. 2. Use with caution those who are allergic to cephalosporins and those who have a history of allergic diseases such as asthma, eczema, hay fever and urticaria. 3. This product has cross allergic reaction with other penicillins. If allergic reaction occurs, stop using this product immediately and take corresponding measures. 4. Patients with renal insufficiency should adjust the dosage or administration interval according to the plasma creatinine clearance rate. 5. For gonorrhea patients who are suspected to have syphilis damage, dark field examination should be conducted before using this product, and serum examination should be conducted once a month for at least four consecutive months. 6. Long-term or high-dose application of this product should regularly check the functions of liver, kidney and hematopoietic system, and detect serum potassium or sodium. 7. Interference of laboratory indicators: (1) False positive can be found in urine sugar test by copper sulfate method, but glucoamylase test method is not affected; (2) It can increase the measured value of serum alanine aminotransferase or aspartate aminotransferase.
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