What Are the Most Common Ampicillin Side Effects?

Bamcillin is a semi-synthetic amino penicillin. It is a new prodrug developed on the basis of ampicillin by Astra Lakemedel Laboratory in Sweden. . It can be completely absorbed by the gastrointestinal tract, and its hydrochloride is usually used as an oral preparation. Bamcillin hydrochloride as a prodrug does not have antibacterial activity itself, but it can be hydrolyzed into active ampicillin and released into the blood after oral administration.

Paroxacillin Hydrochloride

Bamcillin is a semi-synthetic amino penicillin. It is a new prodrug developed on the basis of ampicillin by Astra Lakemedel Laboratory in Sweden. It is 1-ethoxycarbonyl hydroxyethyl ester of ampicillin. . It can be completely absorbed by the gastrointestinal tract, and its hydrochloride is usually used as an oral preparation. Bamcillin hydrochloride as a prodrug does not have antibacterial activity itself, but it can be hydrolyzed into active ampicillin and released into the blood after oral administration.

Drug Name

Paroxacillin Hydrochloride

Foreign name

Bacampicillin Hydrochloride Tablets

Storage method

Airtight storage

Storage

Shading, sealed and stored in a cool place

Bamcillin hydrochloride, bamcillin hydrochloride, baccillin hydrochloride, ampicillin mevaleryl hydrochloride, ampicillin hydrochloride carbonate, baccillin hydrochloride, Bacampicillin Hydrochloride

The antibacterial spectrum and antibacterial activity of bacilcillin are similar to those of ampicillin.

Take an appropriate amount of the fine powder of this product, add anhydrous ethanol to make a solution containing 2mg of ampicillin per 1ml, as a test solution; take a reference of paroxacillin hydrochloride, and add absolute ethanol to make 1ml A solution containing 2mg was used as a reference solution and tested according to thin-layer chromatography (Chinese Pharmacopoeia 1995 Version Two Appendix V B). Two 5l portions of each test solution were pipetted to the same 0.25mm thick silicone G thin layer. On the plate, after drying, take another 5l each of the reference solution, one point in the middle of the two test solution points, and the other point on the one test solution point. After drying, use dichloromethane-chloroform- Ethanol (10: 1: 1) was used as a developing agent. After the development, it was dried and sprayed with butanol-ninhydrin-pyridine (100: 1: 1).

The solution was heated at 100 ° C for 10 minutes, and immediately inspected. Parmoxacillin hydrochloride showed purple spots. The Rf value of the test solution and the Rf value of the spot mixed with the test solution and the reference solution should be the same as the Rf of the spot of the reference solution. The values are consistent.

Take the product for dissolution, according to the dissolution method (Chinese Pharmacopoeia 1995 edition, Appendix XC, second method),

Water was used as the solvent, and the rotation speed was 75 revolutions per minute. According to the law, after 30 minutes, take an appropriate amount of the solution, filter it, and take the filtrate for further use. Another appropriate amount of paroxcillin hydrochloride reference was made with water to make 0.44mg per 1ml. The solution. Take the above two solutions and measure the absorbance at the wavelength of 257nm by spectrophotometry (Appendix IV A of the Second Part of Chinese Pharmacopoeia 1995 Edition). Calculate the dissolution amount of each tablet according to the ratio of the absorbance of the two. The limit is 85% of the labeled amount, which should meet the requirements.

Moisture is taken from this product and measured according to the Moisture Determination Method (Appendix M of the Chinese Pharmacopoeia 1995 Edition, M first method). The moisture content must not exceed 2.5%.

Others shall comply with the relevant provisions under the tablet (Chinese Pharmacopoeia 1995 Edition Appendix II A).

Take 10 tablets of this product, after removing the film coating, weigh it carefully, grind it fine, and accurately weigh an appropriate amount (approximately equivalent to 626mg of ampicillin), place it in a 250ml measuring bottle, add water to dissolve and dilute to the mark, shake well, and use dry filter paper After filtration, take 50ml of the filtrate and place it in a 100ml volumetric flask. Dilute with water to the mark and shake well to obtain a test solution equivalent to approximately 1.25mg / ml of ampicillin. Take 5ml of the precise amount and place it in an iodine bottle. Add 5ml of 1mol / L sodium hydroxide solution, leave it for 15 minutes, add 5ml of 1.2mol / L hydrochloric acid solution, shake well, add 25ml of iodine titration solution (0.01mol / L) precisely, stopper, and avoid light at 20 25 Let stand for 15 minutes, titrate with sodium thiosulfate titration solution (0.01mol / L), add starch indicator solution to the end point, and continue the titration until the blue color disappears; take another precise amount of 5ml of the test solution, place it in an iodine bottle, add 1.00 0.3ml of mol / L hydrochloric acid solution, shake well, add 25ml of iodine titration solution (0.01mol / L) precisely, tightly block, and leave it at 20 25 in the dark for 15 minutes, then use sodium thiosulfate titration solution (0.01mol / L L) Titration. The difference between the two titrations is equivalent to the ampicillin (C16H19N3O4S) contained in the test product. Volume liquid (0.01mol / L) of. Another ampicillin reference substance was measured and calculated according to the same method. (Ampicillin C16H19N3O4S: Bamcillin hydrochloride C21H27N3O7S. HCl = 0.696: 1)

Bamcillin hydrochloride is clinically applicable to treat infections caused by gram-positive and gram-negative bacteria that are sensitive to ampicillin, such as respiratory infections, urogenital infections, skin and soft tissue infections.

Obamacillin has cross-allergies with other penicillins and some cross-allergies with cephalosporins.

Persons who are allergic to bamcillin, infectious mononucleosis or allergic to other penicillin drugs are prohibited.

Use with caution

Use with caution for those allergic to cephalosporins.

Pregnant women, lactating women and newborns should be used with caution.

Use with caution in those with a history of allergic diseases.

Use with caution in severe liver and kidney dysfunction.

Sulfite oxidase deficiency test: Urine samples from those who regularly take bacilcillin hydrochloride will contain ampicillin, which results in a false positive for the sulfite oxidase deficiency test.

Urine glucose test: Bamcillin hydrochloride can cause false increases or decreases in Clinitest readings. Therefore, for patients taking penicillin using the quantitative urine glucose measurement method of Clinitest, qualitative methods such as glucose oxidase test should be used to check the results.

A small number of patients can increase eosinophils, leukocytes, and thrombocytopenia after using this product.

Routine monitoring of liver, kidney function and blood system should be performed during long-term medication.

Adverse effects caused by paroxacillin hydrochloride are similar to those of ampicillin. Common adverse reactions are diarrhea and rash (the incidence of rash is higher than other penicillins, up to 10% or more, and sometimes drug fever). Other adverse reactions include allergic reactions and pseudomembranous colitis. Compared to ampicillin, the overall incidence of gastrointestinal disorders was significantly lower in patients receiving ampicillin.

When the blood system is treated with paroxcillin hydrochloride, anemia, thrombocytopenia, thrombocytopenic purpura, eosinophilia, and leukopenia can occur in a small number of patients.

The cardiovascular system has been reported to cause nodular peripheral arteritis when using this product.

Gastrointestinal effects The most common gastrointestinal adverse reactions of bacillin hydrochloride are diarrhea and epigastric discomfort. Other gastrointestinal reactions include stomatitis, nausea, vomiting, glossitis, black-tongue enterocolitis, and the like. Occasionally pseudomembranous colitis.

kidney / urogenital system can cause kidney poisoning.

The respiratory system can even cause adult respiratory distress syndrome.

The skin can cause rash, pemphigus vulgaris, toxic epithelial necrosis, and drug rash.

Aminoglycosides: It has been reported that aminoglycosides are inactivated both in vivo and in vitro when combined with paroxcillin hydrochloride and aminoglycoside drugs, resulting in a decrease in the efficacy of aminoglycosides.

Chloramphenicol: When combined with chloramphenicol and chloramphenicol, it will inhibit the bactericidal activity of pamoxicillin.

This product should be taken on an empty stomach, so as not to reduce the efficacy.

During the use of this product, if severe persistent diarrhea occurs, it may be pseudomembranous colitis, and the drug must be stopped at this time. Once diagnosed, appropriate antibiotics should be used.

The treatment of overdose of paroxacillin hydrochloride is symptomatic and supportive treatment. Hemodialysis helps to clear paroxcillin from the blood.

Adult

Oral administration: general infection, 400 mg each time, twice daily; severe infection, 800 mg each time, twice daily.

Child

Oral administration: general infection, 25-50mg / (kg · d), divided into two doses; for severe infection, the dosage can be increased as appropriate.

specification

Paroxacillin Hydrochloride Tablets 400mg

Storage method: sealed storage.

Instructions for Paroxacillin Hydrochloride Tablets

Drug Name

Common name: Paroxacillin Hydrochloride Tablets

Product name:

English name: Bacampicillin Hydrochloride Tablets

Phonetic script: Hansuan Ba'anxilin Pian

The main ingredient of this product is bacilcillin hydrochloride. Its chemical name is 1-ethoxyformylethoxy 6- [D (-)-2-amino-2-phenylacetamino] penicillin hydrochloride.

Molecular formula: C21H27N3O7S · HCl

Molecular weight: 501.98

[Character]

This product is a white or off-white film-coated tablet.

[Pharmacology and Toxicology]

Bamcillin is ampicillin mevalerate, which has no antibacterial activity in vitro. It is hydrolyzed by non-specific esterase from the intestinal wall to ampicillin during absorption in vivo to exert its antibacterial effect. Ampicillin sodium is a broad-spectrum semi-synthetic penicillin. This product is effective against a variety of Gram-positive and Gram-negative bacteria. It has strong antibacterial activity against hemolytic streptococcus, streptococcus pneumoniae, and non-penicillinase-producing staphylococcus, but slightly inferior to penicillin. Ampicillin also has a good antibacterial effect on Streptococcus grass green, and it has better effect on Enterococcus and Listeria than Penicillin. This product has antibacterial activity against Corynebacterium diphtheriae, Bacillus anthracis, Actinomyces, Haemophilus influenzae, P. pertussis, Neisseria and anaerobic bacteria other than Bacteroides fragile, and some Proteus mirabilis, Escherichia coli, Salmonella and Shigella bacteria are sensitive to this product.

Ampicillin works by inhibiting bacterial cell wall synthesis.

Pharmacokinetics

The product is rapidly and completely absorbed orally. The prodrug quickly hydrolyzes after absorption, releasing ampicillin. The peak time (Tmax) of the plasma concentration after oral administration of the product is about 0.5 to 1 hour. The peak plasma concentration (Cmax) was 7 mg / L, which was similar to 1 g of ampicillin.

Ampicillin is stable to gastric acid, has good distribution after absorption, and has high drug concentrations in bile and urine. It can reach effective therapeutic concentrations in cerebrospinal fluid, pleural and ascites fluid, joint effusion, and bronchial secretions with inflammation. The plasma protein binding rate was 20%.

The blood elimination half-life (T1 / 2) of this product is about 1 hour. After 3 hours of oral administration, approximately 70% to 75% were excreted through the kidney in the form of ampicillin.

[Indications]

It is suitable for respiratory tract infection, urinary system infection and skin soft tissue infection caused by sensitive bacteria.

Dosage

oral.

Adult: 0.4g once a day, twice a day. In severe cases, 0.8g at a time, twice a day.

Treatment of simple gonorrhea: 1.6g of this product plus probenecid 1g orally.

children: the usual amount of 12.5mg / kg once, twice a day. In severe cases, the dose is doubled.

Adverse reactions

Allergic reactions: maculopapular rash, urticaria, pruritus, exfoliative dermatitis and severe allergic reactions (anaphylactic shock).

gastrointestinal reactions: diarrhea, loose stools, nausea, abdominal pain, cramps, upper abdominal pain and vomiting.

Anemia, thrombocytopenia, eosinophilia and other blood system abnormalities.

abnormal liver function: such as increased serum aminotransferase and serum bilirubin.

I occasionally see interstitial nephritis.

Double infection: Long-term or large-scale application of this product can cause infection with penicillin-resistant Staphylococcus aureus, Gram-negative bacilli, or Candida albicans.

Contraindications

Those who are positive for the penicillin skin test and those who are allergic to the product and other penicillin drugs are prohibited.

Disable patients with infectious mononucleosis, cytomegalovirus infection, lymphocytic leukemia, and lymphoma.

Precautions

Before taking the product, patients must take a penicillin skin test.

Persons who are allergic to cephalosporins and those with a history of allergic diseases such as asthma, eczema, hay fever and urticaria should be used with caution.

This product is cross-allergic with other penicillin drugs. If an allergic reaction occurs, the product should be discontinued immediately and appropriate measures taken.

Patients with impaired renal function should adjust the dose or dosing interval based on plasma creatinine clearance.

For patients with gonorrhea suspected of being infected with syphilis, a dark field examination should be performed before using the product, and a serum test should be performed monthly at least within 4 months.

Those who take this product for a long or large dose should regularly check the function of liver, kidney and hematopoietic system, and detect serum potassium or sodium.

Interference to laboratory test indicators: The copper sulfate method urine test can be false positive, but the glucose enzyme test method is not affected; The serum alanine aminotransferase or aspartate aminotransferase can be measured Rise.

[Medication for pregnant and lactating women]

The product can enter the fetus through the placenta. However, there is not enough controlled studies in humans, so pregnant women generally avoid using it and only use it when there is a clear indication.

This product can be secreted into breast milk, which may cause sensitization of infants and cause diarrhea, rash, infection with Candida, etc. Therefore, breastfeeding women should use it with caution or suspend breastfeeding during medication.

[Child medication]

[Medication for elderly patients]

Elderly patients should adjust the dosage or interval according to renal function.

medicine interactions

probenecid, aspirin, indomethacin, butasone, and sulfa drugs can reduce the excretion of the product in the renal tubules, thus increasing the blood concentration of the product, prolonging the blood elimination half-life (t1 / 2), toxicity May also increase.

When this product is combined with allopurinol, the incidence of rash is significantly increased, so it should be avoided.

This product should not be used in combination with acetaldehyde dehydrogenase inhibitors such as disulfiram.

When this product is used in combination with chloramphenicol for bacterial meningitis, the incidence of long-term sequelae is higher than that when they are used alone.

This product can stimulate estrogen metabolism or reduce its enterohepatic circulation, so it can reduce the effect of oral contraceptives.

Chloramphenicol, erythromycin, tetracyclines, sulfa drugs and other bacteriostatic drugs can interfere with the bactericidal activity of this product, so it should not be combined with this product, especially in the treatment of meningitis or severe infections in need of bactericides.

This product can strengthen the effect of warfarin.

[Drug overdose]

specification

0.4g (calculated as paroxcillin hydrochloride)

Storage

Keep out of light and keep sealed in a cool place.