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At least 19 recordsLinked to original sources
PubMed1978

[Talampicillin hydrochloride: Comparison with amoxicillin and ampicillin in the antibacterial activity and pharmacokinetics (author's transl)].

The antibacterial activities, absorption and excretion of talampicillin hydrochloride were compared with those of amoxicillin and ampicillin. Talampicillin hydrochloride showed a broad-spectrum antibacterial activity against Gram-positive and Gram-negative bacteria as seen in amoxicillin and ampicillin. The antibacterial activities of talampicillin hydrochloride, amoxicillin and ampicillin were quite similar. In experimental murine infection with Staphylococcus aureus, protective effect of talampicillin hydrochloride was superior to ampicillin. For Escherichia coli infection, protective effect of talampicillin hydrochloride was similar to that of amoxicillin, while ampicillin was less active than both talampicillin hydrochloride and amoxicillin. The absorption and excretion of 250 mg equivalent doses of talampicillin hydrochloride, amoxicillin and ampicillin were compared in nine fasting healthy volunteers after oral administration of these antibiotics in randomized triple crossover study. In order to calculate the pharmacokinetic parameters, plasma levels were analyzed using an one-compartment open model, as well as area under the plasma concentration curve (AUC) and urinary excretion. Maximum plasma levels calculated were 2.8 times higher for talampicillin hydrochloride and 1.45 times higher for amoxicillin than for ampicillin. AUC was greater for talampicillin hydrochloride than for amoxicillin and lowest for ampicillin. Urinary excretion of talampicillin hydrochloride as penicillin determined in biological assay was comparable to that of amoxicillin and 1.55 times higher than that of ampicillin. Penicillins can be metabolized to penicilloic acids in the body. After taking into account the penicilloic acid contents in urine, total excretion in urine was 61% for talampicillin hydrochloride, 67% for amoxicillin and 42% for ampicillin during 6 hours after dosing. The absorption of the drugs was evaluated according to the plasma levels, the area under plasma concentration curve and the percentage of excretion in urine. The results obtained showed that talampicillin hydrochloride was well absorbed from the gastro-intestinal tract.

Adult↗
PubMed1978

Bioavailability and metabolism of talampicillin.

Talampicillin is an ester of ampicillin which is readily hydrolysed on absorption to release ampicillin. It is well absorbed from the gastro-intestinal tract resulting in a greater bioavailiability of ampicillin than can be achieved with equivalent doses of ampicillin itself. Dose response studies have confirmed a direct relationship between the dose of talampicillin administered and peak serum ampicillin concentration and urinary excretion of ampicillin. Dosing of ampicillin after food has been shown to adversely affect the total bioavailability of ampicillin. This is not so after dosing with talampicillin. The bioavailability of ampicillin from a 250-mg Talpen tablet dosed after a large meal was significantly greater than that from 250 mg ampicillin dosed in the fasting state. Studies in volunteer subjects at multiples of the proposed therapeutic dose for periods of up to 28 days have indicated its acceptability, bioavailability and lack of side effects on repeated dosing. The fate of the phthalidyl moiety of talampicillin has been investigated in repeated dose studies and in a single dose studies and in a single dose study in which radiolabelled talampicillin was administered. The principal metabolite of the phthalidyl moiety in man has been shown to be 2-hydroxymethylbenzoic acid, which is identical to that in experimental animals used for toxicological investigations.

Adult↗
PubMed1978

The metabolism of talampicillin in rat, dog and man.

1. After administration of [phthalidyl-14C] talampicillin (Talpen) to rat, dog and man, radioactivity was excreted mainly in the urine (90%, 86% and 98% in rat, dog and man respectively). 2. After administration of [ampicillin-14C] talampicillin, radioactivity was excreted in the urine of rats and dogs to a lesser extent (35% in both species) and only a small proportion of the dose was excreted in the bile (6% in rats, less than 0.1% in dogs). 3. The pattern of radiometabolites was very similar in extracts of the urines of radiometabolites was very similar in extracts of the urines of rat, dog and man dosed orally with [phthalidyl-14C]talampicillin. The major metabolite was 2-hydroxymethylbenzoic acid. 4. Unchanged talampicillin was present in the hepatic portal vein blood of dog and thus reached the liver, whereas in rat, no parent compound could be detected in portal vein blood. This result may help to explain differences in toxicity of the compound in rat and dog. 5. Studies in vitro showed that the intestinal wall is an important site of hydrolysis of talampicillin in rat and dog.

Adult↗
PubMed1982

Talampicillin in the treatment and prophylaxis of urinary tract infection in children.

9 children presenting with an ampicillin-sensitive coliform urinary tract infection were treated with talampicillin using 1 week of full-dose treatment followed by low-dose prophylaxis. The bowel coliforms were ampicillin-resistant at the start in one girl and became resistant in the remaining 8 within 4 months. During a total of 44 months of talampicillin therapy, 6 girls (2 with vesico-ureteric reflux) developed a symptomatic re-infection of the urinary tract, a recurrence rate of 1 per 7.3 months, or 1.6 recurrences per annum. A further 12 girls were given prophylactic talampicillin, 9 after an initial therapeutic course of co-trimoxazole for 1 week and 3 following a period of prophylaxis with low-dose co-trimoxazole. The rectal swab from one girl showed partial ampicillin resistance but 9 of the remaining 11 showed that a predominance of ampicillin-resistance coliforms had emerged in the bowel flora within 4 months. 5 of the 12 also developed a symptomatic ampicillin-resistant urinary infection within 4 months, a recurrence rate of 1 per 7.1 months or 1.7 recurrences per annum. Talampicillin, though very effective in treating urinary infection, is not recommended for the prevention of subsequent recurrence.

Ampicillin↗
PubMed1976

Talampicillin: a new derivative of ampicillin.

Talampicillin is a thiazolide carboxylic ester of ampicillin and is hydrolysed in the intestinal mucosa to release free ampicillin. The mean peak serum concentration of ampicillin occurred one hour after a dose of talampicillin and was about twice that attained by an equivalent dose of ampicillin. The presence of food in the stomach reduced and delayed the peak blood levels but did not affect the total amount of antibiotic absorbed or the urinary recovery. Talampicillin had less effect on the faecal flora in volunteers than ampicillin, and no overgrowth with Candida spp or Staphylococcus aureus was seen. Thirty-eight out of 47 urinary infections were eradicated by a seven-day course of talampicillin.

Adsorption↗
PubMed1985

Ampicillin concentrations in human serum, gingiva, mandibular bone, dental follicle, and dental pulp following a single oral dose of talampicillin.

Eighty-one patients who underwent the extraction of impacted mandibular third molars in the nonfasting state were given a single oral dose of talampicillin (500 mg) preoperatively. Specimens of venous blood (n = 132), gingiva (n = 70), mandibular bone (n = 78), dental follicle (n = 63), and dental pulp (n = 59) were obtained during the operation and assayed for ampicillin content. The mean peak concentrations in serum (9.64 micrograms/ml), gingiva (4.72 micrograms/mg), mandibular bone (1.77 micrograms/ml), dental follicle (3.46 micrograms/ml), and dental pulp (5.53 micrograms/mg) all occurred at approximately 150 minutes after administration of talampicillin. The ratios of the corresponding serum concentration to the peak concentrations in the various oral tissues when both were plotted as drug concentration curves were: gingiva, 0.50; mandibular bone, 0.16; dental follicle, 0.34; and dental pulp, 0.52. Talampicillin was absorbed well by the intestine, and sufficient concentrations of the resulting metabolite, ampicillin, were found in oral tissues.

Administration, Oral↗
PubMed1978

Talampicillin and probenecid compared with ampicillin and probenecid for the treatment of gonococcal urethritis in men.

Two hundred and ten men suffering from uncomplicated gonococcal urethritis were treated with one of two treatment schedules. Of 109 patients treated with 3 g ampicillin and 2 g probenecid (group A) there were two recurrences in the first week after treatment and none in the second week. Of 101 patients treated with 1.5 g talampicillin and 2 g probenecid (group B), there were three recurrences in the first week and none in the second week. Both antibiotics were well tolerated, but one patient vomited two hours after taking talampicillin. The sensitivity pattern of Neisseria gonorrhoeae to penicillin at The London Hospital has shown an increase in the proportion of more sensitive strains during the last three years. Talampicillin given in a single dose with probenecid is satisfactory in the treatment of acute gonococcal urethritis but, apart from the smaller dosage, it does not offer any advantage over ampicillin with probenecid.

Adolescent↗
PubMed1982

Treatment of uncomplicated gonorrhoea in women with talampicillin in a single oral 1.5 g dose.

Four hundred and sixty women with uncomplicated gonorrhea were treated with a single oral dose of 1.5 g talampicillin. The success rate among those who attended for at least one follow-up examination after treatment was 99.14%. The antibiotic was well tolerated and no side effects were reported. Talampicillin given under supervision has proved to be the most effective and safest treatment in this area. A smaller dosage of talampicillin than ampicillin is required, the drug is better tolerated by the patient, and the time of nursing staff is saved.

Adult↗
PubMedDate not supplied

Kinetics of talampicillin decomposition in solutions.

Talampicillin stability in aqueous solutions was studied in a broad range of pH values using as medium solutions of hydrochloric acid (pH 0.4-1.8), phosphate buffers (pH 2.05-3.13 and 6.03-8.04), acetate buffer (pH 3.87-5.28) and borate buffer (pH 8.90-9.10) as well as sodium hydroxide solution (pH 11.48). For the determination of talampicillin concentration changes in kinetic studies, two methods were used: iodometric and spectrophotometric in UV (lambda(max) = 254.5 nm). The catalytic velocity constants (k(H+), k(x), k(o)) were established, the log k-pH profile (35 degrees C) was found, thermodynamic parameters were calculated of the hydrolysis reaction of the beta-lactam bond (k(H+): E(A)= 67.9 kJ mol(-1), delta S = -92.4 J K(-1) mol(-1), delta G = 92.6 kJ mol(-1); k(x): E(A) = 31.8 kJ mol(-1), delta S = -347.1 J K(-1) mol(-1), delta G = 131.1 kJ mol(-1); k(o), pH = 5.28: E(A) = 98.0 kJ mol(-1), delta S = -50.3 J K(-1) mol(-1), delta G = 110.3 kJ mol(-1) at 20 degrees C), and the stability of the lactone bond was studied in the medium with the highest stability of beta-lactam bond of talampicillin (pH 5.28: k(o): E(A)= 32.5 kJ mol(-1), delta S = -220.5 J K(-1) mol(-1), delta G = 94.7 kJ mol(-1) in 20 degrees C), at controlled ionic strength (mu = 0.5 mol l(-1)).

Anti-Bacterial Agents↗
PubMed1996

Oral bioavailability and in vitro stability of pivampicillin, bacampicillin, talampicillin, and ampicillin in horses.

OBJECTIVES: To determine the oral bioavailabilities of 3 ampicillin esters (pivampicillin, bacampicillin, and talampicillin) and ampicillin sodium, and to determine in vitro stability of the ampicillin esters in ileal contents (pH 8.3 to 8.5). DESIGN: A crossover design to administer the 4 drugs orally, and ampicillin i.v. to all horses in the study. ANIMALS: 4 healthy adult horses. PROCEDURE: The drugs were administered intragastrically to the horses at a dosage equimolar to 15 mg of ampicillin/kg of body weight. Also, ampicillin sodium was administered i.v. at the same dosage. Blood samples were taken up to 12 hours after drug administration, and ampicillin concentrations in plasma were determined. For the in vitro study, the ampicillin esters were incubated at 37 C in ileal contents obtained from ponies with cecal fistulas. After incubation, the remaining intact ester and the formed ampicillin were measured. RESULTS: Absolute oral bioavailability was 31, 39, 23, and 2% for pivampicillin, bacampicillin, talampicillin, and ampicillin sodium, respectively. In the in vitro study, 90% decomposition of the ester took place in 30, 60, and 5 minutes, for pivampicillin, bacampicillin, and talampicillin, respectively. CONCLUSIONS: Pivampicillin and bacampicillin are promising candidates for oral antibiotic treatment of horses. The rapid decomposition of ampicillin esters is caused by chemical hydrolysis at the high pH of equine ileal contents.

Administration, Oral↗
PubMed1977

Oral talampicillin in the treatment of gonorrhoea.

Talampicillin was effective in eradicating the causitive organism in uncomplicated gonorrhoea, with only four treatment failures (1-6%) in 245 patients seen at least once after treatment. Symptoms, such as discharge, were seen in 61 patients at some stage after treatment but 31 of these cases were clear after one or two follow-up visits. The anitbiotic was well tolerated. One patient developed a maculopapular rash, penicillin allergy was reported in two patients, and a generalised itch (possibly penicillin allergy) in one further patient. A total of 241 out of 245 (98%) cases had the urethral gonococcus successfully eradicated with talampicillin. Talampicillin given in single doses appears to be an extremely good choice of antibiotic in the treatment of uncomplicated gonorrhoea in men.

Administration, Oral↗
PubMed1976

A comparative study of talampicillin and ampicillin in general practice.

Talampicillin hydrochloride, the phthalidyl ester of ampicillin, when given in a dosage containing the equivalent of 125 mg of ampicillin four times daily for six days to general practice patients, has proved to be as effective, both clinically and bacteriologically, as 250 mg of ampicillin given four times daily for six days. Although the over-all incidence of side-effects was similar with both preparations, diarrhoea was significantly reduced in talampicillin-treated patients. Possible reasons for this are discussed. Talampicillin therefore offers certain advantages over ampicillin in producing effectiveness equivalent to that of ampicillin at a lower dosage level with a reduced incidence of diarrhoea.

Adolescent↗
PubMed1985

Concentrations of ampicillin and cefadroxil in human serum and mixed saliva following a single oral administration of talampicillin and cefadroxil, and relationships between serum and mixed saliva concentrations.

The concentrations of ampicillin (ABPC) from talampicillin (TAPC) and cefadroxil (CDX) in serum and mixed saliva were assayed by the thin layer disc plate method. Talampicillin and cefadroxil (500 mg) were given by a single oral administration. The relationships between serum and mixed saliva ampicillin and cefadroxil concentrations were evaluated in the paired specimens collected from 10 different persons, respectively. The means of concentration ratios of mixed saliva to serum ampicillin and cefadroxil were 0.006 +/- 0.003 and 0.025 +/- 0.010 (mean +/- SD), respectively. Significant correlation coefficients between mixed saliva and serum concentrations were found for both ampicillin and cefadroxil, which were r = 0.78, P less than 0.001, and r = 0.67, P less than 0.001, respectively.

Adult↗
PubMed1988

Potential improvement in the shelf life of parenterals using the prodrug approach: bacampicillin and talampicillin hydrolysis kinetics and utilization time.

The utilization time for a parenteral prodrug solution with a bioavailable fraction of unity was defined as the time during which the total of the prodrug concentration and the drug concentration equals or exceeds 90% of the initial prodrug concentration. This utilization time was calculated as a function of pH, buffer, and temperature using the experimentally determined rate expressions for bacampicillin and talampicillin. The results were compared to the shelf life of ampicillin solutions under identical storage conditions. First-order rate constants were determined for conversion of the prodrugs to ampicillin (kc), for beta-lactam degradation of the prodrugs (knc), for the overall loss of prodrugs (ksum), and for beta-lactam degradation of ampicillin (kh) in aqueous solutions at 25.0 to 60.0 degrees C, mu = 0.5, in the pH range 0.90 to 8.4. Loss of bacampicillin proceeded primarily by degradation at pH levels below 4 but was due predominantly to conversion at pH levels above 5. Loss of talampicillin was due primarily to conversion throughout the entire pH range. While the prodrug utilization times were approximately twice the shelf life of ampicillin in acidic solutions, ampicillin was significantly better in neutral solutions. The results illustrate the potential for increased prodrug storage periods when utilization time is defined on the basis of the bioactivity rather than on the prodrug concentration alone.

Ampicillin↗
PubMed1988

Ampicillin concentrations in human dental granuloma after a single oral administration of talampicillin.

Ampicillin concentrations in human serum and dental granulomas of 31 patients were determined after a single oral dose of talampicillin (equivalent to 500 mg of ampicillin) was administered to each. The specimens were taken at 1.5, 2.0, 2.5, 3.0, and 3.5 h after the administration of talampicillin. The mean peak ampicillin concentrations in serum and dental granulomas occurred at identical times, 2.5 h, and were 8.29 micrograms/ml (range, 1.81 to 13.20 micrograms/ml) and 2.94 micrograms/g (range, 1.14 to 7.16 micrograms/g), respectively. The mean dental granuloma/serum ampicillin concentration ratio at the peak time (2.5 h) was 0.42 (range, 0.29 to 0.56). Ampicillin concentrations in dental granulomas exceeded most of the MICs for the bacteria commonly isolated from odontogenic infection.

Administration, Oral↗
PubMed1976

Single oral dose of 1-5g. talampicillin in the treatment of gonorrhoea.

81 patients have been treated with single oral doses of 1-5 g. (6 tablets) of talampicillin without probenecid. The failure rate amongst those followed was only 4-2 per cent. No side-effects were reported. These results were superior to those obtained with 2-0g. or equivalent of ampicillin, amoxycillin, or pivampicillin with probenecid. Talampicillin is thus the most potent ampicillin-like antibiotic so far available for the treatment of gonorrhoea and is capable of curing the disease with a smaller single dose without probenecid than is necessary for other preparations.

Administration, Oral↗
PubMed1988

Ampicillin concentrations in human serum and periodontal membrane following a single oral administration of talampicillin.

1. Ampicillin concentrations in human serum and periodontal membrane after a single oral administration of talampicillin (500 mg) were assayed by the agar diffusion (paper disc) method. 2. The peak times of serum and periodontal membrane were identical, being 150 min after administration. 3. The peak concentrations of serum and periodontal membrane were 7.81 micrograms/ml and 4.11 micrograms/g, respectively. 4. The mean ratio of periodontal membrane to serum concentration at the peak time was 0.53.

Administration, Oral↗