BRL.8988 (talampicillin), a well-absorbed oral form of ampicillin.
The phthalidyl ester (BRL.8988, talampicillin) of ampicillin gave serum levels in man two and a half times those obtained with ampicillin itself.
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The phthalidyl ester (BRL.8988, talampicillin) of ampicillin gave serum levels in man two and a half times those obtained with ampicillin itself.
500 mg of powdered ampicillin (AMP; activity 108%) and 325 mg of talampicillin chlorhydrate (TMP; equivalent to 200 mg ampicillin with an activity of 100%) were administered orally to two groups of 15 fasting patients selected at random. Blood samples were collected after 1/2, 1, 2, 4 and 6 h and urine samples after 1, 2, 4 and 6 h. The AMP concentrations were determined by the microbiologic method. All patients received food 1 h after the drugs administration. Urine samples wee taken daily for the bacteriologic examination. The maximum seric peak for TMP was 4.2 microgram/ml at 1/2 h and for AMP of 4.6 microgram/ml after 1 h. It was stated that TMP is absorbed more quickly than AMP and it was not affected by the presence of food. Nevertheless, no differences were observed in the results of the clinical study.
There are references in the literature describing the influence of bronchial inflammation on the antibiotic concentration in bronchial secretions, including netilmicin concentrations in the bronchial secretion of patients undergoing tracheotomy. Three semi-synthetic penicillins are compared--bacampicillin, amoxicillin and talampicillin--administered frequently in the treatment of various respiratory infections. The three antibiotics were administered successively for two days each, in the same patient, irrespective of other drugs. At the same time the cytologic evaluation of the degree of bronchial inflammation was done. The antibiotic concentrations in bronchial secretions and in sera were measured at the same time. The results showed that the concentration of antibiotics in bronchial secretions of patients undergoing tracheotomy was proportional to the degree of bronchial inflammation. Among the semi-synthetic penicillins investigated the highest degree of concentration in the bronchial secretion was obtained after the bacampicillin.
A comparative double blind study of lenampicillin (LAPC, KBT-1585) and talampicillin (TAPC) was carried out in order to objectively evaluate efficacy, safety and utility of LAPC in treatment of 238 patients with oral infections. Cases accepted by the Central Committee for evaluation of efficacy and utility were 218, consisting of 101 of the LAPC group and 117 of the TAPC group; safety were 234, consisting of 110 of LAPC and 124 of TAPC. Clinical effectiveness as rated by attending doctor was 84.2% for the LAPC group and 82.9% for the TAPC group. The clinical utility rating was 82.2% in the LAPC group and 82.1% in the TAPC group, showing no significant difference between the 2 drugs. Adverse reactions were found in 6 cases (5.5%) in the LAPC group and 5 cases (4.0%) in the TAPC group, showing no significant difference between the 2 drugs. Cases accepted by the controllers for evaluation of efficacy and utility were 236, consisting of 111 cases of LAPC and 125 cases of TAPC. Those for safety were 236, consisting of 111 cases of LAPC and 125 of TAPC. The clinical effectiveness rating was 77.5% in the LAPC group and 79.2% in the TAPC group. Clinical utility rating was 75.7% in the LAPC group and 78.4% in the TAPC group. Rate of adverse reactions was 5.4% in the LAPC group and 4.0% in the TAPC group, showing no significant difference between the 2 drugs. Cases evaluated for efficacy according to numerical rating on the 3rd day were 200 cases, consisting of 93 of LAPC and 107 of TAPC. The effectiveness rate was 83.9% in the LAPC group and 95.3 in the TAPC group, showing a significant difference between the 2 drugs. On the other hand, taking into consideration evaluation scores of the 5th day, the effectiveness rate was 88.7% in the LAPC group and 96.1% in the TAPC group, showing no significant difference between the 2 drugs. The effectiveness rate in cases of isolated organisms was 84.9% in the LAPC group and 79.7% in the TAPC group, showing no significant difference between the 2 drugs. Adverse reactions were mostly of gastrointestinal origin. Symptoms were not serious and disappeared soon after administration was discontinued or immediately after administration was completed.(ABSTRACT TRUNCATED AT 400 WORDS)
The results observed with talampicilline in our clinical study confirmed the observations made by others regarding the activity and the improved tolerance for this drug versus ampicilline. The use of a high daily dosage of 3 g per day was neither a cause of more frequent nor more severe side-effects than the usually smaller posology used in other studies published in the literature.
Talampicillin and amoxycillin were shown to be absorbed twice as well as ampicillin in a triple crossover experiment.
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Parameters for blood concentrations of the peroral antibiotics talampicil in and bacampicillin, in NZW rabbits were determined using a two compartment model. On the basis of these pharmacokinetic parameters, a three compartment model was prepared for the concentrations of these drugs in the tongue, gingiva, submandibular gland, parotid gland, cervical lymph-node and mandibular bone. Simulation curves based on the parameters of tissue concentrations revealed visual conformity to the measured values.
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