Clinical Pharmacology of Pivampicillin

Roholt, K.; Nielsen, B; Kristensen, Ellids

doi:10.1128/aac.6.5.563

Cited by 31 publications

(11 citation statements)

References 15 publications

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“…In the present and a previous study [8], ingestion of a tablet with a meal resulted in an increase of 10% in Cma~, whereas other studies have shown reductions of 3 to 30% [6,9,10]. In the present study, the AUC was almost unchanged (a reduction of 3%) and a reduction of 13 rain was measured for Tma x.…”

Section: Discussioncontrasting

confidence: 53%

Absorption of pivampicillin as related to dose, and tolerability of a 700 mg tablet

et al. 1993

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To evaluate the absorption and tolerability of a new formulation of pivampicillin administered as a 700 mg tablet, 14 healthy volunteers received single doses of 350, 500 and 700 mg p.o. Maximum serum concentrations (Cmax) of 5.73, 7.05 and 8.61 mg/l were obtained. The corresponding values for the area under the concentration/time curve (AUC) were 12.32, 18.99 and 25.30 mg/lxh. Concomitant intake of food increased the Cmax of the 700 mg tablet to 9.5 mg/l, while the AUC remained unchanged. Co-administration of the 700 mg pivampicillin dose with an antacid reduced the Cmax to 7.45 mg/l and the AUC to 17.92 mg/l x h. The tolerance of the 700 mg tablet was evaluated in a double-blind placebo-controlled study involving 57 patients. Six percent of the patients in each treatment group reported minor adverse reactions.

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Section: Discussioncontrasting

confidence: 53%

Absorption of pivampicillin as related to dose, and tolerability of a 700 mg tablet

et al. 1993

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“…Ampicillin suspension , aspirin enteric-coated granules, and digoxin elixir are included in this category, while encapsulated, enteric-coated tablets, or tablet dosage forms of Greenblatt et al (1974) Ethambutol Tablets Ameer et al (1982) Hydralazine Tablets Walden et al (1981) Indoprofen Tablets Johnson et al (1978) Oxazepam Tablets Melander et al (1977e) Oxpi'enolol Conventional and sustained Dawes et al (1979) release tablets Penicillin V (acid) Tablets Peck et al (1958) Phenazone (antipyrine) Combination tablets Melander et al (1977a) Pivampicillin Capsules Roholt et al (1974) Pivmecillinam Parsons et a!. (1977) Prednisone Tablets Tembo et al (1976) Propylthiouracil Tablets Melander et al (1977g) Spiramycin Tablets Kamme et al (1978) Sulphasomidine Tablets Melander et al (1976b) Theophylline Tablets Welling et al (1975a) Tolbutamide Tablets Sartor et al (1980) Tranexamic acid Tablets Pilbrant et al (1981) a Studied in children.…”

Section: Interactions Having No Effect On Drug Absorptionmentioning

confidence: 98%

Interactions Affecting Drug Absorption

Welling¹

1984

Clinical Pharmacokinetics

157

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The influence of drug-drug and drug-food interactions affecting the absorption of orally administered medication is reviewed. Drug-drug interactions can be classified in terms of indirect effects by one drug on gastrointestinal tract physiology influencing the absorption of other drugs, or direct interactions involving altered pH, adsorption, absorption, or chelation. Most, but not all, drug-drug interactions result in reduced or delayed systemic drug availability. Drug-food interactions may result in reduced, delayed, or increased systemic drug availability. The absorption of only a small number of drugs is unaffected by concomitant food intake. The degree of interaction and whether it positively or negatively affects drug absorption depends on a number of factors including the physical and chemical nature of the drug, the formulation, the type of meal, and the time interval between eating and dosing. Mechanisms of drug-food interactions are not well characterised. They clearly involve both direct and indirect factors in a similar fashion to drug-drug interactions, but indirect factors probably predominate. Reduced or delayed drug absorption is generally attributed, at least in part, to delayed stomach-emptying due to food. Increased absorption may also result from delayed stomach-emptying facilitating greater drug dissolution before it passes from the stomach into the small intestine. Increased bioavailability of some drugs, e.g. propranolol, metoprolol and labetalol, may be related to reduced presystemic clearance. The potential clinical implications of drug-drug and drug-food interactions must be taken into account with oral medications in order to minimise variations in systemic drug availability and hence in clinical efficacy.

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“…Unfortunately, since it has proved to be impossible to obtain reliable samples in this kind of patient, we could not measure the urinary recovery of the drugs reliably. We preferred to administer the drug under nonfasting conditions, because pivampicillin is badly tolerated on an empty stomach (1), and food does not seem to impair the absorption of the drug in healthy subjects (3,7,16).…”

Section: Discussionmentioning

confidence: 99%

Absorption of Pivampicillin in Postoperative Patients

Kunst

Mattie

1975

Antimicrob Agents Chemother

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The absorption of orally administered pivampicillin was studied in nine postoperative patients and compared with that of intravenously administered ampicillin. The absorption of pivampicillin was calculated on the basis of comparison of the areas under the serum concentration curves for both modes of administration. After an oral dose of 700 mg the absorption ranged from 40 to 95% (mean, 60%).Despite its relatively good acid stability, ampicillin is absorbed rather poorly from the gastro-intestinal tract, varying from 30 to 50% (8,10,12). One of the attempts to achieve better absorption resulted in the development of pivampicillin, the pivaloyloxymethyl ester of ampicillin, which is rapidly hydrolyzed to ampicillin in the body; 15 min after administration, more than 99% of the drug in the blood is present as ampicillin (18).The serum concentrations of ampicillin after oral administration of pivampicillin have been compared with those after ampicillin given by the oral route (1, 4, 6, 12, 15-17, 19, 20) or intramuscularly (3, 7, 13); only three of these studies were done in patients (6,12,13). The general impression obtained from these studies is that after equimolar doses the mean (peak) serum levels of ampicillin after orally administered pivampicillin are two to three times higher than those seen after orally administered ampicillin and are almost comparable with those after intramuscularly administered ampicillin.Several objections can be raised to most of these studies, however. (i) The amount of the drug absorbed in relation to the dose is difficult to evaluate. (ii) Most of the studies were done in healthy subjects. (iii) The individual variations in absorption, which are important in relation to therapy, were not taken sufficiently into consideration.A more recent study on the absorption of pivampicillin (10) gives better information about the amount of pivampicillin that is absorbed, but this investigation too was done in healthy subjects.In the present study the quantitative absorption of oral pivampicillin was compared with that of intravenously administered ampicillin in postoperative patients. MATERIALS AND METHODSThe investigation was performed in nine adult patients (one female and eight males) aged between 22 and 85 years who had undergone a urological operation recently (within 3 to 7 days). The gastrointestinal function had recovered to the extent that the patients were able to eat normally, and most of them were in the initial phase of postoperative mobilization. Administration of antibiotics was stopped at least 12 h before the study was started. Patients with an allergy to penicillin or (severe) renal failure (serum creatinine more than 250 gmol/liter) were not included. All patients consented to participate in the study after the purpose had been explained.On day 1, 500 mg of ampicillin (Amfipen; Mycofarm, Delft, The Netherlands) was administered intravenously. Blood samples were taken just before and 2, 5,15, 30, 45, 60, 75, 90, 105 (from two patients only), 120, and 180 min after the dru...

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Clinical Pharmacology of Pivampicillin

Cited by 31 publications

References 15 publications

Absorption of pivampicillin as related to dose, and tolerability of a 700 mg tablet

Absorption of pivampicillin as related to dose, and tolerability of a 700 mg tablet

Interactions Affecting Drug Absorption

Absorption of Pivampicillin in Postoperative Patients

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