Species specific pharmacokinetics of rolitetracycline.

Comparative studies on some selected pharmacokinetic parameters of rolitetracycline (effective antimicrobial activity levels) in sheep, pigs, rabbits, chickens and pigeons were carried out after intravenous administration of the drug at a dose of 5 mg/kg. The results revealed that a two-compartment open model was usually optimal. Interspecies differences in the rate (alpha) and the volume of distribution (Vda), the area under the serum concentration time curve (AUC) and the total body clearance (ClB) were small. The values of the elimination half-life (t1/2 beta) found in sheep, pigs, rabbits, chickens and pigeons were 1.51, 3.06, 2.18, 4.33 and 2.51 h respectively. These results and data in mice, rabbits and man taken from literature were analysed to determine any correlation to body mass (W). The log of the elimination half-life values (log t1/2 beta) of rolitetetracycline revealed a significant correlation with log values of (W) between animal species. This relationship was described by the equation t1/2 beta = 1.27.W0.29 (r = 0.93, P < 0.01, n = 5) for mammal species and t1/2 beta = 1.81.W0.24 (r = 0.78, P < 0.05, n = 7) for mammal and bird species.

Sclerotherapy for hydroceles.

Sclerotherapy with 3% sodium tetradecyl sulfate and 3.5% rolitetracycline on an outpatient basis was applied to 55 hydroceles. The over-all cure rate was 96% with an average followup of 13 months. Of the patients 64% were cured after only 1 sclerosant instillation. A post-sclerotherapy operation was necessary in 4% of the patients. Pain of a significant degree occurred after sclerotherapy in only 29% of the patients. Sclerotherapy appears to be an effective, economical and safe form of outpatient therapy for hydroceles.

[Antimicrobial action of rolitetracycline in gelatin sponge packs (Marbagelan) in tympanoplasty]. / Die antimikrobielle Wirksamkeit von Rolitetracyclin in Gelatine-Tamponade (Marbagelan) für die Tympanoplastik.

Gelatine sponge packs (Marbagelan) saturated in rolitetracycline (Reverin) were evaluated. The antimicrobiotic efficacy of the substance was determined in 26 packs before insertion and in 20 packs removed from the external ear meatus after varying periods. High concentrations of rolitetracycline were found independent of saturation grade in the packs before insertion. In the packs removed from the external meatus acceptable antimicrobial activity was found independent of the time the packs remained in the ear. An efficient prophylaxis against infection in ear surgery is guaranteed.

Combined effects of high doses of rolitetracycline and testosterone on the liver of mice.

The effects of rolitetracycline (50 micrograms/g i.v.) and testosterone proprionate (4 X 1 micrograms/g s.c.) singly and combined on liver weight, serum GPT, SDH and bromsulfophthalein clearance have been measured in young mice. Pretreatment with testosterone tended to enhance the effects of rolitetracycline on the serum enzymes but was otherwise not effective.

[Microbiological investigations in tamponades after tympanoplasties (author's transl)]. / Mikrobiologische Untersuchung von Gehörgangstamponaden nach Tympanoplastiken.

In 100 cases microbiological examinations of removed tamponades after tympanoplasties were performed. This paper is concerned with the question, whether there is a correlation between the preoperative status of the middle-ear-mucosa and the postoperative bacterial flora.

Accidental intra-arterial injection.

Accidental intra-arterial injection of intramuscular antibiotic preparations is described in 3 cases in infants. In 2 benzathine penicillin was injected, and in 1 rolitetracycline. The clinical features are dominated by arteriolar obstruction which produces gangrene of the most severely affected limb. In addition, neuroloigcal involvement occurs when vessels to nerves or spinal cord are involved. The arteriolateral aspect of the thigh is preferable to the buttock as a site for intramuscular injection, and a short (2.5 cm) needle should be used to minimise the risk of intra-arterial injection.

Immunization against East Coast fever (Theileria parva infection of cattle) by infection and treatment: chemoprophylaxis with N-pyrrolidinomethyl tetracycline.

Cattle were immunized against East Coast fever by the inoculation of a tick-derived stabilate of Theileria parva infective particles and the intramuscular injection, at daily intervals, of n-pyrrolidinomethyl tetracycline at a dose level of 5 mg/kg. Four doses of the tetracycline, starting on the day of inoculation of the infective stabilate, minimised the ECF reactions in the cattle during immunization. Immunity to homologous T. parva stabilate challenge was demonstrated in 27 out of 27 cattle infected and treated in this manner.

[Tetracycline levels in the sputum in chronic obstructive bronchitis (author's transl)]. / Tetracyclin-Spiegel im Sputum bei chronisch-obstruktiver Bronchitis.

After 3 control days, the tetracycline concentration in the sputum of 34 patients was measured daily on 7 days during treatment with the antibiotic. 14 patients took tetracycline (Hostacyclin) in normal doses (2X500 mg or 2X1000 mg) by mouth. 20 patients received rolitetracycline (Reverin) 2X275 mg i.v. daily. With considerable individual fluctuations, sputum concentrations were attained in all series ranging from 1.5 to 2.0 microgram/ml after intravenous administration and from 1.1 to 1.6 microgram/ml after oral dosage. The higher dosage administered orally had no greater influence on the sputum concentration. In each case, sputum levels were attained which lie above the necessary minimum concentrations (0.5 microgram/ml).

Pharmacokinetic investigations on diminazene and rolitetracycline in comparison to a combination of both.

Serum level tests were carried out on healthy cows with a combination drug of one part Berenil and two parts Reverin. When compared with the commercial preparations Berenil (Diminazene) and Reverin (Rolitetracycline), the kinetic behaviour of Reverin in the combination preparation was identical. In the case of Berenil, administered in the form of the combination drug, the second slow elimination phase with a 63 hour half-life, as found after the administration of Berenil only, could not be observed. Eight hours after administration of the combination only minimal Berenil serum levels were detectable, after 24 hours the levels were lower than the limit of detection. This has a practical bearing on the question of residues.

[The behaviour of creatine phosphokinase in serum after the intramuscular injection of a Tetracyclin preparation (author's transl)]. / Zum verhalten der Kreatinkinase im Serum bei intramuskulärer Injektion von Tetracyclinpräparaten

The single intramuscular injection of 275 mg Rolitetracyclin (Reverin) led to a rise in serum creatine phosphokinase in 11 out of 20 heart healthy patients, 7 cases with values over 100 mU/ml. In sane cases the initial values had still not been reached 72 hours after injection. With Rolitetracyclin given intravenously the creatine phosphokinase values do not alter, as with an isotonic Na-Cl solution given intramuscularly. A rise in the serum creatine phosphokinase was seen in 2 out of 6 cases after an intramuscular injection of Oxytetracyclin (Terramycin -Depot). One is not dealing with a reaction which is typical only to Rolitetracyclin. The cause is thought to be the setting free of enzymes through the musclelesions. The results underline the sensitivity of and problems involved with creatine phosphokinase in the diagnosis of heart-infarction.

[Studies on the absorption and excretion of doxycycline for intravenous use (author's transl)].

The absorption and excretion of a new doxycycline solution for intravenous use (DOTC iv) were studied with the following results. 1. Serum levels following one shot intravenous injection of DOTC iv in glucose solution showed a good dose-response comparable with that of the same dose injection of pyrrolidinomethyltetracycline (PRM-TC). The urinary excretion was also examined. In 200 mg injection, nausea, general warm feeling, odor in mouth and tongue numbness were complained. 2. When DOTC iv was injected intramuscularly, the serum level did not reach the peak value and low level continued for a long time. Moderate local pain was complained at the site of injection. 3. The serum level following drip infection of DOTC dry fill showed a dose-response as well. The local vein tolerated well. 4. No abnormalities were found in clinical and laboratory examinations in all volunteers.