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PubMedDate not supplied

Spectrophotometric determination of aminacrine hydrochloride in creams, jellies, and suppositories: interlaboratory study.

A previously reported visible spectrophotometric method for the analysis of aminacrine hydrochloride in creams, jellies, and suppositories was studied collaboratively by 8 laboratories. Aminacrine hydrochloride was extracted into acidic ethanol and its visible spectrum recorded. The amount present was calculated by determining the net absorbance between the absorbance maximum at about 402 nm and one-half the sum of the absorbance of the minima at about 389 and 412 nm. Each collaborator received 4 creams (0.2%), 1 jel (0.2%), 1 molded suppository (6 mg/3.198 g), and 2 gelatin-encapsulated suppository samples (12 mg/6.661 g and 14 mg/6.863 g). The cream samples included blind duplicates prepared to contain 0.212% aminacrine hydrochloride, 15% sulfanilamide, and 2% allantoin. Mean recovery for the authentic cream was 104.7% with a coefficient of variation (CV) of 9.22%. The commercial products contained these respective amounts (CVs): creams, 100.0% (2.48%) and 101.5% (2.16%); jel, 118.0% (9.58%); molded suppository, 102.7% (1.88%); and gelatin encapsulated suppositories, 93.1% (1.0%) and 94.3% (1.60%). Standard aminacrine hydrochloride provided for the study was 99.6% pure by nonaqueous titration. Thin layer chromatographic identification of aminacrine hydrochloride was also tested collaboratively. The method was not adopted by AOAC.

Aminacrine↗
PubMed1983

Evaluation of fluorometric determination-thin layer chromatographic identification of aminacrine hydrochloride in drug preparations.

Utilizing the fluorescent property of aminacrine hydrochloride and a filter fluorometer, a fluorometric method for aminacrine hydrochloride in drug combinations was developed, collaboratively studied, and adopted as official first action in the 11th edition of Official Methods of Analysis. Identity was confirmed by thin layer chromatography (TLC). Additional analytical work was undertaken with a grating fluorometer to support a change in the method status to official final action. The grating instrument recorded the aminacrine hydrochloride spectrum as opposed to the total fluorescence emission measured by the filter instrument. The spectrum of aminacrine hydrochloride showed that the molecule was exhibiting self-absorption of the emitted radiation even at concentrations of 10(-6)M and that the ratio of the 2 peaks in the emission spectrum varied with concentration. Additional analyses of an authentic cream preparation that also contained sulfanilamide gave an average recovery of 86.0% for aminacrine hydrochloride in 10 replicate portions. Because of these observations, the current Associate Referee's recommendation to delete the fluorometric procedure from the 13th edition of Official Methods of Analysis was adopted. A recommended deletion of the TLC identification test was also adopted.

Aminacrine↗
PubMed1983

Spectrophotometric determination of aminacrine hydrochloride in creams, jellies, and suppositories.

A visible spectrophotometric method has been developed for the quantitation of aminacrine hydrochloride in creams, jellies, and suppositories. Aminacrine hydrochloride was extracted into acidic ethanol and its visible spectrum was recorded. The amount present was calculated by determining the net absorbance between the absorbance maximum at about 402 nm and one-half the sum of the absorbances of the minima at about 389 and 412 nm. Aminacrine and a trace contaminant, 9(10H)-acridone, were independently identified by different thin layer chromatographic systems.

Aminacrine↗
PubMed1997

Multicenter comparison of clotrimazole vaginal tablets, oral metronidazole, and vaginal suppositories containing sulfanilamide, aminacrine hydrochloride, and allantoin in the treatment of symptomatic trichomoniasis.

BACKGROUND AND OBJECTIVES: Trichomonas vaginalis is a common vaginal pathogen. Oral metronidazole is the drug of choice for the treatment of trichomoniasis. Oral metronidazole, however, may cause unpleasant side effects and is contraindicated during the first trimester of pregnancy. In vitro studies and preliminary clinical data have suggested that intravaginal clotrimazole may be effective against this pathogen. GOALS: To compare the efficacy of clotrimazole vaginal tablets, oral metronidazole, and vaginal suppositories containing sulfanilamide, aminacrine, and allantoin (AVC suppositories) in the treatment of women with symptomatic trichomoniasis. STUDY DESIGN: In a multicenter, open-label trial conducted in 1982 and 1983, 168 symptomatic women with microscopically evident vaginal trichomoniasis were randomized to receive any of 2 g of metronidazole as a single oral dose, two 100-mg clotrimazole vaginal tablets once a day for 7 days, or vaginal suppositories containing 1.05 g of sulfanilamide, 14 mg of aminacrine hydrochloride, and 140 mg of allantoin (AVC suppositories) twice a day for 7 days. Wet mounts and cultures were repated at 1 to 2 and 4 to 6 weeks after completion of treatment. RESULTS: The number of patients who had positive cultures after treatment were 40/45 (88.9%) in the clotrimazole group, 35/43 (81.4%) in the AVC suppository group, and 9/45 (20%) in the metronidazole group (P < 0.001). All treatments were associated with a reduction in reported symptoms. Oral metrohidazole was more effective in reducing symptoms than either of the topical preparations. Adverse events, mostly mild or moderate in severity, were reported by 7 (14.6%) of 48 patients who had received oral metronidazole and 4 (7.8%) of 51 women who used AVC suppositories. There were no adverse events reported by the 50 women who used clotrimazole vaginal tablets. CONCLUSIONS: Oral metronidazole was more effective in eradicating T. vaginalis than clotrimazole vaginal tablets or AVC vaginal suppositories. All three regimens reduced symptoms; oral metronidazole was more effective in reducing symptoms than either topical preparation.

Administration, Intravaginal↗
PubMed1975

Influence of tetrahydro-aminacrine on muscle pains after suxamethonium.

The incidence and severity of muscle pains were investigated in patients who had been given suxamethonium and thiopentone anesthesia for bronchoscopy. Group I patients received no other drugs. Groups II and III received d-tubocurarine and THA respectively before suxamethonium. Administration of these drugs resulted in a highly significant reduction in the incidence of severe and moderate pains. The use of d-tubocurarine necessitated a significantly greater amount of suxamethonium to maintain paralysis.

Acridines↗
PubMed1989

Stimulus-dependent pacemaker activity in the distal canine lower esophageal sphincter.

Electrical and mechanical properties of the distal canine lower esophageal sphincter were studied in vitro to investigate possible means of inducing pacemaker activity. Both direct excitation and block of potassium conductance were investigated. The acetylcholine analog, carbachol, induced tissue depolarization and increase in tone but no electrical slow waves. Tetraethylammonium (TEA) chloride induced depolarization and evoked continuous spiking activity and increase in tone. BaCl did not depolarize the tissue but low amplitude spiking activity developed and increased tone. The putative potassium channel blocker, aminacrine at 2 X 10(-4) M, induced electrical slow wave activity in the distal lower esophageal sphincter, with or without superimposed spikes, accompanied by phasic contractile activity. This activity closely resembled the spontaneous pacemaker activity observed previously in the proximal lower esophageal sphincter. The aminacrine-induced activity was abolished by calcium influx blockers. Aminacrine, but not TEA or BaCl, abolished the nonadrenergic nerve-mediated inhibitory junction potentials. In conclusion, block of inhibitory innervation, and induction of electrical slow waves as a control mechanism for phasic contractile activity, seems to require blockade of an aminacrine- but not TEA-sensitive potassium conductance.

Animals↗
PubMed1988

Characterization of inhibitory innervation in porcine colonic circular muscle.

Effects of stimulation of intramural nerves in the circular smooth muscle layer of the porcine colon (Sus scrofa domestica) were studied using the sucrose-gap technique. Electrical field stimulation of the preparation, superfused with Krebs solution at 21 degrees C, induced a transient hyperpolarization of the smooth muscle cell membrane. This hyperpolarization was an inhibitory junction potential (IJP). The responses obtained from circular muscle originating from either the centripetal or centrifugal gyri of the ascending colon did not differ significantly. The IJP was characterized as being mediated by intramural, nonadrenergic, noncholinergic (NANC) nerves. The amplitude and latency of the IJP changed linearly with temperature (15-25 degrees C: +1 mV and -0.1 s per degree Celsius, respectively) reflecting a temperature-dependent synchronization of transmitter release. The membrane resistance decreased during the IJP. The IJP amplitude decreased or increased during conditioning hyperpolarizations or depolarizations, respectively, and reversed at membrane potentials about 30 mV more negative than the resting membrane potential. Potassium conductance blocking agents, barium (1 mM), tetraethylammonium chloride (TEA, 20 mM), 4-aminopyridine (4-AP, 5 mM), apamin (1 microM), and aminacrine (10(-4) M) added to the superfusion medium increased the membrane resistance. Only barium, TEA, and apamin depolarized the smooth muscle cell membrane. The IJP amplitude decreased in the presence of aminacrine and apamin to 75 and 35%, respectively, suggesting that apamin-sensitive Ca2+-activated K+ channels are involved in this response. ATP, adenosine, and related adenine nucleotides in concentrations up to 10(-3) M did not mimic the IJP. Superfusion with ATP for 15 min revealed a gradually increasing attenuation by up to 20% of the IJP. This might suggest that the release of neurotransmitter from intramural NANC nerves is modulated presynaptically via purinoceptors. Exogenously applied vasoactive intestinal polypeptide (VIP) in concentrations of 10(-9) to 10(-4) M did not affect the preparation. Also at elevated temperatures (up to 35 degrees C), VIP (10(-7) to 10(-4) M) did not cause measurable effects. It is concluded that the inhibitory mediator of the intramural NANC nerves present in the circular muscle layers of the porcine colon is neither a purine nor VIP.

Animals↗
PubMed1987

Pregnancy outcomes after first-trimester vaginitis drug therapy.

Prescription frequencies in the first trimester were compared for miconazole, clotrimazole, nystatin, candicidin, aminacrine compounds, and metronidazole before deliveries involving congenital anomalies versus those not linked to congenital anomalies. Prescriptions before spontaneous abortions were compared with those in the first trimester of deliveries and with those before legal abortions. No statistically significant association was observed with any of these agents for the overall frequency of birth defects or for specific birth defects analyzed (cardiovascular defects, oral clefts, and spina bifida). Two hundred fifty miconazole exposures among 4264 spontaneous abortions, compared with 2236 in the first trimester of 55,736 deliveries, provided an estimated relative risk of 1.4 (95% confidence limits 1.2-1.5). One hundred twelve treatments with clotrimazole among the spontaneous abortions, compared with 1086 among the deliveries, provided a relative risk of 1.4 (95% confidence limits 1.1-1.6). In contrast, large numbers of exposures to nystatin and aminacrine compounds did not show this association, suggesting that spontaneous abortions are caused by the imidazole agents miconazole and clotrimazole rather than the condition being treated. Because many associations were examined without previous hypotheses, and because the data were inadequate to show an elevated risk for clotrimazole when comparing spontaneous with legal abortion exposures, these findings are considered to be a signal for further studies rather than definitive in themselves.

Abnormalities, Drug-Induced↗
PubMed1977

Photosensitization by drugs.

UV irradiation (365 nm) of air-saturated methanol solutions of 20 drugs absorbing in the 300--400 nm region gave rise to oxygen uptake, as determined with a polarographic oxygen electrode. The drugs were tested for photosensitizing capability by either a Type I (free radical) or a Type II (single molecular oxygen) mechanism. This testing was done by the inclusion of either acrylamide or 2,5-dimethylfuran in the irradiated drug solution, with observation of the subsequent polymerization or oxidation, respectively. Phenothiazine and thiazide derivatives appear capable of photosensitization by both mechanisms; promethazine, trifluoperazine, and furosemide show relatively high reactivity. Diazepam (weak), hexachlorophene, aminacrine, pyrilamine, tetracycline, demeclocycline, quinine, and anthracene (strong) react only by a Type II mechanism, with a photosensitizing efficiency increasing in the order given. A correlation appears to exist with reports of in vivo photosensitivity.

Acrylamides↗
PubMed1994

Effects of vesicular acetylcholine uptake blockers on frequency augmentation-potentiation in frog neuromuscular transmission.

Vesamicol inhibits the vesicular loading of acetylcholine molecules. The effects of vesamicol and similarly acting compounds on neuromuscular transmission in frogs were investigated to determine whether these inhibitors-inhibit the frequency augmentation-potentiation of transmitter release. Various vesicular acetylcholine transport blockers suppressed the stimulation frequency-related release parameter, k, in a dose-dependent manner. Artane, cetiedil, chloroquine, ethodin, quinacrine, vesamicol and its benzyl-analogue, 2-(4-benzylpiperidino)cyclohexanol, had strong effects, while those of aminacrine, chlorpromazine, fluphenazine, imipramine, pyrilamine and thioridazine were weak. A significant correlation was observed between the biochemically reported values of IC50 and the electrophysiological inhibitory potencies on k at 20 microM. Contrary to expectations from the biochemical data, however, vesamicol and its benzyl-analogue showed equipotent inhibitory actions on the electrophysiological frequency augmentation-potentiation relation. Low sensitivity and low selectivity of the frequency augmentation-potentiation for vesamicol and its benzyl-analogue lead us to conclude that the vesicular acetylcholine transporter is not the site of the electrophysiological action of vesamicol and similarly acting chemicals.

Acetylcholine↗
PubMed1985

Trypanosoma cruzi: possible control of parasite transmission by blood transfusion using amphiphilic cationic drugs.

About 200 clinically used amphiphilic cationic drugs have been shown to be active in vitro against Trypanosoma cruzi at concentrations of less than or equal to 1 mM. Activity against epimastigote and trypomastigote forms was similar, and in both cases the most potent drugs were litracene, maprotiline, thioproperazine, and the acridines: acranil, aminacrine, and mepacrine. Fluorescence microscopy demonstrated that epimastigotes rapidly accumulate acridines initially in discrete subcellular organelles. The amount of drug incorporated during 15 min of incubation was sufficient to produce subsequent lysis of both trypomastigotes and epimastigotes within 24 hr at 4 C. Trypanocidal activity was dependent on the extracellular pH (optimum greater than or equal to 8) and drug exposure time, but was independent of red blood cell density, serum dilution, and temperature (4 to 37 C). Despite their trypanocidal activity, amphiphilic cationic drugs appear to have no significant effect on the energy state of red blood cells at a concentration of 1 mM. These drugs have a possible role in the prevention of Chagas' disease by blood transfusion.

Aminoacridines↗
PubMed1998

A comparison of the bactericidal and photobactericidal activities of aminoacridines and bis(aminoacridines).

An attempt was made to increase the activity of some antibacterial acridines in two ways: (a) via the use of bis-aminacrines (analogues of 1,6-bis-[9-acridinamino]hexane), in order to increase the potential for DNA intercalation and (b) via photoactivation, as several acridines are known to produce the cytotoxin singlet oxygen on irradiation. The bactericidal activity of the simple aminoacridines was much higher than that of the corresponding bis-acridine compounds. In addition, on low-power illumination of the compounds in liquid culture, many of the monomeric compounds exhibited marked increases in activity against both Gram-negative and Gram-positive bacteria, whereas the bis-acridines showed little or no increase.

Aminoacridines↗
PubMed1997

In-vitro photobactericidal activity of aminoacridines.

The toxicities of several aminoacridines were measured against pathogenic strains of both Gram-positive (Staphylococcus aureus, Enterococcus faecalis, Bacillus cereus) and Gram-negative (Escherichia coli, Pseudomonas aeruginosa) organisms. In several cases, illumination at a light dose of 6.3 J/cm2 resulted in considerable decreases in the minimum lethal drug concentrations required, giving up to 50-fold increases in bactericidal activity. Derivatives of 9-aminoacridine (aminacrine) exhibited phototoxicity against one or more of the test organisms, but the established photosensitizing acridines proflavine and acridine orange were photobactericidal against all strains.

Aminoacridines↗
PubMed1974

New antimicrobial nitrofuran, trans-5-amino-3-[2-(5-nitro-2-furyl)vinyl]-delta2-1,2,4-oxadiazole: antimicrobial efficacy in mice, rats, and guinea pigs.

A new antimicrobial nitrofuran designated SQ 18,506 showed some therapeutic activity when administered orally to mice infected with Escherichia coli, Salmonella schottmuelleri, Shigella flexneri, or Klebsiella pneumoniae. Animals infected parenterally with Streptococcus pyogenes, Proteus mirabilis, Mycobacterium tuberculosis, and Candida albicans, or topically with Trichophyton mentagrophytes, did not respond to therapy with the drug at the dosage levels used. The compound was as effective as metronidazole in the topical treatment of experimental trichomonal infections in mice and in guinea pigs and as effective as nystatin, candicidin, or a sulfanilamide-aminacrine hydrochloride cream in the treatment of a candidal vaginal infection in rats. The chemotherapeutic efficacy of SQ 18,506 in experimental vaginitis caused by Escherichia coli in the rat surpassed that shown by four commercial products available for the treatment of bacterial vaginitis.

5-Amino-3-((5-nitro-2-furyl)vinyl)-1,2,4-oxadiazol↗
PubMed1986

A strategy for the prevention of the transmission of Chagas' disease during blood transfusion.

Our strategy for preventing the transmission of Chagas' disease during blood transfusion is discussed. In addition, the possibility that the Peru, Sonya, Tulahuen and Y strains of Trypanosoma cruzi show varying sensitivities to a series of amphiphilic cationic drugs in vitro at 4 degrees C was investigated using a microscope lysis test. All 21 drugs tested at a concentration of 10(-3) M lysed Sonya bloodstream trypomastigotes, but Peru, Tulahuen and Y strains were affected by 17, 17 and 11 drugs, respectively. All four strains were most sensitive to the acridines; acranil, aminacrine and mepacrine. Although some variation was seen in their responses to certain drugs, no one strain was particularly insensitive to the series as a whole. The effects of gentian violet, maprotiline and mepacrine on the infectivity of Sonya trypomastigotes following incubation at 4 degrees C for 24 h were evaluated. Mepacrine, at a concentration of 2.5 X 10(-4) M greatly decreased the viability of trypomastigotes, while 10(-3) M concentrations of both maprotiline, mepacrine, and gentian violet (at low parasite densities only) apparently abolished all infectivity. Although the compounds we tested did not show a significant improvement over gentian violet, the compound currently used in some blood banks, other existing amphiphilic cationic drugs could be of use in preventing the transmission of Chagas' disease during blood transfusion.

Chagas Disease↗
PubMedDate not supplied

Current therapy of vulvovaginitis.

Trichomoniasis is reliably treated with a single 2-g dose of metronidazole; however, with this regimen simultaneous treatment of sexual partners is particularly important. Trichomoniasis in pregnant women, who should not receive metronidazole, might be treated initially with clotrimazole vaginal suppositories, which appear to cure about 50% of cases. Topical antifungal agents of the imidazole class are superior to polyenes in treating vulvovaginal candidiasis. Boric acid powder applied intravaginally in gelatin capsules for 14 days appears as effective as imidazoles. Nonspecific vaginitis is now recognized as involving infection with anaerobic bacteria of the vaginal flora as well as Gardnerella vaginalis. The condition is most successfully treated with a seven-day course of metronidazole, which probably acts by eradicating the anaerobes. In addition, metabolites of metronidazole may act directly on G. vaginalis. Sulfanilamide-aminacrine-allantoin preparations are much less effective than specific therapies and have no role in the treatment of vulvovaginitis.

Antifungal Agents↗