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PubMedDate not supplied

Metabolism of doxylamine succinate in Fischer 344 rats. Part III: Conjugated urinary and fecal metabolites.

Elimination and metabolic profiles of the glucuronide products of doxylamine and its N-demethylated metabolites were determined after the oral administration of (14C)-doxylamine succinate (13.3 and 133 mg/kg doses) to male and female Fischer 344 rats. The cumulative urinary and fecal eliminations of these conjugated doxylamine metabolites at the 13.3 mg/kg dose were 44.4 +/- 4.2% and 47.3 +/- 8.1% of the total recovered dose for male and female rats, respectively. The cumulative urinary and fecal eliminations of conjugated doxylamine metabolites at the 133 mg/kg dose were 55.2 +/- 2.6% and 47.9 +/- 2.5% of the total recovered dose for male and female rats, respectively. The conjugated doxylamine metabolites that were isolated, quantitated, and identified are doxylamine O-glucuronide, N-desmethyl-doxylamine O-glucuronide, and N,N-didesmethyldoxylamine O-glucuronide.

Administration, Oral↗
PubMed1975

Antitussive drugs. II. Bronchopulmonary effects of dextromethorphan and doxylamine.

Unlike codeine, dextromethorphan does not cause pulmonary vasoconstiction in the anesthetized dog. The other effects of dextromethorphan are as follwos: a rise in pulmonary resistance indicating bronchoconstriction, and increase in pulmonary blood flow relating to a positive inotropic action, and a decrease in aortic blood pressure resulting from systemic vasodilation. These effects are blocked by previous injections of doxylamine, an antihistaminic drug. This interaction suggests a rationale for the combined use of dextromethorphan and doxylamine in the treatment of upper respiratory infection.

Airway Resistance↗
PubMed1977

Antenatal exposure to doxylamine succinate and dicyclomine hydrochloride (Benedectin) in relation to congenital malformations, perinatal mortality rate, birth weight, and intelligence quotient score.

In a prospective cohort study of 20, 282 gravidas and their offspring, congenital malformation rates were similar in the children of over 1,000 women exposed and those not exposed to two components of Bendectin (doxylamine succinate and dicyclomine hydrochloride) during the first four lunar months of pregnancy. In a cohort reduced to 41,337 mother-child pairs for technical reasons, mean birth weight and perinatal mortality rates were similar according to exposure or nonexposure to either drug, as were intelligence quotient scores measured at four years of age in 28,358 of the children. Control of potential confounding factors with a variety of multivariate techniques did not materially alter these findings.

Abnormalities, Drug-Induced↗
PubMed1977

[Double-blind long-term study on a combination of tetracycline, theophylline, doxylamine succinate, etafedrine, phenylephedrine and guaifenesine in chronic bronchitis (author's transl)].

The investigations presented were undertaken to find out whether a long-term treatment of chronic bronchitis with a combination of tetracycline, theophylline, doxylamine succinate, etafedrine, phenylephrine and guaifenesine could reduce the frequency of recurrent infections of the respiratory system. Out of 57 patients who all had suffered from at least one exacerbation in the year preceding the trial only 12 showed clinical signs of an ixacerbation during the study. 12 exacerbations occurred during the placebo phase, 6 during the treatment with Ditenate Tetra. It is specified why such a long-term treatment with an antibiotic should be reserved only for patients who are especially endangered by the exacerbation. The results of numerous microbiological investigations of sputa, nose and throat swabs before and during the long-term study are interpreted under certain aspects and questioning.

Adult↗
PubMed1975

Fatal overdose from Bendectin.

A three-year old male ingested approximately 100 tablets of Bendectin. He developed tonic-clonic seizures followed by cardiac arrest. Toxicologic analysis yielded high levels of doxylamine, dicyclomine, and pyridoxine in blood, peritoneal fluid, and tissue homogenates. The antihistamine, doxylamine succinate appears to be the toxic constituent. Analytical methods used to document the case are herein described.

Accidents, Home↗
PubMed1976

Double-blind trial of a long-acting bronchodilator preparation ("Nethaprin Dospan") in bronchospastic disease.

A double-blind, placebo-controlled, crossover study was carried out in 48 patients with bronchospastic disease to assess the efficacy of a long-acting bronchodilator preparation ("Nethaprin Dospan") containing etafedrine hydrochloride, bufylline, doxylamine succinate and phenylephrine. Patients received 1 tablet nightly, with an extra dose in the morning if necessary, of active drug or placebo for 1 week, and were then crossed over to the alternative medication for a further week. All patients had marked disability, apparent on initial clinical examination and on respiratory function tests. The results showed that FEV1 and VC were significantly improved with the active medication, and patients slept better, had improved appetite and suppression of cough.

Asthma↗
PubMed1976

Treatment of migraine attacks with an analgesic combination (Mersyndol).

The relief of acute migraine attacks with an analgesic/antihistamine combination containing paracetamol, codeine phosphate, doxylamine succinate and caffeine (Mersyndol) compared with that achieved with a placebo has been studied in a double-blind, crossover trial. Mersyndol emerged as significantly better than placebo in the complete relief of migraine pain, and was clearly superior to placebo in partially relieving the pain of migraine. These results suggest that it could be a useful alternative to ergotamine, and a comparative trial with ergotamine is suggested. Side effects with this combination were fairly common but mild, and consisted mainly of drowsiness caused by the antihistamine component.

Acetaminophen↗
PubMed1991

Regulation by 1,4-diamines of the ornithine decarboxylase activity induced by ornithine in perifused tumor cells.

Ornithine decarboxylase (ODC) activity of Ehrlich carcinoma cells was increased more than 36-fold after being maintained for 3.5 hr in vitro in a special chamber which allowed continuous perifusion with 0.5 mM ornithine; if incubated in vitro without perifusion the ODC activity was, of course, only 9-fold by the same concentration of ornithine. Ornithine withdrawal from the perifusion medium resulted in a decay of enzyme activity observed after 90 min; this decay was prevented by addition of 55 microM pyridoxal to the medium. The 1,4-diamines putrescine, spermidine, spermine, agmatine, histamine, serotonin, tryptamine, chlorpheniramine and harmaline at 55 microM strongly suppressed ODC induction by 0.5 mM ornithine in perifused Ehrlich ascites cells. Methyl derivatives also behave as strong inhibitors of ODC induction. On the contrary, N-acetylation paralleled with a decrease in the inhibition capacity: 55 microM N-acetyl putrescine, N-acetyl serotonin or N-omega-acetylhistamine suppressed ODC induction by ornithine in 66, 64 and 19%, respectively. The addition to the perifusion medium of the same concentrations of 1,3-diamines (1,3-diaminopropane, 1,3-diamino-2-propanol or the alkaloid gramine) as well as 1,5-diamines (1,5-diaminopentane and the antihistamic doxylamine or cimetidine) failed to suppress the induction of ODC activity by ornithine. Interestingly, 1,4-benzenediamine, which strongly inhibits ODC activity when the induced enzyme is assayed in its presence, did not suppress the induction of the enzyme when both 0.5 mM ornithine and 55 microM 1,4-benzenediamine were present in the perifusion medium. The inhibitory capacity in down-regulating ODC is not due to differences in the diamine uptake by the cells. The results suggest that the N-N distance (6A) and the charge of one amino group are important chemical characteristics for regulatory effects.

Alkaloids↗
PubMed1992

Determination of diphenylmethane antihistaminic drugs and their analogues in body fluids by gas chromatography with surface ionization detection.

Eleven diphenylmethane antihistaminic drugs and their analogues were tested for their detection by capillary gas chromatography (GC) with surface ionization detection (SID). The GC-SID response was highest for doxylamine, diphenhydramine and orphenadrine and lowest for terodiline, clemastine and pipethanate. The detection limits for drugs with the highest response were 2-5 pg (ca. 6-20 fmol) on-column (100-250 pg/ml of body fluid). The detection limits with GC-SID were 10-100 times higher than those with GC with nitrogen-phosphorus detection. A detailed procedure for the isolation of the antihistaminics from human whole blood and urine by the use of Sep-Pak C18 cartridges, prior to GC-SID, is also presented. The recoveries of the drugs (50 or 500 pmol), which had been added to 1 ml of body fluids, were > 60%. The baselines remained steady as the column temperature was increased and the background was clean, especially for whole blood extracts.

Benzhydryl Compounds↗
PubMed1979

Exogenous hormones and other drug exposures of children with congenital heart disease.

A history of oral contraceptive use, hormonal pregnancy tests, prescribed hormones and other drugs was obtained from 390 mothers of infants with congenital heart disease and 1254 mothers of normal infants in Massachusetts. The data show a small positive association between estrogen/progesterone exposure and cardiac malformation, the prevalence ratio estimate of exposed to non-exposed being 1.5 (90 per cent confidence limits are 1.0, 2.1). No association was evident, however, between hormones and trunco-conal or any other class of defect among the cases, an observation which casts doubt on a causal relationship betweem hormones and cardiovascular malformations. Several other drugs were reported more frequently by cases' mothers. These include: ampicillin; aspirin; a combined anti-nausea agent (doxylamine succinate, dicyclomine hydrochloride and pyridoxine hydrochloride); chlordiazopoxide, codeine, diazepam, diphenylhydantoin; insulin; phenobarbital; phenothiazine; phenylephrine; and tetracycline.

Estrogens↗
PubMed1991

N(+)-glucuronidation of aliphatic tertiary amines, a general phenomenon in the metabolism of H1-antihistamines in humans.

1. Representative drugs of the various structural classes of H1 antihistamines were chosen for study. The drugs chosen (class name in parentheses) were chlorpheniramine maleate and pheniramine maleate (alkylamines), diphenhydramine hydrochloride and doxylamine succinate (ethanolamines), pyrilamine maleate and tripelennamine hydrochloride (ethylenediamines), promethazine hydrochloride (phenothiazine), cyclizine lactate (piperazine) and terfenadine (miscellaneous). In each case oral dose(s) were administered over no more than 6 h to two healthy volunteers and the total urine collected for 36 h. 2. Metabolites from urine were separated by h.p.l.c. and individually collected prior to mass spectrometric analysis in the fast atom bombardment mode. The structure of each metabolite identified as a quaternary ammonium-linked glucuronide metabolite was confirmed by direct comparison of its mass spectrum and chromatographic behaviour with that of a synthetic authentic compound. 3. For eight of the nine drugs studied, metabolism by the N(+)-glucuronidation pathway was observed in each of the volunteers. Terfenadine was the exception. 4. The amount of each N(+)-glucuronide in the urine was estimated by h.p.l.c. analysis. The mean proportion of dose excreted as the metabolite was 14.3%, 6.5% and 4.0% for cyclizine, tripelennamine and diphenhydramine, respectively. Promethazine was the only case where the N(+)-glucuronide accounted for less than 1.0% of the administered dose in both volunteers examined.

Adult↗
PubMed1978

Teratogenicity testing in humans: a method demonstrating safety of bendectin.

We investigated the incidence of birth defects in the offspring of women who took Bendectin during pregnancy. Copies of all prescriptions issued for Bendectin in two Cities, Leeds and Liverpool, over periods of 12 and 14 months, respectively, were scanned and a record initiated for each patient. Birth notifications were later searched for matching with indexed patients. Births were traced for 2,298 patients and the incidence of major defects compared with those in the relevant populations. We found no evidence to suggest that Bendectin is teratogenic in humans.

Abnormalities, Drug-Induced↗
PubMed1976

An evaluation of the teratogenicity of certain antinauseant drugs.

In a large, prospective, observational study of pregnancy and child development, the antinauseant drugs prescribed to gravides for nausea and vomiting in the first 84 days of pregnancy were evaluated for their teratogenic potential. The severe congenital anomaly rates per 100 liveborn children and ther perinatal death rates of this group did not differ from the rates of the group with untreated nausea and vomiting. There was no indication that the phenothiazine derivatives, specifically the prochlorperazine derivative, as well as meclizine, cylizine, and Bendectin were associated with teratogenicity. The trimethobenzamide drug gave a slight suggestion of an excess of severe congenital anomalies.

Abnormalities, Drug-Induced↗
PubMed1977

Treatment of pregnancy sickness.

A double-blind comparison was undertaken between Debendox with 10mg of extra pyridoxine and placebo with 10mg of pyridoxine, in 56 women suffering from nausea and/or vomiting during the first 10 weeks of pregnancy. The results of treatment were assessed on the patient's own dialy records of:the time of nausea, the frequency of nausea, and the severity of nausea, retching and vomiting. There were statistically significant differences in favour of Debendox with extra pyridoxine in respect of the days of nausea all day (P les than 0-02), the severity of nausea (P less than 0-05) and the severity of retching (P less than 0.05).

Clinical Trials as Topic↗
PubMed1992

Risk, statistical inference, and the law of evidence: the use of epidemiological data in toxic tort cases.

Toxic torts are product liability cases dealing with alleged injuries due to chemical or biological hazards such as radiation, thalidomide, or Agent Orange. Toxic tort cases typically rely more heavily than other product liability cases on indirect or statistical proof of injury. There have been numerous theoretical analyses of statistical proof of injury in toxic tort cases. However, there have been only a handful of actual legal decisions regarding the use of such statistical evidence, and most of those decisions have been inconclusive. Recently, a major case from the Fifth Circuit, involving allegations that Benedectin (a morning sickness drug) caused birth defects, was decided entirely on the basis of statistical inference. This paper examines both the conceptual basis of that decision, and also the relationships among statistical inference, scientific evidence, and the rules of product liability in general.

Abnormalities, Drug-Induced↗