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PubMed1994

The psychomotor and cognitive effects of a new antihistamine, mizolastine, compared to terfenadine, triprolidine and placebo in healthy volunteers.

Eighteen healthy volunteers received mizolastine 5 mg, 15 mg or 45 mg, terfenadine 60 mg, triprolidine 10 mg or placebo in a 6-way crossover, double blind study. Following each dose, subjects performed a series of tests of cognitive function and psychomotor performance at 1, 3, 5, 8 and 24 hours post-dose. The test battery included critical flicker fusion, choice reaction time, tracking, Stroop and Sternberg memory tests and assessment of subjective sedation. Sedative effects and a concomitant reduction in psychomotor and cognitive function were observed following triprolidine, terfenadine and the highest dose of mizolastine, 45 mg, e.g. triprolidine reduced CFF threshold by 1.5 Hz and increased reaction time by 50 ms, impairments comparable to those caused by blood alcohol concentrations of 50 mg%, the legal limit in many countries. Mizolastine 5 mg did not differ significantly from placebo and at 15 mg differed only at one test point at one time. It may be concluded that mizolastine (5 mg and 15 mg) is free from disruptive effects on cognitive function and psychomotor performance, in contrast to terfenadine 60 mg, triprolidine 10 mg and mizolastine 45 mg.

Adolescent↗
PubMed2005

Antihistamine effects of triprolidine from the transdermal administration of the TPX matrix in rats.

The antihistamine effects of the triprolidine were studied in rats to determine the feasibility of their enhanced transdermal delivery from the poly (4-methyl-1-pentene) (TPX) matrix system containing penetration enhancer and plasticizer. The antihistamine effects were determined by the Evans blue dye procedure by comparing the changes in vascular permeability increase following the transdermal administration. The vascular permeability increase was significantly reduced by transdermal administration of the triprolidine-TPX system containing triethyl citrate (TEC) and polyoxyethylene-2-oleyl ether (POE). Both the plasticizer and penetration enhancer played an important role in the skin permeation of triprolidine and increased the antihistamine effects. These results showed that the triprolidine-TPX matrix system containing plasticizer and penetration enhancer could be a transdermal delivery system providing the increased antihistamine effects.

Administration, Cutaneous↗
PubMed2002

Application of TPX polymer membranes for the controlled release of triprolidine.

Oral administration of triprolidine, antihistamines, may cause many adverse effects such as dry mouth, sedation, dizziness and transdermal drug delivery was considered. Poly(4-methyl-1-pentene) (TPX) membrane, which has good mechanical strength was fabricated by the casting method. TPX membranes was a little brittle and the plasticizers was added for preparing the membranes. The present study was carried out to evaluate the possibility of using the polymer TPX membrane as a controlling membrane and further develop a TPX matrix system for transdermal delivery of triprolidine. The effects of molecular weights of TPX, plasticizers, polyethylene glycol (PEG) 400, drug concentration, and temperature on drug release were studied. The solubility of triprolidine increased exponentially as the increased volume fraction of PEG 400 in saline, and the rate of permeation through TPX membrane was proportional to PEG 400 volume fraction. The release rate of drug from the TPX matrix increased with increased temperature and drug concentration. Among the plasticizers used such as alkyl citrates, phthalates and sebacate, tetra ethyl citrate (TEC) showed the best enhancing effects. Enhancement factor of TEC was 3.76 from TPX matrix at 37 degrees C. The transdermal controlled release of triprolidine system could be developed using the TPX polymer including the plasticizer.

Anti-Allergic Agents↗
PubMed2002

Transdermal delivery of triprolidine using TPX polymer membrane.

Triprolidine-containing matrix was fabricated with poly(4-methyl-1-pentene) (TPX) polymer to control the release of the drug. Effect of penetration enhancer and stripping of skin on the permeation of triprolidine through the excised mouse skin was studied. Penetrating enhancers showed the increased flux probably due to the enhancing effect on the skin barrier, the stratum corneum. Among enhancers used such as glycols, fatty acids and non-ionic surfactants, polyoxyethylene-2-oleyl ether showed the best enhancement. The permeability of triprolidine was markedly increased with stripping the mouse skin to remove the stratum corneum, which acts as a barrier of skin permeation. For the controlling delivery of triprolidine, the TPX matrix containing permeation enhancer could be developed.

Administration, Cutaneous↗
PubMed2002

Controlled release of triprolidine using ethylene-vinyl acetate membrane and matrix systems.

The studies on the permeability of triprolidine through ethylene-vinyl acetate (EVA) copolymer membrane using two-chamber diffusion cell was carried out to develop the controlled delivery system. To evaluate the effect of drug concentration in reservoir, polyethylene glycol (PEG) 400 was added to saline solution as a solubilizer and a sink condition was maintained in the receptor solution. The permeation rate of drug through EVA membrane was proportional to PEG 400 volume fraction. A linear relationship existed between the permeation rate and the reciprocal of the membrane thickness. Triprolidine-containing matrix was fabricated with EVA copolymer to control the release of the drug. The plasticizers was added for preparing the pore structure of EVA membranes to increase the drug release. The effects of PEG 400, vinyl acetate (VA) contents of EVA, membrane thickness, drug concentration, temperature, and plasticizers, on drug release were studied. The release rate of drug from the EVA matrix increased with PEG 400 volume fraction, increased temperature and drug loading doses. An increased vinyl acetate comonomer content in EVA membrane increased the drug release rate and permeability coefficient. Among the plasticizers used such as alkyl citrates and phthalates, tetra ethyl citrate showed the best enhancing effects showing the enhancement factor of 1.88. The release of triprolidine from the EVA matrix follows a diffusion controlled model, where the quantity released per unit area is proportional to the square root of time. The controlled release of triprolidine could be achieved using the EVA polymer including the plasticizer.

Administration, Cutaneous↗
PubMedDate not supplied

Application of HPLC-thermospray ionization mass spectrometry for the analysis of triprolidine and its metabolite hydroxymethyltriprolidine in biological samples.

High-performance liquid chromatography coupled to positive ion mode thermospray ionization mass spectrometry has been used to characterize triprolidine and its known metabolite hydroxymethyltriprolidine. The method allows direct analysis of these compounds in complex biological matrices. Analysis of an extract from a microbial biotransformation experiment with triprolidine was performed and the results included two baseline-resolved chromatographic peaks. The [M + H]+ ion obtained from the mass spectrum of the first peak was consistent with that of hydroxymethyltriprolidine, and the mass spectrum of the second peak corresponded to triprolidine. Under the described conditions, the minimum detectable level of triprolidine without filament enhancement was estimated at about 10 micrograms injected on column.

Chromatography, High Pressure Liquid↗
PubMed1984

Pseudoephedrine and triprolidine in plasma and breast milk of nursing mothers.

Plasma and milk concentrations of pseudoephedrine and triprolidine were determined (by radioimmunoassay) in three lactating mothers over 12-48 h after ingestion of a combination medication containing 60 mg of pseudoephedrine hydrochloride and 2.5 mg of triprolidine hydrochloride monohydrate. Pseudoephedrine concentrations in milk were consistently higher than those in plasma. The total amount of drug in milk, as judged by areas under the respective curves (AUC), was two to three times greater than in plasma. Triprolidine concentrations in milk and plasma were more variable between subjects than those of pseudoephedrine. AUC values for milk and plasma were similar for one subject, while the plasma value exceeded that for milk in another woman. The fraction of the dose excreted in milk was estimated to be 0.4-0.7% for pseudoephedrine and 0.06-0.2% for triprolidine.

Adult↗
PubMed1993

Acute and subchronic effects of the H1-histamine receptor antagonist ebastine in 10, 20 and 30 mg dose, and triprolidine 10 mg on car driving performance.

1. The effects of a new antihistamine, ebastine (10, 20 and 30 mg), on several parameters of driving performance in actual traffic were studied in 15 healthy male volunteers. Subjects were treated for 5 days, and their driving performance tested on day 1 and day 5. The study was double-blind, placebo controlled and included the antihistamine triprolidine (10 mg sustained release) as an active drug control. 2. General tolerability was good except in one case following the reference compound triprolidine. No significant changes in driving performance were found with the new antihistamine ebastine at any dosage, on day 1 or day 5. Triprolidine (10 mg) significantly increased both the amount of weaving and the delay in following speed manoeuvres of a leading car, compared with placebo. 3. The results suggest that ebastine in doses up to 30 mg may be relatively safe for use by those who drive motor vehicles while under medication. The results do not warrant such a conclusion for triprolidine 10 mg.

Adult↗
PubMed1995

Chronic study of triprolidine for oncogenicity in mice.

Triprolidine hydrochloride was fed to groups of 60 B6C3F1 mice per sex at dietary levels of 0, 500, 2000, or 4000 ppm (as the free base) for up to 2 years. Up to 12 mice of each sex and dose group were terminated after 65 weeks for hematology and clinical chemistry. The control and high-dose groups were examined histologically. A complete histopathological examination was performed on the remaining 48 mice from each dose group when removed from study due to moribund condition, early death, or terminal euthanization at 105 weeks. Triprolidine did not significantly alter the survival of either sex. High-dose male and mid- and high-dose female body weights were significantly less than controls at the end of the study. Significant trends toward lower frequency with increasing dose were noted in females for fatty change in the liver and lymphomas (combination of lymphocytic, mixed, and histiocytic lymphomas). Similar negative trends in males were for lymphocytic cellular infiltration in multiple organs and lung alveolar/bronchiolar adenomas or the combination of alveolar/bronchiolar adenomas or carcinomas. Significant trends toward increased frequency with increasing dose were found in female mice for lymphocytic infiltration in multiple organs and cytoplasmic alterations of the acinar cells of the parotid gland. Similar positive trends were found in males for cytoplasmic alterations of the parotid gland and various hepatocellular changes (e.g., hypertrophy and altered foci). While there was a positive dose response trend for hepatocellular adenomas in males the combination of these and hepatocellular carcinomas eliminated the significant trend, and it was concluded that there was no evidence of a carcinogenic response to triprolidine in B6C3F1 mice.(ABSTRACT TRUNCATED AT 250 WORDS)

Animals↗
PubMed1982

The effect of orally administered triprolidine and pseudoephedrine singly and combined on histamine-induced skin reactions.

The effect of a single oral dose of triprolidine and pseudoephedrine, singly and combined, on histamine-induced wheal and flare reactions, was assessed in a fully randomised, placebo-controlled, double-blind crossover study. Triprolidine alone and the combination had a significantly greater effect of (p less than 0.05) in reducing skin reactions than pseudoephedrine alone or placebo, but there was no significant difference between triprolidine ane the combination (p less than 0.05).

Double-Blind Method↗
PubMed1996

Blocking effects of promethazine, triprolidine and their analogues on the excitation caused by the peptide, achatin-I.

An Achatina endogenous tetrapeptide, achatin-I (Gly-D-Phe-Ala-Asp), applied by brief pressure, produced an inward current (Iin) on an Achatina giant neurone type, PON (periodically oscillating neurone). Promethazine, triprolidine and their analogues tested, applied by perfusion, showed a tendency to inhibit the Iin, suggesting that the effective structures vary to a wide extent. With respect to promethazine and its analogues, the presence of 2-bromo, 5-oxo, 3-dimethylsulfamido and 2-methoxy weakened the effects. 10-(2-methylamino-2-methylethyl) instead of 10-(2-dimethylamino-2-methylethyl) of promethazine and the azepine ring instead of phenothiazine ring potentiated the effects. From the dose (pressure duration)-response study of achatin-I, the two promethazine analogues, RP 6497 and RP 6549 (the structures are shown in Fig. 1), inhibited the Iin in partly competitive and partly noncompetitive manners. Regarding triprolidine and its analogues, the compounds in Z-configuration seemed to be more effective than those in E-configuration. The presence of 4-methyl in 1-phenyl, and 1-(4-pyridyl) instead of 1-(2-pyridyl) potentiated the effects. 3-Dimethylamino instead of 3-pyrrolidino weakened the effects. The two triprolidine analogues, Trip Der 3 and Trip Der 6 (the structures in Fig. 2), inhibited the Iin in an uncompetitive manner.

Animals↗
PubMed1984

Comparison of pseudoephedrine and triprolidine, alone and in combination in preventing nasal congestion in subjects with allergic rhinitis using nasal histamine challenge.

The abilities of triprolidine 2.5 mg and pseudoephedrine 60 mg, alone and in combination, to protect against an increase in nasal airway resistance (NAR) after histamine challenge were determined in eighteen individuals with grass pollen allergy. The study was conducted outside the pollen season using a double-blind, placebo controlled crossover design. The prior administration of pseudoephedrine 60 mg and triprolidine 2.5 mg alone or in combination was superior to placebo in reducing the increase in NAR after challenge with 1.0% histamine. However, such NAR measurements did not differentiate between pseudoephedrine 60 mg and triprolidine 2.5 mg administered alone or in combination. Challenge with 0.1% histamine failed to discriminate between any of the test medications.

Adult↗
PubMed1992

Analogues of triprolidine: structural influences upon antihistamine activity.

The synthesis of some geometrical isomers related to triprolidine is reported. Previous configurational assignments, by UV and proton NMR, are validated by high field nuclear Overhauser enhancement methods and the isomeric purity of tested E- and Z-isomers was greater than 99.5% as assessed by an HPLC method developed for these compounds. Affinity constants for triprolidine (E and Z) in guinea-pig ileum showed a potency ratio of approximately 600 whereas at cerebellar sites this ratio was only approximately 100, suggesting that the H1 receptor in these two tissues may not be identical. In-vivo tests using a lethal dose of compound 48/80 (a potent histamine-releasing agent) demonstrated that triprolidine itself was the most active compound to protect the animal among all the isomeric compounds tested: in all isomeric pairs the E-configuration possessed superior activity over Z. The disposition of the aryl groups in these geometrically constrained compounds mimics that seen in the structurally related chiral pheniramines which are sp3 hybridized and whose absolute stereochemistry is known.

Animals↗
PubMed1979

Two doses of triprolidine for treatment of allergic rhinitis.

Two doses of triprolidine (2.5 mg t.i.d. and 1.25 mg t.i.d.) were compared with placebo in 32 patients suffering from allergic rhinitis. Triprolidine 2.5 mg t.i.d. was statistically significantly better than placebo (p less than 0.05) in reducing the symptoms of sneezing and eye irritation. Neither dose of triprolidine produced significant drowsiness during the second week of treatment.

Adolescent↗
PubMed1994

High-performance liquid chromatographic assay for the determination of paracetamol, pseudoephedrine hydrochloride and triprolidine hydrochloride.

The different UV absorption characteristics of paracetamol, pseudoephedrine hydrochloride and triprolidine hydrochloride have been used to facilitate their determination in pharmaceutical preparations by HPLC. The method developed involves isocratic, reversed-phase chromatography. A 'wavelength switching' programme is preferred to the use of a compromise wavelength for all three compounds. This gives reasonable UV responses despite widely different UV characteristics and concentrations of drugs. The limits of quantitation are found to be within 200-700 micrograms ml-1 for paracetamol, 24-84 micrograms ml-1 for pseudoephedrine HCl and 1.0-4.0 micrograms ml-1 for triprolidine HCl. The method performs well in terms of precision and accuracy as indicated by linear regression analysis.

Acetaminophen↗
PubMed1984

Trace analysis of the antihistamines methapyrilene hydrochloride, pyrilamine maleate and triprolidine hydrochloride monohydrate in animal feed, human urine and wastewater by high-performance liquid chromatography and gas chromatography with nitrogen-phosphorus detection.

Toxicological evaluation of the antihistamines methapyrilene hydrochloride, pyrilamine maleate, and triprolidine hydrochloride monohydrate using methapyrilene hydrochloride as the positive indicator was investigated as part of a structure-activity relationship study in rats and mice. Prerequisites for the toxicological tests were the development of analytical procedures to certify the dose, homogeneity and stability of the drugs in animal feed and to monitor human urine for possible exposure and to ensure removal of the test agents from wastewater prior to its discharge into the environment. A high-performance liquid chromatographic (HPLC) system was developed using a fluorescence detector for the determination of methapyrilene hydrochloride and pyrilamine maleate in feed at levels as low as 100 ng/g and in human urine as low as 1 ng/g. An HPLC-UV procedure was developed for the determination of triprolidine hydrochloride monohydrate in feed at levels as low as 10 micrograms/g. Data concerning p-values, extraction efficiencies from feed and stability experiments in feed are presented for these antihistamines. A gas chromatographic procedure using a nitrogen-phosphorus detector was also developed for determining the three antihistamines in admixture in wastewater at levels as low as 10 ng/g.

Animal Feed↗
PubMed1979

Effect of the antihistamines, brompheniramine maleate and triprolidine hydrochloride, on performance in man.

1 Effects of brompheniramine maleate (4 and 12 mg) and triprolidine hydrochloride (2.5 and 10 mg) on visuo-motor coordination, and on subjective assessments of performance, well-being and sleep were each studied in six subjects at 0.5, 1.5, 3.0, 5.0 and 7.0 h after ingestion. The doses refer to immediate and sustained release preparations respectively. 2. Triprolidine hydrochloride (2.5 mg) had an immediate effect on performance which persisted to 3.0 h, and the sustained release preparation (10 mg) impaired performance from 1.5 to 5.0 h. Brompheniramine maleate (4 mg) impaired performance from 1.5 to 3.0 h, and the sustained release preparation (12 mg) impaired performance at 1.5 h. There were no consistent changes in the subjective assessments of performance, or of well-being and sleep. 3. The studies emphasize the variable effects of antihistamines on performance, and suggest that effects on performance of sustained release preparations may be similar to those of the usual form. Sustained release preparations may provide an advantage in clinical practice if the antihistaminic activity is prolonged.

Adult↗
PubMed1980

Effects of pseudoephedrine and triprolidine, alone and in combination, on symptoms of the common cold.

A total of 466 healthy adults from four different regions of England entered a double-blind, randomised trial to test the effectiveness of an antihistamine (triprolidine) and a decongestant (pseudoephedrine), alone or in combination, in relieving symptoms of the common cold. During the study 199 subjects reported a total of 243 colds. Subjects recorded the severity of 12 symptoms during treatment and noted separately the severity of a further seven symptoms that represented unwanted effects of treatment or served as an index of suggestibility. They were then asked about their overall improvement in symptoms during treatment and whether they thought they had taken placebo. Sneezing, nasal obstruction, and overall response to treatment were significantly improved (p <0.01) with psuedoephedrine or pseudoephedrine and triprolidine compared with placebo.

Clinical Trials as Topic↗