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At least 73 records · Page 4Linked to original sources

Increased brain uptake of morphine in the presence of the antihistamine tripelennamine.

Disposition of [6 3H (N)]morphine in plasma, brain and liver of rats was studied 15 min after intravenous injection of either a 2 mg kg-1 dose of morphine or a combination of the same dose of morphine with a 6 mg kg-1 dose of tripelennamine. The concentrations of morphine in brain and the brain to plasma morphine ratios in animals receiving the combination of drugs concurrently were significantly higher than those in the control morphine group. No significant differences were seen in the morphine or morphine metabolite concentrations in plasma and liver or liver to plasma morphine concentration ratios in the 2 groups. Data suggest that pharmacokinetic factors play a role in the potentiation of opiate effects by antihistamine on concurrent i.v. administration of the two drugs.

Animals↗

H1-receptor antagonist, tripelennamine, does not affect arterial hypoxemia in exercising Thoroughbreds.

It has been suggested that pulmonary injury and inflammation-induced histamine release from airway mast cells may contribute to exercise-induced arterial hypoxemia (EIAH). Because stress failure of pulmonary capillaries and EIAH are routinely observed in exercising horses, we examined whether preexercise administration of an H1-receptor antagonist may mitigate EIAH. Two sets of experiments, placebo (saline) and antihistaminic (tripelennamine HCl at 1.10 mg/kg iv, 15 min preexercise) studies, were carried out on seven healthy, exercise-trained Thoroughbred horses in random order 7 days apart. Arterial and mixed venous blood-gas and pH measurements were made at rest before and after saline or drug administration and during incremental exercise leading to maximal exertion at 14 m/s on 3.5% uphill grade for 120 s. Galloping at this workload elicited maximal heart rate and induced exercise-induced pulmonary hemorrhage in all horses in both treatments, thereby indicating that capillary stress failure-related pulmonary injury had occurred. In both treatments, EIAH, desaturation of hemoglobin, hypercapnia, and acidosis of a similar magnitude developed during maximal exertion, and statistically significant differences between the placebo and antihistaminic studies could not be demonstrated. The failure of the H1-receptor antagonist to modify EIAH significantly suggests that pulmonary injury-induced histamine release may not play a major role in bringing about EIAH in Thoroughbred horses.

Animals↗

Pentazocine and tripelennamine ('T's and blue's'): effects on the fetus and neonate.

Three groups of women enrolled in a comprehensive perinatal addiction program were studied. Group I (n = 13) were addicted to pentazocine and tripelennamine (T's and blue's), group II were low-dose methadone-maintained women (n = 46) and group III women were drug-free controls (n = 27). No differences were seen in maternal age, gravidity, obstetrical complications, gestational age or neonatal Apgar scores. Significant differences were observed between drug-exposed and drug-free neonates in birth weight, length and head circumference. An evaluation of neonatal behavior using the Brazelton Neonatal Behavioral Assessment Scale revealed that infants of mothers who used T's and blue's throughout pregnancy demonstrated interactive deficits and withdrawal similar to methadone-addicted newborns.

Adult↗

Acute myocardial infarction associated with intravenous injection of pentazocine and tripelennamine.

This case report describes the evolution of an acute anteroseptal myocardial infarction in a 27-year-old man following intravenous injection of pentazocine and tripelennamine. Subsequent coronary angiography showed normal coronary arteries. Based on the known mechanism of action of these drugs, it is postulated that myocardial infarction resulted from coronary artery spasm secondary to excessive catecholamine stimulation.

Adult↗

Blocking effect of tripelennamine on histamine--induced positive chronotropic and inotropic responses of the dog atrium.

The effects of histamine on inotropic and chronotropic activity were investigated in isolated canine atrium preparations which were suspended in a bath and perfused with arterial blood from a carotid artery of heparinized support dog. Histamine administered into the cannulated sinus node artery in a dose range of 0.3-100 mug produced dose-related positive chronotropic and inotropic effects. The positive responses to histamine were not suppressed by treatment with propranolol in doses which blocked responses to norepinephrine, but these were significantly suppressed by a histamine H1 receptor blocking agent, tripelennamine. On the other hand, these histamine-induced effects were not modified by a histamine H2 receptor blocking agent, burimamide. From these results, it is assumed that positive chronotropic and inotropic effect of histamine may be mediated by histamine H1 receptors in the dog heart.

Animals↗

Fungal transformations of antihistamines: metabolism of methapyrilene, thenyldiamine and tripelennamine to N-oxide and N-demethylated derivatives.

1. Strains of the fungus Cunninghamella elegans ATCC 9245 and 36112 were tested for their ability to transform the antihistamines methapyrilene (I), thenyldiamine (II) and tripelennamine (III). 2. Antihistamine metabolites were isolated by h.p.l.c., and identified by their 1H-n.m.r. and mass spectral properties. 3. All three drugs were transformed by both C. elegans strains to N-oxidized and N-demethylated derivatives. Metabolism during 96 h of incubation amounted to 85% for (I), 64% for (II), and 83% for (III). Metabolites soluble in organic solvents amounted to 62% to 86% of the total metabolism; approximately 88% to 95% of the organic-soluble metabolites were N-oxide derivatives of each antihistamine.

Aminopyridines↗

Pentazocine (Talwin) and tripelennamine (Pyribenzamine): a new drug abuse combination or just a revival?

Interviews were conducted with eight drug abusers at the Cook County Hospital Emergency Department who had used pentazocine (Talwin) and tripelennamine (Pyribenzamine) in combination--also known as "T's and Blues." It was discovered that all those interviewed had been introduced to this combination in Chicago and that nearly all had been users of heroin. Economics seemed to be a major factor contributing to the preference of "T's and Blues" over heroin. A review of the literature showed that there is a striking similarity between "T's and Blues" and "Blue Velvet" which was popular almost 20 years ago.

Adult↗

Abuse of pentazocine combined with tripelennamine: an interaction of pharmacological and demographic characteristics.

Abuse of pentazocine (Talwin) and tripelennamine (Pyrabenzamine) (P and T) was studied in a group (N = 16) of inpatients. They were queried about subjective effects and their drug preferences. P and T use was associated with more anxiety than was the opiate or drug-free state. P and T use did not produce euphoria, and users preferred this drug next to last among other abused drugs. P and T use was further studied in outpatients (N = 628) using Client Oriented Data Acquisition Process information. These patients were younger and more often male, Black, and single or separated when compared with opiate users. They began using the drug later and had many fewer years invested in its use.

Adult↗

Abuse and pulmonary complications of injecting pentazocine and tripelennamine tablets.

A current practice among drug abusers in certain Midwestern and Eastern cities is the intravenous injection of aqueous mixtures prepared from tablets of pentazocine and tripelennamine. Patients present with acute hypoxic episodes and symptoms suggesting physical dependence to pentazocine. Two cases are presented illustrating acute respiratory distress with hypoxia. Available evidence indicates that the respiratory syndrome is produced by talc from the injected tablets. Respiratory support and short-term oxygen therapy have been effective in managing this syndrome. Approaches to the treatment of pentazocine dependence and the role of the antihistamine in potentiating the narcotic activity are also discussed. Physicians, drug abuse counselors, and others should be aware of the abuse potential and pulmonary damage which can result from the intravenous use of this drug combination.

Adult↗

Potentiation of lethality in mice by combinations of pentazocine and tripelennamine.

Quantal dose-response curves were generated to determine the median lethal doses (LD50S) for pentazocine and tripelennamine, either alone or in combination. LD50S of the drug combinations in mice demonstrated significant potentiation when compared with either drug administered alone. Attempts to antagonize the lethality of such combinations have, to date, been unsuccessful.

Animals↗

Toxicological and pathological findings in fatalities involving pentazocine and tripelennamine.

Toxicological and pathological findings are described in fatalities involving pentazocine (Talwin) and tripelennamine (Pyribenzamine). Procedures using thin-layer chromatography, gas chromatography, ultraviolet spectrophotometry, and spectrophotofluorometry are described, as well as the quantitative analysis of biological specimens of drug abuse and homicide victims. Microscopic findings in lung specimens from drug abuse deaths are also described.

Chromatography, Gas↗