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PubMed1983

Pharmacological studies on supersensitization. XII. Inhibitory effect of reserpine on tripelennamine-, N,N-dimethyl-N',N'-dibenzylethylenediamine- and N,N-dibenzyl-N',N'-dimethyl-1,2-propanediamine-induced supersensitivity of isolated vas deferens of guinea pig to acetylcholine.

Effects of tripelennamine, N,N-dimethyl-N',N'-dibenzylethylenediamine (DBED) and N,N-dibenzyl-N',N'-dimethyl-1,2-propanediamine (DBPD) on the isotonic contractions of isolated vas deferens of intact and reserpinized guinea pigs to acetylcholine were examined. Increase in sensitivity to acetylcholine induced by tripelennamine, DBED and DBPD was attenuated remarkably by reserpine. Tripelennamine- and DBED-induced increases in Ca2+-contractions were not affected by reserpine. Acetylcholine-contractions in Ca2+-free Tyrode solution were inhibited by reserpine, but K+-contractions in Ca2+-free Tyrode solution were not affected by reserpine. Tripelennamine- and DBED-induced increases in acetylcholine- and K+-contractions in Ca2+-free Tyrode solution were attenuated or abolished by reserpine. DBPD decreased cholinesterase activity of vas deferens of guinea pig, but DBED did not. These results suggest that, although the Ca2+-storage site utilized for acetylcholine-contraction is different from that for K+-contraction, tripelennamine- and DBED-induced increase in Ca2+-release from superficial Ca2+-binding sites induced by acetylcholine and K+ is inhibited by reserpine. It is also estimated that DBPD-induced supersensitivity to acetylcholine might be due to the inhibition of cholinesterase activity. However, the mechanism of inhibition of DBPD-induced supersensitivity by reserpine remained obscure.

Acetylcholine↗

PubMed1984

Pentazocine-tripelennamine ("T's and Blues") substitution studies in morphine-dependent rodents.

Tripelennamine, pentazocine and various pentazocine-tripelennamine combinations were tested for their ability to substitute for morphine in morphine-dependent rodents. Rats and mice were rendered physically dependent on morphine by the Drug-Admixed Food Method. Pentazocine produced a dose-related partial suppression of morphine withdrawal signs in mice, as well as in both mildly and severely dependent rats. Tripelennamine did not suppress morphine withdrawal signs, but rather aggravated them. Furthermore, tripelennamine did not potentiate the ability of pentazocine to suppress morphine withdrawal signs. It is concluded that the primary reason for the reported "street" abuse of the tripelennamine-pentazocine combinations is not related to any remarkable ability of the combination to effectively suppress the discomfort of heroin withdrawal.

Animals↗

PubMed1991

Metabolic profile of tripelennamine in humans.

Volunteers were injected im with 100 mg of tripelennamine (pyribenzamine).HCl dissolved in saline. Timed urine was collected. Tripelennamine and its metabolites were identified by GC/MS. Amounts of free tripelennamine excreted in the 0-2-, 2-4-, 4-8-, 8-12-, and 12-24-h urine samples were found to be 0.30, 0.56, 0.17, 0.21, and 0.0%, respectively, of the administered dose. In the same time periods, total tripelennamine (free plus conjugated) amounts were found to be 0.92, 1.20, 0.96, 1.30, and 1.31%, respectively, and total amounts 2-[alpha-hydroxybenzyl(2-dimethylaminoethyl)amino]pyridine(alpha- hydroxytripelennamine) plus an unidentified metabolite were found to be 0.16, 3.35, 3.06, 7.46, and 8.85% of the dose, respectively.

Chromatography, Thin Layer↗

PubMed1983

Lethality of pentazocine and tripelennamine combinations in mice housed individually and in groups.

Lethality of 80 mg/kg pentazocine alone; 40 mg/kg tripelennamine alone; 20 mg/kg tripelennamine in combination with 40, 60, and 80 mg/kg pentazocine; and 40 mg/kg tripelennamine in combination with 10, 20, and 40 mg/kg pentazocine was determined in mice housed individually and in groups. Results indicate that the lethality of pentazocine and tripelennamine combinations in mice is (1) dose-dependent, (2) potentiated relative to either drug alone, and (3) greater in group-housed than in individually-housed animals.

Animals↗

PubMed1983

Effects of pentazocine and tripelennamine on analgesia.

The analgesic effects of pentazocine and tripelennamine, alone and in combination, were assessed in rats with a hot plate apparatus. In Experiment 1, the combination of tripelennamine with chronic pentazocine produced analgesia at doses which were not analgesic when the drugs were given alone. This combination also reestablished analgesia in subjects made tolerant to pentazocine's effects. In Experiment 2, development of tolerance to the analgesic effects of pentazocine was delayed by addition of tripelennamine. These data may contribute to a rationale for the current popularity of combined pentazocine and tripelennamine abuse.

Animals↗

PubMed1996

Construction and evaluation of PVC conventional and tubular tripelennamine-selective electrodes: their application in pharmaceutical preparations.

The construction and evaluation of tripelennamine conventionally-shaped ion-selective electrodes and tubular detectors for the determination of this compound in pharmaceutical formulations are described. Electrodes with conventional configuration have been constructed without an internal reference solution, using several types of immobilized ionic sensors in PVC. The different electrode membranes were prepared by using tripelennamine tetraphenylborate as ionic-exchanger, dissolved in 2-nitrophenyl octyl ether (type A), dibutylphthalate (type B) and bis-(2-ethylhexyl)sebacate (type C) as plasticizer solvents. The general working characteristics of the different types of conventional electrodes were evaluated in tripelennamine solutions, with adjusted ionic strength, showing a linear response in the concentration range of about 4 x 10(-5) - 1 x 10(-1) M and a slope near the theoretical value. The electrodes presented a fast response (> 20 s) and a high reproducibility (> or = 0.2 mV per day). The electrode selectivity in the presence of some interferents, such as sodium, potassium, lithium, ammonium, chlorpheniramine, diphenydramine, promethazine, meclizine and pentazocine, was good, particularly for those whose sensor membrane was prepared with tripelennamine tetraphenylborate dissolved in 2-nitrophenyl octyl ether (type A). Tubular detectors were also prepared using the same sensor membrane and were evaluated in a low-dispersion flow-injection manifold. Under these conditions the detectors presented response characteristics similar to those of the corresponding conventionally-shaped electrodes. The analysis of different pharmaceutical forms (creams, syrups and gels) gave good results with mean recoveries of 99.8-100.6% when the experiments were conducted by direct potentiometry and 99.9-100.4% where the same determinations were conducted by flow-injection analysis with tubular detectors.

Chemistry, Pharmaceutical↗

PubMed1985

Selective survival in pentazocine and tripelennamine of Pseudomonas aeruginosa serotype O11 from drug addicts.

The growth of Pseudomonas aeruginosa, particularly serotype O11, in pentazocine and tripelennamine ("T's and Blues") was evaluated as a possible explanation for the association of deep-seated infection with this organism and abuse of these drugs. The mean reduction of growth caused by the drugs was 1,000-fold greater for 49 Pseudomonas strains from normal subjects than for 32 strains from drug addicts (4.2 vs. 1.3 logs of reduction at 2 hr, P less than .0005). A common phenotypic subset of the serotype O11 strains from drug addicts was especially resistant to the inhibitory effects. Twelve strains of Staphylococcus aureus (a frequent cause of infection in heroin, but not in pentazocine and tripelennamine, addicts) were completely inhibited by the drug combination. Dose-response curves (derived from the results of using the tablets as well as pure powders) showed that tripelennamine was responsible for the inhibitory activity, which was partially antagonized by pentazocine. We conclude that an ability of some P. aeruginosa serotype O11 strains, but not S. aureus, to survive in pentazocine and tripelennamine may explain in part a shift from S. aureus to P. aeruginosa as common pathogens of drug addicts in areas where abuse of this combination of drugs has increased.

Drug Interactions↗

PubMed1975

Metabolism, tissue distribution and covalent binding of tripelennamine and its N-nitroso derivative in the rat.

Benzyl-14C-labeled tripelennamine and its N-nitroso derivative (NDT) were administered (20 mg/kg; 50 muc/kg i.p.) separately to control and phenobarbital-pretreated rats. Tissue distribution and covalent binding of the two compounds in liver, lung, kidney, fat and muscle tissues, as well as in the plasma, were determined at 4 and 24 hours after the administration. No specific localization of the test compounds to any tissue or to the plasma was observed. The in vivo covalent binding of both the compounds to the proteins of the tissues and plasma was low; the highest binding occurred in the liver (approximately 25 pmol/mg of protein). Within 24 hours about 78% of the injected tripelennamine and its metabolites was excreted into the urine whereas only about 35% of the radioactivity of NDT was eliminated. Pretreatment with phenobarbital accelerated the elimination of both substances. The metabolites of the drug and NDT were isolated from urine, hydrolyzed by glucuronidase-sulfatase and identified as their trimethylsilyl derivatives by gas chromatography-mass spectrometry. Tripelennamine was found to be extensively metabolized by N-demethylation and aromatic hydroxylation pathways. By contrast most of the NDT was eliminated as NDT and hydroxylated metabolites; very little was excreted as N-demethylated metabolites. The hydroxylated metabolites identified were p-hydroxybenzyl, p-hydroxybenzyl-5-hydroxypyridyl and m,p-dihydroxybenzyl derivatives of the drug, its N-demethylated analog and NDT. The catechol formation with NDT was found to be 4 times that observed with tripelennamine.

Animals↗

PubMedDate not supplied

N-debenzylation of pyrilamine and tripelennamine in the rat. A new metabolic pathway.

Male Sprague-Dawley rats received 20 mg/kg of pyrilamine or tripelennamine intraperitoneally. The extract obtained from an enzymatically hydrolyzed urine was derivatized with or without Tri-Sil Z and analyzed by GC/MS. 2-(2-Dimethylaminoethyl)aminopyridine, 2-(4-hydroxybenzyl)aminopyridine, 2-[4-hydroxybenzyl-(2-dimethylaminoethyl)amino]pyridine, 2-[4-hydroxybenzyl-(2-methylaminoethyl)amino]pyridine, 2-[4-hydroxy-3-methoxybenzyl-(2-dimethylaminoethyl)amino]pyridine, and 2-[3-hydroxy-4-methoxybenzyl-(2-dimethylaminoethyl)amino]pyridine were detected as metabolites of pyrilamine. 2-(2-Dimethylaminoethyl)aminopyridine, 2-(alpha-hydroxybenzyl)aminopyridine, 2-[alpha-hydroxybenzyl-(2-dimethylaminoethyl)amino]pyridine, 2-[4-hydroxybenzyl-(2-dimethylaminoethyl)amino]pyridine, 2-[4-hydroxy-3-methoxybenzyl-(2-dimethylaminoethyl)amino]pyridine, and 2-[3-hydroxy-4-methoxybenzyl-(2-dimethylaminoethyl)amino]pyridine were detected as metabolites of tripelennamine. Thus, N-debenzylation of tripelennamine and N-demethoxybenzylation of pyrilamine occurs in vivo, through an intermediate of alpha-carbon oxidation and represents a new metabolic pathway for these compounds. The identity of the metabolite was confirmed by comparison with an authentic sample of 2-(2-dimethylaminoethyl)aminopyridine. The pharmacological implication of 2-(2-dimethylaminoethyl)aminopyridine, one of the metabolites of pyrilamine and tripelennamine, is discussed.

Aminopyridines↗

PubMed1983

Spontaneous live birth with a maternal history of intravenous use of pentazocine and tripelennamine (T's and blues).

A 24-year-old black female presented a live birth of six-months gestation. The 700-g neonate survived for 11 h. After toxicology revealed the presence of pentazocine and tripelennamine (T's and Blues), the mother admitted to using this combination intravenously 9 h previous to admission. Concentrations of pentazocine and tripelennamine were simultaneously determined by gas-liquid chromatography (GLC) combined with nitrogen selective detection. Analyses were performed on a 3% OV-101 column, with the added internal standard, dexbrompheniramine. Both pentazocine and tripelennamine were qualitatively confirmed by their electron impact mass spectra. Concentrations of pentazocine and tripelennamine in various fluids and tissues were determined.

Adult↗

PubMed1996

The discriminative stimulus effects of tripelennamine in humans.

Twenty volunteers were trained to discriminate between 75 mg tripelennamine (TP) and placebo. During the first four sessions, the drugs were identified prior to ingestion by letter code. During the next six sessions, the procedure was the same except the capsules were not identified. At the end of the 3-h session, participants indicated which capsule they believed they received using the letter codes. When correct, they received a monetary bonus. If they were correct on five sessions, they entered the third phase which had ten additional training and 12 test sessions. During tests, participants received capsules that contained other drugs, including diphenhydramine (50 and 75 mg), chlorpheniramine (4 and 6 mg), diazepam (5 and 10 mg), d-amphetamine (5 and 10 mg), as well as tripelennamine (25, 50 and 75 mg) and placebo. Thirteen participants learned the discrimination and nine entered the third phase. Except for placebo, most participants identified the test compounds as TP and labeled them as sedatives. TP produced significant changes on several subjective and physiological measures. The test compounds produced varied effects which were neither clearly dose-related nor related to the identification as TP or placebo. These results indicate that tripelennamine can function as a discriminative stimulus, but with little evidence of pharmacological specificity.

Adult↗

PubMed1984

Accelerated development of pulmonary complications due to illicit intravenous use of pentazocine and tripelennamine.

To gain information concerning the natural history and prevalence of pulmonary gas exchange abnormalities resulting from intravenous drug abuse, 45 intravenous drug users were studied. Twenty subjects used a mixture of the synthetic opiate pentazocine and the antihistamine tripelennamine, which, under the street name T's and B's, has become very popular in some urban areas as an available substitute for heroin. Compared with the 19 heroin addicts studied, the pentazocine and tripelennamine users had a significantly shorter mean duration of intravenous drug abuse (2.7 +/- 0.4 years versus 7.6 +/- 0.9 years, p less than 0.01), a greater frequency of respiratory symptoms (75 percent versus 36 percent, p less than 0.05), a significant reduction in the mean diffusing capacity of the lung for carbon monoxide (58.4 +/- 3.3 percent predicted versus 75.5 +/- 5.6 percent predicted, p less than 0.01), and abnormal responses to submaximal steady-state exercise testing. The intravenous use of pentazocine and tripelennamine and probably most other drug preparations intended for nonparenteral use represents a particularly noxious form of drug abuse that may lead to early respiratory complications in a large proportion of users.

Adult↗

PubMed1986

Effects of nalbuphine alone and in combination with tripelennamine on rewarding brain stimulation thresholds in the rat.

Reinforcing thresholds for rewarding brain stimulation to the medial forebrain bundle-lateral hypothalamus were determined in rats by means of a rate-free psychophysical method. Nalbuphine, a mixed agonist-antagonist opioid, alone caused a significant, but modest, dose-dependent lowering of the threshold for reinforcing stimulation. Concomitant administration of an ineffective dose of tripelennamine, an antihistamine, with nalbuphine potentiated the threshold lowering effect of nalbuphine. These results are similar to previous results obtained with tripelennamine and pentazocine suggesting that nalbuphine may have abuse potential if combined with tripelennamine.

Animals↗

PubMed1984

Effects of concomitant pentazocine and tripelennamine on brain-stimulation reward.

Reinforcing thresholds for self-stimulation behavior to the medial forebrain bundle were determined in rats by means of a rate-free psychophysical method. The acute administration of either pentazocine or tripelennamine caused a small but significant lowering of the reward threshold. Combined administration of an ineffective dose of tripelennamine with various doses of pentazocine resulted in a potentiation of this lowering effect. These results suggest that the widespread abuse of the combination of pentazocine and tripelennamine may be due to a pharmacologic potentiation rather than just a summation of their two effects.

Animals↗

PubMedDate not supplied

Pentazocine and tripelennamine (T's and Blues) abuse: toxicological findings in 39 cases.

The post mortem findings of pentazocine and tripelennamine ("T's and Blues") in abusers dying in the City of St. Louis between July 1, 1979 and July 30, 1981 are presented. Thirty-three deaths were homicides; 30 black males, ages 21-38; one white male, age 26, died from gunshot wounds; and two black females, age 18 and 32, died of stab wounds. Blood concentrations of pentazocine and tripelennamine in these cases ranged from 0.20 to 3.3 mg/L, (mean +/- SD 0.72 +/- 0.64 mg/L) and 0.02 to 1.8 mg/L (mean +/- SD 0.29 +/- 0.40 mg/L), respectively. The six deaths attributed to T's and Blues abuse involved three black males, ages 20, 28 and 49, and three black females, ages 21, 25, and 45 years. Blood concentrations of pentazocine and tripelennamine ranged from 0.44 to 2.5 mg/L and 0.09 to 4.1 mg/L, respectively. Ethanol and diazepam were also detected in 49% and 13% of all deaths, respectively. Foreign body or talc granulomas in lung were the most common pathological finding relevant to the abuse of T's and Blues.

Adolescent↗

PubMed1980

Pentazocine and tripelennamine: a drug abuse epidemic?

The change in illicit drug use from 1975 to 1978 was studied in Chicago veterans. Barbiturates and amphetamine use has decreased significantly. Nearly a sevenfold increase in pentazocine use has occurred. All but one of the pentazocine users added tripelennamine to the intravenous or subcutaneous injections. Sixty-four instances of medical or psychiatric complications including seizures, abscesses, depression, and psychosis occurred in the 69 pentazocine and tripelennamine users. A possible pharmacologic explanation of the seizures and psychiatric complications is advanced. Most users of pentazocine and tripelennamine started the use in an attempt to withdraw from heroin or because of the poor quality of heroin available.

Adolescent↗

PubMedDate not supplied

Behavioral and developmental effects of prenatal exposure to pentazocine and tripelennamine combinations.

Long-Evans, hooded rats were intubated with one of four dose combinations of pentazocine and tripelennamine on Days 7-20 of pregnancy: 0:0 (mg/kg pentazocine:tripelennamine), 20:10, 40:0, or 40:20. An additional group had free access to lab chow and water throughout pregnancy. At birth, reduced body weights were evident in all drug-treated offspring. Growth deficits were not noted at 5, 10, 15 or 20 days of age. Three measures of activity were collected at 18 days of age, however, none of these measures were differentially affected as a function of prenatal treatment. At 85 days of age, offspring were tested in a two-way shuttle avoidance paradigm. Although the number of avoidances was not significantly affected by prenatal treatment, offspring exposed to these drugs in combination had shorter response latencies than controls with increased training and made more intertrial crossing responses. Additional offspring were tested for seizure susceptibility at 100 days of age. None of the parameters of seizure activity were significantly affected by prenatal drug treatment. Prenatal exposure to pentazocine and tripelennamine resulted in prenatal growth deficits, increased activity during the intertrial interval and decreased response latencies in a shuttle avoidance learning task, suggesting that this polydrug combination may be associated with some long-term behavioral teratogenic risks.

Animals↗

PubMed1980

Medical and psychiatric complications of pentazocine and tripelennamine abuse.

The change in illicit drug use from 1973 to 1979 was studied in Chicago veterans. Barbiturate and amphetamine use has decreased significantly. Nearly a seven-fold increase in pentazocine use has occurred. All but one of the pentazocine users added tripelennamine to the intravenous or subcutaneous injections. Sixty-four instances of medical or psychiatric complications including seizures, abscesses, depression, and psychosis, occurred in the 69 pantazocine and tripelennamine users. A possible pharmacologic explanation of the seizures and psychiatric complications is advanced. Most users of pentazocine and tripelennamine started in an attempt to withdraw from heroin or because of the poor quality of heroin available.

Abscess↗