Disease relevance of Tripelennamine hydrochloride

• Two drug addicts who practiced subcutaneous injection of crushed tripelennamine and pentazocine tablets, a practice known as "skin-popping," developed nephrotic syndrome and demonstrated amyloidosis on renal biopsy [1].
• In recent years, venous access (usually illicit) has been the major predisposing factor to this infection and abuse of pentazocine and tripelennamine has been particularly associated with endocarditis due to this organism [2].
• Selective survival in pentazocine and tripelennamine of Pseudomonas aeruginosa serotype O11 from drug addicts [3].
• 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 [3].
• The intravenous (IV) use of pentazocine (Talwin) and tripelennamine (pyribenzamine) has become a major form of drug abuse seen in the midwestern United States. Complications of this abuse have included psychotic reactions, acute pulmonary insufficiency, convulsions, and various infections [4].

Psychiatry related information on Tripelennamine hydrochloride

• 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 [5].
• The opioid agonist-antagonist pentazocine (1-30 mg/kg) and the partial agonist buprenorphine (0.05-0.25 mg/kg) were tested, alone or in combination with the histamine H1-receptor antagonist tripelennamine (1, 2.5, 5 or 10 mg/kg), on locomotor activity in mice of the CD-1 strain [6].
• When antihistaminics were administered chronically (during the 4 days of morphine addiction), tripelennamine, cyclizine and ranitidine (all at 10 mg/kg) inhibited shaking behavior [7].
• Opiate dependence alters central reward of nalbuphine or pentazocine plus tripelennamine [8].
• Prolonged hallucinations following a modest overdose of tripelennamine [9].

High impact information on Tripelennamine hydrochloride

• The pharmacokinetics of pentazocine and tripelennamine [10].
• The histamine H1 receptor antagonists diphenhydramine and tripelennamine accelerated the recovery [11].
• Outbreak of endocarditis caused by Pseudomonas aeruginosa serotype O11 among pentazocine and tripelennamine abusers in Chicago [12].
• Pentazocine, pentazocine hydrate, and tripelennamine can be detected by thin-layer chromatography of chloroform/isopropanol extracts of heat- and acid-hydrolyzed urine [13].
• The GMBF was assessed during an intravenous infusion of histamine in the presence of tripelennamine [14].

Chemical compound and disease context of Tripelennamine hydrochloride

• The place preferences by some histamine H1 antagonists, such as tripelennamine, optical isomers of chlorpheniramine (dl-, d- and l-forms) and pyrilamine, in rats were evaluated with the conditioned place preference paradigm [15].
• Fatal intracranial hemorrhage associated with phenylpropanolamine, pentazocine, and tripelennamine overdose [16].

Biological context of Tripelennamine hydrochloride

• Tripelennamine was found to be extensively metabolized by N-demethylation and aromatic hydroxylation pathways [17].
• In contrast, intracranial stimulation of the trigeminal nerve root induced increases in both PBF and LBF which were reduced by pre-treatment with tripelennamine, indicating antidromic vasodilatation via the trigeminal sensory nerve [18].
• Metabolism, tissue distribution and covalent binding of tripelennamine and its N-nitroso derivative in the rat [17].
• These findings, which agree with the previously observed capability of tripelennamine to induce DNA repair and fragmentation in rat hepatocytes, strengthen the suspicion of a potential genotoxic risk of this drug to humans [19].
• The total peripheral resistance was considerably lowered by ETX, but this decrease was significantly attenuated in the TPA or RAN-treated groups [20].

Anatomical context of Tripelennamine hydrochloride

• DNA-damaging activity of tripelennamine in primary cultures of human hepatocytes [19].
• Atropine (5 mg/kg), chlorisondamine (2 mg/kg), imipramine (10 mg/kg) and tripelennamine (5 mg/kg), administered i.p., failed to inhibit the histamine-induced, or the spontaneous, gastric acid secretion [21].
• In contrast, pretreatment with tripelennamine attenuated the trigeminal nerve-stimulated blood flow increase, but not that elicited by stimulation of the facial and glossopharyngeal nerves [22].
• The kinetics of quaternary ammonium glucuronidation of cyproheptadine, tripelennamine, amitriptyline, and doxepin in intact human liver microsomes was determined [23].
• In the guinea-pig ileum 10 microg tripelennamine did not reduce the contraction significantly [24].

Associations of Tripelennamine hydrochloride with other chemical compounds

• We previously demonstrated that combination of opioids, pentazocine and dihydrocodeine, with the histamine H1-receptor antagonists tripelennamine and chlorpheniramine could enhance their rewarding effects in rats [25].
• Thus, in addition to N- and O-demethylation, hydroxylation, and glucuronidation, N-debenzylation, N-depyridination and N-dedimethylaminoethylation were shown to be novel pathways for metabolism of tripelennamine and pyrilamine [26].
• Classic antihistamines, namely diphenhydramine, chlorpheniramine, clemastine, perphenazine, hydroxyzine, and tripelennamine, share structural features with substrates and inhibitors of the polymorphic cytochrome P450 (CYP) isozyme CYP2D6 [27].
• These data verify the genotoxicity of pyrilamine and tripelennamine and the failure of methapyrilene to elicit DNA repair, and suggest that doxylamine and thenyldiamine may be weak DNA-damaging agents [28].
• Pretreatment with a dose of more than 20 mg/kg of histamine H1-receptor antagonists such as tripelennamine or diphenhydramine prior to the injection of compound 48/80 (3.0 mg/kg s.c.) attenuated or abolished the effects of compound 48/80 on PRA, hematocrit and plasma extravasation [29].

Gene context of Tripelennamine hydrochloride

• Ranitidine, another H2 receptor antagonist also prevented the histamine-induced cyclic AMP elevation, but the H1 receptor antagonists mepyramine and tripelennamine had no significant effect [30].
• 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 [3].
• Moreover, tripelennamine alone increased renin secretion [31].
• The experiment was performed in the presence of tripelennamine, an H1 antagonist, to focus on the relationship between acid secretion (H2-receptor-mediated response) and GMBF [32].
• Following the secretory event, which is inhibited by the H1 anti-histamine tripelenamine, plasma prolactin level drops below the basal line [33].

Analytical, diagnostic and therapeutic context of Tripelennamine hydrochloride

• Doses of tripelennamine and diphenhydramine that increased rates of nonsuppressed and suppressed responding also maintained self-administration in cocaine-trained squirrel monkeys under a second-order schedule of i.v. injection [34].
• Acute myocardial infarction associated with intravenous injection of pentazocine and tripelennamine [35].
• Determination of pentazocine and tripelennamine in blood of T's and Blue addicts by gas-liquid chromatography with a nitrogen detector [36].
• Effects of pentazocine and tripelennamine on analgesia [37].
• A time control group of experiments, in which no drugs were infused, as well as groups receiving adrenaline plus either tripelennamine or cimetidine, were also performed [38].

References