Tripelennamine toxicity

Tripelennamine as antihistamine, 1, 177 biological activity, 4, 911 toxicity, 4, 912 Tripelennamine, p-bromo-as antihistamine, 2, 520 a-Tripiperideine synthesis, 3, 510 Triprolidine... 

Toxicity. The estimated minimum lethal dose is 0.3 g, although recovery after ingestion of 1.2 g has been reported. Blood concentrations of 1 pg/ml or more may be lethal. Some cases of abuse have been reported resulting in a mild form of addiction. Pentazocine abuse has been reported to be widespread among street addicts in the United States of America, in combination with tripelennamine ( T s and Blues ). 

Tripelennamine is contraindicated in patients with known hypersensitivity to similar chemical structures, such as pyrilamine in neonates, other infants, and breastfeeding women because young children may be more susceptible to the toxic effects of antihistamines during asthma attacks because it thickens bronchial secretions and in patients who have taken MAO inhibitors within the preceding two weeks. 

Tripelennamine as antihistamine, 1, 177 biological activity, 4, 911 toxicity, 4, 912 Tripelennamine, p-bromo-as antihistamine, 2, 520 a-Tripiperideine synthesis, 3, 510 Triprolidine as antihistamine, 1, 177 Triptolide, 7, 192 Tripyrroles synthesis, 4, 415, 416 1,6,6a A4-T riselenapentalenes CNDO calculations, 6, 1052 PE spectra, 6, 1057 Trisilacyclobutanes synthesis, 1, 601... 

The overall activity of this drug seems to be very much identical to tripelennamine but it is pronounced to have much less toxicity. 

SAR to Thonzylamine. The only difference between this drug and tripelennamine is the presence of a pyrimidine nucleus instead of the pyridine nucleus in the latter, which perhaps retards its toxicity profile to an appreciable extent because of its comparatively faster metabolism in vivo. 

Chlorothen is similar in structure to tripelennamine, the only difference being that the benzyl group in the latter is substituted by the 5-halothenyl moiety. It has been observed that the halogen-substitution enhances the antihistaminic activity and renders the compound less toxic than its corresponding non-halogenated version. 

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