The effect of tripelennamine alone in combination with opiates to produce antinociception in mice

Hui, Ferdinand W.; Sun, Chengyu; Tocus, E.C.; Hanig, Joseph P.

doi:10.1016/0024-3205(83)90857-3

Cited by 23 publications

(2 citation statements)

References 14 publications

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“…It is speculated that antihistamines may facilitate the binding of opioids to the opioid receptor 6 or augment the release of cyclic GMP, which could then act as a central analgesic. 7 Other proposed mechanisms include replacement of opioids bound to nonspecific receptors by antihistamines, thereby making more opioid available for specific opioid receptors, 6 and interactions with substance P and phospholipase A 2 . 4 Hydroxyzine is the antihistamine that has been most widely studied for its adjuvant analgesic activity.…”

Section: Discussionmentioning

confidence: 99%

Diphenhydramine as an Analgesic Adjuvant in Refractory Cancer Pain

Santiago-Palma¹,

Fischberg²,

Kornick³

et al. 2001

Journal of Pain and Symptom Management

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Clinical and animal data suggest that antihistamines may have efficacy in the management of pain. While many mechanisms of action have been proposed for the analgesic action of antihistamines, the exact mechanism is unknown. Controlled clinical trials in different pain models have demonstrated that antihistamines have direct and adjuvant analgesic activity. We report three patients with advanced cancer pain refractory to adjuvants and oral, intravenous, and epidural opioids, who achieved sustained pain relief after the repeated administration of diphenhydramine. Diphenhydramine may be useful in the treatment of neuropathic and nociceptive pain that has failed to respond to treatment with opioids and adjuvant analgesics. We suggest a starting dose of 25 mg of oral or parenteral diphenhydramine every 6 to 8 hours, with titration to effect.

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Section: Discussionmentioning

confidence: 99%

Diphenhydramine as an Analgesic Adjuvant in Refractory Cancer Pain

Santiago-Palma¹,

Fischberg²,

Kornick³

et al. 2001

Journal of Pain and Symptom Management

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“…Some of these include the possible interaction with opioid receptor sites, but antihistamines that lack such an action (e.g. tripelennamine) (15) are antinociceptive and their antinociceptive effects are not blocked by the opioid antagonist naloxone (16). An action at presynaptic histamine autoreceptors, with consequent inhibition of histamine release (17), has been proposed as an antinociceptive mechanism.…”

Section: Antihistaminesmentioning

confidence: 99%

Antihistamines as analgesics

Raffa

2001

J Clin Pharm Ther

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Histamine activates pain-transmitting nerve fibres, releases pain-related neuropeptides, and is painful when injected into the skin. Histamine agonists mimic these effects, suggesting that histamine plays a role in mediating the signal transduction of tissue damage or other painful stimulus. Certain 'antihistamines' (histamine H1 receptor antagonists) and other antihistaminics are 'analgesic' in preclinical or clinical models. Potential sites of action of these agents include the brain and spinal cord and a specific histamine receptor subtype might be involved (three subtypes have been identified). However, it is possible that other mechanisms account for the analgesic effect.

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Abuse of Pentazocine-Naloxone Combination

Reed

Schnoll²

1986

JAMA

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The combination of pentazocine hydrochloride and tripelennamine hydrochloride (T's and blues) has been abused as a heroin substitute. In response to this abuse, the formulation of pentazocine has been changed to include naloxone hydrochloride, a short-acting narcotic antagonist, in the tablet (Talwin Nx). Two cases of abuse of the new pentazocine and naloxone formulation along with tripelennamine are reported. Potential reasons for the failure of naloxone to block the effects of pentazocine are discussed.

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The effect of tripelennamine alone in combination with opiates to produce antinociception in mice

Cited by 23 publications

References 14 publications

Diphenhydramine as an Analgesic Adjuvant in Refractory Cancer Pain

Diphenhydramine as an Analgesic Adjuvant in Refractory Cancer Pain

Antihistamines as analgesics

Abuse of Pentazocine-Naloxone Combination

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