Carvedilol inhibits the cardiostimulant and thermogenic effects of MDMA in humans

British Journal of Pharmacology

Volumn 166, Issue 8, 2012, Pages 2277-2288

  Hysek, C M ^a   Schmid, Y ^a   Rickli, A ^a   Simmler, L D ^a   Donzelli, M ^a   Grouzmann, E ^b   Liechti, M E ^a  

^a UNIVERSITY OF BASEL   (Switzerland)

^b LAUSANNE UNIVERSITY HOSPITAL   (Switzerland)

Author keywords

3,4 methylenedioxymethamphetamine; carvedilol; ecstasy; MDMA; noradrenaline; and adrenoceptors

Indexed keywords

3,4 METHYLENEDIOXYMETHAMPHETAMINE; ALPHA 1 ADRENERGIC RECEPTOR; BETA ADRENERGIC RECEPTOR; CARVEDILOL; PLACEBO;

ADULT; ANTIHYPERTENSIVE ACTIVITY; ARTICLE; BLOOD PRESSURE; BODY TEMPERATURE; CONTROLLED STUDY; CROSSOVER PROCEDURE; DOUBLE BLIND PROCEDURE; DRUG EFFECT; FEMALE; HEART RATE; HEART STIMULATION; HUMAN; HUMAN EXPERIMENT; MALE; NORMAL HUMAN; PRIORITY JOURNAL; PSYCHOMETRY; RANDOMIZED CONTROLLED TRIAL; THERMOGENESIS; UNSPECIFIED SIDE EFFECT;

EID: 84864482361     PISSN: 00071188     EISSN: 14765381     Source Type: Journal    
DOI: 10.1111/j.1476-5381.2012.01936.x     Document Type: Article

References (83)

1. 1b-adrenergic receptors: relationship between functional and nonfunctional dopamine release. J Neurosci 22: 9150-9154. (Pubitemid 35356155)
2. Bachmakov I, Werner U, Endress B, Auge D, Fromm MF, (2006). Characterization of β-adrenoceptor antagonists as substrates and inhibitors of the drug transporter P-glycoprotein. Fundam Clin Pharmacol 20: 273-282.
3. Battaglia G, Brooks BP, Kulsakdinun C, De Souza EB, (1988). Pharmacologic profile of MDMA (3,4-methylenedioxymethamphetamine) at various brain recognition sites. Eur J Pharmacol 149: 159-163.
4. Berlin I, Lechat P, Deray G, Landault C, Maistre G, Chermat V, et al,. (1993). Beta-adrenoceptor blockade potentiates acute exercise-induced release of atrial natriuretic peptide by increasing atrial diameter in normotensive healthy subjects. Eur J Clin Pharmacol 44: 127-133. (Pubitemid 23047747)
5. 1-adrenoceptor subtypes in the effects of methylenedioxy methamphetamine (MDMA) on body temperature in the mouse. Br J Pharmacol 153: 591-597. (Pubitemid 351199018)
6. Boehrer JD, Moliterno DJ, Willard JE, Hillis LD, Lange RA, (1993). Influence of labetalol on cocaine-induced coronary vasoconstriction in humans. Am J Med 94: 608-610. (Pubitemid 23166707)
7. Brody SL, Slovis CM, Wrenn KD, (1990). Cocaine-related medical problems: consecutive series of 233 patients. Am J Med 88: 325-331. (Pubitemid 20147265)
8. Brogden RN, Sorkin EM, (1990). Ketanserin. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in hypertension and peripheral vascular disease. Drugs 40: 903-949. (Pubitemid 120032437)
9. Bruggisser M, Ceschi A, Bodmer M, Wilks MF, Kupferschmidt H, Liechti ME, (2010). Retrospective analysis of stimulant abuse cases reported to the Swiss Toxicological Information Centre during 1997-2009. Swiss Med Wkly 140: w13115.
10. Bunzow JR, Sonders MS, Arttamangkul S, Harrison LM, Zhang G, Quigley DI, et al,. (2001). Amphetamine, 3,4-methylenedioxymethamphetamine, lysergic acid diethylamide, and metabolites of the catecholamine neurotransmitters are agonists of a rat trace amine receptor. Mol Pharmacol 60: 1181-1188. (Pubitemid 33144888)
11. Dafters RI, (1995). Hyperthermia following MDMA administration in rats: effects of ambient temperature, water consumption, and chronic dosing. Physiol Behav 58: 877-882.
12. Derogatis LR, Rickels K, Rock AF, (1976). The SCL-90 and the MMPI: a step in the validation of a new self-report scale. Br J Psychiatry 128: 280-289.
13. Di Cara B, Maggio R, Aloisi G, Rivet JM, Lundius EG, Yoshitake T, et al,. (2011). Genetic deletion of trace amine 1 receptors reveals their role in auto-inhibiting the actions of ecstasy (MDMA). J Neurosci 31: 16928-16940.
14. Dittrich A, (1998). The standardized psychometric assessment of altered states of consciousness (ASCs) in humans. Pharmacopsychiatry 31 (Suppl. 2): 80-84. (Pubitemid 28396276)
15. Docherty JR, Green AR, (2010). The role of monoamines in the changes in body temperature induced by 3,4-methylenedioxymethamphetamine (MDMA, ecstasy) and its derivatives. Br J Pharmacol 160: 1029-1044.
16. 1b-adrenergic receptors control locomotor and rewarding effects of psychostimulants and opiates. J Neurosci 22: 2873-2884. (Pubitemid 37465836)
17. Dumont GJ, Verkes RJ, (2006). A review of acute effects of 3,4-methylenedioxymethamphetamine in healthy volunteers. J Psychopharmacol 20: 176-187.
18. Dumont GJ, Kramers C, Sweep FC, Touw DJ, van Hasselt JG, de Kam M, et al,. (2009). Cannabis coadministration potentiates the effects of 'ecstasy' on heart rate and temperature in humans. Clin Pharmacol Ther 86: 160-166.
19. Eisenhofer G, Rundquist B, Aneman A, Friberg P, Dakak N, Kopin IJ, et al,. (1995). Regional release and removal of catecholamines and extraneuronal metabolism to metanephrines. J Clin Endocrinol Metab 80: 3009-3017.
20. Elsinga PH, Hendrikse NH, Bart J, van Waarde A, Vaalburg W, (2005). Positron emission tomography studies on binding of central nervous system drugs and P-glycoprotein function in the rodent brain. Mol Imaging Biol 7: 37-44. (Pubitemid 41348874)
21. Esler M, Jennings G, Lambert G, Meredith I, Horne M, Eisenhofer G, (1990). Overflow of catecholamine neurotransmitters to the circulation: source, fate, and functions. Physiol Rev 70: 963-985. (Pubitemid 20364820)
22. Fantegrossi WE, Kiessel CL, Leach PT, Van Martin C, Karabenick RL, Chen X, et al,. (2004). Nantenine: an antagonist of the behavioral and physiological effects of MDMA in mice. Psychopharmacology (Berl) 173: 270-277. (Pubitemid 38703800)
23. Farre M, Abanades S, Roset PN, Peiro AM, Torrens M, O'Mathuna B, et al,. (2007). Pharmacological interaction between 3,4-methylenedioxymethamphetamine (ecstasy) and paroxetine: pharmacological effects and pharmacokinetics. J Pharmacol Exp Ther 323: 954-962. (Pubitemid 350146071)
24. Forget B, Wertheim C, Mascia P, Pushparaj A, Goldberg SR, Le Foll B, (2011). Noradrenergic alpha1 receptors as a novel target for the treatment of nicotine addiction. Neuropsychopharmacology 35: 1751-1760.
25. Freedman RR, Johanson CE, Tancer ME, (2005). Thermoregulatory effects of 3,4-methylenedioxymethamphetamine (MDMA) in humans. Psychopharmacology (Berl) 183: 248-256. (Pubitemid 41609277)
26. Graff DW, Williamson KM, Pieper JA, Carson SW, Adams KF, Jr, Cascio WE, et al,. (2001). Effect of fluoxetine on carvedilol pharmacokinetics, CYP2D6 activity, and autonomic balance in heart failure patients. J Clin Pharmacol 41: 97-106.
27. Green AR, Cross AJ, Goodwin GM, (1995). Review of the pharmacology and clinical pharmacology of 3,4-methylenedioxymethamphetamine (MDMA or 'Ecstasy'). Psychopharmacology 119: 247-260.
28. Grunau BE, Wiens MO, Brubacher JR, (2010). Dantrolene in the treatment of MDMA-related hyperpyrexia: a systematic review. CJEM 12: 435-442.
29. Hall AP, Henry JA, (2006). Acute toxic effects of 'Ecstasy' (MDMA) and related compounds: overview of pathophysiology and clinical management. Br J Anaesth 96: 678-685. (Pubitemid 43786681)
30. Halpern P, Moskovich J, Avrahami B, Bentur Y, Soffer D, Peleg K, (2011). Morbidity associated with MDMA (ecstasy) abuse: a survey of emergency department admissions. Hum Exp Toxicol 30: 259-266.
31. Harris GC, Hedaya MA, Pan WJ, Kalivas P, (1996). β-adrenergic antagonism alters the behavioral and neurochemical responses to cocaine. Neuropsychopharmacology 14: 195-204.
32. Henry JA, Jeffreys KJ, Dawling S, (1992). Toxicity and deaths from 3,4-methylenedioxymethamphetamine ('ecstasy'). Lancet 340: 384-387.
33. Hoffman RS, (2008). Cocaine and beta-blockers: should the controversy continue? Ann Emerg Med 51: 127-129.
34. Hysek CM, Vollenweider FX, Liechti ME, (2010). Effects of a β-blocker on the cardiovascular response to MDMA (ecstasy). Emerg Med J 27: 586-589.
35. Hysek CM, Simmler LD, Ineichen M, Grouzmann E, Hoener MC, Brenneisen R, et al,. (2011). The norepinephrine transporter inhibitor reboxetine reduces stimulant effects of MDMA ('ecstasy') in humans. Clin Pharmacol Ther 90: 246-255.
36. 2-adrenergic agonist clonidine on the pharmacodynamics and pharmacokinetics of methylenedioxymethamphetamine in healthy volunteers. J Pharmacol Exp Ther 340: 286-294.
37. Kolbrich EA, Goodwin RS, Gorelick DA, Hayes RJ, Stein EA, Huestis MA, (2008). Physiological and subjective responses to controlled oral 3,4-methylenedioxymethamphetamine administration. J Clin Psychopharmacol 28: 432-440.
38. Lange RA, Cigarroa RG, Flores ED, McBride W, Kim AS, Wells PJ, et al,. (1990). Potentiation of cocaine-induced coronary vasoconstriction by β-adrenergic blockade. Ann Intern Med 112: 897-903. (Pubitemid 20193673)
39. Liechti ME, Vollenweider FX, (2000). Acute psychological and physiological effects of MDMA ('Ecstasy') after haloperidol pretreatment in healthy humans. Eur Neuropsychopharmacol 10: 289-295. (Pubitemid 30394604)
40. Liechti ME, Vollenweider FX, (2001). Which neuroreceptors mediate the subjective effects of MDMA in humans? A summary of mechanistic studies. Hum Psychopharmacol 16: 589-598. (Pubitemid 34036939)
41. 2 antagonist ketanserin in healthy humans. Neuropsychopharmacology 23: 396-404.
42. Liechti ME, Gamma A, Vollenweider FX, (2001). Gender differences in the subjective effects of MDMA. Psychopharmacology (Berl) 154: 161-168. (Pubitemid 32186501)
43. Liechti ME, Kunz I, Kupferschmidt H, (2005). Acute medical problems due to ecstasy use. Case-series of emergency department visits. Swiss Med Wkly 135: 652-657.
44. Martin TL, Chiasson DA, Kish SJ, (2007). Does hyperthyroidism increase risk of death due to the ingestion of ecstasy? J Forensic Sci 52: 951-953. (Pubitemid 46918574)
45. Mazzeo RS, Carroll JD, Butterfield GE, Braun B, Rock PB, Wolfel EE, et al,. (2001). Catecholamine responses to α-adrenergic blockade during exercise in women acutely exposed to altitude. J Appl Physiol 90: 121-126. (Pubitemid 32038511)
46. Mills EM, Banks ML, Sprague JE, Finkel T, (2003). Pharmacology: uncoupling the agony from ecstasy. Nature 426: 403-404.
47. Mills EM, Rusyniak DE, Sprague JE, (2004). The role of the sympathetic nervous system and uncoupling proteins in the thermogenesis induced by 3,4-methylenedioxymethamphetamine. J Mol Med 82: 787-799.
48. Mo W, Arruda JA, Dunea G, Singh AK, (1999). Cocaine-induced hypertension: role of the peripheral sympathetic system. Pharmacol Res 40: 139-145. (Pubitemid 29378093)
49. Morgan T, (1994). Clinical pharmacokinetics and pharmacodynamics of carvedilol. Clin Pharmacokinet 26: 335-346. (Pubitemid 24148199)
50. Newton TF, (2011). A perhaps unexpected role of norepinephrine in actions of MDMA. Clin Pharmacol Ther 90: 215-216.
51. O'Mathuna B, Farre M, Rostami-Hodjegan A, Yang J, Cuyas E, et al,. (2008). The consequences of 3,4-methylenedioxymethamphetamine induced CYP2D6 inhibition in humans. J Clin Psychopharmacol 28: 523-529.
52. Omvik P, Lund-Johansen P, Myking O, (1992). Effects of carvedilol on atrial natriuretic peptide, catecholamines, and hemodynamics in hypertension at rest and during exercise. J Cardiovasc Pharmacol 19 (Suppl. 1): S90-S96.
53. Pan WH, Sung JC, Fuh SM, (1996). Locally application of amphetamine into the ventral tegmental area enhances dopamine release in the nucleus accumbens and the medial prefrontal cortex through noradrenergic neurotransmission. J Pharmacol Exp Ther 278: 725-731. (Pubitemid 27167039)
54. Parrott AC, (2012). MDMA and temperature: a review of the thermal effects of 'ecstasy' in humans. Drug Alcohol Depend 121: 1-9.
55. Parrott AC, Lock J, Conner AC, Kissling C, Thome J, (2008). Dance clubbing on MDMA and during abstinence from Ecstasy/MDMA: prospective neuroendocrine and psychobiological changes. Neuropsychobiology 57: 165-180.
56. Pedersen NP, Blessing WW, (2001). Cutaneous vasoconstriction contributes to hyperthermia induced by 3,4-methylenedioxymethamphetamine (ecstasy) in conscious rabbits. J Neurosci 21: 8648-8654. (Pubitemid 33051462)
57. Ramoska E, Sacchetti AD, (1985). Propranolol-induced hypertension in treatment of cocaine intoxication. Ann Emerg Med 14: 1112-1113. (Pubitemid 16201424)
58. Rothman RB, Baumann MH, Dersch CM, Romero DV, Rice KC, Carroll FI, et al,. (2001). Amphetamine-type central nervous system stimulants release norepinephrine more potently than they release dopamine and serotonin. Synapse 39: 32-41.
59. Rudnick G, Wall SC, (1992). The molecular mechanism of 'ecstasy'[3,4-methylenedioxy-methamphetamine (MDMA)]: serotonin transporters are targets for MDMA-induced serotonin release. Proc Natl Acad Sci USA 89: 1817-1821.
60. Rusyniak DE, Banks ML, Mills EM, Sprague JE, (2004). Dantrolene use in 3,4-methylenedioxymethamphetamine (ecstasy)-mediated hyperthermia. Anesthesiology 101: 263.
61. Rusyniak DE, Tandy SL, Hekmatyar SK, Mills E, Smith DJ, Bansal N, et al,. (2005). The role of mitochondrial uncoupling in 3,4- methylenedioxymethamphetamine-mediated skeletal muscle hyperthermia and rhabdomyolysis. J Pharmacol Exp Ther 313: 629-639. (Pubitemid 40604163)
62. Schmitz N, Hartkamp N, Kiuse J, Franke GH, Reister G, et al,. (2000). The Symptom Check-List-90-R (SCL-90-R): a German validation study. Qual Life Res 9: 185-193.
63. Selken J, Nichols DE, (2007). Alpha1-adrenergic receptors mediate the locomotor response to systemic administration of (±)-3,4- methylenedioxymethamphetamine (MDMA) in rats. Pharmacol Biochem Behav 86: 622-630. (Pubitemid 46829314)
64. Shioda K, Nisijima K, Yoshino T, Kuboshima K, Iwamura T, Yui K, et al,. (2008). Risperidone attenuates and reverses hyperthermia induced by 3,4-methylenedioxymethamphetamine (MDMA) in rats. Neurotoxicology 29: 1030-1036.
65. Sofuoglu M, Sewell RA, (2009). Norepinephrine and stimulant addiction. Addict Biol 14: 119-129.
66. Sofuoglu M, Brown S, Babb DA, Pentel PR, Hatsukami DK, (2000a). Carvedilol affects the physiological and behavioral response to smoked cocaine in humans. Drug Alcohol Depend 60: 69-76. (Pubitemid 30255987)
67. Sofuoglu M, Brown S, Babb DA, Pentel PR, Hatsukami DK, (2000b). Effects of labetalol treatment on the physiological and subjective response to smoked cocaine. Pharmacol Biochem Behav 65: 255-259. (Pubitemid 30100271)
68. Sofuoglu M, Poling J, Hill K, Kosten T, (2009). Atomoxetine attenuates dextroamphetamine effects in humans. Am J Drug Alcohol Abuse 35: 412-416.
69. Spahn-Langguth H, Schloos J, (1996). Evidence of significant contribution of carvedilol metabolites to β-receptor antagonism: p.o. and i.v. data. Naunyn Schmiedebergs Arch Pharmacol 353: S158.
70. 3-adrenoreceptor antagonists. Br J Pharmacol 142: 667-670. (Pubitemid 38969661)
71. Sprague JE, Mallett NM, Rusyniak DE, Mills E, (2004b). UCP3 and thyroid hormone involvement in methamphetamine-induced hyperthermia. Biochem Pharmacol 68: 1339-1343. (Pubitemid 39179392)
72. Sprague JE, Moze P, Caden D, Rusyniak DE, Holmes C, Goldstein DS, et al,. (2005). Carvedilol reverses hyperthermia and attenuates rhabdomyolysis induced by 3,4-methylenedioxymethamphetamine (MDMA, Ecstasy) in an animal model. Crit Care Med 33: 1311-1316. (Pubitemid 40827383)
73. Sprague JE, Yang X, Sommers J, Gilman TL, Mills EM, (2007). Roles of norepinephrine, free fatty acids, thyroid status, and skeletal muscle uncoupling protein 3 expression in sympathomimetic-induced thermogenesis. J Pharmacol Exp Ther 320: 274-280. (Pubitemid 46028482)
74. Studerus E, Gamma A, Vollenweider FX, (2010). Psychometric evaluation of the altered states of consciousness rating scale (OAV). PLoS ONE 5: e12412.
75. Tham TC, Guy S, McDermott BJ, Shanks RG, Riddell JG, (1995). The dose dependency of the α- and β-adrenoceptor antagonist activity of carvedilol in man. Br J Clin Pharmacol 40: 19-23.
76. Vanderschuren LJ, Beemster P, Schoffelmeer AN, (2003). On the role of noradrenaline in psychostimulant-induced psychomotor activity and sensitization. Psychopharmacology 169: 176-185. (Pubitemid 37129969)
77. Verrico CD, Miller GM, Madras BK, (2007). MDMA (ecstasy) and human dopamine, norepinephrine, and serotonin transporters: implications for MDMA-induced neurotoxicity and treatment. Psychopharmacology 189: 489-503. (Pubitemid 44791219)
78. 1- Noradrenergic system role in increased motivation for cocaine intake in rats with prolonged access. Eur Neuropsychopharmacol 18: 303-311. (Pubitemid 351246717)
79. Wellman P, Ho D, Cepeda-Benito A, Bellinger L, Nation J, (2002). Cocaine-induced hypophagia and hyperlocomotion in rats are attenuated by prazosin. Eur J Pharmacol 455: 117-126. (Pubitemid 35351606)
80. White TL, Justice AJ, de Wit H, (2002). Differential subjective effects of d-amphetamine by gender, hormone levels and menstrual cycle phase. Pharmacol Biochem Behav 73: 729-741. (Pubitemid 35251831)
81. Wittchen HU, Wunderlich U, Gruschwitz S, Zaudig M, (1997). SKID-I: Strukturiertes Klinisches Interview für DSM-IV. Hogrefe-Verlag: Göttingen.
82. Woolverton WL, (1987). Evaluation of the role of norepinephrine in the reinforcing effects of psychomotor stimulants in rhesus monkeys. Pharmacol Biochem Behav 26: 835-839.
83. Zerssen DV, (1976). Die Beschwerden-Liste. Münchener Informationssystem. Psychis: München.