The non-hallucinogen 2-bromo-lysergic acid diethylamide as preventative treatment for cluster headache: An open, non-randomized case series

Hannover Medical School, Hannover, Germany.
Cephalalgia (Impact Factor: 4.89). 09/2010; 30(9):1140-4. DOI: 10.1177/0333102410363490
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    • "While lysergide (lysergic acid diethylamide, LSD; Figure 3) was once a common drug of misuse and a substance that might still have therapeutic potential, there has been little or no clinical or illicit use of other 'N-alkyl derivatives of lysergamide'. That situation changed when it was found that 2-bromo-LSD (aka BOL-148; Figure 3) had value in the treatment of cluster headaches, [33] a condition that often fails to respond to any conventional means of control. Because of the ambiguity of the above definition, there is no straightforward answer to the question 'Is 2-bromo-LSD a controlled drug?' "
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    ABSTRACT: The concept of a 'derivative' is used widely in chemistry, where its precise meaning depends on the circumstances. However, numerous examples of derivative also occur in domestic drugs legislation, some of which stem from the 1961 United Nations Single Convention on Narcotic Drugs. There is a commonly held view that only 'first-order' derivatives should be considered: substances that can be created from a parent structure in a single chemical reaction. In other words, 'derivatives of derivatives' are excluded. However, some substances related to ecgonine (e.g. 2-carbomethoxytropinone) are clearly convertible to cocaine, even though this may require more than one reaction step. It follows that 2-carbomethoxytropinone is a controlled drug, a situation that most chemists would regard as perverse. A more extreme example of the complexity of 'derivative' is shown by the conversion of thebaine to buprenorphine. Even though this requires six or more stages, the US Drug Enforcement Administration successfully argued in a 1986 case that for the purposes of the Controlled Substances Act, the number of steps required was irrelevant; buprenorphine was a derivative of thebaine. Because the term derivative is rarely defined in statutes, the legal status of some substances, such as 2-bromo-LSD, is uncertain. Although a number of definitions of derivative can be found in the chemical literature, no single definition is adequate to describe all situations where it occurs in legislation. Unless qualified, it is suggested that the term derivative should be avoided in any future legislation. Copyright © 2013 John Wiley & Sons, Ltd.
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    • "Many nonpsychedelic indole alkaloids that are structurally related to psilocybin, (e.g., methysergide, ergotamine, dihydroergotamine, and methylergonovine) are used as treatments for cluster headache, although they do not abort cluster periods or extend remission period as psilocybin is noted to do. Recent reports that the non-psychoactive LSD analog BOL-148 is also effective in treating cluster headache (Karst et al., 2010) suggest that the therapeutic effects of these drugs are not mediated by 5-HT 2A ; in fact, a dissociation between the autonomic and the psychoactive properties of psilocybin has already been described (Fischer, 1968). "
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    ABSTRACT: Psilocybin is a well-characterized classic hallucinogen (psychedelic) with a long history of religious use by indigenous cultures, and nonmedical use in modern societies. Although psilocybin is structurally related to migraine medications, and case studies suggest that psilocybin may be efficacious in treatment of cluster headache, little is known about the relationship between psilocybin and headache. This double-blind study examined a broad range of psilocybin doses (0, 5, 10, 20, and 30 mg/70 kg) on headache in 18 healthy participants. Psilocybin frequently caused headache, the incidence, duration, and severity of which increased in a dose-dependent manner. All headaches had delayed onset, were transient, and lasted no more than a day after psilocybin administration. Possible mechanisms for these observations are discussed, and include induction of delayed headache through nitric oxide release. These data suggest that headache is an adverse event to be expected with the nonmedical use of psilocybin-containing mushrooms as well as the administration of psilocybin in human research. Headaches were neither severe nor disabling, and should not present a barrier to future psilocybin research.
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