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JP-2026076279-A - Methods for gradually increasing the dosage of psychedelic drugs

JP2026076279AJP 2026076279 AJP2026076279 AJP 2026076279AJP-2026076279-A

Abstract

[Problem] To provide a method for administering psychedelic drugs that avoids or reduces undesirable side effects. [Solution] A method for administering a psychedelic drug to avoid the side effects of hallucinations and perceptual disturbances, comprising: the step of administering the psychedelic drug to an individual in an escalating dosing regimen; and the step of reducing the side effects of hallucinations and perceptual disturbances. [Selection Diagram] None

Inventors

  • バロウ，ロバート
  • カーリン，ダニエル アール．

Assignees

  • デフィニウム セラピューティクス ユーエス， インコーポレイテッド

Dates

Publication Date
20260511
Application Date
20260130
Priority Date
20210503

Claims (20)

  1. A method of administering psychedelic drugs to avoid the side effects of hallucinations and perceptual disturbances: The steps include administering the psychedelic drug to an individual in a gradual increase in dosage regimen; A method that includes steps to mitigate side effects such as hallucinations and perceptual disturbances.
  2. The administration step further involves administering an initial dose to the individual; Increasing the dose by a set amount over a set period of time, and administering the increased dose to the individual; The method according to claim 1, defined as repeating the increasing and administering steps over the period during which the individual is being treated until the desired maximum dose is reached.
  3. The method according to claim 2, wherein the initial dose is a dose below the perceptual dose.
  4. The method according to claim 2, wherein the initial dose is 10 μg and is increased by 10 μg at regular intervals.
  5. The method according to claim 2, wherein the aforementioned period is selected from the group consisting of hours, days, weeks, months, and years.
  6. The method according to claim 2, wherein the dose is increased by an amount selected from the group consisting of 10, 20, 30, and 50 μg.
  7. The method according to claim 1, wherein the administration step is further defined as administering an initial dose of a loading dose and subsequent doses of a subsensory dose.
  8. The aforementioned psychedelic drugs include lysergic acid diethylamide (LSD), psilocybin, mescaline, 5-methoxy-N,N-dimethyltryptamine (5-MeO-DMT), dimethyltryptamine (DMT), 2,5-dimethoxy-4-iodoamphetamine (DOI), The method according to claim 1, selected from the group consisting of 2,5-dimethoxy-4-bromoamphetamine (DOB), its salts, its tartrates, its analogs, and its homologs.
  9. A kit for administering an escalating dosing regimen of a psychedelic drug, comprising a pharmaceutically effective amount of the drug in dosage forms divided into packages according to the dose and time of administration in the escalating dosing regimen, and instructions for use.
  10. The aforementioned psychedelic drugs include lysergic acid diethylamide (LSD), psilocybin, mescaline, 5-methoxy-N,N-dimethyltryptamine (5-MeO-DMT), dimethyltryptamine (DMT), 2,5-dimethoxy-4-iodoamphetamine (DOI), The kit according to claim 9, selected from the group consisting of 2,5-dimethoxy-4-bromoamphetamine (DOB), its salts, its tartrates, its analogues, and its homologues.
  11. The kit according to claim 9, wherein the dosage form comprises an initial dose and an additional increased dose.
  12. The kit according to claim 11, wherein the initial dose is of a different color or size than the additional increased dose.
  13. Claim 11, wherein the additional increased dose is a single dosage form or a plurality of separate dosage forms. The kit described above.
  14. The kit according to claim 9, wherein the packaging indicates the period during which each dose should be taken.
  15. The kit according to claim 9, wherein the packaging is a blister pack.
  16. A method of treating individuals with psychedelic drugs: A gradual increase in dosage regimen includes the step of administering the psychedelic drug to the individual having a certain condition or disease; A method that includes steps to mitigate side effects such as hallucinations and paresthesia during treatment.
  17. The condition or disorder being treated is anxiety disorder, depression, headache disorder, obsessive-compulsive disorder (OCD), The method according to claim 16, selected from the group consisting of personality disorders, stress disorders, drug disorders, gambling disorders, eating disorders, body dysmorphic disorder, pain, neurodegenerative disorders, motor disorders, autism spectrum disorders, eating disorders, and neurological disorders.
  18. The administration step further involves administering an initial dose to the individual; Increasing the dose by a set amount over a set period of time, and administering the increased dose to the individual; The method according to claim 16, defined as repeating the increasing and administering steps over the period during which the individual is being treated until a desired maximum dose is reached.
  19. The method according to claim 18, wherein the initial dose is a dose below the perceptual dose.
  20. The method according to claim 18, wherein the initial dose is 10 μg and is increased by 10 μg at regular intervals.

Description

Background of the Invention 1. Technical Field The present invention relates to a composition and method for administering psychedelic drugs. 2. Background Technology Psychedelic drugs, including lysergic acid diethylamide (LSD), are substances that can induce unique subjective effects, including altered consciousness, positive emotions, enhanced introspection, altered perception of the environment, body, and self, as well as synesthesia, mystical experiences, and ego disintegration (Carhart-Harris et al., 2016b; Dolder et al., 2016; Holze et al., 2021; Lie chti, 2017; Passie et al., 2008; Schmid et al., 2015). All serotonergic psychedelic drugs, including LSD, psilocybin, DMT, and mescaline, are nonspecific serotonin agonists with agonist activity at the serotonin 5-HT2A receptor (Rickli et al., 2016), and therefore can generally produce very similar effects. Furthermore, psychedelic substances produce their acute effects in humans through activation of the serotonin 5-HT2A receptor, as specifically demonstrated in clinical studies of LSD (Holze et al., 2021; Preller et al., 2017). And other hallucinogens are partial agonists of the serotonin 5-HT2A receptor (Lopez-Gime nez, et al. Hallucinogens and Serotonin 5-HT2A Receptor-Mediated Signaling Pathw ays. Curr Top Behav Neurosci. 2018;36:45-73;Canal CE. Serotonergic Psychedelics : Experimental Approaches for Assessing Mechanisms of Action. Handb Exp Pharmaco l. 2018;252:227-260). The acute effects of psychedelic drugs that may contribute to their therapeutic benefits include, as described in more detail elsewhere, enhancing therapeutic relationships through increased openness, feelings of trust, connection or emulsion, the ability to grasp psychological issues, and stimulation of the neurogenesis process (Vollenweider & Preller, 2020). The administration of psychedelic drugs, especially at doses considered therapeutic, has side effects such as hallucinations or paresthesia (Ungerleider, J. THOMAS. "The acute side effects from LSD."). ”The problems and prospects of LSD (1968): 61-68), (Nichols, Psychedelics, Ph. (armacol Rev 68:264-355). These side effects make it unsafe for subjects to be administered psychedelic drugs outside of direct physician supervision, and even under physician supervision, they can pose a significant safety risk to patients if side effects occur while the patient is driving or operating machinery. These side effects, characteristic of psychedelic drug administration, are mediated by the drug's activity at the serotonin 5-HT2A receptor, as evidenced by the fact that blocking this activity (by administering 5-HT2A antagonists such as ketanserine) can reduce these psychostimulant/hallucinogenic side effects (Holze et al., 2020). While repeated administration of psychedelic drugs (e.g., daily) has been shown to qualitatively have clinical benefits, the hallucinogenic/perceptual disturbances, as outlined by Buchborn (2016), may disappear several days after treatment due to tachyphylaxis (i.e., via downregulation of the 5-HT2A receptor). Nevertheless, during the first few days after administration of psychedelic drugs, subjects may experience common adverse events such as hallucinations, perceptual disturbances, and other potentially risky outcomes for the patient. The Cleveland Clinic states that dose escalation is a method of limiting potential side effects by taking time to observe how a person's body responds to the drug. Here, drug administration is started at a low dose and then increased every two to three weeks until the maximum effective dose (target dose) is achieved or side effects occur. Caffrey, e t al. (Ther Adv Drug Saf. 2021 Jan 19; 11: 2042098620958910) states that dose escalation is necessary to provide treatment at the lowest possible dose while minimizing drug use and side effects. Generally, it is described as being used for drugs with a narrow therapeutic index. This is a patient-centered approach to providing personalized medicine. Dosage escalation is used for antibiotics, anticoagulants, anticonvulsants, antidepressants, antidiabetic drugs, antipsychotics, opioids, and stimulants. This is a graph of dose over time. Detailed Description of the Invention The present invention provides a method for administering psychedelic drugs to an individual in an escalating dosing regimen, thereby avoiding the side effects of hallucinations and paresthesia while preserving the desired therapeutic benefits, by mitigating the side effects of hallucinations, paresthesia, and other immediately detectable effects of psychedelic drugs. More specifically, an escalation regimen may include administering an initial dose to an individual, increasing the dose to a set amount over a set time, administering the increased dose to the individual, and repeating these steps over the duration the individual is being treated until the desired maximum dose is reached. A regimen can generally be described by the following formula: dose = X (initial