Chemistry:Octodrine
Octodrine, also known as dimethylhexylamine (DMHA) and sold under the brand name Vaporpac among others, is a sympathomimetic and stimulant medication that was formerly used in the treatment of hypotension (low blood pressure).[1][2]
It has been studied in a dozen animal studies from the 1940s through the 1970s. These studies found that octodrine can increase blood pressure and cardiac output in animals. The drug was previously approved for use by the Food and Drug Administration (FDA) as an inhalant (i.e., Vaporpac and Tickle Tackle Inhaler) and in Germany as an oral medication as part of a multi-component medication (i.e., Ambredin and Ordinal), but is no longer available.[3]
DMHA has also been found as an adulterant in sports supplements and is sold online as a designer drug.[3][4] The presence of a reductive amination byproduct confirms its synthetic origin.[5]
In the United States, the FDA considers DMHA to be an unsafe ingredient in dietary supplements.[6] In 2019, the FDA issued nine warning letters to US manufacturers of dietary supplements containing DMHA as an unsafe food additive, deeming such products to be adulterated and illegal for marketing.[7]
Side effects
Reported side effects of octodrine include hypertension, dyspnea, and hyperthermia.[2]
Pharmacology
It is described as a sympathomimetic, vasoconstrictor, and local anesthetic.[2][8]
Pharmacokinetics
Heptaminol is an active metabolite of octodrine.[9]
Chemistry
Related compounds
- Isometheptene
- Methylhexanamine (1,3-DMAA)
- Tuaminoheptane
- 1,3-Dimethylbutylamine (DMBA)
- 1,4-Dimethylamylamine (1,4-DMAA)
- Iproheptine (N-isopropyloctodrine)
- Heptaminol (hydroxyoctodrine)
- Oenethyl
Society and culture
Names
Octodrine is the generic name of the drug and its INN and USAN.[8][1] It is also known by its former developmental code name SKF-51.[8]
As an unsafe dietary ingredient
In the United States, DMHA is not eligible for use as a dietary ingredient, is not approved for use in manufactured foods or dietary supplements, and is not considered to be safe for human consumption (is not GRAS); in regarding DMHA as an unsafe food additive, the FDA has warned manufacturers that dietary supplements containing DMHA are adulterated and illegal for marketing.[6][7]
References
- ↑ 1.0 1.1 Concise Dictionary of Pharmacological Agents: Properties and Synonyms. Springer Netherlands. 2012. p. 206. ISBN 978-94-011-4439-1. https://books.google.com/books?id=tsjrCAAAQBAJ&pg=PA206. Retrieved 30 August 2024.
- ↑ 2.0 2.1 2.2 "Octodrine: New Questions and Challenges in Sport Supplements". Brain Sci 8 (2): 34. February 2018. doi:10.3390/brainsci8020034. PMID 29461475.
- ↑ 3.0 3.1 "Four experimental stimulants found in sports and weight loss supplements: 2-amino-6-methylheptane (octodrine), 1,4-dimethylamylamine (1,4-DMAA), 1,3-dimethylamylamine (1,3-DMAA) and 1,3-dimethylbutylamine (1,3-DMBA)". Clinical Toxicology 56 (6): 421–426. June 2018. doi:10.1080/15563650.2017.1398328. PMID 29115866.
- ↑ "Designer Stimulants: What Athletes Should Know | USADA". 24 January 2019. https://www.usada.org/spirit-of-sport/education/designer-stimulants-what-athletes-should-know/.
- ↑ "1,5-Dimethylhexylamine (octodrine) in sports and weight loss supplements: Natural constituent or synthetic chemical?". Journal of Pharmaceutical and Biomedical Analysis 152: 298–305. April 2018. doi:10.1016/j.jpba.2018.02.008. PMID 29454882.
- ↑ 6.0 6.1 "DMHA in Dietary Supplements". US Food and Drug Administration. 6 March 2023. https://www.fda.gov/food/information-select-dietary-supplement-ingredients-and-other-substances/dmha-dietary-supplements.
- ↑ 7.0 7.1 "FDA Acts on Dietary Supplements Containing DMHA and Phenibut". US Food and Drug Administration. 29 April 2019. https://www.fda.gov/food/cfsan-constituent-updates/fda-acts-dietary-supplements-containing-dmha-and-phenibut.
- ↑ 8.0 8.1 8.2 The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and Bibliographies. Springer US. 2014. p. 802. ISBN 978-1-4757-2085-3. https://books.google.com/books?id=0vXTBwAAQBAJ&pg=PA802. Retrieved 30 August 2024.
- ↑ "Is heptaminol a (major) metabolite of octodrine?". Drug Test Anal 11 (11–12): 1761–1763. November 2019. doi:10.1002/dta.2737. PMID 31763761.
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