Octopalean Octopamine Hcl
Also known as: Octopamine HCl, DL-Octopamine hydrochloride, Epirenor, Norden, Norfen, Octopamine hydrochloride
Overview
Octopamine hydrochloride is a naturally occurring biogenic amine structurally related to norepinephrine, found endogenously in invertebrates, trace amounts in mammals, and some plants. It is included in dietary supplements primarily for its purported ability to enhance fat metabolism, aid in weight management, and improve sports performance. Pharmacologically, octopamine acts as a sympathomimetic agent, though it exhibits low affinity for mammalian α- and β-adrenergic receptors, producing pressor effects mainly at high doses. While it has been used medically as an antihypotensive agent, clinical data on its efficacy and safety in humans are very limited. Most mechanistic understanding is derived from invertebrate models and animal studies, with a notable absence of high-quality human clinical evidence, such as systematic reviews or meta-analyses, to support its use as a supplement.
Benefits
Octopamine may mobilize fat from adipocytes by stimulating lipolysis, but there is no conclusive evidence from human studies that this leads to meaningful or sustained weight loss. The released fatty acids are likely rapidly reabsorbed by other tissues, limiting clinical significance. It can increase blood pressure and stimulate motor activity, suggesting potential use in hypotension or fatigue, but these effects are dose-dependent and not well characterized in humans. No robust clinical trials demonstrate benefits in specific populations like athletes or obese individuals. There are no randomized controlled trials (RCTs) with adequate sample sizes and statistical significance to quantify effect sizes for weight loss or performance enhancement. Pharmacokinetic data indicate a half-life of approximately 175-243 minutes after administration, but the long-term clinical effects remain unclear.
How it works
Octopamine functions as a sympathomimetic amine, exhibiting weak binding to mammalian α- and β-adrenergic receptors, with an affinity 400- to 2,000-fold lower than that of norepinephrine. In invertebrates, it modulates cyclic AMP (cAMP) signaling pathways, influencing motor activity and learning. In mammals, it is thought to mobilize fat by stimulating lipolysis in adipocytes, but it does not strongly activate adrenergic receptors. It is poorly transported by dopamine transporters and has limited penetration into the central nervous system. Oral bioavailability is limited, with peak serum levels typically achieved within a few hours.
Side effects
Octopamine is generally considered to have a low safety profile, primarily due to its sympathomimetic effects, especially at higher doses. Common side effects are not well documented in humans but may include increases in blood pressure and heart rate. Uncommon side effects (1-5%) could involve nervous system stimulation or other cardiovascular effects. Rare side effects (<1%) are unknown due to the lack of extensive human clinical trials. There is a potential for dangerous interactions with other stimulants or hypertensive agents, which could significantly increase the risk of hypertension. Octopamine is contraindicated in individuals with pre-existing cardiovascular disease, hypertension, or known sensitivity to sympathomimetics. Safety data for special populations, such as pregnant or nursing individuals and children, are completely lacking, making its use in these groups highly unadvisable.
Dosage
There is no established minimum effective dose or optimal dosage range for octopamine hydrochloride for fat loss or performance enhancement in humans. Pharmacokinetic studies have observed serum levels after 2-8 mg oral or intravenous doses, but the clinical relevance of these levels is unclear. The maximum safe dose has not been well defined, and high doses carry a significant risk of cardiovascular side effects. Due to insufficient clinical data, there are no specific recommendations regarding timing of administration or preferred forms. While intravenous administration shows better absorption, oral bioavailability is limited. There are no known required cofactors for its absorption or efficacy.
FAQs
Is it safe?
It may increase blood pressure and heart rate. Caution is advised, especially when combined with other stimulants, due to potential cardiovascular risks.
When should it be taken?
There are no evidence-based recommendations for the optimal timing of octopamine supplementation due to a lack of clinical data.
Does it improve athletic performance?
No robust human trials have confirmed that octopamine provides significant benefits for athletic performance.
Is it banned in sports?
Yes, the World Anti-Doping Agency (WADA) lists octopamine as a prohibited stimulant during competition.
Research Sources
- https://drugs.ncats.io/drug/37YAS5L9HQ – This source from the NCATS Inxight Drugs database provides pharmacokinetic data for octopamine, indicating a half-life of 175-243 minutes after 2-8 mg doses in adults. It highlights limited oral bioavailability and rapid clearance, suggesting challenges for sustained clinical effects.
- https://en.wikipedia.org/wiki/Octopamine – This Wikipedia entry provides a general overview of octopamine, including its classification as a sympathomimetic amine and its structural relation to norepinephrine. It notes octopamine's lower affinity for mammalian adrenergic receptors compared to norepinephrine, which explains its weaker pharmacological effects.
- https://pubmed.ncbi.nlm.nih.gov/32277043/ – This PubMed entry refers to a neuroscience study in Drosophila, which demonstrates that octopamine modulates learning via cAMP pathways. While this research highlights octopamine's important role in invertebrate neural signaling, its direct applicability to human physiology and supplement efficacy is limited.
