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Golden Thinker ® – Encyclopedia of Substances – Galantamine Hydrobromide

Golden Thinker ® – Encyclopedia of Substances – Galantamine Hydrobromide

Galantamine Hydrobromide - Check Product Availability for your country

Galantamine Hydrobromide – Check Product Availability for your country

Galantamine Hydrobromide
What is Galantamine Hydrobromide?

Galantamine Hydrobromide (HBR) is a powerful small molecule drug which acts as a cholinesterase inhibitor.

Cholinesterases break down choline-based neurotransmitters, such as acetylcholine, into their component parts. For example, acetylcholine is broken down into choline and acetic acid. This means that galantamine can increase the amount of acetylcholine present in the brain by preventing cholinesterase molecules from breaking it down.

While galantamine is often synthesised and standardised in a lab, the molecule can be derived from natural original too. The molecule can be found in a variety of different plants, and have been used for many years across Russia and Eastern Europe to remedy conditions such as muscle weakness, movement problems and other central nervous system issues.

Galantamine HBR is an FDA approved drug for the treatment of Alzheimer’s. There have also been a variety of human and animal studies which has revealed that this drug may benefit a variety of other medical conditions such as diabetes, inflammatory disorders and other psychiatric disorders (such as autism and schizophrenia).

Brain Benefits and Mode of Action
Improves Cognition and Memory

A wealth of research has demonstrated that galantamine may be a powerful treatment for improving cognition. In particular, galantamine appear to help with a condition called mild cognitive impairment (MCI).

Human studies have shown that patients who were given 4mg of galantamine twice daily for one week had significantly improved performance on memory tasks. These patients also reported improvement in cognition and mental clarity. A similar human study has reported that galantamine improved reaction times and episodic memory.

Studies have suggested that galantamine may be an effective treatment for more severe age-related diseases, such as dementia and Alzheimer’s disease. In fact, galantamine has been proposed to be more effective that the traditionally used cholinesterase inhibitors which are currently used to treat Alzheimer’s disease. Galantamine has also been reported to be just as effective, but more economical, than donepezil – another drug of choice in current Alzheimer’s treatment.

The biological hallmark of these conditions are beta-amyloid plaques which build up around neurons and are thought to impair function. Animal studies have found that galantamine can reduce the presence of these plaques and ease related memory impairments.

Preliminary studies have also highlighted that galantamine may be effective in improving sleep and mood in human patients with dementia.

Mode of action: The mechanisms behind galantamine’s ability to improve cognitive function remain relatively under-researched at present. However, neuroscientists believe the effects are likely a result of the compound’s modulation of the acetylcholine, through inhibiting cholinesterases and regulating acetylcholine nicotinic receptors.

Some preliminary research suggests that galantamine can activate a nicotinic receptor subunit (α7) and a muscarinic receptor (M1) to promote brain growth. There’s also some evidence from animal studies which suggests that various doses of galantamine can increase levels of the molecule IGF-2 in the brain. IGF-2 is a growth factor which supports cell growth and maintenance, which may be a mechanism through which galantamine can increase neuronal growth.

Some studies have also suggested that galantamine can promote a sleep cycle stage known as REM sleep. REM sleep is a critical part of the sleep cycle during which memories are consolidated. This improved quality of REM sleep may confer benefits to memory storage and recall.

Neuroprotective Effects

Some scientific studies suggest that galantamine may decrease brain inflammation. Other studies also suggest that galantamine may provide antioxidant benefits. Both inflammation and oxidative stress are strongly linked with neurodegenerative conditions such as Alzheimer’s and Parkinson’s disease. Hence, these anti-inflammatory effects may prove beneficial in the prevention and treatment of these conditions.

Some preliminary animal studies have shown that galantamine can protect against the effects of toxic poisoning from compounds such as diisopropylfluorophosphate. In rodent models, galantamine has also been shown to lower levels of endotoxins, such as pro-inflammatory cytokines and other inflammatory molecules.

Mode of action: Early indications from research suggest that galantamine can activate an anti-inflammatory cholinergic pathway. By doing so, it looks as though galantamine can reduce the production of pro-inflammatory molecules (cytokines) by up 50-75%. There are additional studies which support the finding that galantamine can activate this anti-inflammatory pathway from different research groups. Some research also suggests that galantamine may regulate some of the well-characterised pathways of inflammations, such as NF-κB and TNF-α.

How to Use

How you use galantamine will depend on your desired outcomes and current condition. If you plan to use galantamine to treat or aid with any medical issues, you must consult your doctor before commencing.

Galantamine is available in immediate release tablets or oral solutions. There are also extended-release capsules available on the market. Some clinical studies report that the immediate release form of the drug can increase the likelihood of side-effects, without adding any additional clinical benefit. The most effective form of galantamine will vary across individuals.

It’s important to build up the dose gradually and start at a low dose. The compound should be taken consistently on a daily basis.

If you miss 2-3 doses, you should restart the medication at the lowest dose and gradually build back up to your target dose. This will help you to avoid any side effects associated with galantamine.

Galantamine does carry a number of side effects; these should be weighed up against the benefits of the compound to your health. It is useful to consult a medical professional when making this decision. Some of the side effects associated with galantamine include nausea, vomiting, diarrhoea, loss of appetite and drowsiness. If these side effects persist or become worse, you must contact a medical professional.

More severe side effects include fainting, seizures, blood in the stool, dark or blood coloured vomit, irregular heartbeat and stomach pain. You must consult a doctor immediately if you have any of these side effects.

Allergic reactions to galantamine are rare. However, it’s important to be vigilant of these reaction symptoms: rash, trouble breathing, swelling of the face/throat, intense dizziness and trouble breathing.

Since the medication can cause drowsiness, medical professionals’ advice against the use of machinery or driving when consuming the drug.

If you’re pregnant or breastfeeding you must consult a doctor before trialling the medication. You must inform your doctor or dentist that you’re taking galantamine before having any kind of surgical procedure.

While some of these side effects may seem severe, the results gained from galantamine may outweigh the risks.

As with most nootropics, it’s important to take plenty of fluids with the supplement. The safe upper level (24mg daily, or 16mg in cases where there is an underlying renal or liver condition) should never be exceeded. More information of suggested dosages can be found in the following section.

Recommended Dose: 4mg – 8mg twice daily

Galantamine dosages depend a lot on individual factors. This in includes your age, severity of condition and other pre-existing medical conditions.

Generally, adults are recommended a starting dose of 4mg taken a maximum of twice daily. After 4 weeks, this dose may be increase to 8-12mg, depending on your needs. It’s best to consult your doctor on this dosage. Always notify your doctor before you begin taking a new medication.

If you have any liver or renal problems, the dose should not exceed 16mg daily.

You should start with the lowest dose and monitor how this affects you. If you’re thinking of increasing the dose, this should be done gradually and not exceed 24mg daily.

Classification: Memory, Cognition, Protection

We’ve classified galantamine as a powerful protector of memory and cognition. Early reports indicate that the drug may be an excellent method of treating and protecting against neurodegenerative disorders and age-related cognitive decline. Galantamine also appears to have potent anti-inflammatory effects, meaning it may play a role as a neuroprotectant.

References
  1. Alagiakrishnan K. (2010). Galantamine in the treatment of minor depression with mild to moderate Alzheimer’s dementia in an elderly woman. Primary care companion to the Journal of clinical psychiatry, 12(3), PCC.09l00905. https://doi.org/10.4088/PCC.09l00905gry
  2. Ali, M. A., El-Abhar, H. S., Kamel, M. A., & Attia, A. S. (2015). Antidiabetic Effect of Galantamine: Novel Effect for a Known Centrally Acting Drug. PloS one, 10(8), e0134648. https://doi.org/10.1371/journal.pone.0134648
  3. Blacker CVR, Greenwood DT, Wesnes KA, et al. Effect of Galantamine Hydrobromide in Chronic Fatigue Syndrome: A Randomized Controlled Trial. JAMA. 2004;292(10):1195–1204. doi:10.1001/jama.292.10.1195
  4. D. Tsvetkova, D. Obreshkova, D. Zheleva – Dimitrova and L. Saso, “Antioxidant Activity of Galantamine and Some of its Derivatives”, Current Medicinal Chemistry (2013) 20: 4595. https://doi.org/10.2174/09298673113209990148
  5. Hyde C, Peters J, Bond M, Rogers G, Hoyle M, Anderson R, Jeffreys M, Davis S, Thokala P, Moxham T. Evolution of the evidence on the effectiveness and cost-effectiveness of acetylcholinesterase inhibitors and memantine for Alzheimer’s disease: systematic review and economic model. Age Ageing. 2013 Jan;42(1):14-20. PubMed.
  6. Hwang, T. Y., Ahn, I. S., Kim, S., & Kim, D. K. (2016). Efficacy of Galantamine on Cognition in Mild-to-Moderate Alzheimer’s Dementia after Failure to Respond to Donepezil. Psychiatry investigation, 13(3), 341–348. https://doi.org/10.4306/pi.2016.13.3.341
  7. Kita, Y., Ago, Y., Takano, E. et al. Galantamine increases hippocampal insulin-like growth factor 2 expression via α7 nicotinic acetylcholine receptors in mice. Psychopharmacology 225, 543–551 (2013). https://doi.org/10.1007/s00213-012-2841-7
  8. Lykhmus, O., Mishra, N., Koval, L., Kalashnyk, O., Gergalova, G., Uspenska, K., Komisarenko, S., Soreq, H., & Skok, M. (2016). Molecular Mechanisms Regulating LPS-Induced Inflammation in the Brain. Frontiers in molecular neuroscience, 9, 19. https://doi.org/10.3389/fnmol.2016.00019
  9. Tracey K. J. (2009). Reflex control of immunity. Nature reviews. Immunology, 9(6), 418–428. https://doi.org/10.1038/nri2566
  10. Li, G., Zhou, C. L., Zhou, Q. S., & Zou, H. D. (2016). Galantamine protects against lipopolysaccharide-induced acute lung injury in rats. Brazilian journal of medical and biological research = Revista brasileira de pesquisas medicas e biologicas, 49(2), e5008. https://doi.org/10.1590/1414-431X20155008
  11. Woo, F. Y., Basri, M., Masoumi, H. R., Ahmad, M. B., & Ismail, M. (2015). Formulation optimization of galantamine hydrobromide loaded gel drug reservoirs in transdermal patch for Alzheimer’s disease. International journal of nanomedicine, 10, 3879–3886. https://doi.org/10.2147/IJN.S80253
  12. Zhaoxuan Wu, Lingling Zhao, Xinxin Chen, Xiaoying Cheng, Yan Zhang. Galantamine attenuates amyloid-β deposition and astrocyte activation in APP/PS1 transgenic mice. (2015). Experimental Gerontology, Volume 72, Pages 244-250, ISSN 0531-5565, https://doi.org/10.1016/j.exger.2015.10.015.
  13. https://www.researchgate.net/publication/322329948_Evaluation_of_nootropic_effects_of_galantamine_and_sildenafil_as_a_combination_in_mice
  14. https://www.drugbank.ca/drugs/DB00674

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