Galantamine Hydrobromide (500mg) – Product Details

Galantamine Hydrobromide
CAS Number	357-70-0
Molar Mass	287.359 g·mol−1
Chemical Formula	C17H21NO3
IUPAC Name	(4aS,6R,8aS)-5,6,9,10,11,12-Hexahydro-3-methoxy-11-methyl-4aH-[1]benzofuro[3a,3,2-ef][2]benzazepin-6-ol

What is Galantamine Hydrobromide?

An inhibitor of the enzyme acetylcholinesterase (AChE) that is both reversible and competitive; it is currently authorized for use in the treatment of Alzheimer’s disease. In addition to this, it functions as an allosteric modulator of nicotinic acetylcholine receptors (nAChR). Apoptosis can be prevented, and neuroprotection can be achieved as a result, through the activation of nAChR in conjunction with the upregulation of the anti-apoptotic protein Bcl-2.

In its natural state, Galantamine is a tertiary alkaloid. It wasn’t until the early 1950s that it was identified and isolated from plant sources like Galanthus nivalis. In the beginning, studies of Galantamine were conducted on patients suffering from neuropathic pain and paralytic conditions. These conditions included post-polio paralytic conditions, myopathies, and the reversal of neuromuscular blockade.

Despite this, the discovery of its acetylcholine esterase inhibiting property has revolutionized the field of medicine. It was investigated as a potential treatment for a wide range of psychiatric conditions. However, due to the challenges involved in Galantamine’s extraction and synthesis, the redevelopment of Galantamine as a treatment for Alzheimer’s disease did not begin until the early 1990s. In 2001, the FDA gave their approval to Galantamine as a treatment for Alzheimer’s disease which ranges from mild to moderate to severe. [R]

How Does Galantamine Hydrobromide Work?

Galantamine hydrobromide(Hbr) has a unique, dual mode of action. It is the only compound that is actively marketed for the treatment of Alzheimer’s disease and has proven activity as an allosteric modulator of nicotinic acetylcholine receptors. It is also a reversible, competitive inhibitor of acetylcholinesterase (AChE), which is an enzyme that breaks down acetylcholine (nAChRs).

This latter activity is thought to be particularly important due to the fact that decreases in the expression and activity of nAChRs make a large contribution to the reduction in central cholinergic neurotransmission site observed in patients diagnosed with Alzheimer’s disease (AD).

Galantamine has improved pharmacokinetic characteristics, such as predictable linear elimination kinetics at the recommended maintenance doses (16 and 24 mg/day), a relatively short half-life (approximately 7 hours), and high bioavailability. It has a low potential for clinically significant  interactions because it is extensively metabolized in numerous pathways, the majority of which occur in the liver and are catalyzed by the cytochrome P450 enzymes CYP2D6 and CYP3A4, and because of this, clinically significant drug-drug interactions are unlikely to occur.[R]

Galantamine is a one-of-a-kind compound that acts as an allosteric potentiator of 42 and presynaptic -7 nicotinic acetylcholine receptors. This action promotes acetylcholine release from presynaptic neurons, lending clinical significance to its dual mode of action. Nicotinic acetylcholine receptors (nAChR) in the central nervous system are predominantly expressed at the membranes of presynaptic neurons and control the release of several neurotransmitters associated with memory, thinking, and learning, including ACh, GABA, glutamate, norepinephrine, dopamine, and serotonin. nAChR agonists improve cognitive functions, whereas nAChR antagonists hinder cognitive processes. [R]

Galantamine Hydrobromide Research

Numerous animal and human studies have been conducted on the potential application of Galantamine Hydrobromide . On this page below follows some of the relevant findings:

Galantamine Hydrobromide on Chronic post-stroke Aphasia

The effect of Galantamine on linguistic function was investigated in a study of 45 patients with chronic aphasia. Language evaluation was done at week 0 and week 16 of the study. The starting dose of Galantamine was 8 milligrams per day (mg/day) for the first four weeks, followed by 16 mg/day for the subsequent 12 weeks.

The effectiveness of the test was determined by adding up the scores for four different categories: spontaneous speech, comprehension, repetition, and naming. It was discovered that the administration of Galantamine had a beneficial effect on chronic post-stroke aphasia. This effect was found to be more prominent in subcortical dominant lesions [R] 

Galantamine Hydrobromide on “Substitution Therapy” into the Treatment of Smoking

The high morbidity and mortality caused by smoking emphasize the need to investigate new strategies for quitting or reducing smoking. The preliminary data suggest that Galantamine has the potential to reduce smoking behavior even in the absence of additional interventions. It was proposed to introduce the term “substitution therapy” into smoking cessation treatments.

The result could pave the way for a novel treatment strategy for groups of patients with typically low motivation to change. [R]

Galantamine Hydrobromide on Autism

Research was conducted to investigate whether or not Galantamine can be beneficial to adults who were diagnosed with autism before the age of three in accordance with DSM-IV-TR Axis I clinical criteria.

It is possible that cholinergic stimulation of the serotonergic subsystem of the central nervous system (CNS) with Galantamine will improve expressive language and communication in adults with autism. Adjuvant therapy with Galantamine needs to be investigated in clinical trials for patients in this category. [R]

Galantamine Hydrobromide on Organophosphorus Poisoning

Organophosphorus (OP) compounds, such as nerve agents and pesticides, have been studied for a long time to find ways to treat people who have been poisoned by OP. There is also proof that 100% of guinea pigs can live when the right doses of Galantamine and atropine are given 30-45 minutes after the animals are exposed to 1 x LD50 soman.

Galantamine stops neurodegeneration and changes to the nicotinic cholinergic system that happen when guinea pigs are exposed to 1 x LD50 soman all at once. The results shown here support the idea that Galantamine is a good way to treat OP poisoning. [R]

Galantamine Hydrobromide on Rheumatoid Arthritis

Rheumatoid arthritis (RA), is a chronic autoimmune disease with an unknown cause that is characterized by the production of inflammatory cytokines and a reduction in joint mobility. Evidence from a rat model study suggests that Galantamine can be used in order to inhibit the anti-inflammatory responses that are caused by RA. [R]

 

Potential Adverse Effects: [R]

• Cardiovascular system: Inhibition of sinoatrial activity results in sinus bradycardia.
• Gastrointestinal system: Appetite loss, nausea, vomiting, diarrhea, and weight loss are the most frequent gastrointestinal adverse effects.
•  Skin: skin lesion, e.g., rash,
• Respiratory system: Galantamine’s cholinomimetic effect can make people more susceptible to developing bronchospasm.
• Nervous system: The most common adverse reactions include headaches and lightheadedness.

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