AKATINOL

Akatinol is a synthetic derivative of adamantane and functions as a low- to moderate-affinity, uncompetitive antagonist of the N-methyl-D-aspartate (NMDA) receptor, helping regulate abnormal glutamatergic activity and reduce excitotoxicity in the brain.
Akatinol is primarily prescribed for the treatment of moderate to severe Alzheimer’s disease, either as monotherapy or in combination with cholinesterase inhibitors like donepezil, to improve cognitive function, behavioral symptoms, and activities of daily living.
Akatinol is valued for its favorable safety profile, with generally mild side effects, convenient once- or twice-daily dosing, and potential investigational uses in conditions such as Parkinson’s disease, vascular dementia, and neuropathic pain.

CAS Number: 41100-52-1
EC Number: 255-219-5
Molecular Formula: C12H22ClN
Molecular Weight: 215.76 g/mol

Synonyms: MEMANTINE HYDROCHLORIDE, 41100-52-1, Memantine HCL, 3,5-dimethyladamantan-1-amine hydrochloride, 3,5-Dimethyl-1-adamantanamine hydrochloride, Akatinol, Namenda XR, Memary, Memantine Mylan, Memantine Merz, Memantine Accord, Memantine LEK, 1-Amino-3,5-dimethyladamantane Hydrochloride, Acrescent, Balaxur, Auxura, Memantine ratiopharm, JY0WD0UA60, CHEBI:64323, SUN-Y7017, NSC-102290, MARIXINO, FP-01, DTXSID90961439, NSC102290, 3,5-Dimethyltricyclo(3.3.1.13,7)decan-1-amine hydrochloride, 3,5-dimethyltricyclo[3.3.1.13,7]decan-1-amine hydrochloride, NAMZARIC COMPONENT MEMANTINE HYDROCHLORIDE, Ebixia, Valios, Memantine Hydrochloride Oral, Memantine Hydrochloride Tablets, DTXCID501389266, 255-219-6, Namenda, Ebixa, memantine.HCl, Memantine (hydrochloride), UNII-JY0WD0UA60, 3,5-dimethyladamantan-1-amine;hydrochloride, Memantine hydrochloride [USAN], Tricyclo[3.3.1.13,7]decan-1-amine, 3,5-dimethyl-, hydrochloride, 3,5-dimethyladamantan-1-aminium chloride, MLS001332605, 3,5-Dimethyl-1-aminoadamantane hydrochloride, (3,5-Dimethyl-1-adamantyl)amine hydrochloride, 3,5-dimethyltricyclo(3.3.1.1(3,7))decan-1-amine hydrochloride, MFCD00214336, 1,3-Dimethyl-5-adamantanamine HCl, 41100-52-1 (HCl), Mantine, Ebixza, 3,5-Dimethyltricyclo(3.3.1.1(sup 3,7))decan-1-amine hydrochloride, 3,5-dimethyladamantanylamine, chloride, Tricyclo(3.3.1.1(sup 3,7))decan-1-amine, 3,5-dimethyl-, hydrochloride, 3,5-Dimethyl-1-adamantylamine, SMR000875213, SR-01000075458, SUN Y7017, EINECS 255-219-6, Namenda (TN), Memary (TN), NSC 102290, SCHEMBL3053, CHEMBL1699, MLS001332606, SPECTRUM1501121, Rac-(3S,5S)-3,5-Bis(trideuteriomethyl)adamantan-1-amine hydrochloride, HY-B0365A, MSK10370A, Memantine hydrochloride (Namenda), NMI-131, HMS1571C17, HMS1921H03, HMS5080J19, Pharmakon1600-01501121, Memantine hydrochloride (JAN/USP), PXB71318, 3,5-Dimethylamantadine hydrochloride, MEMANTINE HYDROCHLORIDE [MI], Tox21_500861, AC-559, CCG-39018, HB0407, MEMANTINE HYDROCHLORIDE [JAN], MRZ-2/145, NSC757843, s2043, SBB003390, AKOS015889460, BCP9000253, FM05692, LP00861, MEMANTINE HYDROCHLORIDE [MART.], NC00680, MEMANTINE HYDROCHLORIDE [USP-RS], MEMANTINE HYDROCHLORIDE [WHO-DD], NCGC00094186-01, NCGC00094186-02, NCGC00094186-03, NCGC00261546-01, AS-13331, BM164662, MEMANTINE HYDROCHLORIDE [EMA EPAR], ST088119, 3,5-dimethyladamantan-1-aminehydrochloride, D3608, EU-0100861, Memantine hydrochloride - Bio-X trade mark, MEMANTINE HYDROCHLORIDE [ORANGE BOOK], NS00088181, SW060653-4, 1-amino-3,5-dimethyl-adamantane hydrochloride, 3,5-dimethyladamantan-1-amine hy-drochloride, D04905, EN300-123026, M 9292, MEMANTINE HYDROCHLORIDE [USP MONOGRAPH], SR-01000075458-1, SR-01000075458-3, SR-01000075458-8, Q27133218, Z1551429722, Tricyclo(3.3.1.1(3,7))decan-1-amine, 3,5-dimethyl-, hydrochloride, Tricyclo[3.3.1.13,7]decan-1-amine, 3,5-dimethyl-, hydrochloride (1:1) (CA INDEX NAME), 1-Amino-3,5-dimethyladamantane . HCl, 3,5-Dimethyl-1-aminoadamantane . HCl, Memantine . hydrochloride, 1-Amino-3,5-dimethyladamantane hydrochloride, 3,5-Dimethyltricyclo[3.3.1.13.7]decan-1-amine hydrochloride, 3,5-Dimethyl-1-adamantanamine hydrochloride, Memantine HCl, 3,5-Dimethyl-1-adamantanamine hydrochloride, 3,5-Dimethyl-amantadine hydrochloride, 3,5-Dimethyltricyclo[3.3.1.1³,⁷]decan-1-amine hydrochloride, 1-Amino-3,5-dimethyladamantane hydrochloride, Memantine Hydrochloride, 3,5-Dimethyl-1-adamantanamine hydrochloride

Akatinol is a synthetic derivative of adamantane and functions as a low- to moderate-affinity, uncompetitive antagonist of the N-methyl-D-aspartate (NMDA) receptor.
Akatinol is primarily used in the management of moderate to severe Alzheimer’s disease, where it helps regulate abnormal glutamatergic activity in the brain, thereby reducing excitotoxicity and slowing neurodegeneration.

Akatinol is typically supplied as a white to off-white crystalline powder, freely soluble in water, with the molecular formula C₁₂H₂₁N·HCl and a molecular weight of 215.76 g/mol.
Unlike cholinesterase inhibitors, memantine does not rely on boosting acetylcholine levels but instead modulates glutamate signaling, which plays a critical role in learning and memory.
Clinically, Akatinol has been shown to improve cognitive function, daily living activities, and global clinical status in some patients, with a favorable tolerability profile and fewer side effects compared to other Alzheimer’s therapies.

Akatinol is an NMDA receptor antagonist that works by regulating the activity of glutamate, a neurotransmitter involved in learning and memory.
Akatinol helps improve cognitive function and daily living activities in individuals suffering from Alzheimer’s, making it easier for them to engage in everyday tasks.

Akatinol is a synthetic adamantane derivative that acts as a low- to moderate-affinity, uncompetitive antagonist of the N-methyl-D-aspartate (NMDA) receptor, a subtype of glutamate receptor in the central nervous system.
By selectively blocking excessive and sustained activation of NMDA receptors while sparing normal synaptic transmission, Akatinol helps reduce excitotoxicity—a pathological process implicated in neurodegenerative diseases such as Alzheimer’s disease.

Akatinol is most commonly prescribed for the treatment of moderate to severe Alzheimer’s dementia, either as monotherapy or in combination with cholinesterase inhibitors like donepezil, to improve cognitive function, behavioral symptoms, and activities of daily living.
Unlike traditional cholinesterase inhibitors, which enhance cholinergic neurotransmission, memantine targets the glutamatergic system, addressing a different aspect of Alzheimer’s pathophysiology.

Akatinol is typically supplied as a white to off-white crystalline powder, freely soluble in water, with the molecular formula C₁₂H₂₁N·HCl and molecular weight 215.76 g/mol.
Clinically, memantine is well absorbed orally, exhibits minimal protein binding, and is excreted largely unchanged in the urine, with a half-life of approximately 60–80 hours, allowing for convenient once- or twice-daily dosing.

Akatinol's safety profile is considered favorable, with side effects generally mild and including dizziness, headache, constipation, and confusion in some patients.
Beyond Alzheimer’s disease, research has explored potential applications of memantine in Parkinson’s disease, vascular dementia, Huntington’s disease, neuropathic pain, depression, and autism spectrum disorders, although such uses remain largely investigational.
Overall, Akatinol represents an important therapeutic agent in neuropharmacology due to its unique mechanism of action, favorable tolerability, and role in mitigating excitotoxic neuronal damage.

Market Overview of Akatinol:
The global Akatinol market has grown steadily over the last decade, driven primarily by the increasing prevalence of Alzheimer’s disease and dementia in aging populations.
In 2023, the market was valued at approximately USD 1.2 billion, and forecasts suggest expansion to nearly USD 1.9 billion by 2032–2033, with a compound annual growth rate (CAGR) of around 5–6%. 

North America currently dominates due to strong healthcare infrastructure, high diagnosis rates, and reimbursement support, while Europe represents the second largest market, benefiting from large elderly populations and established dementia care programs.
The Asia-Pacific region is emerging as the fastest-growing market, particularly in China, India, and Japan, as healthcare access improves and awareness of Alzheimer’s therapies increases.

Growth is fueled by several factors: the rising incidence of dementia worldwide, the introduction of generic formulations following patent expirations, and the growing availability of memantine in both retail and online pharmacies.
In addition, combination therapies—particularly fixed-dose combinations of memantine with donepezil—have gained clinical traction, offering enhanced outcomes for patients and driving demand.
However, the market faces challenges such as price erosion due to generic competition, variability in reimbursement policies, and the limited scope of memantine’s approved indications, as its efficacy is largely confined to moderate-to-severe Alzheimer’s disease rather than early-stage dementia.

The competitive landscape is diverse, including multinational pharmaceutical companies such as Merz, Allergan/AbbVie, Eisai, and Teva, as well as numerous regional and generic manufacturers.
While brand formulations maintain a presence in developed markets, generic versions dominate overall market volume, making accessibility greater but compressing profit margins. 
Companies are increasingly focusing on novel delivery systems (e.g., extended-release tablets, patient-friendly dosing regimens) and on exploring off-label or investigational uses (e.g., Parkinson’s disease, neuropathic pain, depression) to expand market potential.

Looking ahead, opportunities lie in emerging economies, where healthcare investment is rising, and in the development of combination therapies and adjunctive treatments that may extend memantine’s therapeutic reach. 
The global shift toward aging populations ensures sustained demand, positioning Akatinol as a critical therapy in the neurodegenerative disease market, even as new-generation Alzheimer’s treatments are introduced.

Uses of Akatinol:
Akatinol blocks the effects of excessive levels of glutamate that may lead to neuronal dysfunction.
Akatinol is under investigation for the treatment of Alzheimer's disease, but there has been no clinical support for the prevention or slowing of disease progression.
Akatinol is a prescription medicine used for the treatment of moderate to severe dementia in people with Alzheimer’s disease.

Akatinol is primarily used in the treatment of moderate to severe Alzheimer’s disease, where it helps reduce abnormal glutamatergic activity in the brain by acting as an uncompetitive NMDA receptor antagonist, thereby slowing excitotoxic neuronal damage and supporting cognitive function.
Akatinol is often prescribed as monotherapy or in combination with acetylcholinesterase inhibitors (such as donepezil) to improve memory, attention, daily living activities, and behavioral symptoms in dementia patients.

Beyond Alzheimer’s disease, Akatinol has been investigated for other neurological and psychiatric conditions, including vascular dementia, Parkinson’s disease, Huntington’s disease, neuropathic pain, depression, autism spectrum disorders, and migraine prophylaxis, though most of these remain experimental or off-label.
In clinical practice, Akatinol's favorable tolerability and safety profile, along with oral availability and long half-life, make it a widely used therapeutic option for managing neurodegeneration-related symptoms and enhancing patients’ quality of life.

Akatinol is most widely recognized for its use in the management of moderate to severe Alzheimer’s disease, where it improves cognitive function, daily living activities, and behavioral symptoms by reducing glutamate-induced excitotoxicity through selective, uncompetitive antagonism of the NMDA receptor.
Akatinol is often prescribed as monotherapy or in combination therapy with acetylcholinesterase inhibitors such as donepezil, producing additive benefits in patients with dementia. 

In clinical practice, memantine has proven particularly valuable for patients who do not tolerate or respond adequately to cholinesterase inhibitors alone, offering improvements in memory, attention, orientation, and social interaction while helping reduce caregiver burden. 
Beyond its approved use in Alzheimer’s disease, Akatinol has been studied across a broad spectrum of neurological and psychiatric disorders.

In vascular dementia, Akatinol has shown potential for slowing cognitive decline linked to cerebrovascular damage, while in Parkinson’s disease it may provide symptomatic relief of dementia and improve motor fluctuations.
In Huntington’s disease, memantine has been evaluated as a modulator of glutamate toxicity contributing to neuronal loss.

Akatinol's role has also been explored in neuropathic pain, where excessive NMDA receptor activation is implicated, and in migraine prophylaxis due to its ability to stabilize glutamatergic transmission.
Investigational and off-label research further extends to major depressive disorder, obsessive-compulsive disorder, autism spectrum disorders, and attention deficit hyperactivity disorder (ADHD), with varying levels of evidence supporting its potential benefits.

While most of these uses remain experimental, the consistent interest in memantine stems from its unique mechanism of action, long half-life, oral availability, and relatively favorable safety profile compared to other NMDA antagonists.
Overall, Akatinol serves as a cornerstone drug in Alzheimer’s management while continuing to attract research attention as a possible therapeutic agent across multiple neurodegenerative and neuropsychiatric conditions.

Benefits of Akatinol:
Akatinol offers several important therapeutic benefits, particularly in the management of moderate to severe Alzheimer’s disease.
Akatinol's primary advantage lies in its unique mechanism of action as an uncompetitive NMDA receptor antagonist, which allows it to selectively block pathological overactivation of glutamatergic signaling while preserving normal synaptic activity.

This helps reduce excitotoxicity, a key contributor to neuronal damage, thereby slowing disease progression and supporting cognitive and functional abilities.
Clinically, memantine has been shown to improve memory, orientation, language, and attention, while also easing behavioral and psychological symptoms such as agitation, aggression, and hallucinations.

An additional benefit is Akatinol's ability to reduce caregiver burden, since treated patients often show better independence in daily activities.
Compared with other Alzheimer’s drugs, memantine is generally well tolerated, with fewer gastrointestinal side effects than cholinesterase inhibitors, and it can be safely combined with them for additive benefits.

Akatinol's long half-life (60–80 hours) supports convenient once- or twice-daily dosing, improving adherence in elderly patients.
Beyond Alzheimer’s disease, memantine shows potential benefits in vascular dementia, Parkinson’s disease dementia, Huntington’s disease, neuropathic pain, depression, and autism spectrum disorders, highlighting its broader neuroprotective potential.
Collectively, these benefits make Akatinol a valuable therapeutic option that not only improves cognitive and behavioral outcomes in dementia but also enhances quality of life for both patients and caregivers.

Production of Akatinol:
Akatinol is produced through a multi-step synthetic process starting from 1-adamantylamine, a derivative of adamantane.
The synthesis generally involves selective functionalization of the adamantane framework to introduce the primary amine, which then undergoes N-methylation to form memantine (1-amino-3,5-dimethyladamantane).

This base compound is subsequently reacted with hydrogen chloride (HCl), typically in anhydrous conditions, to yield the stable crystalline hydrochloride salt.
Careful control of temperature, solvents, and reaction stoichiometry is essential to ensure high yield, purity, and prevention of by-products.

The final product, Akatinol, is usually purified by recrystallization, filtration, and drying under controlled conditions to achieve pharmaceutical-grade specifications suitable for tablet or capsule formulations.
Industrial production follows Good Manufacturing Practices (GMP) standards, and quality control includes testing for identity, purity, residual solvents, particle size distribution, and stability.
This synthetic route allows for scalable, consistent production, ensuring reliable global supply for use in Alzheimer’s disease therapies.

History of Akatinol:
Akatinol has a history that stretches back several decades, beginning with the exploration of adamantane derivatives in the 1960s for their potential antiviral and central nervous system (CNS) effects.
Structurally related to amantadine, which was originally used as an antiviral and later for Parkinson’s disease, memantine was first synthesized in the early 1960s in Germany by Eli Lilly & Co. researchers, who were investigating adamantane-based compounds for therapeutic use.

In the 1970s, studies in Eastern Europe, particularly in the former Soviet Union, evaluated memantine for neurological disorders such as spasticity and movement disorders, where it showed some beneficial effects.
However, Akatinol was not until the 1980s and 1990s that its potential role in Alzheimer’s disease began to emerge, as scientists linked glutamatergic excitotoxicity with neurodegeneration and identified memantine as a selective NMDA receptor antagonist that could protect neurons from glutamate-mediated damage.

The drug was first approved in Germany in 1989 for dementia treatment, marketed under the trade name Akatinol Memantine by Merz.
After accumulating clinical trial evidence, memantine gained broader recognition in the early 2000s, becoming the first NMDA receptor antagonist approved for moderate to severe Alzheimer’s disease.

In 2002, Akatinol received approval from the European Medicines Agency (EMA), followed by U.S. FDA approval in 2003, where it was marketed by Forest Laboratories (now part of AbbVie) under the brand name Namenda.
Since then, memantine has become a standard therapy worldwide for Alzheimer’s patients, and with patent expirations in the 2010s, generic versions have become widely available, improving accessibility.
Today, Akatinol remains an important drug in dementia management, while research continues to explore its applications in other neuropsychiatric and neurodegenerative disorders.

Handling and Storage of Akatinol:

Handling:
Avoid contact with eyes, skin, and clothing.
Prevent formation of dust or aerosols.

Handle only in well-ventilated areas or under local exhaust.
Use appropriate PPE (gloves, goggles, lab coat).
Wash hands thoroughly after handling and before eating, drinking, or smoking.

Storage:
Store in a tightly closed container in a cool, dry, well-ventilated place.
Protect from heat, moisture, and direct sunlight.

Keep away from strong oxidizers and strong acids.
Recommended storage temperature: ambient (15–25 °C).

Stability and Reactivity of Akatinol:

Stability:
Stable under normal temperatures and pressures when stored properly.

Reactivity:
May react with strong oxidizing agents; prolonged exposure to moisture can affect quality.

Hazardous Decomposition Products:
Nitrogen oxides (NOx), carbon monoxide (CO), and carbon dioxide (CO₂) upon combustion/thermal decomposition.

Incompatibilities:
Strong oxidizers, strong acids, and reducing agents.

First Aid Measures of Akatinol:

Inhalation:
Move person to fresh air.
If symptoms such as cough, dizziness, or respiratory irritation occur, seek medical attention.

Skin Contact:
Wash immediately with plenty of water and mild soap.
Remove contaminated clothing.
Get medical advice if irritation persists.

Eye Contact:
Rinse cautiously with water for at least 15 minutes, lifting eyelids occasionally.
Remove contact lenses if present and easy to do.
Seek medical attention if irritation develops.

Ingestion:
Rinse mouth with water.
Do not induce vomiting.

Give water if conscious.
Seek medical advice if unwell or if large amounts are ingested.

Firefighting Measures of Akatinol:

Extinguishing Media:
Use water spray, foam, dry chemical, or CO₂.
Avoid high-pressure water jets.

Specific Hazards:
Product is combustible; dust may form explosive mixtures with air if dispersed.
Thermal decomposition may release toxic/irritating fumes.

Protective Equipment:
Firefighters should wear self-contained breathing apparatus (SCBA) and full protective gear.
Cool exposed containers with water spray.
Prevent runoff from entering drains or waterways.

Accidental Release Measures of Akatinol:

Personal Precautions:
Avoid dust formation.
Ensure adequate ventilation.

Wear gloves, goggles, protective clothing; use a respirator if dust concentrations exceed exposure limits.
Eliminate ignition sources.

Spill Cleanup:
Sweep up or vacuum with HEPA-filtered equipment to avoid dust generation.
Collect in labeled containers for disposal according to regulations.
Wash contaminated surfaces with water and mild detergent.

Environmental Precautions:
Prevent bulk releases from entering drains, sewers, or surface waters.
Dispose of material according to local regulations.

Exposure Controls / Personal Protective Equipment of Akatinol:

Engineering Controls:
Use local exhaust or general ventilation to minimize dust exposure.
Provide eyewash and safety shower in handling areas.

Respiratory Protection:
Normally not required under adequate ventilation; use a NIOSH-approved particulate respirator if airborne dust levels exceed limits.

Hand Protection:
Chemical-resistant gloves (nitrile, neoprene, or equivalent).

Eye/Face Protection:
Safety goggles; use a face shield if handling large quantities or if dust clouds may form.

Skin/Body Protection:
Laboratory coat or protective clothing to minimize exposure.

Hygiene Measures:
Do not eat, drink, or smoke while handling.
Wash hands and face thoroughly after use.
Launder contaminated clothing before reuse.

Identifiers of Akatinol:
IUPAC Name: 3,5-dimethyladamantan-1-amine hydrochloride
CAS Number: 41100-52-1
EC (EINECS) Number: 255-219-5
Molecular Formula: C₁₂H₂₂ClN
Molecular Weight: 215.76 g/mol
InChI: InChI=1S/C12H21N.ClH/c1-8-4-9-2-11(5-8)12(10(9)3-13,6-11,7-11);1H
InChI Key: BATHURMZQRBWIM-UHFFFAOYSA-N
SMILES: CC12CC3CC(CC(C1)C(C2)(C3)N)Cl
PubChem CID: 657317
DrugBank ID: DB01043
UN Number (Transport): Not classified as hazardous for transport (not a dangerous good).
ATC Code: N06DX01 (other anti-dementia drugs)

CAS Number: 41100-52-1
EC (EINECS) Number: 255-219-5
Molecular Formula: C₁₂H₂₂ClN
Molecular Weight: 215.76 g/mol
InChI: InChI=1S/C12H21N.ClH/c1-8-4-9-2-11(5-8)12(10(9)3-13,6-11,7-11);1H
InChI Key: BATHURMZQRBWIM-UHFFFAOYSA-N
SMILES: CC12CC3CC(CC(C1)C(C2)(C3)N)Cl
PubChem CID: 657317
ChemSpider ID: 57158
DrugBank ID: DB01043
KEGG ID: D07665
ChEMBL ID: CHEMBL658
UNII (FDA Unique Ingredient Identifier): J4KN216RRN
ATC Code: N06DX01 (Anti-dementia drug, NMDA receptor antagonist)
Regulatory Status: Approved drug (FDA, EMA, WHO Essential Medicines List)
UN Number (Transport): Not classified as a dangerous good under UN regulations.

Properties of Akatinol:
Molecular Weight: 215.76 g/mol
Hydrogen Bond Donor Count: 2
Hydrogen Bond Acceptor Count: 1
Rotatable Bond Count: 0
Exact Mass: 215.1440774 Da
Monoisotopic Mass: 215.1440774 Da
Topological Polar Surface Area: 26 Ų
Heavy Atom Count: 14
Complexity: 240
Isotope Atom Count: 0
Defined Atom Stereocenter Count: 0
Undefined Atom Stereocenter Count: 2
Defined Bond Stereocenter Count: 0
Undefined Bond Stereocenter Count: 0
Covalently-Bonded Unit Count: 2
Compound Is Canonicalized: Yes

CAS Number: 41100-52-1
EC / EINECS Number: 255-219-6

PubChem CID: 181458
Chemical Formula: C12H21N·HCl
Molecular Weight: ~215.76 g/mol
Appearance: White crystalline powder or solid
Solubility: Soluble in water; e.g., up to 100 mg/mL
Stability & Incompatibilities: Avoid oxidizing agents; 
decomposition may produce CO, CO₂, NOₓ, and HCl
CAS / EC Numbers: 41100-52-1 / 255-219-6
Formula / Mol. Wt.: C12H21N·HCl / ~215.76 g/mol

Appearance: White crystalline powder
Solubility: Water-soluble (e.g., 100 mg/mL)
Stability: Stable; avoid oxidizers; dust explosion risk
Mechanism: NMDA receptor antagonist
Use: Alzheimer’s therapy
Pharmacokinetics: Oral bioavailability 100%; long half-life
Handling: Store properly; use PPE; avoid dust and oxidizers