What is the mechanism of action for memantine?

Memantine is a clinically useful drug in many neurological disorders, including Alzheimer’s disease. The principal mechanism of action of memantine is believed to be the blockade of current flow through channels of N-methyl-d-aspartate (NMDA) receptors–a glutamate receptor subfamily broadly involved in brain function.

How does memantine work in the body?

Memantine works by blocking the receptors in the brain that glutamate would normally bind to. This decreases the harmful effect of glutamate in the brain and may help improve your symptoms of dementia.

How does memantine block NMDA?

While excessive levels of glutamate result in neurotoxicity, in part through the over-activation of NMDARs, memantine—as a partial NMDAR antagonist, blocks the NMDA glutamate receptors to normalize the glutamatergic system and ameliorate cognitive and memory deficits.

How does Namenda work in the brain?

It does not cure Alzheimer’s disease, but it may improve memory, awareness, and the ability to perform daily functions. This medication works by blocking the action of a certain natural substance in the brain (glutamate) that is believed to be linked to symptoms of Alzheimer’s disease.

What receptor does memantine use?

Memantine is an antagonist of the NMDA (N-Methyl-D-Aspartate)-receptor subtype of glutamate receptor. It is used to slow the neurotoxicity thought to be involved in Alzheimer disease and other neurodegenerative diseases.

How is memantine absorbed?

Memantine is well absorbed from the gastrointestinal tract after oral administration, and its absorption is unaffected by food (Forest Laboratories 2003). It reaches a maximum plasma concentration (Cmax) after a single dose in 3–7 hours, and it has a plasma half-life of about 60–80 hours.

What does memantine 5mg look like?

Memantine 5mg tablets are white to off white coloured, approximately 10 x 4 mm, capsule shaped, biconvex, film-coated tablets, debossed with “5” on one side and plain on the other side.

What color is memantine?

00205287: This medicine is a white, oblong, film-coated, tablet imprinted with “ZF 40”.

Is memantine an antagonist?

Memantine is a moderate affinity, uncompetitive NMDA receptor antagonist with strong voltage-dependency and fast kinetics.

Is memantine a channel blocker?

From whole-cell and single-channel recording experiments, the mechanism of action of memantine is deduced to be open-channel block, similar to MK-801; however, unlike MK-801, memantine is well tolerated clinically.

What is the difference between Namenda and memantine?

Namenda (also called Memantine) was approved by the FDA in 2003 for use in people with “moderate to severe” Alzheimer’s disease or other types of dementia.

What type of inhibitor is memantine?

11Cholinesterase inhibitors and memantine for dementia. The three cholinesterase inhibitors, donepezil, rivastigmine, galantamine, and the NMDA receptor antagonist, memantine, are currently the only effective licensed treatments for dementia (O’Brien 2017).