Indantadol

An overview of the drug Indantadol

Indantadol
INN
Drug class
Routes of administration
Pregnancy category
Bioavailability
Metabolism
Elimination half-life
Excretion
Legal status
CAS Number
PubChem
DrugBank
ChemSpider
KEGG

Indantadol is a pharmaceutical compound that has been investigated for its potential use as an analgesic. It is known for its dual mechanism of action, which includes both NMDA receptor antagonism and monoamine oxidase inhibition. This unique combination of effects makes it a subject of interest in the treatment of chronic pain conditions.

Mechanism of Action

Indantadol functions primarily through two mechanisms:

NMDA Receptor Antagonism

Chemical structure of Indantadol

Indantadol acts as an antagonist at the NMDA receptor, which is a subtype of glutamate receptor. By inhibiting these receptors, Indantadol can reduce the excitatory neurotransmission that is often associated with chronic pain states. NMDA receptor antagonists are known to play a role in diminishing central sensitization and neuropathic pain.

Monoamine Oxidase Inhibition

In addition to its effects on NMDA receptors, Indantadol also inhibits monoamine oxidase (MAO), an enzyme responsible for the breakdown of monoamines such as serotonin, dopamine, and norepinephrine. By inhibiting MAO, Indantadol may increase the levels of these neurotransmitters in the brain, contributing to its analgesic and potentially antidepressant effects.

Pharmacokinetics

The pharmacokinetic profile of Indantadol includes its absorption, distribution, metabolism, and excretion. As with many drugs, these parameters can influence its efficacy and safety profile.

Absorption

Indantadol is typically administered orally, and its absorption can be affected by factors such as food intake and gastrointestinal pH.

Distribution

Once absorbed, Indantadol is distributed throughout the body. It is known to cross the blood-brain barrier, which is essential for its central nervous system effects.

Metabolism

Indantadol is metabolized primarily in the liver. The specific pathways and metabolites involved in its metabolism are subjects of ongoing research.

Excretion

The excretion of Indantadol occurs through renal and hepatic pathways. Understanding its excretion is important for dosing considerations, especially in patients with renal or hepatic impairment.

Clinical Applications

Indantadol has been studied for its potential use in various pain conditions, including:

Chronic Pain

Chronic pain, such as that associated with fibromyalgia or neuropathic pain, may be alleviated by the dual action of Indantadol on NMDA receptors and monoamine oxidase.

Potential Antidepressant Effects

Due to its action on monoamine levels, Indantadol may also have potential as an antidepressant, although this application requires further investigation.

Side Effects

As with any medication, Indantadol may cause side effects. Common side effects include:

• Nausea
• Dizziness
• Headache

More serious side effects, although rare, may include:

• Hypertension
• Serotonin syndrome

Related Pages

• NMDA receptor antagonist
• Monoamine oxidase inhibitor
• Chronic pain management