(R)-Baclofen

(R)-Baclofen Uses, Dosage, Side Effects, Food Interaction and all others data.

(R)-Baclofen, or STX209, is the R-enantiomer of baclofen. It is believed to be a selective gamma-amino butyric acid type B receptor agonist, and has been investigated as a treatment for autism spectrum disorder and fragile X syndrome in randomized, double blind, placebo controlled trials. It has also been investigated as a treatment for spasticity due to multiple sclerosis and spinal cord injury. (R)-Baclofen was investigated as a treatment for gastroesophageal reflux disease (GERD); however, with disappointing results.

(R)-Baclofen
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	(R)-Baclofen
Generic	Arbaclofen
Arbaclofen Other Names	(R)-Baclofen, Arbaclofen
Type
Formula	C₁₀H₁₂ClNO₂
Weight	Average: 213.661 Monoisotopic: 213.05565634
Groups	Investigational
Therapeutic Class
Manufacturer
Available Country
Last Updated:	September 19, 2023 at 7:00 am

Uses

Investigated in clinical trials as a potential treatment for spasticity in multiple sclerosis, autism spectrum disorder, and social withdrawal in fragile X syndrome.

How (R)-Baclofen works

(R)-Baclofen, or R-baclofen, acts upstream of the mGluR5 receptor to increase inhibitory neurotransmission. It is the isomer of baclofen which harbors antispastic activity.

Elimination Route

Unlike baclofen, absorption of arbaclofen is not limited to the upper small intestine. (R)-Baclofen can also be absorbed in the lower small intestine and the colon, allowing for the development of sustained release formulations.

Clearance

Blood clearance of an IV bolus of R-baclofen in rats, monkeys, and dogs, resulted in a half life of 1.6-3.4hours, in one study. Total blood clearance was reported to be 0.51±0.13L/h/kg in rats, 0.31±0.11L/h/kg in monkeys, and 0.24±0.01L/h/kg in dogs. (2)