Baclofen
Systematic (IUPAC) name
4-amino-3-(4-chlorophenyl)-butanoic acid
Identifiers
CAS number	1134-47-0
ATC code	M03BX01
PubChem	2284
DrugBank	APRD00551
Chemical data
Formula	C10H12NClO2
Mol. weight	213.661 g/mol
Pharmacokinetic data
Bioavailability	?
Protein binding	30%
Metabolism	?
Half life	1.51 hours
Excretion	?
Therapeutic considerations
Pregnancy cat.	? Image File history File links Download high-resolution version (666x610, 7 KB) structure of Baclofen created with ChemDraw File links The following pages on the English Wikipedia link to this file (pages on other projects are not listed): Baclofen ... IUPAC nomenclature is a systematic way of naming organic chemical compounds. ... CAS registry numbers are unique numerical identifiers for chemical compounds, polymers, biological sequences and alloys. ... The Anatomical Therapeutic Chemical Classification System is used for the classification of drugs. ... A section of the Anatomical Therapeutic Chemical Classification System. ... PubChem is a database of chemical molecules . ... DrugBank is a database available at the University of Alberta that provides information about thousands of products. ... A chemical formula (also called molecular formula) is a concise way of expressing information about the atoms that constitute a particular chemical compound. ... General Name, Symbol, Number carbon, C, 6 Chemical series nonmetals Group, Period, Block 14, 2, p Appearance black (graphite) colorless (diamond) Atomic mass 12. ... This article is about the chemistry of hydrogen. ... General Name, Symbol, Number nitrogen, N, 7 Chemical series nonmetals Group, Period, Block 15, 2, p Appearance colorless Atomic mass 14. ... General Name, Symbol, Number chlorine, Cl, 17 Chemical series halogens Group, Period, Block 17, 3, p Appearance yellowish green Atomic mass 35. ... General Name, Symbol, Number oxygen, O, 8 Chemical series Nonmetals, chalcogens Group, Period, Block 16, 2, p Appearance colorless (gas) very pale blue (liquid) Atomic mass 15. ... The molecular mass of a substance (less accurately called molecular weight and abbreviated as MW) is the mass of one molecule of that substance, relative to the unified atomic mass unit u (equal to 1/12 the mass of one atom of carbon-12). ... In pharmacology, bioavailability is used to describe the fraction of an administered dose of medication that reaches the systemic circulation, one of the principal pharmacokinetic properties of drugs. ... Many drugs are bound to Blood plasma proteins. ... Overview of the citric acid cycle The citric acid cycle, one of the central metabolic pathways in aerobic organisms. ... The elimination half-life of a drug (or any xenobiotic agent) refers to the timecourse necessary for the quantity of the xenobiotic agent in the body (or plasma concentration) to be reduced to half of its original level through various elimination processes. ... Excretion is the process of eliminating waste products of metabolism and other materials that are of no use. ... The pregnancy category of a pharmaceutical agent is an assessment of the risk of fetal injury due to the pharmaceutical, if it is used as directed by the mother during pregnancy. ...
Legal status
Routes	Oral, intrathecal

Baclofen (brand names Kemstro® and Lioresal®) is a derivative of gamma-aminobutyric acid, and is an agonist specific to mammalian but not fruit fly (Drosophila) GABA_B receptors[1][2]. It is used for the treatment of spastic movement, especially in instances of spinal cord injury, spastic diplegia and multiple sclerosis. Its beneficial effects result from actions at spinal and supraspinal sites. Baclofen can also be used to treat hiccups. The regulation of therapeutic goods, that is drugs and therapeutic devices, varies by jurisdiction. ... In pharmacology and toxicology, a route of administration is the path by which a drug, fluid, poison or other substance is brought into contact with the body 1. ... Intrathecal: Delivered into the spinal canal (intrathecal space surrounding the spinal cord), as in a spinal anaesthesia. ... Gamma-aminobutyric acid (usually abbreviated to GABA) is an inhibitory neurotransmitter found in the nervous systems of widely divergent species. ... Agonists An agonist is a substance that binds to a receptor and triggers a response in the cell. ... GABAB receptors (GABABR) are metabotropic transmembrane receptors that are linked via G-proteins to potassium channels (Chen et al. ... Spasticity is a disorder of the bodys motor system in which certain muscles are continuously contracted. ... The Spinal cord nested in the vertebral column. ... Spastic diplegia refers to a type of cerebral palsy that is a neuromuscular condition of hypertonia and spasticity in the muscles of the lower extremities, usually those of the legs, hips and pelvis. ... A hiccup is an involuntary spasm of the diaphragm. ...

Description of compound

Baclofen is a white to off-white, odorless or practically odorless crystalline powder, with a molecular weight of 213.66 g/mol. It is slightly soluble in water, very slightly soluble in methanol, and insoluble in chloroform. Crystal (disambiguation) Insulin crystals A crystal is a solid in which the constituent atoms, molecules, or ions are packed in a regularly ordered, repeating pattern extending in all three spatial dimensions. ... The molecular mass of a substance (less accurately called molecular weight and abbreviated as MW) is the mass of one molecule of that substance, relative to the unified atomic mass unit u (equal to 1/12 the mass of one atom of carbon-12). ... It has been suggested that this article or section be merged with Solution. ... Methanol, also known as methyl alcohol, wood alcohol or wood spirits, is a chemical compound with chemical formula CH3OH. It is the simplest alcohol, and is a light, volatile, colourless, flammable, poisonous liquid with a distinctive odor that is somewhat milder and sweeter than ethanol (ethyl alcohol). ... Chloroform, also known as trichloromethane and methyl trichloride, is a chemical compound with formula CHCl3. ...

Routes of administration

Baclofen can be administered either orally or intrathecally (directly into the spinal fluid). Intrathecal administration is often indicated in spasticity patients, as very little of the oral dose actually reaches the spinal fluid.

Intrathecal administration is particularly used in patients with multiple sclerosis who have severe painful spasms which are not controllable by oral baclofen, or patients with spastic diplegia in whom managament of spasticity is made easier by regular self-ministering of the drug through its pump. A test dose is given to assess the effect, and if successful a chronic intrathecal catheter is inserted and connected to a computer-controlled implanted pump. The reservoir in the pump can be replenished by percutaneous injection. These pump systems are quite sophisticated and expensive, so careful patient selection is required. Intrathecal: Delivered into the spinal canal (intrathecal space surrounding the spinal cord), as in a spinal anaesthesia. ... Spastic diplegia refers to a type of cerebral palsy that is a neuromuscular condition of hypertonia and spasticity in the muscles of the lower extremities, usually those of the legs, hips and pelvis. ... In surgery, percutaneous pertains to any medical procedure where access to inner organs or other tissue is done via needle-puncture of the skin, rather than by using an open approach where inner organs or tissue are exposed (typically with the use of a scalpel). ...

History

Historically Baclofen was designed to be a drug for epilepsy in the 1920’s, and was derived from GABA. The effect on epilepsy was disappointing but it was found that in certain patients spasticity decreased. Baclofen was and is still given orally with variable effects. In the severely affected children, the oral dose is so high that side effects appear and the treatment loses its benefit. How and when Baclofen came to be used in the spinal sac is not really clear but this is now an established method for the treatment of spasticity in many conditions. Gaba may refer to: Gabâ or gabaa (Philippines), the concept of negative karma of the Cebuano people GABA, the gamma-amino-butyric acid neurotransmitter GABA receptor, in biology, receptors with GABA as their endogenous ligand Gaba 1 to 1, an English conversational school in Japan Marianne Gaba, a US model...

How Baclofen works

Baclofen affects the spinal cord, which is the main connection between the brain and the rest of the body. The spinal cord plays a role as a reflex system that functions as a feedback loop. Our most obvious reflex is the withdrawal of our appendages from extreme heat. Baclofen works on this reflex circuit's Renshaw cells. These cells are very sensitive to a neurotransmitter produced by the nervous system, GABA (gamma-amino-butyric-acid), which slows this reflex circuit down. Baclofen mimics the effects of GABA. The dose of intrathecal Baclofen necessary to slow down the reflex circuit is variable but is generally one thousand times (three orders of magnitude) smaller than the oral dose. Gaba may refer to: Gabâ or gabaa (Philippines), the concept of negative karma of the Cebuano people GABA, the gamma-amino-butyric acid neurotransmitter GABA receptor, in biology, receptors with GABA as their endogenous ligand Gaba 1 to 1, an English conversational school in Japan Marianne Gaba, a US model...

Pharmacokinetics

The drug is rapidly absorbed after oral administration and is widely distributed throughout the body. Biotransformation is low and the drug is predominantly excreted in the unchanged form by the kidneys.

Overdose

Symptoms of a baclofen overdose include vomiting, weakness, drowsiness, slow breathing, seizures, unusual pupil size, and coma. A drug overdose occurs when a chemical substance (i. ... This article or section does not cite its references or sources. ... Comatose redirects here. ...

Underdose

Symptoms of baclofen underdose (via intrathecal delivery) include itching, hypotension, paresthesias, fever, and altered mental state (including delusions and hallucinations).

See also

• Intrathecal baclofen pump

Intrathecal pump is a medical device used to delivery very small quantities of medications to the spinal fluid. ...

References

• Intrathecal Baclofen Therapy Cleveland Clinic Information Center. 15 June 2001.

External links

• Patient Site for Intrathecal Baclofen Treatment for Spasticity as a result of Cerebral Palsy

• Links to external chemical sources