Baclofen: profile and news






Intrathecal Catheter Granuloma Associated with Isolated Baclofen ...  Feb 21, 2006
Intrathecal (IT) baclofen is an effective management strategy for controlling spasticity in patients unresponsive to maximal oral therapy. ... - Anesthesia & Analgesia (subscription),

Brave step forward  Mar 5, 2006
Menges said she had heard about the Medtronic intrathecal baclofen therapy, so she set up an appointment in late January with York Neurosurgical Associates in ... - York Daily Record,

CVS faces pharmacy reviews  Feb 9, 2006
And a patient at a Brockton CVS received Baclofen pills, used to treat symptoms of multiple sclerosis, that were twice as strong as prescribed. ... - Boston Globe,

SELF-DIAGNOSIS OF SINUS HEADACHE OFTEN AN ERROR  Jan 26, 2006
...immobilize a person. Trihexyphenidyl and baclofen are two medicines that might alleviate your muscle cramping. Botox, the diluted ... - Charlotte Sun-Herald,

A Horrific Case of Hiccups, a Novel Treatment  Jan 9, 2006
...had essentially been tried on everything," Dr. Payne said, including a major tranquilizer, chlorpromazine; a muscle relaxant, baclofen; and metoclopramide ... - New York Times,

XenoPort to Release Fourth Quarter Financial Results on February 1 ...  Jan 18, 2006
...herpetic neuralgia. XenoPort has also completed two Phase 1 clinical trials of XP19986, a Transported Prodrug of R-baclofen. These ... - Yahoo! News (press release)

XenoPort Partners Asian Rights To Lead Product With Astellas  Dec 1, 2005
...pipeline. Beyond XP13512, XenoPort also continues to advance XP19986, a Transported Prodrug of the GABA-B agonist R-baclofen. Already ... - BioWorld Online (subscription),

XenoPort and Astellas Enter a License Agreement on XP13512 in ...  Nov 30, 2005
...of 2006. XenoPort has also completed an initial Phase 1 clinical trial of XP19986, a Transported Prodrug of R-baclofen. This trial ... - Yahoo! News (press release)

LePharmacy.com Distributes Award Winning ALS Documentary ...  Nov 28, 2005
...will distribute free DVD’s of an award winning documentary to their customers living with ALS who purchase low cost Rilutek, Gabapentin, Baclofen, Allegra D ... - PR Web (press release),

XenoPort to Present at the Lazard Capital Markets Life Science ...  Nov 17, 2005
...herpetic neuralgia. XenoPort has also completed an initial Phase 1 clinical trial of XP19986, a Transported Prodrug of R-baclofen. This ... - Yahoo! News (press release)

ALS Patients Look To New Treatment  Oct 1, 2005
Eventually, they won't work at all. Baclofen helps control the symptoms of ALS. ... Surgeons implant a small baclofen-filled pump in the abdomen. ... - Pittsburgh Channel.com,

Cutting into alcoholism  Oct 6, 2005
Several other drugs, including the anticonvulsant topiramate and another drug called baclofen, also are being studied for their potential to help the alcohol ... - Louisville Courier-Journal,

Tightened nerves are common with MS  Sep 11, 2005
Spasticity can be relieved by medications such as Baclofen, a muscle-relaxant that works in the spinal cord, sedatives or Botox injections. ... - Orlando Sentinel,

Can Alcoholism Be Treated?  Sep 13, 2005
Ameisen researched the literature and came across rat studies showing that baclofen, a generic drug used to control muscle spasms, could suppress the desire to ... - BusinessWeek

Lakhs offered for busts; not a penny for poor patient  Sep 29, 2005
...and spasticity. He requires an intrathecal baclofen pump implant, which involves an expenditure of nearly Rs 2 lakh. Rajesh’s ... - The Tribune,

XenoPort Appoints Gary D. Tollefson, Former Lilly Executive, to ...  Sep 6, 2005
...of 2006. XenoPort has also completed an initial Phase 1 clinical trial of XP19986, a Transported Prodrug of R-baclofen. This trial ... - Yahoo! News (press release)

Naltrexone Treatment for Alcohol Dependency  Aug 23, 2005
...established in randomized trials with the oral administration of the craving-reducing agents naltrexone, 3 topiramate, 4 and low-dose baclofen, 5 and in an open ... - Journal of American Medical Association (subscription),

XenoPort Reports Second Quarter Financial Results  Aug 10, 2005
A Phase 1 clinical trial demonstrated that XP19986 was well absorbed and rapidly converted to the R-isomer of baclofen, and that it provided a ... - PR Newswire (press release),

Naltrexone Treatment for Alcohol Dependency—Reply  Aug 23, 2005
...alcoholism. Baclofen is a promising medication 5 and offers another potential pharmacological approach to treatment of alcoholism. ... - Journal of American Medical Association (subscription),

Anticraving Medications for Relapse Prevention: A Possible New ...  Aug 14, 2005
The GABA B agonist baclofen has also been reported to reduce cocaine use (70), and it is now the subject of a multiclinic trial. ... - RedNova.com,

Drug therapy holds promise for treating alcoholism  Aug 24, 2005
...cravings. Researchers have been testing a muscle spasm drug called baclofen to see if it discourages people from drinking alcohol. ... - Minnesota Public Radio,

When a child has a stroke  Aug 9, 2005
Because the stroke affected his muscle tone, particularly in his legs and his left hand, he receives a muscle relaxer called baclofen and Botox. ... - Pittsburgh Post Gazette,

Can Alcoholism Be Treated?  Aug 4, 2005
Ameisen researched the literature and came across rat studies showing that baclofen, a generic drug used to control muscle spasms, could suppress the desire to ... - BusinessWeek

XenoPort Announces Results from an Initial Phase 1 Clinical Trial ...  Jul 11, 2005
...(Nasdaq: XNPT - News) today announced the successful completion of an initial Phase 1 clinical trial of XP19986, a Transported Prodrug(TM) of R-baclofen. ... - Yahoo News (press release)

Medication Development for Addictive Disorders: The State of the ...  Jul 29, 2005
Baclofen, a -aminobutyric acid (GABA) B agonist (60 mg/day), has been reported to reduce the craving for cocaine in a clinical pharmacology setting (49). ... - Am J Psychiatry (subscription)

Pharmacotherapy and Pharmacogenetics of Nicotine Dependence  Jul 29, 2005
One promising compound is baclofen, a -aminobutyric acid type B receptor antagonist, which has been shown to decrease intravenous self-administration of ... - Am J Psychiatry (subscription)

'Strummin' for Bryce'  Jul 29, 2005
In the past year, he has started talking and sleeping through the night. The family owes these advances to a baclofen pump implanted in Bryce’s stomach. ... - Mesabi Daily News

Treating Drug Addicts With More Drugs  Aug 2, 2005
...have already been approved for other ailments including epilepsy, muscle cramping and nausea and fall under the names topiramate, baclofen and ondansetron. ... - Emediawire (press release)

New medications help addicts  Jul 30, 2005
Topiramate - approved to treat epilepsy - for alcoholism and cocaine addiction. Baclofen - approved for muscle tightness, cramping and spasms - for alcoholism. ... - St. Louis Post-Dispatch

XenoPort Announces Positive Results of a Phase 2b Clinical Trial ...  Aug 2, 2005
...of 2006. XenoPort has also completed an initial Phase 1 clinical trial of XP19986, a Transported Prodrug of R-baclofen. A Phase ... - PharmaLive.com (press release)

Anticraving Medications for Relapse Prevention: A Possible New ...  Jul 29, 2005
The GABA B agonist baclofen has also been reported to reduce cocaine use (70), and it is now the subject of a multiclinic trial. ... - Am J Psychiatry (subscription)

Tourette Syndrome  Jul 19, 2005
These medications may have serious side effects, so researchers are studying baclofen (Lioresal) and botulinum toxin type A (Botox) used together, as well as ... - rarediseases.about.com

Acute Akathisia Associated With Quetiapine Use  Jul 6, 2005
...haloperidol. Clonazepam (0.5 mg tid) and baclofen (10 mg tid) were added to the patient’s regimen, and the akathisia abated. Although ... - Psychosomatics (subscription)

When home remedies for hiccups fail, medicines can usually end ...  Jul 20, 2005
...remedies. Medicines have to be turned to. Chlorpromazine, omeprazole, metoclopramide and baclofen are often successfully used. In ... - Yuma Sun


Other information


Indication
For the alleviation of signs and symptoms of spasticity resulting from multiple sclerosis, particularly for the relief of flexor spasms and concomitant pain, clonus, and muscular rigidity

Pharmacology
Baclofen is a muscle relaxant and antispastic. Baclofen is useful for the alleviation of signs and symptoms of spasticity resulting from multiple sclerosis, particularly for the relief of flexor spasms and concomitant pain, clonus, and muscular rigidity. Although Baclofen is an analog of the putative inhibitory neurotransmitter gamma-aminobutyric acid (GABA), there is no conclusive evidence that actions on GABA systems are involved in the production of its clinical effects. In studies with animals, Baclofen has been shown to have general CNS depressant properties as indicated by the production of sedation with tolerance, somnolence, ataxia, and respiratory and cardiovascular depression. Baclofen is rapidly and extensively absorbed and eliminated. Absorption may be dose-dependent, being reduced with increasing doses. Baclofen is excreted primarily by the kidney in unchanged form and there is relatively large intersubject variation in absorption and/or elimination.

Mechanism Of Action
Baclofen is a direct agonist at GABAB receptors. The precise mechanism of action of Baclofen is not fully known. It is capable of inhibiting both monosynaptic and polysynaptic reflexes at the spinal level, possibly by hyperpolarization of afferent terminals, although actions at supraspinal sites may also occur and contribute to its clinical effect.

Drug Category
Muscle Relaxants; Skeletal Muscle Relaxants; GABA Agonists; ATC:M03BX01

Brand Names/Synonyms
Apo-Baclofen; Ba 34647; Baclofen; Baclon; C 34647ba; Kemstro; Lioresal; Lioresal Intrathecal; Novo-Baclofen; Nu-Baclofen; Pms-Baclofen

Dosage Forms
TABLET; INTRATHECAL INJECTION;

Absorption
Rapidly and extensively absorbed

Interactions
-->Interactions for Baclofen:
Injection

There is inadequate systematic experience with the use of baclofen injection in combination with other medications to predict specific drug-drug interactions. Interactions attributed to the combined use of baclofen injection and epidural morphine include hypotension and dyspnea.

SIDE EFFECTS (KEMSTRO)

The most common adverse reaction during treatment with baclofen is transient drowsiness (10-63%).

In one controlled study of 175 patients, transient drowsiness was observed in 63% of those receiving baclofen tablets compared to 36% of those in the placebo group. Other common adverse reactions are dizziness (5-15%), weakness (5-15%) and fatigue (2-4%). Others reported:

Neuropsychiatric: Confusion (1-11%), headache (4-8%), insomnia (2-7%); and, rarely, euphoria, excitement, depression, hallucinations, paresthesia, muscle pain, tinnitus, slurred speech, coordination disorder, tremor, rigidity, dystonia, ataxia, blurred vision, nystagmus, strabismus, miosis, mydriasis, diplopia, dysarthria, epileptic seizure.

Cardiovascular: Hypotension (0-9%). Rare instances of dyspnea, palpitation, chest pain, syncope.

Gastrointestinal: Nausea (4-12%), constipation (2-6%); and, rarely, dry mouth, anorexia, taste disorder, abdominal pain, vomiting, diarrhea, and positive test for occult blood in stool.

Genitourinary: Urinary frequency (2-6%); and, rarely, enuresis, urinary retention, dysuria, impotence, inability to ejaculate, nocturia, hematuria.

Other: Instances of rash, pruritus, ankle edema, excessive perspiration, weight gain, nasal congestion.

Some of the CNS and genitourinary symptoms may be related to the underlying disease rather than to drug therapy. The following laboratory tests have been found to be abnormal in a few patients receiving baclofen: increased SGOT, elevated alkaline phosphatase, and elevation of blood sugar.

The adverse experience profile seen with KEMSTROTM was similar to that seen with baclofen tablets.



Chemical IUPAC Name
4-amino-3-(4-chlorophenyl)-butanoic acid

Chemical Formula
C10H12ClNO2

Half Life
1.51 hours

Drug Type
Approved Drug

# Accession No
APRD00551

CAS Registry Number
1134-47-0


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