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Dr. Bob is Robert Hsiung, MD,
bob@dr-bob.orgShown: posts 1 to 8 of 8. This is the beginning of the thread.
Posted by JohnX2 on November 17, 2001, at 7:07:53
I don't find much information on this news
group regarding baclofen. Baclofen is a GabaB
med. This is an anti-spasmodic that also can treat
tardive-dyskinesia. It also has
been shown to prevent sensitization to stimulants.
So it seems to have many potential uses in psychiatry.Does this thing suck with regards to side effects,
or is it a dead medicine because it is long off
patent and therefore has no marketing thrust?-john
Posted by Cam W. on November 17, 2001, at 17:44:42
In reply to baclofen, posted by JohnX2 on November 17, 2001, at 7:07:53
John - Lioresal™ (baclophen) has also been shown to have some effect in certain types of neuropathic pain, by inhibiting monosynaptic and polysynaptic reflexes at the spinal level. These effects are probably as result of the drug's ability to hyperpolarize afferent terminals. Baclofen may also have some action at supraspinal sites, which would also contribute to it's clinical effects. I looked into the use of baclophen in neuropathic pain for a presentation that I gave to family physicians. The following is some of what I found.
You are correct in saying that baclofen's use is limited by it's side effect profile. The incidence with which people get side effects from it far outweighs it's minimal therapeutic efficacy, even when used as a muscle relaxant/antispasmotic in those with signs and symptoms of spasticity resulting from multiple sclerosis (it's original indication).
Also, baclophen must be used with caution in people with cormorbid conditions. It is tricky to find an optimal dose in those with impaired renal function (about 85% of the drug is excreted unchanged in urine). People who have had a stroke respond poorly to the drug and generally, baclophen is poorly tolerated in this population. When given to pregnant rats, the fetuses show an increased incidence in abdominal hernias and ossification defects (bones are not properly calcified during their development from cartilage). Baclofen has also been seen to cause deterioration in seizure control in those with epilepsy or those who have a history of convulsive disorders and this needs to be monitored with frequent EEGs (expensive and time consuming over the long run). Exacerbations of bladder sphincter hypertonia (possibly as a result of prostate problems) is also seen with those taking baclophen
Other populations where baclophen must be used with caution are those with peptic ulceration, hepatic problems, elevated blood sugars, respiratory problems, compliance problems and the elderly with cerebrovascular disorders.
Due to baclophen's high incidence of nausea (approx. 10%), as well as it's ability to cause abdominal pain, vomiting, and diarrhea; as well occasionally causing bloody stools (black in color), baclophen should be used with caution in those with peptic ulcers.
Baclophen can cause elevations in AST, alkaline phosphatase, and blood sugar, therefore the drug must be used with caution in those with liver disease, diabetes mellitus, and those who are predisposed to developing type-II diabetes (eg. those who are overweight or are taking olanzapine or clozapine). Baseline and frequent monitoring with appropriate laboratory tests are recommended.
Elderly patients, especially those at risk for, or already have cerebrovascular disorder must be closely monitored while taking baclophen. Palpitations, syncope, and chest pain are seen. Also, elderly patients are more susceptible to the CNS side effects of baclophen. The effects of antihypertensives are increased, resulting ina drop in blood pressure, is commonly seen; requiring a dosage adjustment of the antihypertensive.
Baclophen, especially when combined with other medications that can cause CNS effects, has profound effects sedative effects. This side effect seems to impair daily function, including driving a car or any other activity requiring alertness. TCA, MAOI and benzodiazepine activity, as well as the effects of alcohol and opiates are exacerbated by baclophen. The respiratory depression caused by these medications is also more pronounced.
Patients with psychotic disorders (psychosis, schizophrenia, confusional states, Parkinsonism, etc.) should use baclophen only under close supervision. Baclophen can exacerbate these conditions. This is probably the main reason that baclophen is not used very often in psychiatry.
Euphoria, excitement, confusion, hallucinations slurred speech, muscle incoordination and hypotonia, paresthesia, tremor, ataxia, dystonia are common side effects of baclophen.
Abrupt cessation of baclophen results in a withdrawl syndrome. This is characterized by visual and auditory hallucinations; status epilepticus (convulsions); dyskinesia; confusion; psychotic, manic, and paranoid states; anxiety with tachycardia and swaeting; insomnia; and worsening of spasticity. A slow tapering of the drug, over a 2 or 3 week period, is recommended.
Sorry for the long-winded post, John. I think that the answer to your question should be in here, somewhere ;^)
- Cam
Posted by JohnX2 on November 17, 2001, at 18:07:49
In reply to Re: baclofen » JohnX2, posted by Cam W. on November 17, 2001, at 17:44:42
Thanks cam.My doctor is going after the anti-spasmodic
dart board. Coincidentally memantine is a
skeletal muscle relaxant, but that is not why
I thought it would help me! So I guess I'm trying
to find out if there is a skeletal muscle relaxant
that makes sense for my psychiatric problems too.
I have also heard of tizanidine, which is
related to clonodine. Both are a2 agonists.
Any poop on tizanidine?I guess I'm wondering how much I should rally
for the memantine. It seems the side effects
are minimal from everything I gather.-john
> John - Lioresal™ (baclophen) has also been shown to have some effect in certain types of neuropathic pain, by inhibiting monosynaptic and polysynaptic reflexes at the spinal level. These effects are probably as result of the drug's ability to hyperpolarize afferent terminals. Baclofen may also have some action at supraspinal sites, which would also contribute to it's clinical effects. I looked into the use of baclophen in neuropathic pain for a presentation that I gave to family physicians. The following is some of what I found.
>
> You are correct in saying that baclofen's use is limited by it's side effect profile. The incidence with which people get side effects from it far outweighs it's minimal therapeutic efficacy, even when used as a muscle relaxant/antispasmotic in those with signs and symptoms of spasticity resulting from multiple sclerosis (it's original indication).
>
> Also, baclophen must be used with caution in people with cormorbid conditions. It is tricky to find an optimal dose in those with impaired renal function (about 85% of the drug is excreted unchanged in urine). People who have had a stroke respond poorly to the drug and generally, baclophen is poorly tolerated in this population. When given to pregnant rats, the fetuses show an increased incidence in abdominal hernias and ossification defects (bones are not properly calcified during their development from cartilage). Baclofen has also been seen to cause deterioration in seizure control in those with epilepsy or those who have a history of convulsive disorders and this needs to be monitored with frequent EEGs (expensive and time consuming over the long run). Exacerbations of bladder sphincter hypertonia (possibly as a result of prostate problems) is also seen with those taking baclophen
>
> Other populations where baclophen must be used with caution are those with peptic ulceration, hepatic problems, elevated blood sugars, respiratory problems, compliance problems and the elderly with cerebrovascular disorders.
>
> Due to baclophen's high incidence of nausea (approx. 10%), as well as it's ability to cause abdominal pain, vomiting, and diarrhea; as well occasionally causing bloody stools (black in color), baclophen should be used with caution in those with peptic ulcers.
>
> Baclophen can cause elevations in AST, alkaline phosphatase, and blood sugar, therefore the drug must be used with caution in those with liver disease, diabetes mellitus, and those who are predisposed to developing type-II diabetes (eg. those who are overweight or are taking olanzapine or clozapine). Baseline and frequent monitoring with appropriate laboratory tests are recommended.
>
> Elderly patients, especially those at risk for, or already have cerebrovascular disorder must be closely monitored while taking baclophen. Palpitations, syncope, and chest pain are seen. Also, elderly patients are more susceptible to the CNS side effects of baclophen. The effects of antihypertensives are increased, resulting ina drop in blood pressure, is commonly seen; requiring a dosage adjustment of the antihypertensive.
>
> Baclophen, especially when combined with other medications that can cause CNS effects, has profound effects sedative effects. This side effect seems to impair daily function, including driving a car or any other activity requiring alertness. TCA, MAOI and benzodiazepine activity, as well as the effects of alcohol and opiates are exacerbated by baclophen. The respiratory depression caused by these medications is also more pronounced.
>
> Patients with psychotic disorders (psychosis, schizophrenia, confusional states, Parkinsonism, etc.) should use baclophen only under close supervision. Baclophen can exacerbate these conditions. This is probably the main reason that baclophen is not used very often in psychiatry.
>
> Euphoria, excitement, confusion, hallucinations slurred speech, muscle incoordination and hypotonia, paresthesia, tremor, ataxia, dystonia are common side effects of baclophen.
>
> Abrupt cessation of baclophen results in a withdrawl syndrome. This is characterized by visual and auditory hallucinations; status epilepticus (convulsions); dyskinesia; confusion; psychotic, manic, and paranoid states; anxiety with tachycardia and swaeting; insomnia; and worsening of spasticity. A slow tapering of the drug, over a 2 or 3 week period, is recommended.
>
> Sorry for the long-winded post, John. I think that the answer to your question should be in here, somewhere ;^)
>
> - Cam
>
Posted by Willow on November 17, 2001, at 22:28:29
In reply to Re: baclofen » Cam W., posted by JohnX2 on November 17, 2001, at 18:07:49
John
Are you considering the baclofen for neck/jaw pain? If so give it a try, I've had very good success with it. I use to get very painful spasms in my neck but now I haven't had any since taking this medication. I've tried cutting it out but the pain in noticeable in days again. It may take a few days to feel the affects. If you have a hard time getting to sleep it may help there as drowsiness is a side-effect.
Cam listed a lot of side effects, but the only one I've had is drowsiness withing half an hour so I take it close to bedtime, once I'm in bed.
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Willowps i'm also on mirapex. It undoes all the good the effexor does for my concentration, but my legs don't hurt and i don't twitch the same way on it. It also puts me on edge, the mirapex.
Posted by JGalt on November 19, 2001, at 14:04:20
In reply to Re: baclofen, posted by Willow on November 17, 2001, at 22:28:29
Wish I could obtain a sample of this for experimentation. Being a GABA(b) agonist it's effects are similar to GHB, and I'm wondering if careful experimentation with it could lead to the GHB antisuicidal, antiruminating thoughts effects. I doubt my Pdoc would allow such experimentation...but I'm sure I could find some way to get it prescribed. Like GHB, I would expect its dose-response curve to be very steep and require careful experimentation to achieve the right effects.
Posted by geno on November 25, 2001, at 18:08:21
In reply to Re: baclofen, posted by JGalt on November 19, 2001, at 14:04:20
> Wish I could obtain a sample of this for experimentation. Being a GABA(b) agonist it's effects are similar to GHB, and I'm wondering if careful experimentation with it could lead to the GHB antisuicidal, antiruminating thoughts effects. I doubt my Pdoc would allow such experimentation...but I'm sure I could find some way to get it prescribed. Like GHB, I would expect its dose-response curve to be very steep and require careful experimentation to achieve the right effects.
WILLOW,
by golly i was thinking the same thing too. I believe yesterday i posted such on google board. i myslef is a g addict, looking for something similar to get off this, or help kick habbit. Benzos work ok, but still dont get the socialble effect nor the mood lifting capabilities g induces. Maybe Baclofen with an SSRI or Mao, would reselble ghb effectiveness. mmmm
Posted by edgaras on April 30, 2007, at 21:41:38
In reply to Re: baclofen » JohnX2, posted by Cam W. on November 17, 2001, at 17:44:42
Here are couple recent studies on baclofen, that might be of interest:
The GABA(B) receptor agonist baclofen prevents heroin-induced reinstatement of heroin-seeking behavior in rats.
* Spano MS,
* Fattore L,
* Fratta W,
* Fadda P.Department of Neuroscience, University of Cagliari, Cittadella Universitaria di Monserrato, Monserrato (Cagliari), Italy; Centre of Excellence "Neurobiology of Dependence", University of Cagliari, Cittadella Universitaria di Monserrato, Monserrato (Cagliari), Italy.
Opiate addiction is a chronic relapsing disorder characterized by high rates of relapse. The gamma-aminobutyric acid GABA(B) receptor agonist baclofen is known to affect the reinforcing effects of several drugs of abuse, including heroin, as well as to decrease cue-maintained responding for heroin, cocaine and nicotine and suppress alcohol deprivation effect in rats. Here we studied the effect of baclofen on the reinstatement of extinguished heroin-seeking behavior triggered by a priming injection of heroin in abstinent rats trained to stably self-administer heroin (30mug/kg per infusion) under a continuous reinforcement schedule. Following extinction, the effect of non-contingent non-reinforced primings with heroin, baclofen or heroin/baclofen combination on the resumption of responding was evaluated. Results indicate that heroin priming (0.25mg/kg) promptly reinitiated heroin-seeking behavior, an effect dose-dependently reduced by baclofen at doses (0.625 and 1.25mg/kg) not affecting responding per se. Importantly, baclofen did not affect locomotion either alone or in combination with heroin, dispelling any doubt as to the eliciting of possible non-specific (motor) effects. The present results show that GABA(B) receptor activation may reduce the propensity to resume drug-induced heroin-seeking behavior thus offering a possible approach in maintaining opiate abstinence.
-------------------------------------
Differential effects of chronic amphetamine and baclofen administration on cAMP levels and phosphorylation of CREB in distinct brain regions of wild type and monoamine oxidase B-deficient mice.* Yin HS,
* Chen K,
* Kalpana S,
* Shih JC.Department of Anatomy and Cell Biology, College of Medicine, National Taiwan University, Taipei, Taiwan. hsyin@ha.mc.ntu.edu.tw
Roles of GABA(B) transmission were explored in the action of amphetamine (Amph) on the brain. Adult male wild type (WT) and monoamine oxidase B-knocked out (MAOBKO) mice received i.p. injections of saline, d-Amph (5 mg/kg), plus baclofen (GABA(B) receptor agonist, 10 mg/kg), or baclofen and Amph, twice daily for 3 days and single treatments on day 4, followed by immuno-cyclic-AMP (cAMP) and immunoblotting assays on the brain tissue. The WT mice responded with higher levels of behavioral responses than the KO to the daily Amph injection; however, baclofen blocked the Amph-induced behavioral hyperactivity of both WT and KO mice. After the last treatment, levels of cAMP and phosphorylated (p) cyclic-AMP response element binding protein (CREB) were up-regulated in the striatum and somatosensory cortex of Amph-treated WT mice, while similar to the saline-controls in the baclofen+Amph-treated group, indicating the blockade by baclofen to Amph. Baclofen similarly suppressed the Amph-induced increases in pCREB levels of WT hippocampus and amygdala, and decreases of olfactory bulb and thalamus. For MAOBKO mice, baclofen hindered the Amph-generated increases in motor cortical cAMP and pCREB, and amygdaloid pCREB, and the decrease in olfactory bulb pCREB, whereas did not affect the Amph-raised hippocampal pCREB. Furthermore, the levels of CREB were variably modified in distinct regions by the drug exposures. The data reveal that the GABA(B)-mediated intracellular signaling differentially participates in mechanisms underlying Amph perturbation to various regions, and may thereby contribute explanations to the behavioral consequences. Moreover, MAOB is region-dependently involved in responses of the brain to Amph and baclofen, supporting interactions between GABA and monoamines.
Posted by edgaras on August 2, 2007, at 21:15:55
In reply to Re: baclofen, posted by edgaras on April 30, 2007, at 21:41:38
Baclofen was initially effective for my jaw pain, but I developed tolerance, went up to 80 mg then decided not to increase any more as there were some personality changes. Withdrawal not as pleasant either - serious agitation.
This is the end of the thread.
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