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What Is Baclofen?

Baclofen is a GABA-like drug, which has been used for decades as a treatment for spasticity. It has some recreational effects that are similar to Phenibut. Research has also explored baclofen for alcohol dependence and other substance use disorders.

Among the positive effects are muscle relaxation, euphoria, sedation, pain relief, and anxiety reduction. The negative effects may include respiratory depression, dizziness, drowsiness, memory loss, and confusion.

It has long been used for spasticity originating with various.conditions. This remains its greatest application, though, other potential uses for the drug have appeared.

In addition to oral use, it may also be taken intrathecally. It allows it to be delivered more directly to the spine. A lower dose can be used preventing some of the negative effects.

The non-medical effects are generally compared to those of GHB. It tends to produce less euphoria than GHB and is believed to have a lower abuse potential in medical settings.

Baclofen is similar to Phenibut in its effects, however, it appears to provide less anxiety reduction, is more sedating and has a faster onset. |Given this, it's a fairly subtle drug capable of providing some anxiety reduction, muscle relaxation, and sedation.

Baclofen has been studied as a treatment for alcohol dependence since it may be able to function as both an antique craving drug and a replacement. There is conflicting research in this area and it is possible the required dose is in the hundreds of milligrams per day for which we definitely need more research.

It appears Baclofen may reduce tremor, anxiety, agitation, sweating and other alcohol withdrawal symptoms. The drug may also help people reduce their drinking or maintain abstinence.

Less data exists regarding the effect on other dependencies. It might have more generalized anti-addiction effects due to antagonizing dopamine activity associated with addictive drugs and activities.

Orally the drug lasts for 3 to 6 hours and it begins working in 15 to 45 minutes. Doses above the strong range may last significantly longer.

Baclofen exists as an R and S isomer with R Baclofen being far more potent. It's a GABA analog that is very close in structure to Phenibut. The drug's primary action is a GABA-B agonist, which means it can inhibit excitatory neurotransmitter activity. That action is responsible for its core effects.

Baclofen is normally used at 30 to 75 milligrams per day for spasticity. And that dose is split up throughout the day. A light dose is 10 to 20 milligrams; a common dose is 20 to 50 milligrams; a strong dose is 50 to 75 milligrams.

Baclofen History

Heinrich Keberle, a chemist at Sibugay, synthesized the drug in 1962. It was originally developed as a treatment for epilepsy, but it didn't end up being used in that way. Baclofen was instead introduced in the late 1960s as a treatment for spasticity. Studies around this time found it was quite effective. In these studies, it was often compared to diazepam and had a similar or sometimes superior efficacy.

The first overdose appears to have been reported in 1972. Baclofen tumors were identified in 1975. Later that decade, there were multiple hospitalizations due to people experimenting with the drug. Those cases involved diversion from medical use.

Baclofen was approved by the FDA in 1977 for spasticity associated with conditions like multiple sclerosis. Some of the earliest research on the GABA-B receptor involved the drug. Norman Bowery, the discoverer of GABA B, found in 1980 that Baclofen operated like GABA in providing effects, which could not be attributed to the already identified GABA receptor. Bowery also found our Baclofen was more active enantiomer.

Intrathecal administration of the drug appeared in the mid-1980s allowing patients to avoid some of the negative effects while potentially receiving more relief.

Currently, Baclofen is widely prescribed for spasticity and interest has grown in its potential application in many other conditions. There is also some recreational use of the drug due to its Phenabut-like effects.

Baclofen is prescription-only rather than a controlled drug in the US. It is usually prescription only or entirely uncontrolled in other countries.

Baclofen overdose

Common doses generally have few negative effects beyond stomach upset and tiredness. Overdoses can be much more problematic and severe overdoses can be fatal. A classic overdose generally occurs with over 200 mg, but even 100mg can bring some negative effects. Once you reach 100mg, coma, confusion, delirium, respiratory depression and seizures become potential outcomes. It's also possible to have bradycardia or tachycardia, hypotension or hypertension, and meiosis or mitosis.

There have occasionally been reports of visual effects, but those primarily appear in very large overdoses and in withdrawal. Overdoses are not only problematic because of their effects, but because the duration of action may extend to 24 hours or more. There can be multiple peaks in Baclofen's effects during this time. And it's possible to have CNS depression that lasts beyond the presence of large serum concentrations.

There are a number of cases where more than 1000mg has been used. Those cases usually result in mechanical ventilation and extended coma. Though, people tend to be fine upon leaving the hospital. Of course, in the absence of medical attention, those overdoses would have been fatal. Cases of coma lasting three or more days do exist and they've occasionally mimicked brain death.

In one report the prognosis was grim enough for an organ transplant process to be set in motion. However, the patient did come out of the coma. When coming out of a Baclofen coma, it is common for there to be agitation, hyperthermia, delirium, tachycardia, hallucinations and other issues.

Those problems sometimes necessitate a prolonged stay in the hospital. While overdose is managed by medical professionals usually result in survival, some deaths have been recorded. Some of those deaths occurred with 1 to 2.5 grams, however, even 200 to 300 mg could be very problematic in the absence of help.

Seizures are an established concern with the drug and our particular concern in those with a history of seizures. If you have impaired renal function, overdoses can occur with lower amounts including at normal medical doses.

Baclofen withdrawal and addiction

Tolerance to Baclofen does build, but it seems to do so fairly slow over a period of weeks rather than a few days. Tolerance to the pain-relieving and sedating effects you build faster. Withdrawal can be dangerous and it may include issues like seizures, hallucinations, insomnia, agitation, delirium, tachycardia and hyperthermia.

Abruptly stopping the drug is more of a concern if someone has been taking the drug for months. Some of the risky combinations include other depressants like alcohol and benzodiazepine.