Прегабалин — Википедия

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Прегабалин — Википедия

Прегабалин (Лирика)

Death may result when gabapentinoids are combined with other depressants such as opiates , benzodiazepines , barbiturates , thienodiazepines , alcohol or other GABAergic substances. It is strongly discouraged to combine these substances, particularly in common to heavy doses. WARNING: Always start with lower doses due to differences between individual body weight, tolerance, metabolism, and personal sensitivity. See responsible use section. It is not a recommendation and should be verified with other sources for accuracy. Pregabalin also known as 3-isobutyl GABA and by the trade-name Lyrica is a depressant substance of the gabapentinoid class. Pregabalin is a common prescription drug, which is typically used to treat neuropathic pain, anxiety , restless leg syndrome , and as an adjunct drug in the treatment of seizures. Pregabalin has a pharmacological profile comparable to that of gabapentin as they both share similar mechanisms of action and induce similar subjective effects. The advantages pregabalin has over gabapentin include greater bioavailability and potency, \\\\\\\\\\\\[5\\\\\\\\\\\\] as well as a wider variety of accepted medical applications for pregabalin not seen with gabapentin, such as its successful use in the treatment of anxiety, in which the use of gabapentin was not successful, excluding some more severe cases. Pregabalin is a structural analog of GABA gamma-aminobutyric acid , with an isobutyl group substituted on the beta carbon of the aminobutyric chain. Pregabalin is similar in structure to other gabapentinoids , such as gabapentin and phenibut. Pregabalin contains a carboxylated chain of hexane called hexanoic acid. This carbon chain is substituted with an amine group through a methyl bridge in S conformation at R 3 and a methyl group at R 5. Advantages to pregabalin over gabapentin include higher bioavailability and potency. By binding to this site, Pregabalin reduces the release of several excitatory neurotransmitters, including glutamate , substance P , acetylcholine and norepinephrine. One study has also shown that pregabalin promotes deep sleep, thus enhancing sleep quality. This may be substantial because reductions in slow-wave sleep have been associated with anxiety and fibromyalgia. The endogenous neurochemical thrombospondin also binds to this site and is important for the generation of new excitatory synapses. Gabapentin and pregabalin, having a high affinity for this site, block this action and result in lower levels of excitatory synapses in animal models. As pregabalin treats conditions and neurotransmitters associated with overexcitability of the brain anxiety, epilepsy, neuropathic pain , its modulation results in the sedating or calming effects of pregabalin on the nervous system. Pregabalin is rapidly absorbed when administered on an empty stomach, with peak plasma concentrations occurring within 1 to 1. Pregabalin undergoes negligible metabolism in humans. The primary metabolite is N-methyl pregabalin. Pregabalin is eliminated from the systemic circulation primarily by renal excretion as unchanged substance. Each individual can have a very different reaction to pregabalin, thus it is essential to start at lower doses to ensure that it does not have any severe adverse effects such as peripheral edema or muscle pain. Disclaimer: The effects listed below are cited from the Subjective Effect Index SEI , which relies on assorted anecdotal reports and the personal experiences of PsychonautWiki contributors. As a result, they should be taken with a healthy amount of skepticism. Likewise, adverse effects become much more likely on higher doses and may include serious injury or death. Anecdotal reports which describe the effects of this compound within our experience index include:. Pregabalin is used in a medical setting, usually prescribed in capsules, to treat epilepsy, neuropathic pain, fibromyalgia, and generalized anxiety disorder. Its use for epilepsy is as an add-on therapy for partial seizures with or without secondary generalization in adults. Some off-label uses of pregabalin include restless leg syndrome, prevention of migraines, social anxiety disorder, and alcohol withdrawal. Pregabalin is useful when added to other treatments, when those other treatments are not controlling partial epilepsy. Its use alone is less effective than some other seizure medications. It is unclear how it compares to gabapentin for this use. The European Federation of Neurological Societies recommends pregabalin as a first line agent for the treatment of pain associated with diabetic neuropathy, post-herpetic neuralgia, and central neuropathic pain. A minority obtain substantial benefit, and a larger number obtain moderate benefit. Other first line agents, including gabapentin and tricyclic antidepressants, are given equal weight as first line agents, and unlike pregabalin, are available as less expensive generics. The World Federation of Biological Psychiatry recommends pregabalin as one of several first line agents for the treatment of generalized anxiety disorder, but recommends other agents such as SSRIs as first line treatment for obsessive-compulsive disorder and post-traumatic stress disorder. It appears to have anxiolytic effects similar to benzodiazepines with less risk of dependence. The effects of pregabalin appear after 1 week of use and is similar in effectiveness to lorazepam, alprazolam, and venlafaxine, but pregabalin has demonstrated superiority by producing more consistent therapeutic effects for psychosomatic anxiety symptoms. Long-term trials have shown continued effectiveness without the development of tolerance, and, in addition, unlike benzodiazepines, it has a beneficial effect on sleep and sleep architecture, characterized by the enhancement of slow-wave sleep. It produces less severe cognitive and psychomotor impairment compared to those drugs and may be preferred over the benzodiazepines for these reasons. Anecdotal reports \\\\\\\\\\\\[22\\\\\\\\\\\\] exist of successful discontinuation of opioid use by supplementing with pregabalin. Pregabalin also reduced the measure of subjective 'liking' after smoking a cigarette. Both showed positive results. The patients also showed reduced anxiety levels and better cognitive functioning. Pregabalin was well tolerated. This toxicity and harm potential section is a stub. As such, it may contain incomplete or even dangerously wrong information. You can help by expanding or correcting it. We also recommend that you conduct independent research and use harm reduction practices when using this substance. Pregabalin likely has a low toxicity relative to dose. However, it is potentially lethal when mixed with depressants like alcohol or opioids. It is strongly recommended that one use harm reduction practices when using this substance. In terms of humans, there exists a case report of a man who ingested 8,mg pregabalin and eventually fell into a coma but was managed with supportive care alone until he regained consciousness. Pregabalin was initially thought to be non-addictive with a low abuse potential and little tolerance development. However, recreational use of the substance has caused a re-evaluation of this assessment. The euphoric effects of the substance and the development of tolerance can lead to the use of dosages far above the therapeutic range, which suggests both the potential for recreational use and addiction. Tolerance will develop to the depressant effects within several months of continuous use. After cessation, the tolerance returns to baseline in 7 - 14 days. Withdrawal symptoms or rebound symptoms are likely to occur after ceasing usage abruptly following a few months or longer of steady dosing and may necessitate a gradual dose reduction. The withdrawal effects of abrupt cessation of chronic use include anxiety, insomnia, sweating, muscle spasms, gastrointestinal problems, hot and cold flashes, nausea, and a flu-like feeling. One report of a patient entering serotonin syndrome following perioperative oxycodone and pregabalin exists. Pregabalin is not a serotonin reuptake inhibitor and does not act as a glutamate receptor antagonist. If pregabalin has serotonergic effects, it could interact negatively with other serotonergic substances, including SSRIs , MDMA , various analgesics, and possibly other recreational and medical substances. Given the total lack of evidence for any serotonergic activity in multiple studies, it seems possible that the one reported adverse event was a freak accident, caused by unknown factors. Physical effects. Visual effects. Disconnective effects. Cognitive effects. Auditory effects. Wesche, H. A randomized, double-blind, placebo-controlled, fixed-dose, multicenter study of pregabalin in patients with generalized anxiety disorder. Placebo-controlled study of gabapentin treatment of panic disorder. Journal of clinical psychopharmacology Identification of the alpha2-delta-1 subunit of voltage-dependent calcium channels as a molecular target for pain mediating the analgesic actions of pregabalin. Cell, 2 , — Epilepsy Research, 73 2 , — A double-blind study in healthy volunteers to assess the effects on sleep of pregabalin compared with alprazolam and placebo. Sleep, 28 2 , — Psychiatrische Praxis, 39 7 , —2. Effects of pregabalin on smoking behavior, withdrawal symptoms, and cognitive performance in smokers. Psychopharmacology, 3 , — Pregabalin for alcohol dependence: A critical review of the literature. Advances in Therapy, 29 11 , — Human Psychopharmacology: Clinical and Experimental, 23 4 , — Journal of Medical Toxicology, 6 4 , — Serotonin syndrome with perioperative oxycodone and pregabalin. Pain Physician, 16 October , E Pregabalin: From molecule to medicine. European Neuropsychopharmacology, 16, S—S Marks et al. Categories : All articles with unsourced statements Articles with unsourced statements Substance Psychoactive substance Depressant Anxiolytics Gabapentinoid. Navigation menu Personal tools Create account Log in. Namespaces Page Discussion. Views Read View source View history. Community Network YouTube Good vibes. Summary sheet: Pregabalin.

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Прегабалин — Википедия

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