|
Gabapentinoids
Gabapentinoids, also known as α2δ ligands, are a class of drugs that are chemically derivatives of the inhibitory neurotransmitter gamma-Aminobutyric acid (GABA) (i.e., GABA analogues) which bind selectively to the α2δ protein that was first described as an auxiliary subunit of voltage-gated calcium channels (VGCCs). Clinically used gabapentinoids include gabapentin, pregabalin, and mirogabalin, as well as a gabapentin prodrug, gabapentin enacarbil. Further analogues like imagabalin and atagabalin have been tested in clinical trials but their development has been halted. Other gabapentinoids which are used in scientific research but have not been approved for medical use include 4-methylpregabalin and PD-217,014. Additionally, phenibut has been found to act as a very low affinity gabapentinoid in addition to its action as a GABAB receptor agonist. Medical uses Gabapentinoids are approved for the treatment of epilepsy, postherpetic neuralgia, neuropathic pain asso ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pregabalin
Pregabalin, sold under the brand name Lyrica among others, is an anticonvulsant, analgesic, and anxiolytic amino acid medication used to treat epilepsy, neuropathic pain, fibromyalgia, restless legs syndrome, opioid withdrawal, generalized anxiety disorder (GAD), and shingles. Pregabalin also has allodynia, antiallodynic properties. Its use in epilepsy is as an add-on therapy for partial seizures. When used before surgery, it reduces pain but results in greater sedation and visual disturbances. It is taken oral administration, by mouth. Common side effects can include headache, dizziness, somnolence, sleepiness, euphoria, confusion, trouble with memory, Ataxia, poor coordination, dry mouth, problems with vision, and weight gain. Serious side effects may include angioedema, kidney damage and drug misuse. As with all other drugs approved by the FDA for treating epilepsy, the pregabalin labeling warns of an increased suicide risk when combined with other drugs. When pregabalin i ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Gabapentin
Gabapentin, sold under the brand name Neurontin among others, is an anticonvulsant medication primarily used to treat neuropathic pain and also for partial seizures of epilepsy. It is a commonly used medication for the treatment of neuropathic pain caused by diabetic neuropathy, postherpetic neuralgia, and central pain. It is moderately effective: about 30–40% of those given gabapentin for diabetic neuropathy or postherpetic neuralgia have a meaningful benefit. Gabapentin, like other gabapentinoid drugs, acts by decreasing activity of the α2δ-1 protein, coded by the CACNA2D1 gene, first known as an auxiliary subunit of voltage gated calcium channels. However, see Pharmacodynamics, below. By binding to α2δ-1, gabapentin reduces the release of excitatory neurotransmitters (primarily glutamate) and as a result, reduces excess excitation of neuronal networks in the spinal cord and brain. Sleepiness and dizziness are the most common side effects. Serious side effects in ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Restless Legs Syndrome
Restless legs syndrome (RLS), also known as Willis–Ekbom disease (WED), is a neurological disorder, usually chronic, that causes an overwhelming urge to move one's legs. There is often an unpleasant feeling in the legs that improves temporarily by moving them. This feeling is often described as aching, tingling, or crawling in nature. Occasionally, arms may also be affected. The feelings generally happen when at rest and therefore can make it hard to sleep. Sleep disruption may leave people with RLS sleepy during the day, with low energy, and irritable or depressed. Additionally, many have limb twitching during sleep, a condition known as periodic limb movement disorder. RLS is not the same as habitual foot-tapping or leg-rocking. Signs and symptoms RLS sensations range from pain or aching in the muscles, to "an itch you can't scratch", a "buzzing sensation", an unpleasant "tickle that won't stop", a "crawling" feeling, or limbs jerking while awake. The sensations typically ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Postherpetic Neuralgia
Postherpetic neuralgia (PHN) is neuropathic pain that occurs due to damage to a peripheral nerve caused by the reactivation of the varicella zoster virus ( herpes zoster, also known as shingles). PHN is defined as pain in a dermatomal distribution that lasts for at least 90 days after an outbreak of herpes zoster. Several types of pain may occur with PHN including continuous burning pain, episodes of severe shooting or electric-like pain, and a heightened sensitivity to gentle touch which would not otherwise cause pain or to painful stimuli. Abnormal sensations and itching may also occur. Postherpetic neuralgia is the most common long-term complication of herpes zoster, and occurs in approximately 20% of patients with shingles. Risk factors for PHN include older age, severe prodrome or rash, severe acute zoster pain, ophthalmic involvement, immunosuppression, and chronic conditions such as diabetes mellitus and lupus. The pain from postherpetic neuralgia can be very severe an ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Prodrug
A prodrug is a pharmacologically inactive medication or compound that, after intake, is metabolized (i.e., converted within the body) into a pharmacologically active drug. Instead of administering a drug directly, a corresponding prodrug can be used to improve how the drug is absorbed, distributed, metabolized, and excreted (ADME). Prodrugs are often designed to improve bioavailability when a drug itself is poorly absorbed from the gastrointestinal tract. A prodrug may be used to improve how selectively the drug interacts with cells or processes that are not its intended target. This reduces adverse or unintended effects of a drug, especially important in treatments like chemotherapy, which can have severe unintended and undesirable side effects. History Many herbal extracts historically used in medicine contain glycosides (sugar derivatives) of the active agent, which are hydrolyzed in the intestines to release the active and more bioavailable aglycone. For example, sal ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Epilepsy
Epilepsy is a group of Non-communicable disease, non-communicable Neurological disorder, neurological disorders characterized by a tendency for recurrent, unprovoked Seizure, seizures. A seizure is a sudden burst of abnormal electrical activity in the brain that can cause a variety of symptoms, ranging from brief lapses of awareness or muscle jerks to prolonged convulsions. These episodes can result in physical injuries, either directly, such as broken bones, or through causing accidents. The diagnosis of epilepsy typically requires at least two unprovoked seizures occurring more than 24 hours apart. In some cases, however, it may be diagnosed after a single unprovoked seizure if clinical evidence suggests a high risk of recurrence. Isolated seizures that occur without recurrence risk or are provoked by identifiable causes are not considered indicative of epilepsy. The underlying cause is often unknown, but epilepsy can result from brain injury, stroke, infections, Brain tumor, ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Agonist
An agonist is a chemical that activates a Receptor (biochemistry), receptor to produce a biological response. Receptors are Cell (biology), cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an Receptor antagonist, antagonist blocks the action of the agonist, while an inverse agonist causes an action opposite to that of the agonist. Etymology The word originates from the Ancient Greek, Greek word (''agōnistēs''), "contestant; champion; rival" < (''agōn''), "contest, combat; exertion, struggle" < (''agō''), "I lead, lead towards, conduct; drive." Types of agonists Receptor (biochemistry), Receptors can be activated by either endogenous agonists (such as hormones and neurotransmitters) or exogenous agonists (such as medication, drugs), resulting in a biological response. A physiological agonism an ...[...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
GABAB Receptor
GABAB receptors (GABABR) are G protein-coupled receptor, G-protein coupled receptors for gamma-aminobutyric acid (GABA), therefore making them metabotropic receptors, that are linked via G-proteins to potassium channels. The changing potassium concentrations hyperpolarize the cell at the end of an action potential. The reversal potential of the GABAB-mediated IPSP (inhibitory postsynaptic potential) is −100 mV, which is much more hyperpolarized than the GABAA receptor, GABAA IPSP. GABAB receptors are found in the central nervous system and the autonomic nervous system, autonomic division of the peripheral nervous system. The receptors were first named in 1981 when their distribution in the CNS was determined, which was determined by Norman Bowery and his team using radioactively labelled baclofen. Functions GABABRs stimulate the opening of Potassium channel, K+ channels, specifically G protein-coupled inwardly-rectifying potassium channel, GIRKs, which brings the neuro ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Phenibut
Phenibut, sold under the brand name Anvifen among others, is a central nervous system (CNS) depressant with anxiolytic effects, and is used to treat anxiety, insomnia, and for a variety of other indications. It is usually taken oral administration, orally (swallowed by mouth), but may be given intravenously. Side effects of phenibut can include sedation, sleepiness, nausea, irritability, psychomotor agitation, agitation, dizziness, euphoria, and sometimes headache, among others. Overdose of phenibut can produce marked central nervous system depression including unconsciousness. The medication is structurally related to the neurotransmitter γ-aminobutyric acid (GABA), and hence is a GABA analogue. Phenibut is thought to act as a GABAB receptor, GABAB receptor agonist, similarly to baclofen and γ-hydroxybutyrate (GHB). However, at low concentrations, phenibut mildly increases the concentration of dopamine in the brain, providing Stimulant, stimulatory effects in addition to the ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
PD-217,014
PD-217,014 is a drug developed by Pfizer and related to gabapentin, which similarly binds to the α2δ calcium channels ( 1 and 2). It was developed as a potentially more potent successor to gabapentin and pregabalin Pregabalin, sold under the brand name Lyrica among others, is an anticonvulsant, analgesic, and anxiolytic amino acid medication used to treat epilepsy, neuropathic pain, fibromyalgia, restless legs syndrome, opioid withdrawal, generalized anx ..., along with several other analogues such as atagabalin and 4-methylpregabalin, but while PD-217,014 produces visceral analgesic effects in animal studies with higher potency and efficacy than gabapentin, it was not developed further for clinical use because of its comparatively more complex synthesis, compared to other related analogues. References Abandoned drugs Analgesics Calcium channel blockers GABA analogues Gamma-Amino acids Drugs developed by Pfizer {{analgesic-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
4-methylpregabalin
4-Methylpregabalin is a drug developed by Pfizer and related to pregabalin, which similarly acts as an analgesic with effectiveness against difficult to treat "atypical" pain syndromes such as neuropathic pain. The effectiveness of pregabalin and its older relative gabapentin against pain syndromes of this kind (which tend to respond poorly to other analgesic drugs) has led to their widespread use, and these drugs have subsequently been found to be useful for many other medical applications, including as anticonvulsants, muscle relaxants, anxiolytics and mood stabilisers. However these drugs are still of relatively low potency, and scientists have struggled for years to come up with an improvement on pregabalin, with increasing pressure to find a suitably improved replacement before the patent on pregabalin expired in 2018. While it was determined that the mechanism of action involves modulation of the α2δ calcium channel subunits ( 1 and 2), derivatives that appeared to be m ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
