|
Crisugabalin
Crisugabalin (HSK16149) is a selective GABA analog in development for the treatment of chronic pain. It has a wider therapeutic index than pregabalin, which has a similar mechanism of action. In China, it was approved in May 2024 for the treatment of diabetic peripheral neuropathic pain and approved in July 2024 for the treatment of postherpetic neuralgia. In the United States, it is in Phase III trials as of 2023. The drug can be administered with or without food. See also * List of investigational analgesics This is a list of investigational analgesics, or analgesics that are currently under development for clinical use but are not yet approved. ''Chemical/generic names are listed first, with developmental code names, synonyms, and brand names in par ... References GABA analogues Drugs with unknown mechanisms of action {{analgesic-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
GABA
GABA (gamma-aminobutyric acid, γ-aminobutyric acid) is the chief inhibitory neurotransmitter in the developmentally mature mammalian central nervous system. Its principal role is reducing neuronal excitability throughout the nervous system. GABA is sold as a dietary supplement in many countries. It has been traditionally thought that exogenous GABA (i.e., taken as a supplement) does not cross the blood–brain barrier, but data obtained from more recent research (2010s) in rats describes the notion as being unclear. The carboxylate form of GABA is γ-aminobutyrate. Function Neurotransmitter Two general classes of GABA receptor are known: * GABAA in which the receptor is part of a ligand-gated ion channel complex * GABAB metabotropic receptors, which are G protein-coupled receptors that open or close ion channels via intermediaries (G proteins) Neurons that produce GABA as their output are called GABAergic neurons, and have chiefly inhibitory action at receptors in t ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Chronic Pain
Chronic pain is pain that persists or recurs for longer than 3 months.https://icd.who.int/browse/2025-01/mms/en#1581976053 It is also known as gradual burning pain, electrical pain, throbbing pain, and nauseating pain. This type of pain is in contrast to acute pain, which is pain associated with a cause that can be relieved by treating the cause, and decreases or stops when the cause improves. Chronic pain can last for years. Persistent pain often serves no apparent useful purpose. The most common types of chronic pain are back pain, severe headache, migraine, and facial pain. Chronic pain can cause very severe psychological and physical effects that sometimes continue until the end of life. Analysis of the grey matter (damage to brain neurons), insomnia and sleep deprivation, metabolic problems, chronic stress, obesity, and heart attack are examples of physical disorders; and Depression (mood), depression, and neurocognitive disorders are examples of mental disorders. A wide ra ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Therapeutic Index
The therapeutic index (TI; also referred to as therapeutic ratio) is a quantitative measurement of the relative safety of a drug with regard to risk of overdose. It is a comparison of the amount of a therapeutic agent that causes toxicity to the amount that causes the therapeutic effect. The related terms therapeutic window or safety window refer to a range of doses optimized between efficacy and toxicity, achieving the greatest therapeutic benefit without resulting in unacceptable side-effects or toxicity. Classically, for clinical indications of an approved drug, TI refers to the ratio of the dose of the drug that causes adverse effects at an incidence/severity not compatible with the targeted indication (e.g. toxic dose in 50% of subjects, TD) to the dose that leads to the desired pharmacological effect (e.g. efficacious dose in 50% of subjects, ED). In contrast, in a drug development setting TI is calculated based on plasma exposure levels. In the early days of pharmaceu ... [...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] |
Mechanism Of Action
In pharmacology, the term mechanism of action (MOA) refers to the specific biochemical Drug interaction, interaction through which a Medication, drug substance produces its pharmacological effect. A mechanism of action usually includes mention of the specific molecular targets to which the drug binds, such as an enzyme or receptor (biochemistry), receptor. Receptor sites have specific affinities for drugs based on the chemical structure of the drug, as well as the specific action that occurs there. Drugs that do not bind to receptors produce their corresponding therapeutic effect by simply interacting with chemical or physical properties in the body. Common examples of drugs that work in this way are antacids and laxatives. In contrast, a Mode of action, mode of action (MoA) describes functional or anatomical changes, at the cellular level, resulting from the exposure of a living organism to a substance. Importance Elucidating the mechanism of action of novel drugs and medicati ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Neuropathic Pain
Neuropathic pain is pain caused by a lesion or disease of the somatosensory nervous system. Neuropathic pain may be associated with abnormal sensations called dysesthesia or pain from normally non-painful stimuli (allodynia). It may have continuous and/or episodic (paroxysmal) components. The latter resemble stabbings or electric shocks. Common qualities include burning or coldness, "pins and needles" sensations, numbness and itching. Up to 7–8% of the European population is affected by neuropathic pain, and in 5% of persons it may be severe. The pain may result from disorders of the peripheral nervous system or the central nervous system (brain and spinal cord). Neuropathic pain may occur in isolation or in combination with other forms of pain. Medical treatments focus on identifying the underlying cause and relieving pain. In cases of peripheral neuropathy, the pain may progress to insensitivity. Diagnosis Diagnosis of pain conditions relies on the character of the pain w ... [...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] |
List Of Investigational Analgesics
This is a list of investigational analgesics, or analgesics that are currently under development for clinical use but are not yet approved. ''Chemical/generic names are listed first, with developmental code names, synonyms, and brand names in parentheses.'' This list was last comprehensively updated in June 2017. It is likely to become outdated with time. Opioid receptor modulators * Axelopran/oxycodone – combination of a centrally active μ-opioid receptor agonist and a peripherally selective μ-, κ-, and δ-opioid receptor antagonist. * Cebranopadol (GRT-6005) – non-selective μ-opioid receptor, nociceptin receptor, and δ-opioid receptor full agonist and κ-opioid receptor partial agonist * Desmetramadol (''O''-desmethyltramadol; Omnitram) – μ-opioid receptor agonist, norepinephrine reuptake inhibitor (NRI), and 5-HT2C receptor antagonist. * Deumitragynine (KUR-101) – atypical μ-opioid receptor agonist related to mitragynine (found in kratom) * (GRT-6 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
GABA Analogues
GABA (gamma-aminobutyric acid, γ-aminobutyric acid) is the chief inhibitory neurotransmitter in the developmentally mature mammalian central nervous system. Its principal role is reducing neuronal excitability throughout the nervous system. GABA is sold as a dietary supplement in many countries. It has been traditionally thought that exogenous GABA (i.e., taken as a supplement) does not cross the blood–brain barrier, but data obtained from more recent research (2010s) in rats describes the notion as being unclear. The carboxylate form of GABA is γ-aminobutyrate. Function Neurotransmitter Two general classes of GABA receptor are known: * GABAA receptor, GABAA in which the receptor is part of a ligand-gated ion channel complex * GABAB receptor, GABAB metabotropic receptors, which are G protein-coupled receptors that open or close ion channels via intermediaries (G proteins) Neurons that produce GABA as their output are called GABAergic neurons, and have chiefly inhibito ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
