WordNet
- a drug used to treat or prevent convulsions (as in epilepsy) (同)anticonvulsant_drug, antiepileptic, antiepileptic_drug
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出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2015/03/18 21:19:44」(JST)
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A convulsant is a drug which induces convulsions and/or epileptic seizures, the opposite of an anticonvulsant. These drugs generally act as stimulants at low doses, but are not used for this purpose due to the risk of convulsions and consequent excitotoxicity. Most convulsants are antagonists (or inverse agonists) at either the GABAA or glycine receptors, or ionotropic glutamate receptor agonists. Many other drugs may cause convulsions as a side effect at high doses (e.g. bupropion, tramadol, pethidine, dextropropoxyphene, clomipramine) but only drugs whose primary action is to cause convulsions are known as convulsants. Nerve agents such as sarin which were developed as chemical weapons, produce convulsions as a major part of their toxidrome, but also produce a number of other effects in the body and are usually classified separately.[1][2][3][4]
Uses
Some convulsants such as pentetrazol and flurothyl were previously used in shock therapy in psychiatric medicine, as an alternative to electroconvulsive therapy. Others such as strychnine and tetramethylenedisulfotetramine are used as poisons for exterminating pests. Bemegride and flumazenil are used to treat drug overdoses (of barbiturates and benzodiazepines respectively), but may cause convulsions if the dose is too high. Convulsants are also widely used in scientific research, for instance in the testing of new anticonvulsant drugs. Convulsions are induced in captive animals, then high doses of anticonvulsant drugs are administered.[5][6][7]
Examples
- GABAA receptor antagonists, inverse agonists or negative allosteric modulators
- Bemegride
- Bicuculline
- Cicutoxin
- Cyclothiazide
- DMCM
- FG-7142
- Fipronil
- Flumazenil
- Flurothyl
- Gabazine
- Laudanosine
- Oenanthotoxin
- Pentetrazol
- Picrotoxin
- Sarmazenil
- Securinine
- Sinomenine
- Tetramethylenedisulfotetramine
- Thujone
- GABA synthesis inhibitors
- 3-Mercaptopropionic acid
- Allylglycine
- Glycine receptor antagonists
- Bicuculline
- Brucine
- Colubrine
- Diaboline
- Gelsemine
- Hyenandrine
- Laudanosine
- Oripavine
- RU-5135 (also GABA antagonist)
- Sinomenine
- Strychnine
- Thebaine
- Tutin
- Ionotropic glutamate receptor agonists
- AMPA
- Domoic acid
- Kainic acid
- NMDA
- Quinolinic acid
- Quisqualic acid
- Tetrazolylglycine
- Acetylcholine receptor agonists
References
- ^ Mares P, Folbergrová J, Kubová H. Excitatory aminoacids and epileptic seizures in immature brain. Physiology Research. 2004;53 Suppl 1:S115-24. PMID 15119942
- ^ Calabrese EJ. Modulation of the epileptic seizure threshold: implications of biphasic dose responses. Critical Reviews in Toxicology. 2008;38(6):543-56. DOI 10.1080/10408440802014261. PMID 18615309
- ^ Johnston GA. Advantages of an antagonist: bicuculline and other GABA antagonists. British Journal of Pharmacology. 2013 May;169(2):328-36. DOI 10.1111/bph.12127. PMID 23425285
- ^ de Araujo Furtado M, Rossetti F, Chanda S, Yourick D. Exposure to nerve agents: from status epilepticus to neuroinflammation, brain damage, neurogenesis and epilepsy. Neurotoxicology. 2012 Dec;33(6):1476-90. DOI 10.1016/j.neuro.2012.09.001. PMID 23000013
- ^ Löscher W. Animal models of epilepsy for the development of antiepileptogenic and disease-modifying drugs. A comparison of the pharmacology of kindling and post-status epilepticus models of temporal lobe epilepsy. Epilepsy Research. 2002 Jun;50(1-2):105-23. PMID 12151122
- ^ Löscher W. Preclinical assessment of proconvulsant drug activity and its relevance for predicting adverse events in humans. European Journal of Pharmacology. 2009 May 21;610(1-3):1-11. DOI 10.1016/j.ejphar.2009.03.025. PMID 19292981
- ^ Rubio C, Rubio-Osornio M, Retana-Márquez S, Verónica Custodio ML, Paz C. In vivo experimental models of epilepsy. Central Nervous System Agents in Medicinal Chemistry. 2010 Dec 1;10(4):298-309. PMID 20868357
UpToDate Contents
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English Journal
- Nephrotoxicity of epigenetic inhibitors used for the treatment of cancer.
- Scholpa NE1, Kolli RT1, Moore M1, Arnold RD2, Glenn TC3, Cummings BS4.
- Chemico-biological interactions.Chem Biol Interact.2016 Aug 16. pii: S0009-2797(16)30328-3. doi: 10.1016/j.cbi.2016.08.010. [Epub ahead of print]
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- Anticonvulsant effects of iridoid glycosides fraction purified from Feretia apodanthera Del. (Rubiaceae) in experimental mice models of generalized tonic-clonic seizures.
- Taiwe GS1, Dabole B2, Tchoya TB3, Menanga JR3, Dzeufiet PD3, De Waard M4,5,6.
- BMC complementary and alternative medicine.BMC Complement Altern Med.2016 Aug 12;16(1):285. doi: 10.1186/s12906-016-1269-8.
- BACKGROUND: Despite the increasing number and variety of antiepileptic drugs, nearly 30 % of epileptic patients who receive appropriate medical attention have persisting seizures. Anticonvulsant activity has been demonstrated for different iridoid glycoside-rich plant extracts. This study was desig
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- The alerted presence in recent decades of pharmaceuticals has become an issue of environmental concern, and most of the mechanisms of biotransformation and biochemical and physiological responses to them in fish are still unknown, as well as the influence of water temperature in their ability to cop
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Japanese Journal
- 抗けいれん療法 (特集 急性脳炎・脳症の概念) -- (急性脳炎・脳症の予防・治療)
Related Links
- A convulsant is a drug which induces convulsions and/or epileptic seizures, the opposite of an anticonvulsant. These drugs generally act as stimulants at low doses, but are not used for this purpose due to the risk of convulsions and ...
- con·vul·sant (k n-v l s nt). adj. Causing or producing convulsions. n. An agent, such as a drug, that causes convulsions. convulsant. a drug which causes convulsions. Patient discussion about convulsant. Q. my friend has convulsions what can i ...
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抗痙攣薬、抗けいれん薬
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- Antiseizure drug(s)
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- anticonvulsant agent、anticonvulsant drug、anticonvulsants、anticonvulsive、antiseizure、antiseizure drug
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- anticonvulsant、anticonvulsant drug、anticonvulsants、antiseizure drug