Convulsant
Encyclopedia
A convulsant is a drug which induces convulsion
s and/or epileptic seizures, the opposite of an anticonvulsant
. These drugs generally act as stimulant
s 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 agonist
s) at either the GABAA or glycine
receptor
s, or ionotropic
glutamate receptor
agonist
s. Many other drugs may cause convulsions as a side effect at high doses (e.g. bupropion
, tramadol
, pethidine
, dextropropoxyphene
) but only drugs whose primary action is to cause convulsions are known as convulsants.
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 benzodiazepine
s 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.
Glycine receptor antagonists
Ionotropic glutamate receptor agonists
Convulsion
A convulsion is a medical condition where body muscles contract and relax rapidly and repeatedly, resulting in an uncontrolled shaking of the body. Because a convulsion is often a symptom of an epileptic seizure, the term convulsion is sometimes used as a synonym for seizure...
s and/or epileptic seizures, the opposite of an anticonvulsant
Anticonvulsant
The anticonvulsants are a diverse group of pharmaceuticals used in the treatment of epileptic seizures. Anticonvulsants are also increasingly being used in the treatment of bipolar disorder, since many seem to act as mood stabilizers, and in the treatment of neuropathic pain. The goal of an...
. These drugs generally act as stimulant
Stimulant
Stimulants are psychoactive drugs which induce temporary improvements in either mental or physical function or both. Examples of these kinds of effects may include enhanced alertness, wakefulness, and locomotion, among others...
s at low doses, but are not used for this purpose due to the risk of convulsions and consequent excitotoxicity
Excitotoxicity
Excitotoxicity is the pathological process by which nerve cells are damaged and killed by excessive stimulation by neurotransmitters such as glutamate and similar substances. This occurs when receptors for the excitatory neurotransmitter glutamate such as the NMDA receptor and AMPA receptor are...
. Most convulsants are antagonists
Receptor antagonist
A receptor antagonist is a type of receptor ligand or drug that does not provoke a biological response itself upon binding to a receptor, but blocks or dampens agonist-mediated responses...
(or inverse agonist
Inverse agonist
In the field of pharmacology, an inverse agonist is an agent that binds to the same receptor as an agonist but induces a pharmacological response opposite to that agonist....
s) at either the GABAA or glycine
Glycine receptor
The glycine receptor, or GlyR, is the receptor for the amino acid neurotransmitter glycine. GlyR is an ionotropic receptor that produces its effects through chloride current...
receptor
Receptor (biochemistry)
In biochemistry, a receptor is a molecule found on the surface of a cell, which receives specific chemical signals from neighbouring cells or the wider environment within an organism...
s, or ionotropic
Ligand-gated ion channel
Ligand-gated ion channels are one type of ionotropic receptor or channel-linked receptor. They are a group of transmembrane ion channels that are opened or closed in response to the binding of a chemical messenger , such as a neurotransmitter.The binding site of endogenous ligands on LGICs...
glutamate receptor
Glutamate receptor
Glutamate receptors are synaptic receptors located primarily on the membranes of neuronal cells. Glutamate is one of the 20 amino acids used to assemble proteins and as a result is abundant in many areas of the body, but it also functions as a neurotransmitter and is particularly abundant in the...
agonist
Agonist
An agonist is a chemical that binds to a receptor of a cell and triggers a response by that cell. Agonists often mimic the action of a naturally occurring substance...
s. Many other drugs may cause convulsions as a side effect at high doses (e.g. bupropion
Bupropion
Bupropion is an atypical antidepressant and smoking cessation aid. The drug is a non-tricyclic antidepressant and differs from most commonly prescribed antidepressants such as SSRIs, as its primary pharmacological action is thought to be norepinephrine-dopamine reuptake inhibition...
, tramadol
Tramadol
Tramadol hydrochloride is a centrally acting synthetic opioid analgesic used in treating moderate pain. The drug has a wide range of applications, including treatment for restless legs syndrome and fibromyalgia...
, pethidine
Pethidine
Pethidine or meperidine Pethidine (INN) or meperidine (USAN) Pethidine (INN) or meperidine (USAN) (commonly referred to as Demerol but also referred to as: isonipecaine; lidol; pethanol; piridosal; Algil; Alodan; Centralgin; Dispadol; Dolantin; Mialgin (in Indonesia); Petidin Dolargan (in Poland);...
, dextropropoxyphene
Dextropropoxyphene
Dextropropoxyphene, manufactured by Eli Lilly and Company, is an analgesic in the opioid category. It is intended to treat mild pain and has, in addition, anti-tussive and local anesthetic effects. It has been taken off the market in Europe and the US due to concerns of fatal overdoses and...
) but only drugs whose primary action is to cause convulsions are known as convulsants.
Uses
Some convulsants such as pentetrazol and flurothylFlurothyl
Flurothyl is a volatile liquid drug from the halogenated ether family, related to inhaled anaesthetic agents such as diethyl ether, but having the opposite effects, acting as a stimulant and convulsant...
were previously used in shock therapy
Shock therapy
Shock therapy or shock treatment may refer to:* A form of aversion therapy in which an electric shock is used as a negative stimulus* Electroconvulsive therapy, or electroshock, a psychiatric treatment in which seizures are electrically induced in anaesthetized patients for therapeutic effect*...
in psychiatric medicine, as an alternative to electroconvulsive therapy
Electroconvulsive therapy
Electroconvulsive therapy , formerly known as electroshock, is a psychiatric treatment in which seizures are electrically induced in anesthetized patients for therapeutic effect. Its mode of action is unknown...
. Others such as strychnine
Strychnine
Strychnine is a highly toxic , colorless crystalline alkaloid used as a pesticide, particularly for killing small vertebrates such as birds and rodents. Strychnine causes muscular convulsions and eventually death through asphyxia or sheer exhaustion...
and tetramethylenedisulfotetramine
Tetramethylenedisulfotetramine
Tetramethylenedisulfotetramine is an organic compound that is used as a rodenticide . It is an odorless, tasteless white powder that is slightly soluble in water, DMSO and acetone, and insoluble in methanol and ethanol. It is a sulfamide derivative...
are used as poisons for exterminating pests. Bemegride
Bemegride
Bemegride is a central Nervous System stimulant and antidote for barbiturate poisoning.- John Bodkin Adams case :...
and flumazenil
Flumazenil
Flumazenil is a benzodiazepine antagonist available for injection only, and the only benzodiazepine receptor antagonist on the market today.It was first introduced in 1987 by Hoffmann-La Roche under the trade name Anexate, but only approved by...
are used to treat drug overdoses (of barbiturates and benzodiazepine
Benzodiazepine
A benzodiazepine is a psychoactive drug whose core chemical structure is the fusion of a benzene ring and a diazepine ring...
s 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.
Examples
GABAA receptor antagonists, inverse agonists or negative allosteric modulators- BemegrideBemegrideBemegride is a central Nervous System stimulant and antidote for barbiturate poisoning.- John Bodkin Adams case :...
- BicucullineBicucullineBicuculline is a light-sensitive competitive antagonist of GABAA receptors. It was originally identified in 1932 in plant alkaloid extracts and has been isolated from Dicentra cucullaria, Adlumia fungosa, Fumariaceae, and several Corydalis species. Since it blocks the inhibitory action of GABA...
- CicutoxinCicutoxinCicutoxin is a poisonous polyyne and alcohol found in various plants, most notably water hemlock . It is structurally related to the oenanthotoxin of hemlock water dropwort....
- CyclothiazideCyclothiazideCyclothiazide is a benzothiadiazide diuretic and antihypertensive that was originally introduced in the United States in 1963 by Eli Lilly and was subsequently also marketed in Europe and Japan...
- DMCMDMCMDMCM is a drug from the beta-carboline family. It acts as an inverse agonist of benzodiazepine receptors, meaning that it causes the opposite effects to the benzodiazepine class of drugs...
- FG-7142
- FipronilFipronilFipronil is a broad spectrum insecticide that disrupts the insect central nervous system by blocking the passage of chloride ions through the GABA receptor and glutamate-gated chloride channels, components of the central nervous system. This causes hyperexcitation of contaminated insects' nerves...
- FlumazenilFlumazenilFlumazenil is a benzodiazepine antagonist available for injection only, and the only benzodiazepine receptor antagonist on the market today.It was first introduced in 1987 by Hoffmann-La Roche under the trade name Anexate, but only approved by...
- FlurothylFlurothylFlurothyl is a volatile liquid drug from the halogenated ether family, related to inhaled anaesthetic agents such as diethyl ether, but having the opposite effects, acting as a stimulant and convulsant...
- GabazineGabazineGabazine is a drug that acts as an antagonist at GABAA receptors. It is used in scientific research and has no role in medicine, as it would be expected to produce convulsions if used in humans....
- OenanthotoxinOenanthotoxinOenanthotoxin is a toxin extracted from hemlock water dropwort and other plants of the genus Oenanthe. It is a central nervous system poison, and acts as a noncompetitive gamma-aminobutyric acid antagonist. This toxin played some role in euthanasia in ancient Sardinia, for inducing risus...
- Pentetrazol
- PicrotoxinPicrotoxinPicrotoxin, also known as cocculin, is a poisonous crystalline plant compound, first isolated by Pierre Boullay in 1812. The name "picrotoxin" is a combination of the Greek words "picros" and "toxicon" ....
- SarmazenilSarmazenilSarmazenil is a drug from the benzodiazepine family. It acts as a partial inverse agonist of benzodiazepine receptors, meaning that it causes the opposite effects to most benzodiazepine drugs, and instead acts as an anxiogenic and convulsant...
- Securinine
- TetramethylenedisulfotetramineTetramethylenedisulfotetramineTetramethylenedisulfotetramine is an organic compound that is used as a rodenticide . It is an odorless, tasteless white powder that is slightly soluble in water, DMSO and acetone, and insoluble in methanol and ethanol. It is a sulfamide derivative...
- ThujoneThujoneThujone is a ketone and a monoterpene that occurs naturally in two diastereomeric forms: -α-thujone and -β-thujone. It has a menthol odor. Even though it is best known as a chemical compound in the spirit absinthe, recent tests show absinthe contains only small quantities of thujone, and may or may...
Glycine receptor antagonists
- BrucineBrucineBrucine is a bitter alkaloid closely related to strychnine. It occurs in several plant species, the most well known being the Strychnos nux-vomica tree, found in South-East Asia.While brucine is related to strychnine, it is not as poisonous...
- Colubrine
- Diaboline
- Gelsemine
- Hyenandrine
- StrychnineStrychnineStrychnine is a highly toxic , colorless crystalline alkaloid used as a pesticide, particularly for killing small vertebrates such as birds and rodents. Strychnine causes muscular convulsions and eventually death through asphyxia or sheer exhaustion...
- TutinTutin (toxin)Tutin is a poisonous plant derivative found in the New Zealand tutu plant . It acts as a potent antagonist of the glycine receptor, and has powerful convulsant effects...
Ionotropic glutamate receptor agonists
- AMPAAMPAAMPA is a compound that is a specific agonist for the AMPA receptor, where it mimics the effects of the neurotransmitter glutamate....
- Domoic acidDomoic acidDomoic acid , the neurotoxin that causes amnesic shellfish poisoning , also known as zombie acid, is a kainic acid analog, heterocyclic amino acid associated with certain harmful algal blooms.-Occurrence:...
- Kainic acidKainic acidKainic acid is a natural marine acid present in some seaweed. It is a specific agonist for the kainate receptor used as an ionotropic glutamate receptor which mimics the effect of glutamate...
- NMDANMDAN-Methyl-D-aspartic acid or N-Methyl-D-aspartate is an amino acid derivative which acts as a specific agonist at the NMDA receptor mimicking the action of glutamate, the neurotransmitter which normally acts at that receptor...
- Quisqualic acidQuisqualic acidQuisqualic acid is an agonist for both AMPA receptors and group I metabotropic glutamate receptors. It causes excitotoxicity and is used in neuroscience to selectively destroy neurons in the brain or spinal cord...
- TetrazolylglycineTetrazolylglycineTetrazolylglycine is a potent and selective NMDA receptor agonist, stimulating the NMDA receptor with higher potency than either glutamate or NMDA. It is a potent convulsant and excitotoxin and is used in scientific research....