Anxiolytic
Encyclopedia
An anxiolytic is a drug
used for the treatment of anxiety
, and its related psychological and physical symptoms. Anxiolytics have been shown to be useful in the treatment of anxiety disorder
s.
Beta-receptor blockers such as propranolol and oxprenolol
, although not anxiolytics, can be used to combat the somatic
symptoms of anxiety.
Anxiolytics are also known as minor tranquilizer
s. The term is less common in modern texts, and was originally derived from a dichotomy with major tranquilizers, also known as neuroleptics or antipsychotics.
sedation
is needed. Longer-term uses include treatment for severe anxiety. There is a risk of a benzodiazepine withdrawal and rebound syndrome after continuous usage for longer than two weeks, and tolerance and dependence may occur if patients stay under this treatment for longer. There is also the added problem of the accumulation of drug metabolite
s and adverse effects. Benzodiazepines include:
Benzodiazepines exert their anxiolytic properties at moderate dosage. At higher dosage hypnotic
properties occur.
s in the treatment of depression, anxiety disorder
s, and some personality disorder
s. SSRIs are primarily classified as antidepressants and typically higher dosages are required to be effective against anxiety disorders than to be effective against depression but nevertheless most SSRIs have anxiolytic properties, but are anxiogenic
when first initiating treatment, and in some individuals continue to be anxiety-provoking. For this reason, a low dose of a benzodiazepine is often used for several weeks when initiating SSRI/SNRI therapy in order to counteract the initial anxiety caused by the drugs until the therapeutic delay of the SSRI/SNRI is finished and the drug becomes effective. Older tricyclic antidepressants (TCAs) are very anxiolytic as well, however, side effects are greater. Examples include: imipramine, doxepin, amitriptyline, and the unrelated trazodone. Mono-amine oxidase inhibitors (MAOIs) are very effective for anxiety, but due to drug dangers, are rarely prescribed. Examples include: Nardil and Parnate.
agonist
s. They lack the sedation and the dependence
associated with benzodiazepines and cause much less cognitive impairment. They may be less effective than benzodiazepines in patients who have been previously treated with benzodiazepines as they do not provide the sedation that these patients may expect or equate with anxiety relief. Currently approved azapirones include buspirone
(Buspar) and tandospirone
(Sediel). Gepirone
(Ariza, Variza) is also in clinical development.
s exert an anxiolytic effect linked to the sedation they cause. The risk of abuse and addiction is high. Many experts consider these drugs obsolete for treating anxiety but valuable for the short-term treatment of severe insomnia, though only after benzodiazepines or non-benzodiazepines have failed. They are rarely prescribed anymore.
(Atarax) is an old antihistamine
originally approved for clinical use by the FDA in 1956. It possesses anxiolytic properties in addition to its antihistamine properties and is also licensed for the treatment of anxiety and tension. It is also used for its sedative properties as a premed before anesthesia or to induce sedation after anesthesia. It has been shown to be as effective as benzodiazepines in the treatment of generalized anxiety disorder, while producing fewer side-effects.
's therapeutic effect appears 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 psychic and somatic anxiety symptoms. Long-term trials have shown continued effectiveness without the development of tolerance, and, in addition, unlike benzodiazepines, it does not disrupt sleep architecture
and produces less severe cognitive and psychomotor impairment; it also has a low potential for abuse and dependence and may be preferred over the benzodiazepines for these reasons.
is a prodrug
formed by combining niacin
with GABA
that is able to cross the blood-brain barrier and is then hydrolyzed into GABA and niacin. It is theorized that the GABA released in this process activates GABA receptors, with potential to produce an anxiolytic response.
Picamilon is sold in the United States as a dietary supplement, while in Russia it is sold over the counter.
Chlorpheniramine (Chlor-Trimeton) and diphenhydramine
(Benadryl) have hypnotic
and sedative
effects with mild anxiolytic-like properties (off-label use). These drugs are approved by the FDA for allergies
, rhinitis
, and urticaria
.
Medication
A pharmaceutical drug, also referred to as medicine, medication or medicament, can be loosely defined as any chemical substance intended for use in the medical diagnosis, cure, treatment, or prevention of disease.- Classification :...
used for the treatment of anxiety
Anxiety
Anxiety is a psychological and physiological state characterized by somatic, emotional, cognitive, and behavioral components. The root meaning of the word anxiety is 'to vex or trouble'; in either presence or absence of psychological stress, anxiety can create feelings of fear, worry, uneasiness,...
, and its related psychological and physical symptoms. Anxiolytics have been shown to be useful in the treatment of anxiety disorder
Anxiety disorder
Anxiety disorder is a blanket term covering several different forms of abnormal and pathological fear and anxiety. Conditions now considered anxiety disorders only came under the aegis of psychiatry at the end of the 19th century. Gelder, Mayou & Geddes explains that anxiety disorders are...
s.
Beta-receptor blockers such as propranolol and oxprenolol
Oxprenolol
Oxprenolol is a non-selective beta blocker with some intrinsic sympathomimetic activity...
, although not anxiolytics, can be used to combat the somatic
Somatic
The term somatic means 'of the body',, relating to the body. In medicine, somatic illness is bodily, not mental, illness. The term is often used in biology to refer to the cells of the body in contrast to the germ line cells which usually give rise to the gametes...
symptoms of anxiety.
Anxiolytics are also known as minor tranquilizer
Tranquilizer
A tranquilizer, or tranquilliser , is a drug that induces tranquility in an individual.The term "tranquilizer" is imprecise, and is usually qualified, or replaced with more precise terms:...
s. The term is less common in modern texts, and was originally derived from a dichotomy with major tranquilizers, also known as neuroleptics or antipsychotics.
Benzodiazepines
Benzodiazepines are prescribed for short-term relief of severe and disabling anxiety. Benzodiazepines may also be indicated to cover the latent periods associated with the medications prescribed to treat an underlying anxiety disorder. They are used to treat a wide variety of conditions and symptoms and are usually a first choice when short-term CNSCentral nervous system
The central nervous system is the part of the nervous system that integrates the information that it receives from, and coordinates the activity of, all parts of the bodies of bilaterian animals—that is, all multicellular animals except sponges and radially symmetric animals such as jellyfish...
sedation
Sedation
Sedation is the reduction of irritability or agitation by administration of sedative drugs, generally to facilitate a medical procedure or diagnostic procedure...
is needed. Longer-term uses include treatment for severe anxiety. There is a risk of a benzodiazepine withdrawal and rebound syndrome after continuous usage for longer than two weeks, and tolerance and dependence may occur if patients stay under this treatment for longer. There is also the added problem of the accumulation of drug metabolite
Metabolite
Metabolites are the intermediates and products of metabolism. The term metabolite is usually restricted to small molecules. A primary metabolite is directly involved in normal growth, development, and reproduction. Alcohol is an example of a primary metabolite produced in large-scale by industrial...
s and adverse effects. Benzodiazepines include:
- AlprazolamAlprazolamAlprazolam is a short-acting anxiolytic of the benzodiazepine class of psychoactive drugs. Alprazolam, like other benzodiazepines, binds to specific sites on the GABAA gamma-amino-butyric acid receptor...
(Xanax) - ChlordiazepoxideChlordiazepoxideChlordiazepoxide, is a sedative/hypnotic drug and benzodiazepine. It is marketed under the trade names Angirex, Klopoxid, Librax , Libritabs, Librium, Mesural, Multum, Novapam, Risolid, Silibrin, Sonimen and Tropium.Chlordiazepoxide was the first benzodiazepine to be synthesised and...
(Librium) - ClonazepamClonazepamClonazepamis a benzodiazepine drug having anxiolytic, anticonvulsant, muscle relaxant, and hypnotic properties. It is marketed by Roche under the trade name Klonopin in the United States and Rivotril in Australia, Brazil, Canada and Europe...
(Klonopin) - DiazepamDiazepamDiazepam , first marketed as Valium by Hoffmann-La Roche is a benzodiazepine drug. Diazepam is also marketed in Australia as Antenex. It is commonly used for treating anxiety, insomnia, seizures including status epilepticus, muscle spasms , restless legs syndrome, alcohol withdrawal,...
(Valium) - EtizolamEtizolamEtizolam is a thienodiazepine drug which is a benzodiazepine analog. The etizolam molecule differs from most other benzodiazepines in that the benzene ring has been replaced by a thiophene ring...
(Etilaam) - LorazepamLorazepamLorazepam is a high-potency short-to-intermediate-acting 3-hydroxy benzodiazepine drug that has all five intrinsic benzodiazepine effects: anxiolytic, amnesic, sedative/hypnotic, anticonvulsant, antiemetic and muscle relaxant...
(Ativan) - OxazepamOxazepamOxazepam , is a drug which is a short to intermediate acting 3-hydroxy benzodiazepine derivative...
(Serax)
Benzodiazepines exert their anxiolytic properties at moderate dosage. At higher dosage hypnotic
Hypnotic
Hypnotic drugs are a class of psychoactives whose primary function is to induce sleep and to be used in the treatment of insomnia and in surgical anesthesia...
properties occur.
- TofisopamTofisopamTofisopam is a drug which is a benzodiazepine derivative. Like other benzodiazepines, it possesses anxiolytic properties but unlike other benzodiazepines it does not have anticonvulsant, sedative, skeletal muscle relaxant, motor skill-impairing or amnestic properties...
(Emandaxin and Grandaxin) is a drug that is a benzodiazepine derivative. Like other benzodiazepines, it possesses anxiolytic properties, but, unlike other benzodiazepines, it does not have anticonvulsant, sedative, skeletal muscle relaxant, motor skill-impairing, or amnestic properties.
SSRIs
Selective serotonin reuptake inhibitors or serotonin-specific reuptake inhibitor (SSRIs) are a class of compounds typically used as antidepressantAntidepressant
An antidepressant is a psychiatric medication used to alleviate mood disorders, such as major depression and dysthymia and anxiety disorders such as social anxiety disorder. According to Gelder, Mayou &*Geddes people with a depressive illness will experience a therapeutic effect to their mood;...
s in the treatment of depression, anxiety disorder
Anxiety disorder
Anxiety disorder is a blanket term covering several different forms of abnormal and pathological fear and anxiety. Conditions now considered anxiety disorders only came under the aegis of psychiatry at the end of the 19th century. Gelder, Mayou & Geddes explains that anxiety disorders are...
s, and some personality disorder
Personality disorder
Personality disorders, formerly referred to as character disorders, are a class of personality types and behaviors. Personality disorders are noted on Axis II of the Diagnostic and Statistical Manual of Mental Disorders or DSM-IV-TR of the American Psychiatric Association.Personality disorders are...
s. SSRIs are primarily classified as antidepressants and typically higher dosages are required to be effective against anxiety disorders than to be effective against depression but nevertheless most SSRIs have anxiolytic properties, but are anxiogenic
Anxiogenic
An anxiogenic substance is one that causes anxiety. Anxiogenic effects can be measured by, for example, the hole-board test in rats and mice. A number of agents are used to provoke anxiety or panic in experimental models...
when first initiating treatment, and in some individuals continue to be anxiety-provoking. For this reason, a low dose of a benzodiazepine is often used for several weeks when initiating SSRI/SNRI therapy in order to counteract the initial anxiety caused by the drugs until the therapeutic delay of the SSRI/SNRI is finished and the drug becomes effective. Older tricyclic antidepressants (TCAs) are very anxiolytic as well, however, side effects are greater. Examples include: imipramine, doxepin, amitriptyline, and the unrelated trazodone. Mono-amine oxidase inhibitors (MAOIs) are very effective for anxiety, but due to drug dangers, are rarely prescribed. Examples include: Nardil and Parnate.
Azapirones
Azapirones are a class of 5-HT1A receptor5-HT1A receptor
The 5-HT1A receptor is a subtype of 5-HT receptor that binds the endogenous neurotransmitter serotonin . It is a G protein-coupled receptor that is coupled to Gi/Go and mediates inhibitory neurotransmission...
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. They lack the sedation and the dependence
Substance use disorder
Substance use disorders include substance abuse and substance dependence. In DSM-IV, the conditions are formally diagnosed as one or the other, but it has been proposed that DSM-5 combine the two into a single condition called "Substance-use disorder"....
associated with benzodiazepines and cause much less cognitive impairment. They may be less effective than benzodiazepines in patients who have been previously treated with benzodiazepines as they do not provide the sedation that these patients may expect or equate with anxiety relief. Currently approved azapirones include buspirone
Buspirone
Buspirone is an anxiolytic psychoactive drug of the azapirone chemical class, and is primarily used to treat generalized anxiety disorder Bristol-Myers Squibb gained FDA approval of buspirone in 1986 for treatment of GAD...
(Buspar) and tandospirone
Tandospirone
Tandospirone , also known as metanopirone, is an anxiolytic and antidepressant used in China and Japan, where it is marketed by Dainippon Sumitomo Pharma...
(Sediel). Gepirone
Gepirone
Gepirone is a psychoactive drug and research chemical of the piperazine and azapirone chemical classes. It is currently under clinical development in an extended release form as an anxiolytic and antidepressant agent...
(Ariza, Variza) is also in clinical development.
Barbiturates
BarbiturateBarbiturate
Barbiturates are drugs that act as central nervous system depressants, and can therefore produce a wide spectrum of effects, from mild sedation to total anesthesia. They are also effective as anxiolytics, as hypnotics, and as anticonvulsants...
s exert an anxiolytic effect linked to the sedation they cause. The risk of abuse and addiction is high. Many experts consider these drugs obsolete for treating anxiety but valuable for the short-term treatment of severe insomnia, though only after benzodiazepines or non-benzodiazepines have failed. They are rarely prescribed anymore.
Hydroxyzine
HydroxyzineHydroxyzine
Hydroxyzine is a first-generation antihistamine of the diphenylmethane and piperazine classes. It was first synthesized by Union Chimique Belge in 1956 and was marketed by Pfizer in the United States later the same year, and is still in widespread use today....
(Atarax) is an old antihistamine
Antihistamine
An H1 antagonist is a histamine antagonist of the H1 receptor that serves to reduce or eliminate effects mediated by histamine, an endogenous chemical mediator released during allergic reactions...
originally approved for clinical use by the FDA in 1956. It possesses anxiolytic properties in addition to its antihistamine properties and is also licensed for the treatment of anxiety and tension. It is also used for its sedative properties as a premed before anesthesia or to induce sedation after anesthesia. It has been shown to be as effective as benzodiazepines in the treatment of generalized anxiety disorder, while producing fewer side-effects.
Pregabalin
PregabalinPregabalin
Pregabalin is an anticonvulsant drug used for neuropathic pain and as an adjunct therapy for partial seizures with or without secondary generalization in adults. It has also been found effective for generalized anxiety disorder and is approved for this use in the European Union. It was designed...
's therapeutic effect appears after 1 week of use and is similar in effectiveness to lorazepam
Lorazepam
Lorazepam is a high-potency short-to-intermediate-acting 3-hydroxy benzodiazepine drug that has all five intrinsic benzodiazepine effects: anxiolytic, amnesic, sedative/hypnotic, anticonvulsant, antiemetic and muscle relaxant...
, alprazolam
Alprazolam
Alprazolam is a short-acting anxiolytic of the benzodiazepine class of psychoactive drugs. Alprazolam, like other benzodiazepines, binds to specific sites on the GABAA gamma-amino-butyric acid receptor...
, and venlafaxine
Venlafaxine
Venlafaxine is an antidepressant of the serotonin-norepinephrine reuptake inhibitor class. First introduced by Wyeth in 1993, now marketed by Pfizer, it is licensed for the treatment of major depressive disorder , as a treatment for generalized anxiety disorder, and comorbid indications in...
, but pregabalin has demonstrated superiority by producing more consistent therapeutic effects for psychic and somatic anxiety symptoms. Long-term trials have shown continued effectiveness without the development of tolerance, and, in addition, unlike benzodiazepines, it does not disrupt sleep architecture
Sleep architecture
Sleep architecture describes the structure and pattern of sleep and encompasses several variables. Sleep quotas refer to the amount of time spent in REM and NREM sleep. Sleep duration is the total time spent asleep in a 24 hour period. The duration of a NREM-REM cycle is also an important aspect...
and produces less severe cognitive and psychomotor impairment; it also has a low potential for abuse and dependence and may be preferred over the benzodiazepines for these reasons.
Herbal treatments
Certain natural substances are reputed to have anxiolytic properties, including the following:- Bacopa monnieriBacopa monnieriBacopa monnieri is a perennial, creeping herb whose habitat includes wetlands and muddy shores...
(Brahmi) - Lactuca virosaLactuca virosaLactuca virosa is a plant in the Lactuca genus, ingested often for its mild psychotropic effects which are often described as being similar to that of opium. It is related to common lettuce Lactuca virosa is a plant in the Lactuca (lettuce) genus, ingested often for its mild psychotropic...
(Opium Lettuce) - Rhodiola roseaRhodiola roseaRhodiola rosea is a plant in the Crassulaceae family that grows in cold regions of the world. These include much of the Arctic, the mountains of Central Asia, the Rocky Mountains, and mountainous parts of Europe, such as the Alps, Pyrenees, Carpathian Mountains, Scandinavia, Iceland, Great...
(Arctic Weed/Golden Root) - Hypericum perforatum (St. John's Wort)
- Matricaria recutita (German Chamomile)
- Mitragyna speciosa (Kratom)
- Piper methysticum (Kava)
- Sceletium tortuosumSceletium tortuosumSceletium tortuosum is a succulent herb commonly found in South Africa, which is also known as Kanna, Channa, Kougoed - which literally means, 'chew things/goodies' or 'something to chew'...
(Kanna) - Scutellaria spp.ScutellariaScutellaria is a genus of flowering plants in the mint family, Lamiaceae. It contains about 300 species, which are commonly known as skullcaps...
(Skullcap)- Scutellaria laterifloraScutellaria laterifloraScutellaria lateriflora, also known as Blue Skullcap, Hoodwort, Virginian Skullcap, Mad-dog Skullcap is a hardy perennial herb native to North America. It is a member of the mint family. It has an upright habit, growing 60 to 80 centimeters in maximum height. It is a wetland-loving species and...
- Scutellaria lateriflora
- Valeriana officinalis (Valerian)
- Salvia splendensSalvia splendensSalvia splendens is a tender herbaceous perennial that is native to Brazil, growing at elevation where it is warm year-round and with high humidity. The native plant, rarely seen in cultivation, reaches tall. Smaller selections are very popular as bedding plants, seen in shopping malls and...
(Not to be confused with Salvia divinorum) - Coriandrum sativum (Coriander)
- Myristica (Nutmeg)
- Salvia Elegans (Pineapple Sage)
- InositolInositolInositol or cyclohexane-1,2,3,4,5,6-hexol is a chemical compound with formula 6126 or 6, a sixfold alcohol of cyclohexane. It exists in nine possible stereoisomers, of which the most prominent form, widely occurring in nature, is cis-1,2,3,5-trans-4,6-cyclohexanehexol, or myo-inositol...
In a double-blind, controlled trial, myo-inositol (18 grams daily) was superior to fluvoxamineFluvoxamineFluvoxamine is an antidepressant which functions as a selective serotonin reuptake inhibitor . Fluvoxamine was first approved by the U.S. Food and Drug Administration in 1993 for the treatment of obsessive compulsive disorder . Fluvoxamine CR is approved to treat social anxiety disorder...
for decreasing the number of panic attacks and had fewer side-effectAdverse effectIn medicine, an adverse effect is a harmful and undesired effect resulting from a medication or other intervention such as surgery.An adverse effect may be termed a "side effect", when judged to be secondary to a main or therapeutic effect. If it results from an unsuitable or incorrect dosage or...
s. - CannabidiolCannabidiolCannabidiol is a cannabinoid found in Cannabis. It is a major constituent of the plant, representing up to 40% in its extracts.It has displayed sedative effects in animal tests...
(Marijuana)
Over-the-counter pharmaceutical drugs
PicamilonPicamilon
Picamilon is a dietary supplement formed by combining niacin with GABA. It was developed in the Soviet Union in 1969 by the All-Union Vitamins Scientific Research Institute and further studied in both Russia and Japan as a prodrug of GABA.Picamilon is sold in the United States as a dietary...
is a prodrug
Prodrug
A prodrug is a pharmacological substance administered in an inactive form. Once administered, the prodrug is metabolised in vivo into an active metabolite, a process termed bioactivation. The rationale behind the use of a prodrug is generally for absorption, distribution, metabolism, and...
formed by combining niacin
Niacin
"Niacin" redirects here. For the neo-fusion band, see Niacin .Niacin is an organic compound with the formula and, depending on the definition used, one of the forty to eighty essential human nutrients.Niacin is one of five vitamins associated with a pandemic deficiency disease: niacin deficiency...
with GABA
Gabâ
Gabâ or gabaa, for the people in many parts of the Philippines), is the concept of a non-human and non-divine, imminent retribution. A sort of negative karma, it is generally seen as an evil effect on a person because of their wrongdoings or transgressions...
that is able to cross the blood-brain barrier and is then hydrolyzed into GABA and niacin. It is theorized that the GABA released in this process activates GABA receptors, with potential to produce an anxiolytic response.
Picamilon is sold in the United States as a dietary supplement, while in Russia it is sold over the counter.
Chlorpheniramine (Chlor-Trimeton) and diphenhydramine
Diphenhydramine
Diphenhydramine hydrochloride is a first-generation antihistamine possessing anticholinergic, antitussive, antiemetic, and sedative properties which is mainly used to treat allergies. Like most other first-generation antihistamines, the drug also has a powerful hypnotic effect, and for this reason...
(Benadryl) have hypnotic
Hypnotic
Hypnotic drugs are a class of psychoactives whose primary function is to induce sleep and to be used in the treatment of insomnia and in surgical anesthesia...
and sedative
Sedative
A sedative or tranquilizer is a substance that induces sedation by reducing irritability or excitement....
effects with mild anxiolytic-like properties (off-label use). These drugs are approved by the FDA for allergies
Allergy
An Allergy is a hypersensitivity disorder of the immune system. Allergic reactions occur when a person's immune system reacts to normally harmless substances in the environment. A substance that causes a reaction is called an allergen. These reactions are acquired, predictable, and rapid...
, rhinitis
Rhinitis
Rhinitis , commonly known as a stuffy nose, is the medical term describing irritation and inflammation of some internal areas of the nose. The primary symptom of rhinitis is nasal dripping. It is caused by chronic or acute inflammation of the mucous membrane of the nose due to viruses, bacteria or...
, and urticaria
Urticaria
Urticaria is a kind of skin rash notable for pale red, raised, itchy bumps. Hives is frequently caused by allergic reactions; however, there are many non-allergic causes...
.
Future drugs
Due to deficits with existing anxiolytics (either in terms of efficacy or side-effect profile), research into novel anxiolytics is active. Possible candidates for future drugs include:- BNC210BNC210BNC210 is a novel anxiolytic drug with unknown mechanism of origin. It demonstrates clinically significant anxiety reduction in both animal models and the Phase I trials....
- CL-218,872CL-218,872CL-218,872 is a sedative and hypnotic drug used in scientific research. It has similar effects to sedative-hypnotic benzodiazepine drugs such as triazolam, but is structurally distinct and so is classed as a nonbenzodiazepine hypnotic....
- L-838,417L-838,417L-838,417 is an anxiolytic drug used in scientific research. It has similar effects to benzodiazepine drugs, but is structurally distinct and so is classed as a nonbenzodiazepine anxiolytic...
- SL-651,498SL-651,498SL-651,498 is an anxiolytic and anticonvulsant drug used in scientific research, with a chemical structure most closely related to β-carboline derivatives such as abecarnil and gedocarnil...