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Anxiolytic Drug [UPD]



Some medications can have multiple effects. The azapirone drug buspirone and the antihistamine drug hydroxyzine are examples of this. They can increase activity in certain cells and decrease it in others.




anxiolytic drug


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Anxiety is a common condition, meaning, anxiolytic drugs are among the most commonly prescribed medications worldwide. In the United States alone, tens of millions of people have prescriptions to treat anxiety. Additionally, medications with anxiolytic effects are common in treating other conditions.


Anxiety is a common condition, so anxiolytics have been a part or focus of study and research for decades. That means healthcare providers have a greater understanding of prescribing and using them safely and effectively.


One of the biggest advantages of anxiolytic medications is that so many different drugs have this effect. That means if one drug doesn't work, there are other options. It may take some trial and error, but generally, it's possible to find a medication or combination of medications that work for you.


There are other possible drawbacks to anxiolytics. Your healthcare provider can tell you more about the possible concerns you might face. The information they provide will be the most relevant to your situation. They can also tell you what you can do to minimize or avoid possible problems.


The length of time you can stay on an anxiolytic depends on many factors. The specific drug you take, the type of anxiety you experience, your health history, personal preferences and more can all affect this.


Non-benzodiazepine drugs. These have a different structure than benzodiazepines, but they too target GABA in your brain. Non-benzodiazepines are also generally reserved for short-term use. Some include:


Beta-blockers. While normally used for heart conditions, your doctor might prescribe a beta-blocker called propranolol as an off-label anxiolytic. These help relieve anxiety symptoms like an elevated heart rate, sweating, and shaking. Beta-blockers might be prescribed if you have a phobia or overwhelming fear during difficult situations.


Overdose. Never take more medication than your doctor prescribes. Taking high doses of anxiolytics can cause poisoning. Barbiturates are especially dangerous. Symptoms include:


Anxiety disorders are the most prevalent group of psychiatric diseases, and have high personal and societal costs. The search for novel pharmacological treatments for these conditions is driven by the growing medical need to improve on the effectiveness and the side effect profile of existing drugs. A huge volume of data has been generated by anxiolytic drug discovery studies, which has led to the progression of numerous new molecules into clinical trials. However, the clinical outcome of these efforts has been disappointing, as promising results with novel agents in rodent studies have very rarely translated into effectiveness in humans. Here, we analyse the major trends from preclinical studies over the past 50 years conducted in the search for new drugs beyond those that target the prototypical anxiety-associated GABA (γ-aminobutyric acid)-benzodiazepine system, which have focused most intensively on the serotonin, neuropeptide, glutamate and endocannabinoid systems. We highlight various key issues that may have hampered progress in the field, and offer recommendations for how anxiolytic drug discovery can be more effective in the future.


Objectives: To review and describe studies of the non-psychotomimetic constituent of Cannabis sativa, cannabidiol (CBD), as an anxiolytic drug and discuss its possible mechanisms of action.


Method: The articles selected for the review were identified through searches in English, Portuguese, and Spanish in the electronic databases ISI Web of Knowledge, SciELO, PubMed, and PsycINFO, combining the search terms "cannabidiol and anxiolytic", "cannabidiol and anxiolytic-like", and "cannabidiol and anxiety". The reference lists of the publications included, review articles, and book chapters were handsearched for additional references. Experimental animal and human studies were included, with no time restraints.


Results: Studies using animal models of anxiety and involving healthy volunteers clearly suggest an anxiolytic-like effect of CBD. Moreover, CBD was shown to reduce anxiety in patients with social anxiety disorder.


Conclusion: Future clinical trials involving patients with different anxiety disorders are warranted, especially of panic disorder, obsessive-compulsive disorder, social anxiety disorder, and post-traumatic stress disorders. The adequate therapeutic window of CBD and the precise mechanisms involved in its anxiolytic action remain to be determined.


An anxiolytic (/ˌæŋksiəˈlɪtɪk, ˌæŋksioʊ-/; also antipanic or anti-anxiety agent)[1] is a medication or other intervention that reduces anxiety. This effect is in contrast to anxiogenic agents which increase anxiety. Anxiolytic medications are used for the treatment of anxiety disorders and their related psychological and physical symptoms.


The etiology of anxiety disorder remains unknown. There are several contributing factors that are still yet to be proved to cause anxiety disorders.[2] These factors include childhood anxiety, drug induction by central stimulant drugs, metabolic diseases or having depressive disorder.


Anti-anxiety medication is any drug that can be taken or prescribed for the treatment of anxiety disorders, which may be mediated by neurotransmitters like norepinephrine, serotonin, dopamine, and gamma-aminobutyric acid (GABA) in the central nervous system. Anti-anxiety medication can be classified into six types according to their different mechanisms: antidepressants, benzodiazepines, buspirone, antiepileptics, antipsychotics, and beta blockers.


The first monoamine oxidase inhibitor (MAOI), iproniazid, was discovered accidentally when developing the new antitubercular drug isoniazid. The drug was found to cause euphoria and improve the patient's appetite and sleep quality.


Benzodiazepines are used for emergent or short-term management. They are not recommended as the first-line anti-anxiety drugs, but they can be used in combination with SSRIs/SNRIs during the initial treatment stage. Indications include panic disorder, sleep disorders, seizures, acute behavioral disturbance, muscle spasm and premedication and sedation for procedures.


Benzodiazepines bind selectively to the GABA receptor, which is the receptor protein found in the nervous system and is in control of the nervous response. Benzodiazepine will increase the entry of chloride ions into the cells by improving the binding between GABA and GABA receptors and then the better opening of the channel for chloride ion passage. The high level of chloride ion inside the nerve cells makes the nerve more difficult to depolarize and inhibit further nerve signal transduction. The excitability of the nerves then reduces and the nervous system slows down. Therefore, the drug can alleviate symptoms of anxiety disorder and make the person less nervous.[5]


SSRIs can increase anxiety initially due to negative feedback through the serotonergic autoreceptors, for this reason a concurrent benzodiazepine can be used until the anxiolytic effect of the SSRI occurs.[citation needed]


Withdrawal symptoms like dizziness, headache and flu-like symptoms (fatigue/myalgia/loose stool) may occur if SSRI is stopped suddenly. The brain is incapable of upregulating the receptors to sufficient levels especially after discontinuation of the drugs with short half life like paroxetine. Both Fluoxetine and its active metabolite have a long half life therefore it causes the least withdrawal symptoms.[8][11]


Tricyclic antidepressants (TCAs) have anxiolytic effects; however, side effects are often more troubling or severe and overdose is dangerous. They are considered effective, but have generally been replaced by antidepressants that cause different adverse effects. Examples include imipramine, doxepin, amitriptyline, nortriptyline and desipramine.[13][14]


Barbiturates are powerful anxiolytics but 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.[17]


Sympatholytics are a group of anti-hypertensives which inhibit activity of the sympathetic nervous system. Beta blockers reduce anxiety by decreasing heart rate and preventing shaking. Beta blockers include propranolol, oxprenolol, and metoprolol.[21][22] The Alpha-1 agonist prazosin could be effective for PTSD.[23] The Alpha-2 agonists clonidine and guanfacine have demonstrated both anxiolytic and anxiogenic effects.[24]


Pregabalin (Lyrica) produces anxiolytic effect after one week of use comparable to lorazepam, alprazolam, and venlafaxine with more consistent psychic and somatic anxiety reduction. Unlike BZDs, it does not disrupt sleep architecture nor does it causecognitive or psychomotor impairment.[27][28]


Phenibut (Anvifen, Fenibut, Noofen) is an anxiolytic[30] used in Russia.[31] Phenibut is a GABAB receptor agonist,[30] as well as an antagonist at α2δ subunit-containing voltage-dependent calcium channels (VDCCs), similarly to gabapentinoids like gabapentin and pregabalin.[32] The medication is not approved by the FDA for use in the United States, but is sold online as a supplement.[33][34]


Fabomotizole (Afobazole) is an anxiolytic drug launched in Russia in the early 2000s. Its mechanism of action is poorly-defined, with GABAergic, NGF and BDNF release promoting, MT1 receptor agonism, MT3 receptor antagonism, and sigma agonism thought to have some involvement.[37][38]


Bromantane is a stimulant drug with anxiolytic properties developed in Russia during the late 1980s. Bromantane acts mainly by facilitating the biosynthesis of dopamine, through indirect genomic upregulation of relevant enzymes (tyrosine hydroxylase (TH) and aromatic L-amino acid decarboxylase (AAAD)).[39][40] 041b061a72


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