|
Setiptiline
Setiptiline (brand name Tecipul), also known as teciptiline, is a tetracyclic antidepressant (TeCA) that acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). It was launched in 1989 for the treatment of depression in Japan by Mochida. Pharmacology Pharmacodynamics Setiptiline acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotonin receptor antagonist, likely at the 5-HT2 subtypes, as well as an H1 receptor inverse agonist/antihistamine. Chemistry Setiptiline has a tetracyclic structure and is a close analogue of mianserin and mirtazapine, with setiptiline being delta(13b,4a),4a-carba-mianserin, and mirtazapine being 6-azamianserin. See also * Aptazapine * Mianserin * Mirtazapine Mirtazapine, sold under the brand name Remeron among others, is an atypical antidepressant, atypical tetracyclic antidepressant, and as such is used primarily to treat Depression (mood), depression. Its effects may take up to ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Noradrenergic And Specific Serotonergic Antidepressants
Noradrenergic and specific serotonergic antidepressants (NaSSAs) are a class of psychiatric drugs used primarily as antidepressants. They act by antagonizing the α2-adrenergic receptor and certain serotonin receptors such as 5-HT2A and 5-HT2C, but also 5-HT3, 5-HT6, and/or 5-HT7 in some cases. By blocking α2-adrenergic autoreceptors and heteroreceptors, NaSSAs enhance adrenergic and serotonergic neurotransmission in the brain involved in mood regulation, notably 5-HT1A-mediated transmission. In addition, due to their blockade of certain serotonin receptors, serotonergic neurotransmission is not facilitated in unwanted areas, which prevents the incidence of many side effects often associated with selective serotonin reuptake inhibitor (SSRI) antidepressants; hence, in part, the "specific serotonergic" label of NaSSAs. List of NaSSAs The NaSSAs include the following agents: * Aptazapine (CGS-7525A) * Esmirtazapine (ORG-50,081) * Mianserin (Bolvidon, Norval, Tolvon) * Mi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tetracyclic Antidepressant
Tetracyclic antidepressants (TeCAs) are a class of antidepressants that were first introduced in the 1970s. They are named after their tetracyclic chemical structure, containing four cyclic compound, rings of atoms, and are closely related to the tricyclic antidepressants (TCAs), which contain three rings of atoms. List of TeCAs Marketed * Maprotiline (Ludiomil) – can also be classified as a TCA and grouped with the secondary amines * Mianserin (Tolvon) * Mirtazapine (Remeron) * Setiptiline (Tecipul) Drugs that contain four rings not all fused together but are sometimes still classified as TeCAs include: * Amoxapine (Asendin) – often classified as a TCA and grouped with the secondary amines * Quetiapine (Seroquel) - an atypical antipsychotic sometimes used as an adjunct antidepressant Miscellaneous * Benzoctamine (Tacitin) – a tetracyclic compound and is closely related to maprotiline, with the two compounds differing only in the length of their side chain, but benzocta ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Noradrenergic And Specific Serotonergic Antidepressant
Noradrenergic and specific serotonergic antidepressants (NaSSAs) are a class of psychiatric drugs used primarily as antidepressants. They act by antagonizing the α2-adrenergic receptor and certain serotonin receptors such as 5-HT2A and 5-HT2C, but also 5-HT3, 5-HT6, and/or 5-HT7 in some cases. By blocking α2-adrenergic autoreceptors and heteroreceptors, NaSSAs enhance adrenergic and serotonergic neurotransmission in the brain involved in mood regulation, notably 5-HT1A-mediated transmission. In addition, due to their blockade of certain serotonin receptors, serotonergic neurotransmission is not facilitated in unwanted areas, which prevents the incidence of many side effects often associated with selective serotonin reuptake inhibitor (SSRI) antidepressants; hence, in part, the "specific serotonergic" label of NaSSAs. List of NaSSAs The NaSSAs include the following agents: * Aptazapine (CGS-7525A) * Esmirtazapine (ORG-50,081) * Mianserin (Bolvidon, Norval, Tolvon) ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Alpha-2 Adrenergic Receptor
The alpha-2 (α2) adrenergic receptor (or adrenoceptor) is a G protein-coupled receptor (GPCR) associated with the Gi alpha subunit, Gi heterotrimeric G-protein. It consists of three highly homologous subtypes, including α2A-adrenergic, α2A-, α2B-adrenergic, α2B-, and α2C-adrenergic, α2C-adrenergic. Some species other than humans express a fourth α2D-adrenergic receptor as well. Catecholamines like norepinephrine (noradrenaline) and epinephrine (adrenaline) signal through the α2-adrenergic receptor in the central nervous system, central and peripheral nervous systems. Cellular localization The Alpha-2A adrenergic receptor, α2A adrenergic receptor is localised in the following central nervous system (CNS) structures: * Brainstem (especially the locus coeruleus as presynaptic & somatodendritic autoreceptor ) * Midbrain * Hypothalamus * Olfactory system * Hippocampus * Spinal cord * Cerebral cortex * Cerebellum * Septum Whereas the Alpha-2B adrenergic receptor, α2B adren ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Antihistamine
Antihistamines are drugs which treat allergic rhinitis, common cold, influenza, and other allergies. Typically, people take antihistamines as an inexpensive, generic (not patented) drug that can be bought without a prescription and provides relief from nasal congestion, sneezing, or hives caused by pollen, dust mites, or animal allergy with few side effects. Antihistamines are usually for short-term treatment. Chronic allergies increase the risk of health problems which antihistamines might not treat, including asthma, sinusitis, and lower respiratory tract infection. Consultation of a medical professional is recommended for those who intend to take antihistamines for longer-term use. Although the general public typically uses the word "antihistamine" to describe drugs for treating allergies, physicians and scientists use the term to describe a class of drug that opposes the activity of histamine receptors in the body. In this sense of the word, antihistamines are subc ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Aptazapine
Aptazapine (developmental code name CGS-7525A) is a tetracyclic antidepressant (TeCA) that was assayed in clinical trials for the treatment of depression in the 1980s but was never marketed. It is a potent α2-adrenergic receptor antagonist with about 10 times the strength of the related compound mianserin and has also been shown to act as a 5-HT2 receptor antagonist and H1 receptor inverse agonist, while having no significant effects on the reuptake of serotonin or norepinephrine. Based on its pharmacological profile, aptazapine may be classified as a noradrenergic and specific serotonergic antidepressant (NaSSA). See also * Mianserin * Mirtazapine Mirtazapine, sold under the brand name Remeron among others, is an atypical antidepressant, atypical tetracyclic antidepressant, and as such is used primarily to treat Depression (mood), depression. Its effects may take up to four weeks but ca ... * Setiptiline References External links * {{Tricyclics Abandoned dru ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
H1 Receptor Antagonists
H1 antagonists, also called H1 blockers, are a class of medications that block the action of histamine at the H1 receptor, helping to relieve allergic reactions. Agents where the main therapeutic effect is mediated by negative modulation of histamine receptors are termed antihistamines; other agents may have antihistaminergic action but are not true antihistamines. In common use, the term "antihistamine" refers only to H1-antihistamines. Virtually all H1-antihistamines function as inverse agonists at the histamine H1-receptor, as opposed to neutral antagonists, as was previously believed. Medical uses H1-antihistamines are used clinically to treat histamine-mediated allergic conditions. These indications may include:Rossi S (Ed.) (2004). ''Australian Medicines Handbook 2004''. Adelaide: Australian Medicines Handbook. * Allergic rhinitis * Allergic conjunctivitis * Allergic skin, dermatological conditions (contact dermatitis) * Rhinorrhea (runny nose) * Urticaria * Angioedema ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pharmacodynamics
Pharmacodynamics (PD) is the study of the biochemistry, biochemical and physiology, physiologic effects of drugs (especially pharmaceutical drugs). The effects can include those manifested within animals (including humans), microorganisms, or combinations of organisms (for example, infection). Pharmacodynamics and pharmacokinetics are the main branches of pharmacology, being itself a topic of biology interested in the study of the interactions of both endogenous and exogenous chemical substances with living organisms. In particular, pharmacodynamics is the study of how a drug affects an organism, whereas pharmacokinetics is the study of how the organism affects the drug. Both together influence dosing, benefit, and adverse effects. Pharmacodynamics is sometimes abbreviated as PD and pharmacokinetics as PK, especially in combined reference (for example, when speaking of PK/PD models). Pharmacodynamics places particular emphasis on dose–response relationships, that is, the relat ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Mirtazapine
Mirtazapine, sold under the brand name Remeron among others, is an atypical antidepressant, atypical tetracyclic antidepressant, and as such is used primarily to treat Depression (mood), depression. Its effects may take up to four weeks but can also manifest as early as one to two weeks. It is often used in cases of depression complicated by anxiety or insomnia. The effectiveness of mirtazapine is comparable to other commonly prescribed antidepressants. It is taken oral administration, by mouth. Common side effects include somnolence, sleepiness, vertigo, dizziness, hyperphagia, increased appetite, and weight gain. Serious side effects may include mania, neutropenia, low white blood cell count, and increased suicide among children. Drug withdrawal, Withdrawal symptoms may occur with stopping. It is not recommended together with a monoamine oxidase inhibitor, although evidence supporting the danger of this combination has been challenged. It is unclear if use during pregnancy i ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Mianserin
Mianserin, sold under the brand name Tolvon among others, is an atypical antidepressant that is used primarily in the treatment of depression in Europe and elsewhere in the world. It is a tetracyclic antidepressant (TeCA). Mianserin is closely related to mirtazapine, both chemically and in terms of its actions and effects, although there are significant differences between the two drugs (for example, its higher noradrenergic activity and lower 5-HT3 receptor antagonism). Medical uses Mianserin at higher doses (30–90 mg/day) is used for the treatment of major depressive disorder. It can also be used at lower doses (around 10 mg/day) to treat insomnia. Contraindications It should not be given, except if based on clinical need and under strict medical supervision, to people younger than 18 years old, as it can increase the risk of suicide attempts and suicidal thinking, and it can increase aggressiveness. While there is no evidence that it can harm a fetus fr ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
