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Cidoxepin

Index Cidoxepin

Cidoxepin (former developmental code name P-4599), also known as cis-doxepin or (Z)-doxepin, is a tricyclic antidepressant which was developed in the 1960s but was never marketed. [1]

21 relations: Allergic rhinitis, Anticholinergic, Antidepressant, Antihistamine, Atopic dermatitis, Biological activity, Central nervous system, Clinical trial, Contact dermatitis, Dermatitis, Doxepin, Esmirtazapine, Histamine H1 receptor, Hives, Mixture, Nordoxepin, Pharmacodynamics, Receptor antagonist, Serotonin–norepinephrine reuptake inhibitor, Stereoisomerism, Tricyclic antidepressant.

Allergic rhinitis

Allergic rhinitis, also known as hay fever, is a type of inflammation in the nose which occurs when the immune system overreacts to allergens in the air.

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Anticholinergic

An anticholinergic agent is a substance that blocks the neurotransmitter acetylcholine in the central and the peripheral nervous system.

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Antidepressant

Antidepressants are drugs used for the treatment of major depressive disorder and other conditions, including dysthymia, anxiety disorders, obsessive–compulsive disorder, eating disorders, chronic pain, neuropathic pain and, in some cases, dysmenorrhoea, snoring, migraine, attention-deficit hyperactivity disorder (ADHD), addiction, dependence, and sleep disorders.

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Antihistamine

Antihistamines are drugs which treat allergic rhinitis and other allergies.

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Atopic dermatitis

Atopic dermatitis (AD), also known as atopic eczema, is a type of inflammation of the skin (dermatitis).

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Biological activity

In pharmacology, biological activity or pharmacological activity describes the beneficial or adverse effects of a drug on living matter.

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Central nervous system

The central nervous system (CNS) is the part of the nervous system consisting of the brain and spinal cord.

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Clinical trial

Clinical trials are experiments or observations done in clinical research.

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Contact dermatitis

Contact dermatitis is a type of inflammation of the skin.

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Dermatitis

Dermatitis, also known as eczema, is a group of diseases that results in inflammation of the skin.

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Doxepin

Doxepin is a tricyclic antidepressant (TCA) used as a pill to treat major depressive disorder, anxiety disorders, chronic hives, and for short-term help with trouble remaining asleep after going to bed (a form of insomnia).

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Esmirtazapine

Esmirtazapine (ORG-50,081) is a drug which was under development by Organon for the treatment of insomnia and vasomotor symptoms (e.g., hot flashes) associated with menopause.

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Histamine H1 receptor

The H1 receptor is a histamine receptor belonging to the family of rhodopsin-like G-protein-coupled receptors.

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Hives

Hives, also known as urticaria, is a kind of skin rash with red, raised, itchy bumps.

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Mixture

In chemistry, a mixture is a material made up of two or more different substances which are mixed.

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Nordoxepin

Nordoxepin, also known as N-desmethyldoxepin, is the major active metabolite of the tricyclic antidepressant (TCA) doxepin (Sinequan). It has been found to play a significant role in the antidepressant effects of doxepin. Nordoxepin is a mixture of (''E'') and (''Z'') stereoisomers. Whereas pharmaceutical doxepin is supplied in an approximate 85:15 ratio mixture of (E)- and (Z)-stereoisomers and plasma concentrations of doxepin remain roughly the same as this ratio with treatment, plasma levels of the (E)- and (Z)-stereoisomers of nordoxepin, due to stereoselective metabolism of doxepin by cytochrome P450 enzymes, are approximately 1:1. Nordoxepin is pharmacologically active similarly to doxepin, but relative to doxepin, is much more potent and selective as a norepinephrine reuptake inhibitor. In general, the demethylated variants of tertiary amine TCAs like doxepin are much more potent inhibitors of norepinephrine reuptake, less potent inhibitors of serotonin reuptake, and less potent in their antiadrenergic, antihistamine, and anticholinergic activities. Nordoxepin is formed from doxepin mainly by CYP2C19 (>50% contribution), while CYP1A2 and CYP2C9 are involved to a lesser extent, and CYP2D6 and CYP3A4 are not involved. Hydroxylation of doxepin and nordoxepin is mediated mainly by CYP2D6. Total exposures to both doxepin and nordoxepin differ by almost 10-fold in CYP2D6 ultra-rapid versus poor metabolizers. Both doxepin and nordoxepin are also transformed into glucuronide conjugates. The elimination half-life of nordoxepin is approximately 31 hours, which is almost twice that of doxepin (mean 17 hours).

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Pharmacodynamics

Pharmacodynamics is the study of the biochemical and physiologic effects of drugs (especially pharmaceutical drugs).

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Receptor antagonist

A receptor antagonist is a type of receptor ligand or drug that blocks or dampens a biological response by binding to and blocking a receptor rather than activating it like an agonist.

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Serotonin–norepinephrine reuptake inhibitor

Serotonin–norepinephrine reuptake inhibitors (SNRIs) are a class of antidepressant drugs that treat major depressive disorder (MDD) and can also treat anxiety disorders, obsessive-compulsive disorder (OCD), attention-deficit hyperactivity disorder (ADHD), chronic neuropathic pain, fibromyalgia syndrome (FMS), and menopausal symptoms.

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Stereoisomerism

In stereochemistry, stereoisomers are isomeric molecules that have the same molecular formula and sequence of bonded atoms (constitution), but differ in the three-dimensional orientations of their atoms in space.

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Tricyclic antidepressant

Tricyclic antidepressants (TCAs) are a class of medications that are used primarily as antidepressants.

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Redirects here:

(Z) Doxepin, (Z) doxepin, (Z)-Doxepin, (Z)-doxepin, Cidoxepine, Cis Doxepin, Cis doxepin, Cis-Doxepin, Cis-doxepin, CisDoxepin, Cisdoxepin, P 4599, P-4599, P4599, Z doxepin, Z-Doxepin, Z-doxepin.

References

[1] https://en.wikipedia.org/wiki/Cidoxepin

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