Desipramine
Encyclopedia
Desipramine is a tricyclic antidepressant
(TCA). It inhibits the reuptake
of norepinephrine
and to a lesser extent serotonin
. It is used to treat depression
, but not considered a first line treatment since the introduction of SSRI antidepressants. Desipramine is an active metabolite
of imipramine
.
Along with other tricyclics, desipramine has found use in treating neuropathic pain
. The mechanism of action
seems to involve the activation, through norepinephrine reuptake inhibition, of descending pathways in the spinal cord
that block pain signals from ascending to the brain
. Desipramine is one of the most potent and selective
medications in this respect. It may also be used to treat symptoms of Attention Deficit Hyperactivity Disorder, as the underproduction of norepinephrine has been increasingly linked to symptoms associated with Attention Deficit Disorder. It may also be used to treat symptoms of cocaine withdrawal.
"The new safety information states that extreme caution should be used when this drug is given to patients who have a family history of sudden death, cardiac dysrhythmias, and cardiac conduction disturbances," according to an alert sent today from MedWatch, the FDA's safety information and adverse event reporting program.
The FDA and the manufacturer also warn that some patients may have seizures before cardiac dysrhythmias and death. Desipramine overdose is more likely to result in death than overdose with other tricyclic antidepressants, notes a company letter sent to healthcare professionals.
The "warnings" and "overdosage" sections of the drug's labeling are being changed to reflect these potential adverse events.
in fruit flies and associated with an increased risk of breast cancer in women.
Tricyclic antidepressant
Tricyclic antidepressants are heterocyclic chemical compounds used primarily as antidepressants. The TCAs were first discovered in the early 1950s and were subsequently introduced later in the decade; they are named after their chemical structure, which contains three rings of atoms...
(TCA). It inhibits the reuptake
Reuptake
Reuptake, or re-uptake, is the reabsorption of a neurotransmitter by a neurotransmitter transporter of a pre-synaptic neuron after it has performed its function of transmitting a neural impulse....
of norepinephrine
Norepinephrine
Norepinephrine is the US name for noradrenaline , a catecholamine with multiple roles including as a hormone and a neurotransmitter...
and to a lesser extent serotonin
Serotonin
Serotonin or 5-hydroxytryptamine is a monoamine neurotransmitter. Biochemically derived from tryptophan, serotonin is primarily found in the gastrointestinal tract, platelets, and in the central nervous system of animals including humans...
. It is used to treat depression
Clinical depression
Major depressive disorder is a mental disorder characterized by an all-encompassing low mood accompanied by low self-esteem, and by loss of interest or pleasure in normally enjoyable activities...
, but not considered a first line treatment since the introduction of SSRI antidepressants. Desipramine is an active 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...
of imipramine
Imipramine
Imipramine , also known as melipramine, is an antidepressant medication, a tricyclic antidepressant of the dibenzazepine group...
.
Along with other tricyclics, desipramine has found use in treating neuropathic pain
Neuropathic pain
Neuropathic pain results from lesions or diseases affecting the somatosensory system. It may be associated with abnormal sensations called dysesthesia, which occur spontaneously and allodynia that occurs in response to external stimuli. Neuropathic pain may have continuous and/or episodic ...
. The mechanism of action
Mechanism of action
In pharmacology, the term mechanism of action refers to the specific biochemical interaction through which a drug substance produces its pharmacological effect...
seems to involve the activation, through norepinephrine reuptake inhibition, of descending pathways in the spinal cord
Spinal cord
The spinal cord is a long, thin, tubular bundle of nervous tissue and support cells that extends from the brain . The brain and spinal cord together make up the central nervous system...
that block pain signals from ascending to the brain
Brain
The brain is the center of the nervous system in all vertebrate and most invertebrate animals—only a few primitive invertebrates such as sponges, jellyfish, sea squirts and starfishes do not have one. It is located in the head, usually close to primary sensory apparatus such as vision, hearing,...
. Desipramine is one of the most potent and selective
medications in this respect. It may also be used to treat symptoms of Attention Deficit Hyperactivity Disorder, as the underproduction of norepinephrine has been increasingly linked to symptoms associated with Attention Deficit Disorder. It may also be used to treat symptoms of cocaine withdrawal.
Cardiac arrhythmia
On December 2, 2009, the US Food and Drug Administration (FDA) and Sanofi-Aventis are warning healthcare professionals to use caution when prescribing the antidepressant desipramine hydrochloride (Norpramin) in patients with a family history of dysrhythmias or sudden cardiac death."The new safety information states that extreme caution should be used when this drug is given to patients who have a family history of sudden death, cardiac dysrhythmias, and cardiac conduction disturbances," according to an alert sent today from MedWatch, the FDA's safety information and adverse event reporting program.
The FDA and the manufacturer also warn that some patients may have seizures before cardiac dysrhythmias and death. Desipramine overdose is more likely to result in death than overdose with other tricyclic antidepressants, notes a company letter sent to healthcare professionals.
The "warnings" and "overdosage" sections of the drug's labeling are being changed to reflect these potential adverse events.
Genotoxicity
Desipramine has been shown to be genotoxicGenotoxic
In genetics, genotoxicity describes a deleterious action on a cell's genetic material affecting its integrity. This includes both certain chemical compounds and certain types of radiation....
in fruit flies and associated with an increased risk of breast cancer in women.
External links
- Desipramine - medicinenet.com
- Desipramine - medlineplus.org
- Desipramine - mentalhealth.com
- Desipramine - medscape.com