A report on Tricyclic antidepressant and Fibromyalgia

Chemical structure of the prototypical and first marketed tricyclic antidepressant imipramine. Notice its three rings.
The location of the 19 pain areas for the Widespread Pain Index of fibromyalgia
Chemical structure of the prototypical and first marketed tricyclic antidepressant imipramine. Notice its three rings.
A woman feeling stress
The location of the nine paired tender points that comprise the 1990 American College of Rheumatology criteria for fibromyalgia
Widespread pain index (WPI) areas
Stress and trauma are strongly linked to fibromyalgia

They are also used in the treatment of a number of other medical disorders, including cyclic vomiting syndrome (CVS) and anxiety disorders such as generalized anxiety disorder (GAD), social phobia (SP) also known as social anxiety disorder (SAD), obsessive-compulsive disorder (OCD), and panic disorder (PD), post-traumatic stress disorder (PTSD), body dysmorphic disorder (BDD), eating disorders like anorexia nervosa and bulimia nervosa, certain personality disorders such as borderline personality disorder (BPD), neurological disorders such as attention-deficit hyperactivity disorder (ADHD), Parkinson's disease as well as chronic pain, neuralgia or neuropathic pain, and fibromyalgia, headache, or migraine, smoking cessation, tourette syndrome, trichotillomania, irritable bowel syndrome (IBS), interstitial cystitis (IC), nocturnal enuresis (NE), narcolepsy, insomnia, pathological crying and/or laughing, chronic hiccups, ciguatera poisoning, and as an adjunct in schizophrenia.

- Tricyclic antidepressant

As of 2018, the only tricyclic antidepressant (TCA) that has sufficient evidence is amitriptyline.

- Fibromyalgia
Chemical structure of the prototypical and first marketed tricyclic antidepressant imipramine. Notice its three rings.

8 related topics with Alpha

Overall
Gate control theory of pain

Neuropathic pain

3 links

Pain caused by damage or disease affecting the somatosensory system.

Pain caused by damage or disease affecting the somatosensory system.

Gate control theory of pain
Microglia (identified by alpha-coronin1a), and neurons in culture. Microglia are proposed to release molecules that alter the excitability of neurons.

First line treatments are certain antidepressants (tricyclic antidepressants and serotonin–norepinephrine reuptake inhibitors), anticonvulsants (pregabalin and gabapentin).

Gabapentin may reduce symptoms associated with neuropathic pain or fibromyalgia in some people.

Duloxetine, an example of an SNRI.

Serotonin–norepinephrine reuptake inhibitor

2 links

Duloxetine, an example of an SNRI.
Timeline of approved SNRIs.
Timeline of development of antidepressant agents.
Inhibiting the reuptake transport protein results in increased concentrations of serotonin and norepinephrine in the synaptic clefts, leading to improvement of depression symptoms.
Aryloxypropanamine scaffold and agents containing it.
Cycloalkanol ethylamine scaffold and agents containing it.
Structure of milnacipran.

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

Over the past two decades, second-generation antidepressants have simply replaced first-generation antidepressants, such as tricyclic antidepressants (TCAs) and monoamine oxidase inhibitors (MAOIs), as the drugs of choice for the treatment of MDD due to their improved tolerability and safety profile.

Chemical structure of morphine, the prototypical opioid.

Opioid

2 links

Opioids are substances that act on opioid receptors to produce morphine-like effects.

Opioids are substances that act on opioid receptors to produce morphine-like effects.

Chemical structure of morphine, the prototypical opioid.
US. Top line represents the number of benzodiazepine deaths that also involved opioids. Bottom line represents benzodiazepine deaths that did not involve opioids.
Locants of the morphine molecule
INTA: selective agonist of KOR-DOR and KOR-MOR heteromers. Does not recruit β-arrestin II. Antinociceptive devoid of aversion, tolerance, and dependence in mice.
A sample of raw opium
US yearly deaths from all opioid drugs. Included in this number are opioid analgesics, along with heroin and illicit .<ref name=NIDA-deaths/>
US yearly deaths involving other, predominately Fentanyl.<ref name=NIDA-deaths/>
US yearly deaths involving prescription opioids. is a category dominated by illegally acquired fentanyl, and has been excluded.<ref name=NIDA-deaths>Overdose Death Rates. By National Institute on Drug Abuse (NIDA).</ref>
US yearly overdose deaths involving heroin.<ref name=NIDA-deaths/>

Guidelines have suggested that the risk of opioids is likely greater than their benefits when used for most non-cancer chronic conditions including headaches, back pain, and fibromyalgia.

Tricyclic antidepressants have painkilling effect as well, but they're thought to do so by indirectly activating the endogenous opioid system.

The skeleton structure of the SNRI venlafaxine, a typical example of an antidepressant.

Antidepressant

1 links

Antidepressants are medications used to treat major depressive disorder, some anxiety disorders, some chronic pain conditions, and to help manage some addictions.

Antidepressants are medications used to treat major depressive disorder, some anxiety disorders, some chronic pain conditions, and to help manage some addictions.

The skeleton structure of the SNRI venlafaxine, a typical example of an antidepressant.
The skeleton structure of the SNRI venlafaxine, a typical example of an antidepressant.
Blister pack of Prozac (fluoxetine), a selective serotonin reuptake inhibitor
The chemical structure of venlafaxine (Effexor), an SNRI
St John's wort
Structural formula of the SSRI sertraline

A 2012 meta-analysis concluded that antidepressants treatment favorably affects pain, health-related quality of life, depression, and sleep in fibromyalgia syndrome.

A discontinuation syndrome can occur after stopping any antidepressant including selective serotonin re-uptake inhibitors (SSRIs), serotonin–norepinephrine reuptake inhibitors (SNRIs), and tricyclic antidepressants (TCAs).

Metabolism of amitriptyline to major active metabolites.

Amitriptyline

1 links

Metabolism of amitriptyline to major active metabolites.
Chemical synthesis of amitriptyline.
Two boxes of amitriptyline (Endep; produced by Alphapharm, Australian market) in 10 and 25 mg doses

Amitriptyline, sold under the brand name Elavil among others, is a tricyclic antidepressant primarily used to treat cyclic vomiting syndrome (CVS), major depressive disorder and a variety of pain syndromes from neuropathic pain to fibromyalgia to migraine and tension headaches.

Chronic pain

1 links

Classified as pain that lasts longer than three to six months.

Classified as pain that lasts longer than three to six months.

For neuropathic pain other drugs may be more effective than opioids, such as tricyclic antidepressants, serotonin-norepinephrine reuptake inhibitors, and anticonvulsants.

Myofascial release has been used in some cases of fibromyalgia, chronic low back pain, and tennis elbow but there is not enough evidence to support this as method of treatment.

Drawing of the pain of IBS

Irritable bowel syndrome

0 links

Functional gastrointestinal disorder characterized by a group of symptoms accompanied together that include abdominal pain and changes in the consistency of bowel movements.

Functional gastrointestinal disorder characterized by a group of symptoms accompanied together that include abdominal pain and changes in the consistency of bowel movements.

Drawing of the pain of IBS
Prevalence of protozoal infections in industrialized countries (United States and Canada) in the 21st century
Percentage of population with IBS reported in various studies in different countries (see sources in the table)

People with IBS, more commonly than others, have gastroesophageal reflux, symptoms relating to the genitourinary system, fibromyalgia, headache, backache, and psychiatric symptoms such as depression and anxiety.

There is good evidence that low doses of tricyclic antidepressants (TCAs) can be effective for IBS.

A picture of 150 mg tablets of the reversible MAOI drug moclobemide, brand name Aurorix.

Moclobemide

0 links

Reversible inhibitor of monoamine oxidase A (RIMA) drug primarily used to treat depression and social anxiety.

Reversible inhibitor of monoamine oxidase A (RIMA) drug primarily used to treat depression and social anxiety.

A picture of 150 mg tablets of the reversible MAOI drug moclobemide, brand name Aurorix.

Unipolar depression. Moclobemide has demonstrated effectiveness and efficacy in the treatment and management of major depressive disorder, with both endogenous and non-endogenous depression responding; in addition moclobemide has a fast onset of action compared to other antidepressants and is significantly more tolerable than the tricyclic antidepressants. Due to a very good safety profile and very low incidence of side effects moclobemide is likely to have a high level of acceptability by individuals suffering from depression. Higher doses (>450 mg/day) may be more effective in severe depression, while patients treated with a lower dose tend to respond less well than those treated with tricyclic antidepressants.

Fibromyalgia, moclobemide has been found to improve pain and functioning in this group of people.