Methysergide is a prescription drug used for prophylaxis of migraine headaches

Migraine

Migraine is a chronic neurological disorder characterized by moderate to severe headaches, and nausea...

 and is sold under the brand names Sansert and Deseril in 2 mg dosages.

Pharmacology

Methysergide interacts with serotonin (5-HT) receptors

5-HT receptor

The serotonin receptors, also known as 5-hydroxytryptamine receptors or 5-HT receptors, are a group of G protein-coupled receptors and ligand-gated ion channels found in the central and peripheral nervous systems. They mediate both excitatory and inhibitory neurotransmission...

. Its therapeutic effect

Therapeutic effect

A therapeutic effect is a consequence of a medical treatment of any kind, the results of which are judged to be desirable and beneficial. This is true whether the result was expected, unexpected, or even an unintended consequence of the treatment...

 in migraine prophylaxis has been associated with its antagonism at the 5-HT_2B receptor.
Furthermore, it is an antagonist

Receptor antagonist

A receptor antagonist is a type of receptor ligand or drug that does not provoke a biological response itself upon binding to a receptor, but blocks or dampens agonist-mediated responses...

 at the 5-HT_2C receptor and at the 5-HT_1A receptor. It is known to have partial agonist

Partial agonist

Partial agonists bind and activate a given receptor, but have only partial efficacy at the receptor relative to a full agonist...

 effects on some of the other 5-HT receptors as well. Methysergide is metabolised into methylergometrine in humans, which is responsible for its psychedelic effects.

Uses

Methysergide is used to treat headaches such as migraine and other recurrent throbbing headaches. Methysergide is one of the most effective medications for the prevention of migraine, but not for the treatment of an acute attack.

It is also used in carcinoid syndrome

Carcinoid syndrome

Carcinoid syndrome refers to the array of symptoms that occur secondary to carcinoid tumors. The syndrome includes flushing and diarrhea, and, less frequently, heart failure and bronchoconstriction...

 to treat severe diarrhea

Diarrhea

Diarrhea , also spelled diarrhoea, is the condition of having three or more loose or liquid bowel movements per day. It is a common cause of death in developing countries and the second most common cause of infant deaths worldwide. The loss of fluids through diarrhea can cause dehydration and...

.

Side effects

It has a known side effect

Adverse drug reaction

An adverse drug reaction is an expression that describes harm associated with the use of given medications at a normal dosage. ADRs may occur following a single dose or prolonged administration of a drug or result from the combination of two or more drugs...

, retroperitoneal fibrosis

Retroperitoneal fibrosis

Retroperitoneal fibrosis or Ormond's disease is a disease featuring the proliferation of fibrous tissue in the retroperitoneum, the compartment of the body containing the kidneys, aorta, renal tract and various other structures. It may present with lower back pain, renal failure, hypertension, deep...

, which is severe, although uncommon. Other severe but uncommon side effects include pleural fibrosis, and subendocardial fibrosis.

In addition, there is an increased risk of left-sided cardiac valve dysfunction.

History

Methysergide was approved by the U.S. Food and Drug Administration (FDA) in 1962.

Novartis

Novartis

Novartis International AG is a multinational pharmaceutical company based in Basel, Switzerland, ranking number three in sales among the world-wide industry...

 withdrew it from the U.S. market after taking over Sandoz

Sandoz

Founded in 2003, Sandoz presently is the generic drug subsidiary of Novartis, a multinational pharmaceutical company. The company develops, manufactures and markets generic drugs as well as pharmaceutical and biotechnological active ingredients....

, but currently lists it as a product.

Related compounds

Its molecular structure is closely related to that of LSD

LSD

Lysergic acid diethylamide, abbreviated LSD or LSD-25, also known as lysergide and colloquially as acid, is a semisynthetic psychedelic drug of the ergoline family, well known for its psychological effects which can include altered thinking processes, closed and open eye visuals, synaesthesia, an...

.

Like LSD, methysergide also produces psychedelic

Psychedelic

The term psychedelic is derived from the Greek words ψυχή and δηλοῦν , translating to "soul-manifesting". A psychedelic experience is characterized by the striking perception of aspects of one's mind previously unknown, or by the creative exuberance of the mind liberated from its ostensibly...

and hallucinogenic

Psychedelics, dissociatives and deliriants

This general group of pharmacological agents can be divided into three broad categories: psychedelics, dissociatives, and deliriants. These classes of psychoactive drugs have in common that they can cause subjective changes in perception, thought, emotion and consciousness...

effects.

About 4 mg is equal to 25mcg of LSD.
Sandoz does not currently list this on their product guide.

External links

• Novartis Sansert site.
• Novartis Sansert product description.
• Migraines.org More detailed information on methysergide.
• neurologychannel.com, general information on migraines.
• History of methysergide in migraine.