Pizotifen
Encyclopedia
Pizotifen or pizotyline (USAN
), trade name Sandomigran, is a benzocycloheptene
based drug used as a medicine, primarily as a preventative to reduce the frequency of recurrent migraine
headaches.
including migraine
and cluster headache
. Pizotifen is one of a range of medications used for this purpose, other options include propranolol, topiramate
, valproic acid
and amitriptyline
. While pizotifen is reasonably effective, its use is limited by side effects, principally drowsiness and weight gain, and it is usually not the first choice medicine for preventing migraines, instead being used as an alternative when other drugs have failed to be effective.
Other applications for which pizotifen may be used include as an antidepressant
, or for the treatment of anxiety
or social phobia
. Animal studies also suggest that pizotyline could be used in the treatment of serotonin syndrome
or MDMA overdose in a similar manner to the closely related antihistamine/antiserotonin drug cyproheptadine
.
include sedation
, dry mouth, drowsiness, increased appetite and weight gain. Occasionally it may cause nausea, headaches, or dizziness. In rare cases, anxiety, aggression and depression may also occur.
acting mainly at the 5-HT2A
and 5HT2C
receptors. It also has some activity as an antihistamine
as well as some anticholinergic activity.
United States Adopted Name
United States Adopted Names are unique nonproprietary names assigned to pharmaceuticals marketed in the United States. Each name is assigned by the USAN Council, which is co-sponsored by the American Medical Association , the United States Pharmacopeial Convention , and the American Pharmacists...
), trade name Sandomigran, is a benzocycloheptene
Benzocycloheptenes
Benzocycloheptenes are cycloheptenes with additional benzene rings attached. Most have two benzene rings, and are called "dibenzocycloheptenes".Some benzocycloheptenes have medical uses as antihistamines or antidepressants.Examples include:...
based drug used as a medicine, primarily as a preventative to reduce the frequency of recurrent migraine
Migraine
Migraine is a chronic neurological disorder characterized by moderate to severe headaches, and nausea...
headaches.
Uses
The main medical use for pizotifen is for the prevention of vascular headacheVascular headache
A vascular headache is an outdated term to describe certain types of headache which were thought to be related to blood vessel swelling and hyperemia as cause of the pain.There is no doubt that some headaches are caused by vascular effects...
including migraine
Migraine
Migraine is a chronic neurological disorder characterized by moderate to severe headaches, and nausea...
and cluster headache
Cluster headache
Cluster headache, nicknamed "suicide headache", is a neurological disease that involves, as its most prominent feature, an immense degree of pain in the head. Cluster headaches occur periodically: spontaneous remissions interrupt active periods of pain. The cause of the disease is currently unknown...
. Pizotifen is one of a range of medications used for this purpose, other options include propranolol, topiramate
Topiramate
Topiramate is an anticonvulsant drug. It was originally produced by Ortho-McNeil Neurologics and Noramco, Inc., both divisions of the Johnson & Johnson Corporation. This medication was discovered in 1979 by Bruce E. Maryanoff and Joseph F. Gardocki during their research work at McNeil...
, valproic acid
Valproic acid
Valproic acid is a chemical compound that has found clinical use as an anticonvulsant and mood-stabilizing drug, primarily in the treatment of epilepsy, bipolar disorder, and, less commonly, major depression. It is also used to treat migraine headaches and schizophrenia...
and amitriptyline
Amitriptyline
Amitriptyline is a tricyclic antidepressant . It is the most widely used TCA and has at least equal efficacy against depression as the newer class of SSRIs...
. While pizotifen is reasonably effective, its use is limited by side effects, principally drowsiness and weight gain, and it is usually not the first choice medicine for preventing migraines, instead being used as an alternative when other drugs have failed to be effective.
Other applications for which pizotifen may be used include as an antidepressant
Antidepressant
An antidepressant is a psychiatric medication used to alleviate mood disorders, such as major depression and dysthymia and anxiety disorders such as social anxiety disorder. According to Gelder, Mayou &*Geddes people with a depressive illness will experience a therapeutic effect to their mood;...
, or for the treatment of anxiety
Anxiety
Anxiety is a psychological and physiological state characterized by somatic, emotional, cognitive, and behavioral components. The root meaning of the word anxiety is 'to vex or trouble'; in either presence or absence of psychological stress, anxiety can create feelings of fear, worry, uneasiness,...
or social phobia
Social anxiety disorder
Social anxiety disorder , also known as social phobia, is an anxiety disorder characterized by intense fear in social situations causing considerable distress and impaired ability to function in at least some parts of daily life...
. Animal studies also suggest that pizotyline could be used in the treatment of serotonin syndrome
Serotonin syndrome
Serotonin syndrome is a potentially life-threatening adverse drug reaction that may occur following therapeutic drug use, inadvertent interactions between drugs, overdose of particular drugs, or the recreational use of certain drugs...
or MDMA overdose in a similar manner to the closely related antihistamine/antiserotonin drug cyproheptadine
Cyproheptadine
Cyproheptadine , sold under the brand name Periactin, is a first-generation antihistamine with additional anticholinergic, antiserotonergic, and local anesthetic properties.- Indications :...
.
Adverse effects
Side effectsAdverse 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...
include sedation
Sedation
Sedation is the reduction of irritability or agitation by administration of sedative drugs, generally to facilitate a medical procedure or diagnostic procedure...
, dry mouth, drowsiness, increased appetite and weight gain. Occasionally it may cause nausea, headaches, or dizziness. In rare cases, anxiety, aggression and depression may also occur.
Contraindications
Pizotifen is contraindicated in patients who suffer from hypersensitivity to any of its components, also Pizotifen is contraindicated in gastric outlet obstruction, pregnancy, angle-closure glaucoma and difficulty urinating.Mechanism
Pizotifen is a serotonin antagonistSerotonin antagonist
A serotonin antagonist is a drug used to inhibit the action at serotonin receptors.Many of the most important medications of this class selectively act at the 5-HT3 receptor, and thus are known as 5-HT3 antagonists...
acting mainly at the 5-HT2A
5-HT2A receptor
The mammalian 5-HT2A receptor is a subtype of the 5-HT2 receptor that belongs to the serotonin receptor family and is a G protein-coupled receptor . This is the main excitatory receptor subtype among the GPCRs for serotonin , although 5-HT2A may also have an inhibitory effect on certain areas such...
and 5HT2C
5-HT2C receptor
The 5-HT2C receptor is a subtype of 5-HT receptor that binds the endogenous neurotransmitter serotonin . It is a G protein-coupled receptor that is coupled to Gq/G11 and mediates excitatory neurotransmission. HTR2C denotes the human gene encoding for the receptor, that in humans is located at the...
receptors. It also has some activity as an antihistamine
Antihistamine
An H1 antagonist is a histamine antagonist of the H1 receptor that serves to reduce or eliminate effects mediated by histamine, an endogenous chemical mediator released during allergic reactions...
as well as some anticholinergic activity.