Medication for motion sickness or vertigo
Cyclizine , sold under a number of brand names, is a medication used to treat and prevent
nausea ,
vomiting and
dizziness due to
motion sickness or
vertigo .
[2] It may also be used for nausea after
general anaesthesia or that which developed from
opioid use.
[2]
[3] It is taken
by mouth , in the
rectum , or
injected into a vein .
[3]
[4]
Common side effects include sleepiness, dry mouth,
constipation , and trouble with vision.
[5] More serious side effects include
low blood pressure and
urinary retention .
[5] It is not generally recommended in young children or those with
glaucoma .
[2]
[6] Cyclizine appears to be safe during
pregnancy but has not been well studied.
[7] It is in the
anticholinergic and
antihistamine family of medications.
[3]
[6]
Cyclizine was discovered in 1947.
[8] It is on the
World Health Organization's List of Essential Medicines .
[9] In the United States it is available
over the counter .
[6]
Medical uses
Primary uses include
nausea ,
vomiting and
dizziness associated with
motion sickness ,
vertigo and post-operatively following administration of
general anesthesia and
opioids . It is sometimes given in
hyperemesis gravidarum , although the manufacturer advises that it be avoided in pregnancy. Off-license use often occurs with specialists in hospitals to treat inpatients who have become severely dehydrated in pregnancy. An off-label use is as an opioid/opiate potentiator.
[10]
The drug Diconal is a combination of cyclizine and the opioid
dipipanone .
[11] Dipipanone is a
schedule I controlled substance in the US.
[12]
Contraindications
Its antimuscarinic action warrants caution in patients with
prostatic hypertrophy , urinary retention, or angle-closure
glaucoma . Liver disease exacerbates its sedative effects.
[10]
Adverse effects
Common (over 10%) —
Drowsiness ,
dry mouth .
Uncommon (1% to 10%) — Headache, psychomotor impairment, dermatitis, and
antimuscarinic effects such as diplopia (double vision),
tachycardia ,
constipation ,
urinary retention and gastro-intestinal disturbances.
Rare (less than 1%) — Hypersensitivity reactions (
bronchospasm ,
angioedema ,
anaphylaxis , rashes and
photosensitivity reactions),
extrapyramidal effects, dizziness, confusion, depression, sleep disturbances,
tremor , liver dysfunction, and
hallucinations .
Pharmacology
Cyclizine is a
piperazine derivative with histamine H1 -receptor antagonist (
antihistamine ) activity. The precise mechanism of action in inhibiting the symptoms of motion sickness is not well understood. It may have effects directly on the
vestibular system and on the
chemoreceptor trigger zone . Cyclizine exerts a central
anticholinergic (
antimuscarinic ) action.
[10]
Synthesis
Cyclizine may be prepared by the
Eschweiler–Clarke methylation of
diphenylmethylpiperazine or by reaction of benzhydryl bromide with
1-methylpiperazine in acetonitrile to form the hydrobromide salt of the drug.
History
Cyclizine was developed in the American division of pharmacy company
Burroughs Wellcome (today
GlaxoSmithKline ) during a research study involving many drugs of the antihistamine group. Cyclizine was quickly clinically found as a potent and long-acting antiemetic. The company named the substance – or more precisely cyclizine's
hydrochloride form which it usually appears in – "marezine hydrochloride" and started to sell it in the United States under trade name Marezine . Selling was begun in
France under trade name Marzine in 1965.
[13]
[14]
The substance received more credit when
NASA chose it as a space antiemetic for the
first crewed Moon flight . Cyclizine was introduced to many countries as a common antiemetic. It is an over-the-counter drug in many countries because it has been well tolerated, although it has not been studied much.
[13]
[15]
Society and culture
Some people using methadone recreationally combine cyclizine with their
methadone dose, a combination that is known to produce strong
psychoactive effects.
[16]
It has also been used recreationally for its
anticholinergic effects to induce hallucinations.
[17]
It has been used illegally in
greyhound racing to sabotage a dog's performance.
[18]
Names
As cyclizine hydrochloride tablets and cyclizine lactate solution for intramuscular or intravenous injection (brand names: Valoid
[10] in UK and South Africa and Marezine, Marzine and Emoquil in US). Cyclizine was marketed as Bonine for Kids in the US, but was discontinued in 2012, and replaced with meclizine.
[19]
Cyclizine derivatives
See also
References
^
"DrugBank: Cyclizine. Pharmacology: metabolism" . DrugBank Database .
Archived from the original on 30 January 2016. Retrieved 5 January 2016 .
^
a
b
c
"Cyclizine 50mg Tablets - Summary of Product Characteristics (SPC) - (eMC)" . www.medicines.org.uk . 27 March 2015.
Archived from the original on 20 December 2016. Retrieved 13 December 2016 .
^
a
b
c Feldman M, Friedman LS, Brandt LJ (2015).
Sleisenger and Fordtran's Gastrointestinal and Liver Disease: Pathophysiology, Diagnosis, Management . Elsevier Health Sciences. p. 218.
ISBN
9781455749898 .
Archived from the original on 20 December 2016.
^
World Health Organization (2019). World Health Organization model list of essential medicines: 21st list 2019 . Geneva: World Health Organization.
hdl :
10665/325771 . WHO/MVP/EMP/IAU/2019.06. License: CC BY-NC-SA 3.0 IGO.
^
a
b
"Cyclizine Side Effects in Detail - Drugs.com" . www.drugs.com .
Archived from the original on 21 December 2016. Retrieved 13 December 2016 .
^
a
b
c
"Cyclizine: Indications, Side Effects, Warnings - Drugs.com" . www.drugs.com .
Archived from the original on 21 December 2016. Retrieved 13 December 2016 .
^
"Cyclizine Use During Pregnancy | Drugs.com" . www.drugs.com .
Archived from the original on 21 December 2016. Retrieved 13 December 2016 .
^ Williams P (2010).
The story of the Wellcome Trust : unlocking Sir Henry's legacy to medical research . Hindringham: JJG. p. 14.
ISBN
9781899163922 .
Archived from the original on 20 December 2016.
^
World Health Organization (2021). World Health Organization model list of essential medicines: 22nd list (2021) . Geneva: World Health Organization.
hdl :
10665/345533 . WHO/MHP/HPS/EML/2021.02.
^
a
b
c
d
"Valoid Tablets by Amdipharm" . Electronic Medicines Compendium . Datapharm. Archived from
the original on 4 March 2016. Retrieved 1 October 2011 .
^
"Diconal Tablets by Amdipharm" . Electronic Medicines Compendium . Datapharm. Archived from
the original on 1 April 2008. Retrieved 5 August 2008 .
^
"Conversion Factors for Controlled Substances" . DEA Diversion Control Division . Retrieved 26 March 2020 .
^
a
b
Sneader W (2005).
Drug discovery: a history . John Wiley & Sons. p. 404.
ISBN
0-471-89979-8 .
Archived from the original on 10 September 2017.
^
Sittig M (1988).
Pharmaceutical manufacturing encyclopedia . William Andrew. p. 406.
ISBN
0-8155-1144-2 .
Archived from the original on 10 September 2017.
^ Rajoo SG.
"Introduction" . In Lobo M (ed.). Anti-emetics - Metoclopramide, Domperidone, Ondansetron, Cyclizine .
Archived from the original on 2 April 2015. Retrieved 9 March 2015 .
^ Ruben SM, McLean PC, Melville J (August 1989). "Cyclizine abuse among a group of opiate dependents receiving methadone". British Journal of Addiction . 84 (8): 929–34.
doi :
10.1111/j.1360-0443.1989.tb00766.x .
PMID
2775912 .
^ Bassett KE, Schunk JE, Crouch BI (September 1996). "Cyclizine abuse by teenagers in Utah". The American Journal of Emergency Medicine . 14 (5): 472–4.
doi :
10.1016/S0735-6757(96)90156-4 .
PMID
8765114 .
^ Conor Ryan for The Independent. June 20, 2013
IGB left with €250k bill after dog doping case
Archived 2016-03-04 at the
Wayback Machine
^
"Bonine for Kids" . Insight Pharmaceuticals. Archived from
the original on 17 September 2010.
^ Lemke TL, Williams DA, Roche VF, Zito SW (2013). Foye's Principles of Medicinal Chemistry (7th ed.). Philadelphia: Wolters Kluwer Health / Lippincott Williams & Wilkins. p. 1056.
ISBN
978-1-60913-345-0 .
External links
"Cyclizine" . Drug Information Portal . U.S. National Library of Medicine.
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