Drugs List

Therapeutic Indications

Uses

Labyrinthine disorders
Motion sickness
Nausea
Nausea and vomiting associated with narcotic analgesics
Nausea or vomiting associated with radiotherapy
Pre-op. emergency surgery: Reduce regurgitation/aspiration gastric contents
Prevention/treatment of post-operative nausea and vomiting
Vertigo
Vomiting

Administration

For intravenous and intramuscular injection only

Cyclizine via the intravenous route is to be administered slowly into the blood stream, with only minimal withdrawal of blood into the syringe.

Contraindications

Neonates
Breastfeeding

Precautions and Warnings

Children under 18 years
Benign prostatic hyperplasia
Epileptic disorder
Gastrointestinal obstruction
Glaucoma
Hepatic disorder
Myocardial infarction
Neuromuscular disorder
Porphyria
Pregnancy
Pyloroduodenal obstruction
Severe cardiac failure
Urinary retention

Advise ability to drive/operate machinery may be affected by side effects
May precipitate glaucoma
Potential for drug abuse
May counteract the haemodynamic benefits of opioids
Advise patient to avoid alcohol during treatment

Intravenous cyclizine should be used with caution in all patients with underlying neuromuscular disorders since cases of transient paralysis have been reported.

Cyclizine should be used with caution in patients with severe heart failure. In such patients, cyclizine may cause a fall in cardiac output associated with increases in heart rate, mean arterial pressure and pulmonary wedge pressure.

Pregnancy and Lactation

Pregnancy

Use cyclizine with caution in breastfeeding.

The manufacturer states that safety in pregnancy is not established and so not advised. Some animal studies are interpreted as indicating that cyclizine may be teratogenic. Though no increased malformations were observed when used in 111 human patients in the first trimester and no link to oral clefts has been found. A retrospective study found that significantly fewer infants with malformations were exposed to antihistamines/antiemetics in the first trimester compared with controls. Furthermore; a large meta-analysis of 24 studies using antihistamines with more than 200,000 participating women showed no risk of major malformations.

Schaefer et al concludes that on the body of evidence, coupled with the fact that cyclizine has been on the market for a long time with no adverse effects reported on newborns, cyclizine is considered safe in human pregnancy.

An association between retrolental fibroplasia in premature infants has been reported with the use of antihistamines in the last 2 weeks of the pregnancy.

The use of all medication in pregnancy should be avoided whenever possible; particularly in the first trimester. Non-drug treatments should also be considered. When essential, a medication with the best safety record over time should be chosen, employing the lowest effective dose for the shortest possible time. Polypharmacy should be avoided. Teratogens taken in the pre-embryonic period, often quoted as lasting until 14 to 17 days post-conception, are believed to have an all-or-nothing effect. Where drugs have a short half-life, and when the date of conception is certain, this may allow women to be reassured where drug exposure has occurred within this time frame. Further advice may be available from the UK National Teratology Information Service (NTIS) and through ToxBase, available via password on the internet ( www.toxbase.org ) or if this is unavailable at the backup site ( www.toxbasebackup.org ).

Lactation

Cyclizine is contraindicated in breastfeeding.

It is not known whether cyclizine or its metabolites are excreted in human milk. At the time of writing, no reports have been located of its used during breastfeeding. Though Lactmed states that occasional doses of cyclizine are probably acceptable during breastfeeding. Large doses or more prolonged use may cause effects in the infant or decrease the milk supply.

Neonates, infants born prematurely, those with low birth weight, those with an unstable gastrointestinal function or who have serious illnesses may require special consideration. For any infant, if a drug is prescribed to the nursing mother, it should be at the lowest practical dose and for the shortest time. When drug administration is unavoidable and breastfeeding is to continue, minimisation of exposure of the infant to the drug may sometimes be achieved by timing the maternal doses to just after a feeding episode. Infants exposed to drugs via breast milk should be monitored for unusual signs or symptoms. Interactions between the drug received by the infant from the mother's milk and medication prescribed for the infant should also be considered, for example, when the drug given to the infant may prevent metabolism of the drug received via breast milk.
Specialist advice is available from the UK Drugs in Lactation Advisory Service at https://www.midlandsmedicines.nhs.uk/content.asp?section=6&subsection=17&pageIdx=1

Side Effects

Agitation
Agranulocytosis
Allergic skin reactions
Anaphylaxis
Angioedema
Apnoea
Arrhythmias
Asthenia
Blood disorders
Blurred vision
Bronchospasm
Chills
Cholestatic hepatitis
Cholestatic jaundice
Chorea
Confusion
Constipation
Convulsions
Depression
Disorientation
Dizziness
Drowsiness
Dry mouth
Dry throat
Dryness of nose
Dyskinesia
Dystonia
Erythema at injection site
Extrapyramidal effects
Fixed drug eruption
Gastro-intestinal disturbances
Glaucoma (closed angle)
Hallucinations
Headache
Hepatic impairment
Hepatitis
Hypersensitivity reactions
Hypertension
Hypotension
Impaired consciousness
Insomnia
Muscle spasm
Nervousness
Oculogyric crisis
Pain / soreness (injection site)
Palpitations
Paraesthesia
Paralysis
Photosensitivity
Pruritus
Psychomotor impairment
Rash
Restlessness
Sensation of heaviness
Sleep disturbances
Somnolence
Speech disturbances
Tachycardia
Thrombophlebitis (injection site)
Tremor
Twitching
Urinary retention
Urticaria

Presentation

Parenteral formulations of cyclizine lactate.

Drugs List

Therapeutic Indications

Uses

Labyrinthine disorders
Motion sickness
Nausea
Nausea and vomiting associated with narcotic analgesics
Nausea or vomiting associated with radiotherapy
Pre-op. emergency surgery: Reduce regurgitation/aspiration gastric contents
Prevention/treatment of post-operative nausea and vomiting
Vertigo
Vomiting

Dosage

Adults

Children

Administration

For intravenous and intramuscular injection only

Cyclizine via the intravenous route is to be administered slowly into the blood stream, with only minimal withdrawal of blood into the syringe.

Contraindications

Neonates
Breastfeeding

Precautions and Warnings

Children under 18 years
Benign prostatic hyperplasia
Epileptic disorder
Gastrointestinal obstruction
Glaucoma
Hepatic disorder
Myocardial infarction
Neuromuscular disorder
Porphyria
Pregnancy
Pyloroduodenal obstruction
Severe cardiac failure
Urinary retention

Advise ability to drive/operate machinery may be affected by side effects
May precipitate glaucoma
Potential for drug abuse
May counteract the haemodynamic benefits of opioids
Advise patient to avoid alcohol during treatment

Intravenous cyclizine should be used with caution in all patients with underlying neuromuscular disorders since cases of transient paralysis have been reported.

Cyclizine should be used with caution in patients with severe heart failure. In such patients, cyclizine may cause a fall in cardiac output associated with increases in heart rate, mean arterial pressure and pulmonary wedge pressure.

Pregnancy and Lactation

Pregnancy

Use cyclizine with caution in breastfeeding.

The manufacturer states that safety in pregnancy is not established and so not advised. Some animal studies are interpreted as indicating that cyclizine may be teratogenic. Though no increased malformations were observed when used in 111 human patients in the first trimester and no link to oral clefts has been found. A retrospective study found that significantly fewer infants with malformations were exposed to antihistamines/antiemetics in the first trimester compared with controls. Furthermore; a large meta-analysis of 24 studies using antihistamines with more than 200,000 participating women showed no risk of major malformations.

Schaefer et al concludes that on the body of evidence, coupled with the fact that cyclizine has been on the market for a long time with no adverse effects reported on newborns, cyclizine is considered safe in human pregnancy.

An association between retrolental fibroplasia in premature infants has been reported with the use of antihistamines in the last 2 weeks of the pregnancy.

The use of all medication in pregnancy should be avoided whenever possible; particularly in the first trimester. Non-drug treatments should also be considered. When essential, a medication with the best safety record over time should be chosen, employing the lowest effective dose for the shortest possible time. Polypharmacy should be avoided. Teratogens taken in the pre-embryonic period, often quoted as lasting until 14 to 17 days post-conception, are believed to have an all-or-nothing effect. Where drugs have a short half-life, and when the date of conception is certain, this may allow women to be reassured where drug exposure has occurred within this time frame. Further advice may be available from the UK National Teratology Information Service (NTIS) and through ToxBase, available via password on the internet ( www.toxbase.org ) or if this is unavailable at the backup site ( www.toxbasebackup.org ).

Lactation

Cyclizine is contraindicated in breastfeeding.

It is not known whether cyclizine or its metabolites are excreted in human milk. At the time of writing, no reports have been located of its used during breastfeeding. Though Lactmed states that occasional doses of cyclizine are probably acceptable during breastfeeding. Large doses or more prolonged use may cause effects in the infant or decrease the milk supply.

Neonates, infants born prematurely, those with low birth weight, those with an unstable gastrointestinal function or who have serious illnesses may require special consideration. For any infant, if a drug is prescribed to the nursing mother, it should be at the lowest practical dose and for the shortest time. When drug administration is unavoidable and breastfeeding is to continue, minimisation of exposure of the infant to the drug may sometimes be achieved by timing the maternal doses to just after a feeding episode. Infants exposed to drugs via breast milk should be monitored for unusual signs or symptoms. Interactions between the drug received by the infant from the mother's milk and medication prescribed for the infant should also be considered, for example, when the drug given to the infant may prevent metabolism of the drug received via breast milk.
Specialist advice is available from the UK Drugs in Lactation Advisory Service at https://www.midlandsmedicines.nhs.uk/content.asp?section=6&subsection=17&pageIdx=1

Counselling

Side effects associated with cyclizine include hallucinations, drowsiness, sedation, confusion, disorientation and blurred vision. Patients suffering from these adverse affects should be advised not to drive or operate machinery.

Patients should avoid alcohol as additive effects of drowsiness and poor co-ordination may occur.

As an antiemetic, cyclizine also makes toxicity from alcohol more dangerous.

Side Effects

Agitation
Agranulocytosis
Allergic skin reactions
Anaphylaxis
Angioedema
Apnoea
Arrhythmias
Asthenia
Blood disorders
Blurred vision
Bronchospasm
Chills
Cholestatic hepatitis
Cholestatic jaundice
Chorea
Confusion
Constipation
Convulsions
Depression
Disorientation
Dizziness
Drowsiness
Dry mouth
Dry throat
Dryness of nose
Dyskinesia
Dystonia
Erythema at injection site
Extrapyramidal effects
Fixed drug eruption
Gastro-intestinal disturbances
Glaucoma (closed angle)
Hallucinations
Headache
Hepatic impairment
Hepatitis
Hypersensitivity reactions
Hypertension
Hypotension
Impaired consciousness
Insomnia
Muscle spasm
Nervousness
Oculogyric crisis
Pain / soreness (injection site)
Palpitations
Paraesthesia
Paralysis
Photosensitivity
Pruritus
Psychomotor impairment
Rash
Restlessness
Sensation of heaviness
Sleep disturbances
Somnolence
Speech disturbances
Tachycardia
Thrombophlebitis (injection site)
Tremor
Twitching
Urinary retention
Urticaria

Overdosage

It is strongly recommended that the UK National Poisons Information Service be consulted on cases of suspected or actual overdose where there is doubt over the degree of risk or about appropriate management.

The following number will direct the caller to the relevant local centre (0844) 892 0111

Information may be obtained if you have access to ToxBase the primary clinical toxicology database of the National Poisons Information Service. This is available via password on the internet ( www.toxbase.org ) or if this is unavailable at the backup site ( www.toxbasebackup.org ).

Further Information

Last Full Review Date: November 2014

Reference Sources

Drugs During Pregnancy and Lactation: Treatment Options and Risk Assessment, 2nd edition (2007) ed. Schaefer, C., Peters, P. and Miller, R. Elsevier, London.

Drugs in Pregnancy and Lactation: A Reference Guide to Fetal and Neonatal Risk, 9th edition (2011) ed. Briggs, G., Freeman, R. and Yaffe, S. Lippincott Williams & Wilkins, Philadelphia.

Medications and Mothers' Milk, 14th Edition (2010) Hale, T. Hale Publishing, Amarillo, Texas.

Summary of Product Characteristics: Cyclizine lactate 50mg/ml injection . AMCo. Revised September 2013.

Summary of Product Characteristics: Valoid injection. Amdipharm. Revised October 2009.

US National Library of Medicine. Toxicology Data Network. Drugs and Lactation Database (LactMed).
Available at: https://toxnet.nlm.nih.gov/cgi-bin/sis/htmlgen?LACT
Cyclizine Last revised: 16 January 2014
Last accessed: 26 November 2014

NICE Evidence Services Available at: www.nice.org.uk Last accessed: 17 August 2017