Drugs List

Therapeutic Indications

Uses

Prevention and treatment of nausea and vomiting including that associated with motion sickness, narcotic analgesics, the post operative period following general anaesthesia and radiotherapy (especially in breast cancer patients since cyclizine does not elevate prolactin levels).

For the relief of vomiting and attacks of vertigo associated with Meniere's disease and other forms of vestibular disturbance.

Administration

For oral use.

Contraindications

Breastfeeding ( See Lactation section )
Porphyria
Neonates

Galactosaemia

Precautions and Warnings

Children 1 month to 6 years of age ( see Dosage - Children )
Pregnancy ( See Pregnancy section )

Cyclizine, as with other anticholinergic agents should be used with caution and appropriate monitoring in the following:
Obstructive disease of the gastrointestinal tract
Prostatic hypertrophy
Urinary retention
Glaucoma
Hepatic disease
Renal impairment
Epilepsy

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.

May counteract the haemodynamic benefits of opioids and caution should be exercised in acute myocardial infarction.

May cause drowsiness. If affected patients should not 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.

Contains lactose and should not be given to patients with lactose intolerance or glucose-galactose malabsorption syndrome.

Cyclizine has been misused for its euphoric or hallucinatory effects.

Use in Porphyria

Contraindicated for use in porphyria

Pregnancy and Lactation

Pregnancy

The manufacturer states that safety in pregnancy is not established. In the absence of any definitive human data, the use of cyclizine in pregnancy is not advised.

Schaefer (2007) indicates cyclizine as an effective and safe treatment for nausea and vomiting in pregnancy.

Briggs (2011) cites that cyclizine is teratogenic in animals but not in humans. No increased malformations were observed when used in 111 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.
On this body of evidence, cyclizine is indicated to be compatible with 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 14-17 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

Contraindicated whilst breastfeeding as it is not known whether cyclizine or its metabolites are excreted in human milk. At the time of writing, no reports of its use during breastfeeding have been located.

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

Dry mouth
Dryness of nose
Dry throat
Blurred vision
Tachycardia
Palpitations
Arrhythmias
Urinary retention
Hypotension
Constipation
Drowsiness
Dizziness
Restlessness
Nervousness
Insomnia
Hallucinations
Convulsions
Sleep disturbances
Extrapyramidal effects
Chorea
Tremor
Depression
Hypersensitivity reactions
Bronchospasm
Angioedema
Photosensitivity
Hepatic impairment
Hepatitis
Cholestatic jaundice
Headache
Agranulocytosis
Urticaria
Rash
Fixed drug eruption
Anaphylaxis
Psychomotor impairment
Gastro-intestinal disturbances
Confusion
Blood disorders
Apnoea
Dystonia
Dyskinesia
Twitching
Muscle spasm
Disorientation
Impaired consciousness
Speech disturbances
Hypertension
Paraesthesia
Allergic skin reactions
Asthenia
Oculogyric crisis
Glaucoma
Aggravation of cardiac failure

Presentation

Oral formulations of cyclizine hydrochloride.

Drugs List

Therapeutic Indications

Uses

Prevention and treatment of nausea and vomiting including that associated with motion sickness, narcotic analgesics, the post operative period following general anaesthesia and radiotherapy (especially in breast cancer patients since cyclizine does not elevate prolactin levels).

For the relief of vomiting and attacks of vertigo associated with Meniere's disease and other forms of vestibular disturbance.

Dosage

Adults

Children

Administration

For oral use.

Contraindications

Breastfeeding ( See Lactation section )
Porphyria
Neonates

Galactosaemia

Precautions and Warnings

Children 1 month to 6 years of age ( see Dosage - Children )
Pregnancy ( See Pregnancy section )

Cyclizine, as with other anticholinergic agents should be used with caution and appropriate monitoring in the following:
Obstructive disease of the gastrointestinal tract
Prostatic hypertrophy
Urinary retention
Glaucoma
Hepatic disease
Renal impairment
Epilepsy

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.

May counteract the haemodynamic benefits of opioids and caution should be exercised in acute myocardial infarction.

May cause drowsiness. If affected patients should not 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.

Contains lactose and should not be given to patients with lactose intolerance or glucose-galactose malabsorption syndrome.

Cyclizine has been misused for its euphoric or hallucinatory effects.

Use in Porphyria

Contraindicated for use in porphyria

Pregnancy and Lactation

Pregnancy

The manufacturer states that safety in pregnancy is not established. In the absence of any definitive human data, the use of cyclizine in pregnancy is not advised.

Schaefer (2007) indicates cyclizine as an effective and safe treatment for nausea and vomiting in pregnancy.

Briggs (2011) cites that cyclizine is teratogenic in animals but not in humans. No increased malformations were observed when used in 111 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.
On this body of evidence, cyclizine is indicated to be compatible with 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 14-17 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

Contraindicated whilst breastfeeding as it is not known whether cyclizine or its metabolites are excreted in human milk. At the time of writing, no reports of its use during breastfeeding have been located.

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

Effects on Ability to Drive and Operate Machinery

As sedation is a potential side effect patients should not drive or operate machinery until they have determined their own response to treatment.

Although there are no data available, patients should be cautioned that there may be additive effects with alcohol.

Counselling

Advise patients that cyclizine may cause drowsiness and if affected they should not 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

Dry mouth
Dryness of nose
Dry throat
Blurred vision
Tachycardia
Palpitations
Arrhythmias
Urinary retention
Hypotension
Constipation
Drowsiness
Dizziness
Restlessness
Nervousness
Insomnia
Hallucinations
Convulsions
Sleep disturbances
Extrapyramidal effects
Chorea
Tremor
Depression
Hypersensitivity reactions
Bronchospasm
Angioedema
Photosensitivity
Hepatic impairment
Hepatitis
Cholestatic jaundice
Headache
Agranulocytosis
Urticaria
Rash
Fixed drug eruption
Anaphylaxis
Psychomotor impairment
Gastro-intestinal disturbances
Confusion
Blood disorders
Apnoea
Dystonia
Dyskinesia
Twitching
Muscle spasm
Disorientation
Impaired consciousness
Speech disturbances
Hypertension
Paraesthesia
Allergic skin reactions
Asthenia
Oculogyric crisis
Glaucoma
Aggravation of cardiac failure

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 ).

Shelf Life and Storage

Store below 25 degrees C.

Further Information

Last Full Review Date: June 2012

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.

Martindale: The Complete Drug Reference, 37th edition (2011) ed. Sweetman, S. Pharmaceutical Press, London.

The Renal Drug Handbook. 3rd edition. (2009) ed. Ashley, C and Currie, Radcliffe Publishing Ltd, Abingdon.

Summary of Product Characteristics: Cyclizine 50mg Tablets. Amdipharm UK Limited. Revised March 2015.

NICE Evidence Services Available at: www.nice.org.uk Last accessed: 18 August 2017