Cyclizine

Generic Name: Cyclizine

 

Cyclizine is only found in individuals that have used or taken this drug. It is a histamine H1 antagonist given by mouth or parenterally for the control of postoperative and drug-induced vomiting and in motion sickness. (From Martindale, The Extra Pharmacopoeia, 30th ed, p935)Vomiting (emesis) is essentially a protective mechanism for removing irritant or otherwise harmful substances from the upper GI tract. Emesis or vomiting is controlled by the vomiting centre in the medulla region of the brain, an important part of which is the chemotrigger zone (CTZ). The vomiting centre possesses neurons which are rich in muscarinic cholinergic and histamine containing synapses. These types of neurons are especially involved in transmission from the vestibular apparatus to the vomiting centre. Motion sickness principally involves overstimulation of these pathways due to various sensory stimuli. Hence the action of cyclizinewhich acts to block the histamine receptors in the vomiting centre and thus reduce activity along these pathways. Furthermore since cyclizine possesses anti-cholinergic properties as well, the muscarinic receptors are similarly blocked.

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Vomiting (emesis) is essentially a protective mechanism for removing irritant or otherwise harmful substances from the upper GI tract. Emesis or vomiting is controlled by the vomiting centre in the medulla region of the brain, an important part of which is the chemotrigger zone (CTZ). The vomiting centre possesses neurons which are rich in muscarinic cholinergic and histamine containing synapses. These types of neurons are especially involved in transmission from the vestibular apparatus to the vomiting centre. Motion sickness principally involves overstimulation of these pathways due to various sensory stimuli. Hence the action of cyclizine which acts to block the histamine receptors in the vomiting centre and thus reduce activity along these pathways. Furthermore since cyclizine possesses anti-cholinergic properties as well, the muscarinic receptors are similarly blocked.

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.

The drug Diconal is a combination of cyclizine and the opioid dipipanone. Dipipanone is a schedule I controlled substance in the US, due to its high abuse potential.

COMMON side effects

If experienced, these tend to have a Less Severe expression

  • Drowsiness

INFREQUENT side effects

If experienced, these tend to have a Less Severe expression

  • Blurred Vision
  • Constipation
  • Difficult Or Painful Urination
  • Dizzy
  • Dry Mouth
  • Stomach Cramps

RARE side effects

If experienced, these tend to have a Less Severe expression

  • Chronic Trouble Sleeping
  • Dryness Of The Nose
  • Fast Heartbeat
  • Loss Of Appetite
  • Nervous
  • Rash
  • Throat Dryness

Adult

Dosage Forms & Strengths

tablet

  • 25mg
  • 50mg

Motion Sickness

Indicated for the prevention and treatment of nausea, vomiting and vertigo associated with motion sickness

50 mg PO taken 30 minutes before departure, may repeat in 4-6 hours if needed, up to 200 mg/day

Pediatric

Dosage Forms & Strengths

tablet

  • 25mg
  • 50mg

tablet, chewable

  • 25mg

Motion Sickness

Indicated for the prevention and treatment of nausea, vomiting and vertigo associated with motion sickness

6-12 years: 25 mg PO up to 3 times/day; not to exceed 75 mg/day

>12 years: 50 mg PO taken 30 minutes before departure, may repeat in 4-6 hr if needed, up to 200 mg/day

Geriatric

Use lowest dose in divided doses in the elderly because of potential anticholinergic effects

May cause confusion or aggravate symptoms of confusion in those with dementia; limit use if possible in the elderly

Constipation and difficulty voiding urine may occur in the elderly

Motion Sickness

Indicated for the prevention and treatment of nausea, vomiting and vertigo associated with motion sickness

50 mg PO taken 30 minutes before departure, may repeat in 4-6 hours if needed, up to 200 mg/day

This medication may cause blurred vision and may impair your thinking or reactions. Be careful if you drive or do anything that requires you to be alert and able to see clearly.

Drinking alcohol can increase certain side effects of cyclizine.

Taking this medicine with other drugs that make you sleepy or slow your breathing can worsen these effects. Ask your doctor before taking cyclizine with a sleeping pill, narcotic pain medicine, muscle relaxer, or medicine for anxiety, depression, or seizures.

Other drugs may interact with cyclizine, including prescription and over-the-counter medicines, vitamins, and herbal products. Tell each of your health care providers about all medicines you use now and any medicine you start or stop using.

Cyclizine is not a suitable drug for everyone. Do not use this medication if you:

  • are allergic to cyclizine or any of the excipients used;
  • suffer from some form of the eye disease called glaucoma.

If you suffer from any other health problems, please consult a doctor to check whether you should take this medicine. Cyclizine can affect the effect of other medicines (and vice versa). A doctor knows which drugs interact with Cyclizine. When ordering please mention any medication you might be taking. You can find more information about this topic in the leaflet.

Pregnancy / driving / alcohol

This medicine should only be taken upon the advice of a doctor during pregnancy or lactation. Cyclizine may cause sleepiness, dizziness and drowsiness particularly in the beginning. Do not participate in traffic if you suffer from these symptoms. Be careful with alcohol: it may trigger or worsen the side effects of this medication.

Do not use this medicine after the expiry date which is stated on the carton and label after EXP. The expiry date refers to the last day of that month.

Store this medicine in a safe place below 25°C.

Do not throw away any medicines via wastewater or household waste. Ask your pharmacist how to throw away medicines you no longer use. These measures will help protect the environment.

Contraindications

Hypersensitivity

Do not use in patients with asthma, glaucoma, emphysema, chronic pulmonary disease, shortness of breath, difficulty in breathing or difficulty in urination due to enlargement of the prostate gland unless directed by a doctor

Cyclizine should not be used concurrently with sedatives, tranquilizers, or anticholinergic medications

Cautions

May have hypotensive effects, which may be confusing or dangerous in postoperative patients

May produce drowsiness; caution while driving or performing other tasks requiring alertness

Pregnancy 

In a study 111 mothers given cyclizine during the first trimester for the control of nausea and vomiting, no increase in the incidence of malformations was noted. In addition, other phenothiazine-type agents used for nausea, including prochlorperazine and meclizine, were not associated with malformations.

One review of 1125 women who took cyclizine during the first trimester noted five cleft palates amongst the offspring of this group. The incidence of cleft palate among babies born to 24,208 mothers not receiving cyclizine was 19, indicating an approximate five-fold increase in cleft palates among cyclizine users. However, the incidence of cleft palate was similar in patients with nausea and vomiting not treated with cyclizine, indicating the condition itself may be to blame.

Summary of Use during Lactation

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, particularly in combination with a sympathomimetic such as pseudoephedrine or before lactation is well established.

Drug Levels

Maternal Levels. Relevant published information was not found as of the revision date.

Infant Levels. Relevant published information was not found as of the revision date.

Effects in Breastfed Infants

Relevant published information on cyclizine was not found as of the revision date. In one telephone follow-up study, mothers reported irritability and colicky symptoms 10% of infants exposed to various antihistamines and drowsiness was reported in 1.6% of infants. None of the reactions required medical attention and none of the infants were exposed to cyclizine.

Effects on Lactation and Breastmilk

Antihistamines in relatively high doses given by injection can decrease basal serum prolactin in nonlactating women and in early postpartum women. However, suckling-induced prolactin secretion is not affected by antihistamine pretreatment of postpartum mothers. Whether lower oral doses of antihistamines have the same effect on serum prolactin or whether the effects on prolactin have any consequences on breastfeeding success have not been studied.

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