Introduction to Cyclizine
Cyclizine is an antihistamine medication belonging to the piperazine derivative class [1.6.4, 1.2.5]. Its primary function is to block histamine H1-receptors in the brain, which helps to alleviate symptoms of nausea, vomiting, and dizziness [1.6.2, 1.6.4]. It is commonly used for motion sickness, vertigo, and nausea following surgery or caused by other medications [1.5.3, 1.5.6]. The medication works by affecting the vestibular system and the chemoreceptor trigger zone in the brain, and it also possesses anticholinergic (antimuscarinic) properties [1.6.4, 1.6.6]. While effective for many, its use is restricted in certain populations and conditions due to a range of potential adverse effects.
Absolute and Relative Contraindications
A contraindication is a specific situation in which a drug should not be used because it may be harmful to the person. It's essential to distinguish between absolute contraindications (situations where the drug must not be used) and relative contraindications (where caution is advised, and the benefits must outweigh the risks).
Absolute Contraindications
- Hypersensitivity: A known allergy to cyclizine or any of its ingredients is an absolute contraindication. Allergic reactions can range from skin rashes to severe anaphylaxis, including swelling of the face, lips, or tongue, and difficulty breathing [1.2.2, 1.5.3].
- Acute Alcohol Intoxication: Cyclizine should not be taken with alcohol. Its anti-vomiting properties can mask and potentially increase the toxicity of alcohol [1.2.7, 1.3.6].
- Children Under 6: Cyclizine tablets are not recommended for use in children under the age of six [1.5.3, 1.3.4].
Conditions Requiring Precaution (Relative Contraindications)
Due to its anticholinergic effects, cyclizine must be used with caution in individuals with certain pre-existing conditions [1.2.8]. A healthcare provider should be consulted if you have any of the following:
- Glaucoma: Cyclizine can increase pressure within the eye, potentially worsening this condition [1.2.2, 1.3.5].
- Urinary Retention & Prostate Enlargement: Men with an enlarged prostate gland may find it more difficult to pass urine, a side effect that cyclizine can exacerbate [1.2.2, 1.3.1].
- Obstructive Bowel Conditions: The medication can worsen issues in patients with conditions like Crohn's disease or diverticulitis that could lead to bowel obstruction [1.2.2, 1.2.3].
- Severe Liver Disease: Since cyclizine is metabolized by the liver, severe hepatic impairment can affect how the drug is processed [1.2.2, 1.2.5].
- Epilepsy: Individuals with epilepsy or other conditions that cause seizures should use cyclizine cautiously as it may affect seizure thresholds [1.2.2, 1.2.3].
- Cardiovascular Disease: In patients with severe heart failure, cyclizine can sometimes cause a fall in cardiac output associated with an increased heart rate [1.2.2, 1.6.9].
- Porphyria: This rare inherited blood disorder is another condition where cyclizine should be avoided [1.2.2, 1.2.3].
- Phaeochromocytoma: A rare tumor of the adrenal glands [1.2.2, 1.2.8].
- Breathing Problems: Patients with conditions like asthma, emphysema, or chronic bronchitis should consult a doctor before use [1.3.1].
Significant Drug Interactions
Cyclizine's effects can be dangerously amplified when combined with other substances that depress the central nervous system (CNS). It's crucial to inform your doctor about all medications you are taking.
- CNS Depressants: Combining cyclizine with alcohol, sleeping pills, opioid painkillers (like hydrocodone or morphine), tranquilizers, or medications for anxiety and depression can lead to increased drowsiness, sedation, and impaired coordination [1.3.2, 1.4.6, 1.4.8].
- Anticholinergic Drugs: Taking other medications with anticholinergic properties (used for various conditions including depression and bladder control) can intensify side effects like dry mouth, blurred vision, and urinary retention [1.2.1, 1.4.5].
- Monoamine Oxidase Inhibitors (MAOIs): Antidepressants like phenelzine can interact with cyclizine [1.4.5].
- QTc-Prolonging Drugs: Cyclizine can interact with numerous drugs that affect heart rhythm, increasing the risk of QTc prolongation, a potentially serious heart rhythm change. Examples include certain antibiotics (azithromycin), antiarrhythmics (amiodarone), and antipsychotics [1.4.1].
Comparison of Anticholinergic Side Effects
Feature | Cyclizine | Scopolamine (another motion sickness drug) |
---|---|---|
Primary Use | Nausea, vomiting, motion sickness [1.5.3] | Motion sickness, postoperative nausea [1.4.7] |
Common Side Effects | Drowsiness, dry mouth, blurred vision [1.3.7] | Dry mouth, drowsiness, blurred vision |
Anticholinergic Potency | Moderate | High |
CNS Effects | Can cause drowsiness, confusion, dizziness [1.2.4] | Can cause significant drowsiness, disorientation |
Risk in Glaucoma | Caution required [1.2.2] | Contraindicated in angle-closure glaucoma |
Warnings and Special Populations
- Pregnancy and Breastfeeding: While sometimes used for severe morning sickness, manufacturers generally advise that cyclizine be avoided during pregnancy unless prescribed by a doctor, as definitive human data is limited [1.2.8, 1.5.5]. The drug is excreted in human milk, and its use is not recommended for breastfeeding women [1.2.8].
- Elderly Patients: Individuals over 65 may have a stronger reaction to cyclizine and may require a smaller dose. They are also more susceptible to side effects like confusion, dizziness, and impairment in judgment [1.3.5, 1.2.3].
- Driving and Operating Machinery: Due to common side effects like drowsiness, blurred vision, and impaired coordination, you should not drive or operate heavy machinery until you know how cyclizine affects you [1.5.1].
Conclusion
Cyclizine is an effective anti-sickness medication, but its use is governed by important contraindications and precautions. Its anticholinergic properties are the primary reason for caution in patients with glaucoma, urinary retention, and certain heart conditions. The most significant risk comes from its additive effects when combined with other CNS depressants like alcohol or opioids. Always consult a healthcare professional or pharmacist before taking cyclizine to ensure it is safe for you, especially if you have pre-existing medical conditions or are taking other medications [1.2.2, 1.3.2].
Disclaimer: This article is for informational purposes only and does not constitute medical advice. Always consult with a qualified healthcare professional before starting or stopping any medication.