levocetirizine/phenylpropanolamine

Action and Spectrum

Actions and Spectrum: 

levocetirizine: 

levocetirizine is an antihistamine. It belongs to the second-generation antihistamines, which are used to relieve allergy symptoms. 

Its primary action is to block the effects of histamine. 

levocetirizine helps reduce symptoms such as sneezing, runny/itchy nose, itchy or watery eyes, and itching of the throat or nose. 

It is commonly used to treat allergic rhinitis (hay fever) and chronic urticaria (hives). 

phenylpropanolamine: 

phenylpropanolamine is a decongestant. 

Its primary action is constricting blood vessels in the nasal passages and reducing swelling and congestion. 

Combining levocetirizine and phenylpropanolamine often relieves multiple allergy and cold symptoms, including congestion and various allergic reactions. 

Drug Interaction

Adverse Reaction

Frequency not defined 

Dryness in mouth 

Insomnia 

Allergic reaction 

Nausea 

Headache 

High blood pressure 

Palpitations 

Fatigue 

Sleepiness 

Black Box Warning

Black Box Warning: 

None 

Contraindication / Caution

Contraindication/Caution: 

Contraindication 

• Hypersensitivity or Allergy: Individuals with a known hypersensitivity or allergy to levocetirizine, phenylpropanolamine, or any other ingredients in the medication should not use it. 
• Cardiovascular Conditions: phenylpropanolamine, a decongestant component, can have stimulant effects on the cardiovascular system.  
• Cerebrovascular Conditions: phenylpropanolamine may increase the risk of stroke or other cerebrovascular events. It should be avoided or used cautiously in individuals with a history of cerebrovascular conditions or increased risk factors. 
• Severe Kidney Disease: levocetirizine and phenylpropanolamine are excreted through the kidneys. People with severe kidney impairment may need dosage adjustments or should avoid this medication altogether. 
• Severe Liver Disease: levocetirizine may have a longer duration of action in individuals with severe liver disease, and phenylpropanolamine can affect liver metabolism. Caution or dosage adjustments may be needed in these cases. 
• Diabetes: phenylpropanolamine may affect blood sugar levels, so individuals with diabetes should use this medication cautiously and monitor their blood sugar closely. 
• Pregnancy and Breastfeeding: The safety of levocetirizine/phenylpropanolamine during pregnancy and breastfeeding is not well-established.  
• Monoamine Oxidase Inhibitors (MAOIs): phenylpropanolamine should not be used in individuals who have taken MAOIs within the last 14 days, as it can lead to serious side effects. 
• Prostate Hypertrophy: phenylpropanolamine can exacerbate symptoms of prostate hypertrophy (enlarged prostate). It should be used cautiously in individuals with this condition. 
• Glaucoma: phenylpropanolamine may increase intraocular pressure and worsen the symptoms of glaucoma. It should be used with caution in individuals with glaucoma. 

Caution 

• Cardiovascular Conditions: phenylpropanolamine, a decongestant component, can have stimulant effects on the cardiovascular system.  
• Cerebrovascular Conditions: phenylpropanolamine may increase the risk of stroke or other cerebrovascular events. Caution is advised in individuals with a history of cerebrovascular conditions or increased risk factors. 
• Prostate Hypertrophy: phenylpropanolamine can exacerbate symptoms of prostate hypertrophy (enlarged prostate). Caution is recommended for individuals with this condition. 
• Diabetes: phenylpropanolamine may affect blood sugar levels, potentially causing fluctuations. Individuals with diabetes should use this medication cautiously and closely monitor their blood sugar. 
• Severe Kidney or Liver Impairment: levocetirizine and phenylpropanolamine are metabolized and excreted through the kidneys and liver. Caution or dosage adjustments may be needed in individuals with severe kidney or liver disease. 
• Thyroid Disorders: phenylpropanolamine may affect thyroid function. Caution is advised in individuals with thyroid disorders, and monitoring may be necessary. 
• Alcohol and Sedatives: phenylpropanolamine can enhance the sedative effects of alcohol and also other central nervous system depressants. Avoid or use caution when consuming alcohol or taking sedative medications while using this combination product. 
• Elderly Individuals: The elderly may be more sensitive to the effects of this medication, especially its cardiovascular and central nervous system effects.  
• Pregnancy and Breastfeeding: The safety of levocetirizine/phenylpropanolamine during pregnancy and breastfeeding is not well-established.  
• Monoamine Oxidase Inhibitors (MAOIs): phenylpropanolamine should not be used in individuals who have taken MAOIs within the last 14 days, as it can lead to serious side effects. 
• Glaucoma: phenylpropanolamine may increase intraocular pressure and worsen the symptoms of glaucoma. Use with caution in individuals with glaucoma. 
• Allergic Reactions: Certain individuals might be sensitive or allergic to components of the medication. If you experience allergic symptoms, discontinue use and seek medical attention. 

Pregnancy / Lactation

Pregnancy consideration:  

US FDA pregnancy category: Not assigned. 

Lactation:   

Excreted into human milk: Not known. 

Pregnancy category: 

• Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 
• <b>Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 
• Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    
• Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.    
• Category X: Drugs listed in this category outweigh the risks over benefits. Hence, these categories of drugs need to be avoided by pregnant women.    
• Category N: There is no data available for the drug under this category. 

Pharmacology

Pharmacology: 

levocetirizine/phenylpropanolamine is a combination medication with distinct pharmacological properties. levocetirizine, the antihistamine component, selectively blocks H1 histamine receptors, thereby reducing the effects of histamine release during allergic reactions. This results in the relief of allergy symptoms such as sneezing, runny nose, and itching. phenylpropanolamine, a decongestant, constricts blood vessels in the nasal passages, reducing swelling and congestion; it is instrumental in addressing nasal congestion associated with allergies and upper respiratory conditions.

Combining these two agents aims to alleviate allergy-related symptoms, including nasal congestion, itching, and rhinorrhea, offering a comprehensive approach to managing allergic rhinitis and related conditions. It’s important to note that phenylpropanolamine has been removed from many over-the-counter products due to safety concerns, and its availability may vary by region and regulation. 

Pharmacodynamics: 

Mechanism of action: levocetirizine/phenylpropanolamine is a combination medication that typically contains two active ingredients: levocetirizine and phenylpropanolamine.  

levocetirizine: 

levocetirizine is a second-generation antihistamine. 

Its mechanism of action primarily involves blocking the effects of histamine, a natural substance produced by the body during an allergic reaction. 

Histamine binds to H1 histamine receptors in various tissues, leading to symptoms like itching, sneezing, runny nose, and watery eyes. 

levocetirizine selectively antagonizes (blocks) H1 histamine receptors, preventing histamine from binding to them. 

By doing so, levocetirizine reduces or alleviates the allergic symptoms associated with histamine release. 

phenylpropanolamine: 

phenylpropanolamine is a sympathomimetic agent and decongestant. 

Its mechanism of action involves stimulating alpha-1 adrenergic receptors in blood vessels, particularly in the nasal mucosa. 

Activation of these receptors causes vasoconstriction, which narrows blood vessels and diminishes blood flow to the nasal passages. 

This constriction of blood vessels in the nasal mucosa reduces nasal congestion and swelling. 

As a result, phenylpropanolamine helps relieve nasal congestion and sinus pressure associated with allergies and upper respiratory conditions. 

The combination of levocetirizine and phenylpropanolamine aims to provide comprehensive relief from various allergy symptoms, including sneezing, runny or stuffy nose, itching, and congestion.  

Pharmacokinetics: 

Absorption 

levocetirizine is well-absorbed from the gastrointestinal tract after oral administration. It reaches peak plasma concentrations within about 1 to 2 hours after ingestion. 

phenylpropanolamine is also well-absorbed from the gastrointestinal tract after oral administration, and it can reach peak plasma concentrations within a couple of hours. 

Distribution 

levocetirizine is extensively distributed throughout the body, with a high degree of protein binding (approximately 90%). It can cross the blood-brain barrier, contributing to its central nervous system effects. 

It is distributed throughout the body, with a relatively short duration of action. The distribution is less extensively studied compared to levocetirizine. 

Metabolism 

levocetirizine undergoes limited hepatic metabolism, primarily via cytochrome P450 (CYP) enzymes, particularly CYP3A4 and CYP2D6. However, the extent of metabolism is relatively low compared to some other antihistamines.  

phenylpropanolamine is metabolized in the liver, primarily by enzymes like CYP2D6, into various metabolites. These metabolites are then eliminated from the body. 

Elimination and Excretion 

Most levocetirizine is excreted unchanged in the urine, with a half-life of approximately 8-9 hours in adults. It is primarily eliminated via renal excretion. 

The elimination half-life of phenylpropanolamine is relatively short, typically around 2 to 3 hours. It is mainly excreted in the urine as both unchanged drugs and metabolites. 

Adminstartion

Administration: 

The administration of levocetirizine/phenylpropanolamine should always follow the specific instructions which is provided by the healthcare provider/the directions on the medication label. It’s crucial to use this combination of medications precisely as directed to ensure its effectiveness and minimize the risk of side effects.  

Dosage: The recommended dosage of levocetirizine/phenylpropanolamine can vary depending on the product and formulation. The dosing instructions should be clearly stated on the product label. Follow these instructions carefully. 

Oral Administration: levocetirizine/phenylpropanolamine is usually taken orally by mouth. It is typically available in tablet or capsule form. 

Timing: Take the medication as your healthcare provider prescribes or as directed on the label. Some medications may be taken once daily, while others may be taken multiple times daily. Follow the dosing schedule strictly. 

With or Without Food: Some medications are recommended to be taken with food to diminish stomach upset, while others can be taken without regard to meals.  

Stay Hydrated: Ensure you drink enough water when taking this medication to stay hydrated.  

Duration of Use: Use levocetirizine/phenylpropanolamine for the duration prescribed by your healthcare provider or as indicated on the label. Do not stop taking it before completing the prescribed course, even if your symptoms improve, unless advised by your healthcare provider. 

Missed Dose: If a dose is missed, taking it as soon as possible is generally recommended. However, if the next scheduled dose is missed, it should be skipped and the following dose should be taken at the appropriate time. It is key to avoid taking a double dose of the drug in order to compensate for the missed dose. 

Storage: Store the medication according to the instructions on the label. Typically, it should be stored at room temperature, away from moisture and heat. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: levocetirizine/phenylpropanolamine 

Why do we use levocetirizine/phenylpropanolamine? 

levocetirizine/phenylpropanolamine is a combination medication sometimes prescribed or used to relieve various symptoms associated with certain medical conditions. The specific uses of this combination medication may vary by region and the availability of different formulations.  

Allergic Rhinitis: levocetirizine/phenylpropanolamine is often used to treat allergic rhinitis, commonly known as the hay fever. It helps relieve symptoms such as: 

• Sneezing 
• Runny or stuffy nose 
• Itchy or watery eyes 
• Itchy throat or nose 
• Nasal congestion 

Chronic Urticaria: This combination of medications can also be used to manage the symptoms of chronic urticaria (hives), including: 

• Itchy, raised welts on the skin 
• Skin redness and inflammation 

Nasal Congestion: phenylpropanolamine, a decongestant component of the medication, helps reduce nasal congestion by constricting blood vessels in the nasal passages. This can benefit individuals with colds, allergies, or sinus congestion.