Side Effects of levocetirizine: A Synthesis of Findings from 25 Studies

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Original Abstract of the Article

Main Research Findings

Levocetirizine is a second-generation antihistamine that has been shown to be effective in treating allergic diseases such as allergic rhinitis and chronic urticaria in many studies. 25 , 4 . Levocetirizine is the active R-enantiomer of cetirizine and has a higher binding affinity to the H1 receptor than cetirizine, with characteristics such as high bioavailability, rapid onset of action, low volume of distribution, and low metabolism. 4 . Levocetirizine has been shown to effectively improve symptoms of allergic rhinitis and chronic urticaria compared to placebo and other second-generation antihistamines. 4 . Levocetirizine has been shown to be safe with few side effects. 4 . A study showed that levocetirizine has no effect on salivary gland function. 13 .

Levocetirizine may have less sedative effects compared to other antihistamines, and it may not affect the ability to drive a car. 12 . However, levocetirizine may cause drowsiness in some people, and caution is needed when driving or operating machinery. 21 , 19 .

Levocetirizine may cause skin reactions such as fixed drug eruption. 17 , 14 . Fixed drug eruption is a rare form of drug allergy that recurs at the same cutaneous or mucosal site in every usage of drug. 14 . Fixed drug eruption appears soon after drug exposure as single or multiple round, sharply demarcated and dusky red plaques. 14 .

Reasons for Side Effects

Levocetirizine is a drug that suppresses allergic reactions by inhibiting histamine H1 receptors. Histamine is a chemical substance involved in allergic reactions, causing vasodilation and leakage of fluid from capillaries. Levocetirizine inhibits these reactions and improves allergic symptoms by inhibiting histamine H1 receptors.

Levocetirizine can cause side effects such as sedation and drowsiness by inhibiting histamine H1 receptors in the brain. This is because histamine is also involved in maintaining wakefulness and attention in the brain.

Common Side Effects

Drowsiness

Levocetirizine may cause drowsiness. 21 , 19 . Drowsiness is caused by levocetirizine inhibiting histamine H1 receptors in the brain. Drowsiness usually improves within a few days of starting levocetirizine. If drowsiness is severe, consult your doctor.

Dry Mouth

Levocetirizine may cause dry mouth. 24 . Dry mouth is caused by levocetirizine suppressing saliva secretion. If you are concerned about dry mouth, drink plenty of water.

Fatigue

Levocetirizine may cause fatigue. 15 . Fatigue is caused by levocetirizine inhibiting histamine H1 receptors in the brain. If fatigue is severe, consult your doctor.

Headache

Levocetirizine may cause headaches. 24 . Headache is caused by levocetirizine inhibiting histamine H1 receptors in the brain. If the headache is severe, consult your doctor.

Gastrointestinal Symptoms

Levocetirizine may cause gastrointestinal symptoms such as stomach pain, diarrhea, or constipation. 24 . Gastrointestinal symptoms are caused by levocetirizine suppressing muscle contractions in the stomach. If you are concerned about gastrointestinal symptoms, consult your doctor.

Skin Reactions

Levocetirizine may cause skin reactions such as rash, itching, or hives. 24 , 17 . Skin reactions are caused by levocetirizine triggering allergic reactions. If you are concerned about skin reactions, consult your doctor.

Other

Levocetirizine may cause other side effects such as dizziness, visual disturbances, dry mouth, and constipation. 24 . If you are concerned about these side effects, consult your doctor.

Countermeasures for Side Effects

Drowsiness

To prevent drowsiness, avoid driving or operating machinery after taking levocetirizine. 21 , 19 . Also, adjust the time of day you take levocetirizine and take it at night.

Dry Mouth

To prevent dry mouth, drink plenty of water. 24 .

Fatigue

To reduce fatigue, get enough rest and maintain a regular sleep schedule. 15 .

Headache

If you are concerned about headaches, take over-the-counter painkillers. 24 . If headaches occur frequently or are severe, consult your doctor.

Gastrointestinal Symptoms

If you are concerned about gastrointestinal symptoms, pay attention to your diet and avoid stimulants. 24 . If gastrointestinal symptoms do not improve, consult your doctor.

Skin Reactions

If you are concerned about skin reactions, consult your doctor. 24 , 17 . If skin reactions are severe, you may need to stop taking levocetirizine.

Comparison between Studies

Commonalities in Studies

Many studies have shown that levocetirizine is an effective second-generation H1 receptor antagonist for treating allergic diseases such as allergic rhinitis and chronic urticaria. 25 , 4 .

Differences in Studies

Studies on the side effects of levocetirizine have reported drowsiness, dry mouth, fatigue, headache, gastrointestinal symptoms, and skin reactions. 24 , 15 . These side effects may vary from person to person. A study showed that levocetirizine has no effect on salivary gland function. 13 . However, while some studies have shown that levocetirizine may not affect the ability to drive, others have shown that it may cause drowsiness. 12 , 21 , 19 . Some studies have reported that levocetirizine may cause skin reactions such as fixed drug eruption. 17 , 14 . Fixed drug eruption is a rare form of drug allergy that recurs at the same cutaneous or mucosal site in every usage of drug. 14 . Fixed drug eruption appears soon after drug exposure as single or multiple round, sharply demarcated and dusky red plaques. 14 .

Precautions for Real-Life Applications

Levocetirizine is an effective drug for treating allergic diseases such as allergic rhinitis and chronic urticaria, but it may cause side effects such as drowsiness. 21 , 19 . Caution is needed when taking levocetirizine, such as avoiding driving or operating machinery. 21 , 19 . Also, levocetirizine may cause skin reactions such as fixed drug eruption. 17 , 14 . If you are concerned about skin reactions, consult your doctor. 17 , 14 .

Limitations of Current Research

Research on the side effects of levocetirizine is still not sufficient. In particular, further research is needed on the long-term side effects of levocetirizine.

Future Research Directions

Research is needed on the long-term side effects of levocetirizine and the potential for levocetirizine to interact with other drugs.

Conclusion

Levocetirizine is an effective drug for treating allergic diseases such as allergic rhinitis and chronic urticaria, but it may cause side effects such as drowsiness. 21 , 19 . Consult your doctor before taking levocetirizine and make sure you understand the side effects before taking it. Further research is needed on the long-term side effects of levocetirizine and the potential for levocetirizine to interact with other drugs.

Literature analysis of 25 papers
Positive Content
22
Neutral Content
1
Negative Content
2
Article Type
4
0
1
4
23
1.

The Efficacy of a Two-Fold Increase of H1-Antihistamine in the Treatment of Chronic Urticaria - the Vietnamese Experience.

Author: ThiHuyen Tran, ThiLan Pham, VanThuong Nguyen, MinhPhuong Pham Thi, TrongHao Nguyen, VanTro Chau, HuuSau Nguyen, MinhTrang Trinh, HuuNghi Dinh, VanTam Hoang, CamVan Tran, HuyenMy Le, HauKhang Tran, ThanhThuy Nguyen, ThiPhuong Hoang, ThuyLinh Nguyen, GandolfiMarco, SatolliFrancesca, FelicianiClaudio, TirantMichael, VojvodicAleksandra, LottiTorello

Chronic urticaria treatment

Chronic urticaria, a common and debilitating condition, often requires increased doses of H1-antihistamines beyond the recommended dose to achieve satisfactory relief.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.

Language : English

3.

Development of safer molecules through chirality.

Author: PatilP A, KothekarM A

Chiral drugs

This review discusses the pharmacokinetic and pharmacodynamic implications of chirality in drug development, focusing on the benefits of replacing racemates with single enantiomers. It highlights successful chiral switches, such as levosalbutamol, S-ketamine, and levocetirizine, which have led to improved safety and efficacy profiles compared to their racemic counterparts.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
ReviewAn article that critically examines existing research on a particular topic and summarizes the current state of knowledge in the field.

Language : English

5.

Clinical and immunologic effects of H1 antihistamine preventive medication during honeybee venom immunotherapy.

Author: MüllerUlrich R, JutelMarek, ReimersAndrea, ZumkehrJudith, HuberClarissa, KriegelCarola, SteinerUrs, HaeberliGabrielle, AkdisMübeccel, HelblingArthur, SchnyderBenno, BlaserKurt, AkdisCezmi

BVIT efficacy
BVIT safety

Levocetirizine significantly reduced side effects during honeybee venom immunotherapy (BVIT) without affecting efficacy. It also modulated the allergen-specific immune response, potentially influencing the expression of histamine receptors and cytokine production.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Randomized Controlled TrialA clinical trial that randomly assigns participants to treatment and control groups to evaluate the effects of an intervention.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

6.

Novel levocetirizine HCl tablets with enhanced palatability: synergistic effect of combining taste modifiers and effervescence technique.

Author: LabibGihan S

Effervescent tablets
Taste-masking

This study investigated the taste-masking effect of different ratios of 2-hydroxypropyl-β-cyclodextrin and mannitol on levocetirizine HCl. The study found that both inclusion complex formation and solid dispersion techniques were effective in masking the taste of levocetirizine HCl. The study also investigated the feasibility of preparing effervescent tablets from the taste-masked blends.

Comparative StudyResearch that compares multiple groups/interventions to determine differences/similarities in outcomes/characteristics.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

7.

Brain histamine H1 receptor occupancy measured by PET after oral administration of levocetirizine, a non-sedating antihistamine.

Author: HiraokaKotaro, TashiroManabu, GroboschThomas, MaurerMarcus, OdaKeiichi, ToyoharaJun, IshiiKenji, IshiwataKiichi, YanaiKazuhiko

Non-sedating antihistamine

Levocetirizine, a second-generation antihistamine, showed less brain H1R occupancy and subjective sleepiness compared to fexofenadine, suggesting a better non-sedating profile.

Controlled Clinical TrialA clinical trial that evaluates the effectiveness of a treatment by comparing a group that receives the intervention with a group that receives a placebo or standard treatment.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

8.

Comparative Efficacy and Safety of Ebastine 20 mg, Ebastine 10 mg and Levocetirizine 5 mg in Acute Urticaria.

Author: GoyalVippan, GuptaAnu, GuptaOnam, LalDhruvendra, GillManharan

Urticaria treatment

Second-generation non-sedating H1 antihistamines are often used as first-line treatment for acute and chronic urticaria.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.

Language : English

9.

Implications of the IQ-CSRC Prospective Study: Time to Revise ICH E14.

Author: DarpoBorje, GarnettChristine, KeirnsJames, StockbridgeNorman

QT assessment

This commentary discusses the use of exposure-response (ER) analysis in early phase clinical studies to evaluate the effect of a drug on cardiac repolarization. The results of a recent study suggest that careful ECG evaluation using ER analysis could replace or serve as an alternative to the thorough QT study.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

11.

Effects of levocetirizine and diphenhydramine on regional glucose metabolic changes and hemodynamic responses in the human prefrontal cortex during cognitive tasks.

Author: KikuchiAsuka, NasirFairuz Binti Mohammadi, InamiAkie, MohsenAttayeb, WatanukiShoichi, MiyakeMasayasu, TakedaKazuko, KoikeDaigo, ItoTakayasu, SasakawaJunpei, MatsudaRin, HiraokaKotaro, MaurerMarcus, YanaiKazuhiko, WatabeHiroshi, TashiroManabu

Antihistamine efficacy
Antihistamine side effects
Cognitive impairment

Antihistamines, especially diphenhydramine, may disrupt the physiological coupling between metabolism and perfusion in the brain, potentially leading to increased energy demands and suppressed vascular permeability.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Randomized Controlled TrialA clinical trial that randomly assigns participants to treatment and control groups to evaluate the effects of an intervention.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

12.

A simulated car-driving study on the effects of acute administration of levocetirizine, fexofenadine, and diphenhydramine in healthy Japanese volunteers.

Author: InamiAkie, MatsudaRin, GroboschThomas, KomamuraHiroshi, TakedaKazuko, YamadaYusuke, MiyakeMasayasu, HiraokaKotaro, MaurerMarcus, YanaiKazuhiko, TashiroManabu

No sedative effects

This study evaluated the sedative effects of levocetirizine, a new-generation antihistamine, in healthy Japanese subjects.

Comparative StudyResearch that compares multiple groups/interventions to determine differences/similarities in outcomes/characteristics.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Randomized Controlled TrialA clinical trial that randomly assigns participants to treatment and control groups to evaluate the effects of an intervention.

Language : English

13.

Evaluation by (99m)Tc-pertechnetate scintigraphy of the effect of levocetirizine on salivary glands function, in allergic rhinitis patients.

Author: SevenBedri, YorukOzgur, VarogluErhan, UcuncuHarun, SahinAli, Kursad AyanArif, SutbeyazYavuz

Allergic rhinitis treatment

This study assessed the effect of levocetirizine on salivary gland function in patients with allergic rhinitis using technetium-99m pertechnetate ((99m)Tc-P) salivary gland scintigraphy. Levocetirizine treatment showed a significantly higher salivary gland function compared to untreated patients and healthy controls, with no side effects.

Controlled Clinical TrialA clinical trial that evaluates the effectiveness of a treatment by comparing a group that receives the intervention with a group that receives a placebo or standard treatment.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.

Language : English

14.

Ursodeoxycholic acid induced generalized fixed drug eruption.

Author: OzkolHatice Uce, CalkaOmer, DulgerAhmet Cumhur, BulutGulay

Fixed drug eruption

Fixed drug eruption (FDE) is a rare form of drug allergy that recurs at the same site with every exposure to the drug. This case report describes a patient who developed generalized FDE after taking ursodeoxycholic acid (UDCA) for cholestasis. This is the first reported case of FDE related to UDCA intake.

Case ReportsIn the medical field, a report that describes in detail a unique case, an unusual medical condition, or the effect of a treatment. Provides new insights and possibilities for treatment through individual patient cases.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.

Language : English

16.

Efficacy and Safety of Up-dosing Antihistamines in Chronic Spontaneous Urticaria: A Systematic Review of the Literature.

Author: Iriarte SotésP, ArmisénM, Usero-BárcenaT, Rodriguez FernándezA, Otero RivasM M, GonzalezM T, Meijide CalderónA, VeleiroB,

Urticaria treatment

This study reviews the clinical evidence on the efficacy and safety of higher-than-licensed dosage of second-generation oral antihistamines in the treatment of chronic spontaneous urticaria (CSU).

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Systematic ReviewA review that systematically collects, evaluates, and integrates relevant research to answer a specific research question.

Language : English

17.

Fixed drug eruption due to levocetirizine.

Author: JhajRatinder, AsatiDinesh Prasad, ChaudharyDeepa

FDE
Scabies

This case report describes a 49-year-old male patient with scabies who developed a fixed drug eruption (FDE) due to levocetirizine. The patient had a history of cetirizine induced FDE in the past.

Case ReportsIn the medical field, a report that describes in detail a unique case, an unusual medical condition, or the effect of a treatment. Provides new insights and possibilities for treatment through individual patient cases.

Language : English

18.

Assessment of the effects of antihistamine drugs on mood, sleep quality, sleepiness, and dream anxiety.

Author: OzdemirPinar Guzel, KaradagAyşe Serap, SelviYavuz, BoysanMurat, BilgiliSerap Gunes, AydinAdem, OnderSevda

Improved sleep quality
Reduced dream anxiety
Daytime sleepiness
Mood disturbances

Both classic and new-generation antihistamines significantly increased daytime sleepiness and nocturnal sleep quality.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Randomized Controlled TrialA clinical trial that randomly assigns participants to treatment and control groups to evaluate the effects of an intervention.

Language : English

21.

Peripheral and central H1 histamine receptor occupancy by levocetirizine, a non-sedating antihistamine; a time course study in the guinea pig.

Author: GuptaA, GillardM, ChristopheB, ChatelainP, MassinghamR, Hammarlund-UdenaesM

Central side effects

Levocetirizine, an antihistamine, exhibits delayed brain H1 receptor occupancy compared to plasma H1 receptor occupancy, suggesting that the blood-brain barrier may play a role in the central side effects of antihistamines.

Comparative StudyResearch that compares multiple groups/interventions to determine differences/similarities in outcomes/characteristics.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

22.

[Antipruritic efficacy of a high-dosage antihistamine therapy. Results of a retrospectively analysed case series].

Author: SchulzS, MetzM, SiepmannD, LugerT A, MaurerM, StänderS

Symptom relief
Not effective at standard doses

High-dosage antihistamines can be effective and safe for treating chronic pruritus of different origins.

Controlled Clinical TrialA clinical trial that evaluates the effectiveness of a treatment by comparing a group that receives the intervention with a group that receives a placebo or standard treatment.
English AbstractA summary of a research paper/publication written in English for a wider audience.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.

Language : German

24.

Allergic rhinitis in family practice: the role of levocetirizine in clinical care.

Author: BuksteinDonald A, LapineThomas J

Allergic rhinitis treatment
Side effects

Allergic rhinitis, affecting over 20% of the US population, significantly impacts quality of life and productivity. While pharmacotherapy is widely used, newer antihistamines, like levocetirizine, offer the promise of enhanced efficacy and tolerability. This article reviews the value of levocetirizine for treating allergic rhinitis based on its pharmacologic profile, efficacy, and safety.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.
ReviewAn article that critically examines existing research on a particular topic and summarizes the current state of knowledge in the field.

Language : English

25.

Levocetirizine: the allergist's arsenal grows larger.

Author: BloebaumR Matthew, GrantJ Andrew

Allergic rhinitis treatment
Chronic urticaria treatment

Levocetirizine, a selective H1-receptor blocker, has shown to be a safe and effective treatment for allergic rhinitis and chronic urticaria.

Clinical TrialA clinical trial is a planned study conducted on humans to evaluate the efficacy and safety of pharmaceuticals, medical devices, and treatment methods. It aims to explore the possibilities of new treatments and improve the health of patients.
Comparative StudyResearch that compares multiple groups/interventions to determine differences/similarities in outcomes/characteristics.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.

Language : English

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