NCBI Bookshelf. A service of the National Library of Medicine, National Institutes of Health.
Carson S, Lee N, Thakurta S. Drug Class Review: Newer Antihistamines: Final Report Update 2 [Internet]. Portland (OR): Oregon Health & Science University; 2010 May.
This publication is provided for historical reference only and the information may be out of date.
Adverse events from head-to-head and active control trials in adults (Original Report)a
| Author Year | Adverse events | Total withdrawals | Withdrawals from AEs |
|---|---|---|---|
| Head-to-head trials | |||
| Ciprandi 199729 L: loratadine 10 mg qd C: cetirizine 10 mg qd | No significant AEs reported | Total: 0 | 0 |
| Hampel 200331 F: fexofenadine 180mg qd C: cetirizine 10mg qd | Total AEs: 16.7% AEs per group: F: 16.9% C: 16.6% F: less overall drowsiness P=0.0110, NS effect on motivation | Total: 3.2% F: 2.8% C: 3.6% | 1.2% AEs 3 efficacy Safety evaluated in AE population |
| Howarth 199932 F1: fexofenadine 120 mg qd F2: fexofenadine 180 mg qd C: cetirizine 10 mg qd P: placebo | Treatment-related AEs: F1: 23% F2: 23% C: 25% P: 25 % | Total: 14% Similar among groups (numbers per group NR) | F: 2% C: <1% P: 2% |
| Prenner 200033 L: loratadine 10 mg qd F: fexofenadine 120 mg qd | F 22.1% vs. L 18.2% had ≥1 AE. Considered treatment related in F 8.3% L 5.3% | NR | NR |
| Van Cauwenberge 200036 L: loratadine 10 mg qd F: fexofenadine 120 mg qd P: placebo | 16.4% of total F: 16.8% L: 17.5% P: 14.7% | Total: 10% F: 9% L: 12% P: 11% | F: 1% L: 2% P: 3% |
| Guerra 199474 L: loratadine 10mg C: cetirizine 10mg P: placebo | 20.7% Total NSD. L: 15.8% C: 27.5% P: 15.8% | C: 1 | C: 2.5% stomach pain |
| Active control trials | |||
| Frolund 199072 L: loratadine 10 mg qd C: clemastine 1 mg bid P: placebo | 32.9% Total L: 15% (P<0.05) C: 58.8%, sedation significant P: 49% placebo | Total: 13.5% L: 9.4% C: 5.8% P: 25.4% | L: 0% C: 1.9%: 1 AE/2 efficacy P: 0% |
| Breneman 199687 C: cetirizine 10mg qd H: hydroxyzine 25 mg tid P: placebo | C: 18% H: 30% P: 6% H vs. P. P=0.001 | Total: 4.8% C: 1.7% H: 6.3% P: 6.1% | Somnolence: C: 1.7% H: 6.3% P: 6.1% |
| Berger 200327 D: desloratadine 5 mg A1: azelastine nasal A2: azelastine nasal + loratadine P: placebo | Most common per treatment: Bitter taste A1: 11% vs. A2: 4% D: Headache 3%, pharyngitis 4% P: headache 7% Somnolence: A1: 2%; A2: 1%; D: 1%; P: 1% | A1: 2% D: 1% P: 1% | A1: 2% (moderate chest pain, lightheadedness) D: 1% (headache and nausea) P: 1% (rash) |
| Dockhorn 198756 L: loratadine 10 mg C: clemastine 2 mg P: placebo | More AEs (considered probably or possibly treatment-related) in C C: 37% L: 21% P: 20% (p≤0.01) More sedation in C: C: 22% L: 6% (p≤0.01) | NR | NR |
- a
Only fair- and good-quality studies are presented in the table. Poor-quality studies are listed in Appendix F.
Abbreviations: bid, twice daily; mg, milligrams; NSD, no significant difference; NR, not reported; qd, once daily; tid, 3 times daily.
Adverse events from studies in adults (includes only studies from update 2003–2005)a
| Type of AE | Adverse event | Cetirizine | Fexofenadine | Loratadine |
|---|---|---|---|---|
| NEUROLOGICAL | ||||
| MAJOR | ||||
| MINOR | Fatigue/Asthenia | 6.8% vs. rupatadine 10.5%, NSD52 | 6.0%; vs. rupatadine 10 mg 10.7%; vs. rupatadine 20 mg 11.7%: NSD55 | |
| Headache | 19.7% vs. 15.3% rupatadine, NSD52 | 2.2% vs. cetirizine 0%, NSD75 5% vs. placebo 3%79 | 18%; vs. fluticasone 17%168 12.1%; vs. rupatadine 10 mg 23.4%; vs. rupatadine 20 mg 14.3%, NSD55 5.8%; vs. ebastine 10 mg 4.3%; vs. ebastine 20 mg 3.2%; vs. placebo 4.3%53 | |
| Somnolence | 2.6% vs. azelastine 1.3%30 8.5% vs. rupatadine 9.6%, NSD52 Drowsiness: 7.7% vs. fexofenadine 4.5%, NSD75 | Drowsiness: 4.5% vs. cetirizine 7.7%, NSD75 | 7.8%; vs. rupatadine 10 mg 12.5%; vs. rupatadine 20 mg 25%, significant but P value not given55 0%; vs. ebastine 10 mg 1.6%; vs. ebastine 20mg 2.7%; vs. NR placebo53 | |
| Unspecified | 0% vs. ebastine 4.6% vs. placebo 0%113 | |||
| GASTROINTESTINAL | ||||
| MAJOR | ||||
| MINOR | Abdominal pain | 0% vs. fexofenadine 2.2%, NSD75 | 2.2% vs. cetirizine 0%, NSD75 | |
| Constipation | 5.8% vs. fexofenadine 0 %, NSD75 | 0% vs. 5.8% cetirizine, NSD75 | ||
| Dry mouth | 1.7% vs. rupatadine 10 mg 1.8% vs. rupatadine 20 mg 3.6%, NSD55 | |||
| Epigastric pain | 3.8% vs. fexofenadine 0%, NSD75 | 0% vs. 3.8% cetirizine, NSD75 | ||
| Unspecified | 0% vs. ebastine 3.2% vs. placebo 3.5%113 | |||
| HEMATOLOGICAL | ||||
| MAJOR | ||||
| MINOR | Abnormalities in complete blood count | |||
| RESPIRATORY | ||||
| MAJOR | 1 patient had asthma requiring hospitalization79 | |||
| MINOR | Cough | 3.8% vs. fexofenadine 0%, NSD75 | 0% vs. 3.8% fexofenadine, NSD75 | 4.3% vs. rupatadine 10 mg 8.0% vs. rupatadine 20 mg 5.4%55 |
| Epistaxis | <1% vs. azelastine 2.0%30 | |||
| Nasal discomfort | <1% vs. azelastine 1.3%30 | |||
| Pharyngitis | 1.7% vs. rupatadine 10 mg 7.1% vs. rupatadine 20 mg 4.5%, NSD55 | |||
| Unspecified | 12.2% vs. ebastine 10 mg 8.5% vs. ebastine 20 mg 7.5% vs. placebo 10.2%53 | |||
| CARDIAC | ||||
| MAJOR | QT interval | No clinically relevant ECG changes vs. placebo79 | Prolonged QTc: 1.6%; vs. ebastine 10 mg 3.2%; vs. ebastine 20 mg 2.2%; vs. placebo 0.5%53 Prolonged QTc: 3.6%; vs. ebastine 20 mg 3.9%; vs. placebo 5.6%113 | |
| MINOR | Unspecified | 2.5%; vs. ebastine 2.8%; vs. placebo 4.2%113 | ||
| OTHER | ||||
| MAJOR | Back pain | 4.3%; vs. rupatadine 10 mg 3.6%; vs. rupatadine 20 mg 4.5%, NSD55 | ||
| MINOR | Bitter taste | <1% vs. azelastine 3.3%30 | ||
| Feet swelling | 0% vs. 2.2% fexofenadine, NSD75 | 2.2% vs. cetirizine 0%, NSD75 | ||
| Hypospadias | OR of hypospadias with loratadine exposure: 1.29 (0.62–2.68)167 Use of nonsedating antihistamines, including loratadine, OR: 1.33 (0.73–2.40)167 | |||
- a
Only fair- and good-quality studies are presented in the table. Poor-quality studies are listed in Appendix F.
Abbreviations: mg, milligrams; NR, not reported; NSD, no significant difference; OR, odds ratio QT, cardiac output; QTc, corrected QT interval for heart rate.
There were no data on desloratadine identified in update 1.
Adverse events from studies in children (Original Report and Update 1)a
| Type of AE | Adverse event | Cetirizine | Desloratadine | Fexofenadine | Loratadine |
|---|---|---|---|---|---|
| NEUROLOGICAL | |||||
| MAJOR | Somnolence and irritability (1 patient, led to withdrawal)110 | ||||
| MINOR | Behavioral screening | NSD vs. placebo117, 147 | |||
| Fatigue | 4.0% vs. chlorpheniramine 6.3% 101 5.3% vs. placebo 0%, NSD109 5.9% vs. placebo 7.5%104 | ||||
| Headache | 6.3% vs. chlorpheniramine 0%101 0% vs. placebo 6.3%, NSD109 15.1% vs. placebo 19.7%99 3.2% vs. placebo 1.6%98 15% vs. placebo 18.8%149 | 1.8 vs. placebo 5.4% (2–5 years)156 1.7 vs. placebo 6.7% (6–11 years)156 | 1–2% in treatment and placebo groups144 | 25% vs. fluticasone 42%103 | |
| Somnolence | 5.5% vs. placebo 0%95 NSD vs. placebo117, 147 21.4% vs. placebo 30.2%148 1/38 patients withdrew due to somnolence vs. 0 in loratadine group110 | 0% vs. dexchlorpheniramine 4.3%102 3% vs. placebo 5%, NSD169 0.5 vs. placebo 1.0%, NSD155 | |||
| Insomnia | 23.8% vs. placebo 44.2%148 | 0 vs. placebo 1.0%, NSD155 | |||
| Irritability | 0 vs. placebo 0.5%, NSD155 | ||||
| Nervousness | 28.6% vs. placebo 44.2%148 | ||||
| Vertigo | 1.6% vs. placebo 0%98 | ||||
| GASTROINTESTINAL | |||||
| MAJOR | |||||
| MINOR | Abdominal pain | 9.6% vs. chlorpheniramine 4.8%101 9.4% vs. placebo 4.5%99 9.3% vs. placebo 4.3%149 | |||
| Abnormal liver function | 9.4% vs. placebo 0%104 NSD vs. placebo in blood chemistry117, 147 | ||||
| Dry mouth | 1.6% vs. placebo 0%98 | ||||
| Increased appetite | 1.6% vs. placebo 0%98 | ||||
| Nausea | 1.6% vs. chlorpheniramine 0%101 | ||||
| HEMATOLOGICAL | |||||
| MAJOR | Neutropenia (asymptomatic) in 1 child100 | ||||
| MINOR | Abnormalities in complete blood count | NSD vs. placebo107 Leucocytosis: 5% vs. placebo 7%104 NSD vs. placebo117, 147 | |||
| CARDIAC | |||||
| MAJOR | QT interval | NSD vs. placebo (2 week follow-up)99 NSD vs. placebo117, 147 NSD QT cetirizine vs. placebo148 NSD QTc vs. placebo149 | NSD rate, PR, QRS or QT vs. placebo156 | NSD QTc vs. placebo92 | |
| RESPIRATORY | |||||
| MAJOR | |||||
| MINOR | Coughing | 3% vs. placebo 5%, NSD169 | |||
| Epistaxis | 7.1% vs. placebo 4.3%99 7.1% vs. placebo 4.3%149 | 4.8% (moderate) vs. dexchlorpheniramine 0%102 4% vs. fluticasone 7%103 | |||
| Pharyngitis | 10.1% vs. placebo 13.6%99 1.6% vs. placebo 4.9%98 10.0% vs. placebo 13.0%149 | 10% vs. fluticasone 16%103 18.8% vs. 18.1%, NSD155 | |||
| OTHER | |||||
| MAJOR | Accidental overdose | 2 children vs. 8 placebo117, 147 | |||
| MINOR | Rash | 3.2% vs. placebo 0%98 1/40 patients withdrew due to rash110 | |||
| Mean increase height and weight | NSD vs. placebo117, 147 | ||||
| Fever | 5.5 vs. placebo 5.4% (2–5 years)156 5.5 vs. placebo 5.4% (6–11 years)156 | 3% vs. placebo 5%, NSD169 | |||
- a
Only fair- and good-quality studies are presented in the table. Poor-quality studies are listed in Appendix F.
Abbreviations: NSD, no significant difference; QT, cardiac output; QTc, corrected QT interval for heart rate.
- Reporting of adverse events - Drug Class Review: Newer AntihistaminesReporting of adverse events - Drug Class Review: Newer Antihistamines
Your browsing activity is empty.
Activity recording is turned off.
See more...