Oral H1 Blockers

Oral H1 Blockers

Medication

Available Preparations

First-generation*

Brompheniramine

Available only as combination products with a decongestant or an antitussive, which are not recommended for children < 6 years

4-, 8-, and 12-mg tablets

2 mg/5 mL elixir

8- and 12-mg tablets (sustained-release, single-entity)

Chlorpheniramine

Available only as combination products with a decongestant or an antitussive, which are not recommended for children < 6 years

2-mg chewable tablets

4-, 8-, and 12-mg tablets

Extended-release: 12-mg tablets or capsules

2 mg/5 mL syrup

Clemastine

1.34- and 2.68-mg tablets

0.67 mg/5 mL syrup

Cyproheptadine

4-mg tablets

2 mg/5 mL syrup

Dexchlorpheniramine

2-mg tablets

2 mg/5 mL syrup

4- and 6-mg tablets (extended-release)

Diphenhydramine

25- and 50-mg capsules or tablets

12.5-mg chewable tablet

12.5 mg/5 mL elixir

12.5 mg/mL syrup

Hydroxyzine

25-, 50-, and 100-mg capsules

10-, 25-, 50-, and 100-mg tablets

10 mg/5 mL syrup

25 mg/5 mL oral suspension

Promethazine

Safer alternatives preferred for allergic disorders in children

12.5-, 25-, and 50-mg tablets

6.25 mg/5 mL and 25 mg/5 mL syrup

Second-generation

Bilastine‡

20-mg tablet

10-mg disintegrating oral tablets

2.5 mg/mL syrup

Cetirizine

5- and 10-mg tablets

1 mg/mL syrup

Desloratadine

5-mg tablets

0.5 mg/mL syrup

Ebastine‡

10-mg tablets

20-mg tablets

20-mg disintegrating oral tablets

1 mg/mL oral solution

Fexofenadine

30-, 60-, and 180-mg tablets

30-mg orally disintegrating tablets

6 mg/mL oral suspension

Levocetirizine

5-mg tablets

0.5 mg/mL oral solution

Loratadine

10-mg tablets and capsules

5-mg chewable tablets

5- and 10-mg disintegrating oral tablets

1 mg/mL syrup

1 mg/mL oral solution

Mizolastine‡

10-mg tablets

Rupatadine‡

10-mg tablets

1 mg/mL oral solution

Cetirizine/pseudoephedrine

5-mg cetirizine plus 120-mg pseudoephedrine tablets

Fexofenadine/pseudoephedrine

60-mg fexofenadine plus 120-mg pseudoephedrine tablets

180-mg fexofenadine plus 240-mg pseudoephedrine tablets

Loratadine/pseudoephedrine

5-mg loratadine plus 120-mg pseudoephedrine tablets

10-mg loratadine plus 240-mg pseudoephedrine tablets

Acrivastine/pseudoephedrine

8-mg acrivastine plus 60-mg pseudoephedrine capsules

* Most first-generation antihistamines have strong anticholinergic properties. Generally, they should not be used in older adults or in patients with glaucoma, benign prostatic hyperplasia, constipation, delirium, dementia, or orthostatic hypotension. These medications commonly cause sedation, dry mouth, blurred vision, urinary retention, constipation, and orthostatic hypotension. Long-term use of some first-generation antihistamines has been linked to cognitive decline and dementia.

In children, first-generation antihistamines should be used only as needed given their potential adverse effects, particularly when combined with other medications; second-generation antihistamines are preferred for allergic rhinitis.

† Usually, brompheniramine and chlorpheniramine are available only in combination with other medications (eg, decongestants, cough suppressants). Brompheniramine and chlorpheniramine combined with other medications (eg, dextromethorphan, phenylephrine) should not be used in children < 6 years.

‡ Not available in the United States.

* Most first-generation antihistamines have strong anticholinergic properties. Generally, they should not be used in older adults or in patients with glaucoma, benign prostatic hyperplasia, constipation, delirium, dementia, or orthostatic hypotension. These medications commonly cause sedation, dry mouth, blurred vision, urinary retention, constipation, and orthostatic hypotension. Long-term use of some first-generation antihistamines has been linked to cognitive decline and dementia.

In children, first-generation antihistamines should be used only as needed given their potential adverse effects, particularly when combined with other medications; second-generation antihistamines are preferred for allergic rhinitis.

† Usually, brompheniramine and chlorpheniramine are available only in combination with other medications (eg, decongestants, cough suppressants). Brompheniramine and chlorpheniramine combined with other medications (eg, dextromethorphan, phenylephrine) should not be used in children < 6 years.

‡ Not available in the United States.