Allergic Rhinitis

Jennifer Kendrick, BScPharm, ACPR, PharmD

Date of Revision: March 16, 2022
Peer Review Date: April 1, 2020

Table 5: Oral Agents for Allergic Rhinitis

Drug/​Cost[a] Dosage Adverse Drug Comments
Effects Interactions

Drug Class: Antihistamines, first-generation

chlorpheniramine​ Adults: 4 mg Q4–6H CNS: sedation, Increased CNS First-generation

[b] PO; maximum fatigue, depression when antihistamines
generics 24 mg/day dizziness, combined with are no longer
Children: impairment of alcohol, recommended
< $10 0.35 mg/kg/day cognition and sedatives, first-line due to
divided Q4–6H PO or performance. tranquilizers, their adverse
Anticholinergic: barbiturates. effect profile.
2–5 y: 1 mg Q4–6H Increased
PO; maximum dry mouth and
eyes, anticholinergic
6 mg/day side effects
constipation,
6–11 y: 2 mg Q4–6H urinary when combined
PO; maximum retention. with TCAs,
12 mg/day scopolamine.
Increased
chlorpheniramine
levels resulting in
increased
adverse effects
when combined
with moderate
CYP2D6
inhibitors, e.g.,
amiodarone,
celecoxib.
Avoid
combination with
strong CYP2D6
inhibitors, e.g.,
bupropion,
paroxetine.

diphenhydramine​ Adults: 25–50 mg CNS: sedation, Increased CNS First-generation

[b] Q6–8H PO; maximum fatigue, depression when antihistamines
Benadryl 300 mg/day dizziness, combined with are no longer
Preparations, Children: impairment of alcohol, recommended
generics 5 mg/kg/day PO cognition and sedatives, first-line due to
given in 3–4 divided performance. tranquilizers, their adverse
< $10 doses Anticholinergic: barbiturates. effect profile.
Maximum: dry mouth and Increased Available in
eyes, anticholinergic pediatric
2–5 y: 37.5 mg/day side effects
constipation, 1.25 mg/mL
6–11 y: 150 mg/day urinary when combined liquid
retention. formulation.
Drug/​Cost[a] Dosage Adverse Drug Comments
Effects Interactions
with TCAs,
scopolamine.
May increase
levels of
CYP2D6
substrates, e.g.,
metoprolol,
venlafaxine.

Drug Class: Antihistamines, second-generation

bilastine Adults and children Minimal to no Bilastine serum First-line in mild

Blexten ≥12 y: 20 mg once anticholinergic levels increase intermittent
daily PO effects. up to 2-fold with allergic rhinitis.
< $10 Children 4–11 y Headache, ketoconazole. Not indicated in
(body wt ≥16 kg): 10 dizziness, Diltiazem can children <4 y or
mg once daily PO somnolence, increase body wt <16 kg.
upper bilastine levels
Available in 2
abdominal pain, by 50%.
pediatric
bradycardia
formulations:
(rare), bundle
10 mg
branch block
orodispersible
(rare).
tablet and 2.5
mg/mL solution.
Orodispersible
tablet can be
placed in the
mouth or
dispersed in
water before
administration.
Administer 1 h
before or 2 h
after meals or
certain fruit
juices; food and
grapefruit juice
can reduce
absorption by
up to 33%.

cetirizine [b]
​ Adults and children Minimal to no Increased CNS First-line in mild
Reactine, ≥6 y: 5–10 mg Q24H anticholinergic depression when intermittent
generics PO; maximum effects. combined with allergic rhinitis.
20 mg/day Headache. alcohol, Cetirizine is the
< $10 Children: May cause sedatives, active
drowsiness in tranquilizers, metabolite of
6–12 months: 2.5 mg barbiturates.
some individuals hydroxyzine.
Q24H PO Increased
especially at Available in
12–23 months: higher doses. anticholinergic pediatric 10 mg
2.5 mg Q24H PO; side effects rapid-dissolve
maximum 2.5 mg when combined tablet and
Q12H with TCAs, 1 mg/mL syrup.
scopolamine.
2–5 y: 2.5 mg Q24H
PO; maximum
Drug/​Cost[a] Dosage Adverse Drug Comments
Effects Interactions
5 mg/day in
1–2 doses

desloratadine Adults and children Minimal to no Pgp inhibitors First-line in mild

[b] ≥12 y: 5 mg Q24H anticholinergic (e.g., intermittent
Aerius, generics PO effects. erythromycin, allergic rhinitis.
Children: Headache. ketoconazole) Desloratadine
< $10 may increase is the active
6–11 months: 1 mg loratadine levels metabolite of
Q24H PO while Pgp loratadine.
1–5 y: 1.25 mg Q24H inducers (e.g., Available in
PO carbamazepine, pediatric
dexamethasone) 0.5 mg/mL
6–11 y: 2.5 mg Q24H
may decrease liquid
PO
loratadine levels; formulation.
clinical effect
probably
minimal.

fexofenadine Adults: 60 mg Q12H Minimal to no Decreased First-line in mild

[b] PO; anticholinergic fexofenadine intermittent
Allegra maximum 180 mg/day effects. level when allergic rhinitis.
(12-h formulation) or Headache. combined with Fexofenadine is
< $10 120 mg/day (24-h aluminum- and the active
formulation) magnesium- metabolite of
Children 2–11 y: containing terfenadine.
30 mg Q12H PO antacids. Only 5% of a
Ingestion of fruit dose is
juices such as metabolized.
apple, grapefruit
or orange may
decrease
bioavailability.

loratadine [b]
​ Adults and children Minimal to no QTc prolongation First-line in mild
Claritin, generics >5 y: 10 mg Q24H anticholinergic reported with intermittent
PO effects. concomitant use allergic rhinitis.
< $10 Children 2–5 y: 5 mg Headache. of loratadine and Available in
Q24H PO amiodarone. pediatric
Caution is 1 mg/mL liquid
advised. formulation as
Pgp inhibitors well as rapid-
(e.g., dissolve
erythromycin, tablets.
ketoconazole)
may increase
loratadine levels
while Pgp
inducers (e.g.,
carbamazepine,
dexamethasone)
may decrease
loratadine levels;
clinical effect
probably
minimal.
Drug/​Cost[a] Dosage Adverse Drug Comments
Effects Interactions

rupatadine Adults and children Minimal to no Increased CNS First-line in mild

Rupall ≥12 y: 10 mg Q24H anticholinergic depression when intermittent
PO effects. combined with allergic rhinitis.
< $10 Children 2–11 y: oral Headache. alcohol, Available in
solution sedatives, pediatric
tranquilizers, 1 mg/mL liquid
10–25 kg: 2.5 mg barbiturates. formulation.
Q24H PO; maximum Grapefruit juice
2.5 mg/day increases
>25 kg: 5 mg Q24H rupatadine
PO; maximum bioavailability
5 mg/day and should be
avoided.
CYP3A4
inhibitors or
inducers may
increase or
decrease
rupatadine
levels,
respectively.

Drug Class: Decongestants

pseudoephedrine Adults and children Mild CNS Beta-blockers: Caution in

[b] ≥12 y: 60 mg Q4–6H stimulation antihypertensive patients with
Tantafed, PO; maximum (nervousness, effects may be heart disease,
generics 240 mg/day excitability, reduced. high blood
Sustained-release: restlessness, Contraindicated pressure, angle
< $10 120 mg Q12H PO; dizziness, with MAOIs and closure
maximum 240 mg/day weakness, ergot derivatives. glaucoma,
Children 6–11 y: insomnia). Concurrent use diabetes,
30 mg Q4–6H PO; Peripheral with or use within hyperthyroidism
maximum 120 mg/day vasoconstriction. 2 wk of MAOIs and prostatic
Tachycardia or may cause enlargement.
palpitation may hypertensive
occur. Blood crisis.
pressure may be Avoid use with
increased in phenothiazines
hypertensive and selective
subjects. May serotonin
adversely affect reuptake
blood sugar inhibitors.
control in
diabetics.

Drug Class: Antihistamine, second-generation/decongestant combinations

cetirizine /​ Adults and children Minimal to no Increased CNS Cetirizine is the

pseudoephedrine ≥12 y: 1 tablet anticholinergic depression when active
[b] (5 mg/120 mg) Q12H effects. combined with metabolite of
Reactine PO Headache. alcohol, hydroxyzine.
Complete Mild CNS sedatives, Caution in
stimulation tranquilizers, patients with
< $10 (nervousness, barbiturates. heart disease,
excitability, high blood
Drug/​Cost[a] Dosage Adverse Drug Comments
Effects Interactions
restlessness, Increased pressure, angle
dizziness, anticholinergic closure
weakness, side effects glaucoma,
insomnia). when combined diabetes,
Peripheral with TCAs, hyperthyroidism
vasoconstriction. scopolamine. and prostatic
Tachycardia or Beta-blockers: enlargement.
palpitation may antihypertensive
occur. Blood effects may be
pressure may be reduced.
increased in Contraindicated
hypertensive with MAOIs and
subjects. May ergot derivatives.
adversely affect Concurrent use
blood sugar with or use within
control in 2 wk of MAOIs
diabetics. may cause
hypertensive
crisis.
Avoid use with
phenothiazines
and selective
serotonin
reuptake
inhibitors.

desloratadine /​ Adults and children Minimal to no Pgp inhibitors Desloratadine

pseudoephedrine ≥12 y: 1 tablet anticholinergic (e.g., is the active
[b] (2.5 mg/120 mg) effects. erythromycin, metabolite of
Aerius Dual Q12H PO Headache. ketoconazole) loratadine.
Action 12 Hour Mild CNS may increase Caution in
stimulation loratadine levels patients with
< $10 (nervousness, while Pgp heart disease,
excitability, inducers (e.g., high blood
restlessness, carbamazepine, pressure, angle
dizziness, dexamethasone) closure
weakness, may decrease glaucoma,
insomnia). loratadine levels; diabetes,
Peripheral clinical effect hyperthyroidism
vasoconstriction. probably and prostatic
Tachycardia or minimal. enlargement.
palpitation may Beta-blockers:
occur. Blood antihypertensive
pressure may be effects may be
increased in reduced.
hypertensive Contraindicated
subjects. May with MAOIs and
adversely affect ergot derivatives.
blood sugar Concurrent use
control in with or use within
diabetics. 2 wk of MAOIs
may cause
hypertensive
crisis.
Avoid use with
phenothiazines
and selective
Drug/​Cost[a] Dosage Adverse Drug Comments
Effects Interactions
serotonin
reuptake
inhibitors.

fexofenadine /​ Adults and children Minimal to no Decreased Fexofenadine is

pseudoephedrine ≥12 y: 1 tablet anticholinergic fexofenadine the active
[b] (60 mg/120 mg) effects. level when metabolite of
Allegra-D Q12H PO Headache. combined with terfenadine.
Mild CNS aluminum- and Only 5% of a
< $10 stimulation magnesium- dose is
(nervousness, containing metabolized.
excitability, antacids. Caution in
restlessness, Ingestion of fruit patients with
dizziness, juices such as heart disease,
weakness, apple, grapefruit high blood
insomnia). or orange may pressure, angle
Peripheral decrease closure
vasoconstriction. bioavailability. glaucoma,
Tachycardia or Beta-blockers: diabetes,
palpitation may antihypertensive hyperthyroidism
occur. Blood effects may be and prostatic
pressure may be reduced. enlargement.
increased in Contraindicated
hypertensive with MAOIs and
subjects. May ergot derivatives.
adversely affect Concurrent use
blood sugar with or use within
control in 2 wk of MAOIs
diabetics. may cause
hypertensive
crisis.
Avoid use with
phenothiazines
and selective
serotonin
reuptake
inhibitors.

loratadine /​ Adults and children Minimal to no QTc prolongation Caution in

pseudoephedrine ≥12 y: 1 tablet anticholinergic reported with patients with
[b] (5 mg/120 mg) Q12H effects. concomitant use heart disease,
Claritin Allergy + PO Headache. of loratadine and high blood
Sinus, Claritin or 1 tablet Mild CNS amiodarone. pressure, angle
Allergy + Sinus (10 mg/240 mg) stimulation Caution is closure
Extra Strength Q24H PO (nervousness, advised. glaucoma,
excitability, Pgp inhibitors diabetes,
< $10 restlessness, (e.g., hyperthyroidism
dizziness, erythromycin, and prostatic
weakness, ketoconazole) enlargement.
insomnia). may increase
Peripheral loratadine levels
vasoconstriction. while Pgp
Tachycardia or inducers (e.g.,
palpitation may carbamazepine,
occur. Blood dexamethasone)
pressure may be may decrease
increased in loratadine levels;
Drug/​Cost[a] Dosage Adverse Drug Comments
Effects Interactions
hypertensive clinical effect
subjects. May probably
adversely affect minimal.
blood sugar Beta-blockers:
control in antihypertensive
diabetics. effects may be
reduced.
Contraindicated
with MAOIs and
ergot derivatives.
Concurrent use
with or use within
2 wk of MAOIs
may cause
hypertensive
crisis.
Avoid use with
phenothiazines
and selective
serotonin
reuptake
inhibitors.

Drug Class: Leukotriene Receptor Antagonists

montelukast Adults and children Headache, Strong CYP2C9 In patients with

Singulair, ≥15 y: 10 mg QHS abdominal pain, and 3A4 concomitant
Montelukast, PO flulike inducers (e.g., asthma, may
other generics Children: symptoms. carbamazepine, be used as an
Serious phenobarbital, alternative to
$10–20 2–5 y: 4 mg QHS PO phenytoin, INCS.
neuropsychiatric
6–14 y: 5 mg QHS effects (e.g., rifampin) may
PO depression, decrease
nightmares, montelukast
temper levels, whereas
tantrums) and strong CYP2C9
suicidal inhibitors (e.g.,
thoughts/actions amiodarone,
have been fluconazole) may
increase
reported.​[52]
montelukast
levels; clinical
significance is
uncertain;
however, monitor
for reduced
efficacy or
adverse effects.

[a] Cost of 10-day supply; includes drug cost only.

[b] Available without a prescription.

Dosage adjustment may be required in renal impairment.

Eligible for prescribing by pharmacists as part of the Ontario minor ailments program starting January 1, 2023.
 Abbreviations: CNS = central nervous system; MAOI = monoamine oxidase inhibitor; Pgp = P-
glycoprotein; TCA = tricyclic antidepressant

References
52. U.S. Food and Drug Administration. FDA requires Boxed Warning about serious mental health side effects for
asthma and allergy drug montelukast (Singulair); advises restricting use for allergic rhinitis [internet]. March 13,
2020. Available from www.fda.gov/drugs/drug-safety-and-availability/fda-requires-boxed-warning-about-
serious-mental-health-side-effects-asthma-and-allergy-drug. Accessed October 30, 2020.

CPhA assumes no responsibility for or liability in connection with the use of this information. For clinical use only and not intended for for use by
patients. Once printed there is no quarantee the information is up-to-date. [Printed on: 05-29-2023 05:29 PM]
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