Allergic rhinitis or conjunctivitis: Oral: 10 mg once daily; alternatively, may be given as needed 2 to 5 hours before exposure to allergen, although this may be less effective than daily administration (Ref).
OTC labeling (patient-guided therapy for symptoms of hay fever or other upper respiratory allergies): 5 to 10 mg once daily (maximum: 10 mg/day).
Angioedema, acute allergic or recurrent idiopathic (off-label use): Note: Not indicated for angioedema with anaphylaxis; use epinephrine if anaphylaxis symptoms are present (ie, risk of airway or cardiovascular compromise is present) (Ref).
Oral: 10 mg once or twice daily; may increase up to 20 mg twice daily (Ref).
Infusion reaction, premedication (adjunct) (alternative agent) (off-label use): Note: Used in some protocols as an alternative to a sedating antihistamine (eg, diphenhydramine). An optimal premedication regimen has not been identified; refer to institutional protocols as variations exist (Ref).
Oral: 10 mg typically administered 30 to 60 minutes prior to infusion of certain chemotherapy agents or biologics; may be given with an H2 antihistamine (eg, ranitidine) and/or a glucocorticoid (Ref).
Urticaria, new onset and chronic spontaneous:
New onset:
Oral (off-label use): Initial: 10 mg once daily. If symptom control is inadequate, may immediately increase to 10 mg twice daily (Ref).
IV: 10 mg once daily as needed.
Chronic spontaneous:
Oral: Initial: 10 mg once daily. If symptom control is inadequate, may increase in increments of 10 mg/day every 1 to 4 weeks up to 20 mg twice daily. Periodically reevaluate necessity for continued treatment (Ref).
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
The renal dosing recommendations are based upon the best available evidence and clinical expertise. Senior Editorial Team: Bruce Mueller, PharmD, FCCP, FASN, FNKF; Jason A. Roberts, PhD, BPharm (Hons), B App Sc, FSHP, FISAC; Michael Heung, MD, MS.
IV: No dosage adjustment necessary (formulation only intended for short-term use).
Oral: Note: Renally adjusted dose recommendations are based on usual doses of 5 to 10 mg once daily.
Altered kidney function:
CrCl >31 mL/minute: No dosage adjustment necessary.
CrCl 11 to ≤31 mL/minute: 5 mg once daily.
CrCl ≤10 mL/minute: 5 mg once every 48 hours; may increase to 5 mg once daily based on tolerability and response for short-term use only (drug may accumulate with prolonged use at this dose (Ref)).
Hemodialysis, intermittent (thrice weekly): <10% dialyzable; 5 mg 3 times per week (Ref); may increase to 5 mg once daily based on tolerability and response for short-term use only (drug may accumulate with prolonged use at this dose (Ref)).
Peritoneal dialysis: Unlikely to be significantly dialyzed (Ref): 5 mg once every 48 hours; may increase to 5 mg once daily based on tolerability and response for short-term use only (drug may accumulate with prolonged use at this dose (Ref).
The liver dosing recommendations are based upon the best available evidence and clinical expertise. Senior Editorial Team: Matt Harris, PharmD, MHS, BCPS, FAST, FCCP; Jeong Park, PharmD, MS, BCTXP, FCCP, FAST; Arun Jesudian, MD; Sasan Sakiani, MD.
Note: Cetirizine has low CNS penetration, is minimally metabolized, and is mainly eliminated in the kidney; however, the elimination half-life is prolonged in patients with liver impairment (Ref).
Liver impairment prior to treatment initiation: Child-Turcotte-Pugh class A to C:
Oral: 5 mg once daily (Ref).
Upper respiratory allergies, urticaria: Oral: 5 mg once daily (maximum dose: 5 mg daily). The previously available prescription product recommended a maximum dose of 10 mg once daily in patients <77 years of age or 5 mg once daily in patients ≥77 years of age (Ref).
(For additional information see "Cetirizine (systemic): Pediatric drug information")
Allergic rhinitis, perennial:
Infants 6 to <12 months: Oral: 2.5 mg once daily.
Children 12 to 23 months: Oral: Initial: 2.5 mg once daily; dosage may be increased to 2.5 mg twice daily.
Allergic symptoms, hay fever:
Children 2 to 5 years: Oral: Initial: 2.5 mg once daily; dosage may be increased to 2.5 mg twice daily or 5 mg once daily; maximum daily dose: 5 mg/day.
Children ≥6 years and Adolescents: Oral: 5 to 10 mg once daily.
Anaphylaxis, adjunctive therapy: Limited data available (Ref): Note: Do not use for initial or sole treatment of anaphylaxis; H1 antihistamines are not effective for upper or lower airway obstruction or shock (Ref). If cutaneous symptoms persist, dose may be repeated in 24 hours (see Urticaria, acute dosing).
Infants ≥6 months and Children <2 years: Oral: 2.5 mg once.
Children 2 to 5 years: Oral 2.5 to 5 mg once.
Children >5 years and Adolescents: Oral: 5 to 10 mg once.
Urticaria, acute:
IV:
Infants ≥6 months to Children ≤5 years: 2.5 mg every 24 hours.
Children 6 to 11 years: 5 mg or 10 mg every 24 hours; reserve higher dose for more severe symptoms.
Children ≥12 years and Adolescents: 10 mg every 24 hours.
Oral: Limited data available (Ref):
Infants ≥6 months and Children <2 years: Oral: 2.5 mg once daily.
Children 2 to 5 years: Oral: 2.5 to 5 mg once daily.
Children >5 years and Adolescents: Oral: 5 to 10 mg once daily.
Urticaria, chronic spontaneous: Limited data available in Children >5 years and Adolescents. Note: Considered first-line therapy for management of chronic urticaria; if response inadequate after 2 to 4 weeks of therapy or symptoms intolerable, consider increasing the dose of cetirizine (as age and weight permits) as second-line treatment rather than changing therapy (Ref).
Infants 6 to <12 months: Oral: 2.5 mg once daily.
Infants ≥12 months and Children <2 years: Oral: Initial: 2.5 mg once daily; dosage may be increased to 2.5 mg twice daily.
Children 2 to 5 years: Oral: Initial: 2.5 mg once daily; dosage may be increased to 2.5 mg twice daily or 5 mg once daily; maximum daily dose: 5 mg/day.
Children 6 to 11 years: Oral: 5 mg once daily or twice daily (Ref).
Children ≥12 years and Adolescents: Oral: 10 mg once daily (Ref).
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
IV: Note: Has only been evaluated for acute indications (short-term therapy).
Infants ≥6 months and Children <6 years: Avoid use in patients with any degree of renal impairment; has not been studied.
Children ≥6 years and Adolescents: Moderate to severe impairment; end-stage renal disease on dialysis: No adjustment necessary; monitor for antihistamine side effects and adjust therapy if needed.
Oral: There are no dosage adjustments provided in the manufacturer's labeling; however, the following adjustments have been recommended (Ref):
Infants, Children, and Adolescents:
GFR ≥30 mL/minute/1.73 m2: No dosage adjustment necessary.
GFR 10 to 29 mL/minute/1.73 m2: Decrease dose by 50%.
GFR <10 mL/minute/1.73 m2: Not recommended.
Intermittent hemodialysis or peritoneal dialysis: Decrease dose by 50%.
IV: Note: Has only been evaluated for acute indications (short-term therapy).
Infants ≥6 months to Children <6 years: Avoid use with hepatic impairment; has not been studied.
Children ≥6 years and Adolescents: No dosage adjustment required; monitor for antihistamine side effects and adjust therapy if needed.
Oral: Infants ≥6 months, Children, and Adolescents: There are no dosage adjustments provided in manufacturer's labeling.
Cetirizine may cause CNS depression, including sedated state, drowsiness, and fatigue (Ref). There are rare reports of psychosis and delusion (Ref). In overdose in children, sedation is more likely to occur than with other second-generation antihistamines (Ref).
Mechanism: Dose-related; low brain uptake, binding to ~30% of H1 cerebral receptors (Ref).
Onset: May occur after 1 or 2 doses (Ref). Onset of psychosis has occurred 2 to 7 days after initiation of cetirizine (Ref).
Risk factors:
• Concurrent alcohol use (Ref)
• Older patients (Ref)
• More sedating than other second-generation antihistamines, including loratadine and fexofenadine, but less sedating than first-generation antihistamines such as diphenhydramine (Ref)
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.
>10%: Nervous system: Drowsiness (adolescents and adults: 11% to 14%; children: 2% to 4%) (table 1) , headache (children: 14%; adults: <1%)
Drug (Cetirizine [Systemic]) |
Placebo |
Population |
Dose |
Number of Patients (Cetirizine [Systemic]) |
Number of Patients (Placebo) |
---|---|---|---|---|---|
4% |
1% |
Children |
10 mg |
215 |
309 |
2% |
1% |
Children |
5 mg |
161 |
309 |
14% |
6% |
Adolescents & adults |
5 mg or 10 mg |
2,034 |
1,612 |
14% |
6% |
Adolescents & adults |
10 mg |
N/A |
N/A |
11% |
6% |
Adolescents & adults |
5 mg |
N/A |
N/A |
1% to 10%:
Cardiovascular: Cardiac failure (<2%), chest pain (<2%), edema (<2%), facial edema (<2%), flushing (<2%), hypertension (<2%), lower extremity edema (<2%), palpitations (<2%), peripheral edema (<2%), syncope (<2%), tachycardia (<2%)
Dermatologic: Acne vulgaris (<2%), alopecia (<2%), bullous rash (<2%), cutaneous nodule (<2%), dermatitis (<2%), diaphoresis (<2%), eczema (<2%), erythematous rash (<2%), furunculosis (<2%), hyperkeratosis (<2%), hypertrichosis (<2%), maculopapular rash (<2%), pallor (<2%), pruritus (<2%), seborrhea (<2%), skin photosensitivity (<2%), skin rash (<2%), urticaria (<2%), xeroderma (<2%)
Endocrine & metabolic: Decreased libido (<2%), dehydration (<2%), diabetes mellitus (<2%), heavy menstrual bleeding (<2%), hot flash (<2%), increased thirst (<2%), intermenstrual bleeding (<2%), weight gain (<2%)
Gastrointestinal: Abdominal pain (children: 4% to 6%), ageusia (<2%), anorexia (<2%), aphthous stomatitis (<2%), constipation (<2%), dental caries (<2%), diarrhea (children: 2% to 3%), dysgeusia (<2%), dyspepsia (<2%), enlargement of abdomen (<2%), eructation (<2%), flatulence (<2%), gastritis (<2%), hemorrhoids (<2%), increased appetite (<2%), melena (<2%), nausea (children: 3%), sialorrhea (<2%), stomatitis (<2%), tongue discoloration (<2%), vomiting (children: 2% to 3%), xerostomia (adolescents and adults: 5%)
Genitourinary: Cystitis (<2%), dysmenorrhea (<2%), dysuria (<2%), hematuria (<2%), leukorrhea (<2%), mastalgia (<2%), urinary frequency (<2%), urinary incontinence (<2%), urinary retention (<2%), urinary tract infection (<2%), vaginitis (<2%)
Hematologic & oncologic: Hemophthalmos (<2%), lymphadenopathy (<2%), purpuric disease (<2%), rectal hemorrhage (<2%)
Hepatic: Hepatic insufficiency (<2%)
Hypersensitivity: Angioedema (<2%), tongue edema (<2%)
Nervous system: Abnormality in thinking (<2%), agitation (<2%), altered sense of smell (<2%), amnesia (<2%), anxiety (<2%), ataxia (<2%), confusion (<2%), depersonalization (<2%), depression (<2%), dizziness (adolescents and adults: 2%), emotional lability (<2%), euphoria (<2%), fatigue (4% to 6%) (table 2) , hyperesthesia (<2%), hypertonia (<2%), hypoesthesia (<2%), impaired concentration (<2%), insomnia (≤9%), malaise (≤4%), migraine (<2%), myasthenia (<2%), nervousness (<2%), nightmares (<2%), pain (<2%), paralysis (<2%), paresthesia (<2%), rigors (<2%), sleep disorder (<2%), twitching (<2%), vertigo (<2%), voice disorder (<2%)
Drug (Cetirizine [Systemic]) |
Placebo |
Population |
Dose |
Number of Patients (Cetirizine [Systemic]) |
Number of Patients (Placebo) |
---|---|---|---|---|---|
4% |
1% |
Children |
5 mg or 10 mg |
N/A |
N/A |
6% |
3% |
Adolescents & adults |
5 mg or 10 mg |
2,034 |
1,612 |
Neuromuscular & skeletal: Arthralgia (<2%), arthritis (<2%), asthenia (<2%), back pain (<2%), hyperkinetic muscle activity (<2%), lower limb cramp (<2%), myalgia (<2%), myelitis (<2%), osteoarthrosis (<2%), tremor (<2%)
Ophthalmic: Accommodation disturbance (<2%), blepharoptosis (<2%), blindness (<2%), conjunctivitis (<2%), eye pain (<2%), glaucoma (<2%), periorbital edema (<2%), visual field defect (<2%), xerophthalmia (<2%)
Otic: Deafness (<2%), otalgia (<2%), ototoxicity (<2%), tinnitus (<2%)
Renal: Polyuria (<2%)
Respiratory: Bronchitis (<2%), bronchospasm (children: 3%), dyspnea (<2%), epistaxis (children: 4%), hyperventilation (<2%), increased bronchial secretions (<2%), nasal polyposis (<2%), pharyngitis (2% to 6%), pneumonia (<2%), respiratory system disorder (<2%), rhinitis (<2%), sinusitis (<2%), upper respiratory tract infection (<2%)
Miscellaneous: Fever (<2%)
<1%:
Cardiovascular: Presyncope
Dermatologic: Hyperhidrosis
Nervous system: Feeling hot
Frequency not defined:
Hepatic: Increased serum transaminases (transient, reversible)
Nervous system: Irritability
Miscellaneous: Fussiness in an infant or toddler
Postmarketing:
Cardiovascular: Severe hypotension
Gastrointestinal: Cholestasis (Fong 2000)
Hematologic & oncologic: Hemolytic anemia, thrombocytopenia
Hepatic: Hepatitis (Pompili 2004), increased serum bilirubin
Hypersensitivity: Anaphylaxis (Afonso 2009)
Nervous system: Aggressive behavior, delusion (Garden 2013), hallucination, psychosis (Croitoru 2021), sedated state (Corsico 2019), seizure, suicidal ideation, suicidal tendencies
Neuromuscular & skeletal: Orofacial dyskinesia (Romo 2011)
Renal: Glomerulonephritis
Hypersensitivity to cetirizine, hydroxyzine, levocetirizine, or any component of the formulation.
Canadian labeling: Additional contraindications (not in US labeling): Hypersensitivity to piperazine derivatives; severe renal impairment (CrCl <10 mL/minute).
Concerns related to adverse effects:
• Pruritus: Rebound pruritus has been reported within several days after stopping cetirizine, usually after long-term (eg, months to years) use.
Disease-related concerns:
• Hepatic impairment: Use with caution; consider dosage adjustment.
• Renal impairment: Use with caution; consider dosage adjustment.
Concurrent drug therapy issues:
• Sedatives: Effects may be potentiated when used with other sedative drugs or ethanol.
Special populations:
• Older adult: Use with caution in older adults; may be more sensitive to adverse effects.
Safety and efficacy for the use of cough and cold products in pediatric patients <4 years of age is limited; the AAP warns against the use of these products for respiratory illnesses in young children. Serious adverse effects including death have been reported. Many of these products contain multiple active ingredients, increasing the risk of accidental overdose when used with other products. The FDA does not recommend OTC uses for these products in pediatric patients <2 years of age and recommends to use with caution in pediatric patients ≥2 years of age. Health care providers are reminded to ask caregivers about the use of OTC cough and cold products in order to avoid exposure to multiple medications containing the same ingredient (AAP 2018; CDC 2007; FDA 2017; FDA 2018).
Some dosage forms may contain propylene glycol; in neonates, large amounts of propylene glycol delivered orally, intravenously (eg, >3,000 mg/day), or topically have been associated with potentially fatal toxicities which can include metabolic acidosis, seizures, renal failure, and CNS depression; toxicities have also been reported in children and adults including hyperosmolality, lactic acidosis, seizures, and respiratory depression; use caution (AAP 1997; Shehab 2009).
Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Capsule, Oral, as hydrochloride:
Allergy Relief (Cetirizine): 10 mg [DSC]
ZyrTEC Allergy: 10 mg
Solution, Intravenous, as hydrochloride [preservative free]:
Quzyttir: 10 mg/mL (1 mL)
Solution, Oral, as hydrochloride:
Allergy Relief Childrens: 5 mg/5 mL (118 mL) [dye free, sugar free; contains propylene glycol, sodium benzoate; grape flavor]
Cetirizine HCl Allergy Child: 5 mg/5 mL (120 mL) [alcohol free, dye free, gluten free, sugar free; contains methylparaben, propylene glycol, propylparaben; grape flavor]
Cetirizine HCl Allergy Child: 5 mg/5 mL (120 mL [DSC]) [alcohol free, sugar free; contains methylparaben, propylene glycol, propylparaben; grape flavor]
Cetirizine HCl Allergy Child: 5 mg/5 mL (118 mL) [dye free, gluten free, sugar free; contains propylene glycol, sodium benzoate; grape flavor]
Cetirizine HCl Childrens Alrgy: 5 mg/5 mL (120 mL [DSC]) [contains methylparaben, propylene glycol, propylparaben]
Cetirizine HCl Childrens Alrgy: 5 mg/5 mL (118 mL) [dye free; contains methylparaben, propylene glycol, propylparaben; grape flavor]
Cetirizine HCl Childrens Alrgy: 5 mg/5 mL (118 mL) [dye free, sugar free; contains propylene glycol, sodium benzoate; grape flavor]
FT All Day Allergy Childrens: 5 mg/5 mL (120 mL) [dye free, sugar free; contains methylparaben, propylene glycol, propylparaben; grape flavor]
FT Allergy Relief Childrens: 5 mg/5 mL (120 mL) [dye free, sugar free; contains propylene glycol, sodium benzoate; bubble-gum flavor]
GoodSense All Day Allergy: 5 mg/5 mL (118 mL) [dye free, gluten free, sugar free; contains propylene glycol, sodium benzoate; grape flavor]
GoodSense All Day Allergy: 5 mg/5 mL (118 mL) [dye free, gluten free, sugar free; contains propylene glycol, sodium benzoate, sorbitol]
ZyrTEC Childrens Allergy: 5 mg/5 mL (118 mL) [dye free, sugar free; contains propylene glycol, sodium benzoate]
ZyrTEC Childrens Allergy: 5 mg/5 mL (30 mL, 118 mL, 236 mL) [dye free, sugar free; contains propylene glycol, sodium benzoate; grape flavor]
Generic: 5 mg/5 mL (120 mL, 240 mL, 473 mL, 480 mL)
Tablet, Oral, as hydrochloride:
Allergy (Cetirizine): 10 mg [scored]
Allergy Relief (Cetirizine): 10 mg
Allergy Relief (Cetirizine): 10 mg [scored]
Allergy Relief Cetirizine: 5 mg [contains corn starch]
Allergy Relief Cetirizine: 10 mg
Allergy Relief Cetirizine: 10 mg [contains corn starch]
FT All Day Allergy: 10 mg
FT All Day Allergy: 10 mg [gluten free]
FT All Day Allergy 24 Hour: 10 mg
FT Allergy Relief Cetirizine: 10 mg [contains corn starch]
GoodSense All Day Allergy: 10 mg [gluten free; contains corn starch, fd&c blue #1 (brill blue) aluminum lake]
ZyrTEC Allergy: 10 mg
Generic: 5 mg, 10 mg
Tablet Chewable, Oral:
ZyrTEC Childrens Allergy: 2.5 mg [dye free; contains corn starch; grape flavor]
Tablet Chewable, Oral, as hydrochloride:
Cetirizine HCl Childrens: 5 mg [DSC], 10 mg [DSC] [contains aspartame, fd&c yellow #6(sunset yellow)alumin lake]
ZyrTEC: 10 mg [dye free; contains corn starch]
ZyrTEC Childrens Allergy: 10 mg [dye free; contains corn starch; grape flavor]
Generic: 5 mg, 10 mg
Tablet Disintegrating, Oral, as hydrochloride:
ZyrTEC Allergy: 10 mg [DSC]
ZyrTEC Allergy Childrens: 10 mg
ZyrTEC Allergy Childrens: 10 mg [citrus flavor]
May be product dependent
Capsules (ZyrTEC Allergy Oral)
10 mg (per each): $0.57
Chewable (Cetirizine HCl Oral)
5 mg (per each): $2.47
10 mg (per each): $2.47 - $5.36
Chewable (ZyrTEC Childrens Allergy Oral)
2.5 mg (per each): $0.98
10 mg (per each): $0.54
Chewable (ZyrTEC Oral)
10 mg (per each): $0.85
Solution (Cetirizine HCl Oral)
5 mg/5 mL (per mL): $0.85
Solution (Quzyttir Intravenous)
10 mg/mL (per mL): $428.86
Solution (ZyrTEC Childrens Allergy Oral)
1 mg/mL (per mL): $0.10
5 mg/5 mL (per mL): $0.10
Tablet, orally-disintegrating (ZyrTEC Allergy Childrens Oral)
10 mg (per each): $1.00
Tablets (Cetirizine HCl Oral)
5 mg (per each): $2.49
10 mg (per each): $0.05 - $2.50
Tablets (ZyrTEC Allergy Oral)
10 mg (per each): $1.06
Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet, Oral, as hydrochloride:
Reactine: 20 mg
Generic: 20 mg
Oral: May be administered with or without food.
Chewable tablet: Chew tablet before swallowing; may be taken with or without water.
IV: Injection: For IV use only; do not administer IM or SUBQ; administer as an IV push over 1 to 2 minutes.
Oral: Administer without regard to food.
Chewable tablet: Chew tablet before swallowing; may be taken with or without water.
Dissolving tablet: Allow tablet to melt in mouth; may be taken with or without water.
Liquid: Administer with an accurate measuring device; do not use a household teaspoon (overdosage may occur).
Parenteral: IV: Administer IV undiluted over 1 to 2 minutes; do not administer IM or SubQ.
Oral:
Allergic rhinitis: Relief of symptoms associated with allergic rhinitis.
Urticaria, chronic spontaneous: Treatment of uncomplicated skin manifestations of chronic spontaneous urticaria.
Injection:
Urticaria, new onset: Treatment of new-onset (acute) urticaria.
Anaphylaxis (adjunct to epinephrine for relief of cutaneous symptoms); Angioedema, acute allergic or recurrent idiopathic; Infusion reaction, premedication
Cetirizine may be confused with sertraline, stavudine
Quzyttir may be confused with Qsymia
ZyrTEC may be confused with Lipitor, Serax, Xanax, Zantac, Zerit, Zocor, ZyPREXA, ZyrTEC-D
The Institute for Safe Medication Practices (ISMP) includes this medication among its list of drugs (pediatric liquid medications requiring measurement) which have a heightened risk of causing significant patient harm when used in error (High-Alert Medications in Community/Ambulatory Care Settings).
Benadryl brand name for cetirizine [Great Britain, Philippines], but also the brand name for acrivastine and pseudoephedrine [Great Britain] and several products containing diphenhydramine [US, Canada]
Procet [Bangladesh] may be confused with Percocet brand name for oxycodone/acetaminophen [US, Israel, Puerto Rico]
Procet brand name for cetirizine [Bangladesh], but also brand name for acetaminophen [Kenya]
Substrate of CYP3A4 (Minor), P-glycoprotein (Minor); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential;
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the drug interactions program by clicking on the “Launch drug interactions program” link above.
Amezinium: Antihistamines may increase stimulatory effects of Amezinium. Risk C: Monitor
Benzylpenicilloyl Polylysine: Coadministration of Antihistamines and Benzylpenicilloyl Polylysine may alter diagnostic results. Management: Suspend systemic H1 antagonists for benzylpenicilloyl-polylysine skin testing and delay testing until systemic antihistaminic effects have dissipated. A histamine skin test may be used to assess persistent antihistaminic effects. Risk D: Consider Therapy Modification
Betahistine: Antihistamines may decrease therapeutic effects of Betahistine. Betahistine may decrease therapeutic effects of Antihistamines. Risk C: Monitor
Certoparin: Antihistamines may increase therapeutic effects of Certoparin. Risk C: Monitor
CNS Depressants: Cetirizine (Systemic) may increase CNS depressant effects of CNS Depressants. Management: Consider avoiding this combination if possible. If required, monitor for excessive sedation or CNS depression, limit the dose and duration of combination therapy, and consider CNS depressant dose reductions. Risk D: Consider Therapy Modification
Gabapentin: Cetirizine (Systemic) may increase CNS depressant effects of Gabapentin. Cetirizine (Systemic) may decrease serum concentration of Gabapentin. Risk C: Monitor
Hyaluronidase: Antihistamines may decrease therapeutic effects of Hyaluronidase. Risk C: Monitor
Pilsicainide: May increase serum concentration of Cetirizine (Systemic). Cetirizine (Systemic) may increase serum concentration of Pilsicainide. Risk C: Monitor
Pitolisant: Antihistamines may decrease therapeutic effects of Pitolisant. Risk X: Avoid
Cetirizine's absorption and maximal concentration are reduced when taken with food. Management: May be taken without regard to meals.
Outcome data following maternal use of cetirizine during pregnancy are available (Etwel 2017, Gilboa 2014, Golembesky 2018, Hansen 2020, Kocatürk 2022). Based on the limitations of available data, second-generation antihistamines are considered acceptable for use during pregnancy, with preference given to agents with more study (EAACI [Zuberbier 2022]).
Algorithms are available for the treatment of acute rhinitis and urticaria. When treatment with a second-generation oral antihistamine is recommended, cetirizine is one of the preferred agents for use during pregnancy. When treating urticaria, doses greater than the standard dose have not been adequately studied in pregnant patients (AAAAI/ACAAI [Dykewicz 2020], EAACI [Zuberbier 2022]).
Cetirizine is present in breast milk.
Data related to the presence of cetirizine in breast milk are available from three lactating patients, 5 to 6 months postpartum, taking cetirizine 10 mg daily for >6 months prior to the study. Breast milk was sampled prior to and at intervals for 24 hours after the dose. The maximum cetirizine concentration in breast milk (49 ng/mL) occurred 2 hours after the maternal dose. Using average breast milk concentrations and average maternal weight, authors of the study calculated the estimated daily infant dose of cetirizine via breast milk to be 3.1 mcg/kg/day providing a relative infant dose (RID) of 1.77% compared to the weight adjusted maternal dose (Wilkerson 2021). In general, breastfeeding is considered acceptable when the RID of a medication is <10% (Anderson 2016; Ito 2000). Additional data are available from a study evaluating a method of analyzing breast milk for the presence of cetirizine. As part of the study, breast milk was collected from 219 lactating patients taking cetirizine 5 to 20 mg/day and 9 patients taking levocetirizine 5 mg/day. All patients in the study were at steady state. Cetirizine/levocetirizine breast milk concentration ranged from 0.65 to 65 ng/mL among 228 samples; 24 samples were below the limits of quantification (Wegler 2022). Adverse events were not observed in three breastfed infants following chronic maternal use of cetirizine 10 mg daily (Wilkerson 2021). Drowsiness and irritability have been reported in breastfed infants exposed to antihistamines (Ito 1993). In general, second-generation antihistamines (eg, cetirizine) are less sedating as compared to their first-generation counterparts. Infants exposed to a second-generation antihistamine via breast milk, should be monitored for irritability, jitteriness, or drowsiness (Butler 2014).
Antihistamines may decrease maternal serum prolactin concentrations when administered prior to the establishment of breastfeeding (Messinis 1985).
According to the manufacturer, the decision to breastfeed during therapy should consider the risk of infant exposure, the benefits of breastfeeding to the infant, and the benefits of treatment to the mother. Use of a second-generation antihistamine is preferred when an oral antihistamine is needed in lactating patients (Butler 2014, EAACI [Zuberbier 2022]).
Relief of symptoms, sedation, mental alertness, and anticholinergic effects.
Competes with histamine for H1-receptor sites on effector cells in the gastrointestinal tract, blood vessels, and respiratory tract
Onset of action: Suppression of skin wheal and flare: Oral: 20 to 60 minutes.
Duration of action: Suppression of skin wheal and flare: Oral: ≥24 hours.
Absorption: Rapid.
Distribution: Children: 0.7 L/kg; Adults: 0.56 L/kg (Simons 1999).
Protein binding, plasma: Mean: 93%.
Metabolism: Limited hepatic.
Half-life elimination: Children: 6.2 hours; Adults: 8 hours.
Time to peak, serum: Oral: 1 hour; IV: 108 seconds.
Excretion: Urine (70%; 50% as unchanged drug); feces (10%).