In adults and children 6 year and above:

- Cetirizine is indicated for the relief of nasal and ocular symptoms of seasonal and perennial allergic rhinitis.

- Cetirizine is indicated for the relief of symptoms of chronic idiopathic urticaria.

Children aged from 6 to 12 years:

5 mg twice daily (a half tablet twice daily).

Adults and adolescents over 12 years of age:

10 mg once daily (1 tablet).

The tablets need to be swallowed with a glass of liquid.

Elderly subjects: data do not suggest that the dose needs to be reduced in elderly subjects provided that the renal function is normal.

Patients with moderate to severe renal impairment: there are no data to document the efficacy/safety ratio in patients with renal impairement. Since cetirizine is mainly excreted via renal route (see section 5.2), in cases no alternative treatment can be used, the dosing intervals must be individualized according to renal function. Refer to the following table and adjust the dose as indicated. To use this dosing table, an estimate of the patient's creatinine clearance (CL_cr) in mL/min is needed. The CL_cr (mL/min) may be estimated from serum creatinine (mg/dl) determination using the following formula:

Dosing adjustments for adult patients with impaired renal function

Group	Creatinine clearance (mL/min)	Dosage and frequency
Normal	≥80	10 mg once daily
Mild	50 – 79	10 mg once daily
Moderate	30 – 49	5 mg once daily
Severe	<30	5 mg once every 2 days
End-stage renal disease - Patients undergoing dialysis	<10	Contra-indicated

In pediatric patients suffering from renal impairment, the dose will have to be adjusted on an individual basis taking into account the renal clearance of the patient, his age and his body weight.

Patients with hepatic impairment: no dose adjustment is needed in patients with solely hepatic impairment.

Patients with hepatic impairment and renal impairment: dose adjustment is recommended (see Patients with moderate to severe renal impairment above).

Hypersensitivity to the active substance, to any of the excipients, to hydroxyzine or to any piperazine derivatives. Patients with severe renal impairment at less than 10 mL/min creatinine clearance. Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose- galactose malabsorption should not take cetirizine film-coated tablet.

At therapeutic doses, no clinically significant interactions have been demonstrated with

alcohol (for a blood alcohol level of 0.5 g/L). Nevertheless, precaution is recommended if

alcohol is taken concomitantly.

Caution in epileptic patients and patients at risk of convulsions is recommended.

The use of the film-coated tablet formulation is not recommended in children aged less than

6 years since this formulation does not allow for appropriate dose adaptation.

Allergy skin tests are inhibited by antihistamines and a wash-out period (of 3 days) is

required before performing them.

Caution should be taken in patients with predisposition factors of urinary retention (e.g. spinal 
cord lesion, prostatic hyperplasia) as cetirizine may increase the risk of urinary retention.

 

Due to the pharmacokinetic, pharmacodynamic and tolerance profile of cetirizine, no interactions are expected with this antihistamine. Actually, neither pharmacodynamic nor significant pharmacokinetic interaction was reported in drug-drug interactions studies performed, notably with pseudoephedrine or theophylline (400 mg/day). The extent of absorption of cetirizine is not reduced with food, although the rate of absorption is decreased.

 

Pregnancy

Pregnancy Category B

For cetirizine very rare clinical data on exposed pregnancies are available. Animal studies

do not indicate direct or indirect harmful effects with respect to pregnancy, embryonal/fetal

development, parturition or postnatal development. Caution should be exercised when

prescribing to pregnant women.

Lactation

Cetirizine is excreted in human milk at concentrations representing 0.25 to 0.90 those

measured in plasma, depending on sampling time after administration. Therefore, caution

should be exercised when prescribing cetirizine to lactating women.

Objective measurements of driving ability, sleep latency and assembly line performance have

not demonstrated any clinically relevant effects at the recommended dose of 10 mg.

Patients intending to drive, engaging in potentially hazardous activities or operating

machinery should not exceed the recommended dose and should take their response to the

medicinal product into account.

In sensitive patients, concurrent use with alcohol or other CNS depressants may cause

additional reductions in alertness and impairment of performance.

		Clinical studies have shown that cetirizine at the recommended dosage has minor undesirable effects on the CNS, including somnolence, fatigue, dizziness and headache. In some cases, paradoxical CNS stimulation has been reported. Although cetirizine is a selective antagonist of peripheral H1-receptors and is relatively free of anticholinergic activity, isolated cases of micturition difficulty, eye accommodation disorders and dry mouth have been reported. Instances of abnormal hepatic function with elevated hepatic enzymes accompanied by elevated bilirubin have been reported. Mostly this resolves upon discontinuation of the treatment with cetirizine dihydrochloride. Clinical trials Double blind controlled clinical trials comparing cetirizine to placebo or other antihistamines at the recommended dosage (10 mg daily for cetirizine), of which quantified safety data are available, included more than 3200 subjects exposed to cetirizine. From this pooling, the following adverse reactions were reported for cetirizine 10 mg in the placebo-controlled trials at rates of 1.0 % or greater: Adverse reactions (WHO-ART) Cetirizine 10 mg (n= 3260) Placebo (n = 3061) Body as a whole – general disorders Fatigue   1.63 %   0.95 % Central and peripheral nervous system disorders Dizziness Headache   1.10 % 7.42 %   0.98 % 8.07 % Gastro-intestinal system disorders Abdominal pain Dry mouth Nausea     0.98 % 2.09 % 1.07 %     1.08 % 0.82 % 1.14 % Psychiatric disorders Somnolence   9.63 %   5.00 % Respiratory system disorders Pharyngitis   1.29 %   1.34 % Although statistically more common than under placebo, somnolence was mild to moderate in the majority of cases. Objective tests as demonstrated by other studies have demonstrated that usual daily activities are unaffected at the recommended daily dose in healthy young volunteers. Adverse reactions at rates of 1 % or greater in children aged from 6 months to 12 years, included in placebo-controlled clinical trials are: Adverse reactions (WHO-ART) Cetirizine (n=1656) Placebo (n =1294) Gastro-intestinal system disorders Diarrhea   1.0 %   0.6 % Psychiatric disorders Somnolence   1.8 %   1.4 % Respiratory system disorders Rhinitis   1.4 %   1.1 % Body as a whole – general disorders Fatigue   1.0 %   0.3 % Post-marketing experience In addition to the adverse reactions reported during clinical studies and listed above, the following undesirable effects have been reported in post-marketing experience. Undesirable effects are described according to MedDRA System Organ Class and by estimated frequency based on post-marketing experience. Frequencies are defined as follows: Very common (≥1/10); common (≥1/100 to <1/10); uncommon (≥1/1,000 to <1/100); rare (≥1/10,000 to <1/1,000); very rare (<1/10,000), not known (cannot be estimated from the available data) Blood and lymphatic disorders: Very rare: thrombocytopenia Immune system disorders: Rare: hypersensitivity Very rare: anaphylactic shock Psychiatric disorders: Uncommon: agitation Rare: aggression, confusion, depression, hallucination, insomnia Very rare: Not known: Tics suicidal ideation Nervous system disorders: Uncommon: paraesthesia Rare: convulsions Very rare: dysgeusia, syncope, tremor, dystonia, dyskinesia Not known: amnesia, memory impairment Eye disorders: Very rare: accommodation disorder, blurred vision, oculogyration Cardiac disorders: Rare: tachycardia Gastro-intestinal disorders: Uncommon: diarrhea Hepatobiliary disorders: Rare: hepatic function abnormal (increased transaminases, alkaline phosphatase, γ-GT and bilirubin)
	Skin and subcutaneous tissue disorders:
	Uncommon:		pruritus, rash
	Rare:		urticaria
	Very rare:		angioneurotic edema, fixed drug eruption
	Renal and urinary disorders:
	Very rare: Not known:		dysuria, enuresis urinary retention.
	General disorders and administration site conditions:
	Uncommon:		asthenia, malaise
	Rare: edema  Ear and labyrinth disorders: Not known:     Vertigo Metabolism and nutrition disorders:  Not known: increased appetite
	Investigations:
	Rare:		weight increased

 

 

 

To report any side effect (s):

 • Saudi Arabia:

The National Pharmacovigilance and Drug Safety Center (NPC)

SFDA Call Center :19999

E-mail: npc.drug@sfda.gov.sa

Website: https://ade.sfda.gov.sa

• Other GCC States:

Please contact the relevant competent authority.

Symptoms

Symptoms observed after an overdose of cetirizine are mainly associated with CNS effects or

with effects that could suggest an anticholinergic effect.

Adverse events reported after an intake of at least 5 times the recommended daily dose are:

confusion, diarrhea, dizziness, fatigue, headache, malaise, mydriasis, pruritus, restlessness,

sedation, somnolence, stupor, tachycardia, tremor, and urinary retention.

Management

There is no known specific antidote to cetirizine.

Should overdose occur, symptomatic or supportive treatment is recommended. Gastric

lavage should be considered following ingestion of a short occurrence.

Cetirizine is not effectively removed by dialysis.

Pharmacotherapeutic group: Piperazine derivatives, ATC code: R06A E07

Cetirizine, a human metabolite of hydroxyzine, is a potent and selective antagonist of

peripheral H₁-receptors. In vitro receptor binding studies have shown no measurable affinity

for other than H1-receptors.

In addition to its anti-H₁ effect, cetirizine was shown to display anti-allergic activities: at a

dose of 10 mg once or twice daily, it inhibits the late phase recruitment of eosinophils, in the

skin and conjunctiva of atopic subjects submitted to allergen challenge.

Studies in healthy volunteers show that cetirizine, at doses of 5 and 10 mg strongly inhibits

the wheal and flare reactions induced by very high concentrations of histamine into the skin,

but the correlation with efficacy is not established.

In a 35-day study in children aged 5 to 12, no tolerance to the antihistaminic effect

(suppression of wheal and flare) of cetirizine was found. When a treatment with cetirizine is

stopped after repeated administration, the skin recovers its normal reactivity to histamine

within 3 days.

In a six-week, placebo-controlled study of 186 patients with allergic rhinitis and

concomitant mild to moderate asthma, cetirizine 10 mg once daily improved rhinitis

symptoms and did not alter pulmonary function. This study supports the safety of

administering cetirizine to allergic patients with mild to moderate asthma.

In a placebo-controlled study, cetirizine given at the high daily dose of 60 mg for seven days

did not cause statistically significant prolongation of QT interval.

At the recommended dosage, cetirizine has demonstrated that it improves the quality of life

of patients with perennial and seasonal allergic rhinitis.

The steady - state peak plasma concentrations is approximately 300 ng/mL and is achieved

within 1.0 ± 0.5 h. No accumulation is observed for cetirizine following daily doses of 10

mg for 10 days. The distribution of pharmacokinetic parameters such as peak plasma

concentration (C_max) and area under curve (AUC), is unimodal in human volunteers.

The extent of absorption of cetirizine is not reduced with food, although the rate of

absorption is decreased. The extent of bioavailability is similar when cetirizine is given as

solutions, capsules or tablets.

The apparent volume of distribution is 0.50 l/kg. Plasma protein binding of cetirizine is 93 ±

0.3 %. Cetirizine does not modify the protein binding of warfarin.

Cetirizine does not undergo extensive first pass metabolism. About two third of the dose are

excreted unchanged in urine. The terminal half-life is approximately 10 hours.

Cetirizine exhibits linear kinetics over the range of 5 to 60 mg.

Special populations

Elderly: Following a single 10 mg oral dose, half-life increased by about 50 % and clearance

decreased by 40 % in 16 elderly subjects compared to the normal subjects. The decrease in

cetirizine clearance in these elderly volunteers appeared to be related to their decreased

renal function.

Children, infants and toddlers: The half-life of cetirizine was about 6 hours in children of 6-

12 years and 5 hours in children 2-6 years. In infants and toddlers aged 6 to 24 months, it is

reduced to 3.1 hours

Renally impaired patients: The pharmacokinetics of the drug were similar in patients with

mild impairment (creatinine clearance higher than 40 mL/min) and healthy volunteers.

Patients with moderate renal impairment had a 3-fold increase in half-life and 70 % decrease

in clearance compared to healthy volunteers.

Patients on hemodialysis (creatinine clearance less than 7 mL/min) given a single oral 10

mg dose of cetirizine had a 3-fold increase in half-life and a 70 % decrease in clearance

compared to normals. Cetirizine was poorly cleared by haemodialysis. Dosing adjustment is

necessary in patients with moderate or severe renal impairment (see section 4.2).

Hepatically impaired patients: Patients with chronic liver diseases (hepatocellular,

cholestatic, and biliary cirrhosis) given 10 or 20 mg of cetirizine as a single dose had a 50 %

increase in half-life along with a 40 % decrease in clearance compared to healthy subjects.

Dosing adjustment is only necessary in hepatically impaired patients if concomitant renal

impairment is present.

Non-clinical data reveal no special hazard for humans based on conventional studies of

safety pharmacology, repeated dose toxicity, genotoxicity, carcinogenic potential, toxicity to

reproduction.

- Microcrystalline cellulose

- Lactose monohydrate

- Povidone 

- Crospovidone

- Colloidal Silicon dioxide

- Magnesium stearate

- Opadry

- Simethicone Emulsion

 

Not applicable.

36 months

Store below 30 °C

Artiz Tablets – 10 tablets: One Aluminum-PVC/PVDC blisters of 10 Tablets each, packed

in a printed carton with folded leaflet

Artiz Tablets – 30 tablets: Three Aluminum-PVC/PVDC blisters of 10 Tablets each, packed

in a printed carton with folded leaflet

No special requirements.