Applicant/PHRC: Hetero Drugs South Africa (Pty) Ltd  
Product proprietary name: Cetorin Oral Solution 2,5 mg/ 5 mL  
Dosage form and strength: Oral solution, Each 5 mL contains 2,5 mg Levocetirizine dihydrochloride  
PROFESSIONAL INFORMATION for CETORIN ORAL SOLUTION 2,5 mg/ 5 mL  
SCHEDULING STATUS  
S1  
1 NAME OF THE MEDICINE  
CETORIN Oral Solution 2,5 mg/ 5 mL  
2 QUALITATIVE AND QUANTITATIVE COMPOSITION  
Each 5 mL contains 2,5 mg of Levocetirizine dihydrochloride  
Contains sugar  
Each 5 mL contains 10 mg of saccharin sodium and 2000 mg maltitol solution  
‘for full list of excipients, see section 6.1’  
3 PHARMACEUTICAL FORM  
Oral solution  
Clear, colorless liquid, with a grape flavour  
4 CLINICAL PARTICULARS  
4.1 Therapeutic indications  
CETORIN Oral Solution is indicated for the relief of symptoms associated with the following allergic  
conditions:  
•
•
•
seasonal allergic rhinitis  
perennial allergic rhinitis  
chronic idiopathic urticaria.  
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Applicant/PHRC: Hetero Drugs South Africa (Pty) Ltd  
Product proprietary name: Cetorin Oral Solution 2,5 mg/ 5 mL  
Dosage form and strength: Oral solution, Each 5 mL contains 2,5 mg Levocetirizine dihydrochloride  
4.2 Posology and method of administration  
Posology  
Adults and adolescents 12 years of age and older:  
The daily recommended dose is 5 mg (10 mL) once daily.  
Special populations  
Elderly  
Adjustment of the dose is recommended in elderly patients with moderate to severe renal impairment (see  
patients with renal impairment below).  
Adults with renal impairment:  
The dosing interval must be individualised 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  
(Clcr) in ml/min is needed. The Clcr (ml/min) may be estimated from serum creatinine (μmol/l) determination  
using the following formula:  
CL  
cr  
=
(140 – age) x body weight in kg  
(0,85 for women)  
serum creatinine (μmol/l)  
Dosing adjustments for patients with impaired renal function:  
Group  
Creatinine clearance (ml/min)  
Dosage and frequency  
5 mg once daily  
Normal  
Mild  
≥ 80  
50-79  
30-49  
<30  
5 mg once daily  
Moderate  
Severe  
End-stage  
5 mg once every 2 days  
5 mg once every 3 days  
Contraindicated  
renal  
disease  
–
<10  
Patients undergoing dialysis  
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Applicant/PHRC: Hetero Drugs South Africa (Pty) Ltd  
Product proprietary name: Cetorin Oral Solution 2,5 mg/ 5 mL  
Dosage form and strength: Oral solution, Each 5 mL contains 2,5 mg Levocetirizine dihydrochloride  
In paediatric 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 and his/her body weight. There are no specific data for children with renal impairment.  
Patients with hepatic impairment  
No dose adjustment is needed in patients with solely hepatic impairment. In patients with hepatic  
impairment and renal impairment, adjustment of the dose is recommended (see Patients with renal  
impairment above).  
Paediatric population  
Children aged less than 2 years  
The administration of CETORIN Oral Solution to infants and toddlers aged less than 2 years is not  
recommended (see section 4.4).  
Children aged 2 to 6 years  
The daily recommended dose is 2,5 mg to be administered in 2 intakes of 1,25 mg (2,5 mL of solution twice  
daily).  
Children aged 6 to 12 years  
The daily recommended dose is 5 mg (10 mL) once daily.  
Duration of use  
Intermittent allergic rhinitis (symptoms < 4 days/week or during less than 4 weeks) has to be treated  
according to the disease and its history; it can be stopped once the symptoms have disappeared and can  
be restarted again when symptoms reappear. In case of persistent allergic rhinitis (symptoms > 4 days/week  
or during more than 4 weeks), continuous therapy can be proposed to the patient during the period of  
exposure to allergens. Clinical experience with CETORIN Oral Solution is currently available for a 6-month  
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Applicant/PHRC: Hetero Drugs South Africa (Pty) Ltd  
Product proprietary name: Cetorin Oral Solution 2,5 mg/ 5 mL  
Dosage form and strength: Oral solution, Each 5 mL contains 2,5 mg Levocetirizine dihydrochloride  
treatment period.  
Method of administration  
For oral administration  
4.3 Contraindications  
CETORIN Oral Solution is contraindicated in  
•
hypersensitivity to the levocetirizine, to any piperazine derivative or to any of the excipients of  
CETORIN Oral Solution (see section 4.4)  
•
•
•
infants and toddlers aged less than 2 years, as safety and efficacy have not been demonstrated  
during breastfeeding of infants and while pregnant (see section 4.6) and lactation  
patients with end-stage renal disease, at less than 10 mL/min creatinine clearance.  
4.4 Special warnings and precautions for use  
Alcohol  
Precaution is recommended with intake of alcohol. CETORIN Oral Solution lacks significant sedative  
effects. Patients should, however be warned that a small number of individuals may experience sedation.  
This effect may be compounded by the simultaneous intake of alcohol or other central nervous system  
depressants (see section 4.5).  
Risk of urinary retention  
Caution should be exercised in patients with predisposing factors of urinary retention (e.g. spinal cord  
lesion, prostatic hyperplasia) as levocetirizine, contained in CETORIN Oral Solution, may increase the risk  
of urinary retention.  
Risk of convulsion  
Caution should be taken in patients with epilepsy and patients at risk of convulsion as CETORIN Oral  
Solution may cause seizure aggravation.  
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Applicant/PHRC: Hetero Drugs South Africa (Pty) Ltd  
Product proprietary name: Cetorin Oral Solution 2,5 mg/ 5 mL  
Dosage form and strength: Oral solution, Each 5 mL contains 2,5 mg Levocetirizine dihydrochloride  
Skin reactions  
Pruritus may occur when levocetirizine, as in CETORIN Oral Solution, is stopped even if those symptoms  
were not present before treatment initiation.  
The symptoms may resolve spontaneously. In some cases, the symptoms may be intense and may require  
treatment to be restarted. The symptoms should resolve when the treatment is restarted.  
Allergic skin tests  
Response to allergy skin tests are inhibited by antihistamines and a wash-out period (of 3 days) is required  
before performing them.  
Information on excipients  
CETORIN Oral Solution contains maltitol and may have a laxative effect. Patients with rare hereditary  
problems of fructose intolerance should not take CETORIN Oral Solution.  
Paediatric population  
Infants and children under 2 years  
The administration of CETORIN Oral Solution to infants and toddlers aged less than 2 years is not  
recommended due to the lack of sufficient data in this age group (see sections 4.2 and 4.3).  
4.5 Interaction with other medicines and other forms of interaction  
No interaction studies have been performed with levocetirizine (including no studies with CYP3A4  
inducers). Studies with the racemate compound cetirizine demonstrated that there were no clinically  
relevant adverse interactions (with antipyrine, ketoconazole, erythromycin, azithromycin, cimetidine,  
pseudoephedrine, glipizide and diazepam).  
Theophylline  
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Applicant/PHRC: Hetero Drugs South Africa (Pty) Ltd  
Product proprietary name: Cetorin Oral Solution 2,5 mg/ 5 mL  
Dosage form and strength: Oral solution, Each 5 mL contains 2,5 mg Levocetirizine dihydrochloride  
A decrease in the clearance of cetirizine (16 %) was observed in a multiple dose study with theophylline  
(400 mg once a day); while the disposition of theophylline was not altered by concomitant cetirizine  
administration.  
Ritonavir:  
In a multiple dose study of ritonavir (600 mg twice daily) and cetirizine (10 mg daily), the extent of exposure  
to cetirizine was increased by about 40 % while the disposition of ritonavir was decreased (-11 %).  
Food:  
The extent of absorption of CETORIN Oral Solution is not reduced with food, although the rate of absorption  
is decreased.  
Alcohol:  
In sensitive patients the simultaneous administration of CETORIN Oral Solution and alcohol or other central  
nervous system (CNS) depressants may have effects on the central nervous system. It is advisable to avoid  
excessive alcohol consumption (see section 4.4).  
4.6 Fertility, pregnancy and lactation  
Pregnancy  
CETORIN Oral Solution is contraindicated in pregnancy as safety has not been demonstrated (see section  
4.3 and 5.3).  
Breastfeeding  
CETORIN Oral Solution is contraindicated in women who are breastfeeding their babies, since the active  
ingredient is excreted in breast milk.  
Fertility  
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Applicant/PHRC: Hetero Drugs South Africa (Pty) Ltd  
Product proprietary name: Cetorin Oral Solution 2,5 mg/ 5 mL  
Dosage form and strength: Oral solution, Each 5 mL contains 2,5 mg Levocetirizine dihydrochloride  
No clinical data relating to levocetirizine effects on fertility is available.  
4.7 Effects on ability to drive and use machines  
CETORIN Oral Solution lacks significant sedative effects. Nevertheless, some patients could experience  
somnolence, fatigue, and asthenia under therapy with CETORIN Oral Solution. Therefore, patients  
intending to drive, engage in potentially hazardous activities or operate machinery should take their  
response to the CETORIN Oral Solution into account.  
4.8 Undesirable effects  
a) Summary of the safety profile  
Mild to moderate side effects most frequently experienced in adults include, headache, somnolence, dry  
mouth, fatigue, with asthenia or abdominal pain occurring less frequently.  
Tabulated list of adverse reactions  
System Organ Class  
Frequency  
Side effects  
Angioedema,  
anaphylaxis  
Immune system disorders Frequency unknown  
hypersensitivity  
including  
Metabolism and nutrition Frequency unknown  
Increased weight, increased appetite  
disorders  
Psychiatric disorders  
Frequency unknown  
Aggression,  
depression,  
nightmare  
agitation,  
insomnia,  
hallucination,  
suicidal  
ideation,  
Nervous  
system Frequent  
Somnolence, headache  
disorders  
Frequency unknown  
Convulsion,  
paraesthesia,  
dizziness,  
syncope, tremor, dysgeusia  
Visual disturbances, blurred vision  
Vertigo  
Eye disorders  
Frequency unknown  
Ear  
and  
labyrinth Frequency unknown  
disorders  
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Applicant/PHRC: Hetero Drugs South Africa (Pty) Ltd  
Product proprietary name: Cetorin Oral Solution 2,5 mg/ 5 mL  
Dosage form and strength: Oral solution, Each 5 mL contains 2,5 mg Levocetirizine dihydrochloride  
Cardiac disorders  
Frequency unknown  
Palpitation, tachycardia  
Dyspnoea  
Respiratory, thoracic and Frequency unknown  
mediastinal disorders  
Gastrointestinal  
disorders  
Frequent  
Diarrhoea, constipation, dry mouth  
Nausea and gastro-intestinal discomfort,  
abdominal pain  
Less frequent  
Vomiting  
Frequency unknown  
Frequency unknown  
Hepato-biliary disorders  
Hepatitis, abnormal liver function test*  
Skin and subcutaneous Frequency unknown  
Rash, urticaria, pruritus, fixed drug eruption  
tissue disorders  
Musculoskeletal,  
connective  
Frequency unknown  
Myalgia, arthralgia  
tissue  
bone  
disorders  
disorders  
Renal  
and  
and  
urinary Frequency unknown  
Dysuria, urinary retention  
disorders  
General disorders and Frequent  
Fatigue  
administration  
conditions  
site Less frequent  
Frequency unknown  
Asthenia, malaise  
Oedema  
c) Description of selected adverse reactions  
After levocetirizine discontinuation, pruritus has been reported.  
d) Paediatric population  
System Organ Class  
Psychiatric disorders  
Frequency  
Side effects  
Frequent  
Sleep disorders  
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Applicant/PHRC: Hetero Drugs South Africa (Pty) Ltd  
Product proprietary name: Cetorin Oral Solution 2,5 mg/ 5 mL  
Dosage form and strength: Oral solution, Each 5 mL contains 2,5 mg Levocetirizine dihydrochloride  
Nervous  
system Frequent  
Less frequent  
Somnolence  
Headache  
disorders  
Gastrointestinal  
disorders  
Frequent  
Diarrhoea, constipation  
Vomiting  
Less frequent  
Reporting of suspected adverse reactions  
Reporting suspected adverse reactions after authorisation of the medicine is important. It allows continued  
monitoring of the benefit/risk balance of the medicine. Health care providers are asked to report any  
suspected adverse to report any suspected adverse reactions to SAHPRA via the “6.04 Adverse  
Drug  
Reactions  
Reporting  
Form”,  
found  
online  
under  
SAHPRA’s  
publications:  
https://www.sahpra.org.za/publications/Index/8 or to the Holder of certificate of registration through the  
mail: pvg.cdma@heterogroups.com  
4.9 Overdose  
Signs and symptoms  
Symptoms of overdose may include drowsiness in adults and initially agitation and restlessness, followed  
by drowsiness in children.  
Management of overdoses  
There is no known specific antidote to CETORIN Oral Solution. Should overdose occur,symptomatic or  
supportive treatment is recommended. Levocetirizine is not effectively removed by haemodialysis.  
5 PHARMACOLOGICAL PROPERTIES  
5.1 Pharmacodynamic properties  
Pharmacotherapeutic group: Antihistamines for systemic use, piperazine derivatives,  
ATC code: R06A E09.  
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Product proprietary name: Cetorin Oral Solution 2,5 mg/ 5 mL  
Dosage form and strength: Oral solution, Each 5 mL contains 2,5 mg Levocetirizine dihydrochloride  
Pharmacological classification: A 5.7.1 Antihistaminics  
Mechanism of action  
Levocetirizine is the R-enantiomer of cetirizine, is a histamine H1-receptors. Binding studies revealed that  
levocetirizine has high affinity for human H1-receptors (Ki = 3,2 nmol/l). Levocetirizine has an affinity2-fold  
higher than that of cetirizine (Ki = 6.3 nmol/l). Levocetirizine dissociates from H1-receptors with a half-life of  
115 ± 38 min. After single administration, levocetirizine shows a receptor occupancy of 90 % at 4 hours and  
57 % at 24 hours.  
Pharmacodynamic studies in healthy volunteers demonstrate that, at half the dose, levocetirizine has  
comparable activity to cetirizine, both in the skin and in the nose.  
5.2 Pharmacokinetic properties  
The pharmacokinetic profile is the same when given as the single enantiomer or when given as cetirizine.  
No chiral inversion occurs during the process of absorption and elimination.  
Absorption  
Levocetirizine is rapidly and extensively absorbed following oral administration. In adults, peak plasma  
concentrations are achieved 0,9 hours after dosing. Steady state is achieved after two days. Peak  
concentrations are typically 270 ng/ml and 308 ng/ml following a single and a repeated 5 mg o.d. dose,  
respectively. The extent of absorption is dose-independent and is not altered by food, but the peak  
concentration is reduced and delayed.  
Distribution  
No tissue distribution data are available in humans, neither concerning the passage of levocetirizine through  
the blood-brain-barrier. In rats and dogs, the highest tissue levels are found in liver and kidneys, the lowest  
in the CNS compartment.  
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Product proprietary name: Cetorin Oral Solution 2,5 mg/ 5 mL  
Dosage form and strength: Oral solution, Each 5 mL contains 2,5 mg Levocetirizine dihydrochloride  
In humans, levocetirizine is 90 % bound to plasma proteins. The distribution of levocetirizine is restrictive,  
as the volume of distribution is 0,4 l/kg.  
Biotransformation  
The extent of metabolism of levocetirizine in humans is less than 14% of the dose and therefore differences  
resulting from genetic polymorphism or concomitant intake of enzyme inhibitors are expected to be  
negligible.  
Metabolic pathways include aromatic oxidation, N- and O- dealkylation and taurine conjugation.  
Dealkylation pathways are primarily mediated by CYP 3A4 while aromatic oxidation involved multiple and/or  
unidentified CYP isoforms. Levocetirizine had no effect on the activities of CYP isoenzymes 1A2, 2C9,  
2C19, 2D6, 2E1 and 3A4 at concentrations well above peak concentrations achieved following a 5 mg oral  
dose. Due to its low metabolism and absence of metabolic inhibition potential, the interaction of  
levocetirizine with other substances, or vice-versa, is unlikely.  
Elimination  
The plasma half-life in adults is approximately 8 hours in adults. The half-life is shorter in small children.  
The mean apparent total body clearance in adults is 0.63 ml/min/kg. The main route of excretion of  
levocetirizine and metabolites is via urine, accounting for a mean of 85 % of the dose. Approximately 13 %  
is excreted in the faeces. Levocetirizine is excreted both by glomerular filtration and active tubular secretion.  
Linearity  
The pharmacokinetics of levocetirizine are linear with dose- and time-independent with low inter subject  
variability  
Pharmacokinetics in special patient groups  
Renal impairment  
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Product proprietary name: Cetorin Oral Solution 2,5 mg/ 5 mL  
Dosage form and strength: Oral solution, Each 5 mL contains 2,5 mg Levocetirizine dihydrochloride  
The apparent body clearance of levocetirizine is correlated to the creatinine clearance. It is therefore  
recommended to adjust the dosing intervals of levocetirizine, based on creatinine clearance in patients with  
moderate and severe renal impairment. In anuric end stage renal disease patients, the total body clearance  
is decreased by approximately 80 % when compared to normal patients. The amount of levocetirizine  
removed during a standard 4-hour hemodialysis procedure was < 10 %.  
Elderly  
Limited pharmacokinetic data are available in elderly patients. Total body clearance in the elderly is  
approximately 33 % lower compared to that in younger adults. The disposition of racemic cetirizine has  
been shown to be dependent on renal function rather than age. This would also be applicable for  
levocetirizine, as both cetirizine and levocetirizine are both predominantly excreted in urine. Therefore, the  
dose of levocetirizine should be adjusted in accordance with renal function in elderly patients.  
Hepatic impairment  
The pharmacokinetics of levocetirizine in hepatically impaired patients have not been tested. Patients with  
chronic liver diseases (hepatocellular, cholestatic, and biliary cirrhosis) given 10 or 20 mg of the racemic  
compound cetirizine as a single dose had a 50 % increase in half-life along with a 40 % decrease in  
clearance compared to healthy patients.  
Gender  
The same daily dose and dosing intervals are applicable for men and women with normal renal function.  
Race  
The effect of race on levocetirizine has not been studied. As levocetirizine is primarily renally excreted, and  
there are no important racial differences in creatinine clearance, pharmacokinetic characteristics of  
levocetirizine are not expected to be different across races. No race-related differences in the kinetics of  
racemic cetirizine have been observed.  
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Product proprietary name: Cetorin Oral Solution 2,5 mg/ 5 mL  
Dosage form and strength: Oral solution, Each 5 mL contains 2,5 mg Levocetirizine dihydrochloride  
Paediatric population  
In children age 6 to 11 years with body weight ranging between 20 and 40 kg the Cmax and AUC values are  
about 2-fold greater than in healthy adults, following oral administration of a single dose of 5 mg  
levocetirizine. Total body clearance is 30 % greater and the elimination half-life 24 % shorter in the  
paediatric population than in adults. Administration of 1,25 mg once daily to children 6 months to 5 years  
of age is expected to result in plasma concentrations similar to those of adults receiving 5 mg once daily.  
6 PHARMACEUTICAL PARTICULARS  
6.1 List of excipients  
•
•
•
•
•
•
•
•
Methyl paraben  
Propyl paraben  
Glycerin  
Sodium acetate trihydrate  
Glacial acetic acid  
Saccharin sodium  
Maltitol solution  
ART Grape FL#10273 Composition  
o
o
Flavouring ingredients approved for use in a regulation of FDA  
Propylene glycol  
6.2 Incompatibilities  
Not applicable  
6.3 Shelf life  
24 months  
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Product proprietary name: Cetorin Oral Solution 2,5 mg/ 5 mL  
Dosage form and strength: Oral solution, Each 5 mL contains 2,5 mg Levocetirizine dihydrochloride  
6.4 Special precautions for storage  
Store at or below 25 °C. Protect from light and moisture.  
KEEP OUT OF REACH OF CHILDREN.  
6.5 Nature and contents of container  
White opaque round shaped polypropylene 185 ml container pack filled with 148 mL, child resistant plastic  
cap with FSE wad, 28 mm  
or  
Amber color polypropylene 115 mL container pack filled with 100 mL, with child resistant plastic cap with  
FSE wad, 28 mm  
6.6 Special precautions for disposal and other handling  
No special requirements  
7 HOLDER OF CERTIFICATE OF REGISTRATION  
Hetero Drugs South Africa (Pty) Ltd  
Waterfall Corporate Campus,  
Building No.2, First Floor,  
74 Waterfall Drive,  
Midrand  
2066  
Telephone number: 012 644 1220  
Fax number: 012 644 1564  
e-mail address: nokuthula.n@hetero.com  
8 REGISTRATION NUMBER  
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52/5.7.1/0935  
9 DATE OF FIRST AUTHORISATION/RENEWAL OF THE AUTHORISATION  
06 September 2022  
10 DATE OF REVISION OF THE TEXT  
11 June 2026  
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