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Levocetirizine Dihydrochloride


Levocetirizine

is a third-generation, non-sedating

antihistamine

, developed from the second-generation

antihistamine

cetirizine

. Chemically,

levocetirizine

is simply the isolated levorotatory enantiomer of

cetirizine

, which is sold as a racemic mixture.
Dosing
Adult dosing:

Idiopathic urticaria

; chronic:

5 mg
orally

once daily

in the evening
; a 2.5-mg

dose

may be adequate for some patients (FDA

dosage

); if symptoms persist after 2 weeks; may increase up to 4 times the standard

dose

(guideline

dosage

)

Pediatric dosing:

Idiopathic urticaria

; chronic:

12 years
or older:
5 mg
orally

once daily

in the evening
; a 2.5-mg

dose

may be.

Adequate for some patients:
6 to
11 years
of age:

2.5 mg

orally

once daily

in the evening
; do not exceed recommended

dose



6 months

to
5 years
of age:

1.25 mg

orally

once daily

in the evening
; do not exceed recommended

dose

.

Perennial allergic rhinitis

:

Oral solution
;

6 months

to
2 years
:

1.25 mg

(2.5mL of the 0.5mg/mL
oral solution
) orally

once daily

in the evening
; do not exceed this

dose

.

Indications
FDA-Labeled Indications:

Idiopathic Urticaria

; Chronic

Perennial allergic rhinitis


Mechanism of Action

Levocetirizine

; an enantiomer of cetirizine; is an

antihistamine

that selectively inhibits the
effect
of H(1)-receptors.
Adverse Effect
Common:
Gastrointestinal:
Constipation (Infants: 7%)
Diarrhea (Infants: 13%)
Painful teething (Infants: 6.7%)
Xerostomia (
Adults
and adolescents: 2% to 3%)

Neurologic:
Somnolence (4.4% to 6%)

Respiratory:
Nasopharyngitis (
Adults
and adolescents: 4% to 6%)
Pharyngitis (
Adults
and adolescents: 1% to 2%)

Other:
Fatigue (
Adults
and adolescents: 1% to 4%)

Serious:
Renal:

Urinary retention


Contraindication
Hemodialysis patients
Hypersensitivity to levocetirizine,

cetirizine

, or any component of the product
Renal disease; end-stage (creatinine clearance less than 10 mL/min)
Renally impaired pediatric patients between

6 months

and
11 years old

Interaction
In vitro data indicate that

levocetirizine

is unlikely to produce pharmacokinetic interactions through inhibition or induction of liver
drug
-metabolizing enzymes. No in vivo
drug
drug
interaction studies have been performed with

levocetirizine

.
Drug
interaction studies have been performed with racemic

cetirizine

.

Antipyrine; Azithromycin; Cimetidine; Erythromycin; Ketoconazole; Theophylline; and Pseudoephedrine:
Pharmacokinetic interaction studies performed with racemic

cetirizine

demonstrated that

cetirizine

did not interact with antipyrine; pseudoephedrine;

erythromycin

;

azithromycin

; ketoconazole; and cimetidine. There was a small decrease (~16%) in the clearance of

cetirizine

caused by a 400 mg

dose

of theophylline. It is possible that higher theophylline

doses

could have a greater effect.

Ritonavir:
Ritonavir increased the plasma AUC of

cetirizine

by about 42% accompanied by an increase in half-life (53%) and a decrease in clearance (29%) of

cetirizine

. The disposition of ritonavir was not altered by concomitant

cetirizine

administration.

Phamacokinetics
Absorption:
Oral
:

Rapid and Extensive

Time for Maximum Plasma Concentration (Tmax): 0.9 hour

Bioavailability:
Oral
; at least 85%

Effect of

food: No effect on AUC

High fat meal:
Delays Tmax by 1.25 hours
Delays Cmax by 36%

Distribution:
Volume of Distribution (Vd):
Adults
: 0.4L/kg
Children (6 to
11 years old
): 0.4L/kg

Plasma Protein binding:
Adults
: 91% to 95%

Metabolism:
Hepatic: Less than 14%

Excretion:
Renal: 85.4% (approximately 80% unchanged)
Fecal: 12.9%

Elimination:
Adults
: 7 to 8 hours
Children: 5.7 hours

Precaution
Concomitant alcohol

use

should be avoided due to potential increase in

CNS depression

and sedation

Concomitant

use of

other

CNS depressants

should be avoided due to potential increase in

CNS depression

and sedation

Renal function, impaired, increased risk of adverse reactions;

dosage

adjustment required

Urinary retention

may occur; increased risk with predisposing factors including spinal cord lesions or prostatic hyperplasia

Pregnancy Category
B (FDA)
Breast Feeding
Infant Risk Cannot Be ruled out.
Monitoring
Improvement in rhinitis symptoms
Urticaria: improvement in itching and/or hives
CNS effects
Renal function
How to Take or Administration
Oral
:

Take with or without food
in the evening
.
Dosage Form
Oral Solution
:

0.5 mg/1ML

Oral Tablet
:

5 mg

Treatment
Management of Mild to Moderate Toxicity:
Observation and supportive care is all that is required for the vast majority of

overdoses

.

Management of Severe Toxicity:
Serious toxicity is not expected after ingestion of

cetirizine

or levocetirizine alone. Patients with

CNS depression

should be monitored to assure that they do not have

respiratory depression

or require airway management.

Toxicology
No specific toxic
dose
has been established.
Patient Counselling or Clinical Teaching
Patient should avoid activities requiring mental alertness or coordination until
drug
effects are realized; because
drug
may cause somnolence, fatigue, and asthenia.
This
drug
may cause nasopharyngitis, xerostomia, and pharyngitis, as well as pyrexia, cough, and epistaxis in children 12 and under.
Inform patient that tablet may be broken in half to achieve correct
dose
for a child.
Patient should not drink alcohol or take other

CNS depressants

while taking this
drug
.












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