CETRAMAC TABLETS
COMPOSITION:
Each film coated tablet contains.
Cetirizine hydrochloride BP 10mg
DESCRIPTION:
Cetirizine, a piperazine derivative, is non-sedating anti-histamine with a potent anti-allergic action.
It possesses strong ability for histamine H, receptors and has no anticholinergic and antiserotoninergic effects. Since it does not cross the blood brain barrier it does not cause sedation or
interfere with mental alertness or memory function.
PHARMACOLOGICALACTION:
Cetirizine is human metabolite of hydroxyzine, is an antihistamine; its principal effects are mediated
via selective inhibition of peripheral H, receptors without any significant anticholinergic and
antiserotonergic effects. At pharmacologically active doss levels, it has no drowsiness effects and
does not cause behavioral changes, which may be explained by the absence of passage through
the blood brain barrier. Cetirizine inhibits the histamine mediated "early" phase of allergic reaction
and also reduces the migration of inflammatory cells and the release of mediators associated with
the "late" allergic response. Cetirizine also provides a protective effect from bronchospasm induced
by inhaled histamine in asthmatics.
PHARMACOKINETICS:
Cetirizine 10 mg achieves peak plasma concentration of 257 mcg/L within 1 hour of administration
(980mcg/L in children). Food does not affect the extent of absorption but may slightly reduce the
rate. The terminal elimination half-life in healthy volunteer’s ranges from 6.7h-10.9h. The half-life of
Cetirizine is slightly shorter in children than in adults, with values of 6.9-7.1h reported. Elimination
may be slightly prolonged in elderly volunteers compared with younger adults (half-life 11.8h v
7.4h). But this is independent of age in itself depending entirely on renal function. A half-life of 19
and 21h is observed in patients with mild and moderate renal impairment respectively. Some
adjustment of dosage may be necessary in such patients. In patients with moderate renal
impairment, the time to peak plasma concentration, is also significantly prolonged. The half-life may
be slightly prolonged in hepatic dysfunction. Haemodialysis does not alter Cetirizine elimination
significantly. Cetirizine is eliminated mainly by renal excretion of the unchanged drug, although there is a small
amount of metabolism in the liver. Approximately, 70% of the dose is excreted in the urine over 5
days. 60% over the first 24h, with only 10% in the faces over 5 days.
During chronic administration, Cetirizine achieves steady state within three days, consistent with its
half-life. The clearance of drug is not altered during chronic administration i.e. there is no auto
induction.
INDICATIONS:
Cetramac is indicated in allergic rhinitis, ocular symptoms like redness, lacrimation and Itching.
Urticaria dermographism, atopic eczema and contact dermatitis, acute allergic reactions due to
drugs, food, insect bites.
DOSAGE:
Adults: 10 mg once or twice daily,
Children (Over 6 years): As directed by physician.
CONTRAINDICATIONS: Pregnancy, lactation and children.
ADVERSE EFFECTS: Cetirizine has little or no effect on psychomotor function with the incidence of sedation being similar in that of placebo. The reported adverse reactions at the recommended dosage are low and similar to that of placebo and include drowsiness, dizziness, agitation, dry mouth and gastrointestinal discomfort.
PRECAUTIONS: Clinical studies of cetirizine at a dose up to 25mg daily in the healthy volunteers have not revealed effect on alertness or reaction time. Patients are advised not to exceed the recommended dose if
driving or operating machinery.
Pregnancy and Lactation: There is inadequate information about safety of cetirizine during pregnancy. Hence its use in pregnancy is not recommended. Nursing mothers are advised no to take this medication.
Elderly:Some dose reduction may be required, if renal function is impaired.
Renal Impairment: Dose amount and frequency will require modifications in patients with impairment of renal function.
DRUG INTERACTIONS:
To date, there are no known interactions with other drugs. Nevertheless, caution should be
recommended with concomitant use of sedatives and alcohol.
STORAGE: Store at a temperature not exceeding 30°C. Protect from light.
PRESENTATION: 10x10 Blister Pack