Composition, form of production and packaging
? Tablets covered with a coat of white or almost white, biconvex, ellipsoidal, with a risk on one side.
1 tab.
cetirizine dihydrochloride 10 mg
Excipients: microcrystalline cellulose, lactose monohydrate, crospovidone, silicon dioxide colloid, magnesium stearate.
Sheath composition: hypromellose, macrogol stearate, microcrystalline cellulose, propylene glycol, titanium dioxide (E171).
7 pcs. - blisters (1) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
The description of the drug was approved by the manufacturer for the 2006 print edition.
PHARMACHOLOGIC EFFECT
The blocker of peripheral histamine H 1 -receptors. A competitive histamine antagonist, a hydroxyzine metabolite. Prevents development and facilitates the course of allergic reactions, has antipruritic and antiexudative action. Affects the early stage of allergic reactions, limits the release of inflammatory mediators in the late stage of allergic reactions, reduces the migration of eosinophils, neutrophils and basophils.
Reduces the permeability of capillaries, prevents the development of edema of tissues, relieves spasm of smooth muscles. Eliminates the skin reaction to the administration of histamine, specific allergens, and also to cooling (with cold urticaria).
Virtually no anticholinergic and antiserotonin action. In therapeutic doses, it does not cause sedation.
The beginning of the drug after a single dose of 10 mg is observed after 20 minutes (in 5% of patients), after 60 minutes (in 95% of patients), the duration of the drug is more than 24 hours. Against the background of course treatment, tolerance does not develop.
After the cessation of treatment, the effect lasts up to 3 days.
PHARMACOKINETICS
Suction
Cetirizine is rapidly absorbed from the digestive tract.
C max in the blood plasma is achieved after 1 hour after ingestion. Simultaneous food intake does not affect the degree of absorption of the drug, but lengthens the time to reach C max for 1 h and reduces C max by 23%.
Distribution
The binding to plasma proteins is 93% and does not change with the concentration of cetirizine in the range of 25-1000 ng / ml. The pharmacokinetic parameters of cetirizine change linearly when administered in a dose of 5 mg to 60 mg.
When taking the drug at a dose of 10 mg 1 time / day for 10 days C ss in blood plasma is observed after 0.5-1.5 hours and is 310 ng / ml.
V d is about 0.5 l / kg. Cetirizine penetrates into breast milk.
Metabolism
Cetirizine is metabolized in small amounts in the liver by O-dealkylation to form a pharmacologically inactive metabolite (unlike other histamine H 1 -receptor blockers metabolized in the liver involving the cytochrome P 450 system ).
The drug does not cumulate.
Excretion
2/3 of the accepted dose of cetirizine are excreted unchanged by the kidneys and about 10% - with feces. Systemic clearance of cetirizine is 53 ml / min. T 1/2 in adults is 7-10 hours, in children aged 6-12 years - 6 hours, at the age of 2-6 years - 5 hours.
Pharmacokinetics in special clinical cases
In elderly patients, T 1/2 is increased by 50%, systemic clearance is reduced by 40% (due to decreased kidney function).
With renal insufficiency (CC less than 40 ml / min) systemic clearance of the drug decreases, T 1/2 is lengthened (so in patients who are on hemodialysis, the system clearance is reduced by 70% and is 0.3 ml / min / kg, and T 1/2 is extended 3 times), which requires appropriate correction of the dosing regimen.
In chronic liver diseases (hepatocellular, cholestatic or biliary cirrhosis), T.sub.l 1/2 of cetirizine is elongated by 50% and the systemic clearance is reduced by 40% (correction of the dosing regimen is required only with a corresponding decrease in the glomerular filtration rate).
Cetirizine is practically not removed during hemodialysis.
INDICATIONS
- seasonal and year-round allergic rhinitis and conjunctivitis (itching, sneezing, rhinorrhea, lacrimation, congestion hyperemia);
- urticaria (including chronic idiopathic urticaria);
- Pollinosis (hay fever);
- angioedema;
itching allergic dermatosis.
DOSING MODE
Adults and children over the age of 6 years are prescribed 10 mg (1 tab.) 1 time / day or 5 mg (1/2 tab.) 2 times / day.
Patients with impaired renal function (QC 30 to 49 ml / min) are prescribed 5 mg / day, with chronic renal failure of severe degree (QC 10 to 29 ml / min) 5 mg / day every other day.
Tablets are taken orally, with a small amount of water.
SIDE EFFECT
From the digestive system: dry mouth, discomfort in the abdominal region.
From the side of the central nervous system: headache, dizziness, migraine.
Allergic reactions: urticaria, angioedema, skin itching, skin rash.
CONTRAINDICATIONS
- Insufficiency of lactase;
- galactosemia;
- glucose-galactose malabsorption syndrome;
- children's age till 6 years;
- Pregnancy;
- lactation period (breastfeeding);
- Hypersensitivity to the components of the drug.
With caution should prescribe the drug to elderly patients, patients with chronic renal failure.
PREGNANCY AND LACTATION
Cetirinax is contraindicated in pregnancy and lactation (breastfeeding).
APPLICATION FOR FUNCTIONS OF THE LIVER
Patients with impaired renal function (QC 30 to 49 ml / min) are prescribed 5 mg / day, with chronic renal failure of severe degree (QC 10 to 29 ml / min) 5 mg / day every other day.
APPLICATION FOR CHILDREN
The drug is contraindicated for children under 6 years.
Children over the age of 6 years are prescribed 10 mg (1 tab.) 1 time / day or 5 mg (1/2 tab.) 2 times / day.
APPLICATION IN ELDERLY PATIENTS
Caution should be given to elderly patients.
SPECIAL INSTRUCTIONS
When the daily dose of 10 mg is exceeded, the ability to rapid reactions decreases.
It should be taken into account that with moderate and severe CKD, correction of the dosing regimen is required.
In recommended doses, the drug does not enhance the effect of ethanol (at a concentration of not more than 0.8 g / l). However, it is recommended to refrain from drinking alcohol while using the drug Cetirinax.
Impact on the ability to drive vehicles and manage mechanisms
During treatment, Cetirinax should refrain from engaging in potentially dangerous activities that require increased attention and speed of psychomotor reactions.
OVERDOSE
Symptoms: with a single admission of the drug at a dose of 50 mg develop drowsiness, anxiety, increased irritability, delayed urination, dry mouth, constipation.
Treatment: gastric lavage, reception of activated charcoal; if necessary, conduct symptomatic therapy. There is no specific antidote. Hemodialysis is ineffective.
DRUG INTERACTION
The pharmacokinetic interaction of cetirizine with pseudoephedrine, cimetidine, ketoconazole, erythromycin, azithromycin, diazepam, glipizide has not been established.
With the simultaneous administration of cetirizine with theophylline (400 mg / day), the systemic clearance of cetirizine decreases. However, the pharmacokinetics of theophylline does not change.
TERMS OF RELEASE FROM PHARMACY
The drug is approved for use as a means of OTC.
TERMS AND CONDITIONS OF STORAGE
The drug should be stored out of the reach of children at a temperature of no higher than 25 В° C. Shelf life - 3 years.
