RIMAZIN [Cetirizine] 10 mg Film-coated tablets
RIMAZIN
instructions for the medical use of the medicinal
product
Tradename
Rimazin, Римазин
International
non-proprietary name or generic name
Cetirizine, Цетиризин
Composition
Each film coated tablet contains:
Active substance: cetirizine (as cetirizine hydrochloride) 10 mg
Excipients: lactose monohydrate, starch, PVP K-30, talc, magnesium
stearate.
Tablets.
Blocker of histamine H1 receptors.
Antiallergic agent
Pharmacodynamics
A competitive histamine
antagonist, a metabolite of hydroxyzine, blocks histamine H1 receptors.
Prevents the development and facilitates the course of allergic reactions, has
antipruritic and antiexudative action. Influences the early stage of allergic reactions,
limits the release of inflammatory mediators at the late stage of an allergic
reaction, reduces the migration of eosinophils, neutrophils and basophils.
Reduces capillary permeability, prevents the development of tissue edema,
relieves smooth muscle spasm.
Eliminates skin reactions to
the introduction of histamine, specific allergens, as well as to cooling (with
cold urticaria).
Virtually no anticholinergic
and antiserotonin action. In therapeutic doses, it practically does not cause
sedation. The onset of action after a single dose of 10 mg of cetirizine -
after 20 - 60 minutes, lasts more than 24 hours. Against the background of a
course of treatment, tolerance to the antihistamine action of cetirizine does
not develop. After stopping treatment, the effect persists for up to 3 days.
It is rapidly absorbed from
the gastrointestinal tract, the time to reach Cmax after oral administration is
1 hour. Food does not affect the completeness of absorption (AUC), but
lengthens the time to reach Cmax by 1 hour and reduces the Cmax value by 23%.
When taken in a dose of 10 mg 1 time / day for 10 days, Css in plasma is 310 ng
/ ml and is noted 0.5-1.5 hours after administration. Plasma protein binding is
93% and does not change when the concentration of cetirizine is in the range of
25-1000 ng / ml. Pharmacokinetic parameters of cetirizine change linearly when
administered at a dose of 5-60 mg. Vd - 0.5 l / kg. In small amounts, it is
metabolized in the liver by O-dealkylation to form a pharmacologically inactive
metabolite (unlike other blockers of histamine H1 receptors, metabolized in the
liver with the participation of the cytochrome P450 system). Does not cumulate.
2/3 of the drug is excreted unchanged by the kidneys and about 10% through the intestines.
Systemic clearance - 53 ml /
min. T1 / 2 in adults - 7-10 hours, in children 6-12 years old - 6 hours, in
children 2-6 years old - 5 hours, in children from 6 months to 2 years old - 3
hours. In elderly patients, T1 / 2 increases by 50%, systemic clearance is
reduced by 40% (decreased renal function).
In patients with impaired
renal function (CC below 40 ml / min), cetirizine clearance decreases, and T1 /
2 lengthens (for example, in patients on hemodialysis, total clearance
decreases by 70% and is 0.3 ml / min / kg, and T1 / 2 is extended 3 times),
which requires a corresponding change in the dosage regimen.
In patients with chronic liver
diseases (hepatocellular, cholestatic or biliary cirrhosis), T1 / 2 lengthening
by 50% and a decrease in total clearance by 40% are noted (correction of the
dosage regimen is required only with a concomitant decrease in the glomerular
filtration rate). Penetrates into breast milk.
• seasonal and year-round allergic rhinitis and conjunctivitis
(itching, sneezing, rhinorrhea, nasal congestion, lacrimation, conjunctival
hyperemia);
• urticaria (including chronic idiopathic urticaria);
• hay fever (hay fever);
• angioedema (Quincke's edema);
• itchy allergic dermatoses.
• hypersensitivity to Rimazin, other components of the
drug;
• reduced renal function (CC 30-49 ml / min);
• chronic renal failure (CC <10 ml / min);
• children under 6 years old;
• pregnancy;
• lactation period.
With caution: elderly age (a decrease in the glomerular
filtration rate is possible), patients with increased convulsive readiness and
epilepsy.
Method of administration and dosage
Inside with plenty of water.
Adults and children over 12 years old
- 10 mg (1 tablet) once a day, children 6-12 years old - 5 mg (1/2 tablet) 2
times a day, the daily dose is 10 mg.
The drug is contraindicated in
patients with creatinine clearance less than 10 ml / min and on dialysis. In
patients with renal insufficiency and in elderly patients, the dose should be
adjusted depending on the value of creatinine clearance (CC). With CC 30–49 ml
/ min - 5 mg once a day, with 10–29 ml / min - 5 mg every other day.
Special instructions and precautions
In patients with spinal cord injury, prostatic
hyperplasia, as well as in the presence of other predisposing factors for
urinary retention, caution is required, since Rimazin may increase the risk of
urinary retention.
Caution should be exercised when treating patients
with epilepsy and seizure tendencies.
In elderly patients, a decrease in renal function is
possible, which should be taken into account when dosing the drug.
Rimazin in tablet form is not recommended for children
under 6 years of age due to difficulty in swallowing. It is recommended to use
a pediatric dosage form in the form of syrup or drops.
When taking Rimazin, you should refrain from drinking
alcohol and antidepressants of the central nervous system, since the drug can
cause increased drowsiness.
Influence on the
ability to drive vehicles and mechanisms
Application during pregnancy and during breastfeeding
It is not recommended
to use the drug during pregnancy and do not prescribe the drug during
lactation, because cetirizine passes into breast milk.
Interaction with other medicinal products
Combined use with theophylline (400 mg / day) leads to
a decrease in the total clearance of cetirizine (the kinetics of theophylline
does not change).
Myelotoxic drugs increase the manifestations of the
drug's hematoxicity.
The simultaneous use of cetirizine with alcohol and
other drugs that depress the central nervous system may contribute to a further
decrease in concentration and speed of reactions, although cetirizine does not
enhance the effect of alcohol (when its concentration in the blood is 0.5 g /
l).
From the digestive system: dry
mouth, dyspepsia.
From the nervous system: dizziness,
headache, drowsiness, fatigue, agitation, migraine.
Allergic reactions: angioedema,
skin rashes, itching, urticaria.
If any of the side effects indicated in the
instructions are aggravated, or you notice any other side effects that are not
listed in the instructions, inform your doctor.
Symptoms:
confusion, diarrhea, dizziness, fatigue, headache,
malaise, mydriasis, itching, anxiety, weakness, sedation, drowsiness, stupor,
tachycardia, tremor, urinary retention.
Treatment:
Gastric lavage or stimulation of vomiting, intake
of activated charcoal, symptomatic and supportive therapy. There is no specific
antidote. Hemodialysis is ineffective.
Store in a dry and
dark place, at a temperature not exceeding 25°C.
Keep out of the reach
of children!
2 years. Do not use
after the expiration date printed on the package.
Dispensed by
prescription.
Release form
10 tablets in aluminum foil blister. 1 blister with instructions for use in a cardboard box.