basic physical and chemical properties: white, oblong, biconvex kaplety-coated;
Ingredients: 1 kapleta contains paracetamol 500 mg and cetirizine hydrochloride 10 mg;
Excipients: microcrystalline cellulose, starch, gelatin, methylparaben, propylparaben, purified water, magnesium stearate, purified talc, colloidal silicon dioxide, sodium lauryl sulfate, sodium starch glycolate, hydroxypropyl methylcellulose, ethyl cellulose, titanium dioxide, propylene glycol.
Release form. Caplet coated tablets.
Pharmacotherapeutic group. Analgesic-antipyretics. Paracetamol in combination with other drugs (except psycholeptics). ATS network code N02B E51.
Pharmacodynamics. Paracetamol has analgesic, antipyretic, anti-inflammatory properties. The mechanism of analgesic effect of paracetamol is associated with inhibition of prostaglandin biosynthesis. By inhibiting tsyklohenazu, it prevents the formation of prostaglandins E2 and F2, which play an important role in the perception of pain are nociceptors and transmission of excitation in the CNS. Paracetamol effectively inhibits cyclooxygenase in CNS cells and much weaker - in peripheral tissues. Antypiretychnyy effect of paracetamol due to inhibition of prostaglandin biosynthesis directly in the hypothalamus, including E1 and E2, which are mediators of thermoregulatory center.
Cetirizine hydrochloride - a selective antagonist of peripheral H1-histamine receptors, hydroxyzine metabolite. It has antiallergic properties due to inhibition of the late phase of cell migration involved in inflammatory reactions (mainly eosinophils) also reduces the expression of adhesion molecules such as ICAM-1 and VCAM-1, which are markers of allergic inflammation. It inhibits the action of other mediators and histamine secretion inducers such as PAF (platelet-activating factor) and substance, almost does not cause anticholinergic and antiserotonin effects. At therapeutic doses, has no sedative effect.
Pharmacokinetics. Absorption. After oral administration of the drug rapidly and almost completely absorbed from the gastrointestinal tract. Use of the drug along with food does not affect the amount of absorption, but slightly reduces its speed.
Distribution. The drug is well distributed in tissues (except adipose tissues) and cerebrospinal fluid.
The binding of paracetamol to plasma proteins is approximately 10% and slightly increased in overdose.
Cetirizine is 93% bound to plasma proteins. The volume of distribution (Vd 0,5 l / kg). The maximum concentration in plasma is reached within 1 hour after oral administration. Food does not affect the integrity of the absorption, but prolongs the process of absorption for 1 hour. The pharmacokinetic parameters of cetirizine have a linear dependence.
Metabolism. Paracetamol is metabolized primarily in the liver by conjugation with glucuronide, sulfate and oxidation with mixed oxidase liver cytochrome P450.
Cetirizine in small amounts is metabolized in the liver by O-dezalkiruvannya to form a pharmacologically inactive metabolite (unlike other blocking H1 histamine receptors, which are metabolized in the liver, with the participation of cytochrome P450). Not cumulates.
Withdrawal. The half-life of paracetamol is 1-3 hours. In patients with cirrhosis the half-life is prolonged. Renal clearance of paracetamol is 5%. Excreted in the urine mainly in the form glucuronid and sulfate conjugates.
After single oral application tsyteryzynu hydrochloride half life is about 10 hours, 2/3 of the drug is excreted unchanged by the kidneys, and about 10% - of the stool. Systemic clearance - 53 mL / min.
Active substance of the drug cross the placenta and excreted in breast milk.
Indications. In the complex treatment of acute and chronic inflammation of the sinuses (sinusitis, sinusitis, sinusitis), acute rhinitis, viral or bacterial origin, allergic rhinitis, pain and inflammatory syndrome in dentistry and in diseases of the throat (pharyngitis, tonsillitis), pain in trauma, burns , fever during infectious and inflammatory diseases, allergic conjunctivitis, dermatitis, accompanied by pruritus, urticaria (including chronic idiopathic urticaria).
Dosage. Dose set individually. In adults and children over 12 years are used to 1 kapleti 2 times a day at intervals of not less than 4 hours. The maximum duration of treatment - 5 -7 days.
In patients with moderate or severe renal impairment apply half the recommended dose.
In elderly patients with normal renal function, dosage adjustment is not required.
Side effects. Gastro-intestinal tract and liver: dry mouth, in rare cases - dyspepsia, prolonged use at high doses - hepatotoxic effects.
Central nervous system: possible mild and shvydkomynayucha drowsiness, headache, fatigue, and in some cases - excitement.
From the hemopoietic system: rarely thrombocytopenia, leukopenia, pancytopenia, neutropenia, agranulocytosis.
Allergic reactions: seldom - angioedema, skin rash, itching, hives.
Contraindications. Hypersensitivity to the drug. Violation of liver and kidney, blood diseases, congenital hyperbilirubinemia, first trimester of pregnancy, lactation, chronic alcoholism, children up to age 12 years.
Overdose. Symptoms may sleep disorders, itching, skin rash, detention sechovyvedennya, fatigue, tremors, tachycardia. After 12-48 h. - Signs of liver damage with the development of liver failure.
Treatment: symptomatic therapy is carried out. Hemodialysis is ineffective
Precautions. Pregnancy and lactation. Use of the drug Milistan Sinus during pregnancy is only possible in cases where the intended benefits to the mother outweighs the potential risk to the fetus. It is advisable to refrain from drug use during lactation or should decide on the termination of breastfeeding.
In patients with benign hyperbilirubinemia, as well as in elderly patients to use the drug under medical supervision.
Effects on ability to drive vehicles and machinery. An objective assessment of the ability to control the car and work with the mechanisms were not significantly detected any reluctance effects when prescribing the recommended dose, and yet, we recommend caution.
When used in therapeutic doses not received information about the interaction with alcohol (for a blood alcohol concentration of 0.5 g / l). Still, better to abstain from alcohol during treatment.
Interaction with other drugs. With the simultaneous use of barbiturates, anticonvulsant drugs, rifampicin and alcohol significantly increases the risk of hepatotoxic action.
While the application of the drug Milistan Sinus of metoclopramide may increase absorption of paracetamol.
While the application of the drug Milistan Sinus and coumarin derivatives may develop small gipoprotrombinemii.
Caffeine may potentiate the analgesic effect of paracetamol.
Terms and conditions. Store at room temperature (15 - 25 ° C) in the dark and out of reach of children.
Shelf life - 3 years.