Cetirizine
Dr. Reddy`s
644 Items
2019-09-19
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Clinical Pharmacology
Histamine N blocker1-receptors. Does not block cholinergic and serotonin receptors. It has an anti-allergic effect, when applied in therapeutic doses does not penetrate the BBB, therefore does not cause any significant sedative effect. Cetirizine affects both the early and late stages of an allergic reaction.
Pharmacokinetics
Suction and distribution
After oral administration cetirizine is well absorbed from the gastrointestinal tract. Reception simultaneously with food practically does not affect absorption. Cmax Cetirizine in the blood is reached 1 hour after administration and is 0.3 μg / ml. Cetirizine is largely bound to plasma proteins.
Metabolism and excretion
It is slightly metabolized in the liver. T1/2 is about 10 hours, in the elderly - about 12 hours, in children - 5-6 hours. Most cetirizine is excreted in the urine unchanged.
Pharmacokinetics in special clinical situations
T1/2 in elderly people it is about 12 hours, in children - 5-6 hours.
Indications
Cetrine is used in adults and children over the age of 6 years to alleviate the symptoms of:
- seasonal and chronic allergic rhinitis;
- allergic conjunctivitis;
- itching of various etiologies;
- urticaria (including chronic idiopathic);
- angioedema (angioedema).
Composition
1 tablet contains:
Active substances: cetirizine dihydrochloride 10 mg.
Excipients: lactose - 106.5 mg, corn starch - 65 mg, povidone (K-30) - 2 mg, magnesium stearate - 1.5 mg.
Shell composition: hypromellose - 3.3 mg, macrogol 6000 - 0.661 mg, titanium dioxide - 0.706 mg, talc - 1.183 mg, sorbic acid - 0.05 mg, polysorbate 80 - 0.05 mg, dimethicone - 0.05 mg.
Cetirizine is marketed under different brands and generic names, and comes in different dosage forms:
| Brand name | Manufacturer | Country | Dosage form |
|---|---|---|---|
| Cetrin | Dr. Reddy`s | India | pills |
| Zyrtec | UCB Pharma | Belgium | pills |
| Cetirizin-Teva | Teva | Israel | pills |
| Cetirizine | Vertex | Russia | pills |
| Cetirizine | Danafa Pharmaceutical Joint | Vietnam | pills |
| Cetirizine | Replepharm | Macedonia | pills |
| Cetirizine | Salyutas Pharma GmbH | Germany | drops |
| Cetirizine | Salyutas Pharma GmbH | Germany | pills |
| Zodac | Zentiva KS | Czech | drops |
| Parlazin | Egis | Hungary | pills |
| Parlazin | Egis | Hungary | drops |
| Zodac | Zentiva KS | Czech | pills |
| Zyrtec | UCB Pharma | Belgium | drops |
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Dosage and Administration
For adults and children older than 6 years, the daily dose is 10 mg, for adults - in 1 reception, the drug is prescribed for children 5 mg 2 times / day. pills washed down with a small amount of water.
In case of impaired renal function, a dose adjustment of the drug is required (as a rule, the dose is reduced by 2 times).
Adverse reactions
From the side of the central nervous system: in some cases - weakness, headache, dizziness, drowsiness, psychomotor agitation.
From the digestive system: dry mouth, gastrointestinal disorders.
Other: extremely rarely - hypersensitivity reactions (skin rash, angioedema). Cetrine is usually well tolerated.
Contraindications
Hypersensitivity to the drug. Pregnancy and lactation (breastfeeding).
Drug interactions
So far, there is no data on the interaction of cetirizine with other drugs, however, caution should be exercised while prescribing the drug with sedatives.
Pregnancy and Lactation
The drug is contraindicated for use during pregnancy and lactation (breastfeeding).
Special instructions
When used in therapeutic doses, cetirizine does not potentiate the action of ethanol, however, alcohol consumption during the use of the drug is not recommended.
Impact on the ability to drive vehicles and other mechanisms that require high concentration of attention
In therapeutic doses, Cetrine does not affect the speed of psychomotor reactions. However, patients involved in potentially hazardous activities need to be careful.
Overdosage
Symptoms: drowsiness; with a significant overdose of the drug (excess therapeutic dose in 30-40 times in adults and children) - drowsiness, anxiety, itching, rash, urinary retention, fatigue, tremor, tachycardia. In all cases, there was a complete normalization of the state.
Treatment: gastric lavage; if necessary, symptomatic therapy. There is no specific antidote. Hemodialysis is ineffective.
- Brand name: Cetrin
- Active ingredient: Cetirizine
- Dosage form: pills, coated.
- Manufacturer: Dr. Reddy`s
- Country of Origin: India
Studies and clinical trials of Cetirizine (Click to expand)
- Double-blind, parallel, randomized pilot study comparing the efficacy and tolerance of cetirizine 10 mg, mequitazine 2 × 5 mg and placebo in the treatment of patients suffering from chronic urticaria: Comparison of suppressive effects on histamine-induced weals and flares
- Ionic Partition Diagram of the Zwitterionic Antihistamine Cetirizine
- Cetirizine: An effective agent in Kimura's disease
- Cetirizine from topical phosphatidylcholine liposomes: Evaluation of peripheral antihistaminic activity and systemic absorption in a rabbit model
- Stereoselective pharmacokinetics of cetirizine in the guinea pig: role of protein binding
- Comparison of HPLC and CE methods for the determination of cetirizine dihydrochloride in human plasma samples
- Precolumn fluorescence labeling method for simultaneous determination of hydroxyzine and cetirizine in human serum
- ChemInform Abstract: The π-Arene Chromium Complex as a Facial Selectivity Control Element: The Enantioselective Synthesis of Cetirizine Hydrochloride
- ChemInform Abstract: A Large-Scale Synthesis of Enantiomerically Pure Cetirizine Dihydrochloride Using Preparative Chiral HPLC.
- ChemInform Abstract: Asymmetric Synthesis of Cetirizine Dihydrochloride.
- Stereoselective regulation of MDR1 expression in Caco-2 cells by cetirizine enantiomers
- Stereoselective and multiple carrier-mediated transport of cetirizine across Caco-2 cell monolayers with potential drug interaction
- Pharmacologic modulation by cetirizine 2 HCl and loratadine of the histamine-induced skin reaction in mice and in humans
- Histamine-induced wheal, flare, and pruritus: Inhibition by cetirizine, terfenadine, and placebo
- A Biomimetic Potentiometric Sensor Using Molecularly Imprinted Polymer for the Cetirizine Assay in Tablets and Biological Fluids
- Chiral separation of cetirizine by capillary electrophoresis
- Chiral separation and quantitation of cetirizine and hydroxyzine by maltodextrin-mediated CE in human plasma: Effect of zwitterionic property of cetirizine on enantioseparation
- Dose dependency of brain histamine H1 receptor occupancy following oral administration of cetirizine hydrochloride measured using PET with [11C]doxepin
- Does cetirizine belong to the new generation of antihistamines? An investigation into its acute and subchronic effects on highway driving, psychometric test performance and daytime sleepiness
- Evaluation of the cognitive, psychomotor and pharmacokinetic profiles of rupatadine, hydroxyzine and cetirizine, in combination with alcohol, in healthy volunteers
- Turbidimetric carbamazepine immunoassay on the ADVIA® 1650 and 2400 analyzers is free from interference of antihistamine drugs hydroxyzine and cetirizine
- Analytical performance evaluation of ADVIA Chemistry Carbamazepine_2 assay: minimal cross-reactivity with carbamazepine 10, 11-epoxide and none with hydroxyzine or cetirizine
- P-glycoprotein influences the brain concentrations of cetirizine (Zyrtec®), a second-generation non-sedating antihistamine
- Study of the inclusion complexes formed between cetirizine and α-, β-, and γ-cyclodextrin and evaluation on their taste-masking properties
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