Compound
Cetirizine dihydrochloride is the active ingredient of the drug. The drops also contain the following auxiliary components: glycerol , sodium saccharinate, methyl parahydroxybenzoate, glacial acetic acid, propylene glycol, sodium acetate trihydrate, propyl parahydroxybenzoate, purified water.
Parlazin tablets contain additional substances such as colloidal anhydrous silicon dioxide, lactose monohydrate, magnesium stearate, MCC. Their shell includes hypromellose, macrogol 400, titanium dioxide, Sunset yellow ariavit.
Parlazin Neo drops for oral administration 5mg/ml 20ml No.1
Name
Parlazin Neo k-li d/pr. orally 5 mg/ml in vial. 20ml per pack. No. 1
Description
Colorless or almost colorless sweet liquid without sediment, with a faint odor of acetic acid.
Main active ingredient
Levocetirizine dihydrochloride
Release form
Brown glass bottles with a thread for screwing on the cap, 20 ml volume, with a polyethylene dropper and a polypropylene cap with an inner polyethylene layer, equipped with special protection against opening by children and control of the first opening. 1 bottle is packed in a cardboard box along with instructions for medical use for patients.
Dosage
5mg/ml in vial. 20ml per pack. No. 1
Indications for use
The drug Parlazin® Neo drops is used to treat allergic disorders. Its active substance, levocetirizine, belongs to a class of drugs called antihistamines. The drug blocks the effect of histamine, which is released during allergic reactions. In adults and children over 6 years of age, it is used to treat the following diseases: - allergic rhinitis (runny nose), hay fever - allergic conjunctivitis - chronic urticaria (often accompanied by itching) In children aged 2-6 years for the treatment of: - hay fever
Directions for use and doses
Always take this drug as directed by these instructions or as directed by your doctor. If you are unsure, you should consult your doctor. The duration of the course depends on the type, duration and dynamics of the patient’s complaints. Dosage regimen Adults, adolescents and children over 6 years of age The daily recommended dose is 5 mg once a day (20 drops from a dropper). Children aged 6-12 years are recommended to be divided into two doses - 10 drops in the morning and evening. Children aged 2-6 years The daily recommended dose is 2.5 mg in two divided doses in equal doses (2 times 5 drops). In patients with impaired renal function, reduced doses may be prescribed depending on the severity of renal damage. The dosage regimen must be determined by your doctor. When prescribing the drug to patients with impaired liver function, no dose changes are required. Directions for use: The required number of drops should be measured using a dropper into a tablespoon or glass of water. Drops should be taken orally immediately after dilution, regardless of food intake. If you have taken too much Parlazin® Neo drops If you think that you have taken an excessive dose of Parlazin® Neo drops, tell your doctor, who will decide what action is necessary. If you forget to take Parlazin® Neo drops Do not take a double dose to make up for the missed dose. Just wait until it is time for your next dose and take the regular dose prescribed by your doctor. If you stop taking Parlazin® Neo drops ahead of schedule Stopping taking Parlazin® Neo drops earlier than prescribed should not cause harm. In this case, the symptoms of the disease can only gradually resume, without becoming more severe than before taking Parlazin® Neo. Do not change the recommended dose. Contact your doctor or pharmacist if you think the effect of the medicine is too weak or strong. If you have any further questions about using this drug, ask your doctor or pharmacist.
Use during pregnancy and lactation
If you are pregnant, breastfeeding, think you may be pregnant, or are planning to become pregnant, tell your doctor. Pregnancy Despite the fact that animal experiments have not revealed the harmful effects of levocetirizine, Parlazin® Neo drops - like other drugs - are not recommended for use during pregnancy. If you accidentally take Parlazin Neo drops during pregnancy, this medicine will not have any adverse effects on the fetus, but you should stop taking the drops. Breastfeeding During breastfeeding, Parlazin® Neo drops should not be taken, as it is expected that the active substance may pass into breast milk. Before taking any medications, consult your doctor.
Precautionary measures
Consult your doctor or pharmacist before taking Parlazin® Neo drops. Be sure to tell your doctor the following information: - if you have a tendency to retain urine (inability to empty your bladder completely), for example due to a spinal cord injury or an enlarged prostate gland. — Parlazin® Neo drops can cause allergic reactions (sometimes late), as they contain methyl parahydroxybenzoate and propyl parahydroxybenzoate. - if you suffer from other diseases, allergies or use other medications (for internal or external use), including those sold without a prescription. Children and adolescents under the age of 18 Parlazin® Neo Drops should not be used in children under 2 years of age due to insufficient data on the use of the drug. The drug Parlazin® Neo drops contain methyl parahydroxybenzoate and propyl parahydroxybenzoate as excipients. Parlazin® Neo drops contain methyl parahydroxybenzoate and propyl parahydroxybenzoate, which can cause allergic reactions (possibly delayed).
Interaction with other drugs
Tell your doctor about any medications you are taking, have recently taken, or plan to take, including those taken without a prescription. Antihistamines can mask skin reactions during allergy skin tests, so Parlazin® Neo should be discontinued at least three days before such a test. Taking with food, drinks and alcohol The drug can be taken regardless of meals. Avoid drinking alcohol while taking this drug as concomitant use of levocetirizine and alcohol may have effects on the nervous system in sensitive patients.
Contraindications
- if you are allergic to the active substance, other substances similar in structure, or any of the excipients of the drug listed in the “Composition” section; - if you have severe renal impairment (creatinine clearance
Compound
Active ingredient: 5 mg of levocetirizine dihydrochloride (corresponding to 4.21 mg of levocetirizine) in each milliliter of solution. Excipients: Glycerin 85%, propylene glycol, sodium saccharinate, sodium acetate trihydrate, methyl parahydroxybenzoate, propyl parahydroxybenzoate, glacial acetic acid, purified water.
Side effect
Like all medicines, Parlazin Neo drops can cause side effects, although not all patients get them. Fatigue, drowsiness, dry mouth, headache, and weakness have been reported. In some cases, allergic reactions were observed (swelling of the lips, tongue, eyelids, itching, inflammatory skin rash), photosensitivity of the skin, skin cracks, swelling, sinus thrombosis, jugular vein thrombosis, paresthesia (changes in skin sensitivity, for example, a feeling of tingling or ants crawling on skin), hypotrichosis (hair loss), gastrointestinal disorders, abdominal pain, palpitations, rapid pulse, angina, cramps, eye inflammation, blurred vision, blurred vision, muscle pain, aggression or restlessness, insomnia, thoughts of suicide, hallucinations, depression, increased runny nose, respiratory failure, liver inflammation, liver dysfunction (changes in laboratory test results), increased appetite, vomiting, dizziness, trembling, loss of consciousness, impaired taste, weight gain, sudden urge to urinate, urinary retention - inability to completely empty the bladder, ineffectiveness of the drug, dry mucous membranes. If you experience any of the side effects listed above, contact your healthcare provider, who will assess the severity of your symptoms and decide what action is necessary. Reporting side effects If you notice any of these side effects or if you experience any effects not listed in this leaflet, please contact your doctor or pharmacist. By reporting side effects, you will be providing additional information about the safety of this drug.
Storage conditions
Store at a temperature no higher than 25°C, out of the reach of children! Do not freeze! Store an open bottle for no more than 6 weeks!
Pharmacodynamics and pharmacokinetics
The active component of the drug is a selective antagonist of H1-histamine receptors . It has antihistamine effects and belongs to the group of piperazine . Affects inflammatory cells by blocking eosinophil chemotaxis and preventing eosinophil . Reduces the accumulation of eosinophils in the skin, as well as reactions to histamine . Inhibits other cells of the inflammatory infiltrate .
Parlazin prevents the appearance and alleviates allergy , has antiexudative and antipruritic properties. In addition, it reduces the degree of capillary , removes smooth muscle spasms and prevents swelling .
The effect of the drug begins 20 minutes after use. The maximum effect is achieved after an hour. The effect of the medicine lasts throughout the day.
This drug is absorbed Food intake has only a minor effect on its effect.
The degree of binding to proteins is 93%. Not biotransformed in the liver. The half-life is generally about 8 hours, in children it is shorter (5-6 hours, depending on age), and in older people, on the contrary, it is about 50% longer. In addition, it may increase in the presence of renal failure .
60% of the active substance is excreted unchanged in the urine during the day. Another 10% of the drug is released over the next 4 days. 10% is excreted in feces in 5 days. The medicine passes into breast milk.
Instructions for use PARLAZIN® NEO tab
The pharmacokinetics of levocetirizine is linear, independent of dose and time, and has small differences between subjects. The pharmacokinetic profiles of the enantiomer and cetirizine are similar. No chiral inversion occurs during absorption or excretion.
Suction
After oral administration, levocetirizine is rapidly and substantially absorbed. The maximum concentration in blood plasma is achieved 0.9 hours after administration. The equilibrium state is reached after two days. Usual peak concentrations after single and multiple (5 mg daily) doses are 270 ng/ml and 308 ng/ml, respectively. The extent of absorption is dose dependent and independent of food, however, in the case of food intake, the peak concentration is reduced and occurs later.
Distribution
There are no data on the distribution of the drug in human tissues and penetration through the blood-brain barrier. In rats and dogs, the highest tissue levels are found in the liver and kidneys and the lowest in the central nervous system.
Levocetirizine is 90% bound to plasma proteins. The distribution of levocetirizine is limited, since the volume of distribution is 0.4 l/kg.
Biotransformation
In humans, less than 14% of the administered dose of levocetirizine undergoes metabolic transformation, and therefore differences associated with genetic polymorphisms or concomitant use of enzyme inhibitors are considered to be minor. Metabolic pathways include oxidation of the aromatic ring, N- and O-dealkylation, and conjugation with taurine. Dealkylation is primarily mediated by CYP3A4, and many and/or unidentified CYP isoforms are involved in aromatic ring oxidation. Levocetirizine does not affect the activities of CYP isoenzymes 1A2, 2C9, 2C19, 2D6, 2E1 and 3A4 at concentrations significantly higher than the peak concentrations achievable after oral administration of 5 mg.
Due to the low rate of metabolism and the absence of possible suppression of metabolism, interaction of levocetirizine with other substances is unlikely.
Removal
The plasma half-life is 7.9 ± 1.9 hours. The average apparent clearance from the whole body is 0.63 ml/min per 1 kg. The main route of excretion of levocetirizine and its metabolites is through the kidneys in the urine; an average of 85.4% of the dose is eliminated this way. Excretion in feces is only 12.9% of the dose. Levocetirizine is excreted by both glomerular filtration and active tubular secretion.
Special patient groups
Renal dysfunction
The total clearance of levocetirizine correlates with creatinine clearance. Therefore, it is recommended that the intervals between doses of levocetirizine be adjusted based on creatinine clearance in patients with moderate or severe renal impairment (see Dosage Regimen). In the anuric stage of renal disease, total body clearance is reduced by approximately 80% compared to healthy subjects. In a standard 4-hour hemodialysis procedure, less than 10% of levocetirizine is eliminated.
Liver dysfunction
The pharmacokinetics of levocetirizine in patients with hepatic impairment have not been studied. In patients with chronic liver dysfunction (hepatocellular, cholestatic or biliary cirrhosis) receiving a single dose of 10 mg or 20 mg of the racemic compound cetirizine, the half-life was increased by 50% and clearance was decreased by 40%, compared with healthy individuals.
Children and teenagers
Data from a study of the pharmacokinetics of levocetirizine in 14 children aged 6 to 11 years weighing from 20 to 40 kg with a single oral dose of 5 mg showed that Cmax and AUC values were approximately 2 times higher than those in healthy adults. The average Cmax value was 450 ng/ml, Tmax averaged 1.2 hours, total clearance taking into account body weight was 30% higher, and T1/2 was 24% shorter in children than the corresponding values in adults. A retrospective pharmacokinetic analysis was conducted in 323 patients (181 children aged 1 to 5 years, 18 children aged 6 to 11 years, and 124 adults aged 18 to 55 years) who received one or more doses of levocetirizine from 1.25 mg to 30 mg. Data obtained during the analysis showed that taking the drug at a dose of 1.25 mg in children aged 6 months to 5 years leads to plasma concentrations corresponding to those in adults when taking 5 mg of the drug 1 time per day.
Elderly patients
Pharmacokinetic data in elderly patients is limited. When repeated dosing of levocetirizine 30 mg once daily for 6 days in 9 elderly patients (age 65 to 74 years) total clearance was approximately 33% lower than that in younger adults. The distribution of cetirizine racemate has been shown to be more dependent on renal function than on age. This statement may also apply to levocetirizine, because Both drugs, levocetirizine and cetirizine, are excreted primarily in the urine. Therefore, in elderly patients, the dose of levocetirizine should be adjusted depending on renal function.
Floor
The pharmacokinetic results of a study involving 77 patients (40 men and 37 women) were analyzed in terms of the possible influence of gender on the effectiveness of the drug. In women, the half-life was slightly shorter than in men ((7.08 ± 1.72 hours and 8.62 ± 1.84 hours, respectively), but weight-adjusted oral clearance was comparable in women and men (0.67 ± 0.16 ml/min/kg and 0.59 ±0.12 ml/min/kg) In men and women, daily doses and intervals between doses are the same.
Ethnicity
The effect of ethnicity on levocetirizine has not been studied. Since levocetirizine is primarily excreted by the kidneys and there are no known ethnic differences in creatinine clearance, differences between pharmacokinetic parameters are not expected in individuals of different ethnic groups. No such differences were found for cetirizine racemate.
Pharmacokinetic / pharmacodynamic dependence
The effect of levocetirizine on histamine-induced skin reactions is independent of its plasma concentration.
Side effects
As a rule, this drug is well tolerated. Side effects may be the following: drowsiness , headache , dizziness , nausea and other negative reactions from the gastrointestinal tract, increased fatigue, migraine , dry mouth, anxiety .
Side effects can be reduced by dividing the daily dose into two doses.
Hypersensitivity reactions to one of the components of the drug, for example, vascular edema or rash , are also possible, but they occur in rare cases.
Instructions for use of Parlazin (Method and dosage)
Before using the drug, you should definitely consult your doctor.
Adults are prescribed 10 mg per day. The instructions for Parlazin tablets indicate that this is 1 tablet per day. Should be taken orally with plenty of liquid. This dosage is also calculated for 20 drops. It is advisable to take the medicine at night. The daily dosage can be divided equally into two doses.
Children from 2 to 6 years old are prescribed 5 mg per day. For those who take Parlazin drops, the instructions for use indicate that the daily dosage is 10 drops. This is also half a tablet. The dose can be divided into two doses. Children 1 to 2 years old need to take 5 drops (2.5 mg) twice daily. And for children aged 6 to 12 years, 5 mg is prescribed 2 times a day to be taken morning and evening (10 drops or half a tablet). Alternatively, they can take 10 mg once a day (preferably in the evening), which equates to one tablet or 20 drops.
The instructions for Parlazin recommend that elderly patients and people with renal failure reduce the daily dosage to 5 mg. The tablets must be taken orally . Drops dissolve in water before taking.
Instructions for use PARLAZIN® tab
Suction
After taking the drug orally, cetirizine is rapidly absorbed from the gastrointestinal tract.
The equilibrium maximum concentration is approximately 300 ng/ml and is achieved within 1.0 ± 0.5 hours. The equilibrium state is achieved on the third day. In volunteers, pharmacokinetic parameters (Cmax and AUC) and distribution are unimodal.
Food does not affect the completeness of absorption, although the rate of absorption decreases. The degree of bioavailability is similar when cetirizine is used in the form of solution, capsules or tablets.
Distribution
In adults, after taking 10 mg of the drug orally, the apparent volume of distribution is approximately 35 l (0.50 l/kg). 93 ± 0.3% of cetirizine is protein bound. Cetirizine does not affect the binding of warfarin to plasma proteins.
Cetirizine is excreted in small quantities in breast milk.
Biotransformation
Cetirizine does not undergo significant pre-systemic metabolism.
Removal
About 2/3 of the dose is excreted unchanged in the urine. The terminal half-life is approximately 10 hours and cetirizine did not accumulate when administered repeatedly for 10 days at a dose of 10 mg/day.
Linearity/nonlinearity
Cetirizine has linear kinetics in the dose range from 5 to 60 mg.
Special patient groups
Elderly
In 16 elderly volunteer subjects, after a single oral dose of cetirizine 10 mg, the elimination half-life was increased by approximately 50% and clearance was reduced by 40%, compared with younger individuals. The decreased clearance of cetirizine in these elderly volunteers was likely due to worsening renal function.
Children and adolescents under 18 years of age
The half-life of cetirizine was approximately 6 hours in children aged 6 to 12 years and 5 hours in children aged 2 to 6 years. In small children and infants aged 6 to 24 months, the half-life is reduced to 3.1 hours.
Patients with impaired renal function
In patients with mild renal failure (creatinine clearance > 40 ml/min), the pharmacokinetics of the drug were similar to those in healthy volunteers. With moderate renal failure (creatinine clearance 10-40 ml/min), compared with healthy volunteers, the half-life increases three times, and clearance decreases by 70%.
Compared with healthy volunteers, in patients on hemodialysis (CrCl <7 ml/min) after a single dose of cetirizine 10 mg, the half-life increased threefold and clearance decreased by 70%. Cetirizine is poorly removed by hemodialysis (<10%). In case of moderate to severe impairment of renal function, a dose adjustment of cetirizine is necessary (see Dosage Regimen).
Patients with liver dysfunction
In patients with chronic liver dysfunction (hepatocellular, cholestatic or biliary cirrhosis), after oral administration of 10 mg or 20 mg cetirizine, the half-life decreased by 50% and clearance decreased by 40%.
Dose changes are only necessary in patients with concurrent impairment of liver and kidney function.
Overdose
When using the drug in high doses, fatigue and drowsiness . anxiety and irritability first . When taking an increased dose once, urinary retention and constipation .
In case of overdose, induce vomiting and rinse the stomach. Therapy is symptomatic. Hemodialysis
is not effective, and there is no specific
antidote .
Reviews about Parlazin
According to reviews, this product quickly copes with allergies , has a convenient dispenser and tastes very pleasant. It is easy to use even for allergies in young children. Reviews of drops for children also report that they are often recommended by pharmacists at pharmacies or prescribed by pediatricians. What parents especially like is that this product is included in the list of free medications for children under 3 years of age, and the packaging is completely safe for children.
On the negative side, reviews of Parlazin sometimes talk about the occurrence of adverse reactions. For some, this remedy is simply not suitable, as it has no effect. Perhaps in this case Parlazin Neo . In addition, patients note that this is a rather expensive remedy for use simply for preventive purposes. Moreover, once the package is opened, the drops are not stored for long.
Instructions for use PARLAZIN® NEO drops for oral administration
The pharmacokinetics of levocetirizine is linear, independent of dose and time, and has small differences between subjects. The pharmacokinetic profiles of the enantiomer and cetirizine are similar. No chiral inversion occurs during absorption or excretion.
Suction
After oral administration, levocetirizine is rapidly and substantially absorbed. The maximum concentration in blood plasma is achieved 0.9 hours after administration. The equilibrium state is reached after two days. Usual peak concentrations after single and multiple (5 mg daily) doses are 270 ng/ml and 308 ng/ml, respectively. The extent of absorption is dose dependent and independent of food, however, in the case of food intake, the peak concentration is reduced and occurs later.
Distribution
There are no data on the distribution of the drug in human tissues and penetration through the blood-brain barrier. In rats and dogs, the highest tissue levels are found in the liver and kidneys and the lowest in the central nervous system.
Levocetirizine is 90% bound to plasma proteins. The distribution of levocetirizine is limited, since the volume of distribution is 0.4 l/kg.
Biotransformation
In humans, less than 14% of the administered dose of levocetirizine undergoes metabolic transformation, and therefore differences due to genetic polymorphisms or concomitant use of enzyme inhibitors are considered to be minor. Metabolic pathways include oxidation of the aromatic ring, N- and O-dealkylation, and conjugation with taurine. Dealkylation is primarily mediated by CYP 3A4, and many and/or unidentified CYP isoforms are involved in aromatic ring oxidation. Levocetirizine does not affect the activities of CYP isoenzymes 1A2, 2C9, 2C19, 2D6, 2E1 and 3A4 at concentrations significantly higher than the peak concentrations achievable after oral administration of 5 mg.
Due to the low rate of metabolism and the absence of possible suppression of metabolism, interaction of levocetirizine with other substances is unlikely.
Removal
The plasma half-life is 7.9 ± 1.9 hours. The average apparent clearance from the whole body is 0.63 ml/min per 1 kg. The main route of excretion of levocetirizine and its metabolites is through the kidneys in the urine; an average of 85.4% of the dose is eliminated this way. Excretion in feces is only 12.9% of the dose. Levocetirizine is excreted by both glomerular filtration and active tubular secretion.
Special patient groups
Renal dysfunction
The apparent clearance of levocetirizine from the whole body correlates with creatinine clearance. Therefore, it is recommended that the intervals between doses of levocetirizine be adjusted based on creatinine clearance in patients with moderate or severe renal impairment (see Dosage Regimen). In the anuric stage of renal disease, total body clearance is reduced by approximately 80% compared to healthy subjects. In a standard 4-hour hemodialysis procedure, less than 10% of levocetirizine is eliminated.
Liver dysfunction
The pharmacokinetics of levocetirizine in patients with hepatic impairment have not been studied. In patients with chronic liver dysfunction (hepatocellular, cholestatic or biliary cirrhosis) receiving a single dose of 10 mg or 20 mg of the racemic compound cetirizine, the half-life was increased by 50% and clearance was decreased by 40%, compared with healthy individuals.
Children and teenagers
Data from a study of the pharmacokinetics of levocetirizine in 14 children aged 6 to 11 years weighing from 20 to 40 kg with a single oral dose of 5 mg showed that Cmax and AUC values were approximately 2 times higher than those in healthy adults. The average Cmax value was 450 ng/ml, Tmax averaged 1.2 hours, total clearance taking into account body weight was 30% higher, and T1/2 was 24% shorter in children than the corresponding values in adults. A retrospective pharmacokinetic analysis was conducted in 323 patients (181 children aged 1 to 5 years, 18 children aged 6 to 11 years, and 124 adults aged 18 to 55 years) who received one or more doses of levocetirizine from 1.25 mg to 30 mg. Data obtained during the analysis showed that taking the drug at a dose of 1.25 mg in children aged 6 months to 5 years leads to plasma concentrations corresponding to those in adults when taking 5 mg of the drug 1 time per day.
Elderly patients
Pharmacokinetic data in elderly patients is limited. When repeated dosing of levocetirizine 30 mg once daily for 6 days in 9 elderly patients (age 65 to 74 years) total clearance was approximately 33% lower than that in younger adults. The distribution of cetirizine racemate has been shown to be more dependent on renal function than on age. This statement may also apply to levocetirizine, because Both drugs, levocetirizine and cetirizine, are excreted primarily in the urine. Therefore, in elderly patients, the dose of levocetirizine should be adjusted depending on renal function.
Floor
The pharmacokinetic results of a study involving 77 patients (40 men and 37 women) were analyzed in terms of the possible influence of gender on the effectiveness of the drug. In women, the half-life was slightly shorter than in men ((7.08 ± 1.72 hours and 8.62 ± 1.84 hours, respectively), but weight-adjusted oral clearance was comparable in women and men (0.67 ± 0.16 ml/min/kg and 0.59 ± 0.12 ml/min/kg) In men and women, daily doses and intervals between doses are the same.
Ethnicity
The effect of ethnicity on levocetirizine has not been studied. Since levocetirizine is primarily excreted by the kidneys and there are no known ethnic differences in creatinine clearance, differences between pharmacokinetic parameters are not expected in individuals of different ethnic groups. No such differences were found for cetirizine racemate.
Pharmacokinetic pharmacodynamic relationship
:
- The effect of levocetirizine on histamine-induced skin reactions does not coincide in phase with plasma concentrations.
