No-shpa - tablets p.o. 24 pcs., Drotaverine 40 mg, for abdominal pain

Transparent, colorless to light yellow solution.

Pharmacodynamic properties

Mechanism of action

Cetirizine - active substance of the drug

Zodak® - is a metabolite of hydroxyzine, has an antihistamine effect with antiallergic effect.

Cetirizine belongs to the group of competitive histamine antagonists and blocks Hα-histamine receptors with little effect on other receptors and practically does not have anticholinergic and antiserotonin effects.

Cetirizine affects the histamine-dependent stage of immediate allergic reactions, and also reduces the migration of eosinophils and limits the release of mediators in delayed-type allergic reactions.

It practically does not pass through the blood-brain barrier and, therefore, is almost unable to reach the central H? Receptors.

Pharmacodynamics

In studies of the effect of histamine on the skin, the effect of cetirizine at a dose of 10 mg began after 1 hour, peaked from 2 to 12 hours and was still observed at statistically significant levels after 24 hours.

In addition to the antihistamine effect, cetirizine also has an anti-inflammatory effect and thus has an effect on the late phase of the allergic reaction:

- At a dose of 10 mg once or twice a day, inhibits the late phase of eosinophil aggregation in the skin

- At a dose of 30 mg per day, inhibits the elimination of eosinophils into the bronchial alveolar fluid after bronchial constriction caused by an allergen

- Inhibits late inflammatory response caused by kallikrein

- Suppresses the expression of inflammatory markers such as ICAM-1 or VCAM-1,

- Inhibits the action of histaminoliberators such as PAF or substance P.

In clinical studies, it has been shown that cetirizine begins to act 20 minutes after ingestion, its effect lasts up to 24 hours.

Pharmacokinetics:

Suction

After oral administration, the drug is rapidly absorbed from the gastrointestinal tract.

Pharmacokinetic parameters of cetirizine when used in doses from 5 to 60 mg change linearly.

Equilibrium concentration is reached after 3 days.

The pharmacokinetic profile of cetirizine is similar in adults and children.

In children, after taking cetirizine at a dose of 5 mg, the concentration of the active substance in the body is the same as in adults after taking 10 mg.

In adults, after taking cetirizine at a dose of 10 mg, the maximum concentration (Cmax) in the blood plasma is reached after 1 to 2 hours and is 350 ng / ml.

In children, after taking cetirizine at a dose of 5 mg, the maximum concentration (Cmax) in the blood plasma is reached after 1 hour and is 275 ng / ml.

When cetirizine is taken in the form of drops, maximum plasma concentrations are reached at a higher rate.

Distribution

The distribution after taking 10 mg is 35 liters in adults, and the binding to blood plasma proteins is 93%.

In children, the volume of distribution after taking 5 mg is approximately 17 liters.

A small amount of cetirizine is excreted in breast milk.

Metabolism

In adults, 60% of the dose is excreted unchanged by the kidneys.

Withdrawal

After taking 10 mg in adults, the total clearance of cetirizine is 0.60 ml / min / kg

the half-life (T?) is approximately 10 hours.

Taking multiple doses does not alter the pharmacokinetic parameters.

When taking the drug in a daily dose of 10 mg for 10 days, no cumulation of cetirizine was observed.

After the end of treatment, the level of cetirizine in the blood plasma rapidly falls below the determined limits.

Repeated allergy tests can be resumed after 3 days.

Separate patient groups

Elderly patients:

In 16 elderly persons with a single dose of the drug at a dose of 10 mg T?

was 50% higher, and the elimination rate was 40% lower compared to the control group.

The decrease in cetirizine clearance in elderly patients is probably associated with a decrease in renal function in this category of patients.

Children:

In children from 6 to 12 years old, 70% of the dose is excreted from the body unchanged by the kidneys.

After taking 5 mg in children, the total clearance of cetirizine is 0.93 ml / min / kg.

T?

in children from 6 to 12 years old it is 6 hours, from 2 to 6 years old - 5 hours, from 6 months to 2 years old - reduced to 3.1 hours.

Patients with renal impairment:

In patients with mild renal insufficiency (creatinine clearance (CC)> 50 ml / min), pharmacokinetic parameters are similar to those in healthy volunteers with normal renal function.

In patients with moderate renal failure (CC 30 - 49 ml / min) T?

is extended by 3 times, and the total clearance is reduced by 70% relative to healthy volunteers with normal renal function.

In patients on hemodialysis (CC < 7 ml / min), when the drug is taken orally at a dose of 10 mg, the total clearance decreases by approximately 70% relative to healthy volunteers with normal renal function, and T?

lengthens 3 times.

Less than 10% of cetirizine is removed by standard hemodialysis.

Patients with hepatic impairment:

In patients with chronic liver diseases (hepatocellular, cholestatic and biliary cirrhosis), with a single dose of 10 or 20 mg T?

increases by about 50% and clearance decreases by 40% compared to healthy subjects.

A dose adjustment is only necessary if the patient with hepatic impairment also has concomitant renal impairment.

Name ENG

ZODAC

ATX code

R06AE07

Dosage

cetirizine dihydrochloride 10 mg

Structure

1 ml contains:

active substance:

cetirizine dihydrochloride 10 mg

Excipients:

Methyl parahydroxybenzoate, propyl parahydroxybenzoate, glycerol, propylene glycol,

sodium saccharinate dihydrate, sodium acetate trihydrate, glacial acetic acid, water

peeled.

Indications

The use of the drug is indicated in adults and children from 6 months to relieve:

- nasal and ocular symptoms year-round (persistent) and seasonal

(intermittent) allergic rhinitis and allergic conjunctivitis:

itching, sneezing, nasal congestion, rhinorrhea, lacrimation, hyperemia

conjunctiva

- symptoms of chronic idiopathic urticaria.

Application in children from 6 to 12 months is possible only as directed by a doctor and under

strict medical supervision!

INN / Active ingredient

cetirizine dihydrochloride

Storage conditions and periods

At a temperature not higher than 25 degrees.

Expiration date: 3 years

Contraindications

hypersensitivity to cetirizine, hydroxyzine, or others

piperazine derivatives, as well as any other component of the drug

- end-stage renal failure (creatinine clearance < 10 ml / min)

- children's age up to 6 months (due to the limited data on effectiveness and

safety of use)

Specifications

Category

Allergy

Scope of the medicinal product

Respiratory system

Release form

Drops

Manufacturer country

Germany

Package quantity, pcs

one

Scope of application

Allergology

Minimum age from

6 months

Way of introduction

Through the mouth

Vacation conditions

Without recipe

Brand name

A.Nattermann & See GmbH

The amount of the dosage form in the primary package

20 ml

Primary packaging type

Bottle

Type of consumer packaging

Pack of cardboard

Anatomical and therapeutic characteristics

R06AE07 Cetirizine

Dosage form

Drops for oral administration

Expiration date in days

1095

Dosage (volume) of the substance in the preparation

1 ml (20 drops) contains cetirizine dihydrochloride 10 mg

Package weight, g

twenty

Mode of application

:

Inside.

The drug should be taken in the evening, because

symptoms become more severe

in the evening.

If necessary, Zodak® can be taken with a glass of water.

Zodak® can be taken with or without food.

Adults

10 mg (20 drops) once a day.

Alternatively, the dose can be divided into two doses (10 drops each morning and evening).

Children

Application in children from 6 to 12 months is possible only as directed by a doctor and under

strict medical supervision!

Children from 6 to 12 months

2.5 mg (5 drops) once a day.

Children from 1 to 6 years old

2.5 mg (5 drops) 2 times a day, morning and evening

The duration of treatment should not exceed 4 weeks.

Children from 6 to 12 years old

10 mg (20 drops) once a day

The duration of treatment should not exceed 4 weeks.

Alternatively, the dose can be divided into two doses (10 drops each morning and evening).

Children over 12 years old

10 mg (20 drops) once a day https://translate.google.com/translate?hl=&sl=ru&tl=en&u=https://zz.buy-pharm.com/xzxrn.html;Description

Round, biconvex film-coated tablets, yellow, with spa engraving on one side.

Pharmacodynamics

Drotaverine is an isoquinoline derivative that exhibits a potent antispasmodic effect on smooth muscle by inhibiting the type IV phosphodiesterase enzyme (PDE IV).

Inhibition of the enzyme PDE IV leads to an increase in the concentration of cAMP, inactivation of myosin light chain kinase, which further causes relaxation of smooth muscles.

The effect of drotaverine through cAMP, which reduces the concentration of Ca 2+ ions, explains the antagonistic effect of drotaverine in relation to Ca 2+ ions.

In vitro, drotaverine inhibits the PDE IV enzyme without inhibiting the PDE III and PDE V enzymes.

Therefore, the effectiveness of drotaverine depends on the concentrations of PDE IV in different tissues.

PDE IV is most important for suppressing the contractile activity of smooth muscles, and therefore selective inhibition of PDE IV may be useful for the treatment of hyperkinetic dyskinesias and various diseases accompanied by a spastic state of the gastrointestinal tract.

Hydrolysis of cAMP in the myocardium and vascular smooth muscle occurs mainly with the help of the enzyme PDE III, which explains the fact that with high spasmolytic activity, drotaverine does not have serious side effects from the heart and blood vessels and pronounced effects on the cardiovascular system.

Drotaverine is effective for smooth muscle spasms of both neurogenic and muscular origin.

Regardless of the type of autonomic innervation, drotaverine relaxes the smooth muscles of the gastrointestinal tract, biliary tract, and the genitourinary system.

Due to its vasodilating effect, drotaverine improves tissue blood supply.

Thus, the above-described mechanisms of action of drotaverine eliminate smooth muscle spasm, which leads to a decrease in pain.

Pharmacokinetics

Absorption

Compared with papaverine, when taken orally, drotaverine is absorbed faster and more completely from the gastrointestinal tract.

After presystemic metabolism, 65% of the taken dose of drotaverine enters the systemic circulation.

The maximum concentration (C max) of drotaverine in the blood plasma is reached after 45-60 minutes.

Distribution

In vitro, drotaverine has a high binding to plasma proteins (95-98%), especially albumin,?

and? - globulins.

Drotaverine is evenly distributed in tissues, penetrates into smooth muscle cells.

Does not penetrate the blood-brain barrier.

Drotaverine and / or its metabolites can slightly penetrate the placental barrier.

Metabolism

Drotaverine is almost completely metabolized in the liver.

Withdrawal

The half-life of drotaverine is 8-10 hours.

Within 72 hours, drotaverine is almost completely excreted from the body.

About 50% of drotaverine is excreted by the kidneys and about 30% through the gastrointestinal tract.

Drotaverine is mainly excreted in the form of metabolites, the unchanged form of drotaverine is not found in urine.

Name ENG

NO-SPA

Clinical and pharmacological group

Myotropic antispasmodic

ATX code

A03A D02

Dosage

drotaverine hydrochloride - 40 mg

Structure

1 tablet contains:

active substance: drotaverine hydrochloride - 40 mg

excipients: magnesium stearate, talc, povidone K-25, corn starch, lactose

monohydrate, opadry II 85G32431 yellow.

Indications

Spasms of smooth muscles in diseases of the biliary tract: cholecystolithiasis,

cholangiolithiasis, cholecystitis, pericholecystitis, cholangitis, papillitis.

- Spasms of smooth muscles of the urinary tract: nephrolithiasis, urethrolithiasis, pyelitis,

cystitis, bladder spasms.

As adjunctive therapy

- With spasms of smooth muscles of the gastrointestinal tract: peptic ulcer

stomach and duodenum, gastritis, spasms of the cardia and pylorus, enteritis,

colitis, spastic colitis with constipation, irritable bowel syndrome with flatulence.

- With tension headaches.

- With dysmenorrhea (menstrual pain).

Storage conditions and periods

At a temperature of 15-25 degrees. (In the original packaging) - bottles

at a temperature not higher than 25 degrees.

- blisters.

Expiration date: 3 years

5 years - vials

INN / Active ingredient

drotaverine hydrochloride

Contraindications

Hypersensitivity to the active substance or to any of

excipients of the drug.

- Severe hepatic or renal impairment.

- Severe heart failure (low cardiac output syndrome).

- Children under 6 years old.

- Breastfeeding period (lack of clinical data).

- Hereditary galactose intolerance, lactase deficiency and malabsorption syndrome

glucose-galactose (due to the presence of lactose monohydrate in the preparation).

Carefully

- With arterial hypotension.

- In children (lack of clinical experience of use).

- In pregnant women (see the section "Use during pregnancy and breastfeeding

feeding ").

Specifications

Category

Pain relievers

Scope of the medicinal product

General

Release form

Tablet

Manufacturer country

Hungary

Package quantity, pcs

24

Scope of application

Gastroenterology

Minimum age from

6 years

Way of introduction

Through the mouth

Vacation conditions

Without recipe

Brand name

Sanofi

The amount of the dosage form in the primary package

24 pcs.

Primary packaging type

Blister

Type of consumer packaging

Pack of cardboard

Pharmaco-therapeutic group

Antispasmodic

Anatomical and therapeutic characteristics

A03AD02 Drotaverin

Dosage form

Pills

Expiration date in days

1095

Dosage (volume) of the substance in the preparation

40 mg

The target audience

Children

Package weight, g

ten

Mode of application

:

Adults

1-2 tablets at a time 2-3 times a day.

The maximum daily dose is 6 tablets (which

corresponds to 240 mg).

Children

Clinical studies on the use of drotaverine in children have not been conducted.

In the case of the appointment of drotaverine to children:

- from 6 to 12 years: 1 tablet at a time, 1-2 times a day.

Maximum daily dose - 2

tablets (corresponding to 80 mg)

- over 12 years old: 1 tablet at one time 1-4 times a day or 2 tablets at one time 1-2

once a day.

The maximum daily dose is 4 tablets (corresponding to 160 mg).

When taking the drug without consulting a doctor, the recommended duration of administration

the drug is usually 1-2 days.

In cases where drotaverine is used as

auxiliary therapy, the duration of treatment without consulting a doctor may be

more (2-3 days).

If pain persists, the patient should see a doctor.

Information on technical characteristics, delivery set, country of manufacture "