DOLOPROKT

Active material: Fluocortolone, Lidokain
When ATH: C05AX03
CCF: The drug with anti-inflammatory and Valium action for local application in a proctology
ICD-10 codes (testimony): I84, K62.8, L20.8
When CSF: 04.04.05
Manufacturer: INTENDIS GmbH (Germany)

Pharmaceutical form, composition and packaging

Rectal Suppositories yellowish-white, torpedo-shaped, with smooth surface.

Excipients: fat solid (Vitepsol W35).

5 PC. – strips of aluminum foil (1) – packs cardboard.
5 PC. – strips of aluminum foil (2) – packs cardboard.
6 PC. – strips of aluminum foil (1) – packs cardboard.
6 PC. – strips of aluminum foil (2) – packs cardboard.

Rectal cream white, opaque.

Excipients: sodium hydrogen phosphate dodecahydrate, disodium эdetat, sodium dihydrogen phosphate dihydrate, benzyl alcohol, sorbitan stearate, polysorbate 60, cetostearyl alcohol, Liquid paraffin, white petrolatum, Purified water.

10 g – aluminum tuba (1) complete with an applicator – packs cardboard.
15 g – aluminum tuba (1) complete with an applicator – packs cardboard.
30 g – aluminum tuba (1) complete with an applicator – packs cardboard.
50 g – aluminum tuba (1) complete with an applicator – packs cardboard.

Pharmacological action

The drug with anti-inflammatory and Valium action for local application in a proctology.

Fluocortolone – GCS, when exposed to the skin prevents accumulation of neutrophils boundary, It decreases the production of lymphokines and inhibition of macrophage migration, helping to reduce infiltration processes, exudation and granulation. Suppresses inflammatory and allergic skin reactions, and facilitates itching, burning and pain; reduces the dilation of the capillaries, interstitial edema and infiltration of tissues.

Lidokain – mestnый anesthetic; pain relief is achieved by suppressing the formation of nerve impulses and the afferent nerve fibers by depolarization sodium channels.

Pharmacokinetics

Local therapeutic effect is achieved with a low level of active components in plasma.

FLUOCORTOLONE pivalate

Absorption

After a single application 1 g cream or rectal administration 1 rectal suppository, absorption maximum was fluocortolone pivalate 5% by application or administration of the preparation.

When administered daily for 2 suppozitoriâ 3 times / day for 4 weeks fluocortolone content in blood plasma did not reach, have systemic effects.

Metabolism

Fluocortolone pivalate is hydrolyzed by esterases enzymes and inflammatory focus to form fluocortolone, 11-ketofluokortolona and pivalic acid.

Deduction

T_1/2 fluocortolone and its metabolites after rectal administration is about 1.3 and 4 h, respectively. Fluocortolone excreted as metabolites predominantly in the urine.

Lidokain

Absorption

Absorption and bioavailability after rectal administration of lidocaine cream and suppository is about 30% and 24% respectively.

Metabolism and excretion

Lidocaine is metabolized by oxidative N-dealkylation, hydrolysis of the amide bond and hydroxylation of the aromatic ring to form a 4-hydroxy-2,6-xylidine, which is the major metabolite. With urine output 70% preparation in the form of metabolita.T_1/2 is 1-2 no.

Testimony

- Hemorrhoids;

- Proctitis;

- Eczema of the anus (rectal cream).

Dosage regimen

Doloprokt recommended after defecation. Before using the drug should carry out hygiene anus (anus).

The duration of treatment should not exceed 2 of the week.

Rectal cream should be applied 2 times / day (in the morning and in the evening). In the first days of treatment cream can be applied 3 times / day. As the relief of symptoms is often sufficient to use the drug 1 time / day.

Forcing your finger on the small amount of cream (about the size of a pea), lubricate the area around the anus and inside the anal ring. To overcome the resistance of the sphincter is necessary to apply the cream with a fingertip.

For the introduction of the cream into the rectum must be screwed into a tube attached applicator and put it into the anus. Then, gently pressing down on the tube, squeeze a small amount of cream into the rectum.

Rectal Suppositories (by 1 PC.) injected deep into the anus 2 times / day, in the morning and in the evening, However, a severe form of the disease in the first 3 day administered by 1 suppozitoriû 3 times / day. At steady improvement in many cases it is enough to be administered 1 suppository / day or every other day.

However, the highly inflamed and, Consequently, painful hemorrhoids, it is recommended to start treatment with a cream. Speakers hemorrhoids should be liberally lubricated cream, vpravlyaya them back gently with your finger.

Side effect

In long-term treatment (more than 4 weeks) there is a risk of local skin changes, such as atrophy, Stretch or teleangiэktazii.

Local reactions: burning sensation (1-10%); rarely – irritation and allergic reactions (0.1-1%).

Contraindications

- Tuberculosis and syphilitic processes in the area of ​​application of the drug;

- Viral diseases (eg, enable vetryanaya, response to vaccination, shingles) in the field of application of the drug;

- I trimester of pregnancy;

- Hypersensitivity to the drug.

Treatment of children and adolescents is not recommended, due to the lack of data on clinical trials.

Pregnancy and lactation

Epidemiological studies suggest a possible increased risk of cleft palate in newborns, whose mothers received corticosteroids into the I trimester of pregnancy. Data on the use of local corticosteroids during pregnancy accumulated enough, however, in this case, the probability of adverse effects are very low due to minimal bioavailability corticosteroids for topical application.

Doloprokt be used with caution during pregnancy. In the appointment of pregnant and lactating women must be weighed the expected benefits of treatment for mother and possible risk to the fetus and infant.

The appointment of the drug during pregnancy and lactation should be short-lived.

Cautions

In the presence of fungal infections, in addition to Doloproktu require appropriate antifungal therapy.

Avoid getting into Doloprokta or eye contact. After applying the cream is recommended to wash hands.

Effects on ability to drive vehicles and management mechanisms

Not found.

Overdose

If you accidentally taking the drug orally (eg, ingestion of a few grams of a cream or more than one suppository) the most severe symptoms can occur with the cardiovascular system (inhibition of the function of the heart, cardiac arrest) and CNS (convulsions, respiratory depression, respiratory arrest) dose dependent.

Drug Interactions

Patients, receiving antiarrhythmic drugs, Doloprokt should use the drug with caution, considering, that the product contains lidocaine. With simultaneous application of lidocaine with antiarrhythmic drugs may prolong the QT interval and, In very rare cases, possible development of AV-block or ventricular fibrillation.

Conditions of supply of pharmacies

The drug is released under the prescription.

Conditions and terms

The drug should be stored out of reach of children at or above 30 ° C. Shelf life rectal cream – 3 year, rectal suppositories – 4 year.