Propitsil - instructions for use, dose, side effects, contraindications

Active substancePropylthiouracilPropylthiouracil

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Dosage form: & nbsppills

Composition:

1 tablet contains:

active substance:
propylthiouracil	50.0 mg
Excipients:
lactose monohydrate	73.9 mg
corn starch	50.0 mg
colloidal silicon dioxide	1.5 mg
povidone	4.0 mg
corn starch pregelatinized starch	10.0 mg
magnesium stearate	0.6 mg

Description:White round biconvex tablets with separating risk.

Pharmacotherapeutic group:antithyroid agent

ATX: & nbsp

H.03.B.A Thiouracil derivatives

H.03.B.A.02 Propylthiouracil

Pharmacodynamics:

Thiouracils act as antithyroid agents that suppress the system of intracythroide peroxidase. They reduce the process of iodination of thyroglobulin and, accordingly, inhibits the formation of thyroxin. In addition, in the molecules of thyroglobulin, the formation of paired bonds between tyrosyl residues already bound to iodine is disrupted. Propylthiouracil contributes to the depletion of iodine in the thyroid gland. Propylthiouracil inhibits the transformation of thyroxine into triiodothyronine in peripheral tissues.

Pharmacokinetics:

Propylthiouracil is well absorbed when administered orally, reaching a peak in the blood plasma 1-2 hours after ingestion.

Antithyroid drugs are concentrated in the thyroid gland by active transfer. Although Propylthiouracil may not be detected in the blood serum after 8 hours after administration, the time of action of a high single dose is from 6 to 8 hours due to pronounced accumulation in the thyroid gland.

The biological availability for oral administration is about 80%.

Indications:

- Thyrotoxicosis in patients with diffuse toxic goiter or toxic adenoma of the thyroid gland;

- preoperative preparation with thyrotoxicosis for resection of the thyroid gland and postoperative therapy;

- Preparation of patients with thyrotoxicosis for treatment with radioactive iodine.

Contraindications:

- Severe side effects (agranulocytosis, severe liver dysfunction) with the previous treatment with propylthiouracil;

- Lactose deficiency, lactose intolerance, glucose-galactose malabsorption;

- hypersensitivity to the drug;

- Lakopenia;

- hypothyroidism;

active hepatitis.

Pregnancy and lactation:

When used during pregnancy, it is necessary to correlate the potential benefit for the mother with the possible risk to the fetus and the baby.

Both thyrotoxicosis and hyperthyroidism in pregnant women are associated with an increase in the incidence of miscarriages, stillbirths and developmental abnormalities.The frequency of developmental abnormalities in cases of treatment with propylthiouracil does not differ from the frequency of spontaneous developmental abnormalities.

The dose of propicil should be as low as possible to avoid miscarriage, as well as the development of hypothyroidism and goiter in the fetus. In the last three months of pregnancy, spontaneous decrease in the expression of thyrotoxicosis is often observed.

Treatment of pregnant women with an antithyroid drug should be done under strict supervision. The concentration of free thyroid hormones should be at the upper limit of the norm, and the concentration of thyrotropic hormone (TSH) should be low enough or not be determined.

In case of diffuse toxic goiter during pregnancy, propicil is prescribed without additional intake of levothyroxine sodium.

During breastfeeding, Propitsil is considered the drug of choice, since its concentration in breast milk is only one-tenth of the concentration in the mother's blood serum. Nevertheless, careful monitoring of the newborn is required, since there are reports of individual cases of hypothyroidism.

Dosing and Administration:

Propitsil taken inside every 6-8 hours.Tablets should be swallowed whole, not liquid and squeezed with a sufficient amount of liquid.

Adults, teenagers and children over 10 years of age. At the beginning of treatment, adults and children over 10 years of age are prescribed 75-100 mg (1.5-2 tablets) per day. The maintenance dose is 50 to 150 mg (1 to 3 tablets) per day. In severe cases and after the previous loading with iodine, the initial daily dose is increased to 300-600 mg (6-12 tablets per day, divided into 4-6 single doses).

Children aged 6 to 10 years PThey receive 50-150 mg (1-3 tablets) a day at the beginning of treatment, and about 25-50 mg (0.5-1 tablet) a day with maintenance treatment.

Children under 3 years the preparation is dissolved in water to a fine suspension, which is prepared immediately before administration.

With hyperthyroidism in newborns prescribe 5-10 mg per 1 kg of body weight per day (the daily dose is divided into 3 doses). If there is no response to treatment, a 50-100% dose increase is recommended. The maintenance dose is 3-4 mg per 1 kg of body weight per day. In accordance with the half-life of the maternal immunoglobulin in 2-3 months, spontaneous restoration of the thyroid gland functions can be expected.

To old people a lower dose is recommended.

According to the existing data in patients with renal insufficiency or on hemodialysis there is no need to adjust the dose.

With liver diseases the drug can be used in recommended doses, taking into account the appropriate contraindications.

The duration of treatment is determined by the individual need of the patient. The experience of the therapeutic use of the drug Propitsil shows that the duration of treatment of thyrotoxicosis with diffuse toxic goiter and toxic adenoma of the thyroid gland should be 1.5-2 years.

When preparing for surgery or treatment with radioactive iodine The duration of application of the drug should correspond to the individual needs of the patient.

Propitsil can be used to treat diffuse toxic goiter both in the form of monotherapy, and in the scheme "block-replace" in combination with levothyroxine sodium.

Side effects:

Agranulocytosis is a severe but rare side effect, accompanied by septic complications. Sometimes there are rashes on the skin, hives, pain in the stomach, arthralgia without signs of joint inflammation, the formation of goiter in a newborn.

In very rare cases and, above all, with application of the drug in high doses, the following side effects were observed: liver damage (hepatocellular necrosis, transient cholestasis), hypersensitivity reactions, drug fever, lymphadenopathy and thrombocytopenia.

There are reports of isolated cases of neuromuscular disorders, polyarthritis, disorders of taste sensitivity and smell, vasculitis, lupus-like syndrome, loss of hearing, nodular periarteritis, gastrointestinal disorders (nausea, vomiting), dizziness, disturbances in erythropoiesis, hemolysis, Coombs positive reactions , interstitial pneumonia, asthma, peripheral edema and alopecia.

In the process of treatment with propitsilom there can be an increase in the thyroid gland.

Agranulocytosis, liver failure and vasculitis are potentially life-threatening conditions, thus requiring careful medical supervision of the patient.

Overdose:

Cases of acute intoxication Propitsil not observed.

Chronic overdose leads to the development of goiter and hypothyroidism with symptoms that are dependent on the severity of hypothyroidism due to the specific effect of the antithyroid agent.

Treatment. There are no special measures / activities.The efficacy of gastric lavage and endoscopic removal of tablet residues is highly questionable due to the rapid absorption of the active substance.

With the development of goiter and hypothyroidism, accompanied by symptoms that correlate with the severity of hypothyroidism, and caused by a chronic overdose of the drug Propitsil, treatment with the drug is discontinued. Substitution therapy with levothyroxine sodium is carried out if this is justified by the severity of hypothyroidism or goiter.

As a rule, after the cancellation of Propitsil, spontaneous restoration of thyroid function is expected.

Interaction:

In the event that treatment with propylthiouracil is carried out according to the "block and replace" scheme in combination with levothyroxine sodium, the dose of propylthiouracil should be increased.

The thyostatic effect of propylthiouracil may decrease with simultaneous or previous use of iodine-containing drugs or radiopaque substances.

In connection with the ability of propylthiouracil to affect the effect of free active fractions of propranolol and coumarin derivatives, an additional dose adjustment of these drugs may be required.

Myelotoxic drugs increase the manifestation of hematotoxicity of the drug.

Special instructions:

Agranulocytosis can develop within a few hours. Since in most cases the development of agranulocytosis can not be predicted even with constant monitoring of the morphological picture of the blood, the patient must be is informed of the clinical symptoms of agranulocytosis (fever, malaise, tonsillar tonsillitis, stomatitis) and the need for immediate examination of the blood picture.

Before starting treatment with Propitsil, a complete blood test is necessary. During treatment with an antithyroid agent, the functional state of the thyroid gland (determination of the concentration of thyroid hormones and / or blood TSH) is necessary.

Treatment with too high doses of an antithyroid agent leads to the appearance or increase of an already existing goiter. This should be borne in mind primarily with the chest or intrathoracic goiter, which is associated with the danger of squeezing the anatomical structures in the mediastinum.

With a pathological change in the number of blood elements and an increase in the activity of transmissions, Propitsil can only be used under the strict supervision of a physician.

Effect on the ability to drive transp. cf. and fur:No.

Form release / dosage:Tablets, 50 mg.

Packaging:

For 20 or 100 tablets in a glass bottle.

The bottle together with the instruction for use is placed in a cardboard box.

Storage conditions:

In a dry, the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

5 years.

Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:П N011863 / 01

Date of registration:16.06.2011

The owner of the registration certificate:Admeda Arzneimittel GmbHAdmeda Arzneimittel GmbH Germany

Manufacturer: & nbsp

HAUPT PHARMA BERLIN GmbH Germany

Representation: & nbspLEX CJSCLEX CJSCRussia

Information update date: & nbsp05.09.2015

Illustrated instructions

Instructions

Propitsil® (Propicil®)