Remestip (terlipressin acetate) solution for injections 0.1 mg/ml. ampoules 2 ml. №5

Description

Remestip (terlipressin acetate) solution for injections 0.1 mg/ml. ampoules 2 ml. №5

Composition

active substance: terlipressin acetate;

1 ml of solution contains terlipressin 0.1 mg in the form of terlipressin acetate;

excipients: sodium chloride; acetic acid; sodium acetate, trihydrate; water for injections.

Medicinal form

Solution for injection.

Main physicochemical properties: transparent colorless solution without mechanical inclusions.

Pharmacotherapeutic group

Hormones of the posterior lobe of the pituitary gland. Vasopressin and analogues.
ATX code H01B A04.

Pharmacological properties

Terlipressin (N-triglycyl-8-lysine-vasopressin) is a synthetic analogue of vasopressin, a natural hormone of the posterior lobe of the pituitary gland, which differs from it in the substitution of arginine for lysine in the 8th position, as well as in the fact that three glycine residues are attached to the terminal amino group of cysteine . The pharmacological effect of terlipressin consists in the combination of the specific effect of substances formed as a result of its enzymatic cleavage. Marked effects of terlipressin are pronounced vasoconstrictor and antihemorrhagic. The most noticeable effect in this regard is a decrease in blood circulation in the parenchyma of internal organs, as a result of which hepatic blood flow and pressure in the portal vein system decrease.

Pharmacodynamic studies have shown that terlipressin, like similar peptides, causes spasm of arterioles, veins and venules mainly in the parenchyma of internal organs, contraction of the smooth muscles of the esophagus wall, increase in tone and peristalsis of the intestines in general.

In addition to the effect on the smooth muscles of the vessels, terlipressin stimulates the smooth muscles of the uterus, including in the absence of pregnancy.

Indication  

Bleeding of the digestive tract and urogenital tract, such as bleeding from varicose veins of the esophagus, gastric and duodenal ulcers; uterine bleeding due to functional disorders or other causes, childbirth, abortion, etc .; bleeding associated with surgery, particularly on the abdominal cavity and pelvis.
Topically – during gynecological interventions on the cervix.

Contraindication

Hypersensitivity to the active substance or to any of the excipients. Septic shock in patients with low cardiac output. Pregnancy.

Dosing and administration:

• Initially, give 2 mg of terlipressin intravenously every 4 hours. Treatment should be continued until 24 hours after the bleeding has stopped, but no longer than 48 hours. After the initial dose, the dose can be adjusted up to 1 mg intravenously every 4 hours for patients weighing <50 kg or in case of adverse reactions.
• Bleeding from varicose veins of the esophagus in adults: 1 mg (1000 mcg) every 4−6 hours for 3-5 days. To prevent recurrence of bleeding, treatment should be continued for 24-48 hours after cessation. The drug is administered intravenously bolus or as a short-term infusion. The drug is used undiluted or diluted with 0.9% sodium chloride solution.
• Other types of gastrointestinal bleeding in adults: 1 mg (1000 mcg) every 4-6 hours. The drug can also be used as a first aid regardless of surgery, if there is a suspicion of bleeding from the upper digestive tract.
• Bleeding from internal organs in children: usually administered at a dose of 8 to 20 μg / kg body weight with an interval of 4-8 hours. The drug should be administered throughout the bleeding period; the general recommendation is to continue the administration to prevent recurrence of bleeding in the same way as in the case of adult bleeding. In the presence of sclerosed varicose nodes of the esophagus appoint a single injection at a dose of 20 μg / kg body weight bolus.
• Genitourinary bleeding: due to the difference in the activity of endopeptidases in blood plasma and tissues, the dosage range is quite wide – from 0.2 to 1 mg, which is prescribed with an interval of 4-6 hours.
• For juvenile uterine bleeding, the recommended dose is from 5 to 20 μg / kg body weight. The drug should be administered intravenously.
• Topical use for gynecological interventions on the cervix: 0.4 mg (400 mcg) is diluted with 0.9% sodium chloride solution to a volume of 10 ml, used intracervically and / or paracervically. In this case, the effect of the drug develops in 5-10 minutes. If necessary, the dose can be increased or re-assigned.

Children

The drug is used to treat children according to the recommended scheme.

Overdose

The recommended dose should not be exceeded (2 mg for 4 hours) due to the fact that the risk of severe cardiovascular side effects is dose-dependent.
150 mg of clonidine intravenously can be used to control hypertension that may develop during treatment with Remestip.
Atropine is administered to relieve bradycardia.

Side effects:

• Cardiac disorders: bradycardia; atrial fibrillation, ventricular arrhythmias, tachycardia, chest pain, myocardial infarction, fluid overload with pulmonary edema, heart failure.
• Vascular disorders: narrowing of peripheral blood vessels, peripheral ischemia, pale skin, hypertension; intestinal ischemia, peripheral cyanosis, hot flushes.
• Disorders of the respiratory system, chest and mediastinum: respiratory distress, respiratory failure; dyspnea.
• Digestive system disorders: transient diarrhea, transient spastic abdominal pain; transient nausea, transient vomiting.
• Nervous system disorders: headache.
• Metabolic disorders: hyponatremia, if fluid balance is not controlled.
• Skin and subcutaneous tissue disorders: local skin necrosis.
• Pregnancy, childbirth and perinatal conditions: impaired contractile activity of the uterus, decreased uterine blood flow.
• General disorders and administration site conditions: injection site necrosis.