Bleeding of the digestive tract and genitourinary tract, such as bleeding from varicose veins of the esophagus , stomach and duodenal ulcers; uterine bleeding due to functional disorders or other causes, childbirth, abortion , etc.; bleeding associated with surgical interventions, in particular on the abdominal and pelvic organs. Locally – for gynecological interventions on the cervix.
active substance: terlipressin acetate;
1 ml of solution contains 0.1 mg of terlipressin in the form of terlipressin acetate;
excipients: sodium chloride; acetic acid; sodium acetate, trihydrate; water for injections.
Solution for injection.
Pharmacological properties Remestip
Terlipressin (N-triglycyl-8-lysine-vasopressin) is a synthetic analogue of vasopressin, a natural hormone of the posterior pituitary gland, which differs from it by replacing arginine in the 8th position with lysine, as well as the fact that three glycine residues are attached to the terminal amino group . The pharmacological action of terlipressin is a combination of the specific effect of substances formed as a result of its enzymatic cleavage. Notable 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 the internal organs, resulting in reduced hepatic blood flow and pressure in the portal vein.
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 smooth muscles of the esophageal wall, increased tone and peristalsis of the intestine in general.
In addition to affecting vascular smooth muscle, terlipressin stimulates uterine smooth muscle, including in the absence of pregnancy.
According to studies of the drug in animals and humans, its maximum activity was observed in the internal organs and skin.
No clinical manifestations of the antidiuretic effect of terlipressin were detected.
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.
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.
The drug is used to treat children according to the recommended scheme.
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.
- 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.
Storage conditions Remestip
Store in a refrigerator (+ 2 to + 8 ° C) in the original package.
Do not freeze.
For 1 month, the drug can be stored at temperatures up to 25 ° C (for example, in an ambulance).
Keep out of reach of children.