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Instruction for use: Granisetron (Granisetronum)

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Pharmacological group

Antiemetics

Serotonergic drugs

Nosological classification (ICD-10)

R11 Nausea and vomiting

Postoperative vomiting, Nausea, vomiting, Vomiting in the postoperative period, Vomiting drug, Vomiting on the background radiation therapy, Vomiting indomitable, Vomiting with radiation therapy, persistent vomiting, anacatharsis, Postoperative nausea, Vomiting during chemotherapy, Vomiting of central origin, Vomiting on the background of cytostatic chemotherapy, persistent hiccups, repeated vomiting

Y43.1 Adverse reactions in the therapeutic use of anticancer antimetabolites

Mercaptopurine Treatment

Y43.2 Adverse reactions in the therapeutic use of natural anticancer drugs

Y43.3 Adverse reactions in the therapeutic use of other anticancer drugs

Z100 * CLASS XXII Surgical practice

Abdominal surgery, adenomectomy, Amputation, Coronary angioplasty, Angioplasty of the carotid arteries, Antiseptic skin treatment for wounds, Antiseptic Hand, Appendectomy, atherectomy, Balloon coronary angioplasty, Vaginal hysterectomy, The coronary bypass, Interventions in the vagina and cervix, Interventions on the bladder, Intervention in the mouth, Restoration and reconstructive surgery, Hand hygiene of medical personnel, Gynecologic surgery, Gynecological intervention, Gynecological surgery, Hypovolemic shock during operations, Disinfection of purulent wounds, Disinfection of wounds edges, Diagnostic intervention, Diagnostic procedures, Cervical Diathermocoagulation, Long-surgery, Replacing the fistula catheters, Infection in orthopedic surgery, Artificial heart valve, cystectomy, Short-term outpatient surgery, Short-term operation, Short surgical procedures, Krikotireotomiya, Blood loss during surgery, Bleeding during surgery and in the postoperative period, Kuldotsentez, laser photocoagulation, laser coagulation, retinal laser coagulation, Laparoscopy, Laparoscopy in Gynecology, CSF fistula, Small gynecological operations, Small surgical procedures, Mastectomy and subsequent plastic, mediastinotomy, Microsurgical operations on the ear, Mukogingivalnye operation, suturing, Minor surgery, neurosurgical operation, Immobilization of the eyeball in ophthalmic surgery, testectomy, pancreatectomy, Perikardektomiya, The period of rehabilitation after surgery, The period of, convalescence after surgery, Percutaneous transluminal coronary angioplasty, Pleural thoracentesis, Pneumonia postoperative and posttraumatic, Preparation for surgical procedures, Preparation for surgery, Preparation of the surgeon's hands before surgery, Preparation of the colon for surgical procedures, Postoperative aspiration pneumonia in neurosurgical and thoracic surgery, Postoperative nausea, Postoperative bleeding, postoperative granuloma, postoperative shock, The early postoperative period, myocardial revascularization, Radiectomy, gastric Resection, bowel resection, uterine Resection, liver Resection, enterectomy, Resection of part of the stomach, Reocclusion of the operated vessel, Bonding tissues during surgical procedures, Removal of sutures, Condition after eye surgery, Condition after surgery, Condition after surgery in the nasal cavity, Condition after gastrectomy, Status after resection of the small intestine, Condition after tonsillectomy, Condition after removal of the duodenum, Condition after phlebectomy, Vascular surgery, Splenectomy, Sterilization of surgical instruments, Sterilization of surgical instruments, sternotomy, Dental surgery, Dental intervention in periodontal tissues, strumectomy, Tonsillectomy, Thoracic surgery, total gastrectomy, Transdermal intravascular coronary angioplasty, Transurethral resection, Turbinektomiya, Removal of a tooth, cataract surgery, Removal of cysts, tonsillectomy, Removal of fibroids, Removing the mobile primary teeth, Removing polyps, Removing broken tooth, Removal of the uterus body, Removal of sutures, Urethrotomy, Fistula likvoroprovodyaschih ways, Frontoetmoidogaymorotomiya, Surgical infection, Surgical treatment of chronic limb ulcersm, Surgery, The surgery in the anal area, The surgery on the colon, Surgical practice, The surgical procedure, Surgical interventions, Surgery on the gastrointestinal tract, Surgical procedures on the urinary tract, Surgical procedures on the urinary system, Surgical intervention of the genitourinary system, Surgical procedures on the heart, Surgical manipulation, surgery, Surgery on the veins, Surgical intervention, Vascular surgery, Surgical treatment of thrombosis, cholecystectomy, Partial gastric resection, transabdominal hysterectomy, Percutaneous transluminal coronary angioplasty, Percutaneous transluminal angioplasty, Coronary artery bypass, tooth Extirpation, Extirpation of milk teeth, pulpectomy, pulsative cardiopulmonary bypass, tooth Extraction, teeth Extraction, cataract extraction, Electrocoagulation, endourological intervention, episiotomy, Etmoidotomiya, Complications after tooth extraction

Z51.0 Course of Radiotherapy

Supplement to external radiation therapy, Local X-ray irradiation, Radiation therapy, Brain edema associated with radiation therapy, Lesion in radiation therapy, Radiotherapy

Z51.1 Chemotherapy for neoplasm

Cystitis hemorrhagic, caused by cytostatics, Urotoxicity of cytostatics

Code CAS

109889-09-0

Characteristic

Granisetron hydrochloride is a white powder. Soluble in aqueous or salt solutions at 20 ° C. Molecular weight of 348.9.

Pharmacology

Pharmacological action - antiemetic, serotonergic.

Selectively blocks serotonin 5-HT3 receptors located in the endings of the vagus nerve and in the trigger zone of the bottom of the fourth ventricle of the brain (practically does not affect other serotonin receptors). Well absorbed in the digestive tract (if there is no vomiting). Associated with plasma proteins by 65%. In the liver it undergoes N-demethylation and oxidation of the aromatic ring, after which it conjugates. The resulting metabolites have antiserotonin activity. T1 / 2 in oral and in / in the introduction of 9 hours, with a wide individual variability. The main route of excretion is with bile, about 12% (after IV injection) is excreted in the urine within 48 hours. Eliminates vomiting that occurs when the parasympathetic nervous system is excited due to the release of serotonin from enterochromaffin cells.

Indications

Nausea, vomiting (symptomatic therapy and prevention in the treatment of cytostatics and radiation therapy, after surgery).

Contraindications

Hypersensitivity, breastfeeding.

Restrictions for use

Partial intestinal obstruction (weakens the motility of the distal colon), pregnancy; children's age up to 12 years (for tablets), up to 2 years (for injection forms) - the efficacy and safety of use have not been established.

pregnancy and lactation

Category of action on the fetus by the FDA - B.

At the time of treatment should stop breastfeeding (data on the penetration into breast milk are not available).

Side Effects

On the part of the digestive tract organs: abdominal pain, constipation or diarrhea, flatulence, increased activity of hepatic transaminases (ALT, AST), dyspepsia; rarely - heartburn, a change in taste.

From the nervous system: headache, insomnia, drowsiness, excessive fatigue or weakness; rarely - anxiety, anxiety, dizziness.

Since the cardiovascular system: arrhythmia, chest pain, decrease or increase in blood pressure.

Allergic reactions: skin rash, hyperthermia, bronchospasm, urticaria, itching; rarely, hypersensitivity reactions.

Other: very rarely - flu-like syndrome.

Interaction

Pharmaceutical incompatible with other drugs. Granisetron does not affect the activity of cytochrome P450 CYP3A4 isoenzymes (responsible for the metabolism of some narcotic analgesics). The effectiveness of granisetron can be enhanced with intravenous dexamethasone (8–20 mg) prior to the start of chemotherapy. Special studies on the interaction with the means for general anesthesia have not been conducted, but granisetron is well tolerated when administered concurrently with similar drugs and narcotic analgesics. With the induction of hepatic enzymes with phenobarbital, an increase in the clearance of granisetron (with i / v administration) was observed by about a quarter. There was no interaction with the simultaneous appointment with benzodiazepines, anti-ulcer drugs and other cytotoxic drugs that cause vomiting.

Overdose

Symptoms: the use of 38 mg granisetron in the form of a single IV injection was not accompanied by the development of serious undesirable effects, except for a light headache.

Treatment: symptomatic therapy. The specific antidote is not known.

Route of administration

In / in, inside.

Precautions

Since granisetron can reduce intestinal motility, patients with signs of partial obstruction of the intestine after administration of the drug should be under the supervision of a physician.

During treatment, it is necessary to control the activity of ALT and AST.

For the treatment and prevention of postoperative nausea and vomiting in children does not apply.

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