Composition, form of production and packaging
Concentrate for solution for infusion 1 ml 1 amp.
nitroglycerin 1 mg 10 mg
Excipients: propylene glycol, dextrose, water d / u.
10 ml - ampoules (5) - packings, cell planimetric (2) - cardboard boxes.
Concentrate for solution for infusion 1 ml 1 fl.
nitroglycerin 1 mg 50 mg
Excipients: propylene glycol, dextrose, water, hydrochloric acid (to maintain the pH level).
50 ml - bottles (1) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the print edition of 2007.
PHARMACHOLOGIC EFFECT
Peripheral vasodilator of a group of nitrates. It causes a relaxation of the tone of the smooth muscles of the vessels, especially the venules and veins. When IV introduction leads to a rapid decrease in preload due to the expansion of peripheral veins. Reduces the flow of blood to the right atrium, helps reduce pressure in a small circle of blood circulation, reduces afterload, the need for myocardium in oxygen. Promotes the redistribution of coronary blood flow to the ischemic subendocardial areas of the myocardium.
When heart failure helps discharge the myocardium mainly by reducing the preload, it also reduces pressure in the small circle of the circulation.
PHARMACOKINETICS
Data on the pharmacokinetics of the preparation of Perlinganit are not available.
INDICATIONS
- Angina pectoris (including unstable angina, angiospastic angina pectoris);
acute myocardial infarction;
acute left ventricular failure;
- hypertensive crisis with cardiac decompensation;
- Controlled hypotension during surgical interventions.
DOSING MODE
Depending on the clinical and hemodynamic parameters, the dose is selected individually for each patient. When used in a hospital setting, treatment should be started at a dose of 0.5-1 mg / h, and if necessary, the dose is gradually increased. The maximum dose is 8-10 mg / h.
In severe angina, the dose is 2-8 mg / h (33-133 Ојg / min). During the infusion it is necessary to constantly monitor central and intracardiac hemodynamics.
In acute left ventricular failure (pulmonary edema), 2-8 mg / h (33-133 Ојg / min) is prescribed for 1-2 days.
With hypertensive crisis with cardiac decompensation under constant control of blood pressure and heart rate, infusion is carried out at a rate of 2-8 mg / h (an average of 5 mg / h).
With controlled hypotension , depending on the type of anesthesia and the required level of blood pressure reduction, the dose is 2-10 Ојg / kg body weight / min under ECG control, central and intracardiac hemodynamics.
In patients with impaired liver or kidney function , the dose should be selected depending on the severity of the disorder.
Perlignanite should be used for long-term intravenous infusions with the help of automatic infusion systems in hospital conditions under constant monitoring of cardiovascular system parameters.
Perlignanite can be administered either undiluted with appropriate equipment or diluted (compatible with commonly used infusion solutions, such as saline solution, 5% dextrose solution, 10% dextrose solution).
Dilution rules
Amount of active substance (nitroglycerin) 10 mg 20 mg 30 mg 40 mg 50 mg
Primary solution volume 10 ml 20 ml 30 ml 40 ml 50 ml
Infusion solution at dilution (ml) 1 + 10 100 200 300 400 500
1 + 20 200 400 600 800 1000
1 + 40 400 800 1200 1600 2000
Ready-made infusion solution (ml) 1 + 10 110 220 330 440 550
1 + 20 210 420 630 840 1050
1 + 40 410 820 1230 1640 2050
Rules of drug administration
Necessary dose of nitroglycerin per hour
1 + 10 1 + 20 1 + 40
Infusion (ml / h)
0.5 mg 5.5 10.5 20.5
0.75 mg 8.25 15.75 30.75
1 mg 11 21 41
1.25 mg 13.75 26.25 51.25
1.5 mg 16.5 31.5 61.5
2 mg 22 42 82
2.5 mg 27.5 52.5 102.5
3 mg 33 63 123
3.5 mg 38.5 73.5 143.5
4 mg 44 84 164
4.5 mg 49.5 94.5 184.5
5 mg 55 105 205
5.5 mg 60.5 115.5 225.5
6 mg 66 126 246
7 mg 77 147 287
8 mg 88 168 328
9 mg 99 189 369
10 mg 110 210 410
Depending on the clinical picture, hemodynamic parameters and ECG treatment can be continued for 3 days or more.
SIDE EFFECT
From the side of the cardiovascular system: often at the beginning of treatment, there may be a headache ("nitrate" headache), which usually passes in a few days with further use of the drug.
Sometimes, with the first application or with an increase in the dose, a decrease in blood pressure or orthostatic hypotension occurs, which can be accompanied by a reflex increase in the pulse rate, inhibition, as well as dizziness and a sense of weakness. With a marked decrease in blood pressure, infusion should be discontinued. In the event that BP does not increase, it is necessary to take appropriate measures.
Rarely with a marked decrease in blood pressure, a decrease in coronary blood flow is possible, which leads to the progression of angina pectoris.
In isolated cases, there are collapoid conditions, sometimes with bradycardia and sudden loss of consciousness (syncope).
From the digestive system: rarely - nausea, vomiting.
Other: redness of the skin, allergic skin reactions; in some cases - exfoliative dermatitis.
When using the drug, the development of tolerance (including cross-over to other drugs of the nitrate group) is possible, therefore long continuous infusions should be avoided.
CONTRAINDICATIONS
- acute vascular insufficiency (shock, vascular collapse);
- cardiogenic shock (if it is impossible to correct the final diastolic pressure of the left ventricle with intra-aortic counterpulsation or preparations with a positive inotropic effect);
- toxic pulmonary edema;
- severe arterial hypotension (systolic blood pressure below 90 mm Hg);
- diseases accompanied by increased intracranial pressure;
- simultaneous administration with inhibitors of phosphodiesterase type 5 (eg, sildenafil);
- hypersensitivity to nitrate compounds.
Caution should be given to the drug with hypertrophic obstructive cardiomyopathy, constrictive pericarditis, cardiac tamponade, aortic aortic stenosis and / or mitral stenosis, with a decrease in the left ventricular filling pressure (for example, with acute myocardial infarction, left ventricular failure, systolic blood pressure lower than 90 mm Hg), propensity to orthostatic reactions, with renal insufficiency, hepatic insufficiency (since the risk of development of methemoglobinemia increases).
PREGNANCY AND LACTATION
During pregnancy and during breastfeeding, the application of Perligenite is possible only in those cases when the expected benefit for the mother considerably exceeds the possible risk for the fetus or the child.
In experimental studies, no damaging effects on the fetus have been identified.
APPLICATION FOR FUNCTIONS OF THE LIVER
With caution should prescribe the drug for kidney failure.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
With caution should prescribe the drug for liver failure (because increases the risk of development of methemoglobinemia).
SPECIAL INSTRUCTIONS
When applying Perlignanite, redistribution of blood flow in the lungs is possible, which can lead to hypoxemia and cause transient myocardial ischemia in patients with IHD.
After the appearance of the first signs of intolerance, the drug should not be used again.
When treating patients with insulin-dependent diabetes mellitus, it should be taken into account that the solution contains about 5% dextrose (glucose).
The solution is sterile, does not contain preservatives. Pearlinite in ampoules or vials should be opened in aseptic conditions immediately before use.
For intravenous administration of Perlignanite, the following materials are used: polyethylene, polypropylene and polytetrafluoroethylene. Infusion materials made of polyvinyl chloride or polyurethane reduce the effectiveness of the drug as a result of absorption, which must be compensated for by increasing the dose.
If the patient has previously been treated with organic nitrates, for example, isosorbide dinitrate, isosorbide-5-mononitrate, then large doses of Perlignanite may be required to achieve the desired hemodynamic effect.
It should be taken into account that the ampoule is already inscribed under the blue dot, so additional nipping is not required.
Impact on the ability to drive vehicles and manage mechanisms
The use of the drug may cause a change in the rate of psychomotor reactions, which may affect the ability to drive vehicles and control mechanisms. This effect is greatly enhanced when combined with the intake of alcohol.
OVERDOSE
Symptoms: a sharp decrease in blood pressure, a reflex increase in the pulse, a feeling of general weakness, dizziness and retardation, as well as headache, redness of the face or upper body, nausea, vomiting and diarrhea. When using the drug in high doses (more than 20 mg / kg body weight), it is possible to develop methemoglobinemia, cyanosis, dyspnea and tachypnea; possibly increased intracranial pressure with cerebral symptoms.
Treatment: it is necessary to monitor the function of vital organs.
With severe arterial hypotension and / or shock, the volume of circulating blood should be increased; in exceptional cases, you can make an infusion of norepinephrine (noradrenaline) and / or dopamine. Contraindicated in the use of epinephrine (adrenaline) and related substances.
With methemoglobinemia, depending on the degree of severity, the following antidotes are recommended: ascorbic acid (1 g inside or IV in the form of a sodium salt); methylene blue (up to 50 mg of 1% solution of methylene blue IV); toluidine blue (initial dose of 2-4 mg / kg body weight IV, if necessary, repeated at intervals of 2 mg / kg body weight). Oxygen therapy, hemodialysis, and blood transfusion are shown.
DRUG INTERACTION
When used simultaneously with other vasodilators (vasodilators), antihypertensive drugs, beta-blockers, calcium channel blockers, phosphodiesterase type 5 inhibitors used to treat erectile dysfunction (eg sildenafil), antipsychotics, tricyclic antidepressants, and also ethanol, hypotensive effect may increase .
With the simultaneous application of Perlignanite with dihydroergotamine, there may be an increase in the concentration of dihydroergotamine in the blood, which leads to an increase in its hypotensive effect.
With the simultaneous use of heparin and Perlignanite, the effect of heparin is weakened. Under the control of blood coagulability indicators, a suitable dose of heparin is selected. After the termination of the infusion of Perlinganite, a significant reduction in blood clotting is possible, which may require a reduction in the dose of heparin.
With the simultaneous application of a solution of Perlignanite and a tissue plasminogen activator, a decrease in the concentration in the blood and a decrease in the efficacy of the latter are described.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
The drug should be stored at a temperature of no higher than 25 В° C. Shelf life - 5 years (the expiration date of the drug is indicated on a cardboard box and on each ampoule).
