With rapid administration of sodium nitroprusside, development is possible. Medicinal reference book geotar. Indications for use of the drug
Recipe (international)
Rp.: Natrii nitroprussidi 0.05
D.t.d.N. 10 in amp.
S. Intravenously, dissolve in 5% glucose solution before use. Administer immediately after preparation (intravenous drip)
pharmachologic effect
Peripheral vasodilator. It has arteriodilatating, venodilating and antihypertensive effects. Naniprus reduces the tone of arteries and veins due to direct myotropic action. By dilating peripheral arterial vessels, sodium nitroprusside reduces afterload, reduces left ventricular filling pressure, and lowers blood pressure. By expanding the peripheral veins, it reduces the preload on the heart, which leads to an improvement in systemic and intracardiac hemodynamics and a decrease in pressure in the pulmonary circulation. In some cases it causes reflex tachycardia. The mechanism of action is associated both with the activation of guanylate cyclase and with an increase in intracellular cyclic guanosine monophosphate, and with the suppression of the current of calcium ions (direct inhibition of the entry of calcium ions through slow channels) and disruption of myosin phosphorylation. The antihypertensive effect develops in the first minute after intravenous administration. The effect of the drug is short-lived due to rapid metabolism in the blood.
Mode of application
For adults: Administered intravenously as an infusion.
Treatment with Naniprus is carried out in a hospital setting with the ability to monitor blood pressure, perform resuscitation measures and if there are funds available for the treatment of cyanide intoxication. IV bolus administration of Naniprus is contraindicated.
The dose is set individually with constant monitoring of blood pressure.
Hypertensive crisis, controlled arterial hypotension during surgery Adults: for patients not receiving antihypertensive drugs, the dose is usually 3 mcg/kg/min. The initial dose is 0.3-1.5 mcg/kg/min. The dose is increased gradually (by 0.5 mcg/kg/min every 5 minutes) until an antihypertensive effect is achieved. The dose is adjusted so that the decrease in blood pressure during the first hour of infusion does not exceed 25% of the initial level, due to the risk of myocardial, cerebral or renal ischemia. The maximum dose for adults is 8-10 mcg/kg/min.
If administration over 10 minutes at a rate of 10 mcg/kg/min does not adequately lower blood pressure, it is recommended to immediately stop the infusion. Do not exceed the dose more than 500 mcg/min. To control arterial hypotension during surgery or while taking antihypertensive drugs 3 hours before the infusion, it is sufficient to administer a total dose of 1 mg/kg body weight. To avoid a compensatory reaction (sharp increase in catecholamines and renin, tachycardia), especially in young patients, the dose should be increased gradually until the desired therapeutic effect is achieved. The rate of administration is also reduced gradually, within 10-30 minutes, to avoid a sharp increase in blood pressure. Children: experience with the use of Naniprus in children is limited. The average dose is the same as for adult patients.
Elderly patients (over 65 years): treatment begins with the administration of Naniprus in low doses, because older patients are more sensitive to the drug (more rapid development of the antihypertensive effect).
Duration of treatment
Once the antihypertensive effect is achieved, administration should be continued for only a few hours to avoid the risk of cyanide toxicity. Treatment with Naniprus should not last more than 72 hours. After stopping the use of the drug, it is necessary to begin alternative treatment with antihypertensive drugs for oral administration.
Heart failure
The initial dose is 10-15 mcg/min, with a gradual increase every 5-10 minutes by 10-15 mcg/min. If necessary, to achieve a satisfactory therapeutic effect, the dose can be increased within the range of 10-200 mcg/min. If symptoms of arterial hypotension, hypoperfusion, or some other adverse reactions develop during drug administration, the infusion rate should be reduced or discontinued.
Infusion administration can be continued until it is safe to switch to oral therapy. As a rule, the drug should be used for no more than 72 hours.
Rules for the preparation and administration of infusion solution Naniprus in the form of lyophilized powder should be used only for the preparation of a diluted infusion solution. The infusion solution is prepared immediately before use (the solution should not be used later than 4 hours after preparation). The contents of 1 ampoule of the drug are diluted in the supplied solvent. The resulting solution is additionally diluted in 500 ml of 5% dextrose (glucose) solution or 0.9% sodium chloride solution, protecting the infusion solution from exposure to light. The infusion is carried out using an infusion pump with continuous monitoring of blood pressure.
The entire infusion set should be isolated from direct sunlight using a black plastic bag. The infusion solution must not be mixed with other medications.
Indications
Hypertensive crisis;
- controlled arterial hypotension during surgical interventions (to reduce blood loss);
- acute heart failure when it is necessary to quickly reduce left ventricular afterload to reduce left ventricular filling pressure;
- acute left ventricular failure with pulmonary edema.
Contraindications
Symptomatic (compensatory) arterial hypertension (with arteriovenous shunting or coarctation of the aorta);
- acute cerebrovascular accident;
- increased intracranial pressure;
- arterial hypotension;
- chronic heart failure associated with reduced peripheral vascular resistance;
- aortic stenosis;
- hypovolemia;
- hypothyroidism (thiocyanate inhibits the absorption and binding of iodine);
- hypovitaminosis of vitamin B12;
- deficiency of sulforyltransferase (rhodanase) in patients with Leber ocular atrophy;
- optic nerve atrophy;
- glaucoma;
- severe liver failure;
- severe renal failure;
- pregnancy;
- lactation period (breastfeeding);
- hypersensitivity to active and auxiliary substances.
In emergency situations (for health reasons), these contraindications are relative.
The drug should be used with caution in patients with hypothermia, hyponatremia, coronary heart disease, and in elderly patients.
Side effects
Adverse reactions are caused by the ability of the drug to quickly and significantly reduce blood pressure or the toxicity of its main metabolites (cyanide and thiocyanate).
Possible: nausea, vomiting, increased sweating, headache, anxiety, dizziness, muscle spasms, hyperreflexia, rapid decrease in blood pressure, tachycardia, bradycardia, chest discomfort, abdominal pain; when used in excessively high doses - the development of cyanide intoxication (vomiting, loss of consciousness, tissue hypoxia); with rapid cessation of infusion - rebound syndrome. These symptoms disappear when the infusion rate is slowed or when the infusion is temporarily stopped.
Dermatological reactions: very rarely - skin rashes, itching, erythema (require stopping the infusion).
Local reactions: redness, swelling, acute phlebitis.
Other: rarely - decreased platelet count; very rarely - hypothyroidism
Release form
Lyophilized (dried by freezing under vacuum) in ampoules of 0.05 g.
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P N012724/01-050210Trade name of the drug: Naniprus.
International nonproprietary name or generic name: sodium nitroprusside
Dosage form:
lyophilisate for the preparation of solution for infusion
Compound
1 ampoule contains:
Active substance: sodium nitroprusside dihydrate 30 mg
Excipients: sodium citrate dihydrate 61.7 mg (in terms of sodium citrate anhydrous 54.15 mg).
Each ampoule with solvent contains: water for injection 5 ml.
Description
Lyophilisate: unformed tablet with a rough mesh structure or coarse powder from light orange with a brownish tint to orange.
Solvent:
Colorless transparent liquid
Lyophilisate solution:
transparent liquid of light brown color.
Pharmacotherapeutic group:
vasodilator.
ATX code:
Pharmacological properties
Pharmacodynamics
Peripheral vasodilator. It has arteriodilatating, venodilating and antihypertensive effects.
The effect of the drug is expressed as follows:
Reduces the tone of arteries and veins due to direct myotropic action. By dilating peripheral arterial vessels, sodium nitroprusside reduces afterload, reduces left ventricular filling pressure, and lowers blood pressure (BP). By expanding the peripheral veins, it reduces the preload on the heart, which leads to an improvement in systemic and intracardiac hemodynamics and a decrease in pressure in the pulmonary circulation. In some cases it causes reflex tachycardia. The antihypertensive effect develops in the first minute after intravenous administration. The effect of the drug is short-lived due to rapid metabolism in the blood. The mechanism of action is associated with both activation of guanylate cyclase and an increase in intracellular cyclic guanosine monophosphate, as well as suppression of the current of calcium ions (direct inhibition of the entry of calcium ions through slow channels) and disruption of myosin phosphorylation.
Pharmacokinetics
When administered intravenously, sodium nitroprusside is rapidly distributed and reaches a volume of distribution corresponding to the extracellular space (volume). Metabolized completely within a few minutes by red blood cell enzymes, with the formation of iron ions, cyanides and methemoglobin. Methemoglobin and cyanide are released slowly into the blood plasma from red blood cells and reaching the liver, they are transformed into thiocyanate with the participation of thiosulfate and the enzyme rhodanase. Thiocyanate is excreted by the kidneys (up to 80%). The half-life from plasma is about 3 days (with insufficiency of renal function it can increase 2-3 times) in patients with normal renal function. Renal clearance of thiocyanate is approximately 2.2 ml/min. Penetrates through the blood-brain and placental barriers and is excreted in small quantities in breast milk.
Indications for use
- hypertensive crisis
- acute left ventricular failure with pulmonary edema
- controlled arterial hypotension during surgery to reduce operative blood loss
- acute heart failure when it is necessary to quickly reduce left ventricular afterload to reduce left ventricular filling pressure.
Contraindications
- Hypersensitivity to the active or excipient;
- Symptomatic (compensatory) arterial hypertension (with arteriovenous shunting or coarctation of the aorta);
- Acute cerebrovascular accident;
- Increased intracranial pressure;
- Arterial hypotension;
- Chronic heart failure associated with reduced peripheral vascular resistance;
- Aortic stenosis:
- Hypovolemia;
- Hypothyroidism (thiocyanate inhibits the absorption and binding of iodine);
- Hypovitaminosis of vitamin B|2;
- Sulforyl transferase (rhodanase) deficiency in patients with Leber ocular atrophy;
- Optic nerve atrophy;
- Glaucoma;
- Severe liver and/or renal failure;
- Pregnancy, lactation period.
In emergency situations (for “vital” indications), these contraindications are relative.
Carefully:
Should be used with caution in patients with hypothermia, hyponatremia, coronary heart disease and the elderly.
Directions for use and doses
Intravenously as an infusion.
Treatment with Naniprus is carried out in a hospital setting with the possibility of monitoring blood pressure, carrying out resuscitation measures and with the availability of means to combat cyanide intoxication.
Intravenous bolus administration of Naniprus is contraindicated!
Naniprus in the form of lyophilized powder should only be used for the preparation of a diluted infusion solution.
Preparation of the solution
The infusion solution is prepared immediately before use (the solution should not be used later than 4 hours after preparation).
Dilute the contents of 1 ampoule of the drug in a solvent (included in the kit). The prepared solution is additionally diluted in 500 ml of 5% dextrose (glucose) solution or 0.9% sodium chloride solution, protecting the solution from exposure to light. The infusion is carried out using an infusion pump with continuous monitoring of blood pressure. The infusion solution must not be mixed with other medications!
Dosage
The dose is set individually with constant monitoring of blood pressure.
Adults: for patients not receiving antihypertensive drugs, the dose is usually 3 mcg/kg/min. Initial dose: 0.3-1.5 mcg/kg/min. The dose is increased gradually (by 0.5 mcg/kg/min every 5 minutes) until an antihypertensive effect is achieved. The dose is adjusted so that the decrease in blood pressure during the first hour of infusion does not exceed 25% of the initial level, due to the risk of myocardial, cerebral or renal ischemia. The maximum dose for adults is 8-10 mcg/kg/min.
If administration over 10 minutes at a rate of 10 mcg/kg per minute does not adequately lower blood pressure, it is recommended to immediately stop the infusion.
Do not exceed a dose of 500 mcg/min.
To control arterial hypotension during surgery or while taking antihypertensive drugs 3 hours before the infusion, it is sufficient to administer a total dose of 1 mg/kg body weight.
To avoid a compensatory reaction (sharp increase in catecholamines and renin, tachycardia), especially in young patients, the dose should be increased gradually until the desired therapeutic effect is achieved. The rate of administration is also reduced gradually, within 10-30 minutes, to avoid a sharp increase in blood pressure.
Children: experience with Naniprus in children is limited. The usual dosage is the same as for adult patients.
Elderly patients (over 65 years): treatment begins with low doses, since older patients are more sensitive to the drug (more rapid development of the antihypertensive effect).
Duration of treatment
Once the antihypertensive effect is achieved, administration should be continued for only a few hours to avoid the risk of cyanide toxicity. Treatment with Naniprus should not last more than 72 hours. After completion, alternative treatment with oral antihypertensive agents should be started.
Heart failure
The initial dose should be 10-15 mcg/min, with a gradual increase every 5-10 minutes by 10-15 mcg/min. If necessary, to achieve a satisfactory therapeutic effect, the dose can be increased within the range of 10-200 mcg/min. If symptoms of arterial hypotension, hypoperfusion, or some other side effects are observed during drug administration, the infusion rate should be reduced or discontinued.
Infusion administration can be continued until it is safe to switch to oral therapy. Typically, infusion administration should not exceed 3 days.
Side effect
Adverse reactions are due to the ability of the drug to quickly and significantly reduce blood pressure or the toxicity of its main metabolites (cyanide and thiocyanate).
Possible: nausea, vomiting, increased sweating, headache, anxiety, dizziness, muscle spasms, hyperreflexia, rapid decrease in blood pressure, tachycardia, bradycardia, chest discomfort, abdominal pain, when used in excessively high doses - the development of cyanide intoxication (vomiting , loss of consciousness, tissue hypoxia), with rapid cessation of infusion - “rebound” syndrome. These symptoms disappear when the infusion rate is slowed or when the infusion is temporarily stopped.
Rarely: decreased platelet count.
Very rarely: skin rashes, itching, erythema (require stopping the infusion); hypothyroidism
Reactions at the injection site: redness, swelling, acute phlebitis.
Overdose
The first signs of overdose are associated with a pronounced decrease in blood pressure. Sometimes the development of lactic acidosis can be an early symptom of overdose. In case of severe overdose, the level of cyanide in the blood plasma increases.
Treatment
If symptoms of overdose appear, stop infusion with Naniprus immediately. As an antidote, it is possible to use a 1% solution of sodium nitrite in combination with 20-50 ml of sodium thiosulfate solution (12.5 g in 50 ml of 5% dextrose (glucose) solution. Respiratory resuscitation, oxygen therapy and symptomatic drugs - analeptics, cardiovascular drugs , water-salt solutions, agents that correct the acid-base state, oxycobalamin 2.5 g (2.5 g in 100 ml of 0.9% sodium chloride solution) for 7.5 minutes.
Interaction with other drugs
Ganglion blockers, general anesthetics, beta-blockers, diuretics, slow calcium channel blockers (diltiazem), angiotensin-converting enzyme inhibitors (captopril) can enhance the antihypertensive effect of sodium nitroprusside. Since sodium nitroprusside is a nitric oxide donor, it should not be used simultaneously with phosphodiesterase-5 inhibitors (sildenafil, vardenafil, tadalafil). When used together with estrogens or sympathomimetics, the antihypertensive effect of Naniprus is reduced.
Mixing Naniprus infusion solution with other medications is not allowed.
special instructions
The development of a hypertensive crisis, with accompanying cerebrovascular events, is not an indication for treatment with Naniprus. The decision is made in the presence of visceral complications with an immediate threat to life. In patients with hyponatremia and renal impairment, prolonged treatment with Naniprus may result in higher plasma concentrations of the major metabolite thiocyanate. Since the latter suppresses the absorption of iodine from the thyroid gland, symptoms of hypothyroidism may appear.
In young patients, to prevent a pronounced compensatory reaction associated with a sharp increase in the levels of catecholamines and renin, the dose is increased and decreased gradually. The entire infusion set should be isolated from direct sunlight using a black plastic bag.
Impact on the ability to drive vehicles and operate machinery
The drug is used only in hospital settings.
Release form
Lyophilisate for the preparation of solution for infusion 30 mg complete with solvent (water for injection)
The lyophilisate in an amount equivalent to 30 mg of sodium nitroprusside dihydrate is placed in 10 ml dark glass ampoules. 5 ml of solvent (water for injection) is placed in 5 ml clear glass ampoules.
One ampoule with lyophilisate, one ampoule with solvent and a black plastic bag to protect the drug from light, along with instructions, are placed in a cardboard package.
Storage conditions
List B.
In a dry place, protected from light, at a temperature not exceeding 25 ° C.
Do not freeze!
Keep out of the reach of children.
Best before date
5 years.
Do not use after the expiration date indicated on the package!
The prepared infusion solution must be used within 4 hours after its preparation.
Conditions for dispensing from pharmacies
For stationary use only!
Manufacturer Sopharma JSC - Bulgaria 1220, Sofia, st. Ilienskoe highway 16
Representative office of Sopharma JSC in Moscow
109004, st. Taganskaya 17-23, fl. 10
Gross formula
C 5 FeN 6 Na 2 OPharmacological group of the substance Sodium nitroprusside
Nosological classification (ICD-10)
CAS code
14402-89-2Characteristics of the substance Sodium nitroprusside
Reddish-brown crystals (or powder). Easily soluble in water.
Pharmacology
pharmachologic effect- antihypertensive, arteriodilating.It has arteriodilatating, venodilating and antihypertensive effects.
Contains a nitroso group (connected through CN groups to an iron atom), which in the body is transformed into nitric oxide (NO), which activates guanylate cyclase. Increases the formation of cGMP and its concentration in the smooth muscle cells of the vascular wall and causes vasodilation. In the mechanism of vasodilatory action, direct inhibition of the entry of calcium ions through slow channels or disruption of myosin phosphorylation is not excluded.
Relaxes the smooth muscles of both arterioles and veins, reduces peripheral vascular resistance and venous tone, reduces blood pressure, post- and preload on the myocardium. Reduces myocardial oxygen demand and improves its function with low output. The hypotensive effect is accompanied by a slight increase in heart rate and a decrease in minute blood volume, and an increase in renin activity. Reduces platelet aggregation.
In patients with acute myocardial infarction, it improves myocardial perfusion due to dilation of the coronary vessels, reduces heart function and myocardial oxygen consumption (reduces pre- and afterload), and helps reduce the size of the infarction zone. In patients with heart failure with SBP above 100 mm Hg. Art. and increased left ventricular pressure may cause increased cardiac output without excessive hypotension. The hypotensive effect occurs within 1-2 minutes after the start of the infusion and continues for 1-10 minutes after its completion. It has been shown to be effective as an adjuvant for myocardial infarction (including in patients with arterial hypertension and persistent chest pain or left ventricular failure) and blood regurgitation due to heart valve insufficiency.
Studies examining carcinogenicity and mutagenicity in humans and animals have not been conducted.
There are no adequate and strictly controlled studies of the effect on pregnancy and reproductive function in humans. There are no data on the teratogenic effect in animals, however, in 3 studies in pregnant sheep, it was shown that nitroprusside crosses the placenta, cyanide concentrations in the fetus depend on the doses received by the mother, and when administered at a high rate of nitroprusside to pregnant sheep, it can create fetus has lethal concentrations of cyanide.
Biotransformed by intraerythrocyte reaction with hemoglobin to form cyanmethemoglobin and cyanide ion. Cyanide ions are partially excreted from the body in the form of exhaled hydrocyanide, but are mainly converted into thiocyanate, which is excreted in the urine (the reaction involves the mitochondrial enzyme of the liver rhodanase - thiosulfate cyanide sulfur transferase - and sulfur donors, primarily thiosulfate, cystine and cysteine). The rate of conversion of cyanide ion to thiocyanate (cyanide clearance) is 1 mcg/kg/min and corresponds to the rate of metabolism of sodium nitroprusside (when a stable concentration is reached) in the case of infusion at a rate slightly exceeding 2 mcg/kg/min (at higher cyanide infusion rates starts to accumulate). Cyanide that is not excreted from the body by the lungs (in the form of hydrocyanide) and the kidneys (in the form of thiocyanate) binds to mitochondrial cytochromes and disrupts oxidative metabolism (cells switch to anaerobic metabolism or die from hypoxia).
The metabolism of nitroprusside leads to the formation of methemoglobin both as a result of the dissociation of cyanmethemoglobin resulting from the initial reaction of nitroprusside with hemoglobin, and due to the direct oxidation of hemoglobin with the release of nitroso groups.
T1/2 of nitroprusside from blood plasma - about 2 minutes, T1/2 of thiosulfate (after IV infusion) - about 20 minutes, thiocyanate - about 3 days (with kidney failure it can increase 2-3 times).
Application of the substance Sodium nitroprusside
Acute and chronic (IIB - III stages, resistant to therapy with diuretics and cardiac glycosides) heart failure, hypertensive crisis, controlled hypotension during surgery, vasospasm caused by ergot poisoning, paroxysmal hypertension during surgery for pheochromocytoma (before and during operations).
Contraindications
Hypersensitivity, congenital optic atrophy and tobacco amblyopia (associated with defective or absent rhodanase), compensatory hypertension in aortic coarctation or arteriovenous shunting; acute congestive heart failure caused by a decrease in peripheral vascular resistance; cerebrovascular accident or critical condition of the patient (when used for controlled hypotension).
Restrictions on use
Insufficiency of cerebral and coronary circulation, increased intracranial pressure (encephalopathy, etc.), dysfunction of the liver, kidneys and lungs, hypothyroidism (thiocyanate suppresses the absorption and binding of iodine), hypovitaminosis B 12; anemia and hypovolemia (when used for controlled hypotension), pregnancy, breastfeeding, old age.
Use during pregnancy and breastfeeding
The potential benefit to the mother may justify use despite the possible risk to the fetus. There are no data on excretion into breast milk, but given the serious potential side effects, you should stop taking the drug or stop breastfeeding (continue treatment if necessary).
Side effects of the substance Sodium nitroprusside
From the nervous system and sensory organs: tinnitus, miosis, dizziness, nervousness, anxiety, muscle twitching, hyperreflexia, restlessness, increased intracranial pressure.
From the cardiovascular system and blood (hematopoiesis, hemostasis): excessive hypotension, rebound phenomenon (severe hypertension) with rapid cessation of infusion, tachycardia, bradycardia, ECG changes, methemoglobinemia, decreased platelet aggregation.
From the gastrointestinal tract: abdominal pain, incl. in the stomach area, intestinal obstruction.
Others: hypothyroidism, headache, sweating, pain or redness at the injection site, facial flushing, skin rash.
Interaction
When used simultaneously with dobutamine, it is possible to increase cardiac output and decrease wedge pressure in the pulmonary capillaries. The hypotensive effect can be reduced by estrogens and sympathomimetic drugs, and increased by other antihypertensive drugs.
Overdose
Overdose of sodium nitroprusside.
Symptoms: excessive hypotension (impaired blood supply to vital organs, irreversible ischemic damage, possible death), methemoglobinemia.
Treatment: for hypotension - slow down or stop the infusion, give the patient a Trendelenburg position; with the development of hypotension from doses effective for restoring pumping function in left ventricular congestive heart failure, additional use of inotropic agents (dopamine, dobutamine) is possible; for methemoglobinemia, administration of methylene blue at a dose of 1-2 mg/kg IV for several minutes.
Thiocyanate poisoning.
Symptoms: ataxia, dizziness, headache, tinnitus, blurred vision, nausea and vomiting, shortness of breath, delirium, loss of consciousness.
Treatment: hemodialysis (clearance during dialysis may approach the speed of blood flow in the dialyzer).
Cyanide poisoning.
Symptoms: absence of reflexes, coma, severe mydriasis, pink skin, loud heart sounds heard at a distance, hypotension, weak pulse, shallow breathing, metabolic acidosis.
Treatment: begin when a reasonable suspicion arises (before receiving the results of laboratory tests). Scheme 1: administration of sodium nitrite (3% solution) at a dose of 4-6 mg/kg IV for 2-4 minutes or inhalation of amyl nitrite, then (immediately after the infusion of sodium nitrite) - sodium thiosulfate at a dose of 150-200 mg/ kg infusion (standard dose for adults is 50 ml of 25% solution). This regimen can be repeated after 2 hours using half doses.
Scheme 2: administration of oxycobalamin (iv over 15 minutes) in a dose equal to double the total dose of sodium nitroprusside (oxycobalamin solution is prepared by diluting 0.1 g in 100 ml of 5% glucose solution), then sodium thiosulfate solution (12.5 g in 50 ml of 5% glucose solution intravenously for 10 minutes). Hemodialysis is ineffective.
Routes of administration
IV, infusion.
Precautions for the substance Sodium nitroprusside
During treatment, continuous monitoring of blood pressure is necessary (sBP should decrease to no more than 100-110 mm Hg), monitoring of acid-base balance, methemoglobin levels (recommended for doses greater than 10 mg/kg and the presence of signs of ischemia) and thiocyanate (at daily intervals against the background of prolonged infusions at a dose of more than 3 mcg/kg/min) in the blood. When prescribed for congestive heart failure, monitoring of hemodynamics (invasive methods) and diuresis is necessary.
If administration over 10 minutes at a rate of 10 mcg/kg per minute does not adequately lower blood pressure, it is recommended to immediately stop the infusion.
It is administered only intravenously by infusion using an infusion, preferably volumetric, pump (the use of conventional intravenous systems is excluded due to insufficient dosing accuracy). Extravascular administration should be avoided due to possible irritant effects.
It should be noted that at infusion rates greater than 2 mcg/kg/min, cyanide ions are formed faster than the body can eliminate them.
The buffering effect of methemoglobin against cyanide is exhausted at a dose of 500 mcg/kg sodium nitroprusside (infusion at 10 mcg/kg/min over less than 1 hour); above this level, cyanide toxicity can be rapid, severe and fatal.
Coadministration of sodium thiosulfate at 5 to 10 times the rate of sodium nitroprusside infusion may reduce the risk of cyanide toxicity, but the potential for increased hypotensive effects (one report), thiocyanate toxicity, and hypovolemia should be considered.
If hypotension is excessive, slow or stop the infusion; symptoms disappear quickly (within 1-10 minutes).
The possibility of tolerance must be considered.
special instructions
The solution is prepared immediately before use. Solutions should not be stored for more than 24 hours.
The freshly prepared solution has a brownish tint. If the solution is yellow-brown, orange, bright red, blue or green, it must be replaced and destroyed.
After preparation, the container with the solution should be wrapped in opaque black paper, plastic film or metal foil included in the package (the solution is sensitive to certain wavelengths of light). Infusion lines and tubing are not wrapped.
Sodium nitroprussidumpharmachologic effect
It is a highly effective peripheral vasodilator (vasodilator). Dilates arterioles and partially veins. When administered intravenously, it has a rapid, strong and relatively short-lived hypotensive (lowering blood pressure) effect; reduces the load on the heart and the need of the myocardium (heart muscle) for oxygen.Indications for use
Sodium nitroprusside is used in complex therapy for acute heart failure, especially in cases resistant to conventional therapeutic measures. Administration of the drug quickly relieves (relieves) the signs of cardiac asthma and threatening pulmonary edema and improves cardiac hemodynamics. It is also prescribed for chronic heart failure, hypertensive crises (a rapid and sharp rise in blood pressure), acute myocardial infarction, hypertensive encephalopathy (a disease of the brain associated with impaired blood circulation).Mode of application
The drug is administered intravenously; when taken orally, it has no hypotensive effect.A solution of sodium nitroprusside is prepared immediately before use. First, dissolve the contents of one ampoule (25 or 50 mg) in 5 ml of a 5% glucose solution, and then dilute an additional 1000; 500 or 250 ml of 5% glucose solution. When diluted in 50 mg of the drug in 500 ml of solution, 1 ml contains 100 mcg (when diluted in 250 or 1000 ml, 200 or 50 mcg, respectively).
The use of undiluted solution is not allowed.
For infusions lasting up to 3 hours, the following doses are recommended per 1 kg of body weight per minute: initial 0.3-1 mcg/kg per minute, average 3 mcg/kg per minute and maximum in adults 8 mcg/kg per minute . For controlled hypotension (controlled decrease in blood pressure) during surgery under anesthesia or while taking antihypertensive (blood pressure-lowering) drugs, it is usually sufficient to administer the drug in a total dose of 1 mg/kg over a 3-hour infusion.
When administered at a rate of 3 mcg/kg per minute, blood pressure usually decreases to 60-70% of the initial level, i.e. by 30-40%. For long-term infusion (days, weeks), the average rate of administration should not exceed 2.5 mcg/kg per minute, which corresponds to 3.6 mg/kg per day. In this case, it is necessary to constantly monitor the cyanide content in the blood or plasma, the concentration of which should not exceed 100 mcg per 100 ml in the blood, and 8 mcg per 100 ml in the plasma. If infusions continue for more than 3 days, the content of thiocyanate should also be monitored, the concentration of which should not exceed 6 mg per 100 ml of blood serum.
In case of tachyphylaxis (rapid decrease in the therapeutic effect upon repeated use of the drug) to sodium nitroprusside, when the hypotensive effect of the drug weakens due to the compensatory reaction of the body (more often this occurs in young people), the maximum doses indicated above cannot be exceeded.
The infusion rate, i.e., the dose of the drug entering the blood per unit of time, is determined individually with constant monitoring of blood pressure levels.
Freshly prepared solutions should be used. Immediately after preparing the solution and filling the system for drip administration, measures are taken to protect the drug from light by wrapping the container with the solution and the transparent parts of the system with opaque black paper, plastic film or metal foil attached to the package.
Sodium nitroprusside is a highly effective peripheral vasodilator, but it must be used with great caution.
The solution must be administered under careful monitoring of blood pressure; systolic pressure (“upper” pressure - blood pressure during the phase of ejection of blood by the heart) should decrease to no more than 100-110 mm Hg. With high concentrations and rapid administration, a rapid decrease in blood pressure, tachycardia (rapid heartbeat), vomiting, dizziness, and unconsciousness are possible. Then the dose should be reduced (slow down the rate of administration) or completely stop administering the drug.
