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Sodium Nitroprusside In 0.9% Sodium Chloride

Prescription

商品名: sodium nitroprusside in 0.9% sodium chloride

剤形
Injection
投与経路
INTRAVENOUS

About This Medication

11 DESCRIPTION Sodium nitroprusside is disodium pentacyanonitrosylferrate (2-) dihydrate, a hypotensive agent whose structural formula is Sodium Nitroprusside has a molecular formula Na 2 [Fe(CN) 5 NO] • 2H 2 O and molecular weight of 297.95. Dry sodium nitroprusside is a reddish-brown powder, soluble in water. Sodium nitroprusside solution is rapidly degraded by trace contaminants, often with resulting color changes [see Dosage and Administration ( 2.1 )]. Sodium Nitroprusside in 0.9% Sodium Chloride Injection, ready to use is supplied as a sterile, unpreserved, colorless to red-brown solution packaged in a single-dose 100-mL vial. Each 100 mL of solution in vial contains 50 mg of sodium nitroprusside (0.5 mg/mL), 900 mg of sodium chloride, USP (9 mg/mL), in sterile water for injection, USP. Sodium Nitroprusside in 0.9% Sodium Chloride Injection, ready to use is also supplied as a sterile, unpreserved, colorless to red-brown solution packaged in a single-dose 100-mL vial. Each 100 mL of solution in vial contains 20 mg of sodium nitroprusside (0.2 mg/mL), 900 mg of sodium chloride, USP (9 mg/mL), in sterile water for injection, USP. Sodium Nitroprusside in 0.9% Sodium Chloride Injection, ready to use is also supplied as a sterile, unpreserved, colorless to red-brown solution packaged in a single-dose 50-mL vial. Each 50 mL of solution in vial contains 10 mg of sodium nitroprusside (0.2 mg/mL), 450 mg of sodium chloride, USP (9 mg/mL), in sterile water for injection, USP. chemical structure

有効成分

成分 含有量
Sodium Nitroprusside -

適応症と用法

1 INDICATIONS AND USAGE Sodium nitroprusside is a direct acting vasodilator indicated for: Immediate reduction of blood pressure ( 1.1 ) Producing controlled hypotension to reduce bleeding during surgery ( 1.2 ) Treatment of acute heart failure to reduce left ventricular end-diastolic pressure, pulmonary capillary wedge pressure, peripheral vascular resistance and mean arterial blood pressure ( 1.3 ) 1.1 Immediate Reduction of Blood Pressure Sodium nitroprusside is indicated for the immediate reduction of blood pressure of adult and pediatric patients in hypertensive crises. 1.2 Induction and Maintenance of Controlled Hypotension Sodium nitroprusside indicated for induction and maintenance of controlled hypotension in adults and children during surgery, to reduce bleeding. 1.3 Treatment of Acute Heart Failure Sodium nitroprusside is indicated for the treatment of acute heart failure to reduce left ventricular end-diastolic pressure, pulmonary capillary wedge pressure, peripheral vascular resistance and mean arterial blood pressure.

作用のしくみ

12.1 Mechanism of Action Sodium nitroprusside interacts with oxyhemoglobin to produce methemoglobin, cyanide, and nitric oxide (NO). NO then reacts with guanylate cyclase in vascular smooth muscle to produce cGMP that reduces intracellular calcium concentrations resulting in relaxation of vascular smooth muscle and consequent dilatation of peripheral arteries and veins. Other smooth muscle (e.g., uterus, duodenum) is not affected. Sodium nitroprusside is more active on veins than on arteries, but this selectivity is much less marked than that of nitroglycerin. Dilatation of the veins promotes peripheral pooling of blood and decreases venous return to the heart, thereby reducing left ventricular end diastolic pressure and pulmonary capillary wedge pressure (preload). Arteriolar relaxation reduces systemic vascular resistance, systolic arterial pressure, and mean arterial pressure (afterload). Dilatation of the coronary arteries also occurs.

用量と投与方法

2 DOSAGE AND ADMINISTRATION Initiate infusion of sodium nitroprusside at a rate of 0.3 mcg/kg/min, and titrate every few minutes until the desired effect is achieved OR the maximum recommended infusion rate of 10 mcg/kg/min has been reached ( 2.2 ). 2.1 Inspection Inspect parenteral drug products for particulate matter and discoloration prior to administration, whenever solution and container permit. Sodium nitroprusside should be a clear colorless to red/brown color; do not use if solution is blue, green, or bright red. Dosing Continuously monitor blood pressure in patients receiving sodium nitroprusside. Start infusion of sodium nitroprusside at a rate of 0.3 mcg/kg/min. Evaluate blood pressure for at least 5 minutes before titrating to a higher or lower dose to achieve the desired blood pressure. The dose may be titrated upward until: the desired effect is achieved, systemic blood pressure cannot be further reduced without compromising the perfusion of vital organs, or the maximum recommended infusion rate of 10 mcg/kg/min has been reached, whichever occurs first. In patients with eGFR <30 mL/min/1.73 m 2 , limit the mean infusion rate to less than 3 mcg/kg/min. In anuric patients, limit the mean infusion rate to 1 mcg/kg/min. 2.3 Administration Do not administer other drugs in the same solution with sodium nitroprusside. Sodium nitroprusside must be delivered by a volumetric infusion pump because small variations in infusion rate can lead to wide, undesirable variations in blood pressure [see Clinical Pharmacology ( 12.2 )].

Side Effects Overview

6 ADVERSE REACTIONS The following adverse reactions are described, or described in greater detail, in other sections: Hypotension [see Warnings and Precautions ( 5.1 )] Cyanide Toxicity [see Warnings and Precautions ( 5.2 )] Thiocyanate Toxicity [see Warnings and Precautions ( 5.3 )] Methemoglobinemia [see Warnings and Precautions ( 5.4 )] Increased Intracranial Pressure [see Warnings and Precautions ( 5.5 )] Anemia and Hypovolemia [see Warnings and Precautions ( 5.6 )] Less common adverse reactions include: Cardiovascular: Bradycardia, electrocardiographic changes, tachycardia, palpitations, retrosternal discomfort Dermatologic: Rash Endocrine: Hypothyroidism Gastrointestinal: Ileus, nausea, abdominal pain Hematologic: Decreased platelet aggregation Musculoskeletal: Muscle twitching Neurologic: Increased intracranial pressure, dizziness, headache Miscellaneous: Flushing, diaphoresis, venous streaking, irritation at the infusion site Most common adverse reactions are hypotension and cyanide toxicity ( 6 ). To report SUSPECTED ADVERSE REACTIONS, contact Slate Run Pharmaceuticals, LLC at 1-888-341-9214 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.

警告と注意事項

禁忌

薬物動態

12.3 Pharmacokinetics Infused sodium nitroprusside is rapidly distributed to a volume that is approximately coextensive with the extracellular space. The drug is cleared by intraerythrocytic reaction with hemoglobin (Hgb), and sodium nitroprusside’s resulting circulatory half-life is about 2 minutes. The products of the nitroprusside/hemoglobin reaction are cyanmethemoglobin (cyanmetHgb) and cyanide ion (CN¯). Metabolism As shown in the diagram below, the essential features of nitroprusside metabolism are: one molecule of sodium nitroprusside is metabolized by combination with hemoglobin to produce one molecule of cyanmethemoglobin and four CN¯ ions; methemoglobin, obtained from hemoglobin, can sequester cyanide as cyanmethemoglobin; thiosulfate reacts with cyanide to produce thiocyanate; thiocyanate is eliminated in the urine; cyanide not otherwise removed binds to cytochromes; and cyanide is much more toxic than methemoglobin or thiocyanate. Cyanide ion is normally found in serum; it is derived from dietary substrates and from tobacco smoke. CN¯ levels in packed erythrocytes are typically less than 1 μmol/L (less than 25 mcg/L); levels are roughly doubled in heavy smokers. At healthy steady state, most people have less than 1% of their hemoglobin in the form of methemoglobin. Nitroprusside metabolism can lead to methemoglobin formation. Relatively large quantities of sodium nitroprusside, however, are required to produce significant methemoglobinemia. At physiologic methemoglobin levels, the CN¯ binding capacity of packed red cells is a little less than 200 μmol/L (5 mg/L). Cytochrome toxicity is seen at levels only slightly higher, and death has been reported at levels from 300 to 3000 μmol/L (8–80 mg/L). A patient with a normal redcell mass (35 mL/kg) and normal methemoglobin levels can buffer about 175 mcg/kg of CN¯, corresponding to a little less than 500 mcg/kg of infused sodium nitroprusside. Thiocyanate (SCN¯) is a normal physiological constituent of serum, with normal levels typically in the range of 50-250 μmol/L (3-15 mg/L). Clearance of SCN¯ is primarily renal. In renal failure, the half-life can be doubled or tripled. When thiosulfate is being supplied only by normal physiologic mechanisms, conversion of CN¯ to SCN¯ generally proceeds at about 1 mcg/kg/min. This rate of CN¯ clearance corresponds to steady-state processing of a sodium nitroprusside infusion of slightly more than 2 mcg/kg/min. CN¯ begins to accumulate when sodium nitroprusside infusions exceed this rate. metabolism of sodium nitroprusside

Frequently Asked Questions

1 INDICATIONS AND USAGE Sodium nitroprusside is a direct acting vasodilator indicated for: Immediate reduction of blood pressure ( 1.1 ) Producing controlled hypotension to reduce bleeding during surgery ( 1.2 ) Treatment of acute heart failure to reduce left ventricular end-diastolic pressure, pulmonary capillary wedge pressure, peripheral vascular resistance and mean arterial blood pressure ( 1.3 ) 1.1 Immediate Reduction of Blood Pressure Sodium nitroprusside is indicated for the immediate reduction of blood pressure of adult and pediatric patients …

2 DOSAGE AND ADMINISTRATION Initiate infusion of sodium nitroprusside at a rate of 0.3 mcg/kg/min, and titrate every few minutes until the desired effect is achieved OR the maximum recommended infusion rate of 10 mcg/kg/min has been reached ( 2.2 ). 2.1 Inspection Inspect parenteral drug products for particulate matter and discoloration prior to administration, whenever solution and container permit. Sodium nitroprusside should be a clear colorless to red/brown color; do not use if solution is blue, green, or bright …

5 WARNINGS AND PRECAUTIONS Thiocynate toxicity ( 5.3 ) Methemoglobinemia ( 5.4 ) Increases in intracranial pressure ( 5.5 ) Diminished capacity to compensate for anemia and hypovolemia with anesthesia during surgery ( 5.6 ) 5.1 Excessive Hypotension Sodium nitroprusside, can cause excessive hypotension leading to hypoperfusion of vital organs. Hypotension should resolve within 1-10 minutes after discontinuation of the nitroprusside infusion; during these few minutes, it may be helpful to put the patient into a head-down (Trendelenburg) position to …

4 CONTRAINDICATIONS Diseases with compensatory hypertension (e.g., coarctation of the aorta, arteriovenous shunting). Inadequate cerebral circulation or in moribund patients (A.S.A. Class 5E) coming to emergency surgery. Patients with congenital (Leber’s) optic atrophy or with tobacco amblyopia. Acute heart failure associated with reduced peripheral vascular resistance. Concomitant use with sildenafil, tadalafil, vardenafil, or riociguat. Diseases with compensatory hypertension (e.g. coarctation of the aorta, arteriovenous shunting) ( 4 ). Inadequate cerebral circulation or moribund patients (A.S.A. Class 5E) coming to emergency …

Sodium Nitroprusside In 0.9% Sodium Chloride is a prescription medication. You will need a valid prescription from a licensed healthcare provider.

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