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Therefore, in the absence of any significant renal or liver disease, nitroprusside is

the preferred treatment for M.R.

Hemodynamic Effects

Nitroprusside has many pharmacologic effects that should improve M.R.’s condition.

It dilates both venous and arterial vessels, thereby increasing venous capacitance and

decreasing the venous return or preload on the heart (see Chapter 14, Heart Failure).

A decrease in the pulmonary capillary wedge pressure and ventricular filling

pressure will ultimately improve M.R.’s pulmonary edema. Afterload is also

decreased as a result of arterial dilation. This action increases cardiac output,

reduces arterial pressure, and increases tissue perfusion.

Concurrent Use of Diuretics

CASE 16-2, QUESTION 3: Should M.R. be given a diuretic before nitroprusside therapy is begun?

Administration of potent IV diuretics is relatively ineffective in the acute treatment

of hypertensive crisis except in patients with concomitant volume overload or HF.

Many patients with hypertensive emergencies are vasoconstricted and have normal or

reduced plasma volumes; therefore, diuretics have little effect and may actually

aggravate renal impairment or cause other adverse effects.

22,64 Furthermore, when

diuretics are given acutely in combination with other antihypertensive agents,

profound hypotension can occur.

The immediate value of diuretics in acute HF is related more to their hemodynamic

effects (venodilation) than to diuresis. Venodilation after IV diuretic administration

decreases right-sided cardiac filling pressures, decreases pulmonary artery and

wedge pressures, and increases cardiac output before diuresis occurs.

65 The presence

of HF and severely elevated BP in M.R. warrants IV administration of a loop

diuretic (e.g., furosemide 40 mg, torsemide [Demadex] 10–20 mg, or bumetanide

[Bumex] 1 mg).

Dosing and Administration

CASE 16-2, QUESTION 4: What dose of nitroprusside should be used initially?

Effective infusion rates range from 0.25 to 10 mcg/kg/minute.

66,67 For M.R., an

infusion of nitroprusside should be initiated at a rate of 0.25 mcg/kg/minute. The dose

should be increased slowly by 0.25 mcg/kg/minute every 5 minutes until the desired

pressure is achieved. A maximum infusion rate of 10 mcg/kg/minute has been

recommended. If adequate BP reduction is not achieved within 10 minutes after

maximal dose infusion, nitroprusside should be discontinued.

4 The dosage must be

individualized according to patient response using continuous intraarterial BP

recording and observing for signs or symptoms of toxicity.

Nitroprusside decomposes on exposure to light, so the solution should be shielded

with an opaque sleeve. It is not necessary to protect the tubing from light.

Reconstituted solutions are stable for 24 hours at room temperature. A change in the

solution’s color from light brown to dark brown, green, orange, or blue indicates a

loss in activity. The solution should be discarded if this change occurs.

Therapeutic End Point

CASE 16-2, QUESTION 5: A nitroprusside infusion is started. What is the goal of therapy?

For most patients BP should be reduced by no more than 25% within the first

minutes to hour, then if stable, therapy can be titrated to achieve a goal BP of

160/100 mm Hg during the next 2 to 6 hours. BPs can be reduced to near-normal

levels within 8 to 24 hours. However, because M.R. has cerebral occlusive disease

(carotid bruits), excessive reduction of his BP should be avoided. Overly aggressive

reduction of BP in the presence of major cerebral vessel stenosis may decrease

cerebral blood flow and produce strokes or other neurologic complications.

Normal cerebral blood flow remains relatively constant over a wide range of

systemic BP measurements through autoregulatory mechanisms.

40,68 The

autoregulatory effects can prevent large alterations in cerebral blood flow from

either slow or rapid changes in systemic arterial pressures. In addition, the arterial

BP required to maintain cerebral perfusion is higher in hypertensive patients than in

normotensive individuals. If M.R.’s BP is reduced excessively, cerebral blood flow

may decrease sharply. Therefore, a DBP of 100 to 105 mm Hg would be a

reasonable initial therapeutic goal for him in the first 6 hours. If hypotension occurs,

nitroprusside should be discontinued and M.R. should be placed in the

Trendelenburg position, in which the head is kept lower than the trunk.

Cyanide Toxicity

CASE 16-2, QUESTION 6: M.R. is being treated with nitroprusside. However, during the last 36 hours, dose

titration to 7 mcg/kg/minute has been necessary to control his BP. His tachycardia angina have resolved. Is he

at risk of developing cyanide toxicity? What indices of toxicity should be monitored? Are there agents available

to prevent toxicity?

A major concern when using sodium nitroprusside is toxicity secondary to the

accumulation of its metabolic by-products, cyanide, and thiocyanate. Sodium

nitroprusside decomposes within a few minutes after IV infusion. Free cyanide,

which represents 44% of nitroprusside by weight, is released into the bloodstream,

producing prussic acid (hydrogen cyanide), which is responsible for the acute

toxicity.

69 The amount of hydrogen cyanide released is dose related.

70 Endogenous

detoxification of cyanide occurs through a mitochondrial rhodanese system, which, in

the presence of a sulfur donor such as thiosulfate, converts cyanide to thiocyanate.

69

Theoretically, cyanide can be expected to accumulate in the body when the rate of the

sodium nitroprusside infusion exceeds 2 mcg/kg/minute for a prolonged period. The

presence of hepatic or renal impairment may also predispose the patient to cyanide

toxicity.

71,72

Symptomatic cyanide toxicity occurs infrequently; however, several deaths have

been reported after the use of sodium nitroprusside.

73 Cyanide toxicity occurs most

commonly when large doses (total dose 1.5 mg/kg) of nitroprusside are administered

rapidly to patients undergoing a surgical procedure that requires induction of

hypotension. However, cyanide toxicity and mortality

p. 341

p. 342

associated with nitroprusside exceed 3,000 and 1,000 cases per year,

respectively, according to two sources.

73,74

Although concurrent sodium thiosulfate administration has been recommended in

high-risk patients, no clinical data are available to indicate that it reduces overall

mortality.

75 Furthermore, this intervention may result in the accumulation of

thiocyanate, particularly if sodium thiosulfate is given at high infusion rates or to

patients with renal insufficiency. Hydroxocobalamin has also been used to reduce the

risk of cyanide toxicity secondary to nitroprusside infusions, but its use is limited

because of poor availability and cost considerations.

72 With the availability of safer

alternatives (e.g., fenoldopam, IV labetalol, IV nicardipine) for use in high-risk

patients, the use of hydroxocobalamin or thiosulfate is rarely required.

Cyanide toxicity can be detected early by monitoring M.R.’s metabolic status.

Lactic acidosis is an early indicator of toxicity because the progressive inactivation

of cytochrome oxidase by cyanide results in increased anaerobic glycolysis.

76,77 A

low plasma bicarbonate concentration and low pH, accompanied by an increase in

the blood lactate or lactate-to-pyruvate ratio could indicate cyanide toxicity.

77

Additional signs of cyanide intoxication include tachycardia, altered consciousness,

coma, convulsions, and the occasional smell of almonds on the breath.

70,77 Measuring

serum thiocyanate levels is of no value in detecting the onset of cyanide toxicity. If

toxicity develops, the infusion should be stopped and appropriate therapy for cyanide

intoxication instituted. The need for such a high-dose infusion of nitroprusside to

maintain M.R.’s pressure may increase his risk for cyanide toxicity, warranting close

monitoring of his acid–base balance.

Thiocyanate Toxicity

CASE 16-2, QUESTION 7: Explain the difference between cyanide toxicity and thiocyanate toxicity. What is

M.R.’s risk for thiocyanate toxicity if he is continued on a dose of 7 mcg/kg/minute? Is monitoring of serum

thiocyanate concentrations necessary?

Sodium nitroprusside is more likely to produce thiocyanate toxicity. Although this

complication is also rare, patients with renal impairment who receive infusions

beyond 72 hours are particularly susceptible. Conversion of cyanide to thiocyanate,

via sulfation by the liver, proceeds relatively slowly. The half-life of thiocyanate is

2.7 days with normal renal function and up to 9 days in patients with renal failure.

78

When sodium nitroprusside is infused for several days at moderate dosages (2–5

mcg/kg/minute), toxic levels of thiocyanate can occur within 7 to 14 days in patients

with normal renal function and 3 to 6 days in patients with severe renal disease.

69

Thiocyanate causes a neurotoxic syndrome manifested by psychosis, hyperreflexia,

confusion, weakness, tinnitus, seizures, and coma.

71,78 Prolonged exposure to

thiocyanate can suppress thyroid function through inhibition of iodine uptake and

binding by the thyroid gland.

78 Measurement of blood levels of thiocyanate is only

recommended in patients with renal disease or when the duration of the nitroprusside

infusion exceeds 3 or 4 days. Nitroprusside should be discontinued if serum

thiocyanate levels exceed 10 to 12 mg/dL.

79,80 Life-threatening toxicity is of concern

when blood thiocyanate levels exceed 20 mg/dL. In emergency cases, thiocyanate can

be readily removed by hemodialysis.

78

For M.R., the potential for thiocyanate toxicity is low because his renal function is

normal and the anticipated infusion duration is relatively short. Therefore,

measurement of thiocyanate levels is not indicated.

Other side effects associated with nitroprusside therapy include nausea, vomiting,

diaphoresis, nasal stuffiness, muscular twitching, dizziness, and weakness. These

effects are usually acute and occur when nitroprusside is administered too rapidly.

They can be reversed by decreasing the infusion rate.

CASE 16-2, QUESTION 8: M.R.’s serum chemistries and arterial blood gas values indicate a metabolic

acidosis. Should the nitroprusside infusion be continued at 7 mcg/kg/minute? What alternatives are available?

Although the duration of M.R.’s nitroprusside therapy has been short, tolerance to

the antihypertensive effect requires the use of a high-dose infusion to maintain BP

control. Thus, acidosis may represent toxicity as a result of cyanide accumulation.

The nitroprusside infusion should be discontinued at this time, and another rapidly

acting, easily titratable parenteral antihypertensive such as fenoldopam or IV

nicardipine should be initiated.

FENOLDOPAM

CASE 16-2, QUESTION 9: What are the advantages and disadvantages of fenoldopam compared with

sodium nitroprusside?

Fenoldopam is a parenteral, rapidly acting, peripheral dopamine-1 agonist used to

manage hypertensive crisis when a rapid reduction in BP is required.

81–84 Stimulation

of the dopamine-1 receptors vasodilates coronary, renal, mesenteric, and peripheral

arteries.

85,86 Fenoldopam has been used to control perioperative hypertension in

patients undergoing cardiac bypass surgery.

87 The use of low-dose fenoldopam had

been evaluated in those with acute kidney injury following cardiac surgery; therapy

was not associated with a reduced risk of renal replacement therapy or 30-day

mortality.

88 This refutes prior theories that dilation of the renal arteries with

fenoldopam may reduce the risk of renal complications.

62,86

Fenoldopam is as effective as sodium nitroprusside for treatment of hypertensive

emergencies and does not cause either cyanide or thiocyanate toxicity.

57–59

Fenoldopam can be considered as an alternative to nitroprusside in patients who are

at high risk for cyanide or thiocyanate toxicity. Over the past several years, the use of

fenoldopam as an antihypertensive has decreased.

20

Clearance of fenoldopam is not altered by renal or liver disease. Like

nitroprusside, fenoldopam also has a short duration of action, with an elimination

half-life of approximately 5 minutes, thus allowing for easy titration.

83,89 BP and heart

rate should be frequently to avoid hypotension and dose-related reflex tachycardia.

Flushing and headache may occur. Serum potassium should be monitored and

repleted as necessary. Fenoldopam should be used cautiously in patients with

glaucoma or intraocular hypertension due to a dose-dependent increase in intraocular

pressure.

90,91

CASE 16-2, QUESTION 10: Which antihypertensive agents should be avoided in M.R.? Why?

Labetalol, a potent, rapidly acting antihypertensive with both α- and β-blocking

activity, is very effective in the treatment of hypertensive emergencies,

91–98 but it

should not be used in M.R. Hemodynamically, labetalol reduces peripheral vascular

resistance (afterload), BP, and heart rate, with almost no change in the resting

cardiac output or stroke volume.

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