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Pronunciation |
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(tole
AZ oh
leen) |
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U.S. Brand
Names |
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Priscoline® |
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Generic
Available |
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No |
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Synonyms |
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Benzazoline Hydrochloride; Tolazoline Hydrochloride |
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Pharmacological Index |
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Vasodilator |
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Use |
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Treatment of persistent pulmonary vasoconstriction and hypertension of the
newborn (persistent fetal circulation), peripheral vasospastic
disorders |
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Pregnancy Risk
Factor |
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C |
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Contraindications |
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Hypersensitivity to tolazoline; known or suspected coronary artery
disease |
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Warnings/Precautions |
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Stimulates gastric secretion and may activate stress ulcers; therefore, use
with caution in patients with gastritis, peptic ulcer; use with caution in
patients with mitral stenosis |
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|
Adverse
Reactions |
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1% to 10%:
Endocrine & metabolic: Hypochloremic alkalosis
Gastrointestinal: GI bleeding, abdominal pain, nausea, diarrhea
Hematologic: Thrombocytopenia, increased agranulocytosis, pancytopenia
Local: Burning at injection site
Neuromuscular & skeletal: Increased pilomotor activity
Ocular: Mydriasis
Renal: Acute renal failure, oliguria
Respiratory: Pulmonary hemorrhage
Miscellaneous: Increased secretions |
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Overdosage/Toxicology |
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Symptoms of overdose include hypotension, shock, flushing
I.V. fluids and Trendelenburg position for hypotension; if pressors are
required, use direct-acting alpha agonists (norepinephrine)
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Drug
Interactions |
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Decreased effect (vasopressor) of epinephrine followed by a rebound increase
in blood pressure
Increased toxicity: Disulfiram reaction may possibly be seen with concomitant
ethanol use |
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Stability |
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Compatible in D5W, D10W, and saline
solutions |
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Mechanism of
Action |
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Competitively blocks alpha-adrenergic receptors to produce brief antagonism
of circulating epinephrine and norepinephrine; reduces hypertension caused by
catecholamines and causes vascular smooth muscle relaxation (direct action);
results in peripheral vasodilation and decreased peripheral
resistance |
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Pharmacodynamics/Kinetics |
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Half-life: Neonates: 3-10 hours, increased half-life with decreased renal
function, oliguria
Time to peak serum concentration: Within 30 minutes
Elimination: Excreted rapidly in urine primarily as unchanged drug
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Usual Dosage |
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Neonates: Initial: I.V.: 1-2 mg/kg over 10-15 minutes via scalp vein or upper
extremity; maintenance: 1-2 mg/kg/hour; use lower maintenance doses in patients
with decreased renal function. Also used in neonates for acute vasospasm
"cath toes" at 0.25 mg/kg/hour (no load); maximum dose: 6-8 mg/kg/hour.
Dosing interval in renal impairment in newborns: Urine output <0.9
mL/kg/hour: Decrease dose to 0.08 mg/kg/hour for every 1 mg/kg of loading dose
Adults: Peripheral vasospastic disorder: I.M., I.V., S.C.: 10-50 mg 4
times/day |
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Dietary
Considerations |
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Alcohol: Avoid use |
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Administration |
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I.V.: Usual maximum concentration: 0.1 mg/mL |
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Monitoring
Parameters |
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Vital signs, blood gases, cardiac monitor |
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Mental Health: Effects
on Mental Status |
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None noted |
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Mental Health:
Effects on Psychiatric
Treatment |
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May cause agranulocytosis, caution with clozapine and carbamazepine; use with
alcohol may produce "disulfiram reaction" |
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Dental Health: Local
Anesthetic/Vasoconstrictor
Precautions |
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No information available to require special precautions |
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Dental Health:
Effects on Dental Treatment |
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No effects or complications reported |
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Patient
Information |
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Side effects decrease with continued therapy; avoid
alcohol |
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Nursing
Implications |
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Dilute in D5W; monitor blood pressure for hypotension; observe
limbs for change in color; do not mix with any other drug in syringe or
bag |
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Dosage Forms |
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Injection, as hydrochloride: 25 mg/mL (4 mL) |
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References |
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Ward RM, Daniel CH, Kendig JW, et al,
"Oliguria and Tolazoline Pharmacokinetics in the Newborn," Pediatrics,
1986, 77(3):307-15. |
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