|
| U.S. Brand
Names |
|
| Priscoline® |

|
|
| Generic
Available |
|
|
No |

|
|
| Synonyms |
|
|
Benzazoline Hydrochloride; Tolazoline Hydrochloride |

|
|
| Pharmacological Index |
|
|
Vasodilator |

|
|
| Use |
|
|
Treatment of persistent pulmonary vasoconstriction and hypertension of the
newborn (persistent fetal circulation), peripheral vasospastic
disorders |

|
|
| Pregnancy Risk
Factor |
|
|
C |

|
|
| Contraindications |
|
|
Hypersensitivity to tolazoline; known or suspected coronary artery
disease |

|
|
| Warnings/Precautions |
|
|
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 |

|
|
| Adverse
Reactions |
|
|
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 |

|
|
| Overdosage/Toxicology |
|
|
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)
|

|
|
| Drug
Interactions |
|
|
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 |

|
|
| Stability |
|
|
Compatible in D5W, D10W, and saline
solutions |

|
|
| Mechanism of
Action |
|
|
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 |

|
|
| Pharmacodynamics/Kinetics |
|
|
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
|

|
|
| Usual Dosage |
|
|
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 |

|
|
| Dietary
Considerations |
|
|
Alcohol: Avoid use |

|
|
| Administration |
|
|
I.V.: Usual maximum concentration: 0.1 mg/mL |

|
|
| Monitoring
Parameters |
|
|
Vital signs, blood gases, cardiac monitor |

|
|
| Mental Health: Effects
on Mental Status |
|
|
None noted |

|
|
| Mental Health:
Effects on Psychiatric
Treatment |
|
|
May cause agranulocytosis, caution with clozapine and carbamazepine; use with
alcohol may produce "disulfiram reaction" |

|
|
| Dental Health: Local
Anesthetic/Vasoconstrictor
Precautions |
|
|
No information available to require special precautions |

|
|
| Dental Health:
Effects on Dental Treatment |
|
|
No effects or complications reported |

|
|
| Patient
Information |
|
|
Side effects decrease with continued therapy; avoid
alcohol |

|
|
| Nursing
Implications |
|
|
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 |

|
|
| Dosage Forms |
|
|
Injection, as hydrochloride: 25 mg/mL (4 mL) |

|
|
| References |
|
|
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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