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| U.S. Brand
Names |
|
| Tao® |

|
|
| Generic
Available |
|
|
No |

|
|
| Synonyms |
|
|
Triacetyloleandomycin |

|
|
| Pharmacological Index |
|
|
Antibiotic, Macrolide |

|
|
| Use |
|
|
Adjunct in the treatment of corticosteroid-dependent asthma due to its
steroid-sparing properties; antibiotic with spectrum of activity similar to
erythromycin |

|
|
| Pregnancy Risk
Factor |
|
|
C |

|
|
| Contraindications |
|
|
Hypersensitivity to troleandomycin, other macrolides, or any component;
concurrent use with cisapride |

|
|
| Warnings/Precautions |
|
|
Use with caution in patients with impaired hepatic function; chronic
hepatitis may occur in patients with long or repetitive
courses |

|
|
| Adverse
Reactions |
|
|
>10%: Gastrointestinal: Abdominal cramping and discomfort (dose-related)
1% to 10%:
Dermatologic: Urticaria, rashes
Gastrointestinal: Nausea, vomiting, diarrhea
<1%: Rectal burning, cholestatic jaundice |

|
|
| Overdosage/Toxicology |
|
|
Symptoms of overdose include nausea, vomiting, diarrhea, hearing loss
Following GI decontamination, treatment is supportive |

|
|
| Drug
Interactions |
|
|
CYP3A3/4 enzyme substrate; CYP3A3/4 and 3A5-7 enzyme inhibitor
|

|
|
| Mechanism of
Action |
|
|
Decreases methylprednisolone clearance from a linear first order decline to a
nonlinear decline in plasma concentration. Troleandomycin also has an undefined
action independent of its effects on steroid elimination. Inhibits RNA-dependent
protein synthesis at the chain elongation step; binds to the 50S ribosomal
subunit resulting in blockage of transpeptidation. |

|
|
| Pharmacodynamics/Kinetics |
|
|
Time to peak serum concentration: Within 2 hours
Elimination: 10% to 25% of dose excreted in urine as active drug; also
excreted in feces via bile |

|
|
| Usual Dosage |
|
|
Oral:
Adjunct in corticosteroid-dependent asthma: 14 mg/kg/day in divided doses
every 6-12 hours not to exceed 250 mg every 6 hours; dose is tapered to once
daily then alternate day dosing
Adults: 250-500 mg 4 times/day |

|
|
| Dietary
Considerations |
|
|
May be administered with food; presence of food delays absorption, but has no
effect on the extent of absorption |

|
|
| Administration |
|
|
Administer around-the-clock instead of 4 times/day |

|
|
| Monitoring
Parameters |
|
|
Hepatic function tests |

|
|
| Mental Health: Effects
on Mental Status |
|
|
Macrolides reported to cause nightmares, confusion, anxiety, or mood
lability |

|
|
| Mental Health:
Effects on Psychiatric
Treatment |
|
|
Contraindicated with pimozide; concurrent use with carbamazepine or triazolam
may produce additive toxicity; monitor |

|
|
| 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 |
|
|
Complete full course of therapy; notify physician if persistent or severe
abdominal pain, nausea, vomiting, jaundice, darkened urine, or fever
occurs |

|
|
| Nursing
Implications |
|
|
Monitor hepatic function tests |

|
|
| Dosage Forms |
|
|
Capsule: 250 mg |

|
|
| References |
|
|
Brenner AM and Szefler SJ,
"Troleandomycin in the Treatment of Severe Asthma," Immunol Allergy Clin
North Am, 1991, 11(1):91-102.
Kamada AK, Hill MR, Brenner AM, et al,
"Effect of Low-Dose Troleandomycin on Theophylline Clearance: Implications for Therapeutic Drug Monitoring,"
Pharmacotherapy, 1992, 12(2):98-102.
Spector SL, Katz FH, and Farr RS,
"Troleandomycin: Effectiveness in Steroid-Dependent Asthma and Bronchitis," J
Allergy Clin Immunol, 1974, 54(6):367-79.
Tartaglione TA,
"Therapeutic Options for the Management and Prevention of Mycobacterium avium Complex Infection in Patients With the Acquired Immunodeficiency Syndrome,"
Pharmacotherapy, 1996, 16(2):171-82.
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