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Pronunciation |
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(troe
lee an doe MYE
sin) |
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U.S. Brand
Names |
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Tao® |
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Generic
Available |
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No |
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Synonyms |
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Triacetyloleandomycin |
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Pharmacological Index |
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Antibiotic, Macrolide |
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Use |
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Adjunct in the treatment of corticosteroid-dependent asthma due to its
steroid-sparing properties; antibiotic with spectrum of activity similar to
erythromycin |
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Pregnancy Risk
Factor |
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C |
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Contraindications |
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Hypersensitivity to troleandomycin, other macrolides, or any component;
concurrent use with cisapride |
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Warnings/Precautions |
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Use with caution in patients with impaired hepatic function; chronic
hepatitis may occur in patients with long or repetitive
courses |
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Adverse
Reactions |
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>10%: Gastrointestinal: Abdominal cramping and discomfort (dose-related)
1% to 10%:
Dermatologic: Urticaria, rashes
Gastrointestinal: Nausea, vomiting, diarrhea
<1%: Rectal burning, cholestatic jaundice |
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Overdosage/Toxicology |
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Symptoms of overdose include nausea, vomiting, diarrhea, hearing loss
Following GI decontamination, treatment is supportive |
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Drug
Interactions |
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CYP3A3/4 enzyme substrate; CYP3A3/4 and 3A5-7 enzyme inhibitor
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Mechanism of
Action |
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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. |
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Pharmacodynamics/Kinetics |
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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 |
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Usual Dosage |
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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 |
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Dietary
Considerations |
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May be administered with food; presence of food delays absorption, but has no
effect on the extent of absorption |
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Administration |
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Administer around-the-clock instead of 4 times/day |
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Monitoring
Parameters |
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Hepatic function tests |
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Mental Health: Effects
on Mental Status |
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Macrolides reported to cause nightmares, confusion, anxiety, or mood
lability |
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Mental Health:
Effects on Psychiatric
Treatment |
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Contraindicated with pimozide; concurrent use with carbamazepine or triazolam
may produce additive toxicity; monitor |
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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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Complete full course of therapy; notify physician if persistent or severe
abdominal pain, nausea, vomiting, jaundice, darkened urine, or fever
occurs |
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Nursing
Implications |
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Monitor hepatic function tests |
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Dosage Forms |
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Capsule: 250 mg |
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References |
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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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