|
| Pronunciation |
|
(me
TYE roe
seen) |

|
|
| U.S. Brand
Names |
|
| Demser® |

|
|
| Generic
Available |
|
|
No |

|
|
| Synonyms |
|
|
AMPT; OGMT |

|
|
| Pharmacological Index |
|
|
Tyrosine Hydroxylase Inhibitor |

|
|
| Use |
|
|
Short-term management of pheochromocytoma before surgery, long-term
management when surgery is contraindicated or when
malignant |

|
|
| Pregnancy Risk
Factor |
|
|
C |

|
|
| Contraindications |
|
|
Hypertension of unknown etiology, known hypersensitivity to
metyrosine |

|
|
| Warnings/Precautions |
|
|
Maintain fluid volume during and after surgery; use with caution in patients
with impaired renal or hepatic function |

|
|
| Adverse
Reactions |
|
|
>10%:
Central nervous system: Drowsiness, extrapyramidal symptoms
Gastrointestinal: Diarrhea
1% to 10%:
Endocrine & metabolic: Galactorrhea, edema of the breasts
Gastrointestinal: Nausea, vomiting, xerostomia
Genitourinary: Impotence
Respiratory: Nasal congestion
<1%: Lower extremity edema, depression, hallucinations, disorientation,
parkinsonism, urticaria, urinary problems, anemia, eosinophilia, hematuria,
hyperstimulation after withdrawal |

|
|
| Overdosage/Toxicology |
|
|
Signs of overdose include sedation, fatigue, tremor; reducing dose or
discontinuation of therapy usually results in resolution of
symptoms |

|
|
| Drug
Interactions |
|
|
Phenothiazines, haloperidol may potentiate EPS |

|
|
| Mechanism of
Action |
|
|
Blocks the rate-limiting step in the biosynthetic pathway of catecholamines.
It is a tyrosine hydroxylase inhibitor, blocking the conversion of tyrosine to
dihydroxyphenylalanine. This inhibition results in decreased levels of
endogenous catecholamines. Catecholamine biosynthesis is reduced by 35% to 80%
in patients treated with metyrosine 1-4 g/day. |

|
|
| Pharmacodynamics/Kinetics |
|
|
Half-life: 7.2 hours
Elimination: Following oral absorption, excreted primarily unchanged in urine
|

|
|
| Usual Dosage |
|
|
Children >12 years and Adults: Oral: Initial: 250 mg 4 times/day,
increased by 250-500 mg/day up to 4 g/day; maintenance: 2-3 g/day in 4 divided
doses; for preoperative preparation, administer optimum effective dosage for 5-7
days |

|
|
| Dietary
Considerations |
|
|
Alcohol: Additive CNS effect, avoid use |

|
|
| Mental Health: Effects
on Mental Status |
|
|
Drowsiness and extrapyramidal reactions are common; may cause depression,
hallucinations, or confusion |

|
|
| Mental Health:
Effects on Psychiatric
Treatment |
|
|
Concurrent use with antipsychotics may increase the risk of extrapyramidal
symptoms |

|
|
| 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 |
|
|
Take plenty of fluids each day; may cause drowsiness, impair coordination and
judgment; notify physician if drooling, tremors, speech difficulty, or diarrhea
occurs; avoid alcohol and central nervous system
depressants |

|
|
| Nursing
Implications |
|
|
Administer plenty of fluids each day; may cause drowsiness, impair
coordination and judgment; notify physician if drooling, tremors, speech
difficulty, or diarrhea occurs; avoid alcohol and central nervous system
depressants |

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

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