Metyrosine

Enzyme Inhibitors

Metyrosine Brand names, Metyrosine Analogs

Metyrosine Brand Names Mixture

No information avaliable

Metyrosine Chemical_Formula

C₁₀H₁₃NO₃

Metyrosine RX_link

http://www.rxlist.com/cgi/generic2/metyrosine.htm

Metyrosine fda sheet

Metyrosine msds (material safety sheet)

Metyrosine Synthesis Reference

No information avaliable

Metyrosine Molecular Weight

195.215 g/mol

Metyrosine Melting Point

312.5 ^oC

Metyrosine H₂O Solubility

Very slightly soluble

Metyrosine State

Solid

Metyrosine LogP

-1.475

Metyrosine Dosage Forms

Capsules for oral administration (250 mg)

Metyrosine Indication

For use in the treatment of patients with pheochromocytoma for preoperative preparation of patients for surgery, management of patients when surgery is contraindicated, and chronic treatment of patients with malignant pheochromocytoma.

Metyrosine Pharmacology

In patients with pheochromocytoma, who produce excessive amounts of norepinephrine and epinephrine, administration of one to four grams of metyrosine per day has reduced catecholamine biosynthesis from about 35 to 80 percent as measured by the total excretion of catecholamines and their metabolites (metanephrine and vanillylmandelic acid). The maximum biochemical effect usually occurs within two to three days, and the urinary concentration of catecholamines and their metabolites usually returns to pretreatment levels within three to four days after metyrosine is discontinued. Most patients with pheochromocytoma treated with metyrosine experience decreased frequency and severity of hypertensive attacks with their associated headache, nausea, sweating, and tachycardia. In patients who respond, blood pressure decreases progressively during the first two days of therapy with metyrosine; after withdrawal, blood pressure usually increases gradually to pretreatment values within two to three days.

Metyrosine Absorption

Well absorbed from the gastrointestinal tract.

Metyrosine side effects and Toxicity

Signs of metyrosine overdosage include those central nervous system effects observed in some patients even at low dosages. At doses exceeding 2000 mg/day, some degree of sedation or feeling of fatigue may persist. Doses of 2000-4000 mg/day can result in anxiety or agitated depression, neuromuscular effects (including fine tremor of the hands, gross tremor of the trunk, tightening of the jaw with trismus), diarrhea, and decreased salivation with dry mouth. The acute toxicity of metyrosine was 442 mg/kg and 752 mg/kg in the female mouse and rat respectively.

Metyrosine Patient Information