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Approximately 90% of a dose of phenylpropanolamine is excreted in the urine unchanged within 24 hours. [4] [6] [7] [5] About 4% of excreted material is in the form of metabolites. [4] The elimination half-life of immediate-release phenylpropanolamine is about 4 hours, with a range in different studies of 3.7 to 4.9 hours.
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Chlorphenamine is often combined with phenylpropanolamine to form an allergy medication with both antihistamine and decongestant properties, though phenylpropanolamine is no longer available in the US after studies showed it increased the risk of stroke in young women. [7] Chlorphenamine remains available with no such risk.
Shannon and co-workers confirmed and extended some of Tainter's studies. After administering phenylethanolamine to dogs intravenously, these investigators observed that 10–30 mg/kg of the drug increased pupil diameter, and decreased body temperature; a dose of 10 or 17.5 mg/kg decreased heart rate, but a 30 mg/kg dose caused it to increase.
Brain death is observed first. Breathing generally stops within seconds. However, euthanasia may be delayed in dogs that have deficient cardiac and circulatory function. [2] The pentobarbital component produces anaesthesia and rapid unconsciousness. A lethal dose causes loss of medullary respiration and vasomotor function.
The primary application for phentolamine is for the control of hypertensive emergencies, most notably due to pheochromocytoma. [5]It also has usefulness in the treatment of cocaine-induced cardiovascular complications, where one would generally avoid β-blockers (e.g. metoprolol), as they can cause unopposed α-adrenergic mediated coronary vasoconstriction, worsening myocardial ischemia and ...