| U.S. Brand Names |
| Ebrantil®; Eupressyl®; Uraprene® |
 |
| Synonyms |
| Urapidil Hydrochloride |
|
| Pharmacological Index |
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Vasodilator |
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| Adverse Reactions |
|
Cardiovascular: Palpitations, bradycardia, hypotension (orthostatic), sinus bradycardia Central nervous system: Headache, dizziness, fatigue Dermatologic: Allergic skin reactions, pruritus Gastrointestinal: Nausea Renal: Enuresis Respiratory: Nasal congestion |
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| Drug Interactions |
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Cimetidine modifies pharmacokinetics such that dosage reduction is necessary |
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| Mechanism of Action |
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Alpha1-adrenoceptor antagonist (peripheral vasodilator); a phenylpiperazine derivative of 4-aminouracil |
|
| Pharmacodynamics/Kinetics |
|
Protein binding: 80% Metabolism: Hepatic to p-hydroxylated urapidil - first pass (20%) Bioavailability: 70% Half-life: Oral: 4.7 hours I.V.: 2.7 hours Elimination: Urine (15% to 30% unchanged) |
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| Usual Dosage |
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Oral: 30-90 mg twice daily I.V.: 25 mg over 20 seconds |
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| Reference Range |
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Dose of 120 mg can cause a urapidil blood level of 750 ng/mL 3-5 hours postingestion |
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| Additional Information |
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20% as potent as prazosin; may increase plasma renin and catecholamine level |
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