| Pronunciation |
 (yu
RAP i
dil) |
 |
| U.S. Brand Names |
| Ebrantil®; Eupressyl®; Uraprene® |
|
| Synonyms |
| Urapidil Hydrochloride |
|
| Pharmacological Index |
|
Vasodilator |
|
| 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 |
|
| Drug Interactions |
|
Cimetidine modifies pharmacokinetics such that dosage reduction is necessary |
|
| Mechanism of Action |
|
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) |
|
| Usual Dosage |
|
Oral: 30-90 mg twice daily I.V.: 25 mg over 20 seconds |
|
| Reference Range |
|
Dose of 120 mg can cause a urapidil blood level of 750 ng/mL 3-5 hours postingestion |
|
| Additional Information |
|
20% as potent as prazosin; may increase plasma renin and catecholamine level |
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