Silodosin
- Atc Codes:G04CA04
- CAS Codes:160970-64-9
- PHARMGKB ID:160970-64-9
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Genes that may be involved
- Substrate of
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Silodyx, Urorec; Bulgaria: Silodyx, Urorec; Czech Republic: Silodyx, Urorec; Estonia: Silodyx, Urorec; Finland: Silodyx, Urorec; Germany: Silodyx, Urorec; Greece: Silodyx, Urorec; Ireland: Silodyx, Urorec; Latvia: Silodyx, Urorec; Lithuania: Silodyx, Urorec; Luxembourg: Silodyx, Urorec; Malta: Silodyx, Urorec; Netherlands: Silodyx, Urorec; Poland: Silodyx, Urorec; Portugal: Silodyx, Urorec; Slovakia: Silodyx, Urorec; Slovenia: Silodyx, Urorec; Spain: Silodyx, Urorec; Sweden: Silodyx, Urorec.
North America
USA: Rapaflo.
Asia
Japan: Urief.
Drug combinations
Chemistry
Silodosin: C~25~H~32~F~3~N~3~O~4~. Mw: 495.53. 1-(3-Hydroxypropyl)-5-[(2R)-2-({2-[2-(2,2,2-trifluoroethoxy)phenoxy]ethyl}amino)propyl]-2,3-dihydro-1H-indole-7-carboxamide. CAS-160970-64-9.
Pharmacologic Category
Selective α-Adrenergic Blocking Agents. α~1~-Adrenergic Receptor Antagonist. (ATC-Code: G04CA04).
Mechanism of action
Silodosin is a selective antagonist of post-synaptic α~1~ adrenoreceptors, which are located in the human prostate, bladder base, bladder neck, prostatic capsule, and prostatic urethra. Blockade of these α~1~ adrenoreceptors can cause the smooth muscle in these tissues to relax, resulting in an improvement in urine flow and a reduction in benign prostatic hyperplasia (BPH) symptoms. In an in vitro study examining binding affinity of silodosin to the three subtypes of the α~1~ adrenoreceptors (α~1A~, α~1B~ and α~1D~) the results demonstrated that silodosin binds with high affinity to the α~1A~ subtype.
Therapeutic use
Treatment of signs and symptoms of benign prostatic hyperplasia.
Pregnancy and lactiation implications
Silodosin is not approved for use in women.
Unlabeled use
Contraindications
Patients with severe renal impairment. Patients with severe hepatic impairment. Concomitant administration with strong CYP3A4 inhibitors (e.g. ketoconazole, clarithromycin, itraconazole, ritonavir).
Warnings and precautions
Postural hypotension, with or without symptoms (e.g. dizziness). In patients with moderate renal impairment, dose should be reduced. Should not be used in combination with other α-blockers. Examine patients thought to have BPH prior to starting therapy, rule out the presence of carcinoma of the prostate. Possibility of intraoperative floppy iris syndrome (IFIS) in cataract surgery. Not intended for use as an antihypertensive drug.