Silodosin

495.53

495.53

1308068-626-2

CUZ39LUY82

DTXSID40167045

C81372

G04CA04|G - Genito urinary system and sex hormones

29339900

97

3.6

White to off-white solid

1.249±0.06 g/cm3(Predicted)

105

601.4±55.0 °C(Predicted)

317.5±31.5 °C

1.552

H2O: Very slightly soluble

2.58E-15mmHg at 25°C

D25 -14.0° (c = 1.01 in methanol)

P201, P202, P264, P270, P273, P280, P281, P301+P310, P301+P312, P302+P352, P305+P351+P338, P308+P313, P310, P321, P330, P332+P313, P362, P405, P501

H300

|Danger|H300 (33.33%): Fatal if swallowed [Danger Acute toxicity, oral]|P201, P202, P261, P264, P270, P271, P273, P280, P281, P301+P310, P301+P312, P302+P352, P304+P340, P305+P351+P338, P308+P313, P310, P312, P321, P330, P332+P313, P362, P403+P233, P405, and P501|Aggregated GHS information provided by 3 companies from 3 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

Most common adverse reactions (incidence > 2%) are retrograde ejaculation, dizziness, diarrhea, orthostatic hypotension, headache, nasopharyngitis, and nasal congestion.

Silodosin has been associated with a low rate of serum aminotransferase elevations (

97% bound to protein

Treatment for symptomatic relief of benign prostatic hyperplasia|FDA Label|Treatment of the signs and symptoms of benign prostatic hyperplasia (BPH)|Treatment of the signs and symptoms of benign prostatic hyperplasia (BPH).,|Treatment of the signs and symptoms of benign prostatic hyperplasia (BPH) in adult men.

Silodosin is a selective alpha-1a adrenergic antagonist used in the therapy of benign prostatic hypertrophy. Silodosin is associated with a low rate of serum aminotransferase elevations and to rare instances of clinically apparent acute liver injury.

Benign Prostatic Hypertrophy Agents

Silodosin is 583 times more selective for human alpha-1A receptors than alpha-1B receptors. It is also 56 times more selective for human alpha-1A receptors than alpha-1D. Silodosin does not prolong the QT interval.

Drugs used in the treatment of urogenital conditions and diseases such as URINARY INCONTINENCE; PROSTATIC HYPERPLASIA; and ERECTILE DYSFUNCTION. (See all compounds classified as Urological Agents.)|Drugs that bind to and block the activation of ADRENERGIC ALPHA-1 RECEPTORS. (See all compounds classified as Adrenergic alpha-1 Receptor Antagonists.)

Quickly absorbed and has a bioavailability of 32% at 8mg/day (therapeutic dose). When 8 mg of silodosin is taken once daily with food, the pharmacokinetic parameters are as follows: Cmax = 61.6 ± 27.54 ng/mL; Tmax = 2.6 ± 0.90 hours; AUC (0h-24h) = 373 ng•hr/ml. The AUC of its metabolite, KMD3213G, is four times greater than silodosin.|Fecal (54.9%); Renal (33.5%)|49.5 L|Plasma clearance = 10 L/h

Extensively metabolized in the liver. The main metabolite is generated via glucuronidation (KMD-3213G) by UDP-2B7. Oxidation by alcohol and aldehyde dehydrogenases produces the second major metabolite, KMD-3293. KMD-3213G accumulates in the plasma as it is very hydrophilic. KMD-3213G is also an active metabolite in which it has 50% of silodosin's inhibitory activity. KMD-3293 is inactive. Cytochrome P450 CYP 3A4 also generates some metabolites.

Silodosin = 13.3 ± 8.07 hours; KMD-3213G = 24 hours;

Benign prostate hyperplasia (BPH), or an enlarged prostate, is a condition found only in men and is characterized by a non-cancerous enlargement of the prostate gland. Symptoms of BPH include urinary difficulty, urinary frequency and an inability to complete bladder emptying. Silodosin is highly uroselective for the alpha (1A) receptors located in the prostate, [urethrea and bladder trigone in the lower urinary tract]. Blocking these receptors relaxes the smooth muscles, resulting in an improvement in urine flow and a reduction in BPH symptoms. The selective binding of silodosin to the alpha (1A) receptors is substantially greater than the binding to the cardiovascular-associated alpha (1B) receptors and thereby maximizes target organ activity while minimizing the potential for blood pressure effects. [Watson Pharmaceutical Inc. Press release] Silodosin is alpha 1A-adrenoceptor selective antagonist which inhibits sympathetic nerve stimulation and relaxation of smooth muscle tone in the lower urinary tract which relieves the pressure from contraction of smooth muscle. The reduction of intraurethral pressure improves voiding and storage issues associated with BPH.

1-(3-hydroxypropyl)-5-(2-(2-(2-(2,2,2-trifluoroethoxy)phenoxy)ethylamino)propyl)indoline-7-carboxamide

Human drugs -> Silodyx -> EMA Drug Category|Urologicals -> Human pharmacotherapeutic group|Human drugs -> Urorec -> EMA Drug Category|Human drugs -> Silodosin Recordati -> EMA Drug Category|Urologicals, Alpha-adrenoreceptor antagonists -> Human pharmacotherapeutic group|Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients