About: Silodosin     Goto   Sponge   NotDistinct   Permalink

An Entity of Type : http://linked.opendata.cz/ontology/drugbank/Drug, within Data Space : linked.opendata.cz associated with source document(s)

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http://linked.open...gbank/description
  • Silodosin is an α1-adrenoceptor antagonist that is selective for the prostate. Silodosin is for symptomatic treatment of benign prostatic hyperplasia. FDA approved Oct 9, 2008. (en)
http://linked.open...y/drugbank/dosage
http://linked.open...generalReferences
  • # Yoshida M, Homma Y, Kawabe K: Silodosin, a novel selective alpha 1A-adrenoceptor selective antagonist for the treatment of benign prostatic hyperplasia. Expert Opin Investig Drugs. 2007 Dec;16(12):1955-65. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/18042003 # Yamada S, Kato Y, Okura T, Kagawa Y, Kawabe K: Prediction of alpha1-adrenoceptor occupancy in the human prostate from plasma concentrations of silodosin, tamsulosin and terazosin to treat urinary obstruction in benign prostatic hyperplasia. Biol Pharm Bull. 2007 Jul;30(7):1237-41. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/17603160 (en)
http://linked.open...gy/drugbank/group
  • approved (en)
http://linked.open...drugbank/halfLife
  • Silodosin = 13.3 ± 8.07 hours; KMD-3213G = 24 hours; (en)
http://linked.open...ugbank/indication
  • Treatment for symptomatic relief of benign prostatic hyperplasia (en)
sameAs
Title
  • Silodosin (en)
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http://linked.open...mechanismOfAction
  • 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. (en)
http://linked.open...y/drugbank/patent
http://linked.open...outeOfElimination
  • Fecal (54.9%); Renal (33.5%) (en)
http://linked.open.../drugbank/synonym
  • KAD 3213 (en)
  • KMD 3213 (en)
  • Rapaflo (en)
  • Urief (en)
http://linked.open...drugbank/toxicity
  • Most common adverse reactions (incidence > 2%) are retrograde ejaculation, dizziness, diarrhea, orthostatic hypotension, headache, nasopharyngitis, and nasal congestion. (en)
http://linked.open...umeOfDistribution
  • 49.5 L (en)
http://linked.open...k/foodInteraction
  • The effect of a moderate fat, moderate calorie meal was variable and decreased silodosin Cmax by approximately 18 − 43% and AUC by 4 − 49% (en)
http://linked.open...nk/proteinBinding
  • 97% bound to protein (en)
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http://linked.open...ugbank/absorption
  • 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. (en)
http://linked.open.../affectedOrganism
  • Humans and other mammals (en)
http://linked.open...casRegistryNumber
  • 160970-54-7 (en)
http://linked.open...drugbank/category
  • (en)
http://linked.open...rugbank/clearance
  • Plasma clearance = 10 L/h (en)
http://linked.open...k/Bioavailability
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