ସିଲଡେନାଫିଲ

ସିଲଡେନାଫିଲ
Clinical data
Pronunciation	/sɪlˈdɛnəfɪl/ sil-DEN-ə-fil
Trade names	Viagra, Revatio, others
AHFS/Drugs.com	monograph
MedlinePlus	a699015
data	EU EMA: yes; US FDA: Sildenafil;
Pregnancy; category	AU: B1 ; US: B (No risk in non-human studies) ; ;
Routes of; administration	By mouth (tablets), IV
ATC code	G04BE03 (WHO) ;
Legal status
Legal status	AU: S4 (Prescription only) ; CA: ℞-only ; UK: Pharmacy medicines ; US: ℞-only ; ℞ (Prescription only);
Pharmacokinetic data
Bioavailability	41% (mean)
Protein binding	~96%
Metabolism	Liver: CYP3A4 (major route), CYP2C9 (minor route)
Metabolites	N-desmethylsildenafil (~50% potency for PDE5)
Elimination half-life	3–4 hours
Excretion	Feces (~80%), urine (~13%)
Identifiers
	IUPAC name 5-{2-Ethoxy-5-[(4-methylpiperazin-1-yl)sulfonyl]phenyl}-1-methyl-3-propyl-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one;
CAS Number	139755-83-2 ; Citrate: 171599-83-0 ;
PubChem CID	5212;
DrugBank	DB00203 ;
ChemSpider	5023 ;
UNII	3M7OB98Y7H;
KEGG	D08514 ;
ChEBI	CHEBI:9139 ;
ChEMBL	CHEMBL192 ;
PDB ligand	VIA (PDBe, RCSB PDB);
ECHA InfoCard	100.122.676
Chemical and physical data
Formula	C22H30N6O4S
Molar mass	474.5764 g/mol
3D model (JSmol)	Interactive image;
	SMILES CCCC1=NN(C2=C1N=C(NC2=O)C3=C(C=CC(=C3)S(=O)(=O)N4CCN(CC4)C)OCC)C;
	InChI InChI=1S/C22H30N6O4S/c1-5-7-17-19-20(27(4)25-17)22(29)24-21(23-19)16-14-15(8-9-18(16)32-6-2)33(30,31)28-12-10-26(3)11-13-28/h8-9,14H,5-7,10-13H2,1-4H3,(H,23,24,29) ; Key:BNRNXUUZRGQAQC-UHFFFAOYSA-N ;
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ସିଲଡେନାଫିଲ (ଇଂରାଜୀ ଭାଷାରେ Sildenafil, ବିକ୍ରୟ ନାମ ଭାଇଏଗ୍ରା/ Viagra) ଏକ ଔଷଧର (medication) ନାମ ଯାହା ଲିଙ୍ଗ ଉତ୍ଥାନ (erectile dysfunction) ସମସ୍ୟା ଓ ପଲମୋନାରି ହାଇପରଟେନସନ (pulmonary arterial hypertension) ଚିକିତ୍ସା ନିମନ୍ତେ ଦିଆଯାଏ । ^[୩] ମହିଳାମାନଙ୍କର ଯୌନ ସମସ୍ୟା ନିମନ୍ତେ ପ୍ରଭାବଶୀଳ କି ନୁହେଁ, ସେ ବିଷୟ ସ୍ପଷ୍ଟ ହୋଇନାହିଁ ।^[୩] ଏହା ପାଟିରେ (by mouth) ବା ଶିରାଭ୍ୟନ୍ତର ଇଞ୍ଜେକସନ (injection into a vein) ଆକାରରେ ଦିଆଯାଏ ।^[୩] ପ୍ରାୟ ୨୦ ମିନିଟ ମଧ୍ୟରେ ଏହା କାର୍ଯ୍ୟକ୍ଷମ ହୁଏ ଓ ୨ ଘଣ୍ଟା ପର୍ଯ୍ୟନ୍ତ ପ୍ରଭାବ ରହେ । ^[୩]

ସାଧାରଣ ପାର୍ଶ୍ୱ ପ୍ରତିକ୍ରିୟାରେ ମୁଣ୍ଡ ବିନ୍ଧା, ଛାତିଜ୍ୱାଳା (heartburn) ଓ ଚର୍ମ ଲାଲ ଦେଖାଯାଏ ।^[୩] ହୃତ୍‌ପିଣ୍ଡ ରକ୍ତନଳୀ ରୋଗ ଥିଲେ (cardiovascular disease) ସାବଧାନତା ସ‌ହିତ ଏହା ଦିଆଯାଏ ।^[୩] କ୍ୱଚିତ ଦୀର୍ଘକାଳୀନ ଲିଙ୍ଗ ଉତ୍ଥାନ (prolonged erection) ରହିପାରେ ଯାହା ଲିଙ୍ଗକୁ ନଷ୍ଟ କରିଦେଇପାରେ ।^[୩] ନାଇଟ୍ରୋଗ୍ଲିସେରିନ (nitroglycerin/ glycerin trinitrate) ଭଳି ନାଇଟ୍ରେଟ (nitrate) ସ‌ହିତ ସିଲଡେନାଫିଲ ଦେଲେ ରକ୍ତଚାପ (blood pressure) ସାଂଘାତିକ ଭାବରେ କମିଯାଉଥିବାରୁ ଏହା ଦିଆଯାଏନାହିଁ ।^[୩]

ସିଜିଏମ‌ପି-ସ୍ପେସିଫିକ ଫସଫୋଡାଇଇସ୍ଟରେଜ ଟାଇପ ୫ (phosphodiesterase 5/ PDE₅), ଏକ ଇଞ୍ଜାଇମ (enzyme) ଯାହା ସାଇକ୍ଲିକ ଗୁଆନୋସିନ ମୋନୋଫସଫେଟ (cGMP) ଭାଙ୍ଗି ଲିଙ୍ଗର (penis) ରକ୍ତସରାବରାହକୁ ନିୟନ୍ତ୍ରଣ କରେ ତାହାକୁ ସିଲଡେନାଫିଲ ଅବରୋଧ କରି କାର୍ଯ୍ୟକ୍ଷମ ହୁଏ ।^[୩] ଏହା କର୍ଯ୍ୟକ୍ଷମ ହେବା ନିମନ୍ତେ ଯୌନ ଉତ୍ତେଜନା (sexual arousal) ରହିବା ଆବଶ୍ୟକ ।^[୩] ଫୁସଫୁସର ଧମନୀଗୁଡ଼ିକ ମଧ୍ୟ ସ୍ଫୀତ ହୋଇଯାଏ । ^[୩]

ସନ ୧୯୮୯ରେ ଫାଇଜର (Pfizer) ପ୍ରଥମେ ହୃତ୍‌ପିଣ୍ଡ ସମ୍ପର୍କୀୟ ଯନ୍ତ୍ରଣା ବା ଆଞ୍ଜାଇନା (heart related chest pain) ଉପଶମ ନିମନ୍ତେ ସିଲଡେନାଫିଲ ଆବିଷ୍କର କରିଥିଲା । ^[୪] ସନ ୧୯୯୮ରେ ଡାକ୍ତରୀ ବ୍ୟବ‌ହାର ନିମନ୍ତେ ଯୁକ୍ତରାଷ୍ଟ୍ର ଆମେରିକା ଓ ୟୁରୋପରେ ଏହା ସ୍ୱୀକୃତ ହୋଇଥିଲା ।^[୩]^[୪] ସନ ୧୦୧୬ରେ ଯୁକ୍ତରାଷ୍ଟ୍ର ଆମେରିକାରେ ପ୍ରାୟ ୨ ନିୟୁତ ସିଲଡେନାଫିଲ ପ୍ରେସକ୍ରିପସନ ଲେଖାଯାଇଥିଲା ।^[୫] ସନ ୨୦୧୭ରେ ଏହା ଜେନେରିକ ଔଷଧ (generic medication) ଭାବରେ ମିଳିଲା ।^[୬] ସଂଯୁକ୍ତ ରାଷ୍ଟ୍ରରେ ଏହା ବିନା ପ୍ରେସକ୍ରିପସନରେ (over the counter) ମିଳେ ।^[୭] ସନ ୨୦୧୮ରେ ଯୁକ୍ତରାଷ୍ଟ୍ର ଆମେରିକାରେ ଏହାର ହୋଲସେଲ ମୂଲ୍ୟ ୧ ଡଲାରରୁ କମ୍ ଥିଲା ।^[୮]

ଆଧାର

↑ Nichols, DJ; Muirhead, GJ; Harness, JA (6 March 2002). "Pharmacokinetics of Sildenafil after Single Oral Doses in Healthy Male Subjects: Absolute Bioavailability, Food Effects and Dose Proportionality". British Journal of Clinical Pharmacology. 53: 5S–12S. doi:10.1046/j.0306-5251.2001.00027.x. PMC 1874258. PMID 11879254.
↑ "Viagra (sildenafil citrate) Tablets, for Oral Use. Full Prescribing Information". Pfizer Labs. Division of Pfizer, Inc., NY, NY 10017. Retrieved 5 November 2016.
↑ ^୩.୦୦ ^୩.୦୧ ^୩.୦୨ ^୩.୦୩ ^୩.୦୪ ^୩.୦୫ ^୩.୦୬ ^୩.୦୭ ^୩.୦୮ ^୩.୦୯ ^୩.୧୦ ^୩.୧୧ "Sildenafil Citrate". The American Society of Health-System Pharmacists. Retrieved 1 December 2014.
↑ ^୪.୦ ^୪.୧ Goldstein, I; Burnett, AL; Rosen, RC; Park, PW; Stecher, VJ (6 October 2018). "The Serendipitous Story of Sildenafil: An Unexpected Oral Therapy for Erectile Dysfunction". Sexual Medicine Reviews. 7 (1): 115–128. doi:10.1016/j.sxmr.2018.06.005. PMID 30301707.
↑ "The Top 300 of 2019". clincalc.com (in ଇଂରାଜୀ). Retrieved 21 November 2018.
↑ "Generic Viagra: Two versions of sildenafil hit the market today" (in ଇଂରାଜୀ). Retrieved 24 November 2018.
↑ LaMattina, John. "With Viagra Now Available Over-The-Counter In The U.K., Will The U.S. Follow Suit?". Forbes (in ଇଂରାଜୀ). Retrieved 24 November 2018.
↑ "NADAC as of 2018-11-21". Centers for Medicare and Medicaid Services (in ଇଂରାଜୀ). Archived from the original on 2019-06-01. Retrieved 24 November 2018.

ବାହ୍ୟ ଲିଙ୍କ

FDA Information
MedlinePLUS information, including side effects
U.S. National Library of Medicine: Drug Information Portal – Sildenafil
Viagra at The Periodic Table of Videos (University of Nottingham)

[1] Nichols, DJ; Muirhead, GJ; Harness, JA (6 March 2002). "Pharmacokinetics of Sildenafil after Single Oral Doses in Healthy Male Subjects: Absolute Bioavailability, Food Effects and Dose Proportionality". British Journal of Clinical Pharmacology. 53: 5S–12S. doi:10.1046/j.0306-5251.2001.00027.x. PMC 1874258. PMID 11879254.

[PI-2] "Viagra (sildenafil citrate) Tablets, for Oral Use. Full Prescribing Information". Pfizer Labs. Division of Pfizer, Inc., NY, NY 10017. Retrieved 5 November 2016.

[AHFS2014-3] ୩.୦୦ ^୩.୦୧ ^୩.୦୨ ^୩.୦୩ ^୩.୦୪ ^୩.୦୫ ^୩.୦୬ ^୩.୦୭ ^୩.୦୮ ^୩.୦୯ ^୩.୧୦ ^୩.୧୧ "Sildenafil Citrate". The American Society of Health-System Pharmacists. Retrieved 1 December 2014.

[Gold2018-4] ୪.୦ ^୪.୧ Goldstein, I; Burnett, AL; Rosen, RC; Park, PW; Stecher, VJ (6 October 2018). "The Serendipitous Story of Sildenafil: An Unexpected Oral Therapy for Erectile Dysfunction". Sexual Medicine Reviews. 7 (1): 115–128. doi:10.1016/j.sxmr.2018.06.005. PMID 30301707.

[5] "The Top 300 of 2019". clincalc.com (in ଇଂରାଜୀ). Retrieved 21 November 2018.

[6] "Generic Viagra: Two versions of sildenafil hit the market today" (in ଇଂରାଜୀ). Retrieved 24 November 2018.

[7] LaMattina, John. "With Viagra Now Available Over-The-Counter In The U.K., Will The U.S. Follow Suit?". Forbes (in ଇଂରାଜୀ). Retrieved 24 November 2018.

[8] "NADAC as of 2018-11-21". Centers for Medicare and Medicaid Services (in ଇଂରାଜୀ). Archived from the original on 2019-06-01. Retrieved 24 November 2018.

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Clinical data


Pronunciation	/sɪlˈdɛnəfɪl/ sil-DEN-ə-fil
Trade names	Viagra, Revatio, others
AHFS/Drugs.com	monograph
MedlinePlus	a699015
data	EU EMA: yes US FDA: Sildenafil
Pregnancy category	AU: B1 US: B (No risk in non-human studies)
Routes of administration	By mouth (tablets), IV
ATC code	G04BE03 (WHO)
Legal status
Legal status	AU: S4 (Prescription only) CA: ℞-only UK: Pharmacy medicines US: ℞-only ℞ (Prescription only)
Pharmacokinetic data
Bioavailability	41% (mean)^[୧]
Protein binding	~96%
Metabolism	Liver: CYP3A4 (major route), CYP2C9 (minor route)
Metabolites	N-desmethylsildenafil (~50% potency for PDE₅)
Elimination half-life	3–4 hours
Excretion	Feces (~80%), urine (~13%)^[୨]
Identifiers
IUPAC name 5-{2-Ethoxy-5-[(4-methylpiperazin-1-yl)sulfonyl]phenyl}-1-methyl-3-propyl-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one
CAS Number	139755-83-2^Y Citrate: 171599-83-0^N
PubChem CID	5212
DrugBank	DB00203^Y
ChemSpider	5023^N
UNII	3M7OB98Y7H
KEGG	D08514^Y
ChEBI	CHEBI:9139^N
ChEMBL	CHEMBL192^Y
PDB ligand	VIA (PDBe, RCSB PDB)
ECHA InfoCard	100.122.676
Chemical and physical data
Formula	C₂₂H₃₀N₆O₄S
Molar mass	474.5764 g/mol
3D model (JSmol)	Interactive image
SMILES CCCC1=NN(C2=C1N=C(NC2=O)C3=C(C=CC(=C3)S(=O)(=O)N4CCN(CC4)C)OCC)C
InChI InChI=1S/C22H30N6O4S/c1-5-7-17-19-20(27(4)25-17)22(29)24-21(23-19)16-14-15(8-9-18(16)32-6-2)33(30,31)28-12-10-26(3)11-13-28/h8-9,14H,5-7,10-13H2,1-4H3,(H,23,24,29)^N Key:BNRNXUUZRGQAQC-UHFFFAOYSA-N^N
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