ଡକ୍ସେପିନ

ଡକ୍ସେପିନ
Clinical data
Trade names	Sinequan, Quitaxon, Aponal, others
Synonyms	NSC-108160
AHFS/Drugs.com	monograph
MedlinePlus	a682390
data	US FDA: Doxepin;
Pregnancy; category	AU: C ; US: B (No risk in non-human studies) ; ;
Routes of; administration	By mouth, topical, intravenous, intramuscular injection
Drug class	Tricyclic antidepressant (TCA)
ATC code	D04AX01 (WHO) ; N06AA12;
Legal status
Legal status	AU: S4 (Prescription only) ; CA: ℞-only ; UK: POM (Prescription only) ; US: ℞-only ;
Pharmacokinetic data
Bioavailability	13–45% (mean 29%)
Protein binding	76%
Metabolism	Hepatic (CYP2D6, CYP2C19)
Metabolites	Nordoxepin, glucuronide conjugates
Elimination half-life	Doxepin: 8–24 hours (mean 17 hours) ; Nordoxepin: 31 hours
Excretion	Urine: ~50%; Feces: minor
Identifiers
	IUPAC name (E/Z)-3-(dibenzo[b,e]oxepin-11(6H)-ylidene)-N,N-dimethylpropan-1-amine;
CAS Number	1668-19-5 ;
PubChem CID	3158;
IUPHAR/BPS	1225;
DrugBank	DB01142 ;
ChemSpider	3046 ;
UNII	5ASJ6HUZ7D;
KEGG	D07875 ;
ChEBI	CHEBI:4710 ;
ChEMBL	CHEMBL1628227 ;
Chemical and physical data
Formula	C19H21NO
Molar mass	279.376 g/mol
3D model (JSmol)	Interactive image;
	SMILES CN(C)CC/C=C1C2=C(C=CC=C2)OCC3=C/1C=CC=C3;
	InChI InChI=1S/C19H21NO/c1-20(2)13-7-11-17-16-9-4-3-8-15(16)14-21-19-12-6-5-10-18(17)19/h3-6,8-12H,7,13-14H2,1-2H3 ; Key:ODQWQRRAPPTVAG-UHFFFAOYSA-N ;
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ଡକ୍ସେପିନ (ଇଂରାଜୀ ଭାଷାରେ Doxepin) ଏକ ଔଷଧ ଯାହା ପ୍ରମୁଖ ଅବସାଦ ବେମାରୀ, ଉଦ୍‌ବେଗ ଅବ୍ୟବସ୍ଥା, କ୍ରନିକ ହାଇଭ୍‌ସ ଓ ନିଦ୍ରା ସମସ୍ୟା (trouble sleeping) ଭଳି ରୋଗମାନଙ୍କ ଚିକିତ୍ସାରେ ଦିଆଯାଏ ।^[୬]^[୭] ହାଇଭ୍‌ସ ରୋଗରେ ଆଣ୍ଟିହିସ୍ଟାମିନ (antihistamines) ଅଧିକ ପସନ୍ଦ କରାଯାଏ ।^[୬] ନିଦ୍ରା ମମସ୍ୟାରେ ଏହା ସାମାନ୍ୟ ବା ମଧ୍ୟମ ଧରଣର ଉପକାର ଦିଏ । ^[୮] ଆଟୋପିକ ଡର୍ମାଟାଇଟିସ, ଲାଇଚେନ ସିମ୍ପ୍ଲେକ୍ସ କ୍ରନିକସ lichen simplex chronicus ରୋଗରେ ହେଉଥିବା ଗଲୁ ନିମନ୍ତେ ଏହା ଏହାର କ୍ରିମ (cream) ବ୍ୟବ‌ହାର କରାଯାଏ ।^[୯]

ଡକ୍ସେପିନର ସାଧାରଣ ପାର୍ଶ୍ୱ ପ୍ରତିକ୍ରିୟାରେ ନିଦ୍ରାଳୁ ଭାବ, ଶୁଷ୍କ ପାଟି, ଅଇ ଓ ଝାପ୍‌ସା ଦୃଷ୍ଟି ହୋଇପାରେ ।^[୬] ପ୍ରତିକ୍ରିୟା ସାଂଘାତିକ ହେଲେ ୨୫ ବର୍ଷ ବୟସରୁ କମ୍ ଲୋକମାନେ ଆତ୍ମହତ୍ୟା ପ୍ରବଣ, ମାନିଆ ଓ ୟୁରିନାରି ରିଟେନସନ ହୋଇପାରେ ।^[୬] ଏହାର ମାତ୍ରା ଶୀଘ୍ର କମେଇ ଦେଲେ ଉଇଥଡ୍ରଆଲ ସିଣ୍ଡ୍ରୋମ (withdrawal syndrome) ହୋଇପାରେ ।^[୬] ଗର୍ଭାବସ୍ଥା ଓ ସ୍ତନ୍ୟପାନ ସମୟରେ ଏହା ଦିଆଯାଏ ନାହିଁ । ^[୧୦]^[୧୧] ଏହା ଏକ ପ୍ରକାର ଟ୍ରାଇସାକ୍ଲିକ ଆଣ୍ଟିଡିପ୍ରେସାଣ୍ଟ ବା ଟିସିଏ (tricyclic antidepressant/ TCA) ଔଷଧ ।^[୬] ଏହାର କାର୍ଯ୍ୟଧାର ଅସ୍ପଷ୍ଟ ଥିଲେ ମଧ୍ୟ ନର୍‌ଏପିନେଫ୍ରିନ ସ୍ତର ବୃଦ୍ଧି କରୁଥାଇପାରେ ।^[୬] ଏହାର ଆଣ୍ଟିହିସ୍ଟାମିନ (antihistamine), ଆଣ୍ଟିକଲିନର୍ଜିକ (anticholinergic) ଓ ଆଣ୍ଟସେରୋଟୋନର୍ଜିକ (antiserotonergic) ପ୍ରଭାବ ଅଛି । ^[୬]

ସନ ୧୯୬୯ରେ ଡାକ୍ତରୀ ବ୍ୟବ‌ହାର ନିମନ୍ତେ ଡକ୍ସେପିନ ଯୁକ୍ତରାଷ୍ଟ୍ର ଆମେରିକାରେ ସ୍ୱୀକୃତ ହୋଇଥିଲା ।^[୬] ଏହା ଜେନେରିକ ଔଷଧ ନାମରେ (generic medication) ବିକ୍ରୟ ହୁଏ ।^[୧୦] ସନ ୨୦୧୯ରେ ସଂଯୁକ୍ତ ରାଷ୍ଟ୍ରରେ (United Kingdom) ଏନଏଚଏସକୁ (NHS) ଏହାର ଏକ ମାସର ଡୋଜ ପିଛା ପ୍ରାୟ ୧୦୦ ପାଉଣ୍ଡ ଖର୍ଚ୍ଚ କରିବାକୁ ପଡ଼ୁଥିଲା ।^[୧୦] ଯୁକ୍ତରାଷ୍ଟ୍ର ଆମେରିକାରେ ଏହି ଔଷଧ ବାବଦ ଏକ ମାସରେ ପ୍ରାୟ ୨୩ ଆମେରିକୀୟ ଡଲାର ଖର୍ଚ୍ଚ ହୁଏ ।^[୧୨] ସନ ୨୦୧୬ରେ ଏହାର ୨ ନିୟୁତରୁ ଅଧିକ ପ୍ରେସକ୍ରିପସନ ହୋଇ ସର୍ବାଧିକ ପ୍ରେସକ୍ରିସନ ତାଲିକାର ୨୩୯ତମ ସ୍ଥାନରେ ଥଲା ।^[୧୩]

ଆଧାର

↑ "Doxepin Hydrochloride". Martindale: The Complete Drug Reference. London, UK: Pharmaceutical Press. 30 January 2013. Retrieved 3 December 2013.
↑ Adis Editorial (1971). "Doxepin". Drugs. 1 (3): 194–227. doi:10.2165/00003495-197101030-00002.
↑ J. Elks (14 November 2014). The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and Bibliographies. Springer. pp. 469–. ISBN 978-1-4757-2085-3.
↑ ^୪.୦ ^୪.୧ ^୪.୨ ^୪.୩ Weber J, Siddiqui MA, Wagstaff AJ, McCormack PL (2010). "Low-dose doxepin: in the treatment of insomnia". CNS Drugs. 24 (8): 713–20. doi:10.2165/11200810-000000000-00000. PMID 20658801.
↑ ^୫.୦ ^୫.୧ ^୫.୨ ^୫.୩ Thomas L. Lemke; David A. Williams (24 January 2012). Foye's Principles of Medicinal Chemistry. Lippincott Williams & Wilkins. pp. 604–. ISBN 978-1-60913-345-0.
↑ ^୬.୦ ^୬.୧ ^୬.୨ ^୬.୩ ^୬.୪ ^୬.୫ ^୬.୬ ^୬.୭ ^୬.୮ "Doxepin Hydrochloride". Drugs.com. American Society of Health-System Pharmacists. Retrieved 20 March 2019.
↑ "Silenor (doxepin) label" (PDF). FDA. 17 March 2010. Retrieved 25 October 2017. For label updates see FDA index page for NDA 022036
↑ Yeung, WF; Chung, KF; Yung, KP; Ng, TH (February 2015). "Doxepin for insomnia: a systematic review of randomized placebo-controlled trials". Sleep Medicine Reviews. 19: 75–83. doi:10.1016/j.smrv.2014.06.001. PMID 25047681.
↑ "Doxepin hydrochloride cream" (PDF). FDA. 20 December 2002. Retrieved 25 October 2017. For label updates see FDA index page for NDA 020126
↑ ^୧୦.୦ ^୧୦.୧ ^୧୦.୨ British national formulary : BNF 76 (76 ed.). Pharmaceutical Press. 2018. p. 372. ISBN 9780857113382.
↑ "Doxepin Use During Pregnancy". Drugs.com (in ଇଂରାଜୀ). Retrieved 21 March 2019.
↑ "NADAC as of 2019-02-27". Centers for Medicare and Medicaid Services (in ଇଂରାଜୀ). Archived from the original on 2019-03-06. Retrieved 3 March 2019.
↑ "The Top 300 of 2019". Clincalc.com. Retrieved 22 December 2018.

ବାହ୍ୟ ଲିଙ୍କ

Drug information from the NIH

[MD-1] "Doxepin Hydrochloride". Martindale: The Complete Drug Reference. London, UK: Pharmaceutical Press. 30 January 2013. Retrieved 3 December 2013.

[Drugs1971-2] Adis Editorial (1971). "Doxepin". Drugs. 1 (3): 194–227. doi:10.2165/00003495-197101030-00002.

[Elks2014-3] J. Elks (14 November 2014). The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and Bibliographies. Springer. pp. 469–. ISBN 978-1-4757-2085-3.

[pmid20658801-4] ୪.୦ ^୪.୧ ^୪.୨ ^୪.୩ Weber J, Siddiqui MA, Wagstaff AJ, McCormack PL (2010). "Low-dose doxepin: in the treatment of insomnia". CNS Drugs. 24 (8): 713–20. doi:10.2165/11200810-000000000-00000. PMID 20658801.

[LemkeWilliams2012-5] ୫.୦ ^୫.୧ ^୫.୨ ^୫.୩ Thomas L. Lemke; David A. Williams (24 January 2012). Foye's Principles of Medicinal Chemistry. Lippincott Williams & Wilkins. pp. 604–. ISBN 978-1-60913-345-0.

[AHFS2019-6] ୬.୦ ^୬.୧ ^୬.୨ ^୬.୩ ^୬.୪ ^୬.୫ ^୬.୬ ^୬.୭ ^୬.୮ "Doxepin Hydrochloride". Drugs.com. American Society of Health-System Pharmacists. Retrieved 20 March 2019.

[FDAInsomnia-7] "Silenor (doxepin) label" (PDF). FDA. 17 March 2010. Retrieved 25 October 2017. For label updates see FDA index page for NDA 022036

[Yeung2016-8] Yeung, WF; Chung, KF; Yung, KP; Ng, TH (February 2015). "Doxepin for insomnia: a systematic review of randomized placebo-controlled trials". Sleep Medicine Reviews. 19: 75–83. doi:10.1016/j.smrv.2014.06.001. PMID 25047681.

[Creamlabel-9] "Doxepin hydrochloride cream" (PDF). FDA. 20 December 2002. Retrieved 25 October 2017. For label updates see FDA index page for NDA 020126

[BNF76-10] ୧୦.୦ ^୧୦.୧ ^୧୦.୨ British national formulary : BNF 76 (76 ed.). Pharmaceutical Press. 2018. p. 372. ISBN 9780857113382.

[11] "Doxepin Use During Pregnancy". Drugs.com (in ଇଂରାଜୀ). Retrieved 21 March 2019.

[NADAC2019-12] "NADAC as of 2019-02-27". Centers for Medicare and Medicaid Services (in ଇଂରାଜୀ). Archived from the original on 2019-03-06. Retrieved 3 March 2019.

[13] "The Top 300 of 2019". Clincalc.com. Retrieved 22 December 2018.

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Clinical data


Trade names	Sinequan, Quitaxon, Aponal, others^[୨]
Synonyms	NSC-108160^[୩]
AHFS/Drugs.com	monograph
MedlinePlus	a682390
data	US FDA: Doxepin
Pregnancy category	AU: C US: B (No risk in non-human studies)
Routes of administration	By mouth, topical, intravenous, intramuscular injection^[୧]
Drug class	Tricyclic antidepressant (TCA)
ATC code	D04AX01 (WHO) N06AA12
Legal status
Legal status	AU: S4 (Prescription only) CA: ℞-only UK: POM (Prescription only) US: ℞-only
Pharmacokinetic data
Bioavailability	13–45% (mean 29%)^[୫]^[୪]
Protein binding	76%
Metabolism	Hepatic (CYP2D6, CYP2C19)^[୪]^[୫]
Metabolites	Nordoxepin, glucuronide conjugates^[୪]
Elimination half-life	Doxepin: 8–24 hours (mean 17 hours) Nordoxepin: 31 hours
Excretion	Urine: ~50%^[୪]^[୫] Feces: minor^[୫]
Identifiers
IUPAC name (E/Z)-3-(dibenzo[b,e]oxepin-11(6H)-ylidene)-N,N-dimethylpropan-1-amine
CAS Number	1668-19-5^Y
PubChem CID	3158
IUPHAR/BPS	1225
DrugBank	DB01142^Y
ChemSpider	3046^Y
UNII	5ASJ6HUZ7D
KEGG	D07875^Y
ChEBI	CHEBI:4710^Y
ChEMBL	CHEMBL1628227^Y
Chemical and physical data
Formula	C₁₉H₂₁NO
Molar mass	279.376 g/mol
3D model (JSmol)	Interactive image
SMILES CN(C)CC/C=C1C2=C(C=CC=C2)OCC3=C/1C=CC=C3
InChI InChI=1S/C19H21NO/c1-20(2)13-7-11-17-16-9-4-3-8-15(16)14-21-19-12-6-5-10-18(17)19/h3-6,8-12H,7,13-14H2,1-2H3^Y Key:ODQWQRRAPPTVAG-UHFFFAOYSA-N^Y
^NY (what is this?) (verify)