ଗାବାପେଣ୍ଟିନ୍

ଗାବାପେଣ୍ଟିନ୍
Clinical data
Trade names	Neurontin, others
AHFS/Drugs.com	monograph
MedlinePlus	a694007
data	US DailyMed: 52049;
Pregnancy; category	AU: B1 ; US: C (Risk not ruled out) ; ;
Routes of; administration	By mouth
ATC code	N03AX12 (WHO) ;
Legal status
Legal status	AU: S4 (Prescription only) ; CA: ℞-only ; UK: POM (Prescription only) ; US: ℞-only ;
Pharmacokinetic data
Bioavailability	27-60% (inversely proportional to dose; a high fat meal also increases bioavailability)
Protein binding	Less than 3%
Metabolism	Not significantly metabolised
Elimination half-life	5 to 7 hours
Excretion	Renal
Identifiers
	IUPAC name 1-(aminomethyl)cyclohexaneacetic acid;
CAS Number	60142-96-3 ;
PubChem CID	3446;
IUPHAR/BPS	5483;
DrugBank	DB00996 ;
ChemSpider	3328 ;
UNII	6CW7F3G59X;
KEGG	D00332 ;
ChEBI	CHEBI:42797 ;
ChEMBL	CHEMBL940 ;
PDB ligand	GBN (PDBe, RCSB PDB);
ECHA InfoCard	100.056.415
Chemical and physical data
Formula	C9H17NO2
Molar mass	171.237 g/mol
3D model (JSmol)	Interactive image;
	SMILES O=C(O)CC1(CN)CCCCC1;
	InChI InChI=1S/C9H17NO2/c10-7-9(6-8(11)12)4-2-1-3-5-9/h1-7,10H2,(H,11,12) ; Key:UGJMXCAKCUNAIE-UHFFFAOYSA-N ;
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ଗାବାପେଣ୍ଟିନ୍, ବ୍ୟବସାୟୀକ ନାମ ନିଉରୋଣ୍ଟିନ, ଏକ ଔଷଧ ଯାହା ଅପସ୍ମାର ବା ଏପିଲେପ୍‌ସି, ସ୍ନାୟୁ ଜନିତ ଯନ୍ତ୍ରଣା, ଗରମ ଅନୁଭବ (ହଟ ଫ୍ଲାସେସ) ଓ ରେସ୍ଟଲେସ ଲେଗ ସିଣ୍ରୋମ୍ ରୋଗମାନଙ୍କର ଚିକିତ୍ସା ନିମନ୍ତେ ଦିଆଯାଏ ।^[୪]^[୫] ଆଂଶିକ ବାତ ମାରୁଥିଲେ ଏହା ବ୍ୟବ‌ହାର କରାଯାଏ ।^[୪] ଡାଏବେଟିକ ନିଉରୋପାଥି, ପୋଷ୍ଟ ହର୍ପେଟିକ ନିଉରାଲଜିଆ ଓ ସେଣ୍ଟ୍ରାଲ ନିଉରୋପାଥି ଭଳି ସ୍ନାୟୁ ରୋଗରେ ଯନ୍ତ୍ରଣା ହେଉଥିଲେ ଏହି ଔଷଧ ଦିଆଯାଏ ।^[୬] ନିଉରୋପାଥିକ ଯନ୍ତ୍ରଣାରେ ୧୪% ଲୋକଙ୍କର ଉପକାର ହୁଏ । ^[୭]

ଗାବାପେଣ୍ଟିନ୍‌ର ସାଧାରଣ ପାର୍ଶ୍ୱ ପ୍ରତିକ୍ରିୟା ହେଉଛି ନିଦୁଆ ଭାବ ଓ ମୁଣ୍ଡ ବୁଲେଇବା (dizziness) । ସାଂଘାତିକ ପାର୍ଶ୍ୱ ପ୍ରତିକ୍ରିୟା ହେଲେ ଆତ୍ମହତ୍ୟା ସଙ୍କଟ, ଆକ୍ରମଣତ୍ମକ ବ୍ୟବ‌ହାର ଓ ଇଓସିନୋଫିଲିଆ ତ‌ଥା ସିସ୍ଟମିକ ଲକ୍ଷଣ ସ‌ହିତ ଔଷଧ ପ୍ରତିକ୍ରିୟା ହୁଏ ।^[୪] ଗର୍ଭାବସ୍ଥା ଓ ସ୍ତନ୍ୟପାନ ସମୟରେ ଏହାର ବ୍ୟବ‌ହାରରେ କ୍ଷତି ହୁଏ କି ନା ତାହା ସ୍ପଷ୍ଟ ନୁହେଁ ।^[୮] ବୃକ୍‌କ ସମସ୍ୟା ଥିଲେ ସ୍ୱଳ୍ପ ମାତ୍ରା ଗାବାପେଣ୍ଟିନ୍‌ ଦେବା ଉଚିତ୍ । ଇନହିବିଟରି ଗାମା ଆମିନୋ ବ୍ୟୁଟିରିକ ଏସିଡ୍‌କୁ (GABA) ଗାବାପେଣ୍ଟିନ୍‌ ପ୍ରଭାବିତ କରେ କିନ୍ତୁ ଏହାର କାର୍ଯ୍ୟ ପ୍ରଣାଳୀ ଅଜ୍ଞାତ ଅଛି ।^[୪]

ଗାବାପେଣ୍ଟିନ୍ ସନ ୧୯୯୩ରେ ପ୍ରଥମେ ମାନ୍ୟତା ଦିଆଗଲା ।^[୯] ଏହାର ହୋଲସେଲ ମୂଲ୍ୟ ଦୈନିକ ପ୍ରାୟ ୧.୩୫ ଆମେରିକୀୟ ଡଲାର ।^[୧୦] ଯୁକ୍ତରାଷ୍ଟ୍ର ଆମେରିକାରେ ଏହା ସନ ୨୦୦୪ରୁ ଜେନେରିକ ଔଷଧ ନାମରେ ଉପଲବ୍‌ଧ ହେଉଛି ।^[୪] ସନ ୨୦୧୫ରେ ଏହାର ମୂଲ୍ୟ ଯୁକ୍ତରାଷ୍ଟ୍ର ଆମେରିକାରେ ୧୦୦ରୁ ୨୦୦ ଆମେରିକୀୟ ଡଲାର ।^[୧୧] ସନ ୧୯୯୦ରେ ଫାଇଜର କମ୍ପାନୀର ଏକ ଶାଖା ପାର୍କ ଡେଭିସ କମ୍ପାନୀ ଏହି ଔଷଧକୁ ଅଣମାନ୍ୟତା ବ୍ୟବ‌ହାର କରିବା ନିମନ୍ତେ ଚିକିତ୍ସକମାନଙ୍କୁ ପ୍ରୋତ୍ସାହିତ କରୁଥିଲା ।^[୧୨]

ଆଧାର

↑ Drugs.com international listings for Gabapentin Page accessed Feb. 9, 2016
↑ ^୨.୦ ^୨.୧ ^୨.୨ ^୨.୩ ^୨.୪ "Neurontin, Gralise (gabapentin) dosing, indications, interactions, adverse effects, and more". Medscape Reference. WebMD. Retrieved 6 April 2014.
↑ ^୩.୦ ^୩.୧ ^୩.୨ ^୩.୩ ^୩.୪ Goa, KL; Sorkin, EM (September 1993). "Gabapentin. A review of its pharmacological properties and clinical potential in epilepsy". Drugs. 46 (3): 409–27. doi:10.2165/00003495-199346030-00007. PMID 7693432.
↑ ^୪.୦ ^୪.୧ ^୪.୨ ^୪.୩ ^୪.୪ "Gabapentin". The American Society of Health-System Pharmacists. Retrieved Oct 23, 2015.
↑ Wijemanne, S; Jankovic, J (June 2015). "Restless legs syndrome: clinical presentation diagnosis and treatment". Sleep medicine. 16 (6): 678–90. doi:10.1016/j.sleep.2015.03.002. PMID 25979181.
↑ Attal N, Cruccu G, Baron R, et al. (September 2010). "EFNS guidelines on the pharmacological treatment of neuropathic pain: 2010 revision". Eur. J. Neurol. 17 (9): 1113–e88. doi:10.1111/j.1468-1331.2010.02999.x. PMID 20402746.
↑ Moore, RA; Wiffen, PJ; Derry, S; Toelle, T; Rice, AS (27 April 2014). "Gabapentin for chronic neuropathic pain and fibromyalgia in adults". The Cochrane database of systematic reviews. 4: CD007938. PMID 24771480.
↑ "Gabapentin Pregnancy and Breastfeeding Warnings". Retrieved 13 March 2016.
↑ Pitkänen, Asla; Schwartzkroin, Philip A.; Moshé, Solomon L. (2005). Models of Seizures and Epilepsy. Burlington: Elsevier. p. 539. ISBN 9780080457024.
↑ "Gabapentin". International Drug Price Indicator Guide. Retrieved 13 March 2016.^{[permanent dead link]}
↑ Hamilton, Richart (2015). Tarascon Pocket Pharmacopoeia 2015 Deluxe Lab-Coat Edition. Jones & Bartlett Learning. p. 327. ISBN 9781284057560.
↑ Henney JE (August 2006). "Safeguarding patient welfare: who's in charge?" (PDF). Annals of Internal Medicine. 145 (4): 305–7. doi:10.7326/0003-4819-145-4-200608150-00013. PMID 16908923.

[drugs.com-1] Drugs.com international listings for Gabapentin Page accessed Feb. 9, 2016

[MSR-2] ୨.୦ ^୨.୧ ^୨.୨ ^୨.୩ ^୨.୪ "Neurontin, Gralise (gabapentin) dosing, indications, interactions, adverse effects, and more". Medscape Reference. WebMD. Retrieved 6 April 2014.

[drugs93-3] ୩.୦ ^୩.୧ ^୩.୨ ^୩.୩ ^୩.୪ Goa, KL; Sorkin, EM (September 1993). "Gabapentin. A review of its pharmacological properties and clinical potential in epilepsy". Drugs. 46 (3): 409–27. doi:10.2165/00003495-199346030-00007. PMID 7693432.

[AHFS2015-4] ୪.୦ ^୪.୧ ^୪.୨ ^୪.୩ ^୪.୪ "Gabapentin". The American Society of Health-System Pharmacists. Retrieved Oct 23, 2015.

[5] Wijemanne, S; Jankovic, J (June 2015). "Restless legs syndrome: clinical presentation diagnosis and treatment". Sleep medicine. 16 (6): 678–90. doi:10.1016/j.sleep.2015.03.002. PMID 25979181.

[Attal2010-6] Attal N, Cruccu G, Baron R, et al. (September 2010). "EFNS guidelines on the pharmacological treatment of neuropathic pain: 2010 revision". Eur. J. Neurol. 17 (9): 1113–e88. doi:10.1111/j.1468-1331.2010.02999.x. PMID 20402746.

[Moore2014-7] Moore, RA; Wiffen, PJ; Derry, S; Toelle, T; Rice, AS (27 April 2014). "Gabapentin for chronic neuropathic pain and fibromyalgia in adults". The Cochrane database of systematic reviews. 4: CD007938. PMID 24771480.

[8] "Gabapentin Pregnancy and Breastfeeding Warnings". Retrieved 13 March 2016.

[9] Pitkänen, Asla; Schwartzkroin, Philip A.; Moshé, Solomon L. (2005). Models of Seizures and Epilepsy. Burlington: Elsevier. p. 539. ISBN 9780080457024.

[10] "Gabapentin". International Drug Price Indicator Guide. Retrieved 13 March 2016.^{[permanent dead link]}

[Ric2015-11] Hamilton, Richart (2015). Tarascon Pocket Pharmacopoeia 2015 Deluxe Lab-Coat Edition. Jones & Bartlett Learning. p. 327. ISBN 9781284057560.

[pmid16908923-12] Henney JE (August 2006). "Safeguarding patient welfare: who's in charge?" (PDF). Annals of Internal Medicine. 145 (4): 305–7. doi:10.7326/0003-4819-145-4-200608150-00013. PMID 16908923.

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Clinical data


Trade names	Neurontin, others^[୧]
AHFS/Drugs.com	monograph
MedlinePlus	a694007
data	US DailyMed: 52049
Pregnancy category	AU: B1 US: C (Risk not ruled out)
Routes of administration	By mouth
ATC code	N03AX12 (WHO)
Legal status
Legal status	AU: S4 (Prescription only) CA: ℞-only UK: POM (Prescription only) US: ℞-only
Pharmacokinetic data
Bioavailability	27-60% (inversely proportional to dose; a high fat meal also increases bioavailability)^[୨]^[୩]
Protein binding	Less than 3%^[୨]^[୩]
Metabolism	Not significantly metabolised^[୨]^[୩]
Elimination half-life	5 to 7 hours^[୨]^[୩]
Excretion	Renal^[୨]^[୩]
Identifiers
IUPAC name 1-(aminomethyl)cyclohexaneacetic acid
CAS Number	60142-96-3^Y
PubChem CID	3446
IUPHAR/BPS	5483
DrugBank	DB00996^Y
ChemSpider	3328^Y
UNII	6CW7F3G59X
KEGG	D00332^Y
ChEBI	CHEBI:42797^Y
ChEMBL	CHEMBL940^Y
PDB ligand	GBN (PDBe, RCSB PDB)
ECHA InfoCard	100.056.415
Chemical and physical data
Formula	C₉H₁₇NO₂
Molar mass	171.237 g/mol
3D model (JSmol)	Interactive image
SMILES O=C(O)CC1(CN)CCCCC1
InChI InChI=1S/C9H17NO2/c10-7-9(6-8(11)12)4-2-1-3-5-9/h1-7,10H2,(H,11,12)^Y Key:UGJMXCAKCUNAIE-UHFFFAOYSA-N^Y
(verify)