Details of the Drug

General Information of Drug (ID: DMGFV3Z)

Drug Name

Nizatidine

Synonyms

Acinon; Antizid; Axid; Calmaxid; Cronizat; Distaxid; Galitidin; Gastrax; Naxidine; Niatidine; Nizatidina; Nizatidinum; Nizax; Nizaxid; Panaxid; Tazac; Ulcosol; Ulxid; Zanizal; Zinga; Axid Ar; Nizatidina [Spanish]; Nizatidinum [Latin]; Splendil ER; LY 139037; Acinon (TN); Axid (TN); LY-139037; Tazac (TN); ZE-101; ZL-101; Nizatidine (JAN/USP/INN); Nizatidine [USAN:BAN:INN:JAN]; N-(2-(((2-((Dimethylamino)methyl)-4-thiazolyl)methyl)thio)ethyl)-N'-methyl-2-nitro-1,1-ethenediamine; N-(4-(6-Methylamino-7-nitro-2-thia-5-aza-6-hepten-1-yl)-2-thiazolylmethyl)-N,N-dimethylamin; (E)-1-N'-[2-[[2-(dimethylaminomethyl)-1,3-thiazol-4-yl]methylsulfanyl]ethyl]-1-N-methyl-2-nitroethene-1,1-diamine; (E)-N-[2-[[2-(dimethylaminomethyl)-1,3-thiazol-4-yl]methylsulfanyl]ethyl]-N'-methyl-2-nitroethene-1,1-diamine; (E)-N-{2-[({2-[(dimethylamino)methyl]-1,3-thiazol-4-yl}methyl)thio]ethyl}-N'-methyl-2-nitroethene-1,1-diamine

Indication

Disease Entry	ICD 11	Status	REF
Acid-reflux disorder	DA22	Approved	[1]
Gastric ulcer	DA60	Approved	[2]
Peptic esophagitis	N.A.	Approved	[2]
Peptic ulcer	DA61	Approved	[2]
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Therapeutic Class

Antiulcer Agents

Drug Type

Small molecular drug

Structure

3D MOL

2D MOL

#Ro5 Violations (Lipinski): 0

Molecular Weight (mw)

331.5

Logarithm of the Partition Coefficient (xlogp)

1.6

Rotatable Bond Count (rotbonds)

Hydrogen Bond Donor Count (hbonddonor)

Hydrogen Bond Acceptor Count (hbondacc)

ADMET Property

BDDCS Class: Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 3: high solubility and low permeability [3]
Bioavailability: The bioavailability of drug is 70% []
Clearance: The drug present in the plasma can be removed from the body at the rate of 9.8 mL/min/kg [4]
Elimination: 61% of drug is excreted from urine in the unchanged form [3]
Half-life: The concentration or amount of drug in body reduced by one-half in 1 - 2 hours [4]
Metabolism: The drug is metabolized via the hepatic []
MRTD: The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 15.08471 micromolar/kg/day [5]
Unbound Fraction: The unbound fraction of drug in plasma is 0.65% [4]
Vd: The volume of distribution (Vd) of drug is 0.8-1.5 L/kg []
Water Solubility: The ability of drug to dissolve in water is measured as 21.65 mg/mL [3]

Chemical Identifiers

Formula: C12H21N5O2S2
IUPAC Name: (E)-1-N'-[2-[[2-[(dimethylamino)methyl]-1,3-thiazol-4-yl]methylsulfanyl]ethyl]-1-N-methyl-2-nitroethene-1,1-diamine
Canonical SMILES: CN/C(=C\\[N+](=O)[O-])/NCCSCC1=CSC(=N1)CN(C)C
InChI: InChI=1S/C12H21N5O2S2/c1-13-11(6-17(18)19)14-4-5-20-8-10-9-21-12(15-10)7-16(2)3/h6,9,13-14H,4-5,7-8H2,1-3H3/b11-6+
InChIKey: SGXXNSQHWDMGGP-IZZDOVSWSA-N

Cross-matching ID

PubChem CID: 3033637
ChEBI ID: CHEBI:7601
CAS Number: 76963-41-2
DrugBank ID: DB00585
TTD ID: D0Q9DK
VARIDT ID: DR00263
INTEDE ID: DR2187
ACDINA ID: D00477

Combinatorial Drugs (CBD)

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Repurposed Drugs (RPD)

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Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Histamine H2 receptor (H2R)	TTQHJ1K	HRH2_HUMAN	Antagonist	[6]

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Drug Transporter (DTP)

DTP Name	DTP ID	UniProt ID	MOA	REF
Organic cation transporter 1 (SLC22A1)	DTT79CX	S22A1_HUMAN	Substrate	[7]
P-glycoprotein 1 (ABCB1)	DTUGYRD	MDR1_HUMAN	Substrate	[8]

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Drug Off-Target (DOT)

DOT Name	DOT ID	UniProt ID	Interaction	REF
Calcitonin (CALCA)	OTZ11LHB	CALC_HUMAN	Gene/Protein Processing	[9]
Protachykinin-1 (TAC1)	OTM842YW	TKN1_HUMAN	Gene/Protein Processing	[9]

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Molecular Interaction Atlas (MIA)

MIA Detail

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Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Disease Different from Nizatidine (Comorbidity)

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Comorbidity	REF
Sodium bicarbonate	DMMU6BJ	Minor	Decreased absorption of Nizatidine due to altered gastric pH caused by Sodium bicarbonate.	Acidosis [5C73]	[10]
Cefuroxime	DMSIMD8	Moderate	Decreased absorption of Nizatidine due to altered gastric pH caused by Cefuroxime.	Acute bronchitis [CA42]	[11]
Glibenclamide	DM8JXPZ	Moderate	Decreased absorption of Nizatidine due to altered gastric pH caused by Glibenclamide.	Acute diabete complication [5A2Y]	[12]
Tolazamide	DMIHRNA	Moderate	Decreased absorption of Nizatidine due to altered gastric pH caused by Tolazamide.	Acute diabete complication [5A2Y]	[12]
Glipizide	DMZA5PQ	Moderate	Decreased absorption of Nizatidine due to altered gastric pH caused by Glipizide.	Acute diabete complication [5A2Y]	[12]
Posaconazole	DMUL5EW	Moderate	Decreased absorption of Nizatidine due to altered gastric pH caused by Posaconazole.	Aspergillosis [1F20]	[13]
Aminophylline	DML2NIB	Moderate	Decreased metabolism of Nizatidine caused by Aminophylline mediated inhibition of CYP450 enzyme.	Asthma [CA23]	[14]
Cefpodoxime	DMJUNY5	Moderate	Decreased absorption of Nizatidine due to altered gastric pH caused by Cefpodoxime.	Bacterial infection [1A00-1C4Z]	[11]
Bacampicillin	DMP54C7	Moderate	Decreased absorption of Nizatidine due to altered gastric pH caused by Bacampicillin.	Bacterial infection [1A00-1C4Z]	[11]
Cefditoren	DMSUVM1	Moderate	Decreased absorption of Nizatidine due to altered gastric pH caused by Cefditoren.	Bacterial infection [1A00-1C4Z]	[15]
Vismodegib	DM5IXKQ	Minor	Decreased absorption of Nizatidine due to altered gastric pH caused by Vismodegib.	Basal cell carcinoma [2C32]	[16]
Pexidartinib	DMS2J0Z	Moderate	Decreased absorption of Nizatidine due to altered gastric pH caused by Pexidartinib.	Bone/articular cartilage neoplasm [2F7B]	[17]
Lapatinib	DM3BH1Y	Moderate	Decreased absorption of Nizatidine due to altered gastric pH caused by Lapatinib.	Breast cancer [2C60-2C6Y]	[18]
HKI-272	DM6QOVN	Major	Decreased absorption of Nizatidine due to altered gastric pH caused by HKI-272.	Breast cancer [2C60-2C6Y]	[16]
Bosutinib	DMTI8YE	Moderate	Decreased absorption of Nizatidine due to altered gastric pH caused by Bosutinib.	Breast cancer [2C60-2C6Y]	[18]
Oxtriphylline	DMLHSE3	Moderate	Decreased metabolism of Nizatidine caused by Oxtriphylline mediated inhibition of CYP450 enzyme.	Cough [MD12]	[14]
Itraconazole	DMCR1MV	Moderate	Decreased absorption of Nizatidine due to altered gastric pH caused by Itraconazole.	Fungal infection [1F29-1F2F]	[19]
Ketoconazole	DMPZI3Q	Moderate	Decreased absorption of Nizatidine due to altered gastric pH caused by Ketoconazole.	Fungal infection [1F29-1F2F]	[20]
GS-5885	DMSL3DX	Moderate	Decreased absorption of Nizatidine due to altered gastric pH caused by GS-5885.	Hepatitis virus infection [1E50-1E51]	[21]
Delavirdine	DM3NF5G	Moderate	Decreased absorption of Nizatidine due to altered gastric pH caused by Delavirdine.	Human immunodeficiency virus disease [1C60-1C62]	[22]
Fosamprenavir	DM4W9B3	Moderate	Decreased absorption of Nizatidine due to altered gastric pH caused by Fosamprenavir.	Human immunodeficiency virus disease [1C60-1C62]	[23]
Rilpivirine	DMJ0QOW	Major	Decreased absorption of Nizatidine due to altered gastric pH caused by Rilpivirine.	Human immunodeficiency virus disease [1C60-1C62]	[24]
Atazanavir	DMSYRBX	Major	Decreased absorption of Nizatidine due to altered gastric pH caused by Atazanavir.	Human immunodeficiency virus disease [1C60-1C62]	[18]
Raltegravir	DMYURI6	Minor	Decreased absorption of Nizatidine due to altered gastric pH caused by Raltegravir.	Human immunodeficiency virus disease [1C60-1C62]	[25]
Ceritinib	DMB920Z	Moderate	Decreased absorption of Nizatidine due to altered gastric pH caused by Ceritinib.	Lung cancer [2C25]	[26]
Dacomitinib	DMOH8VY	Moderate	Decreased absorption of Nizatidine due to altered gastric pH caused by Dacomitinib.	Lung cancer [2C25]	[18]
Selpercatinib	DMZR15V	Major	Decreased absorption of Nizatidine due to altered gastric pH caused by Selpercatinib.	Lung cancer [2C25]	[18]
Acalabrutinib	DM7GCVW	Moderate	Decreased absorption of Nizatidine due to altered gastric pH caused by Acalabrutinib.	Mature B-cell lymphoma [2A85]	[27]
Ponatinib	DMYGJQO	Minor	Decreased absorption of Nizatidine due to altered gastric pH caused by Ponatinib.	Mature B-cell lymphoma [2A85]	[16]
Dabrafenib	DMX6OE3	Moderate	Decreased absorption of Nizatidine due to altered gastric pH caused by Dabrafenib.	Melanoma [2C30]	[16]
Thalidomide	DM70BU5	Moderate	Increased risk of ventricular arrhythmias by the combination of Nizatidine and Thalidomide.	Multiple myeloma [2A83]	[16]
Siponimod	DM2R86O	Major	Increased risk of bradycardia by the combination of Nizatidine and Siponimod.	Multiple sclerosis [8A40]	[16]
Fingolimod	DM5JVAN	Moderate	Increased risk of atrioventricular block by the combination of Nizatidine and Fingolimod.	Multiple sclerosis [8A40]	[28]
Ozanimod	DMT6AM2	Moderate	Increased risk of atrioventricular block by the combination of Nizatidine and Ozanimod.	Multiple sclerosis [8A40]	[29]
Nilotinib	DM7HXWT	Moderate	Decreased absorption of Nizatidine due to altered gastric pH caused by Nilotinib.	Myeloproliferative neoplasm [2A20]	[16]
Dasatinib	DMJV2EK	Major	Decreased absorption of Nizatidine due to altered gastric pH caused by Dasatinib.	Myeloproliferative neoplasm [2A20]	[30]
Prasugrel	DM7MT6E	Minor	Decreased absorption of Nizatidine due to altered gastric pH caused by Prasugrel.	Myocardial infarction [BA41-BA43]	[31]
Axitinib	DMGVH6N	Minor	Decreased absorption of Nizatidine due to altered gastric pH caused by Axitinib.	Renal cell carcinoma [2C90]	[32]
Tolbutamide	DM02AWV	Moderate	Decreased absorption of Nizatidine due to altered gastric pH caused by Tolbutamide.	Type 2 diabetes mellitus [5A11]	[12]
Chlorpropamide	DMPHZQE	Moderate	Decreased absorption of Nizatidine due to altered gastric pH caused by Chlorpropamide.	Type 2 diabetes mellitus [5A11]	[12]
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⏷ Show the Full List of 40 DDI Information of This Drug

Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG

DIG Name	DIG ID	PubChem CID	Functional Classification
Allura red AC dye	E00338	33258	Colorant
D&C red no. 28	E00491	6097185	Colorant
FD&C blue no. 1	E00263	19700	Colorant
FD&C blue no. 2	E00446	2723854	Colorant
Isopropyl alcohol	E00070	3776	Antimicrobial preservative; Solvent
Quinoline yellow WS	E00309	24671	Colorant
Sodium lauryl sulfate	E00464	3423265	Emulsifying agent; Modified-release agent; Penetration agent; Solubilizing agent; Surfactant; lubricant
Sunset yellow FCF	E00255	17730	Colorant
Ammonia	E00007	222	Alkalizing agent
Beta-D-lactose	E00099	6134	Diluent; Dry powder inhaler carrier; Lyophilization aid
Butyl alcohol	E00011	263	Flavoring agent; Solvent
Carmellose sodium	E00625	Not Available	Disintegrant
Eisenoxyd	E00585	56841934	Colorant
Ethanol	E00023	702	Antimicrobial preservative; Penetration agent; Solvent
FD&C red no. 3	E00629	Not Available	Colorant
Ferric hydroxide oxide yellow	E00539	23320441	Colorant
Ferrosoferric oxide	E00231	14789	Colorant
Magnesium stearate	E00208	11177	lubricant
Potassium hydroxide	E00233	14797	Alkalizing agent
Povidone	E00667	Not Available	Binding agent; Coating agent; Disintegrant; Film/membrane-forming agent; Solubilizing agent; Suspending agent
Propylene glycol	E00040	1030	Antimicrobial preservative; Humectant; Plasticizing agent; Solvent
Silicon dioxide	E00670	Not Available	Anticaking agent; Opacifying agent; Viscosity-controlling agent
Talc	E00520	16211421	Anticaking agent; Diluent; Glidant; lubricant
Titanium dioxide	E00322	26042	Coating agent; Colorant; Opacifying agent
Vinylpyrrolidone	E00668	Not Available	Binding agent; Coating agent; Disintegrant; Film/membrane-forming agent; Solubilizing agent; Suspending agent
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⏷ Show the Full List of 25 Pharmaceutical Excipients of This Drug

Pharmaceutical Formulation

Formulation Name	Drug Dosage	Dosage Form	Route
Nizatidine 150 mg capsule	150 mg	Oral Capsule	Oral
Nizatidine 300 mg capsule	300 mg	Oral Capsule	Oral
Nizatidine 75 mg tablet	75 mg	Oral Tablet	Oral

Jump to Detail Pharmaceutical Formulation Page of This Drug

References

1	URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7248).
2	Nizatidine FDA Label
3	BDDCS applied to over 900 drugs
4	Trend Analysis of a Database of Intravenous Pharmacokinetic Parameters in Humans for 1352 Drug Compounds
5	Estimating the safe starting dose in phase I clinical trials and no observed effect level based on QSAR modeling of the human maximum recommended daily dose
6	Does the use of nizatidine, as a pro-kinetic agent, improve gastric emptying in patients post-oesophagectomy J Gastrointest Surg. 2009 Mar;13(3):432-7.
7	Identification of novel substrates and structure-activity relationship of cellular uptake mediated by human organic cation transporters 1 and 2. J Med Chem. 2013 Sep 26;56(18):7232-42.
8	DrugBank 5.0: a major update to the DrugBank database for 2018. Nucleic Acids Res. 2018 Jan 4;46(D1):D1074-D1082. (ID: DB00585)
9	Effects of histamine H(2)-receptor antagonists on human plasma levels of calcitonin gene-related peptide, substance P and vasoactive intestinal peptide. J Pharm Pharmacol. 2002 Nov;54(11):1559-63. doi: 10.1211/002235702117.
10	Albin H, Vincon G, Begaud B, Bistue C, Perez P "Effect of aluminum phosphate on the bioavailability of ranitidine." Eur J Clin Pharmacol 32 (1987): 97-9. [PMID: 3582475]
11	Honig PK, Gillespie BK "Clinical significance of pharmacokinetic drug interactions with over-the-counter (OTC) drugs." Clin Pharmacokinet 35 (1998): 167-71. [PMID: 9784931]
12	Dey NG, Castleden CM, Ward J, et al "The effect of cimetidine on tolbutamide kinetics." Br J Clin Pharmacol 16 (1983): 438-40. [PMID: 6626438]
13	Alffenaar JW, van Assen S, van der Werf TS, Kosterink JG, Uges DR "Omeprazole significantly reduces posaconazole serum trough level." Clin Infect Dis 48 (2009): 839. [PMID: 19220151]
14	Anderson JR, Poklis A, Slavin RG "A fatal case of theophylline intoxication." Arch Intern Med 143 (1983): 559-60. [PMID: 6830388]
15	Product Information. Spectracef (cefditoren). TAP Pharmaceuticals Inc, Deerfield, IL.
16	Cerner Multum, Inc. "Australian Product Information.".
17	Product Information. Turalio (pexidartinib). Daiichi Sankyo, Inc., Parsippany, NJ.
18	Cerner Multum, Inc. "UK Summary of Product Characteristics.".
19	Blum RA, D'Andrea DT, Florentino BM, et al "Increased gastric pH and the bioavailability of fluconazole and ketoconazole." Ann Intern Med 114 (1991): 755-7. [PMID: 2012358]
20	Adachi M, Hinatsu Y, et.al "Improved dissolution and absorption of ketoconazole in the presence of organic acids as pH-modifiers." Eur J Pharm Sci 76 (2015): 225-30. [PMID: 25988287]
21	Product Information. Harvoni (ledipasvir-sofosbuvir). Gilead Sciences, Foster City, CA.
22	Product Information. Rescriptor (delavirdine). Pharmacia and Upjohn, Kalamazoo, MI.
23	Product Information. Lexiva (fosamprenavir). GlaxoSmithKline, Research Triangle Park, NC.
24	Product Information. Edurant (rilpivirine). Tibotec Pharmaceuticals, Titusville, NJ.
25	Product Information. Isentress (raltegravir). Merck & Company Inc, West Point, PA.
26	Product Information. Zykadia (ceritinib). Novartis Pharmaceuticals, East Hanover, NJ.
27	Product Information. Calquence (acalabrutinib). Astra-Zeneca Pharmaceuticals, Wilmington, DE.
28	Product Information. Gilenya (fingolimod). Novartis Pharmaceuticals, East Hanover, NJ.
29	Product Information. Zeposia (ozanimod). Celgene Corporation, Summit, NJ.
30	Product Information. Sprycel (dasatinib). Bristol-Myers Squibb, Princeton, NJ.
31	Product Information. Effient (prasugrel). Lilly, Eli and Company, Indianapolis, IN.
32	Product Information. Inlyta (axitinib). Pfizer U.S. Pharmaceuticals Group, New York, NY.