Details of the Drug

General Information of Drug (ID: DM6TS1N)

Drug Name

Phendimetrazine

Synonyms

Adphen; Antapentan; Dyrexan; Fendimetrazina; Hyrex; Mephenmetrazine; Phendimetrazinum; Sedafamen; Wehless; Adipost (TN); Adphen (base); Appecon (TN); Bontril PDM (TN); Fendimetrazina [INN-Spanish]; Melfiat (TN); Obezine (TN); Phendiet (TN); Phendimetrazine (INN); Phendimetrazine [INN:BAN]; Phendimetrazinum [INN-Latin]; Plegine (TN); Statobex (TN); X-Trozine; Anorex-SR (TN); Prelu-2 (TN); Phendimetrazine, (2S-trans)-isomer; D-2-Phenyl-3,4-dimethylmorpholine; Morpholine, 3,4-dimethyl-2-phenyl; (+)-3,4-Dimethyl-2-phenylmorpholine; (+)-Phendimetrazine; (2R-trans)-3,4-Dimethyl-2-phenylmorpholine; (2S,3S)-3,4-Dimethyl-2-phenylmorpholine; 3,4-Dimethyl-2-phenylmorpholine; 3,4-Dimethyl-2-phenyltetrahydro-1,4-oxazine; 3-Phenyl-2-methylmorpholine

Indication

Disease Entry	ICD 11	Status	REF
Obesity	5B81	Approved	[1]

Therapeutic Class

Anorexigenic Agents

Drug Type

Small molecular drug

Structure

3D MOL

2D MOL

#Ro5 Violations (Lipinski): 0

Molecular Weight (mw)

191.27

Topological Polar Surface Area (xlogp)

1.9

Rotatable Bond Count (rotbonds)

1

Hydrogen Bond Donor Count (hbonddonor)

0

Hydrogen Bond Acceptor Count (hbondacc)

2

ADMET Property

Half-life: The concentration or amount of drug in body reduced by one-half in 19 - 24 hours [2]

Chemical Identifiers

Formula: C12H17NO
IUPAC Name: (2S,3S)-3,4-dimethyl-2-phenylmorpholine
Canonical SMILES: C[C@H]1[C@@H](OCCN1C)C2=CC=CC=C2
InChI: InChI=1S/C12H17NO/c1-10-12(14-9-8-13(10)2)11-6-4-3-5-7-11/h3-7,10,12H,8-9H2,1-2H3/t10-,12+/m0/s1
InChIKey: MFOCDFTXLCYLKU-CMPLNLGQSA-N

Cross-matching ID

PubChem CID: 30487
ChEBI ID: CHEBI:8059
CAS Number: 634-03-7
DrugBank ID: DB01579
TTD ID: D0T6SU
ACDINA ID: D00523

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Adrenergic receptor alpha-1B (ADRA1B)	TTBRKXS	ADA1B_HUMAN	Antagonist	[3]

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Molecular Interaction Atlas (MIA)

MIA Detail

Jump to Detail Molecular Interaction Atlas of This Drug

Drug-Drug Interaction (DDI) Information of This Drug

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

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Comorbidity	REF
Methylene blue	DMJAPE7	Major	Additive hypertensive effects by the combination of Phendimetrazine and Methylene blue.	Acquired methaemoglobinaemia [3A93]	[14]
Droxidopa	DM5YF4M	Moderate	Additive hypertensive effects by the combination of Phendimetrazine and Droxidopa.	Autonomic nervous system disorder [8D87]	[15]
Esketamine	DMVU687	Major	Additive hypertensive effects by the combination of Phendimetrazine and Esketamine.	Depression [6A70-6A7Z]	[16]
Polyethylene glycol	DM4I1JP	Moderate	Increased risk of lowers seizure threshold by the combination of Phendimetrazine and Polyethylene glycol.	Irritable bowel syndrome [DD91]	[17]
Ozanimod	DMT6AM2	Moderate	Increased risk of hyperpyrexia by the combination of Phendimetrazine and Ozanimod.	Multiple sclerosis [8A40]	[14]
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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
FD&C blue no. 1	E00263	19700	Colorant
Hydrazine yellow	E00409	164825	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
Stearic acid	E00079	5281	Emulsifying agent; Solubilizing agent; Viscosity-controlling agent; lubricant
Sunset yellow FCF	E00255	17730	Colorant
Beta-D-lactose	E00099	6134	Diluent; Dry powder inhaler carrier; Lyophilization aid
Brushite	E00392	104805	Diluent
Calcium hydrogenphosphate	E00294	24441	Diluent
Carmellose sodium	E00625	Not Available	Disintegrant
Lactose monohydrate	E00393	104938	Binding agent; Diluent; Dry powder inhaler carrier; Lyophilization aid
Magnesium stearate	E00208	11177	lubricant
Povidone	E00667	Not Available	Binding agent; Coating agent; Disintegrant; Film/membrane-forming agent; Solubilizing agent; Suspending agent
Saccharose	E00091	5988	Binding agent; Coating agent; Cryoprotectant; Diluent; Flavoring agent; Suspending agent; Viscosity-controlling agent
Silicon dioxide	E00670	Not Available	Anticaking agent; Opacifying agent; Viscosity-controlling agent
Talc	E00520	16211421	Anticaking agent; Diluent; Glidant; lubricant
Water	E00035	962	Solvent
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⏷ Show the Full List of 19 Pharmaceutical Excipients of This Drug

Pharmaceutical Formulation

Formulation Name	Drug Dosage	Dosage Form	Route
Phendimetrazine 35 mg tablet	35 mg	Oral Tablet	Oral
Phendimetrazine 105 mg capsule	105 mg	24 HR Extended Release Oral Capsule	Oral

Jump to Detail Pharmaceutical Formulation Page of This Drug

References

1	Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
2	Trend Analysis of a Database of Intravenous Pharmacokinetic Parameters in Humans for 1352 Drug Compounds
3	Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34.
4	Mirtazapine treatment after conditioning with methamphetamine alters subsequent expression of place preference. Drug Alcohol Depend. 2009 Jan 1;99(1-3):231-9.
5	Interaction of neuroleptics and antidepressants with rat brain alpha 2-receptors: a possible relationship between alpha 2-receptor antagonism and antidepressant action. Biol Psychiatry. 1984 Sep;19(9):1283-91.
6	Activation of alpha1-adrenoceptors inhibits growth hormone secretion in humans. Exp Clin Endocrinol Diabetes. 2009 Oct;117(9):460-2.
7	A structure-activity relationship study of benzylic modifications of 4-[1-(1-naphthyl)ethyl]-1H-imidazoles on alpha 1- and alpha 2-adrenergic recep... J Med Chem. 1994 Jul 22;37(15):2328-33.
8	3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents. J Med Chem. 1996 Jan 5;39(1):143-8.
9	An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment o... J Med Chem. 2006 Jun 1;49(11):3116-35.
10	A new arylpiperazine antipsychotic with high D2/D3/5-HT1A/alpha 1A-adrenergic affinity and a low potential for extrapyramidal effects. J Med Chem. 1994 Apr 15;37(8):1060-2.
11	Drug repositioning: identifying and developing new uses for existing drugs. Nat Rev Drug Discov. 2004 Aug;3(8):673-83.
12	Alpha- and beta-adrenoceptors: from the gene to the clinic. 2. Structure-activity relationships and therapeutic applications. J Med Chem. 1995 Sep 15;38(19):3681-716.
13	Alpha- and beta-adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification. J Med Chem. 1995 Sep 1;38(18):3415-44.
14	Ban TA "Drug interactions with psychoactive drugs." Dis Nerv Syst 36 (1975): 164-6. [PMID: 1116424]
15	Product Information. Northera (droxidopa). Chelsea Therapeutics Inc, Charlotte, NC.
16	Cerner Multum, Inc. "Australian Product Information.".
17	Product Information. Suprep Bowel Prep Kit (magnesium/potassium/sodium sulfates). Braintree Laboratories, Braintree, MA.