Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C12H17NO.C4H4O4 |
| Molecular Weight | 307.3416 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 1 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
OC(=O)\C=C\C(O)=O.C[C@H]1[C@@H](OCCN1C)C2=CC=CC=C2
InChI
InChIKey=HQQSFOASVJDTOM-WRTZALMKSA-N
InChI=1S/C12H17NO.C4H4O4/c1-10-12(14-9-8-13(10)2)11-6-4-3-5-7-11;5-3(6)1-2-4(7)8/h3-7,10,12H,8-9H2,1-2H3;1-2H,(H,5,6)(H,7,8)/b;2-1+/t10-,12+;/m0./s1
DescriptionCurator's Comment: description was created based on several sources, including:
https://www.drugs.com/pro/phendimetrazine.html | http://www.wikidoc.org/index.php/Phendimetrazine
Curator's Comment: description was created based on several sources, including:
https://www.drugs.com/pro/phendimetrazine.html | http://www.wikidoc.org/index.php/Phendimetrazine
Phendimetrazine is an appetite suppressant that is FDA approved for the treatment of exogenous obesity. It is clinically available anorectic agent, which display minimal interactions with monoamine transporters in vitro. On the other hand, their medications is known to be psychomotor stimulants when administered in vivo as indicated by their shared properties with illicit drugs like cocaine. The following adverse reactions are described, or described in greater detail, in other sections: Primary pulmonary hypertension; Valvular heart disease; Effect on the ability to engage in potentially hazardous tasks; Withdrawal effects following prolonged high dosage administration. Use of phendimetrazine tartrate is contraindicated during or within 14 days following the administration of monoamine oxidase inhibitors because of the risk of hypertensive crisis.
CNS Activity
Originator
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL238 |
2.56 µM [EC50] | ||
Target ID: CHEMBL222 |
8.3 µM [IC50] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | PHENDIMETRAZINE TARTRATE Approved UsePhendimetrazine tartrate is indicated in the management of exogenous obesity as a short term adjunct (a few weeks) in a regimen of weight reduction based on caloric restriction in patients with an initial body mass index (BMI) of 30 kg/m2 or higher who have not responded to appropriate weight reducing regimen (diet and/or exercise) alone. Below is a chart of Body Mass Index (BMI) based on various heights and weights. BMI is calculated by taking the patient’s weight, in kilograms (kg), divided by the patient’s height, in meters (m), squared. Metric conversions are as follows: pounds ÷ 2.2 = kg; inches x 0.0254 = meters. BODY MASS INDEX (BMI), kg/m2 Height (feet, inches) Weight(pounds) 5’0” 5’3” 5’6” 5’9” 6’0” 6’3” 140 27 25 23 21 19 18 150 29 27 24 22 20 19 160 31 28 26 24 22 20 170 33 30 28 25 23 21 180 35 32 29 27 25 23 190 37 34 31 28 26 24 200 39 36 32 30 27 25 210 41 37 34 31 29 26 220 43 39 36 33 30 28 230 45 41 37 34 31 29 240 47 43 39 36 33 30 250 49 44 40 37 34 31 Phendimetrazine tartrate is indicated for use as monotherapy only. Launch Date1979 |
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
1227 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23211394 |
3.2 mg/kg single, intramuscular dose: 3.2 mg/kg route of administration: Intramuscular experiment type: SINGLE co-administered: |
PHENDIMETRAZINE plasma | Macaca mulatta population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
137 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23211394 |
0.32 mg/kg single, intramuscular dose: 0.32 mg/kg route of administration: Intramuscular experiment type: SINGLE co-administered: |
PHENDIMETRAZINE plasma | Macaca mulatta population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
268 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23211394 |
1 mg/kg single, intramuscular dose: 1 mg/kg route of administration: Intramuscular experiment type: SINGLE co-administered: |
PHENDIMETRAZINE plasma | Macaca mulatta population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
70 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/6688092 |
35 mg single, oral dose: 35 mg route of administration: Oral experiment type: SINGLE co-administered: |
PHENDIMETRAZINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
132945 ng × min/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23211394 |
3.2 mg/kg single, intramuscular dose: 3.2 mg/kg route of administration: Intramuscular experiment type: SINGLE co-administered: |
PHENDIMETRAZINE plasma | Macaca mulatta population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
15.195 ng × min/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23211394 |
0.32 mg/kg single, intramuscular dose: 0.32 mg/kg route of administration: Intramuscular experiment type: SINGLE co-administered: |
PHENDIMETRAZINE plasma | Macaca mulatta population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
35.877 ng × min/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23211394 |
1 mg/kg single, intramuscular dose: 1 mg/kg route of administration: Intramuscular experiment type: SINGLE co-administered: |
PHENDIMETRAZINE plasma | Macaca mulatta population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
112 min EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23211394 |
3.2 mg/kg single, intramuscular dose: 3.2 mg/kg route of administration: Intramuscular experiment type: SINGLE co-administered: |
PHENDIMETRAZINE plasma | Macaca mulatta population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
114 min EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23211394 |
0.32 mg/kg single, intramuscular dose: 0.32 mg/kg route of administration: Intramuscular experiment type: SINGLE co-administered: |
PHENDIMETRAZINE plasma | Macaca mulatta population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
180 min EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23211394 |
1 mg/kg single, intramuscular dose: 1 mg/kg route of administration: Intramuscular experiment type: SINGLE co-administered: |
PHENDIMETRAZINE plasma | Macaca mulatta population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
2 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/6688092 |
35 mg single, oral dose: 35 mg route of administration: Oral experiment type: SINGLE co-administered: |
PHENDIMETRAZINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
3.7 h |
PHENDIMETRAZINE unknown | Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
Doses
| Dose | Population | Adverse events |
|---|---|---|
105 mg 1 times / day steady, oral Recommended Dose: 105 mg, 1 times / day Route: oral Route: steady Dose: 105 mg, 1 times / day Co-administed with:: anorectic agents Sources: |
unhealthy Health Status: unhealthy Condition: exogenous obesity Sources: |
Disc. AE: Pulmonary hypertension... AEs leading to discontinuation/dose reduction: Pulmonary hypertension Sources: |
105 mg 1 times / day steady, oral Recommended Dose: 105 mg, 1 times / day Route: oral Route: steady Dose: 105 mg, 1 times / day Co-administed with:: dexfenfluramine Sources: |
unhealthy Health Status: unhealthy Condition: exogenous obesity Sources: |
Disc. AE: Valvular heart disease NOS... AEs leading to discontinuation/dose reduction: Valvular heart disease NOS Sources: |
105 mg 1 times / day steady, oral Recommended Dose: 105 mg, 1 times / day Route: oral Route: steady Dose: 105 mg, 1 times / day Co-administed with:: fenfluramine Sources: |
unhealthy Health Status: unhealthy Condition: exogenous obesity Sources: |
Disc. AE: Valvular heart disease NOS... AEs leading to discontinuation/dose reduction: Valvular heart disease NOS Sources: |
AEs
| AE | Significance | Dose | Population |
|---|---|---|---|
| Pulmonary hypertension | Disc. AE | 105 mg 1 times / day steady, oral Recommended Dose: 105 mg, 1 times / day Route: oral Route: steady Dose: 105 mg, 1 times / day Co-administed with:: anorectic agents Sources: |
unhealthy Health Status: unhealthy Condition: exogenous obesity Sources: |
| Valvular heart disease NOS | Disc. AE | 105 mg 1 times / day steady, oral Recommended Dose: 105 mg, 1 times / day Route: oral Route: steady Dose: 105 mg, 1 times / day Co-administed with:: dexfenfluramine Sources: |
unhealthy Health Status: unhealthy Condition: exogenous obesity Sources: |
| Valvular heart disease NOS | Disc. AE | 105 mg 1 times / day steady, oral Recommended Dose: 105 mg, 1 times / day Route: oral Route: steady Dose: 105 mg, 1 times / day Co-administed with:: fenfluramine Sources: |
unhealthy Health Status: unhealthy Condition: exogenous obesity Sources: |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Safety and tolerability of intranasal cocaine during phendimetrazine maintenance. | 2016 Jun |
|
| Attenuation of cocaine self-administration by chronic oral phendimetrazine in rhesus monkeys. | 2016 Jun 2 |
|
| Abuse Potential of Oral Phendimetrazine in Cocaine-dependent Individuals: Implications for Agonist-like Replacement Therapy. | 2016 May-Jun |
Sample Use Guides
One extended-release capsule (105 mg phendimetrazine tartrate) in the morning (30 to 60 minutes before morning meal).
Route of Administration:
Oral
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76962624
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80OKD9F9QG
Created by
admin on Sat Dec 16 01:54:11 GMT 2023 , Edited by admin on Sat Dec 16 01:54:11 GMT 2023
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ACTIVE MOIETY
PARENT (SALT/SOLVATE)
SUBSTANCE RECORD
