Details
Stereochemistry | ACHIRAL |
Molecular Formula | C10H15N.ClH |
Molecular Weight | 185.6941 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CC(C)(Cc1ccccc1)N.Cl
InChI
InChIKey=NCAIGTHBQTXTLR-UHFFFAOYSA-N
InChI=1S/C10H15N.ClH/c1-10(2,11)8-9-6-4-3-5-7-9;/h3-7H,8,11H2,1-2H3;1H
Molecular Formula | ClH |
Molecular Weight | 36.4609 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
Molecular Formula | C10H15N |
Molecular Weight | 149.2332 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
DescriptionSources: http://www.drugbank.ca/drugs/DB00191Curator's Comment:: Description was created based on several sources, including https://www.drugs.com/dosage/phentermine.html
Sources: http://www.drugbank.ca/drugs/DB00191
Curator's Comment:: Description was created based on several sources, including https://www.drugs.com/dosage/phentermine.html
Phentermine is an amphetamine that stimulates neurons to release or maintain high levels of a particular group of neurotransmitters known as catecholamines; these include dopamine and norepinephrine. High levels of these catecholamines tend to suppress hunger signals and appetite. The drug seems to inhibit reuptake of noradrenaline, dopamine, and seratonin through inhibition or reversal of the reuptake transporters. It may also inhibit MAO enzymes leaving more neurotransmitter available at the synapse. Phentermine (through catecholamine elevation) may also indirectly affect leptin levels in the brain. It is theorized that phentermine can raise levels of leptin which signal satiety. It is also theorized that increased levels of the catecholamines are partially responsible for halting another chemical messenger known as neuropeptide Y. This peptide initiates eating, decreases energy expenditure, and increases fat storage. Phentermine is indicated in the management of exogenous obesity as a short term (a few weeks) adjunct in a regimen of weight reduction based on caloric restriction. Phentermine hydrochloride is a sympathomimetic amine with pharmacologic activity similar to the prototype drugs of this class used in obesity, the amphetamines. Actions include central nervous system stimulation and elevation of blood pressure. Tachyphylaxis and tolerance have been demonstrated with all drugs of this class in which these phenomena have been looked for.
CNS Activity
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL238 Sources: http://www.drugbank.ca/drugs/DB00191 |
0.31 µM [EC50] | ||
Target ID: CHEMBL1951 Sources: https://www.ncbi.nlm.nih.gov/pubmed/11911838 |
498.0 µM [Ki] | ||
Target ID: CHEMBL2039 Sources: https://www.ncbi.nlm.nih.gov/pubmed/11911838 |
375.0 µM [Ki] | ||
Target ID: CHEMBL222 Sources: http://www.drugbank.ca/drugs/DB00191 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | ADIPEX-P Approved UseADIPEX-P® is a sympathomimetic amine anorectic indicated as a short-term adjunct (a few weeks) in a regimen of weight reduction based on exercise, behavioral modification and caloric restriction in the management of exogenous obesity for patients with an initial body mass index ≥ 30 kg/m2, or ≥ 27 kg/m2 in the presence of other risk factors Launch Date-3.47241611E11 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
44.78 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25668796 |
7.5 mg single, oral dose: 7.5 mg route of administration: Oral experiment type: SINGLE co-administered: TOPIRAMATE |
PHENTERMINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
49.1 ng/mL |
15 mg single, oral dose: 15 mg route of administration: Oral experiment type: SINGLE co-administered: TOPIRAMATE |
PHENTERMINE plasma | Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
2057.33 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25668796 |
7.5 mg single, oral dose: 7.5 mg route of administration: Oral experiment type: SINGLE co-administered: TOPIRAMATE |
PHENTERMINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
2000 ng × h/mL |
15 mg single, oral dose: 15 mg route of administration: Oral experiment type: SINGLE co-administered: TOPIRAMATE |
PHENTERMINE plasma | Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
20.63 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25668796 |
7.5 mg single, oral dose: 7.5 mg route of administration: Oral experiment type: SINGLE co-administered: TOPIRAMATE |
PHENTERMINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
20 h |
15 mg single, oral dose: 15 mg route of administration: Oral experiment type: SINGLE co-administered: TOPIRAMATE |
PHENTERMINE plasma | Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
Funbound
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
82.5% |
15 mg single, oral dose: 15 mg route of administration: Oral experiment type: SINGLE co-administered: TOPIRAMATE |
PHENTERMINE plasma | Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
Doses
Dose | Population | Adverse events |
---|---|---|
37.5 mg 1 times / day single, oral Recommended Dose: 37.5 mg, 1 times / day Route: oral Route: single Dose: 37.5 mg, 1 times / day Sources: Page: nda/2012/202088Orig2s000MedR.pdf - p.12 |
healthy, 18 - 45 years old n = 17 Health Status: healthy Age Group: 18 - 45 years old Sex: M+F Population Size: 17 Sources: Page: nda/2012/202088Orig2s000MedR.pdf - p.12 |
Other AEs: Abdominal pain, Dizziness... Other AEs: Abdominal pain (6%) Sources: Page: nda/2012/202088Orig2s000MedR.pdf - p.12Dizziness (6%) Early satiety (6%) Intermittent headache (6%) Nausea (6%) Swollen lips (6%) Upper respiratory infection (6%) |
37.5 mg 1 times / day single, oral Recommended Dose: 37.5 mg, 1 times / day Route: oral Route: single Dose: 37.5 mg, 1 times / day Sources: Page: nda/2012/202088Orig2s000MedR.pdf - p.12 |
healthy, 18 - 45 years old n = 17 Health Status: healthy Age Group: 18 - 45 years old Sex: M+F Population Size: 17 Sources: Page: nda/2012/202088Orig2s000MedR.pdf - p.12 |
Other AEs: Anorexia, Back pain... Other AEs: Anorexia (6%) Sources: Page: nda/2012/202088Orig2s000MedR.pdf - p.12Back pain (6%) Chapped lips (6%) Dry skin (6%) Dyspepsia (6%) Early satiety (6%) Irregular pulse (6%) Nausea (6%) |
390 mg 1 times / day single, oral Studied dose Dose: 390 mg, 1 times / day Route: oral Route: single Dose: 390 mg, 1 times / day Sources: |
healthy, mean age 30 years n = 2 Health Status: healthy Age Group: mean age 30 years Sex: M+F Population Size: 2 Sources: |
Other AEs: Tachycardia, Hypertension... Other AEs: Tachycardia Sources: Hypertension Visual disorders NEC Nausea Insomnia Anxiety |
15 mg 1 times / day multiple, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: multiple Dose: 15 mg, 1 times / day Co-administed with:: topiramate(92 mg; 1/day) Sources: Page: nda/2012/022580Orig1s000MedR.pdf - p.105 |
unhealthy, mean age 51.9 years n = 295 Health Status: unhealthy Condition: obesity Age Group: mean age 51.9 years Sex: M+F Population Size: 295 Sources: Page: nda/2012/022580Orig1s000MedR.pdf - p.105 |
Disc. AE: Amnesia, Judgement impaired... Other AEs: Disorder sleep, Depression... AEs leading to discontinuation/dose reduction: Amnesia (0.3%) Other AEs:Judgement impaired (0.3%) Memory impairment (0.3%) Paraesthesia (0.3%) Depression (1%) Anxiety (0.3%) Vision blurred (0.3%) Eye pain (0.3%) Abdominal pain (0.3%) Tuberculosis skin test positive (0.3%) Nephrolithiasis (0.3%) Disorder sleep (12.9%) Sources: Page: nda/2012/022580Orig1s000MedR.pdf - p.105Depression (8.1%) Anxiety (9.5%) Cardiac arrhythmia (4.1%) Ischemic heart disease (1%) Disturbance in attention (3.1%) Memory impairment (2%) Cognitive disorders (1.4%) Language disorder (0.3%) Ocular disorders NEC (4.1%) Dyskinesias and movement disorders NEC (1.4%) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Abdominal pain | 6% | 37.5 mg 1 times / day single, oral Recommended Dose: 37.5 mg, 1 times / day Route: oral Route: single Dose: 37.5 mg, 1 times / day Sources: Page: nda/2012/202088Orig2s000MedR.pdf - p.12 |
healthy, 18 - 45 years old n = 17 Health Status: healthy Age Group: 18 - 45 years old Sex: M+F Population Size: 17 Sources: Page: nda/2012/202088Orig2s000MedR.pdf - p.12 |
Dizziness | 6% | 37.5 mg 1 times / day single, oral Recommended Dose: 37.5 mg, 1 times / day Route: oral Route: single Dose: 37.5 mg, 1 times / day Sources: Page: nda/2012/202088Orig2s000MedR.pdf - p.12 |
healthy, 18 - 45 years old n = 17 Health Status: healthy Age Group: 18 - 45 years old Sex: M+F Population Size: 17 Sources: Page: nda/2012/202088Orig2s000MedR.pdf - p.12 |
Early satiety | 6% | 37.5 mg 1 times / day single, oral Recommended Dose: 37.5 mg, 1 times / day Route: oral Route: single Dose: 37.5 mg, 1 times / day Sources: Page: nda/2012/202088Orig2s000MedR.pdf - p.12 |
healthy, 18 - 45 years old n = 17 Health Status: healthy Age Group: 18 - 45 years old Sex: M+F Population Size: 17 Sources: Page: nda/2012/202088Orig2s000MedR.pdf - p.12 |
Intermittent headache | 6% | 37.5 mg 1 times / day single, oral Recommended Dose: 37.5 mg, 1 times / day Route: oral Route: single Dose: 37.5 mg, 1 times / day Sources: Page: nda/2012/202088Orig2s000MedR.pdf - p.12 |
healthy, 18 - 45 years old n = 17 Health Status: healthy Age Group: 18 - 45 years old Sex: M+F Population Size: 17 Sources: Page: nda/2012/202088Orig2s000MedR.pdf - p.12 |
Nausea | 6% | 37.5 mg 1 times / day single, oral Recommended Dose: 37.5 mg, 1 times / day Route: oral Route: single Dose: 37.5 mg, 1 times / day Sources: Page: nda/2012/202088Orig2s000MedR.pdf - p.12 |
healthy, 18 - 45 years old n = 17 Health Status: healthy Age Group: 18 - 45 years old Sex: M+F Population Size: 17 Sources: Page: nda/2012/202088Orig2s000MedR.pdf - p.12 |
Swollen lips | 6% | 37.5 mg 1 times / day single, oral Recommended Dose: 37.5 mg, 1 times / day Route: oral Route: single Dose: 37.5 mg, 1 times / day Sources: Page: nda/2012/202088Orig2s000MedR.pdf - p.12 |
healthy, 18 - 45 years old n = 17 Health Status: healthy Age Group: 18 - 45 years old Sex: M+F Population Size: 17 Sources: Page: nda/2012/202088Orig2s000MedR.pdf - p.12 |
Upper respiratory infection | 6% | 37.5 mg 1 times / day single, oral Recommended Dose: 37.5 mg, 1 times / day Route: oral Route: single Dose: 37.5 mg, 1 times / day Sources: Page: nda/2012/202088Orig2s000MedR.pdf - p.12 |
healthy, 18 - 45 years old n = 17 Health Status: healthy Age Group: 18 - 45 years old Sex: M+F Population Size: 17 Sources: Page: nda/2012/202088Orig2s000MedR.pdf - p.12 |
Anorexia | 6% | 37.5 mg 1 times / day single, oral Recommended Dose: 37.5 mg, 1 times / day Route: oral Route: single Dose: 37.5 mg, 1 times / day Sources: Page: nda/2012/202088Orig2s000MedR.pdf - p.12 |
healthy, 18 - 45 years old n = 17 Health Status: healthy Age Group: 18 - 45 years old Sex: M+F Population Size: 17 Sources: Page: nda/2012/202088Orig2s000MedR.pdf - p.12 |
Back pain | 6% | 37.5 mg 1 times / day single, oral Recommended Dose: 37.5 mg, 1 times / day Route: oral Route: single Dose: 37.5 mg, 1 times / day Sources: Page: nda/2012/202088Orig2s000MedR.pdf - p.12 |
healthy, 18 - 45 years old n = 17 Health Status: healthy Age Group: 18 - 45 years old Sex: M+F Population Size: 17 Sources: Page: nda/2012/202088Orig2s000MedR.pdf - p.12 |
Chapped lips | 6% | 37.5 mg 1 times / day single, oral Recommended Dose: 37.5 mg, 1 times / day Route: oral Route: single Dose: 37.5 mg, 1 times / day Sources: Page: nda/2012/202088Orig2s000MedR.pdf - p.12 |
healthy, 18 - 45 years old n = 17 Health Status: healthy Age Group: 18 - 45 years old Sex: M+F Population Size: 17 Sources: Page: nda/2012/202088Orig2s000MedR.pdf - p.12 |
Dry skin | 6% | 37.5 mg 1 times / day single, oral Recommended Dose: 37.5 mg, 1 times / day Route: oral Route: single Dose: 37.5 mg, 1 times / day Sources: Page: nda/2012/202088Orig2s000MedR.pdf - p.12 |
healthy, 18 - 45 years old n = 17 Health Status: healthy Age Group: 18 - 45 years old Sex: M+F Population Size: 17 Sources: Page: nda/2012/202088Orig2s000MedR.pdf - p.12 |
Dyspepsia | 6% | 37.5 mg 1 times / day single, oral Recommended Dose: 37.5 mg, 1 times / day Route: oral Route: single Dose: 37.5 mg, 1 times / day Sources: Page: nda/2012/202088Orig2s000MedR.pdf - p.12 |
healthy, 18 - 45 years old n = 17 Health Status: healthy Age Group: 18 - 45 years old Sex: M+F Population Size: 17 Sources: Page: nda/2012/202088Orig2s000MedR.pdf - p.12 |
Early satiety | 6% | 37.5 mg 1 times / day single, oral Recommended Dose: 37.5 mg, 1 times / day Route: oral Route: single Dose: 37.5 mg, 1 times / day Sources: Page: nda/2012/202088Orig2s000MedR.pdf - p.12 |
healthy, 18 - 45 years old n = 17 Health Status: healthy Age Group: 18 - 45 years old Sex: M+F Population Size: 17 Sources: Page: nda/2012/202088Orig2s000MedR.pdf - p.12 |
Irregular pulse | 6% | 37.5 mg 1 times / day single, oral Recommended Dose: 37.5 mg, 1 times / day Route: oral Route: single Dose: 37.5 mg, 1 times / day Sources: Page: nda/2012/202088Orig2s000MedR.pdf - p.12 |
healthy, 18 - 45 years old n = 17 Health Status: healthy Age Group: 18 - 45 years old Sex: M+F Population Size: 17 Sources: Page: nda/2012/202088Orig2s000MedR.pdf - p.12 |
Nausea | 6% | 37.5 mg 1 times / day single, oral Recommended Dose: 37.5 mg, 1 times / day Route: oral Route: single Dose: 37.5 mg, 1 times / day Sources: Page: nda/2012/202088Orig2s000MedR.pdf - p.12 |
healthy, 18 - 45 years old n = 17 Health Status: healthy Age Group: 18 - 45 years old Sex: M+F Population Size: 17 Sources: Page: nda/2012/202088Orig2s000MedR.pdf - p.12 |
Anxiety | 390 mg 1 times / day single, oral Studied dose Dose: 390 mg, 1 times / day Route: oral Route: single Dose: 390 mg, 1 times / day Sources: |
healthy, mean age 30 years n = 2 Health Status: healthy Age Group: mean age 30 years Sex: M+F Population Size: 2 Sources: |
|
Hypertension | 390 mg 1 times / day single, oral Studied dose Dose: 390 mg, 1 times / day Route: oral Route: single Dose: 390 mg, 1 times / day Sources: |
healthy, mean age 30 years n = 2 Health Status: healthy Age Group: mean age 30 years Sex: M+F Population Size: 2 Sources: |
|
Insomnia | 390 mg 1 times / day single, oral Studied dose Dose: 390 mg, 1 times / day Route: oral Route: single Dose: 390 mg, 1 times / day Sources: |
healthy, mean age 30 years n = 2 Health Status: healthy Age Group: mean age 30 years Sex: M+F Population Size: 2 Sources: |
|
Nausea | 390 mg 1 times / day single, oral Studied dose Dose: 390 mg, 1 times / day Route: oral Route: single Dose: 390 mg, 1 times / day Sources: |
healthy, mean age 30 years n = 2 Health Status: healthy Age Group: mean age 30 years Sex: M+F Population Size: 2 Sources: |
|
Tachycardia | 390 mg 1 times / day single, oral Studied dose Dose: 390 mg, 1 times / day Route: oral Route: single Dose: 390 mg, 1 times / day Sources: |
healthy, mean age 30 years n = 2 Health Status: healthy Age Group: mean age 30 years Sex: M+F Population Size: 2 Sources: |
|
Visual disorders NEC | 390 mg 1 times / day single, oral Studied dose Dose: 390 mg, 1 times / day Route: oral Route: single Dose: 390 mg, 1 times / day Sources: |
healthy, mean age 30 years n = 2 Health Status: healthy Age Group: mean age 30 years Sex: M+F Population Size: 2 Sources: |
|
Language disorder | 0.3% | 15 mg 1 times / day multiple, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: multiple Dose: 15 mg, 1 times / day Co-administed with:: topiramate(92 mg; 1/day) Sources: Page: nda/2012/022580Orig1s000MedR.pdf - p.105 |
unhealthy, mean age 51.9 years n = 295 Health Status: unhealthy Condition: obesity Age Group: mean age 51.9 years Sex: M+F Population Size: 295 Sources: Page: nda/2012/022580Orig1s000MedR.pdf - p.105 |
Abdominal pain | 0.3% Disc. AE |
15 mg 1 times / day multiple, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: multiple Dose: 15 mg, 1 times / day Co-administed with:: topiramate(92 mg; 1/day) Sources: Page: nda/2012/022580Orig1s000MedR.pdf - p.105 |
unhealthy, mean age 51.9 years n = 295 Health Status: unhealthy Condition: obesity Age Group: mean age 51.9 years Sex: M+F Population Size: 295 Sources: Page: nda/2012/022580Orig1s000MedR.pdf - p.105 |
Amnesia | 0.3% Disc. AE |
15 mg 1 times / day multiple, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: multiple Dose: 15 mg, 1 times / day Co-administed with:: topiramate(92 mg; 1/day) Sources: Page: nda/2012/022580Orig1s000MedR.pdf - p.105 |
unhealthy, mean age 51.9 years n = 295 Health Status: unhealthy Condition: obesity Age Group: mean age 51.9 years Sex: M+F Population Size: 295 Sources: Page: nda/2012/022580Orig1s000MedR.pdf - p.105 |
Anxiety | 0.3% Disc. AE |
15 mg 1 times / day multiple, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: multiple Dose: 15 mg, 1 times / day Co-administed with:: topiramate(92 mg; 1/day) Sources: Page: nda/2012/022580Orig1s000MedR.pdf - p.105 |
unhealthy, mean age 51.9 years n = 295 Health Status: unhealthy Condition: obesity Age Group: mean age 51.9 years Sex: M+F Population Size: 295 Sources: Page: nda/2012/022580Orig1s000MedR.pdf - p.105 |
Eye pain | 0.3% Disc. AE |
15 mg 1 times / day multiple, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: multiple Dose: 15 mg, 1 times / day Co-administed with:: topiramate(92 mg; 1/day) Sources: Page: nda/2012/022580Orig1s000MedR.pdf - p.105 |
unhealthy, mean age 51.9 years n = 295 Health Status: unhealthy Condition: obesity Age Group: mean age 51.9 years Sex: M+F Population Size: 295 Sources: Page: nda/2012/022580Orig1s000MedR.pdf - p.105 |
Judgement impaired | 0.3% Disc. AE |
15 mg 1 times / day multiple, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: multiple Dose: 15 mg, 1 times / day Co-administed with:: topiramate(92 mg; 1/day) Sources: Page: nda/2012/022580Orig1s000MedR.pdf - p.105 |
unhealthy, mean age 51.9 years n = 295 Health Status: unhealthy Condition: obesity Age Group: mean age 51.9 years Sex: M+F Population Size: 295 Sources: Page: nda/2012/022580Orig1s000MedR.pdf - p.105 |
Memory impairment | 0.3% Disc. AE |
15 mg 1 times / day multiple, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: multiple Dose: 15 mg, 1 times / day Co-administed with:: topiramate(92 mg; 1/day) Sources: Page: nda/2012/022580Orig1s000MedR.pdf - p.105 |
unhealthy, mean age 51.9 years n = 295 Health Status: unhealthy Condition: obesity Age Group: mean age 51.9 years Sex: M+F Population Size: 295 Sources: Page: nda/2012/022580Orig1s000MedR.pdf - p.105 |
Nephrolithiasis | 0.3% Disc. AE |
15 mg 1 times / day multiple, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: multiple Dose: 15 mg, 1 times / day Co-administed with:: topiramate(92 mg; 1/day) Sources: Page: nda/2012/022580Orig1s000MedR.pdf - p.105 |
unhealthy, mean age 51.9 years n = 295 Health Status: unhealthy Condition: obesity Age Group: mean age 51.9 years Sex: M+F Population Size: 295 Sources: Page: nda/2012/022580Orig1s000MedR.pdf - p.105 |
Paraesthesia | 0.3% Disc. AE |
15 mg 1 times / day multiple, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: multiple Dose: 15 mg, 1 times / day Co-administed with:: topiramate(92 mg; 1/day) Sources: Page: nda/2012/022580Orig1s000MedR.pdf - p.105 |
unhealthy, mean age 51.9 years n = 295 Health Status: unhealthy Condition: obesity Age Group: mean age 51.9 years Sex: M+F Population Size: 295 Sources: Page: nda/2012/022580Orig1s000MedR.pdf - p.105 |
Tuberculosis skin test positive | 0.3% Disc. AE |
15 mg 1 times / day multiple, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: multiple Dose: 15 mg, 1 times / day Co-administed with:: topiramate(92 mg; 1/day) Sources: Page: nda/2012/022580Orig1s000MedR.pdf - p.105 |
unhealthy, mean age 51.9 years n = 295 Health Status: unhealthy Condition: obesity Age Group: mean age 51.9 years Sex: M+F Population Size: 295 Sources: Page: nda/2012/022580Orig1s000MedR.pdf - p.105 |
Vision blurred | 0.3% Disc. AE |
15 mg 1 times / day multiple, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: multiple Dose: 15 mg, 1 times / day Co-administed with:: topiramate(92 mg; 1/day) Sources: Page: nda/2012/022580Orig1s000MedR.pdf - p.105 |
unhealthy, mean age 51.9 years n = 295 Health Status: unhealthy Condition: obesity Age Group: mean age 51.9 years Sex: M+F Population Size: 295 Sources: Page: nda/2012/022580Orig1s000MedR.pdf - p.105 |
Ischemic heart disease | 1% | 15 mg 1 times / day multiple, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: multiple Dose: 15 mg, 1 times / day Co-administed with:: topiramate(92 mg; 1/day) Sources: Page: nda/2012/022580Orig1s000MedR.pdf - p.105 |
unhealthy, mean age 51.9 years n = 295 Health Status: unhealthy Condition: obesity Age Group: mean age 51.9 years Sex: M+F Population Size: 295 Sources: Page: nda/2012/022580Orig1s000MedR.pdf - p.105 |
Depression | 1% Disc. AE |
15 mg 1 times / day multiple, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: multiple Dose: 15 mg, 1 times / day Co-administed with:: topiramate(92 mg; 1/day) Sources: Page: nda/2012/022580Orig1s000MedR.pdf - p.105 |
unhealthy, mean age 51.9 years n = 295 Health Status: unhealthy Condition: obesity Age Group: mean age 51.9 years Sex: M+F Population Size: 295 Sources: Page: nda/2012/022580Orig1s000MedR.pdf - p.105 |
Cognitive disorders | 1.4% | 15 mg 1 times / day multiple, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: multiple Dose: 15 mg, 1 times / day Co-administed with:: topiramate(92 mg; 1/day) Sources: Page: nda/2012/022580Orig1s000MedR.pdf - p.105 |
unhealthy, mean age 51.9 years n = 295 Health Status: unhealthy Condition: obesity Age Group: mean age 51.9 years Sex: M+F Population Size: 295 Sources: Page: nda/2012/022580Orig1s000MedR.pdf - p.105 |
Dyskinesias and movement disorders NEC | 1.4% | 15 mg 1 times / day multiple, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: multiple Dose: 15 mg, 1 times / day Co-administed with:: topiramate(92 mg; 1/day) Sources: Page: nda/2012/022580Orig1s000MedR.pdf - p.105 |
unhealthy, mean age 51.9 years n = 295 Health Status: unhealthy Condition: obesity Age Group: mean age 51.9 years Sex: M+F Population Size: 295 Sources: Page: nda/2012/022580Orig1s000MedR.pdf - p.105 |
Disorder sleep | 12.9% | 15 mg 1 times / day multiple, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: multiple Dose: 15 mg, 1 times / day Co-administed with:: topiramate(92 mg; 1/day) Sources: Page: nda/2012/022580Orig1s000MedR.pdf - p.105 |
unhealthy, mean age 51.9 years n = 295 Health Status: unhealthy Condition: obesity Age Group: mean age 51.9 years Sex: M+F Population Size: 295 Sources: Page: nda/2012/022580Orig1s000MedR.pdf - p.105 |
Memory impairment | 2% | 15 mg 1 times / day multiple, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: multiple Dose: 15 mg, 1 times / day Co-administed with:: topiramate(92 mg; 1/day) Sources: Page: nda/2012/022580Orig1s000MedR.pdf - p.105 |
unhealthy, mean age 51.9 years n = 295 Health Status: unhealthy Condition: obesity Age Group: mean age 51.9 years Sex: M+F Population Size: 295 Sources: Page: nda/2012/022580Orig1s000MedR.pdf - p.105 |
Disturbance in attention | 3.1% | 15 mg 1 times / day multiple, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: multiple Dose: 15 mg, 1 times / day Co-administed with:: topiramate(92 mg; 1/day) Sources: Page: nda/2012/022580Orig1s000MedR.pdf - p.105 |
unhealthy, mean age 51.9 years n = 295 Health Status: unhealthy Condition: obesity Age Group: mean age 51.9 years Sex: M+F Population Size: 295 Sources: Page: nda/2012/022580Orig1s000MedR.pdf - p.105 |
Cardiac arrhythmia | 4.1% | 15 mg 1 times / day multiple, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: multiple Dose: 15 mg, 1 times / day Co-administed with:: topiramate(92 mg; 1/day) Sources: Page: nda/2012/022580Orig1s000MedR.pdf - p.105 |
unhealthy, mean age 51.9 years n = 295 Health Status: unhealthy Condition: obesity Age Group: mean age 51.9 years Sex: M+F Population Size: 295 Sources: Page: nda/2012/022580Orig1s000MedR.pdf - p.105 |
Ocular disorders NEC | 4.1% | 15 mg 1 times / day multiple, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: multiple Dose: 15 mg, 1 times / day Co-administed with:: topiramate(92 mg; 1/day) Sources: Page: nda/2012/022580Orig1s000MedR.pdf - p.105 |
unhealthy, mean age 51.9 years n = 295 Health Status: unhealthy Condition: obesity Age Group: mean age 51.9 years Sex: M+F Population Size: 295 Sources: Page: nda/2012/022580Orig1s000MedR.pdf - p.105 |
Depression | 8.1% | 15 mg 1 times / day multiple, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: multiple Dose: 15 mg, 1 times / day Co-administed with:: topiramate(92 mg; 1/day) Sources: Page: nda/2012/022580Orig1s000MedR.pdf - p.105 |
unhealthy, mean age 51.9 years n = 295 Health Status: unhealthy Condition: obesity Age Group: mean age 51.9 years Sex: M+F Population Size: 295 Sources: Page: nda/2012/022580Orig1s000MedR.pdf - p.105 |
Anxiety | 9.5% | 15 mg 1 times / day multiple, oral Recommended Dose: 15 mg, 1 times / day Route: oral Route: multiple Dose: 15 mg, 1 times / day Co-administed with:: topiramate(92 mg; 1/day) Sources: Page: nda/2012/022580Orig1s000MedR.pdf - p.105 |
unhealthy, mean age 51.9 years n = 295 Health Status: unhealthy Condition: obesity Age Group: mean age 51.9 years Sex: M+F Population Size: 295 Sources: Page: nda/2012/022580Orig1s000MedR.pdf - p.105 |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/022580Orig1s000ClinPharmR.pdf#page=17 Page: 17.0 |
no | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/022580Orig1s000ClinPharmR.pdf#page=39 Page: 39.0 |
no | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/022580Orig1s000ClinPharmR.pdf#page=39 Page: 39.0 |
no | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/022580Orig1s000ClinPharmR.pdf#page=39 Page: 39.0 |
no | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/022580Orig1s000ClinPharmR.pdf#page=39 Page: 39.0 |
no | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/022580Orig1s000ClinPharmR.pdf#page=39 Page: 39.0 |
no |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/022580Orig1s000ClinPharmR.pdf#page=39 Page: 39,38 |
major | weak (co-administration study) Comment: In the presence of topiramate, phentermine Cmax and AUC0-inf increased 13 and 42%, respectively Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/022580Orig1s000ClinPharmR.pdf#page=39 Page: 39,38 |
PubMed
Title | Date | PubMed |
---|---|---|
Detailed examination of fenfluramine-phentermine users with valve abnormalities identified in Fargo, North Dakota. | 1999 Aug 1 |
|
Serial echocardiographic and clinical evaluation of valvular regurgitation before, during, and after treatment with fenfluramine or dexfenfluramine and mazindol or phentermine. | 1999 Jul |
|
Dose-effect of fenfluramine use on the severity of valvular heart disease among fen-phen patients with valvulopathy. | 1999 Sep |
|
[Obesity: principles of drug therapy]. | 2000 Aug |
|
Complex vascular lesions at autopsy in a patient with phentermine-fenfluramin. | 2000 Jun |
|
A concise review on the therapeutics of obesity. | 2000 Oct |
|
Long-term pharmacotherapy of obesity 2000: a review of efficacy and safety. | 2001 Aug 13-27 |
|
Amphetamine-type central nervous system stimulants release norepinephrine more potently than they release dopamine and serotonin. | 2001 Jan |
|
Pharmacologic options for the treatment of obesity. | 2001 Jul 15 |
|
Fatal 4-MTA intoxication: development of a liquid chromatographic-tandem mass spectrometric assay for multiple matrices. | 2001 Nov-Dec |
|
Operation for anorexigen-associated valvular heart disease. | 2001 Oct |
|
High performance liquid chromatography with UV detection for the simultaneous determination of sympathomimetic amines using 4-(4,5-diphenyl-1H-imidazole-2-yl)benzoyl chloride as a label. | 2001 Oct |
|
Clinical and echocardiographic follow-up of patients previously treated with dexfenfluramine or phentermine/fenfluramine. | 2001 Oct 24-31 |
|
Acute anorectic effect of single and combined drugs in mice using a non-deprivation protocol. | 2001 Sep |
|
The relationship between health-related quality of life and weight loss. | 2001 Sep |
|
Effects of anorexinogen agents on cloned voltage-gated K(+) channel hKv1.5. | 2001 Sep |
|
Pharmacotherapy of obesity: currently marketed and upcoming agents. | 2002 |
|
Effect of fenfluramine-derivative diet pills on cardiac valves: a meta-analysis of observational studies. | 2002 Dec |
|
Pharmacological management of obesity. | 2002 Dec |
|
Morphology of anorexigen-associated valve disease by transthoracic and transesophageal echocardiography. | 2002 Dec 1 |
|
Autopsy findings of heart and lungs in a patient with primary pulmonary hypertension associated with use of fenfluramine and phentermine. | 2002 Feb |
|
[Syncope - a systematic overview of classification, pathogenesis, diagnosis and management]. | 2002 Feb |
|
Automated headspace solid-phase microextraction and in-matrix derivatization for the determination of amphetamine-related drugs in human urine by gas chromatography-mass spectrometry. | 2002 Jan |
|
Reversal of Phen-Fen associated valvular regurgitation documented by serial echocardiography. | 2002 Jun |
|
Effects on serotonin in rat hypothalamus of D-fenfluramine, aminorex, phentermine and fluoxetine. | 2002 Jun 7 |
|
Prevalence of drug use in commercial tractor-trailer drivers. | 2002 May |
|
Enantiomeric separation of methamphetamine and related analogs by capillary zone electrophoresis: intelligence study in routine methamphetamine seizures. | 2002 Nov |
|
Anorexigen-induced cardiac valvulopathy and female gender. | 2003 Apr |
|
Noradrenergic modulation of ephedrine-induced hypophagia. | 2003 Apr |
|
Do these doctors give medicine a black eye? | 2003 Dec |
|
Ischemic colitis after weight-loss medication. | 2003 Dec |
|
Internet pharmacy prescription and phentermine overdose. | 2003 Feb |
|
Obesity drug pipeline not so fat. | 2003 Feb 7 |
|
Risk of valvular heart disease associated with use of fenfluramine. | 2003 Jun 11 |
|
The "steroid dementia syndrome": an unrecognized complication of glucocorticoid treatment. | 2004 Dec |
|
Pharmacological and surgical treatment of obesity. | 2004 Jul |
|
Relationship between collagen fibrils, glycosaminoglycans, and stress relaxation in mitral valve chordae tendineae. | 2004 Jul |
|
Pharmacotherapy for weight loss in adults with type 2 diabetes mellitus. | 2005 Jan 25 |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.drugs.com/dosage/phentermine.html
Usual Adult Dose for Weight Loss
15 to 37.5 mg orally once a day before breakfast or 1 to 2 hours after breakfast.
Usual Pediatric Dose for Weight Loss
17 years or older:
15 to 37.5 mg orally once a day before breakfast or 1 to 2 hours after breakfast.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/10799660
Phentermine inhibited serotonin-metabolizing (MAO-A) activity in rat lung, brain, and liver with K(i) values of 85-88 uM.
Substance Class |
Chemical
Created
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admin
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NCI_THESAURUS |
C29728
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DEA NO. |
1640
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CHEMBL1574
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DBSALT000138
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C29361
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