Details
Stereochemistry | ACHIRAL |
Molecular Formula | C10H15N |
Molecular Weight | 149.2328 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CC(C)(N)CC1=CC=CC=C1
InChI
InChIKey=DHHVAGZRUROJKS-UHFFFAOYSA-N
InChI=1S/C10H15N/c1-10(2,11)8-9-6-4-3-5-7-9/h3-7H,8,11H2,1-2H3
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 Date1958 |
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 |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
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 |
---|---|---|
[Valvular heart disease and primary pulmonary hypertension associated with fenfluramine-phentermine]. | 1998 Dec 1 |
|
[Development of pulmonary hypertension and multi-valvular damage caused by appetite depressants]. | 1998 Dec 1 |
|
Detailed examination of fenfluramine-phentermine users with valve abnormalities identified in Fargo, North Dakota. | 1999 Aug 1 |
|
Echocardiographic improvement over time after cessation of use of fenfluramine and phentermine. | 1999 Dec |
|
Echocardiographic prevalence of mitral and/or aortic regurgitation in patients exposed to either fenfluramine-phentermine combination or to dexfenfluramine. | 1999 Dec 1 |
|
Serial echocardiographic and clinical evaluation of valvular regurgitation before, during, and after treatment with fenfluramine or dexfenfluramine and mazindol or phentermine. | 1999 Jul |
|
Peripheral vasculopathy and nephropathy in association with phentermine. | 1999 Jul |
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Pharmaceutical cost savings of treating obesity with weight loss medications. | 1999 Nov |
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Beneficial effects of pharmacotherapy on weight loss, depressive symptoms, and eating patterns in obese binge eaters and non-binge eaters. | 1999 Sep |
|
Dose-effect of fenfluramine use on the severity of valvular heart disease among fen-phen patients with valvulopathy. | 1999 Sep |
|
Histologic changes in three explanted native cardiac valves following use of fenfluramines. | 1999 Sep-Oct |
|
Valvular abnormalities and cardiovascular status following exposure to dexfenfluramine or phentermine/fenfluramine. | 2000 Apr 5 |
|
[Obesity: principles of drug therapy]. | 2000 Aug |
|
Dose and duration of fenfluramine-phentermine therapy impacts the risk of significant valvular heart disease. | 2000 Jul 1 |
|
Complex vascular lesions at autopsy in a patient with phentermine-fenfluramin. | 2000 Jun |
|
Diet drug-related cardiac valve disease: the Mayo Clinic echocardiographic laboratory experience. | 2000 May |
|
Fenfluramine and phentermine and cardiovascular findings: effect of treatment duration on prevalence of valve abnormalities. | 2000 May 2 |
|
A concise review on the therapeutics of obesity. | 2000 Oct |
|
Appetite suppressants and valvular heart disease. | 2001 Apr |
|
Long-term pharmacotherapy of obesity 2000: a review of efficacy and safety. | 2001 Aug 13-27 |
|
Silver lining to the cloud over anorexogen-related cardiac valvulopathy? | 2001 Feb 20 |
|
Amphetamine-type central nervous system stimulants release norepinephrine more potently than they release dopamine and serotonin. | 2001 Jan |
|
Low risk of significant echocardiographic valvulopathy in patients treated with anorectic drugs. | 2001 Jul |
|
Separation of sympathomimetic amines of abuse and related compounds by micellar electrokinetic chromatography. | 2001 Jul |
|
Pharmacologic options for the treatment of obesity. | 2001 Jul 15 |
|
Acyclic neutral carrier-based polymer membrane electrode for a stimulant, phentermine. | 2001 Jun |
|
Bitter pills, bad medicine. | 2001 Jun 4 |
|
A comparison of cocaine, GBR 12909, and phentermine self-administration by rhesus monkeys on a progressive-ratio schedule. | 2001 Mar 1 |
|
Rapid clot formation and abnormal fibrin structure in a symptomatic patient taking fenfluramine--a case report. | 2001 May |
|
Fenfluramine and phentermine. | 2001 Nov 6 |
|
Herbal therapy for management of obesity: observations from a clinical endocrinology practice. | 2001 Nov-Dec |
|
Monoamine oxidase inhibition is unlikely to be relevant to the risks associated with phentermine and fenfluramine: a comparison with their abilities to evoke monoamine release. | 2001 Oct |
|
Additive effects on rat brain 5HT release of combining phentermine with dexfenfluramine. | 2001 Oct |
|
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 |
|
Effect of fenfluramine-derivative diet pills on cardiac valves: a meta-analysis of observational studies. | 2002 Dec |
|
Autopsy findings of heart and lungs in a patient with primary pulmonary hypertension associated with use of fenfluramine and phentermine. | 2002 Feb |
|
Pregnancy outcomes after first trimester exposure to phentermine/fenfluramine. | 2002 Mar |
|
Phentermine inhibition of recombinant human liver monoamine oxidases A and B. | 2002 Mar 1 |
|
Regression and progression of valvulopathy associated with fenfluramine and phentermine. | 2002 Mar 19 |
|
Appetite suppressants and valvular heart disease. | 2002 Sep |
|
Effects of preexposure to dexfenfluramine, phentermine, dexfenfluramine-phentermine, or fluoxetine on sibutramine-induced hypophagia in the adult rat. | 2003 Apr |
|
The effect of the anorectic agent, d-fenfluramine, and its primary metabolite, d-norfenfluramine, on intact human platelet serotonin uptake and efflux. | 2003 Dec |
|
Medical monitoring for pharmaceutical injuries: tort law for the public's health? | 2003 Feb 19 |
|
Liquid chromatography studies on the pharmacokinetics of phentermine and fenfluramine in brain and blood microdialysates after intraperitoneal administration to rats. | 2003 Jul 5 |
|
Risk of valvular heart disease associated with use of fenfluramine. | 2003 Jun 11 |
|
Malpractice. Conviction upheld for doctor who treated AIDS with fen/phen. | 2003 May 9 |
|
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.
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LIVERTOX |
NBK548947
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ACTIVE MOIETY
SALT/SOLVATE (PARENT)