protriptyline
Trade name: vivactil
Approved
Sep 27, 1967
Protriptyline (trade name Vivactil) is a tricyclic antidepressant, indicated for the treatment of depression. Protriptyline acts by decreasing the reuptake of norepinephrine and to a lesser extent serotonin (5-HT) in the brain. Tricyclic antidepressants act to change the balance of naturally occurring chemicals in the brain that regulate the transmission of nerve impulses between cells. Protriptyline increases the concentration of norepinephrine and serotonin (both chemicals that stimulate nerve cells) and, to a lesser extent, blocks the action of another brain chemical, acetylcholine. The therapeutic effects of protriptyline, like other antidepressants, appear slowly. Maximum benefit is often not evident for at least two weeks after starting the drug. Protriptyline is used primarily to treat depression and to treat the combination of symptoms of anxiety and depression. Like most antidepressants of this chemical and pharmacological class, protriptyline has also been used in limited numbers of patients to treat panic disorder, obsessive-compulsive disorder, attention-deficit/hyperactivity disorder, enuresis, eating disorders such as bulimia nervosa, cocaine dependency, and the depressive phase of bipolar disorder (manic-depressive) disorder. It has also been used to support smoking cessation programs. Like all tricyclic antidepressants, protriptyline should be used cautiously and with close physician supervision. This is especially so in the elderly, or people who have benign prostatic hypertrophy (enlarged prostate gland), or urinary retention, or glaucoma, especially angle-closure glaucoma (the most severe form). Before starting treatment, people should discuss the relative risks and benefits of treatment with their doctors to help determine if protriptyline is the right antidepressant for them. A common problem with tricyclic antidepressants is sedation (drowsiness, lack of physical and mental alertness), but protriptyline is considered the least sedating agent among this class of agents. Its side effects are especially noticeable early in therapy. In most people, early tricyclic side-effects decrease or disappear entirely with time, but, until then, patients taking protriptyline should take care to assess which side-effects occur in them and should not perform hazardous activities requiring mental acuity or coordination. The side-effects are increased when protriptyline is taken with central nervous system depressants, such as alcoholic beverages, sleeping medications, other sedatives, or antihistamines, as well as with other antidepressants including SSRIs, SNRIs or monoamine oxidase Inhibitors. — NCATS
Clinical trial activity
1 trials · 2 clinical orgs · 9 marketing orgs
Earliest trial started Dec 1, 2006 (NCT00754962)
Timeline
1960s
1990s
- Aug 24, 1995
Odyssey Pharmaceuticals — Marketing Organization
- Aug 24, 1995
Heritage Pharma — Marketing Organization
- Aug 24, 1995
Chartwell Pharmaceuticals — Marketing Organization
2000s
- Sep 16, 2008
West-Ward Pharmaceutical — Marketing Organization
- Sep 16, 2008
Hikma — Marketing Organization
2010s
- May 3, 2010
Sigmapharm Laboratories — Marketing Organization
- Nov 19, 2012
Epic Pharma Llc — Marketing Organization
Indications
Approved for
Mechanism of action
- Norepinephrine transporterINHIBITOR
SLC6A2 inhibitor
- Serotonin transporterINHIBITOR
SLC6A4 inhibitor
Approval history
- approvedSep 27, 1967
Chemistry & pharmacology
SMILES
CNCCCC1c2ccccc2C=Cc2ccccc21- Mol. weight
- 263.38 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Achiral Molecule
- Inorganic
- No
- Polymer
- No
- Delivery
- Oral
- Availability
- Prescription Only
Oral
Yes
Parenteral
No
Topical
No
Sources
- ChEMBLCHEMBL668 ↗
- WikipediaProtriptyline ↗
- NCATS4NDU154T12 ↗
- ChEMBLCHEMBL1200332 ↗
Also known as
- 3-(5h-dibenzo[a,d][7]annulen-5-yl)-n-methylpropan-1-amine
- 3-(5h-dibenzo[a,d][7]annulen-5-yl)-n-methylpropan-1-amine
- 3-(5h-dibenzo[a,d]cyclohepten-5-yl)-n-methyl-1-propanamine
- 3-(5h-dibenzo[a,d]cyclohepten-5-yl)-n-methyl-1-propanamine
- 5-(3-methylaminopropyl)-5h-dibenzo[a,d]cycloheptene
- 5-(3-methylaminopropyl)-5h-dibenzo[a,d]cycloheptene
- 7-(3-methylaminopropyl)-1,2:5,6-dibenzocycloheptatriene
- 7-(3-methylaminopropyl)-1,2:5,6-dibenzocycloheptatriene
- amimetilina
- amimetilina
- concordin-10
- concordin-5
- mk-240
- mk-240
- n-methyl-5h-dibenzo[a,d]cycloheptene-5-propanamine
- n-methyl-5h-dibenzo[a,d]cycloheptene-5-propanamine
- n-methyl-5h-dibenzo[a,d]cycloheptene-5-propylamine
- n-methyl-5h-dibenzo[a,d]cycloheptene-5-propylamine
- protriptilina
- protriptilina
- protriptylin
- protriptylin
- protriptyline
- protriptyline
- protriptyline
- protriptyline
- protriptyline
- protriptyline
- protriptyline
- protriptyline
- protriptyline
- protriptyline
- protriptyline hcl
- protriptyline hcl
- protriptyline hcl
- protriptyline hydrochloride
- protriptyline hydrochloride
- protriptyline hydrochloride
- protriptyline hydrochloride
- protriptylinum
- protriptylinum
- protryptyline
- triptil
- vivactil
- vivactil
- vivactil
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT00754962 | N/A | Dec 1, 2006 | Advanced Biomedical Research, Roxane Laboratories |
Organizations
Research & Development (2)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Advanced Biomedical Research | For profit | 1 | 0 | 1 | 2006 |
| Roxane Laboratories | For profit | 1 | 1 | 1 | 2006 |
Marketing (11)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Chartwell Pharmaceuticals | For profit | MKTG | Aug 24, 1995 |
| Epic Pharma Llc | For profit | MKTG | Nov 19, 2012 |
| Heritage Pharma | For profit | SYN | Aug 24, 1995 |
| Heritage Pharma | For profit | MKTG | Aug 24, 1995 |
| Hikma | For profit | MKTG | Sep 16, 2008 |
| Hikma | For profit | SYN | Sep 16, 2008 |
| Merck | For profit | NDA | Sep 27, 1967 |
| Odyssey Pharmaceuticals | For profit | MKTG | Aug 24, 1995 |
| Sigmapharm Laboratories | For profit | MKTG | May 3, 2010 |
| Teva | For profit | NDA2 | Sep 27, 1967 |
| West-Ward Pharmaceutical | For profit | MKTG | Sep 16, 2008 |