hyoscyamine
Hyoscyamine as a natural plant alkaloid derivative and anticholinergic. Hyoscyamine is used to treat a variety of stomach/intestinal problems such as cramps and irritable bowel syndrome. It is also used to treat other conditions such as bladder and bowel control problems, cramping pain caused by kidney stones and gallstones, and Parkinson's disease. In addition, it is used to decrease side effects of certain medications (drugs used to treat myasthenia gravis) and insecticides. Hyoscyamine inhibits specifically the actions of acetylcholine on structures innervated by postganglionic cholinergic nerves and on smooth muscles that respond to acetylcholine but lack cholinergic innervation. These peripheral cholinergic receptors are present in the autonomic effector cells of the smooth muscle, cardiac muscle, the sinoatrial node, the atrioventricular node, and the exocrine glands. At therapeutic doses, it is completely devoid of any action on autonomic ganglia. Side effects include dry mouth and throat, increased appetite leading to weight gain, eye pain, blurred vision, restlessness, dizziness, arrhythmia, flushing, and faintness. Additive adverse effects resulting from cholinergic blockade may occur when hyoscyamine is administered concomitantly with other antimuscarinics, amantadine, haloperidol, phenothiazines, monoamine oxidase (MAO) inhibitors, tricyclic antidepressants or some antihistamines. — NCATS
Clinical trial activity
2 trials · 3 clinical orgs · 0 marketing orgs
Earliest trial started Jul 1, 2014 (NCT02389998)
Timeline
No events for the selected filters.
Indications
Approved for
Studied for
Mechanism of action
- Muscarinic acetylcholine receptorANTAGONIST
Muscarinic acetylcholine receptor antagonist
- Muscarinic acetylcholine receptor M3 (CHRM3) ↗
- Muscarinic acetylcholine receptor M4 (CHRM4) ↗
- Muscarinic acetylcholine receptor M1 (CHRM1) ↗
- Muscarinic acetylcholine receptor M5 (CHRM5) ↗
- Muscarinic acetylcholine receptor M2 (CHRM2) ↗
- Muscarinic acetylcholine receptor M2
- Muscarinic acetylcholine receptor M1
- Muscarinic acetylcholine receptor M4
- Muscarinic acetylcholine receptor M5
- Muscarinic acetylcholine receptor M3
- Muscarinic acetylcholine receptors; M2 & M3
- Muscarinic acetylcholine receptors; M1 & M2
- Muscarinic acetylcholine receptor M1/M5 chimeric protein
- Muscarinic acetylcholine receptor M1 and M3
- Muscarinic acetylcholine receptor M2 and M4
- Muscarinic acetylcholine receptor M2 and M5
Chemistry & pharmacology
SMILES
CN1[C@H]2CC[C@@H]1C[C@@H](C2)OC(=O)[C@H](CO)C3=CC=CC=C3- Mol. weight
- 289.3694 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- WikipediaHyoscyamine ↗
- NCATSPX44XO846X ↗
- ChEMBLCHEMBL1697729 ↗
- ChEMBLCHEMBL1331216 ↗
Also known as
- [3(s)-endo]-α-(hydroxymethyl)benzeneacetic acid 8-methyl-8-azabicyclo[3.2.1]oct-3-yl ester
- [3(s)-endo]-α-(hydroxymethyl)benzeneacetic acid 8-methyl-8-azabicyclo[3.2.1]oct-3-yl ester
- (-)-atropine
- daturin
- daturin
- daturine
- daturine
- duboisine
- duboisine
- hyoscyamin
- hyoscyamin
- hyoscyamine
- hyoscyamine
- hyoscyamine
- hyoscyamine
- hyoscyamine
- hyoscyamine
- hyoscyamine
- hyoscyamine
- hyoscyamine
- hyoscyamine
- (-)-hyoscyamine
- (−)-hyoscyamine
- (−)-hyoscyamine
- hyoscyamine sulfate
- hyoscyamine sulfate
- hyoscyamine sulfate
- hyoscyamine sulphate
- hyoscyamine sulphate
- hyoscyaminum
- hyoscyaminum
- l-atropine
- levsin
- levsin
- levsinex
- levsinex
- levsinex timecaps
- levsin sl
- levsin sl
- l-hyoscyamin
- l-hyoscyamine
- l-hyoscyamine
- l-hyoscyamine
- neoquess
- neoquess
- peptard
- peptard
- (s)-atropine
- (s)-atropine
- (s)-(−)-hyoscyamine
- (s)-(−)-hyoscyamine
- tropine-l-tropate
- tropine-l-tropate
- tropine tropate
- tropine tropate
- tropine tropate
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT03750656 | Phase 4 | Nov 12, 2018 | University of Kansas |
| NCT02389998 | N/A | Jul 1, 2014 | Harvard University, Ohio State University |
Organizations
Research & Development (3)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Harvard University | Academic/Hospital | 1 | 1 | 1 | 2014 |
| Ohio State University | Academic/Hospital | 1 | 0 | 1 | 2014 |
| University of Kansas | Academic/Hospital | 1 | 1 | 1 | 2018 |