trihexyphenidyl Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 2745 | 144-11-6 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
One of the centrally acting MUSCARINIC ANTAGONISTS used for treatment of PARKINSONIAN DISORDERS and drug-induced extrapyramidal movement disorders and as an antispasmodic.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 10 | mg | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 10 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 0.63 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 99 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| May 13, 1949 | FDA |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | N04AA01 | NERVOUS SYSTEM ANTI-PARKINSON DRUGS ANTICHOLINERGIC AGENTS Tertiary amines |
| MeSH PA | D018726 | Anti-Dyskinesia Agents |
| MeSH PA | D000978 | Antiparkinson Agents |
| MeSH PA | D002491 | Central Nervous System Agents |
| MeSH PA | D018678 | Cholinergic Agents |
| MeSH PA | D018680 | Cholinergic Antagonists |
| MeSH PA | D018727 | Muscarinic Antagonists |
| MeSH PA | D018377 | Neurotransmitter Agents |
Drug Use (View source of the data)
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Postencephalitic parkinsonism | indication | 19972008 | DOID:14332 |
| Parkinsonism | indication | 32798002 | |
| Parkinson's disease | indication | 49049000 | DOID:14330 |
| Extrapyramidal disease | indication | 76349003 | |
| Arteriosclerotic Parkinsonism | indication | ||
| Urinary tract obstruction | contraindication | 7163005 | DOID:5200 |
| Chronic obstructive lung disease | contraindication | 13645005 | DOID:3083 |
| Severe chronic ulcerative colitis | contraindication | 14311001 | |
| Disorder of autonomic nervous system | contraindication | 15241006 | |
| Toxic megacolon | contraindication | 28536002 | DOID:1770 |
| Atony of colon | contraindication | 29479008 | |
| Shigellosis | contraindication | 36188001 | |
| Hypertensive disorder | contraindication | 38341003 | DOID:10763 |
| Conduction disorder of the heart | contraindication | 44808001 | |
| Low blood pressure | contraindication | 45007003 | |
| Achalasia of esophagus | contraindication | 45564002 | DOID:9164 |
| Chronic heart failure | contraindication | 48447003 | |
| Dysuria | contraindication | 49650001 | |
| Paralytic ileus | contraindication | 55525008 | DOID:8442 |
| Ulcerative colitis | contraindication | 64766004 | DOID:8577 |
| Hiatal hernia | contraindication | 84089009 | DOID:12642 |
| Open-angle glaucoma | contraindication | 84494001 | DOID:1067 |
| Kidney disease | contraindication | 90708001 | DOID:557 |
| Thyrotoxicosis | contraindication | 90739004 | DOID:7997 |
| Myasthenia gravis | contraindication | 91637004 | DOID:437 |
| Tardive dyskinesia | contraindication | 102449007 | |
| Dysentery | contraindication | 111939009 | |
| Gastrointestinal obstruction | contraindication | 126765001 | |
| Bleeding | contraindication | 131148009 | |
| Gastroesophageal reflux disease | contraindication | 235595009 | DOID:8534 |
| Disease of liver | contraindication | 235856003 | DOID:409 |
| Benign prostatic hyperplasia | contraindication | 266569009 | |
| Retention of urine | contraindication | 267064002 | |
| Fever | contraindication | 386661006 | |
| Angle-closure glaucoma | contraindication | 392291006 | DOID:13550 |
| Pseudomembranous enterocolitis | contraindication | 397683000 | |
| Gastric ulcer | contraindication | 397825006 | DOID:10808 |
| Disorder of coronary artery | contraindication | 414024009 |
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 9.23 | Basic |
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Muscarinic acetylcholine receptor M1 | GPCR | ANTAGONIST | IC50 | 8.89 | CHEMBL | CHEMBL | |||
| Cytochrome P450 2D6 | Enzyme | IC50 | 5.61 | DRUG MATRIX | |||||
| Muscarinic acetylcholine receptor M3 | GPCR | IC50 | 7.58 | CHEMBL | |||||
| Sigma non-opioid intracellular receptor 1 | Membrane receptor | Ki | 7.35 | DRUG MATRIX | |||||
| Muscarinic acetylcholine receptor M5 | GPCR | IC50 | 7.99 | CHEMBL | |||||
| Muscarinic acetylcholine receptor M2 | GPCR | IC50 | 7.73 | CHEMBL | |||||
| Muscarinic acetylcholine receptor M4 | GPCR | IC50 | 8.17 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4019959 | VUID |
| N0000148044 | NUI |
| C0041009 | UMLSCUI |
| D00787 | KEGG_DRUG |
| 6RC5V8B7PO | UNII |
| 1318 | INN_ID |
| 2190009 | SNOMEDCT_US |
| 4019959 | VANDF |
| 10811 | RXNORM |
| 387120000 | SNOMEDCT_US |
| d00970 | MMSL |
| 004664 | NDDF |
| 52-49-3 | SECONDARY_CAS_RN |
| CHEBI:9720 | CHEBI |
| CHEMBL1092 | ChEMBL_ID |
| CHEMBL1490 | ChEMBL_ID |
| DB00376 | DRUGBANK_ID |
| 5572 | PUBCHEM_CID |
| D014282 | MESH_DESCRIPTOR_UI |
| 7315 | IUPHAR_LIGAND_ID |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Trihexyphenidyl Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0121-0658 | SOLUTION | 2 mg | ORAL | ANDA | 13 sections |
| Trihexyphenidyl Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0591-5335 | TABLET | 2 mg | ORAL | ANDA | 9 sections |
| Trihexyphenidyl Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0591-5337 | TABLET | 5 mg | ORAL | ANDA | 9 sections |
| Trihexyphenidyl hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0615-0675 | TABLET | 2 mg | ORAL | ANDA | 9 sections |
| Trihexyphenidyl hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0615-0676 | TABLET | 5 mg | ORAL | ANDA | 9 sections |
| Trihexyphenidyl Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 16571-160 | TABLET | 2 mg | ORAL | ANDA | 13 sections |
| Trihexyphenidyl Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 16571-161 | TABLET | 5 mg | ORAL | ANDA | 13 sections |
| trihexyphenidyl hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 46672-635 | SOLUTION | 2 mg | ORAL | ANDA | 12 sections |
| Trihexyphenidyl Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50090-2994 | TABLET | 2 mg | ORAL | ANDA | 9 sections |
| TRIHEXYPHENIDYL HYDROCHLORIDE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51407-265 | TABLET | 2 mg | ORAL | ANDA | 9 sections |
| TRIHEXYPHENIDYL HYDROCHLORIDE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51407-266 | TABLET | 5 mg | ORAL | ANDA | 9 sections |
| Trihexyphenidyl Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 53808-0633 | TABLET | 2 mg | ORAL | ANDA | 11 sections |
| Trihexyphenidyl Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 53808-0634 | TABLET | 5 mg | ORAL | ANDA | 11 sections |
| Trihexyphenidyl Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 53808-0696 | TABLET | 5 mg | ORAL | ANDA | 9 sections |
| Trihexyphenidyl Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 54738-554 | TABLET | 2 mg | ORAL | ANDA | 11 sections |
| Trihexyphenidyl Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 54738-555 | TABLET | 5 mg | ORAL | ANDA | 11 sections |
| Trihexyphenidyl Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 61748-054 | SYRUP | 2 mg | ORAL | ANDA | 13 sections |
| Trihexyphenidyl Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 63850-0021 | TABLET | 2 mg | ORAL | ANDA | 13 sections |
| Trihexyphenidyl Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 63850-0022 | TABLET | 5 mg | ORAL | ANDA | 13 sections |
| Trihexyphenidyl Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 64725-0161 | TABLET | 5 mg | ORAL | ANDA | 12 sections |
| Trihexyphenidyl Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68151-2782 | TABLET | 2 mg | ORAL | ANDA | 9 sections |
| Trihexyphenidyl Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 69452-241 | TABLET | 2 mg | ORAL | ANDA | 13 sections |
| Trihexyphenidyl Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 69452-242 | TABLET | 5 mg | ORAL | ANDA | 13 sections |
| Trihexyphenidyl Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70518-1021 | TABLET | 2 mg | ORAL | ANDA | 9 sections |
| Trihexyphenidyl Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70518-1140 | TABLET | 5 mg | ORAL | ANDA | 9 sections |
| Trihexyphenidyl Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70518-1612 | TABLET | 2 mg | ORAL | ANDA | 9 sections |
| Trihexyphenidyl Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70518-1657 | TABLET | 5 mg | ORAL | ANDA | 9 sections |
| TRIHEXYPHENIDYL HYDROCHLORIDE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70518-2409 | TABLET | 5 mg | ORAL | ANDA | 9 sections |
| TRIHEXYPHENIDYL HYDROCHLORIDE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70518-2410 | TABLET | 2 mg | ORAL | ANDA | 9 sections |
| TRIHEXYPHENIDYL HYDROCHLORIDE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70954-211 | TABLET | 5 mg | ORAL | ANDA | 9 sections |