terbutaline Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| bronchodilators, phenethylamine derivatives | 2598 | 23031-25-6 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A selective beta-2 adrenergic agonist used as a bronchodilator and tocolytic.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 2 | mg | Inhal.aerosol |
| 2 | mg | Inhal.powder |
| 20 | mg | Inhal.solution |
| 15 | mg | O |
| 15 | mg | P |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 3 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 213 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 56 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 1.11 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 14 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 1.50 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 3.40 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.75 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 15 hours | Lombardo F, Berellini G, Obach RS |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| March 25, 1974 | FDA |
FDA Adverse Event Reporting System (Female)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Asthma | 184.13 | 16.23 | 140 | 7479 | 108832 | 53232615 |
| Wheezing | 74.69 | 16.23 | 67 | 7552 | 65208 | 53276239 |
| Lactic acidosis | 69.73 | 16.23 | 51 | 7568 | 37202 | 53304245 |
| Dyspnoea | 65.12 | 16.23 | 207 | 7412 | 586025 | 52755422 |
| Squamous cell carcinoma of the oral cavity | 44.03 | 16.23 | 10 | 7609 | 307 | 53341140 |
| Allergy to metals | 38.55 | 16.23 | 10 | 7609 | 540 | 53340907 |
| Iodine allergy | 36.35 | 16.23 | 10 | 7609 | 677 | 53340770 |
| Shock haemorrhagic | 35.83 | 16.23 | 20 | 7599 | 9163 | 53332284 |
| Exposure during pregnancy | 34.48 | 16.23 | 63 | 7556 | 124797 | 53216650 |
| Acute kidney injury | 33.00 | 16.23 | 95 | 7524 | 253773 | 53087674 |
| Sputum discoloured | 32.31 | 16.23 | 22 | 7597 | 14317 | 53327130 |
| Bronchospasm | 31.66 | 16.23 | 23 | 7596 | 16575 | 53324872 |
| Forced expiratory volume decreased | 29.82 | 16.23 | 15 | 7604 | 5570 | 53335877 |
| Hyperlactacidaemia | 29.54 | 16.23 | 12 | 7607 | 2713 | 53338734 |
| Tremor | 29.25 | 16.23 | 59 | 7560 | 125677 | 53215770 |
| Post viral fatigue syndrome | 27.37 | 16.23 | 6 | 7613 | 156 | 53341291 |
| Obstructive airways disorder | 26.30 | 16.23 | 21 | 7598 | 17408 | 53324039 |
| Rubber sensitivity | 26.22 | 16.23 | 10 | 7609 | 1915 | 53339532 |
| Cough | 25.85 | 16.23 | 88 | 7531 | 256805 | 53084642 |
| Middle insomnia | 25.49 | 16.23 | 17 | 7602 | 10691 | 53330756 |
| Folate deficiency | 25.36 | 16.23 | 10 | 7609 | 2094 | 53339353 |
| Hepatocellular injury | 25.21 | 16.23 | 26 | 7593 | 29960 | 53311487 |
| Cholestasis | 24.34 | 16.23 | 25 | 7594 | 28670 | 53312777 |
| Nasal discharge discolouration | 24.11 | 16.23 | 9 | 7610 | 1625 | 53339822 |
| Asthmatic crisis | 23.06 | 16.23 | 9 | 7610 | 1834 | 53339613 |
| Premature separation of placenta | 22.94 | 16.23 | 9 | 7610 | 1858 | 53339589 |
| Food allergy | 21.89 | 16.23 | 14 | 7605 | 8204 | 53333243 |
| Rheumatoid arthritis | 21.54 | 16.23 | 9 | 7610 | 314522 | 53026925 |
| Heart rate increased | 20.79 | 16.23 | 40 | 7579 | 82275 | 53259172 |
| Phlebectomy | 20.66 | 16.23 | 4 | 7615 | 55 | 53341392 |
| Sleep disorder due to a general medical condition | 20.60 | 16.23 | 13 | 7606 | 7444 | 53334003 |
| Pleural rub | 20.59 | 16.23 | 4 | 7615 | 56 | 53341391 |
| Exposure to allergen | 20.23 | 16.23 | 5 | 7614 | 222 | 53341225 |
| Haematoma | 19.32 | 16.23 | 24 | 7595 | 33820 | 53307627 |
| Respiratory rate increased | 18.85 | 16.23 | 15 | 7604 | 12368 | 53329079 |
| Eosinophilia | 18.84 | 16.23 | 19 | 7600 | 21316 | 53320131 |
| Maternal drugs affecting foetus | 18.74 | 16.23 | 11 | 7608 | 5535 | 53335912 |
| Fallopian tube disorder | 18.46 | 16.23 | 5 | 7614 | 319 | 53341128 |
| Eosinophilic granulomatosis with polyangiitis | 18.22 | 16.23 | 8 | 7611 | 2191 | 53339256 |
| Premature baby | 18.16 | 16.23 | 18 | 7601 | 19783 | 53321664 |
| Respiratory distress | 17.74 | 16.23 | 23 | 7596 | 33804 | 53307643 |
| Forced expiratory volume abnormal | 17.64 | 16.23 | 4 | 7615 | 122 | 53341325 |
| Productive cough | 17.41 | 16.23 | 30 | 7589 | 56699 | 53284748 |
| Premature labour | 16.76 | 16.23 | 14 | 7605 | 12348 | 53329099 |
FDA Adverse Event Reporting System (Male)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Asthma | 132.62 | 18.65 | 81 | 4577 | 43984 | 32464884 |
| Wheezing | 61.20 | 18.65 | 47 | 4611 | 36827 | 32472041 |
| Dyspnoea | 53.77 | 18.65 | 142 | 4516 | 361903 | 32146965 |
| Chest discomfort | 46.69 | 18.65 | 46 | 4612 | 50184 | 32458684 |
| Cholestasis | 46.03 | 18.65 | 35 | 4623 | 26998 | 32481870 |
| Hyperkaliuria | 44.14 | 18.65 | 9 | 4649 | 163 | 32508705 |
| Exposure during pregnancy | 44.07 | 18.65 | 23 | 4635 | 9206 | 32499662 |
| Forced expiratory volume decreased | 43.17 | 18.65 | 17 | 4641 | 3539 | 32505329 |
| Wolff-Parkinson-White syndrome | 42.10 | 18.65 | 9 | 4649 | 207 | 32508661 |
| Agranulocytosis | 39.09 | 18.65 | 30 | 4628 | 23447 | 32485421 |
| Bronchospasm | 35.08 | 18.65 | 21 | 4637 | 10934 | 32497934 |
| Premature baby | 33.79 | 18.65 | 25 | 4633 | 18493 | 32490375 |
| Nasal disorder | 32.16 | 18.65 | 11 | 4647 | 1539 | 32507329 |
| Gastrointestinal mucosal necrosis | 31.92 | 18.65 | 7 | 4651 | 182 | 32508686 |
| Placental transfusion syndrome | 28.63 | 18.65 | 4 | 4654 | 4 | 32508864 |
| Pulmonary valve stenosis | 27.22 | 18.65 | 7 | 4651 | 364 | 32508504 |
| Unmasking of previously unidentified disease | 27.04 | 18.65 | 8 | 4650 | 701 | 32508167 |
| Penile erythema | 26.79 | 18.65 | 6 | 4652 | 172 | 32508696 |
| Meralgia paraesthetica | 26.56 | 18.65 | 6 | 4652 | 179 | 32508689 |
| Respiratory distress | 25.07 | 18.65 | 28 | 4630 | 35218 | 32473650 |
| Bronchospasm paradoxical | 24.82 | 18.65 | 5 | 4653 | 85 | 32508783 |
| Nasal inflammation | 24.51 | 18.65 | 6 | 4652 | 255 | 32508613 |
| Obstructive airways disorder | 23.75 | 18.65 | 17 | 4641 | 11944 | 32496924 |
| Foetal distress syndrome | 23.66 | 18.65 | 8 | 4650 | 1081 | 32507787 |
| Heart rate increased | 22.78 | 18.65 | 29 | 4629 | 41799 | 32467069 |
| Middle insomnia | 22.25 | 18.65 | 13 | 4645 | 6471 | 32502397 |
| Prothrombin time ratio decreased | 22.09 | 18.65 | 6 | 4652 | 386 | 32508482 |
| Lactic acidosis | 21.08 | 18.65 | 25 | 4633 | 33511 | 32475357 |
| Stillbirth | 20.77 | 18.65 | 5 | 4653 | 198 | 32508670 |
| Ductus arteriosus premature closure | 20.15 | 18.65 | 5 | 4653 | 225 | 32508643 |
| Lung disorder | 19.32 | 18.65 | 24 | 4634 | 33730 | 32475138 |
| Clonic convulsion | 19.01 | 18.65 | 6 | 4652 | 653 | 32508215 |
| Accelerated idioventricular rhythm | 18.88 | 18.65 | 4 | 4654 | 88 | 32508780 |
| Atrial septal defect | 18.76 | 18.65 | 12 | 4646 | 7013 | 32501855 |
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | R03AC03 | RESPIRATORY SYSTEM DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES ADRENERGICS, INHALANTS Selective beta-2-adrenoreceptor agonists |
| ATC | R03CC03 | RESPIRATORY SYSTEM DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES ADRENERGICS FOR SYSTEMIC USE Selective beta-2-adrenoreceptor agonists |
| ATC | R03CC53 | RESPIRATORY SYSTEM DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES ADRENERGICS FOR SYSTEMIC USE Selective beta-2-adrenoreceptor agonists |
| MeSH PA | D018663 | Adrenergic Agents |
| MeSH PA | D000322 | Adrenergic Agonists |
| MeSH PA | D058666 | Adrenergic beta-2 Receptor Agonists |
| MeSH PA | D000318 | Adrenergic beta-Agonists |
| MeSH PA | D018927 | Anti-Asthmatic Agents |
| MeSH PA | D001993 | Bronchodilator Agents |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D018373 | Peripheral Nervous System Agents |
| MeSH PA | D012102 | Reproductive Control Agents |
| MeSH PA | D019141 | Respiratory System Agents |
| MeSH PA | D013566 | Sympathomimetics |
| MeSH PA | D015149 | Tocolytic Agents |
| CHEBI has role | CHEBI:35522 | beta-adrenergic receptor agonist |
| CHEBI has role | CHEBI:35523 | bronchodilator agents |
| CHEBI has role | CHEBI:35524 | sympathomimetic |
| CHEBI has role | CHEBI:35526 | hypoglycemic drug |
| CHEBI has role | CHEBI:38462 | acetylcholine esterase inhibitor |
| CHEBI has role | CHEBI:49167 | anti-asthmatic agents |
| CHEBI has role | CHEBI:66993 | anti-contraction drug |
Drug Use (View source of the data)
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Bronchitis | indication | 32398004 | DOID:6132 |
| Tear film insufficiency | indication | 46152009 | |
| Pulmonary emphysema | indication | 87433001 | |
| Asthma | indication | 195967001 | DOID:2841 |
| Skin irritation | indication | 367466007 | |
| Asthma management | indication | 406162001 | |
| Itching of skin | indication | 418363000 | |
| Acute exacerbation of asthma | indication | 708038006 | |
| Chronic Obstructive Pulmonary Disease with Bronchospasms | indication | ||
| Minor Skin Wound Pain | indication | ||
| Bronchospasm Prevention | indication | ||
| Premature labor | off-label use | 6383007 | |
| Bronchiectasis | off-label use | 12295008 | DOID:9563 |
| Keratoconjunctivitis sicca | off-label use | 302896008 | DOID:12895 |
| Pulmonary edema | contraindication | 19242006 | DOID:11396 |
| Hyperthyroidism | contraindication | 34486009 | DOID:7998 |
| Hypertensive disorder | contraindication | 38341003 | DOID:10763 |
| Hypokalemia | contraindication | 43339004 | |
| Conduction disorder of the heart | contraindication | 44808001 | |
| Ketoacidosis | contraindication | 56051008 | |
| Diabetes mellitus | contraindication | 73211009 | DOID:9351 |
| Compression of umbilical cord | contraindication | 79222000 | |
| Hyperglycemia | contraindication | 80394007 | DOID:4195 |
| Decreased respiratory function | contraindication | 80954004 | |
| Epilepsy | contraindication | 84757009 | DOID:1826 |
| Open wound | contraindication | 125643001 | |
| Seizure disorder | contraindication | 128613002 | |
| Chronic myocardial ischemia | contraindication | 413844008 | DOID:3393 |
| Myocardial ischemia | contraindication | 414795007 | DOID:3393 |
| Placental abruption | contraindication | 415105001 | |
| Denuded skin | contraindication | 418242004 |
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 9.48 | acidic |
| pKa2 | 11.49 | acidic |
| pKa3 | 12.74 | acidic |
| pKa4 | 8.66 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Beta-2 adrenergic receptor | GPCR | AGONIST | Ki | 5.60 | WOMBAT-PK | CHEMBL | |||
| Beta-2 adrenergic receptor | GPCR | Kd | 5.40 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4019941 | VUID |
| N0000148026 | NUI |
| D00688 | KEGG_DRUG |
| 23031-32-5 | SECONDARY_CAS_RN |
| 4018396 | VANDF |
| 4019941 | VANDF |
| C0039542 | UMLSCUI |
| CHEBI:9449 | CHEBI |
| CHEMBL1760 | ChEMBL_ID |
| DB00871 | DRUGBANK_ID |
| CHEMBL1315867 | ChEMBL_ID |
| CHEMBL1160544 | ChEMBL_ID |
| D013726 | MESH_DESCRIPTOR_UI |
| 5403 | PUBCHEM_CID |
| 2616 | INN_ID |
| 560 | IUPHAR_LIGAND_ID |
| N8ONU3L3PG | UNII |
| 10368 | RXNORM |
| 41721 | MMSL |
| 5548 | MMSL |
| d00752 | MMSL |
| 001812 | NDDF |
| 004731 | NDDF |
| 24583009 | SNOMEDCT_US |
| 372745006 | SNOMEDCT_US |
| 45311002 | SNOMEDCT_US |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| TERBUTALINE SULFATE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0115-2611 | TABLET | 2.50 mg | ORAL | ANDA | 23 sections |
| TERBUTALINE SULFATE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0115-2622 | TABLET | 5 mg | ORAL | ANDA | 23 sections |
| Terbutaline Sulfate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0143-9375 | INJECTION | 1 mg | SUBCUTANEOUS | ANDA | 22 sections |
| Terbutaline Sulfate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0143-9746 | INJECTION | 1 mg | SUBCUTANEOUS | ANDA | 22 sections |
| Terbutaline Sulfate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0404-9962 | INJECTION, SOLUTION | 1 mg | SUBCUTANEOUS | ANDA | 11 sections |
| Terbutaline Sulfate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0527-1311 | TABLET | 5 mg | ORAL | ANDA | 23 sections |
| Terbutaline Sulfate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0527-1318 | TABLET | 2.50 mg | ORAL | ANDA | 23 sections |
| Terbutaline Sulfate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10135-579 | TABLET | 2.50 mg | ORAL | ANDA | 23 sections |
| Terbutaline Sulfate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10135-580 | TABLET | 5 mg | ORAL | ANDA | 23 sections |
| Terbutaline Sulfate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10271-101 | INJECTION | 1 mg | SUBCUTANEOUS | ANDA | 23 sections |
| Terbutaline Sulfate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 17478-933 | INJECTION | 1 mg | SUBCUTANEOUS | ANDA | 23 sections |
| Terbutaline Sulfate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 21695-121 | TABLET | 5 mg | ORAL | ANDA | 23 sections |
| Terbutaline Sulfate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 21695-122 | TABLET | 2.50 mg | ORAL | ANDA | 23 sections |
| Terbutaline Sulfate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 24979-132 | TABLET | 2.50 mg | ORAL | ANDA | 23 sections |
| Terbutaline Sulfate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 24979-133 | TABLET | 5 mg | ORAL | ANDA | 23 sections |
| Terbutaline Sulfate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 52584-665 | INJECTION, SOLUTION | 1 mg | SUBCUTANEOUS | ANDA | 11 sections |
| Terbutaline Sulfate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 53808-0312 | TABLET | 2.50 mg | ORAL | ANDA | 22 sections |
| Terbutaline Sulfate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 62559-721 | TABLET | 2.50 mg | ORAL | NDA authorized generic | 22 sections |
| Terbutaline Sulfate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 62559-722 | TABLET | 5 mg | ORAL | NDA authorized generic | 22 sections |
| Terbutaline Sulfate | Human Prescription Drug Label | 1 | 63323-665 | INJECTION, SOLUTION | 1 mg | SUBCUTANEOUS | ANDA | 13 sections |
| Terbutaline Sulfate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 67296-1053 | TABLET | 2.50 mg | ORAL | ANDA | 13 sections |
| Terbutaline Sulfate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 71205-938 | TABLET | 2.50 mg | ORAL | ANDA | 23 sections |
| Terbutaline Sulfate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 71205-939 | TABLET | 5 mg | ORAL | ANDA | 23 sections |
| Terbutaline Sulfate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 71872-7080 | INJECTION | 1 mg | SUBCUTANEOUS | ANDA | 22 sections |
| Terbutaline Sulfate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 71872-7130 | INJECTION, SOLUTION | 1 mg | SUBCUTANEOUS | ANDA | 24 sections |
| Terbutaline Sulfate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72843-101 | INJECTION | 1 mg | SUBCUTANEOUS | ANDA | 23 sections |