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acrivastine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| antihistaminics | 82 | 87848-99-5 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
a second generation antihistamine
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 24 | mg | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 3 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 0.70 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 67 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 1.31 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 18 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| fu (Fraction unbound in plasma) | 0.16 % | Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2A,ACVR2B,AURKA,AXL,BRAF,BTK,CAMK2D,CDK5,CDK9,DYRK1B,EGFR,EIF2AK3,ERBB2,GRK2,IKBKB,ITK,MAP2K6,MAPK10,MAPK7,MAPKAPK2,PDK1,PDK2,PDK4,PIK3CB,PRKDC,STK33,SYK,TEK,TGFBR1 | 29 | |||
| kinase-selectivity-class | ACVR2B,AXL,BRAF,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,GRK2,MAP2K6,MAPK7,SIK2,STK33,TEK,TGFBR1,TTK,ZAP70 | 18 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| March 25, 1994 | FDA | AUXILIUM PHARMS INC |
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-chronic obstructive pulmonary disease overlap syndrome | 361.92 | 35.25 | 75 | 4069 | 4824 | 90619479 |
| Total lung capacity increased | 360.08 | 35.25 | 75 | 4069 | 4946 | 90619357 |
| Hypomania | 338.40 | 35.25 | 79 | 4065 | 8818 | 90615485 |
| Jaundice cholestatic | 328.88 | 35.25 | 79 | 4065 | 9964 | 90614339 |
| Sarcoidosis | 303.78 | 35.25 | 75 | 4069 | 10598 | 90613705 |
| Nasal polyps | 302.35 | 35.25 | 75 | 4069 | 10805 | 90613498 |
| Schizophrenia | 297.86 | 35.25 | 79 | 4065 | 14835 | 90609468 |
| Rhinitis allergic | 274.70 | 35.25 | 76 | 4068 | 16709 | 90607594 |
| Cardiac murmur | 264.11 | 35.25 | 75 | 4069 | 18119 | 90606184 |
| Bronchiectasis | 248.94 | 35.25 | 75 | 4069 | 22255 | 90602048 |
| Psychotic disorder | 244.24 | 35.25 | 80 | 4064 | 31150 | 90593153 |
| Blood bilirubin increased | 222.05 | 35.25 | 81 | 4063 | 43389 | 90580914 |
| Lung neoplasm malignant | 217.63 | 35.25 | 69 | 4075 | 24204 | 90600099 |
| Hepatotoxicity | 210.53 | 35.25 | 79 | 4065 | 45763 | 90578540 |
| Cholelithiasis | 200.11 | 35.25 | 79 | 4065 | 52427 | 90571876 |
| Chronic obstructive pulmonary disease | 177.32 | 35.25 | 80 | 4064 | 73749 | 90550554 |
| Gastrooesophageal reflux disease | 107.11 | 35.25 | 76 | 4068 | 166261 | 90458042 |
| Wheezing | 85.05 | 35.25 | 77 | 4067 | 238003 | 90386300 |
| Hepatic enzyme increased | 74.77 | 35.25 | 87 | 4057 | 360649 | 90263654 |
| Oedema peripheral | 72.32 | 35.25 | 73 | 4071 | 257842 | 90366461 |
| Condition aggravated | 70.23 | 35.25 | 109 | 4035 | 595436 | 90028867 |
| Pneumonia | 54.23 | 35.25 | 101 | 4043 | 637958 | 89986345 |
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 |
|---|---|---|---|---|---|---|
| Spleen congestion | 43.28 | 37.40 | 7 | 632 | 350 | 42620346 |
| Pharyngeal paraesthesia | 43.06 | 37.40 | 8 | 631 | 901 | 42619795 |
FDA Adverse Event Reporting System (Geriatric)
| 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 |
|---|---|---|---|---|---|---|
| Total lung capacity increased | 369.19 | 30.58 | 76 | 4674 | 5036 | 110579513 |
| Asthma-chronic obstructive pulmonary disease overlap syndrome | 352.83 | 30.58 | 76 | 4674 | 6268 | 110578281 |
| Hypomania | 337.62 | 30.58 | 80 | 4670 | 10130 | 110574419 |
| Jaundice cholestatic | 309.15 | 30.58 | 80 | 4670 | 14528 | 110570021 |
| Sarcoidosis | 301.07 | 30.58 | 76 | 4674 | 12503 | 110572046 |
| Nasal polyps | 297.43 | 30.58 | 76 | 4674 | 13124 | 110571425 |
| Rhinitis allergic | 279.01 | 30.58 | 77 | 4673 | 17845 | 110566704 |
| Schizophrenia | 277.33 | 30.58 | 80 | 4670 | 21746 | 110562803 |
| Cardiac murmur | 250.52 | 30.58 | 76 | 4674 | 24552 | 110559997 |
| Bronchiectasis | 221.13 | 30.58 | 76 | 4674 | 36417 | 110548132 |
| Psychotic disorder | 214.38 | 30.58 | 81 | 4669 | 50856 | 110533693 |
| Lung neoplasm malignant | 203.16 | 30.58 | 70 | 4680 | 33772 | 110550777 |
| Hepatotoxicity | 193.78 | 30.58 | 80 | 4670 | 63320 | 110521229 |
| Cholelithiasis | 193.75 | 30.58 | 80 | 4670 | 63342 | 110521207 |
| Blood bilirubin increased | 186.29 | 30.58 | 82 | 4668 | 75890 | 110508659 |
| Chronic obstructive pulmonary disease | 155.10 | 30.58 | 81 | 4669 | 109077 | 110475472 |
| Gastrooesophageal reflux disease | 112.89 | 30.58 | 79 | 4671 | 179897 | 110404652 |
| Hepatic enzyme increased | 89.51 | 30.58 | 88 | 4662 | 320804 | 110263745 |
| Wheezing | 88.48 | 30.58 | 79 | 4671 | 255151 | 110329398 |
| Oedema peripheral | 63.09 | 30.58 | 74 | 4676 | 328586 | 110255963 |
| Condition aggravated | 54.57 | 30.58 | 106 | 4644 | 734730 | 109849819 |
| Pharyngeal paraesthesia | 43.02 | 30.58 | 13 | 4737 | 4119 | 110580430 |
| Pneumonia | 40.81 | 30.58 | 105 | 4645 | 876609 | 109707940 |
| Nausea | 38.36 | 30.58 | 128 | 4622 | 1235562 | 109348987 |
| Salpingo-oophorectomy bilateral | 36.63 | 30.58 | 7 | 4743 | 314 | 110584235 |
| Bone density abnormal | 35.20 | 30.58 | 11 | 4739 | 3892 | 110580657 |
| Spleen congestion | 33.55 | 30.58 | 7 | 4743 | 492 | 110584057 |
| Blood immunoglobulin E | 33.38 | 30.58 | 5 | 4745 | 49 | 110584500 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | R06AX18 | RESPIRATORY SYSTEM ANTIHISTAMINES FOR SYSTEMIC USE ANTIHISTAMINES FOR SYSTEMIC USE Other antihistamines for systemic use |
| FDA MoA | N0000000190 | Histamine H1 Receptor Antagonists |
| MeSH PA | D006633 | Histamine Antagonists |
| MeSH PA | D006634 | Histamine H1 Antagonists |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D018494 | Histamine Agents |
| MeSH PA | D039563 | Histamine H1 Antagonists, Non-Sedating |
| FDA EPC | N0000175587 | Histamine-1 Receptor Antagonist |
| CHEBI has role | CHEBI:37955 | H<small><sub>1</sub></small>-receptor antagonist |
Related Drugs by ATC class:
R06AX Other antihistamines for systemic use 26 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Vasomotor rhinitis | indication | 8229003 | DOID:4730 |
| Allergic rhinitis | indication | 61582004 | |
| Nasal discharge | indication | 64531003 | |
| Nasal congestion | indication | 68235000 | |
| Sneezing | indication | 76067001 | |
| Common cold | indication | 82272006 | DOID:10459 |
| Seasonal allergic rhinitis | indication | 367498001 | |
| Allergic conjunctivitis | indication | 473460002 | DOID:11204 |
| Hyperthyroidism | contraindication | 34486009 | DOID:7998 |
| Hypertensive disorder | contraindication | 38341003 | DOID:10763 |
| Coronary arteriosclerosis | contraindication | 53741008 | DOID:3393 |
| Diabetes mellitus | contraindication | 73211009 | DOID:9351 |
| Benign prostatic hyperplasia | contraindication | 266569009 | |
| Retention of urine | contraindication | 267064002 | |
| Angle-closure glaucoma | contraindication | 392291006 | DOID:13550 |
| Hypertensive urgency | contraindication | 443482000 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 3.78 | acidic |
| pKa2 | 9.42 | Basic |
| pKa3 | 1.55 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Histamine H1 receptor | GPCR | ANTAGONIST | IC50 | 7.16 | WOMBAT-PK | CHEMBL | |||
| Multidrug resistance protein 1 | Transporter | WOMBAT-PK | |||||||
| Histamine H1 receptor | GPCR | IC50 | 5.21 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4020857 | VUID |
| N0000179060 | NUI |
| D02760 | KEGG_DRUG |
| 19959 | RXNORM |
| C0054340 | UMLSCUI |
| CHEBI:83168 | CHEBI |
| CHEMBL1224 | ChEMBL_ID |
| DB09488 | DRUGBANK_ID |
| C043648 | MESH_SUPPLEMENTAL_RECORD_UI |
| 5284514 | PUBCHEM_CID |
| 5548 | INN_ID |
| A20F9XAI7W | UNII |
| 4130 | MMSL |
| d03753 | MMSL |
| 4020857 | VANDF |
| 003921 | NDDF |
| 320813002 | SNOMEDCT_US |
| 391716003 | SNOMEDCT_US |
| A20F9XAI7W | INXIGHT DRUGS |
Pharmaceutical products:
None