pheniramine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 2132 | 86-21-5 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
One of the HISTAMINE H1 ANTAGONISTS with little sedative action. It is used in treatment of hay fever, rhinitis, allergic dermatoses, and pruritus.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 75 | mg | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BA (Bioavailability) | 99 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| S (Water solubility) | 100 mg/mL | Bocci G, Oprea TI, Benet LZ |
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Bocci G, Oprea TI, Benet LZ |
| fu (Fraction unbound in plasma) | 0.37 % | Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| June 8, 1994 | FDA | ALCON |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
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 |
|---|---|---|---|---|---|---|
| Febrile neutropenia | 53.49 | 32.41 | 28 | 543 | 230971 | 79512846 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | D04AA16 | DERMATOLOGICALS ANTIPRURITICS, INCL. ANTIHISTAMINES, ANESTHETICS, ETC. ANTIPRURITICS, INCL. ANTIHISTAMINES, ANESTHETICS, ETC. Antihistamines for topical use |
| ATC | R06AB05 | RESPIRATORY SYSTEM ANTIHISTAMINES FOR SYSTEMIC USE ANTIHISTAMINES FOR SYSTEMIC USE Substituted alkylamines |
| MeSH PA | D018926 | Anti-Allergic Agents |
| MeSH PA | D000982 | Antipruritics |
| MeSH PA | D003879 | Dermatologic Agents |
| MeSH PA | D018494 | Histamine Agents |
| MeSH PA | D006633 | Histamine Antagonists |
| MeSH PA | D006634 | Histamine H1 Antagonists |
| MeSH PA | D018377 | Neurotransmitter Agents |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Sinus headache | indication | 4969004 | |
| Dermatographic urticaria | indication | 7632005 | DOID:743 |
| Vasomotor rhinitis | indication | 8229003 | DOID:4730 |
| Cough | indication | 49727002 | |
| Allergic rhinitis | indication | 61582004 | |
| Nasal discharge | indication | 64531003 | |
| Nasal congestion | indication | 68235000 | |
| Red eye | indication | 75705005 | |
| Sneezing | indication | 76067001 | |
| Common cold | indication | 82272006 | DOID:10459 |
| Urticaria | indication | 126485001 | |
| Headache disorder | indication | 230461009 | |
| Sore throat symptom | indication | 267102003 | |
| Influenza-like symptoms | indication | 315642008 | |
| Seasonal allergic rhinitis | indication | 367498001 | |
| Fever | indication | 386661006 | |
| Itching of skin | indication | 418363000 | |
| Allergic conjunctivitis | indication | 473460002 | DOID:11204 |
| Anaphylaxis Adjunct | indication | ||
| Ocular Itching | indication | ||
| Brain damage | contraindication | 2470005 | |
| Necrotizing enterocolitis in fetus OR newborn | contraindication | 2707005 | |
| Goiter | contraindication | 3716002 | DOID:12176 |
| Ocular hypertension | contraindication | 4210003 | DOID:9282 |
| Gastritis | contraindication | 4556007 | DOID:4029 |
| Hypophosphatemia | contraindication | 4996001 | |
| Tachyarrhythmia | contraindication | 6285003 | |
| Suicidal thoughts | contraindication | 6471006 | |
| Dependent drug abuse | contraindication | 6525002 | |
| Urinary tract obstruction | contraindication | 7163005 | DOID:5200 |
| Alcoholism | contraindication | 7200002 | |
| Alcohol withdrawal delirium | contraindication | 8635005 | |
| Peptic ulcer | contraindication | 13200003 | DOID:750 |
| Chronic obstructive lung disease | contraindication | 13645005 | DOID:3083 |
| Asthenia | contraindication | 13791008 | |
| Hyperkalemia | contraindication | 14140009 | |
| Severe chronic ulcerative colitis | contraindication | 14311001 | |
| Constipation | contraindication | 14760008 | DOID:2089 |
| Disorder of autonomic nervous system | contraindication | 15241006 | |
| Chronic disease of respiratory system | contraindication | 17097001 | |
| Mood swings | contraindication | 18963009 | |
| Hashimoto thyroiditis | contraindication | 21983002 | |
| Myocardial infarction | contraindication | 22298006 | DOID:5844 |
| Glaucoma | contraindication | 23986001 | DOID:1686 |
| Inflammatory bowel disease | contraindication | 24526004 | DOID:0050589 |
| Ventricular tachycardia | contraindication | 25569003 | |
| Acute tuberculosis | contraindication | 25629007 | |
| Alcohol intoxication | contraindication | 25702006 | |
| Shock | contraindication | 27942005 | |
| Toxic megacolon | contraindication | 28536002 | DOID:1770 |
| Atony of colon | contraindication | 29479008 | |
| Hypercapnia | contraindication | 29596007 | |
| Bronchitis | contraindication | 32398004 | DOID:6132 |
| Dehydration | contraindication | 34095006 | |
| Hyperthyroidism | contraindication | 34486009 | DOID:7998 |
| Acute hepatitis | contraindication | 37871000 | |
| Hypertensive disorder | contraindication | 38341003 | DOID:10763 |
| Hypovolemic shock | contraindication | 39419009 | |
| Disorder of gallbladder | contraindication | 39621005 | DOID:0060262 |
| Gastrointestinal ulcer | contraindication | 40845000 | |
| Hypothyroidism | contraindication | 40930008 | DOID:1459 |
| Complete trisomy 21 syndrome | contraindication | 41040004 | DOID:14250 |
| Body fluid retention | contraindication | 43498006 | |
| Conduction disorder of the heart | contraindication | 44808001 | |
| Low blood pressure | contraindication | 45007003 | |
| Achalasia of esophagus | contraindication | 45564002 | DOID:9164 |
| Chronic heart failure | contraindication | 48447003 | |
| Bradycardia | contraindication | 48867003 | |
| Disorder of cardiovascular system | contraindication | 49601007 | DOID:1287 |
| Acidosis | contraindication | 51387008 | |
| Gastrointestinal perforation | contraindication | 51875005 | |
| Vitamin K deficiency | contraindication | 52675005 | DOID:11249 |
| Nasal polyp | contraindication | 52756005 | |
| Coronary arteriosclerosis | contraindication | 53741008 | DOID:3393 |
| Paralytic ileus | contraindication | 55525008 | DOID:8442 |
| Heart disease | contraindication | 56265001 | DOID:114 |
| Peptic reflux disease | contraindication | 57643001 | |
| Acute nephropathy | contraindication | 58574008 | |
| Hepatic failure | contraindication | 59927004 | |
| Ulcerative colitis | contraindication | 64766004 | DOID:8577 |
| Blood coagulation disorder | contraindication | 64779008 | DOID:1247 |
| Arterial thrombosis | contraindication | 65198009 | |
| Drug AND/OR toxin-induced diarrhea | contraindication | 65979008 | |
| Substance abuse | contraindication | 66214007 | |
| Benign intracranial hypertension | contraindication | 68267002 | DOID:11459 |
| Psychotic disorder | contraindication | 69322001 | |
| Poisoning by acetaminophen | contraindication | 70273001 | |
| Agoraphobia | contraindication | 70691001 | DOID:593 |
| Arteriosclerotic vascular disease | contraindication | 72092001 | |
| Diabetes mellitus | contraindication | 73211009 | DOID:9351 |
| Factor II deficiency | contraindication | 73975000 | |
| Reye's syndrome | contraindication | 74351001 | DOID:14525 |
| Gastrointestinal hemorrhage | contraindication | 74474003 | |
| Urethral stricture | contraindication | 76618002 | |
| Thrombotic thrombocytopenic purpura | contraindication | 78129009 | DOID:10772 |
| Spastic paralysis | contraindication | 78403003 | |
| Disturbance of salivary secretion | contraindication | 78948009 | |
| Hyperglycemia | contraindication | 80394007 | DOID:4195 |
| Decreased respiratory function | contraindication | 80954004 | |
| Injury of head | contraindication | 82271004 | |
| Chronic idiopathic constipation | contraindication | 82934008 | |
| Cor pulmonale | contraindication | 83291003 | DOID:8515 |
| Hiatal hernia | contraindication | 84089009 | DOID:12642 |
| Epilepsy | contraindication | 84757009 | DOID:1826 |
| Pulmonary emphysema | contraindication | 87433001 | |
| Gout | contraindication | 90560007 | DOID:13189 |
| Kidney disease | contraindication | 90708001 | DOID:557 |
| Thyrotoxicosis | contraindication | 90739004 | DOID:7997 |
| Hemophilia | contraindication | 90935002 | |
| Myasthenia gravis | contraindication | 91637004 | DOID:437 |
| Dermatitis herpetiformis | contraindication | 111196000 | DOID:8505 |
| Anemia due to enzyme deficiency | contraindication | 111577008 | |
| Acute abdominal pain | contraindication | 116290004 | |
| Procedure on urinary system | contraindication | 118677009 | |
| Gastrointestinal obstruction | contraindication | 126765001 | |
| Neoplasm of brain | contraindication | 126952004 | DOID:1319 |
| von Willebrand disorder | contraindication | 128105004 | DOID:12531 |
| Eye infection | contraindication | 128351009 | |
| Seizure disorder | contraindication | 128613002 | |
| Autonomic dysreflexia | contraindication | 129618003 | |
| Bleeding | contraindication | 131148009 | |
| Liver function tests abnormal | contraindication | 166603001 | |
| Drug-induced psychosis | contraindication | 191483003 | DOID:1742 |
| Obsessive-compulsive disorder | contraindication | 191736004 | DOID:10933 |
| Insomnia | contraindication | 193462001 | |
| Partial atrioventricular block | contraindication | 195039008 | |
| Acute pancreatitis | contraindication | 197456007 | DOID:2913 |
| Impaired renal function disorder | contraindication | 197663003 | |
| Coronary artery bypass graft | contraindication | 232717009 | |
| Myocardial dysfunction | contraindication | 233928007 | |
| Arterial hemorrhage | contraindication | 234003006 | |
| Gastroesophageal reflux disease | contraindication | 235595009 | DOID:8534 |
| Disease of liver | contraindication | 235856003 | DOID:409 |
| Bladder outflow obstruction | contraindication | 236645006 | |
| Morbid obesity | contraindication | 238136002 | DOID:11981 |
| Hypocomplementemic urticarial vasculitis | contraindication | 239945009 | |
| Pyloric obstruction | contraindication | 244815007 | |
| Benign prostatic hyperplasia | contraindication | 266569009 | |
| Retention of urine | contraindication | 267064002 | |
| Anemia | contraindication | 271737000 | DOID:2355 |
| Drowsy | contraindication | 271782001 | |
| Exacerbation of asthma | contraindication | 281239006 | |
| Injury of eye region | contraindication | 282752000 | |
| Pregnancy, function | contraindication | 289908002 | |
| Lesion of brain | contraindication | 301766008 | |
| Thrombocytopenic disorder | contraindication | 302215000 | DOID:1588 |
| Panic disorder | contraindication | 371631005 | DOID:594 |
| Coma | contraindication | 371632003 | |
| Primary adrenocortical insufficiency | contraindication | 373662000 | |
| Operation on gastrointestinal tract | contraindication | 386621005 | |
| Hypoxia | contraindication | 389086002 | |
| Angle-closure glaucoma | contraindication | 392291006 | DOID:13550 |
| Acute coronary syndrome | contraindication | 394659003 | |
| Cardiovascular event risk | contraindication | 395112001 | |
| Pseudomembranous enterocolitis | contraindication | 397683000 | |
| Gastric ulcer | contraindication | 397825006 | DOID:10808 |
| Breastfeeding (mother) | contraindication | 413712001 | |
| Chronic lung disease | contraindication | 413839001 | |
| Chronic myocardial ischemia | contraindication | 413844008 | DOID:3393 |
| Disorder of coronary artery | contraindication | 414024009 | |
| Myocardial ischemia | contraindication | 414795007 | DOID:3393 |
| Myocardial infarction in recovery phase | contraindication | 418044006 | |
| Central nervous system depression | contraindication | 418072004 | |
| Ultrarapid metabolizer due to cytochrome p450 CYP2D6 variant | contraindication | 422681000 | |
| Fever greater than 100.4 Fahrenheit | contraindication | 426000000 | |
| Dysfunction of sphincter of Oddi | contraindication | 430887001 | |
| Hypertensive urgency | contraindication | 443482000 | |
| Acute erosive gastritis | contraindication | 444926003 | |
| Smokes tobacco daily | contraindication | 449868002 | |
| Acute exacerbation of asthma | contraindication | 708038006 | |
| Acute Thromboembolic Stroke | contraindication |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 9.47 | Basic |
| pKa2 | 4.14 | 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 | CHEMBL | CHEMBL | |||||
| Histamine H4 receptor | GPCR | Ki | 5.38 | PDSP | |||||
| Sodium channel alpha subunits; brain (Types I, II, III) | Ion channel | IC50 | 4.48 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4019888 | VUID |
| N0000147973 | NUI |
| D01174 | KEGG_DRUG |
| 132-20-7 | SECONDARY_CAS_RN |
| 4018472 | VANDF |
| 4019888 | VANDF |
| CHEBI:91591 | CHEBI |
| CHEMBL1193 | ChEMBL_ID |
| CHEMBL1653 | ChEMBL_ID |
| 7267 | IUPHAR_LIGAND_ID |
| DB01620 | DRUGBANK_ID |
| 266959 | RXNORM |
| 5271 | MMSL |
| 5666 | MMSL |
| d03086 | MMSL |
| 003388 | NDDF |
| 004794 | NDDF |
| 116546005 | SNOMEDCT_US |
| 373500002 | SNOMEDCT_US |
| 49953001 | SNOMEDCT_US |
| C0031408 | UMLSCUI |
| D010632 | MESH_DESCRIPTOR_UI |
| 105 | INN_ID |
| 4761 | PUBCHEM_CID |
| 134FM9ZZ6M | UNII |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Naphcon A | HUMAN OTC DRUG LABEL | 2 | 0065-0085 | SOLUTION/ DROPS | 3 mg | OPHTHALMIC | NDA | 14 sections |
| Naphcon A | HUMAN OTC DRUG LABEL | 2 | 0065-0085 | SOLUTION/ DROPS | 3 mg | OPHTHALMIC | NDA | 14 sections |
| Naphcon A | HUMAN OTC DRUG LABEL | 2 | 0065-0085 | SOLUTION/ DROPS | 3 mg | OPHTHALMIC | NDA | 14 sections |
| TheraFlu Cold and Flu | HUMAN OTC DRUG LABEL | 3 | 0067-0924 | POWDER | 20 mg | ORAL | Export only | 10 sections |
| TherafluFlu and Sore Throat | HUMAN OTC DRUG LABEL | 3 | 0067-7916 | POWDER, FOR SOLUTION | 20 mg | ORAL | OTC monograph final | 17 sections |
| THERAFLUSINUS AND PAIN | HUMAN OTC DRUG LABEL | 3 | 0067-7920 | POWDER, FOR SOLUTION | 20 mg | ORAL | OTC monograph final | 17 sections |
| THERAFLUSINUS AND PAIN | HUMAN OTC DRUG LABEL | 3 | 0067-7920 | POWDER, FOR SOLUTION | 20 mg | ORAL | OTC monograph final | 17 sections |
| TheraFlu Cold and Flu | HUMAN OTC DRUG LABEL | 3 | 0067-8135 | POWDER | 20 mg | ORAL | Export only | 15 sections |
| TheraFlu Cold and Flu | HUMAN OTC DRUG LABEL | 3 | 0067-8135 | POWDER | 20 mg | ORAL | Export only | 15 sections |
| Eye Allergy Relief | HUMAN OTC DRUG LABEL | 2 | 0363-0430 | SOLUTION/ DROPS | 3.15 mg | OPHTHALMIC | NDA | 14 sections |
| Eye Allergy Relief | HUMAN OTC DRUG LABEL | 2 | 0363-0430 | SOLUTION/ DROPS | 3.15 mg | OPHTHALMIC | NDA | 14 sections |
| Walgreens Wal-Flu Cold and Sore ThroatLemon Flavor | HUMAN OTC DRUG LABEL | 3 | 0363-0601 | GRANULE, FOR SOLUTION | 20 mg | ORAL | OTC monograph final | 14 sections |
| Scot-Tussin Original SF Multi-Symptom | HUMAN OTC DRUG LABEL | 3 | 0372-0004 | LIQUID | 4 mg | ORAL | OTC MONOGRAPH FINAL | 14 sections |
| Eye Allergy Relief | HUMAN OTC DRUG LABEL | 2 | 11673-430 | SOLUTION/ DROPS | 3.15 mg | OPHTHALMIC | NDA | 14 sections |
| Eye Allergy Relief | HUMAN OTC DRUG LABEL | 2 | 11673-430 | SOLUTION/ DROPS | 3.15 mg | OPHTHALMIC | NDA | 14 sections |
| Eye Allergy Relief | HUMAN OTC DRUG LABEL | 2 | 11822-0552 | SOLUTION/ DROPS | 3.15 mg | OPHTHALMIC | NDA | 14 sections |
| Scot-Tussin Original Multi-Symptom Cold and Allergy Relief | HUMAN OTC DRUG LABEL | 3 | 15187-004 | LIQUID | 4 mg | ORAL | OTC MONOGRAPH FINAL | 15 sections |
| Naphazoline Hydrochloride and Pheniramine Maleate | HUMAN OTC DRUG LABEL | 2 | 17478-065 | SOLUTION/ DROPS | 3 mg | OPHTHALMIC | ANDA | 15 sections |
| Opcon-A | HUMAN OTC DRUG LABEL | 2 | 24208-430 | SOLUTION/ DROPS | 3.15 mg | OPHTHALMIC | NDA | 14 sections |
| Opcon-A | HUMAN OTC DRUG LABEL | 2 | 24208-430 | SOLUTION/ DROPS | 3.15 mg | OPHTHALMIC | NDA | 14 sections |
| Topcare Cold and Sore ThroatLemon Flavor | HUMAN OTC DRUG LABEL | 3 | 36800-802 | GRANULE, FOR SOLUTION | 20 mg | ORAL | OTC monograph final | 14 sections |
| Eye Allergy Relief | HUMAN OTC DRUG LABEL | 2 | 49035-430 | SOLUTION/ DROPS | 3.15 mg | OPHTHALMIC | NDA | 14 sections |
| Equate Eye Allergy Relief Drops | HUMAN OTC DRUG LABEL | 2 | 49035-874 | SOLUTION/ DROPS | 3.15 mg | OPHTHALMIC | ANDA | 15 sections |
| Naphcon A | HUMAN OTC DRUG LABEL | 2 | 50090-0185 | SOLUTION/ DROPS | 3 mg | OPHTHALMIC | NDA | 15 sections |
| Naphcon A | HUMAN OTC DRUG LABEL | 2 | 50090-0185 | SOLUTION/ DROPS | 3 mg | OPHTHALMIC | NDA | 15 sections |
| ALAHIST DM | HUMAN OTC DRUG LABEL | 3 | 50991-444 | LIQUID | 12.50 mg | ORAL | OTC monograph final | 16 sections |
| Alahist D | HUMAN OTC DRUG LABEL | 2 | 50991-776 | TABLET | 17.50 mg | ORAL | OTC monograph final | 10 sections |
| Alahist D | HUMAN OTC DRUG LABEL | 2 | 50991-776 | TABLET | 17.50 mg | ORAL | OTC monograph final | 10 sections |
| NAPHCON A | HUMAN OTC DRUG LABEL | 2 | 52959-107 | SOLUTION/ DROPS | 3 mg | OPHTHALMIC | NDA | 11 sections |
| Eye Allergy Relief | HUMAN OTC DRUG LABEL | 2 | 55910-552 | SOLUTION/ DROPS | 3.15 mg | OPHTHALMIC | NDA | 14 sections |