pramocaine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
local anaesthetics	3487	140-65-8

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: pramocaine hydrochloride pramoxine pramoxine hydrochloride pramocain pramocaine pramoxin pramoxine HCl	Molecular weight: 293.41 Formula: C17H27NO3 CLOGP: 3.96 LIPINSKI: 0 HAC: 4 HDO: 0 TPSA: 30.93 ALOGS: -3.12 ROTB: 9 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

pramocaine hydrochloride
pramoxine
pramoxine hydrochloride
pramocain
pramocaine
pramoxin
pramoxine HCl

Molecular weight: 293.41
Formula: C17H27NO3
CLOGP: 3.96
LIPINSKI: 0
HAC: 4
HDO: 0
TPSA: 30.93
ALOGS: -3.12
ROTB: 9

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

None

ADMET properties:

None

Approvals:

Date	Agency	Company	Orphan
Aug. 13, 1976	FDA	SEBELA IRELAND LTD

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
Macular degeneration	749.85	16.83	224	7535	24152	63457111
Chronic sinusitis	284.63	16.83	92	7667	12751	63468512
Procedural pain	199.48	16.83	81	7678	21488	63459775
Paraesthesia oral	197.79	16.83	78	7681	19178	63462085
Female genital tract fistula	142.69	16.83	48	7711	7511	63473752
Vaginal flatulence	112.89	16.83	33	7726	3260	63478003
Proctitis	100.51	16.83	34	7725	5407	63475856
Dyspepsia	92.77	16.83	86	7673	102110	63379153
Therapeutic product effect incomplete	88.81	16.83	92	7667	124964	63356299
Vaginal discharge	83.11	16.83	34	7725	9164	63472099
Radiculopathy	81.82	16.83	33	7726	8578	63472685
Drug ineffective	71.52	16.83	283	7476	1044482	62436781
Frequent bowel movements	63.81	16.83	38	7721	22984	63458279
Oral candidiasis	61.55	16.83	37	7722	22761	63458502
Colitis ulcerative	59.43	16.83	38	7721	26053	63455210
Infusion related reaction	49.50	16.83	99	7660	245422	63235841
Rectal haemorrhage	47.82	16.83	43	7716	48987	63432276
Urticaria thermal	47.62	16.83	11	7748	428	63480835
Salpingo-oophorectomy unilateral	44.68	16.83	12	7747	869	63480394
Haematochezia	44.59	16.83	43	7716	53501	63427762
Sinusitis fungal	44.14	16.83	14	7745	1817	63479446
Sputum increased	40.09	16.83	14	7745	2445	63478818
Colitis	38.58	16.83	38	7721	48490	63432773
Administration site erythema	36.83	16.83	10	7749	755	63480508
Embolism venous	36.69	16.83	14	7745	3140	63478123
Respiratory symptom	35.88	16.83	14	7745	3333	63477930
Weight decreased	35.11	16.83	93	7666	276705	63204558
Nasal polyps	30.93	16.83	15	7744	6024	63475239
Pyrexia	30.66	16.83	126	7633	470352	63010911
Diastolic dysfunction	29.95	16.83	15	7744	6456	63474807
Hypercholesterolaemia	29.71	16.83	23	7736	21311	63459952
Nail bed tenderness	27.65	16.83	7	7752	402	63480861
Erythema	27.47	16.83	64	7695	175687	63305576
Pigmentation disorder	25.20	16.83	12	7747	4627	63476636
Scratch	24.02	16.83	13	7746	6552	63474711
Vitamin B12 deficiency	23.68	16.83	12	7747	5291	63475972
Emphysema	22.62	16.83	15	7744	10923	63470340
Skin plaque	21.15	16.83	13	7746	8307	63472956
Secretion discharge	21.10	16.83	15	7744	12216	63469047
Fungal infection	20.67	16.83	24	7735	36850	63444413
Autonomic neuropathy	20.45	16.83	7	7752	1152	63480111
Dizziness postural	19.97	16.83	12	7747	7364	63473899
Hysterectomy	19.58	16.83	13	7746	9486	63471777
Diverticulum	19.07	16.83	14	7745	11977	63469286
Jarisch-Herxheimer reaction	18.48	16.83	5	7754	372	63480891
Osteoarthritis	17.45	16.83	37	7722	95306	63385957

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
Anal inflammation	85.99	19.67	20	2690	1280	34952941
SARS-CoV-2 test negative	74.43	19.67	17	2693	1003	34953218
Accident	59.15	19.67	20	2690	5027	34949194
Proctalgia	56.68	19.67	20	2690	5703	34948518
Haemorrhoids	53.65	19.67	25	2685	14550	34939671
Body temperature increased	38.11	19.67	21	2689	17347	34936874
Erythema multiforme	26.24	19.67	13	2697	8636	34945585
Pruritus	25.43	19.67	42	2668	141939	34812282
Anticholinergic syndrome	22.96	19.67	7	2703	1262	34952959
Pyrexia	22.07	19.67	66	2644	332947	34621274

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
Chronic sinusitis	278.91	16.45	88	8417	12938	79722945
Macular degeneration	232.23	16.45	74	8431	11222	79724661
Procedural pain	194.35	16.45	78	8427	23006	79712877
Paraesthesia oral	192.75	16.45	75	8430	20396	79715487
Female genital tract fistula	155.90	16.45	47	8458	5928	79729955
Vaginal flatulence	120.59	16.45	32	8473	2543	79733340
Proctitis	95.57	16.45	33	8472	6399	79729484
Dyspepsia	94.27	16.45	84	8421	108603	79627280
Vaginal discharge	90.77	16.45	33	8472	7430	79728453
Radiculopathy	81.84	16.45	32	8473	8792	79727091
Therapeutic product effect incomplete	80.73	16.45	87	8418	141558	79594325
Anal inflammation	72.85	16.45	19	8486	1411	79734472
Frequent bowel movements	59.84	16.45	38	8467	29501	79706382
SARS-CoV-2 test negative	59.29	16.45	16	8489	1355	79734528
Oral candidiasis	54.81	16.45	36	8469	29592	79706291
Colitis ulcerative	54.23	16.45	38	8467	34704	79701179
Pyrexia	50.72	16.45	173	8332	678536	79057347
Urticaria thermal	48.96	16.45	11	8494	434	79735449
Salpingo-oophorectomy unilateral	46.95	16.45	12	8493	822	79735061
Administration site erythema	45.37	16.45	10	8495	361	79735522
Rectal haemorrhage	43.65	16.45	47	8458	76253	79659630
Proctalgia	42.67	16.45	21	8484	9980	79725903
Sinusitis fungal	42.44	16.45	14	8491	2360	79733523
Infusion related reaction	40.42	16.45	81	8424	230156	79505727
Accident	39.04	16.45	19	8486	8812	79727071
Haematochezia	38.34	16.45	47	8458	87598	79648285
Weight decreased	38.16	16.45	103	8402	355095	79380788
Embolism venous	37.99	16.45	15	8490	4224	79731659
Sputum increased	33.38	16.45	14	8491	4599	79731284
Colitis	33.18	16.45	40	8465	73267	79662616
Respiratory symptom	32.87	16.45	14	8491	4777	79731106
Haemorrhoids	30.27	16.45	25	8480	29103	79706780
Nasal polyps	30.11	16.45	15	8490	7312	79728571
Pain	29.95	16.45	151	8354	703651	79032232
Malaise	29.82	16.45	117	8388	489752	79246131
Nail bed tenderness	28.51	16.45	7	8498	407	79735476
Hysterectomy	26.25	16.45	13	8492	6259	79729624
Erythema	25.20	16.45	66	8439	223224	79512659
Pigmentation disorder	24.57	16.45	12	8493	5606	79730277
Scratch	22.73	16.45	13	8492	8350	79727533
Diastolic dysfunction	22.12	16.45	14	8491	10797	79725086
Vitamin B12 deficiency	21.70	16.45	12	8493	7229	79728654
Fungal infection	20.91	16.45	24	8481	41724	79694159
Pruritus	19.87	16.45	89	8416	394559	79341324
Skin plaque	19.73	16.45	13	8492	10732	79725151
Emphysema	19.08	16.45	15	8490	16285	79719598
Vulvovaginal swelling	18.68	16.45	5	8500	410	79735473
Diverticulum	18.06	16.45	14	8491	14882	79721001
Autonomic neuropathy	18.02	16.45	7	8498	1888	79733995
Secretion discharge	17.96	16.45	14	8491	15008	79720875
Chills	17.69	16.45	47	8458	160187	79575696
Completed suicide	16.74	16.45	3	8502	245764	79490119
Tricuspid valve incompetence	16.59	16.45	15	8490	19697	79716186
Dizziness postural	16.56	16.45	12	8493	11537	79724346

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	C05AD07	CARDIOVASCULAR SYSTEM VASOPROTECTIVES AGENTS FOR TREATMENT OF HEMORRHOIDS AND ANAL FISSURES FOR TOPICAL USE Local anesthetics
ATC	D04AB07	DERMATOLOGICALS ANTIPRURITICS, INCL. ANTIHISTAMINES, ANESTHETICS, ETC. ANTIPRURITICS, INCL. ANTIHISTAMINES, ANESTHETICS, ETC. Anesthetics for topical use
MeSH PA	D000777	Anesthetics
MeSH PA	D000779	Anesthetics, Local
MeSH PA	D002491	Central Nervous System Agents
MeSH PA	D002492	Central Nervous System Depressants
MeSH PA	D018373	Peripheral Nervous System Agents
MeSH PA	D018689	Sensory System Agents
CHEBI has role	CHEBI:36333	local anesthetics

Drug Use | Suggest Off label Use Form| |View source of the data|

Disease	Relation	SNOMED_ID	DOID
Otitis externa	indication	3135009
Proctitis	indication	3951002	DOID:3127
Tinea pedis	indication	6020002	DOID:12403
Wound	indication	13924000
Dry skin	indication	16386004
Burn injury	indication	48333001
Hemorrhoids	indication	70153002	DOID:9746
Rectal pain	indication	77880009
Tinea corporis	indication	84849002
Pruritus ani	indication	90446007
Eruption of skin	indication	271807003	DOID:0050486
Skin irritation	indication	367466007
Tinea cruris	indication	399029005
Allergic otitis externa	indication	405821001
Arthropod bite wound	indication	409985002
Itching of skin	indication	418363000
Itching of ear	indication	699392007
Inflammatory dermatosis	indication	703938007
Prevent Minor Bacterial Skin Infection	indication
Minor Skin Wound Pain	indication
Minor Bacterial Skin Infections	indication
Mycosis	contraindication	3218000	DOID:1564
Measles	contraindication	14189004	DOID:8622
Herpes zoster auricularis	contraindication	21954000	DOID:9210
Abscess of intestine	contraindication	24557004
Acute tuberculosis	contraindication	25629007
Hyperthyroidism	contraindication	34486009	DOID:7998
Gastrointestinal fistula	contraindication	37831005
Hypertensive disorder	contraindication	38341003	DOID:10763
Contact dermatitis	contraindication	40275004	DOID:2773
Infectious disease	contraindication	40733004
Hypothyroidism	contraindication	40930008	DOID:1459
Conduction disorder of the heart	contraindication	44808001
Skin ulcer	contraindication	46742003
Chronic heart failure	contraindication	48447003
Anxiety	contraindication	48694002
Perforation of tympanic membrane	contraindication	60442001
Osteoporosis	contraindication	64859006	DOID:11476
Psychotic disorder	contraindication	69322001
Diabetes mellitus	contraindication	73211009	DOID:9351
Third degree burn injury	contraindication	80247002
Open-angle glaucoma	contraindication	84494001	DOID:1067
Herpes simplex	contraindication	88594005	DOID:8566
Kidney disease	contraindication	90708001	DOID:557
Fissure in skin	contraindication	95321009
Open wound	contraindication	125643001
Tuberculosis of ear	contraindication	186269001
Ophthalmic herpes simplex	contraindication	186542001
Anastomosis of intestine	contraindication	235407009
Telangiectasia disorder	contraindication	247479008
Benign prostatic hyperplasia	contraindication	266569009
Diverticulitis of gastrointestinal tract	contraindication	271366000
Varicella-zoster virus infection	contraindication	309465005
Viral ear infection	contraindication	312137007
Fungal ear infection	contraindication	312148000
Adrenal cortical hypofunction	contraindication	386584007	DOID:10493
Atrophoderma	contraindication	399979006
Peripheral vascular disease	contraindication	400047006
Disorder of coronary artery	contraindication	414024009
Denuded skin	contraindication	418242004
Nervousness	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	7.65	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

Target	Class	Pharos	UniProt	Type	Activity value (-log[M])	Bioact source
Sigma non-opioid intracellular receptor 1	Membrane receptor	Q99720	SGMR1_HUMAN	Ki	7.29	DRUG MATRIX
Sodium channel alpha subunits; brain (Types I, II, III)	Ion channel	P35498 Q99250 Q9NY46	SCN1A_HUMAN SCN2A_HUMAN SCN3A_HUMAN	IC50	4.67	CHEMBL
Membrane-associated progesterone receptor component 1	Membrane receptor		PGRC1_RAT	Ki	6.20	DRUG MATRIX

External reference:

ID	Source
4018983	VUID
N0000171570	NUI
D00739	KEGG_DRUG
637-58-1	SECONDARY_CAS_RN
4018197	VANDF
4018983	VANDF
C0071810	UMLSCUI
CHEBI:8357	CHEBI
PX9	PDB_CHEM_ID
CHEMBL1198	ChEMBL_ID
CHEMBL1201171	ChEMBL_ID
DB09345	DRUGBANK_ID
C005548	MESH_SUPPLEMENTAL_RECORD_UI
4886	PUBCHEM_CID
34347	RXNORM
5341	MMSL
5342	MMSL
72272	MMSL
001359	NDDF
004571	NDDF
31872002	SNOMEDCT_US
387175007	SNOMEDCT_US
387284004	SNOMEDCT_US
235	INN_ID
068X84E056	UNII

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
PROCTOFOAMHC	HUMAN PRESCRIPTION DRUG LABEL	2	0037-6822	AEROSOL, FOAM	100 mg	TOPICAL	ANDA	22 sections
PROCTOFOAMHC	HUMAN PRESCRIPTION DRUG LABEL	2	0037-6822	AEROSOL, FOAM	100 mg	TOPICAL	ANDA	22 sections
PROCTOFOAMNS	HUMAN OTC DRUG LABEL	1	0037-6823	AEROSOL, FOAM	150 mg	RECTAL	OTC monograph final	11 sections
EPIFOAM	HUMAN PRESCRIPTION DRUG LABEL	2	0037-6824	AEROSOL, FOAM	100 mg	TOPICAL	ANDA	20 sections
Good Sense Triple Antibioticand Pain Relief	HUMAN OTC DRUG LABEL	4	0113-0679	OINTMENT	10 mg	TOPICAL	OTC monograph final	13 sections
Good Sense HemorrhoidalMaximum Strength Pain Relief	HUMAN OTC DRUG LABEL	4	0113-0944	CREAM	1 g	TOPICAL	OTC monograph final	15 sections
good sense triple antibiotic	HUMAN OTC DRUG LABEL	4	0113-1140	OINTMENT	10 mg	TOPICAL	OTC monograph final	13 sections
Basic Care First Aid Antibiotic Plus Pain Relief	HUMAN OTC DRUG LABEL	4	0113-7679	OINTMENT	10 mg	TOPICAL	OTC monograph final	13 sections
Caladryl	HUMAN OTC DRUG LABEL	3	0187-5465	LOTION	10 mg	TOPICAL	OTC monograph final	14 sections
Caladryl	HUMAN OTC DRUG LABEL	3	0187-5465	LOTION	10 mg	TOPICAL	OTC monograph final	14 sections
Caladryl Clear	HUMAN OTC DRUG LABEL	2	0187-5466	LOTION	10 mg	TOPICAL	OTC monograph final	14 sections
ITCH X	HUMAN OTC DRUG LABEL	2	0225-0495	GEL	1 g	TOPICAL	OTC monograph not final	14 sections
ITCH X	HUMAN OTC DRUG LABEL	2	0225-0495	GEL	1 g	TOPICAL	OTC monograph not final	14 sections
ITCH-X	HUMAN OTC DRUG LABEL	2	0225-0516	SPRAY	1 g	TOPICAL	OTC monograph not final	13 sections
ITCH-X	HUMAN OTC DRUG LABEL	2	0225-0516	SPRAY	1 g	TOPICAL	OTC monograph not final	13 sections
Sarna	HUMAN OTC DRUG LABEL	1	0316-0230	LOTION	10 mg	TOPICAL	OTC monograph not final	13 sections
Sarna	HUMAN OTC DRUG LABEL	1	0316-0230	LOTION	10 mg	TOPICAL	OTC monograph not final	13 sections
Triple Antibiotic with Pain ReliefMaximum Strength	HUMAN OTC DRUG LABEL	4	0363-0123	OINTMENT	10 mg	TOPICAL	OTC MONOGRAPH FINAL	13 sections
Walgreen Anti-Itch	HUMAN OTC DRUG LABEL	1	0363-0263	LOTION	1 g	TOPICAL	OTC monograph not final	13 sections
Hemorrhoidal Cream	HUMAN OTC DRUG LABEL	4	0363-0641	CREAM	1 g	TOPICAL	OTC monograph not final	15 sections
Hemorrhoidal Cream	HUMAN OTC DRUG LABEL	4	0363-0641	CREAM	1 g	TOPICAL	OTC monograph not final	15 sections
Hemorrhoidal Cream	HUMAN OTC DRUG LABEL	4	0363-0641	CREAM	1 g	TOPICAL	OTC monograph not final	15 sections
Hemorrhoidal Cream	HUMAN OTC DRUG LABEL	4	0363-0641	CREAM	1 g	TOPICAL	OTC monograph not final	15 sections
First Aid Antibiotic	HUMAN OTC DRUG LABEL	4	0363-0841	OINTMENT	10 mg	TOPICAL	OTC monograph final	13 sections
First Aid Antibiotic	HUMAN OTC DRUG LABEL	4	0363-0841	OINTMENT	10 mg	TOPICAL	OTC monograph final	13 sections
Walgreens Maximum Strength Hemorrhoidal	HUMAN OTC DRUG LABEL	4	0363-1760	CREAM	0.01 mg	TOPICAL	OTC monograph final	13 sections
Walgreens Kids Multi-Antibiotic with Pain Relief Cream	HUMAN OTC DRUG LABEL	3	0363-2122	CREAM	10 mg	TOPICAL	OTC monograph not final	11 sections
Walgreens Multi-Antibiotic with Pain Relief Cream	HUMAN OTC DRUG LABEL	3	0363-2123	CREAM	10 mg	TOPICAL	OTC monograph not final	9 sections
Triple Antibiotic	HUMAN OTC DRUG LABEL	4	0363-2900	OINTMENT	10 mg	TOPICAL	OTC monograph final	13 sections
Triple Antibiotic	HUMAN OTC DRUG LABEL	4	0363-2900	OINTMENT	10 mg	TOPICAL	OTC monograph final	13 sections