AI ASSISTANT
Ask DrugCentral
Explore drug information in your own words.
Type a question in the search bar above to get started. Each question is answered independently.
Try a sample question
Select a question to fill the search bar, then submit it or edit it first.
AI can make mistakes. Verify answers against the original sources before relying on them.
pilocarpine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| tricyclic compounds | 2166 | 92-13-7 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A slowly hydrolyzed muscarinic agonist with no nicotinic effects. Pilocarpine is used as a miotic and in the treatment of glaucoma.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 15 | mg | O |
| 10 | mg | P |
| 0.40 | ml | None |
| 40 | mg | ointment |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| fu (Fraction unbound in plasma) | 0.92 % | Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K |
| BA (Bioavailability) | 100 % |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 0.203 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 1.905 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 7.430 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 2.877 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 76.270 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 69.520 | % | High | 1 |
| herg | hERG pIC50 | 4.192 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 1.197 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 3.981 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 63.850 | % | High | 1 |
| kinase-safety-class | ACVR2A,ACVR2B,AXL,BRAF,BTK,CAMK2D,CDK5,CDK9,DYRK1B,EIF2AK3,ERBB2,GRK2,MAP3K21,MAPK7,NTRK2,PDK1,PDK2,PRKDC,SIK2,STK33,TEK | 21 | |||
| kinase-selectivity-class | GRK2 | 1 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 2.234 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 7.907 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 79.510 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 3.119 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 83.590 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 1.758 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 91.460 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 67.880 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 914.113 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| July 29, 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 |
|---|---|---|---|---|---|---|
| Glaucoma | 64.23 | 15.97 | 34 | 8743 | 20721 | 90598949 |
| Dry eye | 58.61 | 15.97 | 47 | 8730 | 57884 | 90561786 |
| Vitreous detachment | 56.37 | 15.97 | 17 | 8760 | 2361 | 90617309 |
| Eye pain | 53.77 | 15.97 | 40 | 8737 | 44128 | 90575542 |
| Limb injury | 53.50 | 15.97 | 35 | 8742 | 31473 | 90588197 |
| Occult blood | 51.98 | 15.97 | 14 | 8763 | 1297 | 90618373 |
| Angioplasty | 50.33 | 15.97 | 14 | 8763 | 1463 | 90618207 |
| Eye irritation | 46.42 | 15.97 | 33 | 8744 | 33945 | 90585725 |
| Calcification of muscle | 45.90 | 15.97 | 9 | 8768 | 200 | 90619470 |
| Peripheral vascular disorder | 43.19 | 15.97 | 18 | 8759 | 6413 | 90613257 |
| Vision blurred | 42.68 | 15.97 | 53 | 8724 | 110240 | 90509430 |
| Visual impairment | 40.98 | 15.97 | 57 | 8720 | 132308 | 90487362 |
| Choking | 40.91 | 15.97 | 21 | 8756 | 12012 | 90607658 |
| Vitreous floaters | 40.41 | 15.97 | 18 | 8759 | 7531 | 90612139 |
| Vitreoretinal traction syndrome | 39.23 | 15.97 | 6 | 8771 | 27 | 90619643 |
| Transient ischaemic attack | 35.33 | 15.97 | 31 | 8746 | 43145 | 90576525 |
| Crepitations | 34.66 | 15.97 | 17 | 8760 | 8835 | 90610835 |
| Corneal oedema | 34.18 | 15.97 | 11 | 8766 | 1890 | 90617780 |
| Hot flush | 32.16 | 15.97 | 34 | 8743 | 59454 | 90560216 |
| Spinal osteoarthritis | 31.84 | 15.97 | 21 | 8756 | 19127 | 90600543 |
| Coronary artery disease | 31.30 | 15.97 | 26 | 8751 | 33597 | 90586073 |
| Acute myocardial infarction | 30.46 | 15.97 | 26 | 8751 | 34864 | 90584806 |
| Iritis | 27.07 | 15.97 | 11 | 8766 | 3675 | 90615995 |
| Cardiac failure congestive | 26.87 | 15.97 | 40 | 8737 | 98654 | 90521016 |
| Tanning | 26.40 | 15.97 | 5 | 8772 | 92 | 90619578 |
| Haemorrhage | 26.28 | 15.97 | 33 | 8744 | 69336 | 90550334 |
| Sputum discoloured | 26.01 | 15.97 | 19 | 8758 | 20372 | 90599298 |
| Intraocular pressure increased | 25.92 | 15.97 | 13 | 8764 | 7080 | 90612590 |
| Bronchial wall thickening | 25.19 | 15.97 | 9 | 8768 | 2122 | 90617548 |
| Iron deficiency | 24.89 | 15.97 | 14 | 8763 | 9598 | 90610072 |
| Urinary retention | 24.84 | 15.97 | 24 | 8753 | 37720 | 90581950 |
| Body temperature fluctuation | 24.61 | 15.97 | 9 | 8768 | 2266 | 90617404 |
| Blood pressure increased | 24.50 | 15.97 | 57 | 8720 | 197160 | 90422510 |
| Accommodation disorder | 24.09 | 15.97 | 6 | 8771 | 408 | 90619262 |
| Pulmonary congestion | 22.31 | 15.97 | 17 | 8760 | 19416 | 90600254 |
| Psychiatric decompensation | 22.19 | 15.97 | 8 | 8769 | 1935 | 90617735 |
| Myocardial infarction | 22.05 | 15.97 | 38 | 8739 | 105934 | 90513736 |
| Conjunctival hyperaemia | 21.72 | 15.97 | 9 | 8768 | 3160 | 90616510 |
| Visual acuity reduced | 21.57 | 15.97 | 18 | 8759 | 23392 | 90596278 |
| Ocular hyperaemia | 21.33 | 15.97 | 21 | 8756 | 33777 | 90585893 |
| Blood pressure diastolic increased | 21.08 | 15.97 | 14 | 8763 | 12892 | 90606778 |
| Productive cough | 20.64 | 15.97 | 31 | 8746 | 77032 | 90542638 |
| Bicytopenia | 20.21 | 15.97 | 9 | 8768 | 3762 | 90615908 |
| Blood pressure systolic decreased | 20.02 | 15.97 | 12 | 8765 | 9258 | 90610412 |
| Increased tendency to bruise | 19.67 | 15.97 | 13 | 8764 | 11877 | 90607793 |
| Instillation site pain | 19.29 | 15.97 | 6 | 8771 | 924 | 90618746 |
| Headache | 19.26 | 15.97 | 146 | 8631 | 862600 | 89757070 |
| Acne | 18.52 | 15.97 | 18 | 8759 | 28489 | 90591181 |
| Open fracture | 18.40 | 15.97 | 5 | 8772 | 479 | 90619191 |
| Pulmonary oedema | 18.11 | 15.97 | 26 | 8751 | 62054 | 90557616 |
| Vasculitis | 17.97 | 15.97 | 16 | 8761 | 22677 | 90596993 |
| Post procedural discharge | 17.95 | 15.97 | 5 | 8772 | 525 | 90619145 |
| Endometritis | 17.78 | 15.97 | 6 | 8771 | 1194 | 90618476 |
| Photopsia | 17.75 | 15.97 | 9 | 8768 | 5015 | 90614655 |
| Ulcerative keratitis | 17.74 | 15.97 | 8 | 8769 | 3445 | 90616225 |
| Platelet count increased | 17.10 | 15.97 | 15 | 8762 | 20844 | 90598826 |
| Myalgia | 16.91 | 15.97 | 46 | 8731 | 175079 | 90444591 |
| Exposure to communicable disease | 16.85 | 15.97 | 5 | 8772 | 657 | 90619013 |
| Systemic lupus erythematosus | 16.82 | 15.97 | 7 | 8770 | 361889 | 90257781 |
| Epstein-Barr virus associated lymphoma | 16.52 | 15.97 | 5 | 8772 | 703 | 90618967 |
| Retinal tear | 16.47 | 15.97 | 6 | 8771 | 1496 | 90618174 |
| Toxicity to various agents | 16.14 | 15.97 | 4 | 8773 | 287842 | 90331828 |
| Pupillary disorder | 16.13 | 15.97 | 4 | 8773 | 267 | 90619403 |
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 |
|---|---|---|---|---|---|---|
| Vitreous detachment | 100.48 | 24.93 | 19 | 1474 | 997 | 42618845 |
| Visual impairment | 96.39 | 24.93 | 41 | 1452 | 43072 | 42576770 |
| Retinal tear | 75.36 | 24.93 | 15 | 1478 | 1029 | 42618813 |
| Retinal detachment | 74.30 | 24.93 | 21 | 1472 | 6504 | 42613338 |
| Vitreous floaters | 73.49 | 24.93 | 19 | 1474 | 4211 | 42615631 |
| Intraocular pressure increased | 52.51 | 24.93 | 16 | 1477 | 6417 | 42613425 |
| Rhegmatogenous retinal detachment | 45.75 | 24.93 | 7 | 1486 | 100 | 42619742 |
| Vitreoretinal traction syndrome | 41.93 | 24.93 | 5 | 1488 | 7 | 42619835 |
| Vision blurred | 41.74 | 24.93 | 25 | 1468 | 53674 | 42566168 |
| Ocular hyperaemia | 41.70 | 24.93 | 17 | 1476 | 15946 | 42603896 |
| Photopsia | 37.94 | 24.93 | 10 | 1483 | 2382 | 42617460 |
| Lens dislocation | 36.67 | 24.93 | 6 | 1487 | 134 | 42619708 |
| Tumour flare | 34.37 | 24.93 | 8 | 1485 | 1145 | 42618697 |
| Headache | 31.22 | 24.93 | 40 | 1453 | 239329 | 42380513 |
| Eye pain | 30.84 | 24.93 | 14 | 1479 | 17016 | 42602826 |
| Treatment failure | 28.75 | 24.93 | 21 | 1472 | 62603 | 42557239 |
| Miosis | 27.37 | 24.93 | 12 | 1481 | 13434 | 42606408 |
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 |
|---|---|---|---|---|---|---|
| Glaucoma | 79.52 | 16.06 | 37 | 8131 | 22480 | 110558651 |
| Limb injury | 66.87 | 16.06 | 39 | 8129 | 37597 | 110543534 |
| Vitreous detachment | 59.01 | 16.06 | 17 | 8151 | 2648 | 110578483 |
| Angioplasty | 54.69 | 16.06 | 15 | 8153 | 1956 | 110579175 |
| Vitreous floaters | 51.90 | 16.06 | 21 | 8147 | 9113 | 110572018 |
| Occult blood | 50.92 | 16.06 | 14 | 8154 | 1842 | 110579289 |
| Calcification of muscle | 48.87 | 16.06 | 9 | 8159 | 188 | 110580943 |
| Intraocular pressure increased | 48.36 | 16.06 | 21 | 8147 | 10855 | 110570276 |
| Vitreoretinal traction syndrome | 47.76 | 16.06 | 7 | 8161 | 31 | 110581100 |
| Choking | 44.73 | 16.06 | 22 | 8146 | 15088 | 110566043 |
| Dry eye | 44.06 | 16.06 | 35 | 8133 | 55758 | 110525373 |
| Peripheral vascular disorder | 42.90 | 16.06 | 18 | 8150 | 8558 | 110572573 |
| Crepitations | 38.86 | 16.06 | 18 | 8150 | 10817 | 110570314 |
| Eye pain | 38.64 | 16.06 | 31 | 8137 | 50068 | 110531063 |
| Transient ischaemic attack | 37.87 | 16.06 | 34 | 8134 | 63948 | 110517183 |
| Lens dislocation | 36.47 | 16.06 | 7 | 8161 | 184 | 110580947 |
| Visual impairment | 36.09 | 16.06 | 47 | 8121 | 134381 | 110446750 |
| Corneal oedema | 35.47 | 16.06 | 12 | 8156 | 3161 | 110577970 |
| Hot flush | 29.41 | 16.06 | 30 | 8138 | 66006 | 110515125 |
| Cardiac failure congestive | 27.61 | 16.06 | 44 | 8124 | 150956 | 110430175 |
| Sputum discoloured | 27.51 | 16.06 | 20 | 8148 | 27925 | 110553206 |
| Tanning | 27.35 | 16.06 | 5 | 8163 | 100 | 110581031 |
| Haemorrhage | 26.62 | 16.06 | 36 | 8132 | 106656 | 110474475 |
| Urinary retention | 26.32 | 16.06 | 29 | 8139 | 69654 | 110511477 |
| Tumour flare | 26.01 | 16.06 | 8 | 8160 | 1559 | 110579572 |
| Spinal osteoarthritis | 25.88 | 16.06 | 17 | 8151 | 20166 | 110560965 |
| Vision blurred | 25.54 | 16.06 | 39 | 8129 | 128983 | 110452148 |
| Iritis | 24.06 | 16.06 | 10 | 8158 | 4642 | 110576489 |
| Bronchial wall thickening | 23.98 | 16.06 | 9 | 8159 | 3198 | 110577933 |
| Blood pressure increased | 23.45 | 16.06 | 56 | 8112 | 258317 | 110322814 |
| Body temperature fluctuation | 22.56 | 16.06 | 9 | 8159 | 3764 | 110577367 |
| Coronary artery disease | 22.31 | 16.06 | 27 | 8141 | 71663 | 110509468 |
| Eye irritation | 22.25 | 16.06 | 19 | 8149 | 33433 | 110547698 |
| Miosis | 22.24 | 16.06 | 16 | 8152 | 21967 | 110559164 |
| Conjunctival hyperaemia | 21.89 | 16.06 | 10 | 8158 | 5821 | 110575310 |
| Pulmonary congestion | 21.44 | 16.06 | 18 | 8150 | 30948 | 110550183 |
| Endometritis | 20.62 | 16.06 | 6 | 8162 | 968 | 110580163 |
| Acne | 20.20 | 16.06 | 18 | 8150 | 33502 | 110547629 |
| Iron deficiency | 19.97 | 16.06 | 14 | 8154 | 18462 | 110562669 |
| Blood pressure diastolic increased | 19.75 | 16.06 | 14 | 8154 | 18793 | 110562338 |
| Open fracture | 19.31 | 16.06 | 5 | 8163 | 523 | 110580608 |
| Productive cough | 19.12 | 16.06 | 32 | 8136 | 114273 | 110466858 |
| Myocardial infarction | 18.92 | 16.06 | 43 | 8125 | 192040 | 110389091 |
| Ocular surface disease | 18.75 | 16.06 | 4 | 8164 | 180 | 110580951 |
| Exposure to communicable disease | 18.70 | 16.06 | 5 | 8163 | 592 | 110580539 |
| Headache | 18.61 | 16.06 | 120 | 8048 | 882257 | 109698874 |
| Accommodation disorder | 18.26 | 16.06 | 5 | 8163 | 648 | 110580483 |
| Ocular hyperaemia | 17.77 | 16.06 | 18 | 8150 | 39268 | 110541863 |
| Instillation site pain | 17.60 | 16.06 | 5 | 8163 | 741 | 110580390 |
| Bicytopenia | 17.58 | 16.06 | 9 | 8159 | 6715 | 110574416 |
| Acute myocardial infarction | 17.54 | 16.06 | 26 | 8142 | 83751 | 110497380 |
| Post procedural discharge | 17.36 | 16.06 | 5 | 8163 | 777 | 110580354 |
| Ulcerative keratitis | 17.34 | 16.06 | 8 | 8160 | 4758 | 110576373 |
| Weight increased | 17.30 | 16.06 | 69 | 8099 | 419575 | 110161556 |
| Rhegmatogenous retinal detachment | 17.17 | 16.06 | 4 | 8164 | 270 | 110580861 |
| Visual acuity reduced | 16.90 | 16.06 | 16 | 8152 | 32157 | 110548974 |
| Choroidal effusion | 16.73 | 16.06 | 5 | 8163 | 885 | 110580246 |
| Angle closure glaucoma | 16.35 | 16.06 | 7 | 8161 | 3492 | 110577639 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | N07AX01 | NERVOUS SYSTEM OTHER NERVOUS SYSTEM DRUGS PARASYMPATHOMIMETICS Other parasympathomimetics |
| ATC | S01EB01 | SENSORY ORGANS OPHTHALMOLOGICALS ANTIGLAUCOMA PREPARATIONS AND MIOTICS Parasympathomimetics |
| ATC | S01EB51 | SENSORY ORGANS OPHTHALMOLOGICALS ANTIGLAUCOMA PREPARATIONS AND MIOTICS Parasympathomimetics |
| FDA MoA | N0000000104 | Cholinergic Muscarinic Agonists |
| FDA MoA | N0000175369 | Cholinergic Agonists |
| MeSH PA | D008916 | Miotics |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D018678 | Cholinergic Agents |
| MeSH PA | D018679 | Cholinergic Agonists |
| MeSH PA | D018721 | Muscarinic Agonists |
| FDA EPC | N0000175884 | Cholinergic Receptor Agonist |
| CHEBI has role | CHEBI:39456 | antiglaucoma drug |
| CHEBI has role | CHEBI:35610 | antineoplastic agent |
| CHEBI has role | CHEBI:66981 | ophthalmology drug |
Related Drugs by ATC class:
N07AX Other parasympathomimetics 2 drugs
S01EB Parasympathomimetics 9 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Ocular hypertension | indication | 4210003 | DOID:9282 |
| Presbyopia | indication | 41256004 | DOID:11638 |
| Open-angle glaucoma | indication | 84494001 | DOID:1067 |
| Aptyalism | indication | 87715008 | |
| Xerostomia Secondary to Radiation Therapy | indication | ||
| Xerostomia Secondary to Sjogren's Syndrome | indication | ||
| Primary Closed Angle Glaucoma | indication | ||
| Bronchospasm | contraindication | 4386001 | |
| Keratitis | contraindication | 5888003 | DOID:4677 |
| Chronic obstructive lung disease | contraindication | 13645005 | DOID:3083 |
| Retinal detachment | contraindication | 42059000 | DOID:5327 |
| Hepatic failure | contraindication | 59927004 | |
| Iritis | contraindication | 65074000 | DOID:1406 |
| Cholecystitis | contraindication | 76581006 | DOID:1949 |
| Kidney stone | contraindication | 95570007 | |
| Disorder of biliary tract | contraindication | 105997008 | DOID:9741 |
| Acute disease of cardiovascular system | contraindication | 128487001 | |
| Calculus in biliary tract | contraindication | 266474003 | |
| Angle-closure glaucoma | contraindication | 392291006 | DOID:13550 |
| Anterior uveitis | contraindication | 410692006 | DOID:1407 |
| Acute exacerbation of asthma | contraindication | 708038006 | |
| Psychiatric Disturbance | contraindication | ||
| Pupillary Block Glaucoma | 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 | 7.04 | Basic |
Orange Book patent data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
|---|---|---|---|---|---|---|---|---|---|---|
| 0.4% | QLOSI | ORASIS PHARMS | N217836 | Oct. 17, 2023 | RX | SOLUTION/DROPS | OPHTHALMIC | 10639297 | Aug. 18, 2037 | TREATMENT OF PRESBYOPIA |
| 0.4% | QLOSI | ORASIS PHARMS | N217836 | Oct. 17, 2023 | RX | SOLUTION/DROPS | OPHTHALMIC | 11129812 | Aug. 18, 2037 | TREATMENT OF PRESBYOPIA |
| 0.4% | QLOSI | ORASIS PHARMS | N217836 | Oct. 17, 2023 | RX | SOLUTION/DROPS | OPHTHALMIC | 11974986 | Aug. 18, 2037 | TREATMENT OF PRESBYOPIA |
| 0.4% | QLOSI | ORASIS PHARMS | N217836 | Oct. 17, 2023 | RX | SOLUTION/DROPS | OPHTHALMIC | 9867810 | Aug. 18, 2037 | TREATMENT OF PRESBYOPIA |
| 1.25% | VUITY | ABBVIE | N214028 | Oct. 28, 2021 | DISCN | SOLUTION/DROPS | OPHTHALMIC | 10610518 | April 24, 2039 | TREATMENT OF PRESBYOPIA IN ADULTS BY ADMINISTRATION OF PILOCARPINE HCI FORMULATION ONCE DAILY |
| 1.25% | VUITY | ABBVIE | N214028 | Oct. 28, 2021 | DISCN | SOLUTION/DROPS | OPHTHALMIC | 10610518 | April 24, 2039 | TREATMENT OF PRESBYOPIA IN ADULTS BY ADMINISTRATION OF PILOCARPINE HCI FORMULATION TWICE DAILY |
| 1.25% | VUITY | ABBVIE | N214028 | Oct. 28, 2021 | DISCN | SOLUTION/DROPS | OPHTHALMIC | 10610518 | April 24, 2039 | USE OF VUITY FOR THE TREATMENT OF PRESBYOPIA IN ADULTS |
| 1.25% | VUITY | ABBVIE | N214028 | Oct. 28, 2021 | DISCN | SOLUTION/DROPS | OPHTHALMIC | 11285134 | April 24, 2039 | TREATMENT OF PRESBYOPIA IN ADULTS BY ADMINISTRATION OF PILOCARPINE HCI FORMULATION ONCE DAILY |
| 1.25% | VUITY | ABBVIE | N214028 | Oct. 28, 2021 | DISCN | SOLUTION/DROPS | OPHTHALMIC | 11285134 | April 24, 2039 | TREATMENT OF PRESBYOPIA IN ADULTS BY ADMINISTRATION OF PILOCARPINE HCI FORMULATION TWICE DAILY |
| 1.25% | VUITY | ABBVIE | N214028 | Oct. 28, 2021 | DISCN | SOLUTION/DROPS | OPHTHALMIC | 11285134 | April 24, 2039 | USE OF VUITY FOR THE TREATMENT OF PRESBYOPIA IN ADULTS |
Orange Book exclusivity data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| 1.25% | VUITY | ABBVIE | N214028 | Oct. 28, 2021 | DISCN | SOLUTION/DROPS | OPHTHALMIC | March 28, 2026 | ADDITION OF SECOND DOSE FOR TREATMENT OF PRESBYOPIA IN ADULTS |
| 0.4% | QLOSI | ORASIS PHARMS | N217836 | Oct. 17, 2023 | RX | SOLUTION/DROPS | OPHTHALMIC | Oct. 17, 2026 | NEW PRODUCT |
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Muscarinic acetylcholine receptor M3 | GPCR | AGONIST | EC50 | 6.97 | SCIENTIFIC LITERATURE | IUPHAR | |||
| Muscarinic acetylcholine receptor M1 | GPCR | AGONIST | EC50 | 7.02 | SCIENTIFIC LITERATURE | ||||
| Muscarinic acetylcholine receptor M2 | GPCR | AGONIST | EC50 | 6.95 | SCIENTIFIC LITERATURE | ||||
| Muscarinic acetylcholine receptor M4 | GPCR | AGONIST | EC50 | 7.15 | SCIENTIFIC LITERATURE | ||||
| Muscarinic acetylcholine receptor M5 | GPCR | AGONIST | EC50 | 7 | SCIENTIFIC LITERATURE | ||||
| Muscarinic acetylcholine receptor M1 | GPCR | Ki | 5.51 | CHEMBL | |||||
| Muscarinic acetylcholine receptor M1 | GPCR | EC50 | 5.16 | CHEMBL | |||||
| Muscarinic acetylcholine receptor DM1 | GPCR | Ki | 5.55 | CHEMBL | |||||
| Muscarinic acetylcholine receptor | GPCR | Ki | 7.08 | CHEMBL | |||||
| Muscarinic acetylcholine receptor M2 | GPCR | Ki | 5.01 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| D00525 | KEGG_DRUG |
| 148-72-1 | SECONDARY_CAS_RN |
| 54-71-7 | SECONDARY_CAS_RN |
| 4018207 | VANDF |
| 4018208 | VANDF |
| 4018209 | VANDF |
| 4020904 | VANDF |
| C0031923 | UMLSCUI |
| CHEBI:8207 | CHEBI |
| 9PL | PDB_CHEM_ID |
| CHEMBL550 | ChEMBL_ID |
| DB01085 | DRUGBANK_ID |
| CHEMBL1200330 | ChEMBL_ID |
| CHEMBL611494 | ChEMBL_ID |
| CHEMBL1213136 | ChEMBL_ID |
| D010862 | MESH_DESCRIPTOR_UI |
| 5910 | PUBCHEM_CID |
| 305 | IUPHAR_LIGAND_ID |
| 01MI4Q9DI3 | UNII |
| 103244 | RXNORM |
| 1396 | MMSL |
| 20709 | MMSL |
| 3317 | MMSL |
| 44345 | MMSL |
| 5299 | MMSL |
| 5300 | MMSL |
| 72427 | MMSL |
| 73122 | MMSL |
| d04031 | MMSL |
| 001693 | NDDF |
| 001694 | NDDF |
| 001695 | NDDF |
| 372895002 | SNOMEDCT_US |
| 387035001 | SNOMEDCT_US |
| 395827004 | SNOMEDCT_US |
| 90356005 | SNOMEDCT_US |
| 01MI4Q9DI3 | INXIGHT DRUGS |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| VUITY | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0074-7098 | SOLUTION/ DROPS | 12.50 mg | OPHTHALMIC | NDA | 26 sections |
| Pilocarpine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0115-5911 | TABLET, FILM COATED | 7.50 mg | ORAL | ANDA | 23 sections |
| Pilocarpine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0115-5922 | TABLET, FILM COATED | 5 mg | ORAL | ANDA | 23 sections |
| Pilocarpine hydrochloride | Human Prescription Drug Label | 1 | 0228-2801 | TABLET, FILM COATED | 5 mg | ORAL | NDA AUTHORIZED GENERIC | 21 sections |
| Pilocarpine hydrochloride | Human Prescription Drug Label | 1 | 0228-2837 | TABLET, FILM COATED | 7.50 mg | ORAL | NDA AUTHORIZED GENERIC | 21 sections |
| Pilocarpine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0527-1313 | TABLET, FILM COATED | 5 mg | ORAL | ANDA | 24 sections |
| Pilocarpine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0527-1407 | TABLET, FILM COATED | 7.50 mg | ORAL | ANDA | 24 sections |
| Pilocarpine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10135-589 | TABLET, FILM COATED | 5 mg | ORAL | ANDA | 22 sections |
| Pilocarpine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10135-590 | TABLET, FILM COATED | 7.50 mg | ORAL | ANDA | 22 sections |
| Pilocarpine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10135-680 | TABLET, FILM COATED | 5 mg | ORAL | ANDA | 23 sections |
| Pilocarpine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 17478-223 | SOLUTION/ DROPS | 10 mg | OPHTHALMIC | ANDA | 24 sections |
| Pilocarpine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 17478-224 | SOLUTION/ DROPS | 20 mg | OPHTHALMIC | ANDA | 24 sections |
| Pilocarpine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 17478-226 | SOLUTION/ DROPS | 40 mg | OPHTHALMIC | ANDA | 24 sections |
| PILOCARPINE HYDROCHLORIDE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 21695-368 | SOLUTION/ DROPS | 10 mg | CONJUNCTIVAL | NDA | 14 sections |
| Pilocarpine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 21695-601 | TABLET | 5 mg | ORAL | ANDA | 23 sections |
| Pilocarpine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50268-652 | TABLET, FILM COATED | 5 mg | ORAL | ANDA | 24 sections |
| Pilocarpine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 54868-5436 | TABLET, FILM COATED | 5 mg | ORAL | ANDA | 24 sections |
| Salagen | Human Prescription Drug Label | 1 | 59212-705 | TABLET, FILM COATED | 5 mg | ORAL | NDA | 21 sections |
| Salagen | Human Prescription Drug Label | 1 | 59212-775 | TABLET, FILM COATED | 7.50 mg | ORAL | NDA | 21 sections |
| Pilocarpine Hydrochloride | Human Prescription Drug Label | 1 | 59651-224 | TABLET, FILM COATED | 5 mg | ORAL | ANDA | 20 sections |
| Pilocarpine Hydrochloride | Human Prescription Drug Label | 1 | 59651-224 | TABLET, FILM COATED | 5 mg | ORAL | ANDA | 20 sections |
| Pilocarpine Hydrochloride | Human Prescription Drug Label | 1 | 59651-225 | TABLET, FILM COATED | 7.50 mg | ORAL | ANDA | 20 sections |
| Pilocarpine Hydrochloride | Human Prescription Drug Label | 1 | 59651-225 | TABLET, FILM COATED | 7.50 mg | ORAL | ANDA | 20 sections |
| Pilocarpine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 60219-1745 | SOLUTION/ DROPS | 10 mg | OPHTHALMIC | ANDA | 23 sections |
| Pilocarpine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 60219-1746 | SOLUTION/ DROPS | 20 mg | OPHTHALMIC | ANDA | 23 sections |
| Pilocarpine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 60219-1747 | SOLUTION/ DROPS | 40 mg | OPHTHALMIC | ANDA | 23 sections |
| Pilocarpine Hydrochloride Ophthalmic | HUMAN PRESCRIPTION DRUG LABEL | 1 | 60219-2366 | SOLUTION/ DROPS | 12.50 mg | OPHTHALMIC | ANDA | 23 sections |
| Pilocarpine Hydrochloride Ophthalmic | HUMAN PRESCRIPTION DRUG LABEL | 1 | 60219-2649 | SOLUTION/ DROPS | 12.50 mg | OPHTHALMIC | ANDA | 23 sections |
| Pilocarpine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 60219-5922 | TABLET, FILM COATED | 5 mg | ORAL | ANDA | 23 sections |
| Pilocarpine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 61314-203 | SOLUTION/ DROPS | 10 mg | OPHTHALMIC | NDA authorized generic | 23 sections |