demecarium

Trade name: humorsol

Small moleculeapproved

Approved

Aug 5, 1959

Demecarium (HUMORSOL®) is an indirect-acting parasympathomimetic agent, also known as a cholinesterase inhibitor and anticholinesterase. Cholinesterase inhibitors prolong the effect of acetylcholine, which is released at the neuroeffector junction of parasympathetic postganglion nerves, by inactivating the cholinesterases that break it down. Application of demecarium (HUMORSOL®) to the eye produces intense miosis and ciliary muscle contraction due to inhibition of cholinesterase, allowing acetylcholine to accumulate at sites of cholinergic transmission. These effects are accompanied by increased capillary permeability of the ciliary body and iris, increased permeability of the blood-aqueous barrier, and vasodilation. Myopia may be induced or, if present, may be augmented by the increased refractive power of the lens that results from the accommodative effect of the drug. Demecarium (HUMORSOL®) indirectly produces some of the muscarinic and nicotinic effects of acetylcholine as quantities of the latter accumulate. — NCATS

Clinical trial activity

0 trials · 0 clinical orgs · 1 marketing orgs

Phase 1
0
Phase 2
0
Phase 3
0
Phase 4
0

Timeline

1950s

  1. Aug 5, 1959

    Merck — Earliest FDA Approval

  2. Aug 5, 1959

    Merck — NDA Organization

Indications

Mechanism of action

Approval history

  • approvedAug 5, 1959

Chemistry & pharmacology

Loading structure…

SMILES

CN(CCCCCCCCCCN(C)C(=O)Oc1cccc([N+](C)(C)C)c1)C(=O)Oc1cccc([N+](C)(C)C)c1
Mol. weight
556.79 g/mol
Lipinski Ro5
2 violation(s)
Rule of 3
No
Chirality
Achiral Molecule
Inorganic
No
Polymer
No
Delivery
Topical
Availability
Discontinued

Oral

No

Parenteral

No

Topical

Yes

Sources

Also known as

  • demecarium
  • demecarium
  • demecarium
  • demecarium
  • demecarium
  • demecarium
  • demecarium
  • demecarium
  • demecarium bromide
  • demecarium bromide
  • demecarium bromide
  • demecarium bromide
  • demecarium bromide
  • demecarium bromide
  • demecarium bromide
  • demecastigmine
  • demekarium bromide
  • demekastigmine bromide
  • demekastigmine bromide
  • demekastigmine bromide
  • hafslund nycomed brand of demecarium bromide
  • humorsol
  • humorsol
  • humorsol
  • humorsol
  • merck brand of demecarium bromide
  • tosmilen
  • tosmilen
  • tosmilen

Organizations

Marketing (1)

OrganizationOrg typeRelationshipDate
MerckFor profitNDAAug 5, 1959