A review of the clinical pharmacokinetics of pilocarpine, moxisylyte (thymoxamine), and dapiprazole in the reversal of diagnostic pupillary dilation. 1992

M J Doughty, and W M Lyle
School of Optometry, University of Waterloo, Ontario, Canada.

An alpha-adrenergic blocking drug, dapiprazole, is now marketed in eyedrop form. Dapiprazole is being promoted as an agent suitable for reversing the diagnostic mydriasis produced by tropicamide or tropicamide and phenylephrine. The mechanism of action of dapiprazole is thought to be the same as that of moxisylyte (thymoxamine). The human pharmacokinetics for these drugs are reviewed and compared to pilocarpine. Published data indicate that either dapiprazole (0.5%) or moxisylyte (0.5%) enhance recovery from the mydriasis produced by tropicamide, phenylephrine, or their combination. However, because the published studies differ substantially in the doses of these mydriatics or in the miotics actually used, it is not possible to make any firm recommendations on how many drops of these new miotics should be instilled.

UI MeSH Term Description Entries
D007498 Iris The most anterior portion of the uveal layer, separating the anterior chamber from the posterior. It consists of two layers - the stroma and the pigmented epithelium. Color of the iris depends on the amount of melanin in the stroma on reflection from the pigmented epithelium.
D010656 Phenylephrine An alpha-1 adrenergic agonist used as a mydriatic, nasal decongestant, and cardiotonic agent. (R)-3-Hydroxy-alpha-((methylamino)methyl)benzenemethanol,Metaoxedrin,Metasympatol,Mezaton,Neo-Synephrine,Neosynephrine,Phenylephrine Hydrochloride,Phenylephrine Tannate,Neo Synephrine,Tannate, Phenylephrine
D010862 Pilocarpine A slowly hydrolyzed muscarinic agonist with no nicotinic effects. Pilocarpine is used as a miotic and in the treatment of glaucoma. Isopilocarpine,Isoptocarpine,Ocusert,Pilocarpine Hydrochloride,Pilocarpine Mononitrate, (3S-cis)-Isomer,Pilocarpine Nitrate,Pilocarpine, Monohydrochloride, (3S-cis)-Isomer,Salagen,Hydrochloride, Pilocarpine,Nitrate, Pilocarpine
D010879 Piperazines Compounds that are derived from PIPERAZINE.
D011680 Pupil The aperture in the iris through which light passes. Pupils
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000317 Adrenergic alpha-Antagonists Drugs that bind to but do not activate alpha-adrenergic receptors thereby blocking the actions of endogenous or exogenous adrenergic agonists. Adrenergic alpha-antagonists are used in the treatment of hypertension, vasospasm, peripheral vascular disease, shock, and pheochromocytoma. Adrenergic alpha-Receptor Blockaders,alpha-Adrenergic Blocking Agents,alpha-Adrenergic Receptor Blockaders,alpha-Blockers, Adrenergic,Adrenergic alpha-Blockers,alpha-Adrenergic Antagonists,alpha-Adrenergic Blockers,Adrenergic alpha Antagonists,Adrenergic alpha Blockers,Adrenergic alpha Receptor Blockaders,Agents, alpha-Adrenergic Blocking,Antagonists, alpha-Adrenergic,Blockaders, Adrenergic alpha-Receptor,Blockaders, alpha-Adrenergic Receptor,Blockers, alpha-Adrenergic,Blocking Agents, alpha-Adrenergic,Receptor Blockaders, alpha-Adrenergic,alpha Adrenergic Antagonists,alpha Adrenergic Blockers,alpha Adrenergic Blocking Agents,alpha Adrenergic Receptor Blockaders,alpha Blockers, Adrenergic,alpha-Antagonists, Adrenergic,alpha-Receptor Blockaders, Adrenergic
D013948 Moxisylyte An alpha-adrenergic blocking agent that is used in Raynaud's disease. It is also used locally in the eye to reverse the mydriasis caused by phenylephrine and other sympathomimetic agents. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1312) Thymoxamine,Thymoxyalcylamine,Acetoxythymoxamine,Carlytène,Icavex,Moxisylyte Hydrochloride,Hydrochloride, Moxisylyte
D014230 Triazoles Heterocyclic compounds containing a five-membered ring with two carbon atoms and three nitrogen atoms with the molecular formula C2H3N3. Triazole
D014331 Tropicamide One of the MUSCARINIC ANTAGONISTS with pharmacologic action similar to ATROPINE and used mainly as an ophthalmic parasympatholytic or mydriatic. Colircusi Tropicamida,Minims Tropicamide,Mydral,Mydriafair,Mydriaticum,Mydrum,N-Ethyl-N-(4-pyridylmethyl)tropamide,N-Ethyl-alpha-(hydroxymethyl)-N-(4-pyridinylmethyl)benzeneacetamide,Ocu-Tropic,Tropicacyl,Tropicamide Faure,Tropicamide Minims,Tropicamide Monofree,Tropicamide Monohydrochloride, (R)-Isomer,Tropicamide Monohydrochloride, (S)-Isomer,Tropicamide, (+-)-Isomer,Tropicamide, (R)-Isomer,Tropicamide, (S)-Isomer,Ocu Tropic,OcuTropic

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