Product Name

Timolol

CAS Number

26839-75-8

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Product Name:
Timolol
CAS Number:
26839-75-8
Indication:
In its oral form it is used to treat high blood pressure and prevent heart attacks, and occasionally to prevent migraine headaches. In its opthalmic form it is used to treat open-angle and occasionally secondary glaucoma.
Mode of Action:

Like propranolol and nadolol, timolol competes with adrenergic neurotransmitters such as catecholamines for binding at beta(1)-adrenergic receptors in the heart and vascular smooth muscle and beta(2)-receptors in the bronchial and vascular smooth muscle. Beta(1)-receptor blockade results in a decrease in resting and exercise heart rate and cardiac output, a decrease in both systolic and diastolic blood pressure, and, possibly, a reduction in reflex orthostatic hypotension. Beta(2)-blockade results in an increase in peripheral vascular resistance. The exact mechanism whereby timolol reduces ocular pressure is still not known. The most likely action is by decreasing the secretion of aqueous humor.

Pharmacodynamics:

Similar to propranolol and nadolol, timolol is a non-selective, beta-adrenergic receptor antagonist. Timolol does not have significant intrinsic sympathomimetic, direct myocardial depressant, or local anesthetic (membrane-stabilizing) activity, but does possess a relatively high degree of lipid solubility. Timolol, when applied topically to the eye, has the action of reducing elevated, as well as normal, intraocular pressure, whether or not accompanied by glaucoma. Elevated intraocular pressure is a major risk factor in the pathogenesis of glaucomatous visual field loss and optic nerve damage.

Metabolism:

Primarily hepatic (80%) via the cytochrome P450 2D6 isoenzyme.

Toxicity:

LD50=1190 mg/kg (oral, mice), LD50=900 mg/kg (oral, rat). Symptoms of overdose include drowsiness, vertigo, headache, and atriventricular block.

IUPAC:
tert-butyl(2-hydroxy-3-{[4-(morpholin-4-yl)-1, 2, 5-thiadiazol-3-yl]oxy}propyl)amine
ATC:
C07AA06 S01ED01
PubChem:
5478
DrugBank:
DB00373 (APRD00229, DB08625)
Formula:
C16H13Cl3N2OS
Molecular Mass:
316.42
Synonyms:
Timolol maleate Timololum [INN-Latin]
SMILES:
CC(C)(C)NCC(O)COC1=NSN=C1N1CCOCC1
AHFS Code:
52:92.00 24:24.00
InChi:
BLJRIMJGRPQVNF-UHFFFAOYSA-N
General Reference:
General Reference:

  1. Link

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