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PubChem
Name: Timolol
PubChem Compound ID: 33624
Description: A beta-adrenergic antagonist similar in action to PROPRANOLOL. The levo-isomer is the more active. Timolol has been proposed as an antihypertensive, antiarrhythmic, antiangina, and antiglaucoma agent. It is also used in the treatment of MIGRAINE DISORDERS and tremor.
Molecular formula: C13H24N4O3S
Molecular weight: 316.421 g/mol
Synonyms:
Lopac-T-6394; NCGC00016798-01; Istalol; SPBio_003075; 194288-09-0; Prestwick0_000948; (S)-1-(1,1-(Dimethylethyl)amino)-3-((4-(4-morpholinyl)-1,2,5-thiadiazol-3-yl)oxy)-2-propanol; Prestwick1_000948; 2-Propanol, 1-((1,1-dimethylethyl)amino)-3-((4-(4-morpholinyl)-1,2,5-thiadiazol-3-yl)oxy)-, (2S)-; 26921-17-5.
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DrugBank
Identification
Name: Timolol
Name (isomeric): DB00373
Drug Type: small molecule
Description: A beta-adrenergic antagonist similar in action to PROPRANOLOL. The levo-isomer is the more active. Timolol has been proposed as an antihypertensive, antiarrhythmic, antiangina, and antiglaucoma agent. It is also used in the treatment of MIGRAINE DISORDERS and tremor.
Synonyms:
Timololum [INN-Latin]; Timolol maleate
Brand: Apo-Timop, Timoptic OcuDose, Novo-Timol, Timoptol, Apo-Timol, Timoptic-XE, Timopic, Tim-AK, Nu-Timolol, Blocadren, Timoptic, Betimol, Tenopt, Temserin, Timacor, Timacar, Aquanil, Betim, Istalol, Phoxal-timolol, Timoptic in Ocudose, Proflax
Brand name mixture: Timpilo 2(Pilocarpine Hydrochloride + Timolol Maleate), Combigan(Brimonidine Tartrate + Timolol Maleate), Xalacom(Latanoprost + Timolol Maleate), Cosopt(Dorzolamide Hydrochloride + Timolol Maleate), Timolide Tab(Hydrochlorothiazide + Timolol Maleate), Timpilo 4(Pilocarpine Hydrochloride + Timolol Maleate)
Category: Adrenergic beta-Antagonists, Anti-Arrhythmia Agents, Antihypertensive Agents
CAS number: 26839-75-8
Pharmacology
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.
Pharmacology:
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...
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Mechanism 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 ...
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Absorption: Bioavailability is about 60%
Protein binding: ~10%
Biotransformation: Primarily hepatic (80%) via the cytochrome P450 2D6 isoenzyme.
Route of elimination: Timolol and its metabolites are primarily excreted in the urine.
Half Life: 2.5-5 hours
Toxicity: LD50=1190 mg/kg (oral, mice), LD50=900 mg/kg (oral, rat). Symptoms of overdose include drowsiness, vertigo, headache, and atriventricular block.
Affected organisms: Humans and other mammals
Interactions
Drug interaction:
GlycodiazineThe beta-blocker, timolol, may decrease symptoms of hypoglycemia.
MethyldopaPossible hypertensive crisis
CimetidineCimetidine may increase the serum concentration of timolol by decreasing its metabolism.
KetoprofenThe NSAID, Ketoprofen, may antagonize the antihypertensive effect of Timolol.
LidocaineThe beta-blocker, timolol, may increase the effect and toxicity of lidocaine.
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