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Timolol
drug data and news
Timolol drug data, resources, and news articles (when available). Onconews.org provides news on cancer research. This section, which includes profiles on medicines that may or not be cancer-related is in beta form. If things run smoothly we will be releasing a new format late in the summer of 2006.
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| Generic name | Timolol | ||
| Brand Names/Synonyms | Apo-Timol; Apo-Timop; Aquanil; Betim; Betimol; Blocadren; HSDB 6533; Istalol; Novo-Timol; Proflax; Temserin; Tenopt; Tim-Ak; Timacar; Timacor; Timolol; Timolol Base; Timolol Maleate; Timololum [Inn-Latin]; Timopic; Timoptic; Timoptic in Ocudose; Timoptic-Xe; Timoptol | ||
| Indication | For the treatment of hypertension, angina pectoris, cardiac arrhythmias, migraine and for the reduction of mortality following myocardial infarction. Ophthalmic solutions of timolol are used in the treatment of glaucoma to reduce intraocular pressure. | ||
| Sponsored links | Description | Not Available | |
| Pharmacology | Similar to propranolol and nadolol, timolol is a nonselective, beta-adrenergic receptor antagonist. Timolol does not demonstrate appreciable intrinsic sympathomimetic or membrane-stabilizing activities but possesses a relatively high degree of lipid solubility and is subject to first-pass metabolism by the liver. | ||
| 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 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. | ||
| Timolol News (When available) |
Study Demonstrates Benefits of Combination Treatment for Glaucoma May 11, 2006 NEW STUDY DEMONSTRATES A SINGLE COMPOUND AS EFFECTIVE AS A FIXED ... May 3, 2006 Allergan Reports First Quarter Operating Results; Pharmaceutical ... May 3, 2006 Allergan Posts Q1 Loss, Forecasts Q2 Results Below Wall Street ... May 3, 2006 (BW) Alcon's First Quarter Sales Rise 8.1 Percent, Net Earnings ... Apr 24, 2006 Alcon Q1 Net Earnings Rise 18.5% Primarily On Healthy Sales Growth ... Apr 24, 2006 Glaucoma treatment has options Apr 23, 2006 | ||
| Dosage Forms | DROPS; LIQUID; SOLUTION; SOLUTION (LONG-ACTING); TABLET | ||
| Drug_Category | Antihypertensive Agents; Antiarrhythmic Agents; EENT Drugs; ATC:C07AA06; ATC:S01ED01 | ||
| Absorption | Bioavailability is about 60% | ||
| Interactions |
-->Interactions for Timolol: Beta-adrenergic blocking agents: Patients who are receiving a beta-adrenergic blocking agent orally and Timolol GFS should be observed for potential additive effects of beta-blockade, both systemic and on intraocular pressure. Patients should not usually receive two topical ophthalmic beta-adrenergic blocking agents concurrently. Calcium antagonists: Caution should be used in the co-administration of beta-adrenergic blocking agents, such as Timolol GFS, and oral or intravenous calcium antagonists because of possible atrioventricular conduction disturbances, left ventricular failure, or hypotension. In patients with impaired cardiac function, co-administration should be avoided. ENDOCRINE Masked symptoms of hypoglycemia in diabetic patients. SPECIAL SENSES Signs and symptoms of ocular irritation including blepharitis, keratitis, and dry eyes; ptosis; decreased corneal sensitivity; cystoid macular edema; visual disturbances including refractive changes and diplopia; pseudopemphigoid; tinnitus and choroidal detachment following filtration surgery. UROGENITAL Retroperitoneal fibrosis, decreased libido, impotence and Peyronieís disease. The following additional adverse effects have been reported in clinical experience with ORAL timolol maleate or other ORAL beta-blocking agents and may be considered potential effects of ophthalmic timolol maleate: Allergic: Erythematous rash, fever combined with aching and sore throat, laryngospasm with respiratory distress; Body as a Whole: Extremity pain, decreased exercise tolerance, weight loss; Cardiovascular: Worsening of arterial insufficiency, vasodilatation; Digestive: Gastrointestinal pain, hepatomegaly, vomiting, mesenteric arterial thrombosis, ischemic colitis; Hematologic: Nonthrombocytopenic purpura, thrombocytopenic purpura, agranulocytosis; Endocrine: Hyperglycemia, hypoglycemia; Skin: Pruritus, skin irritation, increased pigmentation, sweating; Musculoskeletal: Arthralgia; Nervous System/Psychiatric: Vertigo, local weakness, diminished concentration, reversible mental depression progressing to catatonia, an acute reversible syndrome characterized by disorientation for time and place, emotional lability, slightly clouded sensorium, and decreased performance on neuropsychometric tests; Respiratory: Rales, bronchial obstruction; Urogenital: Urination difficulties. | ||
| Toxicity | LD50=1190 mg/kg (oral, mice), LD50=900 mg/kg (oral, rat), symptoms of acute overdoses lead to drowseiness, vertigo, headache and atriventricular block. | ||
| Organisms Affected | Humans and other mammals | ||
| Chemical IUPAC Name | 1-[(4-morpholin-4-yl-1,2,5-thiadiazol-3-yl)oxy]-3-tert-butylamino-propan-2-ol | ||
| Chemical Formula | C13H24N4O3S | ||
| Molecular Weight | 316.421 g/mol | ||
| Smiles String | CC(C)(C)NCC(COC1=NSN=C1N2CCOCC2)O | ||
| Melting Point | 201.5-202.5 °C | ||
| Water Solubility | 2.7 mg/mL | ||
| State | Solid | ||
| LogP/Hphobicity | 1.761 | ||
| Isoelectric Point | 3.9 | ||
| Biotransformation | Primarily hepatic (80%) | ||
| Half Life | 2.5-5 hours | ||
| Protein Binding [%] | ~10% | ||
| RxList Link | RXlist | ||
| Sponsored links | |||
| Drug Reference |
http://www.drugs.com/cons/Timolol.html http://www.rxlist.com/cgi/generic3/timololgfs.htm http://www.inchem.org/documents/pims/pharm/timolol.htm | ||
| Drug Type | Approved Drug | ||
| Accession No | APRD00229 | ||
| CAS Registry Number | 26839-75-8 | ||
| KEGG Compound ID | C07141 | ||
| PubChem ID | SID:175467 | ||
| PharmGKB ID | PA451690 | ||
| SwissProt ID | Not Available | ||
| GenBank ID | Not Available | ||
| Drug ID Number [DIN] | 2242276 |
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