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.

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.
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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
...achieved clinically significant additional reduction in intraocular pressure (IOP) when treated with CosoptĀ® (dorzolamide hydrochloride/timolol maleate) alone ... - DG News

NEW STUDY DEMONSTRATES A SINGLE COMPOUND AS EFFECTIVE AS A FIXED ...  May 3, 2006
...bimatoprost) is as effective alone at lowering intraocular pressure (IOP) as a fixed combination (XALACOM) of latanoprost (Xalatan) combined with timolol. ... - ITNews,

Allergan Reports First Quarter Operating Results; Pharmaceutical ...  May 3, 2006
...for Medicinal Products for Human Use (CHMP) recommended that the European Commission approve GANFORT(R), Allergan's LUMIGAN(R)/timolol combination product ... - Genetic Engineering News,

Allergan Posts Q1 Loss, Forecasts Q2 Results Below Wall Street ...  May 3, 2006
...the Committee for Medicinal Products for Human Use recommended that the European Commission approve GANFORT, Allergan's LUMIGAN/timolol combination product for ... - Trading Markets,

(BW) Alcon's First Quarter Sales Rise 8.1 Percent, Net Earnings ...  Apr 24, 2006
DuoTrav(TM), a fixed combination of travoprost 0.004% and timolol 0.5%, received a positive recommendation for approval in the European Union by the ... - Houston Chronicle,

Alcon Q1 Net Earnings Rise 18.5% Primarily On Healthy Sales Growth ...  Apr 24, 2006
DuoTrav, a fixed combination of travoprost 0.004% and timolol 0.5%, received a positive recommendation for approval in the European Union by the Committee for ... - Trading Markets,

Glaucoma treatment has options  Apr 23, 2006
For example, beta blockers such as levobunolol (Betagan) or timolol (Betimol, Timoptic) can reduce the production of aqueous humor, and prostaglandin analogues ... - Fort Wayne Journal Gazette,

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
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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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