药品详细
Timolol(噻吗洛尔)
化学结构式图
中文名
噻吗洛尔
英文名
Timolol
分子式
C13H24N4O3S
化学名
tert-butyl(2-hydroxy-3-{[4-(morpholin-4-yl)-1,2,5-thiadiazol-3-yl]oxy}propyl)amine
分子量
Average: 316.42
Monoisotopic: 316.156911344
Monoisotopic: 316.156911344
CAS号
26839-75-8
ATC分类
C07A 未知;S01E 抗青光眼制剂及缩瞳药
药物类型
small molecule
阶段
approved
商品名
Apo-Timol;Apo-Timop;Aquanil;Betim;Betimol;Blocadren;Istalol;Novo-Timol;Nu-Timolol;Phoxal-timolol;Proflax;Temserin;Tenopt;Tim-AK;Timacar;Timacor;Timopic;Timoptic;Timoptic in Ocudose;Timoptic OcuDose;Timoptic-XE;Timoptol;
同义名
Timolol maleate;Timololum [INN-Latin];
基本介绍
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. [PubChem]
生产厂家
- Akorn inc
- Aton pharma inc
- Bausch and lomb inc
- Bausch and lomb pharmaceuticals inc
- E fougera div altana inc
- Falcon pharmaceuticals inc
- Falcon pharmaceuticals ltd
- Fdc ltd
- Hi tech pharmacal co inc
- Ista pharmaceuticals
- Merck research laboratories div merck co inc
- Mylan pharmaceuticals inc
- Novex pharma
- Pacific pharma
- Pacific pharma inc
- Quantum pharmics ltd
- Sandoz inc
- Santen oy
- Teva pharmaceuticals usa inc
- Usl pharma inc
- Watson laboratories inc
- Wockhardt ltd
封装厂家
- Akorn Inc.
- Alcon Laboratories
- Allergan Inc.
- Apotex Inc.
- A-S Medication Solutions LLC
- Aton Pharma Inc.
- Bausch & Lomb Inc.
- Dispensing Solutions
- E. Fougera and Co.
- Endo Pharmaceuticals Inc.
- Falcon Pharmaceuticals Ltd.
- Hi Tech Pharmacal Co. Inc.
- ISTA Pharmaceuticals
- Major Pharmaceuticals
- Medisca Inc.
- Merck & Co.
- Murfreesboro Pharmaceutical Nursing Supply
- Mylan
- Novex Pharma
- Novopharm Ltd.
- Pacific Pharma Lp
- Pack Pharmaceuticals
- Palmetto Pharmaceuticals Inc.
- PCAS Finland Oy
- Person & Covey
- Pharmedix
- Physicians Total Care Inc.
- Prasco Labs
- Qualitest
- Sandhills Packaging Inc.
- Sandoz
- Santen Inc.
- Vistakon Pharmaceuticals LLC
参考
| Synthesis Reference | Not Available |
| General Reference |
剂型
规格
化合物类型
| Type | small molecule |
| Classes | Not Available |
| Substructures | Not Available |
适应症
ANTIHYPERTENSIVES 降血压;
药理
| 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. |
| 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. |
| 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. |
| Absorption | Bioavailability is about 60% |
| Volume of distribution | Not Available |
| Protein binding | ~10% |
| Metabolism |
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 |
| Clearance | Not Available |
| 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 |
|
| Pathways | Not Available |
理化性质
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| State | solid | ||||||||||||||||||||||||||||||||||||||||||
| Experimental Properties |
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| Predicted Properties |
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药物相互作用
| Drug | Interaction |
|---|---|
| Acetohexamide | The beta-blocker, timolol, may decrease symptoms of hypoglycemia. |
| Aminophylline | Antagonism of action and increased effect of theophylline |
| Celecoxib | The NSAID, Celecoxib, may antagonize the antihypertensive effect of Timolol. |
| Chlorpropamide | The beta-blocker, timolol, may decrease symptoms of hypoglycemia. |
| Cimetidine | Cimetidine may increase the serum concentration of timolol by decreasing its metabolism. |
| Clonidine | Increased hypertension when clonidine stopped |
| Diclofenac | The NSAID, Diclofenac, may antagonize the antihypertensive effect of Timolol. |
| Diflunisal | The NSAID, Diflunisal, may antagonize the antihypertensive effect of Timolol. |
| Dihydroergotamine | Ischemia with risk of gangrene |
| Dihydroergotoxine | Ischemia with risk of gangrene |
| Diltiazem | Additive effects of decreased heart rate and contractility may occur. Increased risk of heart block. |
| Disopyramide | The beta-blocker, timolol, may increase the toxicity of disopyramide. |
| Dyphylline | Antagonism of action and increased effect of theophylline |
| Epinephrine | Hypertension, then bradycardia |
| Ergonovine | Ischemia with risk of gangrene |
| Ergotamine | Ischemia with risk of gangrene |
| Etodolac | The NSAID, Etodolac, may antagonize the antihypertensive effect of Timolol. |
| Fenoprofen | The NSAID, Fenoprofen, may antagonize the antihypertensive effect of Timolol. |
| Fenoterol | Antagonism |
| Flurbiprofen | The NSAID, Flurbiprofen, may antagonize the antihypertensive effect of Timolol. |
| Formoterol | Antagonism |
| Gliclazide | The beta-blocker, timolol, may decrease symptoms of hypoglycemia. |
| Glipizide | The beta-blocker, timolol, may decrease symptoms of hypoglycemia. |
| Glisoxepide | The beta-blocker, timolol, may decrease symptoms of hypoglycemia. |
| Glyburide | The beta-blocker, timolol, may decrease symptoms of hypoglycemia. |
| Glycodiazine | The beta-blocker, timolol, may decrease symptoms of hypoglycemia. |
| Indomethacin | Risk of inhibition of renal prostaglandins |
| Insulin Glargine | The beta-blocker, timolol, may decrease symptoms of hypoglycemia. |
| insulin inhaled | The beta-blocker, timolol, may decrease symptoms of hypoglycemia. |
| Isoproterenol | Antagonism |
| Ketoprofen | The NSAID, Ketoprofen, may antagonize the antihypertensive effect of Timolol. |
| Ketorolac | The NSAID, Ketorolac, may antagonize the antihypertensive effect of Timolol. |
| Lidocaine | The beta-blocker, timolol, may increase the effect and toxicity of lidocaine. |
| Lumiracoxib | The NSAID, Lumiracoxib, may antagonize the antihypertensive effect of Timolol. |
| Meclofenamic acid | The NSAID, Meclofenamate, may antagonize the antihypertensive effect of Timolol. |
| Meloxicam | The NSAID, Meloxicam, may antagonize the antihypertensive effect of Timolol. |
| Methyldopa | Possible hypertensive crisis |
| Methysergide | Ischemia with risk of gangrene |
| Nabumetone | The NSAID, Nabumetone, may antagonize the antihypertensive effect of Timolol. |
| Naproxen | The NSAID, Naproxen, may antagonize the antihypertensive effect of Timolol. |
| Orciprenaline | Antagonism |
| Oxaprozin | The NSAID, Oxaprozin, may antagonize the antihypertensive effect of Timolol. |
| Oxtriphylline | Antagonism of action and increased effect of theophylline |
| Pipobroman | Antagonism |
| Pirbuterol | Antagonism |
| Piroxicam | Risk of inhibition of renal prostaglandins |
| Prazosin | Risk of hypotension at the beginning of therapy |
| Procaterol | Antagonism |
| Repaglinide | The beta-blocker, timolol, may decrease symptoms of hypoglycemia. |
| Salbutamol | Antagonism |
| Salmeterol | Antagonism |
| Sulindac | The NSAID, Sulindac, may antagonize the antihypertensive effect of Timolol. |
| Terazosin | Increased risk of hypotension. Initiate concomitant therapy cautiously. |
| Terbinafine | Terbinafine may reduce the metabolism and clearance of Timolol. Consider alternate therapy or monitor for therapeutic/adverse effects of Amytriptyline if Timolol is initiated, discontinued or dose changed. |
| Terbutaline | Antagonism |
| Theophylline | Antagonism of action and increased effect of theophylline |
| Tiaprofenic acid | The NSAID, Tiaprofenic acid, may antagonize the antihypertensive effect of Timolol. |
| Tolazamide | The beta-blocker, timolol, may decrease symptoms of hypoglycemia. |
| Tolbutamide | The beta-blocker, timolol, may decrease symptoms of hypoglycemia. |
| Tolmetin | The NSAID, Tolmetin, may antagonize the antihypertensive effect of Timolol. |
| Treprostinil | Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use. |
| Verapamil | Additive effects of decreased heart rate and contractility may occur. Increased risk of heart block. |
食物相互作用
Not Available
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