26921-17-5 Usage
Description
(S)-Timolol maleate is the maleic acid salt of the active (S)-enantiomer of timolol, which is a non-selective β-adrenergic receptor antagonist. It is a white solid and has been found to be effective in blocking human β1-, β2-, and β3-adrenoceptors. The (S) enantiomer is responsible for the β-blocking effects of racemic timolol, while the (R) isomer contributes to maintaining a beneficial effect on intraocular pressure without causing bronchial constriction.
Uses
Used in Pharmaceutical Industry:
(S)-Timolol maleate is used as a beta-adrenergic blocker for treating conditions related to excessive sympathetic activity, such as hypertension and glaucoma. Its selective action on β-adrenergic receptors helps in reducing intraocular pressure and managing blood pressure.
Used in Ophthalmology:
(S)-Timolol maleate is used as an anti-glaucoma agent for reducing intraocular pressure in research models of ocular hypertension and glaucoma. It has been used alone and in fixed combinations with either prostaglandin analogs or carbonic anhydrase inhibitors to enhance its therapeutic effects.
Used in Cardiovascular Medicine:
(S)-Timolol maleate is used as an anti-hypertensive agent for managing high blood pressure. Its non-selective β-adrenergic receptor antagonist properties help in reducing the heart rate and myocardial contractility, thereby lowering blood pressure.
Biological Activity
β 1 -adrenergic blocker.
Clinical Use
Beta-adrenoceptor blocker: Hypertension Angina Glaucoma Migraine prophylaxis
Veterinary Drugs and Treatments
Timolol maleate is used primarily to prevent the development of
primary glaucoma in the contralateral eye of a dog which has developed
primary glaucoma in one eye. It only reduces intraocular
pressure 3 – 10 mmHg and, therefore is of minimal usefulness in
patients requiring treatment of primary acute congestive glaucoma.
Timolol’s mechanism of action: decreases cyclic-AMP synthesis in
non-pigmented ciliary epithelium resulting in decreased aqueous
humor production. It may also cause slight miosis in dogs and cats.
Timolol maleate is rarely used alone but is combined with dorzolamide
solution (Cosopt?). Caution is advised with use of Beta
blocking agents in cats with concurrent asthma. As timolol maleate
is now available in generic form, it is the primary Beta blocker agent
now used.
Drug interactions
Potentially hazardous interactions with other drugs
Anaesthetics: enhanced hypotensive effect.
Analgesics: NSAIDs antagonise hypotensive effect.
Anti-arrhythmics: increased risk of myocardial
depression and bradycardia; increased risk of
bradycardia, myocardial depression and AV block
with amiodarone; increased risk of myocardial
depression and bradycardia with flecainide.
Antidepressants: enhanced hypotensive effect with
MAOIs.
Antihypertensives: enhanced hypotensive effect;
increased risk of withdrawal hypertension with
clonidine; increased risk of first dose hypotensive
effect with post-synaptic alpha-blockers such as
prazosin.
Antimalarials: increased risk of bradycardia with
mefloquine.
Antipsychotics: enhanced hypotensive effect with
phenothiazines.
Calcium-channel blockers: increased risk of
bradycardia and AV block with diltiazem;
hypotension and heart failure possible with
nifedipine and nisoldipine; asystole, severe
hypotension and heart failure with verapamil.
Cytotoxics: possible increased risk of bradycardia
with crizotinib.
Diuretics: enhanced hypotensive effect.
Fingolimod: possibly increased risk of bradycardia.
Moxisylyte: possible severe postural hypotension.
Sympathomimetics: severe hypertension with
adrenaline and noradrenaline and possibly with
dobutamine; also response to adrenaline may be
reduced.
Metabolism
Timolol undergoes significant hepatic metabolism, but first pass metabolism is low. The metabolites are excreted in the urine with some unchanged timolol.
Check Digit Verification of cas no
The CAS Registry Mumber 26921-17-5 includes 8 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 5 digits, 2,6,9,2 and 1 respectively; the second part has 2 digits, 1 and 7 respectively.
Calculate Digit Verification of CAS Registry Number 26921-17:
(7*2)+(6*6)+(5*9)+(4*2)+(3*1)+(2*1)+(1*7)=115
115 % 10 = 5
So 26921-17-5 is a valid CAS Registry Number.
InChI:InChI=1/C13H24N4O3S.C4H4O4/c1-13(2,3)14-8-10(18)9-20-12-11(15-21-16-12)17-4-6-19-7-5-17;5-3(6)1-2-4(7)8/h10,14,18H,4-9H2,1-3H3;1-2H,(H,5,6)(H,7,8)/b;2-1+/t10-;/m1./s1
26921-17-5Relevant articles and documents
Substituted aromatic amino-alcohol compound, and preparation method and application thereof
-
Paragraph 0127-0131, (2019/01/05)
The invention relates to a compound of a formula (I) or pharmaceutically acceptable salts thereof. In the formula (I), Ar is an aryl, a heteroaryl or the aryl or the heteroaryl which is substituted byone or more of C1-C6 alkyl, halogen, hydroxyl, amido, sulfydryl, aryl or heterocyclyl; X is O, NH or S; R is C1-C4 fatty alkyl or the C1-C4 fatty alkyl which is substituted by halogen or phenyl; n equals to 1 to 3. The invention also provides a preparation method and application of the compound of the formula (I) or the pharmaceutically acceptable salts thereof. The compound provided by the invention can be used for treatment of hemangiomas or vascular malformations. (The formula (I) is shown in the description).
Novel methods and compounds employed therein
-
, (2008/06/13)
Preparation of an optically active alkamine in the sinister configuration, or a derivative of said alkamine, which is reacted with an 3-X-4-chloro(or RO-- where R is hydrogen or an alkali metal)-1,2,5-thiadiazole to prepare S-3-X-4-(3-substituted amino-2-hydroxypropoxy)-1,2,5-thiadiazole beta adrenergic blocking agents. Novel 3-morpholino-4-chloro(or RO--)-1,2,5-thiadiazoles and their preparation also are described.
