Timolol

Brand names: Betimol®Blocadren®Istalol™Timoptic® in Ocudose®Timoptic® OcumeterTimoptic-XE®

Chemical formula:

Drug Forms:
• Timolol tablets (below)
• Timolol eye solution or eye gel-forming solution
• Timolol Maleate Ophthalmic drops, solution
• Timolol Maleate Oral tablet
• Timolol Hemihydrate Ophthalmic drops, solution
• Timolol Maleate Ophthalmic gel forming solution
• Timolol Maleate Ophthalmic gel forming solution ER

Español:
• Tabletas de timolol
• Solución ocular formadora de gel o solución ocular de timolol
• Maleato de timolol, Solución para gotas oftámicas
• Maleato de timolol, Tableta oral
• Hemihidrato de timolol, Solución para gotas oftámicas
• Maleato de timolol, Solución oftálmica formadora de gel
• Maleato De Timolol, Gel oftálmico que forma solución ER

Timolol tablets

What are timolol tablets?

TIMOLOL (Blocadren®) belongs to a group of medicines called beta-blockers. Beta-blockers reduce the workload on the heart and help it to beat more regularly. Timolol controls, but does not cure, high blood pressure (hypertension). High blood pressure may not make you feel sick, but it can lead to serious heart problems. Timolol can be used to improve symptoms in patients with heart disease. It is sometimes given after a heart attack to reduce heart-related adverse events. Timolol is also used to prevent migraine headaches. Generic timolol tablets are available.

What should I tell my health care provider before I take this medicine?

They need to know if you have any of these conditions:
• angina (chest pain)
• asthma, bronchitis or bronchospasm
• circulation problems, or blood vessel disease (such as Raynaud's disease)
• depression
• diabetes
• emphysema, or other lung disease
• history of heart attack or heart failure
• kidney disease
• liver disease
• low blood pressure
• muscle weakness or disease
• pheochromocytoma
• psoriasis
• thyroid disease
• an unusual or allergic reaction to timolol, other beta-blockers, medicines, foods, dyes, or preservatives
• pregnant or trying to get pregnant
• breast-feeding

How should I take this medicine?

Take timolol tablets by mouth. Follow the directions on the prescription label. Swallow the tablets with a drink of water. Take your doses at regular intervals. Do not take your medicine more often than directed. Do not stop taking except on your prescriber's advice.

This medicine is not for use in children.

What if I miss a dose?

What drug(s) may interact with timolol?

• antiinflammatory drugs (NSAIDs, such as ibuprofen)
• atropine
• cimetidine
• clonidine
• cocaine
• ergotamine
• hawthorn
• levodopa
• medicines for high blood pressure
• medicines for colds and breathing difficulties
• medicines for diabetes
• medicines for mental depression
• medicines for mental problems and psychotic disturbances
• medicines to control heart rhythm
• monoamine oxidase inhibitors (Azilect®, Eldepryl®, Emsam®, Marplan®, Nardil®, Parnate®, Zelapar™)
• theophylline
• water pills

Tell your prescriber or health care professional about all other medicines you are taking, including nonprescription medicines, nutritional supplements, or herbal products. Also tell your prescriber or health care professional if you are a frequent user of drinks with caffeine or alcohol, if you smoke, or if you use illegal drugs. These may affect the way your medicine works. Check with your health care professional before stopping or starting any of your medicines.

What should I watch for while taking timolol?

Check your heart rate and blood pressure regularly while you are taking timolol. Ask your prescriber or health care professional what your heart rate and blood pressure should be while taking this drug.

Do not stop taking this medicine suddenly. This could lead to serious heart-related effects.

You may get drowsy or dizzy. Do not drive, use machinery, or do anything that requires mental alertness until you know how timolol affects you. To reduce the risk of dizzy or fainting spells, do not sit or stand up quickly. Alcohol can make you more drowsy, and increase flushing and rapid heartbeats. Therefore, it is best to avoid alcoholic drinks.

Timolol can affect blood sugar levels. If you have diabetes, check with your prescriber or health care professional before you change your diet or the dose of your diabetic medicine.

If you are going to have surgery, tell your prescriber or health care professional that you are taking timolol.

What side effects may I notice from taking timolol?

Side effects that you should report to your prescriber or health care professional as soon as possible:
• changes in blood sugar
• cold hands or feet
• confusion, hallucinations (seeing and hearing things that are not really there)
• difficulty breathing, wheezing
• difficulty sleeping, nightmares
• dizziness or fainting spells
• irregular heartbeat, palpitations, chest pain
• skin rash, itching, peeling skin
• slow heart rate (less than 50 beats per minute)
• swelling of the legs or ankles
• vomiting

Side effects that usually do not require medical attention (report to your prescriber or health care professional if they continue or are bothersome):
• dark colored skin
• diarrhea
• dry sore eyes
• hair loss
• nausea
• sexual difficulties (impotence or decreased sexual urges)
• weakness or tiredness

Where can I keep my medicine?

Keep out of the reach of children in a container that small children cannot open.

Store at room temperature between 15 and 30 degrees C (59 and 86 degrees F). Protect from light. Keep container tightly closed. Throw away any unused medicine after the expiration date.

Last updated: 8/5/2003 1:37:00 PM

Important Disclaimer: The drug information provided here is for educational purposes only. It is intended to supplement, not substitute for, the diagnosis, treatment and advice of a medical professional. This drug information does not cover all possible uses, precautions, side effects and interactions. It should not be construed to indicate that this or any drug is safe for you. Consult your medical professional for guidance before using any prescription or over the counter drugs.

A β-adrenergic blocking agent with antihypertensive and antiarrhythmic properties. Also used to decrease aqueous production in the management of glaucoma.

The noun has one meaning:

Meaning #1: a beta blocker (trade name Blocadren) administered after heart attacks
  Synonym: Blocadren

Timolol
Systematic (IUPAC) name
(S)-1-(tert-butylamino)-3-[(4-morpholin-4-yl-1,2,5-thiadiazol-3-yl)oxy]propan-2-ol
Identifiers
CAS number	26839-75-8
ATC code	C07AA06
PubChem	5478
DrugBank	APRD00229
Chemical data
Formula	C13H24N4O3S
Mol. mass	316.421 g/mol
SMILES	eMolecules & PubChem
Pharmacokinetic data
Bioavailability	60%
Metabolism	Hepatic: 80%
Half life	2.5-5 hours
Excretion	Renal
Therapeutic considerations
Pregnancy cat.	C(AU) C(US)
Legal status	℞ Prescription only
Routes	oral, Ophthalmic
Y(what is this?)  (verify)

Timolol maleate is a non-selective beta-adrenergic receptor blocker. In its oral form (Blocadren), it is used to treat high blood pressure and prevent heart attacks, and occasionally to prevent migraine headaches. In its ophthalmic form (brand names Timoptol in Italy; Timoptic), it is used to treat open-angle and occasionally secondary glaucoma by reducing aqueous humour production through blockage of the beta receptors on the ciliary epithelium. The pharmacological mechanism by which it actually does this is still unknown.

Contents 1 Side effects 2 Usual dosage 3 Formulations 4 Brand names

Side effects

The most serious possible side effects include cardiac arrhythmias and severe bronchospasms. Timolol can also lead to fainting, congestive heart failure, depression, confusion, worsening of Raynaud's syndrome and impotence.

Usual dosage

• Children and Adults: Ophthalmic: Initial: 0.25% solution, instill 1 drop twice daily; increase to 0.5% solution if response not adequate; decrease to 1 drop/day if *controlled; do not exceed 1 drop twice daily of 0.5% solution Adults: Oral:
• Hypertension: Initial: 10 mg twice daily, increase gradually every 7 days, usual dosage: 20-40 mg/day in 2 divided doses; maximum: 60 mg/day
• Prevention of myocardial infarction: 10 mg twice daily initiated within 1-4 weeks after infarction
• Migraine headache: Initial: 10 mg twice daily, increase to maximum of 30 mg/day

Formulations

• Gel-forming solution, ophthalmic, as maleate (Timoptic-XE): 0.25% (2.5 mL, 5 mL); 0.5% (2.5 mL, 5 mL)
• Solution, ophthalmic, as hemihydrate (Betimol): 0.25% (5 mL, 10 mL, 15 mL); 0.5% (5 mL, 10 mL, 15 mL) [contains benzalkonium chloride]
• Solution, ophthalmic, as maleate: 0.25% (5 mL, 10 mL, 15 mL); 0.5% (5 mL, 10 mL, 15 mL) [contains benzalkonium chloride]
• Timoptic: 0.25% (5 mL, 10 mL); 0.5% (5 mL, 10 mL) [contains benzalkonium chloride]
• Solution, ophthalmic, as maleate [preservative free] (Timoptic OcuDose): 0.25% (0.2 mL);0.5% (0.2 mL) [single use]
• Tablet, as maleate (Blocadren): 5 mg, 10 mg, 20 mg

For ophthalmic use, timolol is also available combined with other medications:

• Combigan - timolol and brimonidine
• Cosopt - timolol maleate and dorzolamide hydrochloride
• DuoTrav - timolol and travoprost

Brand names

• In Canada: Apo-Timol, Apo-Timop, Gen-Timolol, Nu-Timolol, Phoxal-timolol, PMS-Timolol, Tim-AK, Timoptic, Timoptic-XE.
• In United States: Betimol, Blocadren, Istalol, Timoptic, Timoptic-XE, Timoptic OcuDose.

v • d • e Adrenergics Receptor Ligands α α1 Agonists: Amidephrine • Cirazoline • Dopamine • Epinephrine (Adrenaline) • Etilefrine • Isoprenaline • Levonordefrin • Metaraminol • Methoxamine • Methyldopa • Norepinephrine (Noradrenaline) • Oxymetazoline • Phenylephrine Antagonists: Alfuzosin • Arotinolol • Carvedilol • Doxazosin • Indoramin • L-765,314 • Labetalol • Moxisylyte • Nantenine • Phentolamine • Phenoxybenzamine • Prazosin • Silodosin • Tamsulosin • Terazosin • Tolazoline • Trimazosin • Urapidil α2 Agonists: (R)-3-Nitrobiphenyline • 4-NEMD • Amitraz • Apraclonidine • Brimonidine • Clonidine • Detomidine • Dexmedetomidine • Dopamine • Epinephrine (Adrenaline) • Etilefrine • Guanabenz • Guanfacine • Guanethidine • Guanoxabenz • Levonordefrin • Lofexidine • Medetomidine • Methyldopa • Norepinephrine (Noradrenaline) • Octopamine • Romifidine • Tizanidine • Tolonidine • Xylazine • Xylometazoline Antagonists: 1-PP • Atipamezole • BRL-44408 • Buspirone • Cirazoline • Efaroxan • Gepirone • Idazoxan • Ipsapirone • Mianserin • Mirtazapine • NAN-190 • Phentolamine • Phenoxybenzamine • Rauwolscine • SB-269,970 • Setiptiline • Spiroxatrine • Tandospirone • Tolazoline • Yohimbine α? Agonists: Anisodamine • Ephedrine • Ergotamine • Indanidine • Mephentermine • Midodrine • Mivazerol • Naphazoline • Phenylpropanolamine • Pseudoephedrine • Rilmenidine • Synephrine • Talipexole • Tetrahydrozoline β β1 Agonists: Denopamine • Dobutamine • Dopamine • Epinephrine (Adrenaline) • Etilefrine • Levonordefrin • Methyldopa • Norepinephrine (Noradrenaline) Antagonists: Acebutolol • Alprenolol • Amosulalol • Arotinolol • Atenolol • Bupranolol • Carvedilol • Celiprolol • Betaxolol • Bisoprolol • Dichloroisoprenaline • Esmolol • Labetalol • Metipranolol • Metoprolol • Nadolol • Nebivolol • Oxprenolol • Penbutolol • Pindolol • Practolol • Pronethalol • Propranolol • Sotalol • Tertatolol • Timolol • Tilisolol • Xamoterol β2 Agonists: Arformoterol • Bambuterol • Bitolterol • Carbuterol • Clenbuterol • Dopamine • Dopexamine • Epinephrine (Adrenaline) • Etilefrine • Fenoterol • Formoterol • Hexoprenaline • Indacaterol • Levonordefrin • Levosalbutamol • Methyldopa • Norepinephrine (Noradrenaline) • Orciprenaline • Pirbuterol • Procaterol • Reproterol • Rimiterol • Ritodrine • Salbutamol • Salmeterol • Terbutaline • Tulobuterol Antagonists: Alprenolol • Amosulalol • Arotinolol • Bupranolol • Butaxamine • Carvedilol • Dichloroisoprenaline • ICI 118551 • Labetalol • Metipranolol • Nadolol • Oxprenolol • Penbutolol • Pindolol • Pronethalol • Propranolol • Sotalol • Tertatolol • Timolol • Tilisolol β3 Agonists: Amibegron • Arotinolol • Dopamine • Epinephrine (Adrenaline) • Etilefrine • Labetalol • Levonordefrin • Methyldopa • Norepinephrine (Noradrenaline) • Solabegron Antagonists: Carvedilol • SR 59230A β? Agonists: Arbutamine • BAAM • Befunolol • Broxaterol • Buphenine • Cimaterol • Ephedrine • Higenamine • Isoetarine • Isoxsuprine • Mabuterol • Methoxyphenamine • Oxyfedrine • Prenalterol • Pseudoephedrine • Ractopamine • Tretoquinol • Zilpaterol • Zinterol Reuptake Inhibitors Plasmalemmal NET Inhibitors Norepinephrine Reuptake Inhibitors: Atomoxetine (Tomoxetine) • Ciclazindol • Mazindol • Nisoxetine • Reboxetine • Tandamine • Tapentadol • Viloxazine; Norepinephrine-Dopamine Reuptake Inhibitors: Amineptine • Bupropion (Amfebutamone) • Fencamine • Fencamfamine • Lefetamine • LR-5182 • Manifaxine • Methylphenidate • Nomifensine • O-2172 • Radafaxine; Serotonin-Norepinephrine Reuptake Inhibitors: Bicifadine • Desvenlafaxine • Duloxetine • Milnacipran • Sibutramine • Tramadol • Venlafaxine; Serotonin-Norepinephrine-Dopamine Reuptake Inhibitors: Brasofensine • Diclofensine • DOV-102,677 • DOV-21,947 • DOV-216,303 • JNJ-7925476 • JZ-IV-10 • Methylnaphthidate • Naphyrone • NS-2359 • PRC200-SS • SEP-225,289 • SEP-227,162 • Tesofensine; Tricyclic Antidepressants: Amitriptyline • Butriptyline • Cianopramine • Clomipramine • Desipramine • Dosulepin • Doxepin • Imipramine • Lofepramine • Nortriptyline • Protriptyline • Trimipramine; Tetracyclic Antidepressants: Amoxapine • Maprotiline • Mianserin • Oxaprotiline; Others: Cocaine • Nefazodone • Nefopam • Ziprasidone TRPC6 Activators Adhyperforin • Hyperforin Vesicular VMAT Inhibitors Ibogaine • Reserpine • Tetrabenazine Releasing Agents Oxazolines: 4-Methylaminorex (4-MAR, 4-MAX) • Aminorex • Clominorex • Cyclazodone • Fenozolone • Fluminorex • Pemoline • Thozalinone; Phenethylamines (also Amphetamines, Cathinones, Phentermines, etc): 2-Hydroxyphenethylamine (2-OH-PEA) • 4-Methylamphetamine (4-MA) • 4-Methylmethamphetamine (4-MMA) • α-Ethylphenethylamine (α-Et-PEA) • Alfetamine • Amphetamine (Dextroamphetamine, Levoamphetamine) • Amphetaminil • Amfepentorex • β-Methylphenethylamine (β-Me-PEA) • Benzodioxolylbutanamine (BDB) • Benzodioxolylhydroxybutanamine (BOH) • Benzphetamine • Buphedrone • Butylone • Cathine • Cathinone • Clobenzorex • Clortermine • Diethylcathinone (Diethylpropion, Amfepramone) • Dibutylone • Dimethoxyamphetamine (DMA) • Dimethoxymethamphetamine (DMMA) • Dimethylamphetamine • Dimethylcathinone (Dimethylpropion, Metamfepramone) • Ephedrine (EPH) • Ethcathinone (Ethylpropion) • Ethylamphetamine • Ethylbenzodioxolylbutanamine (EBDB) • Ethylone • Fenethylline • Fenproporex • Flephedrone • Fludorex • Furfenorex • Hordenine • Indanorex • Indanylamphetamine (IAP) • Lisdexamfetamine • Lophophine (Homomyristicylamine) • Mefenorex • Mephedrone • Mephentermine • Methamphetamine (Desoxyephedrine, Methedrine; Dextromethamphetamine, Levomethamphetamine) • Methcathinone (Methylpropion) • Methedrone • Methoxymethylenedioxyamphetamine (MMDA) • Methoxymethylenedioxymethamphetamine (MMDMA) • Methylbenzodioxolylbutanamine (MBDB) • Methylenedioxyamphetamine (MDA; Tenamfetamine) • Methylenedioxyethylamphetamine (MDEA) • Methylenedioxyhydroxyamphetamine (MDOH) • Methylenedioxymethamphetamine (MDMA) • Methylenedioxymethylphenethylamine (MDMPEA; Homarylamine) • Methylenedioxyphenethylamine (MDPEA; Homopiperonylamine) • Methylone • Naphthylamphetamine (NAP) • Ortetamine • Oxaflozane • Parabromoamphetamine (PBA) • Parachloroamphetamine (PCA) • Parafluoroamphetamine (PFA) • Parafluoromethamphetamine (PFMA) • Parahydroxyamphetamine (PHA) • Paraiodoamphetamine (PIA) • Paramethoxyamphetamine (PMA) • Paramethoxyethylamphetamine (PMEA) • Paramethoxymethamphetamine (PMMA) • Paredrine (Norpholedrine, Oxamphetamine) • Phendimetrazine • Phenethylamine (PEA) • Phenmetrazine • Pholedrine • Phenpentermine • Phenpromethamine • Phentermine • Phenylpropanolamine (PPA) • Propylamphetamine • Pseudoephedrine (PSE) • Tiflorex (Flutiorex) • Tyramine (TRA) • Xylopropamine • Zylofuramine; Piperazines: 2,5-Dimethoxy-4-bromobenzylpiperazine (2C-B-BZP) • Benzylpiperazine (BZP) • Methoxyphenylpiperazine (MeOPP; Paraperazine) • Methylbenzylpiperazine (MBZP) • Methylenedioxybenzylpiperazine (MDBZP; Piperonylpiperazine) • Parafluorophenylpiperazine (pFPP; Fluoperazine); Others: 2-Aminoindane (2-AI) • 2-Aminotetralin (2-AT) • 2-Benzylpiperidine (2-BP) • 4-Benzylpiperidine (4-BP) • Clofenciclan • Cyclopentamine • Cypenamine • Cyprodenate • Feprosidnine • Gilutensin • Heptaminol • Hexacyclonate • Isometheptene • Methylhexanamine • Octodrine • Phthalimidopropiophenone • Propylhexedrine (PHX) • Tuaminoheptane (Tuamine) Enzyme Inhibitors Anabolism PAH Inhibitors 3,4-Dihydroxystyrene TH Inhibitors 3-Iodotyrosine • Aquayamycin • Bulbocapnine • Metirosine • Oudenone AAAD Inhibitors Benserazide • Carbidopa DBH Inhibitors Disulfiram • Nepicastat • Tropolone PNMT Inhibitors CGS-19281A • SKF-64139 • SKF-7698 Catabolism MAO Inhibitors Nonselective: Iproclozide • Iproniazid • Isocarboxazid • Nialamide • Phenelzine • Pheniprazine • Tranylcypromine; MAO-A Selective: Befloxatone • Brofaromine • Cimoxatone • Clorgiline • Harmala Alkaloids • Minaprine • Moclobemide • Pirlindole • Toloxatone • Tyrima; MAO-B Selective: Lazabemide • Pargyline • Rasagiline • Selegiline * Note that MAO-B inhibitors also influence norepinephrine/epinephrine levels since they inhibit the breakdown of their precursor dopamine. COMT Inhibitors Entacapone • Tolcapone Others Precursors L-Phenylalanine → L-Tyrosine → L-DOPA (Levodopa) → Dopamine • L-DOPS (Droxidopa) Cofactors Ferrous Iron (Fe2+) • S-Adenosyl-L-Methionine • Vitamin B3 (Niacin, Nicotinamide → NADPH) • Vitamin B6 (Pyridoxine, Pyridoxamine, Pyridoxal → Pyridoxal Phosphate) • Vitamin B9 (Folic Acid → Tetrahydrofolic Acid) • Vitamin C (Ascorbic Acid) • Zinc (Zn2+) Others Activity Enhancers: Benzofuranylpropylaminopentane (BPAP) • Phenylpropylaminopentane (PPAP); Release Blockers: Bretylium • Guanethidine

v • d • e Ophthalmologicals: antiglaucoma preparations and miotics (S01E) Sympathomimetics Apraclonidine • Brimonidine • Clonidine • Dipivefrine • Epinephrine Parasympathomimetics muscarinic Aceclidine • Pilocarpine muscarinic/nicotinic Acetylcholine • Carbachol Acetylcholinesterase inhibitors Demecarium • Ecothiopate • Stigmine (Fluostigmine, Neostigmine, Physostigmine) • Paraoxon Carbonic anhydrase inhibitors/ (sulfonamides) Acetazolamide • Brinzolamide • Diclofenamide • Dorzolamide • Methazolamide Beta blocking agents Befunolol • Betaxolol • Carteolol • Levobunolol • Metipranolol • Timolol Prostaglandin analogues (F2α) Bimatoprost • Latanoprost • Tafluprost • Travoprost • Unoprostone Other agents Dapiprazole • Guanethidine

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