Timolol

What is Timolol

Timolol is a nonselective, beta-adrenergic receptor antagonist similar to propranolol and nadolol.

Timolol does not demonstrate appreciable intrinsic sympathomimetic or membrane-stabilizing activities.

Like propranolol, timolol possesses a relatively high degree of lipid solubility and is subject to first-pass metabolism by the liver.

Timolol is available as oral tablets (Blocadren) and in a variety of ophthalmic formulations.

Timolol maleate was first approved by the FDA for optical use in 1978, and for oral use in 1981.

The US patents for Timoptic ophthalmic solution (timolol maleate) and Timoptic-XE gel-forming ophthalmic drops expired on September 26, 1995 and September 25, 1996, respectively.

Betimol, an ophthalmic formulation of timolol hemihydrate, was approved in 1995; this product lacks an equivalent generic salt formulation.

Istalol, a once-daily timolol ophthalmic solution, was approved by the FDA on June 4, 2004.

Indications

  • angina
  • glaucoma
  • hypertension
  • migraine prophylaxis
  • myocardial infarction prophylaxis
  • ocular hypertension
  • reduction of cardiovascular mortality
  • tremor

Side Effects

  1. agranulocytosis
  2. alopecia
  3. anaphylactoid reactions
  4. angina
  5. angioedema
  6. arrhythmia exacerbation
  7. arthralgia
  8. asthenia
  9. AV block
  10. blurred vision
  11. bradycardia
  12. bronchospasm
  13. cardiac arrest
  14. chest pain (unspecified)
  15. confusion
  16. conjunctivitis
  17. cough
  18. depression
  19. diabetes mellitus
  20. diaphoresis
  21. diarrhea
  22. diplopia
  23. dizziness
  24. drowsiness
  25. dyspepsia
  26. dyspnea
  27. edema
  28. elevated hepatic enzymes
  29. emotional lability
  30. exfoliative dermatitis
  31. fatigue
  32. fever
  33. foreign body sensation
  34. hallucinations
  35. headache
  36. heart failure
  37. hepatomegaly
  38. hyperglycemia
  39. hyperhidrosis
  40. hypertension
  41. hypertriglyceridemia
  42. hypoglycemia
  43. hypotension
  44. impotence (erectile dysfunction)
  45. insomnia
  46. lacrimation
  47. laryngospasm
  48. libido decrease
  49. memory impairment
  50. musculoskeletal pain
  51. myalgia
  52. myasthenia
  53. nausea
  54. nightmares
  55. ocular discharge
  56. ocular irritation
  57. ocular pain
  58. ocular pruritus
  59. palpitations
  60. paresthesias
  61. pruritus
  62. psoriasis
  63. ptosis
  64. pulmonary edema
  65. purpura
  66. rash
  67. sinus tachycardia
  68. skin hyperpigmentation
  69. skin irritation
  70. syncope
  71. tremor
  72. urticaria
  73. vertigo
  74. vomiting
  75. weakness
  76. withdrawal
  77. xerosis

Monitoring Parameters

  • blood pressure
  • heart rate
  • intraocular pressure
  • ophthalmologic exam
  • serum creatinine/BUN

Contraindications

  • abrupt discontinuation
  • acute bronchospasm
  • asthma
  • AV block
  • beta-blocker hypersensitivity
  • bradycardia
  • breast-feeding
  • bronchitis
  • cardiogenic shock
  • cerebrovascular disease
  • children
  • chronic obstructive pulmonary disease (COPD)
  • contact lenses
  • depression
  • diabetes mellitus
  • dialysis
  • driving or operating machinery
  • emphysema
  • geriatric
  • heart failure
  • hepatic disease
  • hyperthyroidism
  • hypotension
  • infants
  • myasthenia gravis
  • neonates
  • peripheral vascular disease
  • pheochromocytoma
  • pregnancy
  • psoriasis
  • pulmonary disease
  • pulmonary edema
  • Raynaud’s phenomenon
  • renal disease
  • renal failure
  • renal impairment
  • sick sinus syndrome
  • surgery
  • thyroid disease
  • thyrotoxicosis
  • vasospastic angina
  • ventricular dysfunction

Interactions

  • Acetaminophen; Aspirin, ASA; Caffeine
  • Acetaminophen; Caffeine; Magnesium Salicylate; Phenyltoloxamine
  • Acetaminophen; Caffeine; Phenyltoloxamine; Salicylamide
  • Acetaminophen; Propoxyphene
  • Adenosine
  • Albiglutide
  • Aldesleukin, IL-2
  • Alemtuzumab
  • Alfentanil
  • Alfuzosin
  • Aliskiren; Amlodipine
  • Aliskiren; Amlodipine; Hydrochlorothiazide, HCTZ
  • Alogliptin; Metformin
  • Alpha-blockers
  • Alpha-glucosidase Inhibitors
  • Alprostadil
  • Amifostine
  • Amiodarone
  • Amlodipine
  • Amlodipine; Atorvastatin
  • Amlodipine; Benazepril
  • Amlodipine; Celecoxib
  • Amlodipine; Hydrochlorothiazide, HCTZ; Olmesartan
  • Amlodipine; Hydrochlorothiazide, HCTZ; Valsartan
  • Amlodipine; Olmesartan
  • Amlodipine; Telmisartan
  • Amlodipine; Valsartan
  • Amobarbital
  • Amyl Nitrite
  • Antithyroid agents
  • Apomorphine
  • Apraclonidine
  • Aripiprazole
  • Artemether; Lumefantrine
  • Articaine; Epinephrine
  • Asenapine
  • Aspirin, ASA
  • Aspirin, ASA; Butalbital; Caffeine
  • Aspirin, ASA; Butalbital; Caffeine; Codeine
  • Aspirin, ASA; Caffeine; Dihydrocodeine
  • Aspirin, ASA; Caffeine; Orphenadrine
  • Aspirin, ASA; Carisoprodol
  • Aspirin, ASA; Carisoprodol; Codeine
  • Aspirin, ASA; Citric Acid; Sodium Bicarbonate
  • Aspirin, ASA; Dipyridamole
  • Aspirin, ASA; Omeprazole
  • Aspirin, ASA; Oxycodone
  • Aspirin, ASA; Pravastatin
  • Atazanavir
  • Atazanavir; Cobicistat
  • Baclofen
  • Belladonna Alkaloids; Ergotamine; Phenobarbital
  • Beta-agonists
  • Bismuth Subsalicylate
  • Bismuth Subsalicylate; Metronidazole; Tetracycline
  • Bosentan
  • Bretylium
  • Brexpiprazole
  • Bupivacaine
  • Bupivacaine Liposomal
  • Bupivacaine; Lidocaine
  • Bupropion
  • Bupropion; Naltrexone
  • Cabergoline
  • Caffeine; Ergotamine
  • Canagliflozin; Metformin
  • Carbidopa; Levodopa
  • Carbidopa; Levodopa; Entacapone
  • Cariprazine
  • Ceritinib
  • Cevimeline
  • Chloroprocaine
  • Chlorthalidone; Clonidine
  • Choline Salicylate; Magnesium Salicylate
  • Cimetidine
  • Cinacalcet
  • Citalopram
  • Clevidipine
  • Clonidine
  • Clozapine
  • Co-Enzyme Q10, Ubiquinone
  • Cobicistat
  • Cocaine
  • Colesevelam
  • Conivaptan
  • Crizotinib
  • Dapagliflozin; Metformin
  • Darunavir
  • Darunavir; Cobicistat
  • Darunavir; Cobicistat; Emtricitabine; Tenofovir alafenamide
  • Dasabuvir; Ombitasvir; Paritaprevir; Ritonavir
  • Delavirdine
  • Desflurane
  • Dexmedetomidine
  • Dextromethorphan; Quinidine
  • Diazoxide
  • Digoxin
  • Dihydroergotamine
  • Diltiazem
  • Dipeptidyl Peptidase-4 Inhibitors
  • Dipyridamole
  • Disopyramide
  • Donepezil
  • Donepezil; Memantine
  • Doxazosin
  • Dronedarone
  • Dulaglutide
  • Duloxetine
  • Dutasteride; Tamsulosin
  • Eliglustat
  • Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Alafenamide
  • Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Disoproxil Fumarate
  • Empagliflozin; Linagliptin; Metformin
  • Empagliflozin; Metformin
  • Enalapril; Felodipine
  • Encainide
  • Enflurane
  • Epoprostenol
  • Ergonovine
  • Ergotamine
  • Ertugliflozin; Metformin
  • Escitalopram
  • Estradiol
  • Estradiol Cypionate; Medroxyprogesterone
  • Etomidate
  • Exenatide
  • Felodipine
  • Fingolimod
  • Fish Oil, Omega-3 Fatty Acids (Dietary Supplements)
  • Flecainide
  • Fluorescein
  • Fluoxetine
  • Fluoxetine; Olanzapine
  • food
  • Fospropofol
  • Galantamine
  • General anesthetics
  • Ginger, Zingiber officinale
  • Glipizide; Metformin
  • Glucagon
  • Glyburide; Metformin
  • Guanabenz
  • Guanfacine
  • Haloperidol
  • Halothane
  • Hydralazine; Isosorbide Dinitrate, ISDN
  • Icosapent ethyl
  • Iloperidone
  • Iloprost
  • Imatinib
  • Incretin Mimetics
  • Insulin Degludec; Liraglutide
  • Insulin Glargine; Lixisenatide
  • Insulins
  • Intravenous Lipid Emulsions
  • Iobenguane I 131
  • Isocarboxazid
  • Isoflurane
  • Isosorbide Dinitrate, ISDN
  • Isosorbide Mononitrate
  • Isradipine
  • Ivabradine
  • Ketamine
  • Lacosamide
  • Lanreotide
  • Lasmiditan
  • Levobupivacaine
  • Levodopa
  • Levothyroxine
  • Levothyroxine; Liothyronine (Porcine)
  • Levothyroxine; Liothyronine (Synthetic)
  • Lidocaine
  • Lidocaine; Prilocaine
  • Linagliptin; Metformin
  • Linezolid
  • Liothyronine
  • Liraglutide
  • Lithium
  • Lixisenatide
  • Lofexidine
  • Lopinavir; Ritonavir
  • Lovastatin; Niacin
  • Lurasidone
  • Magnesium Salicylate
  • Mefloquine
  • Meglitinides
  • Mephobarbital
  • Mepivacaine
  • Mepivacaine; Levonordefrin
  • Mestranol; Norethindrone
  • Metformin
  • Metformin; Pioglitazone
  • Metformin; Repaglinide
  • Metformin; Rosiglitazone
  • Metformin; Saxagliptin
  • Metformin; Sitagliptin
  • Methacholine
  • Methohexital
  • Methylergonovine
  • Methysergide
  • Milrinone
  • Mirabegron
  • Nefazodone
  • Nesiritide, BNP
  • Neuromuscular blockers
  • Niacin, Niacinamide
  • Niacin; Simvastatin
  • Nicardipine
  • Nifedipine
  • Nimodipine
  • Nisoldipine
  • Nitrates
  • Nitroglycerin
  • Nitroprusside
  • Non-Ionic Contrast Media
  • Nonsteroidal antiinflammatory drugs
  • Octreotide
  • Olanzapine
  • Ombitasvir; Paritaprevir; Ritonavir
  • Oritavancin
  • Oxymetazoline
  • Paliperidone
  • Paroxetine
  • Pasireotide
  • Peginterferon Alfa-2b
  • Pentoxifylline
  • Perindopril; Amlodipine
  • Phenelzine
  • Phenothiazines
  • Phenoxybenzamine
  • Phentolamine
  • Pilocarpine
  • Pramlintide
  • Prazosin
  • Prilocaine
  • Prilocaine; Epinephrine
  • Procainamide
  • Procaine
  • Propafenone
  • Propofol
  • Propoxyphene
  • Quinidine
  • Quinine
  • Ranolazine
  • Rasagiline
  • Remifentanil
  • Reserpine
  • Risperidone
  • Ritonavir
  • Rivastigmine
  • Rolapitant
  • Ropivacaine
  • Salsalate
  • Selegiline
  • Semaglutide
  • Sevoflurane
  • SGLT2 Inhibitors
  • Silodosin
  • Siponimod
  • Sufentanil
  • Sulfonylureas
  • Sympathomimetics
  • Tacrine
  • Tamsulosin
  • Tasimelteon
  • Terazosin
  • Tetrabenazine
  • Tetracaine
  • Thalidomide
  • Thiazolidinediones
  • Thiopental
  • Thyroid hormones
  • Tizanidine
  • Trandolapril; Verapamil
  • Tranylcypromine
  • Trazodone
  • Vemurafenib
  • Verapamil
  • Yohimbine
  • Ziprasidone
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