III. Mechanism

  1. Nonselective Beta Blocker (Beta-1 and Beta-2 Adrenergic Blockade)

IV. Dosing

  1. Start 10 mg orally twice daily
  2. Target 20-40 mg/day divided twice daily
  3. Maximum 60 mg/day

V. Pharmacokintics

  1. Mildly lipophilic
  2. Moderate first pass liver metabolism
  3. Hepatic elimination
  4. CYP2D6 metabolism

VI. Adverse Effects

VII. Safety

  1. Pregnancy Category C
  2. Safe in Lactation

IX. References

  1. (2019) Presc Lett, Resource #350503, Comparison of Oral Beta Blockers
  2. (2020) Med Lett Drugs Ther 62(1598): 73-80
  3. Olson (2020) Clinical Pharmacology, Medmaster Miami, p. 66-7
  4. Hamilton (2020) Tarascon Pocket Pharmacopoeia

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Related Studies

Cost: Medications

timolol (on 11/23/2022 at Medicaid.Gov Survey of pharmacy drug pricing)
TIMOLOL 0.5% EYE DROP Generic $26.42 per ml
TIMOLOL 0.5% GEL-SOLUTION Generic $30.70 per ml
TIMOLOL 0.5% GFS GEL-SOLUTION Generic $30.18 per ml
TIMOLOL MALEATE 0.25% EYE DROP Generic $0.69 per ml
TIMOLOL MALEATE 0.5% EYE DROP Generic $4.67 each
TIMOLOL MALEATE 0.5% EYE DROPS Generic $1.15 per ml

Ontology: Blocadren (C0005763)

Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH D013999
English 2-Propanol, 1-((1,1-dimethylethyl)amino)-3-((4-(4-morpholinyl)-1,2,5-thiadiazol-3-yl)oxy)-, hemihydrate, (S)-, Blocadren

Ontology: Timolol (C0040233)

Definition (NCI) A propanolamine derivative and a non-selective beta-adrenergic antagonist with antihypertensive property. Timolol competitively binds to beta-1-adrenergic receptors in the heart and vascular smooth muscle and beta-2-receptors in the bronchial and vascular smooth muscle, resulting in a decrease in beta-adrenergic stimulation. 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 ultimate results include vasodilation, and negative chronotropic and inotropic cardiac effects. In addition, timolol reduces intra-ocular pressure possibly by decreasing aqueous humor production by reduction of blood flow to the ciliary processes and cAMP synthesis.
Definition (MSH) 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.
Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH D013999
SnomedCT 372880004, 85591001
LNC LP16293-0, MTHU018379, LA14716-7
English Timolol, (S)-1-((1,1-Dimethylethyl)amino)-3-((4-(4-morpholinyl)-1,2,5-thiadazol-3-yl)oxy)-2-propanol, 2-Propanol, 1-((1,1-dimethylethyl)amino)-3-((4-(4-morpholinyl)-1,2,5-thiadiazol-3-yl)oxy)-, (S)-, (S)-1-(tert-Butylamino)-3-((4-morpholino-1,2,5-thiadiazol-3-yl)oxy)propan-2-ol, timolol (ophthalmic) (medication), timolol (medication), timolol (ophthalmic), Timolol, Ophthalmic, timolol ophthalmic, timolol, Timolol [Chemical/Ingredient], TIMOLOL, Timolol (product), Timolol (substance)
Swedish Timolol
Czech timolol
Finnish Timololi
Russian TIMOLOL, ТИМОЛОЛ
Japanese チモレート, チマバック, ファルチモ, ブルンネ, チモプトール, マレイン酸チモロール, リズモン, チアブート, チモロールT, チモロール
Polish Timolol
Spanish timolol (producto), timolol (sustancia), timolol, Timolol
French Timolol
German Timolol
Italian Timololo
Portuguese Timolol