Absorption, Distribution and Excretion
80% Metabolism/Metabolites Liver Biological Half-Life 20 hours

Effects During Pregnancy and Lactation
◉ Overview of Use During Lactation
Based on its physicochemical properties and ocular route of administration, zobuprofen appears to pose a low risk to breastfed infants. Some guidelines indicate that gel formulations are preferred over solution formulations. After using eye drops, to significantly reduce the amount of medication entering breast milk, press the tear duct at the corner of the eye for at least 1 minute, then blot away any excess medication with absorbent paper. ◉ Effects on Breastfed Infants
A study of mothers taking beta-blockers while breastfeeding found a numerically increased number of adverse events in mothers taking any beta-blocker, but this was not statistically significant. Although the infants were age-matched to control infants, the age of affected infants was not specified. None of the mothers were taking zobuprofen. ◉ Effects on Lactation and Breast Milk
As of the revision date, no published information was found regarding the effects of beta-blockers or zobuprofen during normal breastfeeding. A study of six patients with hyperprolactinemia and galactorrhea found that serum prolactin levels did not change after β-adrenergic blockade with propranolol.

[1]. Injectable drug depot engineered to release multiple ophthalmic therapeutic agents with precise time profiles for postoperative treatment following ocular surgery. Acta Biomater. 2018 Jun;73:90-102.

[2]. Extended levobunolol release from Eudragit nanoparticle-laden contact lenses for glaucoma therapy. Futur J Pharm Sci 6, 109 (2020).

[3]. Superior oblique myokymia treated with levobunolol. J AAPOS. 2018 Feb;22(1):67-69.e2.

Levobunolol is a cyclic ketone with the structure 3,4-dihydronaphthyl-1-one, substituted at position 5 with 3-(tert-butylamino)-2-hydroxypropoxy (S-enantiomer). It is a non-selective β-adrenergic receptor antagonist (in its hydrochloride form) used to treat glaucoma. It is both an anti-glaucoma drug and a β-adrenergic receptor antagonist. It is a propanolamine, cyclic ketone, and aromatic ether. It is the conjugate acid of Levobunolol (1+). It is derived from the hydride of tetrahydronaphthyl.
A non-selective β-adrenergic receptor antagonist used to treat glaucoma.
Levobunolol is a β-adrenergic blocker. The mechanism of action of Levobunolol is as a β-adrenergic receptor antagonist.
Levobunolol is a naphthone-type non-selective β-adrenergic receptor antagonist with anti-glaucoma activity. After instillation, levobenolol blocks β-adrenergic receptors, thereby causing vasoconstriction. Levobunolol also reduces the production of aqueous humor in the ciliary body, thus decreasing the amount of aqueous humor.
Levobunolol isoform.
See also: Levobunolol hydrochloride (salt form).

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Drug Indications
For the reduction of intraocular pressure (IOP), it can be used to treat patients with chronic open-angle glaucoma or high intraocular pressure.
FDA Label

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Mechanism of Action
The mechanism of action of levobenolol in reducing intraocular pressure is not fully understood, but it is believed to reduce aqueous humor production by blocking the increase in intraocular cyclic adenosine monophosphate (cAMP) concentration stimulated by endogenous catecholamines.

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Pharmacodynamics
Levobunolol is an ophthalmic β-receptor blocker that is effective against both β(1)- and β2 receptors. Levobunolol acts on the β2 receptor site. Regardless of whether a patient has glaucoma, levobenolol can lower intraocular pressure (IOP) to normal or normal levels. In patients with elevated IOP, levobenolol can reduce mean IOP by approximately 25-40% from baseline. Because this drug is a non-selective beta-adrenergic blocker, topical application to the eye can produce systemic pulmonary and cardiovascular effects. These effects include pulmonary adverse reactions (such as bronchoconstriction and increased airway resistance) as well as decreased blood pressure and heart rate.

C17H25NO3.HCL

327.84624

327.16

27912-14-7

Levobunolol;47141-42-4

39468

White to off-white solid powder

464.4ºC at 760mmHg

209-211°

234.7ºC

2.01E-09mmHg at 25°C

3.526

2

4

6

21

350

1

O=C1CCCC2=C1C=CC=C2OC[C@@H](O)CNC(C)(C)C.[H]Cl

IXHBTMCLRNMKHZ-LBPRGKRZSA-N

InChI=1S/C17H25NO3/c1-17(2,3)18-10-12(19)11-21-16-9-5-6-13-14(16)7-4-8-15(13)20/h5-6,9,12,18-19H,4,7-8,10-11H2,1-3H3/t12-/m0/s1

5-[(2S)-3-(tert-butylamino)-2-hydroxypropoxy]-3,4-dihydro-2H-naphthalen-1-one

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

DMSO : ≥ 62.5 mg/mL (~190.64 mM)
H2O : ~50 mg/mL (~152.51 mM)

Solubility in Formulation 1: ≥ 2.08 mg/mL (6.34 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

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Solubility in Formulation 2: ≥ 2.08 mg/mL (6.34 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.08 mg/mL (6.34 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

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Solubility in Formulation 4: 50 mg/mL (152.51 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication.

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 (Please use freshly prepared in vivo formulations for optimal results.)