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Cardiovascular Drugs during Pregnancy
Published in “Bert” Bertis Britt Little, Drugs and Pregnancy, 2022
Timolol is a beta-blocker used to treat hypertension, migraine headaches, and glaucoma (topical). Published reports of timolol in human pregnancy is limited to three case reports. Only 10 infants were exposed to timolol in the first trimester in the Swedish Birth Defects Registry (Kallen, 2019). In animal studies of timolol in pregnant rats, rabbits and mice, the frequency of birth defects was not increased at 40 times the usual human dose; however, the rate of pregnancy loss was increased.
Drug side effects on the distal phalanx
Published in Robert Baran, Dimitris Rigopoulos, Chander Grover, Eckart Haneke, Nail Therapies, 2021
Paronychia and periungual pyogenic granulomas represent one of the most common and bothersome dermatologic toxicities observed with ErbB inhibitors. With the use of topical propanolol or of timolol, nearly two-thirds of patients showed at least a partial response after 1 month of therapy (Sibaud et al. 2019).
Timolol
Published in Anton C. de Groot, Monographs in Contact Allergy, 2021
Timolol is a propanolamine derivative and a non-selective β-adrenergic antagonist with antihypertensive property. It competitively binds to β1-adrenergic receptors in the heart and vascular smooth muscle and β2-receptors in the bronchial and vascular smooth muscle, resulting in a decrease in β-adrenergic stimulation. This leads to a decrease in resting and exercise heart rate and cardiac output, and a decrease in both systolic and diastolic blood pressure. β2- 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 from reduction of blood flow to the ciliary processes and reduced cAMP synthesis. The oral form of timolol is used to treat high blood pressure and prevent heart attacks, and occasionally to prevent migraine headaches. Ophthalmic timolol is indicated for the treatment of open-angle and occasionally secondary glaucoma and is the most widely used anti-glaucoma drug (1).
Systemic side effects of glaucoma medications
Published in Clinical and Experimental Optometry, 2022
Amirmohsen Arbabi, Xuan Bao, Wesam Shamseldin Shalaby, Reza Razeghinejad
Timolol, a non-selective beta blocker, is the most commonly prescribed topical beta blocker worldwide. The majority of the reports on beta blockers side effects are on timolol. Arrhythmia, heart failure, syncope, sudden death, bronchospasm, dyspnoea, cerebrovascular accident, recurrent dizziness, worsening of myasthenia gravis, and amaurosis fugax are among the systemic side effects of timolol.61–64 CYP2D6 inhibitors, such as paroxetine, increase the plasma concentration of topical timolol, thereby increasing the risk of adverse cardiovascular effects (orthostatic hypotension, bradycardia, and arrhythmias), especially in elderly patients.65 Third-degree atrioventricular block and sick sinus syndrome were reported with timolol eye drops.66,67 Given the mechanism of action, the side effects of timolol are applicable to other non-selective beta blockers as well.
Fractional 2940-nm Er:YAG laser-assisted drug delivery of timolol maleate for the treatment of deep infantile hemangioma
Published in Journal of Dermatological Treatment, 2021
Li Sun, Chenxia Wang, Yuting Cao, Xinxiang Lv, Limin Tian, Dandan Liu, Lizhong Li, Wenchao Zhao
Infantile hemangiomas (IH) are the most common benign vascular tumors with a reported incidence rate of 4–10% (1,2), and usually appears after several days to several weeks after birth. The initial manifestations of IH include congestive, telangiectatic patches (3). Consecutive photographs of children showed the fastest growth of IH between 5.5 weeks and 7.5 weeks after birth (4), reaching 80% of the final volume by 3 months (5). After that, there is a slow proliferating period from 6 to 9 months, which then gradually fades away after several years (6). IHs are classified into superficial, deep and mixed according to the depth of the tumor (7). Oral propranolol is the first-line treatment for deep IH (3), but is associated with adverse reactions such as hypoglycemia, low blood pressure, slow heart rate, bronchial spasm, wheezing, temporary dyspnea, drowsiness, etc in children (8). In recent years, topical beta blockers were used for treating superficial and deep hemangiomas. Timolol is a nonselective hydrophilic beta blocker (8), and topical treatment of it effectively reduces systemic adverse reactions. Because of the barrier effect of the skin and the hydrophilicity of timolol, the percutaneous penetration of the drug is affected. Hence, fractional 2940-nm Er:YAG laser was used for transdermal delivery of 0.5% timolol maleate eye drops to treat deep IHs in children and evaluate its effectiveness and safety.
Adrenergic agonists and antagonists as antiglaucoma agents: a literature and patent review (2013–2019)
Published in Expert Opinion on Therapeutic Patents, 2019
Alessio Nocentini, Claudiu T. Supuran
Timolol, a nonselective β-blocker, inhibits aqueous humor production and reduces IOP [24]. Many studies have shown that timolol reduces IOP by 27 to 35% during long term treatment [25]. Timolol is available in 0.1, 0.25 and 0.5% solutions and should be applied twice daily (Timoptic®, Timopol®, Loptomit®, Betimol®). A gel formulation (Timoptic-XE®) enables a once daily application. Patients with a dark iris need the higher concentration of timolol because timolol binds to the iris pigment and may lose some of its efficacy [26]. Therapy with timolol initially markedly decreases IOP that therefore will stabilize at a slightly higher level [25]. Timolol causes few ocular adverse effects such as hyperemia of the conjunctiva, burning, stinging or superficial punctate keratitis, but β-blockers may induce severe systemic adverse effects by blocking the β1-adrenoceptors of the heart [27]. Timolol may cause bradycardia, arrhythmia, congestive heart failure, and syncope by Adam-Stokes syndrome [27]. Furthermore, by blocking the β2-adrenoceptors of the bronchioles, timolol can cause bronchospasm and status asthmaticus in patients with chronic obstructive pulmonary disease (COPD) or asthma [27]. Often unnoticed, timolol may induce anxiety, depression, sexual impotence, fatigue, confusion, disorientation and hallucinations [27]. Compression of the nasolacrimal punctum during the local application can reduce the plasma levels of timolol up to 70% because hindering its uptake via the epithelium of the nasopharynx [25].