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Drug Design, Development and Therapy 2018Eyebrows serve as a key feature of the face and have many roles, including cosmetic appearance and social communication. Eyebrow hypotrichosis, which refers to reduction... (Review)
Review
Eyebrows serve as a key feature of the face and have many roles, including cosmetic appearance and social communication. Eyebrow hypotrichosis, which refers to reduction or absence of the eyebrow hair, could be a major problem that leads to negative functional, psychological, and social consequences. Bimatoprost is an ophthalmic prostamide analog that is approved by the United States Food and Drug Administration for the treatment of eyelash hypotrichosis. Its proposed mechanism is stimulation of the prostaglandin receptor in dermal papilla and melanocyte, thus leading to a prolonged anagen phase and increased melanogenesis. The hair follicle then increases in thickness, length, and darkness. The efficacy of bimatoprost for the treatment of eyebrow hypotrichosis has been supported by well-controlled studies. Bimatoprost, which is noninvasive, effective, and well tolerated, is worth considering as a treatment option for eyebrow hypotrichosis.
Topics: Bimatoprost; Eyebrows; Hair Follicle; Humans; Hypotrichosis; Receptors, Prostaglandin; Treatment Outcome
PubMed: 29503529
DOI: 10.2147/DDDT.S156467 -
Indian Dermatology Online Journal 2018Bimatoprost is a prostamide analogue used for treatment of glaucoma in ophthalmology. Surprisingly, the side effects such as increased pigmentation of eyelids and...
Bimatoprost is a prostamide analogue used for treatment of glaucoma in ophthalmology. Surprisingly, the side effects such as increased pigmentation of eyelids and hypertrichosis in patients being treated with prostaglandin analogues for glaucoma have opened new areas of application in various dermatological disorders such as alopecia mainly affecting eyelashes, eyebrows, and vitiligo.
PubMed: 29854658
DOI: 10.4103/idoj.IDOJ_62_16 -
International Journal of Molecular... Nov 2022Prostaglandin analogues (PGAs), including bimatoprost (BIM), are generally the first-line therapy for glaucoma due to their greater efficacy, safety, and convenience of...
Cytotoxicity, Mitochondrial Functionality, and Redox Status of Human Conjunctival Cells after Short and Chronic Exposure to Preservative-Free Bimatoprost 0.03% and 0.01%: An In Vitro Comparative Study.
Prostaglandin analogues (PGAs), including bimatoprost (BIM), are generally the first-line therapy for glaucoma due to their greater efficacy, safety, and convenience of use. Commercial solutions of preservative-free BIM (BIM 0.03% and 0.01%) are already available, although their topical application may result in ocular discomfort. This study aimed to evaluate the in vitro effects of preservative-free BIM 0.03% vs. 0.01% in the human conjunctival epithelial (HCE) cell line. Our results showed that long-term exposure to BIM 0.03% ensues a significant decrease in cell proliferation and viability. Furthermore, these events were associated with cell cycle arrest, apoptosis, and alterations of ΔΨ. BIM 0.01% does not exhibit cytotoxicity, and no negative influence on conjunctival cell growth and viability or mitochondrial activity has been observed. Short-time exposure also demonstrates the ability of BIM 0.03% to trigger reactive oxygen species (ROS) production and mitochondrial hyperpolarisation. An in silico drug network interaction was also performed to explore known and predicted interactions of BIM with proteins potentially involved in mitochondrial membrane potential dissipation. Our findings overall strongly reveal better cellular tolerability of BIM 0.01% vs. BIM 0.03% in HCE cells.
Topics: Humans; Bimatoprost; Preservatives, Pharmaceutical; Conjunctiva; Oxidation-Reduction
PubMed: 36430590
DOI: 10.3390/ijms232214113 -
Clinical Ophthalmology (Auckland, N.Z.) 2014Prostaglandins are approved by the European Glaucoma Society guidelines as first-line treatment for glaucoma. This review focuses on latanoprost, an ester prodrug of... (Review)
Review
Prostaglandins are approved by the European Glaucoma Society guidelines as first-line treatment for glaucoma. This review focuses on latanoprost, an ester prodrug of prostaglandin (PG) F2α, which was the first of the currently available topical PGF2α analogs to be launched for glaucoma or ocular hypertension and which still accounts for the majority of prescriptions. It is better absorbed than the parent compound through the cornea, and peak concentration of the active drug is in the aqueous humor 1-2 hours after topical dosing (15-30 ng/mL). Metabolism occurs mainly in the liver. Latanoprost (0.005%) has been very well studied in clinical trials and meta-analyses that show it to be generally as effective as the other PG analogs (bimatoprost, travoprost, and tafluprost) and more effective than timolol, dorzolamide, and brimonidine. Latanoprost has good short- and long-term safety and tolerability profiles. In common with other prostaglandins, it lacks systemic effects, but can cause ocular adverse events such as conjunctival hyperemia, pigmentation of the iris, periocular skin or eyelashes, hypertrichosis, and ocular surface effects or irritation. Latanoprost is significantly better tolerated than either bimatoprost or travoprost. Patients treated with latanoprost have better compliance and persist with therapy longer than those that are given other drugs. An improved formulation of latanoprost without the preservative benzalkonium chloride has recently been developed. It is as effective as conventional latanoprost, has a lower incidence of hyperemia, and can be stored at room temperature. In conclusion, latanoprost has the best efficacy-tolerability ratio of the PG analogs available for glaucoma treatment, and has good compliance and persistence. These factors should be improved further by the recent development of preservative-free latanoprost.
PubMed: 25328381
DOI: 10.2147/OPTH.S59162 -
Journal of Ophthalmology 2021Within the clinical setting, some patients have been identified as lacking in response to PGAs. This meta-analysis study aimed to evaluate the responsiveness of... (Review)
Review
AIM
Within the clinical setting, some patients have been identified as lacking in response to PGAs. This meta-analysis study aimed to evaluate the responsiveness of latanoprost, travoprost, bimatoprost, and tafluprost in OAG/OHT patients, latanoprost nonresponders (LNRs), and the IOP-reducing efficacy and safety.
METHODS
A literature search was conducted on PubMed, Embase, and the Cochrane Controlled Trials Register. The primary clinical endpoint was the number of responders at the end of the study. The secondary clinical endpoint was the IOP reduction at the endpoint from baseline. Safety evaluation included five common adverse events: conjunctival hyperemia, hypertrichosis, ocular burning, ocular itching, and foreign-body sensation.
RESULTS
Eleven articles containing ten RCTs were included in this meta-analysis study. The results highlighted that, in the OAG/OHT population, there was no statistically significant difference in the responsiveness of the four PGAs. Bimatoprost had a better IOP-reducing efficacy than latanoprost. There was no significant difference in the IOP-reducing efficacy of travoprost, latanoprost, and tafluprost. In LNRs, the responsiveness of bimatoprost, travoprost, and latanoprost did not show statistical differences. Bimatoprost reduced IOP with a greater extent than latanoprost and travoprost in LNRs, while there was no significant difference in the IOP-reducing efficacy of travoprost and latanoprost. No serious adverse events occurred with the treatment of the four PGAs. The prevalence of conjunctival hyperemia due to bimatoprost or tafluprost was significantly higher than that of latanoprost. Other adverse events had no significant difference between the four drugs.
CONCLUSION
The existing studies cannot prove that latanoprost, travoprost, bimatoprost, and tafluprost have different responsiveness in OAG/OHT patients. Switching to bimatoprost or travoprost cannot achieve a significant improvement in responsiveness in LNRs. Bimatoprost has a better IOP-reducing efficacy than latanoprost and travoprost. No serious adverse events occurred during treatment with any medication we studied.
PubMed: 34123413
DOI: 10.1155/2021/5586719 -
Journal of Clinical Medicine Jun 2022This study aimed to evaluate whether the therapeutic switch from a formulation of Bimatoprost 0.1 mg/mL with benzalkonium chloride (BAK) or Bimatoprost 0.3 mg/mL...
Ocular Tolerability of Bimatoprost 0.1 mg/mL Preservative-Free versus Bimatoprost 0.1 mg/mL with Benzalkonium Chloride or Bimatoprost 0.3 mg/mL Preservative-Free in Patients with Primary Open-Angle Glaucoma.
This study aimed to evaluate whether the therapeutic switch from a formulation of Bimatoprost 0.1 mg/mL with benzalkonium chloride (BAK) or Bimatoprost 0.3 mg/mL preservative-free to a formulation of Bimatoprost 0.1 mg/mL preservative-free could improve eye surface conditions in patients with glaucoma; intraocular pressure (IOP) was also evaluated. All patients meeting the inclusion criteria were eligible for the therapeutic switch to Bimatoprost 0.1 mg/mL preservative-free. At each check visit, enrolled patients underwent a break-up time (BUT) test, an ocular surface disease index (OSDI) test, and a three-point tonometric curve. A total of 40 patients were enrolled (23 were in therapy with Bimatoprost 0.1 mg/mL with BAK and 17 with Bimatoprost 0.3 mg/mL preservative-free). Significant differences of OSDI and BUT between Bimatoprost 0.1 mg/mL with BAK at baseline vs. Bimatoprost 0.1 mg/mL preservative-free at 14 and 28 days (p < 0.0001 and p = 0.0003, respectively) were recorded. Similarly, significant differences of OSDI and BUT between Bimatoprost 0.3 mg/mL preservative-free at baseline vs. Bimatoprost 0.1 mg/mL preservative-free at 14 and 28 days (p < 0.0001 for both) were found. Bimatoprost 0.1 mg/mL preservative-free has a better tolerability profile associated with non-therapeutical inferiority in the control of IOP compared to the other Bimatoprost formulations.
PubMed: 35743588
DOI: 10.3390/jcm11123518 -
International Journal of Women's Health Aug 2013Hair loss is a commonly encountered problem in clinical practice, with men presenting with a distinctive pattern involving hairline recession and vertex balding... (Review)
Review
Hair loss is a commonly encountered problem in clinical practice, with men presenting with a distinctive pattern involving hairline recession and vertex balding (Norwood-Hamilton classification) and women exhibiting diffuse hair thinning over the crown (increased part width) and sparing of the frontal hairline (Ludwig classification). Female pattern hair loss has a strikingly overwhelming psychological effect; thus, successful treatments are necessary. Difficulty lies in successful treatment interventions, as only two medications - minoxidil and finasteride - are approved for the treatment of androgenetic alopecia, and these medications offer mediocre results, lack of a permanent cure, and potential complications. Hair transplantation is the only current successful permanent option, and it requires surgical procedures. Several other medical options, such as antiandrogens (eg, spironolactone, oral contraceptives, cyproterone, flutamide, dutasteride), prostaglandin analogs (eg, bimatoprost, latanoprost), and ketoconazole are reported to be beneficial. Laser and light therapies have also become popular despite the lack of a profound benefit. Management of expectations is crucial, and the aim of therapy, given the current therapeutic options, is to slow or stop disease progression with contentment despite patient expectations of permanent hair regrowth. This article reviews current perspectives on therapeutic options for female pattern hair loss.
PubMed: 24039457
DOI: 10.2147/IJWH.S49337 -
British Journal of Pharmacology Feb 2008The prostamides are part of a large and continually expanding series of pharmacologically unique neutral lipids. They are COX-2 derived oxidation products of the... (Review)
Review
The prostamides are part of a large and continually expanding series of pharmacologically unique neutral lipids. They are COX-2 derived oxidation products of the endocannabinoid/endovanniloid anandamide. Prostamide pharmacology is unique and, as in the case of the endocannabinoids anandamide and 2-arachidonylglycerol, bears little resemblance to that of the corresponding free acids. By virtue of its close relationship to the anti-glaucoma drug bimatoprost, prostamide F(2alpha) has received the greatest research attention. Prostamide F(2alpha) and bimatoprost effects appear independent of prostanoid FP receptor activation, according to a litany of agonist studies. Studies involving freshly isolated and separate feline iridial smooth muscle cells revealed that bimatoprost and FP receptor agonists stimulated different cells, without exception. This suggests the existence of receptors that preferentially recognize prostamide F(2alpha). The recent discovery of prostamide antagonists has provided further support for prostamide receptors as discrete entities. The prototypical prostamide antagonists, AGN 204396 and 7, blocked the effects of prostamide F(2alpha) and bimatoprost but not those of PGF(2alpha) and FP receptor agonists in the feline iris. Second generation more potent prostamide antagonists, such as AGN 211334, should allow the role of prostamides in health and disease to be elucidated. From the therapeutics standpoint, the prostamide F(2alpha) analogue bimatoprost is the most efficacious ocular hypotensive agent currently available for the treatment of glaucoma.
Topics: Amides; Animals; Bimatoprost; Cloning, Molecular; Cloprostenol; Cyclooxygenase 2; Dinoprostone; Ethanolamines; Humans; Prostaglandins; Receptors, Prostaglandin
PubMed: 17721551
DOI: 10.1038/sj.bjp.0707434 -
Indian Journal of Ophthalmology Jun 2016
Topics: Antihypertensive Agents; Bimatoprost; Glaucoma, Open-Angle; Humans; Male; Middle Aged; Ophthalmic Solutions; Orbital Diseases; Prostaglandins
PubMed: 27488155
DOI: 10.4103/0301-4738.187676 -
Journal of Current Glaucoma Practice 2023This review summarizes current data on Rho-kinase (ROCK) inhibitors use in ocular diseases, primarily glaucoma. (Review)
Review
AIM
This review summarizes current data on Rho-kinase (ROCK) inhibitors use in ocular diseases, primarily glaucoma.
BACKGROUND
Translational research over the last decade culminating in the development of ROCK inhibitors has provided a much-needed shot in the arm to glaucoma pharmacopeia. ROCK pathway is intricately involved in cytoskeletal modulation with action on cell morphology, cell motility, cell adhesion, cell apoptosis, and smooth muscle contraction. This cytoskeletal modulation property has been utilized to modify trabecular meshwork (TM) resistance, resulting in the discovery of ROCK inhibitors to increase trabecular outflow.
REVIEW RESULTS
Multicentric trials on ROCK inhibitors for antiglaucoma medications are summarized. The focus is on linking pharmacological action to the clinical utility of these drugs. While the Rho Kinase Elevated intraocular Pressure (IOP) Treatment (ROCKET) trials compared monotherapy with ROCK inhibitor netarsudil vs timolol, MERCURY trials compared a fixed dose combination of latanoprost and ROCK inhibitor netarsudil [fixed combination netarsudil-latanoprost (FCNL)] vs monotherapy with either and bimatoprost-timolol combination. While ROCKET trials showed ROCK inhibitors to be non-inferior to timolol, MERCURY trials showed FCNL achieving a much greater IOP reduction than monotherapy with either. Conjunctival hyperemia was the most common side effect reported with ROCK inhibitor use.
CONCLUSION
Moderate efficacy of ROCK inhibitors with a common side effect of conjunctival hyperemia, makes it an adjunctive antiglaucoma drug of choice and not a first-line therapy.
CLINICAL SIGNIFICANCE
ROCK inhibitors' action on diseased TM is more physiological compared to available antiglaucoma medications that either reduce aqueous secretion or enhance uveoscleral outflow. The property of ROCK inhibition to stabilize the endothelium of both retinal vasculature and cornea has opened a new chapter in the treatment of diabetic retinopathy and corneal decompensation.
HOW TO CITE THIS ARTICLE
Singh K, Singh A. Rho-kinase Inhibitors in Ocular Diseases: A Translational Research Journey. J Curr Glaucoma Pract 2023;17(1):44-48.
PubMed: 37228304
DOI: 10.5005/jp-journals-10078-1396