Fenylefrineoogdruppels 2,5% en 5%

Data on the use, the mydriatic activity and the systemic adverse effects of phenylephrine eyedrops are reviewed in order to ascertain whether mydriatic concentrations lower than 10% should be included in theFormulary of Dutch Pharmacists (FNA). From the available data it is deduced that 2,5% and 5% may be useful mydriatic concentrations, whereupon their mode of preparation is discussed.Samenvatting Teneinde na te gaan of mydriatische fenylefrineconcentraties lager dan 10% in het Formularium der Nederlandse Apotherkers (Fna) kunnen worden opgenomen, zijn gegevens over het gebruik, de mydriatische effectiviteit en de systemische bijwerkingen van fenylefrineoogdruppels verzameld. Uit de beschikbare gegevens wordt afgeleid dat 2,5% en 5% bruikbare mydriatische concentraties kunnen zijn, waarna de bereidingswijze van deze concentraties wordt besproken.     

Travoprost 0.004%/timolol 0.5% fixed combination

Fixed-combination travoprost/timolol solution consists of travoprost 0.004% and timolol 0.5%. Several studies have demonstrated the efficacy and safety of this medication used once daily for the treatment of open-angle glaucoma and ocular hypertension. This fixed combination has been compared to travoprost and timolol used concomitantly, latanoprost and timolol used concomitantly, latanoprost/timolol fixed combination and travoprost and timolol monotherapy. Fixed-combination medicines such as travoprost/timolol offer the potential of maximizing patient adherence by decreasing the burden of using multiple topical agents that lower intraocular pressure, and by potentially decreasing the overall cost to both the patient and the health-care system. We discuss the benefits of fixed-dose medications, report on previous clinical trials and summarize the existing data on the performance of travoprost/timolol.     

Comparison of the safety and efficacy of loteprednol 0.5%/tobramycin 0.3% withdexamethasone 0.1%/tobramycin0.3% in the treatment of blepharokeratoconjunctivitis

ABSTRACT

Objective: This study compared the safety and efficacy of loteprednol etabonate 0.5%/tobramycin 0.3% (LE/T; Zylet) with dexamethasone 0.1%/tobramycin 0.3% (DM/T; Tobradex) in the treatment of ocular inflammation associated with blepharokeratoconjunctivitis.

Research design and methods: This was a multicenter, randomized, investigator-masked, parallel-group study. Subjects with clinically diagnosed blepharokeratoconjunctivitis in at least one eye were randomized to LE/T (n?=?138) or DM/T (n?=?138) administered four times per day, for 14 days. The primary efficacy endpoint was the change from baseline to Day 15 (± 1?day) in the signs and symptoms composite score using a non-inferiority metric to compare LE/T to DM/T. Safety endpoints included visual acuity (VA), biomicroscopy, intraocular pressure (IOP) assessments, and adverse events.

Results: At Day 15, the mean (SD) change from baseline in the signs and symptoms composite score was ?15.2 (7.3) for LE/T-treated subjects and ?15.6 (7.7) for DM/T-treated subjects. The upper bound of the 90% confidence interval for the difference in change from baseline was less than the non-inferiority margin not only at Day 15 but also at Day 7 and Day 3 for both the intent-to-treat and per protocol populations. Subjects treated with DM/T experienced a significant increase in IOP versus those treated with LE/T at Day 7, Day 15, and overall (mean [SD] of 0.6 [2.3] vs, ?0.1 [2.2], p?=?0.03, 1.0 [3.0] vs. ?0.1 [2.4], p?=?0.01, and 2.3 [2.3] vs. 1.6 [1.7], p?=?0.02, respectively).

Conclusions: LE/T satisfied the condition of non-inferiority to DM/T in decreasing the signs and symptoms of ocular inflammation associated with blepharokeratoconjunctivitis. Subjects treated with DM/T experienced more of an increase in IOP.

Limitation: Although the single-masked design of this study could be considered a limitation, care was taken to ensure that the investigator was masked.     

Pupillometry study of brimonidine tartrate 0.2% and apraclonidine 0.5%

This study investigated possible effects of brimonidine tartrate 0.2% and apraclonidine 0.5% on pupil diameter. Ten subjects between 20 and 40 years of age participated. A Colvard pupillometer (Oasis Medical) was used to measure pupil diameter. Baseline and serial measurements were obtained at 3 luminance levels (>6.4, <0.82-0.4, and <0.2-0.02 cd/m(2)) during a 4-hour interval following instillation of 1 drop of brimonidine tartrate 0.2% or apraclonidine 0.5% in one eye versus a placebo in the contralateral eye. The measurements for each drug were obtained on different days. A nested random effects model controlling for subject's age, race, and sex was used for statistical analysis. A maximum reduction in pupil diameter was observed at 90 minutes from instillation (1.40 mm at >6.4 cd/m(2), 1.69 mm at <0.82-0.4 cd/m(2), and 1.55 mm at <0.2-0.02 cd/m(2)) for brimonidine tartrate 0.2%. At all time intervals and illumination levels, miosis (P < .01) occurred. Apraclonidine 0.5% did not produce a significant effect on pupil diameter. Brimonidine tartrate 0.2% produced a moderate miotic effect. No effect was observed for apraclonidine 0.5%. A predominant agonistic effect on α-2 receptors of the iris dilator may explain this behavior.     

In vitro and in vivo bactericidal activities of 10%, 2.5%, and 1% povidone-iodine solution

The bactericidal action of three formulations of a povidone-iodine (PVI) complex in vitro, in vivo, and in the presence of competing organic matter was evaluated. Bacterial organisms included Staphylococcus aureus ATCC 25923 and 25 clinical isolates of Staph. aureus, designated KU 1-25. For the in vitro studies, 1.0 mL of bacterial inoculum containing 10(7) organisms was introduced into 9.0 mL of chemically stable 10% and 1% PVI formulations in sterile culture tubes, and 1.0-mL samples were withdrawn at set intervals. Samples were plated by using standard techniques and incubated for 24 hours, after which colony-forming units were counted. For in vivo studies, 0.1 mL of 10(6) Staph. aureus ATCC 25923 or KU inoculum was deposited on the dorsum of the hand of healthy human subjects. This area was wiped with a cotton swab saturated with 1%, 2.5%, or 10% PVI formulations. Samples were taken at 15 and 30 seconds after application of the iodophor. To test the bactericidal activity of the three formulations in the presence of a competing substrate, a swab soaked with sterile sheep's blood was applied to the skin and allowed to dry. The percentage of 10(4) Staph. aureus inoculum recovered allowed for comparison of the three products. In vitro, the 1% PVI formulation was bactericidal for 10(7) Staph. aureus within two minutes, as compared with the four minutes required by 10% PVI. On the skin contaminated with 10(6) organisms, the rates of killing within 30 seconds were comparable for both solutions.(ABSTRACT TRUNCATED AT 250 WORDS)     

Stability of milrinone in 0.45% sodium chloride, 0.9% sodium chloride, or 5% dextrose injections

The stability of milrinone in 0.45% and 0.9% sodium chloride injections and in 5% dextrose injection in glass and plastic containers was studied. Admixtures containing milrinone 0.2 mg/mL were prepared in three 500-mL glass containers, three 500-mL polyethylpolypropyl copolymer plastic containers, and three 1-L flexible plastic containers of each solution. Milrinone content was determined by high-performance liquid chromatography at intervals during 72 hours of storage at room temperature; one sample of each solution and container type was protected from light. Duplicate assays of each sample were performed, and samples were observed for visual and pH changes. In all samples milrinone concentrations were more than 97% of the initial concentration. No changes in pH or appearance occurred. Milrinone at a concentration of 0.2 mg/mL is stable for 72 hours at room temperature in 0.45% and 0.9% sodium chloride injections and in 5% dextrose injection in glass or plastic containers.     

Lidocaine patch 5%

Lidocaine patch 5% comprises a soft, stretchy adhesive patch (l0 by 14 cm) containing 5% lidocaine (700 mg) for the topical treatment of pain associated with postherpetic neuralgia (PHN). Lidocaine provides analgesic relief by blocking neuronal sodium channels. In clinical trials (conducted over 12 hours to 24 days) involving patients with allodynia associated with PHN, treatment with lidocaine patch 5% resulted in a significant reduction in pain intensity and increased pain relief compared with vehicle patch. Lidocaine patch 5% was associated with few adverse events, the most frequent being mild skin redness or irritation at the application site which occurred with a similar incidence with lidocaine and vehicle patch.     

From dorzolamide 2%/timolol 0.5% to brinzolamide 1%/timolol 0.5% fixed combination: a 6-month,multicenter, open-label tolerability switch study

Purpose: To assess ocular surface status and tolerability after switching glaucoma patients from dorzolamide/timolol to brinzolamide/timolol fixed combination (FC).

Methods: Six-month, multicenter, open-label, prospective study that switched 72 patients from dorzolamide/timolol to brinzolamide/timolol FC. Intraocular pressure (IOP), tear film break-up-time (TF-BUT), fluorescein staining and Glaucoma Symptom Scale (GSS) questionnaire were recorded at baseline and after 6 months.

Results: Median interquartile range (IQR) IOP was 16 (IQR 15 – 18) mmHg at baseline and 16 (15 – 17) mmHg and 6 months. TF-BUT significantly improved (p < 0.0001); the regression analysis found a negative association between TF-BUT changes and age at baseline and at month 6 (r = ?0.32; p = 0.0082 and r = ?0.31; p = 0.0085). Patients with no corneal fluorescein staining statistically increased after substitution (p = 0.04). Quality of life – as examined by the GSS symptoms (SYMP) score – statistically improved (p < 0.0001), revealing an association between GSS SYMP score and age [coefficient ?0.67, 95% confidence interval (CI) ?1.13 to ?0.21, p = 0.0005), superficial keratitis (coefficient ?8.26, 95% CI ?15.73 to ?0.80, p = 0.031) and TF-BUT (coefficient 4.94, 95% CI 1.71 to 8.17, p = 0.003).

Conclusion: Brinzolamide/timolol FC is associated with reduced topical discomfort and improved signs of ocular surface disease. The good tolerability and comfort of this FC might contribute to good patient adherence.     

Ciprofloxacin 0.3% + dexamethasone 0.1% for the treatment for otitis media

Introduction: Ciprofloxacin 0.3% with dexamethasone 0.1% (ciprofloxacin/dexamethasone) is an ototopical preparation for acute otitis externa, otorrhea with tympanostomy tubes, and is frequently used to treat chronic suppurative otitis media (CSOM). The advantage of topical therapy is the ability to deliver higher concentration of antibiotics to the treatment site when compared with oral or parenteral antibiotics. The delivery of a high concentration of antibiotics significantly decreases treatment failure and makes the development of resistant organisms unlikely. Previous ototopical preparations contained antibiotics such as aminoglycosides that are known to be ototoxic making treatment of otic infections without an intact tympanic membrane difficulty.

Areas covered: A literature search of PubMed was performed as the basis for a literature-based discussion on the clinical efficacy of ciprofloxacin/dexamethasone compared to oral antibiotics and ototopical therapy without a steroid component. The potential ototoxicity of ototopical therapies is discussed, including evidence demonstrating the lack of ototoxicity of fluoroquinolone and dexamethasone containing drops.

Expert opinion: Because multiple studies have demonstrated that fluoroquinolones are not ototoxic, fluoroquinolone ototopical drops should be a first-line treatment for otorrhea without an intact membrane. The addition of dexamethasone 0.1% to ciprofloxacin 0.3% has been shown to decrease granulation tissue, improve clinical cure and achieve greater rates of bacterial eradication when compared to ciprofloxacin 0.3% alone.     

Stability of vancomycin hydrochloride in 5% dextrose and 0.9% sodium chloride injections

The stability of vancomycin hydrochloride mixed with 5% dextrose and 0.9% sodium chloride injections was studied. Vancomycin hydrochloride powder was mixed with each of the two diluents in final concentrations of 5 mg/mL. Duplicate samples of each admixture were divided into four parts and stored at 24 degrees C in glass and in plastic i.v. bags for 17 days and at 5 degrees C and -10 degrees C in glass for 63 days. To additional samples, hydrochloric acid or phosphate buffer was added; these were stored at 24 degrees C for 17 days. At various storage times, clarity and pH of the samples were recorded and vancomycin concentrations were measured in triplicate by high-performance liquid chromatography. Except for the buffered samples, all solutions remained clear and pH was unchanged. Vancomycin concentrations decreased less than 6% during 17 days at room temperature. In the refrigerated and frozen samples, vancomycin concentrations decreased less than 1% throughout the study. Vancomycin hydrochloride is stable in admixtures with 5% dextrose injection and 0.9% sodium chloride injection for 17 days at 24 degrees C and for 63 days at 5 degrees C and -10 degrees C.     

Stability of zidovudine in 5% dextrose injection and 0.9% sodium chloride injection

The stability of zidovudine at a concentration of 4 mg/mL in 5% dextrose injection and 0.9% sodium chloride injection in polyvinyl chloride infusion bags stored at room and refrigerated temperatures for up to eight days was studied. Zidovudine was diluted in 5% dextrose injection and in 0.9% sodium chloride injection to a concentration of 4 mg/mL. Six admixtures were prepared with each diluent; three were stored at room temperature (25 +/- 1 degree C) and three were refrigerated (4 +/- 1 degree C). At 0, 3, 6, 24, 48, 72, and 192 hours, 2-mL aliquots were removed. One milliliter of each aliquot was diluted to a zidovudine concentration of approximately 40 micrograms/mL and assayed in duplicate by a stability-indicating high-performance liquid chromatographic method. Visual inspection was performed at each sampling time for precipitation, turbidity, color change, and gas formation. Sample pH was recorded at 0 and 192 hours. In all admixtures, more than 97% of the initial zidovudine concentration remained throughout the study period. No visual or pH changes were observed. Zidovudine 4 mg/mL in admixtures with 5% dextrose injection or 0.9% sodium chloride injection stored in polyvinyl chloride infusion bags was stable for up to 192 hours (eight days) at room temperature and under refrigeration.     

A randomized comparison of to-aqueous penetration of ketorolac 0.45%, bromfenac 0.09% and nepafenac 0.1% in cataract patients undergoing phacoemulsification

Abstract

Objective:

To compare the peak to-aqueous penetration of three nonsteroidal anti-inflammatory drugs: ketorolac tromethamine 0.45%, bromfenac 0.09%, nepafenac 0.1%, and amfenac (the active metabolite of nepafenac) in patients undergoing phacoemulsification.     

2.5%、5%和10%进口过氧化苯甲酰凝胶与5%国产过氧化苯甲酰凝胶比较治疗寻常痤疮临床疗效及安全性评估

目的过氧化苯甲酰是治疗痤疮的一种外用制剂,主要对炎性损害有效,也有中度角质松解和抑制皮脂活性。进口过氧化苯甲酰凝胶和国产过氧化苯甲酰凝胶均是过氧化苯甲酰的一种外用制剂,本研究目的是评价2.5%,5%和10%进口过氧化苯甲酰凝胶和5%国产过氧化苯甲酰凝胶对比治疗寻常痤疮的疗效和安全性,每天外用2次,疗程6周。方法在6周末对炎性损害总数的减少率,2.5%进口过氧化苯甲酰为65.62%（国产过氧化苯甲酰81.94%,P<0.01);5%进口过氧化苯甲酰为79.50%（国产过氧化苯甲酰81.43%,P>0.05）;10%进口过氧化苯甲酰为81.75%（国产过氧化苯甲酰82.84%,P>0.05）。对非炎性损害总数的减少率,2.5%进口过氧化苯甲酰为2.02%（国产过氧化苯甲酰26.08%,P<0.05);5%进口过氧化苯甲酰为10.41%（国产过氧化苯甲酰35.24%,P>0.05）;10%进口过氧化苯甲酰为28.54%（国产过氧化苯甲酰20.49%,P>0.05）。最终疗效显示2.5%进口过氧化苯甲酰有效率64.52%（国产过氧化苯甲酰93.55%,P<0.01);5%进口过氧化苯甲酰为83.87%（国产过氧化苯甲酰90.32%,P>0.05）;10%进口过氧化苯甲酰为87.88%（国产过氧化苯甲酰87.10%,P>0.05）。各治疗组均有轻中度刺激性皮炎病例发生,但患者耐受性尚好。2.5%进口过氧化苯甲酰药物不良反应发生率35.48%（国产过氧化苯甲酰74.19%,P<0.01);5%进口过氧化苯甲酰46.88%（国产过氧化苯甲酰71.88%,0.01<P<0.05）;10%进口过氧化苯甲酰60.61%（国产过氧化苯甲酰65.63%,P>0.05）。本研究证实过氧化苯甲酰治疗痤疮的临床有效性,以5%和10%的浓度疗效最佳。     

Evaluation of the effects on choroidal thickness of bimatoprost 0.03% versus a brinzolamide 1.0%/timolol maleate 0.5% fixed combination

Objective: To investigate the effects of two different medical treatment options on choroidal thickness (CT) in cases of open-angle glaucoma (OAG).

Methods: Sixty-seven eyes newly diagnosed with OAG and 52 healthy eyes constituting the control group were included in the study. Glaucomatous eyes were randomly divided into two subgroups; Group I was started on bimatoprost 0.03% and Group II on a brinzolamide 1.0%/timolol maleate 0.5% fixed combination (BTFC). Intraocular pressure (IOP), ocular pulse amplitude (OPA) and subfoveal CT measurements were performed in all eyes in the study before treatment and on weeks 2, 4 and 8 after treatment.

Results: Mean initial IOP values in groups I and II and the control group were 25.5?±?4.7, 25.1?±?5.2 and 16.1?±?2.9?mmHg, mean OPA values were 3.7?±?1, 3.6?±?1.4 and 2.4?±?0.6?mmHg and mean CT values were 269.4?±?83, 264.5?±?84.4 and 320.1?±?56.6?μm, respectively. Eight weeks after treatment, mean IOP values in Groups I and II and the control group were 18.3?±?2.6, 18.1?±?3.4 and 15.7?±?2.9?mmHg, mean OPA values were 2.9?±?1.2, 2.8?±?1.5 and 2.3?±?0.8?mmHg and mean CT values were 290.2?±?87.3, 271.8?±?82.5 and 319.3?±?56.8?μm, respectively. No significant difference was determined in terms of the decrease in IOP and OPA obtained after treatment in Group I and Group II. However, a significant difference was observed between the two groups in terms of choroidal thickening after treatment.

Conclusion: The use of topical ocular hypotensive medication in eyes with OAG results in an increase in CT. This increase is relatively greater with bimatoprost 0.03% therapy compared to BTFC.     

Circadian IOP-lowering efficacy of travoprost 0.004% ophthalmic solution compared to latanoprost 0.005%

PURPOSE: The primary objective of this study was to determine the intraocular pressure- (IOP) lowering efficacy over two consecutive 24-h periods of travoprost 0.004% ophthalmic solution (Travatan) compared to latanoprost 0.005% (Xalatan) dosed once daily in patients with primary open-angle glaucoma or ocular hypertension. METHODS: This was a double-masked trial conducted at the Hospital Clínico San Carlos, Madrid, Spain. The primary objective of this study was to determine the IOP lowering efficacy of travoprost and latanoprost. During the eligibility visit, patients' IOP was measured throughout two consecutive 24-h periods every 4 h. Patients were then randomized to travoprost or latanoprost (one drop at 8 p.m. daily for 2 weeks). Sixty-two patients were randomized (travoprost n = 32; latanoprost n = 30). IOP was measured at week 2 every 4 h throughout two 24-h periods. All measurements were taken in both supine and sitting positions with the aid of Perkins applanation tonometry. Limitations of the study include a small sample size (due to the difficulty in recruiting patients in a study of this type) which enrolled only Caucasian patients and a short study duration. However, with 25 subjects per group, there was at least 90% power to detect a mean IOP change from baseline of 2.9 mmHg and 80% power to detect a difference of 2.5 mmHg between treatments. RESULTS: Patients on travoprost therapy showed lower mean IOP levels than those on latanoprost. This difference was statistically significant (p < 0.05) at 12, 16, 20, 24, 36, 40, and 48 h after the last dose for the supine position. The mean IOPs in the supine position throughout the first and the second 24-h period of the week 2 visit as well as for the 48-h visit were statistically lower (p < 0.05) for the travoprost group. Adverse events were mild and included hyperemia and corneal staining. Travoprost and latanoprost were both well tolerated. CONCLUSION: Mean IOP values were significantly lower for patients on travoprost for the majority of time points in the supine position.