[Streptomycin sensitivity elicited by the use of streptomycin through drug instillation and nebulization therapy].
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Instillation, Drug↗
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Dimethylsulfoxide enhances the absorption of chemotherapeutic drug instilled into the bladder.
We examined the effect of dimethylsulfoxide (DMSO) on the absorption of a chemotherapeutic drug instilled into the bladder. Female Wistar rats with bladder tumors underwent intravesical instillation of normal saline (S group) or 50% DMSO (D group) prior to the administration of pirarubicin (tetrahydropyranyl-Adriamycin). The absorption of pirarubicin was estimated histologically by observing its fluorescence. In the S group, fluorescence of pirarubicin was observed only in the epithelial layer of normal or hyperplastic regions and in the cells of superficial layers of the tumor. In the D group fluorescence was observed in the entire bladder wall of normal or hyperplastic regions and extended to deeper regions of the tumors than in the S group. These findings indicate enhancement of the absorption of pirarubicin by pretreatment with DMSO.
Absorption↗
Pharmacokinetic prediction of the ocular absorption of an instilled drug with ophthalmic viscous vehicle.
We previously developed an in vivo pharmacokinetic model that accounts for the corneal diffusion in albino rabbits and predicts the concentration of beta-blockers in the anterior segments. The purpose of this study is to pharmacokinetically predict the ocular absorption and characterize the systemic absorption of instilled drug with ophthalmic viscous vehicle to assist in its design and evaluation. Tilisolol and carboxymethylcellulose sodium salt (CMC) were used as the model ophthalmic drug and viscous polymer, respectively. After instillation of tilisolol with CMC vehicle in rabbits, the disposition of the drug in tear fluid, aqueous humor, and plasma were determined by HPLC. The ocular and systemic absorption were analyzed by a mathematical model including a diffusion process and a two-compartment model with first-order absorption, respectively. CMC vehicle increased the area under the concentration-time curve (AUC) of tilisolol in the tear fluid and aqueous humor and slightly reduced the AUC in plasma. The concentrations of tilisolol in the aqueous humor after instillation with CMC vehicle were accurately predicted from the tear concentrations by using the in vivo ocular pharmacokinetic model. CMC vehicle improved the ocular delivery of tilisolol.
Absorption↗
Effects of topically instilled drugs on intraocular pressure in rabbits.
The effect of the ocular instillation of some drugs on the intraocular pressure of non-anaesthetized rabbits was studied, using the Schiötz tonometer. The risk of systemic absorption of drugs follwoing ocular instillation was evaluated by 1. measuring the spreading of effects from the treated eye to the contralateral one and 2. studying the effects on blood pressure or on blood pressure responses to noradrenaline. The results showed that trazodone, epinephrine and acetazolamide produced hypotension on the treated eye; there was no spreading of effects to the contralateral one. These data could suggest that the primary site of action of these drugs is the eye. Naphazoline reduced the intraocular pressure both on the treated eye and, with a constant delay, on the contralateral one. This was interpreted as a combination of a local action and systemic absorption. The effects of chlorpromazien were more complex. This drug produced hypertension and a strong irritation on the treated eye as well as a hypotensive effect on the contralateral one. The rise in intraocular pressure was probably caused by irritation; the hypotensive effect by systemic absorption. The following drugs were inactive: amphetamine, chlorothiazide and pilocarpine.
Acetazolamide↗
Pharmacokinetics of instilled drugs in the human eye.
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Animals↗
[Transthoracic intracavernous drug instillation].
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Adult↗
[Cellulose and cellophane membranes used as model of corneal permeability for instilled drugs].
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Animals↗
Sector pupil dilation with phenylephrine and tropicamide.
A comparison of sector pupil dilation produced with 2.5% phenylephrine and 1.0% tropicamide was carried out on nine subjects. We found that 2.5% phenylephrine produced a significant increase in the vertical as compared to the horizontal diameter at 10, 20, 30, 40, and 50 min after instillation of the drug with the maximum vertical diameter occurring at 40 min. The pupil diameter in the vertical and horizontal meridians before drug instillation was 3.7 mm +/- 0.2 (mean +/- SE) whereas at 40 min the vertical and horizontal diameters were 6.7 mm +/- 0.4 and 5.2 mm +/- 0.3, respectively. Instillation of 1% tropicamide produced equal dilation of the vertical and horizontal diameters, which was maximum at 40 min. Before drug instillation, the pupils were 3.7 mm +/- 0.2 (mean +/- SE) in both the horizontal and vertical meridians. At 50 min the pupil diameter was 7.0 mm +/- 0.2 in both meridians in the eye that received tropicamide.
Adult↗
Mydriatic effect of ocular decongestants studied by pupillography.
The mydriatic effect of three ocular decongestants, containing 0.1% tetrahydrozoline hydrochloride, 0.3% chlorpheniramine maleate, and 0.05% tetrahydrozoline hydrochloride in combination with 0.3% pheniramine maleate, respectively, was evaluated in 10 healthy volunteers. The study was carried out using a single dose of the tested drug, instilling 2 drops in one eye and 2 drops of a placebo in the other. The papillary diameters were measured by photographic pupillography under basal conditions and 15, 30, 45, 60, 90, and 120 min after each treatment. Near and distance visual acuity and tonometry were evaluated under basal conditions and 50 and 95 min after instillation of drugs. No statistical significant differences between the treated and the control pupil diameters were found after instillation of 0.1% tetrahydrozoline hydrochloride or 0.3% chlorpheniramine maleate. The combination of 0.05% tetrahydrozoline hydrochloride with 0.3% pheniramine maleate caused a significant mydriasis from 30 min up to 120 min (p < 0.01 and p < 0.0005) after instillation, more pronounced in light irides. No local and systemic effects and no effects on visual acuity and ocular pressure were detected. On the basis of our results, it is possible to conclude that the persistent mydriatric action of the two-drug combination is due to a synergism; the use of these eyedrops should be avoided in subjects with narrow-angle glaucoma, light irides, narrow iridocorneal angle, and low anterior chamber for the risk of ocular pressure increase.
Adult↗
Comparison of deep and shallow endotracheal administration of dionosil in dogs and effect of manual hyperventilation.
The endotracheal route has been used as a second route of choice for administration of emergency drugs for several years; however, the optimal technique for administration of drugs by this route has not been clearly defined. One important aspect of technique involves the question of how distribution to the distal-most endobronchial tree is influenced by initial depth of endotracheally administered drug instillation and use of forced manual hyperventilation. This study demonstrates that depth of instillation of drugs administered by the endotracheal route may not be an important factor in the delivery of medications to absorptive sites in the lung. It appears, however, that forced manual hyperventilation is essential to assure bilateral and optimal distal delivery of endotracheally administered medications.
Animals↗
The effect of terodiline on hyperreflexia (in vivo) and the in vitro response of isolated strips of rabbit bladder to field stimulation, bethanechol and KCL.
Hyperreflexia, a condition characterized by contractions of the urinary bladder, is not mediated by a micturition reflex. The contractions can be of neurogenic origin through spinal or supraspinal reflexes or of myogenic origin, independent of neuronal mediation. There is a clear relationship between hyperreflexia and symptoms such as urgency, frequency, nocturia and urinary incontinence. Therapies to reduce the presence of uninhibited bladder contractions include oral drug therapy, instillation drug therapy and parasympathetic nerve ablation. The current study characterizes the ability of terodiline to inhibit an experimental form of hyperreflexia and compares the efficacy and potency of terodiline and other agents on hyperreflexia and evoked contractions. The results can be summarized as follows: (1) terodiline inhibits the amplitude of the hyperreflexia at lower concentrations than it inhibits the frequency of hyperreflexia; (2) terodiline had no statistically significant effect on mean blood pressure at any concentration utilized; (3) terodiline had approximately the same potency for inhibition of 2 and 32 Hz stimulation for both the bladder body and base; (4) terodiline inhibited the maximum contractile response to bethanechol and also shifted the curve to the right, demonstrating that terodiline is a mixed inhibitor, and (5) terodiline was a noncompetitive inhibitor of KCl.
Animals↗
[Interventional therapy for the chronic seminal vesiculitis].
OBJECTIVES: To investigate the efficacy of transperineal seminal vesicle puncture under ultrasound guidance and continuous transcatheter antibiotic drugs instillation for the treatment of chronic seminal vesiculitis. METHODS: Forty-two patients with hemospermia were treated from April 1988 to January 2001. Of them 35 patients with urogenital inflammation were treated by transperineal seminal vesicle puncture under ultrasound guidance and continuous transcatheter antibiotic drugs instillation. RESULTS: Transperineal seminal vesicle puncture and continuous transcatheter antibiotic drugs instillation therapy was adopted for 35 patients with urogenital inflammation and the cure rate was 91.43%. CONCLUSIONS: Transperineal seminal vesicle puncture under ultrasound guidance and continuous transcatheter antibiotic drugs instillation was an effective method for diagnosis and treatment of chronic seminal vesiculitis.
Adult↗
Consensual pupillary responses to mydriatic and miotic drugs.
1. Three experiments were conducted to examine whether mydriatic or miotic drugs instilled into one eye have any effect on the diameter of the pupil of the untreated fellow eye, in healthy volunteers. 2. In Experiment 1, the effects of four subjects, using photography in an illuminated room to assess pupil diameter. The drug evoked a dose-dependent mydriasis in the index eye which was accompanied by a simultaneous dose-dependent miosis in the fellow eye. 3. In Experiment 2, the same method was used to assess pupil diameter as in Experiment 1. The effects of mydriatic (methoxamine and tyramine) and of miotic (pilocarpine) drugs instilled into the fellow eye, were studied on the sizes of pupillary responses to the same drugs instilled into the index eye. The presence of a mydriatic drug in the fellow eye resulted in a decrease in the size of the mydriatic responses in the index eye. 4. In Experiment 3, the effects of three concentrations of phenylephrine hydrochloride (0.15-0.60 M) and of three concentrations of pilocarpine hydrochloride (0.002-0.008 M), were studied in darkness using an infra-red binocular television pupillometer, in seven subjects. Phenylephrine evoked dose-dependent mydriasis and pilocarpine evoked dose-dependent miosis. The pupillary responses of the index eye were not accompanied by any changes in the diameter of the pupil of the fellow eye. 5. It is concluded that drug-induced mydriasis in the index eye is accompanied by a consensual miosis in the fellow eye.(ABSTRACT TRUNCATED AT 250 WORDS)
Adolescent↗
A comparison of the relative efficacy and clinical performance of olopatadine hydrochloride 0.1% ophthalmic solution and ketotifen fumarate 0.025% ophthalmic solution in the conjunctival antigen challenge model.
OBJECTIVE: The purpose of this study was to compare the relative efficacy and clinical performance of olopatadine hydrochloride 0.1% ophthalmic solution and ketotifen fumarate 0.025% ophthalmic solution in the conjunctival antigen challenge model. METHODS: This was a prospective, randomized, double-masked, contralaterally controlled, single-center, antigen challenge study. Of the 53 subjects screened, 32 were enrolled and completed the study. The study comprised 3 visits. Primary efficacy variables were ocular itching (assessed at visits 2 and 3) and subject satisfaction (assessed at visit 3). Tolerability variables were slit-lamp findings (all visits), visual acuity (all visits), ocular comfort after drug instillation (visit 3), and adverse events (visits 2 and 3). At visit 1, the antigen concentration that elicited a positive ocular allergic response was determined, and this concentration was confirmed at visit 2. Subjects graded itching on a 5-point scale at 3, 5, and 10 minutes postchallenge. The scores from this visit were used as baseline scores and compared with scores from visit 3 to determine drug efficacy. At visit 3, subjects were randomly assigned to 2 treatment groups. Group A received 1 drop of olopatadine in the right eye and I drop of ketotifen in the left eye. Group B received 1 drop of olopatadine in the left eye and 1 drop of ketotifen in the right eye. Following drug instillation, the subjects assessed the comfort level in each eye. Twelve hours after instillation, subjects were challenged with the antigen concentration that elicited a positive response at the previous visits. Itching was subjectively graded at 3, 5, and 10 minutes postchallenge. Subjects were asked to choose which therapy they were more satisfied with. RESULTS: Twelve hours after administration, efficacy scores for olopatadine were significantly higher than those for ketotifen at 3 and 5 minutes postchallenge (1.84 and 1.75 vs 1.25 and 1.34; P < 0.05). Olopatadine-treated eyes were rated significantly more comfortable than those treated with ketotifen immediately after drug instillation (1.25 vs 2.09; P < 0.05) and 12 hours later, as measured by patient ratings of ocular comfort. Of the 22 subjects who had a preference, 16 (73%) were more satisfied with olopatadine than with ketotifen. CONCLUSIONS: Olopatadine is more effective than ketotifen in reducing the itching associated with allergic conjunctivitis in the antigen challenge model. Olopatadine caused less ocular discomfort than ketotifen and was preferred by approximately 3 times as many patients as was ketotifen.
Allergens↗
Medicosurgical approach to diagnosis and treatment of ectopic pregnancy.
Early ectopic pregnancy screening using vaginal ultrasonographic technology together with measurement of beta human chorionic gonadotropin (beta-hCG) and human chorionic somatomammotropin is possible within the first 2 weeks of the missing menses, prior to the appearance of symptoms. This article summarizes the main available treatment modalities, focusing primarily on the pelviscopic surgical tube-conserving approach and on instillation of intrachorionic drugs (methotrexate alone or in combination with ornipressin) and injection of prostaglandin F2 alpha. While the pelviscopic surgical approach can be applied in nearly all cases of ectopic pregnancy, irrespective of pregnancy duration, the pelviscopic medicosurgical approach is only appropriate for the treatment of early ectopic pregnancies until the 8th week of gestation in patients without fluid collection in the pouch of Douglas and beta-hCG values below 2000 mU/mL. The transvaginal intrachorionic drug instillation as a simple medicosurgical approach performed under ultrasonographic guidance without anesthesia remains restricted to the treatment of early viable ectopic pregnancy. A brief account of the expectant treatment of patients with nonviable ectopic pregnancy is given, underlining the prerequisites of decreasing beta-hCG values and the absence of fluid in the pouch of Douglas. Although spontaneous resorptions have been observed in a number of cases of the disease, no clear evidence is available on the reconstitution of tubal function and patency.
Chorionic Gonadotropin↗
[Internal medicine treatment of pleural empyema].
We made a retrospective analysis with regard to the bacteriology and to the therapy of all patients with pleural empyema who were treated in the district lung hospital from 1. 1. 1982-31. 12. 1986. 92 patients had a non-specific empyema, only 3 patients had a specific empyema. All patients were aspirated repeatedly with physiological saline solution instillation and antimicrobic drug instillation in the pleural cavity. This daily aspiration and lavage was successfully in 65 patients. This method was ineffective in 30 patients. We treated 7 patients of this group by the closed drainage (rubber-tube drain), in 4 patients successfully. 3 patients had to be treated by a surgical operation. An insufficient obliteration of the cavity of empyema occurred also in 23 patients of this group. A systematic daily aspiration for a longer time led to regression of the cavity in 4 cases, whereas a surgical operation was necessary in 19 patients. We consider the daily aspiration and lavage as an effective method in patients in early acute stages of empyema.
Bacterial Infections↗
Non-specific nasal provocation in children with chronic allergic rhinitis.
Twenty-three children with chronic allergic rhinitis (Group A) and eleven normal non-atopic subjects (group C) were submitted to non-specific nasal provocation tests with histamine (0.03; 0.06; 0.125; 0.25; 0.5; 1.0; 2.0 and 4.0 mg/ml), and one week later with methacholine (0.025; 0.1; 0.25, 0.5; 1.0; 2.5; 5.0 and 10.0 mg/ml). Measurements of total nasal resistance were performed by active anterior rhinomanometry (Berger, S.A.) and symptoms were recorded. Challenges were carried out in the morning with all children in an acclimatized room (25 degrees C/77 degrees F). Concentrations of the tested drugs were increasingly instilled, and after 5 min were followed by total nasal resistance, FEV, and FVC measurements. Considering as positive those tests in which total nasal resistance had a 100% increase, we observed that both histamine and methacholine caused an increase in total nasal resistance as instilled drug concentration rose; histamine provocations were significantly more positive among group A than group C patients (91% sensitivity, 80.8% positive predictive value). This was not observed with methacholine (55% sensitivity, 75% positive predictive value). In neither provocation was there correlation between the concentration that induced a positive response and symptoms. There were no changes in spirometric values during the tests. Nasal provocations with histamine and methacholine are safe and well tolerated. Histamine seems to be more adequate for differentiating children with allergic rhinitis from normal controls.
Adolescent↗
Effect of proparacaine on central corneal thickness values: an evaluation using noncontact specular microscopy and pentacam.
PURPOSE: To study the effect of 1 drop of 0.5% proparacaine on central corneal thickness values monitored by nonspecular microscopy and Pentacam, a corneal topographer with rotating Scheimpflug camera. METHODS: Forty subjects were divided into 2 groups with 1 group measured with a noncontact specular microscope and the other group with Pentacam (Oculus, Inc., Wetzlar, Germany). One eye was randomly selected, and corneal thickness values were monitored every 30 seconds for 10 minutes. Baseline corneal thickness values were defined as the average of all measurements taken over 10 minutes. One drop of 0.5% proparacaine was instilled, and the corneal thickness values were monitored by the same instrument every 30 seconds for another 10 minutes after drug instillation. RESULTS: The 2 groups shared similar age range, refractive error, and baseline corneal thickness values. The spontaneous variation of corneal thickness values was within 3 mum for 10 minutes before drug instillation. There was no obvious trend of corneal thickness value change after the instillation of local anesthetics. The variation of corneal thickness values against the baseline was within 5 mum. CONCLUSION: One drop of 0.5% proparacaine does not produce any significant change in central corneal thickness.
Adult↗