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OBJECTIVE: To examine the effects of isoforskolin (isoF) and forskolin (FSK) suspensions administered topically in eyes with ocular hypertension (OHT) and to observe the local drug irritation. METHODS: Intraocular pressure (IOP) was measured with a pneumotonometer in screen spontaneous or water-loading induced OHT rabbits for evaluation of drug effects, and the irritation indices were also recorded. RESULTS: In screen OHT rabbits, isoF significantly lowered IOP from 0.5 to at least 4.5 hours after administration (p < 0.05, paired t test versus contralateral control eyes), with the maximum decreased of 0.25% and 1% isoF reaching 8.1 and 7.0 mmHg (1 mmHg = 0.133 kPa) at about 1.5 hours later, respectively. In water-loaded OHT rabbits, both 0.06%, 0.1%, 0.25% and 1% isoF and 1% FSK concentration-dependently suppressed the increments of IOP (p < 0.05, with the exception of 0.06% isoF) induced by water-loading, and the peak effects of the optical concentration of 0.25% isoF and 1% FSK were 7.1 and 6.9 mmHg (difference of IOP between bilateral eyes), respectively. The results also indicated that basically neither 0.25% isoF or FSK suspension displayed any irritation, but 1% induced slightly irritated responses during the experiment. CONCLUSIONS: Both isoF and FSK had suppressing effects on OHT in rabbits with the optical concentration being 0.25% and 1%, respectively; at a concentration of 0.25%, topically, basically neither drug displayed any irritation, while 1% of the drugs may induce mildly irritated responses.LA: Chinese
Dr. X. Lie, Yunnan Pharmacological Laboratories of Natural Products, Kunming Medical College, Kunming 650031, China. YMX2000@yahoo.com
11.14 Investigational drugs; pharmacological experiments (Part of: 11 Medical treatment)