Compromise of the tissue circulation plays a significant role in the development of optic nerve damage in normal-tension glaucoma (NTG). To evaluate the effect of nifedipine on the blood flow of peripapillary retina, blood flow of 7 NTG patients were measured using Heidelberg Retina Flowmeter before and 1 hour after oral administration of nifedipine 5 mg.Before treatment, NTG eyes had significantly reduced blood flow than control eyes (245.99+/-132.91 vs.303.38 +/-121.07, p=0.036).After treatment, nifedipine increased blood flow (245.99 +/-132.91 vs.329.37 +/-189.17, p=0.005)and decreased intercapillary square (49.78 +/-17.30 micrometer vs.47.13 +/-15.13 micrometer , p=0.049)significantly in the NTG eyes, but did not affect blood flow in the control eyes (303.38 +/-121.07 vs.309 +/-85.53, p=0.756).These results show that glaucomatous optic nerve damage is accompanied with blood flow deficits and nifedipine improve ocular hemodynamics in normal-tension glaucoma.
Administration, Oral ; Flowmeters ; Glaucoma ; Hemodynamics ; Humans ; Nifedipine* ; Optic Nerve ; Retina

BACKGROUND: Intranasal drug administration has been suggested to be method for the treatment of various systemic cardiovascular disorders such as systemic hypertension and angina pectoris. Nifedipine is usually administered sublingually. We examined the efficacy of intranasal nifedipine for the treatment of hypertension during laparoscopic cholesystectomy. METHODS: After CO2 insufflation, we selected patients with blood pressures increased by 25%. Group I (n = 10) received nifedipine 10 mg intranasally and group II (n = 10) nifedipine 10 mg sublingually. Blood pressures and heart rates were recorded at 0, 1, 2, 3, 4, 5, 10, and 15 minutes after nifedipine administration. RESULTS: Significant decreases in blood pressure were observed from 2 to 15 minutes after administration in the intranasal group. Significant decreases in blood pressure in sublingual group were observed later than in the intranasal group. Significant increases in heart rate were observed from 4 to 15 minutes in the intranasal group, but no significant changes of heart rate in the sublingual group. CONCLUSIONS: Our results suggest that the administration of intranasal nifedipine is faster, more effective, and more convenient than sublingual nifedipine for the immediate control of hypertension associated with CO2 insufflation during laparoscopic cholecystectomy.
Administration, Intranasal ; Angina Pectoris ; Blood Pressure ; Cholecystectomy, Laparoscopic* ; Heart Rate ; Humans ; Hypertension* ; Insufflation ; Nifedipine*

The effect of intranasal nifedipine drops in 20 randomly chosen patients with diethyl-ether induced hypertension by inhalation anesthesia was observed. Patients were placed in two groups: the first group received intranasal nifedipine at the time of induction and the second group received intranasal nifedipine at the time to skin incision. The change in mean arterial pressure in the first group was not significant, but in the second group, the increase in mean arterial pressure was significant immediately after intranasal administration of nifedipine at the time of skin incision. An increase in pulse rate was noted with the increase in mean arterial pressure and this is thought to result from the stimulation of catecholamine secretion and baroreceptor reflex. Since the difference in mean arterial pressure between the two groups was minimal at ten minutes and twenty minutes after skin incision, it is suggested that the onset of intranasal nifedipine is quite fast. Based on the authors' experience, intranasal administration of nifedipine is very useful in preventing or treating hypertension during inhalation anesthesia using diethyl-ether.
Administration, Intranasal* ; Anesthesia, Inhalation ; Arterial Pressure ; Baroreflex ; Ether* ; Heart Rate ; Humans ; Hypertension ; Nifedipine* ; Skin

It is well known that hypertension is associated with left ventricular diastolic dysfunction which frequently precede systolic dysfunction. To determine whether nifedipine could improve left ventricular diastolic function in hypertensive patients, we studied 15 hypertensive patients and 15 normotensive subjects matched for sex, age with Doppler echocardiography. After oral administration of 10mg of nifedipine, there were no significant changes in Doppler-derived transmitral diastolic filling indexes of normotensive subjects. On the other hand, although peak flow velocity in atrial systole(PFVA), time velocity integral in atrial systole(TVIA) did not change significantly after nifedipine, nifedipine significantly increased peak flow velocity in early diastole(PFVE) from 40.2+/-6.4cm/sec to 46.5+/-10.9cm/sec(p<0.005), time velocity integral in early diastole(TVIE) from 5.24+/-1.2cm to 5.97+/-1.43cm(p<0.001), the ratio of PFVE/PFVA from 0.69+/-0.11 to 0.76+/-0.12(p<0.05), the ratio of TVIE/TVIA from 1.18+/-0.21 to 1.29+/-0.24(p<0.05), deceleration slope(DS) from 244.9+/-51.9cm/sec2 to 289.9+/-49.1cm/sec2 (p<0.001) and decreased isovolumic relaxation time(IVRT) from 132.3+/-10.3msec to 117.2+/-13.5msec(p<0.001), deceleration time(DT) from 168.8+/-30.3msec to 154.9+/-29.8msec(p<0.05) in hypertensive patients. These fimdings indicated that nifedipine improves Doppler-derived early diastolic filling indexes in hypertensive patients and may be related to improvement of active relaxation of left ventricle in early diastole.
Administration, Oral ; Deceleration ; Diastole ; Echocardiography, Doppler* ; Hand ; Heart Ventricles ; Humans ; Hypertension ; Nifedipine* ; Relaxation

OBJECTIVETo explore the in vitro anti-platelet effects of Ginsenoside -2A,a purified extract from Panax notoginseng.

METHODSPlatelet rich plasma (PRP) was prepared routinely from venous blood samples of patients with essential hypertension and normal persons. PRP was incubated with different concentrations of Nifedipine, Ginsenoside-2A ,and SK&F96365. Maximal platelet aggregation rate[ PAG (M) ] induced by 2 micromol/L ADP was taken as the observed index. Five-minute PAG( M) was determined for 5 consecutive times.

RESULTS(1) PAG (M) in essential hypertension group was 0. 89 +/- 0. 06, which was higher than that in the normal group (0. 68 +/-0. 07 ) with significant difference (P <0.01). (2)Nifedipine of two concentrations (10 p.mol/L,20 pVmol/L) had no effect on PAG(M) in either essential hypertension group or normal group(P >0. 05). (3)Different concentrations of SK&F96365 (2.5 micromol/L,5 micromol/L,10 micromol/L and 20 micromol/L) could inhibit the PAG(M) in essential hypertension group; (4) Differen concentrations of Ginsenoside -2A (2. 5 micromol/L, 5 micromol/L, 10 micromol/L and 20 micromol/L) could inhibit PAG ( M) in essential hypertension group; three concentrations of Ginsenoside -2A (5 micromol/L, 10 micromol/L, 20 micromol/L) could inhibit the PAG(M) in the normal group (all P <0.05).

CONCLUSIONPlatelet aggregating function in essential hypertension patients was obviously higher than that in the normal persons and platelets was in the high reactive status. Nifedipine had no inhibitive effect on platelet aggregation. SK&F96365 could inhibit the platelet aggregation. Ginsenoside-2A could inhibit platelet aggregation, and had the definite anti-platelet action.

Drugs, Chinese Herbal ; administration & dosage ; pharmacology ; Ginsenosides ; administration & dosage ; pharmacology ; Humans ; Imidazoles ; administration & dosage ; pharmacology ; Nifedipine ; administration & dosage ; pharmacology ; Platelet Aggregation Inhibitors ; administration & dosage ; pharmacology

AIMTo study the pharmacokinetics of m-nifedipine (m-Nif) in Beagle dogs.

METHODSThe Beagle dogs were divided into two groups. m-Nif was intravenously administered to the Beagle dogs in group 1 at the dose of 0. 288 mg x kg(-1), and it was orally administered to the Beagle dogs in group 2, 3 and 4 at the dose of 1.152, 3.456 and 10.370 mg x kg(-1), respectively. m-Nif in plasma was detected by reversed phase high performance liquid chromatography. The pharmacokinetic parameters were calculated by 3P97 software.

RESULTSWhen m-Nif was intravenously administered, the plasma concentration-time curve was fit to a two-compartment model and T1/2beta was 117 min. When m-Nif was orally administered, the plasma concentration-time curve was fit to a one-compartment model. T1/2 (Ke) and Cmax were 147 min and 20 microg x L(-1); at the low dose of 1.152 mg x kg(-1). T1/2 (Ke) was 122 min and Cmax was 36 microg x L(-1) at the middle dose of 3.456 mg x kg(-1). T1/2 (Ke) was 144 min and Cmax was 69 microg x L(-1) at the high dose of 10.37 mg x kg(-1), respectively.

CONCLUSIONIt was showed that the speed of elimination of m-Nif was high in Beagle dogs. The absolute bioavailability of m-Nif given orally was very low.

Administration, Oral ; Animals ; Area Under Curve ; Biological Availability ; Calcium Channel Blockers ; administration & dosage ; pharmacokinetics ; Dogs ; Injections, Intravenous ; Isomerism ; Nifedipine ; administration & dosage ; pharmacokinetics

AIMTo prepare nifedipine (NP) rapid release mini-tablet, sustained release mini-tablets, pulsed release mini-tablets and delayed-onset sustained release mini-tablets and develop multiplied pulsed drug delivery system (DDS), site-specific DDS, zero-order DDS and quick/slow DDS by various ways.

METHODSVelocity-time (v-t) equation of each mini-tablet was deduced by non-linear least square model fit. The difference of combinations in v-t profiles between theoretical value and test value was compared.

RESULTSAccording to the v-t equations, the combined release behaviors were observed directly from v-t profiles and the test values coincided with the theoretical profiles.

CONCLUSIONThe programmed DDS, which consist of a variety of mini-tablets with different dosages and combinations in capsules, could be predicted by summing up the v-t equation of each tablet.

Capsules ; Delayed-Action Preparations ; Drug Delivery Systems ; Models, Chemical ; Nifedipine ; administration & dosage ; chemistry ; Polyethylene Glycols ; administration & dosage ; chemistry ; Povidone ; administration & dosage ; analogs & derivatives ; chemistry ; Solubility ; Starch ; chemistry ; Tablets

AIMTo study unitary-core osmotic pump tablet for delivering water-insoluble drug for 24 hours.

METHODSUnitary-core osmotic pump tablet was prepared using nifedipine as the model drug. The effects of various core formulation variables on drug release were studied.

RESULTSPolyethylene oxide and potassium chloride have comparable positive effects on drug release, whereas, nifedipine has markedly negative effect on drug release.

CONCLUSIONUnitary-core osmotic pump tablet is very easy in preparation and it can deliver water-insoluble drug in substantially constant rate for 24 hours.

Calcium Channel Blockers ; administration & dosage ; chemistry ; Delayed-Action Preparations ; Drug Delivery Systems ; Nifedipine ; administration & dosage ; chemistry ; Osmosis ; Polyethylene Glycols ; pharmacology ; Potassium Chloride ; pharmacology ; Solubility ; Tablets ; Technology, Pharmaceutical ; methods

AIMTo evaluate the hemodynamic effects of aminophylline and nifedipine in patients with HAPE.

METHODS10 patients with HAPE undergone Swan-Ganz catheter. The parameters of hemodynamics and arterial blood gases in HAPE were measured before and after administration of nifedipine 20 mg sublingually and aminophylline 0.25 g intravenously respectively.

RESULTSAfter administering 0.25 g aminophylline the mPAP and PVR significantly decreased, the cardiac output and the level of PaO2, SaO2 increased obviously, the mSAP, HR did not change so much. After using 20 mg nifedipine, the mPAP, PVR and mSAP also decreased, while the cardiac output, HR and the level of PaO2, SaO2 did not show any changes.

CONCLUSIONBoth of aminophylline and nifedipine can attenuate pulmonary hypertension in patients with HAPE, but the effect of aminophylline was better than the effect of nifedipine.

Adult ; Altitude ; Altitude Sickness ; drug therapy ; Aminophylline ; administration & dosage ; therapeutic use ; Humans ; Hypertension, Pulmonary ; drug therapy ; Male ; Nifedipine ; administration & dosage ; therapeutic use ; Treatment Outcome

OBJECTIVETo compare the clinical efficacy and safety of sublingual nifedipine and intravenous urapidil in the treatment of acute postoperative hypertension.

METHODSThe clinical data of 215 patients with APH after tumorectomy were retrospectively analyzed, among whom 165 were treated with sublingual nifedipine and 50 with intravenously urapidil.

RESULTSTreatment with sublingual nifedipine caused a reduction of the systolic blood pressure by 5.9% and diastolic blood pressure by 5.2%. Urapidil treatment resulted in significantly greater reductions in the systolic and diastolic blood pressures (by 12.1% and 8.6%, respectively) (P(s)<0.001, P(d)=0.019). Urapidil treatment was associated with a significantly higher rate of adequate antihypertensive effect than nifedipine treatment (68% vs 35.8%, P<0.001).

CONCLUSIONAlthough both urapidil and nifedipine are associated with minimal adverse effects, intravenous urapidil shows better therapeutic effect than sublingual nifedipine and is more suitable for the treatment of APH.

Administration, Sublingual ; Aged ; Antihypertensive Agents ; administration & dosage ; Female ; Humans ; Hypertension ; drug therapy ; etiology ; Injections, Intravenous ; Male ; Middle Aged ; Neoplasms ; surgery ; Nifedipine ; administration & dosage ; Piperazines ; administration & dosage ; Postoperative Complications ; drug therapy ; Retrospective Studies