Cerebral vasospasm (CVS) is a frequent and serious neurosurgical complication, without sufficient therapy. This retrospective study was performed to analyze if nimodipine can improve prognosis and reduce ischaemia secondary to delayed CVS after intracranial tumour surgery. A retrospective review was performed over the years 2011 to 2012 for patients with an anterior cranial fossa tumour and underwent intracranial tumour surgery. The surgical field was soaked with nimodipine solution or normal saline. Transcranial Doppler ultrasonography was used to measure velocity in the middle cerebral artery (MCA) and the distal extracranial internal carotid artery (eICA). Follow-up was performed using the Glasgow Outcome Scale (GOS) after discharge. There were 94 patients that met the inclusion criteria. They included 50 males and 44 females, with a mean age of 49.6 years. In the nimodipine group, CVS occurred in 13 patients; 9 patients had CVS between 4 and 7 days, and 4 had CVS between 8 and 14 days. In the normal saline group, 19 patients had CVS, 3 presented with CVS within 3 days, 11 between 4-7 days and 5 between 8-14 days. A significant difference in the occurrence of CVS was observed between the two groups. Preoperative and postoperative the MCA velocities were compared, revealing a significant change in the normal saline group but not in the nimodipine group. Nimodipine markedly improves prognosis and significantly reduces ischaemia secondary to delayed CVS after intracranial tumour surgery, as well as the risks of mortality and morbidity.

• Klíčová slova
• cerebral vasospasm, intracranial tumour surgery, ischaemia, nimodipine,
• MeSH
• arteria cerebri media diagnostické zobrazování   chirurgie   účinky léků   MeSH
• časové faktory MeSH
• dospělí MeSH
• intrakraniální vazospazmus * etiologie   farmakoterapie   diagnostické zobrazování   MeSH
• lidé středního věku MeSH
• lidé MeSH
• nádory mozku * chirurgie   MeSH
• nimodipin * terapeutické užití   aplikace a dávkování   MeSH
• pooperační komplikace etiologie   prevence a kontrola   MeSH
• retrospektivní studie MeSH
• senioři MeSH
• Check Tag
• dospělí MeSH
• lidé středního věku MeSH
• lidé MeSH
• mužské pohlaví MeSH
• senioři MeSH
• ženské pohlaví MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• nimodipin * MeSH

The present work studied the effect of calcium channel blocker (nimodipine) on epileptic seizures elicited by electrical stimulation of somatosensory cortex in young rats exposed to hypoxia. Rats were exposed to different patterns of short-term hypoxia (hypobaric or normobaric) and reactions of cortical neurones were registered. In the youngest animals (12-day-old), the effect was minimal, in older rats prolongation or shortening of evoked epileptic seizures were registered after two types of hypoxia. The decrease of the duration of evoked epileptic seizures in control 12-day-old rats and any effect in older animals (in 25- and 35-day-old) after nimodipine administration was observed. In older rats (25- and 35-day-old) exposed to hypobaric hypoxia after pre-treatment with nimodipine (L-type calcium channel antagonist) the duration of epileptic seizures after repeated stimulation was increased.

• MeSH
• blokátory kalciových kanálů farmakologie   MeSH
• elektrická stimulace MeSH
• epilepsie etiologie   patofyziologie   MeSH
• hypoxie patofyziologie   MeSH
• krysa rodu Rattus MeSH
• nimodipin farmakologie   MeSH
• potkani Wistar MeSH
• somatosenzorické korové centrum patofyziologie   MeSH
• tlak vzduchu MeSH
• zvířata MeSH
• Check Tag
• krysa rodu Rattus MeSH
• mužské pohlaví MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• práce podpořená grantem MeSH
• Názvy látek
• blokátory kalciových kanálů MeSH
• nimodipin MeSH

The results of a comprehensive study of the dissolution of the calcium antagonist nimodipine in aqueous solutions of nine cyclodextrins are reported. The used cyclodextrins were native beta-cyclodextrin (beta-CD), its derivatives hydroxyethyl-beta-CD (HE-beta-CD), three hydroxypropyl-beta-CD (HP-beta-CD) with various degree of substitution and methyl-beta-CD (M-beta-CD), native alpha-cyclodextrin (alpha-CD), hydroxypropyl-alpha-CD (HP-alpha-CD) and hydroxypropyl-gamma-CD (HP-gamma-CD). The nimodipine dissolution was studied as a function of time (up to 14 days) and cyclodextrin concentration up to 0.07 mol/l, excepting the less soluble beta-CD. In this range of cyclodextrin concentration, linear phase diagrams of nimodipine solubility in the cyclodextrin solutions were observed. From them we derived the stability constants of the inclusions complexes nimodipine-cyclodextrin (1:1) as well as the empirical linear equations for the calculation of the saturated nimodipine concentration at a given cyclodextrin concentration. The most efficient solubiliser of nimodipine was M-beta-CD, a good solubilizing efficiency was also shown by HE-beta-CD and HP-beta-CDs (with a low degree of substitution), which may be acceptable for the preparation of parenteral nimodipine solutions.

• MeSH
• blokátory kalciových kanálů chemie   MeSH
• cyklodextriny chemie   MeSH
• farmaceutická chemie MeSH
• nimodipin chemie   MeSH
• rozpustnost MeSH
• Publikační typ
• anglický abstrakt MeSH
• časopisecké články MeSH
• práce podpořená grantem MeSH
• Názvy látek
• blokátory kalciových kanálů MeSH
• cyklodextriny MeSH
• nimodipin MeSH

Nifedipine [1,4-dihydro-2,6-dimethyl-4-(2-nitrophenyl)-3,5-pyridinedicarboxylic+ ++ acid dimethyl ester] and nimodipine [1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylic+ ++ acid 2-methoxyethyl 1-methylethyl ester], incorporated into diheptanoylphosphatidylcholine liposomes, which were used as a drug carrier system, slightly inhibited lipid peroxidation (induced by tert-butylhydroperoxide and Fe2+) in rat heart homogenate. Illumination of nimodipine had no effect on its antioxidant potency, whereas illuminated nifedipine was several times more effective than nonilluminated drug. On illumination, nifedipine converts to 2,6-dimethyl-4-(2-nitrosophenyl)-3,5-pyridinedicarboxylic acid dimethyl ester (NTP). NTP formed stable radicals when interacting with the rat heart homogenate and dioleoylphosphatidylcholine, as detected by EPR spectroscopy. No radical formation was observed if nonilluminated nifedipine and nimodipine or illuminated nimodipine were used. The spin density of the unpaired electron in the NTP-adduct was centered on the nitrogen derived from its nitroso group. The motion of the NTP-adduct radical was restricted, indicating that the radicals were located in the membrane of the homogenate and not in the buffer system. Only NTP (not nifedipine or nimodipine) was effective in trapping free radicals formed by the thermal or photoinduced decomposition of 2,2'-azobisisobutyronitrile and radicals formed by photolysis of di-tert-butylperoxide. The antioxidant and spin-trapping properties of NTP in our systems were attributed to its nitroso group.

• MeSH
• antioxidancia farmakologie   MeSH
• dihydropyridiny metabolismus   MeSH
• elektronová paramagnetická rezonance MeSH
• krysa rodu Rattus MeSH
• nifedipin metabolismus   farmakologie   MeSH
• nimodipin metabolismus   farmakologie   MeSH
• peroxidace lipidů účinky léků   MeSH
• srdce účinky léků   MeSH
• světlo MeSH
• volné radikály MeSH
• zvířata MeSH
• Check Tag
• krysa rodu Rattus MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• 2,6-dimethyl-4-(2'-nitrosophenyl)-3,5-pyridinedicarboxylic acid dimethyl ester MeSH Prohlížeč
• antioxidancia MeSH
• dihydropyridiny MeSH
• nifedipin MeSH
• nimodipin MeSH
• volné radikály MeSH

BACKGROUND: The blood supply to tissues is reduced as a result of arterial occlusions. Angiogenesis, collateral circulation and reverse flow mechanisms go into operation to restore a continued adequate supply of blood. Ca++ channels undertake the major part of this function. As a result of the increasing tension on the arterial walls, vascular autonomy is affected, and ischemia and even necrosis are observed. METHOD: Adult 100 male hybrid rabbits were used in this study. The bilateral carotid arteries were ligated at the carotid bifurcation. The rabbits were divided into 2 main groups: treatment and control, and then both groups were further divided into 5 subgroups consisting of 10 rabbits each. The rabbits were sacrificed between the first day and the end of 8 weeks for histopathological examination of the basilar artery in two groups. RESULTS: In control groups, after 24 hours of the occlusion partial swelling and minor endothelial damage were observed in histopathological sections of the basilar artery. Luminal flattening started to decrease, and expanding of the diameter continued. The increase in the diameters of the basilar artery was higher in animals treated by nimodipine, and that difference was statistically significant (P=0,000). CONCLUSION: This study revealed that the intimal and medial alterations arising from the increased blood flow rate in the basilar artery might be lessened and even partially prevented by the use of nimodipine.

• MeSH
• arteria basilaris účinky léků   patologie   MeSH
• arteria carotis communis fyziologie   chirurgie   MeSH
• blokátory kalciových kanálů farmakologie   MeSH
• králíci MeSH
• ligace MeSH
• nimodipin farmakologie   MeSH
• rychlost toku krve MeSH
• vazodilatancia farmakologie   MeSH
• zvířata MeSH
• Check Tag
• králíci MeSH
• mužské pohlaví MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• blokátory kalciových kanálů MeSH
• nimodipin MeSH
• vazodilatancia MeSH

Nimodipine, a calcium antagonist, was administered to 33 patients with subarachnoidal haemorrhage as prophylaxis of late ischaemic neurological deficiency. Despite the relatively high frequency of vasospasm during repeated angiographic examinations (27%), the general therapeutic effect in the group of treated patients was favourable. 52% patients improved and had no or only a minimal neurological deficit. Possible mechanisms of the favourable effect of nimodipine in subarachnoidal haemorrhage are mentioned in the discussion.

• MeSH
• dospělí MeSH
• lidé středního věku MeSH
• lidé MeSH
• nimodipin terapeutické užití   MeSH
• senioři MeSH
• subarachnoidální krvácení komplikace   MeSH
• tranzitorní ischemická ataka etiologie   prevence a kontrola   MeSH
• Check Tag
• dospělí MeSH
• lidé středního věku MeSH
• lidé MeSH
• mužské pohlaví MeSH
• senioři MeSH
• ženské pohlaví MeSH
• Publikační typ
• anglický abstrakt MeSH
• časopisecké články MeSH
• Názvy látek
• nimodipin MeSH

The dissolution curves of the substance of the calcium antagonist nimodipine in aqueous solutions of four cyclodextrins were determined at ambient temperature in the course of 14 days. The used cyclodextrins were alpha-cyclodextrin (alpha-CD), hydroxypropyl-alpha-cyclodextrin (HP-alpha-CD), methyl-beta-cyclodextrin (M-beta-CD, random-methylated), and hydroxypropyl-gamma-cyclodextrin (HP-gamma-CD) and their respective concentrations were always 0.05 mol/l. According to the measured dissolution curves, M-beta-CD in aqueous medium was a highly efficient solubiliser, capable to dissolve otherwise sparingly soluble nimodipine into a time-stable aqueous solution, with the saturated concentration of nimodipine 5.15 x 10(-4) mol/l (21.5 mg/100 ml) under the given conditions. M-beta-CD thus appeared to be a more efficient solubiliser than the previously studied HP-beta-CD. The solubilising power of HP-alpha-CD and HP-gamma-CD was much lower and alpha-CD practically did not improve long-term solubility of nimodipine in water. However, in the presence of alpha-CD, HP-alpha-CD, and HP-gamma-CD, respectively, repeated shortterm episodes of formation of supersaturated solutions of nimodipine were observed on the dissolution curves, characterised by peaks of nimodipine concentration. Similar supersaturation episodes were previously observed in the presence of HP-beta-CD. Since the supersaturation caused by cyclodextrins reportedly substantially improved the biological availability of some drugs, the above-mentioned cyclodextrins, and especially natural alpha-CD, could be useful for the enhancement of the low availability of nimodipine from solid oral drug preparations.

• MeSH
• blokátory kalciových kanálů chemie   MeSH
• cyklodextriny chemie   MeSH
• nimodipin chemie   MeSH
• rozpustnost MeSH
• roztoky MeSH
• Publikační typ
• anglický abstrakt MeSH
• časopisecké články MeSH
• práce podpořená grantem MeSH
• Názvy látek
• blokátory kalciových kanálů MeSH
• cyklodextriny MeSH
• nimodipin MeSH
• roztoky MeSH

BACKGROUND: Clinically symptomatic vasospasm leading to delayed ischemic neurological deficits occurs in up to 30% of patients with subarachnoid hemorrhage (SAH). Vasospasm can result in a serious decline in clinical conditions of patients with SAH, yet the algorithm for vasospasm treatment and prevention remains unclear. Intra-arterial administration of vasodilators is one of the modalities used for vasospasm therapy. METHODS: Over the last 7 years, we have treated 27 female and 7 male patients with vasospasm using intra-arterial administration of either nimodipine or milrinone; all had suffered aneurysm rupture. Of these patients, 28 were treated surgically (clip), and 6 patients had their aneurysm coiled. Spasmolytics were applied from day 2 to day 18 after rupture. RESULTS: Of the 53 procedures, angiographic improvement was documented in 92% of cases with a mean flow velocity decrease of 65 cm/s. Brain metabolism changes were monitored after the procedure. The highest level of immediate clinical improvement was observed in conscious patients with a focal neurological deficit (aphasia, hemiparesis). Overall clinical outcomes (Glasgow outcome scale, GOS) were as follows: GOS 5 (12 patients), GOS 4 (5 patients), GOS 3 (5 patients), GOS 2 (6 patients), and GOS 1 (6 patients). CONCLUSIONS: Intra-arterial administration of spasmolytics is a safe and potent method of vasospasm treatment. It is most effective when applied to conscious patients with a focal deficit. For unconscious patients, its therapeutic benefits are inconclusive. Patients in severe clinical states would further require use of other diagnostic tools such as multimodal brain monitoring to complement vasospasm therapy.

• Klíčová slova
• Angiography, Cerebral vasospasm, Microdialysis, Milrinone, Nimodipine, Outcome, Spasmolytics, Transcranial dopplerometry,
• MeSH
• angioplastika škodlivé účinky   metody   MeSH
• dospělí MeSH
• intraarteriální infuze škodlivé účinky   MeSH
• intrakraniální vazospazmus farmakoterapie   MeSH
• lidé středního věku MeSH
• lidé MeSH
• nimodipin aplikace a dávkování   terapeutické užití   MeSH
• subarachnoidální krvácení farmakoterapie   MeSH
• vazodilatancia aplikace a dávkování   terapeutické užití   MeSH
• Check Tag
• dospělí MeSH
• lidé středního věku MeSH
• lidé MeSH
• mužské pohlaví MeSH
• ženské pohlaví MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• nimodipin MeSH
• vazodilatancia MeSH

Aneurysmal subarachnoid hemorrhage (aSAH) is a life-threatening condition associated with the development of early brain injury (EBI) and delayed cerebral ischemia (DCI). Pharmacological treatment of vasospasm following aSAH currently mainly comprises nimodipine administration. In the past few years, many drugs that can potentially benefit cases of subarachnoid hemorrhage have become available. The objective of this review is to critically assess the effects of non-steroidal anti-inflammatory drugs (NSAIDs) following aSAH. A systematic literature review was conducted following PRISMA guidelines. The search was aimed at studies addressing aSAH and NSAIDs during the 2010 to 2019 period, and it yielded 13 articles. Following the application of search criteria, they were divided into two groups, one containing 6 clinical articles and the other containing 7 experimental articles on animal models of aSAH. Inflammatory cerebral changes after aneurysm rupture contribute to the development of EBI, DCI and cerebral vasospasm. It appears that NSAIDs (especially coxibs) are even more effective in reducing vasospasm than nimodipine. Other beneficial effects of NSAIDs include reduction in mortality, improved functional outcome and increased hypoaggregability. However, despite these positive effects, there is only one randomized, double-blind, placebo-controlled trial showing a tendency towards a better outcome with lower incidence of vasospasm or mortality in patients following aSAH.

• Klíčová slova
• Aneurysmal subarachnoid hemorrhage, Cerebral ischemia, Non-steroidal anti-inflammatory drugs, Vasospasms,
• MeSH
• antiflogistika nesteroidní terapeutické užití   MeSH
• dvojitá slepá metoda MeSH
• intrakraniální vazospazmus farmakoterapie   etiologie   patofyziologie   MeSH
• ischemie mozku farmakoterapie   etiologie   patofyziologie   MeSH
• lidé MeSH
• nimodipin terapeutické užití   MeSH
• randomizované kontrolované studie jako téma metody   MeSH
• subarachnoidální krvácení komplikace   farmakoterapie   patofyziologie   MeSH
• Check Tag
• lidé MeSH
• Publikační typ
• časopisecké články MeSH
• systematický přehled MeSH
• Názvy látek
• antiflogistika nesteroidní MeSH
• nimodipin MeSH

Native and substituted cyclodextrins (CDs) were used as chiral selectors both in high-performance liquid chromatography and capillary electromigration separations (HPCE and MEKC). Chromatographic data of five dihydropyridine calcium antagonists obtained on three beta-CD chiral stationary phases in reversed-phase mode were compared with those of capillary electrophoresis using beta-CDs in the presence and absence of sodium dodecyl sulfate (SDS). Competition of separated compounds with SDS molecules for penetration into the CD cavity can limit their necessary interaction with the chiral selector and consequently even preclude enantiomer separation. Some insight into this problem can be brought about by comparing the experimental data with computer-aided energy minimization of CD-solute and CD-SDS inclusion complexes.

• MeSH
• amlodipin analýza   chemie   MeSH
• blokátory kalciových kanálů analýza   chemie   MeSH
• cyklodextriny chemie   MeSH
• dihydropyridiny analýza   chemie   MeSH
• dodecylsíran sodný chemie   MeSH
• elektroforéza kapilární MeSH
• elektrolyty chemie   MeSH
• isradipin analýza   chemie   MeSH
• mikrosféry MeSH
• molekulární konformace MeSH
• nimodipin analýza   chemie   MeSH
• nisoldipin analýza   chemie   MeSH
• nitrendipin analýza   chemie   MeSH
• povrchově aktivní látky chemie   MeSH
• pufry MeSH
• rozpouštědla chemie   MeSH
• stereoizomerie MeSH
• vysokoúčinná kapalinová chromatografie MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• amlodipin MeSH
• blokátory kalciových kanálů MeSH
• cyklodextriny MeSH
• dihydropyridiny MeSH
• dodecylsíran sodný MeSH
• elektrolyty MeSH
• isradipin MeSH
• nimodipin MeSH
• nisoldipin MeSH
• nitrendipin MeSH
• povrchově aktivní látky MeSH
• pufry MeSH
• rozpouštědla MeSH