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PubMedDate not supplied

Inappropriate medication prescribing for the elderly by office-based physicians.

OBJECTIVE: To estimate the prevalence of inappropriate medications prescribed by office-based physicians for patients 65 years or older. DESIGN: A nationwide cross-sectional survey of office visits by the elderly. SETTING: The National Ambulatory Medical Care Survey (NAMCS) 1992, a national probability sample survey of office visits by ambulatory patients within the continental US. SUBJECTS: A national probability sample of patients 65 years or older visiting office-based physicians. National estimates are based on the National Center for Health Statistics weighting procedure for the NAMCS sample. MAIN OUTCOME MEASURES: Prevalence of 20 inappropriate medications that should be entirely avoided in the elderly, using criteria developed by a panel of national experts in geriatric medicine and geriatric pharmacology. RESULTS: In the US during 1992, an estimated 8.47 million (95% CI 7.66 million to 9.28 million) office visits by the elderly indicated prescribing of at least 1 of the 20 inappropriate medications. Approximately 7.75 million (95% CI 6.98 million to 8.52 million) visits by the elderly involved 1 inappropriate medication and 0.72 million (95% CI 0.51 million to 0.93 million) visits included 2 inappropriate medications. According to the NAMCS, office-based physicians prescribed at least 1 inappropriate medication to 7.58% of the elderly who received prescriptions. The most frequently prescribed inappropriate medications were propoxyphene, amitriptyline, dipyridamole, diazepam, and chlorpropamide. Elderly patients rarely received prescriptions from office-based physicians for drugs such as secobarbital, isoxsuprine, trimethobenzamide, and carisoprodol. Furthermore, office-based physicians did not prescribe cyclandelate, pentobarbital, or phenylbutazone for the elderly. CONCLUSIONS: The prescribing of inappropriate medications by office-based physicians raises concerns regarding the quality of care for the elderly in ambulatory settings. The crux of improving patient care in ambulatory settings rests with collaborative efforts between physicians and pharmacists.

Aged↗
PubMed1979

Effects of vasodilators on microcirculation of the rat cremaster muscle: a microscopic method for screening drugs.

Effects of vasodilating drugs on microcirculation of the rat cremaster muscle were investigated microscopically. Topical application and intravenous injection of papaverine produced dilatation of arterioles. Cyclandelate applied topically dilated the arterioles to a considerable extent. Topical application of bamethan induced arteriolar dilatation while bamethan given intravenously constricted the arterioles. Kallikrein applied topically induced a slight dilatation of arterioles, and intravenous administration of kallikrein produced an appreciable vasodilatation. Topical administration of bradykinin produced a vasodilatation of arterioles of the rat cremaster muscle. These results indicate that direct action of a drug on the microcirculation can be properly evaluated by the microscopic method in the rat cremater muscle, if the drug is applied topically, in the vicinity of small vessels under study.

Acetylcholine↗
PubMed1989

Flunarizine. A reappraisal of its pharmacological properties and therapeutic use in neurological disorders.

Flunarizine is a class IV calcium antagonist with a pharmacological profile which suggests its therapeutic potential in a number of neurological and cerebrovascular disorders. It is an effective prophylactic treatment for common or classic migraine in children and adults, and it appears at least as effective as a number of other agents which act by different pharmacological mechanisms, including pizotifen (pizotyline), cinnarizine, methysergide, nimodipine, metoprolol, propranolol, aspirin and cyclandelate. Flunarizine is also effective in reducing the frequency of seizures, when used as an 'add-on' treatment, in some patients with partial or generalised epilepsy resistant to maximal therapy with a combination of several conventional antiepileptic drugs. Placebo-controlled studies show that flunarizine is effective in the treatment of vertigo and associated symptoms of either peripheral or central origin, and in the treatment of cerebrovascular insufficiency where psychological symptoms, rather than vertigo, are the primary symptoms. In the treatment of vertigo, flunarizine appears at least as effective as cinnarizine and more effective than nicergoline, betahistine dichlorhydrate, pentoxifylline (oxpentifylline) and vincamine. Flunarizine therefore is useful in the prophylaxis of migraine, an effective treatment for vertigo and a worthwhile alternative as 'add-on' therapy in patients with epilepsy resistant to conventional drugs.

Animals↗
PubMed1998

A practical guide to the management and prevention of migraine.

Migraine is a paroxysmal disorder with attacks of headache, nausea, vomiting, photo- and phonophobia and malaise. Mild migraine attacks are treated with antiemetics followed by analgesics such as aspirin (acetylsalicylic acid), paracetamol (acetaminophen) or nonsteroidal anti-inflammatory drugs (NSAIDs). Moderate to severe attacks are treated by antiemetics combined with ergotamine or dihydroergotamine. Sumatriptan, a specific serotonin 5-HT1B/D receptor agonist, is used if attacks do not respond to ergotamine or if intolerable adverse effects occur. The new migraine drugs zolmitriptan, naratriptan, rizatriptan and eletriptan differ in their pharmacological profile from sumatriptan, but this translates into only minor differences in efficacy, headache recurrence and adverse effects. Migraine prophylaxis should be implemented when more than 3 attacks occur per month, if attacks do not respond to acute treatment or if the adverse effects of acute treatment are severe. Substances with proven efficacy include the beta-blockers metoprolol and propranolol and the calcium antagonist flunarizine. Drugs less effective or those with unpleasant adverse effects are the serotonin receptor antagonists (pizotifen, methysergide and lisuride), dihydroergotamine, cyclandelate, NSAIDs, valproic acid (sodium valproate) and amitriptyline. The efficacy of aspirin or magnesium is still under evaluation.

Analgesics↗
PubMed1999

[New prospects in the treatment of migraine].

The options for migraine treatment have increased in the recent years and will expand in the near future. In this work both recent and future options for migraine treatment are critically reviewed. Firstly the late advances in the symptomatic treatment of migraine, including the new 5-HT1B/D agonists "triptans" appeared after sumatriptan, are reviewed. Possible alternative, such as selective 5-HT1D and 5-HT1F agonists, are also discussed. In the second part of this manuscript the new, possible options for the preventive treatment of migraine comprising "antiepileptics", such as valproic acid, gabapentin and topiramate, calcium-antagonists, such as cyclandelate and dotarizin, and a miscellany, including riboflavin, are analysed. Finally, possible compounds for the future, such as the selective inhibitors of neurokinin receptors or drugs acting upon neuronal calcium channels, are commented. From this review we conclude that while there have been relevant advances in the symptomatic treatment of migraine, there is a need for the development of better preventive compounds.

Anticonvulsants↗
PubMed1992

Dihydropyridine- and omega-conotoxin-resistant, neomycin-sensitive calcium channels mediate the depolarization-induced increase in internal calcium levels in cortical slices from immature rat brain.

In order to characterize pharmacologically voltage-operated calcium channels in the rat brain, we have developed a technique to measure intracellular calcium levels ([Ca++]i) in immature rat cortical slices loaded with the fluorescent calcium probe Fura-2. KCl depolarization caused a rapid and reversible increase in cortical [Ca++]i. A significant increase was already observed at 20 mM KCl and the maximal effect was obtained at 77 mM. This response was not modified when extracellular Na+ was substituted by the nonpermeant cation bis(2-hydroxyethyl)-dimethylammonium chloride and was insensitive to the Na+ channel blocker tetrodotoxin (1 microM). In the absence of extracellular Ca++, KCl (50 mM) failed to increase [Ca++]i. The KCl (50 mM)-induced increase in [Ca++]i was not affected by the L-type calcium channel blockers nifedipine and isradipine and was only partially inhibited (by less than 30% at 50 microM) by verapamil and diltiazem. In contrast, nimodipine prevented this response by 41% at 50 microM. Flunarizine (a nonselective T channel blocker) inhibited the KCl response by 47% at 30 microM, whereas nicergoline (another nonselective T channel blocker) reduced this entry by 74% at 300 microM (IC50 = 120 microM). Cyclandelate, an atypical calcium antagonist, inhibited KCl-induced increase in [Ca++]i with a maximal effect of 41% at 30 microM, whereas perhexiline was inactive. The KCl-induced rise in [Ca++]i was only marginally inhibited by omega-conotoxin with a maximal effect of 20% from 1 nM to 1 microM.(ABSTRACT TRUNCATED AT 250 WORDS)

Aminoglycosides↗
PubMed1977

Influence of hypercapnia on the cerebrovascular activities of some drugs used in the treatment of cerebral ischemia.

The effects of twelve substances on local cerebral blood flow (LCBF) were studied in the normocapnic and hypercapnic conscious rabbit. In normocapnia, an increase in LCBF was observed after naftidrofuryl (NAF), cinnarizine (CI), viquidil (VI) and heptaminol acefyllinate (HA). The LCBF was only slightly increased or unchanged after hydrogenated ergot alkaloids (HEA), cyclandelate (CY), hexobendine (HE), ifenprodil (IF), piridoxilate (PI), vincamine (VC) and xantinol niacate (XN). It was reduced by theophylline (TH). In hypercapnia, a more pronounced increase in LCBF than in normocapnia was seen with CY, HE, NAF, and VI and a decrease or lesser effect with HA, IF, VC and XN. The decrease in LCBF with TH was enhanced by hypercapnia. The effects of CI, HEA and PI were not modified. The therapeutic implication of these modifications of drug effects by hypercapnia, is discussed.

Animals↗
PubMed1984

Effects of calcium antagonists and vasodilators on arterial myosin phosphorylation and actin-myosin interactions.

The mechanism of action of many direct-acting vascular smooth muscle relaxant agents is undefined. Moreover, an additional intracellular locus of action for some Ca++ entry blockers has been proposed. We have examined the potential for direct action by some of these agents at the level of smooth muscle contractile proteins by quantitating changes in Ca++-dependent superprecipitation of native arterial actomyosin. Moreover, inasmuch as previous research has linked phosphorylation of the 20,000 dalton myosin light chain to Ca++-dependent regulation of contraction, effects on myosin phosphorylation also were quantitated. Whereas the standard calmodulin antagonist W-7 inhibited both parameters by approximately 50% at 10(-4) M, diazoxide, hydralazine, 3-isobutyl-1-methylxanthine, papaverine, propranolol, nifedipine, nitrendipine, sodium nitroprusside and verapamil did not significantly inhibit either parameter at equimolar concentrations. Cyclandelate significantly delayed the onset of superprecipitation, but did not affect the extent of superprecipitation or myosin phosphorylation. The Ca++ antagonists felodipine and diltiazem inhibited superprecipitation by approximately 25%. However, unlike W-7, or felodipine, diltiazem did not concomitantly inhibit myosin phosphorylation. Inhibition of superprecipitation by diltiazem was apparent at a concentration of 10(-6) M, was manifest by a rightward shift in the pCa relationship and could be attenuated by exogenous calmodulin. These results show that most vasodilators do not have direct effects on smooth muscle contractile protein function. However, diltiazem may inhibit Ca++-dependent arterial actin-myosin interactions by a mechanism which is independent of regulation of myosin light chain phosphorylation.

Actins↗
PubMed1994

[Clinical effect and experimental study of xijian tongshuan pill].

Xijian Tongshuan pill (XJTS), consisted of Siegesbeckia orientalis, Moschus moschiferus, Hirudo nipponica, Prunus Persicae, Carthamus tinctoruis, Ligusticum wallichi, Panax notoginseng, Angelica Sinensis, Borneolum, etc, were used in treating 70 patients with cerebral thrombosis. The marked effective rate was 82.9%, total effective rate was 96.7%. In control group A, Dextranum and Venoruton were used, in control group B cyclandelate capsule were used. The marked effective rate was 61.7% and 61.1% respectively, the total effective rate was 81.7% and 83.3%. The differences were significant (P < 0.01). The improvement of blood rheology and CT of brain were also significant (P < 0.01). The experiment proved that XJTS pill could inhibit and delay the thrombosis of rabbit, inhibit the platelet aggregation. Acute and subacute toxicity tests proved that XJTS pill was safe and effective.

Adult↗
PubMed1997

[Migraine--diagnosis, differential diagnosis and therapy].

Migraine is caused by intermittent brain dysfunction. Attacks result in severe unilateral headache with nausea, vomiting, photophobia, phonophobia and general weakness. The prevalence of migraine is 12 to 20% in women and 8 to 12% in man. Treatment of an acute attack is done by antiemetics in combination with analgesics. Severe migraine attacks are treated with ergotamine or sumatriptan. Parenteral treatment is performed most efficiently and safely with i.v. ASA. Frequent and severe attacks require prophylaxis. Drugs of first choice are metoprolol, propranolol, flunarizine and cyclandelate. Substances of second choice are valproic acid, DHE, pizotifen, methysergide and magnesium. Homeopathic remedies are not superior to placebo. Nonpharmacological treatment consists of sport therapy and muscle relaxation techniques.

Adrenergic beta-Antagonists↗
PubMed1979

Vasodilators in senile dementias: a review of the literature.

The rationale for the use of vasodilators in the aged has changed from the attempt to increase cerebral blood flow to the attempt to improve cerebral metabolism. Review of 102 studies of eight vasodilators showed that significantly more controlled studies claimed practical clinical benefit from drugs supposed to improve neuronal intermediary metabolism with secondary vasodilatation than from drugs supposed to have only vasodilator action (P less than .005). Studies of both classes of drugs often suffered from poor study design, inappropriate and inconsistent application of outcome measurements, as well as negative bias due to selection of severely demented subjects. Future studies should be placebo-controlled investigations of drugs with primarily metabolic action, address questions of dose and time response, consistently use appropriate outcome measurement, and concentrate on the elderly in whom cognitive improvement is possible.

Aged↗
PubMed1987

Inhibition of cellular cholesterol esterification can decrease low density lipoprotein receptor number in human fibroblasts.

In fibroblasts deprived of exogenous cholesterol to induce low density lipoprotein receptors there is a continuing flux of cholesterol esterification. The structurally unrelated inhibitors of acyl-CoA; cholesterol acyl-transferase, progesterone, trimethylcyclohexanyl mandelate and 3-[decyldimethylsilyl]-N-[2-(4-methylphenyl)-1-phenylethyl] propanamide, (58035), could all inhibit this basal rate of esterification within 1h of addition. Exposure of cholesterol-deprived fibroblasts for 17h to progesterone or trimethylcyclohexanyl mandelate caused decreased specific binding and metabolism of low density lipoprotein. The effect was not a direct inhibition of lipoprotein binding; it was time dependent and followed from the reversible inhibition of cholesterol esterification by these two compounds. The irreversible inhibition of esterification by 58035 left the receptor number unaffected. The results indicate that down regulation of low density lipoprotein receptors is initiated by accumulation of cholesterol in a specific intracellular pool. Inhibition of cholesterol esterification by progesterone and trimethylcyclohexanyl mandelate causes accumulation of cholesterol in this pool but 58035 does not.

Amides↗
PubMed1990

The pharmacotherapy of focal cortical ischaemia in the mouse.

The measurement of cortical omega 3 (peripheral-type benzodiazepine binding) site densities provides an accurate index for the detection and quantification of ischaemic brain lesions following middle cerebral artery occlusion (MCAO) in mice. Here, we have used this marker to assess the neuroprotective activity of potential anti-ischaemic drugs belonging to several chemical classes. In untreated mice, the mean infarcted volume measured 96 h after unilateral coagulation of the middle cerebral artery was 27.9 +/- 4.3 mm3 (17.5% of the hemisphere volume) and omega 3 site densities (measured by incubation with 3H-PK 11195) were increased by 107.3 +/- 4.8% (cortical homogenates) or by 81% (coronal brain sections). The administration of the anti-ischaemic agent SL 82.0715 (10 mg/kg i.p.), 5 min, 6 h and 18 h after the occlusion and then twice daily until sacrifice evoked a decrease of similar magnitude (ca. 60-70%) in the volume of the infarction and in the proliferation of omega 3 sites. The constant tissue sparing effect of SL 82.0715 allowed the examination of the window of therapeutic opportunity. A significant diminution of cortical omega 3 sites was still noted when the first administration was delayed until 3 h post-occlusion. Moreover, the protective effect of SL 82.0715 was enhanced by repeated treatment for the first 36 h but not thereafter. Based on the histological, autoradiographic and homogenate binding results obtained with SL 82.0715, we studied the protective effects of several competitive and non-competitive NMDA receptor antagonists. When administered according to the above-described standard protocol, these drugs reduced omega 3 site levels in cortical homogenates from MCAO mice in a dose-dependent manner. The dose preventing by 50% the increase in omega 3 site levels (in mg/kg i.p.) and the maximal inhibition were respectively: MK-801 (0.2, 93%); TCP (1.6, 66%); kynurenate (260, 58%); ifenprodil (7.0, 58%); SL 82.0715 (1.1, 72%); CGS 19755 (46% at 10 mg/kg); dextromethorphan (46% at 30 mg/kg). In contrast, agents acting preferentially upon sigma (sigma) opiate receptors ((+)-3PPP, 1-10 mg/kg i.p. and haloperidol, 0.3-3 mg/kg i.p.) did not provide a significant protection. In general, calcium channel blockers (nimodipine, flunarizine, verapamil, perhexiline, diltiazem) were devoid of a clear neuroprotective potential when administered at non-toxic doses after the coagulation of the middle cerebral artery. Diltiazem (3 and 10 mg/kg i.p.) provided a significant protection when the first administration was performed 10 min prior to the occlusion. Limited protection was observed with adenosine A1 receptor agonists (N6-cyclohexyladenosine and 2-chloro-adenosine).(ABSTRACT TRUNCATED AT 400 WORDS)

Animals↗