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1.
M Chaffman  R N Brogden 《Drugs》1985,29(5):387-454
Diltiazem is an orally and intravenously active calcium channel blocking agent shown to be an effective and well-tolerated treatment for stable angina and angina due to coronary artery spasm. Its efficacy in these diseases has generally been similar to that of nifedipine or verapamil - alternative calcium channel blockers with which diltiazem has many electrophysiological, haemodynamic, and antiarrhythmic similarities. The antianginal mechanism of diltiazem cannot be precisely described; however, it appears to increase myocardial oxygen supply and decrease myocardial oxygen demand, mainly by coronary artery dilatation and/or via both direct and indirect haemodynamic alterations. Diltiazem has also shown substantial efficacy in the treatment of unstable angina, hypertension, and supraventricular tachyarrhythmias, but further study is necessary before its place in the treatment of these diseases may be clearly established. Although headache due to peripheral vasodilatation and depression of atrioventricular nodal conduction may be troublesome, side effects occur in only 2 to 10% of patients receiving diltiazem and are generally minor in nature. Thus, diltiazem offers a worthwhile alternative to other agents currently available for the treatment of angina pectoris. Although the infrequency of serious side effects may offer an advantage, its relative place in therapy compared with that of other calcium channel blockers remains to be clarified.  相似文献   

2.
Tocainide is an antiarrhythmic drug structurally related to lignocaine with similar electrophysiological, haemodynamic and antiarrhythmic effects. In contrast to lignocaine (lidocaine) it is well absorbed after oral administration and has a plasma half-life of about 15 hours. In several open and controlled therapeutic trials in patients with ventricular arrhythmias, often following a myocardial infarction, tocainide has been relatively effective and usually well tolerated. In treating ventricular ectopic beats and/or ventricular tachycardia tocainide has demonstrated effective suppression in 60 to 70% of patients in both open and controlled studies. It has an acute effect when infused in patients with ventricular arrhythmias complicating myocardial infarction, as well as a prophylactic effect when given orally. The majority of these studies have demonstrated tocainide to be more effective than placebo, but trials against other antiarrhythmic agents are few in number and vary in design. One study combining an infusion of tocainide with oral therapy compared to a bolus injection of lignocaine followed by a constant infusion in patients after myocardial infarction, found the two agents to be of similar efficacy. The most common adverse effects are neurological and gastrointestinal in nature, nausea and dizziness occurring most frequently. Adverse effects resulting in termination of therapy have been reported in about 16% of patients. Aggravation of pre-existing heart failure, increased ventricular arrhythmia, deterioration of conduction disturbances, convulsions, and cases of lupus erythematosus syndrome have occasionally been reported. Thus, tocainide appears to offer a worthwhile addition to the other antiarrhythmic agents available for ventricular arrhythmias. However, its relative place in therapy compared with other antiarrhythmic drugs is not yet clearly established.  相似文献   

3.
This study reports the results of long-term (24 weeks) low-dose prophylaxis in 26 young female patients suffering from recurrent uncomplicated urinary tract infection (UTI). The patients were randomized in a double-blind manner to treatment with 100 mg trimethoprim (TMP, 12 patients) or 500 mg cinoxacin (CNO, 14 patients) at bedtime. The duration of prophylaxis in the TMP group was 2016 and in the CNO group 2352 days. Blood chemistry, haematological and urinary parameters were closely monitored during treatment and the latter were followed for a further 4-6 weeks. The prophylactic efficacy of the drugs was equal and significant (p less than 0.05). In the TMP group one recurrence and in the CNO group two recurrences occurred during treatment, two recurrences being observed in each group during the follow-up period of 4-6 weeks. Trimethoprim is well documented and widely used; cinoxacin provides a new alternative for long-term prophylaxis.  相似文献   

4.
J K Errick  R C Heel 《Drugs》1983,26(3):191-211
Nalbuphine is an agonist/antagonist analgesic. After parenteral administration of 'usual' doses it is approximately equipotent in analgesic activity to morphine on a weight basis. In studies in patients with moderate to severe pain, usually following surgery, the characteristics of analgesia with nalbuphine were comparable to those seen with equianalgesic doses of morphine or pentazocine. It also appears to produce satisfactory anaesthesia when used as a component of a 'balanced' anaesthesia technique, although a relatively low 'ceiling' effect for reduction of anaesthetic requirements with nalbuphine may limit its usefulness in this regard. As with other agonist/antagonist analgesics, a 'ceiling' effect to nalbuphine-induced respiratory depression is also seen, beyond which further depression does not readily occur. However, with usual analgesic doses, respiratory depression seen with nalbuphine is comparable to that with morphine. Important haemodynamic changes have not occurred after usual doses of nalbuphine, even in patients with cardiac disease. Like other agonist/antagonist analgesic drugs, the abuse potential of nalbuphine seems relatively low, but only wider clinical use for longer periods can establish this with certainty. Thus, nalbuphine appears to offer a useful alternative to morphine in patients with moderate to severe pain.  相似文献   

5.
H D Langtry  D McTavish 《Drugs》1990,40(5):748-761
Terodiline has both anticholinergic and calcium antagonist properties and, as a result, effectively reduces abnormal bladder contractions caused by detrusor instability. When administered to adult patients with urge incontinence (generally as a 25mg twice-daily dose) terodiline reduces diurnal and nocturnal micturition frequency and incontinence episodes. In studies also assessing cystometric parameters, bladder volume at first urge and bladder capacity are increased. Children with diurnal enuresis respond similarly to a daily 25mg dose. Several studies have shown that terodiline 50 mg/day is preferred by patients when compared with emepronium 600 mg/day or flavoxate 600 mg/day, and tends to reduce voluntary micturition frequency and episodes of incontinence more effectively than these drugs. Terodiline is well tolerated in short and long term (up to 3.5 years) studies. Anticholinergic effects are most commonly reported; other adverse effects occur equally during terodiline and placebo treatment. Thus, terodiline is effective and well tolerated in patients with urge incontinence or neurogenic bladder dysfunction, and will claim an important place in the treatment of such patients in light of the limitations of alternative therapies.  相似文献   

6.
P A Todd  P Benfield 《Drugs》1990,39(1):110-135
Ramipril is a long acting angiotensin converting enzyme (ACE) inhibitor, which exhibits similar pharmacodynamic properties to captopril and enalapril. Like enalapril it is a prodrug, which is hydrolysed after absorption to form the active metabolite ramiprilat which has a long elimination half-life, permitting once daily administration. In hypertensive patients daily doses in the range 2.5 to 20 mg are usually effective in reducing high blood pressure and maintaining satisfactory control during long term treatment. Patients who do not respond adequately to monotherapy with ramipril usually respond with the addition of a diuretic such as hydrochlorothiazide or piretanide. Ramipril 5 to 10 mg once daily shows comparable antihypertensive efficacy to usual therapeutic dosages of captopril, enalapril and atenolol in patients with mild to moderate essential hypertension. Preliminary data indicate that ramipril may be effective in indications such as severe essential hypertension and renal hypertension. It has also displayed beneficial effects in patients with moderate to severe congestive heart failure. Ramipril has been well tolerated and exhibits an adverse effect profile typical of ACE inhibitors as a class. In conclusion, ramipril will likely represent a useful alternative ACE inhibitor for use in patients with hypertension or congestive heart failure.  相似文献   

7.
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9.
D McTavish  K L Goa  M Ferrill 《Drugs》1990,39(4):552-574
Terfenadine is a selective histamine H1-receptor antagonist which, in pharmacodynamic studies, is devoid of central nervous system depressant activity. In clinical studies terfenadine is well tolerated and at a dose of 60mg administered twice daily the drug provides effective relief of symptoms in patients with allergic rhinitis (seasonal and perennial), allergic dermatological conditions (particularly chronic urticaria), and other histamine-mediated disorders. Terfenadine is superior to placebo, has a more rapid onset of action than astemizole and is as effective as most other histamine H1-receptor antagonists, in relieving rhinitis symptoms. In allergic rhinitis, terfenadine relieves ocular symptoms to a greater extent (but nasal symptoms to a lesser extent) than inhaled corticosteroids. Administration of oral terfenadine with inhaled sodium cromoglycate (cromolyn sodium) or an inhaled corticosteroid appears more effective than terfenadine alone. Despite the absence of CNS depressant activity in pharmacodynamic studies, sedation is the adverse effect most frequently associated with terfenadine treatment. However, it is important to realise that the incidence of this adverse effect is similar in terfenadine and placebo recipients, and is less frequent than with traditional histamine H1-receptor antagonists. In conclusion, terfenadine is a clinically effective antihistamine which has an improved adverse effect profile compared with classic histamine H1-receptor antagonists. Like other nonsedating antihistamines, it can be considered as a first-line agent in the treatment of allergic rhinitis and chronic urticaria. With additional clinical experience, the drug could find a similar role in other disorders in which a histamine H1-receptor antagonist is indicated.  相似文献   

10.
A Fitton  M T Buckley 《Drugs》1990,40(1):138-167
Moricizine (moracizine, ethmozine) is an orally active phenothiazine derivative with direct myocardial Class I antiarrhythmic activity and minimal CNS effects. Placebo-controlled studies have confirmed its efficacy in suppressing nonmalignant ventricular arrhythmias (premature ventricular complexes, couplets and runs of nonsustained ventricular tachycardia), including those refractory to previous antiarrhythmic therapy. Preliminary findings have indicated that moricizine is also effective in suppressing atrial ectopic activity, atrioventricular nodal re-entry tachycardia and Wolff-Parkinson-White tachycardias involving accessory pathways. As with other oral antiarrhythmics, malignant ventricular arrhythmias (sustained ventricular tachycardia and ventricular fibrillation) have been shown, both on noninvasive monitoring and programmed electrical stimulation, to be less susceptible to suppression by moricizine than nonmalignant ventricular arrhythmias. The therapeutic potential of moricizine is enhanced by its relatively low incidence of extra-cardiac adverse effects (predominantly gastrointestinal and neurological) and its lack of significant cardiodepressant activity in patients with normal or mildly to moderality depressed left ventricular function. Moricizine has proved to be more effective than disopyramide and propranolol in suppressing ventricular ectopic activity, of comparable efficacy to quinidine, but less effective than encainide and flecainide. The drug appears to be particularly suited to the suppression of ventricular ectopy in patients with preexisting left ventricular dysfunction. Further studies are required to confirm its long term efficacy and effects on mortality when used prophylactically in patients at increased risk of sudden cardiac death.  相似文献   

11.
A N Wadworth  R N Brogden 《Drugs》1991,41(3):378-399
Quinapril is a monoethyl ester which is hydrolysed after absorption to form an active metabolite, quinaprilat, which is a more potent angiotensin converting enzyme (ACE) inhibitor than the parent drug. Quinaprilat has a short elimination half-life but a potent binding affinity for ACE which enables once daily administration. Data from clinical studies indicate that quinapril 10 to 40 mg daily, given as a single dose, is an effective antihypertensive agent, suitable as monotherapy for reducing high blood pressure and maintaining satisfactory control during long term treatment of mild to severe hypertension. Dosages of 80 mg daily have been used in some patients. Concomitant diuretic therapy usually elicits a response in patients who fail to respond adequately to monotherapy. Initial studies suggest that quinapril also has a role in the treatment of mild to severe congestive heart failure. In the few long term studies conducted the beneficial acute haemodynamic effects were maintained during long term treatment and were accompanied by symptomatic and functional improvement. The majority of these patients responded to twice daily administration. Adverse effects associated with the antihypertensive action of quinapril are generally mild, well tolerated and are similar to those of other ACE inhibitors. Thus, quinapril appears to be a useful alternative ACE inhibitor for the treatment of mild to severe hypertension and congestive heart failure.  相似文献   

12.
Nimodipine is a dihydropyridine calcium antagonist which dilates cerebral blood vessels and increases cerebral blood flow in animals and humans. Preliminary findings reveal its potential benefit for the treatment of a wide range of cerebrovascular disorders, particularly for prophylaxis and treatment of delayed ischaemic neurological deficits resulting from cerebral vasospasm in patients with subarachnoid haemorrhage. Studies involving patients aged up to 79 years have confirmed these preliminary findings by showing that nimodipine reduces the incidence of severe ischaemic deficit after subarachnoid haemorrhage. Initial results from studies of patients with acute ischaemic stroke indicate that nimodipine, started within 72 hours of onset, improved recovery, particularly in patients over 65 years. However, other investigators have found no marked difference in 6-month mortality or morbidity rates of stroke patients aged up to 97 years. Findings from other studies suggest that nimodipine may improve symptoms of cognitive dysfunction in elderly patients. Nimodipine is well tolerated by both younger and older patients. The most frequently reported adverse event has been hypotension. Thus, nimodipine therapy offers important benefits as part of the approach to management of patients with subarachnoid haemorrhage and has potential in other cerebral disorders, including stroke and impaired cognitive function, although confirmation of initial results in patients with cerebral impairment are required.  相似文献   

13.
A Fitton  D McTavish 《Drugs》1991,41(2):289-318
Pamidronate [aminohydroxypropylidene diphosphonate disodium (APD), disodium pamidronate] is an orally and intravenously active amino-substituted bisphosphonate which produces potent and specific inhibition of bone resorption at doses devoid of any significant detrimental effect on bone growth and mineralisation. Clinical trials indicate that pamidronate is effective in a variety of conditions characterised by pathologically enhanced bone turnover, including Paget's disease, hypercalcaemia of malignancy, osteolytic bone metastasis, steroid-induced osteoporosis and idiopathic osteoporosis. Pamidronate is highly effective in restoring normocalcaemia in patients with hypercalcaemia of malignancy associated with bone metastases but, in common with other bisphosphonates, is marginally less effective against humoral hypercalcaemia of malignancy. Comparative studies in this area have suggested that, at therapeutic doses, pamidronate has a more pronounced calcium-lowering action than etidronate (etidronic acid) and clodronate (clodronic acid) and provides a longer period of normocalcaemic remission. In Paget's disease arrest and, in some patients, reversal of the progression of osteolytic lesions by pamidronate is associated with a sustained reduction in bone pain, improved mobility and a possible reduced risk of bone fracture. In patients with osteolytic bone metastasis pamidronate reduces skeletal morbidity and slows the progression of metastatic bone destruction. Long term use of low-dose pamidronate in conjunction with conventional antiosteoporotic therapy may halt bone loss in steroid-induced and idiopathic osteoporosis. Pamidronate appears to represent a valuable addition to the drugs currently available for the treatment of symptomatic Paget's disease and cancer-associated hypercalcaemia, and shows promise in the treatment of osteolytic bone metastasis and osteoporosis.  相似文献   

14.
K L Goa  A Ward 《Drugs》1986,32(2):114-129
Buspirone hydrochloride (HCl)1 is a new anxiolytic with a unique chemical structure. Its mechanism of action remains to be elucidated. Unlike the benzodiazepines, buspirone lacks hypnotic, anticonvulsant and muscle relaxant properties, and hence has been termed 'anxioselective'. As evidenced by a few double-blind clinical trials, buspirone 15 to 30 mg/day improves symptoms of anxiety assessed by standard rating scales similarly to diazepam, clorazepate, alprazolam and lorazepam. Like diazepam, buspirone is effective in patients with mixed anxiety/depression, although the number of patients studied to date is small. In several studies, a 'lagtime' of 1 to 2 weeks to the onset of anxiolytic effect has been noted; hence motivation of patient compliance may be necessary. Sedation occurs much less often after buspirone than after the benzodiazepines; other side effects are minor and infrequent. In healthy volunteers, buspirone does not impair psychomotor or cognitive function, and appears to have no additive effect with alcohol. Early evidence suggests that buspirone has limited potential for abuse and dependence. Thus, although only wider clinical use for longer periods of time will more clearly define some elements of its pharmacological profile, with its low incidence of sedation buspirone is a useful addition to the treatments available for generalised anxiety. It may well become the preferred therapy in patients in whom daytime alertness is particularly important.  相似文献   

15.
Pirbuterol is a beta-adrenoceptor agonist which differs structurally from salbutamol in the substitution of a pyridine ring for the benzene ring. In common with salbutamol, pirbuterol demonstrates both bronchodilatory and cardiovascular effects. Generally, improvements of up to 25% are noted in forced expiratory volume in 1 second (FEV1) [versus baseline or placebo] in asthmatic patients treated with pirbuterol for several months. In individual 12-week double-blind comparative studies, pirbuterol aerosol appeared similar to orciprenaline (metaproterenol) aerosol, and orally administered pirbuterol appeared similar to orally administered salbutamol in bronchodilator efficacy. However, well-designed long term comparative studies are needed to more clearly define the comparative efficacy of pirbuterol and alternative beta-adrenoceptor agonists.  相似文献   

16.
Tinidazole, like the structurally-related drug metronidazole, was initially introduced for treating protozoal infections. However, both these nitroimidazole compounds are also active in vitro against most clinically important obligate anaerobes. Most of the clinical experience with tinidazole to date has involved prophylactic use to prevent postoperative anaerobic infection. Prospective placebo-controlled studies demonstrated that a single dose of tinidazole administered orally prior to elective colorectal surgery significantly reduced postoperative infection. Similarly, when given intravenously prior to appendectomy, tinidazole reduced the incidence of postoperative infection in some subgroups of patients. Although results of non-blinded studies with prophylactic tinidazole were encouraging when used in women undergoing gynaecological surgery (mainly hysterectomy), results from double-blind placebo-controlled studies in this situation have been somewhat equivocal. Thus, although the overall weight of evidence suggests that the drug is effective in this area of use, further study is needed to clarify its role in preventing anaerobic infection following gynaecological surgery compared with other antibiotics which can also be used for this purpose. Relatively few studies have been conducted with tinidazole in the treatment of established anaerobic infections, and this is an area needing further investigation. The drug is well tolerated when administered orally or intravenously.  相似文献   

17.
18.
Loperamide, a butyramide derivative is a new agent for use in symptomatic control of acute non-specific diarrhoea and chronic diarrhoea. Unlike diphenoxylate or codeine, loperamide does not appear to exert opiate activity in man at normal therapeutic doses. In acute diarrhoea, loperamide provides more rapid control of symptoms than diphenoxylate when given in a flexible dosage according to unformed bowel movements, and in single dose studies 4mg loperamide has a much longer duration of effect than 5mg diphenoxylate. Loperamide is probably superior to diphenoxylate in providing symptomatic control of chronic diarrhoea such as that associated with chronic inflammatory bowel disease or following gastrointestinal surgery. It has been used for up to 3 years in such conditions without evidence of tolerance. The possibility of once daily dosage of loperamide in chronic diarrhoea is an advantage. Side-effects have not proved a problem.  相似文献   

19.
C Y Chew  J Collett  B N Singh 《Drugs》1979,17(3):161-181
Mexiletine is a new local anaesthetic antiarrhythmic agent whose chemical structure and electrophysiological properties closely resemble those of lignocaine although its anticonvulsant and pharmacokinetic properties differ from that drug. Unlike lignocaine (lidocaine) it is active following oral administration with a plasma half-life varying between 8 and 20 hours so that it can be administered twice or three times daily to sustain therapeutic plasma levels. The drug is effective when given intravenously or by the oral route in controlling ventricular arrhythmias especially following acute myocardial infarction but the side effects are greater during parenteral administration. Side effects during chronic oral therapy with mexiletine have not posed a serious problem. Mexiletine has the pharmacodynamic and pharmacokinetic properties of an agent suitable for the chronic oral prophylaxis of serious ventricular arrhythmias in patients with ischaemic heart disease.  相似文献   

20.
A Ward  R N Brogden 《Drugs》1988,36(6):732-753
Nimesulide is a new non-steroidal anti-inflammatory analgesic agent given orally or rectally on a twice daily basis in a number of inflammatory and pain states. Although still at an early stage of clinical assessment, preliminary evidence suggests that nimesulide 200 to 400mg daily is significantly more effective than placebo in reducing the pain, fever and inflammatory symptoms of chronic rheumatoid arthritis or osteoarthritis, respiratory tract infections, otorhinolaryngological diseases, soft tissue and oral cavity inflammation, dysmenorrhoea, phlebitis/thrombosis, urogenital disease and postoperative pain states. In a number of comparative studies, nimesulide has also been shown to be more effective than piroxicam (in osteoarthritis), paracetamol (acetaminophen) [in respiratory tract inflammation], benzydamine or naproxen (in otorhinolaryngological disease), phenylprenazone (in laryngotracheitis/bronchitis, respiratory inflammation and otorhinolaryngological disease), Serratia peptidases (in postoperative or dental pain, trauma and phlebitis), ketoprofen (in postoperative dental pain) and mefenamic acid (in dysmenorrhoea). In addition, the efficacy of nimesulide has been observed to be comparable with that of aspirin, with or without vitamin C, and mefenamic acid (in respiratory tract infection), ibuprofen (in soft tissue disease), naproxen (in respiratory tract inflammation, dysmenorrhoea and postoperative pain states), suprofen and paracetamol (in postoperative pain states), benzydamine (in genitourinary tract inflammation) and dipyrone, paracetamol or diclofenac (in fever). The safety profile of nimesulide has yet to be fully established, although initial evidence suggests the usual adverse effects associated with non-steroidal anti-inflammatory drugs occur, possibly with a lower incidence of gastrointestinal problems than with other members in its therapeutic class. Nimesulide, therefore, appears to offer a useful alternative to other non-steroidal anti-inflammatory drugs in the treatment of patients with inflammatory conditions and/or pain and fever states. However, further definition of its efficacy and tolerability is clearly required, particularly in comparison with established or other new drugs in its therapeutic class.  相似文献   

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