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Biomedical subjects

R N Brogden

Publications and source records attributed to R N Brogden.

At least 199 records · Page 11Linked to original sources
PubMed1979

Flurbiprofen: a review of its pharmacological properties and therapeutic use in rheumatic diseases.

Flurbiprofen, a phenylalkanoic acid derivative, is a non-steroidal anti-inflammatory, antipyretic, analgesic agent advocated for use in rheumatoid arthritis, degenerative joint disease, ankylosing spondylitis and allied conditions. Published data suggest that flurbiprofen 120 to 150 mg daily is comparable in effectiveness with therapeutic doses of aspirin (3 to 4 g) in rheumatoid arthritis, but generally causes fewer side effects. Flurbiprofen 150 to 300 mg appears to be comparable with 75 to 150 mg of indomethacin in rheumatoid arthritis and degenerative joint disease, and comparable with phenylbutazone or indomethacin in ankylosing spondylitis. In comparison with other non-steroidal agents, flurbiprofen appears to be at least as effective as naproxen, ibuprofen or sulindac, but generally causes more side effects than these drugs. However, as no one of the non-steroidal anti-inflammatory agents is the most suitable drug for all patients requiring such therapy, flurbiprofen should be considered along with other drugs of its type in the arthritic patient.

Animals↗
PubMed1978

Fenoterol: a review of its pharmacological properties and therapeutic efficacy in asthma.

Fenoterol, the 4-hydroxyphenyl derivative of orciprenaline, is a resorcinol derivative with relatively high selectivity for beta2-adrenoceptors. It is active in man after inhalation or oral administration and is indicated in the treatment of bronchospasm associated with asthma, bronchitis and other obstructive airway diseases. Clinical experience has shown that fenoterol is an effective bronchodilator with negligible effects on the cardiovascular system following aerosol administration of usual therapeutic doses. In children, inhaled fenoterol is effective in preventing exercise-induced asthma and administration of the aerosol in young children has been successfully used to terminate acute asthma attacks. In trials in adults, inhaled fenoterol was superior to placebo. In other controlled studies, it showed a tendency to cause a slightly greater maximum improvement in airway function as assessed spirometrically, and to have a longer duration of action than inhaled orciprenaline, salbutamol or terbutaline, although in these trials statistically significant differences were often not found. The onset of maximum effect is less rapid than with isoprenaline but is longer lasting. About 60% of the eventual maximum response to fenoterol is reached in the first few minutes after inhalation. Oral fenoterol is more effective than placebo, ephedrine or orciprenaline, and probably similar to salbutamol and terbutaline. Following usual aerosol doses, side-effects are minimal. Oral administration is associated with a higher incidence of side-effects than inhalation, including fine muscle tremor and tachycardia.

Adolescent↗
PubMed1978

Loperamide: a review of its pharmacological properties and therapeutic efficacy in diarrhoea.

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.

Acute Disease↗
PubMed1978

Cimetidine: a review of its pharmacological properties and therapeutic efficacy in peptic ulcer disease.

Cimetidine is a specific competitive histamine H2-receptor antagonist which effectively inhibits gastric acid secretion and is advocated for the treatment of chronic peptic ulceration, haemorrhage from erosive gastritis, and the control of gastric hypersecretion and peptic ulceration in the Zollinger-Ellison syndrome. Placebo-controlled trials in outpatients have demonstrated its efficacy in promoting the healing of endoscopically diagnosed duodenal ulceration, during a period of 4 to 6 weeks, but its role in the treatment of gastric ulcer is less clear. Preliminary evidence suggests that maintenance therapy with cimetidine reduces the rate of recurrence of duodenal ulcer, but further studies are required to clarify its role in this situation and in the treatment of oesophagitis and acute gastrointestinal haemorrhage. Cimetidine controls the peptic ulceration of Zollinger-Ellison syndrome in most patients when given continuously for up to 2 years. Side-effects have generally been trivial and have very seldom necessitated withdrawal of therapy except in the rare occurrence of gynaecomastia. The haematological abnormalities particularly agranulocytosis, which lead to the withdrawal from clinical use of metiamide, have not been reported with cimetidine, except for 1 case of transient neutropenia. The safety of long-term cimetidine administration has yet to be determined.

Acute Disease↗
PubMed1978

Loxapine: a review of its pharmacological properties and therapeutic efficacy as an antipsychotic agent.

Loxapine is a dibenzoxazepine, tricyclic compound recommended for the treatment of acute and chronic schizophrenia. In its therapeutic effectiveness and profile and incidence of side-effects, loxapine closely resembles the traditional antipsychotic agents. Although loxapine has tended to be less effective than some standard antipsychotic drugs in a few short-term (3 to 4 weeks) studies, it has been superior to a placebo and about as effective as chlorpromazine, haloperidol, trifluoperazine or thiothixene when evaluated after 4 to 12 weeks. Like the phenothiazine (e.g. chlorpromazine) and butyrophenone (e.g. haloperidol) antipsychotic agents, loxapine causes a high incidence of extrapyramidal reactions. Sedation occurs frequently, especially during early stages of treatment. Other, less common side-effects such as anticholinergic effects (dry mouth, blurred vision, etc.), hypotension, tachycardia and precipitation of epileptic seizures, which occur with the older antipsychotic drugs, have also been reported with loxapine.

Animals↗
PubMed1978

Labetalol: a review of its pharmacology and therapeutic use in hypertension.

Labetalol is an orally active adrenoceptor blocking drug which is a competitive antagonist at both alpha- and beta-adrenoceptor sites. Its beta-blocking effects resemble those of propranolol, but its overall haemodynamic effects are akin to those of a comination of propranolol and an alpha-adrenoceptor blocking drugs such as phenoxybenzamine. Unlike with conventional beta-adrenoceptor blocking drugs, acute administration of labetalol reduces peripheral vascular resistance and blood pressure and has little effect on cardiac output. Theoretically, labetalol has advantages over beta-adrenoceptor blocking drugs alone in the treatment of hypertension, but any real advantage, particulary in mild or moderate hypertension, has yet to be conclusively demonstrated in therapeutic trials. Labetalol may be particularly useful in some patients whose blood pressure is not adequately controlled by beta-adrenoceptor blocking drugs alone or combined with a diuretic, but possibly at the expense of a postural hypotensive effect. Postural hypotension is the most troublesome side-effect, occasionally necessitating withdrawal of therapy, but severe side-effects such as are seen with effective antihypertensive dosages of phenoxybenzamine do not occur with labetalol.

Adrenal Gland Neoplasms↗
PubMed1978

Tamoxifen: a review of its pharmacological properties and therapeutic use in the treatment of breast cancer.

Tamoxifen 1 is a triphenylethlene oestrogen antagonist which has partial oestrogen agonist activity in some species. Most therapeutic trials with tamoxifen have involved postmenopausal women with advanced brease cancer, about 25 to 60% of patients showing same improvement while receiving treatment (usually 20 or 40mg daily); however- poorly defined assessment criteria in some studies make it difficult to compare the results of different authors. 7 to 18% of patients have had complete clinical remissions lasting for a few months to several years. Although few comparative studies with other treatments have been done, it nevertheless appears that tamoxifen is at least as effective as standard oestrogen or androgen therapy in postmenopausal women, while producing a lower incidence of troublesome adverse effects. In the only comparison with a cytotoxic treatment regimen, the response rates with tamoxifen and cytotoxic therapy were similar (41% versus 50%) in patients who were more than 5 years postmenopausal and had primarily soft-tissue involvement; but in patients who were within 2 to 5 years of their last menstrual period cytotoxic treatment was more effective. Similarly, most authors have reported a higher response rate with tamoxifen in women several years postmenopausal than in those more recently postmenopausal. Tumours which contain receptors respond more often to tamoxifen than those which do not. Administering tamoxifen concomitantly with other chemotherapeutic agents such as cytotoxic drugs appears to increase the response rate, but as might be expected also increases the incidence of adverse reactions. When used alone tamoxifen has been relatively well tolerated in all studies, the overall withdrawal rate due to side-effects being less than 3%.

Animals↗
PubMed1978

Econazole: a review of its antifungal activity and therapeutic efficacy.

Econazole1 is a recently introduced imidazole antifungal agent which is very closely related structurally to another imidazole derivative, miconazole. For local application the nitrate salt of econazole is used, while in preliminary investigations of systemic use in a few patients econazole base has been administered orally or intravenously. In uncontrolled studies in large numbers of patients, econazole nitrate has been administered topically in the treatment of dermatomycoses due to a wide variety of fungi, and vaginally in the treatment of vaginal candidosis; but it has not been compared with any other antifungal drug in controlled therapeutic trials in mycoses of the skin and has only been compared with nystatin in a few patients with vaginal candidosis. Until adequate comparative studies are done the relative place of econazole in the treatment of dermatomycoses and vaginal condidosis, compared with traditional antifungal agents and with other imidazole derivatives such as miconazole or clotrimazole, cannot be clearly stated. Nevertheless, econazole nitrate is an effective antifungal drug. In dermatological studies about 90% of a large number of patients were cured, often after a relatively short treatment period (2 to 6 weeks, as occurs with other imidazole antifungal agents). The cure rate was only slightly lower (about 85%) in patients with severe mycoses of many years' duration than in those whose infections were of more recent onset. In vaginal candidosis a 3-day treatment regimen using a 150mg suppository once daily was only slightly less effective (85% mycological cure rate) than a 15-day regimen using a 50mg dose (suppository or cream) once daily (90% cure rate). A 3 to 5 day 'higher' dose regimen was slightly more effective than a standard 15-day regimen of nystatin vaginal inserts in a small group of patients with vaginal candidosis. The convenience of the higher-dose shorter term regimen would likely be an important advantage to most patients. Whether other agents useful in vaginal candidosis would be as effective as econazole were they to be used in this way, has not been determined. Topical or intravaginal econazole nitrate has usually been well tolerated, side effects being limited to local irritation in about 1 to 4% of patients in most studies.

Adult↗
PubMed1978

Mianserin: a review of its pharmacological properties and therapeutic efficacy in depressive illness.

Mianserin is a tetracyclic compound advocated for the treatment of depressive illness and depression associated with anxiety. It combines antidepressant activity with a sedative effect and has an EEG and clinical activity profile similar to that of amitriptyline. It has an overall efficacy comparable with amitriptyline and imipramine in depressive illness, but at dosages which have achieved a similar overall clinical improvement, mianserin causes significantly fewer anticholinergic side effects than amitriptyline or imipramine and also appears less likely than these drugs to cause serious cardiotoxicity on overdosage. Mianserin also has anti-anxiety activity, but its role in treating patients with anxiety associated with primary depression has still to be clarified. Mianserin appears to be well tolerated by the elderly and by patients with cardiovascular disease, including those recovering from a recent myocardial infarction, and does not appear to antagonise the action of adrenergic neurone blocking antihypertensive drugs or affect the anticoagulant action of phenprocoumon.

Amitriptyline↗
PubMed1978

Metronidazole in anaerobic infections: a review of its activity, pharmacokinetics and therapeutic use.

Metronidazole which has been widely used for many years in the treatment of trichomoniasis, amoebiasis and giardiasis, has recently been shown to be active against anaerobic bacteria. Serum, cerebrospinal fluid and tissue concentrations bactericidal for Bacteroides species are attained after usual dosages given orally or intravenously or higher dosages given rectally (suppository). Prospective studies have demonstrated that the addition of metronidazole to regimens for pre-operative bowel preparation, decreases the frequency of postoperative infection and eliminates anaerobic infection. Similarly, anaerobic infection after acute appendicectomy or hysterectomy has been virtually eliminated by metronidazole given before and up to 1 week after surgery. Metronidazole has been successfully used in the treatment of anaerobic infections of the chest, head, gastrointestinal and female genitourinary tract, and of anaerobic septicaemia and bacteraemia. Metronidazole is the most active agent available against obligate anaerobes and is likely to be of major value in the treatment of serious infections due to these organisms. Although the absence of formal comparative trials in many areas of use makes it difficult to clearly state the relative therapeutic efficacy of metronidazole, compared with other drugs such as clindamycin, chloramphenicol or penicillin, it is nevertheless a very effective agent in the treatment and prevention of anaerobic infections.

Anaerobiosis↗
PubMed1978

Disopyramide: a review of its pharmacological properties and therapeutic use in treating cardiac arrhythmias.

Disopyramide is a new antiarrhythmic drug with a pharmacological profile of action similar to that of quinidine and procainamide. In a few controlled therapeutic trails and a large number of uncontrolled studies in patients with arrhythmias, often following a myocardial infarction, disopyramide has been relatively effective (more so in ventricular than in atrial arrhythmias) and usually well tolerated. In treating premature atrial and ventricular contractions, the best-studied area of its therapeutic use, disopyramide was superior to a placebo and of similar efficacy to but better tolerated than quinidine; the drop-out rate due to adverse effects of the disopyramide group (10%) being less than one-third that of the quinidine group (36%). In an open ward setting, disopyramide used prophylactically after myocardial infarction appeared to reduce both the incidence of reinfarction and the mortality rate, while in patients treated in coronary care units although the incidence of reinfarction was lower with disopyramide than with a placebo, the mortality rate was not significantly different. Further well-designed trials with adequate numbers of patients are needed before the routine use of disopyramide in infarct patients treated in either setting can be justified. Comparative studies are also required to determine if disopyramide has advantages over other antiarrhythmic agents in this area of use. Side-effects with disopyramide are usually a result of its anticholinergic activity, a dry mouth and difficulty in urination being the most common. Like other antiarrhythmic agents, disopyramide exerts a negative inotropic action on cardiac muscle, and development of acute heart failure has been reported. Development of worsening of heart block and hypotension have also occurred. Disopyramide is largely excreted unchanged and dosage should be reduced in patients with impaired renal function, in accordance with creatinine clearance values.

Arrhythmias, Cardiac↗
PubMed1977

Dantrolene sodium: a review of its pharmacological properties and therapeutic efficacy in spasticity.

Dantrolene sodium or dantrolene1 is 1([5-(nitrophenyl)furfurylidend] amino) hydantoin sodium hydrate. It is indicated for use in chronic disorders characterised by skeletal muscle spasticity, such as spinal cord injury, stroke, cerebral palsy and multiple sclerosis. Dantrolene is believed to act directly on the contractile mechanism of skeletal muscle to decrease the force of contraction in the absence of any demonstrated effects on neural pathways, on the neuromuscular junction, or on the excitable properties of the muscle fibre membranes. Controlled trials have demonstrated that dantrolene is superior to placebo in adults or children with spasticity from various causes, as evidenced by clinical assessments of disability and daily activities, and by muscle and reflex responses to mechanical and electrical stimulation. It is somewhat less effective in patients with multiple sclerosis than in those with spasticity from other causes. There has been a general clinical impression in controlled trials that dantrolene caused less sedation than would have been expected from therapeutically comparable doses of diazepam. In 2 controlled trials, there was no significant difference between dantrolene and diazepam in terms of reductions in spasticity, clonus, and hyperreflexia, but side-effects such as drowsiness and inco-ordination occurred significantly more frequently on diazepam. Long-term studies have indicated continuing benefit for patients taking dantrolene, though the incidence of side-effects has often been high and there has been a suggestion of exacerbation of seizures in children with cerebral palsy. Dantrolene may be of value in the medical treatment of spasm of the external urethral sphincter due to neurological and non-neurological disease, and animal studies suggest a potential use in the management of malignant hyperpyrexia. Chemical evidence of liver dysfunction may occur in 0.7 to 1% of patients on long-term treatment with dantrolene, with symptomatic hepatitis in 0.35 to 0.5% and fatal hepatitis in 0.1 to 0.2%. The drug commonly causes transient drowsiness, dizziness, weakness, general malaise, fatigue and diarrhoea at the start of therapy. Muscle weakness may be the principal limiting side-effect in ambulant patients, particularly in those with multiple sclerosis, and therapy could be hazardous in patients with pre-existing bulbar or respiratory weakness. The dosage of dantrolene has been fixed in most controlled trials, though long-term studies have indicated the need for individualisation of dosage. The initial dose is usually 25mg once daily, increasing to 25mg two, three or four times daily, and then by increments of 25mg up to as high as 100mg two, three or four times daily. The lowest dose compatible with optimal response is recommended.

Adult↗
PubMed1977

Sodium valproate: a review of its pharmacological properties and therapeutic efficacy in epilepsy.

Sodium valproate has a broad spectrum of anticonvulsant activity, but is structurally unrelated to conventional antiepileptic drugs. Its proposed mode of action is mediated through effects on the function of brain gamma-aminobutyric acid (GABA). However, the elevations in brain and cerebellar GABA, and the concomitant reductions in levels of cyclic guanosine monophosphate, occur in animals at dose levels which are unlikely to be achieved during treatment of epileptic patients.

Administration, Oral↗