Biomedical subjects

R N Brogden

Publications and source records attributed to R N Brogden.

At least 109 records · Page 6Linked to original sources

PubMed1987

l-Carnitine. A preliminary review of its pharmacokinetics, and its therapeutic use in ischaemic cardiac disease and primary and secondary carnitine deficiencies in relationship to its role in fatty acid metabolism.

l-Carnitine occurs naturally as an essential cofactor of fatty acid metabolism which is synthesised endogenously or obtained from dietary sources. In patients with primary carnitine deficiencies, which may be life-threatening, and some secondary deficiencies such as organic acidurias, the exogenously administered compound is clearly beneficial: by abolishing hypotonia, motor skills are improved, as are muscle weakness and wasting. In preliminary clinical trials in patients with ischaemic cardiac disease, therapy with l-carnitine has shown beneficial effects on myocardial function and metabolism and has improved exercise tolerance in patients with angina pectoris-findings which require further substantiation in larger controlled studies. Moreover, while some interesting evidence suggests that l-carnitine may find potential use in such diverse conditions as carnitine deficiencies secondary to prolonged total parenteral nutrition supplementation or chronic haemodialysis, hyperlipidaemias and the prevention of toxicity induced by anthracyclines and valproate, such findings must be regarded as preliminary. Exogenously administered l-carnitine is very well tolerated. Thus, while its role in primary deficiencies is established, with its profile of negligible toxicity l-carnitine is worthy of further investigation to more clearly define its therapeutic applications in a variety of conditions which may be indirectly related to alterations in fatty acid metabolism.

Carnitine↗

PubMed1987

Disopyramide. A reappraisal of its pharmacodynamic and pharmacokinetic properties, and therapeutic use in cardiac arrhythmias.

Disopyramide is a widely used class IA antiarrhythmic drug with a pharmacological profile of action similar to that of quinidine and procainamide. Over the past 10 years disopyramide has demonstrated its efficacy in ventricular and atrial arrhythmias. In therapeutic trials, usually involving small numbers of patients, the efficacy of disopyramide was comparable with that of mexiletine, perhexiline, tocainide, propafenone or prajmalium. Recent comparisons with quinidine have confirmed the similar efficacy and better tolerability of disopyramide. The suggestion from initial studies that disopyramide may be less effective than amiodarone or flecainide requires further investigation. In addition, studies have failed to demonstrate that the early administration of disopyramide after acute myocardial infarction decreases important arrhythmias or early mortality. Thus, disopyramide is now well established as an effective antiarrhythmic drug in ventricular and supraventricular arrhythmias although its role in therapy relative to that of recently introduced antiarrhythmic agents is not clear.

Arrhythmias, Cardiac↗

PubMed1987

Human insulin. A review of its biological activity, pharmacokinetics and therapeutic use.

Human insulin, whether produced by recombinant DNA techniques (biosynthetic, insulin crb) or enzymatic modification of porcine insulin (semisynthetic, insulin emp) is equivalent in biological activity to porcine insulin following intravenous administration. Slight differences between human and porcine insulin in hypoglycaemic activity after subcutaneous injection appear to be related to differences in absorption, and are unlikely to be of major clinical importance. Similarly, reported minor differences in counterregulator hormone response to human insulin compared with porcine insulin need further study, but they are unlikely to have important clinical implications. In clinical use the therapeutic efficacy of human insulin is similar to that of porcine insulin. The lower antigenicity with human insulin relative to purified porcine insulin is of potential therapeutic value, and it is logical to use human insulin in newly diagnosed diabetics, in patients treated intermittently with insulin, in cases of immunological insulin resistance, and in patients with allergy and local reaction against animal insulin. Thus, human insulin seems to have no disadvantages compared with purified porcine insulin and may have some advantages. While there appears to be no compelling reason to change patients whose diabetes is presently well controlled with purified porcine insulin to human insulin, the availability of human insulin at a price equal to or less than that of animal origin makes such a change logical. In the meantime, human insulin should be considered the insulin of 'first choice' for newly diagnosed diabetics requiring insulin therapy and in carbohydrate intolerance and diabetes occurring during pregnancy.

Animals↗

PubMed1987

Celiprolol. A preliminary review of its pharmacodynamic and pharmacokinetic properties and its therapeutic use in hypertension and angina pectoris.

Celiprolol is a new 'cardioselective' beta-adrenoceptor blocking drug with intrinsic sympathomimetic (partial agonist) activity and a weak vasodilating effect. Celiprolol appears not to cause bronchoconstriction or inhibit the effect of bronchodilating drugs in asthmatic patients and there is some evidence that it may have mild bronchodilating activity in such patients. Some studies suggest that celiprolol, because of vasodilation, may be less likely to reduce blood flow to the peripheries than other beta-adrenoceptor blocking drugs and hence cause fewer peripheral vascular side effects. Significant inhibition of exercise tachycardia occurs 24 hours after a single oral dose of celiprolol. In preliminary therapeutic trials celiprolol 200 to 600mg once daily was similar in efficacy to propranolol 40mg to 80mg twice daily or atenolol 100mg once daily in patients with mild to moderate hypertension or angina pectoris. If the apparent pharmacodynamic advantages of celiprolol are confirmed in well designed therapeutic trials then celiprolol should represent a definite advance in beta-adrenoceptor blocking therapy.

Adrenergic beta-Antagonists↗

PubMed1987

Encainide. A review of its pharmacological properties and therapeutic efficacy.

Encainide is an antiarrhythmic drug with class IC activity which has been used in the treatment of life-threatening ventricular arrhythmias, symptomatic ventricular arrhythmias and supraventricular arrhythmias. The antiarrhythmic activity is due to the parent drug and its two principal active metabolites, and in the extensive metabolising phenotype (90% of patients), metabolites are present in plasma at higher concentrations than encainide itself. Encainide produces little haemodynamic change in patients with left ventricular dysfunction and thus has considerable therapeutic potential in view of its efficacy in patients with ventricular tachycardia, premature ventricular complexes and the Wolff-Parkinson-White syndrome. However, this potential is reduced by a tendency for encainide to aggravate arrhythmia in a proportion of patients. At present there is no reliable method of identifying patients at risk for this potentially serious side effect. The most common non-cardiac side effects are dizziness and blurred vision which seldom necessitate withdrawal of treatment. Thus, encainide has proved effective in controlling ventricular tachyarrhythmias including those which have not been controlled by other antiarrhythmic drugs.

Anilides↗

PubMed1987

Nedocromil sodium. A preliminary review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in the treatment of reversible obstructive airways disease.

Nedocromil sodium is a sodium cromoglycate-like drug which inhibits activation and mediator release from inflammatory cells such as eosinophils, neutrophils, macrophages, monocytes, mast cells and platelets. Non-comparative and placebo-controlled therapeutic studies in adult patients of up to 52 weeks duration have demonstrated the tolerability and efficacy of nedocromil 4 mg twice or 4 times daily in the management of reversible obstructive airways disease producing significant improvements in asthma symptom scores and pulmonary function tests. When added to existing therapy, nedocromil sodium permits reductions of 20 to 70% in concomitant bronchodilator use and appears to have a moderate steroid sparing effect in patients receiving inhaled corticosteroids. To date no controlled studies have been published comparing nedocromil sodium with sodium cromoglycate and other established therapies in adult reversible obstructive airways disease or asthma, which limits the overall conclusions which can be drawn about the position of nedocromil sodium relative to other treatments. However, preliminary clinical data suggest that although nedocromil sodium cannot substitute completely for bronchodilators or inhaled corticosteroids, with its additive and dose-sparing effects and the convenience of a twice daily dosage it is a promising prophylactic adjunctive agent for the management of reversible obstructive airways disease.

Animals↗

PubMed1987

Propafenone. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic use in the treatment of arrhythmias.

Propafenone is a Class I antiarrhythmic agent with weak beta-adrenoceptor antagonist activity which can be given both intravenously and orally. Dosage must be individualised because of dose-dependent pharmacokinetics, a wide range of clinically effective plasma concentrations (64 to 3271 micrograms/L) after comparable doses, the presence of an active metabolite (5-hydroxy-propafenone) and genetically determined metabolic oxidation. In non-comparative studies propafenone 450 and 900 mg/day orally significantly suppressed premature ventricular complexes and couplets in 96% and 75% of patients, respectively, and abolished ventricular tachycardia in 75% of patients. Efficacy was confirmed in placebo-controlled studies in which propafenone 300 to 900mg daily suppressed premature ventricular complexes (greater than 80%) in 77% of patients; 87% of patients had significant reductions in couplets and abolition of ventricular tachycardia. In patients with ventricular arrhythmias refractory to other antiarrhythmic agents, propafenone 450 to 1200 mg/day suppressed arrhythmias in 63% of patients (in long term therapy 66%). Electrically induced arrhythmias were prevented by intravenously administered propafenone in 12 to 23% of patients. However, long term oral therapy was effective in 77% of patients selected using programmed electrical stimulation. Propafenone was also effective in suppressing atrial and AV nodal/junctional re-entrant tachycardias and Wolff-Parkinson-White tachycardias involving accessory pathways. A limited number of comparisons with other antiarrhythmic drugs indicate that the antiarrhythmic efficacy of propafenone is superior or similar to that of quinidine, disopyramide and tocainide, and comparable to that of lignocaine (lidocaine), flecainide and metoprolol against ventricular arrhythmias and a smaller number of atrial arrhythmias. Cardiovascular side effects indicate a proarrhythmic effect similar to that with other Class I drugs, occasional precipitation of congestive heart failure and conduction abnormalities; the latter two occur more often in patients with underlying ventricular dysfunction. Non-cardiovascular side effects (neurological, gastrointestinal) are well tolerated and generally resolve with continued therapy or dosage reduction. Thus, propafenone is an effective antiarrhythmic agent, and is a useful addition to currently available drugs, although further studies will be required to determine clearly its place in therapy compared with more established antiarrhythmic drugs.

Arrhythmias, Cardiac↗

PubMed1986

Non-steroidal anti-inflammatory analgesics other than salicylates.

The largest group of non-narcotic analgesics are the arylalkanoic acid derivatives, comprising derivatives of arylacetic acid, propionic acid, heteraryl acetic acid and indole acetic acid. Common to all of these drugs is their inhibition of prostaglandin biosynthesis, which contributes to their analgesic and other pharmacological properties as well as to their principal side effect, gastrointestinal irritation. Although these drugs all cause some gastric microbleeding, they do so to a lesser extent than aspirin. The arylalkanoic acid derivatives, as well as the anthranilic acid and oxicam derivatives, are peripherally acting as evidenced by their lack of activity in classical tests of central analgesic activity. After oral administration of these drugs, their peak plasma concentrations are generally attained in 1 to 3 hours; absorption is not generally influenced by food. Volume of distribution is mostly low (less than 0.2 L/kg) and protein binding is high (usually 95 to 99%). Elimination is by glucuronide formation for several of the propionic acid derivatives and generally by biotransformation for derivatives of arylacetic acid, indole and indene acetic acid, and the oxicams. The elimination half-life of the arylalkanoic acid derivatives is in most instances about 2 to 5 hours, although notable exceptions include carprofen (approximately equal to 20 h), fenbufen (10 h), naproxen (12-15 h) and sulindac (16 h for the active metabolite). The elimination half-life of indomethacin varies considerably between and within individuals. Piroxicam has the longest half-life, averaging 45 hours. The pharmacokinetic properties of the anthranilic acid derivatives (fenamates, glafenine) generally resemble those of the arylacetic acids. Few clinically significant drug interactions are associated with concomitant administration of the arylalkanoic acids or piroxicam and other drugs. Since the arylalkanoic acids are highly bound to plasma proteins (mainly albumin) there is a theoretical potential for displacement reactions with drugs that are used at plasma concentrations high enough to exceed the binding capacity of their own primary binding sites. However, such reactions have rarely been reported. Although the concomitant administration of aspirin and several of the propionic acid derivatives results in a significant decrease in the plasma concentration of the latter, the clinical significance of such interactions is uncertain and probably minimal.(ABSTRACT TRUNCATED AT 250 WORDS)

Anti-Inflammatory Agents, Non-Steroidal↗

PubMed1986

Pyrazolone derivatives.

In many countries, the pyrazolone derivatives, which include dipyrone, antipyrine, aminopyrine and propyphenazone, are widely used analgesics. Dipyrone, the most widely used pyrazolone, has been the most studied. The pyrazolidine derivatives, phenylbutazone and oxyphenbutazone, which are not generally used for analgesia since they differ from the pyrazolones in terms of efficacy and tolerance, are not discussed in this article. Dipyrone is an inhibitor of cyclo-oxygenase but, unlike aspirin, its effect is rapidly reversible. The inhibition of prostaglandin biosynthesis contributes to the analgesic activity of the pyrazolone derivatives. Peak plasma concentrations of the pyrazolone derivatives generally occur 1 to 1.5 hours after oral administration. Half-lives vary from 1 to 2 hours with propyphenazone, to about 7 hours with dipyrone (2 hours for the active metabolite of dipyrone, 4-methylaminoantipyrine, MAA). Half-life of antipyrine varies considerably between individuals (5 to 35 hours). Unlike the NSAIDs generally, the pyrazolone derivatives antipyrine, aminopyrine and propyphenazone are minimally bound to plasma proteins. The pyrazolones undergo extensive biotransformation, aminopyrine and dipyrone being converted to active metabolites. Dipyrone is the only drug for which results of recent double-blind trials are available. Oral dipyrone has been shown to be more effective than an equal dose of aspirin or paracetamol in alleviating postoperative pain, and intravenous dipyrone 2.5g was similar in efficacy to pethidine 50 mg. In patients with acute ureteral or biliary colic, dipyrone 2.5g intravenously was similar in efficacy to indomethacin 50 mg or pethidine 50 mg. The most frequently reported side effects of the pyrazolone derivatives are skin rashes. Gastrointestinal side effects are rare. Blood dyscrasias, mostly associated with aminopyrine, have received wide attention in the medical literature, but their true incidence with dipyrone is considerably lower than the often quoted incidence for amidopyrine reported more than 30 years ago.

Anti-Inflammatory Agents, Non-Steroidal↗

PubMed1986

Aztreonam. A review of its antibacterial activity, pharmacokinetic properties and therapeutic use.

Aztreonam (azthreonam; SQ 26,776) is the first member of a new class of beta-lactam antibiotics, the monobactams. Aztreonam is selectively active against Gram-negative aerobic bacteria and inactive against Gram-positive bacteria. Thus, in vitro, aztreonam is inhibitory at low concentrations (MIC90 less than or equal to 1.6 mg/L) against Enterobacteriaceae except Enterobacter species, and is active against Pseudomonas aeruginosa, 90% of pseudomonads being inhibited by 12 to 32 mg/L. Aztreonam is inactive against Gram-positive aerobic bacteria and anaerobes, including Bacteroides fragilis. Therefore, when administered alone, aztreonam has minimal effect on indigenous faecal anaerobes. Aztreonam must be administered intravenously or intramuscularly when used to treat systemic infections, since absolute bioavailability is very low (about 1%) after oral administration. Since elimination half-life is less than 2 hours, 6- or 8-hourly administration is used in the treatment of moderately severe or severe infections, although 12-hourly injection is adequate in less severe systemic and some urinary tract infections. Therapeutic trials have shown aztreonam to be effective in Gram-negative infections including complicated infections of the urinary tract, in lower respiratory tract infections and in gynaecological and obstetric, intra-abdominal, joint and bone, skin and soft tissue infections, uncomplicated gonorrhoea and septicaemia. In comparisons with other antibiotics, aztreonam has been at least as effective or more effective than cefamandole in urinary tract infections and similar in efficacy to tobramycin or gentamicin. Where necessary, aztreonam and the standard drug have both been combined with another antibiotic active against Gram-positive and/or anaerobic bacteria. Aztreonam has been effective in eradicating pseudomonal infections in most patients (except in patients with cystic fibrosis), but the inevitably limited number of pseudomonal infections available for study prevents any conclusions as to the relative efficacy of aztreonam compared with other appropriate regimens against these infections. Thus, with an antibacterial spectrum which differs from that of other antibiotics, aztreonam should be a useful alternative to aminoglycosides or 'third generation' cephalosporins in patients with proven or suspected serious Gram-negative infections.

Anti-Bacterial Agents↗

PubMed1986

Etodolac. A preliminary review of its pharmacodynamic activity and therapeutic use.

Etodolac is a new non-steroidal agent (NSAID) with anti-inflammatory and analgesic activity. It has been studied in rheumatoid arthritis, osteoarthritis, and pain resulting from minor surgery. In the latter setting, etodolac is at least as effective as aspirin in terms of overall pain relief, and the duration of analgesic effect of a dose of 200 to 400mg is longer than that of aspirin. In rheumatoid arthritis, etodolac, administered twice daily, appears comparable in efficacy to moderate doses of aspirin (3 to 4g daily), but is better tolerated. To date, etodolac has not been compared clinically with analgesics other than aspirin and sulindac. As with other non-steroidal agents, gastrointestinal complaints are the most frequently reported side effects, but the incidence of most gastrointestinal effects was only slightly higher than with placebo. Thus, from studies in small numbers of patients etodolac appears at least as effective as aspirin and better tolerated. The relatively low incidence of gastrointestinal side effects in these studies awaits confirmation in well designed comparisons with widely used NSAIDs.

Acetates↗

PubMed1986

Metoprolol. An updated review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy, in hypertension, ischaemic heart disease and related cardiovascular disorders.

During the intervening years since metoprolol was first reviewed in the Journal (1977), it has become widely used in the treatment of mild to moderate hypertension and angina pectoris. Although much data have accumulated, its precise mechanisms of action in these diseases remain largely uncertain. Optimum treatment of hypertension and angina pectoris with metoprolol is achieved through dose titration within the therapeutic range. It has been clearly demonstrated that metoprolol is at least as effective as other beta-blockers, diuretics and certain calcium antagonists in the majority of patients. Although a twice daily dosage regimen is normally used, satisfactory control can be maintained in many patients with single daily doses of conventional or, more frequently, slow release formulations. Addition of a diuretic may improve the overall response rate in hypertension. Several controlled trials have studied the effects of metoprolol administered during the acute phase and after myocardial infarction. In early intervention trials a reduction in total mortality was achieved in one moderately large trial of prolonged treatment, but in another, which excluded patients already being treated with beta-blockers or certain calcium antagonists and where treatment was only short term, mortality was significantly reduced only in 'high risk' patients. Overall results with metoprolol have not demonstrated that early intervention treatment in all patients produces clinically important improvement in short term mortality. Thus, the use of metoprolol during the early stages of myocardial infarction is controversial, largely because of the requirement to treat all patients to save a small number at 'high risk'. This blanket coverage approach to treatment may be more justified during the post-infarction follow-up phase since it has been shown that metoprolol slightly, but significantly, reduces the mortality rate for periods of up to 3 years. Metoprolol is generally well tolerated and its beta 1-selectivity may facilitate its administration to certain patients (e.g. asthmatics and diabetics) in whom non-selective beta-blockers are contraindicated. Temporary fatigue, dizziness and headache are among the most frequently reported side effects. After a decade of use, metoprolol is well established as a first choice drug in mild to moderate hypertension and stable angina, and is beneficial in post-infarction patients. Further study is needed in less well established areas of treatment such as cardiac arrhythmias, idiopathic dilated cardiomyopathy and hypertensive cardiomegaly.

Adult↗

PubMed1986

Cefonicid. A review of its antibacterial activity, pharmacological properties and therapeutic use.

Cefonicid is a 'second generation' cephalosporin administered intravenously or intramuscularly. It is similar to cefamandole in its superiority to first generation cephalosporins against several enterobacteriaceae as well as its activity against Haemophilus influenzae, including beta-lactamase-producing strains. Its activity against Staphylococcus aureus is similar to that of cefoxitin and inferior to cefamandole and first generation cephalosporins. It has excellent in vitro activity against Neisseria gonorrhoeae, but is inactive against Pseudomonas, Acinetobacter, Serratia, and Bacteroides fragilis. Due to high achievable plasma concentrations and a relatively long half-life, in most clinical trials cefonicid has been administered once daily. It was comparable in efficacy with cefamandole or cefazolin in the treatment of patients with urinary tract, lower respiratory tract, and soft tissue and bone infections. It has also been compared with penicillin in the treatment of uncomplicated gonorrhoea. Results from a small series of patients with endocarditis appear to indicate that cefonicid should not be used in patients with serious staphylococcal infections. Single doses of cefonicid given preoperatively appear to offer a similar degree of protection against post-surgical infection as multiple doses of other antibiotics, but further data from studies involving larger numbers of patients are needed to confirm these impressions. Patients who require prolonged antibiotic therapy, such as those with osteomyelitis being treated as outpatients after a relatively short inpatient course, could benefit from the once daily dose regimen of cefonicid.

Bacterial Infections↗

PubMed1986

Oxaprozin. A preliminary review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy.

Oxaprozin is a newer non-steroidal anti-inflammatory drug advocated for use in painful rheumatic and inflammatory conditions. As is the case with some other newer non-steroidal anti-inflammatory drugs, oxaprozin offers the convenience of once-daily administration. Published data suggest that oxaprozin 1200 mg once daily is comparable in effectiveness with usual dosages of aspirin, ibuprofen, indomethacin, naproxen, piroxicam and sulindac in the treatment of rheumatoid arthritis and osteoarthritis. More controlled clinical trials in adequate numbers of patients are necessary to evaluate its potential in other rheumatic and inflammatory conditions. Oxaprozin produced fewer gastrointestinal side effects than aspirin, and the short term tolerability of oxaprozin was similar to that of other non-steroidal anti-inflammatory drugs. If further definition of its efficacy and tolerability compared with other non-steroidal anti-inflammatory drugs during long term therapy confirms these initially favourable results, then oxaprozin would appear to offer a useful and convenient alternative in the treatment of painful rheumatic and inflammatory conditions.

Animals↗

PubMed1985

Ceftazidime. A review of its antibacterial activity, pharmacokinetic properties and therapeutic use.

Ceftazidime is a new 'third generation' cephalosporin administered intravenously or intramuscularly. Similarly to other third generation cephalosporins it has a broad spectrum of in vitro activity against Gram-positive and Gram-negative aerobic bacteria, is particularly active against Enterobacteriaceae (including beta-lactamase-positive strains) and is resistant to hydrolysis by most beta-lactamases. Importantly, in vitro ceftazidime is presently the most active cephalosporin available against Pseudomonas aeruginosa, but it is less active against Staphylococcus aureus than first and second generation cephalosporins. Only larger comparative trials are likely to discern any statistically significant differences in clinical efficacy which may exist between ceftazidime and other antibiotics, but ceftazidime appears to be similar in efficacy to 'standard' comparative drugs in lower respiratory tract infections and complicated and/or chronic urinary tract infections among debilitated or hospitalised patients. Thus, in patients having Gram-negative infections at these sites and in whom the potential toxicity of the aminoglycosides is a concern, ceftazidime may be a valuable alternative in that it apparently lacks serious side effects and does not require routine drug plasma concentration monitoring. In fibrocystic patients having acute respiratory tract infections, ceftazidime is highly effective at both reducing symptoms of infection and temporarily reducing the sputum counts of Pseudomonas species. However, in these patients resistance to ceftazidime may develop, as seen with other beta-lactam antibiotics. In the treatment of fever of unknown origin or documented infections in immunocompromised adults and children, ceftazidime appears to be similar in efficacy to various 2- or 3-drug combinations. Nevertheless, the coadministration of an antibiotic having greater efficacy against Gram-positive bacteria should be considered in immunocompromised patients. Results from a small number of comparative trials suggest that ceftazidime may be as effective as the aminoglycosides in intra-abdominal, obstetric and gynaecological, and skin and soft tissue infections. However, further clinical experience, particularly a few well designed comparative studies, is needed to clarify the comparative efficacy in these conditions as well as in septicaemia/bacteraemia, meningitis, and bone and joint infections.

Aging↗

PubMed1985

Tiaprofenic acid. A review of its pharmacological properties and therapeutic efficacy in rheumatic diseases and pain states.

Tiaprofenic acid is a new non-steroidal anti-inflammatory agent advocated for use in rheumatoid arthritis, osteoarthritis, musculoskeletal disorders, soft-tissue injuries and inflammatory conditions and acute pain of varying origin. Published data suggest that tiaprofenic acid 600 mg daily in 2 or 3 divided doses is comparable in effectiveness with aspirin, diclofenac, ibuprofen, indomethacin, naproxen, piroxicam and sulindac in the treatment of rheumatoid arthritis and osteoarthritis. More controlled clinical trials are necessary to evaluate its potential in rheumatic conditions other than rheumatoid arthritis and osteoarthritis. In controlled studies in patients with acute pain following surgery or trauma, tiaprofenic acid was more effective than placebo and as effective as aspirin and indomethacin. While tiaprofenic acid produced fewer side effects than aspirin in rheumatoid arthritis treatment, and indomethacin in the treatment of osteoarthritis, results have generally shown the short term tolerability of tiaprofenic acid to be similar to that of other non-steroidal anti-inflammatory drugs. As no one of the non-steroidal anti-inflammatory agents is the most suitable drug for all patients requiring such therapy, tiaprofenic acid should be considered along with other drugs of this type in the therapy of arthritic conditions and of acute postoperative or posttraumatic pain.

Anti-Inflammatory Agents, Non-Steroidal↗

PubMed1985

Ciclopirox olamine 1% cream. A preliminary review of its antimicrobial activity and therapeutic use.

Ciclopirox olamine is a substituted pyridone antimycotic, unrelated to the imidazole derivatives, with activity against a broad spectrum of dermatophytes, yeasts, actinomycetes, molds, other fungi, and a variety of Gram-positive and Gram-negative bacteria. The efficacy of ciclopirox olamine cream has been demonstrated in open and placebo-controlled studies in patients with superficial dermatophyte or yeast infections, and in double-blind comparative trials in patients with dermatomycoses, topical ciclopirox olamine was comparable to or better than clotrimazole in efficacy and caused a similar number of side effects. Ciclopirox olamine penetrates through fingernails and in preliminary studies has been successfully used in onychomycoses. However, further studies are needed to establish the role of ciclopirox in the treatment of onychomycoses and dermatomycoses relative to that of the more recently introduced antigungal agents.

Animals↗

PubMed1985

Diltiazem. A review of its pharmacological properties and therapeutic efficacy.

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.

Angina Pectoris↗