Biomedical subjects

R N Brogden

Publications and source records attributed to R N Brogden.

At least 181 records · Page 10Linked to original sources

PubMed1980

Nefopam: a review of its pharmacological properties and therapeutic efficacy.

Nefopam is a non-narcotic analgesic not structurally related to other analgesic drugs. It is effective by the oral and parenteral routes, and when appropriate dose ratios were compared in short term studies it was shown to produce analgesia comparable to that with the oral analgesics aspirin, dextropropoxyphene and pentazocine, as well as that with 'moderate' doses of parenteral morphine, pethidine and pentazocine. However, when 'higher' dose ratios were compared, morphine and pethidine were usually more effective than nefopam, possibly due to a 'ceiling effect' for analgesia which may occur with higher doses of nefopam, as with other simple analgesics. Although a few patients with chronic pain have received nefopam for several weeks, further studies are needed to clarify its continued effectiveness and safety when used over long periods. In most patients nefopam has been relatively well tolerated, the most frequent side effects being sweating, nausea and in some studies sedation.

Administration, Oral↗

PubMed1980

Flunisolide: a review of its pharmacological properties and therapeutic efficacy in rhinitis.

Flunisolide, a derivative of fluocinolone acetonide, is advocated for intranasal inhalation for the treatment of perennial and seasonal allergic rhinitis. It is rapidly absorbed by all routes of administration, but it quickly undergoes extensive first-pass metabolism to a 6 beta-hydroxylated metabolite, which possesses only weak corticosteroid effects. Intranasal flunisolide relieves nasal symptoms (but not eye symptoms) in both perennial and seasonal allergic rhinitis, being most effective in patients who have an allergic component to their rhinitis; and like other corticosteroids it may reduce the need for systemic antihistamines in such patients, expecially during peak pollen periods. A few well designed comparative studies have shown flunisolide to be as effective as intranasal beclomethasone, and (in a single study) more effective than intranasal sodium cromoglycate solution. Only transient side effects have occurred, including nasal stinging and throat irritation. No Candida infections have been clinically apparent in short or longer term trials. Resting morning plasma cortisol levels have not been suppressed by usual therapeutic doses of intranasal flunisolide, but the drug's effects on hypothalamo-pituitary-adrenal (HPA) axis integrity during conditions of stress have not been evaluated.

Beclomethasone↗

PubMed1980

Nadolol: a review of its pharmacological properties and therapeutic efficacy in hypertension and angina pectoris.

Nadolol is a nonselective beta-adrenoceptor blocking drug without intrinsic sympathomimetic or membrane stabilising activity. Its inherently long duration of activity makes it suitable for once daily administration in both hypertension and angina pectoris, and in these conditions it has been as effective as propranolol given in a traditional regimen 4 times daily. However, other beta-blocking drugs can also be given with reduced frequency, especially in hypertension; and some, such as atenolol (a longer acting 'cardioselective' agent) or long-acting preparations of other beta-blockers, have also been given once daily in angina prophylaxis. Nevertheless, nadolol is one of a few beta-blocking drugs which have clearly been shown to be effective in both hypertension and angina with once daily administration. Other specific properties of nadolol, such as its excretion entirely in unmetabolised form, may offer advantages over other existing beta-blocking drugs in specific patients, while some properties (such as lack of 'cardioselectivity') may be disadvantageous in others. The choice of a beta-blocking drug should thus be based on a knowledge of the pharmacodynamic and pharmacokinetic properties of the different beta-blocking drugs, and a careful consideration of how such properties can best be applied to benefit the individual patient.

Adrenergic beta-Antagonists↗

PubMed1980

Diclofenac sodium: a review of its pharmacological properties and therapeutic use in rheumatic diseases and pain of varying origin.

Diclofenac sodium, a phenylacetic acid derivative, is a non-steroidal, anti-inflammatory, analgesic agent advocated for use in rheumatoid arthritis, degenerative joint disease, ankylosing spondylitis and allied conditions, and in the treatment of pain resulting from minor surgery, trauma and dysmenorrhoea. Published data indicate that diclofenac 75 to 150mg daily (25 to 50mg 3 times daily) is comparable in efficacy with ordinary aspirin 3 to 5g daily and indomethacin 75 to 150mg daily in rheumatoid arthritis and with indomethacin in osteoarthritis. Available data suggest that in patients with osteoarthritis diclofenac sodium is comparable in efficacy and tolerability with naproxen, ibuprofen, sulindac and diflunisal. As oral diclofenac is generally given in 3 divided daily doses it may be at a disadvantage relative to less frequent administration with naproxen, diflunisal and sulindac in rheumatoid arthritis, although there is some evidence of diclofenac's efficacy when administered twice daily, or once daily as a slow release tablet. The drug is also available as suppositories and ampoules for intramuscular injection. No one of the non-steroidal anti-inflammatory agents is the most suitable drug for all patients requiring such therapy, and diclofenac should be considered along with other drugs of its type in the arthritic patient.

Adult↗

PubMed1980

Clobazam: a review of its pharmacological properties and therapeutic use in anxiety.

Clobazam1 is a 1,5-benzodiazepine with antianxiety and anticonvulsant properties, advocated for the treatment of primary anxiety and that associated with organic or functional disorders. Clobazam itself has a half-life of 18 hours, but that of the principal metabolite, N-desmethylclobazam, is about 50 hours. Although the metabolite is pharmacologically less active than the parent drug, steady-state plasma concentrations of the metabolite are 8 times higher than those of the unchanged drug. Therapeutic trials indicate that the antianxiety effect of clobazam 30 to 80 mg daily is comparable with that of half its dose of diazepam. Clobazam has minimal muscle relaxant and hypnotic activity. Although subjective drowsiness has occurred with similar frequency with clobazam and diazepam in some studies, clobazam causes less objectively measured sedation or psychomotor impairment in experimental studies. Results of studies of vigilance and psychomotor performance during therapeutic use in patients are less conclusive, but clobazam may be useful in anxious patients who experience such impairment with other benzodiazepines.

Adolescent↗

PubMed1980

Ipratropium bromide: a review of its pharmacological properties and therapeutic efficacy in asthma and chronic bronchitis.

Ipratropium bromide is an anticholinergc bronchodilator administered by inhalation. Although producing bronchodilation in most patients with obstructive airways disease, it is somewhat less effective than beta 2-adrenoceptor agonist drugs such as salbutamol or fenoterol in patients with asthma, but is at least as effective as these agents in bronchitis. As with the beta 2-adrenoceptor agonists, the onset of maximum effect with ipratropium (about 1.5 to 2 hours) is slower than with isoprenaline (although significant bronchodilation usually occurs within seconds or minutes of ipratropium inhalation), and the duration of effect (about 4 to 6 hours) is longer. Studies of concomitant use of ipratropium and other agents such as beta 2-adrenoceptor agonists, theophylline, or sodium cromoglycate, have usually shown a greater response in many patients than with single drug therapy, as might be expected from the different mechanisms of action of these groups of drugs. Usual inhaled doses of ipratropium were well tolerated in all studies. Ipratropium thus appears to be a suitable alternative to beta 2-adrenoceptor agonist drugs in patients not fully responding to these agents, and combined therapy with ipratropium and other bronchodilating drugs may prove to be an important area of use in patients failing to respond adequately to a single drug regimen. (nevertheless, in asthma patients in whom a 'non-responsive' state is developing, initiation of corticosteroid therapy should not be delayed). Ipratropium may also be useful in the occasional patient in whom side effects such as palpitations or tremor are troublesome with usual inhaled doses of beta 2-adrenoceptor agonists.

Asthma↗

PubMed1980

Ticarcillin: a review of its pharmacological properties and therapeutic efficacy.

Ticarcillin is a semisynthetic penicillin for parenteral administration. The antibacterial activity of ticarcillin is similar to that of carbenicillin except that it is two to four times more active in vitro against Pseudomonas aeruginosa, generally less active against Gram-positive cocci and more active against most Gram-negative bacilli. As the pharmacokinetics of ticarcillin and carbenicillin are also similar, ticarcillin should theoretically be clinically effective when administered at a lower dosage than carbenicillin. There is some evidence that ticarcillin is comparable in efficacy with carbenicillin when given in half to two-thirds the dosage, when the drugs are given in combination with an aminoglycoside and in clinical situations where these drugs are agents of choice. Ticarcillin has been used successfully in the treatment of complicated urinary tract infection, pulmonary infection in cystic fibrosis and bacteraemia and is effective when combined with an aminoglycoside in severe infections in patients with granulocytopenia. The efficacy in anaerobic infections is at present poorly documented, although preliminary results are promising. Tolerability has generally been good with hypokalaemia being the most frequently reported side effect. At the dosages used, bleeding and fluid overload have seldom occurred.

Animals↗

PubMed1980

Captopril: a preliminary review of its pharmacological properties and therapeutic efficacy.

Captopril is the first orally active inhibitor of angiotensin-converting enzyme to become available. It has been studied primarily in hypertension. In mild to moderate essential hypertension captopril is about as effective as usual doses of hydrochlorothiazide or propranolol, about one-half of such patients needing the addition of a diuretic to achieve satisfactory control of blood pressure. In severe hypertension captopril plus a diuretic (and in some patients a beta-blocker) usually reduced blood pressure significantly more than could be achieved with 'standard triple therapy' in patients not responding adequately to such a regimen, and often resulted in an improved feeling of well-being in severely hypertensive patients previously receiving intensive multiple drug therapy. Indeed, at the present stage of the drug's development, patients not responding to or not tolerating 'traditional' antihypertensive therapy represent the most suitable candidates for captopril treatment. While captopril has been well tolerated in most patients, some troublesome or potentially serious side effects have been reported, including agranulocytosis, dysgeusia and reduced renal function; although a clear causal relationship with captopril was not always established, it would appear that the final place of captopril in the treatment of hypertension may ultimately depend on further clarification of its adverse effects profile. In addition to studies in hypertension, captopril has produced encouraging improvement in a small number of patients with severe congestive heart failure resistant to conventional therapy. Captopril must be considered an exciting addition to the therapeutic armamentarium; it, and pharmacologically related compounds of the future, will continue to generate much interest as their final place in therapy becomes better defined through additional well designed studies and wider clinical experience.

Aldosterone↗

PubMed1979

Cefoxitin: a review of its antibacterial activity, pharmacological properties and therapeutic use.

Cefoxitin is a beta-lactam antibiotic derived from cephamycin C, a naturally occurring substance produced by Streptomyces lactamdurans. Its resistance to destruction by beta-lactamases results in a broad spectrum of antibacterial activity which includes anaerobic as well as Gram-positive and Gram-negative aerobic bacteria, including many resistant to cephalothin and other cephalosporins. Given by intravenous or intramuscular injection, cefoxitin is effective against a wide variety of infections caused by Gram-positive or Gram-negative aerobes as well as by anaerobic bacteria. It is generally well tolerated, thrombophlebitis, skin rash and some degree of discomfort after intramuscular injection, being the most commonly reported side effects. Cefoxitin has not been shown to cause adverse effects on renal function.

Bacteria↗

PubMed1979

Timolol: a review of its therapeutic efficacy in the topical treatment of glaucoma.

Timolol maleate is a nonselective beta-blocking drug used for the topical treatment of increased intraocular pressure in patients with chronic open angle glaucoma. In comparative studies it has had a somewhat greater ocular hypotensive effect than the sympathomimetic agent adrenaline (epinephrine), or lower to medium concentrations (up to 4%) of the miotic drug pilocarpine, usually lowering intraocular pressure by about 30 to 35% (absolute pressure reduction). Timolol has been well tolerated by most patients, producing fewer subjective complaints than the comparison drugs, and objective measurements of ophthalmic status have not revealed any marked changes. Although some patients have been treated for extended periods without serious adverse effects or loss of effectiveness, further published reports in larger numbers of patients treated over several years are needed to confirm the drug's apparent long term safety and continued efficacy. Nevertheless, on the basis of present evidence, timolol appears to represent an important advance in the topical treatment of glaucoma.

Glaucoma↗

PubMed1979

Buprenorphine: a review of its pharmacological properties and therapeutic efficacy.

Buprenorphine, a derivative of the morphine alkaloid thebaine, is a strong analgesic with marked narcotic antagonist activity. In studies in relatively small groups of postoperative patients with moderate to severe pain, one or a few doses of buprenorphine parenterally (by intramuscular or slow intravenous injection) or sublingually were at least as effective as standard doses of other strong analgesics such as morphine, pethidine or pentazocine, and buprenorphine was longer acting than these agents. Only a small number of patients with chronic pain have received repeated doses, but in such patients there was no need for increased doses during several weeks to months of treatment. Buprenorphine appears to produce side effects which are similar to those seen with other morphine-like compounds, including respiratory depression. There is apparently no completely reliable specific antagonist for buprenorphine's respiratory depressant effect, since even very high doses of the antagonist drug naloxone may produce only a partial reversal. The respiratory stimulant drug doxapram has overcome respiratory depression in volunteers and in a few patients in a clinical setting, but such studies have not been done in an overdose situation. Animal studies and a direct addiction study in a few volunteers suggest that the dependence liability of buprenorphine may be lower than that of other older morphine-like drugs. However, a slowly emerging abstinence syndrome did occur on withdrawal after very high doses administered for 1 to 2 months. A definitive statement on the drug's dependence liability and abuse potential cannot be made until it has had much wider use for a longer period of time.

Animals↗

PubMed1979

Cefuroxime: a review of its antibacterial activity, pharmacological properties and therapeutic use.

Cefuroxime is a new semisynthetic cephalosporin for parenteral administration. It is resistant to destruction by beta-lactamases produced by staphylococci and most Gram-negative aerobic bacteria and is active against many bacteria resistant to cephalothin. Cefuroxime is the most active of the cephalosporins against gonococci and Haemophilus influenzae particularly against beta-lactamase producing strains. Given by intramuscular or intravenous injection cefuroxime is effective against a wide variety of infections caused by Gram-positive or Gram-negative aerobes, but has no effect against infections caused by Pseudomonas aeruginosa or B. fragilis. Cefuroxime is of value in the treatment of respiratory infections due to Haemophilus influenzae and Streptocococcus pneumoniae and is useful against cephalosporin-resistant Klebsiella and Enterobacter infections. Cefuroxime is an alternative to spectinomycin for the treatment of beta-lactamase producing Neisseria gonorrhoeae infections. It is generally well tolerated and appears not to be nephrotoxic when given alone at usual dosages.

Adult↗

PubMed1979

Atenolol: a review of its pharmacological properties and therapeutic efficacy in angina pectoris and hypertension.

Atenolol is a beta-selective (cardioselective) adrenoceptor blocking drug without partial agonist or membrane stabilising activity. Its profile of action most closely resembles that of metoprolol which differs only in that it has some membrane stabilising activity. Atenolol has been well studied and is effective in the treatment of hypertension and in the prophylactic management of angina. Its narrow dose response range obviates the need for highly individualised dose titration. In patients with angina its long duration of beta-blocking activity allows once daily dosage, whereas other beta-blockers, unless in sustained release dosage forms, need to be given in divided doses. Other beta-blockers can be given once daily in hypertension, but at presnt the evidence for effective control with a once daily regimen is more convincing with atenolol. Further studies are need to clarify any important differences in blood pressure control between the various beta-blocking drugs, both in conventional or sustained release dosage forms. As with metoprolol, atenolol is preferable to non-selective beta-blockers in patients with asthma or diabetes mellitus. Atenolol has been well tolerated in most patients, its profile of adverse reactions generally resembling that of other beta-blocking drugs, although its low lipid solubility and limited penetration into the brain results in a lower incidence of central nervous system effects than seen with propranolol. Atenolol is eliminated virtually entirely as unchanged drug in the urine and dosage needs to be reduced in patients with moderate to severely impaired renal function (glomerular filtration rate less than 30 ml/min). There is no need for modification of dosage of atenolol in liver disease.

Adrenergic beta-Antagonists↗

PubMed1979

Nomifensine: A review of its pharmacological properties and therapeutic efficacy in depressive illness.

Nomifensine is a tetrahydoisoquinoline antidepressant which is chemically unrelated to the tricyclic or tetracyclic antidepressants, the monoamine oxidase inhibitors or the recently introduced agents. Nomifensine resembles the tricyclic antidepressants in many of its pharmacological effects in animal models of depressive illness, but differs from them in that it strongly inhibits the re-uptake of dopamine as well as noradrenaline and is a relatively weak inhibitor of serotonin uptake. It has an overall efficacy comparable with that of imipramine and amitriptyline in depressive illness, but at dosages which have achieved a similar overall clinical improvement, nomifensine causes little or no sedation, fewer and milder anticholinergic side effects, and also appears less likely than these drugs to cause serious cardiotoxicity on overdosage. Nomifensine may aggravate the psychopathology of patients with schizo-affective disorders and intensification of the psychosis may require neuroleptic therapy. Nomifensine also has antianxiety activity, but its role in treating anxiety associated with primary depression has still to be clarified. Nomifensine appears to be well tolerated by the elderly.

Animals↗

PubMed1979

Dextranomer: a review of its general properties and therapeutic efficacy.

Dextranomer is a hydrophilic dextran polymer advocated as a 'cleansing agent' for various types of exudating wounds or ulcers, including stasis (venous) ulcers and decubitus ulcers. It appears to exert its effect by a capillary action which absorbs wound exudate, as well as wound debris and micro-organisms, into the dextranomer beads or into the spaces between the beads, thus removing such products from the wound surface. Dextranomer is an aid to wound or ulcer management, and does not directly affect tissue repair in such ulcers, but as with other 'cleansing' agents or techniques, removal of debris (and possibly micro-organisms) from the wound could be expected to promote natural healing. Reports of its effectiveness in open studies, often in patients with seemingly resistant lesions, have been encouraging. Similarly, in comparative trials results have usually favoured dextranomer, but a clear indication of the relative efficacy and benefits as compared with other treatments used for exudating lesions has not yet emerged. Further well designed comparative studies are needed to provide such information.

Animals↗

PubMed1979

Amoxycillin injectable: a review of its antibacterial spectrum, pharmacokinetics and therapeutic use.

Amoxycillin, an acid stable semisynthetic penicillin shown to be effective against a wide range of infections when given orally, is now available for intramuscular and intravenous injection. Amoxycillin has an antibacterial spectrum and level of activity essentially the same as for ampicillin. Amoxycillin has been shown to have more rapid and complete bactericidal action than ampicillin against E. coli in vitro and in animal models of infection, but the clinical importance of this difference has not yet been determined. Amoxycillin is present in therapeutic amounts in the cerebrospinal fluid of meningitis patients given the drug intravenously and parenteral amoxycillin has been successfully used in the treatment of meningitis, and in urinary tract infections, septicaemia, upper and lower respiratory tract infections and a variety of other infections caused by Gram-negative and Gram-positive aerobic bacteria. However, the extent of experience is limited compared with ampicillin, and thus further studies are needed to more clearly delineate its relative therapeutic role. Parenteral amoxycillin is generally well tolerated. Pain at the site of intramuscular injection occurs in about one-third of patients, but can be minimised by the use of lignocaine or procaine hydrochloride.

Amoxicillin↗

PubMed1979

Naproxen up to date: a review of its pharmacological properties and therapeutic efficacy and use in rheumatic diseases and pain states.

Naproxen is a propionic acid derivative with analgesic and anti-inflammatory activity which has been widely used in the treatment of rheumatic diseases. Naproxen has been well studied in rheumatoid arthritis and is as effective as aspirin but better tolerated, thus enabling more patients to continue with treatment. For this reason some clinicians now prefer to try propionic acid derivatives, such as naproxen, before aspirin in arthritic patients. In comparative studies with other non-steroidal anti-inflammatory drugs, such as indomethacin, ibuprofen, fenoprofen and others, all drugs were usually of similar overall efficacy although naproxen was sometimes preferred: but as with other non-steroidal anti-inflammatory agents, not all patients will respond to naproxen and in such cases other agents should also be tried until the most satisfactory drug is found for each patient. Naproxen is also effective in degenerative joint diseases of the hip and knee, although further well designed studies are needed to more clearly define its relative place compared with newer drugs such as diclofenac or diflunisal. Results of other comparative studies have shown that naproxen is a suitable alternative to phenylbutazone or indomethacin in ankylosing spondylitis and to aspirin in juvenile rheumatoid arthritis. Naproxen appears to be effective in reducing pain and swelling in acute gout and is an effective analgesic in patients with pain following surgery or trauma and in pain of dysmenorrhoea. Naproxen has generally been better tolerated than aspirin or indomethacin at the dosages used. Because of its relatively long plasma half-life, naproxen can with convenieice be given twice daily, and there is some evidence that once daily dosage is as effective in rheumatoid arthritis.

Animals↗

PubMed1979

Glipizide: a review of its pharmacological properties and therapeutic use.

Glipizide is a 'second generation' oral hypoglycaemic agent similar in potency to glibenclamide. It is completely absorbed after oral administration and has a rapid onset of action, but the duration of its hypoglycaemic effect is shorter than that of glibenclamide. It is rapidly metabolised to inactive metabolites which are excreted in the urine. Therapeutic trials have shown the efficacy of glipizide in maturity onset diabetes mellitus to be comparable with that of glibenclamide and chlorpropamide in newly diagnosed patients unresponsive to diet as well as in patients previously treated with oral hypoglycaemic drugs. Glipizide is well tolerated, but careful adjustment of dosage and attention to diet may be needed to avoid hypoglycaemic symptoms a few hours after a single daily dose.

Animals↗