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Hospice approach to the treatment of patients with advanced dementia of the Alzheimer type.

A program that limits the extent of medical treatment in patients with advanced dementia of the Alzheimer type was initiated on an intermediate medical ward. Five levels of care were designed to define options that stress maintenance of patient comfort without striving for a maximal period of survival (hospice approach). An optimal care level for each patient recommended by the staff correlated highly with the severity of dementia, but care levels assigned during meetings of family members with the multidisciplinary team for 40 patients correlated poorly with the staff recommendations and the severity of dementia. Intensive nursing care and comfort measures, which included antipyretics, analgesics, and (if necessary) oxygen and anticholinergics, were provided during the terminal phase. Preliminary results indicate that the mortality did not increase significantly during the first year of this program, although the extent of medical care was limited in all patients, and 62% were not treated with antibiotics if they developed symptoms of pneumonia or urinary tract infection.

Aged↗

Evaluation of a new pharmaceutical form of nimesulide for the treatment of influenza.

In 39 outpatients suffering from a seasonal epidemic influenza, the antipyretic, analgesic and anti-inflammatory activity of nimesulide granules was compared with that of aspirin + vitamin C granules. The drugs were administered b.i.d., dispensed in one-dose sachets containing either 100 mg of nimesulide or 500 mg aspirin + 300 mg vitamin C. The efficacy of the two treatments was comparable: both drugs brought about a rapid complete recovery in all treated patients. However, nimesulide was better tolerated: only one case of slight gastralgia was recorded in the nimesulide group vs the six cases of side-effects complained of in the aspirin + vitamin C group.

Adolescent↗

Analgesic, anti-inflammatory and oxy-radical scavenger activity of imidazole and imidazole derivatives.

The author describes the recent work of his laboratory on imidazole. It increased the analgesic effects of morphine, and rivalled acetylsalicylic acid as an analgesic antipyretic agent. At 160 mg/kg, imidazole protected rats against indomethacin-induced gastric ulcers. It was equal to acetylsalicylic acid in reducing carrageenan inflammation, and was superior to it as anti-arthritic drug. Imidazole 2-hydroxybenzoate caused 36% inhibition of synovial fluid depolymerization.

Animals↗

Developing drug-use profiles from drug-charge records.

The potential for developing a drug-use profile from drug-charge records was studied at an 830-bed community hospital. Patient drug charges were reviewed retrospectively for one year (1975) to identify: (1) which key drugs accounted for a high percentage of cost and usage; (2) where key drugs were used within the hospital; (3) how they were used; and (4) who were the chief prescribers. Of the drugs used, 8% accounted for 80% of total drug product costs. Seven drug groups (10% of the total drug groups) appeared in the top 10 of both drug cost and quantity categories. Six individual drugs also appeared in the top 10 of both categories. According to cost, cephalosporin antibiotics were ranked first among drug groups but were sixth according to quantity. Analgesics-antipyretics were ranked first among drug groups by quantity and second by cost. Cephalothin was ranked first among individual drugs by cost and was not in the top 10 in quantity. Diazepam was ranked first among individual drugs by quantity and third by cost. Patients' drug-charge records can be used effectively to generate drug-use profiles for ongoing drug use review, quality assurance and cost containment programs.

California↗

Research on heterocyclic compounds. XV. Substitution influence on the pharmacological activity in a series of imidazo[1,2-a]pyridines.

We have taken into consideration a group of 28 imidazo [1,2-a]pyridine derivatives, some of which were already known, whereas the others have been synthesized and characterized to complete the series. Antiinflammatory, analgesic, antipyretic and ulcerogenic activities of such compounds were evaluated in comparison with indomethacin. The pharmacological data demonstrated the effects exerted on activity by the presence on the heterocyclic system of methyl substituents and/or an acidic moiety.

Animals↗

[Unexpected anti-inflammatory activity of rigid structures derived from antihypertensive 6-arylpyridazinones. III. Synthesis and activity of 7-fluoro- and 5-keto-5H-indeno(1,2-c)pyridozines].

5H-Indeno[1,2-c]pyridazine (Ia) and its 3-oxo- and 4,4a-dihydro-3-oxo derivatives, already known to have antiinflammatory activity, were subjected to 7-fluoro substitution or to oxidation of the 5-methylene to a carbonyl group. The pharmacological evaluation of the resulting compounds indicated that the antiinflammatory activity disappeared in the fluoro derivatives, while it was still present in the 5-keto derivatives (I e), (II c). Moreover, the analgesic-antipyretic component of (I e) proved to be strongly enhanced compared with that of (I a).

Animals↗

[Off-label use of lincomycin hydrochloride in 2 horses. Dysbacteriosis and fatal complications due to inadequate symptomatic therapy].

A lawyer inquired about the possible harmful effects of 'off-label use' of lincomycin in two trotting horses. From information in the relevant dossier it could be concluded that there was no direct indication to use antibiotics. In addition, mistakes were made in the medicinal treatment of horses, namely, the off-label use of lincomycin without prior consultation with the manufacturer, fluid and electrolyte replacement therapy not continued for long enough, and incorrect use of antipyretic analgesics. The intravenous administration of gentamicin to dehydrated patients is permissible only in combination with adequate administration of fluids and electrolytes.

Animals↗

Benzydamine Hydrochloride (Tantum) in the management of oral inflammatory conditions.

Benzydamine HCL (Tantum) is a topical nonsteroidal anti-inflammatory drug (NSAID) with anti-inflammatory, analgesic, antipyretic and local anesthetic activity. This paper reviews the pharmacology of benzydamine and surveys the existing literature relating to its applications in medicine and dentistry. Guidelines for its use in dentistry are offered.

Benzydamine↗

[Effects of various dosage of ketoprofen salt suppositories in acute inflammatory disease in infants (3-36 month old) and children (3-13 year old)].

In two multicentric randomized, double-blind, parallel design trials the more appropriate dose of ketoprofen lysine salt suppositories, by considering benefit-risk ratio, was determined in children affected by acute inflammatory disease of respiratory or urinary tract with fever and pain. Fifty-three children ranging 6-36 months (infants) randomly assigned to 20, 30, 40 mg dose levels, and 54 children ranging 3-13 years (children) randomly assigned to 40, 60, 80 mg dose levels were included in the studies. Efficacy variables considered were hyperthermia and pain; body temperature was measured rectally, at fixed intervals and pain was evaluated by Maunuskela scale at the same interval times. Standard laboratory test were obtained at the beginning and end of treatment, and blood arterial pressure and heart rate were recorded regularly. Systemic and local tolerability were also determined. In infants all doses were associated with analgesia and temperature reduction; antipyretic effect was statistically significant starting from the first hour (p = 0.007). The dose of 30 mg resulted different from 20 mg dose from third hour (p < 0.05). The appropriate dose that better relate antipyretic and analgesic efficacy with a good tolerability was 30 mg. In children the analgesic and antipyretic efficacy was well established at all doses tested, however the effects were more marked and prolonged at 60 and 80 mg doses, with a better tolerability for 60 mg dose. The tolerability of all doses studied was good. Doses of 30 mg in infants and 60 mg in children correspond to a range of 2.0-3.5 mg of ketoprofen lysine salt for kg body weight, for each administration.

Acute Disease↗

General pharmacology of [2,2-dimethyl-6-(4-chlorophenyl)-7-phenyl-2,3- dihydro-1H-pyrrolizine-5-yl]-acetic acid in experimental animals.

[2,2-Dimethyl-6-(4-chlorophenyl)-7-phenyl-2,3-dihydro-1H-pyrrolizine-5- yl]-acetic acid (ML 3000) is a newly synthesized compound with analgesic, antipyretic and anti-inflammatory activity. The general pharmacological effects of ML 3000 following oral administration were investigated in experimental animals. The results showed that with regard to the CNS, ML 3000 did not affect behaviour in the Irwin test, locomotor activity or hexobarbital-induced sleep at doses of 30, 100 and 300 mg/kg. ML 3000, at a single dose of 100 mg/kg administered intraduodenally, had no notable effect on the cardiovascular system or respiration in anaesthestised rats and dogs nor on neuromuscular function in anaesthetised cats. No evidence of gastric damage or disturbance of peristalsis was observed following oral administration of ML 3000. In vitro, ML 3000 evoked a weak spasmogenic response in the guinea-pig ileum with a dose-related inhibition of acetylcholine, histamine and barium chloride-induced responses. A small transient reduction in urine volume was observed after the highest dose accompanied by decreases in electrolyte excretion at doses of 100 and 300 mg/kg in rats. The results demonstrate that ML 3000 has no notable general pharmacological effects under the experimental conditions reported.

Acetates↗

Inhibition of dihydrofolate reductase activity by alcoholic extracts from Fraxinus excelsior, Populus tremula and Solidago virgaurea.

Aqueous-ethanolic extracts of Fraxinus excelsior, Populus, tremula and Solidago virgaurea in a combination of 1: 3: 1 (v/v/v) are the components of the plant drug Phytodolor N (abbreviated as PD), which exhibits antipyretic, analgesic and antirheumatic activity. Similar to a broad variety of synthetic non-steroidal anti-inflammatories the mentioned plant extracts inhibit dihydrofolate reductase. The following concentrations as percentage in the test volumes represent the individual I50-values: F. excelsior = 0.26% (v/v); P. tremula = 0.46% (v/v) and S. virgaurea = 0.6% (v/v). The combined extracts in PD exhibit an I50 at 0.3% (v/v). Testing the activity of the water-soluble compounds of corresponding dry extracts, the activity of F. excelsior with an apparent I50-value of 0.008% (w/v) by far dominates the inhibitory overall effect of the combination (I50 = 0.014%, w/v).

Animals↗

Antioxidative properties of alcoholic extracts from Fraxinus excelsior, Populus tremula and Solidago virgaurea.

Aqueous-ethanolic extracts from Fraxinus excelsior, Populus tremula and Solidago virgaurea inhibit biochemical model reactions representing inflammatory situations to various extents. These model reactions include xanthine oxidase, diaphorase in the presence of the autoxidizable quinone juglone, lipoxygenase and photodynamic reactions driven by riboflavin or rose bengal. The tested extracts are the components of the phytomedicine Phytodolor N (abbreviated as PD) which possesses antipyretic, analgesic, antiinflammatory and antirheumatic activity. Since several reactive oxygen species produced by the mentioned model systems are also involved in inflammatory processes, the beneficial activities of the complete drug may at least in part be due to the reported antioxidative functions of the individual components.

Animals↗

[Polypharmacotherapy in the elderly hypertensive patient].

We asked 53 elderly hypertensives from our outpatient clinic which and how many drugs they took, and analysed factors that could have affected the intake, as sex, age and school instruction. The most frequent drug groups found were, in decreasing order, antihypertensives, benzodiazepines, nitrates and non-steroidal anti-inflammatory drugs. 53.3% of the patients took only angiotensin converting enzyme inhibitors and/or calcium-channel antagonists as antihypertensive drugs. Twenty four patients used occasional medications, sometimes as much as 6 different drugs, specially analgesics, antipyretics and anti-inflammatory agents. These patients took, in mean, 5.2 different drugs daily, 2.1 of which antihypertensive, in a total of 8.5 pills. Females took more drugs (9.4 +/- 3.6 pills per day against 7.1 +/- 3.0 in the male gender, Z < 0.03). Age and school instruction did not affect the intake.

Age Distribution↗

Pharmacoepidemiology of drug use at two primary health care centres in northern India.

There is a consensus amongst most health care centers that limited drugs should be available to meet most requirements at the first tier of health care. However, few studies have addressed themselves to determining this. The objectives of this study were to provide a description of the availability and prescription of modern pharmaceuticals at 2 selected Primary Health Care Centres in Northern India. The main results of this study are: documentation of age/sex of patients on prescriptions was not kept in all cases; prescribing by both generic/brand names was observed with generics predominating; most patients received 0-2 drugs; dosages were not specified in 10% of the cases, duration not specified in 30% of the cases, and dosage form not indicated in 30% of all drugs prescribed; treatment was sought for problems pertaining to gastrointestinal, respiratory, dermatological and musculoskeletal systems; and the most prescribed drugs were analgesics, antipyretics, antimicrobials, hematinics and antihistaminics.

Ambulatory Care Facilities↗

Anti-inflammatory properties of 3-methylpyrazolin-5-(4 H)-one-4-[3'-methoxy-4' (2'',3'',4'',6''-tetra-O-acetyl-beta-D-glycopyranosyl]benzylidene (compound IIIA).

Oral treatment of compound IIIA exhibited dose related inhibitory action in acute tests of carrageenan, histamine and dextran-induced oedema in rats. Marked inhibitory action of the compound was found when it was administered intraperitoneally in animals. It displayed prominent anti-arthritic activity in chronic tests of adjuvant and formaldehyde-induced arthritis in rats. It prevented the arthritis associated rise in total leucocyte count and erythrocyte sedimentation rate. It also lowered the levels of exudate volume and migration of leucocytes in carrageenan induced pleurisy in rats. It did not exhibit any analgesic, antipyretic or ulcerogenic effect. No mortality was recorded up to 2 g/kg in mice on oral or intraperitoneal treatment over a period of 72 hr.

Animals↗

[Incidence and probable etiology of toxic agranulocytosis in a definite population in the province of Buenos Aires (1963-1976)].

The medical records of 55 patients with toxic agranulocytosis (unrelated to radiation, anticancer drugs or known industrial toxics) were reviewed in a well defined population of the Province of Buenos Aires during 1963-1976. There were 65 episodes in 30 women and 25 men, age average 49 years. Nine patients repeated the episode by reexposure to the same drug. The annual incidence rate was 8.4 cases per million/year. Nineteen (35.5%) of the patients died. Forty-three episodes (64.3%) were associated with analgesic-antipyretics, mainly dipyrone (34 cases). In most situations, drugs were prescribed for mild complaints such as pharyngitis, arthralgias or abdominal pain. Although toxic agranulocytosis is an infrequent disease, its relationship with drugs is well known and its mortality remains high.

Adolescent↗

Pharmacological profile of a new pyrrolizine derivative inhibiting the enzymes cyclo-oxygenase and 5-lipoxygenase.

2,2-Dimethyl-6-(4-chlorophenyl)-7-phenyl, 2,3-dihydro-1H-pyrrolizine-5-yl)-acetic acid (ML 3000) is a dual inhibitor of the enzymes cyclo-oxygenase and 5-lipoxygenase in bovine and human thrombocytes and granulocytes. In animal experiments the compound has antiphlogistic, analgesic, antipyretic, antiasthmatic and antiaggregative activity at a dosage that causes no gastrointestinal damage.

Acetates↗