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At least 685 records · Page 38Linked to original sources
PubMed1982

4-aminopyridine-a review.

4-aminopyridine is the first of the aminopyridines to be used in clinical practice. It blocks potassium channels and thereby increases acetylcholine, and possibly noradrenaline, release at nerve terminals. In man the drug has a significant action at the neuromuscular junction, but has little effect on the autonomic nervous system or muscle (smooth, skeletal, or cardiac) although such actions have been demonstrated in animals. It may be clinically useful in the reversal of nondepolariser blockade and a role in antibiotic associated block has been proposed. It may be used effectively as an analeptic agent. It appears to be a useful therapeutic agent in myasthenia gravis and Eaton Lambert syndrome, although of limited use in botulism. It effects on the central nervous system are considerable. These account for the major side effects of the drug which include tremor, excitability and convulsions.

4-Aminopyridine↗
PubMed1983

Improvement in ventilation-perfusion matching by almitrine in COPD.

Almitrine, a peripheral chemoreceptor stimulating drug, was given 100 mg orally to six patients with advanced chronic obstructive pulmonary disease (COPD), and its effects on hemodynamics, blood gases, lung mechanics, and the distribution of ventilation/perfusion ratios (VA/Q), determined by the inert gas elimination technique, were investigated. Arterial Po2 increased from 52 +/- 4 to 59 +/- 3 mm Hg, mean +/- SEM, p less than 0.01, arterial Pco2 decreased from 46 +/- 3 to 43 +/- 3 mm Hg, p less than 0.05, and venous admixture from 30 +/- 6 to 19 +/- 3 percent, p less than 0.02. No change occurred in ventilation, variables of lung mechanics, systemic and pulmonary hemodynamics, except an increase in pulmonary vascular resistance (from 364 +/- 103 to 438 +/- 99 dyne.s.cm-5, p less than 0.05). A reduction in VA/Q inequality could be demonstrated with a redistribution of blood flow into the lungs by a diversion of 15 percent of total blood flow from units with low VA/Q (between 0.08 and 0.4) to units with normal VA/Q (between 0.5 and 1.8). These changes might be explained by an enhancement of hypoxic pulmonary vasoconstriction. Pharmacologic peripheral chemoreceptor stimulation, at an infra-ventilatory analeptic dosage, might be of therapeutic interest to patients with respiratory insufficiency due to VA/Q inequality.

Administration, Oral↗
PubMed1991

Piracetam. An overview of its pharmacological properties and a review of its therapeutic use in senile cognitive disorders.

Piracetam is the first of the so-called 'nootropic' drugs, a unique class of drugs which affect mental function. In animal models and in healthy volunteers, the drug improves the efficiency of the higher telencephalic functions of the brain involved in cognitive processes such as learning and memory. The pharmacology of piracetam is unusual because it protects against various physical and chemical insults applied to the brain. It facilitates learning and memory in healthy animals and in animals whose brain function has been compromised, and it enhances interhemispheric transfer of information via callosal transmission. At the same time, even in relatively high dosages it is devoid of any sedative, analeptic or autonomic activities. How piracetam exerts its effects on memory disorders is still under investigation, although among other proposed mechanisms of action it is thought to facilitate central nervous system efficiency of cholinergic neurotransmission. Results from trials involving elderly patients with senile cognitive disorders have been equivocal, as have the results obtained when piracetam has been combined with acetylcholine precursors. Piracetam seems to be almost completely devoid of adverse effects, and is extremely well tolerated. In conclusion, opinion is divided as to the benefits of piracetam in the treatment of senile cognitive decline. Although double-blind studies in the elderly have produced mixed results, some such trials (particularly those involving larger numbers of patients) have reported favourable findings, thus offering some reason for cautious optimism in a notoriously difficult area of therapeutics. However, further investigations of piracetam alone and in combination therapy are required before any absolute conclusions can be drawn.

Aged↗
PubMed1982

Suppressive action of picrotoxin, a GABA antagonist, on labyrinthine spontaneous nystagmus and vertigo in man.

There is evidence that GABA acts as the excitatory neurotransmitter at synapses between vestibular hair cells and the afferent fibres in the mammalian labyrinth. The question arose as to whether certain vestibular dysfunctions such as labyrinthine vertigo could be treated in patients by influencing the peripheral GABA system by means of the GABA antagonist picrotoxin, a well known analeptic drug. With the application of slow infusion rates of only milligrams of picrotoxin a distinct suppression of peripheral spontaneous nystagmus, caloric excitability of labyrinths, and labyrinthine vertigo, without general CNS-induced arousal effect, was observed. A latent central spontaneous nystagmus can become manifest, whereas a manifest central spontaneous nystagmus remains unchanged. A future application of picrotoxin as a diagnostic and therapeutic tool in cases involving vestibular disorders is discussed.

Dose-Response Relationship, Drug↗
PubMed1976

Lethal effect of the serotonin-xylocaineR association in ganglion-blocked rats.

In rats anestetized with urethane and under ganglionic blockade by hexamethonium (20 mg/kg, i.v.), the i.v. injection of serotonin (60 mug/kg) determined apnea, ECG alterations and a brief hypotensive response which is similar to that as elicited when 5-HT is given to intact rats. During the hypertension which follows that initial response, apnea is still present along with more severe ECG changes. After that, blood pressure falls into a prolonged hypotension, which is invariably accompanied by death. Neither norepinephrine, nor respiratory analeptics (CoramineR, RemeflinF) were able to prevent the fatal outcome. Only artificial respiration was found to be useful in some instances. It was concluded that the association serotonin plus lidocaine becomes lethal when given to ganglion-blocked rate, and this toxic effect can be ascribed mainly to the respiratory depressor activity of the drugs.

Animals↗
PubMed1997

[Study on effect of reinforcing kidney and invigorating spleen principle on severe asthma].

OBJECTIVE: To explore on prevention and treatment of severe asthma with reinforcing the Kidney and invigoration the Spleen Principle (RKISP) and its mechanism. METHODS: Patients were treated with steroid aerosol (as control group), and both steroid aerosol and RKISP (as test group) respectively. RESULTS: The markedly effective rate of the test group was higher than that of the control group, the doses of beta-analeptic and the side-effect rates of the test group were lower than that of the control group, the pulmonary function of the test group was more remarkably improved. After treatment, the T cell hyperplasia response to specific allergen, the basophilic cell releasing capacity, the serum IgE and eosinophil of the test group were all reduced more obviously than those of the control group. In the control group, the neutrophil increased and the neutrophil phagocytic capability as well as the function of adrenal cortex were declined. While in the test group, the neutrophil phagocytic capability was raised, the neutrophil and the function of adrenal cortex had no significant changes. CONCLUSIONS: RKISP cooperated with steroid in relieving attack of asthma, and it was more important for it to display an obvious modulation action on immune and neuroendocrine system.

Administration, Inhalation↗
PubMed1975

[Cyclizine-intoxication in six children (author's transl)].

Cyclizine hydrochloride (Marezine, Echnatol) an antihistaminic drug is commonly used for the treatment of motion sickness. During the past two years we observed six cases of accidental moderate intoxication with an average of 200 mg of cyclizine hydrochloride in children between 2 and 4 years of age. The symptoms became obvious about 1 to 2 hours following ingestion. Among the main symptoms our patients revealed were such as excitement, incoordination, ataxia, athetoid movements and severe hallucinationes. The faces were flushed, the pupils dilated, but dryness of the mouth and hoarseness were never found. Convulsions did not occur. The treatment is purely symtomatic, histamine, apomorphine, phenothiazines and analeptics should not be used.

Adrenal Cortex Hormones↗
PubMed1976

[Effect of fominoben on ventilation, oxygen uptake and blood gases in patients with obstructive ventilation disorders].

The substituted benzylamin-derivative fominoben (PB 89 Noleptan) was intravenously administered to 12 patients with chronic obstructive lung disease in order to determine, whether an analeptic action on respiration, which had been found by others in animal studies and in healthy subjects, can also be demonstrated in patients with COLD. Time ventilation showed no statistically significant change. Respiratory rate was increased for a short time, alveolar ventilation showed a slight but significant increase 35 minutes after i.v. injection of fominoben, however no significant change in the first 10 minutes after injection.--Arterial pO2 was slightly but not significantly increased in the first 10 minutes after fominoben, while the same patients showed a significant decrease of pO2 after injection of placebo. As alveolar ventilation at this time had not significantly changed, the increase in pO2 can only be explained by an improvement of regional ventilation-perfusion ratio by fominoben. -In conclusion it can be stated, that a marked stimulative action on respiration by fominoben could not be demonstrated. There was, however, no depression of respiration as it is associated with most other caugh medications. As the drug has been shown to be an excellent caugh sedative, lack of respiratory depression can be considered as a considerable advantage.

Adult↗
PubMed1975

[Clinico-immunologic shifts in pleural empyema in patients of different age].

In 218 patients the causes of pleural empyema, the state of immunological indices and treatment have been studied in relation to patient's age. It is demonstrated that the most inadequate protection potential, conditioned by an insufficient specific resistance, is observed in children and patients over 50 years of age. The treatment of pleural empyema is usually started with a puncture method of administering antibiotics, enzymes and general analeptic drugs. In children due to a rapidly progressing intoxication and pulmonary insufficiency thoracocentesis was employed in 55.5%, in patients aged from 16 to 50 years pleurectomy and other operative procedures were accomplished. In patients over 50 years of age a puncture method and thoracocentesis were applied, surgery being used only in 10.4 per cent.

Adolescent↗
PubMed1992

[Development of continuous monitoring of spontaneous respiration in the postoperative phase. 2. Cutaneous oxygen and carbon dioxide partial pressures following i.v. bolus application of fentanyl, buprenorphine, naloxone and amiphenazole in healthy adult subjects].

METHODS: In an attempt to develop a noninvasive monitoring technique for patients in the early postoperative period, cutaneous O2 and CO2 pressures (pctO2, pctCO2) were monitored in ten healthy adult volunteers of both sexes (5 male, 5 female, age 29 +/- 5 years, weight 68 +/- 11 kg) who received, in several sessions after a 60-min equilibration period, i.v. bolus doses of fentanyl (3 micrograms/kg and, 60 min later, another 1.5 micrograms/kg), buprenorphine (3 and 1.5 micrograms/kg), naloxone (1.8 and 0.9 micrograms/kg), and the respiratory analeptic amiphenazole (2 and 1 mg/kg) as well as combinations of fentanyl/amiphenazole or buprenorphine/naloxone in the aforementioned dosages. Data were collected and stored by a personal computer using the TCM3 system with a combination electrode for simultaneous measuring of pctO2 and pctCO2 (TINA, Radiometer) at 30-s intervals. The overall observation period was 240 min. Means, standard deviations, and ranges were calculated for individual data and data pooled for 15-min intervals. Groups were compared by means of Student's t-test and analysis of variance. RESULTS: Following i.v. fentanyl 3 micrograms/kg, pctO2 decreased and pctCO2 increased rapidly and statistically significantly. The changes were of similar intensity after the first and second doses (1.5 micrograms/kg) and normalized about 60 min after each injection. In contrast, following i.v. buprenorphine (3 and 1.5 micrograms/kg) the cutaneous partial pressures changed continuously and progressively during the observation period and did not reach the control values after 240 min. Naloxone and amiphenazole injections had no obvious influence on the time course of the blood gas tensions. If opiates and antagonists were combined, neither the fentanyl/amiphenazole group nor the buprenorphine/naloxone group differed significantly from the respective opiate groups. DISCUSSION AND CONCLUSION: As was discussed in detail in a previous communication, monitoring of opiate-induced respiratory depression must be nonstimulant and, preferably, noninvasive. Whereas the precision and/or limitations of monitoring partial oxygen saturations by pulse oximetry is well documented in the literature, knowledge of the value of cutaneous partial pressure monitoring is still limited and controversial for the adult patient population. The present study was performed to define the usefulness of cutaneous blood gas analysis in healthy volunteers receiving opiate dosages well known in recovery room patients. It is concluded that continuous monitoring of pctO2 and pctCO2 can indeed detect opiate-induced respiratory depression in adults. The well-known difference in respiratory pattern for fentanyl and buprenorphine could easily be determined. It was confirmed that naloxone and amiphenazole in the dosage range studied do not influence spontaneous respiration in healthy adults. Thus, the authors are convinced that continuous monitoring of cutaneous partial pressures of oxygen and carbon dioxide is sensitive enough to be used, in combination with pulse oximetry, in a monitoring concept for patients recovering from surgery and anaesthesia. Results in patients undergoing conventional pain management or patient-controlled analgesia with relatively high opiate dosages will be presented in following papers. Concerning the controversy about clinically relevant interactions between fentanyl and amiphenazole or buprenorphine and naloxone, the present study did not confirm any useful antagonism. Whether this is due to limitations of cutaneous monitoring, the difference between volunteers and patients, or pharmacological reasons must be evaluated in further investigations.

Adult↗
PubMed1963

Controlled observations on the single case.

Valuable information can be gained from studies of a single case, provided bias on the part of physician and patient can be minimized. Use of the double-blind method achieves this. Some pitfalls in such studies are mentioned, and it is emphasized that skill, judgment and knowledge all play a part in the design and interpretation of investigations of this nature. As an example, a trial of three analeptics in the treatment of a narcoleptic patient, using a simple rating scale, is described.

Central Nervous System Stimulants↗
PubMed1977

[Paroxysmal alveolar hypoventilation syndrome (author's transl)].

The case of a 42-year-old female patient with central disturbance of respiration was reported which, contrary to the previously described forms of central alveolar hypoventilation, could be characterized by paroxysmal-like apnoic conditions without any feeling of suffocation. Clinically, initial cardiopulmonary complications were primary in this central disturbance of respiration. The possibility of isolated apnoic paroxysms as an expression of a true cerebro-organic nature of the attacks was described. In addition, the attempt was made to localize the morphological or functional disturbance at the basis of the observed pathological process in the bulbopontine area of the brain stem on the ventral side of the medulla in the area of the point of exit of the seventh to the twelfth cranial nerves. With anticonvulsive and analeptic treatment, a distinct improvement could be observed in the disease after the cardiopulmonary complications had subsided.

Adult↗
PubMed1965

THE CHEMOTHERAPY OF CARDIAC ARREST.

Direct-air ventilation, external cardiac compression, and external defibrillation are established techniques for patients who unexpectedly develop cardiac arrest. The proper use of drugs can increase the incidence of successful resuscitation. Intracardiac adrenaline (epinephrine) acts as a powerful stimulant during cardiac standstill and, in addition, converts fine ventricular fibrillation to a coarser type, more responsive to electrical defibrillation. Routine use of intravenous sodium bicarbonate is recommended to combat the severe metabolic acidosis accompanying cardiac arrest. Lidocaine is particularly useful when ventricular fibrillation or ventricular tachycardia tends to recur. Analeptics are contraindicated, since they invariably increase oxygen requirements of already hypoxic cerebral tissues. The following acrostic is a useful mnemonic for recalling the details of the management of cardiac arrest in their proper order: A (Airway), B (Breathing), C (Circulation), D (Diagnosis of underlying cause), E (Epinephrine), F (Fibrillation), G (Glucose intravenously), pH (Sodium bicarbonate), I (Intensive care).

Acidosis↗
PubMed1959

A barbiturate antidote. Use of methylethyl-glutarmide in barbiturate intoxication and in terminating barbiturate anesthesia.

Methylethylglutarimide was administered to 488 patients ranging in age from 7 to 89 years, in a study on sleep-reversal after harbiturate anesthesia. Sodium surital or sodium pentothal were the barbiturates used. The drug was administered intravenously in doses varying from 25 to 200 mg. Dosage below 25 mg. was found to be ineffective. Almost all patients showed signs of awakening as evidenced by the return of corneal and conjunctival reflexes, the opening of the eyes, and stirring or moving about. Many responded to questioning. Almost all showed evidence of greater responsiveness within five minutes. No untoward reactions were noted. No convulsions were produced. Five patients ranging in age from 24 to 70 years were treated for barbiturate poisoning with Mikedimide(R) given intravenously in doses varying from 550 mg. to 1950 mg. All recovered consciousness within 30 minutes to an hour. No convulsions were produced. While it is not known whether Mikedimide is a direct barbiturate antagonist, or whether it is an analeptic, it appears to be a useful drug in reversing the respiratory depression and the cerebral depression produced by harbiturate intoxication and barbiturate anesthesia.

Anesthesia↗
PubMed2003

[Blood pressure disorders during idiopathic Parkinson's disease].

SEVERAL EXPLANATIONS FOR THE HIGH PREVALENCE: In Parkinson's disease, the prevalence of symptomatic orthostatic hypotension (OH) concerns more than 20% of the patients. At least 2 factors explain this high prevalence. Dopamine-mimetic drugs may induce or enhance the occurrence of OH. Parkinson's disease is a cause of primary autonomic failure with involvement of the peripheral nervous system. CHARACTERISTIC HISTOLOGICAL AND PHARMACOLOGICAL ELEMENTS: Histology indicates that Lewy bodies exist in the sympathetic glands. Pharmacology reveals cardiac sympathetic denervation. These histological and pharmacological characteristics clearly differentiate autonomic failure of Parkinson's disease from multiple system atrophy (Shy-Drager's syndrome). If autonomic abnormalities appear to be present since the early stages of the disease, the early onset, within the first year, of symptomatic OH in the course of a parkinsonian syndrome can be considered as an exclusion criterion for idiopathic Parkinson's disease. REGARDING TREATMENT: No specific clinical trials have assessed the efficacy of antihypotensive drugs in the treatment of OH in Parkinson's disease. The management of this symptom requires education of the patient and the development of non-pharmacological measures. Drug therapy should be reserved for symptomatic patients who do not improve with the preceding methods. Among the drugs available, domperidone, although widely used, has no proven effect on OH like the cardiovascular analeptics. The alpha1-adrenergic agonists (midodrine) or mineralocorticosteroids (fludrocortisone) are the most frequently used drugs.

Adrenergic alpha-Agonists↗
PubMedDate not supplied

[Changes in individual resistance of cardiovascular and respiratory systems of rats to posthemorrhagic hypoxia after pharmacological impact on brain function].

In experiments on rats it was shown that injection to rats before hemorrhage of analeptic corasol or prior injections during three days of the inhibitory mediator sodium oxybutyrate decrease individual resistance of the respiratory and circulatory systems (arterial blood pressure, cardiac output, organ portal blood flow) to posthemorrhagic hypoxia. Injection to animals before the hemorrhage of GABA-A antagonist picrotoxin significantly raises individual resistance to massive bleeding. Individual resistance to acute hemorrhage correlates with individual sensitivity of cardiovascular and respiratory systems to corasol.

Animals↗
PubMed2003

[Chocolate in some french pharmaceutical or medicinal books from XVIIth, XVIIIth and XIXth centuries. Its beneficent and inconvenient, proved or imaginary, effects].

Rapidly after its appearance in France, interesting properties were attributed to chocolate and it was used in medicine,often wrongly, to treat digestive, pulmonary, nervous, even infectious diseases, and also for its nutritive and aphrodisiacal capability... But it was already charged with insomnia or constipation. During the XIXth century, chocolate was used as food and as an excipient for dissimulation and transportation of drugs. Medicinal chocolates were essentially nutritive and analeptic, pectoral, stomachic, purgative or anthelmintic. All of them have disappeared today, but the pharmacological interest of chocolate remains with its antidepressive activity and the promising proposes of some of its components. However, chocolate is still considered to be responsible of constipation, headache or pimples...

Books↗
PubMed1991

Effects of age and drugs on food and fluid intake.

In young adults rats (5-month-old) d-amphetamine (2 mg/kg/d), administered on a long-term basis via drinking water, caused a moderate reduction in the intake of nutriments, which in part normalized within three weeks. Self-administration of a daily dose of 20 mg per kg diazepam over a period of 26 days led neither to hypodipsia nor to anorexia. Pentylenetetrazol (70 mg/kg/d) primarily produced a hypodipsia. The three drugs did not influence body weight. In 27-month-old rats d-amphetamine and pentylenetetrazol had the same qualitative effects. Intake of nutriments and the development of body weight were influenced more strongly than in young rats. Diazepam also had a marked effect in old animals. Nootropics (piracetam, pyrithinol, hydergin, centrophenoxin, aniracetam) had no effects on the parameters observed. When the agents were given in combination in both age groups the nootropic piracetam (230 mg/kg/d) weakened the effects induced by d-amphetamine, pentylenetetrazol or diazepam alone. The benzodiazepine, however, enhanced the loss of body weight and fluid intake in old rats caused by the stimulant or analeptic, whereas food intake remained unaffected. The results support the hypothesis that an organism's adaptivity to external and internal stimuli is reduced in later life. The behavior of young and old rats in the open field was not affected by any drug medication.

Aging↗