Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0010200 (cough)
 23,843 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Benazepril (CGS 14824A HCl) is a new prodrug type angiotensin converting enzyme (ACE) inhibitor. The active form is considered to be benazeprilat, a diacid hydrolyzed compound. Benazepril and benazeprilat inhibited the contraction induced by exposure with angiotensin I, not angiotensin II, in the isolated rabbit aorta. The ACE inhibiting activity of benazeprilat was 1000 times more potent than that of benazepril in this experiment. Benazepril as well as benazeprilat and captopril exerted little influence on norepinephrine, serotonin and high K(+)-induced contraction or bradykinin-induced relaxation in isolated blood vessel preparations, thus angiotensin II synthesis inhibition seemed to be the main cause for its vasodilation. Benazepril, unlike benazeprilat or captopril showed considerable influence on prostaglandin (PG)-induced responses at higher concentrations. The vasocontraction induced by PGF2 alpha was competitively antagonized at 10(-5)-10(-4) mol/l, while vascular responses induced by PGE1, PGE2 or PGI2 was inhibited at 3 x 10(-4) mol/l of benazepril. Although these influences on PGs might not contribute much to its vasodilatory mechanism, the action seemed interesting in relation to cough induction, a known side effect of ACE inhibitors in the market. Benazepril has two asymmetric carbon atoms, thus four optical isomers are possible, SS (benazepril), SR (CGP 14'829A), RS (CGP 42'454A), RR (CGP 42'456A). The SS configuration was the most potent for antagonizing angiotensin I-induced vasocontraction, which seemed to be the best fitted for the ACE molecule.
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PMID:Antihypertensive mechanism of action of the novel angiotensin converting enzyme inhibitor benazepril. Effect on isolated vascular preparations. 208 Sep 46

4-carbomethoxythiazolidine HCl has been administered to 24 patients (aged between 64 and 86) suffering from new acute stages of chronic bronchitis. The patients have been submitted to a double-blind test and have been subdivided into four groups; each of them was administered a placebo or the a.m. product. Dosage: 200, 400 and 600 mg/d. The following symptoms have been evaluated: cough; dyspnea; bronchial breathings; expectoration; expectorate's viscosity; expectorate's volume. The data have been submitted to a statistic analyses, this research leads to the followings considerations. A dosage of 200 mg/d. is not significantly active on any on the considered parameters. The 400 mg dosage turns out to be noticeably more effective than the placebo on all parameters (except the difficulty in expectoration). A dosage of 600 mg/d. has a significant effect on all the measurable parameters. Finally, a 200 mg dosage of 4-carbomethoxythiazolidine three times a day results to be the best posology in the symptomatic treatment of the respiratory manifestations of chronic bronchitis.
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PMID:[Therapeutic efficacy and general tolerability of 4-carbomethoxythiazolidine chlorohydrate in patients with exacerbated chronic bronchitis]. 210 5

It is sometimes necessary for the practitioner to transfuse the ruminant with whole blood or plasma. These techniques are often difficult to perform in practice and are time-consuming, expensive, and stressful to the animal. Acute loss of 20-25% of the blood volume will result in marked clinical signs of anemia, including tachycardia and maniacal behavior. The PCV is only a useful tool with which to monitor acute blood loss after intravascular equilibration with other fluid compartments has occurred. An acutely developing PCV of 15% or less may require transfusion. Chronic anemia with PCV of 7-12% can be tolerated without transfusion if the animal is not stressed and no further decline in erythrocyte mass occurs. Seventy-five per cent of transfused bovine erythrocytes are destroyed within 48 hours of transfusion. A transfusion rate of 10-20 ml/kg, recipient weight, is necessary to result in any appreciable increase in PCV. A nonpregnant donor can contribute 10-15 ml of blood/kg body weight at 2-4 week intervals. Sodium citrate is an effective anticoagulant, but acid citrate dextrose should be used if blood is to be stored for more than a few hours. Blood should not be stored more than 2 weeks prior to administration. Heparin is an unsuitable anticoagulant because the quantity of heparin required for clot-free blood collection will lead to coagulation defects in the recipient. Blood crossmatching is only rarely performed in the ruminant. In field situations, it is advisable to inject 200 ml of donor blood into the adult recipient and wait 10 minutes. If no reaction occurs, the rest of the blood can probably be safely administered as long as volume overload problems do not develop. Adverse reactions are most commonly seen in very young animals or pregnant cattle. Signs of blood or plasma transfusion reaction include hiccoughing, tachycardia, tachypnea, sweating, muscle tremors, pruritus, salivation, cough, dyspnea, fever, lacrimation, hematuria, hemoglobinuria, collapse, apnea, and opisthotonos. Intravenous epinephrine HCl 1:1000 can be administered (0.2 to 0.5 ml) intravenously or (4 to 5 ml) intramuscularly if clinical signs are severe. Pretreatment with antipyretics and slowing the administration rate may decrease the febrile response. Blood or plasma administered too rapidly will also result in signs of cardiovascular overload, acute heart failure, and pulmonary hypertension and edema. Furosemide and slower administration of blood or plasma should alleviate this problem.(ABSTRACT TRUNCATED AT 400 WORDS)
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PMID:Use of blood and blood products. 217 38

The pharmacological actions of double-enkephalin (biphalin; (HCl-Try-D-Ala-Gly-Phe-NH-)2) an analogue of enkephalin, on nociception, respiration and the cough reflex were compared with those of morphine in anesthetized rats. Double-enkephalin (D-Enk), injected i.p., produced significant analgesia at doses of 10 and 20 mg/kg in a hot-plate test. The analgesic effect of D-Enk was antagonized by pretreatment with naloxone (5 mg/kg, i.p.). D-Enk and morphine (M) produced a dose-dependent decrease in the frequency of respiration (RF) and in the tidal volume (Vt). However, the effects of D-Enk on RF and Vt were significantly weaker than those of M. The 50% antitussive dose (AtD50) of D-Enk and M were 0.63 and 0.48 mg/kg, i.p., respectively. The antitussive effect of D-Enk was antagonized by pretreatment with naloxone (0.4 mg/kg, i.p.). These results suggest that D-Enk exerted an antitussive effect similar to that of morphine, and that the involvement of opiate receptors is associated with the antitussive effect of D-Enk.
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PMID:Effects of double-enkephalin (biphalin), an enkephalin analogue, on respiration and the cough reflex in rats. 321 86

Vadocaine hydrochloride (2',4'-dimethyl-6'-methoxy-3-(2-methylpiperidyl) propionanilide hydrochloride, OR K-242-HCl; INN: vadocaine) is a novel antitussive compound structurally resembling local anaesthetics. Its antitussive profile was studied in several animal models. In guinea-pigs, vadocaine reduced by about 70% the cough episodes induced by sulphur dioxide or ammonia. The effective dose was 2.5 mg/kg p.o., and codeine phosphate was less effective. In cats, vadocaine (3 mg/kg i.v.) inhibited by about 80% for 10 min the cough reflex initiated by mechanical irritation of the trachea. When vadocaine was given via the vertebral artery, it was about 10 times more active than by the intravenous route. Codeine was 3 times as active as vadocaine by both routes. This result indicates an important central component in the antitussive action of vadocaine. In another cat model, 5 mg/kg of vadocaine was somewhat weaker than 1 mg/kg of codeine in inhibiting the cough caused by electrical stimulation of the laryngeal nerve (Domenjoz' method). In dogs, both oral and intravenous doses of 6 mg/kg of vadocaine and 2 mg/kg of codeine were approximately equiactive, inhibiting by 60-80% the cough induced by electrical stimulation of the trachea. Concentrations of vadocaine in serum were around 1 microgram/ml during oral administration. By both routes, the antitussive activity (inhibition of cough by 50% or more) lasted at least 2 h. Vadocaine caused local anaesthesia in the guinea-pig wheal preparation at concentrations of 0.25% and 0.5%, and on the guinea-pig cornea at 0.5%. Duration of anaesthesia was longer than that of lidocaine. Vadocaine did not affect the guinea-pig tracheal strip preparation.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Antitussive action of the new anilide derivative vadocaine hydrochloride compared with codeine phosphate in four animal models. 339 94

Vadocaine hydrochloride (2',4'-dimethyl-6'-methoxy-3-(2-methylpiperidyl)propionanilide+ ++ hydrochloride, OR K-242-HCl; INN: vadocaine) is a new anilide derivative which resembles lidocaine in chemical structure. The safety and antitussive effects of this new compound were studied in 6 healthy male volunteers in the first Phase I clinical trial. Vadocaine was administered in single doses of 5, 10, 15, 20, 30 and 50 mg. At these dose levels vadocaine had no effects on the cardiovascular system, the haematological variables, blood biochemistry or urinary sediment examined as safety evaluation. The antitussive properties of the compound were studied using inhaled citric acid for induction of the cough response. The antitussive properties of vadocaine were most effective at a dose of 15 mg, although no statistical significance was found. Neither was any dose-response relationship noted. However, at this dose level vadocaine is apparently safe and its antitussive properties seem promising enough for further evaluation.
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PMID:First human studies on the safety and antitussive activity of vadocaine hydrochloride. 339 1

Vadocaine hydrochloride (2',4'-dimethyl-6'-methoxy-3-(2-methylpiperidyl)propionanilide+ ++ hydrochloride, OR K-242-HCl; INN: vadocaine) is a novel compound with potent antitussive and local anaesthetic action. The antitussive profile of this compound was evaluated in 40 healthy volunteers in double-blind, placebo-controlled cross-over study design using inhaled citric acid a cough inducer. In Part I, vadocaine was compared in 20 healthy volunteers at two dose levels (10 and 30 mg) with codeine phosphate (50 mg) and a placebo. In part II, vadocaine (30 mg) and a placebo were compared in 20 healthy volunteers. In Part I, no statistically significant differences were found between the 3 compounds tested. However, statistically significant rises from the pre-dose value in the cough threshold stimulus level were observed following 10 and 30 mg doses of vadocaine. Neither codeine phosphate nor the placebo produced any statistically significant change in the cough threshold stimulus level. In Part II, vadocaine at a dose of 30 mg dose was found to be a potent antitussive with a statistically significant difference (p less than 0.0001) as compared with the placebo. The maximum cough threshold stimulus level was achieved 2 h after administration and was 72.6% higher than at pre-dose. With the placebo the cough threshold stimulus level also rose to some extent after 4 h, although the change was not statistically significant. The use of inhaled citric acid in graded concentrations for induction of the cough response was found to be a reliable method when the baseline cough threshold stimulus level is maintained within narrow limits throughout the entire study population.
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PMID:Assessment of the antitussive effect of vadocaine hydrochloride using citric acid-induced cough in healthy volunteers. 339 3

Vadocaine hydrochloride (2',4'-dimethyl-6'-methoxy-3-(2-methylpiperidyl)propionanilide+ ++ hydrochloride, OR K-242-HCl; INN: vadocaine) is an anilide derivative with antitussive and local anaesthetic action. The safety of this new compound was studied in 8 healthy male volunteers in a Phase I clinical trial. Vadocaine was administered orally as a single dose of 50, 100, 200, 300, 400 and 500 mg. At the two highest dose levels used, 400 and 500 mg, vadocaine induced side-effects originating in the central nervous system; ECG analysis revealed small prolongations in the P-Q interval and QRS complex after 400 and 500 mg. At a dose of 500 mg the P-Q interval was prolonged by a maximum of 38% (184 ms at 0.5 h; 134 ms pre-dose). The compound had no effect on blood and urinary parameters measured for safety evaluation. On the basis of these results, a 300 mg dose of vadocaine appears to be safe in man in all respects. This dose level is 10 times the therapeutic dose (30 mg). Vadocaine is sufficiently safe for future clinical trials in patients with cough.
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PMID:Assessment of the safety margin of vadocaine hydrochloride in man. 339 4

Concern about upper respiratory tract irritation and other symptoms among workers at a glass bottle manufacturing plant led to an epidemiologic and an industrial hygiene survey. Questionnaire responses from 35 hot end and 53 cold end workers indicated that the incidence of wheezing, chest pain, dyspnea on exertion, and cough was significantly elevated among hot end workers. Among both smokers and nonsmokers, hot end workers reported higher, but not significantly higher, rates of wheezing and chest pain. Among smokers, hot end workers reported significantly higher rates of dyspnea on exertion and cough than did cold end workers. Data suggest that reported exposure to stannic chloride solution likely caused these symptoms. The industrial hygiene survey, conducted when stannic chloride use had been reduced, cleaning had been done, and ventilation improved, focused on measuring air contaminants that might possibly cause symptoms. Levels of hydrogen chloride, which apparently was formed by the combination of stannic chloride and water in the presence of heat, were elevated. The finding of increased prevalence of respiratory symptoms among hot end workers was consistent with this exposure. Recommendations were made to reduce hazardous exposures at this plant. Individuals responsible for occupational health should be aware that relatively benign substances, such as stannic chloride and water, can combine spontaneously to form hazardous substances.
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PMID:Respiratory symptoms among glass bottle makers exposed to stannic chloride solution and other potentially hazardous substances. 399 80

We evaluated the role of antimicrobials in the treatment of chronic maxillary sinusitis in children with respiratory allergy. Night and day cough, nasal obstruction, rhinorrhea, postnasal seen. Eighty-four children were treated in a double-blind manner with either amoxicillin, erythromycin, trimethoprim-sulfamethoxazole, or an antihistamine decongestant (carbinoxamine maleate-pseudoephedrine HCl). Radiographic and clinical responses were best with amoxicillin, but trimethoprim-sulfamethoxazole was an adequate alternative. This study demonstrates that allergic children with chronic sinusitis with associated chronic respiratory symptoms are likely to respond clinically and radiologically with antimicrobial treatment.
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PMID:Chronic sinusitis in children with respiratory allergy: the role of antimicrobials. 706 74


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