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)

In a randomized double-blind study, 107 patients with extrinisic, intrinsic or mixed bronchial asthma and impaired lung function received either picumast dihydrochloride (3,4-dimethyl-7-[4-(4-chlorobenzyl)piperazine-1-yl]propoxycoumarin dihydrochloride) 1 mg or placebo twice daily for 6 weeks after a 2-week placebo phase. Patients given picumast dihydrochloride demonstrated significant improvements compared with baseline in morning and evening peak flow and asthmatic symptoms like morning tightness, cough, dyspnoea, obstruction, number of asthma attacks during night and day, sum of asthmatic symptom scores, in vital capacity and Tiffeneau index, and a significant reduction of inhaled adjuvant medications. In contrast, placebo recipients improved significantly only in daytime asthma attacks, obstruction, sum of symptom scores, and Tiffeneau index. The differences between the picumast dihydrochloride and placebo groups significantly favoured picumast dihydrochloride for improvements in mean number of daytime asthma attacks, morning tightness, aerosol use and sum of symptom scores. Adverse reactions were minor and infrequent; no tiredness occurred with picumast dihydrochloride. Tolerability of both picumast dihydrochloride and placebo was rated as "good" to "very good" by patients and physicians.
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PMID:Efficacy and tolerability of picumast dihydrochloride in comparison with placebo in asthmatic patients. 257 65

The antitussive effect of the new compound 1, 2, 3, 4a, 9b-hexahydro-8, 9b-dimethyl-4-[3-(4-methyl-piperazine-1-yl) propionamide] dibenzofuran-3-one dihydrochloride (RU-20201) was investigated in dogs and guinea pigs, including its sites of action. The antitussive effect of RU-20201 was about 1/10 as potent as that of codeine phosphate in dogs with the puncture electrode-induced cough (PEC) method and about 1/12 and 1/4 as potent as that of codeine phosphate in guinea pigs with the PEC and chemical stimulation methods, respectively. When RU-20201 was administered in a dose range of 1 to 10 mg into the vertebral artery toward the brain in lightly anesthetized dogs, no antitussive effect was observed against the coughing elicited by electrical stimulation of the central cut end of the superior laryngeal nerve. However, a stimulative effect on respiration, especially on respiratory rate occurred. The peripheral effect of RU-20201 on the cough was investigated using the in situ upper trachea perfusion preparation which allows a direct drug administration to the local site around the tracheal mucosa, this site being electrically stimulated to induce coughing. A close i.a. infusion of RU-20201 in doses of 1 and 3 mg/min into the tracheal vascular bed for 5 min inhibited the cough response elicited by mucosal stimulation. The above findings suggest that RU-20201 has a significant antitussive activity, the site of action being probably, at least, at the cough receptor level.
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PMID:Antitussive effect of RU-20201--central and peripheral actions. 672 71

Oxatomide (CAS 60607-34-3), a diphenylmethyl-piperazine benzimidazole derivative is a new oral antiallergic drug useful in asthma in preventing allergic attacks. Using the model of citric acid-induced coughing in the unanesthetized, unrestrained guinea pig the antitussive effect of oxatomide was investigated. The animals were treated with logarithmically increasing doses of oxatomide (0.5, 1, 2 mg/kg, suspended in 0.5 ml of polyethylene glycol 200 + 0.5 ml of saline) and with the vehicle alone administered intraperitoneally (1 ml) 45 min before the challenge. Oxatomide reduced the number of coughs during the 3 min of challenge, lengthened the time of onset and reduced the number of coughs after cessation of the challenge significantly and a linear dose-effect regression was observed.
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PMID:Antitussive effect of oxatomide on citric acid-induced cough in conscious guinea pig. Preliminary communication. 810 Oct 81

Studies are described on the metabolism and the toxicologic analysis of the nonopioid cough suppressant dropropizine [R,S-3-(4-phenyl-1-piperazinyl)1,2-propandiol, DRO] in human urine using gas chromatography-mass spectrometry (GC-MS). The metabolism studies showed that DRO was metabolized in humans mainly by hydroxylation of the aromatic ring, by N-dealkylation of the parent drug and of the hydroxyl-metabolite to the corresponding N-phenylpiperazines, and by degradation of the piperazine moiety. The authors' systematic toxicologic analysis (STA) procedure using full-scan GC-MS after acid hydrolysis, liquid-liquid extraction, and microwave-assisted acetylation allowed the unambiguous detection of DRO and its above-mentioned metabolites in human urine up to about 32 hours after intake of a single common therapeutic dose. The target analytes were found to be the parent compound DRO (earlier phase of excretion) and the hydroxylated metabolite para-hydroxy-DRO (later phase of excretion). Both allowed unambiguous detection of an intake of DRO and also differentiation from other phenylpiperazine derivatives.
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PMID:Studies on the human metabolism and the toxicologic detection of the cough suppressant dropropizine in urine using gas chromatography-mass spectrometry. 1525 75

Transient receptor potential vanilloid 1 (TRPV1) plays an integral role in modulating the cough reflex, and it is an attractive antitussive drug target. The purpose of this study was to characterize a TRPV1 antagonist, 4-(3-trifluoromethyl-pyridin-2-yl)-piperazine-1-carboxylic acid (5-trifluoromethyl-pyridin-2-yl)-amide (JNJ17203212), against the guinea pig TRPV1 receptor in vitro followed by a proof-of-principle study in an acid-induced model of cough. The affinity of JNJ17203212 for the recombinant guinea pig TRPV1 receptor was estimated by radioligand binding, and it was functionally characterized by antagonism of low-pH and capsaicin-induced activation of the ion channel (fluorometric imaging plate reader and electrophysiology). The nature of antagonism was further tested against the native channel in isolated guinea pig tracheal rings. Following pharmacokinetic characterization of JNJ17203212 in guinea pigs, pharmacodynamic and efficacy studies were undertaken to establish the antitussive efficacy of the TRPV1 antagonist. The pK(i) of JNJ17203212 for recombinant guinea pig TRPV1 was 7.14 +/- 0.06. JNJ17203212 inhibited both pH (pIC(50) of 7.23 +/- 0.05) and capsaicin (pIC(50) of 6.32 +/- 0.06)-induced channel activation. In whole-cell patch clamp, the pIC(50) for inhibition of guinea pig TRPV1 was 7.3 +/- 0.01. JNJ17203212 demonstrated surmountable antagonism in isolated trachea, with a pK(B) value of 6.2 +/- 0.1. Intraperitoneal administration of 20 mg/kg JNJ17203212 achieved a maximal plasma exposure of 8.0 +/- 0.4 microM, and it attenuated capsaicin evoked coughs with similar efficacy to codeine (25 mg/kg). Last, JNJ17203212 dose-dependently produced antitussive efficacy in citric acid-induced experimental cough in guinea pigs. Our data provide preclinical support for developing TRPV1 antagonists for the treatment of cough.
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PMID:Pharmacology and antitussive efficacy of 4-(3-trifluoromethyl-pyridin-2-yl)-piperazine-1-carboxylic acid (5-trifluoromethyl-pyridin-2-yl)-amide (JNJ17203212), a transient receptor potential vanilloid 1 antagonist in guinea pigs. 1769 Feb 51

To evaluate the safety and efficacy of Linkus, Aminophylline with Diphenhydramine group and Acefyllin Piperazine with Diphenhydramine cough syrup on children having cough and sleep difficulty associated with cough. To determine the effects of Linkus polyherbal syrup (group A) and compared with other parallel allopathic groups (Group B and C) for cough on children and associated sleep quality and improvement. 360 children having cough inducted in 3 different groups randomly selected. Three parallel groups were the part of the study. The first study group was the herbal syrup Linkus, second group of children were taking a syrup of multinational pharmaceutical industry having Aminophylline plus Diphenhydramine however the third group received another famous brand having Acefyllin Piperazine with Diphenhydramine. Informed assent and informed consent have taken from the study subjects and their parents. Subjects with acute cough were included in the study however the subjects with chronic cough considered to be excluded. Every group of individual in the study was informed about the investigational drugs provided. Ethnic groups, frequency of cough and diseases illness (<0.05) were determine on every group on the investigational syrup. Cough impact on child and its sleep of three different syrups (every group) were assessed on day1 and day 14(p<0.001) via a likert scale. For the evaluation of pain assessment Wong baker face scale were used and level of significance in each group (p<0.001). Significant results were observed in the Linkus Group as compared to the other parallel groups including Aminophylline plus Diphenhydramine and Acefyllin Piperazine with Diphenhydramine on day 14 (p<0.001). Side effects on group B and group C (Aminophylline with Diphenhydramine and Acefyllin Piperazine with Diphenhydramine) were almost similar in number however Linkus syrup has minimum side effects on study duration. Polyherbal syrup Linkus shows better results in treatment of cough including side effects as compare to the other parallel groups B and C (Aminophylline with Diphenhydramine and Acefyllin Piperazine with Diphenhydramine). For nocturnal sleep Linkus providing better results in cough and associated problems. Pain were significantly reduce on day 14 with the herbal Linkus syrup group A (<0.001). Group B and C found less effective with more side effects as compared to Linkus syrup. Poly herbal Linkus syrup could substantially improve the clinical effect and relieves coughs and benefit lung functions and better sleep facilitation.
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PMID:Efficacy and safety of Linkus, Aminophylline diphenhydramine and acefyllin piperazine for the treatment of cough in children. 2738 95

The aim of the study is to determine the efficacy of polyherbal linkus with the other pharmaceutical marketed syrup having Acefyllin Piperazine, Diphenhydramine group and Aminophylline Diphenhydramine group on the basis of interquartile ranges on children. It was open label multi centric randomize control trial. The study was conducted on different private schools of East and West Malir, Karachi Pakistan with the special approval from the school's honors .informed consent and assents were taking before the enrollment of the study subjects .The study enrolled participants were 147 who evaluate on cough. Participants were divided into 3 interventional group according to the treatment regimen .One group of participant received Linkus Syrup however the 2nd group received Acefyllin Piperazine and 3rd group received Aminophylline Diphenhydramine group. The frequency of the cough on linkus syrup was considered to be achieved on the basis of interquartile relationship and impact has been observed on child and parent sleep and found significant (p <0.01).Poly herbal Linkus Syrup has the significant impact on cough frequency and associated problem on children and parent's sleep with minimum side effects (p<0.01) however the pharmacological treatments are considered to be more unwanted effects on human subjects.
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PMID:An interquartile relationship between polyherbal extract based lozenges linkus a phase IV comparative randomised control trial. 2865 92

Cetirizine, a piperazine-derivative second-generation antihistaminic, is used for a wide variety of disorders such as urticaria, eczema, and allergies. Adverse reactions due to this drug are usually rare, especially fixed drug eruption (FDE), a delayed cell-mediated hypersensitivity reaction, is scarce. Here, we report a case of cetirizine-induced FDE. A 34-year-old female developed hyperpigmented, itchy patches over both forearms, legs, feet, and right side of the chest after taking tablet cetirizine for dry cough with similar episode 2 years back on the same sites. The patient responded slowly with conservative treatment and the lesions disappeared after 10 days. She was advised to avoid the causative in near future. This case report highlighted FDE due to an antihistaminic which themselves will be prescribed to treat allergies.
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PMID:Cetirizine-Induced Fixed Drug Eruption. 3005 Sep 65