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)

The antitussive effect of two different drugs A (Codeine, Phenyltoloxamine) and B (Dihydrocodeine, Remedacen) was compared in a double blind clinical trial by measuring the frequency and strength of cough attacks for 7 hours. The cough attacks were measured by a pressure-monitoring device which was externally fastened to the throat. Drug B suppressed the strenght and frequency for at least 9 hours after application while the effectiveness of drug A lasted only for about 6 hours after application. In any case the respiratory drive was unaffected.
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PMID:[Comparison of the antitussive effect of two different drugs regarding frequency and strength of cough attacks (author's transl)]. 92 5

Codeine is often used as a standard antitussive against which new antitussives are compared. However there is little information available about the effects of codeine on cough associated with upper respiratory tract infection. The present study investigated the effects of codeine syrup B.P. (30 mg/10 ml, q.d.s.) or syrup vehicle on cough frequency and the subjective severity of cough during a 3-h laboratory phase and a 4-day home phase of treatment. Cough frequency and subjective scores of cough severity were significantly decreased during the 3-h laboratory phase but at no time point was there a significant difference between the codeine- and placebo-treated groups. The results of the 4-day home phase diary were similar to those of the laboratory phase as at no time point was there a significant difference between the mean scores for the codeine- and placebo-treated groups. The results indicate that codeine, either as a single 30-mg dose or in a total daily dose of 120 mg, is no more effective than the syrup vehicle in controlling cough associated with acute upper respiratory tract infection.
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PMID:Lack of effect of codeine in the treatment of cough associated with acute upper respiratory tract infection. 163 79

Experiments were performed to determine whether cough could be elicited in paralyzed cats ventilated on a respiratory cycle-triggered pump. Midcollicular decerebrate cats were paralyzed and artificially ventilated on a phrenic-triggered pump. Phrenic and cranial iliohypogastric nerve efferent activities were recorded. Cough was elicited by electrical stimulation of the superior laryngeal nerve (SLN) or probing the intrathoracic trachea. Fictive coughs induced by electrical stimulation of the SLN or mechanical stimulation of the intrathoracic trachea consisted of large-amplitude bursts in phrenic discharge immediately followed by large bursts in cranial iliohypogastric discharge. During fictive cough, phrenic postinspiratory discharge was reduced relative to control cycles. Codeine (0.03-1 mg/kg iv) decreased both SLN- and probe-induced fictive cough. I conclude that fictive cough can be produced in paralyzed cats ventilated on a phrenic-triggered pump. Furthermore, fictive cough can be produced in the absence of afferent feedback associated with active expiration.
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PMID:Fictive cough in the cat. 177 30

The effect that codeine has on the process of addiction and recovery is unclear. Confusion about definitions, study endpoints, and a lack of well-controlled clinical studies has led to this uncertainty. Codeine addiction is uncommon in people who do not have existing vulnerability to addiction, including alcoholism. Codeine use can sustain addiction or increase the risk of relapse in patients afflicted with addiction. The risk of relapse must be considered when treating conditions such as pain or cough in a person recovering from addiction. Codeine use may be circumvented with the appropriate use of alternative treatments for pain or cough. If codeine use becomes necessary, cautious prescribing and reliance on the patient's recovery support network become imperative.
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PMID:Safe use of codeine in the recovering alcoholic or addict. 200 86

The influence of replacing the phenolic hydroxyl by the methoxy group on opioid receptor binding, analgesic and antitussive action was investigated in the corresponding couples morphine-codeine, hydromorphone-hydrocodone and O-desmethyltramadol (L 235)-tramadol. Binding was studied on rat whole brain membranes (without cerebellum) with the radioligands dihydromorphine (mu-site), ethylketocyclazocine (k-site), D-Ala2-D-Leu5-enkephalin (delta-site) and naloxone (no selective binding). Analgesia (tail flick) and antitussive action (NH3-vapour induced cough) was investigated in rats and ED50 values 10 min after i.v. application were calculated to compare efficacy. All free hydroxyl compounds had higher opioid receptor affinities than the corresponding methoxy derivatives and were more active at the mu-site. The methoxy derivatives codeine and tramadol only had low affinities lacking selectivity towards mu-, kappa-, or delta-binding. Hydrocodone in contrast showed strong and mu-selective binding. The hydroxy compounds had higher analgesic activity than the methoxy congeners and analgesia appeared to correlate with mu-binding affinity. Codeine and hydrocodone were weaker antitussives than the corresponding hydroxy compounds, whereas no significant difference was found between O-desmethyltramadol and tramadol. Only in the tramadol group the methoxy substitution increased antitussive potency in relation to analgesic potency.
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PMID:Receptor binding, analgesic and antitussive potency of tramadol and other selected opioids. 284 50

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

In order to understand the relationship between the cough and respiratory centers in the brain stem, we investigated the effects of antitussive drugs such as codeine, dextromethorphan, eptazocine and fominoben on respiratory movement and the cough reflex. Coughs were induced using electrical stimulation of the central cut end of the right superior laryngeal nerve in lightly anesthetized dogs. The drugs were administered intraarterially into the vertebral artery. Rate (RR), amplitude (RA) and volume (RV) of the respiration and number (NC) and amplitude (AC) of the cough reflex evoked were measured as indices. Codeine produced a decrease in RR, RV and NC at 0.3 mg and, additionally, AC at 1 mg. Dextromethorphan increased RR and RV and rather enhanced NC and AC at 0.3 mg, but the agent reduced NC and AC at 3 mg even if it increased RR and RV. Eptazocine produced decreases in RA, NC and AC at 1 mg, and, additionally, RV at 10 mg. Fominoben increased RR, RA and RV dose-dependently at 0.3-3 mg, although it depressed NC and AC at 3 mg. These findings suggest that the thresholds for the cough responses and respiratory responses to antitussive drugs are different from drug to drug and that the respiratory centers and cough center in the brain stem are affected in a different manner even qualitatively.
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PMID:[Difference in the effects of antitussive drugs on respiration and cough reflex]. 622 55

Opiates are known for their stereospecificity. The following studies show that l-codeine was active in the mouse tail-flick test as well as in the hot plate test whether given p.o. or s.c. The ED50 in the first test was 4.09 mg/kg s.c. (2.01-8.34 mg/ kg) and 13.41 mg/kg p.o. (6.91-26.0 mg/kg). In the second antinociceptive test, the ED50 was 20.66 mg/kg s.c. (11.52-37.08 mg/kg) and 20.47 mg/kg p.o. (14.63-28.57 mg/kg). The d-isomer of codeine was inactive ina both tests up to 100 mg/kg but caused hyperexcitability, convulsions and ultimately death. Although l-codeine was more potent than d-codeine inhibiting the cough reflex in the anesthetized cat, the d-compound did have good activity. The ED50 of the l-isomer was 0.27 mg/kgi.v. (0.14-0.47 mg/kg) and that of the d-isomer was 1.61 mg/kg i.v. (0.98-2.65 mg/kg). In these animals, l-codeine did not significantly affect the cardiovascular parameters at the doses tested, whereas d-codeine caused a significant but transient decrease in the blood pressure and heart rate. The specific and nonspecific properties of d- and l-codeine were further delineated in the opiate receptor binding assay. l-Codeine inhibited the stereospecific binding of 2.2 x 10(-9) M [3H]dihydromorphine in mouse brain homogenate with the IC50 being 1.6 x 10(-5) M (1.2 x 10(-5)--2.0 x 10(-5) M). d-Codeine had no effect up to 10(-4) M.
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PMID:Comparative studies of the pharmacological effects of the d- and l-isomers of codeine. 625 35

The cough threshold to citric acid inhalation was measured in eight subjects by single inhalations of increasing concentrations of citric acid until a cough was consistently produced. The cough threshold was measured before and after 60 mg glaucine, 60 mg codeine and matched placebo on three separate days a week apart. Base-line cough threshold in each subject was consistent from week to week. Codeine increased the threshold by more than one citric acid concentration in three subjects. Placebo and glaucine did not produce a threshold change of more than one citric acid concentration. We conclude that the citric acid threshold is a simple measure of antitussive activity. No such activity was found with glaucine.
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PMID:Assessment of antitussive effects by citric acid threshold. 634 1

Antitussive and respiratory effects of three newly synthesized methanobenzazonine derivatives and their d- and l-isomers were investigated to understand the relationship between the cough and respiratory centers. Antitussive effects were evaluated with the PEC (puncture electrode-induced cough) method in conscious d-, dl-, and l-ST-2123; d-, dl-, and l-ST-2121 into the right carotid artery at a dose range of 0.2-0.8 mg caused no effect on respiration. dl-ST-2121 at 0.4 to 0.8 mg and l-ST-2121 at 0.2 to 0.8 mg depressed respiration dose-dependently. Codeine (0.2-0.8 mg) depressed respiration slightly. Morphine (0.2-0.8 mg) depressed respiration more strongly. All the methanobenzazonine derivatives used, when given intraperitoneally, showed antitussive potencies that were 1/3-1/2 the potency of codeine. The antitussive potencies of the d-, dl-, and l-isomers of the three derivatives used were discussed on the bases of chemical structures and drug receptors. These results provide evidence of a discrepancy between the cough and respiratory centers in the brain stem.
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PMID:[Effects of methanobenzazonine (2,3,4,5,6,7-hexahydro-1,6-methano-1H-4-benzazonine) derivatives on the cough reflex and respiration]. 717 33


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