Cough reflex inhibition

Oxolamine [959-14-8] (57) is sold in Europe. It is an oxadiazole, and its general pharmacological profile is described (81). The compound possesses analgesic, antiinflammatory, local anesthetic, and antispasmodic properties, in addition to its antitussive activity. Although a central mechanism may account for some of the activity, peripheral inhibition of the cough reflex may be the dominant effect. The compound has been shown to be clinically effective, although it is less active than codeine (82,83). The synthesis of oxolamine is described (84). 

The cough-suppressant (antitussive) effect produced by inhibition of the cough reflex is independent of the effects on nociception or respiration (antitussives codeine, noscapine). 

Mechanism of Action-. An opioid agonist that binds to opioid receptors at many sites in the CNS, particularly in the medulla. This action inhibits the ascending pain pathways. Therapeutic Effect Alters the perception of and emotional response to pain, suppresses cough reflex. 

They are central cough suppressants and act centrally to raise the threshold of cough centre and inhibit the cough reflex by... 

Stemona japonica (BI.) Miq. S. tubemsa Lour. Bai Bu Dei Ye Bei Bu (root) Stemonine, isotemonidine, stemonidine, protostemonine.33 50 Suppress excitation of the respiratory center and inhibit the cough reflex. Antitubercular, antibacterial, antifugal. 

The effects of morphine, codeine, and heroin in the brain are dose-related. Small doses produce drowsiness, decreased anxiety and inhibition, reduced concentration, muscle relaxation, pain relief, depressed respiration, constricted pupils, nausea, and a decreased cough reflex, which is why codeine found its way into cough suppressants. At slightly higher doses, morphine and heroin can produce a state of intense elation or euphoria. 

Some of the commonly used antitussives are listed in Table 26-1. As shown in the table, codeine and similar opiate derivatives suppress the cough reflex by a central inhibitory effect.21,124 Other nonopioid antitussives work by inhibiting the irritant effects of histamine on the respiratory mucosa or by a local anesthetic action on the respiratory epithelium. The primary adverse effect associated with most antitussives is sedation. Dizziness and gastrointestinal upset may also occur. 

Codeine Many trade names Inhibits cough reflex by direct effect on brainstem cough center... 

Patel HJ, Birrell MA, Crispino N, Hele DJ, Venkatesan P, Barnes PJ, Yacoub MH, Belvisi MG (2003) Inhibition of guinea-pig and human sensory nerve activity and the cough reflex in guinea-pigs by cannabinoid (CB2) receptor activation. Br J Pharmacol 140 261 -268... 

The phytomedicines that inhibit the cough-centre Codeine, glaucine, noscapine and semisynthetic ethyphine. The phytomedicines that inhibit the cough-reflex Mucilaginous herbs such as Althea root and Icelandic moss. 

Hydrocodone bitartrate/homatropine methylbromide is an antitussive combination. Hydrocodone suppresses the cough reflex stimulates opiate receptors iu the CNS and peripherally blocks pain impulse geueratiou. Atropine inhibits action of acetylcholine or other cholinergic stimuli at postgauglionic cholinergic receptors. They are used for symptomatic relief of cough. 

Hydromorphone hydrochloride is an opioid analgesic that relieves pain by stimulating opiate receptors in CNS it also causes respiratory depression, inhibition of cough reflex, peripheral vasodilation, inhibition of intestinal peristalsis, sphincter of Oddi spasm, stimulation of chemoreceptors that cause vomiting, and increased bladder tone. It is indicated for the relief of moderate to severe pain and control of persistent nonproductive cough. 

Cromolyn and nedocrotnil inhibit mediator release from bronchial mast cells reverse the increased functional activation in leukocytes obtained from the blood of asthmatic patients suppress the activating effects of chemotactic peptides on human neutrophils, eosinophils, and monocytes inhibit parasynqtathetic and cough reflexes and inhibit leukocyte trafficking in asthmatic airways. 

It is a potent antitussive agent. It usually acts by inhibiting transmission of impulses of the cough reflex in the vagal nuclei of the medulla and predominantly depresses polysynaptic spinal reflexes. It is regarded as a cough suppressant acting both centrally and peripherally... 

Hanus L, Breuer A, TchUibon S et al, (1999) HU-308 a specific agonist for CB(2), a peripheral cannabinoid receptor, Proc Natl Acad Sci USA 96 14228-14333 Harris J, Drew LJ, Chapman V (2000) Spinal anandamide inhibits nociceptive transmission via cannabinoid receptor activation in vivo. Neuroreport 11 2817-2819 Higenbottam T (2002) Chronic cough and the cough reflex in common lung diseases, Pulm Pharmacol Ther 15(3) 241-247... 

---