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Deconamine Pharmacology, Pharmacokinetics, Studies, Metabolism - Guaifenesin; Hydrocodone; Pseudoephedrine
CLINICAL PHARMACOLOGY
Hydrocodone is a semisynthetic narcotic analgesic and antitussive with multiple actions qualitatively similar to those of codeine. Most of these involve the central nervous system and smooth muscle. Hydrocodone suppresses the cough reflex by depressing the medullary cough center. The precise mechanism of action of hydrocodone and other opiates is not known, although it is believed to relate to the existence of opiate receptors in the central nervous system.
Hydrocodone:
Onset of action: Narcotic analgesic: 10-20 minutes
Duration: 4-8 hours
Distribution: Crosses placenta
Metabolism: Hepatic; O-demethylation;N-demethylation and 6-ketosteroid reduction
Half-life elimation: 3.3-4.4 hours
Excretion: Urine
Pseudoephedrine hydrochloride is an orally effective nasal decongestant that acts on alpha-adrenergic receptors in the mucosa of the respiratory tract producing vasoconstriction. Pseudoephedrine shrinks swollen nasal mucous membranes, reduces tissue hyperemia, edema and nasal congestion and increases nasal airway patency. Drainage of sinus secretions is increased and obstructed Eustachian ostia may be opened. Pseudoephedrine produces little if any rebound congestion.
Pseudoephedrine:
Onset of action: Decongestant: Oral: 15-30 minutes
Duration: Immediate release tablet: 4-6 hours
Extended release: < or equal to 12 hours
Absorption: rapid
Metabolism: Partially hepatic
Half-life elimination: 9-16 hours
Excretion: Urine (70% to 90% as unchanged drug, 1% to 6 % as active norpseudoephedrine)
Guaifenesin is an expectorant which enhances the flow of respiratory tract secretions. The enhanced flow of less viscid secretions lubricates irritated respiratory tract membranes, promotes cilliary action and facilitates the removal of inspissated mucus. As a result, sinus and bronchial drainage is improved and nonproductive coughs become more productive and less frequent.
Guaifenesin:
Absorption: well absorbed
Half-life elimination: ~ 1 hour
Excretion: urine (as unchanged drug and metabolites)
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