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Fixed-drug eruptions on the glans was described as burning, itching, and sharply marginated, erythematous, vesicular plaques and well-demarcated erosions on the shaft in 2 adult males, occurring within 6 to 8 hours after taking melatonin for jet lag. Lesions dissipated within 10 days.
In humans: orally, as capsules, tablets, or liquid, sublingually, or as transdermal patches. In lab animals: also injection.
Mechanism of Action
The binding of melatonin to melatonin receptors activates a few signaling pathways.[5]
MT1 receptor activation inhibits the adenylyl cyclase and its inhibition causes a rippling effect of non activation; starting with decreasing formation of cyclic adenosine monophosphate (cAMP), and then progressing to less protein kinase A (PKA) activity, which in turn hinders the phosphorylation of cAMP responsive element-binding protein (CREB binding protein) into P-CREB.[4] MT1 receptors also activate phospholipase C (PLC), affect ion channels and regulate ion flux inside the cell.[5][6][7]The binding of melatonin to MT2 receptors inhibits adenylyl cyclase which decreases the formation of cAMP.[7]
As well it hinders guanylyl cyclase and therefore the forming of cyclic guanosine monophosphate (cGMP). Binding to MT2 receptors probably affects PLC which increases protein kinase C (PKC) activity. Activation of the receptor can lead to ion flux inside the cell.[7]
When melatonin receptor agonists activate their receptors it causes numerous physiological processes.[7][8]
MT1 and MT2 receptors may be a target for the treatment of circadian and non circadian sleep disorders because of their differences in pharmacology and function within the SCN. The SCN is responsible for maintaining the 24 hour cycle which regulates many different body functions ranging from sleep to immune functions.[9]
Melatonin receptors have been identified in the cardiovascular system. Evidence from animal studies points to a dual role of melatonin in the vasculature.
Activation of MT1 receptors mediates vasoconstriction and the activation of MT2 receptors mediates vasodilation. Melatonin is involved in regulating immune responses in both human and animals through activation of both MT1 and MT2 receptors.
MT1 and MT2 receptors are widespread in the eye and are involved in regulating aqueous humor secretion, which is important for glaucoma, and in phototransduction. This is not a complete list since many of the possible processes need further confirmation
Structure
There is limited information regarding Melatonin Structure in the drug label.
Pharmacodynamics
There is limited information regarding Pharmacodynamics of Melatonin in the drug label.
Pharmacokinetics
There is limited information regarding Pharmacokinetics of Melatonin in the drug label.
Nonclinical Toxicology
There is limited information regarding Nonclinical Toxicology of Melatonin in the drug label.
Clinical Studies
There is limited information regarding Clinical Studies of Melatonin in the drug label.
How Supplied
There is limited information regarding Melatonin How Supplied in the drug label.
Storage
There is limited information regarding Melatonin Storage in the drug label.
Images
Drug Images
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