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Methylphenidate: Difference between revisions
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==Pharmacology== | ==Pharmacology== | ||
Methylphenidate primarily acts as a [[ | Methylphenidate primarily acts as a [[norepinephrine]]-[[dopamine]] [[reuptake inhibitor]] (NDRI). It is most active at modulating levels of dopamine and, to a lesser extent, norepinephrine.<ref>Methylphenidate and its Isomers | http://link.springer.com/article/10.2165%2F00023210-200620090-00002</ref> Methylphenidate binds to and blocks dopamine transporters and norepinephrine transporters.<ref>Neurotransmitter transporters and their impact on the development of psychopharmacology (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pmc/articles/PMC1760736/</ref> | ||
While both [[amphetamine]] and methylphenidate are dopaminergic, it should be noted that their methods of action are somewhat distinct. Specifically, methylphenidate is a dopamine reuptake inhibitor while amphetamine is both a releasing agent and reuptake inhibitor of [[dopamine]] and [[norepinephrine]]. Each of these drugs have a corresponding effect on norepinephrine which are weaker than their effects on dopamine. Methylphenidate's mechanism of action at dopamine-norepinephrine release is still debated, but is fundamentally different from most other phenethylamine derivatives as methylphenidate is thought to increase general firing rate, whereas amphetamine reduces firing rate and reverses the flow of the monoamines via TAAR1 activation.<ref>Dopamine transporter occupancies in the human brain induced by therapeutic doses of oral methylphenidate. (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/9766762</ref><ref>Neurotransmitter transporters and their impact on the development of psychopharmacology (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pmc/articles/PMC1760736/</ref><ref>Focalin XR review | http://www.pharma.us.novartis.com/product/pi/pdf/focalinXR.pdf</ref><ref>Concerta Xl slow release | http://www.medicines.org.uk/emc/medicine/8382/SPC/Concerta#PHARMACOLOGICAL_PROPSSPC</ref> | While both [[amphetamine]] and methylphenidate are dopaminergic, it should be noted that their methods of action are somewhat distinct. Specifically, methylphenidate is a dopamine reuptake inhibitor while amphetamine is both a releasing agent and reuptake inhibitor of [[dopamine]] and [[norepinephrine]]. Each of these drugs have a corresponding effect on norepinephrine which are weaker than their effects on dopamine. Methylphenidate's mechanism of action at dopamine-norepinephrine release is still debated, but is fundamentally different from most other phenethylamine derivatives as methylphenidate is thought to increase general firing rate, whereas amphetamine reduces firing rate and reverses the flow of the monoamines via TAAR1 activation.<ref>Dopamine transporter occupancies in the human brain induced by therapeutic doses of oral methylphenidate. (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/9766762</ref><ref>Neurotransmitter transporters and their impact on the development of psychopharmacology (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pmc/articles/PMC1760736/</ref><ref>Focalin XR review | http://www.pharma.us.novartis.com/product/pi/pdf/focalinXR.pdf</ref><ref>Concerta Xl slow release | http://www.medicines.org.uk/emc/medicine/8382/SPC/Concerta#PHARMACOLOGICAL_PROPSSPC</ref> | ||