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BMS60046

Drugs acting at the NMDA receptor

QuestionAnswer
NMDA endogenous agonsits glutamate, aspartate, glycine (co-agonist)
NMDA endogenous antagonists Zn and Mg
Mg SE when increased, decreases excitabiilty; lowers HR, BP tendon reflex, muscle force, CNS
NMDA exogenous antagonists ketamine; memantine
ketamine analgesic; doesn't repress respiratory activity; non-competitive; has sympathomimetic anaesthesia, parasympathomimetic anaesthesia, and psychotomimetic anaesthesia; is a mix of isomers
what other receptors does ketamine work at? GABA agonist, blocks Na channel, Ca channel, M receptor, nicotinic receptor, sigma receptor; kappa agonist; NOS inhibitor; receptor inhibitor for NE, dopamine, 5HT
what are the sympathomimetic effects of ketamine? bronchodilation; increased RR, HR, BP, oxygen consumption; not good for CAD pts; good as asthmatic last resort
what are the parasympathomimetic effects of ketamine? bronchorrhea; sialorrhea
what would you use to alleviate the parasympathomimetic effects of ketamine? atropine (muscarinic antagonist) b/c it will dry everything up.
what are ketamine's psychotomimetic effects? vivid dreams; use a GABA agonist
esketamine pure S (+) ketamine (good guy)
memantine prevention of dementia/improvement of mental performance in elderly (memory); more rapid removal of Mg (unblocking of NMDA); doesn't affect inhibition of AChesterase
Methadone mu- and NMDA-antagonist (double analgesia); slow onset, variable t1/2; metabolite has long t1/2; accumulation/sedation; 4-12 Mo
where are opiod receptors located? mainly CNS (spinal and supraspinal)
mu-opiod receptors open K channels --> hyperpolarization; supraspinal
kappa opiod receptors inhibit Ca channels --> reduce transmitter release; spinal
delta opiod receptors modulate mu-receptor acitivity
what are the endogenous opiod peptides? enkephaline (delata); endorphine (mu); dynorphine (kappa)
what are the NMDA anti-epileptic drugs? Lamotrigine, Felbamate, Topiramate
Lamotrigine glutamate-release inhibitor; Na channel blocker
Felbamate Glycine (NMDA)- Antagonist; GABA-Agonist
topiramate AMPA-Antagonist; GABA-Agonist; dopamine release inhibitor; makes you lose weight (unlike other anti-seizure meds); SE: impaired memory, inhibits carbonic anhydrase, increases occular pressure (myopia and glaucoma)
Created by: cbart004
Popular Pharmacology sets

 

 



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