Pharma Cardinal 1.2 Flashcards
It acts on the presynaptic and postyneptic side of the pain synapse
It modulates it by reducing the sensation of pain
Pre synaptically it reduces the conduction of calcium thus reducing activation
Post synaptically it activatesK+ conductance reducing excitability and keeping the cell hyperpolarized
What is codeine
It is a prodrug for morphine
Itself it doesn’t do anything so it needs to be transformed into morphine
What is hydromorphone
To complete agonist and it is twice as powerful as morphine
What is methadone and why is it so important
It is a complete agonist but it is important because it has a very long half life
What is the difference between a dependency and tolerance
Dependency is a addiction that occurs when a substance becomes necessary to maintain a healthy equilibrium
The level of dependency can be measured by the sober syndrome symptoms that is how bad does the patient feel if he doesn’t take the drugs
Tolerance on the other hand is the progressive loss of sensibility to the medication which requires an increase in the dose of the medication to attain the same effect
physique et/ou psychique
Describe receptor desensibalization
The over stimulation in a continuous way of GPCR receptors can lead to
* decoupling of the receptor from the signaling path
* internalization of a receptor or
* even degradation and ** downregulation of their production**
Describe at a high level how tolerance occurs in neural circuits
The continuous activation of modulation pathways the opioid stimulation elites to an increase in activity of modulatory pathways
And so the descending pathways become tolerant that is they reduce their inhibition on the pain synapse
what is the advantage of methadone over the mix of buprénorphine-naloxone as substitution drugs for addicts
Methadone has a higher program retention rate
It is less recommended for people that have a high risk of leaving the treatment
Those are usually patients that inject opioids intravenously
What is a factor that will push you to putting a patient on suboxone treatment
buprénorphine-naloxone Has shown to be preferable for opioid users that have stable lives and professional and family obligations
buprénorphine-naloxone Or methadone which has the lowest risk of overdose
buprénorphine-naloxone
Because it is the partial agonist
The majority of receptors that are targeted by medication are of what type
They are membrane-bound receptors mainly gpcrs
Why do people that for those on opioids have respiratory arrests
Because of the new opioid receptors in the respiratory area in the brain stem that has G I Mu opioid receptors
alpha adrénergiques vs β-adrénergique vs mu-opioïde difference
alpha adrénergiques: bound to Gq -> phospholipase C
β-adrénergique: Gs stimulates adenylate cyclase
mu-opioïde: Gi inhibits adenylate cyclase
What does an alpha adrenergic receptor lead to muscle contraction
It is bound to AGQ molecule which activates phospholipase C which activates ip three which leads to a release of calcium in the cell through a pore in the endoplasmic reticulum
The calcium in the cell leads to contraction of muscles
True or false
β adrénergique Receptor activation leads to muscle contraction
False
stimulates PKA and thus leads to relaxation of muscle
récepteurs α1 -> vasoconstriction
récepteurs b2 -> vasodilatation
