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Pharma 12

Pharma 12

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Published by hamza jassar

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Published by: hamza jassar on Oct 28, 2008
Copyright:Attribution Non-commercial


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We talked in the previous lecture that Acetylcholine is hydrolyzed byacetylcholine esterase and that contaminate the action of acetyl choline.Catecholamine is terminated by uptake into the nerve terminal andstorage. This occurs in two steps:1- from synapse to the axoplasm2- from axplasm into the synaptic vesicleNote: Certain drugs affect these processes and are important intherapeutics.
From synapse to the axoplasm: 
We have 2 classes of drugs acting on this transport mechanism: Cocaineand Tricyclic antidepressant.* Cocaine (a drug of abuse) inhibits this reuptake mechanism. Cocaineincreases the levels of catecholamine at the synapse-Catecholamines –In general- in CNS can be stimulated. Cocaine is astimulating agent –so causing addiction-.*Also Tricyclic antidepressant drugs increase the level of catecholaminein synapse by inhibiting the uptake mechanism.
From axoplasm into the synaptic vesicle 
:It is inhibited by 2 classes of antihypertensive agents: Reserpine andBretylium guanithidine.*Reserpine is a drug used to treat hypertension and acts by inhibitingreuptake or transform into the synaptic vesicle.-When you prevent the storage in the synaptic vesicle
it goes underdepletion (the amount of catecholamines in the synaptic vesicle is small)so if nerve stimulation occurs, the amount of catecholamines leaving thevesicle is small
so we will have normal blood pressure.-Note: Blood pressure depends on: catecholamine, cardiac output andperipheral vascular system.* Bretylium guanithidine: these agents inhibit the release ofcatecholamines. So it participates in reducing blood pressure.*Catecholamine scheme is more complicated and controlled thanAcetylcholine one.In acetylcholine scheme, there are factors can be used to inhibit certainprocesses but they are not important therapeutically. But they areimportant therapeutically in catecholamine.* What will happen if catecholamines diffused from the vesicle to theaxoplasm and catecholamines can't return back to the synapse?Catecholamines will be metabolized by mitochondrial enzymes.-However if catecholamines are secreted to the blood, they will go withthe blood flow to the liver and then metabolized there.
Catecholamine synthesis: 
Dopa: Dihydroxyphenyl alanine.
Types of catecholamine: Dopamine, Norepinephrine andEpinephrine.
Dopamine doesn't contain a hydroxyl group on C (take a look at thefigure).
Norepinephrine contains a hydroxyl group on C. This hydroxyl group(which is found in norepinephrine but not in dopamine) makes manydifferences between norepinephrine and dopamine: differentreceptors, actions and locations.
If we methylate the amine group in norepinephrine (nor methyl) wewill have epinephrine. This methyl group makes the Epinephrinemore selective to the
-receptors than norepinephrine. (More bulk
more selective for
(in the same figure)-
A monoamine compoundderived from theamino acid tyrosineby L- amino acid decarboxylase.-
It is taken up by the same transport mechanisms forcatecholamines and get stored in the vesicles.-
It displaces catecholamine.-
At the beginning, tyramine released into the vesicles in largenumbers causing hypertensive crises (due to the large amount).-
Synthesized in the body but in small amounts. Found also in: cheese(especially stored cheese) and wine. If the person eats too much

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