Autonomic nervous system 3 Flashcards
What are the catecholamines?
Dopamine, Adrenaline, Noradrenaline
What determines what kind of catecholamine receptor there will be?
The enzymes present, because they are all derived form the same pathway
What is the rate limiting step in the synthesis of the catecholamines?
- Tyrosine to DOPA
* Tyrosine hydroxylase
What are the enzymes present in the catecholamine pathway?
- Tyrosine hydroxylase
- DOPA decarboxylase
- Dopamine beta-hydroxylase (DBH) (membrane bound)
- PNMT
Where is PMNT located?
Mainly in the adrenal medulla
What induces PMNT?
Adrenal cortex hormones
What can inhibit tyrosine hydroxylase?
Catecholamines
Which catecholamine pathway enzyme is targeted in treating the hypertension in pregnancy?
DOPA decarboxylase
Targets the production of noradrenaline
What is methydopa?
Inhibits DOPA decarboxylase- treatment of Parkinson’s
What is noradrenaline release facilitated by?
Calcium ions
What receptors are present of the presynaptic terminal?
α2 adrenoreceptors
What is the role of α2 adrenoreceptors
- Binding of noradrenaline signals that there is enough noradrenaline
- Decreases the Ca 2+ influx
- Therefore decreases noradrenaline release
What happens to noradrenaline in the synaptic cleft?
- ~75% recaptured by neurones
- Norepinephrine transporter (back into the neurone) (NET)
- Repackaged by vesicular monoamine transporter
What is noradrenaline uptake and degradation affected by?
- Sympathomimetic drugs
- Monoamine oxidase inhibitors
- Uptake inhibitors
How do monoamine oxidase inhibitors work?
Dopinergic transmission stops the internal degradation of dopamine/noradrenaline so there is more to release - important in the treatment of mental disorders
How do uptake inhibitors work?
Prevents the uptake, prolonging the duration of effect at the junction
How do amphetamines act as a drug of abuse?
- Hijacks the transport system and displaces the noradrenaline
- NET transporter in reverse: takes amphetamine up and forces noradrenaline out meaning it is released (also from vesicles and amphetamine causes vesicles to be released)
Which drugs affect catecholamine synthesis?
Methyldopa
Which drugs affect catecholamine release?
- Drugs that act on the α2 adrenoreceptors e.g. clonidine
* Drugs that are indirectly acting sympathomimetics e.g. amphetamines
Which drugs are inhibitors of catecholamine uptake?
• NET inhibitors e.g. cocaine, tricyclic antidepressants
Which drugs inhibit catecholamine metabolic degradation?
Monoamine oxidase inhibitors used in depression
What class of receptors are adrenergic receptors?
Metabotropic receptors
What are the two main groups of adrenoreceptors?
α(1 and 2)
β (1,2 and 3)
β3
Adipocytes very little drugs target it