Saturday, July 3, 2021

Therapy in Parkinson's Disease. What is "End of Dose" phenomenon?

 

End of Dose Phenomenon

Parkinson’s disease is a progressive neuro-degenerative disease where the dopaminergic neurons in the substantia niagra and the nigro-striatal pathway degenerate gradually and irreversibly over a period of time.

Under normal physiology, dopamine is stored in vesicles in the pre-synaptic vesicle and released in the synaptic cleft upon arrival of an action potential. This event is highly “regulated” and exocytosis of neurotransmitter is “demand” based, occurring as and when required for the smooth execution of muscle action.

In early stages of Parkinson’s disease, exogenously administered dopamine as replacement therapy tend to get stored in the pre-synaptic vesicle and is released on “demand”, thus mimicking the normal physiology. The physiology of storage, release and re-uptake is still intact and dopamine replacement provides immense symptomatic relief to the patient.

As the diseases progresses, the number of dopaminergic neurons decreases due to degeneration. The capacity of the dopaminergic pathway to store the neurotransmitter and release on “demand” is impaired. Relief of symptoms becomes short lasting. Increase in amount and frequency of dose provide only limited benefit. Patient is alternately “well” and “not well”.  This is known as the “on-off” effect or “switch” phenomenon or “end of dose” phenomenon or the “all or none” response. In the terminal phase, when the majority of the neurons are destroyed, abnormal movements (dyskinesia) occurs with administration of dopamine and as soon as the effect of dopamine wanes, severe hypokinesia and rigidity returns.

No comments:

Post a Comment

Lidocaine and phenytoin- both are sodium channel blockers. Lidocaine is a local anaesthetic and an anti-arrhythmic. Phenytoin is an anticonvulsant. What explains their differential action? Is it because of their difference in pharmacokinetics.

 Drugs, more than often, have multiple actions. The ability of drugs to interact with different targets and sometimes same target in differe...