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DO YOU KNOW?-3

DO YOU KNOW?-3
CREATININE CHEMISTRY

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Wednesday, 13 July 2016

CNS-PART-IV-DEPRESSION AND MANIA-Contd...

DEPRESSION -TREATMENTS

Here we deal with the detailed treatment options for depression.

Tricyclic Antidepressants:-

1.Tertiary Amines:-

a)Amitriptyline
b)Imipramine
c)Doxepin
d)Clomipramine
e)Trimipramine

Secondary Amines:-

a)Amoxapine
b)Maprotiline
c)Protriptyline
d)Desipramine
c)Nortriptyline
Among the above-listed drugs the secondary amines have a wider therapeutic index and safer than tertiary amines as they are effective with less sedation, hypotension, and anticholinergic effects. But they are more likely to cause schizophrenia and psychoses.

Mechanisms:-

The mechanism of actions of all tricyclics is by blocking the reuptake of norepinephrine and serotonin at the CNS synapses and thereby increase there availability and neuronal effects.
They also block histamine, cholinergic, and alpha-adrenergic receptors. The later effects of blockades account and contribute to their side effects.
Tricyclics have additional therapeutic benefits by causing the downregulation of monoamine receptors.
These drugs are not to be used as mood elevators in normal individuals as they are not CNS stimulants like caffeine.

Therapeutics:-

1.Depression
2.Panic disorders
3.Anxiety
4.Post-traumatic tension and stress.
5.Obsessive and Compulsive Disorders (Clomipramine)
6.Pain Disorders
7.Enuresis in children (Imipramine)

Route:-

Oral route.
Readily enter into the blood-brain barrier.

Kinetics

First, pass metabolism in the liver and excreted in urine as glucuronates.

Side Effects:-

1.Anticholinergic effects such as constipation,drymouth,blurred vision,confusion,and urinary retension.
2.Orthostatic hypotension.
3.Arrhythmias, and ECG changes such as the widening of the QRS angle.
4.Weight gain
5.Histamine blockade results in sedation.
6.Seizures.

 



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