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Truthometer

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  1. Welbutrin (Bupropion) is a dopamine-norepinephrine reuptake inhibitor; its occupancy at dopamine transporter (DAT) is 23%; whereas over 75% causes euphoria (ex. cocaine). A dopamine reuptake inhibitor (DRI) is a class of drug which acts as a reuptake inhibitor of the monoamine neurotransmitter dopamine by blocking the action of the dopamine transporter (DAT). Reuptake inhibition is achieved when extracellular dopamine not absorbed by the postsynaptic neuron is blocked from re-entering the presynaptic neuron. This results in increased extracellular concentrations of dopamine and increase in dopaminergic neurotransmission. I am currently taking Abilify 400 mg every 3 weeks (~ 20 mg / day) and 300 mg of Welbutrin. I was complaining to my psychiatrist about the side effects of Abilify I was suffering from; depression (low mood), sexual dysfunction, anhedonia, from a condition called "Neuroleptic Induced Deficit Syndrome" . I complained that I had totally lost my motivation, drive, and initiative and was experiencing anhedonia (lack of pleasure), emotional suppression, etc. It is like living in a mental restraint "straigthjacket". So my psychiatrist added Welbutrin. Abilify dampens down dopaminergic activity in three of the four dopaminergic pathways; It is the only Antipsychotic that I know of that can increase mesocortical dopaminergic activity. Other partial agonists like Brexiprazole and Cariprazine might do this also, whereas a silent antagonist cannot. Welbutrin has treated my low mood; I am euthymic now, but I am still anhedonic from Abilify being so frequent for such a dose; I am taking the daily equivalent of 20 mg: 400 mg per 3 weeks. At lower doses Abilify has a more stimulating effect. The Welbutrin he added certainly helps; but is unfortunately not enough. I am considering adding a dopamine full agonist such as Ropinirole, Rotigotine, Cabergoline and Pramipexole to my prescription meds. Some dopamine agonists are useful at treating depression resistant to SSRI-treatment. Dopamine agonists can be given to counteract the side effects of antipsychotics and serotonergic antidepressants. No doubt that dopamine antagonism has a negative effect on mood. In the mesolimbic pathway *(reward pathway)* Aripriprazole reduces dopaminergic activity; which reduces motivation - salience (liking, rewarding), which can be identified as a major source of anhedonia. Aripriprazole does not reduce dopamine transmission in the mesocortical pathway in people whose mesocortical pathway has .less than normal activity. The dopamine boost that Welbutrin provides keeps me stable; counterbalances some of the negative effects of Abilify. I just need more help in alleviating this zombified state of existence in which I am alienated from my own real self. and cannot enjoy the things I used to enjoy; food, drugs, sex. I live in anhedonia, a state of a loss of pleasure; due to the neurological inhibition caused by Abilify. Welbutrin works as a wakefullness promoting agent, a mild stimulant.
  2. Aripriprazole: Intrinsic activity = 60% on post-synaptic D2 ; up to 75% on pre- synaptic D2 receptors.[1] Brexiprazole: Intrinsic activity = Up to 46% [2] Cariprazine: Intrinsic activity = Up to 71% [3] Aripriprazole is a partial agonist with functionally antagonist activity on receiving neurons and functionally agonist activity on firing neurons; both of which dampen down dopaminergic neurotransmission. Aripriprazole can increase dopaminergic activity in the mesocortical pathway, unlike dopamine blockers, Aripriprazole partially agonizes D2, D3, 5HT1A and to a lesser extent D4 receptors; antagonist at 5HT2A, as other atytpical antipsychotics.[1] Brexpiprazole has more blocking and less stimulating activity at the dopamine receptors than its predecessor, aripiprazole, which may decrease its risk for agitation and restlessness. Specifically, where Aripiprazole has an intrinsic activity or agonist effect at the D 2 receptor of 60%+, Brexpiprazole has an intrinsic activity at the same receptor of about 45%. [2] Cariprazine is a dopamine D2- and D3-receptor partial agonist, with higher affinity for D3 receptors, as opposed to the D2antagonism of most older antipsychotic agents.Cariprazine has lower intrinsic activity at D 2 receptors than aripiprazole. Its intrinsic activity is up to 71% [3 ]
  3. The Pharmacological Profile of Ability D1 (Antagonist) but insignificant D2 (Partial Agonist), 60% - 75% D3 (Partial Agonist) D4 (Partial Agonist) D5 (Antagonist) but insignificant 5HT1A (Partial Agonist), 68%, which causes dopamine release in the prefrontal cortex. 5HT2A (Antagonist), as all atypical antipsychotics. Has purported antipsychotic and antimanic properties.
  4. Abilify (Aripriprazole) is a partial agonist on dopamine receptors with 60% the activity of dopamine on receiving neurons and 75% activity of dopamine on firing neurons [1]. Abilify is the only antipsychotic which can increase dopaminergic activity in the mesocortical pathway through dopamine partial agonism. Abilify is a 5HT1A partial agonist (68%), which causes dopamine levels to go up in the prefrontal cortex. Abilify is also a 5HT2A antagonist; which has antipsychotic and antimanic properties [2]. Here are the Four Dopaminergic Pathways and Abilify's Effect on them 1. Mesolimbic (Abilify decreases activity) 2. Mesocortical (Abilify increases activity) 3. Nigrostriatal (Abilify dampens down) 4. Tuberoinfundibular (Abilify does not cause prolactin release unlike dopamine antagonist antipsychotics. In fact, even low doses of Abilify can reduce prolactin release caused by dopamine blockers). Abilify reduces neurotransmission in three of the four dopaminergic neuronal pathways.
  5. Aripriprazole is a dopamine D2 partial agonist (30%) on posynaptic receptors and partial agonist (75%) on presynaptic receptors . At low doses it has an stimulating effect. At high doses it has a sedative effect. Aripriprazole is a 5HT1A partial agonist (68%) also; which leads to dopamine release in the prefrontal cortex. Due to partial agonism on D2, D3, D4, Aripriprazole modulates dopamine levels in the mesocortical pathway; by increasing activity where it is absent or low; and reducing activity where it is high. Aripriprazole is also a 5HT2A antagonist as are atypical antipsychotics; this has antipsychotic and anti-manic effects. Look out for dopamine supersensitivity; The long term use of antipsychotics causes extra dopamine receptors to be produced by the brain; this is called upregulation. The brain's dopamine receptors upregulate under the blockade of the antipsychotic agent. Antipsychotics cover 70% - 90% of dopamine receptors. The brain, in an effort to maintain homeostatic equilibrium produces more dopamine receptors on receiving neurons in order to sensitize the neurons to dopamine called "dopamine supersensitivity" which is associated with a risk of relapse. Antipsychotics have withdrawal effects; So taper off the antipsychotic; do not abruptly withdraw the drug.
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