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Thread: Abilify (Aripriprazole) works by Partial Agonism on dopmine receptors.

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    Default Abilify (Aripriprazole) works by Partial Agonism on dopmine receptors.

    DA = Dopamine, a full agonist on the dopamine D2 receptor.
    FGA = First Generation Antipsychotic = TYPICAL ANTIPSYCHOTIC, a full antagonist
    APZ = Aripriprazole, a partial agonist



    Abilify is a partial agonist on D2, D3, and D4 receptors. with highest affinity on D2. Abilify's intrinsic activity once bound to the receptor is recorded to be between 30%-60% on postynaptic D2 and up to 75% on presynaptic D2 . where presynaptic neurons receptors are autoreceptors, which shut down the nerve's dopamine release when activated, causes production of dopamine to slow down as well as release of dopamine from firing cells to reduce.

    Abilify blocks dopamine receptors D1 and D5 but with low affinity.

    Abilify is a partial agonist on 5HT1A which causes dopamine release in the prefrontal cortex.

    Abilify is an antagonist on 5HT2A which causes dopamine release to reduce in the prefrontal cortex.
    5HT2A antagonism causes dopamine release in the nigrostriatal pathway.
    Last edited by Petros Agapetos; 11-25-2018 at 07:28 AM.

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    Abilify (Aripriprazole) is used to treat mania, bipolar disorder, manic-depression, psychosis, and schizophrenia.

    Most antipsychotics are dopamine blocking agents, which are "silent antagonist" on those receptors; they exert no intrinsic activity (IA = 0%).But Abilify is a partial agonist, which blocks but partially activates dopamine receptors;
    Its overall effect is to reduce dopaminergic activity in the mesolimbic pathway due to D2 and D3 partial agonism with 75% intrinsic activity on presynaptic neurons.; (which produce and send the chemical messenger); autoreceptor activation causes the nerve to release less dopamine [/I] release from firing cells. On the D2 receptors of postsynaptic neurons, Abilify's intrinsic activity is between 30% and 60% which is equivalent to saying antagonism by 40-70%.
    Last edited by Petros Agapetos; 11-25-2018 at 08:59 PM.

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    Aripriprazole (Abilify) is a partial agonist on D2. Dissociate more easily from receptor than typical antipsychotics; better side effect profile.
    Abilify (Aripriprazole) is a partial agonist on serotonin receptor: 5HT1A; this action causes dopamine to be released in the prefrontal cortex , thereby Abilify might treat negative and cognitive symptoms of psychosis, schizophrenia; reversing neuroleptic-induced deficit syndrome; caused by dopamine antagonists. Abilify is used after dopamine antagonist treatment, in order to treat the depression, anhedonia, and blunting of affect they cause. Abilify has more moderate side effects due to this reason as well.

    Abilify reduces the activity of the mesolimbic (reward) pathway and increases the mesocortical pathway activity (good for treating negative and cognitive symptoms); Abilify is an antagonist on serotonin 5HT2A, which when activates *by an agonist* would increase dopamine release in the prefrontal cortex; thereby preventing dopamine release there.

    As a partial agonist, Abilify, increases dopamine activity where it is low in the brain ; and reduces dopamine activity where it is excessive.
    PARTIAL AGONISM ON D2: Treats Positive Symptoms
    PARTIAL AGONISM ON 5HT1A: Treats Negative and Cognitive Symptoms
    ANTAGONISM ON 5HT2A: Treats positive symptoms; Abilify blocks this receptor, which when activated by dopamine, would increase dopamine release in the prefrontal cortex (involved in executive mental functions, self-consciousness, and judgement, etc.). 5HT2A antagonism causes dopamine release in the nigrostriatal pathway, less motor side effects than with typical antipsychotics or antagonists of the second generation.

    Consider a partial agonist for your treatment of mania, psychosis, schizoaffective disorder, schizophrenia etc.
    Last edited by Petros Agapetos; 11-25-2018 at 07:30 AM.

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    Aripiprazole’s proposed mechanism of action on dopamine receptors is that of partial agonism,

    Rather than antagonism, as is the case for other SGAs. In theory, Aripiprazole antagonizes postsynaptic D2 receptors and activates presynaptic D2 autoreceptors, with subsequently decreased dopamine production and further stabilization of the dopamine system.

    Its antagonism of 5-HT2A is similar to other SGAs (Second Generation Antipsychotic).

    Background
    : The treatment of schizophrenia is challenging due to the wide range of symptoms (positive, negative, cognitive) associated with the disease. Typical antipsychotics that antagonize D2 receptors are effective in treating positive symptoms, but extrapyramidal side-effects (EPS) are a common occurrence.

    Atypical antipsychotics targeting 5-HT2A and D2 receptors are more effective at treating cognitive and negative symptoms compared to typical antipsychotics, but these drugs also result in side-effects such as metabolic syndromes.
    Last edited by Petros Agapetos; 11-25-2018 at 09:04 PM.

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    I couldnt sit for a minute still and slept very bad with abilify

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    Quote Originally Posted by Hadouken View Post
    I couldnt sit for a minute still and slept very bad with abilify
    That condition is called akathisia, all antipsychotics cause it, if you take them long term.
    Akathisia = inability to sit still or remain still; constant pacing, psychomotor restlessness.

    Abilify blocks serotonin 5HT2A which activates dopaminergic neurons in the nigrostriatal pathway.

    Since Abilify is a partial agonist, not an antagonist like most other antipsychotics, it has a milder side effects profile. It does not silently block dopamine receptors; but rather mildly activates them; modulates nerve activity; it makes the firing neurons to release less dopamine, and affect receiving neurons less than dopamine would; but higher than an antagonist. Moreover, constant dopamine blockade (through partial agonism) causes the brain to synthesize 40% or more dopamine receptors in return ; and those extra D2 receptors on the nigrostriatal pathway are associated with movement disorders, extrapyramidal symptoms; etc. This might explain why Abilify causes akathisia.

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    Quote Originally Posted by Petros Agapetos View Post
    That condition is called akathisia, all antipsychotics cause it, if you take them long term.
    Akathisia = inability to sit still or remain still; constant pacing, psychomotor restlessness.

    Abilify blocks serotonin 5HT2A which activates dopaminergic neurons in the nigrostriatal pathway.

    Since Abilify is a partial agonist, not an antagonist like most other antipsychotics, it has a milder side effects profile. It does not silently block dopamine receptors; but rather mildly activates them; modulates nerve activity; it makes the firing neurons to release less dopamine, and affect receiving neurons less than dopamine would; but higher than an antagonist. Moreover, constant dopamine blockade (through partial agonism) causes the brain to synthesize 40% or more dopamine receptors in return ; and those extra D2 receptors on the nigrostriatal pathway are associated with movement disorders, extrapyramidal symptoms; etc. This might explain why Abilify causes akathisia.
    I didnt have it on seroquel and perazine though

    I had it with abilify and a little with amisulpride

    btw. I stopped taking my antipsychotic med 5 days ago and I feel weird as fuck . I have headaches too . I was slightly psychotic too some moments . I hope this will be gone soon

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    Antipsychotics which are dopamine (flat) antagonists cause prolactin levels to increase in the blood. Dopamine tonically inhibits prolactin release. When dopamine activity reduces in the brain; more prolactin is released from the brain. Dopamine counteracts prolactin increases in the tubero-infundibular pathway. which connects the midbrain to the hypothalamus (which releases hormones to the bloodstream).

    However, Abilify is a partial agonist. Low doses of Abilify given can reduce antagonist induced prolactin release.
    Abilify partially activates D2 and D3 receptors, that is why less prolactin is released in the case of Abilify treatment, than say with Risperidone.

    Prolactin terminates orgasms. Prolactin is released into the bloodstream after an orgasm in order to bring about its end.
    Prolactin is a lactation hormone, which can cause breast tissue formation (even in men). This is particularly seen with Antipsychotics such as Haloperidol and Risperidone. Elevated levels of prolactin decrease the levels of sex hormones — estrogen in women and testosterone in men. This is how dopamine blocking agents reduce testosterone levels.

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    Quote Originally Posted by Hadouken View Post
    I didnt have it on seroquel and perazine though

    I had it with abilify and a little with amisulpride

    btw. I stopped taking my antipsychotic med 5 days ago and I feel weird as fuck . I have headaches too . I was slightly psychotic too some moments . I hope this will be gone soon
    Can you describe your psychosis?
    Did it have an affective (mood) component? i.e. were you manic or depressed.
    Did you have 1. Hallucinations 2. Delusions 3 Disorganized thinking and behaviour
    Antipsychotics cause withdrawal effects. Soon you will enter a brain state in which you have more dopamine receptors than you had before antipsychotic treatment. This is called "SUPERSENSITIVITY PSYCHOSIS"
    If this withdrawal is too abrupt for you, consider small doses of Antipsychotics (I recommend a very low dose of Abilify, 2 mg) for 7 days, so that you can land more safely into a normal brain state. I don't want you to go off your meds in such a way that causes relapse of symptoms. Gradual withdrawal is recommended.

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    Quote Originally Posted by Petros Agapetos View Post
    Can you describe your psychosis?
    Did it have an affective (mood) component? i.e. were you manic or depressed.
    Did you have 1. Hallucinations 2. Delusions 3 Disorganized thinking and behaviour
    Antipsychotics cause withdrawal effects. Soon you will enter a brain state in which you have more dopamine receptors than you had before antispsychotic treatment.
    If this withdrawal is too abrupt for you, consider small doses of Antipsychotics (I recommend a very low dose of Abilify, 2 mg) for 7 days, so that you can land more safely into a normal brain state. I don't want you to go off your meds in such a way that causes relapse of symptoms. Gradual withdrawal is recommended.
    I had delusions and disorganized thinking yes . I was also depressed and anxious with it

    I think I stopped the antipsychotic too abruptly but my doc said I can try it :-/ I was taking half a perazine for a month before I stopped and perazine is a mild antipsychotic

    it is 5 days now . today I am somewhat okay so far

    I hope I wont be psychotic again . it is the worst thing in the world along with severe panic attacks

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