Haloperidol depot spc

Aripiprazole's mechanism of action is different from those of the other FDA-approved atypical antipsychotics (., clozapine , olanzapine , quetiapine , ziprasidone , and risperidone ). [45] [49] [50] [51] [52] [53] [54] [55] Rather than acting as a pure antagonist of the dopamine D 2 receptor , aripiprazole shows functional selectivity at the D 2 receptor, acting as a silent antagonist of some subpopulations of D 2 receptors but as a high-efficacy partial agonist ( intrinsic activity = 75%) of other D 2 -receptor subpopulations. [45] It appears to show predominantly antagonist activity on postsynaptic D 2 receptors and partial agonist activity on presynaptic D 2 receptors. [56] Aripiprazole is also a partial agonist of the D 3 receptor . [45] In healthy human volunteers, D 2 and D 3 receptor occupancy levels are high, with average levels ranging between approximately 71% at 2 mg/day to approximately 96% at 40 mg/day. [57] [58] Most atypical antipsychotics bind preferentially to extrastriatal receptors, but aripiprazole appears to be less preferential in this regard, as binding rates are high throughout the brain. [59]

It should not be used concomitantly with medications known to prolong the QTc interval (. 5-HT3 antagonists , tricyclic antidepressants , citalopram , etc.) as this may lead to an increased risk of QTc interval prolongation. [16] [2] Neither should it be given concurrently with lithium (medication) as it may increase the risk of lithium toxicity and neuroleptic malignant syndrome . [4] [5] [16] It should not be given concurrently with other antipsychotics due to the potential for this to increase the risk of side effects, especially neurological side effects such as neuroleptic malignant syndrome . [4] [5] [16] It should be avoided in patients on CNS depressants such as opioids, alcohol and barbiturates. [16]

In clinical trials with oral olanzapine, clinically meaningful QTc prolongations (Fridericia QT correction [QTcF] ≥ 500 milliseconds [msec] at any time post-baseline in patients with baseline QTcF<500 msec) were uncommon (% to 1%) in patients treated with olanzapine, with no significant differences in associated cardiac events compared to placebo. In clinical trials with olanzapine powder for solution for injection or ZYPADHERA, olanzapine was not associated with a persistent increase in absolute QT or in QTc intervals. However, caution should be exercised when olanzapine is prescribed with medicines known to increase QTc interval, especially in the elderly, in patients with congenital long QT syndrome, congestive heart failure, heart hypertrophy, hypokalaemia or hypomagnesaemia.

The influence of renal impairment on the pharmacokinetics of haloperidol has not been evaluated. About one-third of a haloperidol dose is excreted in urine, mostly as metabolites. Less than 3% of administered haloperidol is eliminated unchanged in the urine. Haloperidol metabolites are not considered to make a significant contribution to its activity, although for the reduced metabolite of haloperidol, back-conversion to haloperidol cannot be fully ruled out. Even though impairment of renal function is not expected to affect haloperidol elimination to a clinically relevant extent, caution is advised in patients with renal impairment, and especially those with severe impairment, due to the long half-life of haloperidol and its reduced metabolite, and the possibility of accumulation (see section ).

Haloperidol depot spc

haloperidol depot spc

The influence of renal impairment on the pharmacokinetics of haloperidol has not been evaluated. About one-third of a haloperidol dose is excreted in urine, mostly as metabolites. Less than 3% of administered haloperidol is eliminated unchanged in the urine. Haloperidol metabolites are not considered to make a significant contribution to its activity, although for the reduced metabolite of haloperidol, back-conversion to haloperidol cannot be fully ruled out. Even though impairment of renal function is not expected to affect haloperidol elimination to a clinically relevant extent, caution is advised in patients with renal impairment, and especially those with severe impairment, due to the long half-life of haloperidol and its reduced metabolite, and the possibility of accumulation (see section ).

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