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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 ).

☞ Instruct patient to immediately report signs or symptoms of serious adverse reactions, such as unusual weakness, yellowing of skin or eyes, difficulty breathing, or symptoms of neuroleptic malignant syndrome (such as fever, muscle pain or rigidity, rapid or irregular pulse, increased sweating, change in urination pattern, or decreased mental acuity).
• Advise patient to minimize GI upset by eating frequent, small servings of food and drinking adequate fluids.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, herbs, and behaviors mentioned above.

Haloperidol is a typical butyrophenone type antipsychotic that exhibits high affinity dopamine D 2 receptor antagonism and slow receptor dissociation kinetics. [41] It has effects similar to the phenothiazines . [17] The drug binds preferentially to D 2 and α 1 receptors at low dose (ED 50 = and  mg/kg, respectively), and 5-HT 2 receptors at a higher dose (ED 50 =  mg/kg). Given that antagonism of D 2 receptors is more beneficial on the positive symptoms of schizophrenia and antagonism of 5-HT 2 receptors on the negative symptoms, this characteristic underlies haloperidol's greater effect on delusions, hallucinations and other manifestations of psychosis. [42] Haloperidol's negligible affinity for histamine H 1 receptors and muscarinic M 1 acetylcholine receptors yields an antipsychotic with a lower incidence of sedation, weight gain, and orthostatic hypotension though having higher rates of treatment emergent extrapyramidal symptoms .

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