Asenapine Pharmacokinetics in Hepatic and Renal Impairment

Peeters, Pierre; Bockbrader, Howard N.; Spaans, Edwin; Dogterom, Peter; Lasseter, Kenneth C.; Marbury, Thomas; Gibson, Gordon L.; Greef, Rik de

doi:10.2165/11590490-000000000-00000

Cited by 31 publications

(18 citation statements)

References 18 publications

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“…[22,25] Mild or moderate hepatic impairment did not affect asenapine exposure, or that of its metabolites; however, compared with healthy controls, severe hepatic impairment increased asenapine exposure 7-fold. [26] Compared with healthy controls, mild renal impairment increased asenapine exposure by »30%; however, moderate and severe renal impairment increased asenapine exposure by only 3% and 6%, respectively. [26] Asenapine dosage adjustment is not necessary in patients with renal impairment, or in patients with mild or moderate hepatic impairment.…”

Section: Pharmacokinetic Profilementioning

confidence: 90%

“…[26] Compared with healthy controls, mild renal impairment increased asenapine exposure by »30%; however, moderate and severe renal impairment increased asenapine exposure by only 3% and 6%, respectively. [26] Asenapine dosage adjustment is not necessary in patients with renal impairment, or in patients with mild or moderate hepatic impairment. [26] 3.…”

Section: Pharmacokinetic Profilementioning

confidence: 90%

“…Data on the pharmacokinetic properties of asenapine are available from several studies in healthy volunteers, [22][23][24][25] or patients with hepatic or renal impairment; [26] all of which are published as abstracts.…”

Section: Pharmacokinetic Profilementioning

confidence: 99%

“…[26] Asenapine dosage adjustment is not necessary in patients with renal impairment, or in patients with mild or moderate hepatic impairment. [26] 3. Therapeutic Efficacy…”

Section: Pharmacokinetic Profilementioning

confidence: 99%

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Asenapine

Weber

McCormack

2009

CNS Drugs

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Asenapine is a novel psychopharmacological agent that binds with high affinity and specificity to numerous dopamine, serotonin, noradrenaline (norepinephrine) and histamine receptor subtypes. It is being developed for the treatment of schizophrenia and bipolar mania. In two randomized, controlled trials of asenapine monotherapy and in one randomized, controlled trial of adjunctive asenapine therapy in adult patients with bipolar I disorder, sublingual asenapine produced significantly greater reductions from baseline than placebo in clinician-assessed Young Mania Rating Scale (YMRS) total score at 3 weeks. In two randomized, controlled trials in adult patients with acute schizophrenia, treatment with asenapine reduced from baseline the clinician-assessed Positive and Negative Syndrome Scale (PANSS) total score to a significantly greater extent than placebo at 6 weeks. In schizophrenic patients with predominant, persistent, negative symptoms, asenapine at 26 weeks reduced the Negative Symptom Assessment (NSA-16) total score from baseline to an extent similar to that observed with olanzapine. Sublingual asenapine was generally well tolerated in clinical trials, with most treatment-emergent adverse events being of mild to moderate severity. Incidence rates of clinically significant weight gain, extrapyramidal symptoms, hyperprolactinaemia and alterations in glucose or lipid metabolism were generally low.

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Section: Pharmacokinetic Profilementioning

confidence: 90%

Section: Pharmacokinetic Profilementioning

confidence: 90%

Section: Pharmacokinetic Profilementioning

confidence: 99%

“…[26] Asenapine dosage adjustment is not necessary in patients with renal impairment, or in patients with mild or moderate hepatic impairment. [26] 3. Therapeutic Efficacy…”

Section: Pharmacokinetic Profilementioning

confidence: 99%

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Asenapine

Weber

McCormack

2009

CNS Drugs

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“…In short-term trials of adult bipolar patients, asenapine increased mean ALT 8.9 units/l, and 2.5% of patients had elevated levels greater than three times the upper limit of normal. 12 Increased serum transaminase levels can be seen in up to 2% of patients taking paliperidone. 13 Currently it is not known whether patients with GH are predisposed to drug-induced liver injury or at risk for altered hepatic synthetic or metabolic function.…”

mentioning

confidence: 99%

Drug-Induced Liver Injury in the Setting of Glycogenic Hepatopathy

2017

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Pregnancy and Breastfeeding

2021

The Maudsley Prescribing Guidelines in Psychiatry

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Lifestyle factors have an important influence on pregnancy outcome. It is well established that smoking cigarettes, eating a poor diet and drinking alcohol during pregnancy can have adverse consequences for the foetus. The manufacturers of cariprazine have advised against its use in pregnancy because of an increased risk of malformations noted in animal studies. Women who take antidepressants during pregnancy may be at increased risk of developing hypertension, preeclampsia and postpartum haemorrhage. Lithium exposure during pregnancy has been associated with an increased risk of congenital anomalies. Anxiety disorders and insomnia are commonly seen in pregnancy. The long‐term benefits of breastfeeding on child physical health and cognitive development are well known. Discussions about the safety of drugs in breastfeeding should be held as early as possible ideally before conception or early in pregnancy. It is usually advisable to continue the antidepressant prescribed during pregnancy.

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Asenapine Pharmacokinetics in Hepatic and Renal Impairment

Cited by 31 publications

References 18 publications

Asenapine

Asenapine

Drug-Induced Liver Injury in the Setting of Glycogenic Hepatopathy

Pregnancy and Breastfeeding

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