Drugs online research references
Biol Psychiatry. 2001 Jul 1;50(1):13-21.
Is the beneficial antidepressant effect of coadministration of pindolol really due to somatodendritic autoreceptor antagonism?
Cremers TI, Wiersma LJ, Bosker FJ, den Boer JA, Westerink BH, Wikstrom HV.
Department of Medicinal Chemistry, University of Groningen, Groningen, The Netherlands.
BACKGROUND: We investigated the combination of selective serotonin reuptake inhibitors (SSRIs) with the beta-adrenoceptor/serotonin 1A (5-HT(1A)) antagonist pindolol, based on the concept that 5-HT(1A) receptor blockade would eliminate the need for desensitization of presynaptic 5-HT(1A) receptors and therefore hasten the onset of action and improve the efficacy of SSRIs. However, since pindolol plasma levels after 2.5 mg three times a day are about 60 nmol/L, and the K(i) for the 5-HT(1A) receptor is 30 nmol/L, it is questionable whether pindolol levels in the brain would be sufficient to antagonize 5-HT(1A) receptors. Using microdialysis in the guinea pig, we correlated brain and plasma levels of pindolol with its capability of augmenting paroxetine-induced increases in brain 5-HT levels. In addition, central beta-receptor antagonism of pindolol was studied by investigating blockade of beta-agonist-induced increases in brain cyclic adenosine monophosphate (cAMP) formation. METHODS: Using microdialysis and jugular vein catheterization, we studied the ability of systemically administered pindolol to antagonize central 5-HT(1A) and beta-adrenoceptors, while simultaneously monitoring pindolol plasma and brain concentrations. RESULTS: Augmentation of paroxetine-induced increases in extracellular 5-HT levels in the ventral hippocampus was only observed at steady state plasma levels exceeding 7000 nmol/L (concurrent brain levels 600 nmol/L). In contrast, antagonism of beta-agonist-induced increases of brain cAMP levels was already observed at pindolol plasma levels of 70 nmol/L (concurrent brain levels < 3 nmol/L). CONCLUSIONS: At plasma levels that are observed in patients after 2.5 mg three times a day ( approximately 60 nmol/L), pindolol produces only a partial blockade of presynaptic 5-HT(1A) autoreceptors and does not augment the SSRI-induced 5-HT increase in the guinea pig brain. It is therefore very unlikely that the favorable effects of combining pindolol with SSRIs, as reported in a number of clinical studies, are due to 5-HT(1A) antagonism. Since pindolol completely blocks central beta-adrenoreceptors at clinically relevant plasma levels, it is possible that beta-adrenoceptor antagonism is involved in mediating pindolol's beneficial effects.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=11457419&dopt=Abstract
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farmasi.uio.no
BACKGROUND: This article presents an overview of the excretion of the SSRIs citalopram, paroxetine, fluoxetine, fluvoxamine and sertraline in breast milk. MATERIAL AND METHODS: Published articles on selective serotonin reuptake inhibitors and excretion in breast milk were identified and reviewed. In addition, drug concentrations were measured in milk from eight women using paroxetine (n = 4), citalopram (n = 3) or fluvoxamine (n = 1). RESULTS: Data from the literature indicate that the relative dose to the infant is lowest for fluvoxamine and sertraline, somewhat higher for paroxetine and highest for citalopram and fluoxetine. Adverse effects were reported in three of the 119 breastfed infants. Our own results show minimal excretion of fluvoxamine, small excretion of paroxetine and higher excretion of citalopram into breast milk. INTERPRETATION: If treatment with a selective serotonin reuptake inhibitor is started during the postpartum period, fluoxetine should not be the first alternative. High doses of citalopram should also be used with caution. However, when the use of an SSRI is clearly indicated in a breastfeeding woman, available data generally indicate that the positive effects of breast-feeding outweigh the risks for pharmacological effects in the infant.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=11475200&dopt=Abstract
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Br J Psychiatry. 2001 Aug;179:163-6.
Use of sertraline, paroxetine and fluvoxamine by nursing women.
Hendrick V, Fukuchi A, Altshuler L, Widawski M, Wertheimer A, Brunhuber MV.
Department of Psychiatry, UCLA Neuropsychiatric Institute and Hospital, Los Angeles, California 90095, USA.
BACKGROUND: The pharmacological treatment of depression in nursing women requires information on the magnitude of medication exposure to the infant that may occur through breast milk. AIMS: To examine serum concentrations of antidepressants in infants exposed to these medications through breast-feeding. METHOD: Maternal and infant serum concentrations of sertraline, paroxetine and fluvoxamine were determined with high-performance liquid chromatography (limit of detection=1 ng/ml). RESULTS: No detectable medication was present in any infant exposed to paroxetine (n=16) or fluvoxamine (n=4). Among infants exposed to sertraline (n=30), detectable medication was present in 24% of serum samples. A significant negative correlation was found between infant age and infant serum concentration. Sertraline was significantly more likely to be detected in an infant if the mother's daily dose was 100 mg or higher. No adverse sequelae occurred in any infant. CONCLUSIONS: This study shows that paroxetine, fluvoxamine and sertraline produce minimal exposure to infants when taken by nursing mothers.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=11483479&dopt=Abstract
note: kwd match paxil online literature
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