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citalopram escitalopram Lexapro [The transfer of selective serotonin reuptake inhibitors to human milk]
[Article in Norwegian]
Nordeng H, Bergsholm YK, Bohler E, Spigset O.
Institutt for farmakoterapi Postboks 1065 Blindern 0316 Oslo. h.m.e.nordeng 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 source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=11475200&dopt=Abstract citalopram escitalopram Lexapro
citalopram escitalopram Lexapro Serotonin reuptake inhibitors fluoxetine and citalopram relax intestinal smooth muscle.
Pacher P, Ungvari Z, Kecskemeti V, Friedmann T, Furst S.
Institute of Pharmacology and Pharmacotherapy, Semmelweis University, Budapest, Hungary. ppacher hotmail.com
Selective serotonin reuptake inhibitor antidepressants (SSRIs) exert depressant effects on cardiac myocytes and vascular smooth muscle cells by inhibiting Ca2+ channels. We hypothesized that the SSRIs fluoxetine and citalopram affect the contractile activity of intestinal smooth muscle by interfering with Ca2+ entry and (or) signaling pathways. The effects of fluoxetine and citalopram on contractions of guinea-pig ileum longitudinal muscle-myenteric plexus preparations (LMMP) were compared with the effects of the voltage-operated Ca2+ channel inhibitors nifedipine and diltiazem. In a concentration-dependent manner, nifedipine, diltiazem, fluoxetine, and citalopram elicited relaxation of LMMPs contracted by electrical field stimulation (EC50 values of 4 x 10(-7) M, 1.4 x 10(-6) M, 1.4 x 10(-5), and 6.8 x 10(-6) M, respectively). Nifedipine, diltiazem, fluoxetine, and citalopram also relaxed LMMPs contracted with a depolarizing concentration of KCl (48 mM; EC50 values of 1.8 x 10(-8) M, 1.4 x 10(-7) M, 3.7 x 10(-6) M, and 6.3 x 10(-6), respectively), a response that could be reversed by increasing the extracellular Ca2+ concentration (2.5-30 mM). These data suggest that fluoxetine and citalopram elicit relaxation of intestinal smooth muscle, likely by inhibiting Ca2+ channel(s). This effect may be of clinical importance.
Online source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=11478591&dopt=Abstract citalopram escitalopram Lexapro
citalopram escitalopram Lexapro Methylphenidate augmentation of citalopram in elderly depressed patients.
Lavretsky H, Kumar A.
Department of Psychiatry and Biobehavioral Sciences, UCLA School of Medicine, Los Angeles, CA, USA.
The authors followed 10 elderly depressed patients (mean age=79.8 years; in an open trial of methylphenidate (MPH) augmentation of citalopram used to accelerate and enhance their antidepressant response. Eight of the 10 patients demonstrated clinically significant improvement by Week 8. Four of the seven patients with augmentation initiated during the first week of treatment with citalopram met the criteria for rapid response at Week 2. No patient discontinued treatment. These preliminary observations suggest that a combination of MPH and citalopram may be an effective, relatively well tolerated treatment in this patient population and may accelerate onset of action. However, patients may require dosage adjustment for tolerability of this combination.
Online source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=11481139&dopt=Abstract citalopram escitalopram Lexapro
citalopram escitalopram Lexapro Acute and chronic effects of citalopram on cerebral glucose metabolism in geriatric depression.
Smith GS, Kramer E, Hermann CR, Goldberg S, Ma Y, Dhawan V, Barnes A, Chaly T, Belakhleff A, Laghrissi-Thode F, Greenwald B, Eidelberg D, Pollock BG.
Department of Psychiatry Research, Hillside Hospital and the Neuroscience Institute of the North Shore-Long Island Jewish Health System, Glen Oaks, NY 11004, USA. gsmith lij.edu
OBJECTIVE: In vivo studies of serotonin function have been limited by the lack of safe and selective pharmacologic agents and availability of suitable radiotracers. In the present study, the authors evaluated the cerebral metabolic effects of acute and continued administration of the selective serotonin reuptake inhibitor citalopram in patients with geriatric depression as a potential marker of serotonin dysfunction. METHODS: Six patients with geriatric depression and five comparison subjects underwent two resting positron emission tomography (PET) studies, performed after administration of a placebo infusion (Day 1) and a citalopram infusion (40 mg, Day 2). The patients were re-scanned after 8 weeks of treatment with the oral medication. RESULTS: The elderly comparison subjects demonstrated greater right-hemisphere cortical decreases than the patients. The depressed patients demonstrated greater left-hemisphere cortical decreases than comparison subjects. The depressed patients demonstrated greater increases in the right putamen and left occipital cortex. After 8 weeks of citalopram treatment, regional decreases and increases in metabolism were observed. CONCLUSION: These findings suggest regional deficits and also compensatory responses in the acute metabolic response to citalopram in the patients. These preliminary results suggest that the cerebral metabolic response to citalopram may be a useful marker of the pathophysiology of serotonin function in geriatric depression.
Online source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=12427580&dopt=Abstract citalopram escitalopram Lexapro
citalopram escitalopram Lexapro Citalopram for social phobia: a clinical case series.
Simon NM, Sharma SG, Worthington JJ, Marzol PC, Pollack MH.
Anxiety Disorders Program, Massachusetts General Hospital, Boston 02114, USA. nsimon partners.org
Social anxiety disorder is a common illness with significant associated disability. Serotonin selective reuptake inhibitors (SSRIs) have become first-line treatment given their improved tolerability; however, there are few reports on the use of citalopram. Nine consecutive patients with a primary diagnosis of DSM-IV generalized social phobia were prospectively treated with citalopram. Citalopram was generally well-tolerated, and seven patients achieved responder status. This series of patients improved significantly on all measures. Results suggest that citalopram may be a safe and effective treatment for social anxiety disorder.
Online source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=11513360&dopt=Abstract citalopram escitalopram Lexapro
citalopram escitalopram Lexapro Second-generation SSRIs: human monoamine transporter binding profile of escitalopram and R-fluoxetine.
Owens MJ, Knight DL, Nemeroff CB.
Laboratory of Neuropsychopharmacology, Department of Psychiatry and Behavioral Sciences, Emory University School of Medicine, 1639 Pierce Drive, Atlanta, GA 30322, USA.
BACKGROUND: Single isomers of the selective serotonin reuptake inhibitors citalopram (escitalopram, S-citalopram) and fluoxetine (R-fluoxetine) are currently under development for the treatment of depression and other psychiatric disorders. Previous studies conducted in laboratory animals have revealed that the biological effects on serotonin reuptake for citalopram reside in the S enantiomer. In contrast, both enantiomers of fluoxetine contribute to its biological activity. METHODS: In the present study, the potency and selectivity of escitalopram, R-fluoxetine, and all of the other currently available selective serotonin reuptake inhibitors were compared for binding affinity at the human serotonin, norepinephrine, and dopamine transporters and several select neurotransmitter receptors using radioligand binding assays. RESULTS: Both escitalopram and R-fluoxetine were potent inhibitors of the serotonin transporter (K(i) = 1.1 and 1.4 nmol/L, respectively). Escitalopram was the most serotonin transporter-selective compound tested and was approximately 30-fold more potent than R-citalopram. CONCLUSIONS: As noted previously, paroxetine and sertraline possess moderate affinity (<50 nmol/L) for the human norepinephrine transporter and dopamine transporter, respectively. R-Fluoxetine, unlike the other selective serotonin reuptake inhibitors, possesses moderate affinity (K(i) = 64 nmol/L) for the serotonin 2C receptor. Potential clinical correlates of these unique attributes of escitalopram and R-fluoxetine are discussed.
Online source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=11543737&dopt=Abstract citalopram escitalopram Lexapro
citalopram escitalopram Lexapro Action of selective serotonin reuptake inhibitor on aggressive behavior in adult rat submitted to the neonatal malnutrition.
Medeiros JM, Silva CM, Sougey EB, Costa JA, Castro CM, Castro RM.
Departamento de Nutricao, Universidade Federal de Pernambuco, Recife, PE, Brasil.
The effect of the malnutrition during suckling on the aggressiveness was investigated in adult rats treated or not with citalopram, a selective serotonin reuptake inhibitor (SSRI). The animals were divided into two groups according to the diet used: nourished group - the rats received the control diet with 23% protein during the life; and malnourished group - the rats had its mothers submitted to diet with 7.8% protein during suckling. At 120 days of age, each group was sub-divided according to the treatment: acute - consisting a single i.p. injection of saline solution or 20-mg/Kg citalopram; chronic - consisting the single injections (1 per day during 14 days) of saline or 20 mg/Kg citalopram. The acute or chronic treatment with SSRI reduces aggressive response in nourished rats, but not in malnourished ones. Thus, the malnutrition during the critical period of brain development seems to induce durable alterations in the function of the serotoninergic neurotransmission
Online source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=11588625&dopt=Abstract citalopram escitalopram Lexapro
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