Tyramine exerts hypolipidemic and anti-obesity effects in vivo

Abstract Obesity and dyslipidemia are conditions often associated with cardiovascular risk, inflammation, oxidative stress, and death. Thus, a new approach has been highlighted to promote research and development of pharmacological tools derived from natural sources. Among the most widely studied groups of substances, polyphenols such as tyramine stand out. This study investigated hypolipidemic and anti-obesity properties of tyramine. Oral toxicity evaluation, models of dyslipidemia and obesity were used. To induce dyslipidemia, Poloxamer-407 (P-407) was administered intraperitoneally. In the hypercholesterolemic and obesity model, specific diet and oral tyramine were provided. After 24h of P-407 administration, tyramine 2 mg/kg (T2) decreased triglycerides (TG) (2057.0 ± 158.5 mg/dL vs. 2838 ± 168.3 mg/dL). After 48h, TG were decreased by T2 (453.0 ± 35.47 vs. 760.2 ± 41.86 mg/dL) and 4 mg/kg (T4) (605.8 ± 26.61 760.2 ± 41.86 mg/dL). T2 reduced total cholesterol (TC) after 24h (309.0 ± 11.17 mg/dL vs. 399.7 ± 15.7 mg/dL); After 48h, 1 mg/kg (T1) (220.5 ± 12.78 mg/dL), T2 (205.8 ± 7.1 mg/dL) and T4 (216.8 ± 12.79 mg/dL), compared to P-407 (275.5 ± 12.1 mg/dL). The treatment decreased thiobarbituric acid reactive substances and nitrite in liver, increased superoxide dismutase, reduced the diet-induced dyslipidemia, decreasing TC around 15%. Tyramine reduced body mass, glucose, and TC after hypercaloric feed. Treatment with 5 mg/L (0.46 ± 0.04 ng/dL) and 10 mg/L (0.44 ± 0.02 ng/dL) reduced plasma insulin (1.18 ± 0.23 ng/dL). Tyramine increased adiponectin at 5 mg/L (1.02 ± 0.02 vs. 0.83 ± 0.02 ng/mL) and 10mg/L (0.96 ± 0.04 ng/mL). In conclusion, tyramine has low toxicity in rodents, has antioxidant effect, reduces plasma triglycerides and cholesterol levels. However, further studies should be conducted in rodents and non-rodents to better understand the pharmacodynamic and pharmacokinetic properties of tyramine

Phenylpropanoid amides from whole plants of Corydalis edulis / 中国中药杂志

Ten phenylpropanoid amides were isolated from the whole plants of Corydalis edulis Maxim. by various of column chromatographies including silica gel, Sephadex LH-20, and ODS. Their structures were identified on the basis of physicochemical properties, MS, NMR, and IR spectroscopic data. These compounds were identified as N-trans-sinapoyl-3-methoxytyramine-4'-O-β-glucoside(1), N-trans-sinapoyl-3-methoxytyramine(2), N-trans-sinapoyltyramine(3), N-trans-p-coumaroyltyramine(4), N-trans-sinapoyl-7-hydroxytyramine(5), N-cis-feruloyltyramine(6), N-cis-p-coumaroyltyramine(7), N-trans-feruloyltyramine(8), N-trans-feruloyl-3-methoxytyramine(9), and N-trans-feruloyl-7-hydroxytyramine(10). Compound 1 is a new compound. Compounds 2-7 are obtained from the plants of Papaveraceae for the first time, while compounds 8-10 are firstly isolated from C. edulis.

Isolation and identification of allergens and biogenic amines of Prosopis juliflora genotypes

Background: Prosopis, or mesquite (Prosopis juliflora (Sw.) DC.), was introduced in Saudi Arabia several decades ago and is heavily used in street, roadside, and park plantations. It shows great adaptation to the prevailing climatic conditions such as high temperature, severe drought, and salinity and spreads naturally in many parts of the Kingdom. This research was conducted to isolate allergen proteins and biogenic amines from the pollen grains of P. juliflora genotypes in Saudi Arabia from two regions, namely Al-Qassim and Eastern regions. Results: The results showed that 18 different allergen proteins were detected in P. juliflora genotypes, with molecular weight ranging from 14 to 97 kDa. Moreover, P. juliflora genotypes from the two studied regions contained eight biogenic amines, namely histamine, tyramine, tryptamine, ß-phenylethylamine, butricine, codapherine, spermidine, and spermine. All genotypes from the Al-Qassim region were found to contain all eight amines, while in the Eastern region, histamine was absent in three genotypes, spermine was absent in six genotypes, and spermidine was absent in three genotypes. Genotypes B23, E20, and E21 had the lowest biogenic amine quantity. Conclusions: All identified proteins from mesquite trees from both regions (Eastern and Al-Qassim) cause allergies in patients who are sensitive to pollen grains. Bioamines, except histamine and tyramine, were recorded at varying concentrations in different genotypes.

Metabolomic analysis of healthy human urine following administration of glimepiride using a liquid chromatography-tandem mass spectrometry

Glimepiride, a third generation sulfonylurea, is an antihyperglycemic agent widely used to treat type 2 diabetes mellitus. In this study, an untargeted urinary metabolomic analysis was performed to identify endogenous metabolites affected by glimepiride administration. Urine samples of twelve healthy male volunteers were collected before and after administration of 2 mg glimepiride. These samples were analyzed by liquid chromatography-tandem mass spectrometry (LC-MS/MS), and then subjected to multivariate data analysis including principal component analysis and orthogonal partial least squares discriminant analysis. Through this metabolomic profiling, we identified several endogenous metabolites such as adenosine 3′, 5′-cyclic monophosphate (cAMP), quercetin, tyramine, and urocanic acid, which exhibit significant metabolomic changes between pre- and posturine samples. Among these, cAMP, which is known to be related to insulin secretion, was the most significantly altered metabolite following glimepiride administration. In addition, the pathway analysis showed that purine, tyrosine, and histidine metabolism was affected by pharmacological responses to glimepiride. Together, the results suggest that the pharmacometabolomic approach, based on LC-MS/MS, is useful in understanding the alterations in biochemical pathways associated with glimepiride action.

Acetyl Eburicoic Acid from Laetiporus sulphureus var. miniatus Suppresses Inflammation in Murine Macrophage RAW 264.7 Cells

The basidiomycete Laetiporus sulphureus var. miniatus belongs to the Aphyllophorales, Polyporaceae, and grows on the needleleaf tree. The fruiting bodies of Laetiporus species are known to produce N-methylated tyramine derivatives, polysaccharides, and various lanostane triterpenoids. As part of our ongoing effort to discover biologically active compounds from wood-rotting fungi, an anti-inflammatory triterpene, LSM-H7, has been isolated from the fruiting body of L. sulphureus var. miniatus and identified as acetyl eburicoic acid. LSM-H7 dose-dependently inhibited the NO production in RAW 264.7 cells without any cytotoxicity at the tested concentrations. Furthermore it suppressed the production of proinflammatory cytokines, mainly inducible nitric oxide synthase, cyclooxygenase-2, interleukin (IL)-1beta, IL-6 and tumor necrosis factor alpha, when compared with glyceraldehyde 3-phosphate dehydrogenase. These data suggest that LSM-H7 is a crucial component for the anti-inflammatory activity of L. sulphureus var. miniatus.

A new feruloyl tyramine glycoside from the roots of Achyranthes bidentata / 中国天然药物

AIM@#To study the chemical constituents of the roots of Achyranthes bidentata Bl.@*METHODS@#The chemical constituents were isolated and purified by macroporous adsorptive resin D101, silica gel, and ODS column chromatographies and preparetive HPLC. Their structures were elucidated on the basis of 1D and 2D NMR analyses.@*RESULTS@#Two feruloyl tyramine glycosides and seven triterpenoid saponins were obtained and identified as N-trans-feruloyl-3-methoxytyramine-4'-O-β-D-glucopyranoside (1), N-trans-feruloyl-3-methoxytyra mine-4-O-β-D-glucopyranoside (2), PJS-1 (3), chikusetsusaponin IVa (4), oleanolic acid 3-O-[β-D-glucuronopy ranoside-6-O-methyl ester]-28-O-β-D-glucopyranoside (5), oleanolic acid 3-O-[β-D-glucuronopyran-oside-6-O-ethylester]-28-O-β-D-glucopyranoside (6), oleanolic acid 3-O-[β-D-glucuronopyranoside-6-O-butyl ester]-28-O-β-D-glucopyranoside (7), ginsenoside R(0) (8) and hederagenin-28-O-β-D-glucopyranosyl ester (9).@*CONCLUSION@#Compound 1 is a new feruloyl tyramine glycoside, while compounds 2 and 9 are reported from A. bidentata for the first time.

Effect of Botulinum Toxin A Injection into the Salivary Glands for Sialorrhea in Children with Neurologic Disorders

OBJECTIVE: To determine the 9 month period effect of botulinum toxin A (BoNT-A) injection into the salivary gland in children with neurologic disorders and sialorrhea by qualified parent/caregiver-administered questionnaires. METHOD: A total of 17 patients (age 7.6+/-4.24 years) were enrolled in this study. The degree of sialorrhea was assessed at the baseline, 2 weeks, 1, 2, 4, 6 and 9 months after injection. The Drooling Count (DC) was assessed as an objective measurement. The Drooling Frequency and Severity Scale (DFS) and the Teacher Drooling Scale (TDS) were evaluated as a subjective measurement. BoNT-A (0.5 unit/kg) was injected into each submandibular and parotid gland under ultrasonography-guidance. RESULTS: DC, DFS and TDS showed significant improvement at 2 weeks, 1, 2, 4, 6, and 9 months follow-up (p<0.05). Twelve of 17 cases (70.5%) showed more than 50% reduction in DC from the baseline value. CONCLUSION: Ultrasonography-guided BoNT-A injection into the submandibular and parotid gland was a safe and effective method to treat sialorrhea in children with neurologic disorders.

Effects of the purified extracts from Lycii Cortex Radicis and ginger on lipid statusand serum cytokine levels in rats fed high fat diet

The present study was to investigate the effects of Lycii Cortex Radicis (LCR), the root bark of lycium (Lycium chenese Miller) and ginger (Gin) on body lipid status and serum levels of cytokines. Sprague-Dawley (SD) male rats weighing 193.6 +/- 16.8 g were divided into five groups, including one low fat (LF) and four high fat groups, i.e. HF-Control, HF-LCR, HF-Gin and HF-LCR + Gin groups. Diets for HF-LCR, HF-Gin and HF-LCR + Gin groups contained purified extracts having 0.2 g LCR tyramine, ginerol and 0.1 g tyramine plus 0.02 g gingerol per kg, respectively. Compared with those of the HF-Control total serum cholesterol level decreased, and HDL-cholesterol level increased in the HF-LCR group and serum triglyceride levels decreased in the three experimental groups fed the purified extracts. Liver cholesterol level was lower in the HF-LCR group than the HF-Control group, but triglyceride levels, which were increased by high fat diets were not changed by significantly by LCR or ginger extracts. Fecal lipid excretion was higher in the HF-LCR and HF-Gin groups, but cholesterol excretion was lower in the HF-Gin group than in the HF-Control group. The activities of liver cytosolic glucose-6-phosphate dehydrogenase and malic enzyme were lower in the HF-LCR + Gin group than in the HF-Control group. Serum adiponectin levels did not differ among the five groups, while leptin level was lower in the HF-Gin group and C-reactive protein levels were lower in the HF-Gin and the HF-LCR + Gin groups than in the HF-Control group. It is concluded that LCR can be utilized as an ingredient for lipid-lowering functional foods in the form of purified extract and addition of small amount of ginger extract would be useful for reducing one of the inflammatory cytokines to help prevent atherosclerosis.

Correlation between Serum Total Testosterone and the AMS and IIEF Questionnaires in Patients with Erectile Dysfunction with Testosterone Deficiency Syndrome

PURPOSE: This study was conducted to investigate the relationship between serum total testosterone levels and scores on the Aging Male's Symptom (AMS) scale and the International Index of Erectile Function (IIEF) in men with erectile dysfunction with testosterone deficiency syndrome (TDS). MATERIALS AND METHODS: From January 2005 to July 2008, 134 patients who complained of sexual dysfunction such as erectile dysfunction or decreased libido as the main symptoms of TDS with serum total testosterone levels less than 3.5 ng/ml were evaluated by independent t-test and linear regression analysis, respectively. Patients with treated hypogonadism within 6 months, with a history of taking a PDE5 inhibitor or an antidepressant for a depressive disorder, or who had metabolic syndrome were excluded from this study. RESULTS: The AMS scale and its 3 subdomain scores were not significantly correlated with the total testosterone level. By contrast, the total IIEF score and the score of each IIEF domain except sexual desire showed a weakly significantly positive correlation with serum total testosterone. CONCLUSIONS: In TDS patients with erectile dysfunction, there was a low relationship between serum total testosterone levels and the AMS scale and a weakly positive correlation between total testosterone levels and all IIEF domains except sexual desire. There was a low relationship between the AMS scale, the sexual desire domain score of the IIEF, and total testosterone. We should understand these limitations when evaluating patients with erectile dysfunction with TDS. New scales should be developed for the evaluation of erectile dysfunction in these patients.

Study on the hypochlolesterolemic and antioxidative effects of tyramine derivatives from the root bark of Lycium chenese Miller

The aim of the present study was to investigate the hypocholesterolemic effect and potential of tyramine derivatives from Lycii Cortex Radicis (LCR), the root bark of lycium (Lycium chenese Miller) in reducing lipid peroxidation. The activities of enzymes, hepatic 3-hydroxy 3-methylglutaryl (HMG) CoA reductase and acyl-CoA:cholesterol acyltransferase (ACAT) and LDL oxidation were measured in vitro and animal experiments were also performed by feeding LCR extracts to rats. The test compounds employed for in vitro study were trans-N-p-coumaroyltyramine (CT) and trans-N-feruloyltyramine (FT), LCR components, N-(p-coumaroyl)serotonin (CS) and N-feruloylserotonin (FS) from safflower seeds, ferulic acid (FA) and 10-gingerol. It was observed that FT and FS at the concentration of 1.2 mg/mL inhibited liver microsomal HMG CoA reductase activity by ~40%, but no inhibition of activity was seen in the cases of CT, CS, FA and 10-gingerol. Whereas, ACAT activity was inhibited ~50% by FT and CT, 34-43% by FS and CS and ~80% by 10-gingerol at the concentration of 1 mg/mL. A significant delay in LDL oxidation was induced by CT, FT, and 10-gingerol. For the animal experiment, five groups of Sprague-Dawley male rats were fed high fat diets containing no test material (HF-control), 1 and 2% of LCR ethanol extract (LCR1 and LCR2), and 1% of extracts from safflower seed (Saf) and ginger (Gin). The results indicated that total cholesterol level was significantly lower in Saf, LCR2 and Gin groups, and HDL cholesterol level was lower only in Gin group when compared with HF-control group; while there was no difference in the serum triglyceride levels among the five experimental groups. The level of liver cholesterol was significantly lower in LCR1 and LCR2 groups than HF-control. Serum levels of TBARS were significantly lower only in LCR2 group when compared with HF-control group. From the observed results, we concluded that LCR can be utilized as a hypocholesterolemic ingredient in combination with ginger, especially for functional foods.

Effect of Testosterone Replacement Treatment in Testosterone Deficiency Syndrome Patients with Metabolic Syndrome

PURPOSE: This study was conducted to investigate the effect of testosterone replacement treatment (TRT) in testosterone deficiency syndrome (TDS) patients with metabolic syndrome. MATERIALS AND METHODS: We reviewed the data of 200 men who were diagnosed with TDS and were undergoing TRT between August 2006 and August 2009. The 200 patients were divided into two groups (group 1: 71 patients with metabolic syndrome, group 2: 129 patients without metabolic syndrome) depending on metabolic syndrome, which was diagnosed according to the NCEP III criteria for Asians. Age, BMI (body mass index), waist circumference, serologic tests, AMS (the Aging Males' Symptoms scale), and IIEF (International Index of Erectile Function) were measured. RESULTS: In group 1, waist circumference and fasting glucose were significantly decreased; hemoglobin and total testosterone were increased; and the somatovegetative scale score of the AMS, the total AMS score, the erectile function score of the IIEF, the overall satisfaction score of the IIEF, and the total IIEF score were significantly improved after TRT. On the other hand, in group 2, waist circumference, BMI, total cholesterol, LDL, and fasting glucose were significantly decreased; hemoglobin and total testosterone were increased; and the 2 subscale scores of the AMS (psychologic and somatovegetative), the total AMS score, all subscale scores of the IIEF, and the total IIEF score were significantly improved after TRT. CONCLUSIONS: Overall, the patients who had TDS with metabolic syndrome showed less improvement in AMS, IIEF, and serum variables. Therefore, the correction of metabolic syndrome, such as diabetes, obesity, and hypertension, should be considered during TRT.

Effect of Testosterone Replacement Treatment in Testosterone Deficiency Syndrome Patients with Metabolic Syndrome

PURPOSE: This study was conducted to investigate the effect of testosterone replacement treatment (TRT) in testosterone deficiency syndrome (TDS) patients with metabolic syndrome. MATERIALS AND METHODS: We reviewed the data of 200 men who were diagnosed with TDS and were undergoing TRT between August 2006 and August 2009. The 200 patients were divided into two groups (group 1: 71 patients with metabolic syndrome, group 2: 129 patients without metabolic syndrome) depending on metabolic syndrome, which was diagnosed according to the NCEP III criteria for Asians. Age, BMI (body mass index), waist circumference, serologic tests, AMS (the Aging Males' Symptoms scale), and IIEF (International Index of Erectile Function) were measured. RESULTS: In group 1, waist circumference and fasting glucose were significantly decreased; hemoglobin and total testosterone were increased; and the somatovegetative scale score of the AMS, the total AMS score, the erectile function score of the IIEF, the overall satisfaction score of the IIEF, and the total IIEF score were significantly improved after TRT. On the other hand, in group 2, waist circumference, BMI, total cholesterol, LDL, and fasting glucose were significantly decreased; hemoglobin and total testosterone were increased; and the 2 subscale scores of the AMS (psychologic and somatovegetative), the total AMS score, all subscale scores of the IIEF, and the total IIEF score were significantly improved after TRT. CONCLUSIONS: Overall, the patients who had TDS with metabolic syndrome showed less improvement in AMS, IIEF, and serum variables. Therefore, the correction of metabolic syndrome, such as diabetes, obesity, and hypertension, should be considered during TRT.

Effects of Botulinum Toxin A Injection into Salivary Glands of Patients with Brain Lesion Suffering from Posterior Drooling

OBJECTIVE: The aim of the study was to evaluate the effectiveness of ultrasouond-guided salivary gland injection of botulinum toxin A (BTX-A) for posterior drooling. METHOD: 11 patients with brain lesion (9 cerebral palsy, 1 hypoxic ischemic encephalopathy and 1 mental retardation) with posterior drooling (an initial PDAS score greater than 2) and related pulmonary problems were recruited. Drooling severity was measured at baseline, 4 weeks, 3 months and 6 months after botulinum toxin A injection, by using Teacher Drooling Scale (TDS), Visual Analogue Scales (VAS), Drooling Score System (DSS)-severity, frequency and Posterior Drooling/Aspiration System (PDAS). RESULTS: The TDS, DSS-severity, DSS-frequency, VAS, PDAS were significantly reduced at 4 weeks and 3 months after BTX-A injection into salivary glands compared to pre-injection (p<0.05). However, there were no significant changes at 6 months compared to pre-injection level. CONCLUSION: BTX-A injection into salivary glands may improve anterior drooling in patients with brain lesions. Furthermore BTX-A injection into salivary glands may also decrease the posterior drooling which might related to respiratory symptoms in aspiration pneumonia.

Testosterone replacement therapy and monitoring for the male patients with testosterone deficiency syndrome

Since the elderly population has been increasing recently in our country, old male patients with testosterone deficiency syndrome (TDS) with a significantly decreasing quality of life are becoming increasingly common. TDS in males is defined as a biochemical syndrome associated with advancing age and characterized by clinical manifestation and a deficiency in the serum testosterone level. These patients should be treated with extrinsic testosterone to improve quality of life. TDS in males should be diagnosed in the case of clinical manifestation with serum total testosterone 12 nmol/L (350 ng/dL). Products for testosterone replacement therapy (TRT) are administrated orally, transdermally, and through injectable preparations. Daily testosterone undecanoate is widely used for oral administration with good results and no hepatotoxicity. Short-acting intramuscular preparations are very effective but show wide swings in the resulting supra-physiological level of serum testosterone. Long-acting intramuscular preparations is also very effective and lasting for 3 months with normal physiologic levels. Many products for TRT on the market are effective and generally safe. However, those have a few significant adverse events each other. The ideal product should have notable effectsand few side effects, (such as selective androgen receptor modulators), be easy to administrate, maintain physiologic serum concentration, and be inexpensive. TDS in males can easily be correct by TRT. However, the advantages and disadvantages of the individual products and follow-up management of complicated adverse events should be understood before starting and maintaining TRT.

Tiramina en la orina de los parkinsonianos idiopáticos / Urine excretion of tyramine in idiopathic parkinson disease

Hemos tabulado los datos, recuperados por pubmed.gov, de la excreción urinaria de la tiramina pues sus niveles anormales, previos a la aparición de signos clínicos, permitirían la identificación preclínica precoz de los parkinsonianos idiopáticos. El tamizado para excreción de tiramina en la orina debería realizarse, especialmente en enfermos con Parkinson, antes de cualquier tratamiento farmacológico, y en grupos de alto riesgo,. Se deben llevar a cabo estudios cuantitativos para completar las cifras normales de tiramina en la orina según el sexo, la edad, el ritmo circadiano, la dieta y otros factores que puedan afectar dicha excreción.

Alkaloids from Senecio scandens / 中国中药杂志

<p><b>OBJECTIVE</b>To investigate the alkaloids from Senecio scandens.</p><p><b>METHOD</b>Compounds were isolated with silica gel and Sephadex LH-20 column chromatography and their structures were determined by spectral analysis and chemical evidence. The hepatic cytotoxicity of isolated compounds was tested by MTT method in vitro.</p><p><b>RESULT</b>Six alkaloids were obtained and identified as adonifoline (1), 7-angeloylturneforcidine (2), hordenine (3), 1, 3, 6, 6-tetramethyl-5, 6, 7, 8-tetrahydro-isoquinolin-8-one (4), 4-(pyrrolidin-2-one) -phenyl acetic acid (5), (4-pyrrolidinophenyl) acetic acid (6).</p><p><b>CONCLUSION</b>Compound 6 is a new natural product, compounds 3, 4 were obtained from the genus Senecio for the first time, compounds 2, 5 were obtained from this plant for the first time. Compound 1 showed significant growth inhibitory effect against hepatocyte at 100 micromol x L(-1).</p>

The effect of transdermal scopolamine plus intravenous dexamethasone for the prevention of postoperative nausea and vomiting in patients with epidural PCA after major orthopedic surgery / 대한마취과학회지

BACKGROUND: Postoperative nausea and vomiting (PONV) is common complication of Patient-Controlled Analgesia (PCA) after surgery. The authors sought to determine whether a transdermal scopolamine (TDS) patch in combination with IV dexamethasone is more effective than IV dexamethasone alone or IV dexamethasone plus IV ramosetron for reducing PONV in patients receiving epidural PCA after major orthopedic surgery. METHODS: 120 patients that received epidural PCA with hydromorphone and ropivacaine after major orthopedic surgery under spinal anesthesia were allocated to 3 groups: Group D (n = 40) received IV dexamethasone 8 mg, Group DR (n = 40) received IV dexamethasone 8 mg plus IV ramosetron 0.3 mg, Group DS (n = 40) received IV dexamethasone 8 mg plus a TDS patch (Group DS, n = 40). Nausea and vomiting incidences, VAS for nausea, the use of additional antiemetics, and adverse effects (a dry mouth, blurred vision, drowsiness) during the first 24 hours postoperatively were subjected to analysis. RESULTS: The DS Group had a significantly higher rate of complete remission of PONV than the D and DR groups (82.5% vs 47.5%, and 50.0%, respectively), and had lower rates of nausea (17.5% vs 55.0%, and 50.0%), and vomiting (10.0% vs 50.0%, and 25.0%), and required less antiemetics (5.0% vs 35.0%, 22.5%) than group D and Group DR during the first 24 hours after surgery. Furthermore, no inter-group differences were observed with respect to adverse effects in the three groups. CONCLUSIONS: The prophylactic use of a TDS patch plus dexamethasone was found to be a more effective means of preventing PONV in patients that received epidural PCA after major orthopedic surgery than dexamethasone alone or dexamethasone plus ramosetron without adversely affecting side effects.

Oral Testosterone Undecanoate Versus Transdermal Testosterone Gel for the Treatment of Testosterone Deficiency Syndrome: A Retrospective Comparative Study / 대한남성과학회지

PURPOSE: Oral testosterone undecanoate and transdermal testosterone gel are the testosterone formulas widely prescribed as hormonal replacement for tesosterone deficiency syndrome (TDS) in male patients. We evaluated the changes in serum testosterone level and the effects of these medicines. MATERIALS AND METHODS: The medical records of 162 patients who were diagnosed with TDS based on serum testosterone (0.05). The initial and final testosterone levels of the two groups were not significantly different. However, the peak level during treatment was significantly higher in group II (p<0.05). The maximal increment of testosterone level was also significantly higher in group II. Initially, group II reached its peak testosterone level earlier than group I. The final serum levels were not significantly different after adjustment of dosages in group I. Testosterone replacement significantly decreased the AMS scales in both groups. CONCLUSIONS: Both oral testosterone undecanoate and transdermal testosterone gel improved the serum testosterone level and symptom score for those with TDS. Transdermal testosterone gel may reach the peak serum testosterone level faster than oral testosterone undecanoate. Large prospective studies are required to assess the precise role of testosterone replacement therapy.

Concentrações plasmáticas de triptamina, tiramina e feniletilamina em eqüinos sob efeitos de sobrecarga de carboidratos e antiinflamatórios não esteroidais / Plasmatic concentrations of tryptamine, tyramine end phenylethylamine in horses under the effect of carbohydrate overload and non-steroid antinflammatory compounds

As concentrações plasmáticas das aminas triptamina (TRP), tyramina (TYR) e pheniletilamina (PEA) foram determinadas por cromatografia gasosa (CG) de 20 eqüinos sob efeito de sobrecarga por carboidratos (SC). Após 36h da SC os animais foram aleatoriamente divididos em quatro grupos (n=5) e receberam a cada 12h por via iv: solução salina 10mL (GC), ketoprofeno 2,2mg/kg (GK), fenilbutazona 4,4mg/kg (GF) e flunixin meglumine 1,1mg/kg (GFM). As concentrações das aminas TYR e PEA variaram de 0,18 a 164,2mg/L, com diferenças nos tempos avaliados, mas não entre os tratamentos (p<0,01). A concentração plasmática de TRP apresentou diferenças entre os tempos e também entre os tratamentos. O GC diferiu dos demais nos momentos 48h e 60h e as concentrações nos grupos GK e GFM foram menores que nos grupos GF e GC às 72h (P= 0,0012). Conclui-se que nas doses utilizadas os antiinflamatórios não esteroidais avaliados não interferem nas concentrações de TYR e PEA. Entretanto, o ketoprofeno e o flunixin meglumine foram efetivos em diminuir a concentração plasmática de TRP.

The concentrations of the bioactives amines tryptamine (TRP), tyramine (TYR) and phenylethylamine (PEA) were determined by gas chromatography in plasma samples of 20 horses submitted to carbohydrate overload. Thirty hours after the overload, the horses were randomly distributed in four groups (n=5) and were submitted to four IV treatments every 12 hours: 10ml of saline (GC), ketoprofen 2.2mg/kg (GK), phenylbutazone 4.4mg/kg (GF), and flunixin meglumine 1.1mg/kg (GFM). Blood samples were collected at various times after the overload (0-72 h). Plasma TYR and PEA concentrations ranged from 0.18 to 164.2mg/L, and differed significantly with time (p<0.01), but did not differ in the treatments. Plasma concentrations of TRP differed between times and treatments. The GC was significantly major than other treatments at 48h and 60h after the overload, and the plasma concentration of TRP in groups GK and GFM was significantly lower than in groups GF and GC at 72 h (p=0.0012). We concluded that the anti-inflammatory drugs evaluated do not interfere in the plasma concentration of TYP and PEA. For TRP, ketoprofen and flunixin meglumine was effective to reduce de plasmatic concentration of this amine.