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PubMed1975

[Studies on cerebrospinal fluid diffusion of trimethoprim in children].

Full quantitative fluorometric analysis of TMP in serum and cerebrospinal fluid in 91 infants and children (all anyhow designed for lumbar puncture for other reasons) 1/2 - 12 hours after i. v. injection of TMP in a single dose of 4 mg/kg (73 cases, tab. 1-2, fig. 1) or 12 mg/kg (18 cases, tab. 3, fig. 2). TMP in serum and cerebrospinal fluid showed regularly high plateaus for the whole time investigated, i.e. 12 hours after i. v. injection (fig. 1-2). The c.s.f./serum ratio for TMP (2-12 hours after injection) was 30-40%(fig. 1). After a dose of 12 mg/kg the ratio was even 50% and more (fig. 2). There were - in our material - no differences of the ratio according to c.s.f. state (normal - tab. 1, or pathological-tab. 2), or age. Considerating published data on enteral resorption of trimethoprim-sulfamethoxazole and c.s.f. diffussion of SMZ together with our results, we can expect a very intensifying proportion TMP: SMZ near 1:10 in cerebrospinal fluid after intake of officinal TMP-SMZ (Co-trimoxazol). This might have diagnostic and therapeutic consequences.

Child↗

PubMed2002

In vitro permeation of tetramethylpyrazine across porcine buccal mucosa.

AIM: To examine the in-vitro transport route of tetramethylpyrazine (TMP) across porcine buccal mucosa and to investigate the effects of drug concentration, pH in donor chamber, and 1-octanol/buffer partition coefficient on transbuccal permeation. METHODS: In-vitro permeation of TMP through porcine buccal mucosa was studied by using in-line flow through diffusion cells at 37 . The permeability of TMP was evaluated at different donor pH and drug concentration. Permeability of unionized (Pu) and ionized TMP (Pi) was calculated by using the Scientist software. RESULTS: The steady state flux of TMP increased linearly with the donor concentration (r2=0.96) at pH 7.4. The permeability and the partition coefficient increased with pH. Pu and Pi were 9.05 x 10(-6) cm.s(-1) and 2.99 x 10(-7) cm.s(-1), respectively. The total permeability coefficient increased with the fraction of unionized form. CONCLUSION: TMP permeated through buccal mucosa by a passive diffusion process. The partition coefficient and pH dependency of drug permeability indicated that the drug was transported mainly via the transcellular route by a partition mechanism.

Absorption↗

PubMed1992

[Effects of tetramethylpyrazine on rabbit basilar artery ring and canine vertebroarterial circulation].

Tetramethylpyrazine (TMP) inhibited the contraction of rabbit basilar artery and mesenteric arteries caused by KCl with an IC50 of 1.3 mmol.L-1 and 7.5 mmol.L-1 (P < 0.01). The contraction of the rabbit basilar and mesenteric artery ring evoked by KCl, CaCl2 and norepinephrine was inhibited noncompetitively by TMP with the pD2' values of 2.18 +/- 0.16 and 1.83 +/- 0.18 (P < 0.01), 2.13 +/- 0.12 and 2.08 +/- 0.12 (P > 0.05), 3.08 +/- 0.16 and 2.57 +/- 0.08 (P < 0.01), respectively. The contraction of rabbit basilar artery and saphenous veins evoked by 5-HT was also inhibited by TMP with an IC50 of 0.22 mmol.L-1 and 2.2 mmol.L-1 (P < 0.01), respectively. TMP antagonized the myogenic activity of rat portal vein strips. TMP increased canine vertebroarterial blood flow and had no effect on femoral artery blood pressure. The results suggested that TMP may block the calcium channel, inhibit the contraction of rabbit basilar artery, and improve the canine vertebroarterial circulation selectively.

Animals↗

PubMed1992

Defining the involvement of HOCl or Cl2 as enzyme-generated intermediates in chloroperoxidase-catalyzed reactions.

Peroxidatic substrates, catechol (CAT) and 2,4,6-trimethylphenol (TMP) were used as probes of thechloride dependent reactions catalyzed by chloroperoxidase (CPO). TMP is consumed only in the presence of chloride. TMP is a competitive inhibitor versus CAT, but CAT is a noncompetitive inhibitor versus TMP in chloride-dependent CPO-catalyzed peroxidation reactions. The ratio of TMP versus CAT consumed by the chloride-dependent CPO reaction in direct competition studies increases as the chloride concentration is increased from 1.0 to 400 mM. Ratios of non-enzymatic HOCl reactions under conditions otherwise similar to those of the CPO reactions are relatively insensitive to changes in chloride concentration and are experimentally indistinguishable from the values attained by the enzyme system at high chloride concentrations. Comparison of enzymatic ratios with those of the HOCl reactions indicate that the proportion of the enzymatic reaction involving a freely dissociable, enzyme-generated, oxidized halogen species varies from 10% at low chloride concentrations to essentially 100% at high chloride concentrations. All data are consistent with a mechanism in which chloride competes with CAT for binding to both CPO compound I and the CPO chlorinating intermediate (EOCl). Chloride binding to CPO compound I leads to the formation of EOCl and initiates the CPO chloride-dependent pathway. When CAT binds to either compound I or EOCl, it is directly oxidized to product. When chloride binds to EOCl, it either induces release of HOCl or reacts with EOCl to produce Cl2, which is released from the enzyme. TMP and CAT compete for reaction with the free oxidized halogen species. This is the first direct evidence for kinetically significant involvement of a free oxidized halogen species as an intermediate in any CPO-catalyzed reaction.

Catechols↗

PubMed2003

[Effects of tetramethylpyrazine on cytosolic free calcium concentration in penis corpus cavernsum smooth muscle cells in rabbits].

OBJECTIVE: To study the effects of Chinese medicine tetramethylpyrazine (TMP) on intracellular free calcium ([Ca2+]i) in cultured penis corpus cavernosum smooth muscle cell (PCSMC) in rabbits. METHODS: By using laser scanning confocal microscope (LSCM), the [Ca2+]i fluorescence signal changes was investigated in cultured PCSMC loaded with Ca2+ indicator Fluo-3/AM and divided into potassium chloride(KCl) group and norepinephrine (NE) group. Compared with verapamil (Ver), the effects of TMP was observed in different concentrations on [Ca2+]i increase induced by high potassium and NE. RESULTS: TMP had no obvious effect on resting PCSMC [Ca2+]i. It was found that 1, 10, 100 mumol/L TMP significantly inhibited [Ca2+]i increase induced by high potassium-depolarization. The peak inhibition rates were (38.6 +/- 3.0)%, (44.1 +/- 2.4)% and (53.7 +/- 4.1)% respectively. TMP could also inhibit cytosolic calcium pool release induced by 1 mumol/L NE. The peak inhibition rates were (13.9 +/- 2.7)%, (21.2 +/- 1.9)% and (29.5 +/- 3.6)% respectively. CONCLUSIONS: TMP can inhibit rabbit PCSMC [Ca2+]i significantly by suppressing voltage-dependent calcium channel and cytosolic calcium pool release. The effect, similar to Ver, signifies the important mechanism of erectile dysfunction (ED) therapy.

Animals↗

PubMed2004

Inhibition of shear-induced platelet aggregation in rat by tetramethylpyrazine and salvianolic acid B.

Tetramethylpyrazine (TMP) and salvianolic acid B (SAB) are effective ingredients of Rhizoma Ligustici chuanxiong Hort. and Radix Salviae miltiorrhizae Bge., accordingly. The inhibitive effects of TMP, SAB and their combination on shear-induced platelet aggregation (SIPA) were investigated in the present study. SD rats were used as blood donors to collect anticoagulated blood, the concentration of platelet-rich-plasma (PRP) was adjusted to 5 x 10(5) microl. HAAKE rheometer RS 600 with sensor C60/0.5 degrees was used as shear generator. Different doses of TMP and SAB and their combinations were added to the PRP. After constant shear of 15 Pa at 37 degrees C for 360 seconds, PRP was transferred to a platelet aggregometer and SIPA was determined by turbidity. SIPA was inhibited by TMP and SAB in a dose-dependent manner. SIPA was decreased from 48.6 +/- 4.6% of the control to 12.5 +/- 2.1% in the presence of TMP (1.46 mM) and SAB (10 microM) (P < 0.0001). In conclusion, TMP and SAB have additive effects on inhibiting platelet aggregation induced by high shear stress.

Animals↗

PubMed2004

[Effect of tetramethylpyrazine on lipopolysaccharides induced macrophage cyclo-oxidase-2 expression and apoptosis of cardiac myocytes].

OBJECTIVE: To observe the effect of tetramethylpyrazine (TMP) on lipopolysaccharides (LPS) induced macrophage cyclo-oxidase-2 (COX-2) gene expression and activity in RAW264.7 mice, and to further investigate the effect and mechanism of TMP on LPS induced apoptosis of cardiac myocytes in suckling mice. METHODS: RT-PCR and Western Blot (WB) were used to investigate the macrophage COX-2 gene expression, ELISA was used to measure its activity, fluorescence microscopy was used to determine the apoptosis of murine neonatal cardiac myocyte, and fluorescence spectrophotometry was used to detect the concentration of intracellular calcium ion (Ca2+). RESULTS: TMP of 10(-6) mol/L could significantly reduce the COX-2 mRNA and protein expression (P < 0.05), in 10(-5) mol/L and 10(-4) mol/L could significantly decrease the COX-2 expression (P < 0.01) stimulated by LPS, but couldn't influence the activity of COX-2 by different TMP concentration. TMP in 10(-5) mol/L could significantly lower the concentration of intracellular Ca2+ in cardiac myocyte, and antagonize the LPS induced apoptosis of cardiac myocyte in suckling mice (P < 0.05). CONCLUSION: TMP has the pharmacological effect in inhibiting LPS induced macrophage COX-2 expression and apoptosis of cardiac myocyte in suckling mice.

Animals↗

PubMed2005

[Experimental study of evaluation on neuroprotective effect for tetramethylpyrazine against focal cerebral ischemic injury with diffusion-weighted magnetic resonance imaging].

OBJECTIVE: To evaluate the neuroprotective effect of tetramethylpyrazine (TMP) against focal cerebral ischemic injury in rats with diffusion-weighted magnetic resonance imaging (DWMRI). METHODS: Rat models of focal cerebral ischemic injury were established in 16 male SD rats. They were randomly divided into the TMP group and the control group, eight in each group, and pretreated with TMP and normal saline respectively before modeling. Change of infarcted cerebral focus was observed with DWMRI at 1, 2, 6, 12 and 24 hrs after infarction, and the infarction volume (IV) at 24 hrs after modeling was estimated by triphenyltetrazolium chloride (TTC) stain. RESULTS: The IV in all time points observed in the TMP group with DWMRI was significantly smaller than that in the control group (P<0.01). Compared with that at 1 hr after infarction, in the control group at 2, 6, 12 and 24 hrs after modeling, the IV enlarged by 13.3%, 29.7%, 50.3% and 57.3% respectively, while that in the TMP group 9.9%, 21.3%, 37.1% and 40.5% respectively. The cerebral IV estimated by TTC stain 24 hrs after modeling was larger than that estimated by DWMRI. CONCLUSION: TMP pretreatment before modeling was effective in protecting brain against cerebral ischemic damage in rats. DWMRI dynamic scanning observation has important significance in observing the cerebral ischemic developing process and evaluating the effectiveness of brain protective measures.

Animals↗

PubMed2005

[Prediction of 2-year outcome by combining TIMI myocardial perfusion grading with sum ST segment resolution in patients with acute myocardial infarction].

OBJECTIVE: To evaluate the value of combining TIMI myocardial perfusion (TMP) grading with sum ST segment resolution (sumSTR) in prediction of the 2-year outcome and heart function in patients with acute myocardial infarction (AMI) after emergency percutaneous intervention (PCI). METHODS: Seventy-seven consecutive patients of AMI with elevated ST segment, 62 males and 15 females, aged 63 +/- 12 (30-91), underwent PCI. TMP grading was used in combination of electrocardiography to calculate the sumSTR so as to evaluate the effect of myocardial reperfusion. The patients with TMP grade 2-3 and sumSTR > or = 30% were included in the group of better perfusion, and those with the TMP grade 0-1 and sumSTR < 30% were included in the group of lower perfusion. The cardiac events, including death, reinfarction, revascularization, angina pectoris, and heart failure were recorded. The left ventricular end-diastolic dimension (LVEDD) and left ventricular ejection fraction (LVEF) were measured by echocardiography 72 hours and 2 years after the PCI. RESULTS: There were 37 patients in the lower perfusion group and 39 patients in the better perfusion group. Cos regression showed that TMP grade 0-1 associated with sumSTR < 30% was an independent factor for 2-year cardiac events (RR = 13.186, 95% CI 2.149 - 80.917, P = 0.005). The LVEDD 2 years after PCI was 60 mm +/- 4 mm, significantly higher than that 72 hours after PCI (53 mm +/- 4 mm. P < 0.01) in the lower perfusion group. The LVEDD increased by 7.1 mm +/- 1.9 mm two years after PCI in the lower perfusion group, significantly more than that in the better perfusion group (1.5 mm +/- 1.2 mm, P < 0.01). The myocardial perfusion after PCI was closely correlated with the extent of heart function improvement 2 years after (chi(2) = 50.58, P < 0.01). CONCLUSION: TMP grading combined with sumSTR helps predict the 2-year outcome and heart function in the patients with AMI after emergency PCI.

Adult↗

PubMed1991

[Community-acquired urinary infection: the in vitro activity of trimethoprim and cotrimoxazole].

To evaluate the in vitro sensitivities of trimetoprim (TMP) in our area and to compare them with those to co-trimoxazole (CMX) a prospective study was carried out in females with uncomplicated lower urinary tract infection (UCLUTI), as a preliminary step for the possible use of a monodose of TMP in these patients. Fifty-five cases of UCLUTI were included. Escherichia coli was the predominating organism (70.9%). The general sensitivity to CMX was 80% and that to TMP 76.4%. The E. coli sensitivity to CMX was 79.5%, and 76.9% to TMP. The difference in the sensitivities to both antimicrobials was not statistically significant (p = 0.5). The routine introduction of TMP in the antibiogram would permit to evaluate the resistance to this antimicrobial in each area and, on the basis of the results, to assess the effectiveness of TMP in the treatment of UCLUTI.

Adolescent↗

PubMed1991

Ocular and cardiovascular pharmacology of tetramethylpyrazine isolated from Ligusticum wallichii Franch.

Tetramethylpyrazine (TMP), the active principle in Ligusticum wallichii, D-timolol, and L-timolol were compared for their effects on retinal and choroidal blood flow (RCBF), blood pressure (BP), and heart rate (HR). TMP (10 mg.kg-1) increased RCBF by 44% and did not affect systemic BP or HR. D-Timolol (4 mg.kg-1 iv) had a tendency to increase RCBF but did not affect systemic BP and HR either. L-Timolol (0.4 mg.kg-1 iv), on the other hand, decreased RCBF by 18% and reduced both systemic BP and HR. In isolated preparations, TMP increased coronary artery blood flow with slight vasodilation, but vasoconstriction in renal, femoral and mesenteric arteries. These results indicate that TMP could be used to prevent or alleviate certain ischemic retinal degenerations without producing significant cardiovascular side effects. The in vitro vasoconstriction actions of TMP (0.2 mg.ml-1) were blocked by propranolol and phenoxybenzamine, indicating that adrenergic mechanism might be involved in TMP action.

Animals↗

PubMed1990

[Infection prophylaxis in patients with hematological malignancies (I)--Successful prophylaxis of Pneumocystis carinii pneumonitis with sulfamethoxazole-trimethoprim].

In a retrospective study to evaluate the efficacy of sulfamethoxazole-trimethoprim (SMX-TMP) for the prevention of Pneumocystis carinii pneumonitis, we studied 1760 patients wit hematological malignancies over a twenty-year period (1970-1989). 449 patients received oral SMX-TMP, most of all received 400 mg of SMX and 80 mg of TMP twice per day. None of the patients receiving SMX-TMP developed P carinii pneumonitis, whereas twenty-six (2.0%) of the 1311 patients who did not receive SMX-TMP developed P carinii pneumonitis (p less than 0.01). We found that the SMX-TMP was very effective in the prevention of P carinii pneumonitis in patients with hematological malignancies, and was well tolerated.

Administration, Oral↗

PubMed1989

Trimethoprim-sulfamethoxazole pharmacokinetics during continuous ambulatory peritoneal dialysis (CAPD).

Ten adult patients on continuous ambulatory peritoneal dialysis (CAPD) received one dose of trimethoprim-320 mg (TMP) and sulfamethoxazole 1600 mg (SMX) orally (p.o.), intravenously (i.v.), and intraperitoneally (i.p.) on three separate occasions to characterize the pharmacokinetics of both drugs. Concentrations of both TMP and SMX were measured in serum and dialysate by HPLC to 48 h. Half-life, total body clearance (TBC), and peritoneal clearance (PCl) were determined. The mean half-life of TMP was 28 h, while for SMX it was 12.5 h. Relative to the i.v. dose, the bioavailability following oral administration for TMP was 98% and 87% for SMX. Intraperitoneal bioavailability was 73% for TMP and 65% for SMX after a 4-h dwell. After 24 h, regardless of the route of administration, less than 3% of TMP and less than 6% of SMX appeared in dialysate. We conclude that peritoneal losses contribute insignificantly to TMP/SMX elimination during CAPD.

Administration, Oral↗

PubMed1987

Pharmacokinetics of co-trimazine after single and multiple doses.

Plasma and urinary levels of trimethoprim (TMP), sulfadiazine (SDZ) and N4-acetylsulfadiazine (N4-SDZ) were determined after administration of 1 g co-trimazine (equivalent to 180 mg TMP and 820 mg SDZ) (Kombinax) as a single dose and again once daily for 7 days to 6 normal subjects. Both TMP and SDZ were rapidly absorbed from the gastrointestinal tract with peak plasma levels being achieved within 4 h in all subjects. Elimination half-lives ranged from 8 to 13 h for TMP and from 9 to 15 h for SDZ. Approximately 50% of the administered dose of SDZ was recovered in urine within 24 h of the single dose (32% as unchanged drug and 17% as the N4-acetylmetabolite). For TMP, the urinary recovery during the 24 h following the single dose averaged 39%. Mean plasma levels of TMP, SDZ and N4-SDZ at steady state were moderately higher than those observed after a single dose, but no change in absorption or disposition kinetics of these compounds was seen after repeated dosing.

Adult↗

PubMed1983

In vitro susceptibilities of canine urinary bacteria to selected antimicrobial agents.

Antimicrobial susceptibility tests were conducted on bacteria that were isolated from urine specimens collected by antepubic cystocentesis from dogs with urinary tract infections. Antimicrobics to which greater than or equal to 90% of these urinary bacteria were susceptible in vitro included trimethoprim-sulfamethoxazole (TMP-SMZ), nitrofurantoin, cephalexin, nalidixic acid, and gentamicin for isolates of Escherichia coli; ampicillin, TMP-SMZ, cephalexin, nalidixic acid, and gentamicin for isolates of Proteus mirabilis; ampicillin chloramphenicol, TMP-SMZ, nitrofurantoin, cephalexin, kanamycin, and gentamicin for isolates of coagulase-positive staphylococci; cephalexin, nalidixic acid, and gentamicin for isolates of Klebsiella pneumoniae; ampicillin, TMP-SMZ, and gentamicin for isolates of Streptococcus faecalis, Str faecium, and Str zymogenes; ampicillin, chloramphenicol, TMP-SMZ, and gentamicin for isolates of Str viridans; and ampicillin, chloramphenicol, TMP-SMZ, nitrofurantoin, cephalexin, kanamycin, and gentamicin for isolates of Str canis. No antimicrobial agent tested was effective in vitro at the 90% level for isolates of Pseudomonas aeruginosa, but gentamicin was closest, at 89%.

Animals↗

PubMedDate not supplied

Antimicrobial therapy of chancroid: an evaluation of five treatment regimens correlated with in vitro sensitivity.

One hundred fifty-one men with genital ulcer disease were assigned randomly to treatment with one of five oral antimicrobial regimens: (1) sulfadimidine (1 g four times daily for seven days); (2) tetracycline (500 mg four times daily for seven days); (3) trimethoprim-sulfamethoxazole (TMP-SMZ; 160 mg of TMP and 800 mg of SMZ twice daily for seven days); (4) doxycycline (300 mg as a single dose); or (5) TMP-sulfametrole (640 mg of TMP and 3,200 mg of sulfametrole once as a single dose). Haemophilus ducreyi was isolated from 81 (54%) of the men, and 35 strains were available for testing of antimicrobial susceptibility. The TMP-SMZ and TMP-sulfametrole regimens were more effective than sulfadimidine, tetracycline, or single-dose doxycycline in curing ulcers. Only one of 35 strains tested was susceptible to tetracycline (less than or equal to 8 mg/liter), and only ten of 35 strains were susceptible to doxycycline (less than or equal to 4 mg/liter), whereas all were susceptible to trimethoprim (less than or equal to 2 mg/liter). The correlation between in vitro susceptibility and bacteriologic response to the antimicrobial agents requires further investigation. In particular, sulfonamide resistance did not always identify failure to respond to sulfadimidine.

Chancroid↗

PubMed1983

[Trial of trimedin action on chickens].

Investigations were carried out with a total of 421 broiler birds (four-line Cornish X Plymouth Rock hydbrids) within the age range of 2 days to 5 weeks. Determined was the acute toxicity of the combination sulfadimidine (SDM) + trimetoprim (TMP)--5 + 1 and the water-soluble formula of trimedin following the intraingluvial introduction with week-old birds. LD50 of the combinations SDM+TMP (5+1) was 3980 mg/kg (2780: 5690), and that of trimedin was 2038 mg/kg body mass. The biologic half-life of SDM ranged from 4.77 to 5.34 h, and that of TMP--from 4.81 to 5.71 h at the intraingluvial introduction of the combination SDM+TMP (5+1) at the rate of 0.06 g/kg. Demonstrated were the therapeutic levels of SDM and TMP during the whole period (10 days) of treatment with the combination SDM+TMP (5+1) given with the feed in conc. 500 ppm or at the application of trimedin alone via the drinking water in conc. 0.05%. It was found that trimedin used for 10 days with the drinking water in conc. 0.05 per cent with broilers at the experimental infection with Salmonella gallinarum-pullorum protected about 40 per cent of the birds, the latter remaining, however, carriers of the infection.

Animals↗

PubMed1980

Evaluation of in vitro sensitivity testing methods of detecting sulphamethoxazole trimethoprim synergy. Correlation with mouse protection assay.

To evaluate the applicability of sensitivity tests in the detection of synergy between sulphamethoxazole (SMX) and trimethoprim (TMP) hospital strains of Escherichia coli were tsted by the disc sensitivity and the agar dilution tests using Isosensitest agar; sensitivity to SMX, TMP and 20 parts sulphamethoxazole plus 1 part trimethoprim (SXT) was determined. Ten of 19 strains of E. coli showed larger zones of inhibition with the SXT discs than with either SMX or TMP discs. Yet all 19 E. coli strains showed appreciably lower MIC for SXT than either SMX or TMP in the agar dilution test. It is concluded that disc sensitivity tests do not detect synergy between SMX and TMP. Demonstration of a lower MIC with SXT than either SMX or TMP in the agar dilution test is a better indication of synergy. This conclusion is confirmed in the mouse protection tests.

Animals↗