Analgesic effects of piritramide in acute postoperative pain - comparison of intramuscular administration with patient-controlled intravenous analgesia and impact of OPRM1 and ABCB1 polymorphisms.

Aims: The aim of this study was to compare the efficacy, consumption and safety after piritramide administered either intramuscularly (IM) on demand or via patient-controlled intravenous analgesia (PCA) and to examine the impact of OPRM1 and ABCB1 gene polymorphisms on the drug efficacy/safety in both regimens.

Methods: One hundred and four patients scheduled for elective inguinal hernioplasty received piritramide with PCA or IM for postoperative pain management. We evaluated piritramide consumption, pain intensity using visual analogue scale (VAS) and adverse effects.

Impact of smoking on metabolic changes and effectiveness of drugs used for lung cancer.

Objective: This article reviews the published studies dealing with the influence of cigarette smoking on metabolic changes and effectiveness of drugs used in the systemic chemotherapy of the lung cancer.

Methods: The literature search of interactions between cigarette smoking and drugs used for lung cancer was carried out. The abstracted data mostly involved some induction of key drug-metabolizing enzymes of cytochrome CYP1A1/2, CYP2D6, CYP3A4 and isoforms of UDP-glucuronosyltransferase.

Epidural analgesia with sufentanil in relation to OPRM1 and ABCB1 polymorphisms.

The aim of this study was to evaluate the association between OPRM1 and ABCB1 polymorphisms on pain relief with epidural sufentanil in 69 patients after rectosigma resection for cancer. The median number of injections (SD) 2.31 (1.

Treatment of tobacco dependence as a standard part of oncology care.

After the oncological diagnosis, smoking has a major impact on survival, course and effectiveness of oncology treatment, and quality of the further life. Smoking worsens surgery outcomes, reduces the effectiveness of radiation therapy and chemotherapy, increases the risk of side effects of oncology treatment, and increases the incidence of tumor duplication or other comorbidities like venous thrombosis, cardiovascular diseases or infections. The article contains a summary of practical recommendations for oncology patients, including smoke-free environments, the importance of zero exposure to tobacco smoke, clear advice to stop smoking to smokers and offer of tobacco dependence treatment.

Correction to: Pupillometry as an indicator of L-DOPA dosages in Parkinson's disease patients.

Unfortunately, original article has been published without acknowledgement section.

Pupillometry as an indicator of L-DOPA dosages in Parkinson's disease patients.

Dopamine was shown to induce mydriasis by excitation of alpha-adrenergic receptors at the dilator pupillae muscle. Pupilla diameter may thus serve as an indirect measure of peripheral pharmacokinetics of L-DOPA and dopamine. The aim of this study is to evaluate the effect of L-DOPA dosage on pupillometric parameters in Parkinson's disease (PD) patients.

[Smoking and pharmacological interactions].

Cigarette smoking can affect drug metabolism via pharmacokinetic and pharmacodynamic mechanisms, and a sudden change in smoking status can render patients at risk of serious adverse reactions, eg. after clozapine. Patients should be regularly monitored with regard to their smoking status and extent of cigarette consumption and doses of relevant medications adjusted accordingly.

Pleiotropic effects of niacin: Current possibilities for its clinical use.

Niacin was the first hypolipidemic drug to significantly reduce both major cardiovascular events and mortality in patients with cardiovascular disease. Niacin favorably influences all lipoprotein classes, including lipoprotein[a],and belongs to the most potent hypolipidemic drugs for increasing HDL-C. Moreover, niacin causes favorable changes to the qualitative composition of lipoprotein HDL.

OPRM1 and ABCB1 polymorphisms and their effect on postoperative pain relief with piritramide.

Genetic factors may contribute to the differential response to opioids. The aim of this study was to evaluate the association between polymorphisms of µ1-opioid receptor gene OPRM1 (rs1799971), and P-glycoprotein transporter gene ABCB1 (rs1045642, rs2032582), and piritramide efficacy under postoperative patient-controlled analgesia (PCA). In 51 patients, OPRM1 variant was associated with decreased efficacy in early postoperative period evidenced by sum of pain intensity difference in the 0-6 h postoperative period (SPID(0-6)), (F=3.

Niacin in the Treatment of Hyperlipidemias in Light of New Clinical Trials: Has Niacin Lost its Place?

Niacin is considered to be a powerful drug for the treatment of lipid and lipoprotein abnormalities connected with "residual cardiovascular risk", which persist in high-risk patients even when the target goals of LDL-C are achieved with statin therapy. Recent large randomized clinical studies - AIM-HIGH (Atherothrombosis Intervention in Metabolic Syndrome With Low HDL/High Triglycerides) and HPS2-THRIVE (Heart Protection Study 2-Treatment of HDL to Reduce the Incidence of Vascular Events) - delivered some disappointing results, leading to the conclusion that no further benefit (decreased parameters of cardiovascular risk) is achieved by adding niacin to existing statin therapy in patients with high cardiovascular risk. Moreover, in these studies, several adverse effects of the treatment were observed; therefore, niacin treatment for hypolipidemias is not recommended.

Nabumetone and 6-MNA Pharmacokinetics, Assessment of Intrasubject Variability and Gender Effect.

In this open-label, laboratory-blinded, 2-way single dose study in 24 volunteers of both sexes we found that (1) nabumetone reaches mean Cmax ± SD of 0.56 ± 0.20 mg·L at mean tmax of 8.

[Effect of liver cirrhosis on pharmacokinetics and pharmacodynamics of drugs].

Metabolic liver functions are significantly involved in the total clearance of a number of drugs. In liver cirrhosis the reduced drug elimination is a result of the blood flow through the liver, hepatocytes function and volume of hepatic tissue. Pharmacokinetic and pharmacodynamic changes depend on the nature and degree of hepatic impairment and on the characteristics of the dosed drug.

Impact of MDR1 genetic polymorphisms on postoperative piritramide analgesia.

Objectives: The aim of prospective study was to evaluate the therapeutic efficacy of piritramide in patients after removal of parathyroid glands in relation to MDR1 genotype. In the treatment of moderate acute postoperative pain, piritramide plays a major role. It is difficult to predict its optimal therapeutic efficacy and tolerability in individual patients.

Lipid-lowering effect of fluvastatin in relation to cytochrome P450 2C9 variant alleles frequently distributed in the Czech population.

Background: CYP2C9*3 allele has been reported to correlate with increased plasma concentration of fluvastatin active form in healthy volunteers. We analyzed the correlation between the CYP2C9 genotype and cholesterol-lowering effect of fluvastatin in human hypercholesterolemic patients.

Material/methods: The study was prospective, without any interventions to standard procedures of hypolipidemic treatment.

Tramadol efficacy in patients with postoperative pain in relation to CYP2D6 and MDR1 polymorphisms.

Objectives: The aim of our study was to evaluate impact of CYP2D6 and MDR1 polymorphisms on the analgesic efficacy of tramadol in patients after a knee arthroscopy.

Background: Pharmacokinetics of tramadol and its metabolites is stereoselective and displays high interindividual variability correlating with polymorphic CYP2D6 in the population. Available data provide controversial results regarding the analgesic efficacy of tramadol in subjects with different CYP2D6 genotypes.

Genetic polymorphisms of CYP2C8 in the Czech Republic.

Aim: CYP2C8 represents 7% of the hepatic cytochrome system and metabolizes around 5% of drugs in phase I processes. It also plays a significant role in metabolism of endogenous compounds. More than 20 single-nucleotide polymorphisms (SNPs) have been noted, mainly in exons 3, 5, and 8.

[Our experience with maraviroc treatment in HIV positive patients].

Unlabelled: BACKGROUND; Although antiretroviral therapy has changed the clinical course of HIV infection, AIDS remains an incurable disease. Virus entry inhibitors, including maraviroc as the only registered representative of the class, represent a newly emerged group of anti-retrovirals with novel mechanism of action. The primary endpoint is to evaluate the clinical efficacy parameter of maraviroc by measuring viral load at the end of the 4 week treatment period.

Pupillometry in healthy volunteers as a biomarker of tramadol efficacy.

What Is Known And Objective: The opioid effect of tramadol, which can be detected by pupillary response, is predominantly mediated by the O-demethylated metabolite, formed via CYP2D6. This study was designed to evaluate the effects of tramadol using different parameters of pupillometry as biomarkers.

Methods: Sixty-nine healthy volunteers received tramadol hydrochloride drops orally at a dose of 0·7 mg/kg.

[Determination of nabumetone and 6-methoxy-2-naphthylacetic acid in plasma using HPLC with UV and MS detection].

The study aimed to establish and validate an analytical method for the determination of nabumetone and 6-methoxy-2-naphthylacetic acid (6-MNA) in human plasma after a single therapeutic dose of the drug. Two methods based on HPLC with UV and MS detection were compared. Optimal results in sample preparation were achieved using solid phase extraction.

[Infrared pupilometry as a biomarker of drug effects].

Background: Measurement of the size of the pupil is used as a biomarker of drug efficacy, assessing mainly their effect on the central nervous system. The aim of our study was to evaluate sensitivity of various pupilometric parameters as biomarkers of widely used opioid analgesic drug tramadol.

Methods And Results: Pharmacodynamic action of tramadol drops given orally in standardized dose of 0.

Cytochrome P450 2D6 polymorphism and drug utilization in patients with oral lichen planus.

Objective: Oral lichen planus (OLP) is one of the commonest diseases of the oral mucosa. The etiology of the disease is unknown. Our goal was to determine frequencies of functionally important alleles which determine the metabolic rate (phenotype) of individuals with OLP and to compare drug utilization, with focus on CYP2D6, with that of a control group.

The role of diclofenac and piritramide in the management of acute postoperative pain in hernioplasty.

Objectives: The aim of the study was to compare the effects of diclofenac and piritramide in acute postoperative pain after hernioplasty.

Background: In the treatment of moderate acute postoperative pain, non-steroidal anti-inflammatory drugs and opioids play the major role. The data on safety and effect of analgesia based on opioid and non-opioid drugs are still a controversial topic.

Enantiomeric determination of tramadol and O-desmethyltramadol in human plasma by fast liquid chromatographic technique coupled with mass spectrometric detection.

A rapid and sensitive method using liquid chromatography-tandem mass spectrometry (LC-MS/MS) for enantiomeric determination of tramadol and its primary phase metabolite O-desmethyltramadol in human plasma has been developed. Tramadol hydrochloride-(13)C, d(3), was used as an isotopic labeled internal standard for quantification. The method involves a simple solid phase extraction.

Human urinary metabolomic profile of PPARalpha induced fatty acid beta-oxidation.

Activation of the peroxisome proliferator-activated receptor alpha (PPARalpha) is associated with increased fatty acid catabolism and is commonly targeted for the treatment of hyperlipidemia. To identify latent, endogenous biomarkers of PPARalpha activation and hence increased fatty acid beta-oxidation, healthy human volunteers were given fenofibrate orally for 2 weeks and their urine was profiled by UPLC-QTOFMS. Biomarkers identified by the machine learning algorithm random forests included significant depletion by day 14 of both pantothenic acid (>5-fold) and acetylcarnitine (>20-fold), observations that are consistent with known targets of PPARalpha including pantothenate kinase and genes encoding proteins involved in the transport and synthesis of acylcarnitines.