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At least 793 records · Page 44Linked to original sources
PubMed2006

Treating itch in psoriasis.

Itch is an important, but underestimated symptom in psoriasis. Many therapies are available for pruritus; however, few are effective for psoriatic itch. Antipruritic therapies that are potentially effective in psoriasis include coal tar products, topical corticosteroids, topical salicylates, menthol and pramoxine, capsaicin, phototherapy, vitamin D analogs, topical immunomodulators, methotrexate, oral mirtazapine, and biologics. Using these therapies can benefit psoriasis patients in the outpatient clinical setting.

Administration, Cutaneous↗
PubMed1991

Combined effect of cyclic monoterpenes and ethanol on percutaneous absorption of diclofenac sodium.

The combined effect of cyclic monoterpenes and ethanol on the percutaneous absorption of diclofenac sodium (DFS) from gel ointments was investigated in vivo in rats. The enhancing activity of terpenes was significantly affected by the concentration of ethanol formulated in the gel ointments. At a lower concentration of ethanol (20%), 1,8-cineole was observed to be the most effective. On the other hand, d-limonene showed strong activity when the large amount of ethanol was formulated (40%). A synergistic effect between terpenes and ethanol on the percutaneous absorption of DFS was significantly observed in cases of 1,8-cineole and l-menthol using an analysis of variance (ANOVA). When the diclofenac (DF) free form was formulated in gel ointment, the percutaneous absorption was significantly reduced. The reduction of the percutaneous absorption was closely related to the decrease in pH of the gel ointment owing to the free form of DF which was formulated.

Analysis of Variance↗
PubMed1990

Percutaneous absorption enhancing effect and skin irritation of monocyclic monoterpenes.

The percutaneous absorption promoting effect and skin irritancy of cyclic monoterpenes were investigated in rats and with rabbits, respectively. Ketoprofen (KPF) was applied to rat skin in gel ointments containing various cyclic monoterpenes. Plasma concentrations of KPF markedly increased with the addition of the hydrocarbons of cyclic monoterpenes such as trans-p-menthane and d-limonene, whereas no significant enhancing effect was observed in the cases of other terpenes such as l-menthol, l-menthone and 1,8-cineole. The lipophilicity of the enhancers seems the important factor in promoting penetration of KPF through the skin. The enhancing activity of d-limonene was found to be much higher than that of Azone. Irritancy of the hydrocarbons of cyclic monoterpenes and Azone to the skin was evaluated using a Draize scoring method with rabbits. No change was observed on the skin surface when ethanol containing 2% of the hydrocarbons was applied to the dorsal skin, though a slight edema and erythema were observed in the case of Azone. In particular, an obvious difference was observed in the erythema formation between Azone and the hydrocarbons of cyclic monoterpenes.

Animals↗
PubMed1990

[Etiology of alveolitis and its therapy with indomethacin].

The local antiphlogistic therapy of alveolitis was founded from the importance of inflammation in the etiology. Indomethacin (3% age oily solution) was analysed on their effectiveness. In the control group was treated with chlorphenol-camphor-menthol-solution (ChKM) with addition of procain substance on the gauze strip. Indomethacin is significantly more active with regard to effectiveness, decrease of pain intensity and achievement of painlessness. The local therapy of alveolitis, is free of risk with solution out of Metindol--vials under dosage up to 6 milligram indomethacin substance.

Adult↗
PubMed1987

Drug-induced Ca2+ release from isolated sarcoplasmic reticulum. II. Releases involving a Ca2+-induced Ca2+ release channel.

Calcium ions that have been preloaded into isolated sarcoplasmic reticulum subfractions in the presence of ATP and pyrophosphate may be released upon addition of a large number of diverse pharmacologic substances. We report here that not only caffeine, but also Ca2+ ions, thymol, quercetin, menthol, halothane, chloroform, 1-ethyl-2-methylbenzimidazole, ryanodine, tetraphenylboron, ketoconazole, miconazole, clotrimazole, W-7, doxorubicin, 5,5'-dithiobis-(2-nitrobenzoic acid), p-chloromercuribenzoic acid, and low concentrations of Ag+ induce Ca2+ release from such triadic sarcoplasmic reticulum. All these drugs induce increased undirectional Ca2+ efflux. We believe all these drug-induced Ca2+ releases are mediated by Ca2+ efflux through the same ion channel since these releases are all greatly attenuated when light sarcoplasmic reticulum is substituted for triads and are even more pronounced when transverse tubule-free terminal cisternae are substituted for triads, and all these forms of drug-induced Ca2+ release are inhibited by submicromolar concentrations of ruthenium red, and by submillimolar concentrations of tetracaine, 9-aminoacridine, and Ba2+, yet they are not affected by nifedipine even at a concentration of 50 microM.

Animals↗
PubMed1989

Drug metabolism in drug-induced liver diseases: pathogenetic role of active metabolites.

Three cases with drug-induced liver diseases (hepatitis caused by hydralasine, steatosis caused by methimazole, choletasis caused by birth control pill) were investigated with respect to their drug metabolising ability. Clinical diagnoses were based on the exclusion of other pathogenetic factors, on histological findings of liver biopsy specimens and on the clinical chemical tests. Investigation of biotransforming ability was carried out using test materials (menthol loading, antipyrine, sulfadimidine, caffeine, indocyanine green kinetics) and measurement of D-glucaric acid excretion. In all cases the results show a defective capacity in some respect of drug metabolism. Possible pathogenetic role of reactive metabolites is discussed in the pathomechanism of genesis of drug-induced liver diseases.

Adult↗
PubMed1988

Examination of the substrate specificity of cloned rat kidney phenol UDP-glucuronyltransferase expressed in COS-7 cells.

A cDNA encoding a rat kidney UDP-glucuronyltransferase (UDPGT) was subcloned into the vector pKCRH2. Expression driven by the SV40 promoter produced enzymatically active UDPGT in COS-7 cells cultured in vitro. The appearance of enzyme activity was associated with an immunodetectable glycosylated UDPGT protein (Mr 53 kDa) in the cells. The expressed enzyme rapidly catalyzed the glucuronidation of 1-naphthol, 4-methylumbelliferone, and 4-nitrophenol. Studies using more than 20 compounds showed that the cloned UDPGT exhibited a restricted specificity towards planar phenols. A crude description of the molecular conformation of 4-alkylphenols accepted within the active site of the protein was obtained. The glucuronidation of morphine, thymol, menthol, testosterone, androsterone, or estrone was not catalyzed by this enzyme.

Animals↗
PubMed1986

Disorders of biotransformation during the progression of alcoholic liver disease.

Biotransformation capacity was investigated in patients with various degrees of alcoholic liver damage. Aim of the investigation was to study the impairment of biotransformating ability during progression of liver damage. Four groups of patients with various liver diseases (alcoholic fatty liver, chronic persistent hepatitis, chronic active hepatitis, alcoholic cirrhosis) and two groups as controls were studied. The investigations were carried out with exogenous test substances (antipyrine, menthol and sulphadimidine) and by determination of D-glucaric acid excretion. It has been concluded that the depression of biotransformating ability in patients with alcoholic liver diseases is progressing during development of diseases. The changes in various metabolic pathways are different, and they seem to be more marked in the first phase of biotransformation than in the second phases.

Biotransformation↗
PubMed1987

Binding of 3H-estradiol-17 beta-(beta-D-glucuronide), a cholestatic organic anion, to rat liver plasma membranes. Evidence consonant with identification of organic anion carriers.

The binding of 3H-estradiol-17 beta(beta-D-glucuronide) (3H-E2 17G), a cholestatic organic anion, was examined in rat liver plasma membranes, and two saturable, specific binding sites were identified. The binding parameters are Kd1 = 3.9 X 10(-7) M, Bmax1 = 69 pmol/mg of protein; Kd2 = 4.90 X 10(-6) M, Bmax2 = 495 pmol/mg of protein according to Scatchard analysis of equilibrium experiments. Kinetic dissociation experiments showed that 3H-E2 17G binding was reversible and revealed two components. The dissociation rate constants did not vary with the method of dilution of radioligand, i.e., by "infinite" volume, or excess unlabeled ligand, ruling out the possibility of cooperativity. The rate of association of 3H-E2 17G binding was very rapid, so that maximal binding was reached within 15 sec at 4 degrees. Na+ was not required for binding and binding was not decreased in the presence of high osmolarity buffer (125 mM sucrose), indicating that transport into vesicles was not involved. The ability of a series of compounds to inhibit the binding of 3H-E2 17G was also examined. Taurocholate, cholate, taurodehydrocholate, and testosterone glucuronide were identified as ligands selective for the high affinity site (site 1). The A- and D-ring glucuronide conjugates of estradiol and estriol, bromosulfophthalein, dibromosulfophthalein, and the glucuronide conjugates of phenolphthalein, 4-methylumbelliferone, and menthol inhibited binding of 3H-E2 17G to both sites. Morphine glucuronide, estradiol, and glucuronic acid did not inhibit binding to either site. The substrate specificities of binding to the low affinity site (site 2) are consistent with data characterizing the transport of these substrates in hepatocytes and supports the postulate that site 2 represents a non-bile acid organic anion carrier. Site 1 is postulated to represent a carrier shared by the bile acids and non-bile acid organic anions.

Animals↗
PubMed1983

Postsynaptic effects of magnesium and calcium at the mouse neuromuscular junction.

The effects of elevated magnesium and calcium concentrations on height and time course of miniature endplate currents (MEPCs) at the mouse neuromuscular junction were studied. With both ions, MEPC height was decreased; the rate of decay of MEPCs was reduced in high magnesium and was unchanged in high calcium. Raised Mg2+ or Ca2+ both acted to modify the effects on MEPC time course of procaine, scopolamine, atropine, lidocaine, and quinidine, all of which act to cause biphasic decay of MEPCs in a manner consistent with reversible "plugging" of endplate channels, with rate constants for blocking and unblocking that are sensitive to postsynaptic transmembrane potential. Both the blocking and unblocking rate constants were decreased by increasing divalent ion concentration. No such reduction of rate constants was observed using menthol or pentobarbital, which appear to block channels in a voltage-independent manner. It is concluded that the divalent ions act to alter the channel environment via interactions with charged groups in or near the endplate channels.

Anesthetics, Local↗
PubMedDate not supplied

Investigation of biotransformation capacity in patients with chronic liver diseases by pharmacokinetic methods: experimental trials.

The drug metabolizing capacity of patients with liver disease varies with the characteristics and the state of the disease. The aim of our studies on patients with various chronic liver diseases was to get information about the rational dosage for these patients. Our method in the first phase was antipyrine kinetics (hydroxylation), in the second phase sulfadimidine kinetics (acetylation) and menthol loading (glucuronidation). The induced state was investigated by D-glucaric acid excretion. Experimental trials: 1) comparison of groups of patients with moderate and severe liver diseases with each other, or with the normal control (two sample t test); 2) comparison of various groups of patients with each other and with the normal control (variance analysis); 3) research of potential correlation between the kinetic and biochemical parameters (correlation analysis); 4) reclassification studies with the use of kinetic and biochemical parameters (discrimination analysis). We discuss the practical advantage of the various experimental trials. The most important conclusion is that the reclassification by discrimination analysis gives important data to the economic planning of experiments.

Antipyrine↗
PubMed1980

Protective and defensive airway reflexes in premature infants.

The incidence of respiratory reactions to stimulation of the nasal and propharyngeal mucose was studied in 44 newborn premature infants. The inhalation of menthol fumes or the administration of drops of Mukoseptonex to the nasal mucosa caused transient respiratory arrest or a drop in the respiration rate. The heart rate rose during chemical stimulation of the nasal mucosa, possibly in association with a general arousal reaction. Mechanical stimulation of the nasal mucosal with a nylon fibre elicited an expulsive reaction in 95% of the cases. As distinct from experimental animals, sneezing was not preceded by a deep initial inspiration. Stimulation of the oropharyngeal region produced transient apnoea in 24.5% of the cases, in 18% expiratory reactions reminiscent of the expiration reflex, in 33% independent, intensive inspiratory reactions and in 24.5% cough. Cough from both the oropharyngeal and the laryngeal region had a pronounced inspiratory component. Independent inspiratory reactions may to some extent be co-responsible for the high incidence of aspirations in the neonatal period.

Cough↗
PubMed1984

[Excitable actions of counterirritants on cutaneous sensation].

Studies were conducted on the actions of counterirritants on sensory receptors in the skin and spinal monosynaptic reflex. Nerve discharges in the cat's saphenous nerve were promoted by the external application of menthol and nonylic vanillyl amide ( NVA ) dissolved in ethanol on the receptive field. When plasters containing counterirritants were externally applied on the receptive field, marked activation was recognized in touch-pressure-pin prick fibers immediately after the application as seen with plaster without drugs, but significantly high activity was maintained thereafter, and the increased firing rate in touch-pressure-pin prick-cold fibers lasted for 60 min. The activity of pressure-pin prick fibers was increased with the lapse of time and warm fibers was not influenced. Effects on activities of spinal dorsal horn cells were almost similar to the changes in activities of primary afferent from the skin. Monosynaptic reflex elicited by stimulation on the medial gastrocnemius nerve was weekly inhibited (significantly different from control at P less than 0.05), by the external application of plasters, and motoneuron receiving IPSP from the skin lightly touched on was observed. These findings suggest that the receptors activated with counterirritants were thought to be as follows: A delta and C polymodal nociceptors, A delta and C cold nociceptors, and slow adapting cutaneous mechanoreceptors. The cutaneous mechanoreceptors were also activated by the application of plasters. The volley from sensory nerve excited with counterirritants was thought to cause a suppression on the spinal monosynaptic reflex resulting from an inhibition on the motoneuron.

Administration, Topical↗
PubMed1994

Evaluation of the efficacy and tolerability of a new locally acting preparation of flurbiprofen in scapulohumeral periarthritis.

This randomised, double-blind, placebo-controlled, parallel-group trial was carried out to assess the efficacy and tolerability of a new, locally acting, transcutaneous flurbiprofen preparation (flurbiprofen LATTM, Boots Company PLC) in the treatment of scapulohumeral periarthritis. The new preparation consists of a nonwoven polyester patch supporting a mentholated formulation containing flurbiprofen 40 mg. Eighty patients suffering from the acute, painful phase of scapulohumeral periarthritis entered the trial, three of which failed to provide follow-up data. Each patient applied one patch every 12 hours for the 14 day trial period. Efficacy was assessed in terms of reduction of pain, improvement in shoulder movement and overall clinical assessment of the severity of the condition after treatment. Statistically significant improvements from baseline were observed in both treatment groups, with a constant overall trend in favour of flurbiprofen. The differences between the two treatment groups, however, did not reach statistical significance.

Administration, Cutaneous↗
PubMed1996

Remedies for common family ailments: 10. Nasal decongestants.

Nasal congestion and sinusitis are common effects of cold and flu viruses. One treatment for nasal congestion is oral doses of vasoconstrictors such as ephedrine which mimic the action of the sympathetic nervous system. Care should be taken before these are prescribed or recommended as these drugs are contraindicated in patients on certain drugs or with certain conditions. Vasoconstrictors can also be given as nasal drops or sprays but for a limited period to avoid rebound congestion. Aromatic volatile oils, e.g. menthol, eucalyptus, can be given as rubs or inhalants (see manufacturers' instructions for use with young children).

Common Cold↗
PubMed1996

Unusual cause of seizure.

INTRODUCTION: This case report of camphor ingestion in a 15-month-old child illustrates the potential toxicity of a common household product. Details of the patient presentation are reported along with a review of the literature. METHODS: Patient information was collected using the records of Poison Control, the Emergency Department, and the Health Records at the Hospital for Sick Children in Toronto, Ontario, Canada. A comprehensive review of the literature was conducted using the MEDLINE database for the time period 1966 to April 1995. DISCUSSION: Oral ingestion of camphor is unusual, given that these products have both unpleasant taste and texture. This patient ingested 70 ml of an over-the-counter medicated ointment containing 4.73% camphor, 2.6% menthol, and 1.2% eucalyptus oil. While the concentration of camphor in this product is low, an estimated 280 mg/kg of camphor was consumed. With significant ingestion of camphor (> 50 mg/kg), neurologic toxicity is common. In this patient, prolonged generalized tonic-clonic seizure activity was noted approximately two hours post single acute ingestion of camphor. This delay in onset of seizure activity is atypical, as seizures have previously been noted to occur in the 90 minutes following ingestion. CONCLUSION: Readily available medicated ointments containing camphor have potential for serious or fatal consequences when ingested by children.

Anti-Infective Agents, Local↗
PubMed1997

Coughs and colds: advising on what to take.

Take special care when recommending a product to people with a pre-existing medical condition (e.g., high blood pressure, stomach problems, asthma). It is safer to advise them to consult their pharmacist or doctor if there is a possibility of adverse drug interaction. Be aware of the possibility of overdosage (e.g., some patients take a large number of remedies simultaneously and may unwittingly be taking too much paracetamol, aspirin or ibuprofen). Green or yellow sputum suggests the patient has a bacterial infection in addition to a cold, and consulting a doctor is advisable. Enquire whether a cough is productive ("loose" or "chesty") or non-productive "dry, "tricky" or "irritating") so that you can advise on appropriate product. Productive coughs are helped by expectorants. Dry coughs are helped by suppressants. Cough preparations often contain antihistamine which may cause drowsiness, so be aware of this when advising a patient. For young children a paediatric formulation is advisable. Many of the main brands of cough and cold medicines have infant or junior varieties. Vapour products, often using substances like menthol placed on a tissue near the child but out of reach, can be very effective for blocked noses. Sugar-free preparations should be used for children (and adults) where possible, to avoid the risk of tooth decay. If patients suffer from repeated colds and coughs, and complain of feeling "run down", questioning may reveal that they have a poor diet. In that case, recommending a vitamin supplement or tonic and advice on a healthier diet may be appropriate. A persistent cough should receive medical attention.

Adult↗
PubMed1997

Glucuronidation of opioids, carboxylic acid-containing drugs, and hydroxylated xenobiotics catalyzed by expressed monkey UDP-glucuronosyltransferase 2B9 protein.

UDP-glucuronosyltransferase (UGT) 2B9, isolated from a cynomolgus monkey liver cDNA library, is 89% identical to human UGT2B7 in primary amino acid sequence, and the two expressed enzymes were previously shown to catalyze the glucuronidation of many common endogenous substrates. The purpose of the present study was to characterize the reactivity of expressed UGT2B9 with important therapeutic agents and other xenobiotics. UGT2B9, stably expressed in human embryonic kidney 293 cells, catalyzes the 3-O- and 6-O-glucuronidation of morphine and the 6-O-glucuronidation of codeine. A number of other morphinan (e.g. naloxone, naltrexone, and nalorphine) and oripavine (e.g. buprenorphine) derivatives are substrates for this enzyme. In general, morphinan derivatives are glucuronidated at higher rates, compared with oripavines; however, glucuronidation efficiency values (Vmax/KM) for the compounds are similar. Stably expressed UGT2B9 also catalyzes the glucuronidation of profen nonsteroidal anti-inflammatory drugs, fibrate hypolipidemic agents, and straight-chain fatty acids at the carboxylic acid moiety. Monoterpenoid alcohols and propanolol are glucuronidated at aliphatic hydroxyl positions. Expressed UGT2B9 exhibits enantioselective glucuronidation for (R/S)-ibuprofen, (R/S)-propanolol, and (+)/(-)-menthol. The data suggest that monkey UGT2B9 and human UGT2B7 are functionally similar.

Animals↗