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At least 37 records · Page 2Linked to original sources
PubMedDate not supplied

[Comparative antiallergic and anti-inflammatory action of F1865, mepyramine maleate, desonide and disodium cromoglycate after cutaneous administration].

The actions of F 1865 (ethyl 4' methoxy 4 phenyl thiazolyl 2 oxamate), an inhibitor of the release of histamine from mast cell, desonide, a corticosteroid, mepyramine maleate, an anti-H1 antihistaminic, and disodium cromoglycate were compared after cutaneous application in various experimental models of allergy and inflammation. F 1865 decreased IgE- and IgG-dependent passive cutaneous anaphylaxis in rats at doses having no effect on histamine- and serotonin-induced capillary permeability. Disodium cromoglycate showed the same activity spectrum, but its action was only found after intradermal application. The reduction of cutaneous anaphylaxis by desonide was found parallel to its inhibition of histamine effects, and to a lesser extent of serotonin effects. In the case of mepyramine, the antiallergic effect may be explained by its antihistaminic action. Desonide was highly active on cantharidin-induced non-immune inflammation and on non-immune and delayed hypersensitivity reactions induced by picryl chloride in mouse ear. Although far less active than the corticosteroid, F 1865, mepyramine and disodium cromoglycate did reduce the three types of reactions in mice. This evidenced a part played by histamine in such inflammations. Then it is likely that the inhibition of histamine release by F 1865 plays an important part in the effect of the compound observed in the various inflammations studied. However we cannot exclude actions against other mediators involved in these reactions.

Administration, Topical↗
PubMed1990

[Cutaneous administration of liposomes--a review of the literature with special reference to findings from keratinocyte cultures, animal experiments and clinical studies].

Recent findings regarding the topical application of liposomes are reviewed under 3 headings: (1) keratinocyte cultures, (2) animal experiments, and (3) clinical studies. Under cell culturing conditions, liposomes are able to get into direct contact with living keratinocytes--just as in cutaneous application when the barrier of the horny layer is missing (i.e. in case of superficial skin defects or unkeratinized mucocutaneoaus surfaces). Under these circumstances, keratinocytes show liposomal alterations of the cell structure, proliferation, and lipid fluidity. Animal experiments and clinical studies have pointed out that, in comparison with a conventional formulation, a liposomal way of application can enhance the penetration of various substances as well as their toposelective enrichment in the skin, since the dermal-vascular absorption is diminished.

Animals↗
PubMedDate not supplied

Cutaneous administration of nitroglycerin: a review.

Chronic administration of nitroglycerin may have important therapeutic effects in patients with angina, acute myocardial infarction, congestive heart failure and peripheral vascular disease. Because of unpredictable oral absorption and short duration of action, topical preparations provide an alternative mode of administration. New controlled release transdermal preparations appear to produce constant plasma nitroglycerin concentrations of 0.2-0.3 ng/ml that persist for up to 24 hours. Additional clinical trials of the therapeutic response to this drug form are necessary, particularly in regard to the relative hemodynamic efficacy and side-effect profile of sustained vs. fluctuating plasma nitroglycerin concentrations.

Administration, Topical↗
PubMed1989

The generation of antigen-specific, major histocompatibility complex-restricted cytotoxic T lymphocytes of the CD4+ phenotype. Enhancement by the cutaneous administration of interleukin 2.

We have examined an in vitro system in which PBMC from purified protein derivative (PPD)-sensitized patients generate CTL after in vitro activation with antigen. These cells selectively destroy mycobacterial antigen PPD-pulsed monocyte targets. These CTL are of the CD4+ phenotype and exhibit MHC class II restriction. After exposure to antigen these cells require 5-7 d for maximal development, whereas, a separate antigen-independent population is generated within 3-4 d. CD8+ cells are poorly, if not at all, cytotoxic under similar conditions. Cells with properties of the NK and LAK lineage are also present in these cultures and kill other specific targets. Human rIL-2 was injected into the skin of lepromatous patients at 10-micrograms doses, given at 48-h intervals, for three doses. Peripheral blood cells obtained 8-14 d after the initiation of IL-2 injection demonstrated enhanced antigen-dependent destruction of monocyte targets. The efficacy of antigen-dependent and -independent populations and their amplification by IL-2-dependent mechanisms is discussed in terms of the local destruction of parasitized macrophages and the subsequent disposal of M. leprae.

Antigens, Bacterial↗
PubMedDate not supplied

Pharmacokinetics of cutaneous Sulconazole nitrate in the hairless rat: absorption, excretion, tissue concentrations.

After cutaneous application of radioactive solutions of Sulconazole nitrate in the hairless rat, the total absorption of the substance by the skin, estimated from the sum of the cumulative urinary and fecal excretions over 96 h, was 2.4% of the dose administered. The elimination reached a maximum between 6 and 24 h and was virtually complete after 96 h. The excretion was almost equally distributed between the urine and the feces, which corresponds to an intense elimination via the biliary tract. The quantities present in the stratum corneum, epidermis and dermis at the end of the period of contact constituted another estimation of the total absorption of the substance which confirmed the previous estimation (3.6% of the dose). The measurement of the concentrations of Sulconazole and its metabolites in the various layers of the skin revealed a high affinity of the substance for the stratum corneum, where it remained present in large quantities for more than 48 h. This affinity is due to the very intense lipophilia of the molecule. The concentrations in the other tissues were inversely proportional to the distance from the surface of the skin and were virtually nil in the circulating blood. These results suggest the absence of risk of systemic effects after cutaneous administration of Sulconazole and support the recommended therapeutic protocol in man (one administration per day).

Administration, Cutaneous↗
PubMedDate not supplied

Formulation study and anti-inflammatory efficacy of topical semi-solids containing a nitro ester of flurbiprofen.

A new nitro-oxybutylester of flurbiprofen (NO-FP) is a promising anti-inflammatory drug in the treatment of dermatological disorders, and the feasibility of its cutaneous administration was evaluated. Four different semi-solid formulations were evaluated in order to assess the influence of the composition on the drug amount retained in the stratum corneum and epidermis (SCE). The lipophilic ointment induced the highest NO-FP amount retained in the SCE and, therefore, skin permeation enhancers (Transcutol), Lauroglycol), oleic acid and isopropyl myristate) were added to this formulation. The in vitro NO-FP amounts retained in the SCE were correlated with the solubility parameters, and a good linear correlation was found (r(2) = 0.925). The formulation of the lipophilic ointment was optimized, and the activity of this preparation was verified in methyl-nicotinate-induced contact urticaria and UV-induced erythema obtaining good results in terms of efficacy and safety.

Administration, Cutaneous↗
PubMed1992

Bioavailability and metabolism of isosorbide dinitrate from a transdermal spray.

The plasma pharmacokinetics of isosorbide dinitrate (ISDN), isosorbide-2-nitrate (IS-2-N) and isosorbide-5-nitrate (IS-5-N) were investigated in 12 healthy volunteers after a single cutaneous administration of 60 mg ISDN (CAS 87-33-2) in the form of a solution sprayed onto the skin (TD Spray Iso Mack), in comparison with an intravenous infusion of 5 mg ISDN. After the intravenous dose, the apparent steady state volume of ISDN distribution came to 179.9 l, total body clearance was 3.14 l min-1, and terminal half-life was 79 min, on average. The transdermal absorption resulted in an average peak plasma concentration of 6.9 ng ISDN ml-1 at 5 h after the administration. ISDN concentrations between 1 and 5 ng ml-1 were maintained over at least 15 h. On average, 16.5% of the topically applied ISDN reached the systemic circulation. Total variations in Cmax (CV = 47.9%) and AUC (CV = 36.0%) of transdermal ISDN were similar to those usually observed after oral ISDN.

Administration, Cutaneous↗
PubMed1991

[Immunotherapy with cutaneous dinitrochlorobenzene in papillomavirus infection of the cervix uteri].

The authors report their experience after the treatment of 30 patients with condyloma acuminatum of endocervix who were diagnosed by cytology (Papanicolaou), colposcopy and biopsy. The women were treated with dinitrochlorobenzene applied on the arm's skin. The sensitization procedure with DNCB, with a cutaneous administration every fifteen days, is described. Some aspects of the HPV infection, the increased number of patients suffering this viral infection and the concern about the relationship between cervical cancer and types 16 and 18 HPV are described. Basic concepts in regard of immunological treatment are discussed. The results were = eighty seven (87%) per cent of the 30 women were fully healed.

Administration, Cutaneous↗
PubMed2006

Angioedema and maculopapular eruptions associated with carbamazepine administration.

Cutaneous rashes and eruptions can be caused by many medications, including carbamazepine. The presentation can be varied depending on severity. Cutaneous eruptions occur in 3% of individuals administered carbamazepine. Angioedema, a rare side effect of carbamazepine, involves vascular leakage in dermis and subcutis mediated by immunoglobulin E and/or bradykinins. Angioedema is more common in females and in the third decade of life. We report the case of a 27-year-old Indian woman who developed maculopapular rash and angioedema secondary to carbamazepine administration. The patient responded successfully to withdrawal of the drug and treatment with antihistamines. Due to the potentially life-threatening complications of this condition and the increasing use of anticonvulsants in the treatment of mood disorders, psychiatrists must be aware of the diagnosis and treatment of this condition.

Adult↗
PubMed1993

Evaluation of the teratogenic risk of cutaneously administered retinoids.

In current cutaneous retinoid therapy systemic exposure is low and the risk of teratogenesis appears to be limited. However, new indications, altered posologies and the introduction of new synthetic retinoids demand continuous assessment of the teratogenic risk. Teratogenicity testing of new substances in animals is only of value if accompanied by detailed pharmacokinetic analysis to establish the relationships between the levels of parent compound and metabolite in both maternal plasma and fetal tissues and teratogenic events. This information should be compared to the maximum of relevant pharmacokinetic data which can be ethically obtained in man or from human tissues. The presence or absence of teratogenic effects following cutaneous administration of retinoids in animals has, as such, little direct bearing on the risk in man. Two special cases exist where teratogenic risk can be evaluated directly in man without reference to animal studies. The first concerns substances whose teratogenic potential has been established in man by other routes of administration permitting a comparison with the cutaneous route on a pharmacokinetic basis. The second concerns the cutaneous administration of endogenously occurring substances and their eventual disturbance of systemic retinoid equilibrium.

Administration, Topical↗