Nonsteroidal anti-inflammatory drugs: cyclooxygenase 2 inhibitors

OBJETIVO: Analisar os antiinflamatórios não-hormonais (AINH) inibidores seletivos da Cox 2 quanto ao mecanismo de ação, principais indicações, posologia e efeitos adversos mais comuns. FONTES DOS DADOS: MEDLINE e LILACS, sites da Food and Drug Administration (FDA) e da Agência Nacional de Vigilância Sanitária (ANVISA). Foram selecionados os artigos mais importantes, com destaque para as publicações dos últimos 5 anos. SíNTESE DOS DADOS: As principais indicações dos AINH são o controle da dor e da inflamação aguda e crônica. Não existem evidências que demonstrem maior efetividade de um AINH sobre outro. Até a presente data, nenhum inibidor da Cox2 foi liberado para uso na faixa etária pediátrica. Apenas o meloxicam e o etoricoxibe podem ser prescritos para adolescentes (13 e 16 anos, respectivamente). Os inibidores seletivos da Cox 2 são indicados em pacientes com efeitos adversos comprovadamente relacionados aos AINH não seletivos. Em alguns casos de alergia à aspirina, os Cox 2 seletivos podem ser prescritos, mas seu uso deve ser cuidadoso. Os principais efeitos adversos incluem os cardiovasculares e os fenômenos trombóticos. CONCLUSÕES: Os inibidores seletivos da Cox 2 são medicamentos que vêm sendo utilizados em algumas situações clínicas bem determinadas e podem oferecer algumas vantagens com relação aos AINH não seletivos. No entanto, devido ao custo mais elevado e aos potenciais efeitos adversos cardiovasculares, seu emprego deve ser criterioso.

OBJECTIVE: To analyze selective COX 2 inhibitor nonsteroidal anti-inflammatory drugs (NSAID) in terms of their mechanism of action, principal indications, posology and most common adverse effects. SOURCES: MEDLINE and LILACS databases and Food and Drug Administration (FDA) and National Agency for Sanitary Vigilance (ANVISA - Agência Nacional de Vigilância Sanitária) websites. The most important articles were selected and preference was given to articles published within the last 5 years. SUMMARY OF THE FINDINGS: The principal indications for NSAID are for control of pain and acute and chronic inflammation. There is no overwhelming evidence that demonstrates the superiority of one NSAID over another in terms of effectiveness. To date none of the COX 2 inhibitors has been liberated for use in the pediatric age group. Only meloxicam and etoricoxib can be prescribed for adolescents (13 and 16 years, respectively). Selective COX 2 inhibitors are indicated for patients with adverse effects that have proven to be associated with nonselective NSAID use. Selective COX 2 inhibitors can be prescribed in some cases of allergy to aspirin, but they must be used with care. Principal adverse effects include cardiovascular events and thrombotic phenomena. CONCLUSIONS: Selective COX 2 inhibitors are medicines that have been used in certain well-defined clinical situations and which may offer certain advantages over nonselective NSAID. Nevertheless, taking into consideration the higher cost involved and the potential for adverse cardiovascular effects, they should be employed only in accordance with strict criteria.

Evaluation of E-721B, an indigenous herbal combination in experimental models of immediate hypersensitivity.

E-721B, an indigenous herbal combination was investigated for its usefulness in immediate hypersensitivity using different animal models. The drug inhibited the mast cell degranulation induced both by antigen and compound 48/80, the Schultz-Dale response in sensitized guinea pig ileum smooth muscle preparation and the production of precipitating antibodies in 50% of tested rats. It also inhibited the mast cell degranulation in passively sensitized rats indicating its suppressive action on production of reaginic antibody (IgE). However, the drug did not inhibit the 48 hours passive cutaneous anaphylaxis reaction in rats, indicating that a single dose of the drug does not have cromoglycate like properties. All the above results indicate the inhibitory effect of E-721B on immediate hypersensitive reactions such as asthma.

Pharmacodynamic bioequivalence: evaluation of different brands of terfenadine hydrochloride.

Terfenadine is a selective histamine H1 receptor antagonist which binds preferentially to peripheral receptors in vivo and is devoid of central nervous system depressant activity and thus has an improved adverse effect profile (1). Hence, terfenadine may be considered to be a first line agent in the treatment of allergic rhinitis and chronic urticaria. In man terfenadine is rapidly absorbed following a single oral dose and a peak terfenadine plasma concentration is reached within 1-2 hr after the drug administration (2). The present study was carried out to compare the bioequivalence of two terfenadine hydrochloride preparations marketed by Kopran Chem. Co. and Marrel Dow U.K. (Triludan) by evaluating their ability to inhibit the skin reaction to intradermally injected histamine (3).

Comparación de la eficacia y seguridad de loratadina en pacientes de 3 a 12 años con alergias crónicas de la piel / Effectiveness and security comparation of loratadine in patients from 3 to 12 years old with chronic allergies of the skin

Se realizó un estudio local, randomizado triple ciego, por grupos paralelos, de 14 días de duración comparativo entre Loratadina (5-10 mg), administrada una vez al día y Terfenadina (15-30 mg), administrada dos veces al día, en pacientes pediátricos entre 3 y 12 años de edad, con enfermedades alérgicas crónicas de la piel. Después de una semana de tratamiento, se observó una importante mejoría de los síntomas, siendo la Loratadina más efectiva que la Terfenadina. La mejoría fue más evidente durante la segunda semana de tratamiento. Los datos obtenidos mostraron que ambos medicamentos fueron seguros y bien tolerantes