MDMA e antidepressivos inibidores seletivos de recaptação de Serotonina

Portas da Percepção

hempadao 2 março, 2017

por Fernando Beserra

Um tópico que gera muitas dúvidas é a interação entre antidepressivos e MDMA. O tópico poderia parecer simples à primeira vista, mas não é. Inicialmente, é preciso compreender que existem algumas classes de antidepressivos, dentre as quais:

· Os antidepressivos tricíclicos (ADT), como a amitriptilina (Amytril), a clomipramina, a imipramina (Tofranil), a doxepina, dentre outros. Os ADT agem na inibição da recaptação da noradrenalina e da serotonina, o que aumenta a concentração destas monoaminas na fenda sináptica (espaço de ligação entre células nervosas). Há atualmente cautela com seu uso, pois pode provocar problemas cardíacos. Também, em uma classe semelhante, existem os tetracíclicos;

· Os mais atuais: inibidores seletivos de recaptação de serotonina (ISRS). A sigla em inglês SSRIs. Nesta classe encontramos a sertralina (Zoloft), a fluoxetina (Prozac), a paroxetina (Pondera, Paxil), o citalopram (Citalopram), dentre outros. De maneira geral, os ISRS produzem menos efeitos colaterais que os tricíclicos;

· Inibidores da monoamino-oxidase (IMAO), a exemplo da tranilcipromina (Parnate), da fenelzina (Nardir) e a isocarboxazida. A monoamino-oxidase (MAO) é enzima mitocrondial que tem a função de degradar monoaminas (deaminação oxidativa): dopamina, serotonina, adrenalina e noradrenalina, de forma a desativar o excesso destes compostos. Ela é encontrada em tecidos neurais e não-neurais, como o intestinal e o hepático (PORTAL EDUCAÇÃO, S/d). Os inibidores de MAO (IMAO), em sua atuação, ao inibirem o efeito degradador da MAO, resultam em aumento da quantidade de monoaminas no sistema nervoso;

Os efeitos do MDMA, no que concerne a elementos farmacocinética, podem ser divididos em três mecanismos neuroquímicos:

1. A inibição da recaptação da serotonina (5-hidroxitriptamina, 5HT), isto é, o MDMA provoca o bloqueio do retorno deste neurotransmissor, quando se encontra na fenda sináptica, à membrana pré-sináptica. Com este mecanismo, o neurotransmissor permanece na fenda sináptica e é provocado o aumento da serotonina no cérebro.

2. O MDMA provoca o aumento da liberação de 5HT;

3. O MDMA provoca o aumento da liberação de dopamina (MALBERG; BONSON, 2001), embora em menor medida do que seus efeitos na serotonina.

O enfoque do texto é na interação do MDMA com o ISRS e nos IMAOs. Os efeitos do MDMA na liberação de 5HT podem ser bloqueados por inibidores de recaptação da serotonina como o citalopram (LIECHTI e outros, 2000). Liechti e outros (2000) investigaram se o efeito do uso prévio de citalopram (40mg iv) reduziria os efeitos psicológicos de 1,5mg/kg de MDMA (uso oral) em voluntários saudáveis. O estudo contou com 16 participantes da pesquisa e adotou uma metodologia de duplo-cego com controle placebo (grupo experimental e grupo controle c/placebo). Os grupos foram os seguintes:

Pré-dose

Dose

Placebo

Placebo

Citalopram

Placebo

Placebo

MDMA

Citalopram

MDMA

Após os participantes chegarem no Hospital Universitário Psiquiátrico recebiam 40mg de citalopram em uma solução salina de 500ml ou placebo (solução salina) infundida por 90 minutos (330ml/h). Depois da remoção do cateter intravenoso recebiam MDMA (1,5ml/kg) ou placebo em capsulas para uso oral. Os participantes tiveram 4 sessões no total, com um lapso de 15 dias entre sessões (LIECHTI e outros, 2000).

Os efeitos psicológicos da dose de MDMA foram reduzidos significativamente com o uso prévio do citalopram. Destaca-se, nos resultados, que embora com efeitos menos proeminentes, o efeito foi prolongado nas sessões dos participantes que utilizaram o citalopram (LIECHTI e outros, 2000) para uma média de duração de 5 horas. Portanto, há indícios que MDMA + ISRS prolonga o efeito e reduz o impacto psicológico na experiência de uma mesma dose.

Em uma tabela presente no artigo de Liechti e outros (2000) pode-se ter mais clareza acerca desta inibição dos efeitos psicológicos do MDMA após o uso de um clássico ISRS, o citalopram. Em escalas de estados alterados de consciência, os efeitos oceânicos, típicos dos psicodélicos, foi menor quando o participante da pesquisa havia ingerido, anteriormente, o citalopram e bem menores quando não houve uso de MDMA. O mesmo ocorreu com os efeitos da dissolução do ego ansiosa e a chamada reestruturação visionária. Na escala abaixo é possível ter mais clareza sobre alguns dados da escala.

Nesta tabela vemos que em todos os escores o efeito do uso combinado (pré-uso de citalopram, seguido por MDMA) resultou em efeitos psicológicos menos pronunciados. Apesar disso, em outro gráfico, o mesmo artigo situa que o MDMA+Citalopram não reduziram, de forma significativa, a excitabilidade emocional e o aumento da sensitividade provocadas pelo MDMA sozinho.

Tal como as medicações ISRS, o MDMA também não deve ser utilizado em conjunto com IMAOs. O MDMA pode agir como um inibidor da monoamino oxidase (IMAO), mecanismo que já conhecem bem os pesquisadores e usuários da ayahuasca. No caso, como o MDMA já pode agir desta forma, o uso concomitante de outras substâncias que sejam IMAO podem levar ao quadro de crise hipertensiva, em especial com o IMAO A. Além disso, este uso conjunto pode provocar a síndrome serotoninérgica (SS). Este assunto ainda merece uma investigação mais pormenorizada. Mas por hoje, pode-se concluir com a redução dos efeitos psicológicos de ISRS + MDMA e com o risco acentuado/grave de interagir MDMA + IMAO.

Referências:

EROWID (Compiled by Erowid et al.). MDMA & SSRIs. 2005. Disponível em: <https://erowid.org/chemicals/mdma/mdma_info9.shtml>.

LIECHTI, M. E.; BAUMANN, C.; GAMMA, A.; VOLLENWEIDER, F. X. Acute psychological effects of 3-4, methylenedioxymethamphetamine (MDMA, “Ecstasy”) are attenuated by the serotonina uptake inhibitor Citalopram. Neuropsychopharmacology. v. 22, nº 5, 2000. p. 513-521. Disponível em: <http://www.nature.com/npp/journal/v22/n5/pdf/1395472a.pdf>.

Portal Educação. Curso de psicofarmacologia. Programa de Educação Continuada a Distância. s/d.

Mais sobre MDMA no Hempadão:

BESERRA, F. R. MDMA e neurotransmissores. Hempadão. 2016. Disponível em: <https://hempadao.com/mdma-e-neurotransmissores/>.

BESERRA, F. R. Testando as balas e os MDs. Hempadão. 2016. Disponível em: <https://hempadao.com/testando-as-balas-e-os-mds-portas-da-percepo/>.

BESERRA, F. R. PMA ou 4-MA: adulterações perigosas. Hempadão. 2016. Disponível em: <https://hempadao.com/pma-ou-4-ma-adulteraes-perigosas/>.

BESERRA, F. R. MDMA e redução de danos. Em: Hempadão. 2016. Disponível em: <https://hempadao.com/mdma-e-reducao-de-danos/>.

BESERRA, F. R. Os cuidados para abrir as portas do coração. Hempadão. 2016. <https://hempadao.com/ecstasy-os-cuidados-ao-abrir-as-portas-do-corao/ >.

BESERRA, F. R. Superando o trauma: psicoterapia com MDMA. Hempadão. 2016. Disponível em: <https://hempadao.com/superando-o-trauma-psicoterapia-com-mdma/>.

BESERRA, F. R. MDMA no tratamento da esquizofrenia? Em: Hempadão. 2016. Disponível em: < https://hempadao.com/mdma-no-tratamento-da-esquizofrenia/>.

BESERRA, F. R. MDMA e ilegalidade: parte 1. Em: Hempadão. 2016. Disponível em: <https://hempadao.com/legalidade-e-ilegalidade-do-mdma-ndash-parte-1/>.

BESERRA, F. R. MDMA e ilegalidade: parte 2. Em: Hempadão. 2016. Disponível em: <https://hempadao.com/legalidade-e-ilegalidade-do-mdma-ndash-parte-ii/>.

BESERRA, F. R. MDMA e depressão. Hempadão. 2015. Disponível em: <https://hempadao.com/mdma-e-depressao/>.

BESERRA, F. R. MDMA e depressão: parte 2. Hempadão. 2015. <https://hempadao.com/mdma-e-depressao-parte-2/>.

BESERRA, F. R. Psicoterapia com MDMA. Hempadão. 2015. Disponível em: – <https://hempadao.com/pt/infumacao/portas-da-percepcao/3155-psicoterapia-com-mdma.html>.

BESERRA, F. R. MDMA e psicopatia: um amor possível? Hempadão, 2015. Disponível em: <https://hempadao.com/pt/infumacao/portas-da-percepcao/2977-mdma-e-psicopatia-um-amor-possivel.html>.

BESERRA, F. R. Ecstasy em debate. Hempadão. 2015. Disponível em: <https://hempadao.com/ecstasy-em-debate/>.



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