Pharmacology of Botulinum Toxins: From Poison to Remedy

Abstract

Botulinum toxin (BTX) is produced by autolysis of several strains of Clostridium botulinum, a gram-positive, spore-forming, rod-shaped, strictly anaerobic bacterium. However there are also non-clostridial microorganisms that are enable to produce the toxin. As some other beneficial poison, BTX also fits well the quotations by old scientists and philosophers like “Almost every substance can become a poison but only thing is the dose discriminating the difference” (Paracelsus, XVI century) or “Poisons can be employed as a means for the destruction of life or as agents for the treatment of the sick” (Claude Bernard, XIX century) or “Poison is a medicine, medicine is a poison” (Ahi Evran, XIII century). In the 1980's, Alan Scott first published articles on the use of BTX for the treatment of strabismus. The Food and Drug Administration of the USA (FDA) first approved botulinum toxin for the treatment of strabismus (crossed eye) blepharospasm (uncontrollable eye blinking) in 1989 and for glabellar rhytides in 2002, the first cosmetic indication. Since then BTX has been used for a verity of indications not only dermatological but also non-dermatological indications including on-labelled as well as off-labelled uses. In this review you will find the pharmacological profile of botulinum toxins, i.e., mode of action, pharmacokinetics, adverse effects, indications and contrindications, drug interactions, duration and site of action, etc. Furthermore, current commercial products and novel dosage forms as well as new perspective of BTX use will also be discussed.

Keywords

• botulinum toxin
• pharmacology
• poison
• remedy
• esthetic
• muscle
• pain

Botulinum Toksinlerinin Farmakolojisi: Zehirden Çareye

Abstract

Botulinum toksini (BTX) Gram (+), sporlu, çubuk şekilli ve mutlak anareobik bir bakteri olan Clostridium botulinum’un parçalanması sonucu üretilir. Ancak bu toksini üretebilen Clostridium-olmayan mikroorganizmalar da bulunmaktadır. Faydalı olabilen bazı toksinler gibi BTX de, eski bilim insanları ya da filozofların “Hemen herşey zehir olabilmektedir, farkı yaratan dozdur” (Paracelsus, XVI yüzyıl) veya “Zehirler yaşamı tahrip etmek veya hastaları tedavi etmek için kullanılabilir” (Claude Bernard, XIX yüzyıl) ya da “Zehir ilaçtır, ilaç zehirdir” (Ahi Evran, XIII yüzyıl) gibi tanımlamalarına çok uymaktadır. 1980’lerde Alan Scott, şaşılık tedavisinde BTX’in kullanımı ile ilgili ilk makaleleri yayımlamıştır. Amerikan Gıda ve İlaç Dairesi (FDA), 1989’da strabismus (şaşılık) and blefarospazm (kontrol edilemeyen göz kırpması) tedavisi için, 2002’de de ilk kozmetik indikasyon olarak kaş-arası dikey kırışıklıklarının tedavisi için ilk kez BTX’i onaylamıştır. O günden beri BTX, sadece dermatolojik değil aynı zamanda dermatolojik-olmayan pek çok indikasyonda, hem onaylı hem de onaysız olarak kullanılmaktadır. Bu derlemede botulinum toksininin etki mekanizmaları, farmakokinetiği, yan etkileri, indikasyon ve kontrindikasyonları, ilaç etkileşmeleri, etki yerleri ve etki süresi vd pek çok açıdan farmakolojik profilini bulacaksınız. Ayrıca mevcut ticari ürünleri ve yeni dozaj formları ve aynı zamanda BTX’in gelecekteki kullanımı konusu da tartışılacaktır.

Keywords

• botulinum toksini
• farmakoloji
• zehir
• çare
• estetik
• kas
• ağrı

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