Pharmacological aspects of therapeutic botulinum toxin preparations

Therapeutic preparations of botulinum toxin (BT) consist of botulinum neurotoxin (BNT), complexing proteins, and excipients. Depending on the target tissue, BNT can block cholinergic neuromuscular innervation of intra- and extrafusal muscle fibres or cholinergic autonomic innervation of sweat, lacrimal, and salival glands and smooth muscles. Indirect CNS effects are numerous; direct ones have not been reported after intramuscular application. Botulinum toxin type A is distributed as Botox, Dysport, Xeomin, Hengli/CBTX-A, and Neuronox and BT type B as NeuroBloc/Myobloc. Differences in potency labelling,of therapeutic BT preparations can be corrected by introduction of a conversion factor of 1:3 between Botox and Dysport, of 1:1 between Botox and Xeomin, and of 1-40 between Botox and NeuroBloc/Myobloc. Acute adverse effects of BT can be obligate, local or systemic. Adverse effect profiles of the different preparations are similar. However, BT type B frequently produces additional autonomic systemic adverse effects. Long-term application does not produce additional adverse effects. BNT can be partially or completely blocked by antibodies. Risk factors include the amount of BNT applied at each injection series, the interval between injection series, and the specific biological potency (SBP) of the BT preparation used. The SBP is 5 equivalent mouse units/ng BNT for NeuroBloc, 60 for Botox, 100 for Dysport, and 167 for Xeomin. Xeomin should therefore have a particularly low antigenicity. Clinical confirmation of this predicition, however, is lacking.