Botulinum toxin type A



Botulinum toxin type A is a purified form of botulinum toxin type A used to block acetylcholine release in the treatment of chronic sialorrhea, muscle spasticity, and dystonia, as well as in cosmetic applications.

Brand Names
Botox, Botox Cosmetic, Dysport, Xeomin
Generic Name
Botulinum toxin type A
DrugBank Accession Number

In 2002, botulinum toxin A, also known as onabotulinumtoxinA or Botox, was the first type A botulism toxin to be introduced into the market for cosmetic use.8 With a wide variety of applications and favourable safety profile, Botulinum toxin A injection is a minimally invasive and promising treatment for cosmetic imperfections, muscle spasms, and other conditions.7,20 A popular use for Botox is the treatment of facial wrinkles and lines, however, there are many uses for the botulinum toxin A in the treatment of dystonia, incontinence, migraine, blepharospasm, and hyperhidrosis.15,19

Approved, Investigational
Biologic Classification
Protein Based Therapies
Other protein based therapies
Protein Structure
Protein Chemical Formula
Protein Average Weight
900000.0 Da
>Botulinum Toxin Type A Sequence
Download FASTA Format
  • AbobotulinumtoxinA
  • Botulinum A neurotoxin
  • Botulinum antitoxin type A
  • Botulinum toxin A
  • Botulinum toxin type A
  • BTX-A
  • EvabotulinumtoxinA
  • IncobotulinumtoxinA
  • OnabotulinumtoxinA
  • Prabotulinumtoxin A
  • Toxina botulínica A
  • Toxine botulinique A
External IDs
  • AGN 191622
  • ANT-1207
  • ANT-1401
  • ANT-1403
  • CNT 52120
  • NT 201



Botulinum toxin A is indicated for a variety of conditions, depending on the preparations. Cosmetically, it is used for the treatment of facial fine lines and wrinkles, specifically for upper facial rhytides, including forehead, lateral canthus, and glabellar lines.19

In addition to the above indications, botulinum toxin A is used for the following conditions: treatment of adults with symptomatic overactive bladder with or without incontinence, treatment of incontinence in adult patients who are not candidates for anticholinergic therapy, treatment of Neurogenic Detrusor Overactivity (NDO) in patients over 5 years who cannot undergo anticholinergic therapy. Botulinum toxin A is indicated for the prevention of chronic migraines, for the treatment of muscle spasms, cervical dystonia, axillary hyperhidrosis, strabismus,15 and disorders of the 7th cranial nerve.20

Off-label, botulinum toxin A is used for a variety of conditions such as temporomandibular joint (TMJ) disorders and myofascial pain12, neurogenic thoracic outlet syndrome, epicondylitis, post-stroke pain, post-herpetic neuralgia, diabetic neuropathy, trigeminal neuralgia, neuropathic pain, spinal cord injury, and bladder pain.13

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Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Treatment ofBladder pain••• ••••••••••••••• ••••••• •••••••••••• ••• ••••••••
Treatment ofBlepharospasm••••••••••••••••••••••••••• ••••••• •••• •••••••••••••••••• ••••••••••••••••• ••••••• ••• ••••••••
Management ofBlepharospasm•••••••••••••••••••••• ••••••••
Management ofCervical dystonia••••••••••••••••••••••••••• ••••••••
Prophylaxis ofChronic migraine••••••••••••••••••••••••••• ••••••••
Contraindications & Blackbox Warnings
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Botulinum toxin A inhibits the release of acetylcholine, relieving muscle contraction and spasm associated with many conditions, such as incontinence and dystonia. Cosmetically, botulinum toxin A paralyses muscles in the face to temporarily treat wrinkles.9,19 The maximum effects of muscle paralysis occur four to seven days after a dose.6 When injected at therapeutic doses, botulinum toxin A causes partial chemical denervation of muscle tissue, causing local reduction of muscle activity. Muscle atrophy may result, axonal sprouting may begin, and extrajunctional acetylcholine receptors can be formed. Reinnervation of the muscle may occur, reversing muscle denervation caused by botulinum toxin A.15

Mechanism of action

Botulinum toxin is a 150-kDa molecular weight protein consisting of a light chain (50 kDa) and heavy chain (100 kDa) linked by a single disulfide bond. The crystal structure reveals 3 lobes - the light chain, the amino-terminal portion of the heavy chain, and the carboxyl-terminal portion of the heavy chain.11

Botulinum toxin type A blocks neuromuscular transmission on motor or sympathetic nerve terminals, inhibiting the release of acetylcholine.15 Botulinum toxins have actions on various regions: the neuromuscular junction, autonomic ganglia, and both postganglionic sympathetic and parasympathetic nerve endings. The heavy chain of the toxin binds selectively at the presynaptic surface of cholinergic neurons in an irreversible fashion. After binding, the toxin-receptor complex is transported into the cell by endocytosis. The disulfide bond between the two chains is cleaved and the botulism toxin enters the cytoplasm. The light chain specifically interacts with SNAP-25 in the nerve terminals to block binding of acetylcholine vesicles with the cell membrane. SNAP-25 is required for successful binding and release of acetylcholine from vesicles in nerve endings.6

ASynaptosomal-associated protein 25
URho-related GTP-binding protein RhoB

The chemical complexity of botulinum toxin type A combined with its extreme potency limits the opportunity to study its pharmacokinetic profile in humans.15 For this reason, human pharmacokinetic studies have not been performed. Animal studies using radio labeled botulinum toxin suggest it is absorbed systemically after subcutaneous and intranasal administration. Clinical relevance is unknown.11

Volume of distribution

There are extremely limited data about the pharmacokinetics of botulinum toxin in humans.15 An animal study demonstrated that botulinum toxin accumulates in the liver and spleen in rats and mice when injected subcutaneously or administered intranasally.11

Protein binding

A pharmacokinetic study in mice and rats revealed significant binding to albumin after subcutaneous injection or intranasal administration.11


Metabolism information for botulinum A toxin is not readily available in the literature.11,15

Route of elimination

Elimination information for botulinum A toxin is not readily available in the literature.11,15


There is no readily available data about the pharmacokinetics of botulinum toxin in humans.15 The elimination half-life for non-metabolized botulinum toxin in blood and serum ranged from 230 to 260 min in a pharmacokinetic study of rats and mice.11


Clearance information for botulinum A toxin is not readily available in the literature.11,15

Adverse Effects
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The intraperitoneal LD50 of botulinum toxin A in mice is 160 ng/kg.22 An overdose of botulinum toxin A is expected to produce neuromuscular weakness, manifested by a variety of symptoms that may not appear immediately after injection. Dysphagia, dysphonia, weakness, dyspnea or respiratory distress may indicate distant spread of botulinum toxin A effects.14 If an overdose is suspected or confirmed, patients should be monitored for several weeks closely for local and distant neurologic effects. Hospitalization or further medical evaluation and appropriate intervention should be provided immediately.15

Not Available
Pharmacogenomic Effects/ADRs
Not Available


Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
1,2-BenzodiazepineThe risk or severity of CNS depression can be increased when Botulinum toxin type A is combined with 1,2-Benzodiazepine.
AcetazolamideThe risk or severity of CNS depression can be increased when Botulinum toxin type A is combined with Acetazolamide.
AcetophenazineThe risk or severity of CNS depression can be increased when Botulinum toxin type A is combined with Acetophenazine.
AcetyldigitoxinThe risk or severity of Cardiac Arrhythmia can be increased when Botulinum toxin type A is combined with Acetyldigitoxin.
AclidiniumThe risk or severity of adverse effects can be increased when Aclidinium is combined with Botulinum toxin type A.
Food Interactions
No interactions found.


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Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
BotoxPowder, for solution200 unit / vialIntramuscularAbbvie2023-10-11Not applicableCanada flag
BotoxPowder, for solution50 unit / vialIntramuscularAbbvie2023-06-20Not applicableCanada flag
BotoxPowder, for solution100 unit / vialIntramuscularAbbvie1992-12-31Not applicableCanada flag
BOTOX CosmeticPowder, for solution100 unit / vialIntramuscularAbbvie2001-05-07Not applicableCanada flag
BOTOX CosmeticPowder, for solution50 unit / vialIntramuscularAbbvieNot applicableNot applicableCanada flag


ATC Codes
M03AX01 — Botulinum toxin
Drug Categories
Chemical TaxonomyProvided by Classyfire
Not Available
Organic Compounds
Super Class
Organic Acids
Carboxylic Acids and Derivatives
Sub Class
Amino Acids, Peptides, and Analogues
Direct Parent
Alternative Parents
Not Available
Not Available
Molecular Framework
Not Available
External Descriptors
Not Available
Affected organisms
  • Humans and other mammals

Chemical Identifiers

CAS number


Synthesis Reference

Alexander Zabudkin, Jun Krasnopolsky, Aleksandr Itkin, Dmitry Itkin.(2003). Pharmaceutical preparation of botulinum neurotoxin, methods of synthesis and methods of clinical use (US). Patent number WO2003101483A1.

General References
  1. Montecucco C, Molgo J: Botulinal neurotoxins: revival of an old killer. Curr Opin Pharmacol. 2005 Jun;5(3):274-9. [Article]
  2. Brin MF, Lew MF, Adler CH, Comella CL, Factor SA, Jankovic J, O'Brien C, Murray JJ, Wallace JD, Willmer-Hulme A, Koller M: Safety and efficacy of NeuroBloc (botulinum toxin type B) in type A-resistant cervical dystonia. Neurology. 1999 Oct 22;53(7):1431-8. [Article]
  3. Shukla HD, Sharma SK: Clostridium botulinum: a bug with beauty and weapon. Crit Rev Microbiol. 2005;31(1):11-8. [Article]
  4. Eisenach JH, Atkinson JL, Fealey RD: Hyperhidrosis: evolving therapies for a well-established phenomenon. Mayo Clin Proc. 2005 May;80(5):657-66. [Article]
  5. Schurch B, Corcos J: Botulinum toxin injections for paediatric incontinence. Curr Opin Urol. 2005 Jul;15(4):264-7. [Article]
  6. Nigam PK, Nigam A: Botulinum toxin. Indian J Dermatol. 2010;55(1):8-14. doi: 10.4103/0019-5154.60343. [Article]
  7. Naumann M, Jankovic J: Safety of botulinum toxin type A: a systematic review and meta-analysis. Curr Med Res Opin. 2004 Jul;20(7):981-90. doi: 10.1185/030079904125003962. [Article]
  8. Lorenc ZP, Kenkel JM, Fagien S, Hirmand H, Nestor MS, Sclafani AP, Sykes JM, Waldorf HA: A review of onabotulinumtoxinA (Botox). Aesthet Surg J. 2013 Mar;33(1 Suppl):9S-12S. doi: 10.1177/1090820X12474629. [Article]
  9. Satriyasa BK: Botulinum toxin (Botox) A for reducing the appearance of facial wrinkles: a literature review of clinical use and pharmacological aspect. Clin Cosmet Investig Dermatol. 2019 Apr 10;12:223-228. doi: 10.2147/CCID.S202919. eCollection 2019. [Article]
  10. Lu B: The destructive effect of botulinum neurotoxins on the SNARE protein: SNAP-25 and synaptic membrane fusion. PeerJ. 2015 Jun 30;3:e1065. doi: 10.7717/peerj.1065. eCollection 2015. [Article]
  11. Ravichandran E, Gong Y, Al Saleem FH, Ancharski DM, Joshi SG, Simpson LL: An initial assessment of the systemic pharmacokinetics of botulinum toxin. J Pharmacol Exp Ther. 2006 Sep;318(3):1343-51. doi: 10.1124/jpet.106.104661. Epub 2006 Jun 16. [Article]
  12. Mor N, Tang C, Blitzer A: Temporomandibular Myofacial Pain Treated with Botulinum Toxin Injection. Toxins (Basel). 2015 Jul 24;7(8):2791-800. doi: 10.3390/toxins7082791. [Article]
  13. Padda IS, Tadi P: Botulinum Toxin . [Article]
  14. Omprakash Hm, Rajendran Sc: Botulinum Toxin Deaths: What is the Fact? J Cutan Aesthet Surg. 2008 Jul;1(2):95-7. doi: 10.4103/0974-2077.44169. [Article]
  15. FDA Approved Products: Botox (onabotulinumtoxinA) for injection [Link]
  16. World Health Organization: Botulism [Link]
  17. Allergan MSDS: Botox [Link]
  18. DermNet NZ: Botulinum toxin [Link]
  19. Product monograph: Botox Cosmetic (botulinum toxin A) for injection [Link]
  20. Product Monograph: Botox (Clostridium botulinum type A neurotoxin complex ) powder for injectable solution [Link]
  21. FDA Approved Drug Products: XEOMIN (incobotulinumtoxinA) for injection, for intramuscular or intraglandular use [Link]
  22. Allergan MSDS: OnabotulinumtoxinA [Link]
KEGG Compound
PubChem Substance
Therapeutic Targets Database
RxList Drug Page
FDA label
Download (115 KB)

Clinical Trials

Clinical Trials
4Active Not RecruitingPreventionKeloids Scars1
4Active Not RecruitingTreatmentIncreased frequency of urination / Overactive Bladder Syndrome (OABS) / Urinary Urge Incontinence (UUI) / Urinary Urgency1
4CompletedBasic ScienceHealthy Volunteers (HV)1
4CompletedBasic ScienceMigraine1
4CompletedOtherForehead Rhytides / Forehead Wrinkles1


Not Available
  • Allergan Inc.
  • Tercica Inc.
Dosage Forms
Injection, powder, for solutionIntramuscular125 U
Injection, powder, for solutionIntramuscular
Injection, powder, for solution100 IU
PowderIntramuscular100 unit/1vial
Powder, for solutionIntramuscular100 unit / vial
Powder, for solutionIntramuscular200 unit / vial
Injection, powder, for solutionIntramuscular100 U
InjectionIntramuscular100 U
Injection, powder, for solutionIntradermal; Intramuscular100 units
Injection, powder, for solutionIntradermal; Intramuscular; Subcutaneous200 Units
Injection, powder, for solutionIntradermal; Intramuscular; Subcutaneous50 Units/vial
Injection, powder, for solutionIntradermal; Intramuscular200 U
SolutionIntramuscular100 UI
Injection, powder, for solutionIntramuscular500 unit/1vial
Injection, powder, for solutionIntramuscular; Subcutaneous300 U
Injection, powder, for solutionIntramuscular; Subcutaneous500 UI
Injection, powder, lyophilized, for solutionIntramuscular300 [USP'U]/1
SolutionIntramuscular500.000 U
Injection, powder, for solution300 unit/1vial
Injection, powder, lyophilized, for solutionIntramuscular; Subcutaneous300 U
Injection, solutionIntramuscular500 U
Powder, for solutionIntramuscular300 unit / vial
Powder, for solutionIntramuscular500 unit / vial
Injection, powder, lyophilized, for solutionIntramuscular; Subcutaneous500 U
PowderIntramuscular200 unit/1vial
PowderIntramuscular50 unit/1vial
Injection, powder, for solution
SolutionIntramuscular100 U
Injection, powder, lyophilized, for solutionIntramuscular; Subcutaneous50 U
Injection, powder, lyophilized, for solutionIntramuscular; Subcutaneous100 IU
Injection, powder, lyophilized, for solutionIntramuscular200 IU
Injection, powder, for solutionIntramuscular50 U
Injection, powder, for solutionParenteral4 AU/0.1ml
Injection, powder, for solutionParenteral4 AU/ 0.1 ml
SolutionParenteral50.000 U
Injection, powder, for solution50 IU
Injection, powder, for solutionParenteral100 U
Injection, powder, for solutionParenteral200 U
Injection, powder, for solutionParenteral50 U
Powder, for solutionIntramuscular50 unit / vial
Injection, powder, for solution50 LD50 Units
Injection, powder, for solutionIntramuscular100 LD50 units
Injection, powder, for solutionIntramuscular50 LD50 units
Injection, powder, lyophilized, for solutionIntramuscular100 U
Injection, powder, lyophilized, for solutionIntramuscular50 U
Injection, powder, for solution100 unit/1vial
Injection, powder, lyophilized, for solution100 unit/1vial
Injection, powder, for solution50 unit/1vial
Unit descriptionCostUnit
Botox 200 unit vial1260.0USD vial
Dysport 500 unit vial852.0USD vial
Botox 100 unit655.2USD vial
Botox 100 unit vial630.0USD vial
Botox cosmetic 100 unit vial630.0USD vial
Botox cosmetic 50 unit vial346.8USD vial
Botox (100 - 200 unit/Vial)3.74USD vial
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
CA2280565No2005-11-152019-08-20Canada flag
CA2310845No2001-05-152014-06-07Canada flag


Experimental Properties
melting point (°C)85.5-86.5
water solubility>10 mg/ml
isoelectric point5.6


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Pharmacological action
General Function
Syntaxin-1 binding
Specific Function
t-SNARE involved in the molecular regulation of neurotransmitter release. May play an important role in the synaptic function of specific neuronal systems. Associates with proteins involved in vesi...
Gene Name
Uniprot ID
Uniprot Name
Synaptosomal-associated protein 25
Molecular Weight
23314.905 Da
  1. Zhou JY, Wang ZF, Ren XM, Tang MZ, Shi YL: Antagonism of botulinum toxin type A-induced cleavage of SNAP-25 in rat cerebral synaptosome by toosendanin. FEBS Lett. 2003 Dec 4;555(2):375-9. [Article]
  2. Flynn TC: Myobloc. Dermatol Clin. 2004 Apr;22(2):207-11, vii. [Article]
  3. Straughan D: Progress in applying the Three Rs to the potency testing of Botulinum toxin type A. Altern Lab Anim. 2006 Jun;34(3):305-13. [Article]
  4. Vaidyanathan VV, Yoshino K, Jahnz M, Dorries C, Bade S, Nauenburg S, Niemann H, Binz T: Proteolysis of SNAP-25 isoforms by botulinum neurotoxin types A, C, and E: domains and amino acid residues controlling the formation of enzyme-substrate complexes and cleavage. J Neurochem. 1999 Jan;72(1):327-37. doi: 10.1046/j.1471-4159.1999.0720327.x. [Article]
  5. FDA Approved Products: Botox (onabotulinumtoxinA) for injection [Link]
Pharmacological action
General Function
Gtpase activity
Specific Function
Mediates apoptosis in neoplastically transformed cells after DNA damage. Not essential for development but affects cell adhesion and growth factor signaling in transformed cells. Plays a negative r...
Gene Name
Uniprot ID
Uniprot Name
Rho-related GTP-binding protein RhoB
Molecular Weight
22123.185 Da
  1. Ishida H, Zhang X, Erickson K, Ray P: Botulinum toxin type A targets RhoB to inhibit lysophosphatidic acid-stimulated actin reorganization and acetylcholine release in nerve growth factor-treated PC12 cells. J Pharmacol Exp Ther. 2004 Sep;310(3):881-9. Epub 2004 May 12. [Article]


Pharmacological action
General Function
Toxic substance binding
Specific Function
Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
Gene Name
Uniprot ID
Uniprot Name
Serum albumin
Molecular Weight
69365.94 Da
  1. Ravichandran E, Gong Y, Al Saleem FH, Ancharski DM, Joshi SG, Simpson LL: An initial assessment of the systemic pharmacokinetics of botulinum toxin. J Pharmacol Exp Ther. 2006 Sep;318(3):1343-51. doi: 10.1124/jpet.106.104661. Epub 2006 Jun 16. [Article]

Drug created at June 13, 2005 13:24 / Updated at April 09, 2024 18:11