Mesylate

• Benztropine mesylate tablets, USP are indicated for use as an adjunct in the therapy of all forms of parkinsonism. Useful also in the control of extrapyramidal disorders (except tardive dyskinesia - see PRECAUTIONS ) due to neuroleptic drugs (e.g., phenothiazines).

• Hypersensitivity to benztropine mesylate tablets or to any component of the tablets. Because of its atropine-like side effects, this drug is contraindicated in pediatric patients under three years of age, and should be used with caution in older pediatric patients.contraindicated

Benztropine mesylate tablets should be used when patients are able to take oral medication. The injection is especially useful for psychotic patients with acute dystonic reactions or other reactions that make oral medication difficult or impossible. It is recommended also when a more rapid response is desired than can be obtained with the tablets. Because of cumulative action, therapy should be initiated with a low dose which is increased gradually at five or six-day intervals to the smallest amount necessary for optimal relief. Increases should be made in increments of 0.5 mg, to a maximum of 6 mg, or until optimal results are obtained without excessive adverse reactions. Postencephalitic and Idiopathic Parkinsonism - The usual daily dose is 1 to 2 mg, with a range of 0.5 to 6 mg orally or parentally. As with any agent used in parkinsonism, dosage must be individualized according to age and weight, and the type of parkinsonism being treated. Generally, older patients, and thin patients cannot tolerate large doses. Most patients with postencephalitic parkinsonism need fairly large doses and tolerate them well. Patients with a poor mental outlook are usually poor candidates for therapy. In idiopathic parkinsonism, therapy may be initiated with a single daily dose of 0.5 to 1 mg at bedtime. In some patients, this will be adequate; in others 4 to 6 mg a day may be required. In postencephalitic parkinsonism, therapy may be initiated in most patients with 2 mg a day in one or more doses.

Safe use in pregnancy has not been established. Benztropine mesylate may impair mental and/or physical abilities required for performance of hazardous tasks, such as operating machinery or driving a motor vehicle. When benztropine mesylate is given concomitantly with phenothiazines, haloperidol, or other drugs with anticholinergic or antidopaminergic activity, patients should be advised to report gastrointestinal complaints, fever or heat intolerance promptly. Paralytic ileus, hyperthermia and heat stroke, all of which have sometimes been fatal, have occurred in patients taking anticholinergic-type antiparkinsonism drugs, including benztropine mesylate, in combination with phenothiazines and/or tricyclic antidepressants. Since benztropine mesylate contains structural features of atropine, it may produce anhidrosis. For this reason, it should be administered with caution during hot weather, especially when given concomitantly with other atropine-like drugs to the chronically ill, the alcoholic, those who have central nervous system disease, and those who do manual labor in a hot environment. Anhidrosis may occur more readily when some disturbance of sweating already exists. If there is evidence of anhidrosis, the possibility of hyperthermia should be considered. Dosage should be decreased at the discretion of the physician so that the ability to maintain body heat equilibrium by perspiration is not impaired. Severe anhidrosis and fatal hyperthermia have occurred.

The adverse reactions below, most of which are antichlolinergic in nature, have been reported and within each category are listed in order of decreasing severity. Cardiovascular Tachycardia. Digestive Paralytic ileus, constipation, vomiting, nausea, dry mouth. If dry mouth is so severe that there is difficulty in swallowing or speaking, or loss of appetite and weight, reduce dosage, or discontinue the drug temporarily. Slight reduction in dosage may control nausea and still give sufficient relief of symptoms. Vomiting may be controlled by temporary discontinuation, followed by resumption at a lower dosage. Nervous System Toxic psychosis, including confusion, disorientation, memory impairment, visual hallucinations; exacerbation of preexisting psychotic symptoms; nervousness; depression; listlessness; numbness of fingers. Special Senses Blurred vision, dilated pupils. Urogenital Urinary retention, dysuria. Metabolic/Immune or Skin Occasionally, an allergic reaction, e.g., skin rash, develops. If this cannot be controlled by dosage reduction, the medication should be discontinued. Other Heat stroke, hyperthermia, fever.

Manifestations - May be any of those seen in atropine poisoning or antihistamine overdosage: CNS depression, preceded or followed by stimulation; confusion; nervousness; listlessness; intensification of mental symptoms or toxic psychosis in patients with mental illness being treated with neuroleptic drugs (e.g., phenothiazines); hallucinations (especially visual); dizziness; muscle weakness; ataxia; dry mouth; mydriasis; blurred vision; palpitations; tachycardia; elevated blood pressure; nausea; vomiting; dysuria; numbness of fingers; dysphagia; allergic reactions, e.g., skin rash; headache; hot, dry, flushed skin; delirium; coma; shock; convulsions; respiratory arrest; anhidrosis; hyperthermia; glaucoma; constipation. Treatment - Physostigmine salicylate, 1 to 2 mg, SC or IV, reportedly will reverse symptoms of anticholinergic intoxication. * A second injection may be given after 2 hours if required. Otherwise treatment is symptomatic and supportive. Induce emesis or perform gastric lavage (contraindicated in precomatose convulsive, or psychotic states). Maintain respiration.

• Apr 1, 1968NDANDA016267Mitem Pharma
• Jun 28, 1978NDANDA017962Esjay Pharma
• Nov 2, 1990NDANDA019668Viatris
• Mar 14, 1997NDANDA020779Agouron Pharms
• Dec 8, 1997NDANDA020148Bausch
• Jun 21, 2002NDANDA020919Viatris
• Apr 18, 2003NDANDA021588Novartis
• Apr 30, 2003NDANDA021503Agouron Pharms

1. 1Death9,5335.3%
2. 2Gastrointestinal Haemorrhage8,4834.7%
3. 3Nausea7,6674.3%
4. 4Diarrhoea7,1884.0%
5. 5Drug Ineffective7,0433.9%
6. 6Fatigue6,6923.7%
7. 7Fall6,2633.5%
8. 8Dyspnoea6,1943.4%
9. 9Dizziness5,7563.2%
10. 10Cerebrovascular Accident5,0482.8%
11. 11Asthenia4,8272.7%
12. 12Anaemia4,5972.6%
13. 13Headache4,5122.5%
14. 14Vomiting4,4672.5%
15. 15Off Label Use4,2412.4%

Recent PubMed references pinned to Mesylate as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

• Exploring ethyl methane sulphonate induced, L-cysteine HCl resistant Bacillus subtilis putative mutant and its immobilization for enhanced acetoin synthesis.
  Archives of microbiology · 2026 · Ahmad MU, Ali S, Ain NU, et al.
  PMID 42126597DOI 10.1007/s00203-026-04954-y
• Replacing Ecologically Risky Trifluoroacetic Acid and Acetonitrile With Methanesulfonic Acid and Dimethyl Carbonate in High-Performance Liquid Chromatography Analyses of Small Molecule Drugs.
  Journal of separation science · 2026 · Steinicke FPN, El-Jourani TB, Haegner J, et al.
  PMID 42087586DOI 10.1002/jssc.70425
• A liquid chromatography-tandem mass spectrometry method for therapeutic drug monitoring of treosulfan.
  Laboratory medicine · 2026 · Ryu J, Kim S, Lee SH, et al.
  PMID 42048559DOI 10.1093/labmed/lmag017
• [Erjing Wan ameliorates busulfan-induced oligoasthenospermia in mice by inhibiting p38 MAPK/NF-κB pathway].
  Zhongguo Zhong yao za zhi = Zhongguo zhongyao zazhi = China journal of Chinese materia medica · 2026 · Xie F, Yao GP, Peng M, et al.
  PMID 42011621DOI 10.19540/j.cnki.cjcmm.20251210.705
• Ethyl methanesulfonate mutagenesis in fungi: genetic mechanisms, applications, and implications for agricultural biotechnology.
  Archives of microbiology · 2026 · Holman DE, Abrahams AI, Hattingh K, et al.
  PMID 42008003DOI 10.1007/s00203-026-04858-x
• Busulfan pharmacokinetics in adults - a real-world evaluation of intra-individual variability and the impact of obesity and deferasirox.
  Bone marrow transplantation · 2026 · Langebrake C, Wansing EA, Janson D, et al.
  PMID 41981079DOI 10.1038/s41409-026-02833-0
• Treosulfan-fludarabine conditioning in infants with severe combined immunodeficiencies: Extended study of the UK paediatric treosulfan study.
  British journal of haematology · 2026 · Lum SH, Greener S, Memon IL, et al.
  PMID 41958357DOI 10.1111/bjh.70453
• Intra-ovarian busulfan administration: an effective and relatively safe method for depleting endogenous germ cells in the female marine teleost yellow drum (Nibea albiflora).
  Fish physiology and biochemistry · 2026 · Zhang Z, Yu L, Yang Y, et al.
  PMID 41902885DOI 10.1007/s10695-026-01668-2

The 10 most recently updated of 2,006 ClinicalTrials.gov registrations naming Mesylate as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Efficacy and Safety of the CloB2M (Clofarabine Combined With Busulfan and Melphalan) Conditioning Regimen in Allogeneic Hematopoietic Stem Cell Transplantation for Adult Patients With Acute Myeloid Leukemia in First Complete Remission
  Not yet recruiting · Interventional · 30 enrolled · Institute of Hematology & Blood Diseases Hospital, China
  NCT07644481updated 2026-06-12
• Stem Cell Transplantation for Participants With Germline RUNX1 Associated Blood Cancers
  Not yet recruiting · Phase 2 · Interventional · 98 enrolled · National Cancer Institute (NCI)
  NCT07524530updated 2026-06-12
• A Phase Ib/II Clinical Study of Camrelizumab and Apatinib Plus GP in the Treatment of Advanced Biliary Tract Cancer
  Completed · Phase 1 · Phase 2 · Interventional · 48 enrolled · Sun Yat-sen University
  NCT05742750updated 2026-06-12
• A Study of Bomedemstat (IMG-7289/MK-3543) Compared to Best Available Therapy (BAT) in Participants With Essential Thrombocythemia and an Inadequate Response or Intolerance of Hydroxyurea (MK-3543-006)
  Recruiting · Phase 3 · Interventional · 340 enrolled · Merck Sharp & Dohme LLC
  NCT06079879updated 2026-06-12
• Testing Trametinib and Dabrafenib as a Potential Targeted Treatment in Cancers With BRAF Genetic Changes (MATCH-Subprotocol H)
  Active not recruiting · Phase 2 · Interventional · 44 enrolled · National Cancer Institute (NCI)
  NCT04439292updated 2026-06-12
• Base Editing for Mutation Repair in Hematopoietic Stem & Progenitor Cells for X-Linked Chronic Granulomatous Disease
  Recruiting · Phase 1 · Phase 2 · Interventional · 10 enrolled · National Institute of Allergy and Infectious Diseases (NIAID)
  NCT06325709updated 2026-06-11
• MYELOMATCH: A Screening Study to Assign People With Myeloid Cancer to a Treatment Study or Standard of Care Treatment Within myeloMATCH (MyeloMATCH Screening Trial)
  Recruiting · Phase 2 · Interventional · 2,000 enrolled · National Cancer Institute (NCI)
  NCT05564390updated 2026-06-11
• Atezolizumab With or Without Eribulin Mesylate in Treating Patients With Recurrent Locally Advanced or Metastatic Urothelial Cancer
  Active not recruiting · Phase 2 · Interventional · 72 enrolled · National Cancer Institute (NCI)
  NCT03237780updated 2026-06-11
• Asciminib Roll-over Study
  Recruiting · Phase 4 · Interventional · 347 enrolled · Novartis Pharmaceuticals
  NCT04877522updated 2026-06-10
• Sorafenib, Busulfan and Fludarabine in Treating Patients With Recurrent or Refractory Acute Myeloid Leukemia Undergoing Donor Stem Cell Transplant
  Active not recruiting · Phase 1 · Phase 2 · Interventional · 74 enrolled · M.D. Anderson Cancer Center
  NCT03247088updated 2026-06-10

Frequently asked questions

What is Mesylate used for?

According to FDA labeling, Mesylate carries indications including: Benztropine mesylate tablets, USP are indicated for use as an adjunct in the therapy of all forms of parkinsonism. Useful also in the control of extrapyramidal disorders (except tardive dyskinesia - see PRECAUTIONS ) due to neuroleptic drugs (e.g., phenothiazines).. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What are the contraindications for Mesylate?

Mesylate labeling lists contraindications including: Hypersensitivity to benztropine mesylate tablets or to any component of the tablets. Because of its atropine-like side effects, this drug is contraindicated in pediatric patients under three years of age, and should be used with caution in older pediatric patients.. Always consult the full prescribing information and a clinician.