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Brand Name :
Cogentin
Synonyms :
Benzatropina, benzatropine, Benzatropinum, Benztropine, Tropine benzohydryl ether, benzatropine mesilate
Class :
Neuropsychiatric agent, Muscarnic cholinergic receptor antagonist, Anticholinergic antiparkinson agent
Brand Name :
Cogentin
Synonyms :
Benzatropina, benzatropine, Benzatropinum, Benztropine, Tropine benzohydryl ether, benzatropine mesilate
Class :
Neuropsychiatric agent, Muscarnic cholinergic receptor antagonist, Anticholinergic antiparkinson agent
Dosage Forms & Strengths
Tablet
0.5 mg
1 mg
2 mg
Injectable solution (IV or IM)
1 mg/mL
2 mg/2 mL
Extrapyramidal Reaction
It is indicated in the management of extrapyramidal reactions and also in parkinsonism
For Acute dystonic reaction, the starting dose is one and upto 2 mg via IV/IM, followed by 1 or 2 mg two times per day
To control Drug-induced extrapyramidal disorders, the starting dose is one and upto 2 mg via mouth or via IV/IM 2 or 3 times per day
Adjusting the doses if required is a 0.5 mg increase with a time-interval of 5 or 6 days duration
The usual adult dose for managing extrapyramidal disorders is one upto 4 mg via mouth, which can be taken in single doses or divided doses two times a day with a maximum limit of upto 6 mg once a day
Parkinson’s Disease:
The usual starting dose, which is recommended, is 0.5 mg to 2 mg via mouth or via IV/IM per day
The usual dose is one to two mg via mouth once a day
0.5 mg to 6 mg a day is the dose range that is effective
The maximum limit is upto 6 mg a day
Dose Adjustments
Limited data is available
Dosage Forms & Strengths
Tablet
0.5 mg
1 mg
2 mg
Injectable solution (IV or IM)
1 mg/mL
2 mg/2 mL
Refer to the adult dosing
benzatropine: it may increase the risk of methemoglobinemia agents
benzatropine: it may increase the risk of methemoglobinemia agents
benzatropine: it may increase the risk of methemoglobinemia agents
benzatropine: it may increase the risk of methemoglobinemia agents
benzatropine: it may increase the risk of methemoglobinemia agents
may have an increased risk of adverse effects when combined with benzatropine
may have a decrease in excretion rate when combined with tetradecyl sulfuric acid
may have an increased risk of adverse effects when combined with benzatropine
may have an increasingly adverse effects when combined with benzatropine
it may diminish the therapeutic efficacy when combined with castor oil
it may enhance the risk of QTc prolongation when combined with amifampridine
benzatropine has the potential to reduce the rate of excretion of idebenone, leading to an elevation in levels of serum
When ponesimod is used together with benzatropine, this leads to enhanced risk or seriousness of bradycardia
When benzatropine is used together with adenosine, this leads to enhanced risk or seriousness of QTc prolongation
When benzatropine is used together with givinostat, this leads to enhanced risk or seriousness of Qtc prolongation
an increase in serum level with a decreased excretion rate of almasilate is observed when used in combination with benzatropine
zomepirac may reduce the elimination rate of benzatropine, resulting in a greater serum level
cefpirome leads to a reduction in the rate of excretion of benzatropine which leads to increased level of serum
benzatropine leads to a reduction in the rate of excretion of chromous sulfate, which leads to an increased level of serum
benzatropine leads to a reduction in the rate of excretion of pentaerythritol tetranitrate, which leads to an increased level of serum
benzatropine leads to a reduction in the rate of excretion of potassium acetate, which leads to an increased level of serum
benzatropine leads to a reduction in the rate of excretion of potassium perchlorate, which leads to an increased level of serum
benzatropine leads to a reduction in the rate of excretion of nitric oxide, which leads to an increased level of serum
benzatropine: it may increase the risk of lidoflazine
the adverse effects of benzatropine may be increased when combined with cimetropium
When benzatropine is used together with profenamine, this leads to enhanced risk or seriousness of adverse events
the risk or extent of adverse effects can be raised when benzatropine is combined with benzquinamide
may increase the risk or severity of adverse effects when combined
the excretory rate of benzatropine may be reduced when taken with mofebutazone that, which results in increased serum levels of benzatropine
the risk of QTc prolongation may be increased
the risk of adverse effects may be increased
the risk of adverse effects may be increased
the risk of tachycardia may be increased
the risk of adverse effects will be increased when benzatropine is taken with zotepine
Actions and Spectrum:
Actions:
It is evident from a comparison of the formulas for atropine and diphenhydramine that benzatropine mesilate contains the benzohydryl portion of diphenhydramine and the tropine portion of atropine.
Although only the anticholinergic properties of benatropine have been shown to be clinically significant in the treatment of parkinsonism, the drug also has antihistaminic effects.
The antihistaminic effect and duration of action in lab animals are similar to those of pyrilamine maleate. The anticholinergic activity of this medication is almost equivalent to atropine in the isolated guinea pig ileum; however, benzatropine is only roughly half as potent as atropine when given orally to unanesthetized cats.
Spectrum:
A centrally-acting antimuscarinic medication called benzatropine is used as a supplement to treat Parkinson’s disease. It can also be used to treat EPS (extrapyramidal symptoms) brought on by antipsychotics (e.g., phenothiazines), such as parkinsonism and dystonia. Decreases in dopaminergic activity lead to an imbalance between cholinergic and dopaminergic activity, which is the cause of extrapyramidal reactions and Parkinson’s disease symptoms.
It is believed that anticholinergic medication can help restore this balance, which can alleviate symptoms. Apart from its anticholinergic properties, benzatropine also prevents dopamine from being reabsorbed at nerve terminals through the dopamine transporter. Additionally, benzatropine inhibits the histamine H1 receptor.
Frequency not defined
Nausea
Tachycardia
Vomiting
Severe dry mouth
Constipation
Difficulty in speaking or swallowing
Appetite loss
Weight loss
Toxic psychosis
Disorientation
Hallucinations (visual)
Nervousness
Dilated pupils
Muscle weakness
Little or no urination
Arrythmias
Severe skin rash
Blurred vision
Numbness in the fingers
Memory impairment
Nervousness
Listless-ness
Depression
Dyscuria
Fever
Heartstroke
Hyperthermia
Black Box Warning:
Benzatropine can make it difficult for you to operate machinery or drive. This is exacerbated by alcohol. Discuss your risk with your healthcare physician. (Look up “Are you safe to drive?” on NZTA.) Avoid stopping benzatropine abruptly without first seeing your physician. Your physician might progressively lower the dosage.
Contraindication/Caution:
Contraindications
Cautions
Pregnancy consideration:
No data is available regarding the administration of the drug during pregnancy.
Breastfeeding warnings:
No data is available regarding the excretion of drug in breast milk.
Pregnancy category:
Category A: well-controlled and satisfactory studies show no risk to the fetus in the first or later trimester.
Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women.
Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.
Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.
Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.
Category N: No data is available for the drug under this category.
Pharmacology:
Benzatropine is used in combination with other medications to treat stiffness and tremors that are indicative of Parkinson’s disease.
Moreover, benzatropine is utilized to treat Parkinson-like symptoms brought on by drug usage.
Pharmacodynamics:
Exhibits both antihistaminic and anticholinergic effects. Its in vitro anticholinergic activity closely resembles that of atropine, while in vivo, it is approximately half as potent as atropine. Animal studies indicate that its antihistaminic activity and duration of action are comparable to those of pyrilamine maleate.
Pharmacokinetics:
Absorption
The time to achieve peak effect is 7 hours (oral)
Distribution
Protein-bound is 95%
Metabolism
Hepatic
Elimination and Excretion
The half-life is 16 hours
Only little amount (unchanged) is excreted 85% in feces.
Administration:
The administration of benzatropine necessitates careful consideration to ensure its safe and effective use, with general guidelines spanning various aspects:
Dosage:
Benzatropine is available in oral tablets and intramuscular injection forms. The prescribed dosage varies based on the specific medical condition and individual patient factors. Strict adherence to healthcare providers’ instructions is crucial to ensure proper dosage and administration.
Oral Administration:
When in tablet form, benzatropine is usually taken orally, with or without food. Patients should swallow the tablets whole with a full glass of water, adhering to the prescribed schedule to avoid exceeding recommended dosages.
Intramuscular Administration:
In certain situations, healthcare professionals administer benzatropine through intramuscular injections in a clinical setting. The use of proper aseptic techniques during injection helps minimize the risk of infection.
Patient Monitoring:
Close monitoring is essential for patients receiving benzatropine to detect signs of adverse effects or changes in symptoms. Regular follow-up appointments with healthcare providers are crucial to assess medication efficacy and adjust dosages if necessary.
Adherence to Instructions:
Patients are advised to strictly adhere to healthcare providers’ instructions regarding dosage, frequency, and treatment duration. Any questions or concerns about the medication should be addressed with the healthcare provider.
Contraindications and Precautions:
Healthcare providers need information about the patient’s existing medical conditions, allergies, or other medications. Benzatropine may have contraindications or interactions with other drugs, necessitating careful consideration before administration.
Discontinuation:
Discontinuing benzatropine should be supervised by a healthcare professional. Abrupt cessation may result in withdrawal symptoms or a recurrence of the original symptoms, highlighting the importance of gradual discontinuation under professional guidance.
Patient information leaflet
Generic Name: benzatropine
Pronounced: ben-ZAT-roh-peen
Why do we use benzatropine?
Benzatropine is primarily employed as a pharmaceutical intervention to address symptoms related to Parkinson’s disease and specific adverse effects resulting from antipsychotic medications.
Operating as an anticholinergic agent, it functions by inhibiting the activity of acetylcholine, a neurotransmitter in the brain. Concerning Parkinson’s disease, benzatropine aids in mitigating specific motor symptoms linked to the condition, such as tremors and stiffness.
Moreover, benzatropine may find application in the management of extrapyramidal symptoms (EPS) induced by antipsychotic drugs. These symptoms encompass involuntary muscle movements and spasms, which can manifest as side effects of antipsychotic medications.
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