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The prescribing information for Benztropine Mesylate, an antiparkinson agent used for the symptomatic treatment of Parkinsonism and drug-induced extrapyramidal disorders. It covers indications, contraindications, warnings, precautions, drug interactions, and dosage information.
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Prpdp-BENZTROPINE
Benztropine Mesylate Tablets, USP 1 mg
Benztropine Mesylate Oral Solution 0.4 mg/mL
Antiparkinson Agent
PENDOPHARM, Division of Pharmascience Inc. 6111 Royalmount Avenue, Suite 100
Montréal, Québec
H4P 2T
Submission Control No: 181476
Date of Revision: February 2, 2015
pdp-BENZTROPINE (benztropine mesylate) is contraindicated in:
General Since benztropine mesylate has cumulative action, continued supervision is advisable.
Dry mouth, blurred vision, nausea, vomiting and nervousness may develop. Adjustment of dosage or time of administration sometimes helps to control these reactions. If dry mouth is so severe that there is difficulty in swallowing or speaking or there is loss of appetite and weight, reduce dosage or discontinue temporarily. Vomiting may be controlled by temporary discontinuation, followed by resumption at a lower dosage.
Cardiovascular Since benztropine mesylate has cumulative action, continued supervision is advisable especially in patients with a tendency to tachycardia.
Endocrine and Metabolism Benztropine mesylate may produce anhidrosis. Therefore, it should be given with caution during hot weather, especially to elderly, the chronically ill, the alcoholic, those with Central Nervous System (CNS) disease and those who do manual labour in a hot environment. Anhidrosis may be anticipated to occur more readily when some disturbance of sweating already exists. If there is evidence of anhidrosis, dosage should be decreased at the discretion of the physician so that the ability to maintain body heat equilibrium by perspiration is not impaired.
Gastrointestinal When benztropine mesylate is given concomitantly with phenothiazines or other drugs with anticholinergic activity, advise patients to report gastrointestinal complaints promptly. Paralytic ileus, sometimes fatal, has occurred in patients taking anticholinergic type antiparkinson drugs, including benztropine, in combination with phenothiazines and/or tricyclic antidepressants.
Genitourinary Dysuria may occur. Since benztropine mesylate has cumulative action, continued supervision of patient is advisable, especially in patients with prostatic hypertrophy.
Immune Occasionally, an allergic reaction develops ( e.g. skin rash). This may be controlled by reducing the dosage, but, occasionally, the drug may need to be discontinued.
Musculoskeletal The starting daily dosage of benztropine is 0.5 – 1 mg with a maximum of 6 mg. In large doses (upper range), benztropine mesylate may cause complaints of weakness and inability to move particular muscle groups. For example, if the neck has been rigid and suddenly relaxes, it may feel weak, causing some concerns. In this event, dosage adjustment is required.
Neurologic Mental confusion, visual hallucinations and agitation may occur with large doses, or in susceptible patients.
Tardive dyskinesia may appear in some patients on long-term therapy with phenothiazines and related agents, or may occur after therapy with these drugs has been discontinued. Antiparkinson drugs usually do not alleviate the symptoms of tardive dyskinesia, and in some instances may aggravate or unmask such symptoms. Benztropine mesylate is not recommended in tardive dyskinesia.
Occupational Hazards Benztropine mesylate may impair mental and/or physical abilities required for performance of hazardous tasks, such as operating machinery or driving a motor vehicle.
Ophthalmologic The occurrence of glaucoma is possible. Although the drug does not appear to have any adverse effect on simple glaucoma, it should not be used in narrow angle glaucoma (see CONTRAINDICATIONS).
Psychiatric The psychotogenic potential of antiparkinson drugs should be considered when managing patients with mental disorders. When benztropine mesylate is used to treat extrapyramidal symptoms due to CNS drugs such as phenothiazine derivatives and reserpine in patients with a mental disorder, occasionally, there may be intensification of mental disorders. When using benztropine mesylate in these patients, they should be kept under careful observation, especially at the beginning of treatment or if dosage is increased.
Special Populations
Pregnant Women: The use of this drug in pregnancy has not been studied.
Pediatrics: Because of its atropine-like side effects, pdp-BENZTROPINE is contraindicated in children less than 3 years of age, and should be used with caution in older children.
Geriatrics : Generally, older patients cannot tolerate large doses (see DOSAGE AND ADMINISTRATION).
response to either drug if they are used concurrently.
MAO inhibitors (e.g. moclobemide, phenelzine, tranylcypromine, methylene blue)
Motion sickness medication (e.g. scopolamine, dimenhydrinate) – decrease cholinergic effects/transmission. Additive anticholinergic adverse effects may be seen with concurrent use.
Narcotic pain relievers (e.g. codeine, meperidine, morphine)
Potassium Chloride – Slowed gastric emptying due to the anticholinergic effect of benztropine can increase the risk of gastrointestinal irritation or ulceration associated with solid oral potassium dosage forms. Avoid concurrent use when possible. Liquid forms of potassium may be preferable.
Tricyclic antidepressants (e.g., amitriptyline, doxepin) – decrease cholinergic effects/transmission. Additive anticholinergic adverse effects may be seen with concurrent use.
Drug-Food Interactions Interactions with food have not been established.
Drug-Herb Interactions Interactions with herbal products have not been established.
Drug-Laboratory Interactions False test results may result with certain medical/laboratory tests (including brain scan for Parkinson’s disease).
Drug-Lifestyle Interactions Ethanol can increase the sedative effects of benztropine.
Dosing Considerations Benztropine mesylate has cumulative action, thus, therapy should be initiated with a low dose which is increased gradually at 5 or 6 day intervals to the smallest amount necessary for optimal relief. Initially, 0.5 mg (1.25 mL oral solution) is given daily. Increases should be made in increments of 0.5 mg (1.25 mL oral solution) or until optimal results are obtained without excessive adverse effects (maximum dose of 6 mg (15 mL oral solution)).
There are no adequate and well controlled studies on benztropine mesylate use in pediatric or geriatric patients. The dosage should be individualized based on severity of symptoms, patient characteristics and the type of Parkinsonism being treated. Dosing recommendations are based on clinical experience. In general, treatment should begin at the lowest dose, with gradual increases until maximum improvements are noted or intolerable adverse events occur.
Recommended Dose and Dosage Adjustment
Arteriosclerotic, idiopathic and postencephalitic Parkinsonism:
Adults The usual daily dose is 1 mg to 2 mg (2.5 mL to 5 mL oral solution) with a range of 0.5 mg to 6 mg (1.25 mL to 15 mL oral solution).
Patients with a poor mental outlook are usually poor candidates for therapy.
In arteriosclerotic and idiopathic Parkinsonism , therapy may be initiated with a single daily dose of 0.5 mg to 1 mg (low dose) (1.25 mL to 2.5 mL oral solution) at bedtime. In some patients, this will be adequate; in others, 4 mg to 6 mg (10 mL to 15 mL oral solution) a day may be required. Generally, older patients, thin patients and those with arteriosclerotic Parkinsonism cannot tolerate large doses.
In postencephalitic Parkinsonism , therapy may be initiated with 2 mg a day in 1 or more doses. In highly sensitive patients, therapy may be initiated with 0.5 mg (1.25 mL oral solution) at bedtime, and increased as necessary. Most patients with postencephalitic Parkinsonism need fairly large doses and tolerate them well.
Some patients experience greatest relief by taking the entire daily dose at bedtime; others react more favourably to divided doses (2 to 4 times a day).
Therapy with other agents should not be terminated abruptly when therapy with benztropine mesylate is initiated, but may be reduced or discontinued gradually. Benztropine mesylate may be administered concomitantly with levodopa or a levodopa/carbidopa combination, in which case the dose of each may need adjustment.
Pediatric > 3 years The usual dose is 0.02 mg/kg – 0.05 mg/kg (0.05 mL/kg - 0.125 mL/kg oral solution) administered orally 1-2 times a day.
Drug-induced extrapyramidal symptoms: In treating extrapyramidal disorders due to phenothiazine derivatives or reserpine, the recommended dosage is 1 mg to 4 mg (2.5 mL to 10 mL oral solution) once or twice a day. Dosage must be individualized according to the need of the patient.
In acute dystonic reactions, 2 mg of benztropine mesylate i.v. quickly relieves the condition. Then, 1 mg to 2 mg (2.5 mL to 5 mL oral solution) given orally twice a day usually prevents recurrence.
When extrapyramidal disorders develop soon after initiation of treatment with phenothiazine derivatives or reserpine, they are likely to be transient. One (1 mg) to 2 mg (2.5 mL to 5 mL oral solution), 2 or 3 times a day usually provides relief within 1 to 2 days. After 1 or 2 weeks,
Mechanism of Action Benztropine mesylate contains the tropine portion of the atropine molecule and the benzohydryl portion of diphenhydramine. Thus, it possesses both anticholinergic and antihistaminic effects, although only the former has been established as therapeutically significant in the management of Parkinsonism.
Pharmacokinetics The mean C (^) max of 1.5 PO single dose is 2.5 ng/mL with a mean elimination half-life (t1/2 ) of 7 hours.
Benztropine is well-absorbed from the gastrointestinal tract. When given orally, benztropine has an onset of action of between 1 to 2 hours, though the pharmacologic effects of the drug may not be apparent for 2 to 3 days after initiation of therapy. The duration of action of benztropine, when given orally, is approximately 24 hours. Benztropine is highly protein bounded (95%), has a hepatic metabolism in animals, and is excreted primarily through the urine and bile unchanged.
Store at room temperature (15°C-30°C).
1 mg tablets: Supplied in bottles of 100 and 1000 tablets. Each round, cylindrical, bevelled-edge, flat faced, salmon coloured tablet cross-scored on one side and identified "PMS-1" on the other side contains 1 mg of benztropine mesylate and the following non-medicinal ingredients: FD&C Yellow No. 6 Aluminum Lake, lactose monohydrate, magnesium stearate, microcrystalline cellulose and pregelatinized starch.
0.4 mg/mL oral solution:
Supplied in bottles of 500 mL. Each mL of yellow, orange-flavoured solution contains 0.4 mg of benztropine mesylate and the following non- medicinal ingredients: alcohol, FD&C Yellow No. 6, glycerin methylparaben, orange flavor, propylparaben, purified water, sodium benzoate, sodium saccharin.
Drug Substance
Proper name: Benztropine mesylate
Chemical name: 8-azabicyclo[3.2.1] octane, 3-(diphenylmethoxy)-,endo, methanesulfonate.
Molecular formula and molecular mass: C 21 H 25 NO·CH 4 O 3 S 403.
Structural formula:
Physicochemical properties: Crystalline white powder, very soluble in water.
In the laboratory, the antihistaminic activity of benztropine mesylate approaches that of pyrilamine maleate. Its duration of action also approaches that of pyrilamine maleate.
In the isolated guinea pig ileum, benztropine mesylate anticholinergic activity is about equal to that of atropine; however, when administered orally to unanesthetized cats, it is only about half as active as atropine.
IMPORTANT: PLEASE READ
PART III: CONSUMER INFORMATION Pr (^) pdp-BENZTROPINE
Benztropine Mesylate Tablets, USP, 1 mg
Benztropine Mesylate Oral Solution, 0.4 mg/mL
Read this carefully before you start taking pdp-BENZTROPINE and each time you get a refill. This leaflet is a summary and will not tell you everything about pdp-BENZTROPINE. Talk to your doctor, nurse, or pharmacist about your medical condition and treatment and ask if there is any new information about pdp- BENZTROPINE.
ABOUT THIS MEDICATION
What the medication is used for: pdp-BENZTROPINE is recommended for:
What it does: pdp-BENZTROPINE is an Antiparkinson drug. It acts on the nervous system to correct some of the chemical imbalances that cause the symptoms of Parkinson’s disease and movement disorders.
When it should not be used:
What the medicinal ingredient is: Benztropine mesylate.
What the non-medicinal ingredients are: 1 mg tablets: FD&C Yellow No. 6 Aluminum Lake, lactose monohydrate, magnesium stearate, microcrystalline cellulose and pregelatinized starch. 0.4 mg/mL solution: alcohol, FD&C Yellow No. 6, glycerin methylparaben, orange flavor, propylparaben, purified water, sodium benzoate, sodium saccharin.
What dosage forms it comes in: Tablet (1 mg); solution (0.4 mg/mL).
WARNINGS AND PRECAUTIONS
BEFORE you use pdp-BENZTROPINE talk to your doctor or pharmacist if:
or twitches of the body, face, eyes or tongue, stretching the neck and body)
pdp-BENZTROPINE may affect your ability to sweat. This can lead to dangerous increases in body temperature. Tell your doctor if you have a condition that affects your ability to sweat, and:
Driving and using machines: Before you perform tasks which may require special attention, wait until you know how you respond to pdp-BENZTROPINE.
INTERACTIONS WITH THIS MEDICATION
As with most medicines, interactions with other drugs are possible. Tell your doctor, nurse, or pharmacist about all the medicines you take, including drugs prescribed by other doctors, vitamins, minerals, natural supplements, or alternative medicines.
Drugs that may interact with pdp-BENZTROPINE include:
If you already take other drugs to treat Parkinson’s disease, the doctor may decide to adjust or gradually discontinue them. Do not suddenly stop taking them. Always follow your doctor’s instructions.
IMPORTANT: PLEASE READ
PROPER USE OF THIS MEDICATION
Dosage must be individualized according to the need of the patient. pdp-BENZTROPINE is usually started at a low dose and increased gradually every 5 or 6 days until the smallest effective dose is found. pdp-BENZTROPINE is taken by mouth.
Many factors can affect the dose of medication that a person needs, such as age, body weight, other medical conditions, and other medications. If your doctor has recommended a dose different from the ones listed here , do not change the way you are taking the medication without consulting your doctor.
Usual adult dose: Symptoms of Parkinson’s Disease: Initial dose: 0.5 mg (1/4 teaspoon (1.25 mL) oral solution) a day. Maximum dose: 6 mg (3 teaspoons (15 mL) oral solution) a day.
Usual Dose: 1 mg to 2 mg a day (1/2 to 1 teaspoon (2.5 mL to 5 mL)). The dose can range from 0.5 mg to 6 mg (1/4 to 3 teaspoons (1.25 mL to 15 mL)) a day depending on circumstances.
Your doctor may recommend you take:
Dose for children more than 3 years old: Dosage should be individualized based on the weight of the child. Usual dose: 0.02 mg/kg – 0.05 mg/kg (0.05 mL/kg-0.125 mL/kg oral solution) 1-2 times a day.
Movement Disorders: Recommended dose : 1 mg to 4 mg (1/2 to 2 teaspoons (2.5 mL to 10 mL)) once or twice a day.
Your doctor may recommend you take your dose as one, two or three doses in a day. After 1 or 2 weeks, your doctor may stop pdp-BENZTROPINE to determine if you still need it. pdp- BENZTROPINE may need to be restarted if your movement disorder returns.
Overdose: In case of drug overdose, contact a health care practitioner, hospital emergency department or regional Poison Control Centre immediately, even if there are no symptoms.
Missed Dose: If you miss a dose, take it as soon as you remember. If it is near the time of the next dose, skip the missed dose and resume your usual dosing schedule. Do not double the dose to catch up.
SIDE EFFECTS AND WHAT TO DO ABOUT THEM
Side effects may include:
SERIOUS SIDE EFFECTS, HOW OFTEN THEY HAPPEN AND WHAT TO DO ABOUT THEM
Symptom / effect Talk with your doctor or pharmacist
Stop taking drug and seek immediate medical help
Only if severe
In all cases
Common Severe dry mouth: difficulty swallowing or speaking, loss of appetite and weight
√
Nausea (^) √ Vomiting (^) √
Frequency Unknown
Dysuria: Painful or difficult urination √ Paralytic ileus: (Bowel Obstruction): abdominal pain and discomfort, constipation, nausea, vomiting, excessive burping
√
Tachycardia: fast heartbeat. √ Weakness and an inability to move certain muscle groups
√
Mental Confusion (^) √ Worsening of Mental Disorders √ Hallucinations: see or hear things that are not there
√
Glaucoma: increased pressure in your eyes, eye pain
√
Depression: Feeling sad, unexplained weight change, sleep disturbances, lack of interest in usual activities
√
Uncommon Allergic Reaction: rash, hives, swelling of the face, lips, tongue or throat, difficulty swallowing or breathing
√
This is not a complete list of side effects. For any unexpected effects while taking pdp-BENZTROPINE, contact your doctor or pharmacist.
