Drug Interaction:
Not to be used with other cholinergic drugs that might interfere with the activity of anticholinergic medications May exaggerate the effects of succinyl choline -type muscle relaxants during anesthesia Tobbocco smoking increase its clearance
Indication:
U.S FDA APPROVED DRUGS FROM 01-01-08 TO 31-12-08
Drug name Indication Date of Approval
35. Rivastigmine transdermal patch 28-01-08
(each patch of 5m2 ,10m2,15m2 & 20m2
contain Rivastigmine base 9/18/27/36mm respy
For the treatment of patients with mild to moderately
severe dementia of the Alzheimer type and dementia
associated with Parkinsons disease
EXELON® PATCH (rivastigmine transdermal system)
Initial U.S. Approval: 2000
RECENT MAJOR CHANGES
Dosage and Administration (2.2, 2.4) 1/2015
Warnings and Precautions (5.1, 5.3) 1/2015
Rivastigmine transdermal patch -
Each Transdermal patch of 15cm2 contains
Rivastigmine 27mg (Additional indication)
Indication-
For the treatment of patients with severe dementia of the Alzeheimers type
Approved by FDA on 28-10-2014 (Ref- FDA approved List- 2014)
Mild to moderately dementia in Alzhelmers disease
New Drugs Approved by (DCI) Drug Controller GENERAL - India For Marketing
(Ref- IDMA Publication)
Name of Drug Indication Date of Approval
1.Riovastigmine Caps 31-07-1998
Acetylcholine esterase Inhibitor agent
2.Rivastigmine Transdermal patch 28-01-2008
Each patch of 5M2,10M2,15M2, & 20M2
contain Rivastigmine Base 9/18/27/36mg respy
For the treatment of patients with mild to moderately severe dimentia
of the Alzheimer Type and Dementia associated with Parkinsons disease
3. Rivastigmine Transdermal Patch 28-10-2014
Eachtransdermal patch of 15cm2
contains Rivastigmine 27mg
Addl.stgth
For the treatment of patients with severe Dementia of the Alzheimers type
Adverse Reaction:
Accidental trauma, fatigue, asthenia dizziness, headache, somloence agitation, insomnia, confusion depression, nausea, vomiting diarrhoea, abdominal pain, loss of appetite, dyspepsia upper respiratory tract infetion, urinary tract infection, rarely angina pectoris gastric and duodenunal ulcers GI haemorrhage bradycardia, seizures rashes and syncope serious GI reactions such as anorexia, vomiting and weight loss
Contra-Indications:
Hypersensitivity to other carbamate derivatives. Severe hepatic impirment
Special precautions-
Patients with sick sinus syndrome or conduction defects, respiratory diseases Chloinergic stimulation may increase gastric acid secretion
May execerbate urinary obstruction and seizures Renal impairment, mild moderate hepatic impairment
Monitor body weight, asthma or obstructive pulmonary disease May worsen extrapyrimidal symptoms Pregnancy Lactation
Dosages/ Overdosage Etc:
Indication-
For the treatment of patients with severe dementia of the Alzeheimers type
Mild to moderately dementia in Alzhelmers disease
Dosage-
Adult - initially 1.5mg bid, increasing according to response by 1.5mg at intervals of 2 weeks If treatment is interrupted for > a few days, restart at 1.5mg bid and increase dose accordingly, if required. Max 6mg bid
Patient Information:
PATIENT COUNSELING INFORMATION
Advise the patient to read the FDA-approved patient labeling (Patient Information
and Instructions for Use).
Importance of Correct Usage
Inform patients or caregivers of the importance of applying the correct dose on the
correct part of the body. They should be instructed to rotate the application site
in order to minimize skin irritation. The same site should not be used
within 14 days. The previous day’s patch must be removed before applying
a new patch to a different skin location.
EXELON PATCH should be replaced every 24 hours and the time of day should
be consistent. It may be helpful for this to be part of a daily routine, such as
the daily bath or shower. Only 1 patch should be worn at a time.
Instruct patients or caregivers to avoid exposure of the patch to external heat
sources (excessive sunlight, saunas, solariums) for long periods of time.
Instruct patients who have missed a dose to apply a new patch immediately.
They may apply the next patch at the usual time the next day
Instruct patients to not apply 2 patches to make up for 1 missed.
Inform the patient or caregiver to contact the physician for retitration instructions
if treatment has been interrupted.
Discarding Used Patches
Instruct patients or caregivers to fold the patch in half after use, return the used
patch to its original pouch, and discard it out of the reach and sight of children
and pets.
They should also be informed that drug still remains in the patch after 24-hour usage.
They should be instructed to avoid eye contact and to wash their hands afte
handling the patch. In case of accidental contact with the eyes, or if their eyes
become red after handling the patch, they should be instructed to rinse
immediately with plenty of water and to seek medical advice if symptoms
do not resolve.
Gastrointestinal Adverse Reactions
Inform patients or caregivers of the potential gastrointestinal adverse reactions
such as nausea, vomiting, and diarrhea, including the possibility of dehydration
due to these symptoms.
Explain that EXELON PATCH may affect the patient’s appetite and/or the patient’s
weight. Patients and caregivers should be instructed to look for these
adverse reactions, in particular when treatment is initiated or the dose is increased.
Instruct patients and caregivers to inform a physician if these adverse reactions
persist.
Skin Reactions
Inform patients or caregivers about the potential for allergic contact dermatitis
reactions to occur.
Patients or caregivers should be instructed to inform a physician if application
site reactions spread beyond the patch size, if there is evidence of a more intense
local reaction (e.g., increasing erythema, edema, papules, vesicles) and if
symptoms do not significantly improve within 48 hours after patch removal.
Concomitant Use of Drugs with Cholinergic Action
Inform patients or caregivers that while wearing EXELON PATCH, patients
should not be taking Exelon Capsules or Exelon Oral Solution or other drugs
with cholinergic effects.
Pharmacology/ Pharmacokinetics:
CLINICAL PHARMACOLOGY
1. Mechanism of Action
Although the precise mechanism of action of rivastigmine is unknown, it is thought to
exert its therapeutic effect by enhancing cholinergic function. This is accomplished
by increasing the concentration of acetylcholine through reversible inhibition of its
hydrolysis by cholinesterase. The effect of rivastigmine may lessen as the
disease process advances and fewer cholinergic neurons remain functionally intact.
There is no evidence that rivastigmine alters the course of the underlying dementing process.
2. Pharmacokinetics
Absorption
After the initial application of EXELON PATCH, there is a lag time of 0.5 to 1 hour
in the absorption of rivastigmine. Concentrations then rise slowly typically
reaching a maximum after 8 hours, although maximum values (Cmax) can
also occur later (at 10 to 16 hours) or after of the 24-hour period of application.
At steady state, trough levels are approximately 60% to 80% of peak levels.
Pregnancy and lactation:
USE IN SPECIFIC POPULATIONS
1 Pregnancy
Pregnancy Category B
There are no adequate and well-controlled studies in pregnant women. No dermal
reproduction studies in animals have been conducted.Oral reproduction studies
conducted in pregnant rats and rabbits revealed no evidence of teratogenicity.
Because animal reproduction studies are not always predictive of huma
response, this drug should be used during pregnancy only if clearly needed.
2. Nursing Mothers
Rivastigmine and its metabolites are excreted in rat milk following oral administration
of rivastigmine; levels of rivastigmine plus metabolites in rat milk are approximately
2 times that in maternal plasma. It is not known whether rivastigmine is excreted
in human milk. Because many drugs are excreted in human milk and because
of the potential for serious adverse reactions in nursing infants from
EXELON PATCH, a decision should be made whether to discontinue nursing
or to discontinue the drug, taking into account the importance of the drug to the mother.
3. Pediatric Use
Safety and effectiveness in pediatric patients have not been established.
The use of EXELON PATCH in pediatric patients (below 18 years of age)
is not recommended.
4. Geriatric Use
Of the total number of patients in clinical studies of EXELON PATCH, 88% were
65 years and over, while 55% were 75 years. No overall differences in
safety or effectiveness were observed between these patients and younger
patients, and other reported clinical experience has not identified differences
in responses between the elderly and younger patients, but greater sensitivity
of some older individuals cannot be ruled out.
Manufacturer Details