Drug Information

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.

Rivastigmine hydrogen tartarate-@-Exelon Patch (Oct 2014 )

Drug Interaction

Indication

Adverse Reaction

Contra-Indications

Dosages/ Overdosage Etc

Patient Information

Pharmacology/ Pharmacokinetics

Pregnancy and lactation