Rivastigmine: Difference between revisions

From SEHK Wiki
← Older editNewer edit →
Helen (talk | contribs)
2,599 edits
Zeki (talk | contribs)
1,402 edits
No edit summary
Line 1: Line 1:
[[Category: Drugs]] [[Category: Acetylcholinesterase inhibiting drug]]
[[Category: Drugs]][[Category: Acetylcholinesterase inhibitor]]
'''Rivastigmine''' (中文: [[利凡斯的明]]) is a reversible acetylcholinesterase inhibitor. Rivastigmine is selective for the CNS and is used for the treatment of mild to moderate dementia associated with Parkinson’s disease.  
 
[[:Category: Antidementia Drug | '''Antidementia Drug''']]
 
'''Drug class: [[:Category: Acetylcholinesterase inhibitor | Acetylcholinesterase Inhibitor]]'''
 
'''Rivastigmine (EXELON)''' (中文: [[利凡斯的明]]) is a reversible acetylcholinesterase inhibitor. Rivastigmine is selective for the CNS and is used for the treatment of mild to moderate dementia associated with Parkinson’s disease.  
==Pronunciation==
==Pronunciation==
===Rivastigmine 1.5mg (EXELON 1.5mg)===
===Rivastigmine 1.5mg (EXELON 1.5mg)===
Line 11: Line 16:
[[File:Rivastigmine 4.5mg (EXELON 4.5mg).mp3]]
[[File:Rivastigmine 4.5mg (EXELON 4.5mg).mp3]]


==Mechanism of Action==
==Common Strengths==
Acetylcholinesterase inhibiting drug.
*Oral Capsules: 1.5 mg, 3 mg, 4.5 mg, 6 mg
 
*Transdermal Patches: 4.6 mg/24 hours, 9.5 mg/24 hours, 13.3/24 hour
{| class="wikitable"
!Generic Name
藥名
!HA Code 藥物代碼
!Classification藥物分類
|-
|Rivastigmine Cap 1.5 mg
|RIVA01
|P1S1S3
|-
|Rivastigmine Cap 3 mg
|RIVA02
|P1S1S3
|-
|Rivastigmine Cap 6 mg
|RIVA04
|P1S1S3
|}
 
==Dosage==
The drug can be administered orally or via a transdermal patch; the latter form reduces the prevalence of side effects, which typically include nausea and vomiting.


===By Oral===
==Drug Trade Names==
*initially 1.5 mg twice daily, increased in steps of 1.5 mg twice daily at intervals of at least 2 weeks according to response and tolerance.
*Exelon
*Usual range 3-6 mg twice daily.
*Maximum 6 mg twice daily.
*If treatment interrupted for more than several days, treatment should be retitrated from 1.5 mg twice daily.


Transdermal patches delivering 4.6, 9.5, or 13.3 mg of rivastigmine over 24 hours are also available for once-daily application.  
==Drug Usage==
For managing symptoms of dementia, improving cognitive function and daily living activities in affected individuals. It is not a cure but may help slow the progression of symptoms.


===Transdermal application===
==Mechanism of Action==
*initially apply 4.6 mg/24 hours patch to clean, dry, non-hairy, non-irritated skin on back, upper arm, or chest, removing after 24 hours.
Rivastigmine works by inhibiting acetylcholinesterase, the enzyme responsible for breaking down acetylcholine in the brain. This inhibition leads to increased level of acetylcholine, which is crucial for memory and cognitive function.
*It should not be applied to the abdomen or thigh due to decreased bioavailability.  
*Re-application to the same site should be avoided for 14 days.
*Only one patch should be applied at a time.  


If well tolerated, increase to 9.5 mg/24 hours patch daily.
==Route of Administration==
Rivastigmine can be administered:
*Orally (capsules)
*Transdermally (patch)


After a further 6 months if well tolerated and cognitive deterioration or functional decline are shown, the dose can be increased to 13.3 mg/24 hours patch daily.
==Dosage==
 
*Initial: 1.5 mg orally twice daily; may increase every two weeks up to a maximum of 6 mg twice daily.
However, for patients with a body weight below 50 kg, a maintenance dose of 4.6 mg/24 hours daily may be sufficient.
*Transdermal: Start with a patch delivering 4.6 mg/24 hours, with potential increases based on tolerance.


===Conversion of oral rivastigmine to patches are as follows===
'''Conversion of oral rivastigmine to patches are as follows
*Those taking ≤ 6 mg daily of oral rivastigmine may be switched to 4.6 mg/24 hours patch.
*Those taking ≤6 mg daily of oral rivastigmine may be switched to 4.6 mg/24 hours patch.
*Those taking more than 6 mg daily may be switched to 9.5 mg/24 hours patch.
*Those taking more than 6 mg daily may be switched to 9.5 mg/24 hours patch.
*The first patch should be applied on the day following the last oral dose.  
*The first patch should be applied on the day following the last oral dose.  


Clinical benefit should be assessed on a regular basis.
'''How quickly dose Rivastigmine patch work?
 
===How quickly dose Rivastigmine patch work?===
Rivastigmine may take as long as 12 weeks to begin working and individual response to this medication will vary.
Rivastigmine may take as long as 12 weeks to begin working and individual response to this medication will vary.


==Side Effects==
==Side Effects==
Significant gastrointestinal side effects include
{| class="wikitable"
*Nausea and vomiting
!style="text-align: left"| Frequency
*Loss of appetite
!Adverse reactions
*Weight loss
|-
*Diarrhea
| rowspan="5" | '''Common Side Effects
 
| Nausea
Serious side effects may include:
|-
*Abnormal heart rhythms
| Vomiting
*Difficulty emptying urine from the bladder
|-
*seizures
| Loss of appetite
|-
| Diarrhea
|-
| Dizziness
|-
| rowspan="3" | '''Serious Side Effects
| Sever allergic reactions (e.g. difficulty greathing)
|-
| Seizures
|-
| Involuntary movement or tremors
|}


==Pharmacokinetics==
==Pharmacokinetics==
It is available in two primary formulations: capsules and transdermal patches. The pharmacokinetics of these two forms differ significantly
*The transdermal patch provides a continuous release of rivastigmine over 24 hours, leading to a smoother pharmacokinetic profile with lower peak plasma concentrations compared to oral capsules.
*The patches are designed to minimize fluctuations in drug levels, which can enhance tolerability and compliance among patients.


{| class = "wikitable"
Summary of Key Differences
!style="text-align: left"| Oral bioavailability
{| class="wikitable"
|Donepezil hydrochloride is rapidly and well absorbed from the gastrointestinal tract. Plasma protein binding is about 40%.
!style="text-align: left"| Feature
!Capsules
!Transdermal Patch
|-
|-
!style="text-align: left"| Onset of action
| Absorptions Peak Time
|Peak plasma levels in about one hour after ingestion. Absorption from transdermal patches is slow and peak plasma concentrations are reached in 10 to 16 hours after applying the first patch; with subsequent patches, peak concentrations are reached in about 8 hours.
| ~1 hour
| Continuous over 24 hours
|-
|-
!style="text-align: left"| Metabolism
| Elimination half-life
|Primarily metabolized through hydrolysis. Minimal metabolism occurs via the cytochrome P450. 
| ~1 hour
| ~1 hour
|-
|-
!style="text-align: left"| Elimination half-life
| Dosing Flexibility
|1.5 hours after oral doses and about 3 hours after patch removal.
| Requires titration
| Steady release
|}
|}


Revision as of 23:04, 6 November 2024


Antidementia Drug

Drug class: Acetylcholinesterase Inhibitor

Rivastigmine (EXELON) (中文: 利凡斯的明) is a reversible acetylcholinesterase inhibitor. Rivastigmine is selective for the CNS and is used for the treatment of mild to moderate dementia associated with Parkinson’s disease.

Pronunciation

Rivastigmine 1.5mg (EXELON 1.5mg)

Rivastigmine 3mg (EXELON 3mg)

Rivastigmine 4.5mg (EXELON 4.5mg)

Common Strengths

  • Oral Capsules: 1.5 mg, 3 mg, 4.5 mg, 6 mg
  • Transdermal Patches: 4.6 mg/24 hours, 9.5 mg/24 hours, 13.3/24 hour

Drug Trade Names

  • Exelon

Drug Usage

For managing symptoms of dementia, improving cognitive function and daily living activities in affected individuals. It is not a cure but may help slow the progression of symptoms.

Mechanism of Action

Rivastigmine works by inhibiting acetylcholinesterase, the enzyme responsible for breaking down acetylcholine in the brain. This inhibition leads to increased level of acetylcholine, which is crucial for memory and cognitive function.

Route of Administration

Rivastigmine can be administered:

  • Orally (capsules)
  • Transdermally (patch)

Dosage

  • Initial: 1.5 mg orally twice daily; may increase every two weeks up to a maximum of 6 mg twice daily.
  • Transdermal: Start with a patch delivering 4.6 mg/24 hours, with potential increases based on tolerance.

Conversion of oral rivastigmine to patches are as follows

  • Those taking ≤6 mg daily of oral rivastigmine may be switched to 4.6 mg/24 hours patch.
  • Those taking more than 6 mg daily may be switched to 9.5 mg/24 hours patch.
  • The first patch should be applied on the day following the last oral dose.

How quickly dose Rivastigmine patch work? Rivastigmine may take as long as 12 weeks to begin working and individual response to this medication will vary.

Side Effects

Frequency Adverse reactions
Common Side Effects Nausea
Vomiting
Loss of appetite
Diarrhea
Dizziness
Serious Side Effects Sever allergic reactions (e.g. difficulty greathing)
Seizures
Involuntary movement or tremors

Pharmacokinetics

It is available in two primary formulations: capsules and transdermal patches. The pharmacokinetics of these two forms differ significantly

  • The transdermal patch provides a continuous release of rivastigmine over 24 hours, leading to a smoother pharmacokinetic profile with lower peak plasma concentrations compared to oral capsules.
  • The patches are designed to minimize fluctuations in drug levels, which can enhance tolerability and compliance among patients.

Summary of Key Differences

Feature Capsules Transdermal Patch
Absorptions Peak Time ~1 hour Continuous over 24 hours
Elimination half-life ~1 hour ~1 hour
Dosing Flexibility Requires titration Steady release

Drug Management

Monitoring

  • acetylcholinesterase inhibitor may increase gastric acid secretion, so patients should be monitored closely for GI bleeding, especially those receiving concurrent NSAID drugs.
  • check body weight regularly
  • monitor the cognitive, global functions, and ADL activities
  • monitor the sleeping quality

Caution

  • Cardiovascular conduction disorders such as sick-sinus syndrome
  • Susceptibility to peptic ulcers
  • Asthma, chronic obstructive pulmonary disease
  • People who have a predisposition to seizures
  • Concomitant antipsychotic treatment – increased risk of neuroleptic malignant syndrome

Contraindications

Patients with known hypersensitivity to rivastigmine.

Hepatic impairment

Titrate according to individual tolerability in mild to moderate impairment; use with caution in severe impairment.

Renal impairment

Titrate according to individual tolerability

Effects on ability to drive and use machinery

Rivastigmine can cause fatigue, dizziness and muscles, mainly when initiating or increasing the dose. The treating doctor should routinely evaluate the ability of patients on donepezil to continue driving or operating complex machines.

FAQ

How should I take Rivastigmine?

If you are taking the capsules, swallow them whole with a full glass of water, with your morning and evening meals. Do not open or crush the capsules.

If you are using the patch, apply it to a clean, dry and hairless skin area on your upper or lower back, upper arm, or chest. Do not put the patch over rashes, cuts, or irritated skin. Do not apply to the same area for 14 days.

How often do I change Rivastigmine Patch?

Change the patch every 24 hours around the same time.

What should I avoid while taking?

Avoid abruptly discontinue the medication.

What happen if I overdose?

Contact your primary care doctor. If emergency situation, call 999

What happen if I miss a dose?

Take it as soon as you remember. If it is near the time of the next dose, skip the missed dose. Take your next dose at the regular time. Do not double the dose to catch up.

Retrieved from "https://www.sehk-wiki.org/index.php?title=Rivastigmine&oldid=4819"