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↑ = object drug increased; ↓ = object drug decreased; ↔ = undetermined clinical effect

روش و مقدار مصرف ريواتكس® (مورد تاييد FDA)

1/5 ميلي گرم دوبار در روز  پس از چهار هفته 3 ميلي گرم دوبار در روز پس از چهار هفته 4/5 ميلي گرم دوبار در روز  پس از چهار هفته  6 ميلي گرم دوبار در روز 

Rivatex®

Generic Name: RIVASTIGMINE

Category: Dementia symptoms treatment adjunct.

Composition:

Rivatex® 1.5mg: Each Capsule contain rivastigmine tartrate, equivalent

to 1.5 mg of Rivastigmine.

Rivatex® 3mg: Each Capsule contain rivastigmine tartrate, equivalent

to 3 mg of Rivastigmine.

Rivatex® 4.5mg: Each Capsule contain rivastigmine tartrate, equivalent

to 3 mg of Rivastigmine.

Rivatex® 6mg: Each Capsule contain rivastigmine tartrate, equivalent

to 6 mg of Rivastigmine.

Actions and Pharmacokinetics:

Rivatex®'s primary effect is the reversible inhibition of cholinesterase.

This inhibition is thought to increase the level of acetylcholine available

in the central nervous system. Increased levels of acetylcholine have

been found in the cerebrospinal fluid of patients receiving Rivatex®.

There is no evidence that Rivatex® alters the underlying dementing

process, and its effect may lessen as the disease progresses.

Absorption: Rivatex® is rapidly absorbed. The absolute bioavailability

is about 40%. Rivatex® shows linear pharmacokinetics with doses up to

3 milligrams twice daily but is non-linear at higher doses. There is a 3-

fold increase in area under the curve when the dose is doubled from 3 to

6 milligrams twice daily. Food delays absorption.

Distribution: Mean volume of distribution (VolD) is 1.8 to 2.7 L/kg.

Rivatex® penetrates the blood brain barrier.

Protein binding: Moderate (40%).

Biotransformation: Rivatex® is rapidly metabolized, primarily via

cholinesterase-mediated hydrolysis. The cytochrome 450 isozymes are

minimally involved.

Half-life: Elimination 1.5 hours.

Time to peak concentration: 1 hour.

Duration of action: Anticholinesterase activity is present in CSF for 10

hours

Elimination: Mostly as metabolites via the urine. After a radiolabeled

dose was administered, 97% and 0.4% were recovered in the urine and

feces, respectively, over 120 hours. The sulfate conjugate of the

decarbamylated metabolite represents 40% of the dose in the urine.

Indications:

Rivatex® is indicated for the treatment of mild to moderate dementia

of the Alzheimer's type.

It is also indicated for the treatment of mild to moderate dementia

associated with Parkinson’s disease.

Contraindications:

Except under special circumstances, this medication should not be

used when the following medical problem exists: Known hypersensitivity

to Rivatex® or other carbamate derivatives

Risk-benefit should be considered when the following medical problems

exist:

Asthma, bronchial, active or latent (asthma attack may be precipitated),

Cardiovascular conditions, such as: Bradycardia or Sick sinus syndrome

(vagotonic effect on heart may exacerbate pre-existing conditions),

Epilepsy or history of seizures or Metabolic disorders, unstable (Seizures

may occur), Gastrointestinal or urinary tract obstruction (increased

activity of gastrointestinal tract or urinary bladder may be harmful),

Peptic ulcer, active or history of (increased gastric acid secretion may

exacerbate or reactivate condition).

Note: Because of their pharmacological action, cholinesterase inhibitors

may be expected to increase gastric acid secretion due to increased

cholinergic activity. Therefore, patients should be monitored closely for

symptoms of active or occult gastrointestinal bleeding, especially those

at increased risk for developing ulcers (e.g., those with a history of ulcer

or those receiving concurrent NSAIDs).

Drug interactions:

Combinations containing any of the following medications, depending

on the amount present, may also interact with this medication.

Anticholinergics, Cholinomimetics (e.g., bethanecol) and cholinesterase

inhibitors (e.g., neostigmine)

Neuromuscular blocking agents metabolized by plasma cholinesterase

(e.g., succinylcholine, mivacurium) , NSAIDs.

Precautions:

Rivatex® use is associated with significant gastrointestinal adverse

reactions, including nausea and vomiting, anorexia, and weight loss.

For this reason, patients should always be started at a dose of 1.5 mg

BID and titrated to their maintenance dose.

Pregnancy: Studies in rats showed slightly decreased fetal/pup weights,

usually at doses causing some maternal toxicity; decreased weights

were seen at doses which were several fold lower than the maximum

recommended human dose on a mg/m 2 basis. There are no adequate

or well-controlled studies in pregnant women. Because animal

reproduction studies are not always predictive of human response,

Rivatex® should be used during pregnancy only if the potential benefit

justifies the potential risk to the fetus.

FDA Pregnancy Category: B

Breast-feeding: Problems in humans have not been documented. It is

not known whether Rivatex® is distributed into breast milk. However,

use of Rivatex® is not recommended in nursing mothers.

Pediatrics: No information is available on the relationship of age to the

effects of Rivatex® in the pediatric population. Safety and efficacy have

not been established.

Geriatrics: Clinical trials of Rivatex® have included Alzheimer's disease

patients with a mean age of 73 years of age; information available on the

effects of Rivatex® is based upon this population. Elderly patients are

more likely to have age-related prostate problems, which may require

caution in patients receiving Rivatex®, especially if urinary tract

obstruction is present.

Surgical: Because Rivatex® is a cholinesterase inhibitor, it may be likely

to prolong or exaggerate succinylcholine-type muscle relaxation during

anesthesia.

Adverse Effects:

Because of its cholinomimetic action, Rivatex® may have vagotonic

effects on the heart, including bradycardia, and may increase the activity

of the gastrointestinal and urinary tracts.

Those indicating need for medical attention:

Incidence more frequent:

Gastrointestinal toxicity, specifically anorexia; dyspepsia; vomiting;

diarrhea, nausea .

Rates of gastrointestinal toxicity were higher in women than men.

Incidence less frequent:

Cardiovascular effects, specifically bradycardia; hypertension; syncope.

Incidence rare:

Asthenia; convulsions; mood or mental changes, specifically aggression

nervousness; tremors; urinary obstruction.

Those indicating need for medical attention only if they continue or are

bothersome:

Incidence more frequent:

Abdominal pain or cramping ; dizziness ; constipation ; flatulence;

headache; mental changes, specifically confusion, depression, fatigue ;

hallucinations.

Incidence less frequent:

Insomnia; malaise; rhinitis ; sweating increased.

Administration and Dosage:

Proper use of this medication:

Not taking more medication than the amount prescribed because of

increased risk of adverse effects.

Taking Rivatex® with food, Taking doses at regular intervals for

maximum efficacy.

Missed dose: Taking as soon as possible; not taking if almost time for

next scheduled dose; not doubling doses.

The first dosage increase should be made after a minimum of two weeks

of treatment .

The patient should be carefully observed for side effects following

initiation of therapy and following every dosage increase.

Dosing may be altered in patients who use nicotine due to increased

clearance of Rivatex® in smokers.

Usual Adult Dose:

Alzheimer's dementia Oral: initially 1.5 mg twice daily in the morning

and evening. After at least 2 weeks of treatment if the patient is tolerating

treatment well, the dose may be increased to 3 mg twice daily. Additional

increases to 4.5 mg twice daily and 6 mg twice daily should be attempted

after a minimum of 2 weeks at the previous dose.

Usual adult prescribing limits: 12 mg daily.

Usual Pediatric Dose: Safety and efficacy have not been established.

Usual Geriatric Dose: See usual adult dose.

Storage: Store below 30°C.

Auxiliary labeling: May cause dizziness, Take exactly as directed.

How supplied: Box of 4 blisters of 15 tablets.