AcoEaze

(Acotiamide)

Tablet 100 mg

COMPOSITION

THERAPEUTIC INDICATIONS
Postprandial fullness, upper abdominal fullness, and early satiety in functional dyspepsia
DOSAGE AND METHOD OF ADMINISTRATION
The usual adult dosage is 100 mg of acotiamide hydrochloride hydrate orally administered three times a day before meals.
CONTRAINDICATIONS
Patients with a history of hypersensitivity to the ingredients of this drug
SPECIAL WARNINGS AND PRECAUTIONS FOR USE
Precautions Related to Dosage and Administration
Discontinuation of administration of this drug should be considered if symptoms do not improve after one month of
administration of this drug.
If symptoms persist, the possibility of organic disease should be considered, and in addition to upper gastrointestinal
endoscopy, other examinations should be considered if necessary.
Important Precautions
This drug is an acetylcholinesterase inhibitor and enhances the action of acetylcholine.
If the symptoms continue to improve, consider discontinuing the administration of this drug, and be careful not to administer
it carelessly for a long period of time.
Children
No clinical trials have been conducted in children, etc.
Elderly
If any abnormalities are observed, appropriate measures such as suspension of administration should be taken. In general,
physiological functions (renal function, liver function, etc.) are decreased.

DRUG INTERACTIONS
Precautions for co-administration (Pay attention to co-administration)

Clinical
Drug name, etc. Mechanism/risk factors
symptoms/measures
Drugs with
anticholinergic effects The action of this drug Since this drug has an
o atropine sulfate may be weakened. acetylcholinesterase inhibitory effect,
hydrate concomitant use with anticholinergics
o Butylscopolamine suppresses the action of this drug.
bromide, etc.
 choline enhancers and
cholinesterase inhibitors o The effects of this drug Along with this drug, it has a
Acetylcholine and concomitant drugs receptor-stimulating or stimulating
chloride etc. may be enhanced. effect.
o Neostigmine bromide,etc.

FERTILITY, PREGNANCY, AND LACTATION

Pregnant women
Pregnant women or women who may become pregnant should only be administered if the therapeutic benefits are judged
to outweigh the risks.

Lactating women
Consider the therapeutic benefit and the benefit of breastfeeding and consider continuing or discontinuing breastfeeding. It
has been reported that it is excreted in the milk of rats
EFFECTS ON THE ABILITY TO DRIVE AND USE MACHINES
ADVERSE DRUG REACTIONS
The following adverse reactions may occur. Patients should be carefully monitored, and if any abnormalities are observed,
appropriate measures such as discontinuing administration should be taken.

less than 0.5%

1 or more 0.5 to less than 1%
rash, urticaria
hypersensitivity
Increased white blood cell count
blood
stomach ache
Digestive organ diarrhea, constipation nausea, vomiting
ALT increase, AST Blood bilirubin increased, blood
liver
increase, γ-GTP increase ALP increased
Increased blood prolactin,
metabolism/endocrine
increased blood triglycerides

Reporting of suspected adverse reactions

Reporting suspected adverse reactions after authorization of the medicinal product is important. It allows continued
monitoring of the benefit/risk balance of the medicinal product. Healthcare professionals are asked to report any suspected
adverse reactions at pv@[Link]
OVERDOSE
PHARMACOLOGICAL PROPERTIES
Pharmacodynamics properties
Mechanism of Action
It showed acetylcholinesterase inhibitory action.
Gastrointestinal hypermotility
It was shown to enhance postprandial gastric antrum motility in dogs and rats. In addition, it was shown to improve
clonidine-induced gastric antral hypomotility in dogs and rats.
Improvement of delayed gastric emptying
It was shown to improve clonidine-induced delayed gastric emptying in rats

Pharmacokinetic properties
Blood concentration
Single dose
When 1 tablet of this drug (100 mg of acotiamide hydrochloride hydrate) was administered orally in a single dose to healthy
adult males under fasted conditions, the changes in plasma concentration of unchanged drug and pharmacokinetic
parameters were as follows

Single-dose pharmacokinetic parameters

Dosage T max C max AUC inf T1 /2

(mg) (hr) (ng/mL) (ng・hr/mL) (hr)
100 2.42±0.97 30.82±13.33 171.3±59.43 13.31±6.91
Mean ± standard deviation, n = 6
AUC inf : AUC calculated by extrapolating from the last measurement point to infinity

Repeated doses
Administer 1 tablet (100 mg of acotiamide hydrochloride hydrate) to healthy adult men three times a day for 9 days (single
dose on day 1, before each meal on days 3 to 8, single dose on day 9 ), and when repeatedly administered orally before
meals, the plasma concentration reached a steady state after the third administration on day 3. In addition, the
pharmacokinetics of repeated administration hardly changed.
Absorption
Dietary Effects
When one tablet of this drug (100 mg of acotiamide hydrochloride hydrate) was orally administered to healthy adult males
under fasting conditions, before meals, or after meals, Cmax was the highest when administered before meals and increased
by 62.7% compared to when administered under fasted conditions. In addition, the C max of postprandial administration
was 59.6% of that of preprandial administration. AUC last was the lowest with postprandial administration, and decreased
to 76.8% and 80.0%, respectively, in fasting and preprandial administration.
Distribution
Plasma protein binding rate
The plasma protein binding rate obtained by the in vitro equilibrium dialysis method was 84.21% to 85.95% for human
plasma and 82.64% to 85.10% for human serum albumin. thought to be albumin
Metabolism
Metabolism
When [ 14 C] acotiamide solution (600 mg/103 μCi) was orally administered to 6 healthy adult male subjects under fasting
conditions, unchanged drug accounted for 60.0% of the plasma radioactivity. In addition, de-isopropyl glucuronide,
unchanged glucuronide, and de-isopropyl glucuronide conjugate were found in plasma (non-Japanese data).
Metabolic Enzymes
In vitro metabolism studies using human CYP-expressing microsomes indicate that this drug is metabolized to deisopropyl
by CYP2C8, CYP1A1, or CYP3A4. In addition, an in vitro metabolism test using human UGT-expressing
microsomes suggests that this drug is metabolized to the unchanged glucuronide conjugate by UGT1A8 or UGT1A9.
Excretion
Acotiamide solution (600 mg/103 μCi) was orally administered to 6 healthy adult male subjects under fasted conditions.
5.3% were excreted (foreign data).
PRECLINICAL SAFETY DATA
Information Based on Nonclinical Studies
In a 24-month carcinogenicity study in rats, endometrial adenocarcinoma was observed in 5/50, 8/50, and 5 of the 200
mg/kg/day, 600 mg/kg/day, and 2,000 mg/kg/day groups, respectively. /50 cases, and significantly increased in the 600
mg/kg/day group (approximately 100 times the clinical dose in terms of dosage). On the other hand, no genotoxicity or
estrogenic effects were observed with this drug. In addition, up to 2,000 mg/kg/day (approximately 330 times the clinical
dose) in a 24-month carcinogenicity study in mice, and up to 2,000 mg/kg in a two-stage uterine carcinogenesis study using
genetically modified animals.
PRESENTATION
ACOEAZE 100mg Tablets are available in Alu-Alu blister in a pack size of 20’s (2x10’s) tablets.

STORAGE
Do not store and transport above 30°C.
INSTRUCTIONS
To be sold on the prescription of a registered medical practitioner only.
Protect from sunlight, moisture and heat.
Keep all medicines out of sight & reach of children.
Product contains Lactose.

REGISTRATION NUMBER
ACOEAZE 100mg Tablets : 123123
MANUFACTURING LICENSE NUMBER : 000016

March 2023
SPL/SPC-Aco.T/322-000(001)