Acotiamide

BRAND NAMES

• Gasmotin 

• Acofide

MECHANISM OF ACTION

Acotiamide enhances gastric motility by inhibiting acetylcholinesterase, increasing acetylcholine levels, and stimulating muscarinic receptors, which improves gastric emptying and relieves symptoms of functional dyspepsia.

PHARMACOKINETICS

Absorption

Acotiamide is well absorbed after oral administration, reaching peak plasma concentrations within about 1–2 hours. Its absorption is slightly affected by food, but it remains sufficiently bioavailable to exert its therapeutic effect.

Distribution

Acotiamide has a relatively small apparent volume of distribution (Vd), generally reported as approximately approximately 10–20 L in adults.

Metabolism

Acotiamide is primarily metabolized in the liver through enzymatic pathways, including flavin-containing monooxygenases (FMO), forming inactive metabolites that contribute minimally to its pharmacological activity.

Elimination

Acotiamide is eliminated mainly through renal excretion, with its metabolites being excreted in the urine. A smaller proportion is eliminated via feces.

PHARMACODYNAMICS

Acotiamide is a prokinetic agent that enhances gastrointestinal motility by increasing cholinergic neurotransmission in the stomach. It inhibits acetylcholinesterase, leading to elevated acetylcholine levels, and may block presynaptic muscarinic receptors to further promote its release. This results in improved gastric emptying and accommodation, thereby relieving symptoms such as postprandial fullness, early satiety, and upper abdominal discomfort in functional dyspepsia.

ADMINISTRATION

Acotiamide is administered orally, typically in tablet form, and is usually taken three times daily before meals. It is recommended to take the medication with water, and the dosage may be adjusted based on the patient’s condition and response to treatment.

DOSAGE AND STRENGTH

Acotiamide is commonly available in a strength of 100 mg tablets. The usual recommended dosage is 100 mg taken orally three times daily before meals, although the dose may be adjusted based on clinical response and physician guidance.

DRUG INTERACTIONS

Acotiamide has a low potential for drug interactions but caution is advised when it is used with certain agents. Concomitant use with other cholinergic drugs may enhance gastrointestinal motility and increase side effects such as diarrhea, while anticholinergic medications can reduce its effectiveness. Since acotiamide is primarily metabolized in the liver via flavin-containing monooxygenases, drugs that strongly inhibit or induce these enzymes could alter its plasma levels, although clinically significant interactions are rare. Overall, acotiamide is generally well tolerated and interacts minimally with other medications, but monitoring is recommended when combined with drugs affecting gastrointestinal function or liver metabolism.

FOOD INTERACTIONS

Acotiamide should be taken before meals, as food can slightly delay its absorption but does not significantly reduce its overall bioavailability. Taking it on an empty stomach or just before eating helps optimize its prokinetic effect and symptom relief in functional dyspepsia.

CONTRAINDICATIONS

Acotiamide is contraindicated in patients with known hypersensitivity to the drug or any of its components. It should also be avoided in individuals with severe liver or kidney impairment, as these conditions can significantly affect its metabolism and elimination. Additionally, its use during pregnancy and lactation is generally not recommended unless clearly necessary, due to limited safety data. Care should be taken in patients with other serious gastrointestinal disorders, as increased motility may exacerbate certain conditions.

SIDE EFFECTS

• Mild headache

• Diarrhea

• Abdominal discomfort. 

• Nausea

• Dizziness

• Palpitations.

TOXICITY

Acotiamide is generally safe, with mild side effects like headache, dizziness, or mild gastrointestinal issues. Serious toxicity is rare, and it does not significantly affect the heart or organs, making it well tolerated at therapeutic doses.