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Mechanism of Action
Metoclopramide¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Metoclopramide inhibits gastric smooth muscle relaxation produced by dopamine, therefore increasing cholinergic response of the gastrointestinal smooth muscle. It accelerates intestinal transit and gastric emptying by preventing relaxation of gastric body and increasing the phasic activity of antrum. Simultaneously, this action is accompanied by relaxation of the upper small intestine, resulting in an improved coordination between the body and antrum of the stomach and the upper small intestine. Metoclopramide also decreases reflux into the esophagus by increasing the resting pressure of the lower esophageal sphincter and improves acid clearance from the esophagus by increasing amplitude of esophageal peristaltic contractions. Metoclopramide's dopamine antagonist action raises the threshold of activity in the chemoreceptor trigger zone and decreases the input from afferent visceral nerves. Studies have also shown that high doses of metoclopramide can antagonize 5-hydroxytryptamine (5-HT) receptors in the peripheral nervous system in animals.
Pharmacology
Metoclopramide¿¡ ´ëÇÑ Pharmacology Á¤º¸ Metoclopramide, although chemically related to procainamide, does not possess local anesthetic or antiarrhythmic properties. Metoclopramide is used to enhance GI motility, to treat diabetic gastroparesis, as an antinauseant, and to facilitate intubation of the small bowel during radiologic examination. Metoclopramide may be used to treat chemotherapy-induced emesis and as a radiosensitizing agents in the treatment of non-small cell lung carcinoma and glioblastomas in the future.
Metabolism
Metoclopramide¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Cytochrome P450 2D6 (CYP2D6)
Protein Binding
Metoclopramide¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ 30%
Half-life
Metoclopramide¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 5-6 hr
Absorption
Metoclopramide¿¡ ´ëÇÑ Absorption Á¤º¸ Rapidly and well absorbed (oral bioavailability 80¡¾15.5%).
Pharmacokinetics
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Metoclopramide HClÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
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Toxicity
Metoclopramide¿¡ ´ëÇÑ Toxicity Á¤º¸ Oral, mouse LD50 : 280 mg/kg. Signs of overdose include drowsiness, disorientation, and extrapyramidal reactions.
Drug Interactions
Metoclopramide¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Atovaquone The agent decreases the effect of atovaquoneCyclosporine Metoclopramide increases serum levels of cyclosporineLevodopa Levodopa decreases the effect of metoclopramideSuccinylcholine The agent increases the effect of succinylcholineVenlafaxine Possible serotoninergic syndrome with this combination
CYP450 Drug Interaction
[CYP450 TableÁ÷Á¢Á¶È¸]
Food Interaction
Metoclopramide¿¡ ´ëÇÑ Food Interaction Á¤º¸ Food reduces availability, take 30 minutes before meals. Avoid alcohol.
Drug Target
[Drug Target]
Description
Metoclopramide¿¡ ´ëÇÑ Description Á¤º¸ A dopamine D2 antagonist that is used as an antiemetic. [PubChem]
Dosage Form
Metoclopramide¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Liquid IntramuscularLiquid IntravenousLiquid OralTablet Oral
Drug Category
Metoclopramide¿¡ ´ëÇÑ Drug_Category Á¤º¸ AntiemeticsDopamine AntagonistsProkinetic Agents
Smiles String Canonical
Metoclopramide¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CCN(CC)CCNC(=O)C1=CC(Cl)=C(N)C=C1OC
Smiles String Isomeric
Metoclopramide¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CCN(CC)CCNC(=O)C1=CC(Cl)=C(N)C=C1OC
InChI Identifier
Metoclopramide¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C14H22ClN3O2/c1-4-18(5-2)7-6-17-14(19)10-8-11(15)12(16)9-13(10)20-3/h8-9H,4-7,16H2,1-3H3,(H,17,19)/f/h17H
Chemical IUPAC Name
Metoclopramide¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ 4-amino-5-chloro-N-(2-diethylaminoethyl)-2-methoxybenzamide
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