DEL - General Information
A dopamine D2 antagonist that is used as an antiemetic. [PubChem]
Pharmacology of DEL
DEL, although chemically related to procainamide, does not possess local anesthetic or antiarrhythmic properties. DEL is used to enhance GI motility, to treat diabetic gastroparesis, as an antinauseant, and to facilitate intubation of the small bowel during radiologic examination. DEL 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.
DEL for patients
Metoclopramide may impair the mental and/or physical abilities required for the performance of hazardous tasks such as operating machinery or driving a motor vehicle.The ambulatory patient should be cautioned accordingly.
The effects of metoclopramide on gastrointestinal motility are antagonized by anticholinergic drugs and narcotic analgesics. Additive sedative effects can occur when metoclopramide is given with alcohol, sedatives, hypnotics, narcotics, or tranquilizers.
The finding that metoclopramide releases catecholamines in patients with essential hypertension suggests that it should be used cautiously, if at all, in patients receiving monoamine oxi-dase inhibitors.
Absorption of drugs from the stomach may be diminished (e.g., digoxin) by metoclopramide, whereas the rate and/or extent of absorption of drugs from the small bowel may be increased (e.g., acetaminophen, tetracycline, levodopa, ethanol, cyclosporine).
Gastroparesis (gastric stasis) may be responsible for poor diabetic control in some patients. Exogenously administered insulin may begin to act before food has left the stomach and lead to hypoglycemia. Because the action of metoclopramide will influence the delivery of food to the intestines and thus the rate of absorption, insulin dosage or timing of dosage may require adjustment.
Metoclopramide should not be used whenever stimulation of gastrointestinal motility might be dangerous, e.g., in the presence of gastrointestinal hemorrhage, mechanical obstruction, or perforation.
Metoclopramide is contraindicated in patients with pheochro-mocytoma because the drug may cause a hypertensive crisis, probably due to release of catecholamines from the tumor. Such hypertensive crises may be controlled by phen-tolamine.
Metoclopramide is contraindicated in patients with known sensitivity or intolerance to the drug.
Metoclopramide should not be used in epileptics or patients receiving other drugs which are likely to cause extrapyramidal reactions, since the frequency and severity of seizures or extrapyramidal reactions may be increased.
Additional information about DEL
DEL Indication: For the treatment of gastroesophageal reflux disease (GERD)
Mechanism Of Action: DEL 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. DEL 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. DEL'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.
Drug Interactions: Atovaquone The agent decreases the effect of atovaquone
Cyclosporine DEL increases serum levels of cyclosporine
Levodopa Levodopa decreases the effect of metoclopramide
Succinylcholine The agent increases the effect of succinylcholine
Venlafaxine Possible serotoninergic syndrome with this combination
Food Interactions: Not Available
Generic Name: Metoclopramide
Synonyms: Metaclopramide; Metaclopromide; Methochlopramide; Methoclopramide; Metochlopramide; Metoclopramida [Inn-Spanish]; Metoclopramide Hcl; Metoclopramide Hydrochloride; Metoclopramidum [Inn-Latin]
Drug Category: Antiemetics; Prokinetic Agents; Dopamine Antagonists
Drug Type: Small Molecule; Approved; Investigational
Absorption: Rapidly and well absorbed (oral bioavailability 80±15.5%).
Toxicity (Overdose): Oral, mouse LD50: 280 mg/kg. Signs of overdose include drowsiness, disorientation, and extrapyramidal reactions.
Protein Binding: 30%
Half Life: 5-6 hr
Dosage Forms of DEL: Liquid Oral
Chemical IUPAC Name: 4-amino-5-chloro-N-(2-diethylaminoethyl)-2-methoxybenzamide
Chemical Formula: C14H22ClN3O2
Metoclopramide on Wikipedia: https://en.wikipedia.org/wiki/Metoclopramide
Organisms Affected: Humans and other mammals