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Brand Name :
Gimoti
Synonyms :
metoclopramide intranasal
Class :
Prokinetic agents
Dosage Forms & Strengths
Intranasal solution
15mg/actuation
9.8 ml of each bottle
Indicated for recurrent and acute diabetic gastroparesis
15 mg of 1 spray in a nostril 30 minutes before every meal and at bedtime 4 times daily for 2-8 weeks, based on symptomatic response
Usage is not recommended as there is a risk of extrapyramidal symptoms and tardive dyskinesia
Dosage Forms & Strengths
Intranasal solution
15mg/actuation
9.8 ml of each bottle
Indicated for recurrent and acute diabetic gastroparesis
Not indicated as an initial therapy
Use as an alternative to metoclopramide
15 mg of 1 spray in a nostril 30 minutes before every meal and at bedtime 4 times daily for 2-8 weeks, based on symptomatic response
The effect of either of the drugs is increased
the effects of either of the drug may be altered when administered concomitantly
Actions and Spectrum:
metoclopramide acts as a selective antagonist of dopamine D2 receptors, primarily in the central nervous system’s chemoreceptor trigger zone (CTZ). This antagonism reduces the inhibitory effects of dopamine, thereby increasing gut motility and reducing nausea and vomiting.
metoclopramide enhances gastrointestinal motility by increasing the release of acetylcholine in the myenteric plexus of the gut. This action promotes the forward movement of food and prevents reflux.
Frequency defined
>10%
Restlessness
Lassitude
Fatigue
Drowsiness
Frequency not defined
Dystonic reactions
Hallucinations
Amenorrhea
Hypertension
Hypotension
Fluid retention
Nausea
Hepatotoxicity
Urinary incontinence
Agranulocytosis
Leukopenia
Rash
Angioedema
Porphyria
Black Box Warning:
Excessive use of metoclopramide can cause tardive dyskinesia. Avoid the treatment for more than 12 weeks.
Contraindication/Caution:
Contraindications
Cautions
Pregnancy consideration:
Insufficient data are available for drugs regarding the risks associated with pregnant women
Breastfeeding warnings:
No data is available regarding the excretion of drugs in breast milk.
Pregnancy category:
Category A: well-controlled and satisfactory studies show no risk to the fetus in the first or later trimester.
Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women.
Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.
Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.
Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.
Category N: No data is available for the drug under this category.
Pharmacology:
metoclopramide acts as a dopamine D2 receptor antagonist in the central nervous system, particularly in the chemoreceptor trigger zone (CTZ). By blocking these receptors, it reduces the inhibitory effects of dopamine, leading to increased gut motility and decreased nausea and vomiting.
metoclopramide also has antagonist activity at specific serotonin receptors, specifically 5-HT3 receptors. By blocking these receptors, it further contributes to its antiemetic (anti-nausea and vomiting) effects.
Pharmacodynamics:
metoclopramide also exhibits antagonist activity at 5-HT3 receptors, which mediate nausea and vomiting. By blocking these receptors, it further contributes to the antiemetic effects of the drug.
metoclopramide increases the release of acetylcholine in the myenteric plexus of the gastrointestinal tract. This cholinergic stimulation enhances smooth muscle contraction, particularly in the upper gastrointestinal tract, leading to improved gastric emptying and accelerated transit of food.
Pharmacokinetics:
Absorption
The peak plasma concentration is 41 ng/mL
The peak plasma concentration is achieved in 1.25 hours
The area under the curve is 349 ng⋅hr/mL
Distribution
The protein-bound is 30%
The volume of distribution is 3.5 L/kg
Metabolism
CYP2D6 initially metabolizes the drug; then it forms monodeethylmetoclopramide
Elimination and Excretion
The half-life is 8.1 hours
The drug is excreted in urine
Administration:
metoclopramide can be administered through various routes, including oral, intravenous (IV), intramuscular (IM), and, occasionally, rectal. The appropriate route of administration depends on the specific indication and the severity of the condition.
Patient information leaflet
Generic Name: metoclopramide intranasal
Why do we use metoclopramide intranasal?
metoclopramide intranasal is used to treat gastroparesis.