metoclopramide intranasal

Action and Spectrum

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. 

Drug Interaction

Adverse Reaction

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

Black Box Warning: 

Excessive use of metoclopramide can cause tardive dyskinesia. Avoid the treatment for more than 12 weeks. 

Contraindication / Caution

Contraindication/Caution: 

Contraindications 

• Hypersensitivity 
• Gastrointestinal obstructions 
• Pheochromocytoma 
• Epilepsy or history of seizures 

Cautions 

• Parkinson’s disease 
• Renal/hepatic impairment 
• Cardiovascular disease 
• Depression 
• Mental health disorders 

Pregnancy / Lactation

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

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

Adminstartion

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

Patient information leaflet 

Generic Name: metoclopramide intranasal 

Why do we use metoclopramide intranasal? 

metoclopramide intranasal is used to treat gastroparesis.