mazindol

Action and Spectrum

Actions and Spectrum 

Actions: 

mazindol primarily affects certain neurotransmitters in the brain, particularly dopamine, norepinephrine, and serotonin. It acts as a norepinephrine-dopamine-releasing agent (NDRA), inhibiting these neurotransmitters’ reuptake. By enhancing the release and reducing the reuptake of these neurotransmitters, mazindol increases their availability in the brain, leading to increased feelings of alertness, decreased appetite, and potentially enhanced metabolism. 

Spectrum: 

The use of mazindol is usually considered in cases where the benefits of weight loss outweigh the potential risks and side effects. Its effects tend to diminish over time, making it more suitable for short-term use rather than as a long-term solution. 

Drug Interaction

Adverse Reaction

Frequency not defined 

Skin reaction 

Precordial pain 

Headache 

Paraesthesia 

Convulsion 

Anxiety 

Vertigo 

Psychosis 

Depression  

Tremor 

Menstrual disorder 

Sexual dysfunction 

Diarrhea 

Hallucination 

Black Box Warning

Black Box Warning: 

None 

Contraindication / Caution

Contraindication/Caution: 

Contraindications: 

• Hypersensitivity 
• Advanced arteriosclerosis 
• Cardiovascular disease 
• Hyperthyroidism 
• Glaucoma 

Cautions: 

• Renal impairment 
• Liver impairment 
• History of drug abuse 
• Pregnancy 
• Breastfeeding 

Pregnancy / Lactation

Pregnancy consideration:  

Utilize mazindol with caution during pregnancy. 

Breastfeeding warnings:  

It is not known whether the drug is excreted in the breast milk.  

Pregnancy category: 

Category A: Well-controlled and satisfactory studies show no risk to the fetus in the initial or later trimester. 

<b>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:  

The increased release and extended presence of norepinephrine and dopamine contribute to appetite suppression. These neurotransmitters act on various brain areas involved in appetite regulation, including the hypothalamus. 

mazindol’s effects on norepinephrine and dopamine also increase central nervous system stimulation. This results in increased wakefulness, alertness, and energy levels. 

Pharmacodynamics: 

mazindol acts as a norepinephrine-releasing agent (NRA). This means it increases the release of norepinephrine (noradrenaline) from nerve endings. By enhancing norepinephrine release, mazindol can increase alertness, energy levels, and metabolism. 

mazindol also acts as a dopamine-releasing agent (DRA), increasing dopamine release from nerve terminals. The increased dopamine release can improve mood and a sense of well-being. 

Pharmacokinetics: 

Absorption 

mazindol is well absorbed from the gastrointestinal tract after oral ingestion. The time it takes for mazindol to reach its peak concentration in the bloodstream (peak plasma concentration) can vary, but it’s generally within 2 to 4 hours after ingestion. 

Distribution 

mazindol is distributed throughout the body’s tissues, including the central nervous system, due to its lipophilic (fat-loving) nature. It can cross the blood-brain barrier and affect the central nervous system. 

Metabolism 

mazindol undergoes extensive metabolism in the liver. The primary metabolic pathways involve hydroxylation and conjugation. The significant metabolites of mazindol are inactive and are eliminated from the body through urine. 

Elimination and Excretion 

The elimination half-life of mazindol varies and can range from 10 to 16 hours. This longer half-life is a characteristic feature of mazindol and contributes to its sustained effects. 

Adminstartion

Administration: 

mazindol is usually taken orally as a tablet once daily, in the morning, to help prevent insomnia and other potential sleep disturbances. Taking it early in the day can also help to minimize its stimulant effects on sleep. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: mazindol 

Pronounced as: mah-zin-dole 

Why do we use mazindol? 

• Appetite Suppression: mazindol increases feelings of fullness, and reducing hunger helps individuals consume fewer calories, which is crucial for weight loss. 
• Enhanced Caloric Deficit: mazindol’s effects on metabolism and thermogenesis can increase caloric expenditure, supporting weight loss efforts.