phendimetrazine

Action and Spectrum

Actions and Spectrum: 

phendimetrazine’s specific mode of action is unknown, however it is thought to increase the brain’s production of norepinephrine, dopamine, and serotonin. This causes the metabolism to rise and reduce hunger, which causes weight loss. 

The respiratory system, cardiovascular system, and central nervous system are all affected by the effects of phendimetrazine. Increased alertness, wakefulness, and decreased hunger are some of its effects on the central nervous system.

Moreover, it raises blood pressure, cardiac output, and heart rate, all of which might affect cardiovascular function. Lastly, it can encourage breathing, which might benefit people who have sleep apnoea because of obesity. 

Drug Interaction

Adverse Reaction

Frequency not defined  

Blurred vision 

Dizziness 

Changes in libido 

Tremor 

Urticaria 

Constipation 

Dysphoria 

Dysuria 

Primary pulmonary HTN 

Stomach pain 

Sweating 

Euphoria 

Abnormal heart valve findings 

Palpitation 

Tachycardia 

Agitation 

Increased BP 

Headache 

Diarrhea 

Dryness of the mouth 

Impotence 

Unpleasant taste 

Flushing 

Insomnia 

Nausea 

Black Box Warning

Black Box Warning 

phendimetrazine should only be taken briefly (a few weeks) in conjunction with a low-calorie diet and exercise regimen to manage obesity, according to the caution. Those who have a history of drug misuse should not take the medication, and they should be continuously watched for indications of abuse and dependency.

The medicine should not be taken in individuals with a history of cardiovascular disease, according to the warning, since it may raise the risk of unfavourable cardiovascular events. The substance has a significant potential for misuse, and continuous usage may result in dependency, according to the warning. Moreover, it warns that medication overuse may result in significant cardiovascular side effects like stroke, arrhythmias, and unexpected death. 

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

• Those with a known hypersensitivity to sympathomimetic amines should not use phendimetrazine. 
• Those with a history of cardiovascular illness, including hypertension, coronary artery disease, and arrhythmias, should not use phendimetrazine. 
• When a patient has hyperthyroidism, phendimetrazine is not recommended. 
• In individuals with uncontrolled glaucoma, phendimetrazine is contraindicated. 

Caution: 

• During nursing or while pregnant, phendimetrazine should only be used if the benefits outweigh the dangers. 
• phendimetrazine may make it difficult for diabetic people to regulate their blood sugar levels. 
• Those with renal impairment should take phendimetrazine cautiously since it can build up and have negative consequences. 
• Those who have a history of mental illnesses, such as depression and anxiety, should use phendimetrazine with care. 

Pregnancy / Lactation

Pregnancy warnings:     

Pregnancy category: X 

Lactation: Excretion into human milk is unknown 

Pregnancy Categories:         

Category A: Studies that were well-controlled and met expectations revealed no risk to the fetus in either the first or second trimester. 

Category B: There were lack of studies on pregnant women and no evidence of risk to the foetus in animal experiments.   

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 available 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: There is no data available for the drug under this category

Pharmacology

Pharmacology 

Norepinephrine, dopamine, and serotonin are the neurotransmitters in the brain that are stimulated by the sympathomimetic amine phendimetrazine. These neurotransmitters control how much energy is expended as well as hunger and mood. 

phendimetrazine has both direct and indirect sympathomimetic effects and shares structural similarities with amphetamine.  

Pharmacodynamics 

Norepinephrine is released from presynaptic nerve terminals and its reuptake is inhibited as a result, increasing the amount of norepinephrine in the synaptic cleft. 

phendimetrazine’s pharmacodynamics are mostly influenced by how it affects the central nervous system (CNS). A sympathomimetic amine called phendimetrazine works by causing the brain’s norepinephrine, dopamine, and serotonin levels to rise. These neurotransmitters control how much energy is expended as well as hunger and mood. 

Pharmacokinetics 

Absorption   

After oral treatment, phendimetrazine is quickly absorbed from the digestive system, reaching peak plasma concentrations in 3 hours. The medication is efficiently absorbed and unaffected by eating. 

Distribution 

The brain is one of the many locations where phendimetrazine is found in the body. The medication can exert its central effects on the CNS after crossing the blood-brain barrier. phendimetrazine’s distribution volume is not extensively characterized. 

Metabolism 

The primary metabolite of phendimetrazine is phenmetrazine, which is extensively processed by the CYP3A4 enzyme in the liver. N-desmethyl-phenmetrazine and phenmetrazine-N-oxide are further metabolites. The parent drug’s actions are mostly mimicked by the metabolites, which are pharmacologically active. The metabolites undergo further glucuronidation metabolization before being eliminated in the urine. 

Elimination and excretion 

phendimetrazine has a 3-to-4-hour elimination half-life. A little quantity of the drug’s unmodified form is also eliminated in the urine along with the majority of the drug’s metabolites. The medication is not well bound to plasma proteins and is not anticipated to be significantly cleared by the kidneys. 

Adminstartion

Administration:  

Immediate-release pills, capsules, or extended-release capsules are used to ingest phendimetrazine. Adults should take 35 mg once day, often in the morning, 30 to 60 minutes before to breakfast. The extended-release capsules are taken with or without meals once daily in the morning. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: phendimetrazine 

Why do we use phendimetrazine? 

As a short-term weight reduction assistance for individuals who are obese or overweight and have not been successful in losing weight by diet and exercise alone, phendimetrazine is a sympathomimetic amine. The medication is intended to be used in conjunction with a thorough weight loss regimen that includes dietary adjustments, physical activity, and behavioural therapy.