guanoxan

Action and Spectrum

Actions and Spectrum: 

Action:  

guanoxan works by inhibiting the release of norepinephrine from nerve terminals, leading to decreased sympathetic activity. This ultimately results in relaxation of blood vessels and a reduction in heart rate, leading to lower blood pressure. 

Spectrum: guanoxan was primarily used for the treatment of hypertension (high blood pressure). By reducing sympathetic activity and relaxing blood vessels, it aimed to lower blood pressure and reduce the workload on the heart.  

Drug Interaction

Adverse Reaction

Frequency not defined  

Liver toxicity 

Black Box Warning

Black Box Warning:  

None

Contraindication / Caution

Contraindication/Caution:  

Hypersensitivity: Individuals with a known hypersensitivity or allergic reaction to guanoxan or its components should not use this medication. 

Bradycardia: guanoxan can lower heart rate so that it might be contraindicated in individuals with bradycardia (a slow heart rate). 

Heart Block: guanoxan may affect the heart’s electrical conduction and could be contraindicated in people with heart block or other significant heart rhythm abnormalities. 

Cerebrovascular Disease: Individuals with a history of cerebrovascular disease (such as stroke) might have an increased risk of adverse effects with guanoxan. 

Depression and Mental Health Conditions: guanoxan may exacerbate depression or other mental health conditions, so caution is advised in individuals with these conditions. 

Impaired Liver or Kidney Function: Individuals with impaired liver or kidney function may not be able to effectively metabolize or eliminate guanoxan, potentially leading to increased risks of adverse effects. 

Pregnancy and Breastfeeding: The safety of guanoxan during pregnancy and breastfeeding is not well established. It is generally recommended to avoid using this medication in pregnant or breastfeeding individuals unless the potential benefits outweigh the risks. 

Pregnancy / Lactation

Pregnancy warnings:     

Pregnancy category: N/A 

Lactation: Excreted 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 a lack of studies on pregnant women and no evidence of risk to the fetus 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 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:  

guanoxan belongs to the class of drugs known as sympatholytics or adrenergic neuron blockers. 

Pharmacodynamics:  

guanoxan’s action inhibits the release of norepinephrine from sympathetic nerve endings. It does this by interfering with norepinephrine storage in vesicles within nerve terminals. By reducing the release of norepinephrine, guanoxan decreases sympathetic nervous system activity, decreasing heart rate, blood pressure, and overall sympathetic tone.  

Pharmacokinetics: 

Absorption 

guanoxan is administered orally, and its absorption from the gastrointestinal tract is relatively slow and incomplete. It experiences substantial initial liver metabolism, potentially constraining its bioavailability. 

Distribution 

guanoxan is distributed throughout the body. It is known to have a relatively large distribution volume, suggesting that it can penetrate various tissues. However, specific distribution characteristics are not widely documented. 

Metabolism 

guanoxan undergoes extensive metabolism in the liver. The liver enzymes primarily metabolize it through a process known as hydroxylation. The exact metabolic pathways and metabolites produced may vary.  

Excretion and Elimination 

The metabolites of guanoxan, along with a portion of the unchanged drug, are excreted primarily through the urine. The elimination half-life of guanoxan and its metabolites is relatively long, which may contribute to the drug’s duration of action and dosing frequency. 

Adminstartion

Administration:  

The administration is by oral route. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: guanoxan 

Why do we use guanoxan?  

Hypertension: guanoxan was historically used to treat high blood pressure. By promoting vasodilation and reducing the amount of norepinephrine available to stimulate blood vessels, it helps to lower blood pressure.