amyl nitrite

Action and Spectrum

Actions and Spectrum 

The effects of amyl nitrite can be felt shortly after breathing the medication because of its quick-acting nature. amyl nitrite has short-term effects that typically last 2 to 5 minutes. 

amyl nitrite is primarily used to treat angina and other related heart disorders, according to its therapeutic spectrum. 

Drug Interaction

Adverse Reaction

Frequency defined  

Nausea  

Vomiting 

Orthostatic hypotension 

Dizziness 

Methemoglobulinemia  

Facial flushing 

Vasodilation 

Shock 

Rash 

Weakness 

Headache restlessness 

Hemolytic anemia 

Syncope 

Hypotension 

Tachycardia 

Black Box Warning

Black Box Warning 

According to the warning, amyl nitrite can have major negative effects, such as: 

An uncommon but deadly blood illness known as methemoglobinemia caused by amyl nitrite. This disorder develops when the blood has an excessive quantity of methemoglobin, which might lower the amount of oxygen that is available in the body’s tissues.  

A quick reduction in blood pressure brought on by amyl nitrite may result in fainting, woozy feeling or light headedness. 

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

• People with known hypersensitivity or allergy to the medication or any of its ingredients should not take amyl nitrite. 
• Methemoglobinemia, a disorder that limits the quantity of oxygen available to the body’s tissues, can be brought on by amyl nitrite. Therefore, it should not be used by anyone with severe anemia. 
• amyl nitrite can elevate intraocular pressure, which aggravates glaucoma signs and symptoms. As a result, it should not be used in people with this condition. 

Caution: 

• Sudden reduction in blood pressure brought on by amyl nitrite can be hazardous for people with cardiovascular disease.  
• The kidneys and liver both break down and eliminate amyl nitrite. As a result, care should be taken while giving this medication to people who have renal or hepatic impairment. 
• With continued usage, amyl nitrite can cause tolerance and dependence due to its great propensity for misuse. 

Pregnancy / Lactation

Pregnancy warnings:     

Pregnancy category: C 

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 

A vasodilator known as amyl nitrite works by calming the smooth muscles in the blood arteries. It is an alkyl nitrite prodrug, which means that once it enters the body, it quickly transforms into nitric oxide. 

Pharmacodynamics 

The pharmacodynamics of amyl nitrite are largely attributed to its ability to rapidly convert to nitric oxide in the body, which causes smooth muscle relaxation and vasodilation. 

Cyclic guanosine monophosphate (cGMP) is created when nitric oxide stimulates the enzyme guanylate cyclase. Blood flow increases and blood pressure decreases as a result of cGMP relaxing the smooth muscles in the blood vessels. 

Pharmacokinetics 

Absorption   

A glass ampule containing the liquid medication, which is smashed to release the vapours for inhalation, is generally used to give amyl nitrite by way of inhalation. Through the lungs, the medication is quickly absorbed into the bloodstream. 

Distribution 

amyl nitrite is absorbed into the body and then transported throughout it, including the brain, where it has its psychedelic effects. Due to its high lipophilicity, the medication can easily pass the blood–brain barrier. 

Metabolism 

amyl nitrite is quickly broken down in the liver into a variety of metabolites, such as nitrite, nitrate, and isobutyrate, through oxidation and conjugation. Nitric oxide can be produced in the body by further metabolizing the principal metabolite, nitrite. 

Elimination and excretion 

The urine is the main excretion method for amyl nitrite and its metabolites. The medication has a short elimination half-life, between 1 and 4 minutes. 

Adminstartion

Administration:  

Through inhalation amyl nitrite is used with a glass ampule that contains liquid medication.  

In order to release the vapors for inhalation, the ampule is crushed. The medication is breathed in through the nose or mouth and enters the bloodstream through the lungs. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: amyl nitrite 

Why do we use amyl nitrite? 

amyl nitrite is mostly used to treat angina (chest pain) caused by a heart condition.  

When breathed in, it widens the coronary arteries, boosting heart blood flow and reduces the heart muscle strain.