Amyl nitrite, an organic nitrite, is a vasodilating agent.
Amyl nitrite shares the actions of the other nitrates and nitrites and has been used for acute relief of angina pectoris; however, the drug is seldom, if ever, used for angina pectoris because it is expensive, inconvenient, has a high incidence of adverse effects (e.g., headache, orthostatic symptoms, tachycardia), and has an unpleasant odor.
Amyl nitrite is used as an adjunct in the treatment of cyanide poisoning. Nitrite ions react with hemoglobin to form methemoglobin which unites with cyanide to form cyanmethemoglobin.
Diagnostic Aid for Heart Murmurs
Amyl nitrite also has been used to produce changes in the intensity of heart murmurs†. Murmurs resulting from stenosis of any of the 4 cardiac valves or from idiopathic hypertrophic subaortic stenosis will become louder after amyl nitrite adminis ration. Murmurs resulting from aortic or mitral regurgitation usually decrease in intensity.
Amyl nitrite and other volatile nitrites (“poppers”) have been used illicitly to enhance sexual pleasure. Some initial studies suggested that use of volatile nitrites, including amyl nitrite, may be one of numerous risk factors associated with the development of acquired immunodeficiency syndrome (AIDS) and Kaposi's sarcoma in male homosexuals;100, 101 however, more recent epidemiologic studies, while confirming the frequent use of volatile nitrites by homosexual men, have not found nitrite use to be a significant risk factor,102, 103, 104 and some data suggest that the initial attribution of risk may have been related to an association between nitrite use and certain behaviors and practices associated with enhanced transmission of the human innumodeficiency virus (HIV).104
Misuse and abuse of amyl nitrite and other inhaled volatile nitrites may be associated with potentially life-threatening hypotension and/or hemodynamic compromise when combined with selective phosphodiesterase (PDE) inhibitors, which are used to increase the duration and intensity of erection. (See Drug Interactions: Selective Phosphodiesterase Inhibitors, in the Nitrates and Nitrites General Statement 24:12.08.)
Amyl nitrite is administered by nasal inhalation. The patient should be sitting during and immediately after inhaling amyl nitrite. The ampul, wrapped in a woven absorbent covering, is crushed between the fingers and held to the nostrils for inhalation.
Dosage of amyl nitrite must be adjusted according to the patient's requirements and response.
For acute relief of angina pectoris, the usual dosage of amyl nitrite is 0.18-0.3 mL as required.
For the treatment of cyanide poisoning in adults and children, a 0.3-mL ampul of amyl nitrite is crushed every minute and the vapor is inhaled for 15-30 seconds until an IV sodium nitrite infusion is available. In adults, 300 mg (10 mL of a 3% solution) of sodium nitrite is infused IV at the rate of 2.5-5 mL/minute and immediately followed by 12.5 g (50 mL of a 25% solution) of sodium thiosulfate IV over a period of about 10 minutes. Dosage of sodium nitrite in children must be carefully adjusted to avoid the formation of excessive methemoglobin. In children, the dose of sodium nitrite is 180-240 mg/m2 (6-8 mL/m2 of a 3% solution) or 6 mg/kg (0.2 mL/kg of a 3% solution); dosage in children should not exceed 300 mg. IV sodium thiosulfate should be administered immediately after sodium nitrite; one clinician recommends that children receive 5 mL of a 25% sodium thiosulfate solution for every 1 mL of 3% sodium nitrite solution. If signs of cyanide poisoning reappear in adults and children, 50% of the initial doses of both sodium nitrite and sodium thiosulfate should be given.
Diagnostic Aid for Heart Murmurs
To produce changes in the intensity of heart murmurs†, amyl nitrite is inhaled until reflex tachycardia begins and then is discontinued immediately.
Following nasal inhalation of amyl nitrite, angina pectoris is relieved within 30 seconds and the duration of action is about 3-5 minutes. Following nasal inhalation in patients with or without coronary artery disease, substantial hemodynamic effects such as increased heart rate and decreased brachial artery and left ventricular end-diastolic pressures occur within 30 seconds and persist at least 5 minutes.
Amyl nitrite, an organic nitrite, occurs as a clear yellowish, volatile, flammable liquid having a peculiar, ethereal, fruity odor and pungent aromatic taste and is practically insoluble in water and miscible with alcohol.
Amyl nitrite vapor forms an explosive mixture in air or oxygen at room temperature and may explode if ignited. Amyl nitrite inhalant should be packaged in unit-dose containers, wrapped loosely in gauze or other suitable material, and stored at 2-15°C. A stabilizer, such as diphenylamine or epoxolol, is added to the commercially available products. The drug should be protected from light.
For further information on chemistry and stability, pharmacology, pharmacokinetics, uses, cautions, drug interactions, laboratory test interferences, and dosage and administration of amyl nitrite, see the Nitrates and Nitrites General Statement 24:12.08.
Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.
Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.
Routes | Dosage Forms | Strengths | Brand Names | Manufacturer |
|---|---|---|---|---|
Nasal | Inhalant | Amyl Nitrite Inhalant |
* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name
Only references cited for selected revisions after 1984 are available electronically.
100. Marmor M, Friedman-Kien AE, Laubenstein L et al. Risk factors for Kaposi's sarcoma in homosexual men. Lancet . 1982; 1:1083-7. [PubMed 6122889]
101. Goedert JJ, Neuland CY, `Wallen WC et al. Amyl nitrite may alter T lymphocytes in homosexual men. Lancet . 1982; 1:412-6. [PubMed 6121088]
102. Jaffe HW, Choi K, Thomas PA et al. National case-control study of Kaposi's sarcoma and Pneumocystis carinii pneumonia in homosexual men: part 1, epidemiologic results. Ann Intern Med . 1983; 99:145-51. [PubMed 6603806]
103. Marmor M, Friedman-Kien AE, Zolla-Pazner S et al. Kaposi's sarcoma in homosexual men: a seroepidemiologic case-control study. Ann Intern Med . 1984; 100:809-15. [PubMed 6326631]
104. Friedland GH, Harris C, Butkus-Small C et al. Intravenous drug abusers and the acquired immunodeficiency syndrome (AIDS): demographic, drug use, and needle-sharing patterns. Arch Intern Med . 1985; 145:1413-7. [PubMed 3875327]
105. Newell GR, Adams SC, Mansell PWA et al. Toxicity, immunosuppressive effects and carcinogenic potential of volatile nitrites: possible relationship to Kaposi's sarcoma. Pharmacotherapy . 1984; 4:284-91. [PubMed 6150466]
106. Newell GR, Mansell PWA, Spitz MR et al. Volatile nitrites: use and adverse effects related to the current epidemic of the acquired immune deficiency syndrome. Am J Med . 1985; 78:811-6. [PubMed 2859805]
107. Mayer KH. Inhalation-induced immunosuppression: sniffing out the volatile nitrite-AIDS connection. Pharmacotherapy . 1984; 4:235-6. [PubMed 6504707]