Under inappropriate conditions, the consumption of opioids and cocaine can be highly dangerous. Crucial are the ways of consumption. Under adequate medical supervision, opioids can be taken for decades without lasting damages to the human body. The harms of cocaine use could be crucially minimized. Inhalable preparations of opioids or cocaine delivered via programmable sprays could offer drug users an attractive and safe means of avoiding lethal risks. Adequate medical control of the consumption of the most dangerous addictive substances can relieve our societies of an enormous burden.
The individual, societal, and economic consequences of the currently dysfunctional drug markets are inacceptable. All measures and treatments against opioid and cocaine addiction have little or no measurable impact on global figures and societal costs. Still it is possible to reduce harm. Public disorder, medical, juridical and police costs, deaths by infections and overdoses, can be minimized. We need to understand in detail the health risks that can arise from the use of opioids and cocaine. Addiction is a major existential threat from both.
Permanent abstinence from opioids is rarely possible. More than 90 percent of addicts remain dependent and sooner or later relapse after withdrawal.[1] Every relapse carries the risk of an opioid overdose, one of the leading causes of death. Regular daily use protects against overdose and cravings. Therefore, an opioid agonist treatment (OAT) is the method of choice.
Only in a small minority does cocaine addiction lead to sustained, daily use. Most cocaine users adequately control their consumption most of the time. Short or long breaks in use are common and never lead to unbearable withdrawal symptoms. Even a relapse does not pose an immediate threat to health and life due to overdose. Inappropriate dosing may cause psychosis and promote violent behaviour; some consumption patterns trigger exhaustion and depression.
Injection drug use is attractive for addicts because it delivers the maximum dose to the brain without any loss of substance. Every injection damages the tissues of the skin. Blood leaking from penetrated vessels, paravenous injections, and microscopic particles of cutting agents in illegal drugs cause purulent foci that can develop into abscesses and lead to chronic bacterial infections, endocarditis, and septic death. Viral hepatitis and HIV can be transmitted through shared needles and syringes. Heroin addicts usually inject themselves three times a day, while cocaine addicts often inject dozens or more times a day. Chronic bacterial infections are inevitable after months or years.
Half of opioid users are satisfied with oral methadone or morphine slow-release preparations. Oral intake of opioids or cocaine is insufficiently attractive for many addicts. Chewing leaves of Cocoa or drinking its tea does not provide a sufficient effect for most users. The risks are low in the short or medium term. The long-term health effects of swallowed cocaine have not been sufficiently studied. The vascular diseases observed with other stimulants are a concern. Chronic vasoconstriction can lead to high blood pressure, Raynaud’s syndrome, heart, kidney and brain damage, especially in older consumers.
Taking opioids or cocaine nasally or by inhalation is attractive because they are fast-acting forms of consumption. Within a few seconds, a large part of the substance reaches the central nervous system. Local effects of cocaine are anesthesia and vasoconstriction, followed by rebound hyperemia. Sniffing cocaine affects the mucous tissues of the nasopharynx, i.e. the nasal septum, the paranasal sinuses and the palatal roof of the mouth. Hyperemia causes a chronic runny nose, postnasal drip and, supported by the anesthetic effect, spluttering, coughing and inflammation of the lower respiratory tract. Bronchitis and pneumonia are very common. Inhaling hot gases by smoking or ‘chasing the dragon’ primarily affects the lower airways. All of the local effects of these addictive habits are medically unacceptable. The associated risks are too high. Methods and conditions of consumption are the main causes of harm associated with drug use.
Only as a substance in itself do opioids have no dangerous local effects. But the substance cocaine itself carries also considerable systemic risks. Vasoconstriction by cocaine promotes cerebrovascular and cardiovascular diseases or attacks. This and cocaine associated violence became common reasons for emergency room admissions and death. Epileptic seizures can be triggered by cocaine and by opioids. Unlike cocaine, opioids as substances nearly never cause long-term damage to the body. Physical harm caused by opioids is largely preventable and, in the case of cocaine, largely minimizable. It is a question of appropriate dosing, monitoring and control.[2]
Psychoactive drugs like opioids and cocaine are highly lipophilic. Liposomes are small spheres with a diameter of 3 to 5 µm, made of a lipid membrane. They can be loaded with cocaine or opioids. A watery emulsion of liposomal cocaine, heroin, fentanyl or nicaten can be sprayed and inhaled through the mouth. Without adverse effects on the airways, the full dose reaches the alveoli, where it is quantitatively reabsorbed by the bloodstream.
Inhaled doses reach the brain within a few seconds. The onset of effect is very steep, like a flash, a feeling sought and desired by most users. A spray should deliver doses of 30 or 60 mg per inhaled stroke. If technically feasible, higher doses per inhaler stroke should be considered. Inhalables of cocaine and opioids are attractive to dependent users and in principle medically controllable. [3]
An opioid-tolerant user should be enabled to inhale 180 mg of heroin or the equivalent dose of fentanyl or nicaten within one minute. If full tolerance is established, an additional dose of 180 mg is safe after a minimum intervall of 30 minutes. Most users stabilize their daily heroin dose at about 600 mg; daily doses above 1 g are uncommon. 600 mg heroin per day is effect-equivalent to 100 mg methadone. If opioid-tolerance is doubtful in an addict, the first inhaled doses should be medically supervised and not exceed 30 mg. My recommendations are based on clinical experience in the Swiss federal ProVe trial.[4] They need to be empirically reevaluated. For fentanyl and nicaten, clinically reliable data on equivalent doses are lacking.
The scientific evidence base for a medically safe cocaine-dosing is sparse. [5] Most of the inhaled cocaine passes from the lungs directly to the brain and is absorbed there by the lipophilic nerve tissue.[6] However, effects on the rest of the body are inevitable. Cocaine should not be used by people with cardio-, cerebro- or other vascular risks. Medical controll of cocaine use should strictly focus on harm reduction. All consuption patterns with acceptable risks should be enabled. Daily inhaling use and consumption on every weekend should be avoided. More than rising doses, users tend to rise the frequency of their cocaine consumption. This tachyphylaxis can lead to exhaustion, depression and paranoia. Most cocaine users consume in binges. After inhaling 60 mg of cocaine, a second and third inhalation of 60 mg each might be possible. Is it subsequently necessary to prevent further use of the cocaine spray for the next 30 minutes or even three hours? How many days a week should we allow cocaine use? Optimizing dosing regimens could be a complex task.
By today’s standards, the knowledge available 30 years ago was insufficient for a large-scale trial with inhalables, as conducted on behalf of the Federal Office of Public Health. Due to a lack of safe galenics, the ProVe trials with inhaled cocaine and heroin had to be aborted. Marco Peng[7] and me proposed a spray for cold inhalation of liposome-coated opioids, cocaine, and other stimulants. But in light of the sheer success of Swiss drug policy in the nineties, the development of safe inhalation galenics and dosing schemes for the most dangerous drugs was no longer pursued. As growing drug problems all over the world and even in Switzerland demonstrate, we do wrong.
Safe, medically controllable devices for cold inhalation of liposome-coated opioids, cocaine, and other stimulants are feasible from commercially available components used in sprays and cell-phones: Fingerprint recognition of the user, programmable electronic steering unit, liquid container for liposome-coated drug, inhalation spray built in a robust shell. We may call it cocisafe, opisafe or drugsafe.
→ for a German article on the same topic
[1] Nordt C, Stohler R: Incidence of heroin use in Zurich. Lancet 2006; 367: 1830-34
[2] Seidenberg A, Honegger U, Methadon, Heroin und andere Opioide, Verlag Hans Huber, Bern, 1998. Lehrbuch und medizinische Handlungsanleitungen.
[3] Rihs-Middel M, Lotti H, Seidenberg A: Aerztliche Verschreibung von Betäubungsmitteln: Praktische Umsetzung und wichtigste Ergebnisse, Bundesamt für Gesundheit, Verlag Hans Huber Bern, 2002, ISBN 3-456-82910-8
[4] Ibid.
[5] Gianni Zarotti in Rihs-Middel M, Lotti H, Seidenberg A
[6] Siegel R.K. 1982: Cocaine Smoking, Journal of Psychoactive Drugs, Haight Ashbury Free Medical Clinic, San Francisco 1982:14(4):271-359: Monographie über das Rauchen von Kokain.
[7] Marco Peng 1957-2008, Psychologe und Software-Ingenieur der ProVe-Versuche