Naloxone

Naloxone is a medicinal substance that belongs to the group of opioid agonists, i.e. does not have any opium-like effects itself. Naloxone is used as an antidote to counteract the effects of opioids. Administration is intramuscular, subcutaneous, or intravenous.

What is naloxone?

The substance naloxone is one of the opioid antagonists. Together with the closely related active ingredient naltrexone, naloxone forms the subgroup of competitive antagonists. These act on all opioid receptors without themselves developing the (slightly sedating) effect typical of opioids. This makes it possible for naloxone to reverse the effects of opiates. The drug is therefore also known as an antidote and is mainly used in the case of overdoses of opioids.

An antidote is a substance that inactivates a poison and thus reduces or eliminates its effect ("antidote"). In pharmacology and chemistry, naloxone is described by the chemical molecular formula C 19 - H 21 - N - O 4. The moral mass of the whitish solid is 327.37 g / mol.

In human medicine, naloxone is usually administered intravenously. In exceptional cases, however, administration by subcutaneous or intramuscular routes is also possible. Subcutaneous administration is when the active ingredient is injected under the skin. An intramuscular injection is used when the active ingredient is injected directly into a skeletal muscle. When given intravenously, nalaxone is delivered directly into a vein through a syringe.

Pharmacological effect

Naloxone binds to the same receptors to which opiods also bind (opioid receptors), but does not develop any opium effects there. For this reason, opioids (e.g. opium, heroin or methadone) are prevented from docking with the receptors. These substances now show no effect.

However, naloxone only works competitively. It follows that there must always be a sufficiently large amount of the active ingredient in the blood to keep the opioids away from the receptors permanently. A particularly high dose of naloxone is therefore administered, particularly in situations in which an overdose of opioids is to be treated.

In contrast to the opioids, however, naloxone does not cause any addictions or other abnormalities. This applies both physically and mentally. It is therefore also added to some opioid pain relievers to prevent abuse or to make it unattractive.

Because naloxone is usually administered intravenously, an effect is achieved within seconds. The substance is quickly distributed through the bloodstream and penetrates the brain after only a short time.

The duration of action of naloxone is between one and four hours. It is therefore comparatively short, which can make multiple treatments necessary. The maximum daily dose is 24 mg. The short duration of action of naloxone is due to the fact that it is broken down by the liver and proceeds quickly. Half of the active ingredient is used in just two hours. The substance is excreted in the urine.

Medical application & use

Naloxone is used as an antidote to treat opioid overdoses of all kinds. It does not matter which preparation caused the overdose. Heroin addicts who have overdosed themselves are also treated with naloxone in order to reverse the sedative effect of the drug and thus to keep the patient alive.

Naloxone is also used to treat respiratory depression caused by opioid analgesics (pain relievers). Since the active ingredient is used in most cases in emergencies, it is administered intravenously. Naloxone is then injected directly into the vein through a syringe. As a result, successes can be recorded within seconds.

Naloxone can also be used preventively. For this purpose, it is added to some opioid-containing agents (e.g. tilidine). The addition should prevent abuse or make it unattractive. This succeeds because tilidine (opiate) can only develop an effect through the addition of naloxone when taken orally. An addict will not feel intoxicated by the improper injection of the tilidine-naloxone mixture.

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Risks & side effects

Naloxone can lead to undesirable side effects. The likelihood of this increases if the maximum daily dose is exceeded. Very often patients have an increase in blood pressure. Often there are also gastrointestinal complaints, which manifest themselves in nausea, diarrhea and vomiting.

Especially in patients who have received naloxone due to an overdose of a pain reliever, the pain-relieving effect can be negated. The suppressed pain then comes back to life. Opium addicts can also develop opiate withdrawal syndrome. Then there is a contraindication.

It is also possible that naloxone causes allergic reactions. If possible, it should therefore be checked whether there is an intolerance. Studies have also shown that naloxone can cause skin reactions (especially itching or redness). Hyperventilation (extremely rapid inhalation) or cramps can also occur. It is also possible that severe headaches develop.