Routes

ROUTES OF ADMINISTRATION

PSYCHOACTIVE SUBSTANCES ACT ON THE CENTRAL NERVOUS SYSTEM

  • Psychoactive substances are substances that can affect mood, perception, and behavior, and they act primarily on the central nervous system (CNS).

  • These substances are carried to the brain through the circulatory system.

  • Reinforcement of use is affected by:

    • The speed at which a substance enters the circulatory system.

    • The shorter the route to the brain, the more reinforced the use of the substance.

  • The combination of the onset speed of a substance's effects and the duration of those effects serves as a partial indicator of the potential for addiction to that substance.

BLOOD BRAIN BARRIER

  • The brain is protected by a structure known as the blood-brain barrier (BBB), which is composed of tightly sealed cells.

  • This barrier selectively permits certain substances to enter the brain while typically preventing toxins, viruses, and bacteria from crossing.

  • Most psychoactive substances are fat-soluble, which coincides with the brain’s fatty nature, granting these substances a preference for crossing the barrier.

  • The affinity of a substance for fat enhances its absorption speed into the brain. The greater the fat-solubility, the more rapid the absorption and subsequently intense the response elicited by the psychoactive substance.

ROUTES OF ADMINISTRATION

  • There are several main routes through which psychoactive substances can be administered:

    • Inhaling

    • Injecting

    • Snorting and mucosal exposure

    • Orally

    • Contact or Transdermal

INHALING

  • Inhalation involves vaporizing the substance and allowing it to be absorbed through the lungs into the bloodstream.

  • The process moves quickly from the lungs to the heart and then directly to the brain, making it the fastest delivery method, which takes about 7 to 10 seconds.

  • Users retain some capability to regulate the strength of the effect experienced.

  • Common substances administered through inhalation include:

    • Marijuana

    • Crack cocaine

    • Freebase cocaine

    • Nicotine

INJECTION

  • Injection is recognized as a very quick and potent method of delivering substances, leading to immediate effects.

  • Examples of substances administered via injection are:

    • Heroin

    • Cocaine

    • Methamphetamine

  • The intense rush experienced when substances are directly injected is a key characteristic.

  • There are three primary methods of injection:

    • Intravenous (IV) Injection:

    • Also known as slamming.

    • Direct delivery into the vein takes approximately 15-30 seconds for effects to be felt.

    • Intramuscular (IM) Injection:

    • Delivery involves injecting the substance into muscle mass.

    • Effects are usually felt within 3-5 minutes.

    • Subcutaneous Injection:

    • Referred to as “skin popping,” this method delivers the substance under the skin.

    • Effects also take around 3-5 minutes.

MUCOSAL ABSORPTION

  • Mucosal absorption involves the direct entry of substances through the mucous membranes into the bloodstream.

  • This delivery method is quicker because it bypasses the digestive system and its enzymes.

  • There are three principal methods of mucosal absorption:

    • Insufflation:

    • Inhalation through the nose.

    • Commonly associated with substances like cocaine and heroin.

    • Sublingual/Buccal Administration:

    • Administration occurs under the tongue or in the cheek pouch, examples include chewing tobacco or snuff.

    • Typically takes 3-5 minutes for effects to manifest.

    • Suppository Administration:

    • Involves inserting a substance rectally.

    • Utilized for medications like morphine for terminally ill patients, with effects taking 10-15 minutes.

INGESTING

  • Ingesting substances requires passage through the esophagus and stomach before entering the small intestines, where absorption into the bloodstream occurs.

  • After ingestion, substances must go through the liver for metabolism prior to reaching the heart and brain.

  • The ingestion process dilutes the substance due to the action of saliva, stomach enzymes, and liver processing, which generally results in a delayed effect.

  • Typically, the onset of effects is expected in about 20-30 minutes.

  • Examples of substances commonly ingested include:

    • Alcohol

    • Pills

TRANSDERMAL ABSORPTION

  • Transdermal absorption involves the administration of a substance via a patch applied to the skin.

  • This method provides a slow and sustained delivery of the substance into the bloodstream.

  • The duration of effect from transdermal administration can span from 1 to 7 days.

  • Common examples include nicotine patches and Fentanyl patches for pain management.

PSYCHOACTIVE SUBSTANCES ACT ON THE CENTRAL NERVOUS SYSTEM
  • Psychoactive substances are substances that can affect mood, perception, and behavior by interacting with specific receptors and altering neurotransmission within the central nervous system (CNS).

  • These substances are carried to the brain through the circulatory system, where they exert their effects.

  • Reinforcement of use is significantly affected by:

    • The speed at which a substance enters the circulatory system and reaches the brain.

    • The shorter the route and faster the onset to the brain, the more pronounced and immediate the reinforcing effects, thus increasing the potential for habitual use.

  • The combination of the onset speed of a substance's effects and the duration of those effects serves as a critical indicator of the potential for addiction to that substance; rapid onset coupled with short duration often correlates with higher abuse potential.

BLOOD BRAIN BARRIER
  • The brain is meticulously protected by a specialized structure known as the blood-brain barrier (BBB), which is composed of tightly sealed endothelial cells lining the brain's capillaries and further supported by astrocytes.

  • This barrier functions as a selective filter, permitting essential nutrients and certain substances to enter the brain while rigorously preventing toxins, viruses, bacteria, and many polar molecules from crossing, thereby maintaining a stable neural environment.

  • Most psychoactive substances are highly fat-soluble (lipophilic), which aligns with the brain’s high lipid content, granting these substances a preferential ability to traverse the barrier by diffusing directly through the cell membranes.

  • The affinity of a substance for fat greatly enhances its absorption speed into the brain. The greater the fat-solubility, the more rapid the absorption into brain tissue and subsequently more intense and immediate the psychoactive response elicited by the substance.

ROUTES OF ADMINISTRATION
  • There are several main routes through which psychoactive substances can be administered, each influencing the speed of onset, intensity, and duration of effects:

    • Inhaling

    • Injecting

    • Snorting and mucosal absorption

    • Orally

    • Contact or Transdermal

INHALING
  • Inhalation involves vaporizing the substance and allowing it to be absorbed rapidly through the vast surface area of the lungs' alveoli into the arterial bloodstream.

  • The process moves quickly from the lungs to the heart and then directly to the brain, making it the fastest delivery method, typically taking about 7 to 10 seconds for effects to manifest.

  • This rapid onset contributes to a powerful reinforcing effect. Users often retain some capability to regulate the strength of the effect experienced by controlling the depth and duration of inhalation.

  • Common substances administered through inhalation include:

    • Marijuana

    • Crack cocaine

    • Freebase cocaine

    • Nicotine

INJECTION
  • Injection is recognized as a very quick and potent method of delivering substances, leading to immediate and often intense effects due to the direct and concentrated delivery into the body's circulation.

  • The intense 'rush' experienced when substances are directly injected is a key characteristic, contributing to high abuse potential.

  • This route also carries significant health risks, including infections (e.g., HIV, hepatitis) from shared needles, vein damage, abscesses, and a higher risk of overdose due to the precise and often rapid delivery of concentrated doses.

  • Examples of substances commonly administered via injection are:

    • Heroin

    • Cocaine

    • Methamphetamine

  • There are three primary methods of injection:

    • Intravenous (IV) Injection:

      • Also known as slamming, this method involves direct delivery into a vein, introducing the substance immediately into the bloodstream.

      • Effects are usually felt within approximately 15-30 seconds, leading to the most rapid and intense onset among all injection methods.

    • Intramuscular (IM) Injection:

      • Delivery involves injecting the substance into muscle mass, which is less vascularized than veins but offers a steady absorption rate.

      • Effects are usually felt within 3-5 minutes, allowing for a somewhat slower onset compared to IV.

    • Subcutaneous Injection:

      • Referred to as “skin popping,” this method delivers the substance under the skin into the fatty tissue.

      • Effects also take around 3-5 minutes, similar to IM, but absorption can be less consistent and carries risks of local tissue damage and infection.

MUCOSAL ABSORPTION
  • Mucosal absorption involves the direct entry of substances through the highly vascularized mucous membranes into the bloodstream, bypassing the digestive tract and its associated first-pass metabolism.

  • This delivery method is quicker and allows for higher bioavailability compared to oral ingestion, as it bypasses the digestive system and its metabolizing enzymes in the liver.

  • There are three principal methods of mucosal absorption:

    • Insufflation (Snorting):

      • Involves inhaling the substance through the nose, where it is absorbed through the mucous membranes of the nasal passages which are rich in capillaries.

      • Commonly associated with substances like cocaine and heroin, effects are typically felt within minutes (around 2-5 minutes).

    • Sublingual/Buccal Administration:

      • Administration occurs under the tongue (sublingual) or in the cheek pouch (buccal), allowing for direct absorption into the systemic circulation through the capillaries in the mouth.

      • Examples include chewing tobacco or snuff, and certain medications like buprenorphine.

      • Typically takes 3-5 minutes for effects to manifest, avoiding initial liver metabolism.

    • Suppository Administration:

      • Involves inserting a substance rectally, where it can be absorbed through the rectal mucosa.

      • This method partially bypasses first-pass liver metabolism.

      • Utilized for medications like morphine for terminally ill patients, with effects typically taking 10-15 minutes to onset.

INGESTING
  • Ingesting substances requires passage through the esophagus and stomach before primarily entering the small intestines, where absorption into the bloodstream occurs.

  • After absorption, substances must first go through the liver for metabolism, a process known as 'first-pass metabolism,' which significantly breaks down a portion of the substance before it reaches the systemic circulation, heart, and brain.

  • The ingestion process dilutes and metabolizes the substance due to the action of saliva, stomach acids and enzymes, and liver processing, which generally results in a slower onset and reduced peak effects.

  • Typically, the onset of effects is expected in about 20-30 minutes, but this can vary widely based on factors such as stomach contents, gastric pH, and the specific substance.

  • Examples of substances commonly ingested include:

    • Alcohol

    • Pills (e.g., opioids, benzodiazepines)

TRANSDERMAL ABSORPTION
  • Transdermal absorption involves the administration of a substance via a patch applied to the skin, which is designed to allow the substance to slowly permeate the skin layers and enter the underlying capillaries.

  • This method provides a slow, controlled, and sustained delivery of the substance into the bloodstream, maintaining relatively constant plasma concentrations.

  • The duration of effect from transdermal administration can span from 1 to 7 days, offering convenience and consistent therapeutic levels while avoiding first-pass metabolism.

  • Common examples include nicotine patches for smoking cessation and Fentanyl patches for chronic pain management.