Opiates

Contents

1. Substance group of opiates
2. Historical-medical perspective
3. How does pain arise?
4. Pharmacodynamics and -kinetics
5. Routes of administration
6. Tolerance
7. Withdrawal
8. Problematization

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Substance Group of Opiates

Opiates form a broad substance group:

Natural opiates:

• Opium (from the opium poppy)
• Morphine
• Codeine

Semi-synthetic opiates:

• Heroin (diacetylmorphine)

Fully synthetic opiates:

• Methadone
• Fentanyl
• Polamidon (levomethadone)
• Buprenorphine

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Historical-Medical Perspective

The efforts of 19th-century European physicians to modify the undesired side effects of opium while retaining only the positive effects led to a continuous purification process.

Timeline

Year	Development
1803	A pharmacist first isolates morphine from the opium poppy
~1840	Physician Levin points to possible tolerance/dependence (met with great resistance)
1898	Bayer company produces heroin as a semi-synthetic opiate
Later	Development of fully synthetic opiates (methadone, fentanyl, etc.)

Morphine is still considered the most effective analgesic (pain-relieving medication) to this day.

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How Does Pain Arise?

The body registers a pain impulse that is relayed through the spinal cord to the brain:

1. Pain impulse activates nerve cells
2. Release of transmitters glutamate and substance P
3. Relay through the spinal cord to the limbic system (emotional processing)
4. As a protective reaction: release of endogenous morphines (endogenous analgesics)

This process is called the “neuronal feedback loop”:

Pain sensation → Spinal cord → Limbic system → Spinal cord → Pain site

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Pharmacodynamics and Kinetics

Mechanism of Action

Unlike other pain medications that work locally, opiates affect the nervous system. The effect of morphine lies not in completely eliminating pain but in creating an affective dynamic:

Pain appears to those affected as more bearable, more tolerable, or they become indifferent to it.

Modes of Action

Agonistic opiates (e.g., heroin, morphine):

• Mimic the analgesic dynamics of endorphin neurotransmitters

Opiate antagonists (naltrexone, naloxone):

• Occupy endorphin receptors and thus reverse the effect of exogenous opiates

Effects

Opiate substances exert their effect as:

• Analgesic (pain-relieving)
• Sedative (calming)
• Anxiolytic (anxiety-reducing)
• Euphoriant (euphoria-producing)

Side Effects

Simultaneously provoked bodily reactions:

• Pupil constriction
• Respiratory depression (narrowing of bronchi)
• Depression of intestinal peristalsis

Medical Use

These effects can be medically desired for diarrhea or bronchial conditions.

Opiates not only positively affect physical pain but also produce a pleasantly perceived state of relaxation or euphoria for psychological pain.

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Routes of Administration

Route of Administration	Absorption
Oral / Rectal (suppository)	Slow
Intravenous (e.g., heroin, morphine)	Within seconds/minutes
Inhalation / Smoking	Within minutes

Overdose Risk

With intravenous administration, there is a risk of respiratory depression in case of overdose.

Further medical applications:

• Epidural anesthesia (PDA) — spinal anesthesia during childbirth and operations

Detectability

• Opiates are rapidly metabolized to morphine and codeine (heroin in 3-5 hours)
• Opiate metabolites are detectable for approx. 3-4 days
• Test procedures do not allow conclusions about specific substances

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Tolerance

Opiate dependence manifests as a craving for higher doses and exhibits the following mechanisms:

Physical Mechanisms

• The organism increases the number of opiate-degrading enzymes
• The sensitivity of opiate receptors decreases
• Cross-tolerance with other opiates develops (up to lethal doses)

Psychological Mechanisms (Behavioral Conditioning)

Experiences and associated feelings are triggered (activated) with the help of the opiate effect. Concurrent group experiences during opiate use shape perception and behavior.

Storage occurs through a specific transmitter concentration — new neuronal connections are created that make emotional memory possible and retrievable.

The ecstasy triggered by opiates, combined with setting-related experiences, creates the motivation to repeat the intoxication.

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Withdrawal

The consequences of withdrawal are experienced by those affected as the opposite effect of opiates:

Symptoms

Psychological:

• Intense psychological pain
• Anxiety
• Depression
• Loss of appetite
• Concentration difficulties
• “Craving” (drug hunger)

Physical:

• Intense physical pain
• Nausea, vomiting
• Diarrhea
• Breathing problems

Duration

• Acute withdrawal symptoms: days to weeks
• Protracted abstinence symptoms (depression, craving): for approximately six more months

Social Consequences

• Loss of the reference group
• Social isolation

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Problematization

Set-Related Dispositions

Personality-structural factors can facilitate psychological dependence:

• Low frustration tolerance (reduced psychological resilience in conflicts)
• Avoidance of confrontation with psychological conflicts
• The prospect of being relaxed and happy “at the push of a button”

Setting-Related Factors

The example of massive consumption of “Prozac” (in Germany: Fluctin) in the USA shows that not only the set has an impact but also society.

Psychological problems are not seen as normal reactions to stressful life situations but as unwanted weakness. Social stigmatization and pathologization takes place, demanding a quick and cheap “solution”:

• Problems are made invisible
• People behave “normally” and adapt
• Pharmaceutical companies earn a great deal of money
• The state saves on psychosocial support