Amphetamines

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Last update: Wednesday, 22 May 2024 at 4.08 pm.


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WARNING: THE ARTICLE CONTAINS SERIOUS DEFICIENCIES AND WILL BE REWORKED! For further information, use the recommended study materials, or contact me or the editors . Information improbable , factually incorrect , or lacking a citation of a specific party is marked in italics .

  • Ice, Krystal, Speed
  • Methamphetamine, meth.
  • Amphetamine (illegal in Poland, Germany)
  • drugs: Ephedrine, pseudoephedrine, phentermine, phenmetrazine, methylphenidate[1]

Pharmacology

  • Mechanism of action – structural similarity to dopamine – phenylalkylamines
  • Indirect sympathomimetics - noradrenaline- like effects
  • Amphetamines release or replace neurotransmitters on the nerve endings
  • Amphetamines - agonists of dopamine, noradrenaline, serotonin

Abuse

  • Salts (HCl) – p.o., sniffing, i.v.
  • Base – inhalation, smoking
  • Usual daily doses 2–100 mg
  • Repeated doses in chronic conditions, whiplash, up to 5 g/day
  • Symptoms
    • euphoria, increased performance (doping)
    • risky behavior, spurts of thought at the expense of accuracy, impaired judgement
    • aggressiveness, irritability, psychological lability, anxiety
    • hypertension , anorexia nervosa – suppression of the feeling of hunger
  • Duration of stimulation: 2–4 hours
  • Overdose: restlessness, inability to concentrate, hallucinations, convulsions
Chronic abuse
  • weight loss
  • damage to the cardiovascular system, development of hypertension, cerebral hemorrhage
  • psychoses, punishments , depression , suicidal tendencies
  • the development of psychological dependence
  • development of tolerance

Enantiomer selectivity

  • Catecholamines ( dopamine , ...) and amphetamines - asymmetric atom C*
  • Number of asymmetries – number of enantiomers
  • Endogenous adrenaline and noradrenaline are levorotatory and have higher affinity for receptors and transport proteins than dextrorotatory enantiomers
  • Amphetamine acts as an indirect sympathomimetic. It has one asymmetric carbon. The dextrorotatory enantiomer (dextroamphetamine) has about 4 times stronger CNS stimulatory effects than the levorotatory isomer
  • Ephedrine contains contains 2 centers of asymmetry and therefore has 4 possible optical isomers:
    • (+) a (–) ephedrine
    • (+) a (–) pseudoephedrine
    • The most biologically effective is (–) ephedrine[1]


=== Ephedrine, Pseudoephedrine ===

  • The plant Ephedra vulgaris – a thousand-year tradition of use in China
  • Ephedrine is found in a number of plants
  • Synthetic ephedrine, pseudoephedrine
  • Ephedrine, pseudoephedrine components of composite medicinal products:
  • Ephedrine – direct and indirect sympathomimetic
  • Psychostimulant chronic effect - addiction
  • Ephedrine, pseudoephedrine – precursors of the illegal synthesis of methamphetamine
KHAT

[1]

KHAT

  • The leaves of the Catha edulis plant are chewed - Arabia
  • They contain cathinone and nor-pseudoephedrine
  • Cathinone is metabolized to norephedrine[1]

MDMA, XTC, ECTASY

  • 3,4-methylendioxymethamfetamin
  • MDMA and similar derivatives – entactogens, stimulants
    • en (Greek) – inside
    • tactus (Latin) – touch
    • gen (Greek) – to produce
  • MDMA – pleasant empathetic feelings, penicillin of the soul

Pharmacology

  • MDMA – a serotonin agonist
  • Sympathomimetic reaction ( hyperthermia , hyperactivity, salivation, mydriasis ))
  • Massive release of serotonin from nerve endings into the synapse - decrease in nerve endings - increase in extracellular serotonergic activity, non-specific stimulation of receptors in the CNS - serotonin syndrome
  • MDMA also releases dopamine (cytotoxic) which replaces serotonin in nerve endings – cell damage triggers unwanted biochemical reactions – neurotoxicity of MDMA
  • Repeated use – sensitization, allergy
    • prolongation and intensification of serotonergic syndrome
    • increasing the toxicity of further doses

Abusus

  • Tablets po – different logos, shapes, sizes, colors, unknown content
  • Effective single doses of 50-200 mg
  • Pleasant desirable symptoms: empathy, stimulation (dance drug)
  • Side unpleasant symptoms:
    • dry mouth
    • trismus (difficulty opening the mouth)
    • perspiration
    • fainting
Chronic abuse
  • depression
  • insomnia
  • psychosis
  • psychological dependence
  • tolerance

* development of sensitization ( allergy )

Health complications

  • tachycardia , arrhythmia , cardiac collapse
  • serotonin syndrome – sweating, tremors, hyperthermia , rhabdomyolysis, disseminated intravascular coagulation ( DIC ) – death
  • dehydration, hyponatremia , circulatory failure
  • liver failure (rare)
  • in chronic patients – cognitive disorders, psychoses, hypertension, vascular events

Risk factors

  • unknown contents of illegal tablets, drug cocktails, ethanol
  • individual state of health, receptivity

Ecstasy tablets

  • Tablets po – different logos, shapes, sizes, colors, unknown content
  • Dance drugs, New Synthetic Drugs (NSDs), "Designer drugs"
  • Expected Effect – Stimulant and Psychedelic (Empathy)
  • Psychedelics – natural hallucinogens (mescaline, DMT, etc.)
  • MDMA, a controlled psychotropic substance

NSD - small change in structure - other pharmacological action - dangerous !!![1]

Linkes

References

  1. ↑ a b c d e BALÍKOVÁ, Marie. Abuzus a intoxikace [online]. [cit. 2012-03-09]. <https://el.lf1.cuni.cz/p56355604/>.