Amphetamines

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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

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

=== 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:
  • broncholytics
  • antitussive
  • antipyretics
  • analgesics (NUROFEN)
  • venopharmaceuticals
  • anorexic (norpseudoephedrine)
• Ephedrine – direct and indirect sympathomimetic
• Psychostimulant chronic effect - addiction
• Ephedrine, pseudoephedrine – precursors of the illegal synthesis of methamphetamine

KHAT

KHAT

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

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 !!!

Linkes

Related articles

• Substance Abuse • Drug Addiction and Illicit Production and Possession of Narcotic Substances • Opioid Abuse
• Amphetamines • Cocaine • Cannabinoids • Hallucinogens • LSD • Psychotropic drugs • Barbiturates • Benzodiazepines • Ethanol
• Cannabinoid use disorders • Opioid use disorders