STIMULANTS

STIMULANTS


STIMULANTS 

Introduction:

  • Main substance included – Cocaine.

Cocaine:

  • Derived from “Erythroxylum coca”.
  • Studied by Sigmund Freud.

MOA:

  • Acts primarily by blocking dopamine receptors (D1 & D2) –> increasing dopamine concentration in synaptic cleft.
  • Inhibitor of norepinephrine uptake —> Significant sympathomimetic effect.

Actions & Uses:

  • Vasoconstriction:
    • Marked vasoconstriction of peripheral arteries —> Hypertension.
    • Vasoconstriction of epicardial coronary arteries –> Causes ischemic myocardial injury.
  • Causes seizures –
    • Cocaine (most common) & amphetamines (2nd common) associated with seizures.
  • As LA:
    • Used as LA in eye, nose and throat surgery.
    • MOA: LA effected mediated by blockade of fast, sodium channels.
  • As Inhalation agent:
    • Known as “snorting”.
    • Vasoconstriction of cocaine —> nasal inhalation of cocaine –>nasal congestion –> nasal septal perforation.
  • Long term use:
    • Jet black pigmentation of tongue.
  • Methods of intake:
    • Smoking – Freebasing.
    • Freebasing involves mixing street cocaine (procaine or sugar as adulterants) with freebase (chemically extracted pure cocaine).
    • Crack – Extremely potent freebase form of cocaine smoked & single use can cause intense craving.

Intoxication:

Characterized by euphoria, pupillary dilatation, tachycardia, hypertension & sweating.

Acute intoxication: 

  • On moderate to high dose of cocaine.
  • Paranoid ideations, auditory hallucinations & visual illusions.
  • Cocaine bugs/formication/Magnan phenomenon – Tactile hallucinations (feeling of insects crawling under skin).

Withdrawal symptoms:

  • Strong psychological dependence.
  • Mild physiological dependence (tolerance & withdrawal symptoms).
    • Feeling low, exhaustion, lethargy, fatigue, insatiable hunger.
    • Most severe symptom – Depression & suicidal ideation.

Cocaine-induced psychotic disorder:

  • Most commonly due to intravenous use & crack users.
  • Hallmark presentation – Paranoid delusions (delusion of persecution) & auditory hallucinations. 
  • Visual & tactile hallucinations (cocaine bugs) present. 
  • Symptoms are quite similar to paranoid schizophrenia.
  • Treatment:
    • Psychotherapeutic interventions – Cognitive behavioral therapy, group therapy & support groups (narcotic anonymous).

Exam Important

  • Cocaine is derived from “Erythroxylum coca” and was studied by Sigmund Freud.
  • Cocaine acts primarily by blocking dopamine receptors (D1 & D2) thus increasing dopamine concentration in synaptic cleft.
  • Cocaine causes marked vasoconstriction of peripheral arteries causing hypertension.
  • Vasoconstriction of cocaine causes nasal inhalation then nasal congestion resulting in nasal septal perforation.
  • On long-term use of cocaine jet black pigmentation of tongue occurs.
  • Crack is an extremely potent freebase form of cocaine smoked.
  • Acute intoxication of cocaine causes paranoid ideations, auditory hallucinations & visual illusions.
  • Cocaine bugs/formication/Magnan phenomenon are tactile hallucinations (feeling of insects crawling under skin) resultant of acute intoxication.
  • Withdrawal symptoms have strong psychological dependence & mild physiological dependence.
  • Cocaine induced psychotic disorder have hallmark presentation of paranoid delusions (delusion of persecution) & auditory, visual & tactile hallucinations (cocaine bugs).
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