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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