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Drugs of Abuse. Dawn R. Sollee, Pharm.D., DABAT Florida Poison Information Center-Jax. Cocaine. History. 6th Century - Peruvian Indians chewed for religious and social reasons 1880s - first used for medicinal purposes 1886 - birth of Coca-Cola, decocainized in 1906

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Drugs of abuse

Drugs of Abuse

Dawn R. Sollee, Pharm.D., DABAT

Florida Poison Information Center-Jax


  • 6th Century - Peruvian Indians chewed for religious and social reasons

  • 1880s - first used for medicinal purposes

  • 1886 - birth of Coca-Cola, decocainized in 1906

  • The Harrison Act of 1914 - narcotic labeling

  • 1970 - Drug Prevention and Abuse Act - Schedule II


  • US currently in last phase of the “third cocaine epidemic”

  • One of the most commonly abused substance, 4th to only alcohol, nicotine, and marijuana

  • 1992 - 22.6 million had tried once,

    5 million abused regularly

  • Most abusers are male, < 40 yo, use multiple drugs


  • Cocaine HCl is the natural alkaloid contained in the leaves of Erythroxylon coca plant


  • Pharmacologic effects:

    • local anesthetic effect

    • central nervous system stimulation

    • inhibition of catecholamine re-uptake

Dosage forms
Dosage Forms

  • Cocaine HCl

    • highly water soluble, available as crystals, granules or white powder

    • high melting point so it can’t be smoked

    • snorted intranasally or dissolved in water and injected

    • vasocontrictive properties limits its own absorption

    • onset- 20 min, peak- 60 min, duration- 3 hr

Dosage forms1
Dosage Forms

  • Free base

    • prepared by treating cocaine HCl with a basic solution

    • precipitated free alkaloid is filtered or dissolved in ether which is then removed by drying

    • smoked because it volatilizes at low temps

    • relatively pure and very expensive

    • onset- 1-2 mins, duration- 30min

Dosage forms2
Dosage Forms

  • Crack

    • named for the sound it makes when heated

    • inexpensive, solid form of free base

    • prepared by mixing with baking soda and water

    • heating forms a “rock” and this is smoked

    • onset- secs, peak- 3- 5 min, duration-20 min

Dosage forms3
Dosage Forms

  • Adulterants

    • street cocaine is usually < 15-20% pure cocaine

    • mannitol, sucrose, lactose, caffeine, talc, heroin, organophosphates, strychnine, amphetamine, lidocaine, acetaminophen


  • Once absorbed, cocaine (t1/2 - 60 min) is metabolized by plasma and liver cholinesterases

  • Two inactive metabolites, benzoylecognine and ecgonine methyl ester

  • Metabolites excreted unchanged in urine

  • Urine drug screens qualitatively measure benzoylecognine

    • acute - detectable up to 72 hours

    • chronic - 7 to 21 days

Clinical presentation caine reaction
Clinical Presentation“Caine Reaction”

  • Acute Intoxication

    • early stimulative phase: excitement, HA, N/V, twitching, hypertension, tachypnea, hypernea

    • advanced stimulative phase: seizures, tachycardia, hypertension, cyanosis, dyspnea, rapid or irregular respirations

    • depressive phase: muscle paralysis, loss of reflexes, loss of vital functions, circulatory and respiratory failure, death

Clinical presentation
Clinical Presentation

  • CV - chest pain, palpitations, arrhythmias, severe hypertension, coronary and peripheral vasoconstriction, myocardial infarction, cardiomyopathy

  • Neuro - AMS, seizures, status epilepticus, HA, syncope, ischemic stroke

  • Metabolic - hyperthermia, rhabdomyolysis, renal failure, hepatotoxicity, DIC

Clinical presentation1
Clinical Presentation

  • Chronic Intoxication

    • persistent rhinorrhea, epistaxis, septum perforation, paranoid psychosis, severe anxiety and panic states, depression, perceptual changes, extreme itching, hallucinations

Clinical presentation2
Clinical Presentation

  • Body Packers - swallowing containers, condoms, balloons or other packages to smuggle cocaine

  • Body Stuffers - street entrepreneurs who ingest cocaine to avoid arrest


  • Stabilization (ABCs, IV line, cardiac monitor, EKG)

  • GI decontamination

    • activated charcoal

    • whole bowel irrigation (packers, stuffers)

      • 500 cc/hr, inc. by 500cc/hr to 2L/hr

      • endpoint - clear rectal effluent


  • CNS - benzodiazepines

  • Seizures - benzodiazepines

    • refractory: barbiturates, no role for phenytoin

  • Tachyarrhythmias and Hypertension - benzodiazepines

    • refractory: combination nitroprusside and esmolol

  • Dysrhythmias - lidocaine, magnesium

  • Hypotension - fluids, norepinephine or dopamine


  • MDMA-methylenedioxymethamphetamine

    • Ecstasy, XTC, Adam, E

  • MDEA-methylenedioxyethamphetamine

    • Eve

  • MDA-methylenedioxyamphetamine

    • Eve


  • 1914 - Originally patented as an appetite suppressant, but never actually marketed

  • 1970s - adjunct psychotherapy

  • 1972 - recreational use first reported

  • 1980s - gained popularity and increased use

  • 1985 - Schedule I substance

  • 1986 - Controlled Substances Analogue Enforcement Act


  • Stanford University

    • 1987: 149/369 (39%) used MDMA at least once

    • mean usage 5.4 times/person

  • Tulane University

    • 1990: 307/1264 (24%) used MDMA at least once

    • up from 15.5% in 1986

    • more likely than any other drug to have been used first during college









  • Chemically related to both hallucinogens and stimulants

  • Entactogens - don’t cause classic hallucinogens, but reduce negative feelings, breakdown communication barriers, allow psychotherapeutic breakthroughs

  • Available forms: white powder, capsules, tablets, Red Bull


  • Readily absorbed across most biologic membranes, highly lipid solubility

  • Onset of action: ~ 30 min

  • Duration of effect: 4 - 6 hours

  • Elimination: demethylation to MDA,

    65% unchanged urine

    Dosing: 50-150mg hallucinogenic effect

Mechanism of toxicity
Mechanism of Toxicity

  • Sympathetic receptor stimulation (peripheral and central nervous system)

  • Indirect receptor stimulation causing NT release (primarily serotonin)

  • Inhibition of monoamine oxidase

  • Inhibition of catecholamine reuptake

  • Biotransformation of agents to indolamines related to serotonin

Clinical presentation3

Common effects



tight jaw muscles




Less common effects


tingling of extremities



blurry vision




Clinical Presentation

Acute reactions at therapeutic doses

Clinical presentation4
Clinical Presentation

  • Overdose reactions

    • tachycardia/dysrhythmias

    • hypertension or hypotension

    • hyperthermia

    • muscular rigidity

    • seizures

    • ARDS

    • disseminated intravascular coagulation

    • rhabdomyolysis

    • renal failure

Clinical presentation5
Clinical Presentation

  • Mild residual reactions ( 2 hrs - 2 wks)

    • exhaustion

    • fatigue

    • depression

    • nausea

    • numbness

    • flashbacks

    • anxiety attacks

  • Long term - 5HT neuron damage


  • ABCs

  • GI decontamination - activated charcoal

  • Symptomatic/supportive

    • agitation - benzos, butyrophenones

    • hyperthermia - benzos, cooling with mist and fans, dantrolene

    • seizures - benzos, barbs

    • sinus tach/HTN - nitroprusside and esmolol


  • Ingestion results hallucinations, paranoia, fluctuations in mood

  • Can be in the form of powder, tablet, capsule, sugar cube, drop on blotting paper, in gelatin


  • Other names: blotter, blue caps, brain buster, CA sunshine, cubes, face melter, ghost, heavenly blue, hawk, microdot, pearly gates, royal blue, wedding bells, white lightning, window pane


  • Mechanism of action

    • agonist at presynaptic receptors for 5-HT in the midbrain

    • etiology of flashbacks is unknown

    • tolerance develops after 3-4 daily doses


  • Dissociative anesthetic with sympathomimetic and hallucinogenic properties

  • Thought to stimulate alpha-adrenergic receptors (potentiating NE, Epi, 5-HT)

  • Closely related to ketamine


  • S/Sx:

    • common: nystagmus, htn (57%), violent/agitated behaviour, tachy (30%), delusions/hallucinations

    • uncommon: coma, lethargy, hyperthermia, mydriasis, seizures, miosis


  • “Grievous Bodily Harm”, “Georgia Home Boy”, “Liquid Ecstasy”, “Liquid X”, “Soap”, “Easy Lay”, “Scoop”, “Salty Water”, “Organic Quaalude”, “Somatomax”, “G-riffick”

  • “Max”: GHB + ETOH + amphetamine

  • Falsely promoted for strength training, muscle building, weight loss and insomnia

  • Primarily used by party and nightclub attendees and bodybuilders

  • It is also sold and used as a hallucinogen and a “date rape” drug


  • FDA banned its use in 1991 after reports of seizures and coma in individuals using nutritional and weight loss supplements

  • Illegal to possess in California, Massachusetts, Hawaii, and Florida

  • Schedule I drug in Georgia, Rhode Island, Michigan, Illinois, Texas, Nevada and Hawaii


  • Four-carbon molecule found naturally in the central nervous system (CNS) with higher concentrations in the peripheral tissues

  • GABA metabolite with possible role as a central neurotransmitter

    • inhibition of dopamine at low doses

    • promotes dopamine release at high doses

  • Inhibits release of norepinephrine in the hypothalamus


  • CNS depressant that facilitates slow-wave sleep

  • In animals, produces abnormal EEG activity similar to absence seizures

  • Can be synthesized from G-butyrolactone and sodium hydroxide


  • Readily crosses the BBB

  • Rapidly absorbed after ingestion

  • Elimination t1/2 is 27 minutes

  • Primary route of elimination is expired breath as carbon dioxide

Clinical use
Clinical Use

  • First use was as a general anesthetic

    (50 mg/kg), but no longer used

  • Only FDA approved for investigational uses

    • narcolepsy

  • Outside US

    • opiate and alcohol addiction tx

    • shock

Clinical presentation6
Clinical Presentation

  • 10 mg/kg

    • amnesia, hypotonia

  • 20-30 mg/kg

    • euphoria, somnolence, drowsiness, dizziness

  • 50-70 mg/kg

    • coma, hypotonia, bradycardia, hypotension, bradypnea, N/V

  • Hallucinations, delirium, diaphoresis, hypothermia, seizures

Clinical presentation7
Clinical Presentation

  • Abrupt LOC leading to coma, a strong persistent gag reflex, and rapid awakening without apparent adverse aftereffects

  • Effects potentiated by alcohol and benzos

  • Chronic withdrawal symptoms - insomnia, anxiety, tremor, paranoia, agitation, confusion, delirium, irritability- resolves in 3-12 days without long-term effects

Clinical presentation8
Clinical Presentation

  • Onset

    • IV: 2-15 min

    • PO: 15-30 min

  • Duration

    • coma typically lasts 1-2 hours, with full recovery by 8 hours

    • dizziness may linger for up to 2 weeks


  • Supportive

  • Stabilization and Observation

    • cardiac monitoring, pulse oximetry, airway maintenance and ventilatory support if needed

    • temperature regulation if hypothermia present

  • Standard treatment for polysubstance OD

    • GI decontamination

      • (activated charcoal)

    • naloxone can be considered


  • No clinically effective GHB antagonists have been identified in the literature

  • Undetectable by routine drug screens and doesn’t appear to alter lab studies

  • Because of the lack of distinctive diagnostic markers, R/O all other causes of acute unresponsiveness even if h/o GHB ingestion is known


  • MedTox Laboratories

    • 402 W. County Rd. D, St. Paul, Minn, 55112

    • (612) 636-7466

    • Urine GHB ($97), flunitrazepam ($74)

  • National Medical Services

    • 3701 Welsh Rd, Willow Grove, Penn, 19090

    • (215) 657-4900

    • Urine GHB ($111), flunitrazepam ($169), chain of custody ($29)

Similar agents
Similar Agents

  • Gammabutyrolactone

    • RenewTrient, Blue Nitro, Revivarant, Gamm-G, Pro-G, FireWater, Remforce, GH Revitalizer, Rest Eze

    • 4-butyrolactone, dihydro-2(3H) furanone, 4-butanolide, Borametz, False Borametz

  • 1, 4-butanediol, 1, 4-butylene glycol, tetramethylene glycol, tetrahydrofuran

    • GHRE, OrangeFX Rush, Lemon FX Drop, Pine Needle Extract, Promusol, BVM, Cherry FX Bomb, Enliven, Serenity

Similar agents1
Similar Agents

  • On January 21, 1999 the FDA asked manufacturers to recall their GBL containing products

  • Issued an alert to consumers not to purchase or consume products containing GBL

  • Considering all potential regulatory actions at its disposal if products are not recalled


  • Used as an industrial solvent and dietary supplement

  • Better absorption and bioavailability than GHB

  • Seizures more common than GHB

  • Metabolized to GHB endogenously, converts exogenously in alkaline environment

Typical dosing
Typical Dosing

  • Blue-Nitro ($64.95 for 32 oz)

    • 1 teaspoon, mild relaxant

    • 2 teaspoons, well being

    • 3 teaspoons, sleep inducer

    • 3 tablespoons, deep sleep

    • Each ounce contains 2.5gm of GBL