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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



History
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

  • The Harrison Act of 1914 - narcotic labeling

  • 1970 - Drug Prevention and Abuse Act - Schedule II


Epidemiology
Epidemiology

  • 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


Pharmacology
Pharmacology

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


Pharmacology1
Pharmacology

  • 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


Pharmacokinetics
Pharmacokinetics

  • 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


Treatment
Treatment

  • 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


Treatment1
Treatment

  • 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


Ecstasy
ECSTASY

  • MDMA-methylenedioxymethamphetamine

    • Ecstasy, XTC, Adam, E

  • MDEA-methylenedioxyethamphetamine

    • Eve

  • MDA-methylenedioxyamphetamine

    • Eve


Ecstasy1
ECSTASY

  • 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


Epidemiology1
Epidemiology

  • 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


Pharmacology2
Pharmacology

o

NH

o

CH3

CH3

MDMA


Pharmacology3
Pharmacology

  • 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


Pharmacokinetics1
Pharmacokinetics

  • 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

tachycardia

tremor

tight jaw muscles

bruxism

nausea

headache

Less common effects

numbness

tingling of extremities

hallucinations

ataxia

blurry vision

nystagmus

mydriasis

hyperreflexia

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


Treatment2
Treatment

  • 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


LSD

  • Ingestion results hallucinations, paranoia, fluctuations in mood

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



LSD

  • 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


LSD

  • 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


PCP

  • Dissociative anesthetic with sympathomimetic and hallucinogenic properties

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

  • Closely related to ketamine


PCP

  • S/Sx:

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

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



GHB

  • “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


GHB

  • 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


Pharmacology4
Pharmacology

  • 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


Pharmacology5
Pharmacology

  • 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


Pharmacokinetics2
Pharmacokinetics

  • 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


Treatment3
Treatment

  • 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


Treatment4
Treatment

  • 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


Labs

  • 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


GBL

  • 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



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