Drug abuse and toxicology screening
Dr. Mohamed AL-Tufail
Head of toxicology laboratory, KFSHRC
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 Systematic toxicological analysis (STA) is a major part of the examination in clinical toxicology. STA is aimed at detecting and identifying all substances of toxicological relevance (i.e. drugs, drugs of abuse, poisons and/or their metabolites) in biological material. Particularly, gas chromatography –mass spectrometry
(GC/MS) is a routinely applied screening and confirmation tool in
STA. There is clear trend, however, to complement existing GC/MS procedures with liquid chromatography-mass spectrometry (LC/MS) assays. One competent LC/MS-based approach for untargeted screening analysis makes use of MS/MS under data-dependent acquisition control (DDA) to identify compounds by subsequent library search
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Alcohol Analysis
Equipment: Headspace GC-MS
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BLOOD ALCOHOL
URINE ALCOHOL
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Basic Pharmacology of Alcohol (ethyl alcohol)
Non-potent compound: 80 mg/dL (0.08%)
Nonspecific compound:
(1) Potentiates the inhibitory effects of the transmitter GABA by altering the conformation of the heteropentameric GABA
A receptor and increases Chloride ion entry into neurons.
(2) Inhibits the activation of NMDA-type glutamate receptors reducing Sodium and
Calcium ion entry into neurons.
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Basic Pharmacology of Alcohol (con’t)
 Acute : produces dose-dependent intoxication, loss of behavioral inhibition, sedation, impaired judgment, slurred speech, ataxia. At higher doses: loss of consciousness, anesthesia, coma, respiratory depression, cardiovascular depression.
 Chronic : hepatitis and cirrhosis, gastrointestinal bleeding, hypertension, thiamine deficiency.
 Teratogenicity : fetal alcohol spectrum disorders.
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Basic Pharmacology of Psychostimulants
(cocaine & methamphetamine, dextroamphetamine, methylphenidate)
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Indirect acting sympathomimetics: block the reuptake of the neurotransmitters: dopamine, norepinephrine and serotonin
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Basic Pharmacology of Psychostimulants (con’t)
- Acute: arousal, euphoria, agitation, restlessness, insomnia, anorexia, tachycardia, hyperthermia, seizures.
- Chronic: psychotic delusions and paranoia.
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 Marijuana Tetrahydrocannabinol (THC) is the
Active alkaloid from the cannabis plant
Currently the most commonly used illegal drug
Binds and activates abundant G-protein coupled receptors in brain (CB1 and CB2); reduces neuronal excitability by:
- increasing K+ conductance and
- decreasing Ca+ + conductance
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 Basic Pharmacology of Opiates (heroin, morphine, oxycodone)
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Mu, Kappa, and Delta types opioid receptors
Mu receptor activation induces euphoria, Kappa receptor activation produces dysphoria
Enkephalins, Endorphins and Dynorphins are the endogenous ligands that are released during stress to induce analgesia, immobility (sedation), euphoria or dysphoria.
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Excretion
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Drugs are eliminated from the body either unchanged as the parent drug or as metabolites (a changed form of the drug).
Organs that excrete drugs eliminate polar compounds
(water soluble) more readily than components with high lipid (fat) solubility. The exception to this premise is the lungs.
Lipid soluble drugs are not readily eliminated until they are metabolized to more polar compounds.
Possible sources of excretion include:
Breath
Urine
Saliva
Perspiration
Feces
Milk
Bile
Hair
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DRUG
Amphetamine
Barbiturates
Benzodiazepines
CLASS DETECTION TIME IN URINE
Stimulant Up to 2 days depressants / sedatives / hypnotics short-acting: 2 days long-acting: 1-3 weeks
(based on half-life) depressants / sedatives / hypnotics therapeutic dose: 3 days chronic use: 4-6 weeks or longer
Cocaine (benzoyl ecgonine metabolite)
Codeine
Stimulant Up to 4 days
Analgesic / Opiate 2 days
Ethyl alcohol, ethanol depressants / sedatives / hypnotics urine: 2 to 12 hours serum/plasma: 1 to 12 hours
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DRUG
Heroin
Marijuana, Cannabinoids
Methadone
Methamphetamine
Methaqualone
MDMA(methylenedioxymethamphetamine)
Morphine
Phencyclidine
Propoxyphene
CLASS DETECTION TIME IN URINE
Analgesic /
Opiate
2 days
Hallucinogen Single use: 2 to 7 days
Prolonged, chronic use: 1 to 2 months or longer
Analgesic /
Opiate
Stimulant depressants / sedatives / hypnotics
Stimulant
3 days
Up to 2 days
Up to 14 days
Up to 2 days
Analgesic /
Opiate
2 days
Hallucinogen 8-14 days, but up to 30 days in chronic users
Analgesic /
Opiate
6 hours to 2 days
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Hair Test for Cocaine
It may have a positive result within 8 hours, or at times, only after 7 to days after cocaine use. The substance can remain on the hair for months , even until the hair is trimmed. Cannot be done by a single hair, the procedure requires a samples of hair around 5 inches long.
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Elimination of Alcohol
 The liver is responsible for the elimination - through metabolism - of
95% of ingested alcohol from the body. The remainder of the alcohol is eliminated through excretion of alcohol in breath, urine, sweat, feces, milk and saliva. The body uses several different metabolic pathways in its oxidation of alcohol to acetaldehyde to acetic acid to carbon dioxide and water.
 Healthy people metabolize alcohol at a fairly consistent rate. As a rule of thumb, a person will eliminate 15 ml of alcohol per hour.
Several factors influence this rate. The rate of elimination tends to be higher when the blood alcohol concentration in the body is very high. Also chronic alcoholics may (depending on liver health) metabolize alcohol at a significantly higher rate than the average.
Finally, the body's ability to metabolize alcohol quickly tend to diminish with age.
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Toxicology screening and drug abuse analysis using GC-MS and LC-MS
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Extraction
Clean up
Concentration
Injection on GC-MS or LC-MS
Reporting

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Acid
base
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Theoretically can separate drugs into 5 categories
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1) Blood & Urine
- single basic or acidic extraction
2) Urine 3 ways extraction
- acid
- weakly basic & neutral
- basic
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Basic Extraction – GC/MS Screen
Blood + Base (NH
4
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OH) + Toluene
BACK EXTRACTION (clean up)
Toluene + Acid (H
2
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SO
4
)
Aqueous fraction + Base (NaOH) + Toluene
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GC/MS
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CHROMATOGRAPHY chromatography is a separation process that is achieved by distribution of the substances between a mobile phase and a stationary phase
A mobile
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A stationary
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-5
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Acid and base properties of cocaine and its metabolites
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Drugs of abuse detected in human hair, methods of detection
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Drugs of abuse detected in human hair, methods of detection
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LC-MSMS
QTOF
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LCMSMS TSQ (QUANTUM ACCESS MAX)
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Sibutramin

Sample Number M:34-141 ( Capsules )

Containing
High Quantity of Procymidone ( Pesticide )
Procymidone concentration is 2700 ppb
Maximum residue limit is 100 ppb .
Procymidone

Sample Number M:34-153 ( Herbal Powder )

Contains
2-Pyridinamine
Methyl Salicylate
Acetaminophen

Sample Number M:35-214 ( Herbal Powder )

Royal Honey containing Synthetic drug Tadalafil in Concentration of 1.8 mg/g
Tadalafil is sexual stimulant ( Commericially Cialis )

Royal Honey
Containing Synthetic drug Tadalafil
Tadalafil is sexual stimulant ( Commericially Cialis )

Sample Number M:34-152 ( Sliming )

Sibutramine

Sample Number M: 34-125-1
Herbal Powder

Contaminated with
Aerobic plate count :
2.0x10
5 CFU/mL - Limit 10 5 CFU/mL
Yeast and Moulds :
4.0x10
3 CFU/mL - Limit is 10 3 CFU/mL
Enterobacteriaceae :
1.0x10
3 CFU/mL - Limit is 10 3 CFU/mL
Also contains high cocentration of Arsenic ( 411 ppb )
And high concentration of Lead ( 6472 ppb )

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