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Sialylated derivative of the

Lewis blood group system,
known as Lexa
Immunoassay method are
used for measurement

THERAPEUTIC DRUG MONITORING

Cardioactive Drugs

Drug Treatment for Therapeutic Level Toxic level Toxic effects Other information
Digoxin Atrial arrhythmia and 0.5-2 ng/mL >2 ng/mL Nausea, vomiting, Therapeutic actions and
congenital heart visual disturbances, toxicities can be
failure premature ventricular influenced by serum
contractions and electrolytes
atrioventricular bode 25% of this is protein
blockage bound
Hyperthyroid individuals
are resistant to digoxin
Peak level: 8 hours after
oral dose
Half-life: 38 hours
Lidocaine Used to correct 1.5-4.0 ug/mL >4.0 ug/mL CHF and heart block Can be used as local
(Xylocaine) ventricular arrythmia anesthetic
for treatment of acute (1.5-1.0 sa handouts) CNS depression: It is bound to albumin
myocardial infarction >4-8 ug/mL and AAG
Primary product of
Seizure and decreased hepatic metabolism:
bp and cardiac output: monoethylglycinexylidide
>8 ug/mL (MEGX)
Quinidine For the treatment of 2.3-5.0 ug/mL >5ug/mL Cinchonism, blood 85% protein
arrythmia dyscrasia, and Peak serum level: 2 hours
hepatitis after an oral dose
(sulfate), 4-5 hours
(gluconate)
Procainamide To treat ventricular 4-10 ug/mL >12 ug/mL Reversible lupus-like 20% protein bound
(Pronestyl) arrythmia syndrome (ANA), Hepatic metabolite: N-
nephritic syndrome, acetyl procainamide
urticaria (NAPA)
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Peak serum level: one

hour after dose
Disopyramide Used to treat cardiac 3-5 ug/mL 10 ug/mL Bradycardia and Substitute for quinidine.
arrythmias atrioventricular node It has anticholinergic
blockage effects.
Propranolol Used to treat angina 50-100 ng/mL Bradycardia, arterial Suppresses the
pectoris, insufficiency conversion
hypertension, (Raynaud’s type),
coronary artery platelet disorder, and
disease pharyngitis
Amiodarone Treatment for 1.0-2.5 ug/mL >2.5 ug/mL Bradycardia, hepatitis, It blocks potassium
(Cordarone) ventricular arrythmias photodermatitis, and channels in the cardiac
thyroid dysfunction muscles
It is iodine-containing
drug that causes
hyper/hypothyroidism
Verapamil Treatment for angina, 80-400 ng/mL Hypertension,
hypertension, and peripheral edema, and
supraventricular ventricular fibrillation
arrythmias

ANTIBIOTICS

Drug Treatment for Therapeutic Level Toxic level Toxic effects Other information
Aminoglycosides Treatment for Gram- Amikacin and Nephrotoxicity and Administered through
(Gentamicin, negative bacterial Kanamycin: ototoxicity IM or IV, not well-
Tobramycin, infections >30 ug/mL – peak absorbed from GIT.
Amikacin, level May cause damage to
Kanamycin, 8th cranial nerve
Neomycin, or Gentamicin and
Streptomycin) tobramycin:
12-15 ug/mL – peak
Vancomycin Effective against gram- 5-10 ug/mL – toxic Nephrotoxicity: “Red-man syndrome”, Trough levels are
positive cocci and side effects can occur >10 ug/mL nephrotoxicity, monitored to ensure
bacilli ototoxicity the serum drug
Ototoxicity: concentration is within
>40 ug/mL the therapeutic range
Chloramphenicol >25 ug/mL Blood dyscrasia, Distributed to all
cytoplasmic tissues, concentrates
vacuolation in the CSF.
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50% protein bound,

rapidly absorbed in
GIT.

ANTIEPILEPTIC DRUGS

Drug Treatment for Therapeutic Level Toxic level Toxic effects Other information
Phenobarbital It is a long-acting Nystagmus, stupor, Not used for petit mal
barbiturate that ataxia, and respiratory seizure.
controls grand mal depression. Absorption is low but
tonic- clonic seizure complete.
and focal epileptic. 50% protein bound,
For treating stored in brain.
withdrawal symptoms Renal impairment
in infants-mothers are slows down
addicted to opiate or elimination process.
barbiturate. Inactive proform:
Used to treat cases of primidone (mysoine).
congenital Half-life: 70-100 hours.
hyperbilirubinemia Peak serum level:
Phenobarbital: 20-
40ug/mL
Primidone: 5-12
ug/mL
Phenytoin (Dilatin) It controls seizures 10-20 ug/mL >20 ug/mL Toxicity may be seen Not used for petit mal
(tonic-clonic, simple in therapeutic levels. and atomic seizures.
partial seizures) Free form: Major toxicity: Decreases sodium and
Short-term 1-2 ug/mL initiation of seizures; calcium influx into
prophylactic agent in teratogenic action hyperexcitable
brain injury. (cleft lip and palate) neurons.
and nystagmus IV administered, GIT
absorption incomplete.
87-97% protein bound
Free form: if
biologically active
portion.
Injectable proform:
fosphenytoin
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Valproic Acid Treatment for petit 50-100 ug/mL >100 ug/mL (NLW) >100 ug/mL: Orally administered,
(Depakene) mal (absence of Nausea, lethargy, and GIT is rapid and
seizure), atomic >200 ug/mL (PHH) weight gain complete.
seizure, and grand mal Highly protein bound
seizure >200 ug/mL: (93%).
Pancreatitis, Hepatic dysfunction
hallucinations, can be observed,
hyperammonemia monitoring requires
after 6 months of
therapy
Carbamazepine Effective for grand mal 4-16 ug/mL >12 ug/mL Idiosyncratic effects: Tricyclic compound
(Tegretol) seizures and treating Rashes, leukopenia, related to imipramine
seizures accompanied nausea, vertigo, febrile (TCA).
by pain. reactions. Not frequently used –
has serious toxic effect.
Toxic effects: Orally administered.
Hematologic
dyscrasias, aplastic
anemia, irregular pulse
and ataxia.
Ethosuximide Controlling petit mal 40-100 ug/mL >100 ug/mL Gi disturbances, ataxia, Orally administered.
(Zarontin) (absence) seizure SLE, aplastic anemia Free in serum and not
and pancytopenia protein bound.

Gabapentin Used for partial 2-15 ug/mL Adverse Effect: Chemically similar to
(Neurontin) seizures, adjunctive Dizziness, ataxia, neurotransmitter
therapy fatigue, and gamma aminobutyric
nystagmus. acid (GABA).
Administered orally,
Toxic effects: unbound to plasma
Ataxia and somnolence proteins.

Topiramate, Adjunctive drug for

Lamortigine partial seizures.
(Lamictal)
PSYCHOCTIVE DRUGS

Drug Treatment for Therapeutic Level Toxic level Toxic effects Other information
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Lithium Treatment for manic- 0.8-1.2 mmol/L 1.2-2 mmol/L (ALS) Severe dehydration, Inhibits thyroid
depressive illness >2 mmol/L (SMC) nephrotoxicity, and hormone synthesis
(bipolar disorder). hypothyroidism. and release.
Drug of choice for Inhibits iodine uptake.
prevention of chronic 1.2-2 mmol/L: A cationic metal.
cluster headache Apathy, lethargy, Orally administered
speech difficulties and absorption rapid
and complete.
>2 mmol/L: Lithium and
Seizures, muscle democlocycline inhibit
rigidity, and coma. the effect of ADH in the
kidney.

Tricyclic Treatment for 100-300 ng/mL Drowsiness, blurred Orally administered

Antidepressants depression, insomnia, vision, memory loss, with variability in
(TCAs) extreme apathy, and seizure, cardiac absorption.
loss of libido arrythmia, Highly protein bound
parkinsonian (85-95%).
syndrome, and Examples: imipramine,
unconsciousness amitriptyline, doxepin,
nortriptyline,
trazadone.
Peak serum level: 2-12
hours.
Major metabolite:
desipramine
Flouxetine (Prozac) Treatment for 90-300 ng/mL Attempted suicide, It blocks the re-uptake
obsessive-compulsive decreased libido and of serotonin central
disorders. sexual function. serotonergic
pathways.

BRONCHODILATOR

Drug Treatment for Therapeutic Level Toxic level Toxic effects Other information
Theophylline Treatment for asthma 10-20 ug/mL >20 ug/mL GI bleeding, seizures, Inhibitory to the
and chronic tachycardia and release of histamine
obstructive pulmonary syncope. and other
disease. proinflammatory
Drug for primary agents.
apnea for prematurity 50% protein-bound
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– absence of Initially IV
respiratory effort in administered, then
newborn infants. orally.
Crosses placenta and
can be teratogenic to
pregnant women,
Best predictor of
toxicity is the blood
level of drug not the
signs and symptoms.

IMMUNOSUPPRESSIVE DRUGS

Drug Treatment for Therapeutic Level Toxic level Toxic effects Other information
Cyclosporine Used to prevent 300 ng/mL: >500 ng/mL Renal tubular, Marked affinity with
rejection of allogenic For heart, liver, and glomerular RBC.
organ transplant. pancreatic dysfunctions, GI Temperature
For suppression of disturbances, dependent.
acute graft-versus-host hirsutism, and Orally administered
disease (GVHD) hematologic dyscrasia with 5-50%
absorption
Specimen of choice:
whole blood.

Tacrolimus Same as cyclosporine Thrombus formation, A macrolide lactone

(Prograf/FK-506) (100x more powerful) nephrotoxicity and antibiotic.
neurotoxicity GIT uptake is variable.
Elevated levels
observed in cholestasis
Specimen of choice:
whole blood
Rapamycin Lipid abnormalities Same as tacrolimus
and thrombocytopenia
Mycophenolate Decreases renal
Mofetil allograft rejection
Leflunomide (LFM) Treatment for Inhibits lymphocyte
rheumatoid arthritis proliferation.
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ANTINEOPLASTIC DRUGS

Drug Treatment for Therapeutic Level Toxic level Toxic effects Other information
Methotrexate Effective therapy for a 0.01 umol/L Leukopenia, GI Inhibits DNA synthesis
variety of neoplastic ulceration, in all cells, by blocking
conditions. thrombocytopenia, dihydrofolate
Immunosuppressive cirrhosis reductase.
agent Leucovorin is used to
reverse the action of
methotrexate-
leucovorin rescue.
Busulfan Used to treat Overdose can cause Alkylating agent
leukemias and hepatic occlusive
lymphomas prior to disease
bone marrow
transplantation

ANTI-INFLAMMATORY/ANALGESICS

Drug Treatment for Therapeutic Level Toxic level Toxic effects Other information
Salicylates/Aspirin Commonly used Acute aspirin Direct stimulator of
(Acetylsalicylic Acid) analgesic, antipyretic intoxication-common respiratory system.
and anti-inflammatory cause of fatal drug Inhibitor of Krebs’
drug poisoning in children. Cycle.
Has anticoagulatory
Side effects: activity by inhibiting
GI disturbance, and the action of
interference with cyclooxygenase.
platelet aggregation. Decreases
thromboxane and
prostaglandin
Toxic effects: formation.
Mixed acid-base
disturbance,
hypoglycemia, and
Reye’s syndrome.
Acetaminophen Commonly used as 25 ug/mL >50 ug/mL Overdose of this drug Inhibitor of
(Tylenol) analgesic and may cause prostaglandin
antipyretic drug Hepatic necrosis: hepatotoxicity. metabolism.
100-300 ug/mL
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Toxic Effect:
Cyanosis due to
methemoglobinemia,
CNS depression and
seizure.
Ibuprofen Has analgesic and anti- 10-50 ug/mL >100 ug/mL Nausea, vomiting, Has lower risk of
inflammatory actions blurred vision, toxicities that
abdominal pain, salicylates and
edema acetaminophen

NEUROLEPTICS

Drug Treatment for Therapeutic Level Toxic level Toxic effects Other information
Antipsychotic Major Treatment for acute Cholestasis, orthostatic Blocks the action of
Tranquilizers schizophrenia hypotension, aplastic dopamine and
anemia, muscle serotonin in the limbic
rigidity. system.
Difficult to monitor in
serum due to
abundant metabolites.
Two classes:
Phenotiazines
(chlorpromazine) and
butyrophenones
(haloperidol)
TOXIC AGENTS
ALCOHOL

• Common CNS depressants

• Causes disorientation, euphoria, confusion and may progress to unconsciousness, paralysis and even death.
• Symptoms of intoxication begin when the concentration is >0.05%

ALCOHOL

Alcohol Important Information Symptoms of Intoxication Preferred Method Fetal Dose

Ethanol (Grain Alcohol) Most common abused drug. Blurred vision, Method for testing: Fetal dose:
CNS depressant incoordination, slurred enzymatic, gas-liquid 300-400 mL pure alcohol
Readily absorbed in GIT and speech, and coma; chromatography, and consumed in less than one
diffuses easily in tissue. “hangover symptoms” electrochemical oxidation hour.
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Ethanol abuse can cause

acidosis. Preferred method: Toxic blood level:
Antidote for chronic Enzymatic using alcohol >400 mg/dL
intoxication: DIAZEPAM. dehydrogenase reagent.
Specimen of choice: serum For hemodialysis:
(capillary and arterial >500 mg/dL
samples are preferred).
Major metabolic pathway:
conversion of
ethanol to acetaldehyde and
acetyl coenzyme
A by hepatic alcohol
dehydrogenase
Peak blood level: one hour
after intake.
Methanol (Wood Alcohol) Commonly used solvent and Frank blindness, and Screening test: 60-250 mL
contaminant of homemade metabolic acidosis Computation of osmolal gap
liquors. Toxic Blood Level:
Converted first to Preferred method: >50 mg/dL
formaldehyde, then finally GC-MS
to formic acid.
Isopropyl (Rubbing Rapidly absorbed in GIT. CNS depression and Gas chromatography 250 mL
Alcohol) Metabolized by hepatic hypertension
alcohol dehydrogenase into
acetone Indication of toxicity:
elevated levels of acetone in
the blood and urine
Ethylene Dlycol (1,2- It is common constituent of Metabolic acidosis, HPLC 100 g
ethanediol) hydraulic fluid and depressed reflexes, anuria,
antifreeze. and necrosis.
Converted to oxalic acid and
glycolic acid. Indication of toxicity:
Mode of treatment: inhibit deposition of calcium
the action of alcohol oxalate crystals in renal
dehydrogenase. tubules.
Major metabolite: glycolic
acid

CARBON MONOXIDE
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Carbon Monoxide Characteristics Function Major Toxic Effects Toxic Level Laboratory
Colorless, odorless, Binds with heme Diminish available 20% CO Sample: EDTA whole
tasteless gas. proteins. oxygen to the tissue or blood.
Produced by Has higher affinity for tissue hypoxia due to Definitive method for
incomplete hemoglobin than does inhibition of the testing: cooximetry
combustion of carbon- oxygen. oxyhemoglobin (carboxyhemoglobin
containing substances. Stimulates production saturation measurement).
Indication of acute of nitrous oxide
toxicity: “Cherry red” resulting to Susceptible organs:
color of face hypotension of brain and heart.
neurologic changes.

CYANIDE

Definition/Information Activity Toxic Effect Antidote Toxic Levels

Can exist as solid, gas, Binding to iron containing Inhibition of the electron Sodium thiosulfate, amyl, >2 ug/mL
liquid. substance like hemoglobin transport chain and cell and sodium nitrite
it is a super toxic substance. and cytochrome oxidase. death.
Component of insecticides Inhibits cellular respiration,
and rodenticides; common electron transport, and ATP Indicator of toxication:
suicidal agent. formation Odor of bitter almonds
It is also a pyrolysis breath and altered mental
product. statis.
Toxic symptoms:
tachypnea, convulsions, and
coma.

METALS

Metal Important Information Symptoms of Intoxication Preferred Method Fetal Dose

Arsenic Component of ant poisons, Toxic forms: Used of hairs and nails as Acute fetal dose:
rodenticides, paints, and Sodium arsenate, copper specimen is important in 120 mg-arsenic trioxides
metal alloys. arsenate, carbarsone, evaluation.
Common homicide and typarsamide, and arsenic Blood and urine for 30 ppm – arsenic gas
suicide agent. gas. assessment
Inhibits sulfhydryl enzymes.
Expresses toxicity by high Symptoms of intoxication: Method:
affinity binding to the thiol Hyperpigmentation,
groups. dryness of the mouth,
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difficulty in swallowing, Reinsch test, atomic

Antidote: British anti- anorexia, and bloody absorption
lewsite (BAL) diarrhea. spectrophotometry

Indication of toxicity: odor

of garlic breath and metallic
taste.

Toxic effects: intravascular

hemolysis,
hemoglobinemia,
nephrotoxicity and multi-
organ involvement.
Cadmium Utilized in electroplating Toxicity may result to
and galvanizing. destruction of type 1
Significant environmental epithelial cells in the lung
pollutant. and decreased resistance to
Poisoning result from bacterial infections.
ingestion. May accumulate in the renal
tubules causing tubular
damage.
Toxic renal indicator: (+)
GGT in urine.

Lead Potent enzyme inhibitor. Urinary aminolaevulinic Toxic dose:

Sources: paint and gasoline. acid, free RBC >0.5 mg/day
Mode of acquisition: proporphyrin, and presence Fetal dose:
ingestion/inhalation. of basophilic stippling in 0.5 g
Susceptible areas: central RBC CDC cutoff level for
and peripheral nervous children:
system. <10 ug/dL
Required chelation therapy Toxic blood level:
for children: <25 ug/dL >70 ug/dL – definitive lead
Lead chelators: EDTA and poisoning
dimercaptosuccinic acid
(DMA)
Mercury Binds with sulfhydryl Hypertension, tachycardia, Reinsch test Reference level:
proteins. and sweating – cardinal <10 ug/dL
Potent enzyme inhibitor. signs of pheochromocytoma Sample: whole blood and
Has ability to amalgamate. 24-hour urine Significant exposure:
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Mode of acquisition: or mimic that adrenal gland >50 ug/dL – whole blood
disorder.

General Toxic effects:

Organ dysfunction (lungs,
kidney, CNS)

Major toxic effect of

elemental mercury:
Pink disease (acrodynia)
and erethism

Alkyl mercury:
Congenital minimata
disease

DRUGS OF ABUSE

Drug Important Information Clinical use Toxic Effect

Amphetamines 3,4- Used for treatment of carcolepsy Sign of acute intoxication:
methylenedioxymethamphetamine and attentional deficit disorder. Hyperpyrexia
– ecstacy Increases mental alertness and Acute psychotic syndrome:
Structurally related to dopamine physical capacity and has anorectic Auditory and visual hallucination,
and serotonin. property. suicidal tendency, and paranoia.
Cause of false-positive reaction: Toxic Effect:
presence of antihistamine. Palpitation, hypertension, cardiac
arrythmias, convulsions,
pancytopenia, mental impairment,
and teeth grinding.
Anabolic Steroids Associated to male hormone Chronic hepatitis, atherosclerosis,
testosterone. abnormal platelet aggregation, and
Improves athletic performance by cardiomegaly.
increasing muscle mass
Cannabinoids Marijuana and hashish Paranoia, disorientation, altered
Tetrahydrocannabinol (THC) – physical senses, and
most potent component or bronchopulmonary disorders.
psychoactive substance of
marijuana. Psychologic effects:
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Reddening of the conjunctiva and

increased pulse rate
Cocaine (Crack) An alkaloid salt. Used as additive to foods. Can cause malformation in uterus.
Derived from coca plant. Used as local anesthetic for Can cause sudden death.
A potent CNS stimulant. nasopharyngeal surgery. Overdose of this drug may cause
Easily passes the placenta and violence.
mammary glands. Toxic Effect:
Treatment for cocaine addiction: Hypertension, arrythmias, seizures,
Benzodiazepine and myocardial infarction.
Urine metabolite: benzoylecgonine
Opiates Derived chemically from opium Capable of analgesia, sedation, and Major cause of drug-related death:
poppy. anesthesia darvon overdose combined with
Major metabolite of heroin: N- Codeine is an antitussive drug. alcohol.
acetylmorphine and morphine. Methadone is a non-bicyclic drug Withdrawal symptoms of heroine:
Antagonist for opiate overdose: that binds with morphine in the cold sweats, nightmares,
naloxene brain. hypothermia.
Fentanyl lollipop or patches are
more potent analgesics than
morphine. Toxic Effects:
Respiratory acidosis,
myoglobinuria, cardiopulmonary
failure, and papillary constriction.
Phencyclidine (Angel Dust or Can be inhaled or ingested. Depressant, stimulant, and has Tachycardia, seizure, and coma
Angel Hair) Major metabolite: phencyclidine hallucinogenic and anesthetic (eventually death)
HCl properties.
Psychologic effects: analgesic and
anesthesia.
Sedative Hypnotics Toxicity of this agent is initiated by Has therapeutic roles and they are Cheyne-stroke respiration,
ethanol. CNS depressant. depression, cyanosis, areflexia,
Major metabolite: secobarbital They are used also as potentiate the stupor, coma
(barbiturates) effects of heroine.
Barbiturate chemo adsorbent: Benzodiazepines used for
activated charcoal treatment of cocaine addiction.
Diazepam has a clinical use for
rapid control of acute seizure
activity; minor tranquilizer.
Lysergic Acid Diethylamide (LSD, One of the most potent A semisynthetic indolalkylamine, a Most common adverse reaction:
Lysergide) pharmacologic materials known. hallucinogen panic reaction – “bad trip”.
It produces effect at low doses -
Toxic Effects:
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Blurred or “undulating vision” and

synesthesia
Methaqualone (Quaalude) 2,3-disubstituted quinazoline. Has anesthetic, antihistamine, and Hypertonicity, hyperreflexia, and
It has sedative-hypnotic properties; antitussive properties. myoclonus
a hallucinogen.
Has the same toxicity as
barbiturates.
Chemoadsorbent: activated
charcoal
Piperazines Produced same “pleasant feeling” No available screening or Tachycardia, hypertension,
observed in amphetamines. confirmatory testing for hyperthermia, psychomotor
identification of these drugs. agitation and sore nasal and throat
passages.
Tryptamines Derivatives of serotonin, some are Tachycardia, hypertension,
present in plants. dystonia, seizures, rhabdomyolysis,
Example: N,N-dimethyltryptamine and paralysis.
(DMT) – short-term hallucinogen
“businessman’s lunch”.
Psilocycin is a component of “magic
mushrooms” (psilocybe); a
hallucinogen
Monoamine oxidase inhibitor (β −
carbolines)
enhances the hallucinogenic effect
of
tryptamines
Antagonist: benzodiazepines

Blood Alcohol Level Signs and Symptoms Strongly impaired motor skills
0.01-0.05 No obvious impairment Staggering/slurred speech
0.03-0.12 Mild euphoria 0.27-0.40 Unable to stand or walk
Low inhibitions Vomiting
Some impairment of motor skills. Impaired consciousness
0.09-0.25 Low inhibitions 0.36-0.50 Coma and possible death
Loss of critical judgement
Memory impairment
Diminished reaction time • Reg beer: 5%
0.18-0.30 Mental confusions • Malt liquor: 7%
Dizziness • Wine: 12%
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• Distilled spirits/hard (gin, rum, tequila, vodka, whisky, brandy,

etc.): 40%
• Alcopop/Cider: 4-7%
Unit Alcohol

• Wine: 76 mL
• Beer: 250 mL
• Hard: 25 mL
• Alcopop/Cider: 275 mL
• **no more than 14 units/week
• **distributed in three days/week

No. of drinks Daily Weekly Monthly

5 or more Very heavy Heavy Moderate
3-4 Heavy Moderate Light
2-3 Moderate Light Light
1-2 Moderate Light Light
<1 Light Light Light
None None drinker None drinker Non drinker