ALCOHOL
ALCOHOL is a CNS depressant drug.
When unqualified, alcohol refers to Ethyl alcohol/ Ethanol. Methanol is used as an industrial solvent and to adulterate ethanol
in order to make it unfit to drink. Ethylene glycol is a constituent of antifreeze formulation for car radiators.
Pharmacology of alcohol is important for its presence in beverages, alcoholism and for alcohol intoxication, rather than as a
medicinal substance.
Major source of commercial alcohol is mollases.
ABSOLUTE ALCOHOL: 99% (w/w) ethyl alcohol
RECTIFIED SPIRIT: 90% (w/w) ethyl alcohol
DENATURED ALCOHOL: Ethanol, to which some substances (methanol, aniline dyes etc.) are added.
PHARMACOLOGICAL ACTIONs
PLASMA EFFECT
CONCENTRATION
(mg/dL)
Apparent excitation, euphoria, self-criticism, altered mood & feelings,
30-60 allayed anxiety
⁓ 80 Slurred speech, incoordination, unsteady gait, impaired attention
CNS
80-200 More intense mood lability and greater cognitive deficits, potentially
accompanied by aggressiveness, and blackout, ataxia, mental clouding,
disorganization of thought
Nystagmus, stupor, sedation
>200
≥ 300 Failing vital signs, coma & death
Small doses Cutaneous (on face) vasodilatation
Moderate doses Tachycardia & mild rise in BP (d/t increased muscular activity and
sympathetic stimulation)
CVS
Large doses Fall in BP (d/t direct myocardial as well as vasomotor centre depression)
BLOOD < 30 gm Ethanol (roughly equivalent to 50-100 mL of whiskey) consumption/day without episodes of
heavy drinking has been found to raise HDL level & decrease LDL oxidation and this may be
responsible for lower risk for Coronary artey disease.
Megaloblastic anaemia may occur in chronic alcoholics (d/t interference of folate metabolism)
Hypoglycaemia (as it inhibits gluconeogenesis)
LIVER Fatty liver (because it mobilizes peripheral fat and increases fat synthesis in liver)
Cirrhosis (d/t 1. hepatocyte damage & resulting inflammation, 2. increased oxidative stress &
resulting cellular necrosis f/d fibrosis, 3. increased lipid peroxidation & glutathione depletion and
finally when these factors are combined with vitamin and nutritional deficiencies, may result in
cirrhosis)
KIDNEY Diuresis (d/t water ingested along with drinks as well as alcohol induced inhibition of ADH secretion)
SEXUAL Increases libido but (often) deteriorates performance [alcohol is APHRODISIAC]
Chronic alcoholism can produce impotence, testicular atrophy, gynaecomastia and infertility
FUNCTION
ASTRINGENT (precipitates surface proteins and hardens the skin when applied to surface)
LOCAL ANTISEPTIC (as it precipitates bacterial proteins)
ACTIONS RUBEFACIENT (topical application causes redness of skin)
COUNTERIRRITANT
METABOLISM (in LIVER)
ETHANOL METHANOL
ALCOHOL DEHYDROGENASE
(ADH)
ACETALDEHYDE FOMEPIZOLE FORMALDEHYDE
ALDEHYDE DEHYDROGENASE
(ALDH)
ACETIC ACID DISULFIRAM FORMIC ACID
ACETYL CoA CO2 + H2O
(utilized in TCA cycle, supports fatty acid synthesis and
the storage and accumulation of
triacylglycerides, ketone bodies)
❖ Alcohol follows ZERO-ORDER KINETICS.
❖ FORMIC ACID is responsible for most of the toxic manifestations.
MECHANISM OF ACTION THERAPEUTIC USES of ETHANOL
1. Enhance GABAA receptor mediated Cl- 1. ANTISEPTIC: 70% Ethyl alcohol is used as Antiseptic on skin (before
channel opening giving injections/ before surgical procedures etc.)
2. Inhibits NMDA receptors-operated
cation channels 2. METHANOL POISONING or ETHYLENE GLYCOL POISONING:
Ethyl Alcohol is used (Ethanol is preferentially metabolized by alcohol
Both mechanisms finally result in dehydrogenase over methanol, so it saturates alcohol dehydrogenase
hyperpolarization. and prevents conversion of Methanol to Formic acid, which is highly
toxic)
3. For prevention of BED SORES: Because of its astringent action
(making the skin hard), it prevents the damage against bony points in
bed-ridden patients
4. For sprain, joint pain (as Alcohol is rubefacient & counterirritant)
ACUTE ALCOHOL INTOXICATION
CLINICAL FEATURES MANAGEMENT
Unawareness, unresponsiveness, 1. Keep the patient in a quiet, dark room; protect the eyes from light
stupor, hypotension, gastritis, 2. If patient is disoriented/ comatose: Maintain Airway (endotracheal
hypoglycaemia, respiratory intubation and positive pressure respiration may be needed),
depression, collapse, coma and death.
Breathing, Circulation if necessary (Fluid & Electrolytes balance)
3. Gastric lavage [helpful only when the patient is brought within 2 hours
of ingesting alcohol]
4. Intravenous GLUCOSE [to correct hypoglycaemia]. Thiamine (100 mg
in 500 ml glucose solution infused IV) should be added.
5. HEMODIALYSIS [hasten recovery]
6. IV NaHCO3 [to correct acidosis], if necessary
7. FOMEPIZOLE (A loading dose of 15 mg/kg infused IV over 30 min is
followed by 10 mg/kg every 12 hours till serum methanol falls below 20
mg/ dL) is Drug of choice (for any type of alcohol poisoning)
8. In case Methanol poisoning/ Ethylene glycol poisoning: Ethanol
(10%} in water (via nasogastric tube) can be used. Calcium leucovorin
has been shown to reduce blood formate levels by enhancing its
oxidation.
CHRONIC ALCOHOLISM
1. Impaired mental and physical performance
2. Polyneuritis, pellagra, seizures
3. Wernicke's encephalopathy
4. Korsakoff's psychosis
5. Megaloblastic anaemia
6. Alcoholic cirrhosis of liver
7. Hypertension, Cardiomyopathy, CHF, arrhythmias, stroke
8. Impotence, gynaecomastia, infertility
9. Skeletal myopathy
ALCOHOL ALCOHOL ALCOHOL ALCOHOL CRAVING
DEPENDENCE WITHDRAWAL TOLERANCE
/ ABSTINENCE
SYNDROME
1. Development of Adverse reactions to abrupt After repeated Increase in alcohol seeking
TOLERANCE discontinuation of Alcohol. (continuous & behaviour (persistent desire
2. Alcohol CRAVING Severity depends upon amount prolonged) to use Alcohol)
3. Distressful & duration of consumption of administration, a
WITHDRAWAL Alcohol. given dose of
SYNDROME after alcohol produces
cessation of Alcohol Seizure, sleep disturbances, a decreased
4. Considerable time spent Tachycardia, High BP, Irritation, effect than
for obtaining Alcohol anxiety. expected &
5. Continued use despite larger dose is
health/ social/economic/ needed to obtain
family/ legal problems same previous
effect.
It may be psychological/ physical.
ALCOHOL & PREGNANCY
FETAL ALCOHOL SYNDROME:
1. Dysmorphic facial features (small palpebral fissures, thin vermilion border, smooth filtrum)
2. Prenatal and/or postnatal growth impairment
3. CNS abnormalities (neurological, head size< 10th percentile, global cognitive/ intellectual deficits)
FEW VIVA QUESTIONS
1. BREATH ANALYSER is used to indirectly measure approximate blood concentration of Alcohol: HOW?
The amount present in exhaled air can be measured indirectly to detect the blood concentration (35 µg/100 ml in exhaled air =
80 mg/100 ml in blood).
Permitted level for vehicle driving is < 80 mg/100ml and more than this level is considered ‘under the influence of Alcohol’.
2. Which drugs are used in detoxification of chronic alcohol dependence?
Which drugs are used in alcohol dependency syndrome?
Which drugs are used in alcohol withdrawal during maintenance phase?
Which drugs are used in alcohol dependence to prevent relapse?
Which drugs are used to maintain abstinence in alcohol dependence?
All answers are same.
1. NALTREXONE (Drug of choice)
2. ACAMPROSATE (NMDA receptor antagonist)
3. DISULFIRAM
4. ONDANSETRON
5. TOPIRAMATE
3. NALMEFENE
4. Which drugs are used in alcohol withdrawal syndromes?
(IV) DIAZEPAM/ LORAZEPAM (for withdrawal seizure)
(Oral) CHLORDIAZEPOXIDE (for other conditions after withdrawal)
5. What do you mean by ALCOHOL AVERSION THERAPY?
To render alcohol consumption unpleasant is known as ALCOHOL AVERSION THERAPY. DISULFIRAM is used for aversion
therapy.
(After making sure that the subject has not taken alcohol in the past 12 hours, disulfiram is given and advised not to take
alcohol)
6. What do you mean by ‘DISULFIRAM-LIKE REACTION’?
Disulfiram (ANTABUSE) causes irreversible inhibition of Aldehyde dehydrogenase resulting in accumulation of Acetaldehyde in
tissues & blood.
Patient on Disulfiram after consuming alcohol develops distressing symptoms (hot flushed face, throbbing and pulsatile
headache, nausea, vomiting, chest pain, postural fainting etc.) d/t acetaldehyde.
This is known as DISULFIRAM-LIKE REACTION.
7. Enumerate other drugs which cause ‘DISULFIRAM-LIKE REACTION’?
a) Metronidazole
b) Chlorpropamide
c) Griseofulvin
d) Cefoperazone
8. What is DELIRIUM TREMENS?
After 2 days or more after alcohol withdrawal (last dose) hallucination, delusion, fever, tachycardia etc. may occur. This is
known as DELIRIUM TREMENS.
9. The concentration achieved is higher in women than men after consuming the same amount of alcohol;
WHY?
Because, women have (compared to men):
a) Smaller body weight
b) Less body water
c) Less alcohol dehydrogenase
