11.Somniferous drugs

Somniferous Drugs

• Definition: Drugs that reduce pain (analgesic) and induce sleep.

• Historical Significance:

  • Opium has been known to humans for centuries.

  • Ancient Greeks depicted gods of sleep, night, and death with the poppy symbol.

  • Morphine, derived from the Greek god of dreams, Morpheus.

  • Earliest written records date back to the 5th century B.C. The term "opium" originates from the Greek word "opos," meaning juice.

Opium

• Source: Dried juice of the poppy plant (Papaver somniferum).

• Cultivation: Predominantly grown in India, Afghanistan, and other Eastern countries.

  • Growth: The plant can reach heights of up to 1 meter.

  • Flowers: Colors include white, pink, or purple.

  • Capsules: Each plant bears 5 to 8 capsules, which are incised to collect the white juice.

• Process: The collected juice is dried to produce opium.

• Dry Poppy Capsules: Contain traces of opium.

• Poppy Seeds:

  • Harmless, nutritious, and edible.

  • Appearance: Small, kidney-shaped.

• Oil from Opium Seeds

  • Used for cooking.

  • Contains palmitic acid, stearic acid, oleic acid, and minerals.

• Characteristics of Dried Opium

  • Dark brown color, characteristic odor, and bitter taste.

  • Contains about 20 alkaloids including:

    • Morphine

    • Codeine

    • Thebaine (narcotics)

• Effects of Opium

  • Narcosis: Combined effect of hypnosis and analgesia.

  • Papaverine and narcotine (isoquinoline group) are mainly analgesics.

  • Noscapine acts as a muscle relaxant.

  • Opium has synthetic and semisynthetic derivatives.

  • Considered a drug of addiction and a substance of choice for suicide.

Alkaloid Groups in Opium

• 1. Phenanthrene Derivatives

  • Morphine, Codeine, Thebaine

  • Includes synthetic derivatives like heroin (brown sugar), dionine.

• 2. Benzyl Isoquinoline Derivatives

  • Papaverine, Narcotine

• These are classified as opiates.

• Non-opiate Analogs

  • Drugs with similar actions but not derived from opium:

    • Pethidine

    • Methadone

    • Pentazocine

    • Fentanyl

Pharmacological Action of Opiates

• Opiates act on receptor sites affecting various physiological responses:

  • Receptors Identified:

    • Mu: responsible for analgesia, euphoria, and respiratory depression.

    • Kappa: involved in psychotomimesis and dysphoria.

    • Delta: related to supraspinal analgesia.

• Mechanism of Action

  • Inhibit endorphins and activate receptor

    • Initially stimulate and then depress the CNS.

    • Synergistic effect with alcohol and barbiturates.

Acute Opium Poisoning

• Signs and Symptoms

  • Begin within half an hour of ingestion, 3-4 minutes after injection.

Stages of Poisoning:

1. Stage of Excitement

   • Euphoria, increased well-being, anxiety-free state.

   • Increased mental activity, nervousness, talkativeness, hallucinations.

   • Flushed face, possible maniacal condition.

2. Stage of Stupor/Depression

   • Headache, heaviness, giddiness, drowsiness.

   • Nausea, vomiting; progresses to stupor.

   • Pupils constricted, pulse, and respiration normal.

3. Stage of Coma

   • Deep coma, unresponsive; muscles flaccid, reflexes abolished.

   • Pupils constricted (pinpoint), may dilate later (premortal dilation).

   • Loss of secretions except sweating, skin cold and sweaty.

   • Increased sphincter tone (urinary retention), subnormal temperature, low blood pressure.

   • Slow, high-volume pulse; breathing reduced to 2-3 per minute.

   • Odor: Odor of opium may be present in the breath.

   • Respiratory Symptoms:

     • Irregular pulse.

     • Bradycardia.

     • Cheyne-Stokes type of breathing.

     • Cyanosis and pulmonary edema.

     • Death typically occurs due to respiratory failure.

Fatal Characteristics

• Fatal Dose:

  • Opium: 2gm.

  • Morphine: 200mg.

  • Codeine: 50mg.

• Fatal Period: 6 to 12 hours.

Differential Diagnosis

• Intracranial Hemorrhage:

  • Includes cerebrovascular accidents and brain trauma.

• Poisoning:

  • Alcohol.

  • Barbiturates.

  • Benzodiazepines.

  • Carbolic acid.

  • Carbon monoxide.

  • Organophosphates.

• Metabolic Conditions:

  • Diabetic and uremic.

• CNS Infections:

  • Meningitis.

  • Encephalitis.

  • Cerebral malaria.

• Others:

  • Epileptic and hysterical coma.

  • Heat hyperpyrexia.

Treatment for Opium Poisoning

1. Naloxone:

   • Acts as a physiological antidote.

   • Competes with opioids at receptor sites to reverse effects.

   • Initial dose: 2mg i.v., can repeat every 20-30 minutes up to 10mg total.

2. Airway Maintenance:

   • Endotracheal intubation if necessary.

3. Stomach Wash:

   • 1:5000 KMnO4 solution to oxidize opiates.

   • 100ml in stomach to neutralize secreted morphine.

4. Magnesium Sulphate:

   • 20 gm to keep bowel clear of opiates.

5. Activated Charcoal:

   • Administered as needed.

6. Symptomatic Treatment:

   • As per symptoms.

Postmortem Appearances

• Cyanosis of Face.

• Froth at mouth and nostrils.

• Postmortem Staining: May be black.

• Odor: Smell of opium present on viscera opening.

• Lungs: Congested and edematous.

• Brain: Congested and edematous.

• Stomach: Potential soft brownish lumps of opium present.

Marquis's Test for Detection

• Mixture: 3ml of concentrated sulphuric acid + 3 drops of formalin.

• Result: Purple-red color changes to violet and then blue, indicating presence of alkaloids like opium, opioids, cocaine, and phenethylamines.

Chronic Opium Poisoning (Morphinism)

• Tolerance Development: Can develop with chronic use.

• Addiction: Common in young adults, often perceived as an aphrodisiac.

• Daily Tolerance: Addicts can tolerate 3 to 6 gm per day.

• Physical Symptoms: Dry skin with needle puncture marks, sometimes masked by tattooing, and abscesses.

• Thrombosed veins may be seen in intravenous users (IV users) known as mainliners.

• Users may develop pigmentation and scars on the front of the elbow called "railroad tracks."

• Drug addicts might tattoo this area to conceal the scars.

• Chronic conditions include:

  • Constipation

  • Memory loss

  • Mental fatigue

  • Intellectual and moral deterioration

• Physical symptoms include:

  • Emaciation

  • Weakness

  • Anorexia

  • Constricted pupils

  • Impotence

  • Hallucinations

• Morphine addicts may experience:

  • Cirrhosis of the liver

  • Renal failure

• Intravenous users face risks such as HIV/AIDS due to needle sharing.

Withdrawal Syndrome (Abstinence Syndrome)

• Symptoms occur 18 to 24 hours after drug withdrawal:

  • Yawning, rhinorrhea, lacrimation, sweating, piloerection (goosebumps)

  • Dilated pupils

  • Restlessness and insomnia

  • Pain, alternating waves of heat and cold

• Symptoms worsen over time:

  • 36 hours: Increased restlessness, side-to-side movement

  • 48-72 hours: Severe symptoms, nausea, vomiting, abdominal cramps, diarrhea, fever

• Symptoms typically subside in 5 to 8 days.

Treatment of Withdrawal

• Treatment is more effective in hospitals and involves both medical and psychological measures:

  1. Gradual withdrawal of the drug.

  2. Methadone: 30 to 40 mg daily, gradually reduced.

  3. Diazepam for sleep at bedtime.

  4. Psychological counseling.

Heroin (Brown Sugar)

• Heroin is a semi-synthetic compound of opium, known on the street as Smack, Junk, Dope, or Horse.

• A combination of heroin and cocaine injected intravenously is called a "Speed-ball."

• It is the most dangerous and popular drug of addiction, being four times more toxic than morphine.

• Action: Heroin is metabolized to monoacetyl morphine and then hydrolysed to morphine.

• Routes of administration include:

  1. Mainliners: intravenous use

  2. Skin popping: subcutaneous injection

  3. Chasing the dragon: inhalation using heated aluminum foil

  4. Snorting

• Fatal Dose: 50 mg

• Fatal Period: 12 hours

Signs and Symptoms of Heroin Use

• Immediate effects post-intake include:

  • Excitement and euphoria lasting several minutes

  • Feelings of well-being and hallucinations

  • Followed by drowsiness and sedation.

• Overdose effects:

  • Leads to depression and stage of coma.

  • Constricted pupils.

  • Death occurs due to respiratory paralysis.

Treatment

• Naloxone is administered in cases of acute poisoning.

• Management follows protocols similar to that in morphine poisoning.

• Methadone is used to reduce euphoric effects in drug addicts and to prevent withdrawal symptoms.

Meperidine (Pethidine)

• Description:

  • Meperidine hydrochloride is an opioid.

  • Colorless, crystalline powder with a bitter taste.

  • Administered via intravenous (i.v.) or intramuscular (i.m.) routes for analgesic, antispasmodic, and sedative properties.

• Action:

  • Acts on the cerebral cortex to produce analgesia and sedation.

Methods of Use

• Chasing the Dragon:

  • Involves heating the drug on aluminum foil to smoke it.

Fatal Dosage and Symptoms

• Fatal Dose:

  • 2 grams.

• Fatal Period:

  • 24 hours.

• Signs and Symptoms:

  • Similar to morphine, but causes more dizziness and sedation.

  • Development of tolerance is possible.

  • Addicts may exhibit twitching, tremors, convulsions, dilated pupils, and hallucinations.

  • Withdrawal symptoms develop within 3 to 4 hours and peak by 8 to 12 hours.

Drug Addiction Concerns

• Meperidine is frequently associated with addiction, notably among doctors and nurses.

• Concurrent use with monoamine-oxidase inhibitors and phenothiazines can trigger severe reactions or even death.