DRUGS ACTING ON NERVOUS SYSTEM-PART III (BSc. NURSING)


 DRUGS ACTING ON NERVOUS SYSTEM

PREPARED BY MR. ABHIJIT DAS


ANAESTHETICS

Anaesthetics are substances used to induce a reversible loss of sensation, typically to prevent pain during medical procedures. There are two main types:

1.     General Anaesthetics: These induce a state of controlled unconsciousness and a lack of sensation over the entire body.

2.     Local Anaesthetics: These numb a specific part of the body, allowing a patient to remain conscious.

GENERAL ANAESTHETICS

STAGES OF ANAESTHESIA:

1.     Stage 1: Analgesia

·         Onset: Begins with the administration of the anaesthetic.

·         Symptoms: The patient starts to feel drowsy, experiences a reduction in pain perception, and may remain conscious.

2.     Stage 2: Excitement (Delirium)

·         Onset: Starts with the loss of consciousness.

·         Symptoms: The patient may exhibit irregular breathing, increased heart rate and increased blood pressure. This stage can be marked by agitation or delirium.

3.     Stage 3: Surgical Anaesthesia

·         Onset: Begins as the patient stabilizes into a regular pattern of breathing and relaxation.

·         Symptoms: This stage is characterized by the absence of reflexes, relaxed muscles, and adequate depth of anaesthesia for surgical procedures. Breathing is steady, and the patient's eyes may become fixed.

4.     Stage 4: Overdose

·         Onset: Begins if the anaesthetic depth is too great.

·         Symptoms: Characterized by severe depression of the central nervous system, including the respiratory and cardiovascular systems. This stage can lead to respiratory arrest, cardiovascular collapse, and can be fatal if not promptly corrected.

CLASSIFICATION OF GENERAL ANAESTHETICS:

§  Inhalational Anaesthetics:

1.     Gas: Nitrous Oxide

2.     Volatile Liquid: Isoflurane, Sevoflurane, Desflurane, Ether, Halothane

§  Intravenous (IV) Anaesthetics: Propofol, Thiopental, Etomidate, Ketamine, Midazolam

NITROUS OXIDE

MOA:

Nitrous oxide (N2O) works by entering the neuron and causing disturbances within the cell membrane. This process, known as membrane fluidization, alters the physical properties of the lipid bilayer of the neuron.

As a result, the ion channels embedded in the membrane, particularly those for sodium ions (Na+), are affected. The fluidization of the membrane prevents the normal influx of Na+ ions into the neuron, thereby inhibiting the generation and propagation of action potentials.

This disruption of neuronal signaling leads to a lack of sensation and contributes to the anaesthetic and analgesic effects of nitrous oxide.

ADVERSE EFFECTS:

1.     Respiratory depression

2.     Nausea and vomiting

3.     Hypotension

USES:

1.     Surgical procedures

2.     Sedation for medical procedures

3.     Management of acute pain

DOSE AND ROUTE:

Dose: For general anaesthesia: Usually administered in concentrations ranging from 50% to 70%, mixed with oxygen.

Route of Administration: Inhalation

CONTRAINDICATIONS:

1.     Pneumothorax: Nitrous oxide can expand trapped air, worsening the condition.

[NOTE: Pneumothorax is a medical condition characterized by the presence of air or gas in the pleural cavity, the space between the lung and the chest wall.]

2.     Middle ear blockage: Nitrous oxide can cause further pressure build-up in these areas.

[NOTE: Middle Ear Blockage occurs when the Eustachian tube, which connects the middle ear to the back of the nose and throat, becomes blocked or swollen.]

3.     Pregnancy: Nitrous oxide is contraindicated in the first trimester due to potential teratogenic effects.

ROLE OF NURSE:

1.     Assessing patients for suitability.

2.     Educating patients about the procedure.

3.     Preparing equipment and monitoring patients during administration.

4.     Assisting the healthcare team.

5.     Documenting the procedure and providing post-procedure care.

TECHNIQUES OF INHALATION OF ANAESTHETICS:

1.     Open Drop Method:

·         An older technique where the anaesthetic liquid is dropped onto a gauze or mask.

·         The patient inhales the vapors directly.

2.     Through Anaesthetic Machines:

·         Modern technique using specialized machines.

·         Machines precisely control and deliver a mix of anaesthetic gas and oxygen to the patient.

PRE-ANAESTHETIC MEDICATION:

Medications given before administering anaesthesia to enhance its effectiveness and manage potential side effects.

1.     Sedative/Antianxiety Drugs:

·         Examples: Diazepam, Midazolam

·         Purpose: Reduce anxiety and induce calmness.

2.     Opioids:

·         Examples: Morphine, Fentanyl

·         Purpose: Provide pain relief and sedation.

3.     Anticholinergics:

·         Examples: Atropine, Glycopyrrolate

·         Purpose: Reduce secretions and prevent bradycardia.

4.     Antiemetics:

·         Examples: Ondansetron, Metoclopramide

·         Purpose: Prevent nausea and vomiting.

LOCAL ANAESTHETICS

CLASSIFICATION:

1.     Injectable:

·         Examples: Lidocaine, Bupivacaine, Ropivacaine

2.     Surface:

·         Examples: Benzocaine, Lidocaine, Tetracaine

 

COMMON MOA:

Local anaesthetics block sodium (Na+) channels in the peripheral nervous system (PNS), preventing the transmission of nerve signals and thus blocking sensation.

ADVERSE EFFECTS:

1.     Allergic reactions

2.     Localized swelling or redness

USES:

1.     Minor surgeries

2.     Localized pain relief

ROLE OF NURSE:

1.     Preparation: Nurses ensure all necessary equipment and medications are available and properly set up for the procedure.

2.     Assessment: Nurses evaluate the patient's medical history, allergies, and current condition to determine the suitability for local anaesthetic administration. They also inspect the administration site for any signs of infection or contraindications.

3.     Education: Nurses provide clear and concise information to the patient about the procedure, potential side effects, and post-procedure care instructions.

4.     Assistance: Nurses aid the healthcare provider during local anaesthetic administration, assisting with patient positioning and providing support as required.

5.     Monitoring: Nurses closely monitor the patient's vital signs and response to the local anaesthetic, promptly identifying any signs of allergic reactions or adverse effects.

6.     Documentation: Nurses maintain accurate records of the local anaesthetic administration, documenting the type and dosage given, any adverse reactions observed, and the patient's response to the medication.


STIMULANTS

Stimulants are a class of drugs that stimulates the central nervous system, leading to heightened alertness, increased energy, and improved focus.

 

1. Psychomotor Stimulants

These drugs primarily increase motor activity, enhance alertness, and reduce fatigue by stimulating the central nervous system.


Classes of Psychoactive Drugs

1. Psychomotor Stimulants

These drugs primarily increase motor activity, enhance alertness, and reduce fatigue by stimulating the central nervous system.

a. Methylxanthines

  • Examples and Sources:
    • Caffeine
      • Source: Found in coffee beans, tea leaves, and cacao beans.
      • Description: Caffeine is the most widely consumed stimulant. It works by blocking adenosine receptors, preventing drowsiness, and increasing the release of dopamine and norepinephrine.
    • Theophylline
      • Source: Found in tea leaves (Camellia sinensis) and in small amounts in coffee.
      • Description: Theophylline is used medically to treat respiratory diseases such as asthma and chronic obstructive pulmonary disease (COPD). It relaxes bronchial smooth muscle and has a stimulating effect on the central nervous system.
    • Theobromine
      • Source: Found in cacao beans, making it a component of chocolate, as well as in tea leaves.
      • Description: Theobromine has a milder stimulating effect compared to caffeine and theophylline. It acts as a vasodilator, diuretic, and heart stimulant. It is also used therapeutically for its smooth muscle relaxant properties.

b. Nicotine

  • Example: Tobacco products (cigarettes, cigars, e-cigarettes)
  • Description: Nicotine stimulates nicotinic acetylcholine receptors, leading to increased release of dopamine and norepinephrine. It has a stimulating effect on the central nervous system and is highly addictive.

c. Cocaine

  • Example: Cocaine hydrochloride
  • Description: Cocaine inhibits the reuptake of dopamine, norepinephrine, and serotonin, leading to increased levels of these neurotransmitters in the brain. It produces intense euphoria, increased energy, and alertness but is highly addictive and neurotoxic.

d. Amphetamine

  • Example: Adderall (mixed amphetamine salts)
  • Description: Amphetamines increase the release of dopamine and norepinephrine and inhibit their reuptake, leading to heightened alertness, concentration, and energy. Used medically for ADHD. They have a high potential for abuse.

e. Methylphenidate

  • Example: Ritalin
  • Description: Similar to amphetamines, methylphenidate blocks the reuptake of dopamine and norepinephrine, enhancing focus and alertness. It is primarily used to treat ADHD and narcolepsy.

2. Hallucinogens

These drugs primarily alter perception, mood, and a variety of cognitive processes.

a. LSD (Lysergic Acid Diethylamide)

  • Example: LSD-25
  • Description: A potent hallucinogen that alters perception, thought, and mood. It acts primarily on serotonin receptors in the brain, particularly the 5-HT2A receptor, leading to profound changes in sensory perception and consciousness.

b. Tetrahydrocannabinol (THC)

  • Example: Marijuana (Cannabis)
  • Description: The primary psychoactive component of cannabis. THC acts on cannabinoid receptors in the brain, leading to altered sensory perceptions, mood changes, and cognitive impairments. It can produce euphoria, relaxation, and, in higher doses, hallucinations.

 

ETHYL ALCOHOL

PHARMACOLOGICAL ACTIONS

  • CNS Depressant: Ethanol depresses the central nervous system, leading to sedation, relaxation, and, in higher doses, anesthesia.
  • GABA Modulation: Enhances the inhibitory effects of GABA (gamma-aminobutyric acid) in the brain.
  • Dopamine Release: Increases dopamine release, contributing to its rewarding and reinforcing effects.
  • Cardiovascular Effects: Causes vasodilation, leading to a feeling of warmth and, in higher doses, hypotension.
  • Metabolic Effects: Can lead to hypoglycemia and has caloric content, providing a source of energy.

Adverse Effects

  • Acute Effects: Drowsiness, impaired coordination, slurred speech, nausea, vomiting, and hangover.
  • Chronic Effects: Liver disease (cirrhosis), cardiovascular disease, neuropathy, cognitive impairment, gastrointestinal issues.
  • Psychological Effects: Dependence, withdrawal symptoms, mood disorders, and increased risk of depression and anxiety.

 

METHYL ALCOHOL POISONING

DRUGS USED FOR METHANOL POISONING:

1. Fomepizole

  • Mechanism of Action: Fomepizole is an inhibitor of alcohol dehydrogenase, the enzyme responsible for metabolizing methanol into its toxic metabolites, formaldehyde and formic acid.

2. Ethanol

Mechanism of Action: Ethanol competes with methanol for alcohol dehydrogenase, reducing the formation of toxic metabolites

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