Sedative And Hypnotics Question And Answers

B Pharmacy Important Questions Sedative And Hypnotics Important Notes

1. Sedative And Hypnotics Classification of barbiturates

• Long-acting
  • Phenobarbitone
  • Mephobarbitone
• Short-acting
  • Pentobarbitone
  • Secobarbitone
  • Butobarbitone
• Ultra short-acting
  • Thiopentone
  • Hexobarbitone
  • Methohexitone

Read And Learn More: Pharmacology Question and Answers

2. Classification of sedatives and hypnotics Newer benzodiazepine hypnotics

3. Sedative And Hypnotics Benzodiazepines

• They have a high therapeutic index
• Causes less distortion of sleep
• Do not alter the disposition of other drugs
• Lowers abuse liability
• Withdrawal symptoms are less marked
• Do not affect respiration or cardiovascular functions

4. Sedative And Hypnotics Thiopentone sodium

• It is ultra short-acting
• When injected 4 as 2.5% solution, it produces unconsciousness in 15-20 sec
• Its undissociated form has high lipid solubility and enters the brain almost instantly

B Pharmacy Important Questions Sedative And Hypnotics Long Essays

Question 1. Classify hypnotics. Mention the mechanism, actions, and management of barbiturates.

Answer:

Hypnotics Classification:

1. Hypnotics Barbiturates.

• Long-acting – Phenobarbitone
• Short-acting – Pentobarbitone.
• Ultrashort acting – Thiopentone sodium.

2. Hypnotics Benzodiazepine.

3. Hypnotics Newer hypnotics.

• • Zopiclone, Zolpidem, Zaleplon.

Newer hypnotics Barbiturates:

• Barbiturates are drugs derived from barbituric acid. They are non-selective CNS depressants

Barbiturates Mechanism of Action:

Barbiturate
↓
Bind of GABAa receptor Cl- Channel complex.
↓
Potentiate GABAergic inhibition.
↓
Duration of Cl- channel kept open increases
↓
Increased chloride conductance.
↓
Membrane hyperpolarization.
↓
CNS depression.

Barbiturates Actions:

1. Barbiturates CNS.

• In hypnotic doses, barbiturates induce sleep and prolong the duration of sleep.
• Sedative doses given during the daytime can produce drowsiness, reduction in anxiety, and excitability.
• Barbiturates have anticonvulsant property.
• At higher doses, it produces general anesthesia.

2. Barbiturates Respiration.

• Depresses respiration.

3. Barbiturates CVS.

• Produces a slight decrease in BP and heart rate.

4. Barbiturates Skeletal muscles.

• Depress the excitability of the neuromuscular junction.

5. Barbiturates Kidney.

• The tone and motility of the bowel are decreased.
• Reduces urine flow

Barbiturate poisoning:

• The dosage of barbiturates above 6 -10 g causes acute barbiturate poisoning.

Barbiturate poisoning Management:

• Maintain airway, BP, adequate ventilation, and oxygen administration.
• Maintain blood volume by fluid infusion.
• Use of vasopressor.
• Gastric lavage.
• Hemodialysis is done in severe cases.
• Forced alkaline diuresis with mannitol, frusemide, or sodium bicarbonate is done.

Question 2. Describe the Barbiturate’s uses and adverse effects.

Answer:

Barbiturates:

Barbiturates Uses:

• As pre-anesthetic medication.
• As sedative and hypnotic.
• Thiopentone is used for induction of general anesthesia.
• Phenobarbitone is used in epilepsy.
• Used in the treatment of congenital non-hemolytic jaundice.
• Occasionally employed as an adjuvant in psychosomatic disorders.

Barbiturates Adverse Effects:

1. CNS effects.

• Hangover, mental confusion, impaired performed traffic accidents, distortions of mood.

2. Respiratory.

• Respiratory depression occurs.

3. Hypersensitivity.

• Skin rashes and swelling of the eyelids and lips occur.

4. Tolerance and dependence develop.

5. Withdrawal symptoms.

• Anxiety, restlessness, abdominal cramps, hallucinations, delirium, and convulsions occur.

6. Idiosyncrasy.

7. Megaloblastic anemia – due to prolong used of phenobarbitone.

Question 3. Classify barbiturates. Discuss thiopentone sodium.

Answer:

Barbiturates Classification:

1. Long-acting:

• Phenobarbitone, mephobarbitone.

2. Short-acting.

• Pentobarbitone, butobarbitone.

3. Ultra-short acting.

• Thiopentone, Hexobarbltone, Methohexltone.

Thiopentone sodium:

• Thiopentone sodium is ultra short-acting thiobarblturate

Thiopentone sodium Onset of Action:

• 15-20 sec.

Thiopentone sodium Duration of Action:

• 4 – 7 min.

Thiopentone sodium Properties:

• Highly soluble in water.
• Produces unconsciousness in 15 – 20 s.
• Produces CNS depression.
• Poor analgesic.
• Weak muscle relaxant.
• Causes respiratory depression.
• Highly lipid soluble.
• Prepared freshly before use.
• Extravasation of solution causes Intense pain, necrosis, and gangrene.

Thiopentone sodium Uses:

• Common inducing agent
• Used for short non-painful operations.
• Used to control convulsions.
• Adverse effects:
• Laryngospasm.
• Shivering.
• Deliriums

Thiopentone sodium Dose:

• Injected IV dosage – 3 – 5 mg/kg as 2 – 5% solution.

Question 4. Discuss the mechanism, actions, uses, and adverse effects of benzodiazepines.

Answer:

Benzodiazepines:

• Benzodiazepines are a group of drugs used for sedatives and hypnotics.

Benzodiazepines Mechanism of Action:

Benzodiazepines bind to the specific site on GABAa – BZD
receptors Cl- Channel complex.
↓
This potentiates the inhibitory effect of GABA.
↓
Leads to an increase in the frequency of opening of Cl Channels.
↓
Increased Cl- conductance.
↓
Membrane hyperpolarization.
↓
CNS depression.

Benzodiazepines Actions:

1. CNS actions.

• Hypnosis – increases the duration of sleep.
• Anxiolytic – reduces anxiety.
• Causes CNS depression.
• Anticonvulsant – increases the seizure threshold.
• Amnesia – produces loss of memory for the events happening after drug administration.

2. Skeletal muscle.

• Reduces muscle tone.

3. CVS action.

• At high doses, it decreases BP and heart rate.

4. GIT.

• Decreases gastric acid secretion.

5. Respiration.

• At high doses, causes respiratory depression.

Benzodiazepines Uses:

• As hypnotic – to treat insomnia.
• As anxiolytic – to reduce anxiety.
• As anticonvulsant – 4 diazepam is used.
• As a centrally-acting muscle relaxant
• As pre-anesthetic medication.
• IV midazolam or diazepam is used as an intravenous anesthetic.
• For minor procedures.
• For initial control of mania.
• During alcohol withdrawal.
• Along with analgesics, NSAIDs, spasmolytics, antiulcer, and many other drugs.

Benzodiazepines Adverse effects:

• Benzodiazepines are well-tolerated drugs.
• Common side effects are.
  • Drowsiness, dizziness, vertigo, ataxia, amnesia.
  • The blurring of vision.
  • Dry mouth, sweating.
  • Headache, daytime sedation.
  • Tolerance and dependence.
  • Drug given during labor causes hypotonia and respiratory depression in new-born.

Question 5. Define sedative hypnotics classify. What are the advantages of benzodiazepines over barbiturates as sedative-hypnotics?

Answer:

Definition:

Sedative:

A sedative is a drug that reduces excitement and calms the subject without inducing sleep.

Hypnotics:

Hypnotic is a drug that induces and/or maintains sleep similar to normal sleep.

Advantages of Benzodiazepine over barbiturates:

• Benzodiazepine has a high therapeutic index.
• It induces sleep similar to natural sleep.
• Hypnotic doses do not affect respiration or cardiovascular functions.
• BZDs have practically no action on another body system.
• Causes less distortion of sleep architecture.
• Do not cause microsomal enzyme induction.
• Do not alter the blood level of other drugs.
• Have low abuse liability.
• Tolerance is mild.
• Psychological and physical dependence is less marked.
• Specific BZD antagonist flumazenil is present to use in the cause of poisoning.
• The rebound phenomenon is less marked.

Sedative And Hypnotics Short Essays

Question 1. Classify barbiturates. Write it dose.

Answer:

Barbiturates:

• Barbiturates are non-selective CNS depressants.

Barbiturates Classification:

1. Long-acting.

• Phenobarbitone, mephobarbitone.

2. Short acting.

• Pentobarbitone, secobarbitone, Butobarbitone.

3. Ultra-short acting.

• Thiopentone, methohexitone, and hexobarbitone.

Barbiturates Dose:

• The dose depends on lipid solubility.
• Higher lipid solubility indicates a lower dose.

Barbituratesv Examples:

Question 2. Uses of benzodiazepines (BZDs).

Answer:

Benzodiazepines Uses:

1. As hypnotics

• BZDs are used to treat insomnia.
• They shorten sleep latency and reduce nocturnal awakening.
• In dentistry, it is used to ensure sleep the night before the dental procedure in an apprehensive patient.

2. As anxiolytics and for daytime sedation.

• Reduces anxiety.
• Produces calming effects.

3. As an anticonvulsant

• Increases seizure threshold.
• Used especially in emergency control of status epileptic- cities, febrile convulsions, tetanus, etc

4. Muscle relaxant

• BZDs reduce muscle tone by centrally acting.
• Reduces muscle tone and aches associated with anxiety.

5. As IV anesthesia.

• BZDs induce, maintain and supplement anesthetic

6. As pre-anesthetic medication.

• Used due to its sedative and anxiolytic effects.

7. During alcohol withdrawal

• Reduces the intensity of withdrawal symptoms.
• an In minor procedures like endoscopies, fracture reduction, and cardiac catheterization.

9. In psychiatry.

• For initial control of mania.

Question 3. Barbiturate poisoning.

Answer:

Barbiturate poisoning:

• The dosage of barbiturates above 6 – 10 g causes acute barbiturate poisoning.

Barbiturate poisoning Manifestations:

• Excessive CNS depression.
• Respiration depression with slow and shallow breathing.
• Hypotension.
• Bullous eruptions.
• Cardiovascular collapse.
• Renal shutdown.
• Pulmonary complications.

Question 4. Benzodiazepine as pre-anesthetic medication.

Answer:

Benzodiazepine is used for pre-anesthetic medication because it

• Reduces anxiety.
• Produces sedation.
• Produces amnesia.
• Relieves post-operative pain.
• Make anesthesia safer.
• Sraoothens induction with little respiratory depression.
• Reduces side effects of anesthesia like gastric acidity.
• Diazepam 5 -10 mg is given orally.

Sedative And Hypnotics Short Answers

Question 1. Flumazenil.

Answer:

Flumazenil is benzodiazepine antagonist

• It rarely is a benzodiazepine antagonist
• It rarely induces seizures.
• Its action starts seconds after IV administration and lasts for 1 – 2 hours.

Flumazenil Mechanism:

• It competes with BZD agonists and reverses depressant effects.
• Competes with inverse agonists for BZD receptor and reverses stimulant effects.
• It abolishes the hypnogenic, psychomotor, cognitive, and EEC effects of BZD.

Flumazenil Uses:

• To reverse actions of BZD.
• In benzodiazepine overdosage or poisoning.

Question 2. Define sedatives, hypnotics, and tranquilizers.

Answer:

Sedative:

A sedative is a drug that reduces excitement and calms the subject without inducing sleep.

Hypnotics:

Hypnotic is a drug that induces and/or maintains sleep similar to normal sleep.

Tranquilizer:

• It is an old term.
• It means a drug that reduces mental tension and produces calmness without inducing sleep or depressing mental faculties.

Question 3. Urine should be alkalized in acute barbiturate poisoning? Why?

Answer:

The dosage of barbiturates above 6 -10 g causes acute barbiturate poisoning.

• There is no specific antidote for it, only an alkaline diet- sis is the main treatment for it.
• It is done with mannitol, sodium bicarbonate, and frusemide.
• Barbiturates are weakly acidic drugs.
• But in alkaline urine, they exist in ionized form.
• Thus, they are not reabsorbed while passing through renal tubules.
• As a result, they are rapidly excreted in the urine.

Question 4. Midazolam

Answer:

• It is an ultra-short-acting benzodiazepine
• Duration of action is < 6 hours
• Dose: 7.5-10 mg
• It is used as IV anesthesia because
  • It is faster
  • Short-acting
  • More potent
  • Does not cause respiratory and CVS depression
  • Does not cause pain or irritation at the injection site
  • Used as an adjuvant to general anesthesia