CNS

CNS
Q. Write down the mechanism of action of Diazepam?

The BZ receptors form part of a GABAA receptor-chloride ion channel macromolecular
complex, a pentameric structure assembled from 5 subunits each with 4 transmembrane
domains. A major isoform of the GABAA receptor consists of 2 α1, 2 β2, and 1 γ2 subunits.
In this isoform, the binding site for benzodiazepines is between α1 and the γ2 subunit.
However, benzodiazepines also bind to other GABAA receptor isoforms that contain α2,
α3, and α5 subunits. Binding of benzodiazepines facilitates the inhibitory actions of GABA,
which are exerted through increased chloride ion conductance. Benzodiazepines increase
the frequency of GABA-mediated chloride ion channel opening.
Q. Enlist any SIX clinical uses of Benzodiazepines and Barbiturates with one
example of each use.
1. Anxiety (Diazepam, Alprazolam, Lorazepam)
2. Insomnia (Diazepam, Triazolam, Midazolam, Clonazepam, Flurazepam, Secobarbital)
3. Epilepsy (Diazepam, Clonazepam, Phenobarbital)
4. Anesthesia (Thiopental)
5. Muscle relaxation (Diazepam)
6. Neonatal Jaundice (Phenobarbitone)
7. Control of alcohol or other sedative hypnotic withdrawal states (Diazepam,
Chlordiazepoxide)
8. Bipolar disorder (Clonazepam)
9. Delirium tremens (Lorazepam)
Q. Write a note on Buspirone.

Selective anxiolytic. 5-HT1A partial agonist. Has a slow onset of action (>1 week). Used in
generalized anxiety disorder (less effective in panic disorders). Safe in pregnancy.
Minimal CNS depressant effects. Does not affect driving skills. No anticonvulsant or muscle
relaxant properties. Tolerance development is minimal with chronic use. Little rebound
anxiety or withdrawal symptoms on discontinuance. Side effects include tachycardia,
paresthesias, pupillary constriction, and gastrointestinal distress. Buspirone has minimal
abuse liability.
Q. A 30-year-old female is brought to emergency with convulsions. She was

immediately given I/V injection of Diazepam. Enumerate other indications of this
drug.
1. Reduction of anxiety
2. Induction of sleep
3. Reduction of muscle tone or spasm
4. In anesthetic medication
5. Acute alcohol with-drawl
Q. Define MAC.
The alveolar concentration required to eliminate the response to a standardized painful

stimulus in 50% of patients.
Q. Enlist clinical uses of Ketamine.
1. Short surgical procedures especially in children and young adults --- burn dressing,
forceps.
2. delivery, breech extraction manual removal of placenta and dentistry.
3. Post-operative pain management.
4. As a sedative for painful procedures.
5. Used in asthmatic patients as it causes bronchodilation.
6. OPD surgical procedures.
7. To supplement spinal/epidural anesthesia.
8. Combination with diazepam---- angiography, cardiac catheterization.
Q. A 25-year-old patient was anaesthetized with Nitrous oxide and Halothane to

undergo abdominal surgery. Give three comparative features of Halothane and
Nitrous oxide.
Halothane Nitrous oxide

• Potent anesthetic agent having low • Less potent anesthetic agent having
MAC value. high MAC value.
• It is highly soluble in blood having • It has low solubility in blood having
high blood gas partition-coefficient. low blood gas partition-coefficient.
• It has slow induction rate as • It has fast induction and fast
compared to nitrous oxide. recovery rate.
• It has no analgesic property. • It provides good analgesic effect.
• Halothane sensitizes the heart to • Nitrous oxide does not sensitize the
the effect of catecholamines and heart to the effect of
may cause arrhythmias. catecholamines.
• Post-operative hepatitis and • Megaloblastic anemia and diffusion
malignant hyperthermia are hypoxia are side effects of nitrous
important side effects of halothane. oxide.
Q. Enlist two advantages of Ketamine as general anesthetics.

1. Provides analgesic effect.
2. Provides amnesia and sedation.
3. Potent bronchodilator, useful in asthmatic patients.
4. Mainly used in children and adults for short surgical procedures.
Q. Explain the relationship among tissue pH, drug pKa, and the rate of onset of
local anesthetic action.
pKa is pH at which 50% of drug is ionized.
LA’s more than 50% exists in the lipid soluble nonionized form. Only the non-ionized form
crosses into the nerve cell usually at range 7.4 -8.5.
Decrease in pH shifts equilibrium toward the ionized form, delay in the onset of action.
Lower pH, solution more acidic, gives slower onset of action.
Presence of Pus and inflammation will retard the action of LA. (probably low acidic pH)
therefore,
•LA are more ionized - don’t penetrate very well
•Blood flow is also increased
So, decreased ability of LA to produce effects
Q. List FOUR factors that determine the susceptibility of nerve fibers to local
anesthetic blockade.
Fiber diameter
Myelination
Physiologic firing rate

Anatomic location
Q. Enlist the clinical uses of Succinylcholine.

1. Adjuvants to general anesthetics
2. For endotracheal intubation
3. Control of ventilation in critical ill patients with ventilator failures
4. Short term procedures
5. Status epilepticus
6. Prevention of convulsions and trauma from electroconvulsive therapy (ECT)
Q. What are the major opioid receptors and their proposed action?
Three major opioid receptor subtypes have been extensively characterized pharmacologically: μ, δ,
and κ receptors.
• The μ-receptor activation plays a role in analgesic action, respiratory depressant actions of opioids
and slows gastrointestinal transit.
• κ-receptor activation also appears to be involved in analgesic and sedative actions. Slows
gastrointestinal transit.
• δ-receptor activation may play a role in analgesic action and the development of tolerance.
Q. Write down the symptoms of overdose of opioids, also write down its treatment.
A triad of pupillary constriction, comatose state, and respiratory depression is characteristic; the
latter is responsible for most fatalities.
• Treatment of overdose involves the use of opioid antagonists such as naloxone and other
therapeutic measures, especially ventilatory support.
Q. A 36-year-old woman presented with symptoms of major depression and was

prescribed Sertraline. Write down its mechanism of action.
Sertraline is an anti-depressant of Selective Serotonin Reuptake inhibitors class. They inhibit CNS
neuronal uptake of serotonin and increases the amounts of serotonin in the body.
Q. Explain the following terms:

Wine and Cheese Reaction:
Fatal interaction with tyramine containing foods. Tyramine itself is an indirectly acting catecholamine
that increases release of catecholamines. It is normally broken down by monoamine oxidase. MAOIs
increases tyramine in the body resulting in increased levels of Nor Epinephrine in circulation leading
to hypertensive crisis, intracranial damage and other organ damage.
Serotonin Syndrome:
MAOIs ingested in overdose or MAOIs are combined with SSRIs results in Serotonin Syndrome
leading to hyperthermia, muscle rigidity, myoclonus, rapid changes in mental status and vital signs.
Serotonin syndrome is treated by sedation(benzodiazepines), paralysis, intubation and ventilation,
cyproheptadine/chlorpromazine.
Q. Enumerate therapeutic uses of Opioids.

1. Analgesia
2. Cough Suppression
3. Treatment of Diarrhea
4. Management of Acute Pulmonary Edema
5. Anesthesia
6. Opioid Dependence
Q. What are the autonomic adverse effects of antipsychotic drugs.

1. Loss of accommodation
2. Dry mouth
3. Difficulty urinating
4. Constipation
5. Orthostatic hypotension
6. Impotence
7. Failure to ejaculate
Q. Write down the differences between typical and atypical antipsychotics.
Q. Enlist the adverse effects of antipsychotics on ANS, CNS and Endocrine system. Also
mention the mechanisms of these adverse effects.
Q. A 40-year-old female was suffering from Schizophrenia and taking Chlorpromazine for
last one year. Enlist six common adverse effects which may appear during the treatment.
1. Parkinson-like syndrome with bradykinesia, rigidity, and tremor
2. Tardive dyskinesias
3. Muscarinic receptor blockade, atropine-like effects (dry mouth, constipation, urinary retention,
and visual problems)
4. α-receptor blockade, postural hypotension
5. Endocrine effects include hyperprolactinemia and gynecomastia
6. Sedation
7. Malignant hyperthermic syndrome.
Q. Classify anti-epileptic drugs.
Q. Enlist the dose related adverse effects of Phenytoin.

Therapeutic dose:
1. Gum hypertrophy
2. Hirsutism
3. Coarsening of facial features
4. Hypersensitivity reactions
5. Megaloblastic anemia
6. Osteomalacia
7. Hyperglycemia
8. Fetal hydantoin syndrome
Toxic dose:
1. Ataxia
2. Vertigo
3. Diplopia
4. Nystagmus
5. Drowsiness, behavioral changes, hallucination
6. I/V--- vascular injury, edema & discoloration
Q. What is the rationale for combining Carbidopa with Levodopa?
1. Carbidopa is dopa decarboxylase inhibitor.
2. The effects of levodopa on the CNS can be greatly enhanced by co-administering carbidopa
3. Does not cross the BBB.

4. Carbidopa diminishes the metabolism of levodopa in the gastrointestinal tract and peripheral
tissues
5. It increases the availability of levodopa to the CNS.
6. The addition of carbidopa lowers the dose of levodopa needed by four- to five-fold
7. Decreases the severity of the side effects arising from peripherally formed dopamine
Q. Write down the treatment of Tourette’s syndrome.

D2 receptor blockers / Haloperidol / Pimozide
alpha 2 blocker -clonidine

CNS

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CNS

Q. Write down the mechanism of action of Diazepam?

Q. Write a note on Buspirone.

Q. A 30-year-old female is brought to emergency with convulsions. She was

The alveolar concentration required to eliminate the response to a standardized painful

Q. Enlist clinical uses of Ketamine.

Q. A 25-year-old patient was anaesthetized with Nitrous oxide and Halothane to

Halothane Nitrous oxide

Q. Enlist two advantages of Ketamine as general anesthetics.

Physiologic firing rate

Q. Enlist the clinical uses of Succinylcholine.

Q. A 36-year-old woman presented with symptoms of major depression and was

Q. Explain the following terms:

Q. Enumerate therapeutic uses of Opioids.

Q. What are the autonomic adverse effects of antipsychotic drugs.

Q. Classify anti-epileptic drugs.

Q. Enlist the dose related adverse effects of Phenytoin.

3. Does not cross the BBB.

Q. Write down the treatment of Tourette’s syndrome.

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