QUESTION BANK (Descriptive)

Subject: Pharmacology I (Theory) Year and Sem: S. Y. B. Pharm. Sem IV Rev. 2019

1. Define drug distribution. Enlist various factor affecting drug distribution. Add a note on Blood-brain barrier and
plasma protein binding.
2. Classify the phases of metabolism. Explain the phase- I of metabolism and add a note on enzyme induction.
3. Mention the receptor theories and explain two state theory of receptor. Write a note on the principle of drug action.
4. Enlist various phases of clinical trial. And write the scope and objectives of pharmacovigilance.
5. Define parasympathomimmetics. Classify them and add a detailed note on pharmacology of Cholinergic agonist.
6. Classify the general anesthetics with a detailed mechanism of action of each class. Explain diffusion hypoxia and
the drug causing the same.
7. Explain sedation and hypnosis. Discuss in detail classification, side effect and therapeutic uses of benzodiazepines.
8. Classify the barbiturates and discuss in detail nonbarbiturate anxiolytics
9. Write a note on:
A) Role of lithium in bipolar disorder.
B) Selective serotonin reuptake inhibitors.
10. Classify antipsychotics and Discuss in detail typical antipsychotics.
11. Classify anticholinergics. Give the detailed account of any two classes. Write the uses of anticholinergics.
12. Define metabolism. Enlist various Phase I and Phase II reactions. Add a note on enzyme induction and inhibition.
13. Classify anti-epileptics. Give the mechanism of action and adverse effects of Phenytoin and Valproic acid.
14. A) Define absorption. Add a note on factors affecting absorption.
14. B) Give the advantages and disadvantages of the oral route.
15. Classify the receptors along with the examples. Explain in brief ion channel receptors.
16. What are sympatholytics? Classify them and add a note on the treatment of Glaucoma.
17. Give mechanism of action and anyone therapeutic use of the following drugs: Thiopental, Disulfiram, Ketamine,
and Baclofen.
18. Classify the receptors with examples. Write about the structure of G-protein coupled receptors and discuss
signaltransduction mechanisms pathways of GPCR.
19. Classify antidepressants. Discuss in detail any two classes of antidepressants.
20. Classify muscle relaxants with examples. Write a detailed note on peripherally acting muscle relaxants.
21. Classify general anaesthetics and discuss in detail halogenated anaesthetics. Comment on Preanesthetic agents.
22. A) Discuss the mechanism of action, adverse effects, and therapeutic application of Chlorpromazine.
22. B) Write a note on the pharmacotherapy of Alzheimer’s disease.
23. Classify Opioid analgesics. Explain the pharmacology of Morphine.
24. A) Enlist the types of the receptor along with the example. Explain in brief about enzyme-linked receptors.
24. B) Explain various factors modifying drug action.
25. Classify local anaesthetics. Discuss the mechanism of action and routes of administration.
26. Classify Sedative-Hypnotics. Compare and contrast between barbiturates and benzodiazepines. Enlist the
therapeutic uses of both classes.
27. A) What is pharmacokinetics? Write a note on various mechanisms of membrane transport.
27. B) Enlist the various routes of administration. Explain any two routes in detail with suitable examples.
UNIT 1 GENERAL PHARMOCOLOGY

1. Define drug distribution. Enlist various factor affecting drug distribution. Add a note on Blood-brain barrier and
plasma protein binding.
Ans Drug Distribution :
The movement of drug from systemic circulation to interstitial fluid and various other part of body is known as
Drug Distribution.

Factors Affecting Drug Distribution :

Blood flow
Lipophilicity
Capillary permeability
Plasma Protein binding
Some other factors

BBB (Blood-Brain Barrier)

The anatomical structure of capillary networking in the brain creates a barrier to passage of many drugs in the
CNS. This is called as blood-brain barrier. These barriers are Lipoidal.
The BBB is formed by microvascular endothelial cells lining the cerebral capillaries penetrating the brain and
spinal cord of most mammals and other organisms with a well-developed CNS.
It is considered the largest interface for blood–brain exchange
The BBB is playing a critical role in protecting the brain parenchyma from blood-borne agents and providing a
significant obstacle to the entry of drugs and other exogenous compounds into the central nervous system.
The blood-brain barrier lets some substances, such as water, oxygen, carbon dioxide, and general anesthetics,
pass into the brain.
The blood-brain barrier (BBB) is maintained by glial cells, including astrocytes.

Plasma protein binding

Plasma protein binding refers to the degree to which medications attach to proteins within the blood.
When drug reach into systematic circulation, there are two forms of drugs.

Free drug: Most of free drug bind with albumin. They have good distribution
E.g., Acidic drug bind to albumin whereas basic drug bind to α1 acid glycoprotein.

Bound drug (those drugs which bind with plasma protein):

They have less distribution, because their size increase. So, they cannot cross easily membrane.
Example: Barbiturates bound with albumin whereas methadone binds to α1 acid glycoprotein.

Protein-binding may affect drug activity in one of two ways:

1) Either by changing the effective concentration of the drug at its site of action or by changing the rate at which
the drug is eliminated, thus affecting the length of time for which effective concentrations are maintained.
2) Plasma proteins, by virtue of their high concentration, control the free drug concentration in plasma and in
compartments in equilibrium with plasma, thereby, effectively attenuating drug potency in vivo.
 2. Classify the phases of metabolism. Explain the phase- I of metabolism and add a note on enzyme induction.
12. Define metabolism. Enlist various Phase I and Phase II reactions. Add a note on enzyme induction and inhibition’

Ans. Metabolism also known as biotransformation is the conversion of drug from one chemical form to another.
The primary site for drug metabolism is liver and others are kidney, intestine, plasma, lungs etc.

Phase I reaction:
In this the drugs can be metabolized by oxidation, reduction, hydrolysis and increase polarity of drugs, so drugs can
easily excrete from kidney. These are non-synthetic reaction.
These reactions serve to convert lipophilic drugs into more polar molecules by adding or exposing a polar functional
group such as -NH2 or -OH.

Phase II reaction
It is faster than phase I and also those not excreted after phase I can excreted through phase II. These reactions are more
polar, so drug can easily be excreted by the kidney and liver
It involves conjugation with an endogenous substance such as glucuronic acid, sulphate and glycine

Enzyme Induction:
The phenomena of increase drug metabolizing ability of enzymes by several drugs and chemicals are known as enzyme
induction and agents are called as enzyme inducers
It is due to:
Increase in both liver size and liver blood flow
Increase stability of cytochrome P-450 enzyme

Ex Rifampicin, Phenobarbital

Enzyme Inhibition:
A decrease in the drug metabolizing ability of an enzyme is called as enzyme inhibition
Direct inhibition : Interaction at the enzyme site and change enzyme activity
Indirect : Due to fall in rate of enzyme synthesis or due to nutritional deficiency or hormonal imbalance
14 A) Define absorption. Add a note on factors affecting absorption.
Ans. Absorption:
It is defined as the movement of drug molecule from its site of administration to the systemic circulation.
It is the first and important step of pharmacokinetics, when we take any drug through oral route, it
goes into stomach in which disintegrate and dissolution take place, then drug reach into the intestine.
Now, after dissolution drug absorb into blood from intestine/stomach through membrane.

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14B) Give the advantages and disadvantages of the oral route.
27. A) What is pharmacokinetics? Write a note on various mechanisms of membrane transport.
Ans It is the branch of pharmacology concerned with the movement of drug in body or study about (ADME), absorption,
distribution, metabolism and excretion of drug in bodyi.e what does body does to the drug.

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27. B) Enlist the various routes of administration. Explain any two routes in detail with suitable examples
UNIT 2 – GENERAL PHARMOCOLOGY
3. Mention the receptor theories and explain two state theory of receptor. Write a note on the principle of drug action .
Ans.There are four major theories for drug-receptor interaction. They are as follows:
 Induced fit theory
 Occupation theory
 Rate theory
 Two state model theory

Two State theory of receptor:

It is present in two states and also in equilibrium:
Ra (active) Ri (inactive)

 Up Regulation:
It involves increase in the number of receptors due to external stimulation.
Increase of cellular components
Due to prolonged use of antagonist drug effect increases
An example of up regulation is the response of liver cells exposed to molecules like dioxin.

 Down Regulation:
It involves decrease in the number of receptors on the surface of target cells making the cells less sensitive to a
hormone.
Due to prolonged use of agonist drug effect decreases
An example of insulin receptor down regulation can be cited here.

Principle of drug action.

Principles Drugs do not create any new functions to any physiological system but can only increase, decrease or
replace existing functions by following one of the following principles:
Stimulation: It refers to selective enhancement (increase) of the level of activity in our body.
Example: Caffeine stimulates CNS

Depression: It refers to selective diminution (decrease) of the level of activity in our body.
Example: Barbiturates depress CNS

Irritation: This is a non-selective, often harmful effect and especially applicable to less specific cells
Strong irritation results in inflammation, swelling etc.
Example: Balm
Replacement: When our body fail to produce their original response by selective chemicals, hormones.
Enzymes etc., then some drugs are given in our body which makes up this deficiency.
Example Insulin in diabetes mellitus and iron in anemia.
Chemotherapy: It refers to kill of cells which cause disease in our body without affecting the host cells.
Example use of Rifampicin/Isoniazid in tuberculosis, use of quinine in malaria.

4) Enlist various phases of clinical trial. And write the scope and objectives of pharmacovigilance.
Ans Phases Clinical trial:
In this phase, drugs are applied on human. It involves four phase –
Phase I: In this phase, drug is tested on 20-80 healthy volunteer. Main purpose of this phase is to check the
safety and side effect of the drug.

Phase II:
In this phase, drug is tested on approximate 100-500 patients with that targeted disease.
Length of this phase is months to 2 years.
Main purpose of this phase is to check the efficacy and side effect of the drug.

Phase III:
In this phase, drug is tested on approximate 1000-5000 patients with that targeted disease.
Length of this phase is 1 to 4 years.
Main purpose of this phase is to check the long-term safety, tolerability, drug interaction and assessment of safety
and efficacy.
After completing the phase III trials, drug is undergoes for the approval of FDA.
 Phase IV:
In this phase, collect data of drug that drug is safe or not.
Main purpose of this phase is to perform quality of life trials and collection of long-term safety information.

Scope and objectives of pharmacovigilance :

The scope and objectives of the pharmacovigilance are indicated below:
The main purpose of pharmacovigilance is to reduce the drug related harm to the patients and protect patients and
people
• To create a nation-wide system for patient safety reporting.
• To identify and analyses new signals from the reported cases.
• To analyses the benefit-risk ratio of marketed medications.
• To generate evidence-based information on safety of medicines.
• To support regulatory agencies in the decision-making process on use of medications.
• To communicate the safety information on use of medicines to various stake holders to minimize the risk.
• To emerge as a national center of excellence for pharmacovigilance activities.
• To collaborate with other national centers for the exchange of information and data management.
• To provide training and consultancy support to other national pharmacovigilance centers across globe.
• To identify and analyse new ADR signal from the reported cases.
• To promote rational use of medicines.

15) Classify the receptors along with the examples. Explain in brief ion channel receptors

Ans. Receptors are protein or binding site which present on surface and inside the cells, drugs bind with it and give its
pharmacological response.
Classification of Receptors :
• G-protein coupled receptor
• Ion channel receptor
• Enzyme linked receptors
• JSK-STAT binding receptor
• Receptor that regulate transcription factors

Ion channel receptors:

 Also known as ligand gated ion channel
 These are cell surface receptor
 Ion selective channel for Na+, K+, Ca2+ or Cl-
Mechanism:
 Drug (agonist) bind with ion channel and open the channel
 Ion move inside the cytosol (intercellular)
 Changes in ionic compositon
 Responses such as deporisation/hyper polarization.
 Receptor includes in this category : Nicotinic, cholinergic, GABAA, SHT3 etc

 In these receptors the agonist directly operates ion channel (no requirement of secondary messenger)
 The onset and offset of responses through this class of receptor is the fastest (in milliseconds)
18) Classify the receptors with examples. Write about the structure of G-protein coupled receptors and discuss
signal transduction mechanisms pathways of GPCR.

G-protein Coupled Receptors :

G protein-coupled receptor (GPCR), also called seven-transmembrane receptor or heptahelical
receptor, protein located in the cell membrane that binds extracellular substances and transmits signals from
these substances to an intracellular molecule called a G protein (guanine nucleotide-binding protein).

G-protein-Guanine nucleotide-binding protein

These are the cell surface receptors
It constitutes a large protein family of receptors that sense molecules(ligands) outside the cell(extracellular) and
activate inside transduction pathway and give responses.
It has 7 α-helical membrane which has 3 intracellular and 3 extracellular loops,
G-protein present in trimeric complex form (α,β,Ƴ) in which GDP is attached on α.
The G-protein float in the membrane with their exposed domain lying in the cytosol

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Signal Transduction Mechanism :
It is the mechanism pathway by which receptor’s activation is linked to the response
Eg: M cholinergic receptor acts through G-protein, while N cholinergic receptor gates influx of Na+ ions etc
24A) Enlist the types of the receptor along with the example. Explain in brief about enzyme-linked receptors.
 UNIT 3 DRUG ACTING ON PHERIPHERAL NERVOUS SYSTEM
5. Define parasympathomimetic (Cholinergic drugs), Classify them and add a detailed note on pharmacology of
Cholinergic agonist.
Parasympathomimetic = Parasympatho mean Parasympathetic nervous system + mimetic mean copy the action
These are those chemical agents or drugs which copy the action of parasympathetic nervous system.
These drugs bind with cholinergic receptors (muscarinic and Nicotinic) and give their action.
Pharmacology of cholinergic antagonist.
Cholinergic medications are a category of pharmaceutical agents that act upon the neurotransmitter acetylcholine,
the primary neurotransmitter within the parasympathetic nervous system (PNS). There are two broad categories of
cholinergic drugs: direct-acting and indirect-acting.
There are two main targets of drug action: the postsynaptic receptor and the acetylcholinesterase enzyme, which
breaks down acetylcholine. Cholinergic agonists have a direct action on the receptor for acetylcholine. Some drugs
are specific for the muscarinic receptor; others are specific for the nicotinic receptor.
16) What are sympatholytics? Classify them and add a note on the treatment of Glaucoma.
The agents which antagonize the actions of sympthamimetic agents or sympathetic stimulations are called
sympatholytics. They are classified as

1. α-adrenoceptor antagonist : This are the drugs that inhibits the action of sympathetic stimulations only at the
α-receptor in our bodies. They can be further classified as

2. β-adrenoceptor antagonist : This are the drugs that inhibits the action of sympathetic stimulations only at the
β-receptor in our bodies. They can be further classified as
Selective β1 antagonist : Atenolol, Metoprolol
Selective β2 antagonist : Butoxamine, Levobunolol
Mixed β blockers : Propranolol, Timilol

3. Adrenergic neuron blockers : Guanoxan, Guanethidine

4. Mixed α- and selective β1 adrenoceptor antagonist : Labetalol, Carteolol

Treatment of Glaucoma:
Eye drops, commonly nonspecific beta-blocker or prostaglandin analog drops, generally are the first-line treatment
to reduce intraocular pressure, Ophthalmic timolol is used to treat glaucoma, a condition in which increased
pressure in the eye can lead to gradual loss of vision. Timolol is in a class of medications called beta-blockers.
Because of the lower risk of precipitating side effects, betaxolol is probably the beta-blocker of first choice for use
in glaucoma; timolol or levobunolol are reserved for patients who do not respond satisfactorily to betaxolol and
are quite free of respiratory disease.
 20. Classify muscle relaxants with examples. Write a detailed note on peripherally acting muscle relaxants.

Peripheral Skeletal Muscle Relaxants

There are some drugs which relax skeletal muscles because of their direct action. These are called as peripheral muscle
relaxants, directly acting muscle relaxants or spasmolytics.
Dantrolene is the only drug in this category.
Mechanism of action
Dantrolene acts directly at the contractile mechanisms of voluntary muscles by reducing depolarisation-induced calcium
release from sarcoplasmic reticulum. The contractile responses are not absolutely abolished by Dantrolene. The drug
facilitates action of GABA resulting in depression of functions of brain stem and efferent motor neuron activity. Cardiac
muscles are not affected.
Therapeutic uses It is a drug of choice for the treatment of malignant hyperthermia which is a genetic abnormality.
Dantrolene is also used to treat neurolept-malignant syndrome.
Adverse effects
Generalised muscle weakness, sedation, diarrhoea and occasional hepatitis after prolonged use have been reported.

25 Classify local anaesthetics. Discuss the mechanism of action and routes of administration.
Local anaesthetics (LA) reversibly block the impulse conduction and produce a transient loss of sensation in a
restricted region of the body. These drugs are preferred for performing minor surgery. They neither cause a loss of
consciousness nor need a proper maintenance of vital functions during surgery.
UNIT 4 Pharmacology of drugs acting on central nervous system

19. Classify antidepressants. Discuss in detail any two classes of antidepressants.

Monoamine Oxidase Inhibitors (MAOIs)

One of the first classes of antidepressants developed were monoamine oxidase inhibitors (MAOIs). This
antidepressant class, first discovered in the 1950s, inhibits the action of an enzyme called monoamine oxidase,
whose role it is to break down monoamines.7 By blocking this effect, more neurotransmitters are available for use
in mood regulation.

Examples of MAOIs include: Meclobemide, Clorgyline

MAOIs are less commonly used due to potentially severe reactions with foods high in tyramine.7 If taken
inappropriately, MAOIs can cause tyramine levels to rise, triggering critical increases in blood pressure.

To avoid this, MAOI treatment usually involves dietary restrictions. Other side effects include nausea, dizziness,
drowsiness, restlessness, and insomnia.7

Selective serotonin reuptake inhibitors (SSRIs)

SSRIs work by blocking the re-uptake of serotonin into the presynaptic neuron. Because of this, more serotonin
will be circulating around the synaptic cleft, making it more likely that serotonin will reach the receptors of the
postsynaptic neuron.
If this happens, it means that more serotonin will be working in the brain, resulting in increases in mood and
feelings of happiness.
Examples include: Fluoxetine, Fluvoxamine, Paroxetine Citalopram, Escitalopram

SSRIs tend to have fewer side effects than older antidepressants but are still known to nausea, insomnia,
nervousness, tremors, and sexual dysfunction.4

In addition to treating depressions, SSRIs are also sometimes used to treat obsessive-compulsive disorder (OCD),
generalized anxiety disorder (GAD), eating disorders, and premature ejaculations. 4 They have also proved helpful
during stroke recovery.
UNIT 4 PHARMACOLOGY OF CENTRAL NERVOUS SYSEM

Q6. Classify the general anesthetics with a detailed mechanism of action of each class. Explain diffusion hypoxia and
the drug causing the same.
General Anesthetics are CNS depressants which induce non-awareness of all sensation and loss of pain.
They cause non selective and reversible CNS depression

Classification of GA:
General Anaesthetic are classified according to their nature as follows:

Inhalation general anaesthetics:

They are administered by inhalation
Further subdivided as:
 Gases: Nitrous oxide
 Liquid: Halothane, chloroform, diethyl ether

Intravenous general anesthetics:

They are administered by intravenous route
Further subdivided as:
 Fast inducers:
Barbiturates: Thiopental sodium
 Non-barbiturates: propanidid, propofol.
 Slow inducers:
Benzodiapines, Diazepam, Lorazepam
 Dissociative anaesthetic:
Ketamine

Mechanism of action:
General anesthetic targets the ligand gated ion channels and produce the anesthetic action.
The GABA receptor gated chloride channels are the most important sites and opens to perform the inhibitory
action
N2O and ketamine do not affect the GABA or glycine gated CS Channel, but they selectively inhibit the excitory
NMDA type of glutamate receptor, which belong to calcium-gated channels in the neurons and lead to neuronal
hyperpolarization

7. Explain sedation and hypnosis. Discuss in detail classification, side effect and therapeutic uses of
benzodiazepines.
A sedative is a substance that induces sedation by reducing irritabilityor excitement.
They are CNS depressants and interact with brain activity causing its deceleration.

Sedation indicates decrease in alertness and a decreased responsiveness to any level of stimulation without inducing
sleep

Hypotics are the drugs that induces and maintains sleep, similar to normal arousable sleep

Hypnosis resembles natural sleep but the person can be aroused by strong stimuli like pin prick or the sound of
alarm clock.

Side effects with BZDs:

• BZDs cause dose dependent drowsiness, fatigue, disorientation, lethargy and impairment of psychomotor skills.
• Tolerance develops slowly.
• Dependence is mild.

Therapeutic Uses of benzodiazepines :

(1) As antianxiety agents.
(2) As sedative or to potentiate the action of a hypnotic drug.
(3) Muscle relaxant and anticonvulsant agent.
(4) Psychostimulant agent.
(5) Preanaesthetic medication.
(6) During withdrawal of alcohol in chronic alcoholics.

8. Classify the barbiturates and discuss in detail nonbarbiturate anxiolytics

Ans Barbiturates are substituted derivatives of barbituric acid.
They possess sedative hypnotic properties and anticonvulsant-sedative action.
 Classification:
Depending upon the duration of action barbiturates are divided into four classes like –
(1) Long acting barbiturates (6 hours or more). (e.g., phenobarbital, primidone).
(2) Intermediate acting (3-6 hours). (e.g., amobarbital, butabarbital),
(3) Short acting (less than 3 hours). (e.g., pentobarbital, secobarbital),
(4) Ultra-short acting (I.V.). (e.g., methohexital, thiopental)

10 Classify antipsychotics and Discuss in detail typical antipsychotics.

Antipsychotics, also known as narcoleptics or major tranquilizers, are a class of medication primarily used to manage
psychosis (including delusions, hallucinations), principally in schizophrenia and bipolar disorder.
Antipsychotics are usually effective in relieving symptoms of psychosis in the short term.
Classification antipsychotics drugs :

All typical antipsychotic drugs act as antagonists at D2 and/or D3/D4 dopamine receptors.
Typical antipsychotics produce competitive blockade of post-synaptic D2 receptors in mesolimbic system.

28. Classify Sedative-Hypnotics. Compare and contrast between barbiturates and benzodiazepines. Enlist the
therapeutic uses of both classes.
 Therapeutic Uses of benzodiazepines :
(1) As antianxiety agents.
(2) As sedative or to potentiate the action of a hypnotic drug.
(3) Muscle relaxant and anticonvulsant agent.
(4) Psychostimulant agent.
(5) Preanaesthetic medication.
(6) During withdrawal of alcohol in chronic alcoholics.

Therapeutic Uses:
Barbiturates, depending upon their potency and duration of action, may be clinically employed as –
(1) Non-analgesic sedative - hypnotic drug.
(2) Anticonvulsant agent.
(3) General anaesthetic (basal anaesthetics).
(4) In psychiatric treatments, as diagnostic and therapeutic aids.

13. Classify anti-epileptics. Give the mechanism of action and adverse effects of Phenytoin and Valproic acid.

Epilepsy is a common neurological abnormality characterised by occurrence of seizures.

A seizure means a paroxysmal abnormal discharge at high frequency, from an aggregate of neurons in cerebral
cortex.
Classification of Seizures
Generalised or partial.
Unclassified seizures.

(i) Generalised Seizures: These seizures arise from both cerebral hemispheres and diencephalon simultaneously,
involving the entire body, and have characteristic bilateral pattern in EEG recording.
These are of following types:
(a) Grand mal or Tonic-Clonic Seizures
(b) Petit mal or Absence Seizures
(c) Myoclonic Seizures
(d) Akinetic (Atonic) Seizures
(e) Clonic Seizures
(f) Tonic Seizures

(ii) Partial Seizures (Localised/Focal) These are the most common seizures. The seizure activity is restricted to a
discrete area belonging to one cerebral hemisphere only.
These are of three types:
(a) Simple partial seizures (Jacksonian seizures)
 (b) Complex partial seizures (Psychomotor Epilepsy)
(c) Partial seizures evolving to secondary generalised seizures

(iii) Unclassified Seizures It covers undetermined epilepsies and epileptic syndromes like febrile seizures or
infantile spasm.

Phenytoin:
It is an oldest non-sedative antiepileptic drug. Chemically, it is diphenylhydantoin.

Mechanism of action
In therapeutic plasma levels of 10-20 µg/ml, it blocks use-dependent sodium channels and thus inhibits generation
of repetitive action potentials. At higher doses it also reduces influx of calcium and suppresses repetitive firing of
neurons. Both these actions decrease glutamate release.

Adverse reactions
Following adverse effects are observed with chronic toxicity:
o Gingival hyperplagia and coarsening of facial features.
o Megaloblastic anaemia
o Vitamin K deficiency
o Vitamin D deficiency
o Hirsutism (in females) and acne
o Hyperglycemia, decrease of ADH release

UNIT 5 CNS II