Pharmacology

Quick Revision Notes

 Chapter - 1 General Pharmacology
Pharmacology is the science dealing with drugs. ↓ Absorption → ↓ Bioavailability
Two branches: 2. First Pass metabolism/Pre systemic metabolism
1. PharmacoKinetics → Effect of Body on Drug ↑ First Pass metabolism → ↓ Bioavailability
2.PharmacoDynamics → Effect of Drug on Body ↓ First Pass metabolism → ↓ Bioavailability
Note: If we give a drug by IV route, bioavailability is
PHARMACOKINETICS 100%Q
•• Aka ADME Study Plasma Concentration Vs Time Graph
–– Absorption
–– Distribution
–– Metabolism
–– Excretion

1. Absorption
•• It is the movement of drug from site of administration
to blood. Maximum concentration
Should lie between MTC
•• Lipid Solubility is the most important factor in Cmax obtained by a particular
and MEC
absorption.Q dose
Time in which plasma
When The Medium Is Same, Then The Drug Will Cross
Tmax concentration becomes Tells Rate of absorption
DRUG MEDIUM FORM SOLUBILITY CROSS maximum
Acidic Acidic Non ionized Lipid Soluble  Total area covered by Tells Extent of
AUC
Basic Basic Non ionized Lipid soluble  graphQ absorption
Acidic Basic lonized Water Soluble x
Basic Acidic lonized Water Soluble x 2. Distribution
•• Distribution is a measure of amount of drug in tissues
Bioavailability
after absorption in the systemic circulation
•• It is the fraction of given dose that reaches the
systemic circulation in unchanged form •• It depends upon lipid solubility and plasma protein
binding.
Plasma Protein BindingQ
•• Acidic drugs bind to → Albumin
•• Basic drugs bind to → a1 Acid Glycoprotein
High PPB drugs have
•• Low Vd
•• Long duration of action
•• More drug interactions
Factors affecting: •• Dialysis not useful in poisoning
1. Absorption •• Less Filtration
→ Absorption → ↑ Bioavailability
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Pharmacology
Volume of Distribution (Vd)Q Enzyme InducersQ Enzyme inhibitorsQ
Amount given G -Griseofulvin Vit -Valproate
Vd =
Plasma concentration
P -Phenytoin K -Ketoconazole
•• Volume of Distribution (Vd) ∝ Amount of Drug in
Tissues R -Rifampicin Can’t -Cimetidine

More Vd → More distribution S -Smoking Cause -Ciprofloxacin

Loading Dose [LD] Cell -Carbamazepine Enzyme -Erythromycin

Phone -Phenobarbitone Inhibition -Isoniazid
Initial high dose given to start the action
Cytochrome p450 Enzymes
LD = Vd x Target Plasma Concentration
These are one type of microsomal enzymes.
Maintenance DoseQ CYP3A4 CYP2D6 CYP2C19Q
Repeated doses given to maintain the plasma concentration. C : Cyclosporine 2 : b-Blockers Clopidogrel
MD = CL x Target PC T : Tacrolimus D : Anti-Depressants
S : Statins 6 : Anti-Anthythmies
3. Metabolism
C : CAT (except amiodarone)
Aim of Metabolism → To Make a Drug Water Soluble (Polar)
(Cisapride,
PHASE I REACTIONSQ PHASE II REACTIONSQ
Mostly catabolic Reactions Mostly anabolic reactions Astemizole,
Includes Includes Terfenadine) CYP2C9Q
•• Oxidation (MC) •• Glucuronidation (MC) A :Amiodarone Warfarin
•• Reduction •• Glutathione conjugation
N :Navirs Phenytoin
•• Hydrolysis •• Acetylation
•• Cyclization •• Methylation
Clopidogrel
•• Deamination •• Sulfate conjugation –
CYP2C19 PPI
Purpose of Phase I → Expose the Functional Group on
the drug Active

Purpose of Phase II → Makes the drug water soluble

Therefore, PPIs are avoided with clopidogrel

4. Excretion

Enzymes
•• Divided into Microsomal and Non-microsomal
Microsomal Non-microsomal
Present in smooth Present outside SER
endoplasmic reticulum
Can be induced or Cannot be induced or
inhibited inhibited
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Cerebellum Quick Revision Notes
Glomerular Filtration Formula of Half-life:
•• Lipid soluble as well as water soluble drugs can be 1 0.693
filtered t =
2 K
•• Filtration is inversely proportional to Plasma Protein
binding (where, K is elimination rate constant)
CL
As K=
Tubular Reabsorption Vd
•• 99% of GFR is reabsorbed
So, 1 Vd
–– Lipid soluble drugs reabsorbed t = 0.693 X
2 CL
–– Water soluble drugs excreted

Order of Kinetics
First order kinetics Zero order kineticsQ
→ Fraction is constant → Amount is constant
R a PC R = Constant
CL = Constant CL a 1/ PC
Tubular Secretion
t½ = Constant t½ a PC
•• Due to pumps/transporters in proximal tubules •• Majority of drugs follow First Order Kinetics
•• These transporters are Saturable (One drug can be
transported at one time) Drugs Following Zero Order Kinetics areQ

•• Probenecid prolongs action of penicillins by inhibiting Zero → Zero order Kinetics

tubular secretion W → Warfarin
A → Alcohol/Aspirin
Kinetics of Elimination T → Theophylline
T → Tolbutamide
Half Life [t1/2]
Power → Phenytoin
•• It is the time in which plasma concentration of a
drug becomes half. PHARMACODYNAMICS:
•• Half-life is constant in first order kinetics. It deals with action of a drug as well as the mechanism
of action
Major mechanism of action of a drug are through
enzymes or through receptors.
Question: t1/2= 6hrs, after 1 day
Enzyme inhibitionQ
•• How much drug remains in body → 6.25%
Km Vmax
•• How much drug eliminated from body
→100-remaining→ 93.75% Competitive ↑ -

Importance of t ½: Non competitive - ↓

•• Dose cannot be calculated

Lineweaver Burke Plot:
•• Dosing Interval/ Frequency can be known •• Also known as double reciprocal plot
•• Graph between 1/S (on X-axis) and 1/V (on Y-axis)
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Pharmacology
•• X-axis tells Km and Y-axis tells Vmax 1. lonotropic Receptors
•• If lines intersect at X-axis, it is non-competitive •• The receptors present on ion channels are known as
inhibition ionotropic receptors.
•• If lines intersect at Y-axis, it is competitive •• Fastest acting receptors
inhibition

2. Enzymatic Receptors
•• These are present on cell membrane with
intracellular and extracellular ends.
Classification of DrugsQ •• Drug binds outside and enzyme is activated inside
and action is produced
Drug Intrinsic Activity
•• Aka Tyrosine Kinase Receptors
Agonist Maximum [+1]
Partial Agonist Submaximum [0 to 1]
Inverse Agonist Opposite action [-ve]
Antagonist No action of itself but interfere
with action of other drugs [0]

3. G-Protein Coupled Receptors [GPCR]

Classification of Receptors
Works by one out of the 3 mechanisms

•• By changing the level of cAMP

•• Can act through Ca2+
•• Can open the ion channels
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Cerebellum Quick Revision Notes
Types of G proteins 1. Potency
2. Efficacy
Second/Third
Type Mechanism 3. Slope
messenger
GS Stimulate adenylate cyclase ↑ cAMP
Gi Inhibit adenylate cyclase ↓ cAMP

IP3
Gq Convert PIP2 to IP3 and DAG DAG
Calcium

4. Intracellular Receptors
A. Cytoplasmic Receptors
B. Nuclear Receptors
Potency
•• Only Lipid soluble drugs acts through these
receptors •• To produce a similar response if a drug is required in
lesser dose, it is more potent
•• On log DRC, left-sided curve is more potent drug
whereas right-sided curve is less potent

Efficacy
•• Relates to maximum effect of a drug regardless of
dose
•• Higher the curve, more is efficacy
•• Thus, whether a drug binds the cytoplasmic
H - Height tells aboutQ
receptors or the nuclear receptors, it will finally
work through DNA (nuclear mechanism) E - Efficacy

•• These are also called nuclear recetor superfamilty L - Left side drugs are more

•• These are slowest acting receptors. P - Potent

Receptors Examples
1. Ionotropic GABAA, NMDA, NN, NM, 5HT3
2. Enzymatic Cytokines, Prolactin, Insulin, GH
3. Intracellular
A. Cytoplasmic Vit D, Glucocorticoids,
Mineralocorticoids
B. Nuclear Vit A, Thyroid hormones, Sex
hormones
4. GPCR Most others
C → Most efficacious (Highest curve)
Log Dose Response Curve (Log DRC)
•• S-shaped curve [Sigmoid Curve) D → Least efficacious (Lowest curve)

•• Clinically more useful than DRC D → Most potent (Most left)

•• 3 important parameters obtained from log DRC: B → Least potent (Most right)
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Pharmacology

Quantal DRC Clinical Trials

•• For All or None phenomenon, where grade of response
cannot be plotted.
•• Percentage of subjects responding are kept on Y-axis
•• Tells about effect of a drug in population
Testing of drugs in humans is called clinical trials
•• Licensing Authority to give approval for a new drug
in USA is FDA whereas in India it is DCGI (Drug
Controller General of India)

i) If 50% respond to a particular dose → Then it is

called ED50 (Median Effective dose)
ii) If 50% of animals die after receiving a particular Q

dose it is median lethal dose (LD50).

Therapeutic index = LD50/ED50 Q
•• Therapeutic index is margin of the safety of a drug

The Drugs and Cosmetics Act

–– An act to regulate the import, manufacture, Q
distribution and sales of drugs.
•• Spurious drug: Imitation of or substitute of
another drug in a manner likely to deceive the name
of another drug. The less known pharmaceutical
company try to take advantage of reputation of a
well-known company.
Phase Zero Clinical Trials
•• Misbranded drug: If a drug is not labelled in
prescribed manner or its label contains any •• Micro-dosing study
statement which makes any false claims for the •• It is conducted on humans
drug.
•• Maximum amount of drug given is 100 mcg or
•• Adulterated drug: If it contains filthy, patrid or (1/100)th of Human Equivalent Dose, whichever is
decomposed substances. lower
•• Radiolabeled substances are added with this
sub therapeutic dose to know the Pharmacokinetics
of the drug.
•• It is not mandatory Q
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Cerebellum Quick Revision Notes

Pregnancy Categories: Fixed Dose Combinations (FDC):

Drugs are categorized into 5 groups according to safety When two or more drugs are combined to-
in pregnancy gether in a particular ratio.
Category Special points
Advantages: Disadvantages:
A Safest in pregnancy
•• Compliance •• May be used irrationally.
B
improves •• If adverse effect occurs, it
C
•• One drug may cannot be ascribed to one drug.
D
reduce the adverse •• Drugs with different
X Contra-indicated in pregnancy e.g. ThalidomideQ effects of the pharmacokinetics cannot be
Note: other drug combined.
•• Efficacy may •• Dose of one drug cannot be
•• Schedule X drugs and category X drugs are totally
increase altered independently as per
different.
•• Cost may decrease requirement.
•• Schedule X include narcotic and psychotropic drugs
e.g. ketamine. Prescription Writing
•• Category X contain teratogenic drugs like thalidomide Prescription is the written order by the doctor to the
pharmacist to dispense some medication.Q
•• Schedule H drugs require prescription of a RMP.
SAFE AND UNSAFE DRUGS IN PREGNANCY
Condition Drugs safe in Drugs to beQ
Pregnancy avoided in
Pregnancy
Hypertension Labetalol, ACE Inhibitors and
Methyldopa ARBs
Anti-coagulants Heparin Warfarin
Bipolar disorders Anti-psychotics Valproate (Contra-
indicated)
Lithium (Avoid)
Anti-thyroid Propylthiouracil Carbimazole (1st
trimester)
Note:
Anti-microbials Penicillins, Tetracyclines
Cephalosporins Quinolones •• Without date and signature (initials), the
prescription is invalid.
Macrolides Aminoglycosides
Anti-Epileptics Levetiracetam Valproate
•• Drug name should never be written in short form
(e.g., write paracetamol, not PCM)
Lamotrigine
•• Abbreviations like OD, BD, HS should not be usedQ
Enteric Coating of Drugs: •• In dose of drug
•• This is a coating that dissolves in alkaline medium
–– Leading zeros should always be mentioned
only.
(e.g., 0.5 mg is correct but .5 mg is wrong)
•• It can be used for
–– Trial zeros should never be mentioned (e.g., 5
–– Protecting the acid labile drugs from gastric mg is correct but 5.0 mg is wrong)
acid, e.g., proton pump inhibitors.
–– Microgram should be written as mcg not μg.Q
–– It can protect gastric mucosa from irritant
drugs e.g. NSAIDS
–– It increases the absorption of drugs that are
preferentially absorbed distal to stomach.
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Pharmacology

Previous Years Questions

Q1. Which of the following factor in PC vs time graph is Q8. Which of the following drugs follow zero order
a measure of extent of drug absorption of a drug? kinetics?
A. Area under the curve B. Half life A. Phenytoin B. Diclofenac
C. Cmax D. Tmax C. Morphine D. Propranolol
Q2. Rate of administration of a drug is equal to rate Q9. Identify the type of inhibition from the given graph
of elimination. How will you calculate the dosing rate of
the drug to maintain steady state concentration?
A. Dosing rate = Vd x target plasma concentration
B. Dosing rate = CL x target plasma concentration
C. Dosing rate = Vd/target plasma concentration
D. Dosing rate = CL/target plasma concentration

Q3. Anionic and slightly acidic drugs usually bind to

A. Albumin B. Alpha acid glycoprotein
C. Ceruloplasmin D. Globulin
A. Competitive B. Non-competitive
Q4. High plasma protein binding of a drug results in:
C. Un-competitive D. Allosteric
A. Decreased glomerular filtration
Q10. True about non-competitive inhibition is
B. High volume of distribution
A. Km remains same, Vmax decreases
C. Lowers duration of action
B. Km increases, Vmax remains same
D. Less drug interaction
C. Km decreases, Vmax increases
Q5. A patient with stroke was started on clopidogrel.
D. Km increases, Vmax increases
He developed another episode of stroke 6 months later.
Which of the following is the likely cause? Q11. Identify the missing substance X marked in the
A. Rapid metabolism by CYP 1A2 box in the given diagram
B. Poor metabolism by CYP 2C19
C. Poor metabolism by CYP 2D6
D. Poor metabolism by CYP 2E1

Q6. Which of the following treatment option is utilized

in salicylate poisoning?
A. Alkalinization of urine
B. Acidificaition of urine
C. Alkalinization of blood
D. Acidification of blood
A. G protein B. Protein C
Q7. Elimination rate constant of a drug is 0.05/hr.
What is its half life? C. Cyclic AMP D. Calcium
A. 6.5 hr B. 20 hr
C. 13.9 hr D. 8 hr

Answers
1. - A 3. - A 5. - B 7. - C 9. - A 11. - C
2. - B 4. - A 6. - A 8. - A 10. - A
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Cerebellum Quick Revision Notes
Q12. Which of the following statement is correct A. 1 B. 2
regarding the given graph? C. 4 D. 8

Q17. What does LD50 signifies

A. It is the dose at which 50% of animals will die
B. It is the dose at which 50 animals will die
C. It is the dose at which 50% patients will get the
desired response
D. It is drug that will be effective at 50% dose

Q18. Which of the following statements about these

drugs is true?

A. Drug A is agonist and Drug B represents inverse

agonist
B. Drug C represents agonist and Drug D is inverse
agonist
C. Drug A is agonist and Drug D is inverse agonist
D. Drug B is partial agonist and Drug C is inverse
agonist

Q13. Type of stimulatory G protein in PIP2-Phospholipase

activation pathway is
A. Gs B. Gi
C. Gq D. Go
A. Drug A is most potent
Q14. Drug acting via tyrosine kinase receptor is
B. Drug A and B have equal efficacy but B is more
A. TRH B. TSH potent than drug A
C. Insulin D. MSH C. Drug C is least potent
Q15. Which of the following drugs act through D. Drug B has more potency but less efficacy than drug A
intracellular receptors?
Q19. Which of the following statement is correct about
A. Thyroxin B. Glucagon
clinical trials?
C. Epinephrine D. Parathyroid hormone A. New drug application is filed with Phase 2 clinical
trials
Q16. Find therapeutic index of a drug from the
information given below in the graph B. Phase 0 clinical trials is for checking the pharma-
cokinetics of the drug

C. In Phase 3, open label studies are done

D. Phase 2 is post marketing surveillance.

Answers
12. - C 14. - C 16. - C 18. - A
13. - C 15. - A 17. - A 19. - B
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Pharmacology
Q20. New drug application is filed after which phase of Q25. Variation in drug responsiveness to a particular
clinical trials? dose of the drug in different individuals can be obtained
from:
A. Phase 1 B. Phase 2
A. Graded Dose Response Curve
C. Phase 3 D. Phase 4
B. Efficacy
Q21. Manufacturer of a drug company labels the drug
C. Potency
contains 500 mg paracetamol. On quantitative analysis
by the authorities, it was found to contain only 200 mg D. Quantal Dose Response Curve
of drug. According to drugs and cosmetics act 1940,
this type of drug is known as? Q26. Which of the following statement is true regarding
Fixed Dose Combination of drugs?
A. Spurious drug B. Adulterant drug
A. Adverse effect of one drug may be reduced by the
C. Unethical drug D. Misbranded drug other drug
Q22. Identify the true statement regarding Clinical B. Two drugs with different pharmacokinetics can be
Trials: combined easily
A. Phase 1 is done to determine efficacy in patients C. Dose of one drug can be altered independently as
per requirement
B. Healthy volunteers are recruited for the first time
in Phase II D. Adverse effect can be ascribed to a single drug
Q27. Which of the following drug must be sold by
C. Randomized Controlled Trials in patients is done in retail only production of a prescription by a registered
Phase III medical practitioner?
D. Phase IV is Pharmacokinetics study in animals A. Schedule H B. Schedule G
C. Schedule X D. Schedule M
Q23. All of the following are advantages of enteric
coated tablets except Q28. As an Indian medical intern, which of the following
A. It increases the half-life of the drug is the correct format for prescription of alprazolam?
A. Tablet alprazolam 0.5 mg once a day before
B. It protects acid labile drugs from gastric pH bed time for 7 days
C. It increases the absorption of drugs that are B. Tablet alprazolam 0.5 mg HS for 7 days
preferentially absorbed distal to stomach.
C. Tablet alprazolam 500 mcg one tablet OD
D. It protects stomach from irritant drugs for 7 days
D. Tablet alprazolam ½ mg tablet HS daily
Q24. Category A, B, C, D, X division of drugs is based
on
A. Safety in pregnancy
B. Dose adjustment in renal failure
C. Therapeutic index and safety
D. Over the counter use of drug

Answers
20. - C 22. - C 24. - A 26. - A 28. - A
21. - D 23. - A 25. - D 27. - A
 Chapter - 2 Autonomic Nervous System
Origin:

Neurotransmitters:
It works on cholinergic receptors
Location Neurotrans-
mitter
Preganglionic parasympathetic ACh
Preganglionic sympathetic ACh
Postganglionic parasympathetic ACh
Postganglionic sympathetic
•• At all places NA
•• At sweat glands ACh

Actions:
Location Parasympathetic Sympathetic
Heart ↓↓ +++
Bronchus Bronchoconstriction Bronchodilation Cholinergic Receptors
GIT Diarrhea Constipation Nicotinic Receptor Muscarinic Receptor
NN→ Ganglia M1 → Stomach: ↑HCl
Bladder Contract Relax
NM→ NMJ (require M2 → Heart: ↓ HR, ↓ Conduction
Glands ↑ Secretions ↓ Secretions
optimal stimulation)
M3 → Bronchus : BC
Pupil Miosis Mydriasis
GIT : ↑ Peristalsis
Sexual system Erection Ejaculation
Bladder : ↑ Contraction
Glands : ↑ Secretions
PARASYMPATHETIC SYSTEM Pupil : Miosis

Major neurotransmitter is ACh

 13
Pharmacology

CHOLINERGIC DRUGS: Organophosphate Poisoning:

Drugs stimulating the parasympathetic system can be: Clinical features:
Receptor Feature
Directly Acting Cholinergic Drugs: stimulated
DRUG ACTS ON ACTION INDICATION M1 Aciditiy
Pilocarpine Pupil [M3] Miosis Angle closure
M2 Bradycardia and Hypotension
glaucoma Q
M3 •• Pin point pupil
Indirectly Acting Cholinergic Drugs: •• ↑ Secretions
•• These drugs act by inhibiting AChE. •• Diarrhea
•• These may be reversible or irreversible AChE •• Urination
inhibitors.
•• Bronchoconstriction
•• Reversible AChE inhibitors are used clinically M1, M2, M3 Coma
whereas irreversible AChE inhibitors are toxic.
NM Muscle weakness
Reversible AChE Inhibitors: NN Tachycardia and Hypertension

Note:
•• Nicotinic symptoms (NN) are extremely rare.
•• If pin point pupil with increase in secretions are
present, diagnosis of OP poisoning is almost sure.

Treatment
1. AtropineQ
•• DOC For OP and Carbamate poisoning
•• Given by iv route (every 5 min) till signs of
atropinization occur.
Uses of Neostigmine Q

•• Atropine cannot reverse muscle weakness

Signs of Atropinization
•• ↓ Secretions → Most reliable (Most specific) sign
•• Mydriasis → Most commonly used sign
•• Tachycardia → HR > 100 bpm

Note: Atropine is not used in organochlorine

Irreversible AChE Inhibitors (endrin) poisoning.
Include 2. AChE Reactivators (Oximes)Q
Organophosphates - Malathion
Pralidoxime [PAM]
Parathion
Carbamates - Carbaryl Di Acetyl Monoxime [DAM]
Propoxur •• Not DOC
•• Only effective in OP Poisoning
•• PAM acts only peripherally, DAM has both central
as well as peripheral actions.
14
Cerebellum Quick Revision Notes

ANTICHOLINERGIC DRUGS
Organ Receptor Drugs Uses
blocked
Pirenzepine
Stomach M1 Peptic ulcer
Telenzepine
Bradycardia
Heart M2 Atropine (DOC)
AV block
Ipratropium Bronchial asthma
Bronchus M3
Tiotropium COPD
S- Solefenacin
O- Oxybutynin
Overactive bladderQ
Bladder M3 F- Flavoxate
T - Tolterodine
BladDAR- DARifenacin
Fundoscopy
Atropine
Refraction testing
Homatropine
Iridocyclitis
Cyclopentolate
EYE M3
Tropicamide
Longest acting: Atropine
DOC in children–Atropine eye ointment
Shortest acting: Tropicamide

ATROPINE POISONING: SYMPATHETIC NERVOUS SYSTEM

(ANTICHOLINERGIC POISONING) •• Major neurotransmitter is nor-adrenaline
•• Patient has a history of taking some wild fruit
(Dhatura/Belladona) and presents withQ Adrenergic Receptors
D – Dry mouth, Delirium
a1 a2
H – Hyperthermia
Location Action Presynaptic
A – Agitation Blood vessels Vasoconstriction receptor
T – Tachycardia Eye Mydriasis → Acts like brake to
U – Urinary Prostatic ↓ Outflow sympathetic system
R – Retention urethra

A – Accommodation lost (Blurred vision, Photophobia)

•• DOC for treatment of atropine poisoning is

physostigmine.Q
 15
Pharmacology

b1 b2 b3
Location Action Location Action Location Action
Heart ↑ HR, BP Lungs Bronchodilation Fat Lipolysis
JG cells Renin secretion GIT Constipation Bladder Relax
Bladder ↓ Out flow
Glands ↓ Secretions
Uterus Tocolytic
Blood vessels Vasodilation
Skeletal muscle Tremors
spindle
Liver ↑ Blood sugar

Effect on blood vessels •• It is an addictive drug

A1 -> C α1 – Cause vasoconstriction Q
–– Shows tactile hallucinations (cocaine bugs):
B2 -> D β2 – Cause vasodilation Scratching of skin
Effect on metabolism: –– Cause palatine perforation
•• Sympathetic system protects from hypoglycemia by –– Overdose characterized by
two mechanisms: ƒƒ Agitation
Warning symptoms Hypoglycemia reversal
ƒƒ Ulcers or scratch marks on skin
•• Tachycardia (b1) •• By changing metabolism (b2)
ƒƒ Sympathetic symptoms (Tachycardia,
•• Palpitations (b1) - ⊕ Gluconeogenesis
Mydriasis, Hypertension, MI)
•• Tremor (b2) - ⊕ Glycogenolysis
•• Sweating (M3) - ⊝ Glycogenesis Note: Cocaine does not cause bradycardia since it is a
sympathetic drug.
Directly Acting Drugs
•• Beta Blockers cause (in diabetic patients)
1. Masking of warning symptoms 1.CATECHOLAMINES
2. Prevent reversal of hypoglycemia – Not effective orally
•• So, b blockers are contraindicated in diabetic Endogenous Exogenous
patients.
Adrenaline (a1, a2, b1, b2) Dobutamine (b1)
•• Sweating is only reliable symptom of hypoglycemia
in diabetics on b blocker medication.Q NA (a1, a2, b1) Isoprenaline (b1, b2)
Dopamine (D1, b1, a1) Fenoldopam (D1)

ADRENERGIC DRUGS: Uses of Catecholamines

These can be divided into: Adrenaline
•• Indirectly Acting Drugs 1. Anaphylactic Shock
•• Directly Acting Drugs •• DOC is Adrenaline
Indirectly Acting Drugs •• Route of choice is I.M. or S.C.

COCAINE - It acts by inhibiting reuptake of NAQ •• Concentration is 1:1000 (0.5 ml)Q

2. Cardiac Arrest
•• It is a local anaesthetic
•• CPR is done first
–– All LA cause vasodilation except cocaine
•• Adrenaline is useful
–– Cocaine cause vasoconstriction and
•• Concentration is 1:10,000Q
hypertension
•• Preferred routes are IV > Intraoseous > ET
16
Cerebellum Quick Revision Notes
Nor-Adrenaline Note: Beta-2 agonists can cause following adverse
•• DOC for septic shock effects:
•• Effect is monitored by checking mean blood pressure –– T - Tremors
–– T - Trachycardia
Dopamine
–– T - T-wave changes in ECG (due to hypokalemia)
Acts onQ –– Pulmonary edema - by ritodrine
Receptors Dose (mcg/ Organ Action –– However, b2 agonists do not cause
kg/min) hypoglycemia.Q

D1 <2 Blood Vasodilation (Max

vessels in Renal BV) ANTI - ADRENERGIC DRUGS
These may be alpha blockers or b - Blockers.
b1 2-10 Heart Stimulation
ALPHA BLOCKERS
a1 > 10 Blood Vasoconstriction
These can be non-selective (α1 + α2) blockers or selective
vessels α1 blockers
Uses Non-selective α blocker α1 Blocker
1. CHF 1. Used in severe 1. Used in mild to
2. Shock + Oliguria [DOC] hypertension moderate hypertension
Dobutamine 2. Can cause severe 2. Cannot cause severe
•• Mainly b1 agonist tachycardia tachycardia
•• Used for CHF
Fenoldopam Non-Selective α Blockers
•• Only D1 agonist Irreversible Reversible
•• Used for hypertensive emergencies Phenoxybenzamine Phentolamine, Tolazoline
Isoprenaline Used for Used for

•• ↑ SBP but ↓ DBPQ – Pheochromocytoma – Cheese Reaction

•• Maximum increase in pulse pressure – Clonidine withdrawal

2. NON-CATECHOLAMINES Selective α1 Blockers

•• Prazosin
Stimulates Drugs Action
•• Terazosin
a1 Phenylephrine Mydriasis without
eye drops cycloplegia •• Doxazosin
Methoxamine → Vasoconstriction → Used •• Alfuzosin
Mephentermine in shock Uses
Xylometazoline → Nasal decongestants •• BPH (Due to a1A blockade)
Oxymetazoline
•• Scorpion sting (D.O.C is Prazosin)
Naphozoline
a2 Clonidine → Brake for sympathetic system Adverse Effect
First Dose (Postural) Hypotension
Methyldopa → Used for hypertension
→ a1 blockers always started at bed-time.Q
b2 Salbutamol → Bronchodilation

Terbutaline → Used for asthma by Types of α1 receptors

inhalational route α1A α1B/1D
Salmeterol
On Prostatic Urethra On Blood Vessels
Formoterol
TAMSULOSIN
Ritodrine → Tocolytic
SILODOSIN
Isoxsuprine → Used for preterm labour
•• No postural hypotension
b3 Mirabegron Overactive bladder
•• DOC for normotensives with BPH
 17
Pharmacology

Benign Prostatic Hyperplasia: (BPH) Indications

Cardiac Uses
α1A blockers
1. Hypertension
•• Tamsulosin - Stops the dynamic component and do 2. Classical Angina [C/I in Variant angina]
not affect the size of prostate i.e they are only for
the symptoms of BPH but do not stop the growth 3. MI
of prostate. 4. Chronic CHF [C/I in acute CHF]
5. Arrhythmia
5-α reductase inhibitors:
Non-Cardiac Uses
•• Finasteride - Stops the conversion of Testosterone
to DHT which control/stops the growth of Prostate Play - Performance anxiety (DOC : Propranolol)
in BPH (Static Component).
The – Thyrotoxicosis (DOC : Propranolol)

2. BETA (β) BLOCKERS G – Glaucoma (Timolol is used)

A – Akathisia (DOC : Propranolol)
Beta-1 + Beta-2 # (First Beta-1 # (Second
M – Migraine prophylaxis (DOC : Propranolol)
Generation) Generation)
Cardiac and non-cardiac Only cardiac uses E – Essential tremors (DOC : Propranolol)
uses
Contraindicated in Asthma, Relatively safe Adverse Effects and Contra-indications
DM and PVD
Due to β1 Blockade
1. Beta-1# or Cardio-Selective or 2nd
1. ↓ Rate → Bradycardia (C/I in Sick sinus syndrome)
Generation Beta #
2. ↓ Conduction → AV Block
New → Nebivolol
3. ↓ Contractility → Acute CHF
Beta → Betaxolol
Due to β2 Blockade
Blockers → Bisoprolol
1. Asthma
Act → Acebutolol
2. Peripheral vascular Disease
Exclusively → Esmolol
3. Diabetes mellitus
At → Atenolol
Myo → Metoprolol 4. Variant angina.

Cardium → Celiprolol
GLAUCOMA
→ These are relatively safe in Asthma, PVD & DM → Glaucoma is characterized by ↑ IOP: It may be due
2. Intrinsic Sympathomimetic Activity [ISA] or to
Partial Agonists –– ↑ Aqueous humor production
→ Less chances of causing severe bradycardiaQ –– ↓ Aqueous humor drainage
Contain → Celiprolol
Partial → Pindolol
Agonist → Alprenolol
Activity → Acebutolol
18
Cerebellum Quick Revision Notes

Adverse Effects
MiotiCS
–– Cataract
–– Stenosis of NLD
PGF2a Analogues (Latanoprost)Q
–– Pigmentation of Iris (Heterochromia Iridis)
–– Growth of eyelashes (Hypertrichosis)
–– Fluid in macula (Macular edema)
–– Contra-indicated in uveitis
ApracLonIDine Q

–– Lid retraction
Brimonidine Q

–– Causes Brain suppression in Infants (Leads to

Apnea)
–– C/l in children < 2yrs
Netarsudil (Rho-kinase inhibitor)Q
–– Cornea verticillata.

DRUG OF CHOICE ANS PRACTICALS

1. Ileum graphQ
- POAG – Latanoprost
- Angle closure glaucoma – Acetazolamide
- Acute congestive glaucoma – Mannitol
 19
Pharmacology
2. Dog Blood Pressure ExperimentQ

A: Adrenaline
B: Nor-adrenaline
C: Isoprenaline

Biphasic Response → Effect of high dose of adrenaline

→ Dog is given Phentolamine → α-blocker → BP →

→ Then, Epinephrine (high dose) is given → BP ↓ →No
Biphasic Response produced
→ Called Vasomotor Reversal of Dale

→ Dog is given Atropine first → HR ↑

→ After this, a high dose of ACh given → BP & HR ↑
→ Nicotinic action appear → Stimulate sympathetic ganglia

→ Ephedrine given → BP ↑
→ Same dose is repeated → Less ↑ in BP
→ Called Tachyphylaxis
20
Cerebellum Quick Revision Notes

Previous Years Questions

Q1. Which of the following action is expected on and tears were present. The boy had involuntary
stimulation of muscarinic receptors? urination and diarrhea. On examination, the heart rate
was 58 beats per minute and blood pressure was 80/60
A. Erection mm Hg. Which of the following is the drug of choice for
treatment of this patient?
B. Ejaculation
C. Increased contraction of cardiac muscles A. Atropine
D. Bronchodilation B. N-acetylcysteine
C. Naloxone
Q2. A farmer presented with pin point pupil and increase
in secretions. Likely poisoning is D. Physostigmine

A. Organophosphate poisoning Q7. A study was conducted to see the effect of

different drugs on isolated mammalian intestinal tissue
B. Dhatura poisoning in Dale’s organ bath. The following graph is obtained.
C. Opioid poisoning Which of the following is the likely drug?
D. Atropine poisoning

Q3. Topical antiglaucoma drug dorzolamide act by which

of the following mechanism of action?
A. Carbonic anhydrase inhibition
B. Beta blockade
C. Alpha agonist
D. Prostaglandin analog

Q4. A patient with history of snake bite presented in

emergency with symptoms of fatigue and irritability. A. Acetylcholine
Ten vials of antivenom were administered intravenously B. Barium chloride
but the patient is still having difficulty in swallowing,
ptosis and respiratory distress. What should be the C. Adrenaline
next line of management? D. KCl
A. Atropine and neostigmine
Q8. An experiment on dog blood pressure was done
B. Nebulizer with salbutamol by adding different drugs. The drugs added and the
C. IV hydrocortisone effects are as shown in the given figure. This experiment
is done to demonstrate the
D. Antihistamines

Q5. A patient on treatment of myasthenia gravis

presents with increasing muscle weakness. Which of
the following drug is used to differentiate myasthenia
gravis from cholinergic crisis?
A. Edrophonium B. Pilocarpine
C. Atropine D. Pyridostigmine

Q6. A 20 year old boy was brought to emergency room

after consuming some unknown substance. The patient
was sweating profusely, saliva was drooling from mouth

Answers
1. - A 3. - A 5. - A 7. - C
2. - A 4. - A 6. - A 8. - B
 21
Pharmacology
A. Muscarinic action of ACh A. Cocaine B. Cannabis
B. Nicotinic action of ACh C. LSD D. Heroin
C. Potentiation of ACh Q15. Which dose of dopamine act preferably on beta-1
D. Antagonistic action of ACh receptors?
A. Less than 2 mcg/kg/min
Q9. After eating an unknown plant, A child presented to
emergency in comatose state. The pupils were dilated B. 2-10 mcg/kg/min
and skin was dry. Body temperature is raised and heart
rate is high. These signs and symptoms can occur with C. 10-20 mcg/kg/min
the intake of which of the following substance? D. More than 20 mcg/kg/min
A. Dhatura B. Poppy seeds Q16. A patient was on metoprolol therapy for
C. Mushroom D. Cannabis hypertension. He was also administered verapamil.
Which of the following is likely to happen with above
Q10. Topical atropine is not given in combination therapy?

A. Acute congestive glaucoma A. Torsades de pointes

B. Corneal ulcer B. Ventricular tachycardia
C. Malignant glaucoma C. Ventricular fibrillation
D. Acute anterior uveitis D. Bradycardia with AV block

Q11. All of the following are Side effects of Ritodrine Q17. A 65 years old patient presented with dribbling of
except? urine with urgency. He was started on prazosin therapy
but the patient developed postural hypotension. Which
A. Hypoglycemia B. Tachycardia of the following is the better alternative drug for this
patient?
C. Hypotension D. Pulmonary edema
A. Terazosin B. Tamsulosin
Q12. Which of the following is the action of dopamine
at low doses? C. Timolol D. Phenoxybenzamine

A. It increases renal blood flow Q18. Beta blockers are avoided in all of the following
conditions except
B. It causes vasoconstriciton
C. It has positive chronotropic action A. Glaucoma
D. It causes hypotension B. Peripheral vascular disease
C. Diabetes mellitus
Q13. A lady was stung by many bees. She developed
breathing difficulty and hypotension. Drug used for D. COPD
treatment of this condition is?
Q19. Hypertension and pulmonary edema associated
A. Adrenaline B. Nor-adrenaline with scorpion sting is managed by:
C. Dopamine D. Isoprenaline A. Carvedilol B. Prazosin
Q14. A drug addict patient presented with agitation C. Spironolactone D. Phentolamine
and ulceration on skin. The patient had severe itching
and scratch marks on the body. On examination there is Q20. Which of the following is a contraindication to the
presence of tachycardia, mydriasis and hypertension. use of Beta Blockers?
Likely substance responsible for these symptoms is?
A. Glaucoma B. Tachycardia
C. Bronchial asthma D. Hypertension

Answers
9. - A 11. - A 13. - A 15. - B 17. - B 19. - B
10. - A 12. - A 14. - A 16. - D 18. - A 20. - C
22
Cerebellum Quick Revision Notes
Q21. A known patient of bronchial asthma was started Q24. Anti-glaucoma drug that acts by increasing
on treatment with an anti-glaucoma drug. During the uveoscleral outflow is
course of treatment, asthma worsened. Which drug is
likely responsible for these symptoms? A. Latanoprost B. Timolol

A. Timolol B. Brimonidine C. Pilocarpine D. Dorzolamide

C. Latanoprost D. Pilocarpine Q25. A patient with bronchial asthma presents with

raised intraocular pressure. Treatment of open angle
Q22. A patient had symptoms of redness and glaucoma in this patient is
photophobia. On examination, cells were present in
anterior chamber with keratic precipitates. Intraocular A. Latanoprost B. Alprostadil
pressure was measured to be 38 mm Hg. Which of the C. Gemeprost D. Carboprost
following anti-glaucoma drug should be avoided?
A. PG analogues Q26. Which anti-glaucoma drug acts by increasing
trabecular outflow?
B. Beta blockers
A. Netarsudil B. Timolol
C. Mannitol
C. Acetazolamide D. Brimonidine
D. Carbonic anhydrase inhibitors

Q23. Drug capable of causing ocular hypotension with

apnoea in infants is:
A. Acetazolamide B. Latanoprost
C. Brimonidine D. Apraclonidine

Answers
21. - A 23. - C 25. - A
22. - A 24. - A 26. - A
 Chapter - 3 Autacoids
- Have autocrine effects [Local effects] H1 Blockers
- Based on chemical Structure 1st Generation 2nd Generation
Peptide Autacoids Amine Autacoids Lipid Autacoids Cross BBB, cause sedation Do not cross BBB, no
→ Angiotensin → Histamine → Prostaglandins sedation
→ Bradykinin → 5-HT → Leukotrienes Have Anti-cholinergic action No Anti-cholinergic action
→ Thromboxane → Anticholinergic S/E occur
Useful for allergy and Useful only for allergy
HISTAMINE Possess : Prophylaxis of
Receptors motion sickness
Anti : Akathisia
Location Action Blockers
Cholinergic : Common Cold

H1 CNS Allergy First and Property : Parkinsonism

Bronchus second (Drug induced)

Stimulates RAS
Generation Promethazine FexofenadineQ
Promote
Drugs •• Terfenadine metabolite
wakefulness
Loratidine
H2 Stomach Secrete Acid Ranitidine
Cetirizine
Cimetidine
H3 PreSynaptic BRAKE H3 Inverse
Agonist
Tiprolisant
[Pitolisant]
Used for
Narcolepsy
H4 WBC Chemotaxis

5-HT (SEROTONIN)
Serotonin Receptors

Location Action Drugs Example Uses

5HT1A Presynaptic Brake Agonist BuspironeQ Anxiety
5HT1B/ID BV of Brain Vasoconstriction Agonist Sumatriptan Naratriptan DOC for
Eletriptan Rizatriptan Acute Severe Migraine
5HT2A/2C Brain Blockers Clozapine , Olanzapine Atypical Antipsychotics
5HT3 CTZ Emesis Blockers Ondansetron Granisetron DOC for vomiting due to
Tropisetron Dolasetron Chemotherapy
PalonosetronQ Radiotherapy
Post-operativeQ
5HT4 GIT Prokinetic Agonist Cisapride , Mosapride, As prokinetics for GERD
Prucalopride
24
Cerebellum Quick Revision Notes

MIGRAINE:Q
→ Drug of choice for mild to moderate headache – NSAIDs (Paracetamol, Diclofenac)
→ Drug of choice for Acute severe attack – Triptans
→ Other drug for Acute severe migraine – Ergotamine
→ DOC for prophylaxis of migraine – Propranolol

New Drugs for Migraine: 1. General Effects

Q
1. Lasmiditan (DITANS) •• Fever
•• Stimulates 5HT1F receptor and decreases CGRP •• Pain
release. •• Inflammation
•• This prevents the vasodilation and neuronal
inflammation. 2. Platelets

•• Effective orally. •• TXA2 → Aggregation

•• It is recently approved for acute attacks of •• PGl2 → Inhibition of aggregation

migraine. 3. Heart
•• Advantage over triptans is that it does not induce •• Ductus Arteriosus is kept open by PGE1
peripheral vasoconstriction.
•• PDA [Patent ductus Arteriosus] is treated by
2. Monoclonal Antibodies Against CGRP NSAIDs like
•• Approved for prophylaxis of migraine. –– Aspirin
•• Given by injectable route. –– Indomethacin
–– Erenumab –– Ibuprofen (DOC)
–– Fremanezumab
–– Galcanezumab
4. Uterus

–– Eptinezumab •• PGs Contract upper segment of uterus

Q •• Used for abortion (Misoprostol is used)
3. CGRP Antagonist: (GEPANTS)
5. Stomach
•• Used for acute attack
•• PGE2 protect the stomach from peptic ulcer disease
•• Effective orally
•• For NSAID Induced Peptic Ulcer Disease
•• Drugs are
–– Most specific drug is MisoprostolQ
–– Olcegepant
–– DOC is proton pump inhibitors
–– Rimegepant
–– Ubrogepant
6. Eye
PROSTAGLANDINS PGF2α
→ ↑ Uveo scleral outflow
→ Latanoprost
→ DOC for Primary Open Angle GlaucomaQ
 25
Pharmacology

NON-STEROIDAL ANTI- - Valdecoxib

INFLAMMATORY DRUGS (NSAIDs) - Parecoxib
COX 1 COX-2 - Lumiracoxib
Constitutive Enzyme Inducible enzyme
•• These have lesser risk of causing PUD
Present normally at most Present normally in
•• These increase the risk of MI and stroke
places •• Kidney
•• Endothelium - Etoricoxib Longest acting

•• CNS - Rofecoxib and Valdecoxib Withdrawn because of MI

and stroke
NSAIDS act by inhibiting COX. These may be:
- Parecoxib is given by Parenteral route
Non-Selective COX Inhibitors Selective COX-2 Inhibitors
- Lumiracoxib is withdrawn Due to Liver toxicity
↑ Risk of PUD Less risk of PUD
GOUT
Non-Selective COX Inhibitors
It is characterized by increase in serum uric acid.
Drugs
Acute Gout
- Aspirin : Irreversible COX inhibitor
1. DOC : NSAIDs (except aspirin and paracetamol)
(Antiplatelet), ↑Uric acid
2. Steriods : If NSAIDs do not work
- Paracetamol : COX - 3 inhibitor, safe in CKD
3. Colchicine (Most effective drug):Q
- Ibuprofen : DOC for PDA
- Can cause myopathy and diarrhea
- Diclofenac : Partial COX-2 selective
- Inhibit granulocyte migration
- Indomethacin : Sedation is adverse effect
- Piroxicam : Longest acting NSAID
Chronic Gout
- Nimesulide : Not used in children (hepatotoxic)
Three types of drugs can be used in chronic gout.
- Ketorolac : Given IV
– Drugs decreasing production of uric acid
– Drugs increasing excretion of uric acid
(Uricosuric agents)
– Drugs increasing metabolism of uric acid

Proteins / Purines

Xanthine
Xanthine oxidase
1
Uric acid Excretion 2

In birds Uricase 3

Allantoin
Selective COX 2 Inhibitors
Drugs
- Celecoxib
- Rofecoxib
26
Cerebellum Quick Revision Notes

1. ↓ Formation 2. ↑ Excretion 2. Biological DMARDs:

AllopurinolQ Probenecid i. Drugs Inhibiting TNF-a:Q
•• Inhibit xanthine oxidase Sulfinpyrazone
- All are injectable
•• DOC for chronic gout Lesinurad
Febuxostat A Adalimumab
→ Plenty of fluids should
C Certolizumab
•• Inhibit xanthine oxidase be taken E Etanercept
3.↑ Metabolism Inhibitor lnfliximab
Rasburicase → Recombinant uricase Goli Golimumab
→ ↑ Risk of infections.
Pegloticase → Long acting uricase
These are fastest urate lowering agents for tumor → Contra-indicated in T.B. and Hepatitis B
lysis syndromeQ → Apart from R.A., these drugs can be used for Crohn’s
disease as well as Psoriasis
RHEUMATOID ARTHRITIS
NSAIDs and Steroids DMARDs or SAARDs ii. IL - 1 Receptor Antagonist:Q
•• Slow down the disease ANAKINRA
•• ↓ Pain and lnflammation
progression
•• No effect on disease –– A - 1st letter
Progression
–– KIN - Interleukin
•• Fast acting •• Slow acting
–– R - Receptor
–– A - Antagonist
1. Conventional DMARD:
DMARD of choice in iii. IL - 6 Receptor Antagonists:Q
Cute and Chloroquine
pregnancy Tocilizumab
Used for Cu poisoning/
p Penicillamine → 1st IL- 6 targeted monoclonal Antibody.
Wilson’s disease
→ Approved for treatment of cytokine release
A Azathioprine syndrome also.
G Gold salts Sarilumab
L Leflunomide Fastest acting DMARDQ → Used for rheumatoid arthritis
S - Six
Inhibitors of Tofacitinib
I AR - R.A.
JAK Baricitinib MAB - Monoclonal antibody
DOC, Needs LFT
Malika Methotrexate
Monitoring iv. Co-stimulation InhibitorsQ
DOC for ulcerative •• Abatacept
Sherawat Sulfasalazine
colitis
•• Inhibit the interaction of T-cell and Antigen
Presenting Cells (APC).
 27
Pharmacology

Previous Years Questions

Q1. Most specific antiemetic for Chemotherapy induced Q8. A 60 year old female with renal disease was
vomiting is: admitted for pyelolithotomy. Post operative analgesic
of choice in this patient is?
A. Doxylamine B. Tegaserod
A. Diclofenac B. Indomethacin
C. Granisetron D. Domperidone
C. Naproxen D. Acetaminophen
Q2. Buspirone is a drug used in chronic anxiety. It
produce its action by acting on which of the following Q9. Which of the following is the fastest urate
receptors? lowering therapy in tumor lysis syndrome to prevent
renal damage?
A. 5HT1A B. 5HT1B
A. Allopurinol B. Febuxostat
C. 5HT2 D. 5HT3
C. Rasburicase D. Furosemide
Q3. A boy is planning to travel by bus. Which of the
following drug can be used to prevent motion sickness Q10. A female patient presented with pain and redness
in this person? in great toe. Serum uric acid level is 9.6 mg/dL. Apart
from prescribing analgesics for relieving pain, the
A. Promethazine B. Cetrizine physician prescribed a drug which can decrease the
C. Loratidine D. Fexofenadine formation of uric acid. Which of the following enzyme
is likely to be inhibited by this drug?
Q4. Drug of choice for prophylaxis of migraine is A. Xanthine oxidase
A. Propranolol B. Imipramine B. Thymidylate synthase
C. Flutamide D. Flunarizine C. Phosphpribosyl transferase
D. DHFR
Q5. A young female presented with left sided severe
throbbing headache associated with nausea, vomiting,
photophobia and phonophobia. Which of the following Q11. Drug inhibiting granulocyte migration is:
drug can provide immediate relief to this patient? A. Montelukast B. Cromoglycate
A. Propranolol B. Sumatriptan C. Colchicine D. Felbamate
C. Topiramate D. Flunarizine
Q12. Pegloticase is used for treatment of :-
Q6. Drug of choice in paracetamol overdose is A. Ankylosing spondylosis
A. N-acetylcysteine B. Dopamine B. CPPD
C. Hydralazine D. Furosemide C. Chronic tophaceous gout

Q7. A 34 week pregnant female with polyhydramnios D. Refractory Rheumatoid arthritis

presents with labour pain. She was treated with
indomethacin earlier. Which of the following can be
likely outcome in the baby if delivery occurs at this
time?
A. Patent ductus arteriosus
B. Premature closure of ductus arteriosus
C. Patent ductus venosus
D. Premature closure of ductus venosus

Answers
1. - C 3. - A 5. - B 7. - B 9. - C 11. - C
2. - A 4. - A 6. - A 8. - D 10. - A 12. - C
28
Cerebellum Quick Revision Notes
Q13. A patient diagnosed with Rheumatoid arthritis was A. IL-6 B. IL-12
on medications. After 2 years, he developed blurring
C. IL-2 D. IL-3
of vision and was found to have corneal opacity. Which
drug is most likely to cause this?
Q15. A 40 year old male patient presents to hospital
A. Sulfasalazine B. Chloroquine with pain in great toe. It was diagnosed to be a case
of gout. Which of the following drug increases the
C. Methotrexate D. Leflunomide excretion of uric acid in urine?
Q14. Tocilizumab is an immunosuppressive drug used A. Colchicine B. Probenecid
for Rheumatoid arthritis. It is a monoclonal antibody
C. Allopurinol D. Febuxostat
against

Answers

13. - B 15. - B
14. - A
 Chapter - 4 Diuretics
Diuretics → Cause loss of Na+ & H2O in urine 3. LOOP DIURETICS
→ Act on thick ascending limb of loop of Henle
→ Inhibit Na+ K+ 2Cl– symporter
→ Include
Furosemide
Torsemide
Bumetanide
→ High ceiling diuretics [High efficacy Diuretics]Q
→ Effectve in renal failure
4. THIAZIDES
→ Act on early distal tubule
→ Inhibit Na+ – Cl– symporter
Include
Thiazides Thiazide-like diuretics
Chlorothiazide Indapamide
Methiazide Metolazone
Polythiazide
Classification Based On Site of Action
1. OSMOTIC DIURETICS Uses
•• Hypertension (DOC)Q
→ Includes mannitol
–– Metolazone is effective in renal failure unlike
Uses: other thiazides
•• Acute Congestive GlaucomaQ •• Recurrent renal calcium stones
•• Cerebral edema •• Diabetes insipidus

Contra-Indications: •• Osteoporosis

•• Cerebral hemorrhage •• Recurrent renal calcium stones

•• Pulmonary edema S/E of both Thiazides and Loop diuretics

↓ Na+ ↑ Glucose
2. CARBONIC ANHYDRASE INHIBITORS ↓K +
↑ Uric Acid
↓ Mg 2+
↑ Lipids
→ Acts on Proximal tubule
↓H +
→ Include:
Acetazolamide – Given orally or IV
Note: Loop diuretics cause hypocalcemia whereas
Brinzolamide thiazides leads to hypercalcemia
Given as eye drops
Dorzolamide
5. K+ SPARING DIURETICS
→ Act on collecting ducts
Indications:
(1) Aldosterone Receptor Antagonists
Glaucoma (Angle closure glaucoma)
–– Spironolactone
Mountain Sickness [DOC]Q
–– Epleronone
30
Cerebellum Quick Revision Notes
(2) Epithelial Na+ channel Blockers P → Potassium sparing Diuretics
–– Triamterene A → Amiloride
S → Spironolactone → Cause Gynaecomastia
–– Amiloride
T → Triamterene
These drugs cause E → Epleronone → Do not cause Gynaecomastia
↓ Na+ & H2O → Diuresis
Uses:
↑ K+ → Hyperkalemia
↑ H+ → Metabolic AcidosisQ - DOC for Conn’s Syndrome
- DOC for Edema in Cirrhosis
- DOC for Resistant hypertension

Previous Years Questions A. Intravenous digoxin

B. Oxygen supplementation
Q1. Which of the following drug is a carbonic anhydrase
inhibitor? C. Immediate descent

A. Acetazolamide B. Hydrochlorthiazide D. Acetazolamide

C. Furosemide D. Mannitol Q6. Mannitol is used in the management of:

Q2. A 25 year old male presented to emergency with A. Congestive Cardiac Failure
head trauma due to road traffic accident. In hospital, B. Acute Congestive Glaucoma
the patient developed seizures. Emergency CT scan
revealed widespread cerebral edema. Which of the C. Acute Renal Failure
following is diuretic of choice for cerebral edema in D. Pulmonary edema
this patient?
A. Mannitol B. Spironolactone Q7. A patient of chronic liver cirrhosis presents with
ascites. Which of the following is the best diuretic to
C. Furosemide D. Hydrochlorthiazide be used in this patient?

Q3. A 28 year old male went to Ladakh. He developed A. Eplerenone B. Chlorthiazide

shortness of breath. Which of the following drug will C. Furosemide D. Triamterene
you use for the treatment of mountain sickness at high
altitude? Q8. Which of the following diuretic acts on the site X
A. Acetazolamide B. Furosemide shown in the figure?

C. Epleronone D. Salbutamol A. Furosemide B. Hydrochlorthizide

C. Spironolactone D. Acetazolamide
Q4. Hydrochlorothiazide works by inhibiting
A. Na+ Cl- pump in DCT
B. Na+ Cl- pump in PCT
C. Na+ K+ 2 Cl- pump in descending limb of loop of
Henle
D. Na+ K+ 2 Cl- pump in ascending limb of loop of Henle

Q5. At a high altitude of 3000m, a person complains

of breathlessness. All of the following can be used for
management of this person except

Answers
1. - A 3. - A 5. - A 7. - A
2. - A 4. - A 6. - B 8. - B
 Chapter - 5 Cardiovascular System
CONGESTIVE HEART FAILURE 1. ↓ Work → Vasodilators
In low output CHF, heart is not able to pump enough Venodilators A r t e r i o l a r Veno + Arteriolar
blood. It results in accumulation of fluid in various parts dilators Dilators
of body.
↓ Preload ↓ Afterload ↓ Preload and ↓
ACUTE (DECOMPENSATED) CHF Afterload

Aim of treatment of Acute CHF Nitrates Hydralazine Na Nitroprusside

1. ↓ FLUID → Loop Diuretics ACE inhibitors

Angiotensin receptor
2. ↑ PUMPING → Inotropics blockers

A. b1 Agonists 2. ↓ Fluid → Loop Diuretics

•• Dopamine 3. ↓ LVH [Cardiac Remodeling]
•• Dobutamine It results due to excessive aldosterone
•• Nor-adrenaline
•• Isoprenaline

B. Phosphodiesterase Inhibitors
[Inodilators]
•• Inamrinone
•• Milrinone
CHRONIC CHF (COMPENSATED)

Aim of Treatment in Chronic CHF

1. ↓ Work
2. ↓ Fluid
3. ↓ LVH [Cardiac Remodeling]
4. Inotropic action
Drugs Used In Chronic CHF
→ 4’D’ are used
Diuretics
Dilators
Decrease LVH
→ These drugs decrease mortality in CHFQ
Digoxin
A. Beta Blockers
B. ACE inhibitors
C. Angiotensin Receptor Blockers
D. Aldosterone Antagonists
32
Cerebellum Quick Revision Notes
4.  Contractility (Ionotropics) Drugs for Angina Pectoris
DIGOXIN I. Nitrates
→ Only inotropic drug that can be given Orally II. Calcium Channel Blockers
MOA in CHF III. Beta Blockers
→ Inhibit Na+- K+ pump that ↑ intracellular calcium IV. Potassium Channel Openers
and thus inotropic action.
MOA in Atrial Fibrillation I. Nitrates
→ Vagomimetic effect lead to ↓ AV conduction Q
Mechanism of action:
Adverse Effects
Nitrates
1. Nausea, Vomiting [MC]
↓
2. Arrhythmias Nitric oxide
MC arrhythmia → Ventricular bigeminyQ
↓
Most specific → NPAT with AV BlockQ
Guanylate cyclase
3. Xanthopsia / Yellow VisionQ
↓
4. Gynaecomastia
↑ cGMP
Drugs Causing Gynaecomastia ↓
DI : DIgoxin Vasodilation (Veins >> Arteries)
S : Spironolactone
C : Cimetidine → MOA of nitrates in classical angina - ↓ Preload
K : Ketoconazole → MOA of nitrates in variant angina → Dilation of
O : Oestrogens coronary arteriesQ

Factors ↑ Digoxin Toxicity Drugs

Metabolic Drugs •• Glyceryl Trinitrate / Nitroglycerine [GTN/ NTG]

↑ Ca2+ Quinidine •• Isosorbide Dinitrate [IDN]
↓ K+ Verapamil •• Isosorbide Mononitrate [IMN]
↓ Mg2+ Amiodarone
•• Penta Erythrital Tetra Nitrate [PETN]
Thiazides and Clarithromycin
•• Amyl Nitrite [AN]
Mx of Digitalis ToxicityQ
Nitrates Sildenafil
1. Correct the cause ↓
2. DOC for Digitalis induced arrhythmias → NO
Lignocaine ↓ PDE
↑ cGMP Degraded
3. Digibind for Severe poisoning
↓
VD
ANGINA PECTORIS ↓
Hypotension
Nitrates should not be given with Sildenafil
[Risk of Severe hypotension]Q
 33
Pharmacology
GTN/NTG and IDN DrugsQ

•• DOC for acute attack of angina 1. Trimetazidine

•• Have high 1st pass metabolism 2. Ranolazine

•• Sublingual route preferred → Main mechanism of ranolazine is now assumed to be

inhibition of Late Inward Na channels.
→ IMN has minimum 1st pass metabolism
→ Longest acting → PETN MYOCARDIAL INFARCTION (MI)
→ Shortest acting → AN
Non-STEMI STEMI
→ Amyl nitrite is used in cyanide poisoning as an antidote
→ Tolerance occurs, if nitrates are continuously M → Morphine S → Streptokinase
present in blood O → Oxygen O → Oxygen
N → Nitrates N → Nitrates
→ To avoid tolerance, 6-8 hours of Nitrate Free
A → Aspirin A → Aspirin
Period should be maintainedQ
M → Morphine
ll. L-Type Calcium Channel Blockers
→ DOC for variant angina - CCB like verapamil
HYPERTENSION
and diltiazem 1. First Line Drugs for Hypertension without any
→ Dipines are not used because they can worsen compelling Indications are:
angina due to reflex tachycardiaQ A – ACE inhibitors and ARBQ
B – Beta Blockers (Not considered first line
III. Potassium Channel Opener
drugs now)
NICORANDIL C – Calcium channel blockers
→ NO Releaser + K+ channel openerQ D – Diuretics

IV. Beta Blockers ACE Inhibitors

–– Useful in classical angina (Act by ↓ HR)
–– Contra-indicated in variant angina
New Drugs for Angina Pectoris
1. Bradycardiac Agent → Ivabradine Q
Ivabradine inhibit Na+ channel [Funny current] in SA
node
→ S/E → ↓ Visual acuity (Phosphenes)
2. Rho Kinase Inhibitor → FasudilQ
3. Metabolic Modulators
→ Fatty Acids require more oxygen for same energy
production than glucose
→ Metabolic Modulation → Making heart to utilize
glucose instead of fatty acids
•• Name ends with pril
C → Cough
A → Angioedema
P → Prodrugs except captopril & Lisinopril
T → Taste alteration [Dysgeusia]
O → Orthostatic / Postural hypotension [max
with captopril]Q
P → C/l in Pregnancy
R → C/lin B/L Renal Artery StenosisQ
I → C/I in Increased K+
L → Lower the risk of Diabetic Nephropathy
ARBs [Angiotensin (AT1) Receptors Blockers]
- Name ends with ‘SARTAN‘
- All points about ACE inhibitors apply to ARB
also, except that these do not cause cough and
angioedema and ARB are not pro-drugs.
- Telmisartan is a PPAR-g agonist and can reverse
insulin resistanceQ
34
Cerebellum Quick Revision Notes

2. DOC in special situationsQ ANTI-ARRHYTHMIC DRUGS

Condition DOC Vaughan Williams Classification
HTN in pregnancy Oral Labetalol > Methyldopa → Based on predominant mechanism of action
HTN Emergency in IV Labetalol Class I → Na+ Channel Blockers
pregnancy Class II → b Blockers
HTN Thiazides Class III → K+ channel blockers
Class IV → Ca2+ Channel Blockers
HTN Emergency Nicardipine > Nitroprusside Class V → Others
Resistant Spironolactone Class I DrugsQ
Hypertension
(Resistant to → Na+ Channel blockers
minimum 3 drugs
→ ↓ Slope of Phase 0
including thiazides)
Class Effect on K+ channel Effect on APD QT interval
1a Blocker ↑ ↑QT
PULMONARY HYPERTENSION 1b Opener ↓ ↓QT
Intravenous Vasodilator Testing (on giving IV CCB, 1c No effect - No effect
pulmonary artery pressure decreases)
→ If positive, DOC → CCBQ
→ If negative, DOC → Endothelin antagonistQ

DRUGS USED IN PULMONARY HYPERTENSION

1. Calcium channel blockers:

DHPs like amlodipine are DOC if IV vasodilator testing
is positive (in < 5% cases)
Class 1a Drugs Class 1b Drugs Class 1c
2. Endothelin antagonists: Drugs
Bosentan, ambrisentan like drugs are DOC for pulmo- Quinidine Lignocaine Encainide
Procainamide Phenytoin Flecainide
nary hypertension
Tocainide
3. PDEI [Phosphodiesterase Inhibitors]
→ Sildenafil, Tadalafil Cause QT Prolon- Used only for Ven-
gation tricular arrhythmia
4. Prostaglandins
Class II
PGI2 → lloprost
5. Selexipag → Beta BlockersQ

→ Prostacylin agonist → Used in Tachyarrhythmias

→ Can be given orally Class III
SELE → Selective
→ K+ Channel Blockers
XI → Non injectable [Oral]
B → Bretylium
P → PGI2 I → Ibutilide
AG → Agonist N
D → Dofetilide, Dronedarone
A → Amiodarone
S → Sotalol
→ Sotalol has both Class III [Major] & class II Actions
 35
Pharmacology
AMIODARONE ANTI-DYSLIPIDEMIC DRUGS
→ Longest acting [t1/2 → > 3wks] anti arrhythmic drug 1. Statins
→ MOA MOA
1. Na+ channel Blocker
1. Inhibit HMG-COA Reductase (Rate limiting enzyme
2. Beta-Blocker (Non-competitive) in cholesterol synthesis)Q
3. K+ channel Blocker [Main action] 2. Compensatory ↑ of LDL - R
4. Calcium channel blocker 3. Cholesterol is taken from blood
→ Adverse effect of amiodaroneQ 4. ↓ Serum cholesterol
Examples
The Thyroid (hypo/hyper) (40% iodine is
present in amiodarone) –– Atorvastatin
–– Rosuvastatin [Longest Acting]
Periphery of Peripheral neuropathy
–– Pravastatin
My Myocardial depression
–– Simvastatin
Lung Lung fibrosis
Liver Liver toxicity Important Points
Cornea is Corneal deposits A. Statins have maximum LDL – Cholesterol lowering
Photosensitive Photosensitivity (Rash on exposure potential
to sun)
B. Given at late evening/night
(Bluish: Blue man syndrome)
•• Atorvastatin & Rosuvastatin are long acting, can be
Class IV given at anytime of the day
→ L-Ca2+ Channel Blockers •• Rosuvastatin is longest acting statin.Q
–– Verapamil C. Adverse EffectsQ

–– Diltiazem –– Myopathy → Risk further ↑ with Fibrates

and enzyme inhibitors like clarithromycin and
–– DHPs [Not Used] erythromycin.
→ Used in Tachyarrhythmias –– Hepatotoxicity
→ Should not be combined with β blockers [Risk of Severe –– Hyperglycemia: ↑ Risk of new onset DM.
Bradycardia and AV Block]
D. Pleiotropic EffectsQ
Class V These are additional benefits apart from improving
lipid profile.
Digoxin - Used for AF (in patients with CHF)
PL → Plaque Stabilization
Atropine - DOC for Bradycardia & AV block
E → ↓ Endothelial dysfunction
Adenosine - Shortest acting antiarrhythmic drug (t1/2
< 10s) I → ↓ Inflammation

- DOC for PSVTQ O → ↓ Oxidative Stress

TR → ↓ Thrombosis
Opic
36
Cerebellum Quick Revision Notes

2. Other Drugs
Fibrates Clofibrate • Max TG lowering potential
Fenofibrate • S/E → Gall StonesQ
Ezetimibe Inhibit absorption of cholesterol from intestine Usually combined with statins
BABA Cholestyramine DOC in pregnancy and children
Colestipol S/E → ↑ TG
Niacin Vitamin B3 Max. HDL - C increasing potential

Compliance limiting S/E → Itching & flusing

HyperuricemiaQ

Hepatotoxicity

3. New Drugs
A. PCSK - 9 (Pre Protein ConvertinSubtilisinKexin Type 9) InhibitorsQ
•• PCSK-9 binds to LDL - receptors and take it to lysosomes that result in breakdown of LDL receptors.
•• Thus PCSK 9 inhibitors prevent breakdown of LDL receptors. When more LDL receptors are present, they can
take up more LDL-cholesterol from blood.
•• So, we can use these drugs as hypolipidemic drugs.
•• Alirocumab and Evolocumab are monoclonal antibodies against PCSK-9
B. MTP (Microsomal Triglyceride Triglyceride Transport Protein) Inhibitors
•• Triglycerides are packed in VLDL by MTP
•• Drug inhibiting MTP is Lomitapide
C. Evinacumab
•• Monoclonal antibody against ANGPTL1 (Angiopoietin Like Protein 3)
•• It acts independent of LDL-receptor density.
 37
Pharmacology

Previous Years Questions

Q1. A hypertensive patient has grade 4 renal failure Q6. All of the following drugs are indicated in the
and GFR less than 30 mL/min. The physician wants to treatment of NSTEMI except
prescribe a thiazide diuretic. Which is the best drug
for this patient? A. Clopidogrel B. Aspirin
C. Streptokinase D. Prasugrel
A. Hydrochlorthiazide
B. Chlorthalidone Q7. Which of the following is a K+ Channel Opener?
C. Metolazone A. Ranolazine B. Nicorandil
D. Indapamide C. Verapamil D. Quinidine
Q2. A patient with chronic stable angina presents with Q8. Which of the following is a late inward sodium
pedal edema, breathlessness and other symptoms of channel blocker?
heart failure. Which of the following drug can increase
longevity in this patient? A. Ivabradine B. Ranolazine
A. Nifedipine B. Digoxin C. Trimetazidine D. Fasudil
C. Lisinopril D. Torsemide Q9. Which of the following drug acts at the site marked
by arrow as shown in the diagram
Q3. Drug of choice for treatment of digoxin induced
ventricular arrhythmias is?
A. Atropine B. Lidocaine
C. Amiodarone D. Procainamide

Q4. A patient on digoxin therapy accidently consumed

8 tablets of digoxin 0.25 mg. Two hours later, he
presented to emergency with heart rate of 54 bpm and
ECG evidence of third-degree AV block. What is the
immediate management of this patient?
A. Digoxin immune Fab
B. Lignocaine
C. Phenytoin
D. DC cardioversion

Q5. A patient on digoxin therapy and had a level of 1 ng/

ml. He was receiving several other drugs and presented
2 months later with flattening of T waves in ECG. Now
the plasma level of digoxin is 3.8 ng/ml. Which of the
following drug is likely to be responsible?
A. Triamterene B. Atenolol A. Aliskiren B. Ramipril
C. Clarithromycin D. KCl C. Losartan D. Spironolactone

Answers
1. - C 3. - B 5. - C 7. - B 9. - B
2. - C 4. - A 6. - C 8. - B
38
Cerebellum Quick Revision Notes
Q10. Which of the following antihypertensive drug is Q16. Resistant hypertension is defined as inability to
avoided in patients with high serum uric acid levels? attain goal blood pressure inspite of the concurrent
use of 3 antihypertensive agents of different classes
A. Hydrochlorothiazide prescribed at optimal doses including
B. Enalapril
A. Alpha blockers B. Diuretics
C. Prazosin
C. Reserpine D. Alpha methyl dopa
D. Atenolol
Q17. A 45 year old patient presented with the symptoms
Q11. A 34 weeks pregnant lady presented with seizures. shown in image below. Patient is a known hypertensive
Her blood pressure is 200/110 mm Hg. Which drugs and was taking some antihypertensive drug. Which of
should be used for the treatment of this patient? the following drug is the likely cause of this condition?
A. Oral Labetalol
B. IV labetalol plus magnesium sulphate
C. IV Lorazepam
D. IV Enalapril

Q12. Drug used for treatment of pregnancy induced

hypertension is
A. Alpha methyl dopa B. Lisinopril
C. Hydralazine D. Telmisartan

Q13. A 56 year old patient who is a known case of

hypertension was being treated with antihypertensive
drugs. He is having chronic cough since 2 weeks. He was
started on antimicrobials but cough did not resolve. A. Lisinopril B. Clonidine
Which of the following antihypertensive drug may
induce chronic cough in this patient? C. Nifedipine D. Timolol

A. Lisinopril B. Minoxidil Q18. Which of the following drug should be stopped in a

C. Propranolol D. Amlodipine patient with hyperkalemia?
A. Losartan B. Furosemide
Q14. A 26 year old female came to hospital for pre-
conceptional counselling. Patient is a known hypertensive C. Amlodipine D. Hydrochlorthiazide
compliant to drug therapy. Which of the following drugs
will you advise to stop? Q19. A patient presents with grade 2 pulmonary artery
hypertension. Vaso-reactive stimulation test is negative.
A. Methyl dopa B. Labetalol Which is the most preferred initial management of this
C. Lisinopril D. Nifedipine patient?
A. Epoprostenol B. Amlodipine
Q15.Identify the correct match regarding the drug and
its adverse drug reaction? C. Alprostadil D. Ambrisentan

A. Hydralazine: Heart failure

B. Verapamil: Constipation
C. Aliskiren: Hypokalemia
D. Atenolol: Hemolytic anemia

Answers
10. - A 12. - A 14. - C 16. - B 18. - A
11. - B 13. - A 15. - B 17. - A 19. - D
 39
Pharmacology
Q20. A 65-year-old man comes to OPD with history of
fall. He is hypertensive with history of atrial fibrillation
and is presently on captopril, atenolol, aspirin and
amiodarone. He presents with the following finding as
shown in the image. What is the most probable diagnosis?

A. Quinidine B. Lignocaine
C. Esmolol D. Tocainide

Q23. Which of the following drug should be avoided in

a patient on rosuvastatin therapy?
A. Clarithromycin B. Oxycodone
C. Rivaroxaban D. Adalimumab

Q24. Which of the following hypolipidemic drug acts by

inhibition of PCSK-9?
A. Silver toxicity
A. Atorvastatin B. Evolocumab
B. Lupus pernio
C. Ezetimibe D. Lomitapide
C. Amiodarone induced skin lesion
D. Captopril toxicity Q25. Which of the following anti-dyslipidemic drugs
can result in gall stones?
Q21. Which of the following antiarrhythmic drug
is contraindicated in a patient with interstitial lung A. Statins B. Bile acid sequestrants
disease? C. Niacin D. Fibrates
A. Amiodarone B. Sotalol
C. Quinidine D. Lignocaine

Q22. The figure below shows the effect of a drug on

the action potential of heart as shown by arrow. Which
of the following drug is likely to produce this effect on
action potential?

Answers
20. - C 22. - A 24. - B
21. - A 23. - A 25. - D

PITUITARY HYPOTHALAMIC SYSTEM
Anterior Pituitary
Growth Hormone [GH]
Thyroid Stimulating Hormone
Adreno corticotropic Hormone
Chapter - 6 Endocrine system
Hypothalamic control
GHRH [GH Releasing Hormone]
GHIH [GH Inhibiting Hormone]
Thyrotropin Releasing Hormone
Corticotropin Releasing Hormone
Uses of Dopamine AgonistsQ
Dopamin - Diabetes mellitus type 2 (Bromocriptine)
Agonists - Acromegaly (by decreasing GH)
Suppress - Suppression of lactation.
Plasma - Parkinsonism (Bromocriptine can be used)
Prolactin - Hyperprolactinemia

Gonadotropins GnRH [Gn Releasing Hormone] Drugs for Acromegaly

Prolactin Prolactin Inhibiting Hormone A. Decreased GH release

1. Growth Hormone Inhibiting Hormones [GHIH] –– Octreotide

–– It is also known as Somatostatin –– Cabergoline

SOMA TOSTATIN USESQ –– Bromocriptine

S → Secretory Diarrohea (Carcinoid syndrome, VIPoma) B. GH receptor antagonist
O → Oesophageal Varices –– Pegvisomant
M → Malignancy [Insulinoma, Glucagonoma]
3. Gonadotropin Releasing Hormone [GnRH]
A → Acromegaly
Pulsatile Fashion Continuous Fashion (Non-pulsatile manner)
→ Any drug ending with “tide” is peptide. ↓ ↓
→ Any endogenous substance ending with “in” is a ↑ Gonadotropins ↓ Gonadotropins
peptide ↓ ↓
e.g; Somatostatin
Vasopressin ↑ Estrogen ↓ Estrogen
Oxytocin ↑ Progesterone ↓ Progesterone
→ Peptides cannot be given orally ↑ Testosterone ↓ Testosterone
Somatostatin → Short acting therefore not used Indications of GnRH
Octreotide → Long-acting somatostatin derivative
→ Given by SC route Pulsatile manner Continuous Fashion
1. Anovulatory infertility 1. Carcinoma prostate
2. Prolactin Inhibiting Hormone [PIH] =
2. Hypogonadotropic hypogonadism 2. Endometriosis
Dopamine [DA]
3. Delayed Puberty 3. Precocious Puberty
→ DA acts through D2 Receptors
→ Dopamine D2 Agonists decrease prolactin GnRH AgonistsQ
Examples 1. Leuprolide
Bromocriptine 2. Nafarelin (nasal route)
Cabergoline [Long acting] 3. Goserelin
4. Busurelin
5. Histarelin
→ Not effective orally (Mostly given by subcutaneous
route)
→ Flare up Reaction: When these are given in continuous
 41
Pharmacology
manner, for initial few days, there is aggravation of Vasopressin Receptor Agonists
disease
–– V1 agonist is terlipressin
GnRH AntagonistsQ
•• DOC for esophageal varicesQ
1. Cetrorelix
–– V2 agonist is desmopressin
2. Ganirelix
•• DOC for neurogenic (central) diabetes
3. Abarelix insipidus (Given by nasal route)Q
4. Degarelix
Vasopressin Receptor Antagonists
→ No Flare up reaction
–– VAPTANS: VAsoPressin ANTagonistsQ
→ But they do not ↑ sex hormones (Used only to ↓ sex
hormones) –– Examples
→ Not effective orally Conivaptan - Given via Intravenous route
Tolvaptan - Given via Oral route
ELAGOLIX
–– Used for SIADH
→ Recently approved oral GnRH antagonist
→ Approved for pain due to Endometriosis THYROID
Hypothyroidism
POSTERIOR PITUITARY –– DOC is L-thyroxine (T4)
→ Secretes two main hormones
–– Started at 25 mcg daily
•• Oxytocin
–– Gradually the dose is increased
•• Vasopressin

Oxytocin Hyperthyroidism
–– Main function is to contract the uterus 1. Thyroid Peroxidase Inhibitors (Thioamides)
•• DOC for augmentation of labour Carbimazole (Prodrug)
Propyl Thio Uracil (PTU)
•• DOC for postpartum hemorrhage Methimazole (Active)

–– Other function is ejection of milk → Crosses placenta easily → Less crossing of Placenta

•• DOC for Breast engorgement → DOC for all patients

except in 1st trimester → DOC in 1st trimesterQ
of pregnancy
Vasopressin → Can cause choanal
–– Also known as anti diuretic hormone (ADH) atresia and aplasia cutis → Lesser chance
in developing fetusQ
Vasopressin Receptors
2. Secretion Inhibitors
• Nal
V1 Receptor V2 Receptor
–– Present on BV –– Present on kidney • Kl
–– Cause vasoconstriction –– ↓ Urine. • Lugol’s Iodine
→ Fastest acting anti-thyroid drugs.
→ Given preoperatively:
–– To make the gland small, firm and less vascular
–– To reduce the blood loss during surgery.
42
Cerebellum Quick Revision Notes

3. Radioactive iodine or I131 •• Anterior thigh

→ C/I in pregnancyQ •• Lateral thigh
→ Cause irreversible hypothyroidism •• Arm
→ Physical t ½ is 8 days 2. Intravenous route:
•• Only regular insulin can be given
ENDOCRINE PANCREAS •• So, insulin of choice in diabetic Ketoacidosis
→ Regular insulin
Secretes Action Uses
α cells Glucagon ↑ Blood Sugar Hypoglycemia 3. Inhalational route:

β cells Insulin ↓ Blood Sugar Diabetes mellitus Afreeza → Short acting insulin → So, should be
Amylin given before every meal

δ cells Somatostatin ↓ Insulin Islet cell tumors

↓ Glucagon INSULIN ANALOGUES
Rapid acting Ultra-Long Acting
GLUCAGON •• LISPRO •• GLARGINE
Uses •• ASPART •• DETEMIR
•• GLULISINE •• DEGLUDEC (Longest Acting)Q
1. Hypoglycemia 2. Beta- Blocker Poisoning
– Glucagon is DOCQ
- These are peakless insulins
→ Acts by Glycogenolysis
– Acts by stimulating - These have low risk of hypoglycemia
→ Not useful in hypoglycemia
glucagon receptors on
caused by Side Effects
heart
•• Starvation
1. Hypoglycemia
•• Alcohol induced hypoglycemia
2. HypokalemiaQ

INSULIN
ORAL ANTI DIABETICS DRUGS
Indications
1. Insulin Secretagogues (Act by ↑ Insulin secretion)Q
1. All patients of type 1 DM
–– These drugs secrete insulin and thus can cause
2. Uncontrolled patients of type 2 DM
hypoglycemia
3. Diabetes in pregnancy
Sulfonylureas Meglitinides
4. Diabetic Ketoacidosis
1st Generation Nateglinide
Routes of Administration Repaglinide
Chlorpropamide
1. Sub - cutaneous route:
Tolbutamide
–– MC route (because self-administration is 2nd Generation
possible with this route)
Glipizide
–– All insulin preparations can be given by Gliclazide
subcutaneous route. Glibenclamide
–– Site of administration
Drugs ending with “IDE” can cause - hypoglycemiaQ
•• Entire abdomen except area around umbilicus
(thickness of skin is not uniform, so insulin
absorption is affected)
 43
Pharmacology
2. Drugs Acting by Other Mechanisms C. Acarbose
→ Act by inhibiting the intestinal absorption of
A. Metformin carbohydrates (blood sugar decreases)
Adverse effects → Does not cause hypoglycemia
1. Megaloblastic Anemia → Flatulence → MC side effect
2. Lactic acidosis → C/I in lnflammatory bowel diseaseQ
Risk of lactic acidosis further ↑, if there isQ •• Ulcerative colitis

–– Liver disease (Gluconeogenesis cannot occur) •• Crohn’s disease

–– Renal disease (Lactic acid produced cannot be

NEW ANTIDIABETIC DRUGS
excreted)
1. Incretin – Mimetics
–– Any condition predisposing to hypoxia (e.g.;
Shock, COPD) → Incretins are normal physiological substances
which are released in GIT after food intake that
Thus, metformin is C/I in these patients. stimulate the release of insulin.
→ Most important endogenous incretins are GLP
Indications (Glucagon like peptide) and GIP (Glucose
→ Metformin is DOC for Type 2 DM because: stimulated insulinotropic polypeptide)

–– No risk of hypoglycemia → Functions of Incretins:

–– Max. reduction in HbA1cQ –– Increase insulin release
–– Can cause weight loss or weight neutral (No –– Decrease gastric motility
weight gain) → GLP is metabolized by DPP-4 and becomes inactive

B. Glitazones
E.g. Troglitazone
Rosiglitazone
Pioglitazone

Mechanism
Act by stimulating PPAR-ꝩ → Reversal of Insulin Resistance
Adverse Effects A. GLP analogues:
→ Given subcutaneously (Cannot be given orally since
1. Hepatotoxic
these are peptides)
→ Max. hepatoxicity → Troglitazone [withdrawn]Q
GLP-1 analogues : Used for type 2 DMQ
→ Rosiglitazone and Pioglitazone require LFT
–– Exenatide
monitoringQ
–– Liraglutide
2. Na+ and water Retention → Avoid in CHF and HTNQ
3. Predispose to osteoporotic fractures. GLP-2 analog : Used for short bowel syndromeQ

4. ↑ Risk of Ml by rosiglitazone –– Teduglutide

5. ↑ Risk of urinary bladder carcinoma by PioglitazoneQ Side effects

–– Acute pancreatitis (Major side effect)
–– Increased risk of Medullary carcinoma of
Thyroid
44
Cerebellum Quick Revision Notes
B. DPP - 4 inhibitors: 4. BromocriptineQ
a. Sitagliptin → Decreases insulin resistance and it has been
b. Vildagliptin recently approved for type 2 diabetes treatment.
c. Alogliptin → Given in small dose and taken at early morning
on awakening.
d. Linagliptin

→ Gliptins are oral anti - diabetic drugs. ADRENAL

–– Pancreatitis is the major adverse effect Adrenal Medulla Adrenal Cortex
–– Gliptins are contraindicated in renal failure → Secretes → Secretes
except Linagliptin which is safe in renal failure –– Adrenaline –– Glucocorticoids
2. SGLT-2 Inhibitors: –– Nor-Adrenaline –– Mineralocorticoids
→ Glucose is freely filtered by glomerulus but the –– Dopamine
clearance of glucose in urine is negligible.
Mineralocorticoids
→ Because the reabsorption takes place in proximal
Aldosterone → Major endogenous Mineralocorticoid
tubule by sodium glucose transporter (SGLT-2)
Actions
– Retain Na+ and water
– Remove K+ and H+
Glucocorticoids
Hydrocortisone → Major endogenous Glucocorticoid

CLASSIFICATION OF DRUGS
Glucocorticoids Mineralocorticoids
Short Acting (<12 hours) Aldosterone
Cortisone Fludrocortisone
→ SGLT-2 inhibitors stop the reabsorption of glucose Hydrocortisone DOCA
in PT resulting in glucosuria.
Intermediate Acting (12-36 hours)
Drugs are Q
Prednisone
–– Canagliflozin Prednisolone
–– Dapagliflozin Triamcinolone

–– Empagliflozin Long Acting (> 36 hours)

–– Ertugliflozin Dexamethasone
Betamethasone
–– Most common side effect of SGLT-2 Inhibitors
Paramethasone
is Urinary Tract infections
–– SLGT-2 inhibitors provide cardiovascular benefits.
Special PointsQ
These are approved for treatment of CHF.
Property Drug
3. Amylin Analogs:
Maximum G activity Dexamethasone
→ Amylin is secreted form β - cells of pancreas. Maximum M activity Aldosterone
→ Function of amylin is to ↓ blood sugar. G with max M activity Hydrocortisone

→ Pramlintide is an amylin analogue M with max G activity Fludrocortisone

Triamcinolone
→ It is approved for both type 1 and 2 diabetes.
Selective G Dexamethasone
Betamethasone
 45
Pharmacology

Selective M DOCA Adverse effects

Note: G means glucocorticoid (anti-inflammatory) Major adverse effect is Cushing syndrome
M means mineralocroticoid (Na+ and H2O retaining)

Uses of Corticosteroids
Antenatal Replacement Other Uses
Dexa / Acute Adrenal Inflammation
Betamethasone insufficiency / Auto immune
for fetal Addisonian crisis diseases
lung maturity [by IV] Transplantation
(Glucocorticoids Anticancer therapy
increase Chronic Adrenal Asthma
surfactant lnsufficiency /
production) Addison’s disease
[by oral]

Ante Natal Steroids Total dose Total duration

Betamethasone → IM 12 mg
24 mg 48 hrs.
every 24 hrs. x 2 DosesQ
Dexamethasone → IM 6 mg OSTEOPOROSIS
24 mg 48 hrs
every 12 hrs. x 4 Doses
Drugs used in Osteoporosis
Hypothalamo-Pitutary-Adrenal Axis [HPA Axis]

Inhibit Dual action

Nutritional osteoclast Stimulate – Strontium
factors – Calcitonin osteoblast – Romosozumab
– Calcium – Estrogens – PTH 1-34
HPA Axis Suppression – Vitamin D – SERMs
– Denosumab
→ Occurs when corticosteroids are given continuously – Cinacalcet
for > 2wks
Preventive Measures Nutritional Factors
1. Stop unnecessary use of steroids –– Calcium is given at a dose of 1200 mg/day (It
includes dietary calcium)
2. If indicated, prescribe them for minimum period
–– Vitamin D should be given as 800 IU per day
preferably < 2wks
3. If indicated for long periods, prescribe them on Drugs Inhibiting Osteoclast
alternate day 1. Calcitonin: Given Intranasally
–– Long-acting steroids (dexa, beta and 2. BisphosphonatesQ
paramethasone) are avoided
Alendronate
4. If indicated daily and for longer periods Risedronate
–– Don’t Stop Abruptly Zoledronate

–– Tapering should be done –– Inhibit osteoclasts

–– DOC for Osteoporosis [Osteoporosis due to any
reason]
46
Cerebellum Quick Revision Notes
–– These are indicated for a period of maximum 10 DRUGS STIMULATING OSTEOBLASTS
years
1. Teriparatide
–– Highly toxic to esophagus
–– Parathyroid hormone contains 84 amino acids
Prevention of Oesophagitis Q (i.e., PTH1-84).
– Take empty stomach –– Full molecule stimulates osteoclast and induces
– Take with full glass of water osteoporosis by resorption of bone.
– Remain upright for 30 min
–– Teriparatide is a fraction of parathyroid (PTH
3. Estrogen and SERM 1-34) that stimulates Osteoblast and is used for
Decreased estrogen is responsible for post- osteoporosis treatment.Q
menopausal osteoporosis –– Route of administration - Not effective orally
(given subcutaneously)
Actions of Estrogen
–– PTH 1-34 is recommended for maximum 2 years.
Bone → Prevent resorption
–– Treatment with PTH should be followed by
Blood → ↑ HDL/LDL Ratio 1-34
bisphosphonates.
Breast → ↑ Risk of Carcinoma
Endometrium → ↑ Risk of Carcinoma
Liver → ↑ Clotting Factors → Thromboembolism
DRUGS WITH DUAL ACTIONQ
→ Not preferred for Rx of PM Osteoporosis
–– These have dual activity of stimulating
RaloxifeneQ osteoblast and inhibiting osteoclast
–– It is selective estrogen receptor modulator –– Strontium ranelate and romosozumab act by
dual mechanism
–– It has agonist action on ER in bone, blood and
liver whereas antagonistic action on breast and –– Romosozumab is a monoclonal antibody against
endometrium sclerostin
–– Used in post menopausal osteoporosis ANDROGENS
–– Additional Benefits – – 5 α reductase converts testosterone into
•• ↑ HDL Dihydrotestosterone (DHT) which works on
androgen receptors. Testosterone also can
•• ↓ Breast and Endometrial carcinoma risk directly work on androgen receptors.
–– Major S/E → Thromboembolism
4. Denosumab
–– On the surface of osteoclast cells, RANK
receptors are present. When ligand binds to
RANK receptors, it stimulates the resorption of
bone.
–– Denosumab is a monoclonal antibody against
RANK ligand. It inhibits the osteoclastic activity
and resorption of bone.Q

–– In treatment of prostatic cancer androgen

receptor blockers are commonly used.
–– In treatment of BPH and androgenital alopecia
(Male pattern baldness): 5 α-reductase inhibitors
like finasteride are used.
 47
Pharmacology
–– Both the class of drugs can cause impotence as an 3. EMERGENCY CONTRACEPTIVES
adverse effect
A. Combined Oral Contraceptives
B. Progesterone Only Pills [LNG]
ORAL CONTRACEPTIVES C. Mifepristone
Above 3 drugs should be used with in 72 hrs. of
unprotected intercourse.
D. Ulipristal
→ Can be used within 120 hours of unprotected
intercourse

NON CONTRACEPTIVE BENEFITS

OF OCPs
Other → ↓ Ovarian cyst [DOC for PCOD]
B → ↓ Benign Breast Disease
1. COMBINED ORAL CONTRACEPTIVE PILLS
E → ↓ Endometriosis
→ Drugs
N → ↓ Neoplasia [Endometrial and ovarian cancers]
•• Estrogen - Ethinyl Estradiol
E → ↓ Ectopic pregnancy
•• Progesterone - Levonorgestrel
F → ↓ Fibroid
→ Dosage
I → ↓ Iron deficiency Anemia
•• 1 tablet daily for 21 days from 1st day of
T → ↓ Premenstrual Tension Syndrome
menstrual cycle
S → ↓ Skeletal Disease [Osteoporosis]
•• No tablet for next 7 days
•• To ↑ compliance: 28 tablets strip with 1st
21 tablets contains drug and next 7 tablets OCPs
contains iron

→ Missed Tablets ↑ Risk of ↓ Risk of

–– Cervical Ca –– Endometrial Ca
If one tablet is missed Take 2 tablet on next day
–– Breast Ca –– Ovarian Ca
•• Discard remaining tablets
•• Practice other method of
If 2 or more tablets
contraception with it. POLYCYSTIC OVARIAN DISEASE
missed
•• Start a fresh from next (PCOD)
cycle
–– OCPs are DOC for regulating the menstrual
2. POP / MINIPILLS cycle in PCOD
–– Metformin is used to reverse insulin resistance
–– Used where Combined OCPs cannot be used
–– Ovulation inducers are used to induce ovulationQ
–– Contains LNG
•• Aromatase inhibitors e.g. letrozole is DOC
–– OCP of choice in lactationQ
•• Clomiphene citrate can also be used.
48
Cerebellum Quick Revision Notes

Previous Years Questions Q6. A 28 year old female with Graves’ disease was taking
medication for hyperthyroidism during pregnancy.
Q1. A patient was operated for prostate carcinoma and She delivered a child with congenital anomaly ‘aplasia
during surgery local metastasis was noted. Which of the cutis congenita’. Most likely drug implicated for this
following drug this patient should receive? teratogenic effect is?
A. Leuprolide B. Desmopressin A. Carbimazole B. Levo-thyroxine
C. Octreotide D. Tamsulosin C. Methylthiouracil D. Liothyronine

Q2. Tolvaptan is used for:
A. SIADH
B. Central Diabetes Insipidus
C. Von Willebrand Disease
D. Catecholamine resistant Shock
Q3. A patient presents with pituitary tumor that
overproduces growth hormone. surgical removal of the
tumor was incomplete. What is the first line treatment
of this patient?
A. Leuprolide B. Octreotide
C. Nafarelin D. Goserelin
Q7. Drug of choice for hyperthyroidism in third
trimester of pregnancy is
A. Carbimazole B. Propylthyouracil
C. Sodium iodide D. Radioactive iodine
Q 8. A 30 year old female presented with weight gain
and cold intolerance. On investigations Value of T3 is
70 ng/dl (reference value 100-200 ng/dl),T4 is 3 mcg/
dl (reference value 5-12 mcg/dl) and TSH is 20 mIU/L
(reference value 0.5-5 mIU/L). Which of the following
statement is correct regarding the management of this
patient?
A. Measure T3, T4 and TSH after one month

Q4. A 40 year old male presents with protrusion of chin, B. Start L-thyroxine (T4) treatment 100 mcg once
daily
excessive sweating, impaired glucose tolerance and
enlargement of hands and feet? Which of the following C. Start L-thyroxine (T4) treatment 25 mcg daily and
drugs is a growth hormone receptor antagonist used to gradually increase
treat this condition? D. Start daily L-thyroxine (T4) 100 mcg with Liothy-
ronine (T3) 5 mcg
A. Pegvisomant B. Octreotide
C. Cabergoline D. Olcegepant
Q 9. What is the Drug of choice for Hyperthyroidism in
Q5. A female presented with galactorrhea. Her urine first trimester of Pregnancy?
pregnancy test was negative. MRI of head revealed A. Lugol’s iodine B. Methimazole
a large pituitary tumor. Patient refused to undergo
C. Propylthiouracil D. Carbimazole
surgery for the tumor. Which of the following is the
best drug for the treatment of this patient? Q 10. Which of the following drug is given pre-operatively
A. Octreotide B. Bromocriptine to decrease the risk of intraoperative bleeding in a
hyperthyroid patient planned for thyroidectomy?
C. Promethazine D. Clozapine
A. Potassium iodide B. Propranolol
C. Propylthiouracil D. Methimazole

Answers
1. - A 3. - B 5. - B 7. - A 9. - C
2. - A 4. - A 6. - A 8. - C 10. - A
 49
Pharmacology
Q 11. A 70 year old patient has diabetes mellitus and Q 16. Which of the following drug is given to mother
hypertension. He presents with late stage chronic delivering premature baby for fetal lung maturation?
kidney disease. Which of the following anti-diabetic
A. Aspirin
drugs require least dose modification in renal disease?
B. Dexamethasone
A. Sitagliptin B. Vildagliptin
C. Magnesium sulfate
C. Linagliptin D. Saxagliptin
D. Depot medroxy progesterone acetate
Q 12. A 50 year old patient of type 2 diabetes mellitus
was controlled on oral hypoglycemic drugs. This patient Q 17. A patient presented with the following features
presented to hospital with profuse sweating and after chronic intake of a drug for several years. Which
dizziness. There was presence of hypoglycemia. Which is the likely drug person has consumed?
among the following drugs can result in hypoglycemia in A. Paracetamol B. Prednisolone
this patient?
C. Phenytoin D. Metformin
A. Metformin B. Voglibose
C. Vildagliptin D. Glipizide

Q 13. Which of the following anti-diabetic drugs is

associated with increased risk of fractures in a female
with osteoporosis?
A. Canagliflozin B. Rosiglitazone
C. Voglibose D. Rapaglinide

Q 14. Mechanism of action of exenatide in diabetes

mellitus is
A. It is analogue of GLP released from gut and in-
crease glucose dependent insulin secretion

B. It is DPP-4 inhibitor and result in decreased

breadkdown of GLP

C. It inhibits SGLT-2 and cause glucosuria

D. It is amylin analogue and decrease glucagon Q 18. What is the prenatal dose of dexamethasone
given for lung maturation in premature infants ?
Q 15. To minimize the risk of HPA axis suppression, A. 6 mg 2 doses 12 hours apart
what is the correct method of administration of
B. 12 mg 2 doses 24 hours apart
prednisolone?
C. 6 mg 4 doses 12 hours apart
A. Give at night just before bedtime
D. 6 mg 4 doses 24 hours apart
B. Divide in three doses and give small doses 8 hourly
C. Give on alternate day
D. Replace with betamethasone

Answers
11. - C 13. - B 15. - C 17. - B
12. - D 14. - A 16. - B 18. - C
50
Cerebellum Quick Revision Notes
Q 19. Which of the following is not used in treatment of Q 21. A 22 year old female presents 8 hours after
polycystic ovarian disease? sexual assault. It is the 13th day of her menstrual cycle.
Which emergency contraceptive should be prescribed
A. Letrozole
to her?
B. Clomiphene citrate
A. Levonorgestrel 1.5 g single tablet
C. Ulipristal
B. Injection DMPA
D. Combined oral contraceptives
C. OCP from day 1 of next cycle
Q 20. Combined oral contraceptive pills act by all of the D. Misoprostol
following mechanisms except?
Q 22. Which of the following is not used as emergency
A. Inhibit implantation by bringing change in the uterus
contraceptive?
B. Inhibit ovulation
A. Danazol
C. Makes cervical mucus thick and hostile
B. Levonorgestrel
D. Increase gonadotropin secretion
C. Mifepristone
D. IUCD

Answers
19. - C 21. - A
20. - D 22. - A
 Chapter - 7 Central Nervous System
NEURODEGENERATIVE DISEASES Two ways to treat Parkinsonism
These occur due to age related degeneration of neurons A. Increase dopamine
B. Decrease Ach
ALZHEIMER’S DISEASE
–– It occurs due to age related degeneration of A. DOPAMINERGIC DRUGS
cholinergic neurons in basal nucleus of Meynert.
–– Aβ-amyloid deposition is the underlying cause of
neuronal degeneration.
–– It is characterized by loss of memory (Dementia)

DRUGS USED
1. AChE inhibitors:Q
Lipid soluble drugs which have very high entry in the
brain are preferred.
Donepezil
These are DOC for
Rivastigmine
Alzheimer’s dementia
Gallantamine
2. NMDA receptor antagonist:
–– Memantine is an NMDA receptor antagonist.Q
3. Monoclonal Antibody against Aβ-amyloid:
–– Aducanumab targets the underlying cause
i.e., Aβ-amyloid
1. Levo-dopa

PARKINSONISM
–– In Parkinsonism, there is deficiency of
Peripheral DOPA decarboxylase convert L-dopa to
dopaminergic activity in basal ganglia of brain
Dopamine. So if given alone:
–– Normally, there is balance b/w dopaminergic (DA) → Less efficacious due to less entry in brain.
and cholinergic (ACh) neurons → DA produced outside the brain causes peripheral
–– In Parkinsonism, this balance is lost [Relative side effects like
cholinergic excess]
52
Cerebellum Quick Revision Notes
–– Hypotension Two groups:
–– Arrhythmias 1. Central Anti-cholinergics: Benzhexol [Trihexyphenidyl]
–– Hypertension 2. First Generation Anti-histaminic drugs: Promethazine
–– Vomiting
Carbidopa MULTIPLE SCLEROSIS
Peripheral DOPA Decarboxylase
Benserazide inhibitors –– Demyelinating disease
↓ Condition DOC
Acute Episode Intravenous Steroids
↑ Efficacy
Relapsing Remitting (RRMS) β-IFN
↓ Peripheral S/E
Primary Progressive (PPMS) Ocrelizumab
Psychosis
–– Dyskinesia EPILEPSYQ
–– Abnormal behavior Special
Seizure First Line Drug
→ Psychosis can occur due to excessive DA in brain Feature

–– Central S/E of levodopa cannot be prevented GTCS Valproate, Lamotrigine

by carbi-dopa EEG shows
3 spike
→ Central S/E of levopa cannot be prevented by carbi-dopa Absence Valproate, Ethosuximide
/ wave
pattern
2. AmantadineQ Focal Carbamazepine (DOC)
Temporal
–– Acts by releasing DA from vesicle Oxcarbazepine
lobe
Levetiracetam, (DOC in elderly)
–– Can Cause ankle edema (reversible) and Livedo
Myoclonic Valproate
reticularis (Pinkish pigmentation of skin in form
of meshwork) Atonic Valproate
Lennox
–– Recently approved for treating Levo-dopa
Gastaut Valproate, Rufinamide
induced Dyskinesia as Amantadine acts as a
Syndrome
NMDA Antagonist (Only anti Parkinsonian drug
to treat dyskinesia) Febrile
Diazepam
seizures
3. Metabolism Inhibitors Status
Lorazepam
Selective MAO-B Inhibitors : Selegiline Epilepticus
Also called
COMT Inhibitors : Entacapone Salaam
Infantile seizures
4. Dopamine Agonists ACTH (DOC), Vigabatrin
spasms Seen in
→ Directly works on dopamine receptors West
–– Pramipexole and ropinirole are DOC for syndrome
Parkinsonism MgSO4 (DOC)
Due to
Eclamptic •• First sign of toxicity is loss
high BP in
seizures
B. ANTI-CHOLINERGIC DRUGS pregnancy
of deep tendon reflexes like
patellar reflex
→ These are DOC for Drug Induced Parkinsonism •• Don’t change drug if female is
Epilepsy in already controlled on any AED
-
pregnancy •• Least teratogenic are
lamotrigine and levetiracetam
 53
Pharmacology

Lamotrigine Retigabine
–– DOC for focal seizures in elderly (along with –– Used or Focal seizures
levetiracetam)
–– Does not act on GABA
–– Side effects:
–– Can cause retinitis as side-effect.
•• Steven Johnson Syndrome Q

•• Toxic Epidermal Necrolysis Other uses of AEDs

These side effects can be avoided by gradually
increasing the dose. Bipolar disorder CBZ, Valporate, Topiramate
Migrane prophylaxis Topiramate, Valproate
Sodium Valproate Neuropathic pain Gabapentin, Pregabalin, CBZ
It can cause adverse effects like: Restless leg syndrome Gabapentin (DOC)
–– Liver damage Arrhythmias Phenytoin

–– Pancreatitis Q

–– PCOD ANTI-PSYCHOTIC DRUGS

–– Psychosis occurs due to excessive dopamine in brain.
Phenytoin
–– Anti-phychotics drug can be divided into:
Adverse Effects 1. Typical Anti Psychotics [D2 Blockers]
2. Atypical Anti Psychotics [any other mechanism;
H - Hirsutism, Hypertrophy of gums
mainly 5HT2 Blockers]
O - Osteomalacia
T - Teratogenicity [Fetal Hydantoin syndrome]
Typical Antipsychotics
M - Megaloblastic Anemia [↓ Folate]Q
1. Strong D2 #
A - Arrhythmia [Only in overdose]
L - Lymph node enlargement –– Haloperidol [Highest risk of EPS]

I - ↓ insulin (avoided in DM)Q 2. Weak D2 #

K - ↓ Vitamin K –– Chlorpromazine
A - Ataxias, vertigo [cerebellar symptoms] [only at high dose]
Side effects
Topiramate 1. Extra Pyramidal Symptoms [EPS]
–– Can cause renal stone Extra Pyramidal Symptom Drug of choice
–– Other uses of Topiratmate (COMB) 1. Dystonias [Earliest]Q Benzhexol

2. Akathisia [MC]Q Propanolol

–– Craving of Alcohol
3. Parkinsonism Benzhexol
–– Obesity
–– Migraine prophylaxis 4. Tardive dyskinesia [Very late to appear]
Q Valbenazine

–– Bipolar disorder 5. Malignant Neuroleptic Syndrome Dantrolene

Vigabatrin
2. Hyperprolactinemia
–– Dopamine ↓ prolactin by stimulating D2
receptors. Therefore, antipsychotics can cause
hyperprolactinemia due to D2 blockade.
–– Hyperprolactinemia can result in galactorrhea
and infertility
54
Cerebellum Quick Revision Notes

Atypical Anti Psychotics Interactions

Advantages Drug increasing toxicity are:

–– Lisinopril
1. Lesser risk of EPS and hyperprolactinemia
2. Effective against both Positive as well as negative –– Indomethacin
symptoms –– Thlazides

Side effects Toxicity (DAT)

– Cause lipodystrophy syndrome characterized –– Diarrhea
by –– Agitation & Incordination
•• ↑ Glucose
–– Tinnitis
•• ↑ Lipids
•• Weight gain Actions of LithiumQ
•• Insulin Resistance
L - Leucocytes
– Risk is highest with clozapine Leukocytosis
I - Increase
Clozapine
T - Tremors [MC]
→ DOC for resistant Schizophrenia
H - Hypothyroidism
→ Adverse effects are:
I - Increase
–– Agranulocytosis [Dose independent]Q Polyuria
U - Urine
–– Seizures [Dose dependent]
M - Avoided in Mothers [Lithium in pregnancy
–– Myocarditis
→ Ebstein anomaly]
–– Sedation (Most common adverse effect)
–– Sialorrhea (MC side effect)Q DEPRESSION
–– Earlier it was believed, decrease in Monoamines
ACUTE MANIA (5-HT > NA» DA) causes depression.
–– Patient is usually aggressive and violent –– Later it was linked with decrease in BDNF i.e.,
–– Rx of Acute Episode: Sedatives [Antipsychotics/ when ↑ Monoamines
BZD] + Lithium –– ↑ BDNF → ↑ Neuro Plasticity → ↓ Depression
–– Prophylaxis: Lithium is DOC.
–– Bipolar disorder: DOC is lithiumQ
ANTI DEPRESSANTS
–– Typical Anti-Depressants → Act by ↑ 5HT
Lithium –– Atypical Anti-Depressants → Act by other
mechanisms
Pharmacokinetics
–– Half-life is 24 hours Typical Antidepressants
–– Narrow Therapeutic Index These may be:
–– Given thrice a day
1. MAO - A Inhibitors

Therapeutic drug monitoring –– Moclebemide

–– For measuring plasma concentration: Sample –– Reversible inhibitors of MAO-A]Q
taken at 12 hours after last dose.
–– Plasma concentration of LithiumQ
•• Acute mania → 0.8-1.2 mEq/L
•• Prophylaxis → 0.5-0.8 mEq/L
 55
Pharmacology
–– DOC for severe depression
→ Drugs
–– Venlafaxine
–– Duloxetine
–– Milnacipran
–– Desvenlafaxine
–– Levo-Milnacipran

B. Selective Serotonin Reuptake Inhibitors

→ Drugs
–– Fluoxetine
–– Paroxetine
–– Fluvoxamine
2. Reuptake Inhibitors –– Sertraline
Non Selective Selective
–– Citalopram
–– Es-Citalopram
•• Inhibit reuptake of 5HT •• Inhibit reuptake of 5HT
and NA –– Dapoxetine → For premature ejaculationQ
•• Can be used in cardiac
•• Avoided in cardiac patients Indication of SSRI
patients •• Indicated for mild to •• SSRI are DOC for mild-moderate depression
•• Indicated For severe moderate depression
•• SSRI are DOC for all neurotic disorders like
depression –– GAD
A. Non-Selective Reuptake Inhibitors –– OCD
–– Bulimia
–– Inhibit the reuptake of both 5HT and NA –– Phobia
–– Two classes: TCA and SNRI –– PTSD
–– Impulse control disorders
(i) TCA [Tricyclic antidepressants]
–– Imipramine Adverse Effects of SSRI
–– Desipramine
–– Nausea (Most common)
–– Clomipramine
–– Amitriptyline –– Anxiety (Due to up-regulation of 5HT2
–– Nortriptyline receptors)
–– CNS: Headache, bad dreams
→ Adverse Effects:
–– Sexual:Q
•• ACh#: Dry mouth, blurred vision, C/I in glaucoma
•• α #: Postural hypotension •• Due to 5HT2 receptor stimulation
•• H1 #: Sedation •• Include
•• Seizures ○○ Anorgasmia
•• Arrhythmias
○○ Delayed ejaculation (Dapoxetine used for
•• Metabolic acidosis
Pre mature ejaculation)
→ Treatment of TCA poisoning: •• Discontinuation syndrome (Least with
•• NaHCO3 to correct metabolic acidosis and reverse Fluoxetine)Q
arrhythmiasQ

(ii) SNRI [Serotonin Noradrenaline Reuptake Inhibitors]

–– ↑ 5 HT and ↑ NA
–– Lesser adverse effects than TCAs.
56
Cerebellum Quick Revision Notes

Atypical Anti-Depressants Important Drugs:

–– Less sexual side effects Morphine is used to treat pain but it should not be
→ Drugs used to treat Biliary colic because morphine causes
spasm of sphincter of Oddi which increases the
–– Bupropion - Anti-Smoking drugQ
intra biliary pressure that can result in rupture of
–– Amineptin - ↑ Reuptake of 5-HT bile duct.Q
–– Tianeptin - ↑ Reuptake of 5-HT
–– Vortioxetine
–– Vilazodone
–– Esketamine
–– Brexanolone

Esketamine
–– Acts by blocking NMDA receptors of Glutamate
–– Used as a Nasal spray for treatment resistant
Tramadol
depression
→ Two MOA
Brexanolone/ Allopregnanolone –– Agonist at µ, k, δ receptors (opioid action)

Approved for Post-partum depression. –– ↑ 5HT and NA in spinal cord (Non-opioid action)
Naloxone cannot completely abolish the analgesic
DRUG OF ABUSE effect of tramadol and tapentadol

Opioids
Fentanyl
Morphine
–– Highly lipid soluble drugs
–– Acts on µ, K, δ Receptors
–– Stimulation of µ, K, δ Receptors cause – –– Used for anesthesia
Analgesia –– Cause Post operative muscle rigidity. It is also
known as Wooden chest syndrome
µ Receptor FunctionsQ
S - Sedation
ANTAGONISTS
→ Drugs
A – Analgesia
Naloxone - Short acting, given IVQ
C – Constipation
Naltrexone - Long acting, given Orally
R - Respiratory depression
DOC for acute Opioid poisoning → Naloxone
U - eUphoria
DOC for maintenance in opioid poisoning → NaltrexoneQ
M – Miosis
Kappa receptors cause dysphoria
 57
Pharmacology

Previous Years Questions A. Sedation B. Sudden death

C. Weight gain D. Skin rash
Q 1. An elderly male developed the symptoms of
dementia and was diagnosed as Alzheimer’s disease. Q 8. Which of the following combination of seizure and
Which neurotransmitter level is reduced in this disease? its first line drug is not correct?
A. Dopamine B. Acetylcholine A. Generalized seizure - Valproate
C. Adrenaline D. Serotonin B. Myoclonic - Phenytoin

Q 2. An elderly patient presented with tremors, rigidity C. Focal – Carbamazepine

and bradykinesia. The most likely neurotransmitter D. Absence - Ethosuximide
affected in the brain of this patient is?
Q 9. Topiramate is used for the treatment of
A. Dopamine B. GABA
A. Lennox Gastaut syndrome
C. Adrenaline D. Serotonin
B. Attention deficit hyperkinetic disorder
Q 3. Which of the following drug is the only medication
C. Treatment of migraine
useful in preventing disability progression in a patient
with primary progressive multiple sclerosis? D. Prophylaxis of heat stroke

A. Natalizumab B. Ocrelizumab Q 10. A young boy was brought to hospital with

C. Siponimod D. Rituximab complaints of few episodes of fast blinking and staring
at something for around 20 seconds. ECG shows spike
Q 4. A patient presents with tremors, rigidity and and wave pattern. Which of the following drug should
bradykinesia. Which of the following drugs can be used be used for treatment?
for the treatment of this patient?
A. Phenytoin B. Sodium valproate
A. Selegiline B. Donepezil
C. Diazepam D. Carbamazepine
C. Fluoxetine D. Haloperidol
Q11. ACTH is the treatment of
Q 5. A patient is on long term anticonvulsant therapy.
A. Juvenile myoclonic epilepsy
There is progressive contractility of visual field. The
likely anti-epileptic drug responsible for this adverse B. West syndrome
effect is C. Dravet syndrome
A. Vigabatrin B. Ethosuximide D. Lennox Gastaut syndrome
C. Phenobarbital D. Levetiracetam
Q 12. Which of the following anti-epileptic drug is used
Q 6. Least teratogenic antiepileptic drug in pregnancy in treatment of neuropathic pain ?
is 1. Gabapentin 2. Lamotrigine
A. Valproate B. Phenytoin 3. Carbamazepine 4. Pregabalin
C. Carbamazepine D. Levetiracetam
A. 1 and 2 B. 2 and 3
Q 7. A patient was started on lamotrigine 50 mg daily
C. 1, 2 and 3 D. 1, 3 and 4
for treatment of epilepsy. Gradually, the dose of the
drug is increased every 1-2 weeks to reach the final
dose of 200 mg per day. This step up titration of
lamotrigine dose is done in order to prevent or minimize
the development of
Answers
1. - B 3. - B 5. - A 7. - D 9. - A 11. - B
2. - A 4. - A 6. - D 8. - B 10. - B 12. - D
58
Cerebellum Quick Revision Notes
Q 13. A child born by normal vaginal delivery developed Q 19. A 30 year old patient was started on lithium
repeated attacks of flexion of neck over the trunk carbonate for bipolar disorder. The nurse will gave
and jerks in the hands. EEG shows the presence of instructions on adverse effects of the therapy. The
hypsarrhythmia. Anti-epileptic drug of choice for this patient should report back if the following features are
seen:
patient is?
A. Palpitations, chest pain, raised blood pressure
A. Phenobarbitone B. Phenytoin
B. Sedation, constipation, vomiting
C. ACTH D. Levetiracetam
C. Tinnitus, severe diarrhea, ataxia
Q 14. First sign of MgSO4 toxicity is D. Fever, skin rash, bradycardia
A. Loss of patellar reflex
Q 20. For plasma level monitoring, lithium estimation is
B. Respiratory distress done?
C. Cardiac arrest
A. Immediately after the dose
D. Decrease in urine output
B. 8 hours after last dose
Q 15. Which of the following adverse effect is more C. 12 hours after last dose
with oxcarbazepine as compared to carbamazepine? D. 24 hours after last dose
A. Thrombocytopenia
Q 21. A 25 year old female presented with mania.
B. Dilutional hyponatremia History revealed that her father is taking medications
C. Rash for bipolar disorder. Which of the following drug will
you prescribe for this patient?
D. Hepatotoxicity
A. Sodium valproate B. Lithium
Q 16. A patient of psychosis was being treated with
C. Carbamazepine D. Lamotrigine
risperidone. He presented to emergency with upward
fixed gaze. What will be the treatment of this patient? Q 22. Which of the following anti-depressant drug acts
A. Wait and assurance by inhibiting the reuptake of both serotonin and nor-
adrenaline?
B. Intramuscular Promethazine
C. Injection Diazepam A. Fluoxetine B. Venlafaxine

D. Injection Lorazepam C. Phenelzine D. Nortriptyline

Q 17. A patient was recently started on Fluphenazine. Q 23. A patient had a history of previous child with
down syndrome, currently on lithium therapy present
Few weeks later, he developed tremors, rigidity,
for antenatal checkup. Which of the following condition
bradykinesia and excessive salivation. First line of is the fetus at the greatest risk of?
management for this patient is
A. Ebstein’s anomaly
A. Selegiline B. Trihexyphenidyl
B. Down’s syndrome
C. Pramipexole D. Amantadine
C. Tetralogy of Fallot
Q 18. A psychotropic drug inhibiting the reuptake D. Neural tube defect
of serotonin is likely to cause which of the following
adverse effect? Q 24. A 30 year old female presented to psychiatry OPD
with symptoms of hypomania. She has a past history of
A. Visual disturbance B. Constipation mania and wants to conceive. Which of the following
drug is most teratogenic?
C. Dry mouth D. Sexual dysfunction
Answers
13. - C 15. - B 17. - B 19. - C 21. - B 23. - A
14. - A 16. - B 18. - D 20. - C 22. - B 24. - A

A. Valproate B. Lithium
C. Carbamazepine D. Olanzapine
Q 25. Which of the following is a novel antidepressant
drug?
A. Vilazodone B. Asenapine
C. Flibanserin D. Lurasidone
Q 26. Which of the following antidepressant drug should
be avoided in a patient of angle closure glaucoma?
A. Sertraline B. Amitriptyline
C. Mirtazapine D. Venlafaxine
Q 27. A patient on anti-depressant therapy presents with
elevated body temperature, dilated pupil, palpitations
and low blood pressure. ECG shows tachycardia, broad
QRS complex and right axis deviation. Which of the
following interventions must be done immediately?
A. Wait and watch
B. Intravenous sodium bicarbonate
C. Intravenous esmolol
D. DC cardioversion
Q 28. A patient on lithium therapy developed
hypertension. He was started on thiazides for
hypertension. After few days, he developed coarse
tremors and other symptoms suggestive of lithium
toxicity. Explain the likely mechanism of this interaction.
A. Thiazide inhibits the metabolism of lithium
B. Thiazides act as an add on drug to lithium
C. Thiazides increase the tubular reabsorption of
lithium
D. Thiazides cause loss of water thereby increase
lithium levels.
59
Pharmacology
Q 30. Which of the following is safe plasma concentration
of lithium for treatment of acute attack and prophylaxis
of migraine?
A. 0.6-1.2 mEq/L B. 0.6-1 mEq/L
C. 2-3 mEq/L D. 1-2 mEq/L
Q 31. A patient suffering from depression has to be
started on anti-depressant drug. Which of the following
is least likely to cause sexual side effects?
A. Venlafaxine B. Escitalopram
C. Imipramine D. Bupropion
Q 32. A 22 year old female with bipolar disorder was
on lithium therapy. Which of the following statements
about the therapy is not correct
A. Hemodialysis is not useful in lithium overdose
B. Lithium decreases thyroid function
C. Lithium toxicity is increased by thiazides
D. Lithium is avoided in pregnancy due to its teratogenic
effects
Q 33. Which of the following drug used for pain relief in
arthritis acts by both opioid and non opioid mechanisms?
A. Paracetamol B. Tramadol
C. Ketorolac D. Diclofenac

Q 29. A female patient was on lithium therapy for

bipolar disorder for 6 months. She kept the fast for
few days due to religious reasons and presented with
seizures, coarse tremors, confusion and weakness of
limbs. Which of the following should be done to diagnose
her condition?
A. Serum Electrolytes B.Serum lithium levels
C. ECG D. MRI

Answers
25. - A 27. - B 29. - A 31. - D
33. - B
26. - B 28. - C 30. - A 32. - A
 Chapter - 8 Hematology

DRUGS AFFECTING BLOOD FLOW

ANTI PLATELET DRUGS

Warfarin Overdose:
1. Aspirin Inhibit COX → ↓TXA2
2. Clopidogrel Acts on ADP •• Overdose of Warfarin causes bleeding
Ticlopidine •• Active Factors like IIa, VIIa, IXa, Xa (which are
3. Abciximab Act on GP IIb/IIIa Q Known as Four Factor complex (or) Prothrombin
Factor complex) is the Treatment of choice.Q
Tirofiban
Eptifibatide •• If Four Factor complex is not available, then fresh
frozen plasma can be used.
4. Atopaxar Act on PAR-1 receptors of
Vorapaxar thrombinQ •• If the fresh frozen plasma is also not available,
whole blood should be given
ANTI COAGULANTS •• But the Treatment of choice for bleeding tendency
due to warfarin is Vitamin K
These are divided into oral and parenteral anticoagulants
•• Vitamin K is also antidote for Warfarin overdose.
Oral Anti-Coagulants
•• Vitamin K inhibitors
2. Direct Thrombin Inhibitors
•• Direct thrombin inhibitors
•• Dabigatran - Can be given Orally and does not
•• Factor Xa inhibitor require monitoringQ

1. Vitamin K inhibitors 3. Direct factor Xa inhibitors

→ Includes dicumarol and warfarin Drugs are
Properties of Warfarin: •• Rivaroxaban RIVAR – REVERSIBLE
1. Oral anticoagulant •• Apixaban O – ORAL
2. Inhibit vitamin - K XA – XA
•• Edoxaban
B – BLOCKER (OR)
3. Takes 4-5 days to produce action •• Betrixaban AN – ANTAGONIST
4. Mainly used for maintenance purpose
5. Contraindicated in pregnancy
6. Effect of Warfarin is monitored by PT/INR
 61
Pharmacology

Injectable Anti-Coagulants FIBRINOLYTIC DRUGS

1. Indirect Thrombin Inhibitors •• All drugs in this group are tissue plasminogen
2. Direct Thrombin Inhibitors activators.
1. Indirect Thrombin Inhibitors [Heparin] •• tPA converts plasminogen to plasmin that breaks the
thrombus
UFH Activate Inhibit factor IIa = Xa
•• These are used for acute MI, acute stroke and acute
antithrombin
DVT
LMWH Activate Inhibit factor Xa > llaQ
antithrombin → Drugs
Fondaparinux Activate Only inhibits factor XaQ S – Streptokinase
antithrombin U – Urokinase
R – Reteplase
A – Alteplase
Heparins T – Tenecteplase
1. Route → S.C. or IV
2. Activate anti-thrombin Overdose of thrombolytics
3. Immediate Action → Useful in acute conditions
→ Leads to bleeding
4. Anti-coagulant of choice in pregnancy
→ Antidotes:
5. Monitoring done by a PTT
–– Epsilon Amino Caproic Acid [EACA]
6. Antidote → Protamine Sulphate
–– Tranexamic Acid.
WARFARIN HEPARIN
Route Oral S/C or IV
DRUGS AFFECTING BLOOD CELLS
MOA Inhibit vitamin K Activate AT – III
Onset 4-5 days Immediate •• Hematinics
Use Maintenance Acute condition
•• Growth factors
Pregnancy C/I DOC
Monitoring PT/INR aPTTQ HEMATINICS
Antidote Vitamin K Protamine These are nutritional substances which help in formation
2. Direct Thrombin Inhibitors (DTI) of blood. e.g.
1. Iron (Fe)
•• Bivalirudin, argatroban and melagatran are injectable 2. Folic acid (FA)
DTI.Q 3. Vitamin B12
•• Hirudin and lepirudin are not used now
Iron Deficiency Anemia
•• These are DOC for heparin induced thrombocytopenia
•• Treatment of choice is Oral iron.
(HIT)
Oral Iron
ANTIDOTES OF ANTI-COAGULANTS •• Various preparations like ferrous sulphate, ferrous
Antidote Anticoagulant fumarate are available.
Vitamin K Warfarin –– For adults, tablets are given
Protamine sulfate HeparinQ
–– For children drops are available. These should
Idarucizumab DabigatranQ
be given deep in mouth or else they cause skin
Andexanet-Alpha Factor Xa inhibitors e.g., Apixaban pigmentation
•• Earliest response - ReticulocytosisQ
•• If Hb is improving by 0.5 g/dl/week, that means
adequate response
62
Cerebellum Quick Revision Notes
•• Oral iron treatment is continued for 2-3 months Injectable Iron
even after the Hb levels come to normal to replenish
•• Preparations of injectable iron are:
the iron stores in body.
–– Iron Dextran –Can be given IV as well as IM
•• Factors affecting
–– Iron Sorbital citrate (Used IM only)
–– Ascorbic acid : Increase Absorption
•• Intramuscular iron is given by Z-tract technique to
–– Phytates and oxalates :Decrease Absorption
avoid pigmentation

HEMATOPOIETIC GROWTH FACTORS

Cells Growth Factor Drug Indications
RBC Erythropoietin Darbopoietin Anemia due to chronic renal failure
Anemia due to bone marrow suppression
WBC G-CSF Filgrastim Leukopenia due to bone marrow suppression
GM-CSF Sargramostim
Platelets IL-11 Oprelvekin Thrombocytopenia due to bone marrow suppression

Previous Years Questions

Q1. Which of the following is an oral direct thrombin
inhibitor?

A. Dabigatran B. Rivaroxaban
C. Warfarin D. Lepirudin

Q2. What is the mechanism of action of tPA?

A. Fibrinolysis
B. Inhibition of factor V and VII
C. Inhibition of factor III and V
D. Activation of anti-thrombin III

Q3. A female patient was taking warfarin for prosthetic

heart valves. She became pregnant. What advise will
you give regarding use of this drug in early pregnancy? A. Clopidogrel B. Heparin
A. Continue warfarin without any concern C. Dicumarol D. Alteplase
B. Continue warfarin but add vitamin K to the therapy Q5. A patient presented to hospital with chest pain.
C. Change warfarin to heparin ECG of the patient confirms it to be non ST elevation
myocardial infarction. Which of the following drug useful
D. Terminate the pregnancy in this patient acts by inhibiting platelet aggregation?
Q4. In the given diagram, identify drug Z marked by A. Clopidogrel B.Streptokinase
the arrow
C. Low molecular weight heparin D.Warfarin

Answers
1. - A 3. - C 5. - A
2. - A 4. - C
 63
Pharmacology
Q6. A deep vein thrombosis patient was started on an Drug A Drug B Drug C
anticoagulant therapy. Next day, the patient presented
a Aspirin Vorapaxar Prasugrel
with the features shown in the diagram below. Likely
drug implicated for this adverse effect is b Dipyridamole Eptifibatide Vorapaxar
c Aspirin Eptifibatide Prasugrel
d Dipyridamole Prasugrel Eptifibatide

Q10. Which of the following statements is most correct

regarding mechanism of action of dicumarol?

A. It acts as a calcium chelator and reduces the

A. Heparin B. Rivaroxaban availability of calcium in coagulation pathway

C. Warfarin D. Dabigatran B. It binds and activates anti-thrombin 3 that

accelerates its interaction with thrombin and factor Xa
Q7. Among the following drugs, oral factor Xa inhibitor resulting in their degradation
is: C. It acts as a Vitamin K inhibitor that results in
A. Dabigatran etexilate B. Rivaroxaban inhibition of activation of clotting factors 2,7,9 and 10

C. Fondaparinux D. Bivalirudin D. It inhibits tissue plasminogen activator resulting in

stoppage of conversion of plasminogen to plasmin
Q8. A 45 year old patient being treated with low dose
aspirin since 6 months presented with rectal bleeding.
Inhibition of which of the following substance is likely Q11. Vitamin that increases the absorption of iron from
to responsible for the bleeding? stomach is?
A. Vitamin A B. Vitamin B12
A. TXA2 B. LT
C. Vitamin C D. Vitamin D
C. Bradykinin D. PGI2
Q12. Excessive phytates intake in the diet may lead to
Q9. Mechanism of action of some antiplatelet drugs is deficiency of
shown in the given diagram. Which of the following is A. Proteins B. Iron
correct match:
C. Vitamin B12 D. Vitamin D
Q13. Indication for use of Pegylated Filgrastim is in the
correction of:
A. Anaemia B. Neutropenia
C. Thrombocytopenia D. Pancytopenia

Answers
6. - C 8. - A 10. - C 12. - B
7. - B 9. - C 11. - C 13. - B
 Chapter - 9 Gastrointestinal Tract
PEPTIC ULCER DISEASE Adverse Effects (on long-term use)
→ Due to excessive acid in stomach •• ↓ Ca2+ [Osteoporosis]
Treatment •• ↓ Vit B12 [Megaloblastic anaemia]Q

1. ↓ ACID •• ↑ Infections
→ HCl produced by Parietal cell of stomach
→ Proton Pump [H+-K+-Pump] helps in secretion of acid 2. ANTACIDS
–– Stimulated by → Fastest pain relievers of PUD
ƒƒ ACh [M1] → Include
–– AI [OH]3 → Cause constipation
ƒƒ Histamine [H2]
–– Mg [OH]2 → Cause Diarrhoea
ƒƒ Gastrin [CCK] → Given in combination
–– Inhibited by PGE2
Drugs ↓ Acid 3. ULCER PROTECTIVE DRUGS
M1 blockers H2 blockers PGE2 PPI → Sucralfate
Pirenzepine Cimetidine Misoprostol Omeprazole → Sucralfate acts by Polymerization, requires acidic
Telenzepine Ranitidine Esomeprazole pH [<4]
Famotidine Pantoprazole –– Should not be combined with antacids
Loxatidine Lansoprazole → Inhibits absorption of several drugs like
Rabeprazole phenytoin. So, a gap of minimum 120 minutes
should be kept between two drugs

Most specific drug for NSAID

MisoprostolQ
induced Peptic ulcer
DOC for NSAID induced Peptic
Proton Pump lnhibitorsQ
ulcer

PPls [Proton Pump Inhibitors]

•• Irreversible inhibitors
•• Example of Hit and Run Drugs
•• Exert systemic effect [Do not work locally]
4. ANTI-H. PYLORI DRUGS
•• Given with acid resistant coating (Enteric coating)
• Amoxycillin
• Metronidazole
Indications • Clarithromycin
• DOC for PUD due to any reason
Triple Drug Therapy
• DOC for GERD
•• Used for H. pylori associated PUD
• DOC for Zollinger Ellison Syndrome
•• PPI + 2AMA used
C → Clarithromycin Preferred triple drug therapyQ
A → Amoxycillin Given for 2 weeks

P → PPI
 65
Pharmacology

ANTI-EMETIC DRUGS PROKINETIC DRUGS

1. Chemotherapy induced nausea and vomiting (CINV):
→ Used in GERD
Type Drug of Choice
→ Drugs are
Early CINV 5HT3 antagonistsQ
- Ondansetron 1. D2 Blockers
•• Domperidone
- Granisetron
•• Metoclopramide
- Palonosetron
Delayed CINV Substance P antagonistsQ
2. 5HT4 Agonist

- Aprepitant
•• Mosapride
•• Prucalopride
- Rolapitant
3. Motilin Receptor Agonist
2. D2 Blockers •• Erythromycin

Metoclopramide DomperidoneQ
Cross BBB Do not cross BBB
Can cause dystonia Do not cause dystonia
DOC for Levodopa induced vomiting

Previous Years Questions

Q1. A patient on phenytoin for seizure disorder
was prescribed sucralfate 4 times a day for peptic
ulcer. What should be the minimum duration between
consumption of two drugs?
A. 30 min B. 60 min
C. 90 min D. 120 min
Q2. A female with ovarian cancer was on cisplatin
therapy. He presented to hospital with several episodes
of vomiting. After giving an antiemetic drug, the patient
developed dystonia. The anti-emetic drug most likely to
be responsible for these features is
Q4. A patient presented to hospital with three bouts
of vomiting and treated with anti-emetic drug. Vomiting
subsided but after sometime, he developed abnormal
movements. Which of the following drug is used for
treatment of these motor symptoms?
A. Benzhexol B. Cyproheptadine
C. L-dopa D. Hyoscine
Q5. A patient is planned to receive chemotherapy with
cisplatin. Which of the following drugs are used for
the treatment of chemotherapy induced nausea and
vomiting

A. Metoclopramide B. Meclizine A. Granisetron, aprepitant and dexamethasone

C. Ondansetron D. Scopolamine B. Metoclopramide, dexamethasone and domperidone
C. Prochlorperazine, granisetron and domperidone
Q3. Which of the following is not a prokinetic?
D. Promethazine, doxylamine and metoclopramide
A. 5HT4 agonist B. D2 blocker
C. Macrolides D. Diphenoxymethane

Answers
1. - D 3. - D 5. - A
2. - A 4. - A
 Chapter - 10 Respiratory System

BRONCHIAL ASTHMA Mechanism

→ Inhibit PDE (thereby ↑ cAMP)
→ Adenosine A1 receptor antagonistQ

Adverse effects
Due to PDE inhibition Due to ADEnosine A1 an-
tagonismQ
Nausea, Vomiting, Diarrhea Arrhythmias
Headache Diuresis
Arrhythmias Epileptic seizures
1. Bronchodilators
→ Theophylline is metabolized by microsomal enzymes,
A. Sympathomimetics so prone to drug interactions
b2 Agonists •• Enzyme inducers (like smoking) decrease the effect,
therefore smokers require higher doses
•• Enzyme inhibitors (like ciprofloxacin, clarithromycin
and erythromycin) can result in toxicity (seizures,
arrhythmias etc.)Q

Salmeterol → Slow acting → Only used for prophylaxis

2.Drugs affecting LTs
Formoterol → Fast acting → Used for acute attacks also
Adverse Effects of b2 Agonists
T - Tachycardia
T - Tremors (Most common side effect)
T - Tolerance (Mainly with long-acting beta 2 agonists)
T - T wave changes (Because of hypokalaemia)
These drugs can cause hyperglycaemia (but never
hypoglycemia)
A. Steroids

B. Parasympatholytics → DOC for prophylaxis

→ Also used in acute attack along with bronchodilators
M3 Blockers
Function in acute attack of asthma is to ↑ the
•• Ipratropium
sensitivity of b2 agonists.
•• Tiotropium
→ Preferred by inhalational route
→ Given by inhalational route
–– MC side effect is oropharyngeal candidiasis
C. Phosphodiesterase Inhibitors –– Topical Nystatin or clotrimazole is used to treat
•• Include theophylline and aminophylline candidiasis

•• Given orally or by intravenous route (not available by –– Gargling after every dose will prevent this
inhalational route) adverse effect
 67
Pharmacology
B. LOX inhibitors 4. Omalizumab
–– Zileuton → Monoclonal antibody against IgEQ

C. LT Receptor antagonists → Only used for prophylaxis

–– Zafirlukast → Given subcutaneously

–– Montelukast
GINA (GLOBAL INITIATIVE FOR
3. Mast Cell Stabilizers ASTHMA) GUIDELINES
–– Sodium Cromoglycate •• Drug of choice for treatment of acute attack
of asthma (rescue therapy) is combination of
–– Nedocromil
inhalational formoterol and low dose inhaled
→ Only used for prophylaxisQ corticosteroids.Q
→ Given by inhalational route •• Drug of choice for maintenance therapy in asthma
is also the same combination (Formoterol + Low
dose ICS).Q

Previous Years Questions

Q1. A patient was taking theophylline for bronchial Q2. A patient with COPD was given intravenous
asthma. After starting another drug, symptoms of aminophylline therapy following which the patient
theophylline toxicity started appearing. Which is the developed diuresis. This is due to action on which
likely drug started? effector?
A. Erythromycin A. Adenosine receptors
B. Phenytoin B. Beta 2 adrenergic receptors
C. Griseofulvin C. IL-10
D. Rifampicin D. Histone deacetylase

Answers
1. - A
2. - A
 Chapter - 11 Antimicrobial Agents
These drugs are used to kill or inhibit the growth of micro-organisms

CLASSIFICATION OF ANTIMICROBIALS
Based on activity

CIDAL: STATIC:
These kill the microoganisms These inhibit the growth of microorganisms.
These must be used to treat infections in These cannot be relied upon if there is immunosuppression
immunocompromised person
BEta lactams
VAncomycin
Fluroquinolones
Aminoglycosides

BE VA F A

Based on Mechanism of Action

Cell wall inhibitors Protein inhibitors Metabolism DNA gyrase Drugs acting
inhibitors inhibitors on membranes

Firmly – Fosfomycin Bind at 30S ribosomes: – Sulfonamides – Fluroquinolones – Daptomycin

Bind to – Beta lactans Aminoglycosides – Trimethoprim – Nalidixic acid – Polymyxin B
Bacterial – Bacitracin Tetracyclines – Polymyxin E
Cell – Cycloserine Bind to 50S ribosomes: – Pyrimethamine
Vall – Vancomycin Chloramphenicol
Macrolides
Clindamycin
Quinpristin
Linezolide

•• Vancomycin inhibits transglycosylase and thus chain 1. Penicillins

elongation step in bacterial cell wall synthesis.Q 2. Cephalosporins
•• Beta-lactams inhibit transpeptidase and thus cross- 3. Carbapenems
linking of peptidoglycan chainsQ 4. Monobactams

1. Penicillins
CELL WALL SYNTHESIS
INHIBITORS Penicillin G (Benzyl Penicillin)

A. BETA LACTAMS Limitations

1. Not effective orally [Acid labile]
2. Short acting [Due to rapid tubular secretion]
3. Narrow spectrum
4. Resistance
5. Allergy
 69
Pharmacology

1. Acid Resistant / Oral Penicillins –– Tazobactam + Piperacillin

V → Penicillin V (Phenoxymethyl Penicillin) B. Penicillinase Resistant Penicillins

O → Oxacillin C → Cloxacillin
D → Dicloxacillin O → Oxacillin
N → Nafcillin
K → Cloxacillin D → Dicloxacillin
A → Ampicillin, Amoxycillin O
M → Methicillin [Most resistant]

2. Prolong duration of action MRSA [Methicillin Resistant staph. aureus]

a. Probenecid competes with Penicillin for transporters
in PT → ↑ Duration of action of Penicillin
b. Depot Preparations
•• Benzathine Penicillin G → Longest acting Penicillin
•• Procaine Penicillin G
- Resistance is due to altered Penicillin Binding
Proteins
- All β-lactams are ineffective except 5th gen
cephalosporins
5. Allergy
•• Skin testing done by intradermal injection of drug

–– Depot preparations are given by IM route only •• Cross Allergy → If allergic to one penicillin, all β
lactams can cause allergy except monobactam

3. Spectrum of Penicillins Indications of Penicillins

•• Mainly against gram positive bacteria. Penicillins are First Line Drugs inQ
•• Not effective against most gram negative bacilli. L → Listeria (DOC is ampicillin)
Extended (Wide) Spectrum PenicillinsQ A → Actinomycosis
A → Ampicillin, Amoxycillin S → Syphilis
T → Tetanus
Ci → Carbenicillin
M → Meningococcus
Ty → Ticarcillin
AN → Anthrax
M → Mezlocillin
A → Azlocillin 2. Cephalosporins
P → Piperacillin 1st Gen 2nd Gen 3rd Gen 4th Gen 5th Gen
Cefazolin Cefuroxime Cefixime Cefepime Ceftibiprole

–– All of these are effective against Pseudomonas Cefalexin Cefoxitin Cefotaxime Cefpirome Ceftaroline

except ampicillin and amoxycillin Cefadroxil Cefaclor Ceftizoxime

Cefpodoxime
4. Solving problem of resistance Ceftazidime
Cefoperazone
A. b Lactamase Inhibitors Ceftriaxone

•• β-lactams break the structure of penicillin at Ceftibuten

β-lactam ring
•• Cefazolin is DOC for surgical prophylaxis
•• Clavulanic acid, sulbactam and tazobactam inhibit
•• 5th generation are effective against MRSA
these enzymes and prevent resistance
•• Combinations are: A. Cephalosporins secreted in bile
–– Clavulanic Acid + Amoxycillin •• Safe in renal failure
–– Sulbactam + Ampicillin •• Include
–– Cefoperazone
–– Ceftriaxone
70
Cerebellum Quick Revision Notes

Antimicrobial Agents That are Secreted in Bile Other Carbapenems:

Cef in ---Cefoperazone,Q Meropenem
Ertapenem
Ceftriaxone Cilastatin not required
Doripenem
The --- Tigecycline Lesser risk of seizures
Faropenem
R --- Rifampicin
E --- Erythromycin 4. Monobactam
N --- Nafcillin Only drug in the group is AztreonamQ
A --- Ampicillin
→ Do not show cross allergy
L --- Lincosamides [Clindamycin]
Disease --- Doxycycline → Effective only against Gm -ve bacteria including
Pseudomonas
B. Anti-Pseudomonal Cephalosporins
B. VANCOMYCIN
→ Include:
–– Cefepime → It is not effective orally [Not Absorbed]
–– Cefpirome Adverse Effects:
–– Cefoperazone •• When given by IV route → releases Histamine - Red
–– Ceftazidime [Most effective anti-Pseudomonal man syndromeQ
cephalosporin]Q •• Nephrotoxic
•• Ototoxic
C. Disulfiram Like Reaction
Indications
→ Should not be given with alcohol
•• DOC for MRSA infections
→ Include:
•• Can be used for Pseudomembranous Colitis (Now
•• CefoperazoneQ
DOC is fidaxomicin)
•• Moxalactam
•• Not effective against PseudomonasQ
D. Hypoprothrombinemia (↓ Prothrombin) DOC for MRSA : Vancomycin
→ ↑ Bleeding tendency DOC for VRSA : Daptomycin
→ ↑ Risk of bleeding with warfarin DOC for VRSA pneumonia : Linezolide
→ Avoided in hemophilia patients
→ Include: PSEUDOMEMBRANOUS COLITIS
•• Cefoperazone •• It is a type of superinfection
•• Moxalactam
•• MC bacteria involved: Clostridium difficile
3. Carbapenems •• MC antimicrobials implicated are:
Imipenem: –– 3rd Gen. Cephalosporins > Clindamycin > Ampi or
•• Effective against Gram (+), Gram (-) and Anaerobes Amoxycillin > FQQ
Treatment:
•• Always given with Cilastatin because if given alone
it is broken down by dehydropeptidase enzyme in DOC : Fidaxomicin (Low chances of relapse)Q
the Kidney Alternative : Oral vancomycin, Metronidazole
•• Imipenem is a broad spectrum antibiotic, it is also
Monoclonal Ab against toxin : Bezlotoxumab
effective against Pseudomonas.
Side effect : Seizures
Contraindication : Epileptic patientsQ
 71
Pharmacology

PROTEIN SYNTHESIS INHIBITORS Uses

→ Drugs inhibit protein synthesis by binding to 30S or S – SIADH [Demeclocycline]
50S
R – Rickettsia [DOC]
→ It is rememberred as buy AT - 30, SELL @ 50
I – Granuloma lnguinale
–– Aminoglycosides and Tetracyclines bind at 30S
ribosomes L – LGV
A – Atypical pNeumonia [DOC – Macrolides]
–– Rest all (streptogramins, Erythromycin group,
Linizolid and Lincosamides) bind at 50S ribosomes N

Aminoglycosides K – Cholera [DOC]

A – Luminal Amoebiasis [DOC For amoebiasis →
Drugs Metronidazole]
–– Streptomycin
–– Gentamicin
Resistance:
–– Amikacin •• Due to development of efflux pumps
General Properties Streptogramins
•• Not effective orally [Not absorbed] → Quinpristin + Dalfopristin
•• Active mainly on Gm -ve [Including Pseudomonas] → Can be used for VRSA
•• Not effective on anaerobic bacteria
Macrolides
•• Cidal drugs (Only protein synthesis inhibitors which
–– Erythromycin
are cidal)
–– Clarithromycin
•• These are nephrotoxic, ototoxic and can cause
neuromuscular blockade –– Roxithromycin
–– Azithromycin
Tetracyclines
- Demeclocycline Indications

- Doxycycline DOC forQ

- Minocycline C: Chancroid, Corynebacterium

L: Legionella
Adverse Effects
A: Atypical Pneumonia
K – Kidney Failure – All are C/I except Doxycycline
P: Pertussis
A - Anti-anabolic
P – Phototoxic
Linezolide
I – Insipidus diabetes (Inhibit ADH release)
•• DOC for VRSA pneumoniaQ
L – Liver Failure C/I
•• Now approved for TB also
D – Dentition and Bone problems
•• It is a static drug, so not reliable in immunocompromised
(C/I in pregnancy and children < 8 years)Q patients
E – Not t o be given after Expiry
Lincosamides (Clindamycin)
[Risk of Fanconi Syndrome]
•• Secreted in Bile, so safe in renal failure
V – Vestibular dysfunction
•• Causes Pseudo membranous colitis
•• Used in anaerobic bacterial infections
•• DOC for lung abcess and brain abscessQ
72
Cerebellum Quick Revision Notes

ANTIMETABOLITES Fluoroquinolones
Drugs:
A. Sulfonamides/Sulfa Drugs
•• Norfloxacin
–– Sulfadoxine
•• Ofloxacin
–– Sulfasoxazole •• Ciprofloxacin
–– Sulfamethoxazole •• Levofloxacin
–– Sulfadiazine •• Moxifloxacin
–– Dapsone
General Properties
Adverse Effects •• Oral cidal drugs
A – Aplastic anemia
B - Bilirubin displacement → Cause Kernicterus in •• Wide spectrum [Effective against Gm + ve as well as
Gm -ve]
newbornQ
C - Crystalluria •• C/I in pregnancy and children (<18 yrs) [Cause
R - Rash cartilage and tendon damage]Q
A – Acetylation •• Induce seizures [Avoided in Epilepsy]
S – SLE
H – Hemolysis in G6PD deficiency •• C/I in Renal Failure

•• Sulfonamides are structural analogs of PABA, which ExceptionQ

is essential for synthesis of folic acid. Therefore,
P – Pefloxacin Safe in renal failure
sulfonamides are competitive inhibitors of FA
M – Moxifloxacin Avoided in liver disease
synthase enzyme.
T – Trovafloxacin Not effective in UTI
•• In any infection, where pus is present, which usually
contains PABA, Sulfonamides are unlikely to be Respiratory FQQ
effective.
O – Ofloxacin
B. Combinations M – Moxifloxacin
G – Gatif loxacin
1. Cotrimoxazole Levofloxacin [Isomer of Ofloxacin, Long acting]
Trimethoprim (T) + Sulfamethoxazole (S)
•• Ratio for best bactericidal activity → 1: 20 (T:S) These are active against respiratory infections caused
by
•• Ratio in tablet to attain this ratio → 1: 5 (T:S)
•• Gm +ve bacteria
Cotrimoxazole is DOC For
•• Gm -ve bacteria
P → Pneumocystis jiroveci
•• Atypical bacteria
N → Nocardia
B → Burkholderia cepacian •• Mycobaterium TB

2. Sulfadoxine + Pyrimethamine DRUGS NOT EFFECTIVE AGAINST

•• Indicated in Parasitic infections → Malaria
PARTICULAR BACTERIA
→ Toxoplasmosis Bacteria Resistant to DOC
1. Mycoplasma Cell wall inhibitors Macrolides
DNA GYRASE INHIBITORS 2. MRSA Beta lactams Vancomycin
•• DNA Gyrase - Introduces negative supercoils and Aminoglycoside +
3. Pseudomonas Vancomycin
helps in replication. Ceftazidime
•• DNA gyrase Inhibitors inhibit replication by 4. Enteric fever Aminoglycosides Ceftriaxone
preventing uncoiling. 5. Anaerobes Aminoglycosides Metronidazole

•• The drugs are fluoroquinolones

 73
Pharmacology

TUBERCULOSIS Other First Line Drugs

FIRST LINE DRUGS •• Pyrazinamide causes gout
H → Isoniazid •• Ethambutol causes red-green color blindness (optic
R → Rifampicin [RCIN] neuritis)
Z → Pyrazinamide
E → Ethambutol SECOND LINE DRUGS
S → Streptomycin (Not first line now) A. Cidal Drugs
1. FQ
Activity Bacteria Hepatotoxic Pregnancy
H Cidal Both √ Safe
•• Ofloxacin
R Cidal Both √ Safe •• Moxifloxacin
Z Cidal i/c √√√ Avoided •• Gatifloxacin
E Static Both X Safe •• Levofloxacin
S Cidal e/c X C/I
2. Injectable
lsoniazid (INH) •• Capreomycin
•• INH is activated by catalase peroxidase (formed by •• Kanamycin
Kat G)Q enzyme of mycobacteria. It acts by inhibiting •• Amikacin
the formation of mycolic acid.
•• Streptomycin
•• Causes pyridoxine (Vitamin B6) deficiency resulting
in peripheral neuropathy. So, pyridoxine is used for
treatment as well as prevention B. Drugs used for other conditions, now
approved for TB
•• Hepatotoxic (INH: lsoniazid causes Neuropathy
and Hepatotoxicity)Q 1. Linezolide – Also used for VRSA
2. Clofazimine – Also used for multibacillary leprosy
Rifampicin
C. Other static drugs:
•• Act by inhibiting RNA polymerase of mycobacteria
by binding to its β-subunit. It thus inhibits 1. Cycloserine – Causes neuropsychiatric adverse effects
transcription.
2. Ethionamide – Hepatotoxic
•• Should be given on empty stomach
3. PAS – Causes hypothyroidism
•• Secreted in Bile → Safe in renal failure
4. Thioacetazone – Never given in HIV patients
•• Enzyme Inducer

D. New drugs:
Interactions
Replace with
1. Bedaquiline
Warfarin Heparin 2. Delamanid
Replace with
OCP Other contraceptive method 3. Pretomanid

Other Uses: TREATMENT OF TUBERCULOSIS (NTEP)

•• Leprosy Drug Sensitive TB:
2HRZE + 4 HRE
•• Effective against Gram positive bacteria (including
MRSA)
•• Effective against Gram negative bacteria (including
Pseudomonas)
74
Cerebellum Quick Revision Notes
Drug Resistant TB LEPROSY
Multi drug (MDR) Resistant to H+R Rifampicin 600 mg Once monthly Supervised
Rifampicin resistance Resistant to R but sensitive to H Clofazimine 300 mg Once monthly Supervised
Pre-XDR Resistant to H + R + FQ Clofazimine 50 mg Once daily for Unsupervised
Extensive (XDR) Resistant to H + R + FQ + One of 28 days
Bedaquiline or Linezolide Dapsone 100 mg Once daily for Unsupervised
For TB with HIV 28 days
Above regimen is given for
–– First start treatment of TB (ATT)
– 12 months in multi-bacillary leprosy
–– After 2 weeks, start treatment of HIV (ART) – 6 months in pauci-bacillary leprosy
Lepra Reactions
–– DOC for both type 1 and type 2 Lepra reaction
is steroids
–– MDT for leprosy should continueQ

ANTI-HIV DRUGS

1. Fusion Inhibitors A. Competitive RTI

Enfuvirtide Maraviroc NRTI (Nucleotide or side RT inhibitors)

• Binds with GP 41 of Envelope • Binds with Nucleoside RTI Nucleotide RTI

and Fusion of Virus with T CCR-5
cell is Inhibited Zidovudine Tenofovir
Lamivudine
• Given subcutaneously • Given orally
Stavudine
Didanosine
2. Reverse Transcriptase Inhibitors(RTI)
Zalcitabine
→ Inhibit reverse transcriptase (RNA dependent Emtricitabine
DNA polymerase) Abacavir
→ May be competitive (NRTI) or Non-competitive
(NNRTI)
 75
Pharmacology

NRTI Adverse Effect CLINICAL MANAGEMENT OF HIV

Zidovudine Bone Marrow SuppressionQ 1. Treatment of HIV
Abacavir MI
Zalcitabine Aphthous ulcers in mouth •• Called HAART (Highly Active Anti Retro Viral
Emtricitabine Pigmentation of palms and soles Therapy)
Didanosine Maximum risk of pancreatitis
Stavudine Maximum risk of peripheral neuropa- •• Should be given to All HIV positive patients
thy irrespective of CD4 count
•• Given for life long duration
B. Non-Competitive RTI (NNRTI)
•• Minimum 3 drugs (from minimum 2 groups) should
–– Efavirenz be used
–– Nevirapine •• First line therapy is
–– Delavirdine –– 2 NRTI +1 NNRT/ integrase Inhibitors
3. Integrase Inhibitors –– Commonly used – T + L + E or T + L + DQ
→ Can be given orally [T – Tenofovir, L – Lamivudine, E – Efavirenz, D –
Dolutegravir]
→ One of the first line drugs for HIV now.Q
→ Drugs include
2. Post exposure prophylaxis
–– Raltegravir
→ To prevent development of HIV after exposure
–– Elvitegravir
→ Used commonly in health care workers
–– Dolutegravir
→ Should be started as early as possible after
exposure (within maximum limit of 72 hours)
4. Protease Inhibitors
•• Ritonavir → Should be given for 28 days (4 weeks)Q

•• Lopinavir → All the drugs are given orally

•• Amprenavir → Drugs: Tenofovir +Lamivudine + ProteaseQ

Inhibitors (or integrase inhibitors)
•• Fosamprenavir
•• Atazanavir
ANTI-INFLUENZA DRUGS
•• Saquinavir
Uncoating Neuraminidase inhibitors
•• Nelfinavir
Inhibitors
•• lndinavir
Amantadine Inhibit release of virus from cell
Properties of Protease Inhibitors Rimantadine •• Oseltamivir - Oral
•• Substrates of CYP3A4 •• Zanamivir - Inhalation
•• Inhibitors of CYP 3A4 •• Peramivir - Parenteral
–– Strongest is ritonavirQ D.O.C for Bird flu (H5N1) and Swine
flu (H1N1)
–– Boosts the effect of other protease inhibitors
•• Cause lipodystrophy syndrome ANTI-HERPES VIRUS DRUGS
–– ↑ Glucose •• HSV-1 •• Mucocutaneous Herpes and Herpes
–– ↑ Lipids Encephalitis
–– Insulin resistance •• HSV-2 •• Genital Herpes

–– Weight gain •• VZV •• Chicken pox

•• DOC for all of them is ACYCLOVIR
•• Ganciclovir is DOC for CMV.
76
Cerebellum Quick Revision Notes

ANTI-HEPATITIS VIRUS DRUGS ANTIFUNGAL DRUGS

Hepatitis B 1. TOPICAL ANTIFUNGAL DRUGS:
L : Lamivudine → Used for dermatopytosis e.g. azoles
E : Emtricitabine
→ Used for steroid induced oropharyngeal candidiasis
T : Tenofovir (DOC) e.g. nystatin, clotrimazole

Hepatitis C Drugs:
→ Previously treated with interferon and ribavirin C : Ciclipirox olamine
A : Azoles, Amorolofine
→ Treatment was very toxic
T : Terbinafine
→ Now all oral treatment is used
Sertaconazole (Has anti-inflammatory and
New Oral Drugs for Hepatitis C anti-pruritic activity)

Protease NS 5A Inhibitors NS 5B Inhibitors 2. SYSTEMIC ANTIFUGAL DRUGS

Inhibitors
DRUG MECHANISM USE
Previrs Asvirs Buvirs
Inhibit DOC for Candidasis
Telaprevir Elbasvir Sofosbuvir lanosterol is fluconazole
Azoles
14-a- DOC for Aspergillosis
Simprevir Ledipasvir Dasabuvir
demethylase is voriconazoleQ
Boceprevir Daclatasvir Beclabuvir
Bind to Mucormycosis (DOC)
Grazoprevir Ombitasvir
Amphotericin ergosterol Cryptococcal
Paritaprevir Pimbrentasvir -B and create meningitis (DOC)
pores Kala azar (DOC)
DRUGS FOR COVID-19
Inhibit
•• Caused by Novel corona virus Dermatophytosis
Terbinafine squalene
(DOC)
•• Most cases are self-limiting epoxidase
Important drugs Inhibit
Griseofulvin mitotic Dermatophytosis
1. Steroids spindle
•• Only life saving drugs in COVID-19 pneumonia. With AMB for
Inhibit DNA
•• Safe in children 5-Flucytosine cryptococcal
Polymerase
•• Increase the risk of infections like mucormycosis meningitis
2. Remdesivir Cell wall Candidasis
Caspofungin
inhibitorQ Aspergillosis
•• Inhibit RNA dependent RNA polymerase.Q
Note: AMB is nephrotoxic but Liposomal AMB is less
•• Given intravenously.
nephrotoxic
•• Effective in first 10 days of illness only.
•• Given with steroids (or baricitinib).
•• Only US-FDA approved drug for COVID-19
pneumonia.
3. Monoclonal antibodies against spike protein
•• Drugs include Bebtelovimab
•• Indicated for OPD treatment
•• Decrease risk of hospitalization.
 77
Pharmacology

ANTI-PARASITIC DRUGS AMOEBIASIS

MALARIA Drug of Choice
•• Caused by Plamodium Luminal amoebiasis Diloxanide Furoate (or
•• Transmitted by female Anopheles (Carrier state) Paromomycin)Q
Intestinal and Hepatic Nitroimidazole (Nidazole) e.g.
Treatment of Malaria
amoebiasis Metronidazole, Tinidazole,
DOC in 1st Secnidazole, Ornidazole,
Type of Malaria DOC Satranidazole
Trimester
P. vivax malaria Chloroquine Chloroquine *Nidazoles can cause disulfiram like reaction, so are
C/I in alcoholics
P falciparum malaria ACT Quinine
Complicated or USES OF METRONIDAZOLE:Q
IV
severe or cerebral IV Artesunate G - Giardiasis, Gardnerella vaginalis (bacterial
Artesunate vaginosis)
Malaria
U - Ulcer (Peptic ulcer)
Artemisinin Combination Therapy [ACT]
P - Pseudomembranous colitis
•• Artemisinin + Long acting drug
•• DOC for chloroquine resistant malaria T - Trichomoniasis

•• Given orally A - Amoebiasis, Anaerobic bacterial infections

•• Lumefantrine + Artemether: DOC in North Eastern
States
•• Artesunate + Sulfadoxine - Pyrimethamine : DOC for
rest of India

Radical Cure
•• For P.vivax Malaria
•• DOC is primaquine
•• Given for 14 days
•• C/I in G-6-PD deficiency, pregnancy and infants
•• Tafenoquine is single dose radial cure of P.vivax
malaria
78
Cerebellum Quick Revision Notes

Previous Years Questions

Q1. The given diagram shows the steps in formation of bacterial cell wall. Identify the site of action of beta
lactam antimicrobials:

Q2. Which of the following cephalosporins can increase A. Cilastatin prevents degradation of Imipenem in kidney
the effect of warfarin resulting in raised INR and
increased risk of bleeding? B. Cilastatin increases absorption of Imipenem
C. Inhibits the enzymes that digest Imipenem in stomach
A. Cefoperazone B. Cefixime
D. Reduces side effects of Imipenem.
C. Ceftibiprole D. Ceftazidime
Q5. Mechanism of resistance to penicillins via beta
Q3. Carbapenem with maximum seizure risk is: lactamase is
A. Imipenem B. Meropenem A. Altered penicillin binding proteins
C. Ertapenem D. Doripenem B. Drug efflux
Q4. Cilastatin is given in combination with Imipenem C. Breaks drug structure
because: D. Alteration in 50S ribosome structure

Answers
1. - D 3. - A 5. - C
2. - A 4. - A
 79
Pharmacology
Q6. A patient presented with hospital acquired A. Rifampicin B. Ethionamide
pneumonia. On testing he was found to be allergic to
C. Vancomycin D. Acyclovir
penicillin G. Which of the following drug is likely to be
safe in this patient?
Q14. All of the following are bactericidal drugs against
A. Ceftriaxone B. Ampicillin Mycobacterium except
C. Aztreonam D. Imipenem A. Kanamycin B. Thioacetazone
C. Rifapentine D. Isoniazid
Q7. Mechanism of action of doxycycline is
A. DNA gyrase inhibitor Q15. Which of the following drug will you omit from
the prescription of a patient with XDR tuberculosis in
B. Cell wall synthesis inhibitor pregnancy?
C. Protein synthesis inhibitor
A. Kanamycin
D. DNA dependent RNA polymerase inhibitor
B. Ethambutol
Q8. Drug of choice for Legionnaire’s disease is: C. Moxifloxacin
A. Azithromycin B. Tigecycline D. Amoxycillin-clavulanic acid
C. Streptomycin D. Amoxycillin Q16. From the given diagram, identify the mechanism
of action of isoniazid.
Q9. Which of the following antimicrobials is
contraindicated in a patient with seizure disorder? A. Drug A B. Drug B
A. Ampicillin B. Ofloxacin C. Drug C D. Drug D
C. Doxycycline D. Cefixime

Q10. A pregnant female with urinary tract infection took

antimicrobials for the same. The baby of this female
developed tendon rupture and arthropathy. What is
the likely mechanism of action of the antimicrobial
consumed by the pregnant female?
A. Folic acid synthesis inhibitor
B. Mycolic acid synthesis inhibitor
C. DNA gyrase inhibitor
D. DNA inhibitor

Q11. Drug of choice for prophylaxis against Diphtheria

is
A. Erythromycin B. Rifampicin
Q17. A 48 year old patient presented to OPD with
C. Cloxacillin D. Ciprofloxacin tingling and numbness of fingers. The patient is chronic
alcoholic and was recently started on antitubercular
Q12. Fluoroquinolone contraindicated in liver disease is treatment. What should be the treatment of this
patient?
A. Levofloxain B. Pefloxacin
C. Ofloxacin D. Lomefloxacin A. Vitamin B3 B. Vitamin B6
C. Vitamin B1 D. Vitamin B12
Q13. Which of the following is a second line anti-
tubercular drug?

Answers
6. - C 8. - A 10. - C 12. - B 14. - B 16. - A

7. - C 9. - B 11. - A 13. - B 15. - A 17. - B

80
Cerebellum Quick Revision Notes
Q18. In MDR tuberculosis, which of following drug Q22. A patient developed COVID-19 pneumonia and
combinations show resistance? was treated. Few months later, patient presented with
nasal congestion and swelling of face. There were black
A. Rifampicin and Fluoroquinolones lesions on the nose bridge. A diagnosis of mucormycosis
B. Isoniazid and rifampicin was made. What is the drug of choice for this condition?
C. Isoniazid and Pyrazinamide A. Fluconazole B. Dexamethasone
D. Rifampicin and kanamycin C. Amphotericin B D. Azithromycin

Q19. Which of the following drug acts by inhibiting the Q23. Mechanism of action of Triazoles anti-fungal
transcription of DNA to RNA? drugs is:
A. Rifampicin B. Nitrofurantoin A. Inhibits ergosterol biosynthesis
C. Ciprofloxacin D. Novobiocin B. Inhibits tubulin
C. Inhibits glucan synthesis
Q20. A female taking oral contraceptives acquired
tuberculosis. After prescribing anti-tubercular D. Inhibits cell wall synthesis
therapy, physician advised the patient for alternative
contraception. What is the probable reason of this Q24. Drug of choice for invasive aspergillosis is
advise?
A. Posaconazole B. Voriconazole
A. Rifampicin causes teratogenicity
C. Liposomal AMB D. Caspofungin
B. Isoniazid is teratogenic
Q25. An HIV patient presents with seizures and neck
C. Rifampicin increases the metabolism of oral contraceptives
rigidity. The CSF examination shows the presence of
D. Oral contraceptives decrease the efficacy of ATT organisms on India ink and a diagnosis of cryptococcal
meningitis is made. Which of the following anti-fungal
Q21. A patient of borderline leprosy received multi drug is used for initial treatment of this meningitis?
drug therapy. He developed skin lesions as shown in the
figure below. How should this patient be managed? A. Liposomal amphotericin B
B. High dose fluconazole
A. Stop MDT and give thalidomide
C. Fluconazole + 5 Flucytosine
B. Continue MDT and give thalidomide
D. Voriconazole
C. Stop MDT and give steroids
D. Continue MDT and give steroids Q26. Which of the following drugs can be used for the
treatment of severe covid-19 pneumonia in children?
A. Steroids B. Remdesivir
C. Ivermectin D. All of these

Q27. A newly diagnosed tuberculosis patients was found

to be HIV positive. Which of the following statement is
true about treatment of this patient?
A. Start ATT and ART together
B. ART should be started only if CD4 count is less than 50/mcL
C. ATT should be started first followed by ART 2 weeks later
D. ART should be started first followed by ATT 2 weeks later

Answers
18. - B 20. - C 22. - C 24. - B 26. - A
19. - A 21. - D 23. - A 25. - A 27. - C
 81
Pharmacology
Q28. Which of the following drugs improves Q34. A 30 year old man travelled to Assam. After
bioavailability and prolongs duration of action of coming back he developed fever, chills and rigors and
Saquinavir? altered sensorium. The peripheral smear demonstrated
the presence of P. falciparum. What is the treatment
A. Ritonavir B. Cimetidine of choice for this patient?
C. Vitamin C D. Remdesivir
A. Chloroquine, Sulfadoxine pyrimethamine
Q29. Mechanism of action of Remdesivir is inhibition B. Intravenous Artesunate
of?
C. Quinine
A. RNA dependent RNA polymerase D. Primaquine
B. DNA dependent RNA polymerase
Q35. A 25 year old male has frequent visits to rural
C. Viral protease enzyme areas and need to eat outside food. During one such
D. Cell wall synthesis visit, he developed loose stools. Which of the following
drug should be used to manage this case?
Q30. Mechanism of action of Oseltamivir is A. Metronidazole B. Diphenoxylate
A. DNA polymerase inhibition C. Loperamide D. Octreotide
B. Inhibition of viral mRNA
Q36. A female patient presented with greenish vaginal
C. Blocking viral uncoating discharge and pruritus. On colposcopy, strawberry
D. Neuraminidase inhibition cervix is noted. What is the drug of choice for this
condition?
Q31. Which of the following drug is associated with A. Ceftriaxone B. Metronidazole
causation of pigmentation of hand and soles on chronic
use? C. Acyclovir D. Fluconazole

A. Emtricitabine B. Nevirapine Q37. The drug kit shown in the diagram below is used
C. Zidovudine D. Abacavir for the treatment of
A. Malaria B. Kala azar
Q32. A lady has taken medication of ameiobiasis
infection . In a party she drank alcohol. She has nausea C. HIV D. Syphilis
vomiting and dizziness . Which anti-amoebic drug could
have lead to interaction with alcohol to produce these
symptoms?
A. Metronidazole B. Nitazoxanide
C. Paromomycin D. Diloxanide

Q33. A female patient presented with greenish vaginal

discharge. Clue cells were present and Whiff test was
positive in vaginal discharge. What is the drug of choice
for this condition? Q38. Which of the following drug has highest risk
of causing hemolysis in a patient with deficiency of
A. Doxycycline B. Metronidazole Glucose-6-Phosphate Dehydrogenase enzyme?
C. Ceftriaxone D. Fluconazole A. Primaquine B. Chloroquine
C. Azithromycin D. Pyrimethamine

Answers
28. - A 30. - D 32. - A 34. - B 36. - B 38. - A
29. - A 31. - A 33 - B 35. - A 37. - A
 Chapter - 12 Anti-Cancer Drugs
Anticancer drugs can be divided into Hemorrhagic cystitis
a. Cytotoxic
•• Caused by cyclophosphamide and ifosmide.
b. Targeted
•• Metabolite responsible is acrolein
CYTOTOXIC DRUGS •• Prevented by mesnaQ
Common Adverse Effects
•• Treatment is steroids.
•• BM Suppression
Drugs Causing Pulmonary FibrosisQ
•• Alopecia
•• Mucositis → Diarrhea CYCLOphosphamide :

•• Hyperuricemia
CARmustine :
•• Nausea and vomiting (CINV)
BUSulphan :
1. Alkylating Agents
MethoTRUCKsate :
Drugs:
(Methotrexate)
If – lfosfamide
Bus – Busulfan AmioDaRONE :
Not – Nitrosoureas
• Carmustine (BCNU) BLEOmycin :
• Lomustine (CCNU)
• Semustine (Methyl CCNU)
Present – Procarbazine
Take – Temozolomide 2. Antimetabolites
My – Melphalan, Mitomycin C •• These are S Phase Specific
Cycle – Cyclophosphamide
a. Drugs affecting Folic Acid Metabolism
Important Points Regarding Alkylating Agents •• Example: Methotrexate
Cyclophosphamide Cause Hemorrhagic cystitisQ •• Act by inhibiting dihydrofolate reductase enzyme.
Cause Pulmonary fibrosis
Uses of Methotrexate:
Ifosfamide Cause Hemorrhagic cystitis
•• Choriocarcinoma - D.O.C
Busulfan Cause pulmonary fibrosis
•• Rheumatoid arthritis - D.O.C
Nitrosoureas Cause Delayed neutropenia
Procarbazine Cause disulfiram-like –– Methotrexate toxicity treatment- Folinic acid
reaction (Leucovorin or Citrovorum)
Temozolomide DOC for gliomas
Melphalan Used for multiple myeloma b. Drugs Affecting Purine Metabolism
Mitomycin-C Used topically for 6-Mercaptopurine Hepatotoxic
*Subglottic stenosisQ
*Superficial bladder cancer 6 - Thioguanine Hepatotoxic
Cladribine DOC for Hairy cell LeukamiaQ
Fludarabine DOC for CLLQ
 83
Pharmacology

c. Drugs Affecting Pyrimidine Metabolism

5-Fluorouracil Cause Hand and foot syndrome

[5-FU]
Capecitabine Proding
Gemcitabine DOC for Pancreatic carcinoma
Cytarabine Cause cerebellar side effects

3. Drugs Acting on Mitotic Spindle

→ Specific for M-Phase of cell cycle
Formation inhibitors Breakdown inhibitors
Vincristine
PaclitaxelQ
Vinblastine
S/E → Peripheral neuropathy
SIADH

Vincristine → Marrow sparing anticancer drug

4. Topoisomerase Inhibitors
Topoisomerase I inhibitors Topoisomerase II inhibitors
Irinotecan Etoposide
→ Used for colorectal Anthracyclines
TARGETED ANTICANCER DRUGS
carcinoma •• Doxorubicin
→ Cholinergic Side •• Donorubicin A. SMALL MOLECULES
effects 1. Tyrosine Kinase Inhibitors
•• Epirubicin

Anthracyclines – Cause Cardiotoxicity

5. Miscellaneous Drugs
a. Bleomycin
DOC for Chronic Myeloid Leukemia – Imatinib
•• Marrow sparing
•• Cause pulmonary fibrosis General Properties
1. All end with ‘nib’
•• Causes Flagellated pigmentation of skinQ
2. Orally effective
b. L-Asparaginase Important Tyrosine Kinase Inhibitors
•• Marrow sparing For CMLQ
I - Imatinib [DOC]
•• Used for ALL
N- Nilotinib
•• Cause Allergy D- Dasatinib
•• Cause Acute PancreatitisQ •• Imatinib is DOC for CML and GIST
•• Sorafenib is DOC for hepatocellular carcinoma
•• Lapatinib is used for breast cancerQ
84
Cerebellum Quick Revision Notes

B. MONOCLONAL ANTIBODIES Drugs:

→ End with ‘MAB’ Mnemonic DrugQ Use
→ Injectable Anticancer Drugs New Nivolumab HL, NSCLC
EGFR ANTAGONISTS: Drugs Durvalumab
Act Avelumab
•• Cetuximab: Colorectal carcinoma At Atezolizumab
•• Panitumumab: Colorectal carcinoma Immune Ipilimumab
Check Cemiplimab
MAB AGAINST HER – 2 Point Pembrolizumab Multiple cancers including
•• Trastuzumab endometrial cancer
• Used for breast cancer
•• Pertuzumab • Cardiotoxic
IMMUNOSUPPRESSANTS
1. STEROIDS
MAB AGAINST CD20
2. DRUGS TARGETING THE CALCINEURIN
•• Rituximab : For Non-Hodgkin Lymphoma and CLL
PATHWAY

IMMUNE CHECK POINT

INHIBITORS
•• Normally, T-cells are not activated against normal a. Cyclosprine and
cells because an interaction between PD-1 (receptor Tacrolimus
present on T-cells) and PDL-1 (Ligand present on b. Daclizumab and
normal cells) inhibit T-cells. This is called immune Basiliximab
check point. Tumor cells do not express PDL-1 and c. Sirolimus
thus can be killed by T-cells.
•• Some tumor cells start expressing PDL-1 on their
surface and thus can evade immunity by inhibiting
T-cells.
a. Cyclosporine and TacrolimusQ
•• Immune check point inhibitors are monoclonal •• Inhibit formation of IL-2
antibodies against PD-1 or PDL-1 to stop this
b. Sirolimus and Everolimus
interaction. T-cells now can kill cancer cells.
•• Inhibit action of IL - 2
•• These drugs can result in auto-immune conditions
like autoimmune hepatitis as adverse effects. 3. BIOLOGICAL AGENTS
Formed by recombinant DNA technology
TNF-α inhibitors
A – Adalimumab
C – Certolizumab
E – Etanercept
INhibitor – INfliximab
GOLI – GOLImumab
 85
Pharmacology

Previous Years Questions

Q1. Drug of choice for treatment of hairy cell leukemia is? Q4. A 20 year old boy presented with slow growing mass
on the medial side of thigh. Investigations revealed
A. Interferon alpha
it to be osteosarcoma and patient was started on
B. Fludarabine methotrexate. Mechanism of action of methotrexate
C. Pentostatin as an anticancer drug is
D. Cladribine A. Inhibition of Dihydrofolate reductase
B. Inhibition of N5 tetrahydro folate reductase
Q2. Which of the following drug can cause the side-
effect given in the picture? C. Inhibition of tyrosine kinase
D. Inhibition of purine metabolism
A. Bleomycin
B. Mitomycin C Q5. Topical application of 400 mcg/ml mitomycin C is
C. Doxorubicin used for
D. Actinomycin D A. Subglottic stenosis
B. Tympanoplasty
C. Rhinocerebral mucormycosis
D. Nasopharyngeal bleeding

Q6. Which of the following is not an immune check point

inhibitor?
A. Cetuximab
B. Pembrolizumab
C. Atezolizumab
D. Nivolumab

Q7. Which of the following is true about Rituximab

A. Anti- CD 20, monoclonal antibody

Q3. A 50 year old female presented to oncologist with B. Anti-CD 50, monoclonal antibody
breast lump. On examination and investigations, breast C. Anti-CD 20 polyclonal antibody
cancer was diagnosed. Echocardiography of the patient D. Anti-CD 50 polyclonal antibody
shows ejection fraction of 25 %. Which of the following
drug will you avoid in this patient? Q8. What is mechanism of action of Cyclosporine?
A. Epirubicin A. Calcineurin inhibitor
B. Irinotecan B. mTOR inhibitor
C. Cyclophosphamide C. IL-2 receptor antagonist
D. Methotrexate D. TNF-α inhibitor

Answers
1. - D 3. - A 5. - A 7. - A
2. - A 4. - A 6. - A 8. - A
 Chapter - 13 Anaesthesia
LOCAL ANAESTHETIC AGENTS Non Depolarizing Muscle Relaxants
(NDMR)
Drugs
•• Act by blocking NM receptors competitively
Ester Amide
•• Example is d- Tubocurarine (Curare)
Cocaine Lignocaine
•• It does not cause post opeartive muscle pain
Procaine Bupivacaine
Chlorprocaine Prilocaine •• Release Histamine that causes bronchoconstriction
and hypotensionQ
Tetracaine Etidocaine
Benzocaine Ropivacaine
Other NDMR
Dibucaine
Curium [Release less Curonium [No histamine
Special points: histamine] released]
•• Only LA causing vasoconstriction CocaineQ Pancuronium
Atracurium
•• MC used LA Lignocaine Pipecuronium
Cis-Atracurium
•• Shortest acting LA Chlorpropane Vecuronium
Mivacurium [Shortest
•• LA causing methemoglobinemia Prilocaine Q
Rocuronium
acting]
•• Maximum Cardiotoxic Bupivacaine Q
Rapacuronium

Local Anaesthetic Systemic Toxicity (LAST): •• Cis-atracurium release less histamine than
atracurismQ
→ Characterized by
–– Arrhythmias
Hoffman’s Elimination

–– Cardiovascular collapse •• Shown by Atracurium and Cis-atracurium

–– Seizures •• Muscle relaxant of choice in liver and renal diseaseQ

→ Treatment is Reversal Agents
–– Cardiopulmonary resuscitation
Used to reverse action of NDMR after surgery
–– 20% intralipid (DOC)Q → Neostigmine: Can cause cholinergic adverse effects
→ Suggamadex: No cholinergic side effectsQ
SKELETAL MUSCLE RELAXANTS
NEUROMUSCULAR BLOCKERS:
GENERAL ANAESTHETICS
These may be depolarizing or non-depolarizing skeletal
INDUCING AGENTS (INTRAVENOUS)
muscle relaxants
•• Thiopentone
Depolarizing Muscle Relaxants (DMR) •• Ketamine
•• Acts by stimulating NM receptors •• Propofol
•• Example is Succinylcholine (SCh) Q
•• Etomidate

Succinylcholine (SCh) Thiopentone

•• Shortest acting MR [< 5 min] •• Highly lipid soluble
•• C/I in nerve and muscle injuries [Can cause severe •• Very short acting d/t Redistribution
hyperkalemia]
•• Hyperthermia [precipitate malignant hyperthermia]
•• Fasciculations: Responsible for post operative muscle
pain
 87
Pharmacology
1. MAC (Minimum Alveolar concentration)
Propofol
•• Painful •• Minimum Concentration required in alveoli
to produce anaesthesia
•• DOC for day care SurgeryQ
•• Avoided in patients with egg allergy 1
Mac a
Potency
Etomidate
•• Agent of choice for CVS surgery MAC Potency Drug
•• Causes Adrenal SuppressionQ Maximum Least N2O (104%)
Minimum Most Methoxyflurane
Ketamine
K → Agent of choice in kids 2. Blood Solubility
E → Emergence Rxn (post operative delirium and Measured by blood gas partition coefficient (BGPC)Q
hallucinations)
1
T → Thalamo - Cortical junction (site of action)
BPGC a
Dissociative AnesthesiaQ speed of onset
A → Analgesic
M → Meals (can be given in full stomach) BGPC Onset Drug
I → ↑ BP/IOP/ ICP (Agent of choice in shock) Highest Slowest Methoxyflurane
N → NMDA Blocker Lowest Fastest Xenon

E → Excellent bronchodilatorQ

COLORS OF CYLINDERS
INHALATIONAL AGENTS N2O Blue (NEELA)
N2O Highest MAC (104%) Q
Cyclopropane Orange (SANTRI)
Halothane Causes hepatitis O2 Black and white (Black body and White
Causes malignant hyperthermia shoulder)
Enflurane Seizures (Maximum risk) Entonox –– Blue and White (Blue body and
Isoflurane DOC for cardiovascular and White shoulder)
neurosurgery –– Mixture of 50% N2O and 50%
Sevoflurane DOC for children O2 is Entonox
Methoxyflurane NephrotoxicQ
Desflurane Maximum irritation to respiratory
pathway
Xenon Ideal anaesthetic agent
88
Cerebellum Quick Revision Notes

Previous Years Questions

Q1. Mechanism of action of curare like drugs is A. Succinylcholine B. D-Tubocurarine
A. Competitive, Non depolarizing block at the Nm C. Dantrolene D. Baclofen
cholinergic receptors
Q6. Which of the following drug is associated with post
B. Non-competitive, Non depolarizing block at the Nm operative delirium and hallucinations?
cholinergic receptors
A. Ketamine B. Thiopentone
C. Competitive, Depolarizing block at the Nm cholin-
ergic receptors C. Fentanyl D. Halothane

D. Non-competitive, Depolarizing block at the Nm Q7. Inhalational anesthetic agent with highest
cholinergic receptors respiratory irritation is:
A. Desflurane B. Nitrous Oxide
Q2. Reason for preferring cis-Atracurium over Atracurium C. Sevoflurane D. Halothane
is:
A. Equal potency like Atracurium Q8. Which IV anesthetic does not cause cardiac
depression?
B. Lesser provocation of histamine release
A. Etomidate B. Propofol
C. Short fast action
C. Methohexitone D. Thiopentone
D. Does not undergo Hoffman elimination

Q3. A person was given a muscle relaxant that

competitively blocks nicotinic receptors. Which of the Q9. Inhalational anaesthetic agent of choice in children is
following drug is used for reversal of muscle relaxation
after surgery? A. Isoflurane B. Desflurane
C. Sevoflurane D. Halothane
A. Neostigmine B. Carbachol
C. Succinylcholine D. Physostigmine Q10. A patient of COVID-19 requires oxygen therapy.
Which of the following cylinders should be used to
Q4. An anesthetist injected bupivacaine in a patient provide oxygen to this patient?
for axillary nerve block. Later, the patient developed
restlessness, agitation and cardiovascular collapse.
Next best step in the management would be?
A. Cardiac resuscitation + dopamine
B. Cardiac resuscitation + dantrolene
C. Cardiac resuscitation + sodium bicarbonate
D. Cardiac resuscitation + 20 % intralipid

Q5. A patient was admitted for surgery and halothane

is being planned to be used as an anaesthetic agent.
The patient was explained about the adverse effect
of malignant hyperthermia with this drug. Which
of the following drugs may also result in malignant
A B C D
hyperthermia?

Answers
1. - A 3. - A 5. - A 7. - A 9. - C
2. - B 4. - D 6. - A 8. - A 10. - A
 Chapter - 14 Miscellaneous Topics

ANTI-SMOKING DRUGS Heparin Protamine sulfate

Paracetamol N. AcetylcysteineQ
1. Nicotine Replacement Therapy (NRT)
Atropine Physostigmine
•• Most commonly used anti-smoking drugs Iron Desferrioxamine
•• Available as chewing gums and lozenges Benzodiazepine FlumazenilQ

•• Lozenges have more bioavailabilty than gums Zolpidem Flumazenil

Cyanide Hydroxocobalamin (or Amyl
•• Do not take tea or coffee for 15 minutes after
nitrite)Q
taking NRT
Valproate hepatotoxicity L-carnitine
2. BupropionQ
•• Bupropion is anti-smoking whereas buspirone is MANAGEMENT OF HYPERKALEMIA
anti-anxiety Acute hyperkalemiaQ
3. VarenicilineQ 1. Drugs increasing intracellular movement of K+
•• Most effective anti-smoking drug •• Glucose - Insulin (DOC)
•• Can cause CVS and CNS adverse effects •• Beta 2 agonists e.g. salbutamol, epinephrine
2. Drugs reversing ECG changes
ANTI-OBESITY DRUGS •• Calcium gluconate
O – Orlistat Chronic Hyperkalemia
B – Bupropion + Naltrexone
E – Exenatide •• Long - term oral treatment
S – Semaglutide •• Drugs used:
I – LIraglutide
–– Patiromer
Ty – Tirzepatide
Topiramate + Phentermine
ERECTILE DYSFUNCTION
•• Orlistat is oral lipase inhibitor. It inhibits absorption
of fats. Major adverse effect is steatorrhea.Q •• DOC: PDE-5 inhibitor

•• GLP-1 analogues include exenatide, liraglutide and –– Sildenafil

semaglutide –– Tadalafil (Longest acting)
•• Tirzepatide is dual GLP-1 and GIP agonist.

ANTIDOTES
Poisoning Antidote
Beta blocker GlucagonQ
Organophosphate Atropine
Opioid NaloxoneQ
Methanol FomepizoleQ
Ethylene glycol Fomepizole
Warfarin Vitamin K
90
Cerebellum Quick Revision Notes

CHELATING AGENTS 2. Ca Na2 EDTA

•• Used for heavy metal poisoning Indications

1. BAL (British Anti Lewisite)/ Dimercaprol M– Manganese poisoning

I – Iron poisoning
Indications:
L– Lead poisoning
B - Bismuth poisoning
K– Cadmium poisoning
A - Arsenic poisoning
L - Lead poisoning 3. d- Penicillamine
Contra-Indications
Used for Cu poisoning and Wilson disease
Cadmium poisoning
Fe poisoning 4. Fe chelating agentsQ

Desferioxamine Injectable
DOC for acute Iron poisoning
Deferipirone Oral
Used for chronic Iron over load

Previous Years Questions

Q1. Which of the following is an adverse effect of Q4. An 11-year-old boy presented to emergency with
orlistat? vom iting. Parents gave history of consuming 10-15
tablets of ferrous sulphate a day before. What is the
A. Suicidal tendancy antidote of iron for treatment of this patient?
B. Steatorrhea
A. Dimercaprol
C. Weight gain
B. Desferrioxamine
D. Hyperglycemia
C. d- Penicillamine
Q2. Longest acting phosphodiesterase inhibitor among D. Activated charcoal
the following drugs is?
A. Sildenafil Q5. A patient presented with hyperkalemia. Which of
B. Vardenafil the following drugs can cause intracellular movement of
and thus decrease in extracellular potassium levels?
C. Tadalafil
A. Atropine
D. Phentolamine
B. Lactic acid
C. Epinephrine
Q3. Which of the following is FDA-approved drug for
long term treatment of obesity? D. Glucagon

A. Sibutramine
B. Liraglutide
C. Metformin
D. Fenfluramine

Answers
1. - B 3. - B 5. - C
2. - C 4. - B