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Review of Pharmacology - 9E (2015)

Review

Review of Pharmacology along with cell wall synthesis inhibitors like penicillins. These bind to 30S and 50S ribosomes and freeze initiation, interfere with polysome formation and cause misreading of mRNA code. Pharmacokinetics These are not absorbed orally and do not cross blood brain barrier. These are excreted primarily by glomerular filtration and the dose should be decreased in renal insufficiency. Resistance to these drugs develops due to the formation of inactivating enzymes which acetylate, phosphorylate or adenylate the aminoglycosides. All aminoglycosides except amikacin and netilmicin are susceptible to these enzymes. Thus amikacin and netilmicin may be effective against organisms resistant to other aminoglycosides. Chemotherapy A: General Considerations and Non-specific... 528 Clinical Uses • Gentamicin, tobramycin and amikacin are effective against gram negative organisms including pseudomonas (except salmonella). However these are not reliable for gram positive organisms if used alone. • Aminoglycosides produce synergistic effects against gram positive bacteria when combined with β-lactams or vancomycin. • Streptomycin is the first line drug for the treatment of tuberculosis, plague and tularemia. • Amikacin is a second line drug for the treatment of tuberculosis and is also used for MDR tuberculosis. • Netilmicin is used for serious infections only. • Neomycin and framycetin are used only topically because of their high toxic potential. • Neomycin can also be used orally for gut sterilization in hepatic encephalopathy. • Spectinomycin is a drug related to aminoglycosides, which is used as a single dose treatment for penicillinase producing Neisseria gonorrhoea (PPNG) and for gonorrhea in penicillin -allergic patients. Note: Tobramycin is much less active against enterococcal endocarditis than gentamicin or streptomycin. Toxicity • Ototoxicity: It can occur due to damage to hair cells. This adverse effect is more likely with prolonged use, high serum concentrations (especially with renal impairment), hypovolemia and other ototoxic medications (like ethacrynic acid). Amikacin, kanamycin and neomycin are more likely to cause hearing loss whereas streptomycin and gentamicin cause predominantly vestibular dysfunction. Tobramycin cause both abnormalities equally. Ototoxicity is largely irreversible and progress from base of cochlea (high frequency) to the apex (low frequencies). Very early changes can be reversed by Ca 2+ . Amikacin cause maximum hearing loss whereas streptomycin is most vestibulotoxic. Netilmicin is least ototoxic aminoglycoside. • Nephrotoxicity: It results from toxicity to proximal tubular cells and is almost always reversible. Risk factors for nephrotoxicity include hypokalemia, pre-existing renal disease and concomitant nephrotoxic medications (like AMB, vancomycin etc.). Neomycin is most nephrototoxic and is not indicated for systemic use. Among the systemically used aminoglycosides, gentamicin is most nephrotoxic followed by tobramycin. Streptomycin is least nephrotoxic. • Neuromuscular blockade: This adverse effect can lead to rare but severe respiratory depression. It can occur due to inhibition of pre-synaptic release of ACh and partly by decreased sensitivity of post-synaptic receptors. Hypocalcemia, peritoneal administration, use of neuromuscular blockers and pre-existing respiratory depression constitutes risk factors. This complication can be avoided by slow i.v. infusion (over 30 min.) or by i.m. route. If respiratory depression occurs, it is reversed by i.v. administration of calcium. Neomycin (not used) and streptomycin have maximum https://kat.cr/user/Blink99/

Chemotherapy A: General Consideration and Non-specific Antimicrobial Agents potency of causing neuromuscular block whereas tobramycin is least potent in this regard. These drugs are therefore contra-indicated in mysthenia gravis. Maximum Minimum Nephrotoxicity Neomycin > Gentamicin Streptomycin Ototoxicity Amikacin (Auditory) Netilmicin Streptomycin (vestibular) Neuromuscular blockade Neomycin > Streptomycin Tobramycin Pleuromutilins Puromycin is structurally similar to amino-acyl tRNA. It enters the A site and transfers to growing chain causing premature chain release. It is not selective for either procaryotes or eucaryotes. Retapamulin is a new drug of this class approved for topical treatment of impetigo due to methicillin-sensitive Staphylococcus aureus or Streptococcus pyogenes. It acts by inhibiting protein synthesis after binding to 50S ribosomes. Antimetabolites The drugs that are able to interfere with the role of an endogenous compound in the cellular metabolism are called antimetabolites e.g. sulfonamides, trimethoprim, pyrimethamine, proguanil and methotrexate. Sulfonamides • These drugs are bacteriostatic agents and act by inhibiting folate synthase competitively. • The selective toxicity to bacteria is due to the reason that mammalian cells do not synthesize folic acid and utilize preformed folic acid in the diet. • Sulfonamides are not effective in the presence of pus because it contains large amount of PABA. • These drugs undergo hepatic metabolism by ACETYLATION (Drugs undergoing acetylation are SHIP: Sulfonamides including dapsone, Hydralazine, Isoniazid and Procainamide) and can cause SLE. • The solubility of sulfonamides decrease in the acidic urine, which may result in precipitation of the drug causing crystalluria. Risk is minimum with soluble drugs like sulfisoxazole. • Sulfadoxine is longest acting whereas sulfacytine is shortest acting sulfonamide. Classification • For systemic use as oral agents Short acting: Sulfisoxazole, sulfamethiazole, Sulfacytine Intermediate acting: Sulfamethoxazole, Sulfadiazine Long acting: Sulfadoxine • For use in GIT: Sulfasalazine, olsalazine • For topical use: Sulfacetamide, silver sulfadiazine, mafenide Sulfisoxazole is most soluble sulfonamide. Thus it has minimum risk of causing crystalluria. Chemotherapy A: General Considerations Pharmacology and Non-specific... Clinical Uses • Sulfacetamide is used for ocular infections whereas mafenide and silver sulfadiazine are used in burn patients as topical agents. • Sulfadiazine can be used for nocardiosis and sulfisoxazole for urinary tract infections. • Sulfasalazine and olsalazine are used for the treatment of ulcerative colitis. • Sulfadoxine plus pyrimethamine is used for malaria. • Sulfadiazine and pyrimethamine combination can be used for the treatment of toxoplasmosis and prophylaxis of Pneumocystis jiroveci pneumonia in AIDS patients. 529 https://kat.cr/user/Blink99/

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    Review of Pharmacology Ninth Editio

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    Dedicated to My parents, wife Prave

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    Preface to the Ninth Edition We wan

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    Acknowledgments When emotions are p

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    References • Harrison’s Princip

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    Contents 1. History of Pharmacology

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    CHAPTER 1 History of pharmacology S

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    CHAPTER 2 General Pharmacology Phar

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    General Pharmacology Note: It is si

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    General Pharmacology Drug metaboliz

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    General Pharmacology Order of kinet

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    General Pharmacology Therapeutic Dr

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    General Pharmacology Fig. 2.4: G-pr

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    General Pharmacology sigmoid shaped

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    General Pharmacology Phase 1: Here,

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    General Pharmacology 5. Essential m

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    General Pharmacology (b) Bioavailab

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    General Pharmacology (c) Are highly

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    General Pharmacology (c) Strong aci

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    General Pharmacology (a) 50 mg/hour

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    General Pharmacology 140. Phamacoge

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    General Pharmacology (c) Piroxicam

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    206. Which of the following drugs s

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    General Pharmacology 29. In which t

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    General Pharmacology Explanations 1

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    General Pharmacology • Other fact

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    General Pharmacology -- Suppose, 10

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    General Pharmacology 77. Ans. (a) W

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    = 40 L × 4 mg/L = 160 mg Clearance

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    General Pharmacology 126. Ans. (c)

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    General Pharmacology 154. Ans. (d)

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    General Pharmacology Intolerance is

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    General Pharmacology 6. Ans. (b) b

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    CHAPTER 3 Autonomic Nervous System

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    Autonomic Nervous System Functions

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    Autonomic Nervous System • Carbac

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    Autonomic Nervous System used for g

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    Autonomic Nervous System -- Central

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    Autonomic Nervous System • Theref

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    Autonomic Nervous System • Eye: S

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    Autonomic Nervous System • Dopami

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    Autonomic Nervous System • Phenox

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    Autonomic Nervous System Lipid Inso

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    Autonomic Nervous System Drug of Ch

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    Multiple Choice Questions Autonomic

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    Autonomic Nervous System (c) Organo

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    (c) Physostigmime (d) Hyoscine hydr

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    Autonomic Nervous System (c) Tropic

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    132. A drug that blocks the uptake

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    165. Clonidine is used for: (Kolkat

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    as an effective substitute which do

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    Autonomic Nervous System 13. Which

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    Autonomic Nervous System (c) Increa

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    Autonomic Nervous System 9. Ans. (a

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    Autonomic Nervous System 39. Ans. (

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    Autonomic Nervous System - Temazepa

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    Autonomic Nervous System 103. Ans.

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    Autonomic Nervous System have no ef

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    Autonomic Nervous System 166. Ans.

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    Autonomic Nervous System 194. Ans.

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    Autonomic Nervous System 23. Ans. (

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    CHAPTER 4 Autacoids These are the s

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    Autacoids All second generation ant

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    Autacoids v v v v v Calcium channel

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    Autacoids nary bypass. It can also

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    Autacoids to presence of sulfur con

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    Autacoids Rheumatoid Arthritis Rheu

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    Autacoids It is a monoclonal antibo

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    Autacoids Drug of choice Condition

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    15. Anti-vertigo drug which modulat

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    49. Sumatriptan is: (DPG 1999, TN 2

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    81. All of the following effects ar

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    114. Which prostaglandin helps in c

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    Autacoids 148. Which of the followi

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    Autacoids 30. A 15 year old boy was

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    Autacoids 16. Ans. (b) Dangerous ve

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    Autacoids 56. Ans. (c) Cyclooxygena

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    Autacoids 85. Ans. (b) Aspirin supp

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    Autacoids 125. Ans. (b) Indomethaci

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    Autacoids 13. Ans. (a) Naproxen (Re

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    CHAPTER 5 Cardiovascular System CON

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    Cardiovascular System In atrial fib

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    Cardiovascular System Treatment of

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    Cardiovascular System should be use

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    Cardiovascular System tive α 1 blo

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    Cardiovascular System nifedipine an

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    Cardiovascular System Treatment of

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    Cardiovascular System ANGINA PECTOR

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    Cardiovascular System BETA BLOCKERS

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    Cardiovascular System The action po

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    Cardiovascular System depolarized c

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    Cardiovascular System • Digoxin i

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    Cardiovascular System Contd... •

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    Cardiovascular System DRUG OF CHOIC

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    15. Digoxin toxicity is aggravated

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    (c) Treat digoxin toxicity (d) Rapi

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    (c) Decreases sodium and increases

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    Cardiovascular System 113. All of t

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    146. Which of the following drugs i

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    Cardiovascular System 180. Characte

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    213. In a patient with hypertriglyc

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    247. ACE inhibitors cause: (PGI Dec

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    Cardiovascular System 16. Dialysis

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    Cardiovascular System 53. Which of

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    • Nesiritide is a recombinant BNP

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    Cardiovascular System 43. Ans. (d)

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    Cardiovascular System 81. Ans. (a)

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    Cardiovascular System -- Hypertensi

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    Cardiovascular System Cyanide has v

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    Cardiovascular System 178. Ans. (a)

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    Cardiovascular System 217. Ans. (a)

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    Cardiovascular System 237. Ans. (a)

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    Cardiovascular System 13. Ans (b) P

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    CHAPTER 6 Kidney Diuretics Diuretic

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    Kidney Uses Main use of loop diuret

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    Kidney • Amiloride is more potent

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    Kidney Amiloride It is the agent of

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    Kidney Multiple Choice Questions di

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    30. Which of the following statemen

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    66. Advantage of desmopressin over

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    Kidney Explanations 1. Ans. (b) Hyp

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    16. Ans. (b) Bumetanide (Ref: KDT 6

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    Kidney 55. Ans (d) V 4 : Central Ne

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    CHAPTER 7 Endocrinology Hormones ar

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    Endocrinology Prolactin It causes g

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    Endocrinology • In the liver and

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    Endocrinology I 131 can be used for

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    Endocrinology Drug interactions •

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    Endocrinology Lactic acidosis (more

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    Endocrinology 3. amylin analogs Pra

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    Endocrinology Important Points Maxi

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    Endocrinology • Steroids with sel

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    Endocrinology • Vitamin D 2 is er

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    Endocrinology Denosumab Osteoclasts

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    Endocrinology • SERMs are targete

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    Endocrinology Contd... • Uliprist

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    Endocrinology only pills. Chances o

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    Endocrinology Pharmacokinetics Test

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    Endocrinology Ergot Derivatives Erg

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    Endocrinology Contd... • Hyperpro

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    completion of therapy, the patient

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    (c) Glucose (d) Starch 47. True abo

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    (c) Na + exit/K + entry (d) K + ent

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    Endocrinology 113. Which of the fol

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    147. Bisphosphonates act by: (AI 20

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    180. Women receiving estrogen thera

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    (c) Clomiphene (d) Mifepristone (RU

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    246. Mechanism of Calcitriol is: (R

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    Endocrinology 32. Drug used to cont

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    (b) Glimepiride (c) Repaglinide (d)

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    Endocrinology Explanations 1. Ans.

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    Endocrinology 24. Ans. (c) Propylth

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    Endocrinology • When this drug is

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    Endocrinology Hypoglycemia is cause

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    Endocrinology Drugs causing Addison

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    Endocrinology Raloxifene is a selec

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    Endocrinology • Enzyme inducers l

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    Endocrinology 197. Ans. (b) Blocks

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    Endocrinology A spider angioma (als

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    Endocrinology 4. Ans (c) Glaucoma (

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    Endocrinology 70. Ans. (c) Mifepris

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    NOTES _____________________________

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    CHAPTER 8 Central Nervous System Se

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    Central Nervous System It is admini

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    Central Nervous System • Abnormal

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    Central Nervous System useful in AD

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    Central Nervous System Wilson’s D

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    Central Nervous System Important Dr

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    Central Nervous System • Lamotrig

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    Central Nervous System play a role

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    Central Nervous System According to

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    Central Nervous System bulimia, pre

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    Central Nervous System Anti Manic D

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    Central Nervous System dependence,

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    Central Nervous System increase hea

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    Central Nervous System Actions •

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    Central Nervous System Contd... •

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    (c) Alkalization of the urine will

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    Central Nervous System (c) Ketamine

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    79. Drug of choice for myoclonic ep

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    (c) Phenytoin (d) Valproic acid 112

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    146. Which of the following antipsy

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    (c) Regular measurements of blood c

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    210. A patient Rajnish having depre

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    242. Drug useful in malignant hyper

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    279. Preferred drug for alcohol wit

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    314. Morphine can administered by a

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    (c) Analgesia (d) Mydriasis 348. Di

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    17. Antiparkinson drug known to cau

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    53. Which drug is the most useful i

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    Central Nervous System 15. Ans. (c)

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    Central Nervous System 39. Ans. (b)

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    67. Ans. (a) Phenytoin (Ref: Katzun

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    97. Ans. (a) Hepatitis (Ref: KDT 6/

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    Central Nervous System 145. Ans (c)

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    Central Nervous System 159. Ans. (d

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    Central Nervous System 187. Ans. (b

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    Central Nervous System 212. Ans. (a

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    Central Nervous System 258. Ans. (a

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    Central Nervous System 286. Ans. (b

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    Central Nervous System 303. Ans. (c

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    Central Nervous System 326. Ans. (c

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    Central Nervous System 366. Ans. (b

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    Central Nervous System 60. Ans. (a)

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    CHAPTER 9 Anaesthesia Local Anaesth

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    Anaesthesia trigeminal nerve, cervi

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    Anaesthesia Centrally Acting Muscle

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    Anaesthesia • These drugs release

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    Anaesthesia Anaesthetic MAC (% atm)

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    Anaesthesia Methemoglobinemia and l

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    Anaesthesia Chloroform • It is a

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    Anaesthesia Contd... • It does no

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    Anaesthesia Anaesthetic agents of c

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    Anaesthesia Multiple Choice Questio

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    33. Post dural (Spinal) puncture he

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    (b) Dantrolene (c) Succinylcholine

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    103. Which of the following drugs a

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    Anaesthesia 138. Thiopental sodium

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    Anaesthesia Explanations 1. Ans (c)

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    Anaesthesia 20. Ans. (d) Seizures a

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    Anaesthesia 49. Ans. (b) Meprobamat

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    Anaesthesia • The patient underwe

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    Anaesthesia 91. Ans. (b) Sevofluran

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    Anaesthesia • In pheochromocytoma

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    CHAPTER 10 Hematology HAEMATINICS T

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    Hematology • Deficiency of folic

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    Hematology • Main drugs acting as

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    Hematology 1. Oral Anticoagulants

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    Hematology • Bioavailability of u

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    Hematology • Rodenticides contain

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    Hematology Condition • Anemia Dru

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    (c) Erythropoietin (d) Filgrastim (

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    Hematology 46. Tirofiban is a: (RJ

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    80. The anticoagulant of choice in

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    6. Mechanism of action of clopidogr

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    Hematology Explanations 1. Ans. (c)

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    Hematology 17. Ans. (d) Oprelvekin

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    Hematology 51. Ans. (a) Dabigatran:

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    Hematology 71. Ans. (c) Warfarin (R

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    Hematology 106. Ans. (c) Streptokin

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    CHAPTER 11 Respiratory System Cough

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    Respiratory System fast acting also

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    Respiratory System LT receptor anta

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    Respiratory System Condition • Br

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  • Page 499 and 500: Gastrointestinal Tract Contd... --
  • Page 501 and 502: Gastrointestinal Tract Anti Emetic
  • Page 503 and 504: Gastrointestinal Tract Domperidone
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  • Page 507 and 508: Gastrointestinal Tract Condition
  • Page 509 and 510: (c) Misoprostol (d) Omeprazole 15.
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  • Page 521 and 522: Gastrointestinal Tract 17. Ans. (c)
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  • Page 537 and 538: Clinical Uses Chemotherapy A: Gener
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  • Page 545 and 546: Important Points About Antimicrobia
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    Chemotherapy B: Antimicrobials for

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    Clofazimine It is a dye with lepros

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    Chemotherapy B: Antimicrobials for

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    Foscarnet It is not an antimetaboli

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    Human Immunodeficiency Virus (HIV)

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    Chemotherapy B: Antimicrobials for

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    Chemotherapy B: Antimicrobials for

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    Chemotherapy B: Antimicrobials for

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    Chemotherapy B: Antimicrobials for

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    Chemotherapy B: Antimicrobials for

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    Chemotherapy B: Antimicrobials for

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    Chemotherapy B: Antimicrobials for

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    16. Bactericidal drugs in ATT are:

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    50. Ethambutol should be used very

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    Chemotherapy B: Antimicrobials for

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    120. Regarding ritonavir use in AID

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    ACTs). All of the following combina

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    Chemotherapy B: Antimicrobials for

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    ecent Questions asked by National B

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    Chemotherapy B: Antimicrobials for

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    Explanations Chemotherapy B: Antimi

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    25. Ans. (b) Ethionamide (Ref: KDT

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    Chemotherapy B: Antimicrobials for

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    Chemotherapy B: Antimicrobials for

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    Chemotherapy B: Antimicrobials for

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    Chemotherapy B: Antimicrobials for

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    Chemotherapy B: Antimicrobials for

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    Chemotherapy B: Antimicrobials for

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    CHAPTER 15 Chemotherapy C: Antineop

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    Chemotherapy C: Antineoplastic Drug

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    Chemotherapy C: Antineoplastic Drug

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    4-5 years). Another distinguishing

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    Chemotherapy C: Antineoplastic Drug

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    GnRH Antagonists Cetrorelix, ganire

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    This drug was used in 1960s as a se

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    Chemotherapy C: Antineoplastic Drug

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    Multiple Choice Questions Chemother

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    37. Which of the following statemen

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    Chemotherapy C: Antineoplastic Drug

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    Chemotherapy C: Antineoplastic Drug

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    Chemotherapy C: Antineoplastic Drug

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    Chemotherapy C: Antineoplastic Drug

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    Chemotherapy C: Antineoplastic Drug

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    Chemotherapy C: Antineoplastic Drug

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    Chemotherapy C: Antineoplastic Drug

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    Chemotherapy C: Antineoplastic Drug

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    Chemotherapy C: Antineoplastic Drug

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    CHAPTER 16 Immunomodulators IMMUNOS

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    Immunomodulators 9. Antibodies Poly

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    Immunomodulators Examples of each t

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    Immunomodulators Clinical Diagnosis

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    (b) Podophylline (c) Interferon (d)

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    (c) Cytarabine (d) Cycloserine 51.

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    Immunomodulators Explanations 1. An

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    Immunomodulators 14. Ans. (a) Syste

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    Immunomodulators 33. Ans. (a) Gluco

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    CHAPTER 17 Other Topics and Adverse

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    Other Topics and Adverse Effects Co

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    Other Topics and Adverse Effects Co

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    Other Topics and Adverse Effects Co

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    17. A 2 years old child without fev

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    54. Isotretinoin is: (PGI June, 200

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    Other Topics and Adverse Effects (c

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    Other Topics and Adverse Effects

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    Other Topics and Adverse Effects

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    Other Topics and Adverse Effects 39

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    Other Topics and Adverse Effects 55

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    Other Topics and Adverse Effects Dr

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    CHAPTER 18 Drugs of Choice Drug of

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    Drugs of Choice Contd... Hypertensi

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    Contd... VRSA LINEZOLID/STREPTOGRAM

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    CHAPTER 19 New Drugs 1. Abatacept:

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    New Drugs 52. Canakinumab: A human

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    New Drugs 100. Ecallantide: A plasm

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    New Drugs 153. Laronidase: Recombin

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    New Drugs 204. Peginesatide: A pept

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    New Drugs been approved for the tre

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    New Drugs and B lymphocytes after e

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    New Drugs prevents nausea and vomit

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    CHAPTER 20 Recent Topics TRICYCLIC

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    Recent Topics 2. Drugs 5-HT 2 recep

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    Recent Topics Arginine NOS NO + Cit

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    Recent Topics Contd... Drug Tetracy

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    Recent Topics -- If the patient has

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    CHAPTER 21 Latest Papers AIIMS Nove

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    Latest Papers explanations 1. Ans.

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    • Clindamycin and erythromycin ar

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    Latest Papers AIIMS May 2014 1. Whi

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    Latest Papers explanations 1. Ans.

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    13. Ans. a. Hypokalemia (Ref: Harri

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    NOTES _____________________________

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    Image Based Questions https://kat.c

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    Image Based Questions 1. The result

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    5. A new antiarrhythmic drug is fou

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    10. Amarnath, a 58 year old busines

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    14. A 72-year-old male, Hemraj was

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    (rapid vs slow induction of anesthe

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