Which of the following is/are true regarding phase 1 drug metabolism?
Also known as conjugation reaction
Includes only oxidation
Generally tends to provide a functional group or “handle” to the molecule
NOTA
Which of the following is/are true regarding phase II drug metabolism?
Allows the attachment of small, polar and ionizable endogenous compounds
Allows the termination or attenuation of a biologic activity
serves to protect the body against chemically reactive compounds or metabolites
Which of the following undergo an oxidative reaction?
Olefins
alcohols, aldehydes
aromatic moieties
nitro and azo compounds
Which of the following is/are examples of drugs that are extensively metabolized by the first pass effect?
Lidocaine
Nitroglycerin
Morphine
meperidine
Glucuronidation is the most common conjugative pathway in drug metabolism. Which of the following is/are responsible for this?
readily available supply of D-glucuronic acid
numerous functional groups that can combine enzymatically with glucuronic acid
utilization of D-glucuronic acid to conjugate steroids, heparin, chondroitin, catecholamines and thyroxine
AOTA
Which of the following is/are factors affecting drug metabolism?
Age
economic status
species and strain
gender
Which of the following is/are true regarding methylation?
generally leads to polar or water-soluble metabolites
important in the biosynthesis of many endogenous compounds like epinephrine and melatonin
constitutes only a minor pathway for conjugating drugs or xenobiotics
Which of the following is/are considered slow acetylators?
eskimos
egyptians
filipinos
jews
Which of the following may induce metabolism of other drugs?
phenytoin
cimetidine
meprobamate
rifampicin
The term that denotes the selective metabolism of two or more similar functional groups or two or more similar atoms that are positioned in different regions of a molecule.
stereoisomerism
regioselectivity
selective toxicity
substrate stereoselectivity
The process involved in the biotransformation of amitriptyline to nortriptyline.
N-demethylation
Aromatic hydroxylation
Epoxidation
Ester hydrolysis
The biotransformation of chloral hydrate via aldehyde reduction forms?
desipramine
mesoridazine
trichloroethanol
sulindac
What process is involved in the biotransformation of prednisone to prednisolone?
ketone reduction
O-demethylation
sulfoxide reduction
What process is involved in the biotransformation of phenylbutazone to oxybutazone?
aromatic hydroxylation
N-acetylation
S-oxidation
Which of the following is/are metabolites?
6-mercaptopurine
phenylbutazone
prednisolone
acetaminophen
Which of the following is/are parent drug/s?
digitoxin
hydrocortisone
primidone
propranolol
The property of chemicals to destroy one form of life without harming another.
Which of the following may be used to classify chemotherapeutic agents?
chemical type
biologic properties
therapeutic indications
Which of the following is/are characteristics of an ideal antiseptic?
rapid and sustained lethal action against microorganisms
retain activity in the presence of body fluids
high surface tension
An agent that prevents infection by the destruction of pathogenic microorganisms when applied to inanimate objects.
Antiseptic
disinfectant
antibiotic
sanitizer
Generally accepted other names of alcohol USP
Ethanol
wood alcohol
spiritus vini rectificatus
wine spirit
Ethanol that has been rendered unfit for use in intoxicating beverages by the addition of other substances.
Denatured alcohol
isopropyl alcohol
formaldehyde
Phenol coefficient is defined as the ratio of a disinfectant to the dilution of phenol required to kill a given strain of a bacterium. What microorganism is used in determining the phenol coefficient?
Bacillus subtilis
Enterobacter aerogenes
Pseudomonas aeruginosa
Salmonella typhi
A 2% solution of iodine in 50% alcohol with sodium iodide.
Iodine solution
iodine tincture
lugol’s solution
mayer’s reagent
A preparation of 5% Iodine in water with potassium iodide?
A preparation of 2% iodine in water with sodium iodide?
Povidone-Iodine
Water-soluble complex that releases iodine slowly
provides a non-toxic, non-irritating,non-volatile and non-staining form of iodine
used as an antiseptic for skin application before surgery and injection
A dye available as vaginal suppositories for the treatment of yeast infections.
Malachite green
methylene blue
phenolphthalein
gentian violet
Dye used as an antidote for cyanide poisoning?
A potent antifungal substance with a polyene structure from Streptomyces nodosus
Nystatin
griseofulvin
natamycin
amphotericin B
The aglycone portion of nystatin consisting of a 38-membered ketone ring with a single tetracene and diene chromophores isolated from each other by a methylene group, one carboxyl, one keto, and eight hydroxyl groups.
Mykinac
mycostatin
nystatinolide
candeptin
Polyene antibiotic first isolated in 1951 from a strain of Streptomyces noursei by hanzen and brown.
amphotericin b
Griseofulvin
Recommended for the systemic treatment of refractory ringworm infections
its bioavailability is notoriously poor
it is supplied in “microsize” and “ultramicrosize” forms
A series of synthetic antibacterial agents patterned after nalidixic acid, with an effective antibacterial spectrum largely confined to gram-negative bacteria.
quinolones
dihydrotriazines
biguanides
polyenes
The structure found among the quinolones which is essential for their antibacterial activity is 1,4-dihydro-4-oxo-3-pyridine carboylic acid.
True
False
Its congeners represent important alternatives for the treatment of urinary tract infections caused by strains of Proteus resistant to other agents.
Norfloxacin
cinoxacin
nitrofurantoin
nalidixic acid
Antibiotic
A synthetic product produced as a structural analogue of a naturally occurring antibiotic
it antagonizes the growth or the survival of one or more species of microorganisms
it is effective in low concentration
One who led the isolation of streptomycin from Streptomyces griseus:
Pasteur & Joubert
waksman
Vuillemin
Florey and Chain
Antibiotic that binds with ribosome 30s subunit
Chloramphenicol
tetracycline
erythromycin
lincomycins
Benzylpenicillin binds preferentially to:
PBP 1a & 1b
PBP 2
PBP 3
PBP 6
Methicillin is chemically called as:
2-ethoxy-1-napthylpenicillin
5-methyl-3-phenyl-4-isoxazolyl penicillin
5-methyl-3-(2,6-dichlorophenyl)-4-isoxazolyl-penicillin
2,6-dimethoxyphenyl penicillin
Amoxicillin
D-?-Amino-p-hydroxybenzyl-penicillin
?-Carboxy-3-thienyl penicillin
?-(1-methanesulfonyl-amino) benzylpenicillin
D-?-aminobenzyl penicillin
Structure of the penicillin molecule shows it to contain a fused ring system which is the:
?-lactam thiazolidine
?-lactam penam
6-aminopenicillanic acid
?-lactam phenyl penicillin ring
Members of the 4-isoxazolyl penicillin family require these substituents for effectiveness against ?-lactamase producing Staphylococcus aureus.
3-aryl & 5-methyl group
3-acyl & 6-methyl group
3-phenyl & 2-methoxy group
3-phenyl & 2-methyl group
These are major antigenic determinants that are formed when penicillins or its rearrangement products in vivo react with lysine-e-amino groups of proteins resulting to allergic reactions.
Penicillenic acids
penicilloyl proteins
penicillanic proteins
penicillanic acids
This is prepared by the reaction of ampicillin with acetone
Unipen
hetacillin
unasyn
methicillin
Class 1 ?-lactamase inhibitors have hetero atom leaving at position 1. Which of these is/are Class II inhibitors: I. Carbapenems II. Sulbactam III. Clavulanic Acid
I only
I, II
II, III
III only
Augmentin is a combination of:
K salt of Clavulanic Acid
amoxicillin
ampicillin
sulbactam
Unasyn is a fixed-dose combination of:
clavulanic
Primaxin is a combination of:
Tazocillin
imipenem
piperacillin
cilastatin
Imipenem is the most successful of a series of chemically stable derivatives of thienamycin in which the primary amino group is converted to a non-nucleophilic basic function. Imipenem is also:
5-acetamido thienamycin
n-formimidoyl thienamycin
?-imidazolyl ethylamine
D-(4-amino-4-carboxybutyl) is:
Penicillin N
synnematin B
cephalosporin N
chloramphenicol B
Cephalosporin C contains:
Penicillanic acid
thiazolidine ring
lactone ring
dihydrothiazine ring
A parenteral cephamycin
Cefoxitin
ceftazidime
cephalexin
cefadroxil
Zinacef is the first of a series of a-methoxyimino-acyl-substituted cephalosporins that constitute most of the third generation agents. Zinacef is:
Sterile cefotaxime Sodium, USP
Cefuroxime Sodium, USP
Moxalactam Disodium, USP
Cefepime, USP
The factors that contribute to an extremely long serum half-life of sterile ceftriaxone disodium, USP
High fraction of protein binding in the plasma
slow urinary excretion
it is not metabolized in vivo
This increases stability to ?-lactamases while increasing activity against G(-) bacteria at the same time in monobactams:
4-methyl group
3-methoxy group
oximinoacyl group
2-aryl group
The 1st aminoglycoside antibiotic to be used in chemotherapy:
Amikacin
gentamicin
streptomycin
kanamycin
MOA of Aminoglycosides:
Interferes with cell wall synthesis
act directly on the bacterial ribosome to inhibit the initiation of protein synthesis
interferes with the fidelity of translation of the genetic message
Extrachromosomals which are self-replicative and transferable by conjugation that is responsible for the transfer of resistance from one bacterium to another.
R-factor
F-factor
S-factor
X-factor
SAR of Aminoglycosides: important for characteristic broad-spectrum antibacterial activity & is the primary target for bacterial inactivating enzymes.
Ring I
Ring II
Ring III
Ring IV
Known as Streptomycin B
Streptomycin
Mannisidostreptomycin
Hydroxystreptomycin
Paromomycin Sulfate, USP
Acid hydrolysis of Streptomycin yields:
Streptidine
Streptobiosamine
Deoxystreptamine
Neomycin is obtained from:
S. fradiae
S. rimosus
S. kanamyceticus
Micromonospora purpurea
The synthesis of this semisynthetic aminoglycoside involves simple acylation of the 1-amino group of the deoxystreptamine ring of Kanamycin A with L-amino-a-hydroxybutyric acid (L-AHBA)
Tobramycin
Netilmicin
Gentamicin
A group of antibiotics that are derivatives of an octahydronaphthalene, a hydrocarbon system that comprises four annelated six-membered rings.
Macrolides
sulfonamides
7-Chloro-6-demethyl tetracycline is:
demeclocycline
Oxytetracycline
minocycline
Doxycycline
Macrolide antibiotics have these common characteristics:
Large lactone ring
ketone group
a glycosidically linked amino sugar
an asymmetric carbon atoms in the acylamidopropanediol chain
Bacillus subtilis strain that was isolated from debrided tissue of a compound fracture in 7-year old Margaret Tracy produced this antibiotic.
Gramicidin
Bacitracin
Colistin
Polymyxin
The first of the widely used broad-spectrum antibiotic that was isolated by Ehrlich in 1947 from S. venezuelae
Clindamycin
Vancomycin
Novobiocin
Erythromycin B differs from Erythromycin A only at carbon 12, at which hydroxyl group is replaced by ______, which renders it more acid stable.
Bromine
Chlorine
Hydrogen
Oxygen
These are sulfur-containing antibiotics isolated from S. lincolnensis
novobiocin
vancomycins
7-Chloro-7-deoxy lincomycin
Cleocin
Unasyn
Lincocin
Bacitracin’s bactericidal effect through an inhibition of mucopeptide cell wall synthesis is enhanced by:
P
Zn
Cl
S
Analogue of podophyllotoxin that is an inhibitor of Topoisomerase II which contains methyl as its R group:
Vindoline
Etoposide
Vincristine
Epipodophyllotoxin
The complex structures in vinca alkaloid composed of indole-containing moiety and an indoline-containing moiety:
Indoline
Vindesine
Catharanthine
Is an antineoplastic agent preparation from E. coli containing the enzyme L-asparagine amidohydrolase
Asparaginase
Elspar
Pipobroman
Platinol
An antineoplastic drug active against rapidly proliferating cells in the synthesis phase during which it prevents the formation of deoxyribonucleotides by inhibition of ribonucleotide diphosphate reductase.
Carboplatin
hydroxyurea
mitoguazone
hycanthone
Used primarily for polycythemia vera:
Hexamethylamine
asparaginase
tamoxifen
pipobroman
D-Homo-17a-oxa androsta-1,4-dione prepared by microbial transformation of progesterone
Tamoxifen
testolactone
megestrol
ethinyl estradiol
Interferons are secreted by cells in response to viral infections or other chemical or biologic inducers. The major classes of interferons are:
alpha
Beta
Lambda
Gamma
It is a highly purified protein containing 165 amino acids manufactured from a strain of E.coli bearing a genetically engineered plasmid containing an interferon alfa-2a gene from human leukocytes.
RIFN
IFLrA
Roferon-A
Interon
This is absolutely essential for the in-vitro carbonic anhydrase inhibitory activity and for the production of a diuresis in vivo.
Sulfamoyl group
neptazane
amino group
Imino group
Diamox
Acetazolamide
Hydrochlorothiazide
Dichlorphenamide
Benzothiazine-1,1-dioxide nucleus is contained in:
Carbonic anhydrase inhibitors
thiazide diuretics
loop diuretics
phenoxyacetic acids
4-Chloro-N-furfuryl-5-sulfamoyl anthranilic acid is:
Bumetanide
furosemide
ethacrynic acid
chlorothiazide
Primary compound selected from a host of pteridine analogues and resembles the structure of folic acid and certain dihydrofolate reductase inhibitors.
Spironolactone
amiloride
theophylline
triamterene
A pyrazinoyl guanidine diuretic that inhibits the electrogenic entry of 2% to 3% of the filtered load of Na into the tubule cells.
Triamterene
spironolactone
aldosterone
The major adverse effect of midamor:
hypomagnesemia
hyponatremia
hypocalcemia
hyperkalemia
?-imidazolylethylamine, an autacoid, is widespread in nature being found in ergot and other plants and in all organs and tissues of the human body. It’s also known as:
1H-imidazole-4-ethenamine
histamine
serotonin
The major source of histamine in the body results from the decarboxylation of this amino acid:
Tryptophan
Histidine
Tyrosine
Phenylalanine
Drowsiness is a side effect of antihistamines that is most common to the:
Ethylenediamines
tertiary aminoalkyl ethers
phenothiazines
A propylamine derivative:
Diphenhydramine
Clemastine
Carbinoxamine
Brompheniramine
Dramamine
Doxylamine
Dimenhydrinate
Cyclizine
The piperazine, imidazoline and phenothiazine type antihistamines contain the following moiety:
Aminoalkyl ethers
ethylene diamine
propylamine
butyrophenone
Antihistamine resulting from the chlorination of pheniramine in the para position of the phenyl ring that gives a tenfold increase in potency with no appreciable changes in toxicity.
chlorpheniramine
pyrrobutamine
promethazine
A sulfone derivative investigated initially to be the most effective drug for the treatment of leprosy and has useful antimalarial property but was too toxic.
4,4’-diamidodiphenylsulfide
4,4’-diaminodiphenylsulfone
3,4’-diaminediphenylsulfide
3,4’-diamidodiphenylsulfone
What antibiotic caused a major advance in the treatment of tuberculosis?
Isoniazid
ethionamide
rifampin
cycloserine
Ethambutol is remarkably stereospecific. Toxicities of its isomers are about equal but their activity varies considerably. Factors that have pronounced effect on the activity are:
Length of the alkylene chain
nature of the branching with the alkyl substituents in the nitrogens
extent of N-alkylation
pyranolone ring at the C4 of the compound
Ethionamide is a second-line treatment drug for tuberculosis and used in the treatment of INH-resistant tuberculosis or when the patient is intolerant to INH and other drugs. What is its structural difference with the INH series?
5 - substitution
2 - substitution
addition of a thiazolidine ring
addition of a pyranolone ring