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PHARMACOLOGY EVALS 6 RATIONALIZATION

(AMEBICIDALS, ANTHELMINTICS, ANTIDIARRHEALS/ANTI-MOTILITY DRUGS, AMINOGLYCOSIDES,


GLYCOPEPTIDES & SULFONAMIDES, TREATMENT OF ACID PEPTIC DISEASE)

AMEBICIDALS
1. Emetine is commonly given by which EMETINE
route of administration? • Alkaloid from Ipeca Syrup of Ipecac
• Primarily used as an antitussive drug (mucolytic)
a. Oral • Also used as an antidote due to its powerful emetic effect but is not used anymore
b. Topical because of its cardiac effects.
c. Intravenous Use:
d. Subcutaneous • For SEVERE invasive intestinal and extraintestinal amoebiasis (if metronidazole is
contraindicated)
• Should be administered subcutaneously (preferred) or
intramuscularly
A/E:
• Pain, tenderness, sterile abscesses at the injection site; diarrhea, nausea, vomiting,
muscle weakness, and discomfort
• Cardiac arrythmias, heart failure, hypotension

The correct answer is: D. Subcutaneous


2. Chloroquine is an alternative tissue CHLOROQUINE
amebicidal for the treatment of which form Class:
of amebiasis? • Tissue Amoebicide
• Anti-malarial (DOC)
a. Amebic liver abscess • DMARD (disease-modifying antirheumatic drug)
b. Asymptomatic intestinal infection MOA: Directly toxic to E. histolytica
c. Ameboma Uses:
d. Severe dysentery • Amoebic liver abscesses ONLY
• DOC for non-falciparum malaria
• Chemoprophylaxis (in chloroquine-sensitive areas)
• Rheumatoid arthritis
PK: Concentrated in the liver
S/E: GI irritation, skin rash, retinal damage, auditory impairmen

The correct answer is: A. Amebic liver abscess


3. What is the active anti-amebic compound DILOXANIDE FUROATE
of diloxanide furoate? Class: Dichloroacetamide derivative
MOA: Unknown
a. 10% unabsorbed diloxanide Uses:
b. 90% absorbed diloxanide As single agent: DOC for asymptomatic luminal infection
c. 90% unabsorbed diloxanide In combination w/ metronidazole: For serious intestinal and extraintestinal amoebic
d. 10% absorbed diloxanide infections
PK: Splits into 2 in the gut:
• Diloxanide - 90% absorbed → excreted via urine (Glucoronide) - 10% unabsorbed →
active anti-amoebic substance
• Furoic Acid
A/E: Flatulence (main adverse effect), nausea, vomiting, diarrhea, pruritis CI: Pregnancy

The correct answer is: A. 10% unabsorbed diloxanide


4. Which of the following amebicidals cause METRONIDAZOLE (FLAGYL)
disulfiram-like effect? Class: Nitroimidazole
MOA: Reactive reduction (by the bacteria / protozoans) of the nitro group appears to be
a. Paromomycin antimicrobial)
b. Iodoquinol Uses: ***has antiparasitic and antibiotic activity
c. Metronidazole • DOC for Extraluminal Amoebiasis (Amebic colitis & Amebic liver abscess)
d. Emetine • DOC for Giardiasis (Giardia lamblia)
• DOC for Trichomoniasis (Trichomonas vaginalis)
• Act as antibiotic for Anaerobic infections (Bacteroides, Clostridium difficile,
Helicobacter)
A/E:
• Disulfiram-like effect (flushing, vomiting, headache) if px drinks alcoholic
beverages within 3 days of therapy
• Neurotoxic effects (dizziness, vertigo, encephalopathy, convulsions, ataxia,
paresthesia)
• Dysuria, cystitis, & sense of pelvic pressure
• Cephalosporins (beta-lactam antibiotics which also causes Disulfiram-like effect)
• Disulfiram-like-effect is a result of an accumulation of acetaldehyde due to the inhibition
of acetaldehyde dehydrogenase
• Other adverse effects include headache, dry mouth, fatigue, metallic bitter taste, and GI
distress
• Advise patient to take the medicine after meals and to avoid ANY alcohol-containing
products (including rubbing alcohol and the like)

The correct answer is: C. Metronidazole


5. What is the amebicidal of choice for the PAROMOMYCIN
treatment of asymptomatic amebic Class:
infection? • Aminoglycoside
• Luminal amebicide
a. Tinidazole MOA: Binds to 30s ribosomal subunit
b. Metronidazole Uses
c. Paromomycin Oral prep:
d. Emetine • DOC for asymptomatic Intestinal Amoebiasis
• Cryptosporidiosis
• Giardiasis
Topical:
• Trichomoniasis
Parenteral:
• Visceral leishmaniasis
PK Oral:
• not well absorbed in the GIT
• small amount absorbed is slowly excreted unchanged, mainly by
glomerular filtration
A/E
Oral:
• Rare but includes abdominal pain, cramping, nausea, vomiting, steatorrhea & diarrhea
Parenteral:
• nephrotoxicity- Reversible
• Ototoxicity- irreversible
Precautions: Avoided in patients with renal diseases
Note: Alternative to metronidazole in first trimester of pregnancy

The correct answer is: C. Paromomycin


6. Which of the following amebicidals NITAZOXANIDE
inhibits the pyruvate-ferrodoxin pathway? Class: Nitrothiazolyl-salicylamide prodrug
Tissue amebicide
a. Nitazoxanide MOA: PRODRUG
b. Paromomycin Converted to an active metabolite (TIZOXANIDE) → inhibits pyruvate:ferredoxin
c. Iodoquinol pathway
d. Diloxanide furoate Uses Infections caused by:
• E. histolytica
• Giardia
• T. Vaginalis
• C. parvum
• H. Nana
• T. Trichiura
• Ascaris lumbricoides
• Several tapeworms
• Fasciola hepatic
• Metronidazole-resistant protozoal strains
PK: Excellent bioavailability.
• Hydrolyzed rapidly to Tizoxanide which undergoes conjugation to Tizoxanide
glucuronide.
• Tizoxanide excreted in the urine, bile and feces.
A/E: MC (Rare)
• Abdominal pain
• Diarrhea
• Vomiting
• Headache
• *Greenish tint to the urine
Precautions:
• PREGNANCY CATEGORY B (i.e. Animal reproduction studies have failed to
demonstrate a risk to the fetus and there are no adequate and well-controlled studies in
pregnant women)

The correct answer is: A. Nitazoxanide


7. Paromomycin belongs to what PAROMOMYCIN
classification of antibiotics? Class:
• Aminoglycoside
a. Lincosamides • Luminal amebicide
b. Quinolones
c. Macrolides
d. Aminoglycosides The correct answer is: D. Aminoglycosides
8. Which antibiotic can be used as an Treatment of Specific Forms of Amoebiasis
alternative drug for the treatment of amebic 1) ASYMPTOMATIC INTESTINAL INFECTIONS
colitis for patients who cannot tolerate a) Luminal Amebicide* (DOC for this type of amoebiasis) Supportive Management
Metronidazole? b) Endemic areas → generally not treated Nonendemic areas → luminal
amebicidal Tissue amebicidal is unnecessary
a. Azithromycin 2) AMOEBIC COLITIS
b. Cotrimaxazole a) Metronidazole + Luminal Amebicide (treatment of choice)
c. Tetracycline b) Alternative: Tetracyclines and Erythromycin (but they are not effective against
d. Clindamycin extraintestinal disease)
c) Dehydroemetine or emetine can also be used, but are avoided because of
toxicity
3) EXTRAINTESTINAL INFECTIONS
a) Metronidazole + Luminal Amebicide (treatment of choice)
DOC for Intestinal Amoebiasis: PAROMOMYCIN SULFATE
DOC for Extraintestinal Amoebiasis: METRONIDAZOLE

The correct answer is: C. Tetracycline


9. Which of the following amebicidals is ADVERSE EFFECTS
contraindicated in a patient with a history of a) Metronidazole
congestive heart failure? ● Disulfiram-like effect (flushing, vomiting, headache) if px drinks alcoholic
beverages within 3 days of therapy
a. Metronidazole ● Neurotoxic effects (dizziness, vertigo, encephalopathy, convulsions, ataxia,
b. Emetine paresthesia)
c. Diloxanide furoate ● Dysuria, cystitis, & sense of pelvic pressure
d. Iodoquinol b) Emetine
● Pain, tenderness, sterile abscesses at the injection site; diarrhea, nausea,
vomiting, muscle weakness, and discomfort
● Cardiac arrythmias, heart failure, hypotension
c) Diloxanide furoate
● Flatulence (main adverse effect), nausea, vomiting, diarrhea, pruritis
d) Iodoquinol
● GI upset, abdominal pain, nausea, vomiting
● Iodine toxicity (Dermatitis, urticaria, pruritus, fever)
● Administration of high doses in children has been associated with optic atrophy
& permanent loss of vision

If it is part of the adverse effect, the drug must never be given to patients who have this
disease prior to giving these drugs. It will just worsen the underlying disease.

The correct answer is: B. Emetine


10. An alternative amebicidal to USES
Metronidazole during the first trimester of a) Tinidazole
pregnancy? b) Diloxanide furoate
● As single agent: DOC for asymptomatic luminal infection
a. Tinidazole ● In combination w/ metronidazole: For serious intestinal and extraintestinal
b. Diloxanide furoate amoebic infections
c. Chloroquine c) Choloroquine
d. Paromomycin ● Amoebic liver abscesses ONLY
● DOC for non-falciparum malaria Chemoprophylaxis (in chloroquine- sensitive
areas)
● Rheumatoid arthritis
d) Paromomycin
● Oral prep: DOC for Asymptomatic Intestinal Amoebiasis, Cryptosporidiosis,
Giardiasis
● Topical: Trichomoniasis
● Parenteral: Visceral leishmaniasis
● Alternative to metronidazole in first trimester of pregnancy

The correct answer is: D. Paromomycin


11. All of the following amebicidals are PHARMACOKINETICS
primarily excreted through the urine, a) Paromomycin
except? ● Oral:
○ not well absorbed in the GIT
a. Paromomycin ○ small amount absorbed is slowly excreted unchanged, mainly by
b. Metronidazole glomerular filtration
c. Iodoquinol b) Metronidazole
d. Diloxanide furoate ● Rapidly absorbed orally
● Permeate ALL tissues by simple diffusion except placenta
● Low plasma binding protein
● Excreted in the urine
● t1/2: 7.5 hours
● Plasma clearance of Metronidazole is decreased in patients with impaired liver
function
c) Iodoquinol
● Poorly absorbed since 90% of the drug remains in the intestine, the rest is
excreted via feces
● t1/2: 11-14 hours
d) Diloxanide furoate
● Splits into 2 in the gut:
○ Diloxanide
■ 90% absorbed → excreted via urine (Glucoronide)
■ 10% unabsorbed → active anti-amoebic substance
○ Furoic Acid

The correct answer is: C. Iodoquinol


12. Metronidazole is also the drug of choice USES OF METRONIDAZOLE
for the treatment of which parasitic ● *has antiparasitic and antibiotic activity
infection? ● DOC for Extraluminal Amoebiasis (Amebic colitis & Amebic liver disease)
● DOC for Giardiasis
a. Ascaris ● DOC for Trichomoniasis
b. Giardiasis ● Act as antibiotic for Anaerobic infections (Bacteroides, C. difficile, Helicobacter)
c. Trichuriasis
d. Schistosomiasis The correct answer is: B. Giardiasis
13. greenish-tint to the urine is a notable ADVERSE EFFECTS
side effect of which amebicidal? a) Niazoxanide
• Abdominal pain
a. Nitazoxanide • Diarrhea
b. Iodoquinol
c. Metronidazole • Vomiting
d. Paromomycin • Headache
• *Greenish tint to the urine
b) Iododiunol
• GI upset, abdominal pain, nausea, vomiting
• Iodine toxicity (Dermatitis, urticaria, pruritus, fever)
• Administration of high doses in children has been associated with optic atrophy
& permanent loss of vision
c) Metronidazole
• Disulfiram-like effect (flushing, vomiting, headache) if px drinks alcoholic
beverages within 3 days of therapy
• Neurotoxic effects (dizziness, vertigo, encephalopathy, convulsions, ataxia,
paresthesia)
• Dysuria, cystitis, & sense of pelvic pressure
d) Paromomycin
• Oral → rare but includes pain, cramping, nausea, vomiting, steatorrhea &
diarrhea
• Parenteral → Reversible nephrotoxicity and Irreversible ototoxicity
• Avoided in px with renal diseases

The correct answer is: A. Nitazoxanide


14. Administration of high doses of Adverse Effects of Iodoquinol
iodoquinol in children is associated with • GI upset, abdominal pain, nausea, vomiting
what medical condition or adverse effect? • Iodine toxicity (Dermatitis, urticaria, pruritus, fever)
• Administration of high doses in children has been associated with optic atrophy &
a. Cardiac arrhythmia permanent loss of vision
b. Ototoxicity
c. Optic atrophy
d. Steatorrhea The correct answer is: C. Optic atrophy
15. Alcohol intake is prohibited for patients
Disulfiram-like effect
taking which amebicidal? ● Adverse effect of Metronidazole and Cephalosporins
● Flushing, vomiting, headache
a. Emetine ● If Px drinks alcoholic beverages within 3 days of therapy
b. Iodoquinol ● Result of an accumulation of acetaldehyde due to the inhibition of acetaldehyde
c. Metronidazole dehydrogenase
d. Diloxanide furoate The correct answer is: C. Metronidazole
For numbers 16-20. Matching type. Match the amebicidal with its notable adverse/side effect.
16. Flatulence Adverse effects
a) Metronidazole
a. Metronidazole • Disulfiram-like effect, Neurotoxic, Dysuria, Cystitis, sense of pelvic pressure,
b. Emetine Metallic bitter taste, GI distress, fatigue
c. Paromomycin b) Emetine
d. Diloxanide furoate • Cardiac arrhythmia, heart failure, hypotension, injection site pain, diarrhea,
e. Iodoquinol nausea, muscle weakness, discomfort
c) Paromomycin
• Parenteral: reversible nephrotoxicity, irreversible ototoxicity
• Oral (rare): abdominal pain, cramping, nausea, vomiting
d) Diloxanide furoate
• Flatulence, nausea vomiting, diarrhea, pruritus
e) Iodoquinol
• Iodine toxicity (dermatitis, urticaria, fever), GI upset, nausea
• High doses: Optic atrophy, permanent loss of vision

The correct answer is: D. Diloxanide furoate


17. Irreversible ototoxicity Adverse effects
a) Metronidazole
a. Metronidazole • Disulfiram-like effect, Neurotoxic, Dysuria, Cystitis, sense of pelvic pressure,
b. Emetine Metallic bitter taste, GI distress, fatigue
c. Paromomycin b) Emetine
d. Diloxanide furoate • Cardiac arrhythmia, heart failure, hypotension, injection site pain, diarrhea,
e. Iodoquinol nausea, muscle weakness, discomfort
c) Paromomycin
• Parenteral: reversible nephrotoxicity, irreversible ototoxicity
• Oral (rare): abdominal pain, cramping, nausea, vomiting
d) Diloxanide furoate
• Flatulence, nausea vomiting, diarrhea, pruritus
e) Iodoquinol
• Iodine toxicity (dermatitis, urticaria, fever), GI upset, nausea
• High doses: Optic atrophy, permanent loss of vision

The correct answer is: C. Paromomycin


18. Bitter/metallic taste Adverse effects
a) Metronidazole
a. Metronidazole • Disulfiram-like effect, Neurotoxic, Dysuria, Cystitis, sense of pelvic pressure,
b. Emetine Metallic bitter taste, GI distress, fatigue
c. Paromomycin b) Emetine
d. Diloxanide furoate • Cardiac arrhythmia, heart failure, hypotension, injection site pain, diarrhea,
e. Iodoquinol nausea, muscle weakness, discomfort
c) Paromomycin
• Parenteral: reversible nephrotoxicity, irreversible ototoxicity
• Oral (rare): abdominal pain, cramping, nausea, vomiting
d) Diloxanide furoate
• Flatulence, nausea vomiting, diarrhea, pruritus
e) Iodoquinol
• Iodine toxicity (dermatitis, urticaria, fever), GI upset, nausea
• High doses: Optic atrophy, permanent loss of vision

The correct answer is: A. Metronidazole


19. Pain and sterile abscess at the injection Adverse effects
site a) Metronidazole
• Disulfiram-like effect, Neurotoxic, Dysuria, Cystitis, sense of pelvic pressure,
a. Metronidazole Metallic bitter taste, GI distress, fatigue
b. Emetine b) Emetine
c. Paromomycin • Cardiac arrhythmia, heart failure, hypotension, injection site pain, diarrhea,
d. Diloxanide furoate nausea, muscle weakness, discomfort
e. Iodoquinol c) Paromomycin
• Parenteral: reversible nephrotoxicity, irreversible ototoxicity
• Oral (rare): abdominal pain, cramping, nausea, vomiting
d) Diloxanide furoate
• Flatulence, nausea vomiting, diarrhea, pruritus
e) Iodoquinol
• Iodine toxicity (dermatitis, urticaria, fever), GI upset, nausea
• High doses: Optic atrophy, permanent loss of vision

The correct answer is: B. Emetine


20. Dermatitis, urticaria, pruritus and fever Adverse effects
a) Metronidazole
a. Metronidazole • Disulfiram-like effect, Neurotoxic, Dysuria, Cystitis, sense of pelvic pressure,
b. Emetine Metallic bitter taste, GI distress, fatigue
c. Paromomycin b) Emetine
d. Diloxanide furoate • Cardiac arrhythmia, heart failure, hypotension, injection site pain, diarrhea,
e. Iodoquinol nausea, muscle weakness, discomfort
c) Paromomycin
• Parenteral: reversible nephrotoxicity, irreversible ototoxicity
• Oral (rare): abdominal pain, cramping, nausea, vomiting
d) Diloxanide furoate
• Flatulence, nausea vomiting, diarrhea, pruritus
e) Iodoquinol
• Iodine toxicity (dermatitis, urticaria, pruritus, fever), GI upset
• High doses: Optic atrophy, permanent loss of vision

The correct answer is: E. Iodoquinol


ANTIHELMINTHICS
21. Intake of a high-carbohydrate meal Praziquantel is the DOC for cestodes and trematodes. Its plasma concentrations increase
increases the plasma concentration of when taken with or after a high-carbohydrate meal or with Cimetidine (H2 blocker).
which drug?
Albendazole is erratically absorbed, and fatty meals enhance absorption.
a. Albendazole
b. Praziquantel Pyrantel pamoate and Ivermectin are not affected by food.
c. Pyrantel pamoate
d. Ivermectin The correct answer is: B. Praziquantel
22. Oxantel pamoate is primarily used for Oxantel Pamoate (derivative) for treatment of Trichuriasis only (Trichuris trichiuria – aka
the treatment of which parasitic infection? whipworm)

a. Hookworm infection Source: Antihelminthic Trans 2021 pg. 3


b. Whipworm infection
c. Threadworm infection
d. Pinworm infection The correct answer is: B. Whipworm infection
23. Ivermectin causes paralysis in helminths IVERMECTIN
due to the influx of which neurotransmitter • Drug of choice in treating O. volvulus infections
or ion causing hyperpolarization in muscle Drug class:
or nerve cells? • Semi-synthetic analog of Avermectin B1a (insecticide)
• Derived from the actinomycete Streptomyces avermitilis found in soil
a. Chloride Mode of action:
b. Calcium • Intensifies GABA-mediated neurotransmission in nematodes (inhibitory
c. acetylcholine neurotransmitter)
d. sodium • Binds to glutamate-activated Chloride channels found in nematode nerve or muscle
cells which leads to tonic paralysis to the parasites
Spectrum:
• Broad spectrum of infections by:
o Parasitic nematodes
o Microfilaricidal (Onchocerciasis)
o Arthropods such as scabies (that plague livestock & domestic animals)
• Given with DEC to treat filariasis
Pharmacokinetics:
• Given only orally & rapidly absorbed
• Peak plasma levels = 4 hours
• Widely distributed in the tissues
• t½: 16 hours
• Excretion: almost exclusively in the feces
Uses:
• Drug of choice for STRONGYLOIDIASIS & ONCHOCERCIASIS (O.volvulus: River
blindness)
• Alternative for other helminthic infections
• Control of scabies, lice & cutaneous larva migrans
Adverse Effects:
• Mazzotti reaction inflammatory response due to dying microfilariae -> fever, headache,
dizziness, rashes, pruritus, tachycardia, hypotension, arthralgia
CI: Pregnancy

Source: Antihelminthic Trans 2021 pg. 3-4

The correct answer is: A. Chloride


24. Piperazine is an alternative Alternatives boiiiii
antihelminthic for the treatment of which Neurocysticercosis → Praziquantel
infection? Onchocerciasis → Diethylcarbamazine (which cause Mazzotti reaction)
Schistosomiasis → (di ko nakita sa trans pero snearch ko) Oxamniquine (daw)
a. Neurocysticercosis
b. Ascaris
c. Onchocerciasis
d. Schistosomiasis The correct answer is: B. Ascaris
25. Which of the following antihelminthics Both Ivermectin and Diethylcarbamazine produce the adverse effect Mazzotti reaction
can cause Mazzoti reaction? • Ivermectin - inflammatory response due to dying microfilariae → fever, headache,
dizziness, rashes, pruritus, tachycardia, hypotension, arthralgia
a. Pyrantel pamoate • Diethylcarbamazine - May cause Mazzotti reaction when used for onchocerciasis
b. Praziqunatel
c. Diethylcarbamazine
d. Albendazole The correct answer is: C. Diethylcarbamazine
26. Aside from oral administration, THIABENDAZOLE
Thiabendazole can also be given by which • Alternative to Ivermectin and Albendazole for treatment of Strongyloidiasis and
route? Cutaneous larva migrans
• Given orally but can also be absorbed from the skin (topical)
a. Topical
b. Intramuscular Mnemonics: Thiabendazole = T = Topical
c. Subcutaneous
d. Intravenous Adverse Effects:
• Much more toxic than other BZAs
• Irreversible liver failure and fatal Steven-Johnson syndrome have been reported

Source: Antihelminthic Trans 2021 pg. 5

The correct answer is: A. Topical


27. Bioavailability of this drug is markedly Pharmacokinetics of Praziquantel
reduced with intake of corticosteroids: ● Rapidly absorbed via oral route (80% bioavailable)
● Plasma concentrations increase when the drug is taken with or after a high-
a. Albendazole carbohydrate meal or with Cimetidine (H2-blocker) Ivermectin
b. Praziquantel ● Bioavailability is markedly reduced with some antiepileptics (Phenytoin,
c. Ivermectin Carbamazepine) or with corticosteroids
d. Niclosamide ● CSF concentrations reach 14-20% of drug’s plasma concentration
● Rapidly metabolized to inactive mono- & polyhydroxylated products after first pass in
the liver
● Extensive first-pass metabolism to inactive hydroxylated & conjugated products limits
drug bioavailability
● t1⁄2: 0.8-1.5 hours
● Excretion is mainly via the kidneys (60-80%) and bile (15-35%)

Pharmacokinetics of Albendazole
● Erratically absorbed – fatty meal enhances absorption
● Given on an empty stomach against intraluminal parasites and given with a full meal
against tissue parasites
● Mostly protein bound, distributes well to tissues and enters bile, CSF, and hydrated cyst
(caused by E. granulosus)
● Rapidly metabolized in the liver to become Albendazole sulfoxide (active form)

Pharmacokinetics of Ivermectin
● Given only orally & rapidly absorbed
● Peak plasma levels = 4 hours
● Widely distributed in the tissues
● t1⁄2: 16 hours
● Excretion: almost exclusively in the feces

The correct answer is: B. Praziquantel


28. What is the recommended empiric ALBENDAZOLE
therapy to treat those who return from the Pharmacokinetics
tropics with persistent unexplained • Erratically absorbed – fatty meal enhances absorption
eosinophilia? • Given on an empty stomach against intraluminal parasites and given with a full meal
against tissue parasites
a. Albendazole • Mostly protein bound, distributes well to tissues and enters bile, CSF, and hydrated cyst
b. Piperazine (caused by E. granulosus)
c. Bithionol o Importance of penetrating the CSF is because some parasites can travel across
d. Pyrantel pamoate the brain, specifically the larval stage of T. solium causing Neurocysticercosis
• Rapidly metabolized in the liver to become Albendazole sulfoxide (active form)
• t½: 8-12 hours
• Metabolites are excreted in the urine
Clinical Uses
• Drug of choice for:
o Ascariasis
o Trichuriasis (Whipworm infection)
o Hookworm (caused by Ancylostoma & Necator)
o Pinworm (caused by Enterobius)
• Single dose of 400 mg orally
• Hydatid Disease – common sites are the brain and liver (due to E. granulosus & E.
multilocularis)
o Echinococcus spp. are examples of flatworms or cestodes
o DOC is Albendazole for medical therapy and is a useful adjunct to surgical
removal or aspiration of cysts, making it an exemption from Praziquantel as
DOC.
o More active against E. granulosus than E. multilocularis
o Dose: 400 mg 2x daily with meals for one month or longer
• Neurocysticercosis (Taenia solium)
o Albendazole as DOC due to shorter course, lower cost and improved
penetration into the subarachnoid space
o Dose: 400 mg 2x daily for up to 21 days
o Given with corticosteroids # decrease inflammation caused by dying organisms
• DOC for treatment of other infections such as:
o Cutaneous larva migrans (hookworms)
o Visceral larva migrans (hookworms)
o Intestinal capillariasis (Capillaria philippinensis)
o Microsporidial infections
o Gnathostomiasis
• Has minor activity against: (good to know only)
o Taeniasis
o Trichinosis (Trichinella spp.)
o Clonorchiasis
o Toxocoriasis
o Loiasis
o And to control lymphatic filariasis
• Recommended empiric therapy to treat those who return from the tropics with
persistent unexplained eosinophilia
• Ovicidal & Larvicidal
• Combined with DEC or Ivermectin to treat lymphatic filariasis (W. bancrofti & B. malayi)
Adverse Effects/Contraindications
• Used for 1-3 days # nearly free of significantadverse effects
• Common AE: Mild and transient distress, diarrhea, headache, nausea, dizziness,
lassitude & insomnia
• Blood counts & liver function should be monitored during long term therapy
• CI: Hypersensitivity to benzimidazoles, cirrhosis
• Safety of albendazole in pregnancy and in children <2 years old has not been
established. Hence, it is usually contraindicated.
• Reversible leukopenia, thrombocytopenia, alopecia
• Elevation of serum transaminases
• Rare: Jaundice, cholestasis
• Embryotoxic & teratogenic

Source: Antihelminthic Trans 2021 pg. 2-3

The correct answer is: A. Albendazole


29. Mebendazole is active against what MEBENDAZOLE
stage of nematodes’ life cycle? MOA:
• Inhibits microtubule polymerization by binding to β-tubulin (main)
a. Ova • Inhibits mitochondrial fumarate reductase
b. Larva • Reduce glucose transport
c. Adult worm • Uncoupling of oxidative phosphorylation
d. All of the above Spectrum:
• Ovicidal for Ascaris and Trichuris
• Larvicidal - larval and adult stage of nematodes

The correct answer is: D. All of the above


30. Dichlorvos is the active metabolite of METRIFONATE:
which antihelminthic? an organophosphate compound used first as an insecticide & later an anthelmintic a an
alternative treatment to Schistosoma haematobium infection ONLY
a. Oxamniquine
b. Metrifonate MOA: The active metabolite, DICHLORVOS, is thought to inhibit cholinesterase → paralysis
c. Bithionol AE: Mild & transient cholinergic symptoms (DUMBBELS - wet symptoms) - Diarrhea,
d. Niclosamide Urination, Miosis, Bronchoconstriction, Bradycardia, Emesis, Lacrimation, Salivation

The correct answer is: B. Metrifonate


For numbers 31-35. Match the parasitic infection with the antihelminthic of choice for its treatment.
31. Hydatid disease ALBENDAZOLE
• mostly protein bound, distributes well to tissues, enters bile, CSF, and Hydatid cyst
a. Albendazole (caused by E. granulosus)
b. Pyrantel pamoate • DOC:
c. Diethylcarbamazine o Ascariasis
d. Ivermectin o Trichuriasis (whipworm)
e. Praziquantel o Hookworm (Ancylostoma & Necator)
o Pinworm (Enterobius)
o Hydatid Disease
o Neurocysticercosis (question # 35)
o and other infections such as cutaneous larva migrans (hookworm), visceral larva
migrans (hookworm), intestinal capillariasis (Capillaria philippinensis),
microsporidial infections, Gnathostomiasis
• combined with DEC or Ivermectin to treat lymphatic filariasis (W. bancrofti & B. malayi)

Hydatid Disease
• common sites are the brain and liver due to E. granulosus & E. multilocularis
• Echinococcus spp. are examples of flatworms and cestodes
• DOC is albendazole for medical therapy and is a useful adjunct to surgical removal or
aspiration of cysts, making it an exemption from Praziquantel as DOC
• more active against E. granulosus > E. multilocularis
• Dose: 400 mg 2x daily with meals for one month or longer

Recommended empiric therapy to treat those who return from the tropics with persistent
unexplained eosinophilia

Ovicidal & Larvicidal

The correct answer is: A. Albendazole


32. Hymenolepsis nana infection PRAZIQUANTEL - DOC for cestodes and trematodes
MOA:
a. Albendazole • ↑ permeability of trematode and cestode cell membranes to calcium → spastic
b. Pyrantel pamoate paralysis, dislodgement and death
c. Diethylcarbamazine Uses:
d. Ivermectin • DOC for Schistosomiasis
e. Praziquantel • DOC for:
o Hymenolepis nana infection
o Clonorchiasis
o Opistorchiasis
o Paragonimiasis
o Taeniasis
o Diphyllobothriasis
• Alternative to Albendazole in neurocysticercosis

The correct answer is: E. Praziquantel


33. Strongyloidiasis IVERMECTIN
MOA:
a. Albendazole • Intensifies GABA-mediated neurotransmission in nematodes (inhibitory
b. Pyrantel pamoate neurotransmitter)
c. Diethylcarbamazine • Binds to glutamate-activated chloride channels found in nematode nerve or muscle
d. Ivermectin cells → tonic paralysis to the parasites
e. Praziquantel Uses:
• DOC for strongyloidiasis (caused by Strongyloides stercoralis/threadworm causing
larva currens) & onchocerciasis (caused by Onchocerca volvulus causing river
blindness and dermal nodules)
• Control of scabies, lice & CLM

The correct answer is: D. Ivermectin


34. Brugia malayi infection DIETHYLCARBAMAZINE - piperazine derivative
• Direct effects to microfilariae → apoptosis
a. Albendazole Spectrum: Microfilariae (L3)
b. Pyrantel pamoate Uses:
c. Diethylcarbamazine • DOC for filariasis, loiasis & tropical eosinophilia caused by W. bancrofti, B. malayi,
d. Ivermectin Loa loa
e. Praziquantel • Replaced by Ivermectin for Onchocerciasis

The correct answer is: C. Diethylcarbamazine


35. Neurocysticercosis Neurocysticercosis (Taenia solium)

a. Albendazole ALBENDAZOLE
b. Pyrantel pamoate • DOC due to shorter course, lower cost, and improved penetration into subarachnoid
c. Diethylcarbamazine space (Albendazole can penetrate CSF)
d. Ivermectin • Dose: 400 mg 2x daily for up to 21 days
e. Praziquantel • Given with corticosteroids → decrease inflammation caused by dying organisms

The correct answer is: A. Albendazole


For numbers 36-40. Match the parasitic infection with the alternative drug for its treatment.
36. Strongyloidiasis a) Bithionol - DoC for Fasciola hepatica; alternative for P. Westermani
b) Thiabendazole - alternative for Strongyloides stercoralis, cutaneous larva migrans,
a. Bithionol and Dracunculus medinensis
b. Thiabendazole c) Niclosamide - DoC for Fasciolopsis buski, Heterophyes heterophyes, Metagonimus
c. Niclosamide yokogawai, Taenia saginata, Diphyllobothrium latum, Taenia solium; alternative for
d. Praziquantel Hymenolepis nana
e. Metrifonate d) Praziquantel - DoC (either Praziquantel or Niclosamide) for F. buski, H. heterophyes,
f. Oxamniquine T. saginata, D. latum, T. solium; DoC (Praziquantel only) for H.nana; alternative for
Cysticercosis
e) Metrifonate - alternative for Schistosoma haematobium
f) Oxamniquine - alternative for Schistosoma mansoni

THIABENDAZOLE
MoA: same with Mebendazole → selectively inhibits microtubule synthesis and glucose uptake
in nematodes
Use: see above
Toxicity: GI irritation, headache, dizziness, drowsiness, leukopenia, hematuria, allergic
reactions; irreversible liver failure and SJS. Avoid in pregnant patients, patients with
hepatic/renal disease
ref: Katzung 14th ed. Table 53-1

The correct answer is: B. Thiabendazole


37. Neurocysticercosis PRAZIQUANTEL
MoA: increases membrane permeability to calcium, causing marked contraction initially then
a. Bithionol paralysis of trematode and cestode muscles; this is followed by vacuolization
b. Thiabendazole Use: refer to #36 ratio
c. Niclosamide Toxicity: heaache, dizziness, drowsiness, malaise; Neurologic effects can occur in treatment
d. Praziquantel of neurocysticercosis → intracranial hypertension, seizures; Contraindicated in ocular
e. Metrifonate cysticercosis
f. Oxamniquine
The correct answer is: D. Praziquantel
38. Fascioliasis In the book, there are no alternatives for Fascioliasis (F. buski/ F. hepatica). Bithionol is drug
of choice for F. hepatica
a. Bithionol
b. Thiabendazole BITHIONOL
c. Niclosamide MoA: not in the book
d. Praziquantel Use: refer to #36 ratio
e. Metrifonate Toxicity: nausea/vomiting, diarrhea, abdominal cramps, dizziness, headache, skin rash,
f. Oxamniquine phototoxicity

The correct answer is: A. Bithionol


39. Schistosoma haematobium infection METRIFONATE
MoA: transformed to dichlorvos (active metabolite); Cholinesterase inhibition → temporarily
a. Bithionol paralyzes adult worms → shift from the bladder venous plexus to small arterioles of the lungs,
b. Thiabendazole where they are killed. Not effective against S. haematobium eggs.
c. Niclosamide Use: Refer to #36 ratio
d. Praziquantel Toxicity: mild and transient cholinergic symptoms → nausea/vomiting, diarrhea, abdominal
e. Metrifonate pain, bronchospasm, headache, sweating, fatigue, weakness, dizziness, vertigo;
f. Oxamniquine contraindicated in pregnancy

The correct answer is: E. Metrifonate


40. Hymenolepis nana infection NICLOSAMIDE
MoA: may act by uncoupling oxidative phosphorylation or by activating ATPases
a. Bithionol Use: Refer to #36 ratio
b. Thiabendazole Toxicity: GI distress, headache, rash, fever. Avoid ethanol consumption for 24-48 hours
c. Niclosamide
d. Praziquantel
e. Metrifonate
f. Oxamniquine The correct answer is: C. Niclosamide
ANTI-DIARRHEALS/ ANTI-MOTILITY DRUGS
41. Which of the following is the mechanism Ref: Dr. Ferrer ppt slide #6
of action of dopamine receptor antagonist? ● Dopamine exhibits inhibitory effects on motility by suppressing Ach release from
myenteric motor neurons
a. Enables motility by suppressing ● Dopamine receptor antagonists act by: Antagonizing the inhibitory effect thereby
acetylcholine release enabling GI motility
b. Inhibits motility by suppressing ● May relieve nausea and vomiting by antagonizing the dopamine receptors in the
acetylcholine release chemoreceptor zone in the medulla
c. Enables motility by antagonizing
inhibitory effect of dopamine
d. Inhibits motility by suppressing
dopamine release The correct answer is: C. Enables motility by antagonizing inhibitory effect of dopamine
42. What is the mainstay in the treatment of Ref: 2021 Trans, Drugs Affecting GIT Motility, page 3
diarrhea? Oral Rehydration Therapy
● Main approach to treatment
a. Loperamide ● Components:
b. Probiotics ○ Sodium chloride – 2.6g
c. Racecadotril ○ Potassium chloride – 1.5g
d. Oral rehydration therapy ○ Sodium citrate – 2.9g
○ Glucose – 13.5g
○ Water – 1 liter

The correct answer is: D. Oral rehydration therapy


43. HR, 10 year old male, experienced Adverse effects of the following:
vomiting. He was given a drug that caused a) Hyoscine- constipation, dry mouth
acute dyskinesia. What was this drug? b) Ondansetron- constipation, diarrhea
c) Metoclopramide- extrapyramidal symptoms (i.e. involuntary movements such as
a. Hyoscine dyskinesia and dystonia)
b. Ondansetron d) Diphenhydramine- sedation
c. Metoclopramide
d. Diphenydramine The correct answer is: C. Metoclopramide
44. What is the site of action of 5-HT3
antagonists in preventing emesis?

a. Vestibular nuclei
b. Vomiting center
c. Chemoreceptor trigger zone

5HT3 receptor antagonists suppresses vomiting by acting on the 5HT3


receptors in the chemoreceptor trigger zone

The correct answer is: C. Chemoreceptor trigger zone


45. What is the main site of action of H1 H1 receptor antagonists include diphenhydramine, promethazine and cyclizine. They block
antagonists in preventing emesis? H1 receptors at the vestibular afferents.

a. Vomiting center
b. Vestibular nuclei
c. Chemoreceptor trigger zone The correct answer is: B. Vestibular nuclei
46. TH, 26 y/o female, experienced Adverse effects of the following:
abdominal cramping. He was given a drug a) Dronabinol- dizziness, euphoria
that caused constipation and dry mouth. b) Domperidone- dry mouth, headache
Which among the following most likely c) Diphenhydramine- sedation
caused it? d) Hyoscine- constipation, dry mouth

a. Dronabinol
b. Domperidone
c. Diphenhydramine
d. Hyoscine The correct answer is: D. Hyoscine
47. What is the mechanism of action of The term "motilide" is derived from the words "motilin" and "macrolide," indicating that the
motilides? macrolide antibiotics, such as erythromycin, are motilin agonists and bind to the motilin
receptor. They mimic the effects of motilin which induces the phase III migrating motor complex
a. Stimulates motilin receptors in the activity and increases smooth muscle contractility, affecting mainly the upper GIT.
GI smooth muscle
b. Stimulates dopamine in the GI
smooth muscle
c. Inhibits motilin receptors in the GI The correct answer is: A. Stimulates motilin receptors in the GI smooth muscle
smooth muscle
48. Which of the following is inhibited by Racecadotril is a dipeptide that reduces secretion of water and electrolytes into the intestine
Racecadotril? by inhibiting enkephalinase (Enkephalinase produces encephalin, a potent contractile agent).

a. Enkephalinase
b. Serotonin
c. Dopamine
d. Motilin The correct answer is: A. Enkephalinase
49. MV, 48 y/o female, has breast cancer Ondansetron suppresses vomiting by acting on the 5HT3 receptors in the chemoreceptor
and is undergoing chemotherapy. Which trigger zone. It is the drug of choice for chemotherapy/radiation induced emesis.
among the following anti emetics should be
prescribed to her to prevent emesis?

a. Cyclizine
b. Hyoscine
c. Diphenhydramine
d. Ondansetron The correct answer is: D. Ondansetron
50. What is the common adverse effect of Serotonin Receptor Agonists (i.e., Cisapride, Prucalopride) A/E: Severe constipation. From
anti-diarrheals? Goodman and Gilman’s
Opioids (i.e., Loperamide): Inhibits motility leading to constipation
a. Gastric irritation Muscarinic Receptors (i.e., Dicyclomine): A/E: Constipation, dizziness, and drowsiness
b. Constipation Adsorbents (i.e., Kaolin/Pectin): A/E: Absorbs fluids leading to constipation
c. Dizziness
d. Drowsiness
The correct answer is: B. Constipation
For numbers 51-55. Match the drug with the type of vomiting it will be most effective against.
51. Ondansentron Ondansetron is the drug of choice for chemotherapy/radiation-induced emesis.

a. Cytotoxic drug-induced emesis


b. Vestibular The correct answer is: A. Cytotoxic drug-induced emesis
52. Dronabinol Dronabinol is used for chemotherapy-induced nausea and vomiting in patients who fail to
respond to more conventional anti-emetics
a. Cytotoxic drug-induced emesis
b. Vestibular The correct answer is: A. Cytotoxic drug-induced emesis
53. Diphenhydramine Diphenhydramine works by blocking H1 receptors at the vestibular afferents.

a. Cytotoxic drug-inducd emesis


b. Vestibular The correct answer is: B. Vestibular
54. Metoclopromide For prevention of chemotherapy-induced emesis, metoclopramide can be given.

a. Cytotoxic drug-inducd emesis


b. Vestibular The correct answer is: A. Cytotoxic drug-induced emesis
55. Cyclizine Cyclizine is under the piperazines which are used for motion sickness, vertigo and sedation.
Anti-nausea properties are due to prominent anticholinergic effects.
a. Cytotoxic drug-inducd emesis
b. Vestibular The correct answer is: B. Vestibular
For numbers 56-60. Match the drug with its mechnanism of action.
56. Metoclopromide Metoclopramide is both a dopamine receptor antagonist and a serotonin receptor agonist (5-
HT receptors agonist). Its mechanism of action is to enhance coordinated contraction that
a. 5-HT4 receptor agonist enhance transit of GI material. It mainly affects the upper GIT:
b. Dopamine receptor antagonist ● Increases lower esophageal sphincter tone
c. Motilin receptor antagonist ● Stimulates antral and small intestinal contractions
d. 5-HT3 receptor antagonist
e. Both A and B Dopamine receptor antagonists act by antagonizing the inhibitory effect thereby enabling GI
motility.
● Dopamine exhibits inhibitory effects on motility by suppressing Ach release from
myenteric motor neurons

Serotonin Receptor Agonist act by stimulating 5-HT4 recceptos resulting in increased motility
in the upper GIT
● 5-hydroxytryptamine receptors or 5-HT receptors or serotonin receptors play important
roles in the motor and secretory functions of the gut by triggering the peristaltic reflex

The correct answer is: E. Both A and B


57. Domperidone Domperidone is a dopamine receptor antagonist
● it antagonizes mainly D2 receptors
a. 5-HT4 receptor agonist ● enhances coordinated conditions that enhance transit of GI material
b. Dopamine receptor antagonist
c. Motilin receptor antagonist Dopamine receptor antagonists act by antagonizing the inhibitory effect thereby enabling GI
d. 5-HT3 receptor antagonist motility.
e. Both A and B ● Dopamine exhibits inhibitory effects on motility by suppressing Ach release from
myenteric motor neurons

The correct answer is: B. Dopamine receptor antagonist


58. Cisapride Cisapride is a 5-HT4 receptor agonist (serotonin receptor agonist)
● this drug is a gastroprokinetic agent that increases motility in the upper GI tract
a. 5-HT4 receptor agonist ● it acts directly as serotonin 5-HT receptor agonists
b. Dopamine receptor antagonist
c. Motilin receptor antagonist Serotonin Receptor Agonist act by stimulating 5-HT4 recceptos resulting in increased motility
d. 5-HT3 receptor antagonist in the upper GIT
e. Both A and B ● 5-hydroxytryptamine receptors or 5-HT receptors or serotonin receptors play important
roles in the motor and secretory functions of the gut by triggering the peristaltic reflex

The correct answer is: A. 5-HT4 receptor agonist


59. Erythromycin Erythromycin mimics the effects of motilin. It induces phase III migrating motor complex
activity, increases smooth muscle contractility and affects mainly upper GI
a. 5-HT4 receptor agonist
b. Dopamine receptor antagonist Motilin is a 22-amino acid peptide hormone found in the GI, M cells and in some
c. Motilin receptor antagonist enterochromaffin cells of the small intestines
d. 5-HT3 receptor antagonist ● it is a potent contractile agent
e. Both A and B ● modifies act by directly stimulating motilin receptors in GI smooth muscle and promoting
the onset of a migrating motor complex

The correct answer is: C. Motilin receptor antagonist


60. Ondansentron Ondansetron suppresses vomiting by acting on the 5HT3 receptors in the chemoreceptor
trigger zone.
a. 5-HT4 receptor agonist
b. Dopamine receptor antagonist
c. Motilin receptor antagonist
d. 5-HT3 receptor antagonist
e. Both A and B The correct answer is: D. 5-HT3 receptor antagonist
AMINOGLYCOSIDES, GLYCOPEPTIDES AND SULFONAMIDES
61. Which of these reactions is the process Sulfonamides are metabolized mainly in the liver via acetylation.
for hepatic metabolic alteration of ● It can be disadvantageous because the compound is inactivated but retains the toxic
sulphonamides? properties of the parent compound

a. Hydrolysis
b. Demethylation
c. Glucoronidation
d. Acetylation The correct answer is: D. Acetylation
62. RR is a 61 year old male with Clindamycin inhibits protein synthesis binding to the 50s ribosomal subunit. It is indicated for
uncontrolled diabetes mellitus and the treatment of skin and soft tissue infections caused by Streptococci and Staphylococci
hypertension. He was admitted to the
hospital because of high fever and a local
infection of right big toe 2 cm wound
involving only the skin. Which of these oral
antibiotics would be the best choice for his
condition?

a. Erythromycin
b. Streptomycin
c. Clindamycin
d. Amoxicillin The correct answer is: C. Clindamycin
63. A single dose administration is currently Aminoglycosides are concentration-dependent that is why once daily dosing is preferred
recommended for aminoglycosides largely ● Concentration-dependent killing: increasing concentrations kill an increasing
because they act based on this principle: proportion of bacteria or at a more rapid rate
● It must be given to patients with creatinine clearance of 80-100 mL/min and plasma
a. Pre-antibiotics effect concentrations must be monitored
b. Time-dependent killing
c. Concentration-dependent killing Aminoglycosides also have a post-antibiotic effect (not pre-antibiotic)
d. Synergistic effect ● residual bactericidal activity persisting even after the serum concentration has fallen
below the minimum inhibitory concentration

The correct answer is: C. Concentration-dependent killing


64. GK is a 25-year old male diagnosed with Streptomycin is given only intramuscularly. Other than being a 2nd line treatment for anti-
a gram-negative skin infection. Which of TB, it is also useful for enterococcal infections.
these antibiotics would be the best choice
for his condition? [Natural] Penicillin is administered intravenously and intramuscularly. Natural penicillins have
limited activity against gram-negative organisms, but is considered as drugs of choice for
a. Streptomycin several infections caused by susceptible gram positive aerobic organisms.
b. Penicillin
c. Kanamycin Kanamycin is available in oral, intravenous, and intramuscular forms.
d. Neomycin
Neomycin is mainly indicated for topical medication of susceptible infections.

The correct answer is: D. Neomycin


65. Which of the drugs is considered as Neomycin is too toxic for parenteral use.
“systemic” and most be administered only
parenterally due to lipophilicity? Amikacin
• BROADEST spectrum compared with Gentamicin, Tobramycin, and Netilmicin
a. Amikacin • Most prominent characteristic:
b. Kanamycin o Resistant to many enzymes that inactivate Gentamicin and Tobramycin
c. Neomycin • The activity of Amikacin continues to increase as its plasma level rises above the
d. Tobramycin minimal inhibitory concentration (MIC).
• Amikacin continues to exert antibacterial effects even after plasma levels decrease
below detectable levels

The correct answer is: A. Amikacin


66. The aminoglycoside kanamycin’s Kanamycin is an aminoglycoside, making it an irreversible protein synthesis inhibitor.
mechanism of bactericidal action is:
Glycopeptides are cell wall synthesis inhibitors.
a. Inhibit protein synthesis Sulfonamides inhibit dihydropteroate synthetase, whereas trimethoprim inhibits dihydrofolate
b. Block cell wall synthesis reductase. These enzymes are needed in the synthesis of tetrahydrofolic acid, the active form
c. Folic acid synthesis inhibitor of folate. These makes them folic acid synthesis inhibitors. Moreover, tetrahydrofolic acid is
d. Nucleic acid synthesis inhibitor further on used in the production of DNA, also making these drugs nucleic acid synthesis
inhibitors.
The correct answer is: A. Inhibit protein synthesis
67. PK is a 50 year old female who Neuromuscular blockade is an adverse reaction caused by aminoglycosides. This is most
underwent an emergency abdominal likely to occur in those who receive neuromuscular-blocking agents, who receive general
surgical procedure using general anaesthesia, or who has myasthenia gravis. The other conditions are not adverse effects of
inhalational anesthesia. She was on aminoglycosides.
Aminoglycoside prior to surgery. At the RR,
vital signs were normal but she developed Adverse Reactions of Aminoglycosides:
difficulty of breathing and had to be put on ● Irreversible ototoxicity
temporary ventilation-assist. What could ○ Predominantly cochlear toxicity: Amikacin, Neomycin, Kanamycin
have caused the post-operative event? ○ Predominantly vestibular toxicity: Streptomycin, Gentamicin
○ Equal vestibular and cochlear toxicity: Tobramycin
a. Idiosyncratic truncal rigidity ○ Least ototoxic: Netilmicin
b. Myasthenia gravis ● Nephrotoxicity
c. Neuromuscular blockade ○ Most nephrotoxic: Neomycin
d. Allergy to general anesthetics ○ Least nephrotoxic: Streptomycin
● Neuromuscular blockade
○ Neomycin > Streptomycin > Netilmicin > Kanamycin > Amikacin = Tobramycin
○ Treated with intravenous calcium salts
● Hypersensitivity reactions

The correct answer is: C. Neuromuscular blockade


68. GD is a 30 year old male diagnosed with “Pseudomonas is susceptible to some aminoglycosides, for example gentamicin, amikacin, and
cystic fibrosis. He was admitted to the tobramycin.” The others are not indicated for Pseudomonas infection.
hospital due to a Pseudomonas infection
which of these drugs can be administered
for him?
a. Neomycin
b. Tobramycin
c. Clindamycin
d. Kanamycin The correct answer is: B. Tobramycin
69. Which of these drugs is used as a Streptomycin is a 2nd line treatment for anti-TB; the others are not.
second-line treatment of tuberculosis?

a. Kanamycin
b. Streptomycin
c. Azithromycin
d. Gentamicin The correct answer is: B. Streptomycin
70. WG is a 45 year old male who was Red-neck syndrome occurs if the drug (vancomycin) is given rapidly through IV infusion. The
being administered n Aminoglycoside drug others do not exhibit this adverse effect.
through his vein. As this was being done,
the resident noted pruritus and flushing of
his face, neck and torso. Which of these
drugs may be responsible for the signs and
symptoms?

a. Amikacin
b. Gentamicin
c. Clindamycin
d. Vancomycin The correct answer is: D. Vancomycin
71. PK is a 29 year old male diagnosed with Clindamycin is indicated for treatment of infections caused by susceptible Bacteroides sp and
actinomycoses. Which of these agents other anaerobes (actinomyces in this case). It is recommended for prophylaxis of endocarditis
would be appropriately used to treat him as in patients with specific valvular heart disease who are undergoing certain dental procedures
he is allergic to Penicillin? and have significant Penicillin allergies.

a. Vancomycin Other Clinical Uses of Clindamycin:


b. Clindamycin ● Treatment of skin and soft tissue infections caused by Streptococci and Staphylococci
c. Kanamycin ● May be active against community-acquired strains of methicillin-resistant S. aureus
d. Streptomycin ● In conjunction with Penicillin G to treat Toxic Shock Syndrome or necrotizing fasciitis
caused by Group A Streptococcus
● In combination with an aminoglycoside or cephalosporin to treat penetrating wounds of
the abdomen and the gut; infections originating in the female genital tract
● Clindamycin + Primaquine: alternative to trimethoprim-sulfamethoxazole for moderate
to moderately severe Pneumocystis jiroveci pneumonia in AIDS patients
● In combination with pyrimethamine for AIDS-related toxoplasmosis of the brain

Reference: Katzung 14th Ed.

The correct answer is: B. Clindamycin


72. Which other glycoside drug is used to CYCLOSERINE
treat tuberculosis and sometimes for urinary • It is an antibiotic produced by Streptomyces orchidaceous
tract infection but whose intake must be • It is water soluble and very unstable in acid Ph
monitored vigilantly as it causes CNS • It is active against gram (+) and gram (-) organisms but is used almost exclusively to
toxicity? treat tuberculosis caused by strains of Mycobacterium tuberculosis resistant to first-line
agents
a. Bacitracin • Most of the drug is excreted in active form into the urine
b. Cycloserine • Adverse reactions: serious dose-related CNS toxicity
c. Fosfomycin
d. Clindamycin The correct answer is: B. Cycloserine
73. For the treatment of enterococcal Penicillin (beta-lactam) plus streptomycin (aminoglycoside) is effective for enterococcal
endocarditis,which of these drug groups is endo- carditis and 2-week therapy of viridans streptococcal endocarditis.
best combined with an Aminoglycoside?
a. Beta-lactam from katzung 13th Edition page 802.
b. Macrolide
c. Fluoroquinolone
d. Sulphonamide The correct answer is: A. Beta-lactam
74. Which of these processes is the VANCOMYCIN
mechanism of action of vancomycin? Mechanism of Action: Inhibits cell wall synthesis by interfering with the second stage of
peptidoglycan synthesis
a. Nucleic acid synthesis inhibitor
b. Block cell wall synthesis
c. Inhibit protein synthesis
d. Folic acid synthesis inhibitor The correct answer is: B. Block cell wall synthesis
75. Which of these drug groups will act AMINOGLYCOSIDES
synergistically with Vancomycin to help in • A natural product or synthetic derivatives of certain compounds which are produced by
treating hard-to-treat infections? some soil Actinomyces
• Synergism with beta-lactams or vancomycin: in higher concentrations, beta-lactams
a. Beta-lactams may form complexes which loses its activity
b. Fluoroquinolones
c. Anti-retrovirals
d. Aminoglycosides The correct answer is: D. Aminoglycosides
76. When Daptomycin exerts its mechanism DAPTOMYCIN
of action by inserting its “lipid-tail” into cell • The precise mechanism of action is not fully understood, but it is known to bind to the
membrane, which of the following process cell membrane via calcium-dependent insertion of its lipid tail. This results in
occurs to cause cell death? depolarization of the cell membrane with potassium efflux and rapid cell death

a. Necrosis
b. Apoptosis
c. Repolarization
d. Depolarization
The correct answer is: D. Depolarization
77. Among all the aminoglycosides, which a. Netilmicin shares many characteristics with gentamicin. Nephrotoxicity caused by
drug is the most nephrotoxic? Gentamicin is usually reversible. Therefore, this could also be true regarding Netilmicin.
b. “Nephrotoxicity of tobramycin may slightly be less than that of gentamicin.”
a. Netilmicin c. “The most serious toxic effect of streptomycin is disturbance of vestibular function-
b. Tobramycin vertigo and loss of balance.”
c. Streptomycin d. “All members of the neomycin group have significant nephrotoxicity and
d. Neomycin ototoxicity.”

Source: Katzung 13th Ed. Chapter 45

The correct answer is: D. Neomycin


78. Which of these important and “All Aminoglycosides are ototoxic and nephrotoxic. Ototoxicity and nephrotoxicity are more
irreversible adverse drug reaction/s is likely to be encountered when therapy is continued for more than 5 day, at higher doses, in the
shared by Vancomycin and the elderly, and in the setting of renal insufficiency” - Katzung 14th Ed. Chapter 45
Aminoglycosides?
“Vancomycin: Ototoxicity is rare but nephrotoxicity is still encountered regularly with current
a. Ototoxicity preparations. Administration with another ototoxic or nephrotoxic drug, such as
b. Anemia aminoglycoside, increases the risk of these toxicities. Ototoxicity can be minimized by
c. Allergic drug reactions maintaining peak serum concentrations below 60 mcg/mL.” - Katzung 14th Ed. Chapter 43
d. GIT effects
The correct answer is: A. Ototoxicity
79. Adults taking older sulfonamides are Although all of the choices are effects of sulfonamides, it is specifically crystalluria that is
advised to take plenty of fluids or ensure caused by lack of fluid intake. This is because a portion of absorbed drug is conjugated via
urine output of at least 1200 ml because it acetylation or glucuronidation in the liver. Newer generations of sulfonamides are more soluble
may cause: and do not cause much crystallurria.

a. Crystalluria
b. Hematuria
c. Acute haemolytic anemia
d. Steven-Johnson syndrome The correct answer is: A. Crystalluria
80. The relationship between a) Synergistic - produce a combined effect greater than the sum of their separate effects
sulphonamides and trimethoprim is best b) Potentiation- talking about a singular substance and how it may act when in a synergy
describes as: relationship. Meaning only one drug is effective in producing the effect, the other
enhances it.
a. Synergistic c) Antagonism- There is a blocking of effect, decreasing effectivity
b. Potentiation d) Additive- a substance added to something in small quantities to improve
c. Antagonism
d. Additive In any case, both provide a synergistic activity because of sequential inhibition of folate
synthesis

The correct answer is: A. Synergistic


TREATMENT OF ACID PEPTIC DISEASE
81. Sodium bicarbonate is usually not the A disadvantage of Sodium bicarbonate is systemic alkalosis because sodium bicarbonate is
first line antacid to use because it: also produced by the pancreas. Sodium bicarbonate produced by the pancreas gets absorbed
+ the exogenous sodium bicarbonate neutralizing the stomach = systemic alkalosis.
a. Has a low acid neutralizing action
b. Systemic absorption may induce The other choices, A and C, are effects of the other antiacids Kremil S and magnesium
alkalosis hydroxide + aluminum hydroxide respectively
c. May induce diarrhea
d. All of the above are correct
The correct answer is: B. Systemic absorption may induce alkalosis
82. The best time to administer omeprazole: It should be given 30 minutes before meals so the stomach is not that acidic yet because it’s
acid labile.
a. 2 hours before a meal
b. 1 hour and 2 hours after a meal
c. At bedtime
d. 30 – 60 minutes before a meal The correct answer is: D. 30 – 60 minutes before a meal
83. In areas where high resistance to
Clarithromycin has been known, what
alternative antibioticis used in the Triple
therapy of H pylori associated Duodenal
ulcer:

a. Bismuth subcitrate
b. Amoxicillin
c. Metronidazole
d. Ranitidine

The correct answer is: C. Metronidazole


84. Loss of the antiseptic property of the Sucralfate is recommended more than the PPIs and H2 receptor antagonist (H2RAs) since the
stomach is observed in seriously ill patients PPI and H2RAs inhibit acid secretion of the stomach causing the loss of antiseptic ability of the
given the following, EXCEPT: stomach leading to the ascent of bacteria from the lower respiratory tract causing pneumonia.
Sucralfate does not alter acidity of the stomach thus not losing its antiseptic property
a. Misoprostol
preventing the ascent of pathogenic bacterias so less likely to induce hospital acquired
b. Omeprazole
pneumonia.
c. Ranitidine
d. Sucralfate The correct answer is: D. Sucralfate
85. For H pylori associated peptic ulcer Both Triple and Quadruple therapy of H pylori associated peptic ulcer disease are
disease, the best recommended duration of recommended to be given for 14 days for improved healing rate. Complete eradication also
treatment is: promotes long term healing.

a. 14 days Other guidelines include use of PPIs to elevate pH because H. pylori thrive in acidic
b. 7 days environments.
c. 28 days
d. 10 days The correct answer is: A. 14 days
86. Which isoenzyme/s of CYP is/are a) CYP3A4 - Metabolize omeprazole
inhibited omeprazole? b) Sulfotransferase - not an isoenzyme
c) CYP2C19 - Metabolize omperazole but can be inhibited by omeprazole to inhibit its own
a. CYP 3A4 metabolism
b. Sulfotransferase
c. CYP 2C19
d. All of the above The correct answer is: C. CYP 2C19
87. Diarrhea is an adverse effect of which of MISOPROSTOL A/E:
the following anti-ulcer drug/s? • Allergic Reactions
• Abdominal Cramps
a. Misoprostol • Secretory diarrhea
b. Ranitidine • Abortifacient
c. Omeprazole
d. All of the above RANITIDINE A/E:
• Headache
• Diarrhea
• Hypersensitivity reactions
• Arrhythmias with rapid IV infusion

OMEPRAZOLE A/E:
• Headache
• Diarrhea
• Rashes
• Mask symptoms of gastric cancer
• Loss of antiseptic property of the stomach

The correct answer is: D. All of the above


88. At 20 mcg dose, Misoprostol will Misoprostol- Cytoprotective action caused by COX-1:
produce the following effect/s: • stimulate mucin and bicarbonate secretion (pancreas)
• increase mucosal blood flow
a. Increase mucus and endogenous • maintains tight junction between epithelial cells
bicarbonate production • serve to protect the mucosa of the stomach from the influx of acid
b. Enhance mucosal blood flow • Dose: of 20 mcg
c. Decrease gastric acid secretion
d. All of the above
e. A and B only The correct answer is: E. A and B only
89. The rationale for the use of gastric acid PPI-induced elevations of pH not favorable for H. pylori survival (H. pylori wants an acidic
suppressants in the treatment of H pylori in environment) -> Increase pH prevent antibiotic degradation especially Clarithromycin (some
combination with antibacterials include/s: antibiotics gets destroyed in acidic pH) -> Additional antibacterial drugs to eliminate H. pylori

a. Synergistic Recall (Evals 1: Pharmacodynamics)


b. Potentiation TYPES OF AGONISM:
c. Antagonism Synergism (1 + 1 = 3): When the effect of two drugs is greater than the sum of their individual
d. Additive effects
Potentiation (1 + 0 = 3): The activity of one drug is increased by
another drug that does not possess the same activity (One (1) represents the drug that has the
effect, Zero (0) represents the drug that has no
effect)
Additive (1 + 1 = 2): The total effect of the two drugs is the sum of
the individual effects

ANTAGONISM: May be competitive or noncompetitive; two drugs acting on the same drug
target/site (receptor, enzyme, ion channel,
or transport protein)

The correct answer is: A. Synergistic


90. This drug produces the highest acid
neutralizing action at a 1 gram dose:

a. Magnesium hydroxide
b. Sodium bicarbonate
c. Sucralfate
d. Aluminum hydroxide

The correct answer is: A. Magnesium hydroxide


91. Constipation is a common adverse Constipation is a common adverse effect for both Sucralfate and Aluminum hydroxide but
effect with use of: not with Magnesium hydroxide for the adverse effect it produces is diarrhea.

a. Sucralfate
b. Aluminium hydroxide
c. Magnesium hydroxide
d. All of the above
The correct answer is: E. A and B only
e. A and B only
92. The following statements is/are TRUE
regarding use of antacids in acid peptic
diseases:

a. Oral suspension has a faster acid


neutralizing action than tablet form
b. Produce fast onset of pain relief
c. Inhibit pepsin activity
d. All of the above

The correct answer is: D. All of the above


93. The bioavailability of Omeprazole is A figure was presented during the lecture with the accompanying explanation that addition of
markedly increased (almost 100%) by: NaHCO3 to Omeprazole increases its bioavailability in comparison to enteric coated.

a. Simultaneous administration with


sodium bicarbonate
b. Use of enteric coated preparation
c. Administration 30-60 minutes
before breakfast
d. All of the above
This is a very tricky question. The rest of the choices appear to be right because they were
indeed in the lecture, but if you check the context, they are more of explanations as to why
omeprazole has that particular pharmacokinetics.
Enteric coated preparation- PPI’s must be in enteric coating to bypass the stomach to avoid
destruction of the drug by its acidic environment. PPI’s must first be absorbed and distributed
before going to parietal cell, otherwise, it cannot exert its effect.

Giving 30-60 minutes before breakfast merely proves the point that the drug is acid-labile.

The correct answer is: A. Simultaneous administration with sodium bicarbonate


94. Aside from omeprazole, inhibition of Omeprazole is said to inhibit the enzyme CYP2C19, so it can inhibit its own metabolism
isoenzymes of CYP may be induced by: (mentioned in the lecture). It was also mentioned in the lecture that cimetidine inhibits
isoenzymes of CYP and thus has numerous drug interactions. Ranitidine is said to not be
a. Ranitidine extensively metabolized and thus cannot be the answer. There is no mention in the lecture
b. Cimetidine about Misoprostol inhibiting CYP isoenzymes.
c. Misoprostol
d. All of the above The correct answer is: B. Cimetidine
95. The best treatment option for the It was mentioned in the lecture that the best treatment option for the treatment of non-ulcer
treatment of non-ulcer dyspepsia: dyspepsia is a proton pump inhibitor, which is the drug classification of Omeprazole.

a. Omeprazole Antacid is primarily used as symptomatic treatment (“symptomatic


b. Antacid breakthrough adjunct in PPI or H2RA regimen”)
c. Sucralfate
d. Ranitidine Sucralfate is for stress-related ulcers (occur in the context of severe trauma requiring intensive
care) because it is cytoprotective and does not alter acidity of stomach, which means patients
are less prone to hospital-acquired pneumonia.

Ranitidine is part of quadruple therapy- for gastric and duodenal ulcers.

The correct answer is: A. Omeprazole


96. The best recommended drug for NSAID- This was mentioned in the lecture and this figure was shown, proving that Misoprostol is the
induced gastric ulcer and its complications: best choice:

a. Omeprazole
b. Misoprostol
c. Ranitidine
d. All of the above
H2 blockers such as Ranitidine have unproven benefit and proton pump inhibitors such as
Omeprazole have likely complications.
The correct answer is: B. Misoprostol
97. Bismuth subsalicylate is incorporated in This was mentioned during the lecture. Gastric acid suppressant was not mentioned at all- in
the quadruple therapy of H pylori induced fact, drug is said to promote mucin and bicarbonate production.
ulcers because of the following effects:

a. Antibacterial action against H pylori


b. Cytoprotective action
c. Gastric acid suppressant
d. A and B
e. A and C The correct answer is: D. A and B
98. In the Quadruple therapy of H pylori Mentioned during lecture: Omeprazole 2mg BID + Metronidazole 500mg TID + Bismuth
induced ulcers, Metronidazole 500 mg is subsalicylate 525 mg QID + Tetracycline 500mg QID x 14 days
given:

a. Three times a day


b. Once a day
c. Twice a day
d. Four times a day The correct answer is: A. Three times a day
99. The healing rate is highest with use of This was mentioned during the lecture. In fact, the quadruple therapy in number 98 was the
this Anti-H pylori regimen? most emphasized, because of the 97.1% eradication rate.
This figure was also shown:
a. Triple therapy
b. Bismuth based quadruple therapy
c. Non-bismuth based quadruple
therapy
d. All regimens have equal healing
rates

The correct answer is: B. Bismuth based quadruple therapy


100. This anti-ulcer drugs is now considered Misoprostol Adverse Effects:
a regulated drug because it has been 1. Allergic Reactions
misused as an Abortifacient: 2. Abdominal Cramps
3. Secretory diarrhea
a. Sucralfate 4. Abortifacient
b. Misoprostol From Doc’a ppt. The rest of the choices do not have abortifacient effect. Notes from batch 2020
c. Omeprazole say Misoprostol used to be very popular in Quiapo- search Cytotec (brand name) on FB and you will see
d. Ranitidine people selling and buying the drug.

The correct answer is: B. Misoprostol


RATIONALIZATION HEAD: MAR, RPh

CONTRIBUTORS: 12B led by: JP (#1-7) MAR, RPh (#50-55)


13B led by: MD (#8-14) 19B led by: MM (#56-63)
14B led by: DD (#15-21) 20B led by: KC (#64-70)
15B led by: DT (#22-28) 21B led by: RE (#71-77)
16B led by: JH (#28-35) 22B led by: VH (#78-84)
17B led by: EA (#36-42) 23B led by: LR (#85-92)
18B led by: DA (#43-49) 24B led by: MP (#93-100)

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