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PHARMACOLOGY

PHARMACOTHERAPY OF HELMINTHOSES M04L09


Dr. Calderon
NOV 03 2017

Pharmacotherapy of Helminthoses ALBENDAZOLE


I. Drugs that act against nematodes  Benzimidazole carbamate
II. Drugs that act against trematodes  Administered on an empty stomach when used against
III. Drugs that act against cestodes intraluminal parasites
IV. Cases  Administered with a fatty meal when used against
tissue parasites
Italics – Transers Note, Box – Book, Broken Box – Key points
and Guides

NOTE: SABI NI DOC, MUST KNOW ANG SIGNS AND 3. PYRANTEL PAMOATE
SYMPTOMS OF THE DISEASE, DRUG OF CHOICE FOR  Drug Class: Antihelminthic

THE DISEASE AND SIDE EFFECTS OF THE DRUGS   MOA: Stimulates nicotinic receptors at NMJ of
HAPPY ARAL! nematodes. causes depolarization-induced
paralysis;
DRUGS THAT ACT AGAINST NEMATODES
Note: It doesn’t kill the worm BUT ONLY
1. MEBENDAZOLE PARALYZES it. NOT Ovicidal.
 Drug Class: Antihelminthic

 Clinical Use: Hookworm and roundworm
 MOA: Selectively inhibits microtubule synthesis infections (drug of choice), Pinworms (backup)
(mitosis) and glucose uptake in nematodes;
 Toxicities: GI distress, Headache, Weakness
Ovicidal
 Wide activity against nematodes killing adult
 Clinical Use: Ascariasis, Pinworm, Whipworm worms in the colon but not the eggs
infections (drug of choice), Visceral larval migrans Contraindicated in patients with hepatic
(backup) dysfunction
 Toxicities: Gastrointestinal irritation,
 Combantrin
Agranulocytosis, Alopecia
 Contraindicated in pregnancy
 Antiox 4. THIABENDAZOLE
 Most antihelminthics act like anticancer drugs
because they inhibit the proliferation of cells.  Drug Class: Antihelminthic

 Worms have similar metabolism to humans.  MOA: Selectively inhibits microtubule synthesis
Therefore, systemic toxicity might not be unusual and glucose uptake in nematodes. Inhibits
in treatment of protozoan and worm diseases. fumarate reductase. Ovicidal
 Clinical Use: Trichinosis (drug of choice),
2. ALBENDAZOLE Strongyloidiasis (backup)
 Toxicities: Gastrointestinal irritation, Headache,
 Drug Class: Antihelminthic

Dizziness, Drowsiness, Leukopenia, Hematuria,
 MOA: Inhibits microtubule assembly; Larvicidal Hypersensitivity reactions (SJS), Hepatotoxicity
and ovicidal (intrahepatic cholestasis, liver failure), Reactions
 Clinical Use: Ascariasis, Hookworm, Pinworm, caused by dying parasites
Whipworm infections, Hydatid disease (drug of  Contraindicated in pregnancy
choice), Threadworms, Filariasis, Larva migrans
(backup), Cysticercosis (larval stages of T. solium) Note: DOC for T. spiralis or trichinosis disease (from
 Toxicities: Reversible leukopenia, Alopecia, meat; can infect man and lead to myocitis)
Elevation of liver function tests, Bone marrow
suppression
 Not listed in the Philippine National Drug 5. DIETHYLCARBAMAZINE (DEC)
Formulary. It is only procured by the government  Drug Class: Antihelminthic

 Ideal drug of choice of deworming of children.  MOA: Unknown. Immobilizes microfilariae
 Clinical Use: Filariasis (drug of choice), Eye
worm disease (drug of choice), Onchocerciasis
(backup)
 Toxicities: Headache, Malaise, Weakness,
Anorexia, Filarial fever (fever, rashes, ocular
damage, joint and muscle pain, lymphangitis)

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PHARMACOLOGY DRUGS USED IN HEART FAILURE M03L04

 May cause Mazzotti reaction when used for


onchocerciasis 2. BITHIONOL
 Alternative to triclabendazole for the treatment of
Note: DOC for W. bancrofti or filariasis disease fascioliasis (sheepliver fluke)
 Also an alternative drug in the treatment of
6. IVERMECTIN pulmonary paragonimiasis
 Drug Class: Antihelminthic

 MOA: Intensifies GABA-mediated 3. METRIFONATE
neurotransmission in nematodes. Immobilizes  Alternative drug for the treatment of Schistosoma
parasites. hematobium infections.
 Clinical Use: Onchocerciasis, Cutaneous larva  MOA: cholinesterase inhibition; this inhibition
migrans, Strongyloidiasis (drug of choice) temporarily paralyzes the adult worms
 Toxicities: Mazzotti reaction (fever, headache,  Combined with oxamniquine for mixed infections of
dizziness, rashes, pruritus, tachycardia, S haematobium and S mansoni
hypotension, pain in joints, muscles and lymph
 Toxicities: Nausea and vomiting, diarrhea,
glands)
abdominal pain, bronchospasm, headache, sweating,
 Contraindicated in pregnancy fatigue, weakness, dizziness, and vertigo
Note: Mazzoti reaction- flu-like symptoms that 4. OXAMNIQUINE
results after treatment on Diethylcarbamazine or
Ivermectin  Alternative to praziquantel for the treatment of S
mansoni infections
Onchocerca volvulus  Active against both mature and immature stage of S
- causes onchocerciasis, mansoni but does not appear to be cercaricidal
- transmitted by female blackfly (Simulium).  MOA: Unknown. Contraction and paralysis of the
- clinical findings: dermal nodules worms
hanging groin, lizard skin, river blindness  Effective in instances of praziquantel resistance
 Toxicities: CNS symptoms (dizziness, headache,
DRUGS THAT ACT AGAINST TREMATODES drowsiness), nausea and vomiting, diarrhea, colic,
pruritus, and urticaria. Infrequent adverse effects are
1. PRAZIQUANTEL low-grade fever, orange to red discoloration of the
urine, proteinuria, microscopic hematuria, and a
 Drug Class: Antihelminthic
 transient decrease in leukocytes
 MOA: Increases membrane permeability to
calcium. Causes muscle paralysis, vacuolization DRUGS THAT ACT AGAINST CESTODES
and death.
 Clinical Use: Drug of choice for trematodes 1. NICLOSAMIDE
(Schistosoma, Paragonimus, Clonorchis,  Drug Class: Antihelminthic

Opistorchis) and cestodes (Taenia,
Diphyllobothrium)  MOA: Uncouples oxidative phosphorylation or
by activating ATPases
 Toxicities: Headache, Dizziness, Nausea, Malaise
 Contraindicated in ocular cysticercosis (may  Clinical Use: Alternative drug for cestode
cause irreparable eye damage),
Used with infections (Taenia, Diphyllobothrium)
corticosteroids in treating neurocysticercosis.  Toxicities: Gastrointestinal distress, headache,
rash, fever
Note: S. japonicum-acquired by swimming or drinking  Kills scolices and cestode segments but has no
infected water; effect on ova.Avoid ethanol consumption for 48h
upon drug administration.
Paragonimiasis- acquired by ingestion of raw
crabmeat

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PHARMACOLOGY DRUGS USED IN HEART FAILURE M03L04

CASES 3. A 50 year-old seaport carrier complains of cough for more


than one month, with hemoptysis. TB work-up was negative.
1. A 10-year-old girl from Forbes Park, Makati has had Further history reveals he is fond of eating pickled crabs
abdominal pain and cramps for the past few days. Her (burong talangka) when binge-drinking in his town. A repeat
examination produced normal findings except for nonspecific CXR showed a ring-shadowed opacity, and a sputum
abdominal discomfort with a complete blood count showing examination was positive for eggs. Which is the most
anemia and 22% eosinophilia. A stool specimen revealed the appropriate treatment?
characteristic eggs of A. lumbricoides. Which is the most
appropriate treatment? A. Praziquantel
B. Thiabendazole
A. Albendazole C. Ivermectin

B. Praziquantel D. Albendazole
C. Piperazine
D. Bithionol

2. A 30 year-old Filipino male working in Sudan is being


treated for Onchocerca volvulus infection. He then develops
fever, headache, dizziness, rashes, pruritus, pain in joints,
muscles and lymph glands. The physician suspects that he had
a Mazzotti reaction, which is due to which of the following?

A. Increased GABA-mediated neurotransmission


B. Inflammatory reaction to lysis of the worms
C. Nicotinics stimulation at the myoneural junctions of
nematodes
D. Stress-induced hemolysis 


APPENDIX

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PHARMACOLOGY DRUGS USED IN HEART FAILURE M03 L04

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