Chemotherapy of Helminthiasis Drugs Flashcards
(121 cards)
1
Q
What are the DOC for A. lumbricoides?
A
MAPyPi
Mebendazole
Albendazole
Pyrantel pamoate
Piperazine - used less dt occasional neurotox and hypersensitivity
2
Q
What is less often used due to occasional neurotoxicity and hypersensitivity reactions?
A
Piperazine - it greatly reduces the motility of worms reducing the hazard of migration
3
Q
Used for asymptomatic to moderate ascariasis and used with caution to treat heavy as caries infections alone or with hookworms
A
Mebendazole and albendazole
4
Q
Used for heavy infections and safe for use during pregnancy
A
Pyrantel or piperazine
5
Q
What to feed on host blood and fluids which causes iron deficiency anemia and malnutrition?
A
Hookworm
6
Q
What are the first drug of choice for hookworms?
A
Albendazole and mebendazole
7
Q
Heavy mixed infections with ascariasis
Paralyzes ascaris
A
Pyrantel pamoate
8
Q
It is d/t penetration of skin of humans by larvae of dog hookworm (Ancylostoma brazilianse)
A
Cutaneous larva migrans
9
Q
What is the drug of choice for creeping eruption or cutaneous larva migrans?
A
Albendazole or ivermectin
10
Q
Topical or oral thiobendazole is for?
A
Cutaneous larva migrans
11
Q
What is the most effective and safest drug for T. trichiura?
A
Mebendazole and albendazole
Pyr pam - ineffective
12
Q
What is ineffective for the treatment of whipworm?
A
Pyrantel pamoate
13
Q
What is the best drug for the treatment of Strongyloides stercoralis (threadworm)?
A
Ivermectin
Thiabendazole > albendazole > mebendazole
14
Q
DOC for pinworm
A
Pyrantel pamoate and mendazole
Other treatment: albendazole
15
Q
DOC for T. spiralis
A
Mebendazole and albendazole
Against intestinal forms
16
Q
What controls the acute and dangerous symptoms of trichinella spiralis infection?
A
Glucocorticoids
17
Q
What controls the acute and dangerous symptoms of trichinella spiralis infection?
A
Glucocorticoids
18
Q
DOC for filariasis
A
Diethylcarbamazine
19
Q
Treatment for filariae
A
Diethylcarbamazine and ivermectin
- single oral dose of either together with an oral dose of albendazole
20
Q
Treatment for loaisis
A
Diethylcarbamazine
21
Q
Oncocerciasis treatment
A
Ivermectin
22
Q
Drinking water containing copepods that carry infective larvae?
A
Guinea/dragon/medina worm
AKA
Dracunculus medinensis
23
Q
Drug of choice for Dracunculus medinensis
A
Metronidazole 250 mg TIB x 10 days
24
Q
How do you remove slowly Dracunculus medinensis worm?
A
Draw the live adult female worm out day by day by rolling it on to a small piece of wood
25
Drug of choice for capillaria philippinensis
Albendazole
26
What is the drug of treatment for taenia saginata?
Praziquantel
Can also be: niclosamide
27
What is the drug of choice for the treatment of T. solium?
Praziquantel or niclosamide
Cysticercosis: albendazole and praziquantel
28
What is the drug of choice for D. latum?
Praziquantel
Can also niclosamide
29
What is the drug of choice for Hymenolepis nana?
Praziquantel
30
What is the drug of choice for Echinococcus granulosus?
Albendazole - adjuvant to surgery
31
What organs are involved in schistosoma?
S. mansoni & S. japonicum: liver spleen and GI tract
| S. haematobium: lower gut
32
What is the drug of choice for schistosoma?
Praziquantel
33
What is effective against s haematobium but not effective against s monson e & s japonicum?
Metrifonate
34
What is the drug of choice for paragonimus westermani?
Praziquantel (clinical)
35
DOC for clonorchis sinensis (chinese liver fluke), opisthorchis viverrini and opisthorchis felineus
Praziquantel
36
What is the drug of choice for fasiola hepatica?
Bithionol 30-50mg/kg given on alternate days for 10-15 doses
Also Triclabendazole
37
Drug of choice for fasciolopsis buski
Praziquantel or niclosamide
38
What can interfere with insect sodium transport proteins; neurotoxicity and paralysis
Permethrin
39
5% cream, cream rinse, topical solutions
approved for infants greater than or equal to 2 months old
Permethrin
40
Organochlorine compound
| Induces neuronal hyperstimulation and eventual paralysis of parasites
Lindane
41
Second-line drug due to neurotoxicity
```
Inc toxicity in:
• children and adults less than 110 lbs
• patients with underlying skin disorder
- atopic dermatitis
- psoriasis
```
Lindane
42
Organophosphate
Binds acetylcholinesterase in lice; paralysis and death
Approved for treatment of head lice in children less than or equal to six years old
Malathion
43
5% lotion
Treatment of lice - inhi lice from closing their respiratory spiracles (obstruction of spiracles) asphyxiation of lice
More likely to cause resistance than traditional pesticides
Benzyl alcohol
44
Oral anti helminthic drug
Treatment of onchocerciasis and strongyloidiasis
- also for scabies and lice
Ivermectin
45
What has no major cns toxicity because it does not cross the blood brain barrier?
Ivermectin (200ug/kg, may be repeated after a wk - not used in children <15kg)
S/E: dizziness, somnolence, vertigo, tremor
46
What are other treatments for infestations?
* 10% Crotamiton cream and lotion (Eurax)
* 5% pptd sulfur in petrolatum
* for px in whom Lindane or Permethrin are contraIx
47
What are the Benzimidazoles derivatives?
- Thiabendazole
- Mebendazole (prototype)
- Albendazole
48
What are versitile agents highly effective in ascariasis, intestinal capillariasis, enterobiasis, trichuriasis, and hookworm?
Benzimidazoles (TAM)
49
What is the MOA of Benzimidazoles?
Binds to B-tubulin
50
What contains a thiazole ring at position 2, is active against a wide range of nematodes that infect the GIT?
Thiabendazole
51
What is a newer Benzimidazole that is used worldwide, primarily against a var of int abd tissue nematodes?
Albendazole
52
What are drugs highly effective against the hookworm that cause cutaneous larval migrans?
Albendazole although thiabendazole can be used to topically
53
Abs: limited solubility in water, abs rapidly after oral ingestion
Fate: peak plasma conc after 1 hr
EXCRETION: U w/in 24 hrs as 5-hydroxythiabenzadole, conjugated either as the glucoronide or as sulfate
Thiabendazole
54
DOC for cutaneous larva migrans, S. stercoralis, and trichinosis
Thiabendazole
55
What are the common side effects of thiabendazole?
anorexia
nausea
vomiting
dizziness
56
Stevens-Johnson syndrome can be an occasional side effect of?
Thiabendazole
57
```
angioneurotic edema
shock
tinnitus
convulsions
intrahepatic cholestasis
```
Thiabendazole
58
What is the contraindication of thiabendazole?
Should not be used in pregnancy
59
Abs: poorly and erratically abs
Fate: conc in plasma are low, low sys bioavailability (22%), 95% bound to plasma proteins, active form
EXCRETION: conjugates and its metabolites hav been found in BILE, but little unchanged it appears in urine
Mebendazole
60
What are the therapeutic uses of mebendazole?
Enterobiasis, ascariasis, trichuriasis, hookworm, c. philippinensis
61
In cases of massive infestation and expulsion of GI worms, what are the common side effects of mebendazole?
abdominal pain
distension
diarrhea
62
In high doses, what are the common side effects of mebendazole?
```
allergic reaction
alopecia
reversible neutropenia
agranulocytosis
hypospermia
```
63
What are the contraindications for Mebendazole?
Potent embryotoxin and teratogen
64
Abs: variably and erratically abs; enhanced by presence of fatty food and bile salts
Fate: metabolized rapidly in liver and intestine to Albendazole sulfoxide; well distributed into var tissues inc hydatid cyst (1/5)
ELIMINATION: plasma half life from 4-15 hrs; excreted mainly in urine
Albendazole
65
What are the therapeutic uses of albendazole?
Enterobiasis/ascariasis/trichuriasis/hkwrm
Neurocysticercosis cb larval forms of T. solium
Lymphatic filariasis
66
What are the most common side effects of albendazole?
Increase in serum aminotransferase
| - monitor routine liver function during protracted therapy
67
```
Transient abdominal pain
Diarrhea
Nausea
Dizziness
Headache
```
Common side effects of albendazole
68
```
GIT pain
Severe headaches
Fever
Fatigue
Hair loss
Leukopenia
Thrombocytopenia
Teratogenic and embryotoxic
```
Benzimidazoles side effects
69
Contraindications for albendazole
Patients with hepatic cirrhosis
| Pregnant women
70
What is the first line drug for control and treatment of lymphatic filariasis?
Diethylcarbamazine
71
What is the action of the diethylcarbamazine?
It causes microfilariae to disappear from skin in nodules that contain the adult female
72
It does not affect the microfilaria of w bancrofti in a hydrocele
Diethylcarbamazine
73
It may disrupt arachidonic acid metabolism resulting vasoconstriction and aggregation of hosts platelet and granulocytes
Diethylcarbamazine
74
Abs: rapidly from GIT
Fate: peak plasma lvls: w/in 1-2 hrs after a single oral dose
ELIMINATION: T1/2: 2-10 hrs
Excreted by urinary and extra urinary routes
- alkalinizing the urine - elevate plasma lvls and prolong t1/2
• inc therapeutic effect and toxicity
Diethylcarbamazine
75
W. bancrofti, B. malayi and timori
Microfilaremia
Rapid disappearance of sx of tropical eosinophilia
Oncocerciasis
Therapeutic uses for diethylcarbamazine
76
• Direct toxic reactions
• Anorexia, nausea, headache, vomiting
• Mazzotti reaction
- in patients with oncocerciasis
- occurs within a few hours after first oral dose
- intense itching and rashes
- enlargement and tenderness of lymph nodes
- find papular rash
- fever, tachycardia, arthralgia, and headache
Side effects for diethylcarbamazine
77
Effective and highly potent
Immobilizes affected organism by inducing atonic paralysis of the musculature by acting on glutamate-gated chloride channels
Ivermectin
78
Fate: peak plasma lvls - 4-5 hrd after oral admin
Excretion: T1/2 - 57grs - dt low systemic clearance and large volume of distribution
Ivermectin
79
Oncocerciasis
Lymphatic filariasis
Intestinal nematode infections
Other indications
- first line drug cutaneous larva migrans
Therapeutic uses of ivermectin
80
Toxicity Mazzotti-like reactions
Rarely:
High fever, tachycardia, HPOT, prostration, dizziness, headache, myalgia, arthralgia, diarrhea, and facial and peripheral edema
- responds to glucocorticoid therapy
Side effects of ivermectin
81
Impaired blood brain barrier (African trypanosomiasis and meningitis)
Due to its effect on GABA receptors in CNS
Not approve for children less than 5 and pregnant women
Contraindications of ivermectin
82
Organophosphate compound used for treatment of S. haematobium
Metrifonate (Bilaricil)
83
Alternative to praziquantel for treatment of urinary schistosomiasis caused by s haematobium
Metrifonate (Bilaricil)
| 7.5-10mg/kg given orally 3x at intervals of 2 wks
84
At prescription doses: inhibits activities of plasma cholinesterase and erythrocyte acetylcholinesterase
Metrifonate (Bilaricil)
85
Recovery within weeks of stopping treatment
- patients should be free from recent exposure to insecticide
- should not receive and NMBs for at least 24 hours after treatment
Metrifonate (Bilaricil)
86
Second choice for praziquantel for treating human intestinal infections in the treatment of T. saginata, D. latum, H. nana
Niclosamide (Niclocide)
87
Risk for T. solium ova released from drug-damaged gravid worms dev into larva that can cause cysticercosis
Niclosamide (Niclocide)
88
Second choice to praziquantel for treatment of schistosomiasis
S mansoni - highly susceptible
Oxamniquine (Vansil)
89
Broad spectrum anti helminthic agent
But is ineffective against trichuris
Pyrantel pamoate
90
What is the mode of action of Pyrantel pamoate?
Inhibits cholinesterases
| - worm paralysis (spastic by depolarizing NMB agents)
91
Alternative to mebendazole - ascariasis and enterobiasis
Used in combination with Oxantel
Pyrantel pamoate
92
```
Very large doses cause toxic effects
Transient and mild Gi symptoms
Headache
Dizziness
Rash
Fever
```
Pyrantel pamoate side effects
93
Effective against ascaris lumbricoides and enterobius vermicularis
- causes flaccid paralysis an ascaris that results in expulsion of worm by peristalsis
Piperazine
94
What can be an advantage of Piperazine?
It reduces the motility of the worms her by decreasing the hazard of migration
95
Therapeutic uses:
Ascariasis
Enterobiasis
Piperazine
96
ContraIx in patients with epilepsy
Piperazine
97
• LOWEST EFFECTIVE CONCENTRATION CAUSES INCREASED MUSCULAR ACTIVITY FOLLOWED BY CONTRACTION AND SPASTIC PARALYSIS --> WORMS DETACH FROM BLOOD VESSEL WALLS THEN SHIFT FROM MESENTERIC VEIN TO THE LIVER
Praziquantel
98
Increase concentration causes mental damage
Praziquantel
99
Abs: readily abs after oral admin
Fate: peak plasma lvls (1-2 hrs)
- has extensive 1st oass metab
Excretion: T1/2 - 0.8-3 hrs depending on dose
Praziquantel
100
```
Therapeutic uses:
Schistosomiasis
Liver flukes - C. sinensis
O. viverrini
Int flukes ( F. buski, H. hetero, Metagonimous yokogawi)
P. westermani
Fasciola hepatica - unresponsive
```
- stored at temperature <30°C
- bitter
Praziquantel
101
The high-dose treatment alternative therapy for cysticercosis
Praziquantel
102
Side effects:
Abdominal discomfort, pain and nausea, dizziness, drowsiness, headache
Transient and dose related
Neurocysticercosis (meningismus, seizures, mental changes, CSF pleocytosis)
Praziquantel
103
Indirect effects
Fever, pruritus, urticaria, rashes, arthralgia, and myalgia (occ)
Praziquantel
104
Is Praziquantel safe in children >4 y.o?
Yes
105
ContraIx of Praziquantel bcs px may go blind
Ocular cysticercosis
106
Praziquantel's bioavailability is reduced by
Carbamazepine and phenobarbital
107
Teratogenic drugs
Thiabendazole
Mebendazole
Albendazole
108
DOC for S. stercoralis
Ivermectin
109
What level of prevention? To reduce the impact of an ongoing illness that has lasting effects
Tertiary prevention
110
Managing chronic condition to lessen long-term complications
Tertiary prevention
111
Preventing the spread of dse, illness or infxn once it occurs
Secondary prev
112
Reducing the incidence of dse or injury
Primary prevention
113
Preventing exposure to risk factors that promote dse onset
Primordial prevention
114
Adverse effect of Albendazole therapy for px w subarachnoid neurocysticercosis
Meningeal fibrosis
115
Mazotti reaction
DEC
116
Mazotti-like rxn
Ivermectin
117
MOA
may disrupt arachidonic acid in microfilariae and host endothelial cells w resulting vasoconstriction and aggression of host plts and granulocytes around membrane-damage par
DEC
118
MOA
immobilizes affected org by inducing a tonic paralysis of musculature by actung on glutamate gated Cl-channels
Ivermectin
119
Before giving this drug, u have to check liver fxn test bcs it causes hepatotoxicity
Thiabendazole
120
Before giving this drug, u have to check liver fxn test bcs it causes hepatotoxicity
Thiabendazole
121
Occasional GI upset
Transient neurological effects
Urticarial rxns
Lethal doses - convulsing and respi depression
CIx w epilepsy
Piperazine side effects
