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Spring 2018 Pharm Exam 4 > #4: Anti Hemilith Drugs > Flashcards

#4: Anti Hemilith Drugs Flashcards

1
Q

Types of Parasitic Worms + infxn they cause

  1. Nematodes (roundworms) –>
  2. Trematodes (flukes) –>
  3. Cestodes (tapeworms) –>
A

Types of Parasitic Worms + infxn they cause

  1. Nematodes (roundworms) –> ascaris
  2. Trematodes (flukes) –> schistosoma
  3. Cestodes (tapeworms) –> Taenia
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2
Q
  1. Metabolic NRG production
  2. Motor activity + motility of org
  3. Cytoskeletal filament proteins

targets for

A

Drugs for Anti-Hemiliths target

  1. Metabolic NRG production
  2. Motor activity + motility of org
  3. Cytoskeletal filament proteins
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3
Q

Anti-Hemilith Infxns/Drugs

  1. infxns come from ____ or _____
  2. drugs usu eff vs what two stages of hemilith life cycle
  3. when given Tx w/non-absorbable drugs where are only infxns useful in
A

Anti-Hemilith Infxns

  1. infxns come from eating contaminated food or organisms penetrating skin
  2. drugs eff vs larvae + microfilariae stages
    (efficacy for eggs or adult worms depends on various things)
  3. Tx w/non-absorbable drugs –> only useful for infxns in GI lumen
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4
Q

Benzimidazole Class

  1. What are the 2 drug prototypes
  2. what do both drugs get metab by
  3. CYP inhib (Cimeditine) –> incr drug levels –>
  4. called the ____ _____ _____
A

Benzimidazole Class

  1. What are the 2 drug prototypes
    - Albendazole
    - Mebendazole
  2. both drugs get metab by CY34A
  3. CYP inhib (Cimeditine) –> incr drug levels –> toxicities
  4. Called the Mitotic Spindle poisons
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5
Q

which drugs bind to b-tubulin –> inhibit microtuble polmerization –> microtubules disappear

A

Benzimidazole Class

  • Albendazole
  • Mebendazole
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6
Q

Benzimidazole Class MOA

  1. microtubules disappearing –> lead to what in parasite
  2. How do these drugs exhibit selective toxicity
  3. Overall what do they do (MOA)
A

Benzimidazole Class MOA

  1. microtubules disappearing –> immobilization/death of parasite
  2. Selective toxicity –> greater affinity for parasite b tubulin
  3. Overall –> suppress ATP production in parasite
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7
Q

Albendazole ADME

  1. 2 things that incr abs of drug
  2. Active metabolite albendazole sulfoxide penetrates tissues and hydatid cysts –> contain what/what infxn used for
  3. what 2 types of infxns (locations) is drug used for
A

Albendazole ADME

  1. fatty foods + bile salts incr abs of drug
  2. Active metabolite albendazole sulfoxide penetrates tissues and hydatid cysts –> tapeworms –> for tapeworm infxns
  3. for GI and systemic infxns
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8
Q

Albendazole vs Mebendazole ADME

  1. which is poorly absorbed
    - therefore which is only used for GI tract infxns and not for systemic infxns
A

Albendazole vs Mebendazole ADME

  1. Mebendazole = poorly absorbed –> only for GI tract infxns and not for systemic infxns
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9
Q
  1. Myelosuppression
  2. Alopecia
  3. Liver Abn (incr aminotransferase)

AEs of what drugs

A

Albendazole and Mebendazole AEs

  1. Myelosuppression
  2. Alopecia
  3. Liver Abn (incr aminotransferase)
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10
Q

Albendazole and Mebendazole AEs

  1. who CI in what pop group and age group
  2. what is the unique AE a/w Mebendazole and high dose therapy
A

Albendazole and Mebendazole AEs

  1. CI in preg women + kids < 2
  2. unique AE a/w Mebendazole and high dose therapy = Occipital seizures
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11
Q

Albendazole and Mebendazole Uses

  1. what type of parasitic worm is it used for and where in body (2)
  2. what spp infxn does it tx (hint: swollen LE)
A

Albendazole and Mebendazole Uses

  1. for nematodes
    - GI lumen and systemic infxns
  2. Txts Lymphatic filariasis (elephantiasis)
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12
Q

Albendazole and Mebendazole Uses: Lymphatic filariasis (elephantiasis)

  1. what is the combo therapy used (2 drugs, which in this class
  2. duration of Tx
A

Albendazole and Mebendazole Uses: Lymphatic filariasis (elephantiasis)

  1. combo therapy used = Albendazole + Ivermectin/DEC
  2. long duration of Tx (up to 5 years)
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13
Q

Resistance Mechanisms for Albendazole/Mebendazole

  1. changes in what b tubulin isotype?
  2. point mutation in which isotype?
    - phenylalanine –>
A

Resistance Mechanisms for Albendazole/Mebendazole

  1. b tubulin isotype changes from 1 –> 2 (2 = resis)
  2. point mutation in what b tubulin isotype 1
    - phenylalanine –> tyrosine (now sim to humans)
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14
Q

What drug activates invertebrate-specific Glutamate gated Cl channels –> flaccid muscle paralysis –> microfilariae cant move/feed
(selectivity toxicity for invertebrates)

A

Ivermectin

  • activates invertebrate-specific Glutamate gated Cl channels –> flaccid muscle paralysis –> microfilariae cant move/feed

(selectivity toxicity for invertebrates)

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15
Q

Avermectin Class: Ivermectin

  • what 2 types of parasites is it not eff vs
  • what type is it eff ev
A

Avermectin Class: Ivermectin

  • not eff vs trematodes + cestodes
  • USE = NEMATODE INFXNS
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16
Q

Ivermectin ADME

  1. CYP inhibition by cimetidine –>
  2. CYP induction by phenytoin/CCS –>
A

Ivermectin ADME

  1. CYP inhibition by cimetidine –> toxicity
  2. CYP induction by phenytoin/CCS –> decr drug efficacy
17
Q

Ivermectin Resistance

  1. what transporter when upreg –> incr rug efflux/resis
  2. mutations to what chan –> resis
A

Ivermectin Resistance

  1. upreg ATP-dep P-glycoprotein transporter –> incr rug efflux/resis
  2. mutations ligand gated Cl chan –> resis
18
Q

Pt presents w/ itching, swollen/tender LNs, HA, dizzy, somonlence, fever, tachycardia, HoTN, mylagia arthalgia, diarrhea, and facial/peripheral edema

  1. what drug causes this AE
  2. what is the name of this rxn
  3. how to Tx is (2 lst line options)
    - note: may need steroids
A

Pt presents w/ itching, swollen/tender LNs, HA, dizzy, somonlence, fever, tachycardia, HoTN, mylagia arthalgia, diarrhea, and facial/peripheral edema

  1. d/t Ivermectin
  2. Mazzoti-like rxn
  3. Tx –> ASA or anti-histamines
    - note: may need steroids
19
Q

Ivermectin CI

  1. why CI in pts w/impaired BBB (causes?)
  2. CI in pts w/ what type of infxn
A

Ivermectin CI

  1. CI in pts w/impaired BBB –> CNS depression + ataxia
  2. CI in pts w/ Loa Loa infxn (Loiasis)
20
Q

Ivermectin Uses (Nematode Infxns)

  1. what 2 types of nematode infxns does it Tx
  2. why is it now CI in Loiasis (what does it cause)
A

Ivermectin Uses (Nematode Infxns)

  1. 2 types of nematode infxns
    - Onchocerciasis (African River Blindness)
    - Lymphatic Filariasis
  2. CI in Loiasis b/c a/w life threat encephalopathy
21
Q

Ivermectin Uses

  1. what is used in combo w/ it to Tx Onchhoceriasis
  2. what is used in combo w/ it to Tx Lymphatic filariasis
  3. what can happen if Onchhoceriasis not treated
A

Ivermectin Uses

  1. T x Onchhoceriasis –> Ivermectin + CCS
    (decr inflam resp to dying microfilariae)
  2. Tx Lymphatic filariasis –> Ivermectin + Albendazole
    (Albendazole kills adults)
  3. Untreated Onchhoceriasis –> blindess
22
Q
  1. Alters worm surface mem –> enhance killing
  2. Stimulate plt aggreg
  3. +/- alter AA metab in host immune cells –> immune resp
  4. decr muscle activity in worm –> paralysis
  5. Worm organelle damage + apoptosis

proposed MOAs for what drug

A

proposed MOAs for DEC (Diethylcarbamazine)

  1. Alters worm surface mem –> enhance killing
  2. Stimulate plt aggreg
  3. +/- alter AA metab in host immune cells –> immune resp
  4. decr muscle activity in worm –> paralysis
  5. Worm organelle damage + apoptosis
23
Q

DEC: ADME

  1. what does the t 1/2 depend on
  2. how is it excreted
A

DEC: ADME

  1. t 1/2 depend on urinary pH
  2. Renal excretion
24
Q

DEC: ADME

  1. what type of pH –> drug reabs and toxicity
  2. renally excreted –> who to dose adjust in (2)
A

DEC: ADME

  1. alkalinized pH –> drug reabs and toxicity
  2. renally excreted –> dose adjust in:
    - renal dysfxn
    - pts w/ urinary alkalosis
25
DEC CIs - what type of Nematode infxn is it CI in b/c it worsens the lesions (where)
DEC CIs CI in Onchereriasis - b/c it worsens the lesions in eye
26
What drug can cause Mazzoti like rxn, leukocytosis, Proteinuria, and Eosinophilia - caused by dying microfilariae --> inflam resp What med or dose adjusting --> avoid/limit this
DEC AE Dying microfilariae --> inflam resp --> Mazzoti like rxn, leukocytosis, Proteinuria, and Eosinophilia - Tx = steroids or incr dose gradually to avoid/limit
27
DEC Uses - what 2 nematode infxns is used to tx (which infxn needs combo w/ Albendazole)
DEC Uses 1. Loiasis 2. Lymphatic Filariasis (w/albendazole)
28
What drugs is a depolarizing NM blocker --> rel of ACh at the NMJ and blocks Acetylcholinesterase --> spastic paralysis --> worm expelled from GI tract
Pyro Pamoate - depolarizing NM blocker --> rel of ACh at the NMJ and blocks Acetylcholinesterase --> spastic paralysis --> worm expelled from GI tract
29
Pyrantel Pyromate ADME 1. what type of infxns used for d/t absorption ability 2. at higher doses what occurs in the host
Pyrantel Pyromate ADME 1. only for GI lumen infxns d/t poor absorption 2. higher doses --> NM blockade in host
30
Pyrantel Pyromate Uses: | - what 3 namatodes is it eff vs
Pyrantel Pyromate: 3 nematodes eff vs 1. pinworm 2. Ascariasis 3. Trichostrongylus orientalis
31
Pyrantel Pyromate Uses - what 2 stages does it kill - what is it not eff vs in parasites
Pyrantel Pyromate Uses - kills larvae and adults - not eff vs eggs
32
What drug incr Ca influx - across tegument (outer lining of worm) - in muscle cells --> spastic paralysis
Praziquantel incr Ca influx - across tegument (outer lining of worm) - in muscle cells --> spastic paralysis
33
Praziquantel ADME 1. what does CYP inhib --> (and CYP induction) 2. is resistant a problem for this drug
Praziquantel ADME 1. CYP inhib --> incr risk toxicity CYP induction --> decr drug efficacy (same as other drugs) 2. Resistant not problem for this drug
34
Praziquantel CIs 1. what pt pop is it CI in 2. why is CI in intraocular Cysticercosis - what is the Tx
Praziquantel CIs 1. CI in pregnancy 2. CI in intraocular Cysticercosis b/c --> +/- irrev retinal damage - Tx = surgical excision of larval cysts
35
Praziquantel AEs 1. incr t 1/2 in pts w/ what type of dz/damage - therefore need to decr dose to avoid toxicity
Praziquantel AEs 1. incr t 1/2 in pts w/ liver dz/damage--> decr dose to avoid toxicity
36
Praziquantel Uses 1. what 2 infxns does it tx (how is this diff from most other drugs) --> answer before looking at #2! 2. DoC for what type of trematode infxn
Praziquantel Uses 1. Txs Trematode and Cestode infxns (diff from most other drugs) 2. DoC for Schistosomiasis (trematode infxn)
37
Review: 1. what 2 drugs cause spastic paralysis 2. what drug causes flaccid paralysis
Review: 1. 2 drugs cause spastic paralysis - Pyrantel Pamoate - Praziquantel 2. flaccid paralysis - Ivermectin
38
Anti-Hemilith Drugs and their derivatives 1. which is a Piperazine derivative 2. which is a Tetrahydropyridimine derivative 3. which is a quinolone derivative
Anti-Hemilith Drugs and their derivatives 1. DEC = Piperazine derivative 2. Pyrantel Pamoate = Tetrahydropyridimine derivative 3. Praziquantel = quinolone derivative

Spring 2018 Pharm Exam 4 (7 decks)

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