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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
Q

DEC CIs

  • what type of Nematode infxn is it CI in b/c it worsens the lesions (where)
A

DEC CIs

CI in Onchereriasis
- b/c it worsens the lesions in eye

26
Q

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

A

DEC AE

Dying microfilariae –> inflam resp –> Mazzoti like rxn, leukocytosis, Proteinuria, and Eosinophilia
- Tx = steroids or incr dose gradually to avoid/limit

27
Q

DEC Uses
- what 2 nematode infxns is used to tx
(which infxn needs combo w/ Albendazole)

A

DEC Uses

  1. Loiasis
  2. Lymphatic Filariasis (w/albendazole)
28
Q

What drugs is a depolarizing NM blocker –> rel of ACh at the NMJ and blocks Acetylcholinesterase –> spastic paralysis –> worm expelled from GI tract

A

Pyro Pamoate

  • depolarizing NM blocker –> rel of ACh at the NMJ and blocks Acetylcholinesterase –> spastic paralysis –> worm expelled from GI tract
29
Q

Pyrantel Pyromate ADME

  1. what type of infxns used for d/t absorption ability
  2. at higher doses what occurs in the host
A

Pyrantel Pyromate ADME

  1. only for GI lumen infxns d/t poor absorption
  2. higher doses –> NM blockade in host
30
Q

Pyrantel Pyromate Uses:

- what 3 namatodes is it eff vs

A

Pyrantel Pyromate: 3 nematodes eff vs

  1. pinworm
  2. Ascariasis
  3. Trichostrongylus orientalis
31
Q

Pyrantel Pyromate Uses

  • what 2 stages does it kill
  • what is it not eff vs in parasites
A

Pyrantel Pyromate Uses

  • kills larvae and adults
  • not eff vs eggs
32
Q

What drug incr Ca influx

  • across tegument (outer lining of worm)
  • in muscle cells –> spastic paralysis
A

Praziquantel

incr Ca influx

  • across tegument (outer lining of worm)
  • in muscle cells –> spastic paralysis
33
Q

Praziquantel ADME

  1. what does CYP inhib –> (and CYP induction)
  2. is resistant a problem for this drug
A

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
Q

Praziquantel CIs

  1. what pt pop is it CI in
  2. why is CI in intraocular Cysticercosis
    - what is the Tx
A

Praziquantel CIs

  1. CI in pregnancy
  2. CI in intraocular Cysticercosis b/c –> +/- irrev retinal damage
    - Tx = surgical excision of larval cysts
35
Q

Praziquantel AEs

  1. incr t 1/2 in pts w/ what type of dz/damage
    - therefore need to decr dose to avoid toxicity
A

Praziquantel AEs

  1. incr t 1/2 in pts w/ liver dz/damage–> decr dose to avoid toxicity
36
Q

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
A

Praziquantel Uses

  1. Txs Trematode and Cestode infxns
    (diff from most other drugs)
  2. DoC for Schistosomiasis (trematode infxn)
37
Q

Review:

  1. what 2 drugs cause spastic paralysis
  2. what drug causes flaccid paralysis
A

Review:

  1. 2 drugs cause spastic paralysis
    - Pyrantel Pamoate
    - Praziquantel
  2. flaccid paralysis
    - Ivermectin
38
Q

Anti-Hemilith Drugs and their derivatives

  1. which is a Piperazine derivative
  2. which is a Tetrahydropyridimine derivative
  3. which is a quinolone derivative
A

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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