Exam 2 Drugs Flashcards

1
Q

Entecavir (NRTI)

A

A nucleoside analog with selective and potent activity against Hep B, including Lamivudine-resistant HBV. Most POTENT inhibitor. Slows progression of HBV, and improves liver inflammation and fibrosis that occurs.
SE: diarrhea, headache, fatigue, vomiting, anorexia, chills, upset stomach

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2
Q

Tenofovir PMPA (NtRTI)

A

Acyclic nucleoside phosphonate Diester analog
-available as an ester prodrug
Inhibits viral reverse transcriptase and acts as a DNA chain terminator
*Inhibits both HIV and HBV Replication
-Acts against Lamivudine-resistant HBV

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3
Q

Adefovir (NtRTI)

A

A nucleoTide analog used for the tx of HBV infections.
Adefovir diphosphate replaces deoxyadenosine monophosphate in HBV DNA, resulting in DNA chain termination and thus inhibition of DNA replication.
-Slows the progression and improves liver function
-Acts against Lamivudine-resistant HBV

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4
Q

Interferon alfa-2a, Pegylated interferon alfa-2a or alfa-2b

A

Interferon alfa-2a or 2b acts similarly to endogenous IFN-a
-leads to antiviral, antiproliferative, and immunomodulatory effects
Inhibits viral replication and cleaves ssRNA
AE: flu-like sx, hepatotoxicity, increased risk of infections, and exacerbation of psychiatric conditions
PEGylation: addition of poly(ethylene glycol) increases resistance to proteolytic degradation, increases water solubility, and reduces their antigenicity

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5
Q

True Bacteria

A

Staph. Aureus

E. Coli

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6
Q

Filamentous Bacteria

A

Mycobacterium Tuberculosis

M. Leprae

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7
Q

Spirochete

A

Treponema Pallidum (Syphilis)

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8
Q

Mycoplasma

A

Mycoplasma Pneumonia

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9
Q

Rickettsia

A

Rickettsia Prowazekii (Typhus)

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10
Q

Chlamydia

A

Chlamydia trachomatis (can cause many forms of diseases: sepsis) (blindness)

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11
Q

Colonization

A

The presence of bacteria that are NOT causing disease

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12
Q

Siderophores

A

Iron Receptors (bacteria must have iron to multiply)

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13
Q

Can bacterial proliferation rates surpass the protective response?

A

Yes

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14
Q

Exotoxins

A

Enzymes released during growth causing specific responses.

Immunogenic (anti-toxin production)

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15
Q

Endotoxins

A

Lipopolysaccharides contained in the cell walls of Gram (-) organisms.
Pyrogenic Effects

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16
Q

Bacteremia or Septicemia

A

Presence of bacteria in the blood due to a failure of the body’s defense mechanisms
Usually caused by gram (-) organisms

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17
Q

Bacterial Sepsis

A

Associated w/ ARDS, DIC, Hemodynamics effects, and renal failure

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18
Q

Gram (+) Bacterial Sepsis

A

Staphylococcus Aureus
Streptococcus Pneumoniae
S. Aureus is associated w/ an overall mortality rate ranging b/ 10-30%

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19
Q

Gram (-) Bacterial Sepsis

A

E. Coli
Klebsiella species
Pseudomonas Aeruginosa
-Proeus species, P. Aeruginosa and Acinetobacter species are associated w/ prior antibiotic exposure

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20
Q

Respiratory Infections: Pneumonia

-Community Acquired

A
Pneumococcal pneumonia (streptococcus pneumonia)
Mycoplasma pneumonia in the young
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21
Q

Respiratory Infections: Pneumonia

-Nosocomial Infections (ICU, Ventilators)

A

Staph. Aureus, Klebsiella pneumonia, P. Aeruginosa

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22
Q

Respiratory Infections: Pneumonia

-Immunocompromised patients

A

P. Jiroveci

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23
Q

Respiratory Infections: Pneumonia

-Portal Of Entry

A

Aspiration of oropharyngeal secretions
Inhalation of aerosols
From blood bacteremia

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24
Q

Hepatitis

A

Inflammation of the liver

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25
Acute Viral Hepatitis
Inflammation of the liver that begins suddenly and lasts a few weeks
26
Chronic Viral Hepatitis
Inflammation of the liver that lasts at least 6 months
27
Cirrhosis
Irreversible inflammatory disease of the liver, a leading cause of death
28
Acute Infection Sequence of Viral Hepatitis
Incubation Period Prodromal (pre-icteric) Phase: wt loss, fatigue, anorexia, vomiting, and low grade fever Icteric (Jaundice) Phase: Lasts 2-6 weeks -hepatomegaly, dark urine, clay colored stools, itching, jaundice as bilirubin builds up in the blood Recovery Phase: resolution of jaundice
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Fulminant HBV
Results from impairment or necrosis of hepatocytes
30
Hepatitis B Virus
``` DNA Hepadnaviridae HBsAG - Diagnosis Severe and Chronic Transmission: sexual, Injection-drug use, Perinatal Incubation: 60-180d PX: Hygiene, Vaccine Chronicity: YES Liver Cancer: YES ```
31
Hepatitis C Virus
RNA Flaviviridae Family Anti-HCV= diagnosis Mild to severe Transmission = injection-drug use, Sexual Incubation: 35-60 days Hygiene, Blood screen, IFN-a : prophylaxis Chronicity: YES Liver Cancer: YES
32
HEP B VIRUS
dsDNA Chronic HBV carriers- worldwide reservoir of infection Cirrhosis and Hepatocellular Carcinoma = Complications Vaccine is based on Australian Antigen HBV can cause fulminant hepatitis, and irreversible tissue necrosis which requires a liver transplant Has infected 1/3 of population 360 million chronic carriers
33
HEP C VIRUS
ssRNA | Complications = Chronic infection, Cirrhosis, and Carcinoma
34
Hep B/C Complications
Cirrhosis: scarring of the liver marked increase in fibrous connective tissue, resulting in a firm, modular, distorted liver Decompensated Cirrhosis: increase in portal HTN, Ascites (fluid accumulation in peritoneum), splenomegaly, encephalopathy, Jaundice
35
Respiratory Infections: TB or Mycobacterium Avium Complex (MAC)
TB has the highest death toll of any infectious pathogen POE: airborne transmission TB Detection: Tubercle formation, Caseous necrosis, (+) skin test
36
Respiratory Infections: Acute Bronchitis
Acute infection or inflammation of the airways or bronchi Commonly viral pathogen (can become bacterial) Causes similar sx to pneumonia but does NOT demonstrate pulmonary consolidation and chest infiltrates
37
Respiratory Infections: Acute Epiglottitis
More common in Children Severe, rapidly progressive, life-threatening infection of the epiglottis and surrounding area -usually caused by Haemophilus influenzae type B Manifestations: high fever, sore throat, inspiratory stridor, and severe respiratory distress Tx: Emergency airway and antibiotics
38
UTI
Inflammation of the urinary epithelium following invasion and colonization by some pathogen within the urinary tract - complicated - uncomplicated - persistent
39
UTI Pathogens
E. Coli Staphylococcus Saprophyticus Enterobacter spp
40
Cystitis
Inflammation of the bladder Manifestations: frequency, dysuria, urgency, and lower abdominal and/or Supra pubic pain TX: antimicrobial therapy, increased fluid intake, avoidance of bladder irritants, and urinary analgesics
41
GI Infection: Shigellosis
Seen with dysentery -Causes shigellosis: binds epithelium of GI tract and causes it to die off. Can cause a severe form of diarrhea. (Fecal-oral transmission)
42
GI Infection: Campylobacter Enteritis
By C. Jejuni (Fungus) -Vibrio cholera: will lose close to 1L/ hour of fluid E. Coli (O107): makes an exotoxin
43
Bacterial STD: Campylobacter Jejuni
Disease: Campulobacter enteritis
44
Bacterial STD: Chlamydia trachomatis
Disease: Urogenital infections
45
Bacterial STD: Neiserria Gonorrhoeae
Disease: Gonorrhea
46
Bacterial STD: Shigella
Disease: Shigellosis
47
Bacterial STD: Treponema pallidum
Disease: Syphilis
48
Gonorrhea
Caused by microorganisms of the species Neisseria Gonorrheae (aerobic, non-spore-forming, gram -, diplococcus (round)) -presence of pili helps the microorganisms attach themselves to the epithelial cells of mucous membrane Infections can result in: disseminated gonococcal infection (CGI) and Perihepatits, as well as ophthalmia neonatorum. Transmission: requires contact of epithelial surfaces, Gonorrhea also crosses amniotic membranes. Humans are the only natural hosts
49
Syphilis: appearance of a chancre (boil)
Can spread through the blood as well as the lymph: Secondary Cardiovascular syphilis, Neurosyphilis: Tertiary -Latent syphilis: asymptomatic but potential recurrent infections -Congenital (from mother to fetus)
50
Chlamydial Infections
Trachoma-a leading cause of preventable infectious blindness Nongonococcal or nonspecific urethritis: nonreportable STI, Syndrome caused by most commonly by Chlamydia Trachomatis -Trichomonas vaginalis, herpes simplex virus, ureaplasma urealyticum and mycoplasma
51
Staphylococcus Aureus Infections
Commensal bacteria and opportunistic pathogen Superantigens: enterotoxin and toxic shock syndrome Toxin 1, causes immune overactivation --> toxic shock and food poisoning Children: impetigo and Staph. Scalded-skin syndrome Hospital: MRSA is common Most common cause of food borne outbreaks Can cause SOFT PAINS: Skin infections, Osteomyelitis, Food poisoning, Toxic shock syndrome, Pneumonia, Acute endocarditis, Infective arthritis, Necrotizing fasciitis, and Sepsis
52
B-Lactams
Penicillins and B-Lactamase Inhibitors Cephalosporins & Cephamycins Carbapenems Monobactams ** ALL are active against non-B-Lactamase-producing gram - and gram + bacteria ALL work in the same way/ Time-dependent killing ALL can cause hypersensitivity reactions or seizures at very high doses NONE are active against MRSA
53
B-Lactams: Penicillins
``` Natural Penicillins (Penicillin G): Short t1/2, tx neurosyphilis Antistaphylococcal Penicillin (Nafcillin): resistant to staphylococcal B-lactamases, Hepatic CL, Tx MSSA Extended-Spectrum Penicillins (Ampicillin): aminopenicillins better than others against gram (-), Antipseudomonal Penicillins ```
54
Clavulanic Acid, Sulbactam, & Tazobactam
Inhibit bacterial B-Lactamases Protect hydrolyzible penicillins from inactivation Extends the spectrum of the penicillin to strains that would otherwise inactivate it Predicted on the assumption that the inhibitor is active against the B-lactamase that is produced
55
Cephalosporin and Cephamycins
More resistant to bacterial B-lactamases than penicillins First generation: do NOT cross BBB, used in hospitals, good antistaph Second Generation: Do NOT cross BBB, have extended gram (-) coverage compared to 1st generation, good for anaerobes in upper respiratory infections, community pneumonia, and gonorrhea Third and Fourth Generations: some cross BBB, expanded gram (-) coverage compared to both 1st and 2nd generations, good for P. Aeruginosa, Enterobacteriacaea, S. aureus, and S. pneumonia AE: allergy, Methylthiotetrazole containing Cephamycins can cause bleeding and disulfiram-like reactions
56
Carbapenems: Doripenem, Ertapenem, Imipenem, & Meropenem
Broadest Spectrum ABX NOT active against Klebsiella Pneumonia Carbapenemase-producing strains -Imipenem administered w/ an inhibitor of renal dehydropeptidase, Cilastatin (never administered alone) Good for nosocomial infections and B-lactamase producing GN strains
57
B-Lactam Monobactam: Aztreonam
Limited to aerobic gram (-) rods (including P. Aeruginosa) | No activity against gram + bacteria or anaerobes
58
Glycopeptide: Vancomycin
Active ONLY against gram + bacteria Water soluble and stable. Bind to d-Ala-d-Ala chains on the peptidoglycan wall preventing elongation **Drug of choice for MRSA Can cause red man syndrome due to infusion site rxns (Itching)
59
Cyclic Lipopeptide: Daptomycin
Binds to the cell wall synthesis by inhibiting the synthesis of the cell wall building blocks **punches holes in the cell wall Effective against MRSA and VRE Can cause allergic pneumonitis
60
Fosfomycin
Inhibits bacterial wall synthesis by inhibiting the synthesis of the cell wall building blocks Primarily used for uncomplicated UTI Same applications as Nitrofurantoin
61
Tetracyclines: Tetracycline, Doxycycline, Tigecycline
Good for Rickettsia, Mycoplasma, Chlamydia, some spirochetes, & Plasmodium Resistance: impaired influx or increased effluent, Prod of proteins that interfere w/ tetracycline, Enzymatic inactivation
62
Macrolides: Clarithromycins, Azithromycin, Erthyromycin
Used in outpatient settings for respiratory infections, Mycobacterium Avium, Chlamydia Needs to be checked for interactions via P450 **resistance: Impaired influx or increased efflux, Prod of esterases that hydrolyze macrolides, lincosamides, and stretogramin, Modification of the ribosomal binding site by mutation or by macrolide-inducible or constitutive methylase
63
Lincosamides: Clindamycin
Derivative of lincomycin Good for skin and soft-tissue infections caused by streptococci and staphylococci Resistance: same as macrolides
64
Stretogramins: Quinupristin-Dalfopristin 30:70 ratio
Rapidly bactericidal for most susceptible organisms: MSSA, MRSA, and VRE NOT active against: Enterococcus Faecalis, or Faecium Resistance: same as macrolides
65
Oxazolidinones: Linezolid
Inhibits protein synthesis by preventing formation of the ribosome complex Good for susceptible organisms MSSA, MRSA, VRE, & Enterococcus faecium AE: myelosuppression or thrombocytopenia Resistance: Different from the other classes
66
Aminoglycosides
Irreversible inhibitors of protein synthesis - blocks the initiation complex - miscoding of amino acids - block of translocation on mRNA
67
Amikacin, Gentamicin, Tobramycin, Streptomycin
Concentration-dependent killing Synergistic killing w/ cell wall inhibitors in endocarditis Good for: gram (-) pathogens, Mycobacteria AE: nephro and Ototoxicity Resistance: production of an enzyme which inactivates the aminoglycoside
68
Inhibitors of Folate Synthesis: Trimethoprim/ Sulfonamide
Sulfonamides block dihydropteroate synthase Trimethoprim (pyrimidine) blocks dihydrofolate reductase Used as a combo (TMP/SMX): drug of choice for infections such as Pneumocystis Jiroveci, Toxoplasmosis Good for uncontrolled UTI AE: hematopoietic disturbances, interacts w/ Warfarin
69
Inhibitors of DNA synthesis: Fluoroquinolones- Ciprofloxacin, Levofloxacin, Moxifloxacin, and Gemifloxacin
Synthetic fluoridated analogs of nalidixic acid Blocks bacterial DNA synthesis by inhibiting bacterial topoisomerase II (DNA gyrase) and topoisomerase IV Broad activity for: UTI, Upper and Lower RTI (levo), bacterial Diarrhea (foodbourne illnesses) AE: prolonged QTc, Neuropathy, Cartilage degradation, Achilles' tendon rupture, should be avoided during pregnancy Resistance: altered targets, active efflux, bacterial proteins which protect DNA gyrase or which inactivated quinolones
70
Antimycobacterial Drugs: Isoniazid
Inhibits the synthesis of mycolic acids (precursors of mycobacterium cell wall)
71
Antimycobacterial Drugs: Rifampin
A derivative of Rifamycin inhibits the mycobacterial RNA polymerase
72
Antimycobacterial Drugs:
Also includes Fluoroquinolones, Macrolides, and Streptomycin AE: isoniazid-induced hepatitis and peripheral neuropathy -rifampin colors secretions orange-red (harmless) Resistance: drug unable to penetrate cell wall, Low pH renders drug inactive, drug exported from cell before it reaches target, mutations in DNA repair genes lead to multiple drug resistance, alteration of target protein structure prevents drug recognition
73
Fungal Infections
Eukaryotic Cells with rigid walls Can grow as: molds, yeasts, or both (dimorphic) Resistance to bacterial wall inhibitors Pathogenicity: adapts to host environment, Suppresses the immune defenses
74
Mycoses
Diseases caused by fungi
75
Dermatophytes
Diseases they produce are called tine as (ringworm) | -tinea capitis, tinea pedis, and tinea cururis (groin infection)
76
Candida Associated Disease
Most common fungal pathogen Common in nosocomial infections Commensal in skin, GI, vagina Opportunistic Pathogen due to changes in environment -ABX is can cause oropharyngeal (thrush) and vulvovaginal infections (vaginitis) -immunocompromised pts (HIV, hematologic cancers) present w/ disseminated infections -medical devices can lead to invasive candidiasis Candidemia a major cause of fungal sepsis and septic shock (hypotension, tachycardia, DIC)
77
Antifungal Drugs: Polyene Antifungal: Amphotericin B
Binds to ergosterol in the fungal cell membrane forming pores Broad spectrum with good activity against candida, Cryptococcus AE: infusion-related rxns, Nephrotoxicity Very poorly absorbed orally
78
Nucleoside Analog (Antifungal): Flucytosine (5-FC)
Blocks DNA and RNA polymerization (blocks further replication of DNA) Converted intracellularly first to 5-FU and then to 5-Fluorodeoxyuridine monophophate and fluorouridine triphosphate, which inhibits DNA and RNA synthesis Cryptococcus associated meningitis AE: bone marrow toxicity w/ anemia, leukopenia, and thrombocytopenia, as well as lactic acidosis
79
Imidazole: Ketoconazole Triazoles: Fluconazole, Itraconazole, Voriconazole, Posaconazole
Azoles block ergosterol synthesis from lanosterol Broad spectrum w/ good activity against Candida, C. Neoformans, Endemic mycoses The pharmacology of each of the azoles is unique, some are used topically
80
Echinocandins: Caspofungin, Micafungin, Andulafungin
Inhibits fungal wall synthesis, good for invasive candidiasis
81
Griseofulvin
Oral fungistatic used for dermatophytosis (invasive-penetrates deeper into the skin)
82
Terbinafine
Oral and topical fungicidal that blocks ergosterol synthesis at an earlier step than azoles. (Blocks squalene synthesis)
83
Nystatin
Polyene macrolide much like amphotericin B | It's too toxic for parenteral administration and is only used topically
84
Protozoan Infections
Cryptosporidium --> Crytosporidiosis Giardia Lamblia --> diarrheal syndrome (fecal contam water) Entamoeba Histolytica --> Amebiasis (fecal contam water) Plasmodium --> Malaria (mosquito anopheles)- vector borne Leishmania --> Leishmaniasis (sand flies) Toxoplasma --> Toxoplasmosis
85
Malaria
Protist, can produce asexually or sexually Plasmodium species - through blood can infect liver) Fever and anemai, splenomegaly RBC get destroyed evolution of Sickle cell trait -when have the HbAA/HbAS forms, they are more resistant to Malaria
86
GI Infections: Giardiasis (protozoan)
Most common causes of waterborne illnesses | Caused by Giardia Lamblia
87
Amebiasis (GI infections-Protozoan)
GI bleeding and hemorrhage, can also cause liver disease and fatality) - caused by Entamoeba Histolytica - most imp parasitic disease - Dysentery as a result of toxin on colonic epithelium - can also cause amebic liver disease
88
Sexually Transmitted Parasitic Infections: Trichomoniasis
Caused by Trichomonas vaginalis -anaerobic, unicellular, flagellated, parasitic protozoan Adheres to and damages squamous epithelial cells -urethra, vagina, and Skene and Bartholin glands Accounts for 25% of infectious vaginitis cases Often coexists w/ gonorrhea Presence confirmed by microscopic examination of vaginal secretions or urine
89
Antifungal Drugs: antimalarial drugs
Quinolones, Atovaquone, Artemisinins, Doxycyline | -employed prophylactically and as definite therapy
90
Quinolines: Chloroquine, Mefloquine, Quinine, Primaqine
Oldest and highly effective antimalarial blood schizonticide (quinine from the bark of the cinchona tree) Primaquine also has gametocide activity for all Plasmodium species and is also used to tx P. Jiroveci MOA: not clear how they work but they might affect the ability of the parasites to catabolize hemoglobin AE: hematologic abnormalities, hemolysis, prolonged QTc, hypotension -quinine can cause cinchonism: tinnitus, headache, nausea, dizziness, flushing, and visual disturbances
91
Artemisinin: Artesunate
A sesquiterpene lactose endoperoxide
92
Atovaquone
Used in combo w/ proguanil as quinone-folate antagonist combination for malaria -also used for mild to moderate P. Jiroveci pneumonia
93
Amebicides: Metronidazole, Tinidazole
Amebiasis is infection w/ Entamoeba histolytica Kill trophozoites but not cysts by causing DNA damage Good for anaerobes including Clostridium For protests: Amebiasis, Giardiasis, and Trichomoniasis AE: nausea, dry mouth, metallic taste Metronidazole: is amebicidal, Bacteriacidal, and Trichomonicidal
94
Pentamidine
Used in African Trypanosomiasis-sleeping sickness and Leishmaniasis Also used for pneumocystosis caused by Pneumoscystis Jiroveci -Highly toxic
95
Parasitic Infections: Nematodes (roundworms)
Hookworm disease (ancylostoma duodenale or necator americanus) - -> ascariasis - -> enterobiasis - -> filariasis
96
Parasitic Infections: Flatworms (platyhelminths)
- -> Neuro Cysticercosis (Tania solium) | - -> Schistosomiasis (schistosoma-blood flukes)
97
Parasitic Infections: Lice
- -> Pediculus humans capitis (head louse) - -> Pediculus humanus corporis (body louse) - -> pthirus pubis ("crabs" louse, pubic louse)
98
Parasitic Infections: Scabies
--> Sarcoptes Scabiei
99
Helminth Infections
Parasitic worms infect more than 3 billion people worldwide
100
Skin infections: Scabies
Caused by the adult female itch mite, Sarcoptes Scabiei Transmission: requires prolonged close skin-to-skin contact -typically occurs b/ family members or sexual partners Burrows through the horny layer of the stratum/day -new larval forms appear in about 10 days Classic sx is intense pruritus
101
Antihelminthic Drugs: Albendazole
Inhibits the polymerization of microtubules Used in: Intestinal Parasites- cysticercosis (T. Solium), ascariasis, enterobiasis (pinworms), Hydatid disease (echinococcus via dogs), Neurocysticercosis
102
Antihelminth Drugs: Ivermectin
Caused paralysis by intensifying (GABA)-mediated transmission of signals in peripheral nerves Used in: Onchocerciasis: River blindness (onchocerca volvulus) affects 17-25 million people -microfilaria -and ectoparasties such as scabies