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Pharmacology > Pharm 4 (antibiotics/fungal/viral/parasite, immunosuppressants) > Flashcards

Pharm 4 (antibiotics/fungal/viral/parasite, immunosuppressants) Flashcards

1
Q

Methicillin
Nafcillin
Oxacillin
Dicloxacillin

A

Bind PBP and block transpeptidase cross-linking of peptidoglygan; activate autolytic enzymes

Staphylococcus (use naf for staph) (except MRSA)

Hypersensitivity Rxns; Interstitial nephritis

penicillinase resistant because bulky R group blocks access to β-lactam ring

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2
Q 
Penicillin G (IV, IM)
Penicillin V (oral)
A

Bind PBP & block transpeptidase cross-linking of peptidoglycan; activate autolytic enzymes

Mostly Gram + (S. pneumonia, S. pyogenes, Actinomyces)
Also N. meningitidis & T. pallidum; Bactericidal for Gram + cocci & rods, Gram - cocci & spirochetes

Hypersensitivity Rxns; hemolytic anemia

Penicillinase in bacteria (β-lactamase) cleave βlactam ring

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3
Q

Ampicillin

Amoxicillin

A

Bind PBP & block transpeptidase cross-linking of peptidoglycan; activate autolytic enzymes

Extended-spectrum: H. influenza, E. coli, L. monoctyogenes, P. mirabilis, Salmonella, Shigella, enterococci - (HELPSS kill enterococci)

Hypersensitivity Rxns; rash; pseudomembranous colitis

β-lactamase sensitive - often combine w/ clavulanic acid

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4
Q

Azlocillin
Piperacillin
Ticarcillin

A

Bind PBP & block transpeptidase cross-linking of peptidoglycan; activate autolytic enzymes

antipseudomonals - Pseudomonas spp., Gram - rods

Hypersensitivity Rxns

Sensitive to penicillinase; use w/ β-lactamase inhibitors

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5
Q

β-lactamase inhibitors

A

CAST

Clavulanic Acid, Sulbactam, Tazobactam

often added to penicillins to protect from destruction by β-lactamase (penicillinase)

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6
Q

Cephalosporins

A

β-lactam drugs that inhibit cell wall synthesis but are less susceptible to penicillinase - Bactericidal

Organisms typically not covered by cephalosporins are LAME (Listeria, Atypicals (chlamydia, mycoplasma), MRSA, Enterococci)
Exception - 5th gen (ceftaroline) covers MRSA

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7
Q

Cefazolin

Cephalexin

A

1st Gen - bind to and inhibit PBP

Gram + cocci (PEcK) - P. mirabilis, E. coli, K. pneumonia
Cefazolin used pre-surgery to prevent S. aureus wound infections

Hypersensitivity Rxns, Vit K deficiency, disulfiram effect
Increase the nephrotoxicity of aminoglycosides
Low cross-reactivity w/ penicillins

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8
Q

Cefoxitin
Cefaclor
Cefuroxime
(Cefotetan)

A

2nd Gen - bind to and inhibit PBP

Gram + cocci (HEN PEcKS) - H. influenzae, E. aerogenes, Neisseria spp, P. mirablis, E. coli, K. pneumoniae, Serratia marcescens

Hypersensitivity Rxns, Vit K deficiency, disulfiram effect
Increase nephrotoxicity of aminoglycosides
Low cross-reactivity w/ penicillins

Cefuroxime enters the CNS

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9
Q

Ceftriaxone
Cefotaxime
Ceftazidime
(Cefdinir, Cefixime)

A

3rd Gen - bind to and inhibit PBP

Serious Gram - infections resistant to other β-lactams
Ceftriaxone - meningitis & gonorrhea
Ceftazidime - Pseudomonas

Hypersensitivity Rxns, Vit K deficiency, disulfiram effect
Increase nephrotoxicity of aminoglycosides
Low cross-reactivity w/ penicillins

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10
Q

Cefepime

A

4th Gen - bind to and inhibit PBP

increased activity against Pseudomonas & Gram +

β-lactamase Resistant

Hypersensitivity Rxns, Vit K deficiency, Disulfiram effect
Increase nephrotoxicity of aminoglycosides
Low cross-reactivity w/ penicillins

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11
Q

Ceftaroline

A

5th Gen - bind to and inhibit PBP

Broad Gram + & - coverage including MRSA
Does NOT cover Pseudomonas spp

hypersensitivity Rxns, Vit K deficiency, Disulfiram effect
Increase nephrotoxicity of aminoglycosides
Low cross-reactivity w/ penicillins

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12
Q

Aztreonam

A

Monobactam - binds and inhibits PBP3

Gram - rods only (for penicillin-allergic Pt & those w/ renal insufficiency who can’t tolerate aminoglycosides)

β-lactamse resistant

Usually nontoxic - occasional GI upset
Synergistic w/ aminoglycosides
No cross-allergenicity w/ penicillins

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13
Q

Imipenem
Doripenem
Ertapenem
Meropenem

A

Carbapenems - Bind and inhibit PBP

Gram + cocci, Gram - rods, Anaerobes
Imipenem & Meropenem used in ESBLs

GI distress, skin rash, CNS toxicity (seizures) at high [] (merpenem has reduced risk of seizures)

β-lactamase resistant (carbamenemase sensitive), but limited to life-threatening infections or after other drugs have failed due to significant AE
Imipenem admin w/ cilastatin (inhibits renal dehydropeptidase I) to decrease inactivation

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14
Q

Cilistatin

A

Inhibits renal dehydropeptidase I

Administered w/ imipenem to decrease its inactivation in the renal tubules

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15
Q

Vancomycin

A

Inhibits cell wall peptidoglycan formation by binding D-ala D-ala portion of cell wall precursors - Bactericidal

Gram + only - serious, MDR organisms including MRSA, enterococci & C dif (oral dose for pseudomembranous colitis)

Well tolerated but NOT trouble free (Nephrotoxicity, Ototoxicity, Thrombophlebitis) diffuse flushing (red man syndrome <- prevent by preTx w/ antihistamine & slow infusion rate)

Resistance through AA modification to D-ala D-lac

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16
Q

(Bacitracin)

A

Blocks incorporation of AA & nucleic acids into cell wall

Broad spectrum Gram + & - bacteria
Group A strep are sensitive, GBS resistant

Restricted to topical & ophthalmic ointments

AE - rare (hypersensitivity)

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17
Q

(Fosfomycin)

A

Prevents UDP-N-acetylmuramic acid synthesis - an early step in cell wall synthesis

Broad spectrum including Gram + & -
Commonly used in uncomplicated UTIs in females

AE - rare (hypersensitivity)

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18
Q

(Daptomycin)

A

Lipopeptide - binds membrane & causes depol = bactericidal (insertion into membrane is Ca dependent)

Gram + including MRSA, MDR enterococcus

Resistance by mprF gene mutation increases net + charge of membrane = repels cationic antibiotics

AE - musculoskeletal (myopathy, rhabdomyolysis)

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19
Q

(Polymyxin B)

A

Detergent - binds phospholipids (LPS) in cell membrane & disrupts structure (punch holes) = solubilizes membrane

Primarily Gram - including MDR
topically used for skin infections (in combo w/ bacitracin)

AE - rare

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20
Q

Protein Synthesis Inhibitors

A

Specifically target bacterial 70S ribosome

Buy AT 30, CCEL at 50
30S - Aminoglycosides (cidal), Tetracyclines (static)
50S - Chloramphenicol, Clindamycin, Erythromycin (macrolides) (static) Linexolid (variable)

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21
Q 
Streptomycin
Gentamycin
Neomycin
Tobramycin
Amikacin
(Kanamycin)
A

Aminoglycosides - Bind 30S inhibit formation of initiation complex & cause misreading of mRNA. Also block translocation - Bactericidal

Severe Gram - rod infections; ineffective against anaerobes
Neomycin for bowel surgery
Synergistic w/ β-lactams

Nephrotoxicity (esp w/ cephalosporins), Ototoxicity (esp w/ loop diuretics), Teratogen, Neuromuscular blockade

Bacterial transferase enzymes inactivate via acetylation, phosphorylation, or adenylation

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22
Q

Tetracycline
Doxycycline
Minocycline
(Tigecycline)

A

Tetracyclines - bind 30S & prevent attachment of tRNA
Bacteriostatic

Borrelia burgdorferi, M. pneumonia, Rickettsia & Chlamydia (from drug’s ability to accumulate intracellularly), also used to tx acne
Doxycycline is fecally eliminated = use in renal failure Pt

GI distress, discoloration of teeth & inhibition of bone growth in children, photosensitivity, CI in pregnancy

Do NOT take w/ milk (Ca), antacids (Ca, Mg) or iron-containing preps because divalent cations inhibit absorption in the gut

Resistance from ↑ efflux out of bacterial cells by plasmid-encoded transport pumps (or decreased uptake)

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23
Q

Erythromycin
Clarithromycin
Azithromycin

A

Macrolides - bind 50S (23S rRNA) and inhibit protein synthesis by blocking translocation - Bacteriostatic

Atypical pneumonia (Mycoplasma, Chlamydia, Legionella) STDs (Chlamydia) & Gram + cocci (strep in penicillin allergy)

MACRO - gi Motility, Arrhythmia (prolonged qt), acute Cholestatic hepatitis, Rash, eOsinophilia
↑ serum [ ] of theophyllines & oral anticoagulants (- P450)

Resistance - methylation of 23S rRNA-binding site

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24
Q

Chloramphenicol

A

Bind 50S and prevents peptidyltransferase-Bacteriostatic

2nd line due to toxicities (often used in developing countries because of low cost) - Rocky Mountain Spotted Fever (R. rickettsii), Meningitis (H. influenzae, N. meningitidis, S. pneumoniae)

Anemia, aplastic anemia, Gray Baby Syndrome ( in premature infants because they lack liver UDP-glucouronyl transferase)

Plasmid-encoded acetyltransferase inactivates

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25
Q

Clindamycin

A

Bind 50S & block peptide transfer - bacteriostatic

Anaerobes - in aspiration pneumonia, lung abscesses, & oral infections (above the diaphragm), Also Group A strep (GAS) infections

Pseudomembranous colitis (C. dif), Fever, Diarrhea

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26
Q

(Linezolid)

A

Binds 50S & inhibits formation of ribosomal-fMet-tRNA

Most Gram +
Because of its unique mechanism, it is effective against many penicillin/methicillin/vanco resistant strains including MRSA and MDR enterococci

AE - myelosuppression,

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27
Q

Sulfamethoxazole (SMX)
Sulfisoxazole
Sulfadiazine

A

PABA antimetabolites that inhibit dihydropteroate synthase = inhibits folate synthesis - Bacteriostatic

Gram + & -, Nocardia, Chlamydia
Triple sulfas or SMX for simple UTI

Hypersensitivity, nephrotoxicity, photosensitivity, displace other drugs from albumin (eg warfarin), kernicterus in infancts, hemolysis in G6PD deficiency

resistance through alterations to target enzyme, ↑ PABA, or altered uptake

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28
Q

Trimethoprim (TMP)

Pyrimethamine

A

Inhibits bacterial DHFR = inhibites folate synthesis (used in combo w/ sulfas (TMP-SMX) causing sequential block of folate synthesis) - Bacteriostatic

Gram -; TMP-SMX used for UTIs, Shigella, Salmonella, P. jirovecii penumonia (Tx & prophylaxis),
Pyrimethamine-Sulfadiazine - Toxoplama gondii (Tx and prophylaxis)

Megaloblastic anemia, leukopenia, granulocytopenia (may alleviate w/ folinic acid supplementation)
TMP - Treats Marrow Poorly

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29
Q

Fluoroquinolones

  • sparfloxacin
  • nalidixic acid (a quinalone)
A

Inhibit topoisomerase II (DNA gyrase) & IV - bacteriocidal

Must not be taken w/ antacids!!!

GI upset, superinfections, skin rash, headache, dizziness
Tendonitis, TENDON RUPTURE, myalgia (less commonly)
CI - pregnant, nursing, children <18 (cartilage damage)
some may cause prolonged QT

Resistance - efflux pumps, DNA gyrase mutation (chromosome) and plasmid-mediated resistance

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30
Q

Norfloxacin

A

Group 1 Fluoroquinolone - Inhibit topoisomerase II, IV

Least active - has Gram + & - effects

GI, Cardio (prolonged QT), tendon rupture
bind divalent cations which prevents absorption

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31
Q

Ciprofloxacin
Levofloxacin
Ofloxacin

A

Group 2 Fluoroquinolone - Inhibit topoisomerase II, IV

Gram - (some G+)
Ciprofloxacin - fever w/ neutropenia, UTIs, Prostatitis

GI, Cardio (prolong QT), tendon rupture
bind divalent cations which prevents absorption

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32
Q

Moxifloxacin
Gemifloxacin
(Getifloxacin)

A

Group 3 Fluoroquinolone - Inhibit topoisomerase II, IV

Gram + (some G-)

GI, Cardio (prolong QT), tendon rupture
bind divalent cations which prevents absorption

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33
Q

Metronidazole

A

Forms free radical toxic metabolites in the bacterial cell that damage DNA - Bactericidal, antiprotozoal (PFOR)

Giardia, Entamoeba, Trichomonas, Gardnerella vaginalis, Anaerobes (bacteroides, c.dif), h. Pylori (triple tx w/ PPI & clarithromycin) = GET GAP on the METRO
(Anaerobics below the diaphragm)

GI, headache, metallic taste, disulfiram effect

resistance in bacteria through mutation in rdxA gene (decreases bacterial reduction of prodrug)

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34
Q

Isoniazid (INH)

A

Prodrug converted to active metabolite by bacterial catalase-peroxidase (KatG), active form inhibits synthesis of mycolic acid (bonds proteins required for synthesis)
-bactericidal for actively growing bacilli, penetrates macrophages

M. tuberculosis - Tx & solo prophyaxis

Neurotoxicity, hepatotoxicity (in slow acetylators)
(Pyroxidine (Vit B6) can prevent neurotoxicity, lupus)

INH - Injures Neurons & Hepatocytes

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35
Q

Rifampin

Rifabutin

A

Inhibit DNA-dependent RNA polymerase

In combo for TB and leprosy
meningococcal prophylaxis & chemoprophylaxis in contacts of children w/ H. influenza type B

AE - Minor hepatotoxicity & drug interactions (↑ P450), orange/red body fluids (nonhazardous)

Rifabutin favored in Pt w/ HIV due to less P450 stimulation

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36
Q

Ethambutol

A

inhibits arabinosyltransferase = ↓ carb polymerization of mycobacterial cell wall

Tx - 4 drug TB therapy & in combo against MAC

AE - optic neuropathy (reversible red-green color blindness)

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37
Q

Pyrazinamide

A

Thought to acidify intracellular environment via conversion to pyrazinoic acid. Effective in acidic pH of phagolysosomes

Tx - multidrug Tx of TB

hyperuricemia, hepatoxicity

38
Q

Dapsone

A

Structural analog of PABA = competitive inhibitor or folic acid syntesis

Multidrug Tx of TB (lepromatous & tuberculoid

AE - Acute hemolytic anemia in G6PD deficiency
- can induce non-hemolytic anemia in some Pt

39
Q

Clofazimine

A

Bacterial dye w/ uncertain MoA

Multidrug Tx of lepromatous TB

AE - red-brown to black skin discoloration

40
Q

Iodoquinol

A 
Halogenated hydroxyquinoline (MoA unclear)
-effective at eliminating trophozoites & cysts forms of E. histolytica from lumen of intestine

Tx - asymptomatic amebiasis & following metronidazole in severe (invasive) cases

AE - GI discomfort (take w/ meals to decrease)
**permanent vision loss from optic atrophy from high dose prolonged use in children

41
Q

Paromomycin

A

Aminoglycoside = bind 30S & inhibit protein synthesis (MoA on E. histolytica unknown)
-Effective at eliminating both trophozoite & cyst forms of E. histolytica in lumen (no tissue activity)

Tx - asymptomatic cases of amebiasis & following metronidazole in invasive cases

AE - less toxic than Iodoquinol

42
Q

Nitozaxanide

A

Interferes w/ PFOR = disruption of anaerobic energy metabolism

Oral suspension approved for Tx of Cryptosporidiosis (in immunocompromised/ AIDS Pt) & Giardiasis in Pt > 1yo

43
Q

Chloroquine

A

Blocks detox of heme into hemozoin = heme accumulates & is toxic to plamodia

Tx = asexual erythrocytic stages plasmodial species (except P. falciparum due to high resistance)

Resistance = rapid export

AE - Retinopathy; pruritus (especially in dark-skinned Pt)

44
Q

Quinidine

A

Interferes w/ hemoglobin degredation & detox of metabolites

Eliminates asexual erythrocytic stages of all species of Plasmodium
Use in life-threatening malaria in U.S.

AE - Cinchonism & hypoglycemia (may be problematic in Pt already hypoglycemic due to severe malaria)
-poorest therapeutic toxic ratio of antimalarials

45
Q

Mefloquine

A

MoA unclear, may inhibit detox of heme metabolites

Effective against asexual erythrocytic stages of all Plasmodium species

AE - *Severe neuropsychiatric reactions (0.5%) (people have murdered spouses on this drug)

46
Q

Primaquine

A

interferes w/ mitochondrial e- transport as well as pyrimadine synthesis (need activation by host)

ONLY available agent against hypnozoite form of P. vivax/ovale = DoC for dormant liver forms, and following chloroquine tx of acute ovale/vivax infection

AE - hemolytic anemia in G6PD deficiency

47
Q

Malarone

A

atovaquone/proguanil

Tx & prophylaxis of P. falciparum (highly efficacious)

48
Q

Doxycycline (tetracyclines)

A

Inhibit plasmodium growth by disrupting protein synthesis

Tx & prophylaxis (in combo) w/ all plasmodium species

CI in children & pregnancy
AE - photosensitivity dermatitis, staining of teeth & inhibition of bone growth in children

49
Q

Artemisinin Derivatives

A

From “chinese wormwood” (MoA unknown)

Active against all human malaria parasites, including MDR strains of P. falciparum
artemether/lumefantrine combo FDA approved for P. falciparum treatment

AE - GI (N,D)

50
Q

Albendazole
Mebendazole
Thiabendazole

A

Inhibit parasite mitosis
On empty stomach for lumenal nematodes, w/ fatty meal for tissue dwelling helminths

Albendazole/Mebendazole - single high dose resolves ascarias, pin-, whip- & hookworm infections
Thiabendazole - 2nd line in strongoloides, topical in cutaneous larval migrans

AE - T - GI (N,V) & CNS distrubances
- A/M - GI upset
CI in pregnancy & children <2

51
Q

Ivermectin

A

causes hyperpol in parasitic muscle cells = paralysis (no effect on mammalian cells)

DoC for strongyloidiasis (2 doses recommended)
Tx of tissue dwelling nematodes (L. loa (eye worm), O. volvulus (river blindness) & filarial worms (W. bancrofti & B. malayi)

52
Q

Pyrantel Pamoate

A

Activate cholinergic N receptors in somatic muscle of nematodes = depolarizing neuromuscular blockade

DoC for pinworm (tx entire househole)
Poorly absorbed = selective toxicity for intestinal nematodes

53
Q

Praziquantel

A

↑ Ca permeability in worm’s tegument causing its depol = spastic paralysis in trematodes & ↑ immune detection

DoC in nearly all tapeworm & fluke infections of man (also cysticercosis and schistosomes)

AE - Abdominal discomfort, headache & dizziness
Indirect effects from immune response to dying worm (fever, rash, arthralgia, myalgia)

54
Q

Amphotericin B

A

Binds ergosterol in fungal cell membrane & forms pores = alters membrane permeability - fungicidal

DoC or alternative for many yeast (Candida, Cryptococcus) & mold (Aspergillis, Histoplasma, Coccidioides, Blastomyces, Mucor)
Intrathecally for fungal meningitis

AE - Fever/chills, hypotension, nephrotoxicity, arrhythmias, anemia, IV phlebitis
-Liposomal packaged formulation decreases toxicity

55
Q

Nystatin

A

Binds to ergosterol in fungal cell membrane & forms pores

Tx - candidiasis (oral suspension for thrush, topical for diaper rash/ vaginal candidiasis)

poorly absorbed, toxic & unpleasant taste = only used topically

56
Q

Azoles:
Fluconazole, ketoconazole, clotrimazole, miconazole
itraconazole, voriconazole

A

Inhibit conversion of lanosterol to ergosterol

Tx - local & less serious systemic mycoses

AE - Testosterone synthesis inhibition (gynocomastia esp w/ ketoconazole), liver dysfunction (inhibits P450)

57
Q

Ketoconazole

A

Inhibit conversion of lanosterol to ergosterol

lower selective toxicity but higher degree of P450 inhibition

AE -Testosterone synthesis inhibition & P450 inhibition

58
Q

Fluconazole

A

Inhibit conversion of lanosterol to ergosterol

DoC in candidiasis, crytococcosis & coccidiomycosis
- chronic suppression of cryptococcal meningitis in AIDS patients & candidal infections of all types

Highest therapeutic index of all azoles (lowest level of P450 interaction)

59
Q

Voriconazole

A

Inhibit conversion of lanosterol to ergosterol

DoC for aspergillus
-endemic dimorphic fungi & candida

AE - transient visual distrubances (30%), blurred vision, photophobia & altered perception of color; hallucinations; liver enzyme abnormalities and rash (common)

60
Q

Itraconazole

A

Inhibit conversion of lanosterol to ergosterol

DoC for blastomycosis, coccidioides, histoplasma

requires low gastric pH for absorption (don’t take w/ PPI)
Significant drug interactions

61
Q

Posaconazole

A

Inhibit conversion of lanosterol to ergosterol

Tx - Candida, Aspergillus & agents of mucormycoses; as well as cryptococcus & dimorphic fungi

Absorption improved w/ fatty meals

Strong inhibitor of P450

62
Q

Flucytosine

A

Inhibits DNA & RNA biosynthesis by conversion to 5-FU by cytosine deaminase

Tx- Systemic fungal infections (esp. meningitis caused by Cryptococcus) in combo w/ amphotericin B

Bone marrow toxicity = anemia, leukopenia, thrombocytopenia

63
Q

Caspofungin
Micafungin
Anidulafungin

A

Echinocandins
Inhibit cell wall synthesis by inhibiting synthesis of β-glucan

Tx - Invasive aspergillis & Candida
poor penetration of CNS, but distributed to all other major organs

GI upset, flushing (by histamine release) but generally well tolerated due to selective toxicity

64
Q

Griseofulvin

A

Interferes w/ microtubule function; disrupts mitosis
Deposits in keratin-containing tissues

Oral Tx of superficial inhections - 2nd line in dermatophyte infections (inhibits growth; tinea, ringworm)

↑ P-450 = ↑ warfarin metabolism, ↓ oral contraceptives

Teratogenic, carcinogenic, confusion, headaches

65
Q

Terbinafine

Naftifine

A

Inhibits fungal squalene epoxidase - damages cell membrane of susceptible fungi

Dermatophytosis (1st line in onychomycosis - fungal infection of nails) keratophylic

GI upset, headaches, hepatotoxicity, taste disturbances

Topical preps available in many OTC products for tinea cruris, tinea corporis etc.

66
Q

Clotrimazole

Miconazole

A

Most commonly used as Topical Azoles
Inhibit conversion of lanesterol to ergosterol

Tx - vulvovaginal candidiasis, dermatophyte infections, oral lozenges for oral thrush

Resistance rare, absorption negligible, AE rare

67
Q

Acyclovir
Valacylovir
Famciclovir

A

Monophosphorylated by HSV/VZV thymidine kinase (=not active in uninfected cells) and preferentially inhibits viral DNA pol by chain termination

Tx - HSV & VZV (weak against EBV, no activity against CMV)
=HSV-induced mucocutaneous & genital lesions, encephalitis. prophylaxis in immunocompromised patients
Use famciclovir for herpes zoster

Valacylovier = more orally bioavailable prodrug of Acyclovir

Resistance via mutated viral thymidine kinase

AE - obstructive crystalline nephropathy & acute renal failure if not adequately hydrated

68
Q

Foscarnet

A

Viral DNA polymerase inhibitor that binds to the pyrophosphate-binding site of the enzyme. Does no require activation by viral kinase

CMV retinitis in immunocompromised Pt when ganciclovir fails
acyclovir-resistant HSV

Resistance via mutated DNA pol

AE - Nephrotoxicity

69
Q

Ganciclovir

Valganciclovir

A

converted to 5’-monophosphate by CMV viral kinase (CMV UL97), preferentially inhibits viral DNA pol

Tx - CMV (esp in immunocompromised Pt)
Valganciclovir = more orally bioavailable prodrug

Resistance via mutated DNA pol, or lack of CMV UL97

AE - Leukopenia, neutropenia, thrombocytopenia (myelosuppression), renal toxicity
-more toxic to host enzymes than acyclovir

70
Q

(Trifluridane)

A

Phosphorylated by cellular enzyme & competitively inhibits thymidine for incorporation into newly synthesized genomes

Ocular admin for keratoconjunctivitis & recurrent epithelial karatitis due to HSV-1/2

71
Q

Oseltamivir

Zanamivir

A

Inhibit influenze neuraminidase = ↓ the release of progeny virus

Treatment and prevention of both influenze A & B

O - approved in pt 1+, Z - 7+ yo
Z = inhalable powder = CI in Pt w/ preexisting pulmonary disease

72
Q

(Amantadine)

Rimantadine

A

Inhibit influenze A M2 proteins (ion channel forming protein required for nucleocapsid release)

↓ duration of disease in susceptible Influenze A

high resistance levels from mutation in M2 proteins (rarely used anymore)

73
Q

Ribavarin

A

Inhibits synthesis of guanine nucleotides by competitively inhibiting inosine monophosphate dehydrogenase

Tx - RSV, Chronic Hep C

AE - Hemolytic anemia, *Severe teratogen**

74
Q

(Sofobuvir)

A

Incorporated into newly synthesized RNA by RdRp resulting in premature chain termination

Tx - all HCV genotypes

AE - anemia, fatigue, headache, insomnia, nausea

  • avoid coadmin w/ potent inducers of p-glycoprotein
    (ex. St. John’s wort, rifampin)
75
Q

(Pegylated-Interferon)

A

Signaling through binding to IFN receptors & Jak/Stat pathway to invoke an “antiviral state” in cells

Pegylation = attachment of an inert molecule (polyethylene glycol), which slows absorption and clearance

Tx - HCV (genotypes 1,4,5,6)

AE - flu-like symptoms, myelosuppression, neurotoxicity, autoimmune disorders, injection site inflammation

76
Q 
Abacavir (ABC)
Didanosine (ddI)
Emtricitabine (FTC)
Lamivudine (3TC)
Stavudine (d4T)
Tenofovir (TDF)
Zidovudine (ZDV, formerly AZT)
A

NRTIs - competitively inhibit nucleotide binding to reverse transcriptase & terminate the DNA chain
Tenofovir = nucleotide, others are nucleosides and need to be phosphorylated to be active

HIV antiretrovirals
ZDV = used for general prophylaxis & durin pregnancy to ↓ risk of fetal transmission

AE - Bone marrow suppression (can be reversed w/ G-CSF & erythropoietin), peripheral neuropathy, lactic acidposis, rash, anemia (ZDV), pancreatitis (ddI)

77
Q

Efavirenz
Nevirapine
Delavirdine

A

NNRTIs - bind to & inhibit reverse transcriptase (at dif site than NRTIs), don’t need phosphorylation for activation

HIV antiretrovirals

AE - rash, hepatotoxicity
Vivid dreams & CNS symptoms w/ efavirenz
efavirenz, delavirdine are CI in pregnancy

78
Q 
Atazanavir
Darunavir
Fosamprenavir
Indinavir
Lopinavir
Ritonavir
Saquinavir
A

Protease inhibitors - prevent maturation of new viruses by inhibiting cleavage of the polypeptide products of HIV mRNA into their functional parts by HIV-1 protease

HIV antiretrovirals

Ritonavir can “boost” other drug concentrations as a potent inhibitor of cytochrome P450

AE - hyperglycemia, GI intolerance (N,D), lipodystrophy, nephropathy, hematuria (indinavir)

79
Q

Maraviroc

Enfuvirtide

A

Fusion inhibitors, antiretrovirals

M - Binds CCR-5 on surface of T cells/monocytes = inhibits interaction w/ gp120

E - Binds gp41 = inhibits viral entry

AE - skin reaction at injection site

80
Q

Raltegravir

A

Integrase inhibitor - inhibits HIV genome integration into host cell chromosome by reversibly inhibiting HIV integrase
has a big impact on viral load as it acts upstream of the viral replication process

AE - Hypercholesterolemia

81
Q

Glucocorticoids

A

Immunosuppressant - Inhibit NF-kB = suppress both B & T cell function by ↓ transcription of many cytokines

Tx - transplant rejection prophylaxis, many autoimmune disorders, inflammation

AE - hyperglycemia, osteoporosis, central obesity, muscle breakdown, psychosis, acne, hypertension, cataracts, peptic ulcers

  • can cause iatrogenic Cushing syndrome*
82
Q

Cyclosporin

A

Immunosuppressant - Calcineurin inhibitor - binds cyclophilin = blocks T cell activation by preventing IL-2 TRANSCRIPTION

Tx - transplant rejection prophylaxis, psoriasis, RA

AE - NEPHROTOXICITY, htn, hyperlipidemia, hyperglycemis, tremor, hirsutism, gingival hyperplasia

83
Q

Tacrolimus

A

Immunosuppressant - Calcineurin inhibitor - binds FKBP = blocks T cell activation by preventing IL-2 TRANSCRIPTION

Tx - transplant rejection prophylaxis

AE - NEPHROTOXICITY, ↑ risk diabetes, neurotoxicity, htn, hyperlipidemia, hyperglycemia, tremor

84
Q

Sirolimus

Rapamycin

A

immunosuppressant - mTOR inhibitor - binds FKBP = blocks T & B cell differentiation by preventing IL-2 SIGNAL TRANSDUCTION

Tx - kidney transplant rejection prophylaxis (non-nephrotoxic)

AE - Anemia, thrombocytopenia, leukopenia, insulin resistance, hyperlipidemia

85
Q

Azathioprine

A

immunosuppressant = Antimetabolic precursor of 6-MP = inhibits lymphocyte proliferation by blocking nucleotide synthesis

Tx - transplant rejection prophylaxis, RA, CD, glomerulonephritis, other autoimmune conditions

AE - leukopenia, anemia, thrombocytopenia

86
Q

Basiliximab

A

Immunosuppressant - monoclonal Ab, blocks IL-2R

Tx - Kidney transplant rejection prophylaxis

AE - Edema, HTN, tremor

87
Q

(Mycophenolate Mofetil)

A

rapidly hydrolyzed to mycophenolic acid & selectively inhibits inosine monophosphate dehydrogenase (required for de novo synthesis of guanine nucleotides) = inhibits lymphocyte proliferation

Tx - transplant rejection prophylaxis (often in combo w/ a glucocorticoid & calcineurin inhibitor)

AE - leukopenia, RBC aplasia, NVD
Increases incidence of CMV infections
CI - pregnancy (cleft lip & palate, congenital heart defects)

88
Q

(Antithymocyte Globulin)

A

Rabbit serum containing purified gammaglobulin specific to human thymocytes (Ab to CD2,3,4,8,11a,25,44,45 & HLA I, II) = deplete lymphocytes by complement-mediated cytotoxicity

Tx - prophylactic & induction immunosuppression after transplant, & in acute rejection of solid organ transplants

AE - serum sickness, leukopenia, thrombocytopenia, malignancy
F,C, malaise, HTN (from release of cytokines = can by minimized w/ pre-medication by glucocorticoids)

89
Q

(Muromonab-CD3)

A

Mouse Ab against CD-3 = depletion of T cells through compliment-mediated destruction & functional inactivation of remaining T cells

Tx - reverse glucocorticoid-resistant organ transplant rejection episode (circulating T cells disappear w/in minutes)

Neutralizing Ab can be made = repeat Tx is CI

AE - cytokine storm w/in 30 min (reduced by prior glucocorticoid admin) = F,C, malaise, HTN

  • tremor, NVD, myalgia, arthralgia, weakness
  • Potentially fatal anaphylaxis, PE, ARDS, Cardiac arrest, neoplasm, infection
90
Q

Inflixamab
Adalimumab
(Etanercept)

A

Bind & inhibit TNF-α

Tx - IBD, RA, ankylosing spondylitis, psoriasis

AE - Increase risk of serious infections, lymphomas/other malignancies

I - chimeric mouse/human monoclonal Ab
A - recombinant human IgG1 monoclonal
E - ligand binding portion of human TNF-α receptor attached to Fc of human IgG1

Pharmacology (6 decks)

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