Brainscape's Knowledge GenomeTM


Top Flashcards (Certified)
All Flashcards

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

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

(90 cards)

Start Studying
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

β-lactamase inhibitors

A

CAST

Clavulanic Acid, Sulbactam, Tazobactam

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Cilistatin

A

Inhibits renal dehydropeptidase I

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Clindamycin
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
26
(Linezolid)
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,
27
Sulfamethoxazole (SMX) Sulfisoxazole Sulfadiazine
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
28
Trimethoprim (TMP) | Pyrimethamine
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
29
Fluoroquinolones - sparfloxacin - nalidixic acid (a quinalone)
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
30
Norfloxacin
Group 1 Fluoroquinolone - Inhibit topoisomerase II, IV Least active - has Gram + & - effects GI, Cardio (prolonged QT), tendon rupture bind divalent cations which prevents absorption
31
Ciprofloxacin Levofloxacin Ofloxacin
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
32
Moxifloxacin Gemifloxacin (Getifloxacin)
Group 3 Fluoroquinolone - Inhibit topoisomerase II, IV Gram + (some G-) GI, Cardio (prolong QT), tendon rupture bind divalent cations which prevents absorption
33
Metronidazole
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)
34
Isoniazid (INH)
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
35
Rifampin | Rifabutin
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
36
Ethambutol
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)
37
Pyrazinamide
Thought to acidify intracellular environment via conversion to pyrazinoic acid. Effective in acidic pH of phagolysosomes Tx - multidrug Tx of TB hyperuricemia, hepatoxicity
38
Dapsone
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
Clofazimine
Bacterial dye w/ uncertain MoA Multidrug Tx of lepromatous TB AE - red-brown to black skin discoloration
40
Iodoquinol
``` 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
Paromomycin
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
Nitozaxanide
Interferes w/ PFOR = disruption of anaerobic energy metabolism Oral suspension approved for Tx of Cryptosporidiosis (in immunocompromised/ AIDS Pt) & Giardiasis in Pt > 1yo
43
Chloroquine
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
Quinidine
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
Mefloquine
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
Primaquine
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
Malarone
atovaquone/proguanil Tx & prophylaxis of P. falciparum (highly efficacious)
48
Doxycycline (tetracyclines)
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
Artemisinin Derivatives
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
Albendazole Mebendazole Thiabendazole
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
Ivermectin
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
Pyrantel Pamoate
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
Praziquantel
↑ 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
Amphotericin B
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
Nystatin
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
Azoles: Fluconazole, ketoconazole, clotrimazole, miconazole itraconazole, voriconazole
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
Ketoconazole
Inhibit conversion of lanosterol to ergosterol lower selective toxicity but higher degree of P450 inhibition AE -Testosterone synthesis inhibition & P450 inhibition
58
Fluconazole
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
Voriconazole
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
Itraconazole
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
Posaconazole
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
Flucytosine
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
Caspofungin Micafungin Anidulafungin
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
Griseofulvin
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
Terbinafine | Naftifine
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
Clotrimazole | Miconazole
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
Acyclovir Valacylovir Famciclovir
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
Foscarnet
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
Ganciclovir | Valganciclovir
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
(Trifluridane)
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
Oseltamivir | Zanamivir
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
(Amantadine) | Rimantadine
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
Ribavarin
Inhibits synthesis of guanine nucleotides by competitively inhibiting inosine monophosphate dehydrogenase Tx - RSV, Chronic Hep C AE - Hemolytic anemia, *Severe teratogen**
74
(Sofobuvir)
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
(Pegylated-Interferon)
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
``` Abacavir (ABC) Didanosine (ddI) Emtricitabine (FTC) Lamivudine (3TC) Stavudine (d4T) Tenofovir (TDF) Zidovudine (ZDV, formerly AZT) ```
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
Efavirenz Nevirapine Delavirdine
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
``` Atazanavir Darunavir Fosamprenavir Indinavir Lopinavir Ritonavir Saquinavir ```
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
Maraviroc | Enfuvirtide
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
Raltegravir
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
Glucocorticoids
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
Cyclosporin
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
Tacrolimus
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
Sirolimus | Rapamycin
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
Azathioprine
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
Basiliximab
Immunosuppressant - monoclonal Ab, blocks IL-2R Tx - Kidney transplant rejection prophylaxis AE - Edema, HTN, tremor
87
(Mycophenolate Mofetil)
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
(Antithymocyte Globulin)
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
(Muromonab-CD3)
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
Inflixamab Adalimumab (Etanercept)
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)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2025 Bold Learning Solutions. Terms and Conditions