Pharma Topic List C Flashcards
C.1 General considerations of antimicrobial therapy. Disinfectants and antiseptics - Classes of Disinfectants
- alcohol, glycols (ethanole, isopropanol)
- Aldehydes
- Phenols and Derivatives (chlorhexidine)
- Acids
- Halogens and Halogen containing chemicals (poviodine iodine)
- Metals
- Detergents - Octenidin, invert soaps
C.1 General considerations of antimicrobial therapy. Disinfectants and antiseptics - Drugs
ethanole
isopropylalcohol
chlorhexidine
povidone iodine
octenidin
H2O2
invert soaps
ethanole
Aliphatic alcohol (70%)
it dehydrates and denatures proteins
Bactericidal
Removes lipids from skin - skin disinfectant
C.1 General considerations of antimicrobial therapy. Disinfectants and antiseptics
isopropylalcohol
Aliphatic alcohol
more effective but more toxic than ethanole
C.1 General considerations of antimicrobial therapy. Disinfectants and antiseptics
chlorhexidine
Phenol - Biguanide derivative
component of creams and soaps - no tissue irritation
used to disinfect skin
MoA - absorbed into bacterial membrane causing leakage of cytoplasmic proteins
C.1 General considerations of antimicrobial therapy. Disinfectants and antiseptics
povidone iodine
Halogen
widely used as pre-op skin anti-septic
C.1 General considerations of antimicrobial therapy. Disinfectants and antiseptics
octenidin
halogen derivative
acts against Gram + and - bacteria
used as mucosal, skin antiseptic
CI - open wounds
C.1 General considerations of antimicrobial therapy. Disinfectants and antiseptics
H2O2
Oxidizing Agent
short-lived antimicrobial action via free radical release (catalase)
Bacteriostatic
C.1 General considerations of antimicrobial therapy. Disinfectants and antiseptics
invert soaps
synthetic detergent
Cation active surfactant disinfectant
C.1 General considerations of antimicrobial therapy. Disinfectants and antiseptics - drugs
C.2. Antimycobacterial drugs
isoniazide
rifampin
pyrazinamide
ethambutol
streptomycine
kanamycine
cycloserine
dapson
isoniazide
PRODRUG – activated by bacteria’s catalase peroxidase. Targets the enzyme’s acyl carrier protein reductase and KatA which are essential for mycolic cell wall synthesis. Disrupts cell wall synthesis.
PO, IV – acylated in liver. Most impt TB drug.
TX – TB used as prophylaxis.
SE – neurotoxicity due to pyridoxine (vit b6) def, sideroblastic anemia, Drug Lupus, acute hemolysis in G6PD def patient.
C.2. Antimycobacterial drugs
rifampin
bactericidal.
Inhibits DNA dependent RNA polymerase – transcription inhibitor.
Resist – alteration of polymerase enzyme.
PO, enterohepatic recycling with partial hep met – excreted in feces.
Induces CYP450 (CYP3A4) – accelerates its own metabolism.
TX – TB, leprosy, in combo w vancomycin -MRSA, prophylaxis N. meningitids, H. influenzae, Staph.
SE – thrombocytopenic purpura, orange discoloration, ARF (renal failure).
C.2. Antimycobacterial drugs
pyrazinamide
synthetic PRODRUG – disrupts E metabolism and cell membrane fn.
Bacteriostatic.
Res – mutation in gene encoding enzymes involved in drug activation. Synergistic effect with isoniazid and rifampin. If the TB stand is INH resistant can be used as replacement.
PO, partial hepatic met – eliminate in urine.
SE – non-gout polyarthralgia, hyperuricemia, hepatotoxicity, skin rash.
C.2. Antimycobacterial drugs
ethambutol
Bacteriostatic – inhibits cell wall synthesis.
Resis – alteration of drug target.
PO, eliminated unchanged din urine.
SE - dose dependent visual disturbance, headache, confusion.
C.2. Antimycobacterial drugs
streptomycin
aminoglycoside, protein synthesis inhibitor – inhibits protein synthesis – 2nd line TB.
Parenteral – IM 2-3 w. NO BBB.
TX – miliary TB.
SE – nephrotoxic, ototoxic
C.2. Antimycobacterial drugs
kanamycin
aminoglycoside, protein synthesis inhibitor.
2nd line – only used when streptomycin resistant.
Used in combo regime
C.2. Antimycobacterial drugs
cycloserine
inhibitor of cell wall synthesis – inhibits racemic alanine.
TX – TB resistant to 1st line drugs.
SE – severe CNS
C.2. Antimycobacterial drugs
dapson
inhibitor of folic acid synthesis, bacteriostatic. PO with enterohepatic recycling.
TX – leprosy.
Alternate drug penumocysitis jirovecii pneumonia
C.2. Antimycobacterial drugs
C.3. Antiprotozoal and antihelminthic drugs.
chloroquine
mefloquine
quinine
lumefantrin
artemether
primaquine
metronidazole
atovaquon
proguanil
mebendazol
ivermectin
niclosamid
chloroquine
C.3. Antiprotozoal and antihelminthic
Tx - Malaria - first line
heme polymerase inhibitor - Blood Schizonticidal
combined with primaquine to act on dormant hepatic form
po - rapidly absorbed; large distribution
High rate of resistance - esp P. falciparium
SE: low dose –> skin irritation, rash, headaches
high dose –> retinal damage, Auditory damage, QT prolongation
used as anti-inflammatory in rhumatoid arthritis, lupus
Chloroquine
Mechanism of Action
C.3. Antiprotozoal and antihelminthic
Drug accumulates int he food vacoule (it becomes protonated and trapped) –> inhibits heme polymerization into hemozin - this forms a highly toxic heme-chloroquie complex –> lysis of membrane
mefloquine
C.3. Antiprotozoal and antihelminthic
heme polymerase inhibitor - Blood Schizonticidal
PO
tx and prophylaxis - Malaria
SE - Gi, bradycardia
quinine
C.3. Antiprotozoal and antihelminthic
heme polymerase inhibitor - Blood Schizonticidal
only used to tx P. falciparum
IV, IM, PO
SE: Cinnchoism, QT prolong, Blackwater fever
lumefantrin
C.3. Antiprotozoal and antihelminthic
tx- Blood Schizonticidal
combo with Artemether tx P. falciparium
NEVER USED ALONE
SE - QT prolong
artemether
C.3. Antiprotozoal and antihelminthic
folate synthesis inhibitor - Blood Schizonticidal
MoA: binds to heme and creates free radicals that damage parasitic proteins - effective against all species
Always combine with another anti-malaria in order to avoid resistance
CI - first trimester
primaquine
C.3. Antiprotozoal and antihelminthic
tx - Heaptic form = Hypnozoites
always given with blood schizonticide
PO
SE - drug-induced hemolytic anemia in G6PD def
methemoglobinemia
metronidazole
C.3. Antiprotozoal and antihelminthic
tx - Amebic dysentery caused by Entamoeba histolytics - Antiprotozoal
PO, IV, topical
CI - first trimester
tx - C. diff, H pylori, Lactobacillus, Trichamonas vaginalis, Giardia
SE: headache, stomach cramps
High Dose - causes Disulfiram like rxn - inhibits aldehyde dehydrogenase
C.3. Antiprotozoal and antihelminthic
Metronidazole Mechanism of Action
MOA - non-toxic to human
utilizes bacteria/protozoan’s Ferredoxn enzyme - donates an electron to the metrnidazole creating a free radical that damages the DNA
atovaquon
C.3. Antiprotozoal and antihelminthic
inhibits mitochondrial function
combined with Proguanil - act syngeristically
tx - Extraerythrocytic Schizontocidial
prophylaxis in chloroquin resistance areas
can tx - pneumocystis jirovecii
proguanil
C.3. Antiprotozoal and antihelminthic
Folate synthesis inhibitor
combined with Atovaquone - act syngeristically
tx - Extraerythrocytic Schizontocidial
prophylaxis in chloroquin resistance areas
can tx - pneumocystis jirovecii
mebendazol
C.3. Antiprotozoal and antihelminthic
Anti-helminithic
inhibits the polymerization of beta tubulin of the microtubules
–> inhibition of furmarate-reductase and oxidative phosphorylation = paralysis
PO
tx - roundworms, pinworms, tapeworms
SE: TERATOGENIC
ivermectin
C.3. Antiprotozoal and antihelminthic
Anti-helminithic
tx - roundworms
MoA - enhances GABA effects in the worms - paralysis
SE - mild - caused by the disintergration of the worms
niclosamid
C.3. Antiprotozoal and antihelminthic
Anti-helminithic
tx - tapeworms
MoA - inhibits oxidative phosphorylation
SE - nausea, vomiting, alcohol forbidden for one day
C.4. Antifungal agents
clotrimazole
fluconazole
itraconazole
voriconazole
terbinafine
nystatin
amphothericin B
caspofungin
flucytosin
clotrimazole
C.4. Antifungal agents
fluconazole
C.4. Antifungal agents
itraconazole
C.4. Antifungal agents
voriconazole
C.4. Antifungal agents
terbinafine
C.4. Antifungal agents
nystatin
C.4. Antifungal agents
amphothericin B
C.4. Antifungal agents
caspofungin
C.4. Antifungal agents
flucytosin
C.4. Antifungal agents
C.5. Agents to treat Herpes simplex (HSV), varicella-zoster (VZV) virus, cytomegalovirus (CMV) and respiratory syncytial virus (RSV) infection. Anti-influenza agents - Drugs
aciclovir
valaciclovir
ganciclovir
valganciclovir
cidofovir
foscarnet
oseltamivir
ribavirin
palivizumab
aciclovir
C.5. Agents to treat Herpes simplex (HSV), varicella-zoster (VZV) virus, cytomegalovirus (CMV) and respiratory syncytial virus (RSV) infection. Anti-influenza agents
valaciclovir
C.5. Agents to treat Herpes simplex (HSV), varicella-zoster (VZV) virus, cytomegalovirus (CMV) and respiratory syncytial virus (RSV) infection. Anti-influenza agents
ganciclovir
C.5. Agents to treat Herpes simplex (HSV), varicella-zoster (VZV) virus, cytomegalovirus (CMV) and respiratory syncytial virus (RSV) infection. Anti-influenza agents
valganciclovir
C.5. Agents to treat Herpes simplex (HSV), varicella-zoster (VZV) virus, cytomegalovirus (CMV) and respiratory syncytial virus (RSV) infection. Anti-influenza agents
cidofovir
C.5. Agents to treat Herpes simplex (HSV), varicella-zoster (VZV) virus, cytomegalovirus (CMV) and respiratory syncytial virus (RSV) infection. Anti-influenza agents
foscarnet
C.5. Agents to treat Herpes simplex (HSV), varicella-zoster (VZV) virus, cytomegalovirus (CMV) and respiratory syncytial virus (RSV) infection. Anti-influenza agents
oseltamivir
C.5. Agents to treat Herpes simplex (HSV), varicella-zoster (VZV) virus, cytomegalovirus (CMV) and respiratory syncytial virus (RSV) infection. Anti-influenza agents
ribavirin
C.5. Agents to treat Herpes simplex (HSV), varicella-zoster (VZV) virus, cytomegalovirus (CMV) and respiratory syncytial virus (RSV) infection. Anti-influenza agents
palivizumab
C.5. Agents to treat Herpes simplex (HSV), varicella-zoster (VZV) virus, cytomegalovirus (CMV) and respiratory syncytial virus (RSV) infection. Anti-influenza agents
C.6. Antiretroviral agents. - Drugs
zidovudine
lamivudine
tenofovir
emtricitabine
abacavir
etravirine
darunavir
ritonavir
lopinavir
elvitegravir
maraviroc
zidovudine
C.6. Antiretroviral agents
lamivudine
C.6. Antiretroviral agents
tenofovir
C.6. Antiretroviral agents
emtricitabine
C.6. Antiretroviral agents