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
