Pharma Least C Flashcards
Ethanol& isopropyl alcohol
Disinfectants and antiseptics
Alcohols
Chlorhexidine
Antiseptic & disinfectant
Chlorinated phenols
Hydrogen peroxide H2O2
Oxidising agents
Disinfectants and antiseptics
Povidone iodine
Halogens
Disinfectants antiseptics
Invert soaps
Disinfectants and antiseptics
Cationic surfactant
Octenidine dihydrochloride
Disinfectants and antiseptics
Cationic surfactant
Povidone iodine
Disinfectants and antiseptics
Halogens
Rifampin
Antimycobacterial drug
Mechanism of action:
- Inhibition of DNA-dependent RNA polymeraseàinhibition of transcription
- Bactericidal effect, long PAE
Spectrum + clinical effect:
- M. tuberculosis, M. kansasii, M. avium, M. leprae
- Use: TB treatment, leprosy treatment, prophylaxis
Isoniazid
Antimycobacterial drug
Mechanism of action:
- Inhibits synthesis of mycolic acidàbactericidal effect Spectrum + clinical effect:
- Most important drug used in TB treatment
Pyrazinamide
Antimycobacterial drugs
Mechanism of action:
- Inhibits CoA synthesisàbacteriostatic effect
Spectrum + clinical effect:
- Acts against M. tuberculosis only
Ethambutol
Antimycobacterial drugs
Mechanism of action:
- Inhibits cell wall synthesis (arabinogalactan) Spectrum + clinical effect:
- Mycobacteria only
Streptomycin & Kanamycin
Antimycobacterial drugs 2nd line agent
Mechanism of action:
- Protein synthesis inhibitor (aminoglycoside)àbactericidal effect
Spectrum + clinical effect:
- Streptomycin: Acts only against free mycobacteria (M. kansasii and avium are
resistant)àCOMBINATION TREATMENT!
Dapson
Antimycobucterial drug
Mechanism of action:
- Inhibits folic acid synthesisàbacteriostatic effect
Spectrum + clinical effect:
- Leprosy (M. leprae), pneumocystitis jirovecii pneumonia in AIDS patients
Cycloserine
Antimycobacterial drugs
Mechanism of action:
- Cell wall synthesis inhibitoràinhibit peptidoglycan synthesis
Spectrum + clinical effect:
- TB resistant to 1st line agents
Chloroquine
Antiprotozoal drug
Mechanism:
- Blood schizonticideàinhibit heme-polymeraseàIC heme accumulation is toxic
for the parasite Uses:
- Treatment + prophylaxis for malaria (P. falciparum)
Mefloquine
Antiprotozoal drugs
Similar to chloroquine, slower acting
- Mostly for prophylaxis
Atovaquone/proguanil
Antiprotozoal
Mechanism:
- Atovaquone: inhibits mitochondrial metabolism
- Proguanil: antimetaboliteàanti-folate drug
Uses:
- Treatment + prophylaxis of MDR P. falciparum
Primaquine
Antiprotozoal
Mechanism:
- Tissue schizonticideàkills schizonts in the liver Uses:
- Recurrent malaria
- Eradication of liver stages of P. vivax and P. ovale
Metronidazole
Antiprotozoal
Mechanism of action:
- Interferes with nucleic acid synthesisàproduces toxic intermediary metabolites Spectrum + clinical effect:
- Protozoans (trichomonas, G. lamblia, amoeba, Gardnerella vaginalis)
- Anaerobic gram (-) bacteria
Mebendazole
Antihelmintic drug
Mechanism:
- Inhibits microtubule synthesis + glucose uptake
Uses:
- Roundworms + tapeworms (Ascaris lumbricoides, Enterobius vermicularis, Trichuris
trichuria)
Ivermectin
Antihelmintic drugs
Mechanism:
- Enhances GABA-mediated transmission in roundwormsàimmobilization
Uses:
- RoundwormsàWuchereria bancrofti (filaria)
Niclossmide
Antihelmintic drug
Mechanism:
- Inhibits oxidative phosphorylation Uses:
- Tapeworms (taenia saginata + solium)
Quinine
Antiprotozoal
Blood schizonticide
- Inhibit protozoal DNA
replication
Arthemether
Antiprotozoal
Blood schizonticide
- Production of free radicals
within the plasmodium food vacuoles
Treatment of multidrug- resistant malaria
- Effective against quinine- resistant strains
Niclosamid
Antihelmintic drug
Uncoupling oxidative phosphorylation
Tapeworms:
- Taenia saginata
(beef tapeworm)
- Taenia solium
(pork tapeworm)
- Diphyllobothrium latum
(fish tapeworm
Ivermectin
Antihelmintic drug
Facilitates GABA-mediated transmission in nematodes and causes immobilization of parasites
Intestinal nematodes:
- Strongyloides stercoralis
Tissue/blood nematodes:
- Cutaneous larva migrans
- Oncocerca volvulus
Lumefantrine
Antiprotozoal
Blood schizonticide
- Mechanism unknown In combination with artemether against P. falciparum
Clotrimazole
Antifungal drug
Azoles
Topical formulations treat dermatophytes, superficial candidiasis, vaginal candidiasis
- Available as over-the-counter drug
Itraconazole
Antifungal drug
Azoles
Dimorphic fungi, Blastomyces and Sporothrix infections
- 2nd-line agent for Aspergillus, Coccidioides, Cryptococcus, Histoplasma
Fluconazole
Antifungal
Azoles (trizole 1 St gen)
Esophageal, oropharyngeal, vaginal, and invasive candidiasis
- Coccidioides infections
- Cryptococcus meningitis
Voriconazole
Antifungal drug
Azoles ( trazoles 2nd gen )
Aspergillus infections
- Invasive candida infections (including
sepsis)
Amphoterecin B & nystatin
Antifungal drugs
Polyenes
Amphoteric compounds with both polar and nonpolar structural components →
interact with ergosterol in fungal membranes to form ‘pores’, which disrupt membrane permeability
- Fungicidal effect
- Resistant fungal strains appear to have low ergosterol content in their cell membranes
Caspofugin
Antifungal drug
Echinocandias
Inhibit the synthesis of β(1-3)-glucan, a critical component of fungal cell wall
Candida infections failed to respond to amphotericin B (disseminated and mucocutaneous infections)
- Mucor infection
- Aspergillus infection
Flucyrosine (5-FC)
Antifungal drug
Antimetabolites
Activated by fungal cytosine deaminase to 5-fluorouracil (5-FU), which after tri- phosphorylation is incorporated into fungal RNA
- 5-FU also forms 5-Fd-UMP, which inhibits thymidylate synthase → thymine ↓ (inhibits DNA synthesis)
- Resistance emerges rapidly if used alone; involves decreased activity of the fungal permease
Terbinafine
Antifungal drug
Inhibits squalene epoxidase, interfering with ergosterol synthesis (fungal membrane)
- Fungicidal effect
Systemic drug
Acyclovir
Antiviral
Agents against HSB q/2 VZV
Mechanism of action:
- Guanosine analog
- Acyclovir is converted to its triphosphate form, acyclovir
triphosphate (ACV-TP)àinhibits viral DNA polymerase
- Resistance: involves changes of viral DNA polymerase or
decreased activity of kinase
Ganciclovir
Antiviral
Agents against CMV
Mechanism of action:
- Deoxy-guanosine analog
- Mechanism similar to acyclovir
Spectrum + clinical effect:
- CMV (1st line agent), HSV-1/2, VZV to a lesser extent
Foscarnet
Antiviral drug
Mechanism of action:
- Pyrophosphate analog + not an antimetabolite
- Inhibits viral RNA- and DNA polymerase
Spectrum + clinical effect:
- CMV (2nd line agent)
- Use: CMV retinitis in HIV/AIDS patients, resistant HSV/CMV infections
Oseltamivir
Antiviral agent
Anti influenza agent
Mechanism of action:
- Inhibit neuraminidaseàneuraminidase usually cleave sialic acid bridges and thereby release the ready virion from the cellàprevent this, so the virus is unable to infect new cells
Spectrum + clinical effect:
- Influenza A + B virus
Palivizumab
Antiviral
Agents against RSV
Mechanism of action:
- Prophylactic agent
- Monoclonal antibody against RSV
Spectrum + clinical effect:
- Prophylaxis in immunocompromised children in RSV season
Ribavirin
Antiviral
Agents against RSV
Mechanism of action:
- Guanosine analog
- Inhibits viral RNA polymerase
Spectrum + clinical effect:
- Broad spectrum (HSV, VZV, influenza, RSV)
- Use: immunocompromised children with severe RSV
Zidovudine- thymidine analog
Antiretroviral drug
Nucleoside/nucleotide reverse transcriptase inhibitors (NRTIs):
Mechanism of action:
- Terminate the growing DNA chainàinhibit binding of nucleotides to reverse
transcriptase (RNA-dependent DNA polymerase) Indication:
- HIV-1 + HIV-2 infection
- Lamivudine, emtricitabine and tenofovir for HBV as well
Lamuvidine& emtricitabine- cytidine analogs
Antiretroviral drug
Nucleoside/nucleotide reverse transcriptase inhibitors (NRTIs):
Mechanism of action:
- Terminate the growing DNA chainàinhibit binding of nucleotides to reverse
transcriptase (RNA-dependent DNA polymerase) Indication:
- HIV-1 + HIV-2 infection
- Lamivudine, emtricitabine and tenofovir for HBV as well
Abacavir& tenofovir - purine analogs
Antiretroviral drug
Nucleoside/nucleotide reverse transcriptase inhibitors (NRTIs):
Mechanism of action:
- Terminate the growing DNA chainàinhibit binding of nucleotides to reverse
transcriptase (RNA-dependent DNA polymerase) Indication:
- HIV-1 + HIV-2 infection
- Lamivudine, emtricitabine and tenofovir for HBV as well
Etravirine
Antiretroviral drug
Non-nucleoside reverse transcriptase inhibitors (NNRTIs)
Mechanism of action:
- Bind to a site on reverse transcriptase different from the binding site of NRTIs
Spectrum + clinical effect:
- Only effective against HIV-1
Ritonavir&darunavir&lopinavir
Antiretroviral drugs
Protease inhibitors
Mechanism of action:
- Inhibition of HIV proteaseàthey usually cleave precursor polypeptides (Gag + Gag-
Pol) that form the final structural proteins of the virus
Dolutegravir
Antiretroviral drug
Integrase inhibitors
Binding to the integrase inhibits the integration of pro-viral DNA to host chromosome
- Acts only against HIV-1 infection
- Low cross-resistance, higher genetic barrier
Maravicor
Antiretroviral drug
Entry inhibitors
Mechanism of action:
- CCR5 co-receptor antagonistàprevent interaction between viral gp120 and CD4 on
target cellàno entry Spectrum + clinical effect:
- In combination with other antiretroviral agents in adult patients
Interferon alpha
Anti hepatitis drugs
Mechanism of action:
- Complex antiviral activityàinduces production of more than 20 antiviral proteins
Spectrum + clinical effect:
- Hepatitis B chronic infection
- Hepatitis C infection (acute + chronic)
Tenofovir
Anti hepatitis drug
Mechanism of action:
- Nucleotide analog + antiretroviral agent (NRTI) Spectrum + clinical effect:
- HBV infection
Entecavir
Anti hepatitis drug
Mechanism of action:
- Guanosine analog
- Inhibits HBV DNA polymerase
Spectrum + clinical effect:
- HBV infection
Ribavirin
Anti hepatitis drug
Mechanism of action:
- Guanosine analog
- Inhibits viral RNA polymerase
Spectrum + clinical effect:
- Hepatitis C infection (acute + chronic) in combination with IFN-alpha
- Broad spectrum (HSV, VZV, influenza)àimmunocompromised children with severe RSV
Sofosbuvir
Anti hepatitis drug
Direct acting antivirals
NS5B nucleoside polymerase inhibitors (NPI’s)
Dasbuvir
Anti hepatitis drug
Direct acting antivirals
NS5B non-nucleoside polymerase inhibitors (NNPI’s
Paritaprevir &grazoprevir
Anti hepatitis drug
Direct acting antivirals
NS3/4A protease inhibitors
Velpatasvir & elbasvir
Anti hepatitis drug
Direct acting antivirals
NS5A inhibitors
Penicillin G & penicillin V
Penicillins
Natural penicillin
Spectrum + clinical uses:
- Streptococcal infections (pharyngitis, rheumatic, fever, endocarditis)
- Gram (+) rods (actinomyces isrealii)
- Clostridium perfringens (gas gangrene)
- Enterococci, Neisseria meningitidis
Benzathine-penicillin
Penicillins
Narrow spectrum
Spectrum + clinical uses:
- Syphilis (spirocheteàTreponema pallidum)
- IM depot injection Toxicity and adverse effects:
- Same as natural penicillins
FluclOxacillin
Penicillins
Very narrow spectrum
Beta lactamase resistant Spectrum + clinical uses:
- Staphylococcal infections (endocarditis, osteomyelitis, skin infections)
- Resistant to beta-lactamase produced by staphylococci
- Oral, IV
Amoxicillin&icillin
Penicillins
B-road spectrum
Beta lactamase sensitive
Spectrum + clinical uses:
Spectrum similar to basic penicillins with increased activity against gram (-) rods
- H. influenzae, S. pneumoniae, H. pylori,
- High risk patients prior to dental procedures (prophylaxis)
- Used in combination with clavulanic acid
Piperacillin
Penicillins
Extended spectrum
Beta lactamase sensitive
Spectrum + clinical uses:
- Pseudomonas infectionà‘’anti-pseudomonal penicillins’’
- Together with tazobactam
Toxicity and adverse effects:
- Same as amoxicillin
Cephalexin & cephazolin
1st generation cephalosporins
Spectrum + clinical uses:
- Gram (+) cocci (Staph, Strep)
- Gram (-) UTI causing organisms (Proteus, E.coli, Klebsiella)
- Oral administration
Cefuroxime & cefoxitine
2nd generation cephalosporins
Spectrum + clinical uses:
- Same as 1st generation with extended gram (-) coverage
- H. influenza, M. catarrhalis (cefuroxime)
Cefixime & ceftriaxone& cefotaxime
3d generation cephalosporins B-road spectrum
Spectrum + clinical uses:
- Increased activity against gram (-)
- S. pneumoniae, N. gonorrhea (ceftriaxone)
- Empiric treatment of bacterial meningitis and sepsis
Cefepime
4th generation cephalosporins
Spectrum + clinical uses:
- Broad spectrum, resistant to most beta-lactamase
- Enterobacter, Hemophilus, Neisseria, Pneumococci, Pseudomonas
Ceftolozane & tazobactam ceftarolime fosamil
5th generation cephalosporins
Spectrum + clinical uses:
- MRSA, complicated UTI’s
Ceftazidime
3d generation cephalosporins
Cefiderocol
Cephalosporin
Imipenem & meropenem
Carbapenems
1st generation: ertapenem, 2nd generation: imipenem, meropenem
- Effective against gram (+), gram (-), anaerobes, aerobes à pseudomonas,
Acinetobacter
- Resistant to most beta-lactamases
Calculanate & tazobactam & vaboractam
Beta lactamase inhibitors
A fixed combination of a beta-lactam and a beta-lactamase inhibitor prevents
splitting of the beta-lactam ringàassuring good activity against the beta-lactamase
producing bacteria
Chloramphenicol
Chloramphenicol
Mechanism of action:
- Protein synthesis inhibitor à binds reversibly to the 50S ribosomal subunit à
inhibits peptide bond formation
- Bacteriostatic effect, but bactericidal in N. meningitidis, H. influenzae
Spectrum + clinical uses:
- Wide spectrum
- Gram (+), gram (-), anaerobes, Rickettsiae, Chlamydia, spirochetes
- Used in treatment of bacterial meningitidis, brain abscess, rickettsial infections
Colistin
Colistin
Mechanism of action:
- Polymyxin (cell wall synthesis inhibitor) à cell membrane damaging agent
- Bind + inactive endotoxin
- Bactericidal effect
Spectrum + clinical uses:
- Gram (-) bacteria à Pseudomonas! (Gram+ are resistant)
- Systemic use limited due to severe SEàlimited to topical treatment of superficial
skin infections
Sulfamethoxazole + trimethoprim
Group same as name
Mechanism of action:
- Sulfamethoxazole: inhibit dihydropteroate synthase à bacteriostatic
effect
- Trimethoprim: inhibit bacterial DHF reductase à bacteriostatic effect
- Sulfamethoxazole + trimethoprim: bactericidal effect
Spectrum + clinical uses: (used only in combination, not individually) Sulfonamide à sulfamethoxazole:
- Gram (+) and (-) bacteria, Staphylo, N. meningitidis, Chlamydia, Enterococcus
Proguanil
Malaria prophylaxis (atovaquone)
- Oral, prodrug
Doxycycline
Tetracycline
Spectrum + clinical uses:
- Community-acquired pneumonia, gonorrhea, chlamydia, Lyme disease
- Rickettsia, H. pylori, spirochetes
Tigecycline
Glycylcycline
Spectrum + clinical uses:
- Only glycylcycline
- Broader spectrum than tetracycline à works against tetracycline-resistant species
- MRSA + VRSA as well
- Clinical use: skin + intrabdominal infections
Gentamicin& tonramycin&netilmicin&amikacin
Aminoglycosides
Spectrum + clinical uses:
- Aerobic gram (-) bacteria (E. coli, Enterobacter, Proteus, Pseudomonas)àUTIs
- Used in combination with cell wall synthesis inhibitors (penicillins, cephalosporins)
Streptomycin
Aminoglycosides
Spectrum + clinical uses:
- In combination with penicillin against TB, tularemia, enterococcal endocarditis
Kanamycin& neomycin
Aminoglycosides
Spectrum + clinical uses:
- Used to suppress intestinal flora before bowel surgery
- Neomycinàtopical use
Norfloxacin
Fluroquinolone 1st generation
Spectrum + clinical uses:
- Gram (-) aerobe bacteria (Proteus, E.coli, Klebsiella, H. influenzae, campylobacter)
- Use: UTIs + prostatitis
Ciprofloxacin &ofloxacin
Floroquinolones
2nd generation
Spectrum + clinical uses:
- Gram (-) aerobe bacteria (including Pseudomonas)
- Also some gram (+) bacteria (B. anthracis à ciprofloxacin), atypical agents
(Chlamydophila, mycoplasma)
Levofloxacin
3d generation floroquinolones
Spectrum + clinical uses:
- Less active against gram (-) organisms, but more against gram (+) bacteria
(Staphylococcus, streptococcus, enterococcus)
- Use: community-acquired pneumonia (typical + atypical agents)
Moxifloxacin
4th generation floroquiolones
Spectrum + clinical uses:
- Similar to 3rd generation + extended anaerobic coverage (broad spectrum)
- Use: respiratory tract infections
Roxithromicin
Macrolides
Spectrum + clinical uses:
- Broad spectrum
- Gram (+) and (-) cocci AND Chlamydia, mycoplasma, legionella, campylobacter
- Use: respiratory infections (atypical bacteria), chlamydial infections, penicillin
allergy, Bordetella pertussis
Clarithromycin
Macrolides ( very important)
Spectrum + clinical uses:
- Similar to erythromycin, but more active against Mycobacterium, Toxoplasma Gondii, H. influenzae
- Use: respiratory infections, gastric/duodenal ulcers, urogenital infections
Azithromycin
Macrolides
Spectrum + clinical uses:
- Similar to erythromycin (~roxithromycin)
- More selective to Neisseria, H. influenza
- Acquired pneumonia, urogenital infections caused by chlamydia
Clindamycin
Lincosamide antibiotics
Mechanism of action:
- Bind to the 50S ribosomal subunitàinhibit translocation of tRNA from acceptor to
donor siteàinhibit protein synthesis (MOA similar to erythromycin) Spectrum + clinical uses:
- Gram (+) cocci and anaerobic organisms
Quinupristin/dalfopristin
Streptogramins
Mechanism of action:
- Bind to the 50S ribosomal subunitàblock exit channel on the ribosome
- Bactericidal effect together, bacteriostatic effect separately
Spectrum + clinical uses:
- Gram (+) cocci, MRSA; VRSA
Linezolid
Oxazolidinones
Mechanism of action:
- Binds to the 50S ribosomal subunitàinhibits formation of initiation complex
Spectrum + clinical uses:
- Effective against gram (+) resistant organisms (MRSA, VRE, Penicillin-resistant Str.)
- Use: Vancomycin resistant E. faecium + staphylococcus
Vancomycin & teicoplanin & oritavancin
Glycopeptides
Spectrum + clinical uses:
- Gram (+): S. aureus, MRSA, Clostridium difficile
- Enterococci, pneumococci, endocarditis, meningitis Toxicity and adverse effects:
- VRSAàvancomycin resistant S. aureus
- Nephrotoxicity, ototoxicity, red man syndrome (rapid IV adm. causes flushing)
Fluidic acid
Fusidan ( protein synthesis inhibitors)
Spectrum + clinical uses:
- Protein synthesis inhibitor à inhibits elongation factor
- Gram (+) à STAPHYLOCOCCI! (no action against gram-)
Daptomycin
Lipopeptides ( membrane - active agent )
Spectrum + clinical uses:
- Binds to cytoplasmic membrane à disruption of ionic gradients + membrane
depolarizationàbactericidal effect
- Gram (+) bacteria à MRSA, VRSA
Bacitracin
Polypeptides ( cell wall synthesis inhibitor )
Spectrum + clinical uses:
- Cell wall synthesis inhibitor à interferes with dephosphorylation of the lipid carrier
transferring peptidoglycan subunits across the membrane
- Gram (+) bacteria (strepto, staphylo, clostridium, diphtheria)
Mupirocin
Miscellaneous antibiotic
Spectrum + clinical uses:
- Protein synthesis inhibitoràinhibits isoleucyl-tRNA synthetase
- Gram (+) bacteriaàMRSA (impetigo)
- Topical administration
- Local itching, burning, rash
Metronidazole
Unknown mechanism of action antibiotic
Mechanism of action:
- Interferes with nucleic acid synthesisàproduces toxic intermediary metabolites Spectrum + clinical effect:
- Anaerobic gram (-) bacteria
- Protozoans (trichomonas, G. lamblia, amoeba, Gardnerella vaginalis)
- Intra-abdominal infections + brain abscesses
Fidaxomicin
Macrocyclic antibiotic
Mechanism of action:
- Inhibits bacterial RNA polymeraseàbactericidal effect
Spectrum + clinical uses:
- Narrow spectrumàgram (+) anaerobesàc. difficile
Rifaximin
Antibiotic for enteric bugs
Mechanism of action:
- Derivative of rifampicinàinhibits DNA-dependent RNA polymerase
Spectrum + clinical uses:
- Gram (+) and (-)
- Management of hepatic encephalopathy (decreases nitrogenous compounds)
Nitrofurantoin
Antibiotic for urinary bladder infection
Mechanism of action:
- Urinary antisepticàrapidly excreted into urine and acts there to suppress
bacteriuria Spectrum + clinical uses:
- Urinary tract pathogens (E.coli, but not proteus or pseudomonas)
- Used in uncomplicated lower UTI
Fosfomycin
Antibiotic MUra inhibitor
Mechanism of action:
- Cell wall synthesis inhibitoràinhibits synthesis of N-acetylglucosamine (precursor of cell wall synthesis)
Spectrum + clinical uses:
- Gram (+) and (-) bacteria
- Used in treatment of lower UTIs in womeni
