Unit 5 Drugs in Random Order Flashcards
Maraviroc
Tx: HIV
Mech: Blocks binding site on macrophage preventing entry of virus
Fusion inhibitor
SE:
- Hepatotoxicity
- Allergies
- Increase MI
Ethambutol
Antimycobacterial agent
Mech: Inh arabinosyl transferase
Necessary for CW synth
SE:
- Optic neuritis
- Impaired red/green discrimination
- Decreased vision
Cilastatin
Given w/ impenem
Prevents nephrotoxic product by inh. enzyme
Antimycoplasma agents
NO CELL WALL!
So use non CW inhibitors:
Erythromycin
Tetracycline
Vancomycin
Antibacterial
Class: Non B lactam CW inhibitors
Mech: Binds to dialanine residue on CW and prevents cross linking
Use: Severe infection in which B lactams can’t be used
Primary alt. to penicillins for staph infections.
Spectrum: G+
Route: IV–unless target in gut (pseudomembranous colitis)
SE:
- Nephrotoxicity
- Ototoxicity
- If given rapidly via IV→histamine release→Redman or red neck syndrome
- Flushing
- Rash
- Itching
Resistance:
- Target changed
- Dialanine changed to lactic acid
Dr. Van Ron
Dialanine Residue. Vancomycin. Redman. Ototox. Nephrotox
Sofosbuvir
Antiviral agent
Tx: Hepatitis virus (esp Hep C)
Mech: Inh HCV RNA dep RNA pol
Clindamycin
Antibacterial agent–lincosamide
Mech: like erythromycin-inh. translocation
SE: Severe superinf. w/ C. dificile
Targets:
- Severe anaerobic infections (penetrating gut wound)
- Dental prophylaxis in pts w/ heart valve problems
Rifampin
Antimycobacterial agent
Antibacterial agent
Mech: Inh DNA dep. RNA polymerase
-cidal
SE:
- Hepatic toxicity
- Red color in all body fluids
- Induces P450–very strong
- Can metabolize BC!
Rifampin=red
Will metabolize BC (induce P450) so the sperm will LIVEr
SE of cephalosporins
Allergic cross activity w/ penicillin sensitive pts
Possibility of superinfection
Cidofovir
Antiviral agent
Tx: CMV (herpes virus)
CMV→retinitis+ blindness
Mech: Inhibits viral DNA pol
Prodrug-converted by host kinase
Used if resistance has occured so that host cells convert prodrug
SE: Renal damage
-floxacin
Antibacterial agent
Mech:
- Inh topoisomerase II (DNA gyrase)
- Inh topoisomerase IV
No effect on mammalian topoisomerase
SE:
- May damage developing cartilage
- Not for children or pregnant women
- Tendonitis–achilles tendon rupture
- Phototoxicity (drug in skin responds to sunlight)
- May worsen myasthenia gravis
Spectrum: Broad–G+,G-, Acid fast
Metronidazole
Mech: Prodrug-converted to a free radical active molecule by obligate anaerobic bacteria
Route: IV for severe anaerobic bacterial inf.
Use: Protozoal inf:
- Trichoma (STD)
- Giardia (from water)
SE:
- Seizures
- Peripheral neuropathy
Famciclovir
Antiviral agent
Tx: herpes simplex and zoster
Mech: prodrug converted to acyclovir analog
Chloramphenicol
Antibacterial agent
Mech: inh. peptidyl transferase
SE:
- Inh. P450
- Can cause aplastic anemia
- Gray baby syndrome
- Metabolized by a phase II enzyme that is not active in newborns.
- Can’t metabolize it→baby turns blue and circulatory system inhibited
-previr
Boceprevir
Telaprevir
Simeprevir
Antiviral agent
Tx: Hepatitis virus (esp Hep C)
Mech: HCV protease inh.
Virus makes proteins but cannot be processed to final stage
Used in comb. w/ interferon
Gramicidin
Antibacterial agent
Mixture of 3 diff peptide AB
Mech: forms pores in bacterial CM
Route: topical
NEVER give IV–toxic
Spectrum: G+
Foscarnet
Antiviral agent
Tx: CMV (herpes virus)
CMV→retinitis+ blindness
Mech: Inhibits viral DNA pol
Not a prodrug–directly inh. DNA pol
Route: IV 3x/day
SE: Renal damage
Palivizumab
Antiviral agent
Tx: RNA virus (RSV)
Mech: vs antigenic site of RSV–blocks fusion of virus w/ target
Only used prophylactically
Terbinafine
Class: Antifungal
Mech: Inh. squalene epoxidase→inh. ergosterol synth
Inh. ergosterol synth→Increase in sqalene
Route: Systemic
Not well absorbed on skin
Most excreted unchanged
Metabolized and inhibits P450
SE:
- Headache
- Inhibit P450
- Allergies
- Derived from penicillium mold
- Liver damage
- SquaTer*
- inh. Squalene epoxidase TERbinfine*
Carbenicillin
Tx: Antibacterial
Mech: Bind to PBP→inh. transpeptidation
inhibit an enzyme
Broad spectrum
Does not readily enter CNS
SE:
- Allergic rxns→anaphylactic shock
- High IV doses→seizures
- B lactam ring may inh. GABAergic neurons
Telithromycin
Antibacterial
Class: Macrolides-inhibit protein synth** **
Same sites as erythromycin (50s) but induces less resistance b/c not readily transported out of bacterial cell
SE:
- GI upset, nausea, and heartburn
- Increase in GI activity b/c activates motilin
- Inh P450
- Liver damage-_SEVERE liver toxicity_
- Arrythmias
-
Block cholinergic receptor
- Worsen myasthenia gravis
- Inh long ciliary ganglion→Decrease visual accomodation
macROlides like erythROmycin inh. transLOcation
Motility/ Myasthenia gravis worsens
Arrythmia
Cholestatic hepatitis (liver tox)
Restricts P450
Ocular inh.
Bedaquiline
Antimycobacterial agent
Mech: inh. mycobacterial ATP synthetase
Always used w/ 3 other anti-TB drugs
SE:
- Arrythmias
- Increase incidence of death
*You’re in your bed MASTurbating and you go too hard and have an arrythmia *
_Bed_aquiline. Mycobacterial Atp SyntheTase. Arrythmia.
Penicillin G
Tx: Antibacterial
Mech: Bind to PBP→inh. transpeptidation
inhibit an enzyme
Narrow spectrum: G+
Natural penicillin
Route: IV or IM–hydrolyzed w/ stomach acid
Given w/ procaine to slow release
Destroyed by B lactamase
Does not readily enter CNS
SE:
- Allergic rxns→anaphylactic shock
- High IV doses→seizures
- B lactam ring may inh. GABAergic neurons
Ledipasvir
Antiviral agent
Tx: Hepatitis virus (esp Hep C)
Mech: Binds to and inh. protein thats necessary for HCV replication
Tenofovir
Antiviral agent
Tx: Hep B
Mech: Inh. Hep B reverse transcriptase
SE:
- Lactic acidosis
- Hepatomegaly
Discontinuation→Increase hepatitis symptoms
Isoniazid
Antimycobacterial agent
Mech: Produces inh. of multiply mycobacterial enzymes
Inh CW synth
Prodrug
Cidal, but static for dormant cells
Used alone for prophylaxis–in combo for active tx
Metabolized by acetylation–slow acetylators affected
SE:
- Increase excretion of vit B6→pyroxidase deficiency→niacin deficiency
- Pellegra
- Peripheral neuropathy
- Optic neuritis
- Hepatotoxicity
Isoniazid is IHOPPIN
Inh. mycobacterial enz.
- Hepatotox.
- O**ptic neuritis.
*Peripheral neuropathy + Pellegra. *
Prodrug + Prophylaxis
Increase excretion of vit B6→→
Niacin def.
Fluconazole
Antifungal triazole
-static
Mech: Inh fungal P450, including lanosterol-14-alpha-demethylase
So inh. ergosterol synth
SE:
- Least effect on human P450
- Teratogenic
- Liver damage
- Hallucinations
FLUCking may lead to birth defects (teratogenic)
LUCy in the sky with diamonds=LSD=Hallucinations
Methicillin
Tx: Antibacterial
Mech: Bind to PBP→inh. transpeptidation
inhibit an enzyme
B-lactamase resistant
Narrow spectrum: G+
Does not readily enter CNS
Do not use anymore-too toxic
Amikacin
Antibacterial
Class: Aminoglycosides-inhibit protein synth** **
-cidal
Mech: Irr. binds to 30s subunit
Inh. or alter tRNA binding along mRNA including initiation site
Kanamycin
Antibacterial
Class: Aminoglycosides-inhibit protein synth** **
-cidal
Mech: Irr. binds to 30s subunit
Inh. or alter tRNA binding along mRNA including initiation site
Pyrazinamide
Antimycobacterial agent
Mech: Inh FA synth
Prodrug converted in macrophase where TB lives
SE:
- Gout
- Hepatitis
Valganciclovir
Antiviral agent
Tx: CMV (herpes virus)
CMV→retinitis+ blindness
Mech: Inhibits viral DNA pol
Prodrug-converted to ganciclovir by viral kinase
Voriconazole
Antifungal triazole
-static
Mech: Inh fungal P450, including lanosterol-14-alpha-demethylase
So inh. ergosterol synth
SE:
- Less effect on human P450 (triazole vs imidazole)
- Can cause visual disturbances
_V_oriconazole causes _V_isual disturbances
Mezlocillin
Tx: Antibacterial
Mech: Bind to PBP→inh. transpeptidation
inhibit an enzyme
Broad spectrum
Does not readily enter CNS
SE:
- Allergic rxns→anaphylactic shock
- High IV doses→seizures
- B lactam ring may inh. GABAergic neurons
Amoxicillin
Tx: Antibacterial
Mech: Bind to PBP→inh. transpeptidation
inhibit an enzyme
Broad spectrum
Route: Oral
Does not readily enter CNS
SE:
- Allergic rxns→anaphylactic shock
- B lactam ring may inh. GABAergic neurons
Natamycin
Class: Antifungal
Polyene antibiotics
Route: Topical
Mech: Binds to ergosterol in fungal CM→pores→memb. leakage
Only one approved for use in eye
Tobramycin
Antibacterial
Class: Aminoglycosides-inhibit protein synth** **
-cidal
Mech: Irr. binds to 30s subunit
Inh. or alter tRNA binding along mRNA including initiation site
Ampicillin
Tx: Antibacterial
Mech: Bind to PBP→inh. transpeptidation
inhibit an enzyme
Broad spectrum
Does not readily enter CNS
SE:
- Rash in pts who have mononucleosis +other viral inf.
- Allergic rxns→anaphylactic shock
- High IV doses→seizures
- B lactam ring may inh. GABAergic neurons
Aztreonam
Antibacterial
Class: Monobactam
Route: IV or IM
Not affected by lactamases
Spectrum: Aerobic G- organisms
Not cross reactive w/ allergic pts
SE:
- Seizures
Tetracycline
Tx:
- Rickettsia
- Spirochetes (lyme disease)
- Helicobacter
- Legionella
Mech: Reversibly bind to 30s.
Inhibits the binding of tRNA to the A site
-static
SE
- Deposited in Ca storage sites-bones/teeth-esp fetus or child
- Binds to cations, esp Ca, also Fe and Al.
- Preg risk D
- Renal and hepatic toxicity
- Degrades to toxins–don’t use after expiration date
-gravir
Tx: HIV
Mech: Inh. HIV-1 integrase
Inh. insertion of viral genome into human
Prevents propagation
-zolid
Linezolid
Tedizolid
Mech: Inh. binding of fmet (start codon) tRNA to P site
Prevents initiation of protein synth.
SE
- Anemia
- Pseudomembranous colitis
- Will happen w/ any powerful AB b/c of C. dificile
Clarithromycin
Antibacterial
Class: Macrolides-inhibit protein synth** **
Oral stability
vs. Helicobacter Pylori
* macROlides like erythROmycin inh. transLOcation*
Motility
Arrythmia
Cholestatic hepatitis (liver tox)
Restricts P450
Oral stability
Imipenem
Tx: Antibacterial–mixed infections
Class: Carbapenem
Penicillin analog
Small penicillinase resistant B lactam
Spectrum: Very broad-Better against G+
Route: IV
SE:
- Can enter CNS→Seizures
- Metabolized in kidney to nephrotoxic product
- Given w/ cilastatin which inh. enzyme that produces toxic product
Azithromycin
Antibacterial
Class: Macrolides-inhibit protein synth** **
Longer T1/2 (3 days)
macROlides like erythROmycin inh. transLOcation
Motility
Arrythmia
Cholestatic hepatitis (liver tox)
Restricts P450
O——
Nystatin
Class: Antifungal
Polyene antibiotics
Mech: Binds to ergosterol in fungal CM→pores→memb. leakage
Route: Topical
Can give orally, but only for fungi in gut
Too toxic for parenteral use
Mupirocin
Mech: Binds to bacterial isoleucyl tRNA synthetase
Route: Topical
Use: Staph inf.
Piperacillin
Tx: Antibacterial
Mech: Bind to PBP→inh. transpeptidation
inhibit an enzyme
Broad spectrum
Does not readily enter CNS
SE:
- Allergic rxns→anaphylactic shock
- High IV doses→seizures
- B lactam ring may inh. GABAergic neurons
Antifungals for candida+ ringworm
Miconazole
and other “conazoles”
Route: Topical and systemic
Daptomycin
Antibacterial agent–lipopeptide
Mech: Forms pores in bacterial CM
Targets: Aerobic G+ (staph, strep)
Skin and soft tissue inf. or severe blood inf w/ S. aureus
SE:
- Muscle pain and weakness
- careful w/ statins
- Eosinophilic pneumonia
-amivir
Zanamivir
Oseltamivir
Antiviral agent
Tx: Influenza A+B virus (RNA virus)
Virus leaves cell and is attached by tether of neuraminic acid
Release of virus requires neuraminidase
Mech: Neuraminidase inh.
So virus cannot be released from cell and spread
SE:
- Nausea
- Diarrhea
- Psychosis
- Hallucinations
- Zanamivir is a powder that must be inhaled so asthma issues
Only shorten influenza by about a day
Bacitracin
Antibacterial
Class: Non B lactam CW inhibitors
Polypeptide
Mech: Inh. recycling of bactoprenol carrier
Spectrum: G+
Route: Topically–very toxic
SE:
- Nephrotoxicity–if not given topically
Protease inh.
-navir
Antiviral agent
Tx: HIV
Mech: Protease inh.
Prevent formation of active viral proteins from their peptide precursor
Most inh. P450
Some are absorbed poorly via oral route and 18 capsules must be taken/day
Ritonavir is most potent known P450 inh so it is given w/ the poorly absorbed protease inh to avoid taking so many
Ritonavir given w/: SALTD
- Saquinavir
- Atazanavir
- Lopinavir
- Tipranavir
- Darunavir
SE:
- Alter fat distribution
- Loss of fat in face and limbs
- Gain fait in gut, chest, and back
- Increase diabetes
- Some have sulfur groups→allergies
- Tipranavir
- Fosamprenavir
Sulfisoxazole
PABA*→folic acid→DHFA**→THFA
*→=Dihydropterate synthetase
**→DHFR
Mech: Reversible inh. dihydropterate synthetase
For UTIs
SE:
- Allergic whole body rash (Stevens Johnson syndrome)
- Hemolytic anemia in G6PDH deficient pts
- Megaloblastic anemia
Sulfa drugs have sulf or sul
Efavirenz
Antiviral agent
Tx: HIV
Mech: bind to non active sites and Inh reverse trans
Not competetive inh.
1st gen NNRTI
SE
- CNS- so some people crush it up and smoke it
- hallucinations
- memory loss
- Rash
- Smoke EFavirenz to get EFfed up*
- hallucinations and mem loss*
Posaconazole
Antifungal triazole
-static
Mech: Inh fungal P450, including lanosterol-14-alpha-demethylase
So inh. ergosterol synth
SE:
- Less effect on human P450 (triazole vs imidazole)
Posaconazole is sucha pussy, it hardly inhibits our P450
Ganciclovir
Antiviral agent
Tx: CMV (herpes virus)
CMV→retinitis+ blindness
Mech: Inhibits viral DNA pol
Prodrug-activated by viral kinase
SE:
- Neutropenia
- Thrombocytopenia
- Teratogen
Flucytosine
Antifungal agent
Pyrimidine analog
Mech: Inh thymidine synth. in fungi
Converted to 5-fluororacil→inh. thymidilate synthatase
So inh DNA and RNA synth
Prodrug-enters fungus by specific enzymes
Does not enter human
SE:
- Bone marrow depression→anemia
- Liver toxicity
- GI upset
“-oxacillin”s
Tx: Antibacterial
Mech: Bind to PBP→inh. transpeptidation
inhibit an enzyme
B-lactamase resistant
Narrow spectrum: G+
Does not readily enter CNS
SE:
- Allergic rxns→anaphylactic shock
- High IV doses→seizures
- B lactam ring may inh. GABAergic neurons
OXacillin=OX is strong animal, resistant to penicillinase
Rimantadine
Antiviral agent
Tx: RNA virus (Influenza A virus)
Virus taken up by cell endosome→opens channel in endosome→H enters→virus can release genes
Mech: Blocks process by which H channel forms in endosome
Blocks transporter or ion channel
Used proph. or very early
Widespread resistance
SE: Fewer than amantidine but similar SE
- Renal failure
- Teratogen
- CNS fx
- Dizziness
- Slurred speech
- Confusion
- Seizures
- Nausea
Nafcillin
Tx: Antibacterial
Mech: Bind to PBP→inh. transpeptidation
inhibit an enzyme
B-lactamase resistant
Narrow spectrum: G+
Does not readily enter CNS
SE:
- Allergic rxns→anaphylactic shock
- High IV doses→seizures
- B lactam ring may inh. GABAergic neurons
NAFcillin=Not AFfected by penicillinase
-fungin
Caspofungin
Micafungin
Anidulafungin
Antifungal agent
-cidal
Mech: Inh. synth of fungal CW component
Enzyme inhibitor
Route: Slow IV
Not readily absorbed
SE:
- Rash
- Fever
- Fetal Damage
Enfuvirtide
Tx: HIV
Mech: binds to specific site on virus that binds to target
Fusion inhibitor
SE: Insomnia
Retapamulin
Antibacterial agent
Mech: inh. peptidyl transferase
Route: Topical
Use: skin staph or strep inf.
Lamivudine
Antiviral agent
Tx: Hep B
Mech: Inh. Hep B reverse transcriptase
Discontinuation→Increase hepatitis symptoms
Valacyclovir
Antiviral drug
Tx: Herpes simplex and zoster
Mech: Prodrug converted to acyclovir
Must be given orally-prodrug metab. by 1st pass metab.
Streptomycin
Antibacterial
Class: Aminoglycosides-inhibit protein synth** **
-cidal
Mech: Irr. binds to 30s subunit
Inh. or alter tRNA binding along mRNA including initiation site
Spectrum: Aerobic G-
Must be absorbed by active transport
SE:
- Ototoxicity
- Hearing and balance affected
- hearing loss may be permanent
- Nephrotoxic
- Most common cause of drug induced renal failure
- Used very widely
- High doses
- Neuromuscular blockade
- Decrease in ACh+ ACh receptors on mm
- Fetal damage
- Preg cat. D
- Neuromuscular blockade
- Strippers fornicate*
- Strep. FORNICAT*
Fetal damage
Ototox.
Renal tox
Negative (G-)
Irr. bind 30s
Cidal
*ACh block *
tRNA can’t bind to mRNA
- *
Nevirapine
Antiviral agent
Tx: HIV
Mech: bind to non active sites and Inh reverse trans
Not competetive inh.
1st gen NNRTI
SE
- Hepatotoxicity
- Stevens Johnson syndrome
-virine
Etravirine
Rilpivirine
Antiviral agent
Tx: HIV
Mech: bind to non active sites and Inh reverse trans
Not competetive inh.
2nd gen NNRTI
Differ from first gen:
- Higher potency
- Longer T1/2
- Fewer SE
Ribavirin
Antiviral agent
Tx: RNA virus (RSV)
Only for severe lower resp inf.
Mech: Inh RNA dep DNA pol
Phosphorylated in cell.
SE:
- Preg cat X
- Hemolytic anemia
- Decrease pulmonary fxn in infants
- Cardiac arrest
Not used much anymore. Very expensive
Meropenem
Tx: Antibacterial–mixed infections
Class: Carbapenem
Penicillin analog
Small penicillinase resistant B lactam
Spectrum: Very broad-Better against G-
Route: IV
SE:
- Can enter CNS→Seizures
Cycloserine
Antibacterial
Class: Non B lactam CW inhibitors
Mech: Inh. incorporation of alanine into NAM
Enzyme inhibitor
Used against mycobacterium TB
SE:
- CNS
- Sedation
- Tremor
- Psychosis
- Cyclo- gives you psycho-*
- Go to war in NAM, when you come back you have PTSd*
- Psychosis*
- Tremors*
- Sedation*
Erythromycin
Antibacterial
Class: Macrolides-inhibit protein synth
-static
Mech: Reversibly binds to 50s subunit and inh. translocation of mRNA
Inh binding of tRNA to P site
Spectrum: G+
SE:
- GI upset, nausea, and heartburn
- Increase in GI activity b/c activates motilin
- Inh P450
- Liver damage
- Arrythmias
macROlides like erythROmycin inh. transLOcation
Motility
Arrythmia
Cholestatic hepatitis (liver tox)
Restricts P450
O——
-pristin
Quinupristin (A+P site)
Dalfopristin (P site)
Mech: Inh. A and P sites
Always used together–synergistic
SE: Muscle pain
Spectrum: G+
Amphotericin B
Class: Antifungal
- Polyene antibiotic*
- -cidal*
DOC of systemic mycotic inf.
Mech: Binds to ergosterol in fungal CM→pores→memb. leakage
Route: Slow IV (2-4 mnths) or intrathecal
Must be given w/ detergent b/c not soluble in H2O
Topical too
SE: “amphoterrible”
- Impaired renal fxn
- Fever, chills, vomiting, convulsions, severe headache
- Anemia
Amph SE=ANF (sounds similar)
*Anemia, Nephro fxn impaired, Fever *
or
AMPHTERIC
Anemia
Muscular contractions
Pores in membrane
Headache
Temp increase
Emesis
Renal fxn impaired
IV or intrathecal
Chills
Carbapenems
Tx: Antibacterial–mixed infections
Penicillin analog
Small penicillinase resistant B lactam
Spectrum: Very broad
Route: IV
SE:
- Can enter CNS→Seizures
Lincomycin
Antibacterial agent–lincosamide
Mech: like erythromycin-inh. translocation
SE: Severe superinf. w/ C. dificile
Targets:
- Severe anaerobic infections (penetrating gut wound)
- Dental prophylaxis in pts w/ heart valve problems
Clavulanic acid
Mech: Bind to and inh. B lactamase
Non antibiotic B-lactam ring compounds
Antifungals for ringworm
Tolfnaftate
Ciclopirox
Terbinafines and other “fines”
Route: Topical
Telbivudine
Antiviral agent
Tx: Hep B
Mech: Inh. Hep B reverse transcriptase
SE:
- Lactic acidosis
- Hepatomegaly
Discontinuation→Increase hepatitis symptoms
Nitrofurantoin
Mech: Reduced by bacteria to a highly reactive molecule
Concentrates in urine
Use: UTI
SE:
- Cough
- Chest pain
- Brown urine
Entecavir
Antiviral agent
Tx: Hep B
Mech: Inh. Hep B reverse transcriptase
SE:
- Lactic acidosis
- Hepatomegaly
Discontinuation→Increase hepatitis symptoms
Ticarcillin
Tx: Antibacterial
Mech: Bind to PBP→inh. transpeptidation
inhibit an enzyme
Broad spectrum
Does not readily enter CNS
SE:
- Allergic rxns→anaphylactic shock
- High IV doses→seizures
- B lactam ring may inh. GABAergic neurons
Amantadine
Antiviral agent
Tx: RNA virus (Influenza A virus)
Virus taken up by cell endosome→opens channel in endosome→H enters→virus can release genes
Mech: Blocks process by which H channel forms in endosome
Blocks transporter or ion channel
Used proph. or very early
SE:
- Renal failure
- Teratogen
- CNS fx
- Dizziness
- Slurred speech
- Confusion
- Seizures
- Nausea
Gentamycin
Antibacterial
Class: Aminoglycosides-inhibit protein synth** **
-cidal
Mech: Irr. binds to 30s subunit
Inh. or alter tRNA binding along mRNA including initiation site
**Use: **Ointment for eye
Sulbactam
Mech: Bind to and inh. B lactamase
Non antibiotic B-lactam ring compounds
“-vancin”s
Televancin
Dalbavancin
Antibacterial
Class: Non B lactam CW inhibitors
Lipoglycopeptide
Mech: Binds to dialanine residue on CW and prevents cross linking + disrupt bacterial CM
SE:
- Nephrotoxicity
- Fetal damage
- Metallic taste
Fidaxomycin
Antibacterial agent
Mech: Inh. C. dificile RNA pol
Orally–Not systemically absorbed
Target: C. dificile
Adefovir
Antiviral agent
Tx: Hep B
Mech: Inh. Hep B reverse transcriptase
SE: Liver and renal damage
Discontinuation→Increase hepatitis symptoms
Itraconazole
Antifungal triazole
-static
Mech: Inh fungal P450, including lanosterol-14-alpha-demethylase
So inh. ergosterol synth
SE:
- Strongest effect on human P450 of the triazoles
- Worsen CHF or arrythmias
_I_traconazole is the strongest _I_nhibitor of P450
ItrAConazole→Arrythmias or CHF
Delavirdine
Antiviral agent
Tx: HIV
Mech: bind to non active sites and Inh reverse trans
Not competetive inh.
Not as effective
1st gen NNRTI
SE
- Hepatotoxicity
- Stevens Johnson syndrome
- P450 inh.
Neomycin
Antibacterial
Class: Aminoglycosides-inhibit protein synth** **
-cidal
Mech: Irr. binds to 30s subunit
Inh. or alter tRNA binding along mRNA including initiation site
Route: Topical or oral
**SE: **Very nephrotoxic–so only topically or orally
Ketoconazole
Antifungal imidazole
Mech: Inh fungal P450, including lanosterol-14-alpha-demethylase
So inh. ergosterol synth
SE:
- Nausea
- GI upset
- Hepatic toxicity
- Inh. human P450-Strongest inh. of the conazoles
- Decrease in adrenal and gonal steroid synth
- Decrease cortisol (tx of Cushing’s)
- Decrease test. (tx of prostate cancer)
- Ket…ocon..azole*
- Ket azole=cat asshole*
- So GI, nausea, and prostate cancer tx*
- And cat’s have 9 lives so they LIVEr forever…l_iver tox_*
Netilmicin
Antibacterial
Class: Aminoglycosides-inhibit protein synth** **
-cidal
Mech: Irr. binds to 30s subunit
Inh. or alter tRNA binding along mRNA including initiation site
DROPPED in the US
Griseofulvin
Class: Antifungal
Tx: Nail inf.
Nail inf. must be treated systemically to avoid painful tx
Mech: Binds to fungal microtubules→inh. fungal mitosis
Taken up by growing human skin cells and concentrated in keratin
Route: Systemic
Not well absorbed on skin
Most excreted unchanged
SE:
- Headache
- Induction of P450
- Allergies
- Derived from penicillium mold
- Eat greasy fries and you will get fat *
- Eat grise microtubules (fries) and you will get PHAT*
Griseofulvin binds microtubules. P450 induction, Headache, Allergies, t_reats _Toenail inf.
Fosfomycin
Antibacterial
Class: Non B lactam CW inhibitors
Mech: Blocks synth of NAM
Spectrum: Aerobic G-
Use: Uncomplicated UTI
SE:
- Diarrhea–killing bacteria in gut
Penicillin V
Tx: Antibacterial
Mech: Bind to PBP→inh. transpeptidation
inhibit an enzyme
Narrow spectrum: G+
Route: Oral
Natural penicillin
Absorption unpredictable
Destroyed by B lactamase
Does not readily enter CNS
SE:
- Allergic rxns→anaphylactic shock
- B lactam ring may inh. GABAergic neurons
Acyclovir
Antiviral drug
Tx: Herpes simplex and zoster
Mech: Incorporated into DNA and inh. viral DNA pol
Prodrug-must be phosphorylated by viral kinase
Only occurs in active cells
Much higher affinity for viral DNA pol
Route: IV and oral (not well absorbed though)
SE:
- GI upset
- Renal damage
- CNS problems
- Delerium when given IV
Polymixin B
Antibacterial agent
Mech: Binds to negatively charged sites on LPS of G- bact
→to memb. permeability
Route: Topical
SE: (all reversible)
- Nephrotoxic
- Neurotoxic
- Neuromuscular blockade
- Ataxia
- Perioral paresthesia
- Poly mixes in her PANNNN*
- Polymixin B. Perioral paresthesia. Ataxia. Neurotoxic. Nephrotoxic. Neuromuscular blockade. binds to Negatively charged sites on LPS*
Harvoni
DOC for HCV
Ledipasvir+sofosbuvir
Dapsone
Antimycobacterial agent
Related to sulfonamides
Mech: Reversible inh. dihydropterate synthetase
Use: For mycobacterium leprae (leprosy
Recombinant interferon alpha
Antiviral agent
Tx: Hepatitis virus (esp Hep C)
Cytokine w/ multiple mech
Mech:
- Immunostimulant
- Inh. mRNA processing
- Decrese viral synth
SE:
- Fatigue
- Flu-like symptoms
- Depression
- Hypertensino
- Retinopathy
- Myelosuppression→fewer platelets, granulocytes, etc.
Trimethoprim
Antibacterial agent
Mech: Inh. DHFR (like methotrexate)
Specific for bact. enzyme
*Used in conj. w/ sulfamethoxazole *
SE:
- Megaloblastic anemia
- Can be avoided w/ leucovorin
Targets:
- G- bacteria
- UTIs
- Concentrates in acidic prostate and vaginal tissue
