Dr. Lees Drugs Flashcards
what do you worry about with SABA and LABAs?
systemic effects w/ overdose or long term use -tachycardia, hyperglycemia, hypokalemia, and hypomagnesemia
-minimized when inhaled
treatment strategies in ASTHMA
acute - albuterol (go to SABA)
chronic - beclamethasone (go to ICS)
increase combo therapy as severity increases -> omalizumab
SABA > low dose ICS > LABA > high dose ICS
management of COPD
Roflumilast (go to) -> PDE4 inhibitor in lungs -> increase cAMP -> bronchodilator
- reduce inflammation & exacerbation of COPD
- improve pulmonary function
ICS used last resort bc have risk of bacterial pneumonia
SABA
- albuterol
- levalbuterol
- rapid action -> treat ACUTE asthma
- systemic symptoms w/ overdose
- muscle tremors
LABA
- salmeterol
- formoterol
- indacaterol
- not for mono therapy or acute asthma attacks
- long acting bronchodilaton (12hr.)
LABA that has hypersensitivity to milk proteins
salmeterol
indacaterol
- longest acting LABA (24hr)
- for COPD long term maintenance (masks inflammation)
theophylline
- narrow therapeutic index
- risk of SEIZURES (neurotoxic), and ARRHYTHMIAS (cardiotoxic)
Ipratropium
- muscarinic receptor antagonist
- AE -> dry mouth, bitter taste
Roflumilast
- PDE4 inhibitor in lungs
- main one for COPD exacerbations
- reduce inflammation like ICS
inhaled corticosteroids
- beclamethasone (go to)
- budesonide
- fluticasone
- prophylaxis/prevent long term asthma
- anti-inflammatory
- worry about ORAL CANDIDIASIS
Fluticasone
- ICS that has VASOCONSTRICTIVE & anti-inflammatory properties
- hypersensitivity to milk proteins (lactose)
Cromolyn
mast cell stabilizer -> prevent release of leukotrienes & histamine
omalizumab
monoclonal Ab against IgE -> inhibit binding to mast cells
-slow onset of action (12-16 weeks) -> longer effect
Montelukast
leukotriene receptor antagonist (cysteine leukotriene-1 receptor)
-prophylaxis of chronic asthma & relieve rhinitis
Zileuton
5-LO inhibitor
- prophylaxis of chronic asthma
- risk of HEPATOTOXICITY
side effects of penicillins & cephalosporins
- Hypersensitivity - urticaria most common
- GI distress (diarrhea)
- Nephritis (interstitial)
- Neurotoxicity (seizures)
- Hematologic toxicities - decreased coagulation & cytopenia
Pencillin G & V
drug of choice for SYPHILIS and ACTINOMYCES
MOA of penicillins & cephalosporins
bind to PBP –> inhibit transpeptidation rxn –> lesions in cell walls
what can cause diarrhea when combined with cluvalonic acid in children?
Amoxicillin
piperacillin & ticarcillin
the 2 antipseudomonal penicillins -> treat Pseudomonas infections
-synergistic nephrotoxicity when piperacilin-tazobactam is used in combo with VANCOMYCIN
adverse effect of ticarcillin
CHF/volume overload (high Na+), thrombocytopenia, hypokalemia
Dicloxacillin, Nafcillin, Oxacillin
drugs of choice for MSSA
- beta lactamase resistance
- Nafcillin AE -> leukopenia, inflammation at injection site
- Oxacillin AE -> high liver enzymes
which 2 cephalosporins treat pseudomonas?
ceftazidime (3rd/4th) and cefepime (4th)
cefepime -> also cross blood brain barrier to treat CNS infections
2nd generation cephalosporin for respiratory infections, occasional UTIs
cefaclor
2nd generation cephalosporin that has a disulfuram rxn when combined w/ ETHANOL
Cefotetan
3rd generation cephalosporins
-WORKHORSE group -> respiratory infections, UTIs, meningitis)
- ceftriaxone
- cefotaxime
- ceftazidime
5th generation cephalosporin w/ MRSA coverage
ceftaroline
carbapenems
- treat pseudomonas along with Monobactams
- ANAEROBES
- reserved for resistant gram neg rod infections
Imipenem-cilastatin
cilastatin prevents imipenem degradation by DEHYDROPEPTIDASE in the renal tubule
-high risk of SEIZURES
what carbapenem has a higher mortality when used for gram neg rod pneumonia
doripenem
monobactam (Aztreonam)
- AEROBIC gram neg rods
- NO cross allergenicity
- AE -> NEUTROPENIA in children
vancomycin
- blocks glycopeptide polymerization
- gold standard for MRSA
- RED MAN SYNDROME, ototoxicity
Daptomycin
- binds to cell membrane -> depolarization & rapid cell death** (lipid tail)
- for MRSA & VRE
-inactivated by SURFACTANT
adverse effects of all tetracyclines & glycylcyclines
- GI disturbance
- deposition in bone/teeth
- liver failure
- phototoxicity
- vertigo
-all avoided during pregnancy
tetracyclines MOA
prevent tRNA binding to ribosome inhibiting protein synthesis
what tetracycline is used for SIADH
demeclocycline
most commonly used tetracycline
doxycycline
what tetracycline has skin pigmentation issues w/ long term use
minocycline
tigecycline
- A glycylcycline
- reversible bind to 30S ribosome & inhibit protein synthesis
-has HIGHER MORTALITY
aminoglycosides MOA
bind to and distort 30S ribosome -> misreading and disrupt protein synthesis
- POST antibiotic effect
- SINGLE large dose (less toxic)
aminoglycoside used for more gram neg resistant rod infections
amikacin
aminoglycoside used for pre op bowel prep or hepatic encephalopathy
neomycin
aminoglycoside that is most active against pseudomonas
tobramycin
macrolide
- bind to the 50S ribosome -> inhibit TRANSLOCATION
- treat respiratory tract infections
- risk of jaundice/hepatic dysfunction, prolonged QT, P450 inhibition
macrolide NOT used with myasthenia gravis
Telithromycin
A macrocyclic that treats C. difficile in adults
Fidaxomicin
-inhibits RNA polymerase & protein synthesis -> cell death (bactericidal)
Clindamycin (lincosamide)
- bind to 50S ribosome -> inhibit TRANSLOCATION
- inhibit bacterial toxin production
- increase risk of C. difficile colitis
Linezolid (Oxazolidinones)
- bind to 23S subunit of 50S ribosome -> inhibit formation of 70S initiation complex
- not used with MAO inhibitors
- SEROTONIN SYNDROME if used w/ SSRIs
what is used for SEVERE infections (meningitis, Rickettsia) and can cause GRAY SYNDROME & OPTIC NEURITIS?
chloramphenicol
-binds to the 50S ribosome -> prevent AAs transfer by inhibiting peptidyl transferase
Quinipristin-dalfopristin (streptogramins)
- can cause arthralgia-myalgia syndrome
- inhibit CYP3A4
cotrimoxazole (TMP + SMX)
- bactericidal
- NOT used in pregnancy, renal damage, G6PD deficiency
- used for UTIs & PJP
- drug of choice for NOCARDIOSIS
Sulfonamides
- inhibit DIHYDROPTERATE SYNTHASE
- HYPERSENSITIVITIES due to sulfur -> PAN, SJS
- compete with WARFARIN/methotrexate for sites on albumin -> excess anticoagulation
Trimethoprim
- inhibit DIHYDROFOLATE REDUCTASE
- risk of folate deficiency in pregnancy and Hyperkalemia
fluoroquinolones
- inhibit TOPOISOMERASE
- topo I (DNA gyrase) -> gram neg org.
- topo IV -> gram + org.
-for respiratory tract, skin/soft tissue infections
- avoided in patients w/ prolonged QT*
- risk of TENDON RUPTURE*
what fluoroquinolone is not used with Tizanidine?
Ciprofloxacin
isoniazid
- inhibits acyl carrier protein reductase & beta-ketoacyl-ACP synthase enzyme -> prevent mycolic acid synthesis
- NOT used with rapid/fast acetylators
the 2 most important TB drugs
rifampin and isoniazid
rifampin
- blocks RNA transcription by interacting w/ beta subunit of mycobacterial DNA-dependent RNA polymerase
- ORANGE sweat, urine, tears
- CYP3A4 INDUCER -> enhance elimination rate of many drugs -> problem w/ HIV & pregnancy
what TB drug is preferred for TB patients with HIV+
Rifabutin
what TB drug can lead to acute GOUT & severe hepatic damage?
Pyrazinamide
-increased uric acid levels
ethambutol
- inhibit arabinosyl transferase involved in protein synthesis of arabinogalactan (cell wall)
- AE -> OPTIC NEURITIS & red/green COLORBLINDNESS
what drug is used in combo with the major 4 if TB is severe?
streptomycin
-for resistant TB
what is the preventative treatment for latent TB?
isoniazid for 9 months
most common leprosy drug
dapsone
- inhibits dihydropterate synthase in folate synthesis path
- hemolysis in G6PD deficient patients, methemoglobinemia, agranulocytosis, peripheral neuropathy
clofazimine
- leprosy drug
- treat LEPROMATOUS LEPROSY and ERYTHEMA NODOSUM LEPROSUM
-AE -> pink to brownish-black discoloration of skin
MOA of azoles - antifungals
inhibit 14-alpha demethylase (cyp51A1) -> block demethylation of lanosterol to ergosterol
-all azoles are TERATOGENIC
what azole is the drug of choice for cryptococus neoformans?
fluconazole
what azole is used to treat DIMORPHIC fungi? (blasto, histo, sporothrix, paracocci)
itraconazole
Ketoconazole
- ONLY topical
- treat TINEA, cutaneous candidiasis, SEBORRHEIC dermatitis
-NOT used on scalp that is broken or inflamed
azole used for vulvovaginal candidiasis
miconazole
-can have vulvovaginal burning/pruritis
Voiconazole
- treat invasive ASPERGILLOSIS
- more CYT450 inhibition than others
- can have visual/auditory HALLUCINATIONS & hepatotoxicity
Amphotericin B & Nystatin MOA
bind to ergosterol -> form pores in membrane -> electrolyte leakage
amphotericin B adverse effects
-low TI (toxic), “bake and shake”, kidney failure, hypotension, anemia
Nystatin
- treats mucocutaneous/vaginal/oropharyngeal CANDIDA
- “swish and swallow”
Flucytosine
- 5-FC enters fungi via PERMEASE transporter -> converted to 5-FU -> inhibit nucleic acid synthesis
- used for CHROMOBLASTOMYCOSIS, meningitis, candida UTIs
- can lead to dose-related BONE MARROW SUPPRESSION
Griseofulvin
- disrupt mitotic spindles -> inhibit fungal mitosis
- treat dermatophytosis of SCLAP/HAIR (tinea capitis)
- NOT used with PORPHYRIA
- induce CYP450 -> decrease warfarin effects
- many effects with ETOH
Terbinafine
- inhibit squalene epoxidase -> build up toxic squalane
- treat ONYCHOMYCOSES
- AE -> HEADACHE
Echinocandins
-inhibit synthesis of B(1,3)-D glucan in cell wall
- slow IV infusion prevents FLUSHING
- treat ASPERGILLUS & CANDIDA
Caspofungin
- 1st line for invasive Candidiasis
- do NOT give w/ cyclosporine
Micafungin
PROPHYLAXIS of invasive Candida
