Respiratory Drugs Flashcards
Physiological Bronchial Tone Regulation
Acetylcholine - Muscarinic R (para)’ Stimulation causes CONSTRICTION
Epinephrine - B2 R (symp); Stimulation causes DILATION
Histamine/Leukotrienes - H-1 & LTD4/LTE4 R; Stimulation causes CONSTRICTION
Prostaglandins - PGE2 cuases DILATION; PGF2a causes CONSTRICTION
Short-acting Beta-2-selective agonist (SABAs)
-Albuterol (ok pregnancy)
-Levalbuterol/Pirbuterol
Given by inhalation for acute bronchospasm
Minimal cardiac effects
Bronchodilator
Long-acting beta-2-selective agonist (LABA)
-Salmeterol (ok pregnancy)
-Nocturnal asthma, exercise-induced bronchospasm if many hours of activity
-Inhibits late-phase allergen bronchoconstri
-Not suitable for monotherapy
Bronchodilator
Cholinergic Antagonists
-Ipratropium/ Tiotropium: Muscarinic antagonist
-Best for COPD
Synergistic with B2 blockers (Duoneb)
Adverse: Nasal/mouth dryness, Urine retention especially Males w/ BOH or Prostate CA
Bronchodilator
Theophylline
-Methylxanthine class (caffeine)
-Phosphodiesterase inhibitor - Increase cAMP, a dilator
-2ndary actions: Inhibits mucus secretion, Decreases histamine release
Adverse: CNS&Cardiac stimulation; GI irritation; No antidote for OD
Bronchodilator
Glucocorticoids
Multiple Mechanisms: Decr Inflammation
Outpatient: CAP
No abx in past 3 months
Macrolide
(azithromycin, -thromycin)
- Inhibit bacterial protein synthesis (50s)
Outpatient: CAP
Co-morbidity or abx used in prev 3 mnths
Fluoroquinolone
(levofloxacin, -floxacin)
- Inhibit DNA gyrase and Type IV topoismerase
OR
B-lactam (amoxicillin or ceftriaxone) + macrolide
Inpatient, non-ICU: CAP
Fluoroquinolone (-floxacin)
Ceftriaxone (or amp-sulbactam) + macrolide
Ceph 3; inhibits cell wall synth, extended spectrum pen + B-lactamase inhib, Protein synth inhib
Inpatient, ICU: CAP
Ceftriaxone (or AMP-sublactam)
+
Azithromycin (or fluoroquinolone)
Streptococcus pneumonia
-Levofloxacin
fluoroquinolone
Inhibits DNA gyrase and Type IV topoisomerase
Mycoplasma pneumoniae
-Azithromycin
Macrolide
Inhibits bacterial protein synthesis (50s)
-Doxycycline
Tetracycline
(30s)
-Levofloxacin (+)
Fluoroquinolone
Inhibits DNA gyrase/IV topoisomerase
Haemophilus influenzae
Cefotaxime or Ceftriaxone
3rd gen Cephalosporins
Inhibits cell wall synthesis
Moraxella catarrhalis
Amoxicillin + Calvulanate (Augmentin)
AMOX: extended spectrum pen; inhibits cell wall synthesis
CL: B-Lactamase inhib
Klebsiella pneumoniae
Imipenem
carbapenem, which is a pen-like abx
Broad spectrum and resistant to many B-lactamases
Cilastatin included to prevent renal dehydropeptidase inactivation
Yersinia pestis
Gentamicin
aminoglycoside
inhibits protein synthesis
Bacillus anthracis
Ciprofloxacin
fluoroquinolone
inhibits DNA gyrase and IV topoisomerase
Bordetella pertussis
Azithromycin
Macrolide
inhibits bacerial protein syn
(50s)
Corynebacterium diphtheriae
Erythromycin
macrolide
(50s)
Penicillin also effective
Streptoccosus pyogenes
GAS
-Pen V
B-lactam abx
Narrow-spectrum pen
Inhibits cell wall synthesis
-Amoxicillin (taste)
-Macrolide if pen allergy
CONFIRM GAS before ABX
Pseudomonas aeruginosa
-Piperacillin + Tazobactam
PIP: extended, antipseudomonal pen
TZ: B-lactamase inhib
-Imipenem
carbapenem, pen like abx
broad spectrum and resistant to many B-lactamases
cilastatin for inactivation by renal
-Cefepime
4th gen cephalosporin
inhibits cell wall synth
-Tobramycin
Aminoglycoside
inhibits protein synthesis
Legionella pneumophila
Levofloxacin
fluoroquinolone
inhibits DNA gyrase and IV topoisomerase
Adverse effects:
Penicillin G/V
Amoxicillin
Piperacillin + Tazobactam
Pen: GI, hypersensitivity
Amoxicillin: GI distress, hypdersensitivity
Pip+ Tzbm: GI, yeast infection
Adverse effects:
Cefotaxime/Ceftriaxone
Levofloxacin/Cipro
Doxycycline
Cef: hypersensitivity, yeast inf, cross-sensitivity w/ pen
-floxacin: GI, tendonitis, photo, prolonged QT interval, seizures
Doxy: phototoxicity, discoloration of teeth
Adverse effects:
Azithromycin/erythro
Gentamicin/Tobramy
Imipenem
Azithr: GI distress, Erythro binds receptors for gastric hormone, inducing uncoordinated peristalsis
Gent: nephrotoxic, ototoxic
Imip: hypersensitivity, cross-sensitivity w/ penicillins
1st line drugs for TB
Isoniazid
Ethambutol
Pyrazinamide
Rifampin
resistance: Fluoroquinolone
TB
Newly dx
Latent
Newly dx: isoniazid
Exposed neonates: isoniazid 3 mo
Latent in TST with HIV
Active TB
Isoniazid, rifampin, ethambutol and pyrazinamide
PZA reduces to 6 mo therapy
Isoniazed
Inhibits synthesis of mycolid acid
Activated by mycobacterial catalase peroxide (katG gene)
Isoniazid complex is formed which INHIBITS enoyl reductase
key metabolizing enzyme is acetyltransferase (rate gene determined)
Rifampin
Broad spectrum abx
Binds DNA-dependent RNA polymerase
Results in the inhibition of DNA transcription
selective for bacterial RNA polymerase
Influenza
Oseltamivir
-Neuraminidase inhibitor (give within 48hrs)
Amantadine/Rimantadine
-Blocks M2 proton selective ion channels
prevents acidification of virus and fusion of membranes required for UNCOATING and transfer of viral NA’s
RSV
Palivizumab
-Ab directed at FUSION PROTEIN ON RSV
virus cannot enter cell
Blastomyces dermatidis
Liposomal Amphotericin B
-Polyene abx
Selectively binds ergosterol in fungal membranes
increases membrane permeability
Cryptococcus neoformans
Fluconazole
-inhibits enzyme responsible for converting lanosterol to ergosterol
Amphotericin B
-Polyene abx
Selectively binds ergosterol in fungal membranes
increases membrane permeability
Asperfillus fumigatus
Voriconazole
inhibits enzyme responsible for converting lanosterol to ergosterol
Pneumocystis jirovecii
Trimethoprim + Sulfamethoxazole (TMP-SMX)
Antimetabolites that inhibit folate synthesis in bacteria
Adverse effects: Isoniazid Rifampin Oseltamivir Palivizumab
Isoniazid: liver toxicity, peripheral neuritis (need B6 supplementation)
Rifampin: liver toxicity, reddish-orange body fluids, induces P450
Oseltamivir: rare
Palvizumab: fever, rash
Adverse effects: Fluconazole Vorconazole Amphotericin B TMP-SMX
Fluconazole: many drug interactions (P450)
Vorconazole: many drug interactions (P450); Liver toxicity visual disturbances
Amphotericin B: Nephrotoxic
TMP-SMX: GI distress, Stevens-Johnson syndrome, megaloblastic anemia, photoxicity
