Pharmacology Flashcards
epinephrine
B > alpha agonist
ephedrine
indirect adrenergic agonist, release stored catecholamines (stimulate B for lung effects)
isoproterenol
B1 and B2 agonist
albuterol
B2 agonist
short acting
terbutaline
B2 agonist
short acting
salmeterol
B2 agonist
long acting
used with steroids
formeterol
B2 agonist
long acting
used with steroids
atropine
M antagonist
Tx: asthma/COPD
ipratropium
M antagonist
poorly absorbed with no significant systemic effects
Tx: COPD
tiotropium
M antagonist
long acting
poorly absorbed with no significant systemic effects
Tx: COPD
Umeclidinium
M3 antagonist
Tx: COPD
theophylline
methylxanthine
aminophylline
methylxanthine
cromolyn sodium
Mast cell stabilizer: inhibits mast cell degranulation
alter chloride channel activity, inhibit eosinophilic inflammatory response, inhibit cough, reduces bronchial hyperactivity
AE: (no systemic toxicity) tracheal irritation (cough, bronchospasm), bad taste
RARE: chest pain, restlessness, hypotension, arrhythmia, N/V, CNS depression, seizure, anorexia
PROPHYLAXIS: asthma/COPD
methylxanthines
related to CAFFEINE
PDE inhibition (decrease cAMP degradation)
adenosine antagonist (strengthens diaphragm, inhibits bronchoconstriction)
decrease release of histamine
AE:
5-10 ug/mL serum: N/V, nervous, headache, insomnia
>20 ug/mL: vomit, HYPOKALEMIA, hyperglycemia, tachycardia, arrhythmia, tremor, neuromuscular irritability, seizures
Tx: asthma/COPD
CI: caffeine, CV
B agonist
bronchodilator: increase cAMP
inhibitory effect on release of mediators from mast cell, inhibit microvascular permeability, stimulate mucociliary clearance
Tx: asthma/COPD
AE: N/V, headache
decrease BP, increase HR and cardiac arrhythmias, HYPOKALEMIA-QT prolongation, PaO2 decrease, CNS toxic effects (agitation, convulsions, coma, respiratory and vasomotor collapse), HYPERGLYCEMIA
M antagonist
reduces bronchoconstriction, decreases mucus, enhances B2 bronchodilation
AE: pupillary dilation, cycloplegia
budesonide
corticosteroid
give with FORMOTEROL
fluticasone
corticosteroid
give with SALMETEROL
mometasone
corticosteroid
beclomethasone
corticosteroid
ciclesonide
corticosteroid
oral inhalation
prodrug of des-ciclesonide
prednisone
corticosteroid
oral
prednisolone
corticosteroid
methyprednisolone
corticosteroid
dexamathasone
corticosteroid
oral or IV
corticosteroids
anti-inflammatory
MoA: decrease inflammatory cytokines (NFkB, HDAC2), reduce mucus secretion, reduces bronchial hyperactivity, enhance B2 agonist effect), reduce GATA into nucleus (suppress TH2 cell activity), inhibits PLA2
inhaled AE: oral candidiasis, hoarse, dry mouth, decrease growth (children), decrease bone density (premenopausal women)
oral AE: glucose intolerence, HTN, weight gain, bone demineralization, cataracts, immunosuppression, retarded growth (children), cushingoid syndrome
AE: HYPERGLYCEMIA
Tx: ASTHMA, wegners granulomatosis
not as much COPD
leukotriene receptor blocker
block LTD4: decrease bronchial reactivity and bronchoconstriction, decrease mucosal hyper secretion and mucosal edema, decrease inflammation
AE: GI
PROPHYLAXIS: asthma/COPD
monteleukast
leukotriene receptor blocker
AE: laryngitis, pharyngitis, nausea, otitis, sinusitis, viral infections
CI: possible suicide ideation
zafirlukast
leukotriene receptor blocker
AE: headache, elevated liver enzymes
zileuton
leukotriene synthesis inhibitor (LTB4, LTC4, LTD4, LTE4): decrease sm. muscle contraction and vessel permeability, reduce leukocyte migration
AE: elevated hepatic enzymes
CI: CYP1A2 (interacts with theophylline)
PROPHYLAXIS: asthma/COPD
omalizumab
anti-IgE Ab (use with steroid)
AE: allergic rxn, injection reaction, sore throat/cold sym.
CI: cardiac complications, avoid concurrent agents
Tx: asthma/COPD
B2 receptor
Gs
stimulate AC - cAMP - PKA - increase EPAC and decrease MLCK
first generation antihistamines
short lived
SEDATION
anticholinergic side effects: DON’T give to asthmatics (thickening/drying of mucosa)
mild effect of GI peristalsis
AE: serotonergic: increase appetite
adrenergic: hypotension, tachycardia
antimuscarinic: dry mouth, urinary retention, tachycardia, constipation, blurred vision
minor not clinically important: QT prolongation, ventricular arrhythmia
other AE: resp. distress, potentiation of nasal congestion
Tx: allergy, nausea, insomnia, allergic rhinitis
CI: MAOI, COPD, asthma, peptic ulcer, BPH
second generation antihistamines
longer action
no sedation or anticholinergic SE
Tx: urticaria, seasonal allergic rhinitis
diphenhydramine
1st gen: H1 antagonist
suppresses cough reflex by acting directly on cough center
Tx: cough, anaphylaxis, parkinsonism (not sure if just this one or all H1 antagonists)
HIGHLY sedating
dimenhydrinate
1st gen: H1 antagonist
Tx: anaphylaxis
HIGHLY sedating
clemastine
1st gen: H1 antagonist
HIGHLY sedating
chlorpheniramine
1st gen: H1 antagonist
brompheniramine
1st gen: H1 antagonist
Tx: urticaria
triprolidine
1st gen: H1 antagonist
promethazine
1st gen: H1 antagonist
AE: IV use gangrene, breathing problems in children
HIGHLY sedating
cyclizine
1st gen: H1 antagonist
meclizine
1st gen: H1 antagonist
hydroxyzine
1st gen: H1 antagonist
Tx: N/V, pruritis
tripelennamine
1st gen: H1 antagonist
loratadine
2nd gen: H1 antagonist
terfenadine
2nd gen: H1 antagonist
ANTIFUNGALS: fatal arrhythmia
astemizole
2nd gen: H1 antagonist ANTIFUNGALS: fatal arrhythmia
acrivastine
2nd gen: H1 antagonist
cetirizine
2nd gen: H1 antagonist
telemastine
2nd gen: H1 antagonist
3rd generation antihistamines
greater binding to H1
early gen drugs modified
non sedating, fewer antimuscarinic effects
Tx: allergic conjunctivitis, saesonal allergic rhinits
desloratadine
2nd gen H1 antagonist
long half life
olopatadine
3rd gen: H1 antagonist
inhibits histamine, PGD2, and tryptase release from mast cell
Tx: OCULAR rhinitis
levocabastine
3rd gen: H1 antagonist
most potent and specific
azelastine
3rd gen: H1 antagonist
inhibits histamine and leukotriene receptors
blocks Ca mobilization and 5-lipoxygenase pathway
inhibits PAF receptor
emedastine
3rd gen: H1 antagonist
asthmatic use
mizolastine
3rd gen: H1 antagonist
anti PAF and LTD4
ebastine
3rd gen: H1 antagonist
anti leukotriene and antibradykinin
indacaterol
long acting bronchodilator
Tx: COPD
vilanterol/fluticasone
B2 agonist: long acting
Tx: COPD
doxopram
ICU only: narrow margin of safety
respiratory stimulant: activates PERIPHERAL carotid receptors
AE: HTN, tachycardia, arrhythmias, seizures
Tx: respiratory depression; acute hypercapnia in COPD
Drugs CI in respiratory disease
sedatives
B blockers
COX inhibitors
ACE inhibitors
ambrisentan
endothelin-1 antagonist
AE: peripheral edema
sildenafil
PDE-5 inhibitor
AE: epistaxis, flush, insomnia, dizziness with sudden hearing loss
CYP2C9
tadalafil
PDE-5 inhibitor
AE: back pain, change in color vision (NAION)
diltiazem
Ca Channel Blocker
AE: bradycardia, HA
nifedipine
Ca Channel Blocker
AE: flushing, heartburn
amlodipine
Ca Channel Blocker
AE: fatigue
bosentan
endothelin-1 antagonist
AE: liver enzymes, anemia, nasopharyngitis
interaction: cyclosporine, glyburide
ivacaftor
improves Cl transport through mutated channels CFTR G551D mutation metab: CYP3A4/5, inhibits CYP3A4, P-gp AE: URTI symptoms, GI, rash Tx: CF EXPENSIVE
lumacaftor
protein conformation stabilizer: improves delivery of more fully functional portent apical surface of cell CFTR G551D mutation induces CYP3A4 AE: URTI symptoms, GI, rash Tx: CF EXPENSIVE with IVACAFTOR
poractant alfa
surfactant
Tx: preterm immature lungs
calfactant
surfactant
Tx: preterm immature lungs
beractant
surfactant
Tx: preterm immature lungs
methotrexate
DHFR inhibitor, inhibits AICAR (adenosine accumulation leading to immunosuppression)
AE: myelosuppression, hepatic, PULMONARY FIBROSIS, derm., TERATOGEN, malignant lymphoma, nephrotoxic
Tx: sarcoidosis, SCLC
rituximab
mAb to CD20
AE: HTN, asthenia, pruritis, urticaria, rhinitis, arthralgia
Tx: wegners granulomatosis
azathioprine
prodrug for 6- mercaptopurine: decrease de novo purine synthesis
activated by HGPRT
AE: myelosuppression
Tx: wegners granulomatosis
CI: ALLOPURINOL or febuxostat (metabolized by xanthine oxidase)
cyclophosphamide
alkylating agent
Tx: wegners granulomatosis, SCLC (off label)
AE: HEMORRHAGIC CYSTITIS (give MESNA), myelosuppression, infertility, malignancies, pulm. fibrosis, renal
epoprostenol
prostanoid portable infusion pump AE: catheter infection Tx: PAH (IMPROVE SURVIVAL) SE: jaw pain, diarrhea, arthralgia pump: infection, thrombosis, pump malfunction
iloprost
prostanoid
AE: cough, tongue/back pain, hemoptysis
teprostinil
prostanoid
AE: jaw pain, vasodilation, N/D, injection reaction
CI: CYP2C8 drugs (gemfibrozil decreases clearance, rifampin increases it)
platinum drugs
intrastrand crosslinks
Tx: SCLC (off label)
AE: allergic rxn
taxanes
binds B-tubulin and prevents depolymerization
Tx: NSCLC
AE: peripheral neruopathy
vinca alkaloids
binds B-tubulin and prevents polymerization
folic acid analogs
DHFR inhibitors
EGFR TKI
oral: CYP interactions
ATP binding site
inhibits phosphorylation of dimerized TK receptors and leads to apoptosis
Tx: lung adenocarcinoma with EGFR phenotype
AE: SEVERE bradyarrhythmia, QT prolongation, STEVEN JOHNSON SYNDROME, GI PERFORATION, hepatic, interstitial lung disease, PE, corneal perforation, corneal keratitis
CI: PREGNANCY, breastfeeding
res: KRAS, BRAF mutation, MET phosphorylation of tyrosine
AE: RASH
chromosome: 19 or 21 mutation
ALK TKI
oral: CYP interactions
ATP binding site
inhibits ALK TK: EML4-ALK fusion gene produces oncogene that activates MEK/ERK pathway and cell proliferation
Tx: lung adenocarcinoma with EML4-ALK phenotype
AE: SEVERE bradyarrhythmia, QT prolongation, STEVEN JOHNSON SYNDROME, GI PERFORATION, hepatic, interstitial lung disease, PE, corneal perforation, corneal keratitis
CI: PREGNANCY
cisplatin
platinum durg
Tx: NSCLC
AE: nephrotoxic, ototoxic
docetaxel
taxane
AE: edema (use steroids), neutropenia
paclitaxel
taxane
AE: myelosuppresion,
gemcitabine
pyrimidine analog: DNA pol inhibitor
Tx: NSCLC
AE: myelosuppresion, PERIPHERAL NEUROPATHY, drowsy/fatigue, arthralgia
pemetrexed
DHFR inhibitor
Tx: NSCLC
AE: hepatic, myelosuppression, GI
vinorelbine
vinca alkaloid
Tx: NSCLC
AE: myelosuppression, neutorpenia
CI: intrathecal injection
irinotecan
DNA topo 1 complex stabilizer
Tx: NSCLC, SCLC (off label)
AE: asthenia
doxorubicin
- intercalator
- free radical generator
- topo II inhibitor
Tx: SCLC
AE: CARDIOTOXICITY, hepatic, other malignancies, EXTRAVASIONAL NECROSIS
etoposide (VP-16)
topo II inhibitor: complex stabilizer
Tx: SCLC
AE: HEMATOLOGIC
topotecan
DNA Topo I complex stabilizer
Tx: SCLC
AE: hyperbilirubinemia
carboplatin
platinum drug
AE: myelosuppression, blood dyscrasia, hepatic
ifosfamide
alkylating agentz: intra and inter
Tx: SCLC
AE: blood dycrasias, neurotoxic, hematuria renal failure
vincristine
vinca alkaloid
Tx: SCLC
AE: peripheral neuropathy
afatinib
EGFR TKI
AE: diarrhea, loss of appetite
erlotinib
EGFR TKI
AE: CV, edema, loss of appetite, elevated hepatic enzymes, ophthalmic toxicity, neurotoxic
getfitinib
EGFR TKI
AE: N/V/D, elevated hepatic enzymes, ophthalmic, neuro, renal
ceritinib
ALK TKI
AE: constipation, NVD, fatigue, loss of appetite, elevated hepatic enzymes, hematologic, hyperglycemia
bevacizumab
VEGF inhibitor (false VEGF receptor)
Tx: non-squamous NSCLC with phenotype
AE: wound healing, life treathening HEMORRHAGE, HAND-FOOT syndrome, endocrine, near, proteinuria, TE FISTULA, PE/DVT, PAH, fatigue
CI: SQUAMOUS lung cancer (cavitation predisposes)
works well with CARBOPLATIN
nivolumab
immune checkpoint inhibitor
PD1 inhibitor:
PD1 down regulates T cell activity during immune response
Tx: NSCLC (adenocarcinoma) after failure of platinum based Tx
AE: rash, HYPERkalemia/HYPOnatremia, constipation, decreased appetite, NV, elevated hepatic enzymes, musculoskeletal pain, cough, resp, infection, fatigue
CI: PREGNANCY
dextromethorphan
acts directly on cough center in medulla
CYP2D6 into active metabolite
AE: hallucinations, dizzy, drowsy, insomnia, irritable/excitable
Tx: cough
CI: MAOI, resp. insuffiency, hepatic, allergy to product
codeine
mu receptor: acts directly on cough center
10% to morphine by CYP2D6
Tx: cough
AE: constipation, sedation, histamine release, orthostatic hypotension, dizzy, resp. distress
CI: hypersensitivity, premature labor, pregnancy, BPH, sedatives, ARDS, asthma, COPD, recent tonsil/adenoid surgery, CONSTIPATION
camphor
topical Tx of cough
do NOT use in nostrils, under nose or by mouth
menthol
topical Tx of cough
do NOT use in nostrils, under nose or by mouth
guaifenesin
expectorant: stimulates bronchial gland secretion: loosens and thins
AE: dizzy, dry mouth, rash, uric acid NEPHROLITHIASIS, stomach pain
CI: hypersensitivity
alpha 1 agonist
increases smooth muscle contraction, mydriasis, increase sphincter contraction
Tx: decongestant
AE: HTN, bradycardia, REBOUND CONGESTION
CI: heart block, hypothyroidism, bradycardia, HTN
pseudoephedrine
alpha 1 agonist and release NE
AE: tachycardia, arrhythmia, CNS (restless, insomnia, anxiety, tremor, etc.),
CI: ventricular tachycardia, elderly, children
metab: MOA, COMT, N-demethylation
oxymetazoline
alpha 1 agonist
phenylephrine
alpha 1 agonist
levamfetamine
inhaled decongestant
benzadrex
inhaled decongestant
iodides-iodinated glycerol
SSKI: saturated solution of potassium iodide
expectorant: increase serous fluid
bromohexine
expectorant: secrolytic
acetyl cysteine
expectorant: mucolytic: free sulfhydryl group opens mucus disulfide bonds
AE: bronchospasm
Tx: Tylenol overdose, chest congestion
CI: asthma (unless used with bronchodilator), antibiotics
dornase alfa
DNase: breaks extracellular DNA molecules of bronchial secretions into smaller fragments
Tx: CF, bronchiectasis, chronic bronchitis
AE: voice alteration, pharyngitis/laryngitis, rash, chest pain, conjunctivitis
AE: hypersensitivity to Chinese Hamster Ovary cells
amiloride
diuretic: blocks Na channel: prevents dehydration of mucus
Tx: CF, bronchial asthma
denufosol tetrasodium
binds P2Y2 receptor: inhibits ENaC transport and activates Cl secretion: enhances mucosal hydration and mucus clearance
Tx: CF
prostanoids
PG’s: vasodilation and reduce inflammation
Tx: PAH
AE: hypotension, muscle pain/cramp, flushing, HA
CI: anti-thrombolytics
endothelin-1 antagonists
blocks pulmonary artery vasoconstriction and smooth muscle cell proliferation AE: TERATOGEN, HA CYP, OATP, PGP substrates Tx: PAH interaction: cyclosporin, glyburide
PDE-5 inhibitors
prevent breakdown of cGMP: vasodilation and reduced cellular proliferation
Tx: PAH
AE: HA, indigestion
CI: organic nitrates, CYP interactions (3A4)
Ca channel blocker
block Ca into smooth muscle: vasodilation
AE: edema, hypotension
CYP 3A4 substrate
must pass vasodilator challenge: decrease PAP without decrease in CO
Tx: PAH
crizotinib
ALK TKI
AE: CV, edema, constipation, NVD, ophthalmic toxicity
bupropion
unclear: NE/DA reuptake inhibitor
smoking cessation: better than nicotine replacement
AE: insomnia, dry mouth, nausea, suicidal ideation
varenicline
nicotinic acetylcholine receptor partial agonist; release of dopamine
smoking cessation: BEST
AE: nausea, depression, suicidal ideation, emotional lability
clonidine
smoking cessation (off label): anti-HTN drug: blocks cravings, anxiety, restlessness, tensioning hunger AE: sedation, dry mouth, dizziness
mecamylamine
smoking cessation (off label): ganglionic blocker (nicotinic receptor antagonist) AE: orthostatic hypotension, fatigue, sedation, constipation, dry mouth, N/V CI: coronary or renal insufficiency, glaucoma, uremia
naltrexone
smoking cessation (off label): opiate receptor antagonist
nicotine replacement therapy
smoking cessation: central nicotinic agonist
nicotine replacement therapy PATCH
12 week step down
AE: applicationsite, HA, flu like symptoms
CI: CVD, DM, hepatic impairment, peptic ulcers, pheochromocytoma, hyperthyroidism, smoking (increase CV risk)
nicotine replacement therapy GUM
12 week course
AE: jaw pain, orodental probs, HA, indigestion, nausea
CI: exceeding 24 pieces in a day can cause ADDICTION
nicotine replacement therapy INHALER
12 week course: prescription needed
AE: irritation in mouth, HA, nausea, heartburn, hiccups
nicotine replacement therapy NASAL SPRAY
12 week course min.
AE: nostril irritation, HA, Nausea, heartburn, hiccups
nicotine replacement therapy ORAL LOZENGE
nicotinic agonist
riocigat
stimulate guanylate cyclase: incrase cGMP
Tx: PAH
macitentan
endothelin-1 antagonist
warfarin
anticoagulant of choice for PAH
may IMPROVE SURVIVAL
Small cell lung cancer tx
Etiposide (iranotecan) and a platinum drug
Squamous cell lung carcinoma Tx
Platinum drug with one of these three (topo drug or a taxol or vinca)
EGFR adenocarcinoma tx
Gefitnib
Erlotinib
Afatinib
ALK adenocarcinoma
Certizinib
After failure try other c-nib
Adenocarcinoma Tx
Platinum drugs and (topo or vinca or taxanes)
Large cell carcinoma Tx
Platinum drug and (topo or vinca or taxane)