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Pharm Drugs Midterm Month 1 Weeks 3+4,
Pharm Drugs Midterm Month 1 Weeks 3+4
84
Pharmacology
Graduate
06/22/2018

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Term
short acting beta 2 agonists
Definition
SABA, for acute bronchospasm, rescue inhaler, prevent exercise induced asthma. Albuterol (more potent), Levalbuterol, Pirbuterol. last 3-4 hrs
Term
long acting beta agonists
Definition
Salmeterol (Serevent)(aerosol powder for inhalation), Formoterol (Foradil)(capsule for inhalation or solution through nebulizer), use in combination with inhaled corticosteroids. Black box warning- can inc the rate of asthma related death when used as monotherapy. work in ~2hrs, last ~12 hrs, give 2xday
Term
Combination treatments
Definition
Salmeterol + fluticasone (Advair)
Formoterol + Budesonide (Symbicort)
Formeterol + Mometasone (Asmanex)
Term
inhaled corticosteroid MOA
Definition
direct local inflammatory, reduce hyperresponsiveness, inhibit inflammatory cell migration and activation, most beneficial and effective for long term control of asthma, reduce impairment in lungs and the risk of exacerbation in pts w asthma
Term
inhaled corticosteroid drugs
Definition
beclomethasone (bike in my zone), budesonide (bet on a zone), ciclesonide/desciclesonide (circle solid), flunisolide (fluky solid), fluticasone (flute in zone), mometasone (moment zone), triamcinolone (try my clone)
Term
considerations for inhaled corticosteroids
Definition
can cause systemic side effects, might affect growth velocity in pediatric pts, educate pts to rinse mouth w water after use (prevent fungal infection), takes ~1 week before it starts working
Term
anticholinergic indications
Definition
quick relief of mod-severe asthma in combination w short term beta agonist or as an alternative if pt is intolerant. reduces intrinsic vagal tone of airway
Term
anticholinergic asthma drugs
Definition
ipratropium (Atrovent)- metered dose inhaler or as solution to be administered through nebulization
tiotropium (Spiriva)- inhale contents of capsule
Term
Blurred vision, xerstomia (dry mouth) and tachycardia are side effects of?
Definition
anticholinergics
Term
pathway where leukotriene inhibitors work and leukotriene inhibitor MOA
Definition
pts exposed to allergen -> mast cells and eos release inflammatory markers -> initiates inflammatory cascade -> conversion of arachidonic acid by 5-lipoxygenase enzyme to cysteinyl leukotrienes -> leukotrienes act on cystLT1 receptor -> symptoms of asthma (mucus secretion, bronchoconstriction). Zileuton (Zi-Neuton) inhibits the production of leukotrienes (5-lipoxygenase inhibitor). Drugs that block the action of leukotriene on receptors: Montelukast (Singulair)(Mountain cast), Pranlukast (Prank cast), Zafirlukast (Accolate) (Za fire cast)
Term
leukotriene inhibitor agents indicated when
Definition
moderate to severe persistent asthma, recommended to use in combo w high dose corticosteroid and long term beta agonist. usually considered prior to chronic oral corticosteroids. not usually used as monotherapy
Term
common side effect of Montelukast
Definition
headache
Term
can cause hepatic injury, inc liver enzymes, contraindicated in pts w hepatic impariment
Definition
zafirlukast, zileutin
Term
mast cell stabilizers
Definition
work on inflammatory pathway. Cromolyn (Cromwell). Alternative agent for pts w mild persistent asthma. inferior to inhaled corticosteroids. can be used for exercise-induced bronchospasm. give as metered dose inhaler or nebulizer, can take 2-6 weeks to start working
Term
Methylxanthine MOA
Definition
block PDE enzyme, inc cyclic AMP -> bronchodilation (nonselective phosphodiesterase inhibitor) also anti inflammatory affect -> activation of histone, deacetylase enzyme, decreases the pro-inflammatory gene expression
Term
Methylaxanthine delivery
Definition
give loading dose bc takes time to reach steady state. check blood lvl 30 min after loading dose bc can cause a lot of side effects and toxicity
Term
has side effects of tachycardia, headache, hypertension, nausea, and vomitting and at very high doses can cause hematemesis, hyperglycemia, hyperkalemia, seizures
Definition
methylxanthine (theophylline) (Elixophyllin)
Term
Cimetidine, Macrolides, Quinolones, Systemic Viral Illnesses, Zileutin, and Propanolol affect Methylxanthine clearance how?
Definition
decrease, CYP3A4 inhibitors
Term
Phenytonin, Rifampin, Carbamazepine, Smoking, Phenobarbital, High protein diet affect Methylxanthine clearance how?
Definition
increase, CYP3A4 inducers
Term
Immunomodulator agents
Definition
Omalizumaub (O mail mob) (Xolair)- sub q injection, Mepolizumab (me pale mob) (Nucala- sub q injection), Reslizumab (re sell mob)
Term
Omalizumab MOA
Definition
Monoclonal IgG antibody that inhibits the IgE receptor binding on mast cells and basophils
Term
Omalizumab indication
Definition
long-term use decreases asthma exacerbations and corticosteroid use, alt agent for pts w sensitivity to allergens and severe persistent asthma. but doesn't have any effect on baseline of FEV1 ratio
Term
has SE of anaphylactic reactions and injection-site reactions
Definition
Omalizumab, Mepolizumab, Reslizumab (Immunomodulators)
Term
Mepolizumab MOA
Definition
IgG monoclonal Ab that works by inhibiting the binding of interleukins to eosinophil cell surfaces
Term
Reslizumab MOA
Definition
interleukin-5 receptor antagonist
Term
Mesilzumab indication
Definition
add-on for maintenance treatment of severe asthma w an eosinophilic phenotype
Term
metered-dose inhaler, pt education
Definition
inhaler w canister surrounded by plastic holder and mouthpiece, medication mixed w propellant. tell pt to shake before use, exhale before inhaling medication, seal mouthpiece w lips, breathe in slowly, hold for 10 sec then breathe out
Term
dry-powder inhaler pt education
Definition
hold discus in palm, push thumb grip until clicks into place, slide lever away, seal mouth around mouthpiece, breathe deeply and rapidly, hold breath 10 sec, close mouthpiece
Term
Twisthaler pt education
Definition
used for administering dry-powder medications, twist and lift off cap to load dose, exhale, then twist twisthaler horizontally and breathe in rapidly and deeply then hold breath 10 sec, then close cap
Term
pregnancy and asthma
Definition
usually have worsening of symptoms, preferred to use albuterol as a rescue agent and bedesonide as a maintenance agent. avoid long-acting beta-agonists, avoid omalizumab and zileuton
Term
glucocorticoids and asthma vs COPD
Definition
inhibit inflammation in asthma, variable effect in COPD
Term
Short acting beta-2 agonists for COPD
Definition
albuterol, levalbuterol
Term
Long acting beta-2 agonists for COPD
Definition
arformoterol, formoterol, indacaterol (lasts 24 hrs), oldaterol, salmeterol, vilanterol
Term
Anticholinergic agents for COPD
Definition
short term- ipratropium
long-term- aclininium, tiotropium, umeclidinium
Term
inhaled corticosteroids for COPD
Definition
beclomethasone (bike in my zone), Budesonide (bet on a zone), Ciclesonide (circle solid), Fluticasone (flute in zone), Mometasone (moment zone)
Term
PDE4-Inhibitor for COPD
Definition
Roflumilast (reduces inflammation and breakdown of cyclic AMP), adjunctive therapy for severe COPD pts or pts w prior history of hospitalization for acute exacerbation
Term
has the side effects of sinus tachycardia and hypokalemia
Definition
beta agonists
Term
has the side effects of hoarseness of voice, skin bruising, oral candidiasis, pneumonia
Definition
inhaled corticosteroids
Term
has side effects of diarrhea, nausea, weight loss, insomnia, anxiety, depression, suicidal ideation
Definition
Rofumilast
Term
contraindicated in pts w moderate or severe hepatic impairment
Definition
Rofumilast
Term
antibiotic if COPD pt has infection
Definition
azithromycin or erythromycin
Term
has side effects of nasal dryness, blood-tinged mucus, epistaxis
Definition
intranasal ipratropium bromide
Term
2 antitussive agents
Definition
dextromethorphan (Delsym)-dec's sensitivity of the cough receptors and depresses the medullary cough centers in the brain
codeine- only works on CNS cough centers in the brain
Term
can cause the side effects at high dose of confusion, excitement, irritability, nervousness, serotonin syndrome w monoamine oxidase inhibitors
Definition
dextromethorphan
Term
cases side effects at high dose of altered mental status, visual disturbances, respiratory depression, constipation
Definition
codeine
Term
has black box warning that it can cause respiratory depression and death in some children who receive it following tonsillectomy or adenoidectomy
Definition
Codeine, if child is an ultra-rapid metabolizer (produce morphine when metabolized by CYP enzyme). not recommended to give codeine to children
Term
expectorant agent and how it works
Definition
guaifenesin- increases the effective hydration of the respiratory tract. reduces the mucus viscosity making it easier for pt to cough out. can be found in combo w codeine, dextromethorphan, phenylephrine, pseudoephedrine
Term
decongestant agents and how they work
Definition
pseudoephedrine (Sudafed)(weak stimulant to CNS), phenylephrine (Sudafed PE) (not as strong, less reaches systemic circulation), work by directly stimulating the alpha adrenergic receptors of the respiratory mucosa leading to vasoconstriction and dec blood flow to mucosa layer which helps in relieving congestion and directly stimulate beta adrenergic receptors causing bronchial dilation (only pseudoephedrine does this). both work on alpha-1 receptors but only pseudoephedrine also works on beta-2 receptors
Term
how intranasal itrapropium bromide works
Definition
relieve rhinorrhea and sneezing, reduces volume of nasal discharge but doesn't affect nasal congestion
Term
causes side effects of hypertension and bradycardia
Definition
pseudoephedrine and phenylephrine
Term
inhaled or intranasal glucocorticod agents and how they work
Definition
beneficial for allergic rhinitis but not helpful for cough or cold. beclomethasone and fluticasone.
Term
what is allergic rhinitis
Definition
allergies, most common chronic disease in pediatrics, inflammatory process that is IgE mediated and usually presents with symptoms such as nasal congestion, rhinorrhea, sneezing, nasal itching, lacrimation. can be seasonal, perennial (year-round), intermittent, persistent , or episodic
Term
allergic rhinitis vs asthma
Definition
allergic rhinitis affects upper respiratory tract, asthma affects lower respiratory tract, can have both together
Term
main therapy for allergic rhinitis
Definition
oral antihistamines, usually indicated for sneezing and itching. 1st gen- more sedating and more anticholinergic SEs (diphenhydramine/Benadryl), 2nd gen- less sedating (loratadine/Claritin, desloratadine/Clarinex, fexofenadine/Allegra (least sedating), Cetrizene (Zyrtec), Levocetirizene (xyzal)
Term
Intranasal antihistamines good for, agents
Definition
for allergic rhinitis, faster onset, high efficacy for nasal congestion but more expensive than oral antihistamines. olopatadine, azelastine, azelastine + fluticasone, indicated when symptoms affect quality of life
Term
SE of bitter taste, epistaxis, headache
Definition
intranasal antihistamines, olopatadine, azelastine, azelastine + fluticasone
Term
intranasal corticosteroids used for, agents
Definition
allergic rhinitis. triamcinolone, budesonide, flunisolide, fluticasone, mometasone, ciclesonide
Term
cause side effects of pharyngitis, epistaxis, cough, can affect taste, cause nasal burning or headache
Definition
intranasal corticosteroids, triamcinolone, budesonide, flunisolide, fluticasone, mometasone, ciclesonide
Term
intranasal decongestant, agent, MOA
Definition
oxymetazoline (Afrin), for allergic rhinitis, alpha adrenergic agonist -> nasal arteriolar vasoconstriction, most effective when given in combo w intranasal corticosteroids, do not use >3 days (rebound congestion)
Term
Treatment for increased lacrimation in allergic rhinitis, pt counselling
Definition
naphazoline (Clear Eyes)- vasoconstrictor, antihistamine eye drops- Zaditor, NSAID eye drops- Acular, corticosteroid eye drops- Alrex. All OTC. instruct pt to remove contact lenses before using
Term
causes SEs of ophthalmic irritation, mydiasis, photophobia
Definition
ophthalmic agents- naphazoline (Clear Eyes)- vasoconstrictor, antihistamine eye drops- Zaditor, NSAID eye drops- Acular, corticosteroid eye drops- Alrex
Term
[image]
Definition
cholinomimetic drugs
Term
directing acting cholinoreceptor-activating drugs table
Definition
[image]
acetylcholine is highly susceptible to breakdown and is non-selective, binds to both muscarinic and nicotinic receptors equally, DOA a few sec so not a practical drug to give. methyl choline a lot less susceptible to cholinesterase DOA prolonged, more muscarinic selective
Term
choline ester drugs
Definition
cholinoreceptor-activating, methacholine (met a cool lad and dined), carbachol (carbs and alcohol), bethanechol (bet you won't call), succinylcholine. poorly absorbed in GI tract and CNS (have NH4 component making them charged)
Term
alkaloid drugs
Definition
cholinoreceptor-activating, pilocarpine (pill car pine), lobeline (lobe line) (have NH3, not charged, will absorb in GI tract and CNS)
Term
mnemonic to remember what happens when you give someone cholinoceptor-activating drugs
Definition
DUMBBELS- defecation, urination (relaxation of sphincters), Miosis (narrow pupils), bronchospasm, bronchorrea (bronchial smooth muscle contraction, harder to breathe), Bradycardia (lowering heart rate), emesis (vomiting), lacrimation, salivation, secretory (tears and sweats)
Term
activating nicotinic receptors
Definition
if activate M subtype N(M)- can either get a disorganized fasciculation of each skeletal muscle motor unit, or have a strong contraction of the entire muscle

if activate N subtype receptor N(N)- nerve, either get excitatory postsynaptic potential activation or inhibitory postsynaptic potential, very unpredictable
Term
Excitatory postsynaptic potentials (EPSPs)
Definition
N(N) and M(1)
Term
Inhibitory postsynaptic potentials (IPSPs)
Definition
M(2)
Term
cholinesterase-inhibiting drugs
Definition
inhibit acetylcholinesterase, prolong effects of endogenous acetylcholine, 3 classes:
-simple alcohol w NH4 (charged)- edrophonium (ed phone him)
-carbamates- not charged: physostigmine (fight or stick me), carbaryl (carry a barrel), charged: neostigmine (new stick me), pyridostigmine (pie rid or stick me)
-organoposphates- echothiophate (echo my fate)(charged), malathion (marathon)(not charged), sarin (sawr him)(not charged)

-highly liposoluble (rapid CNS penetration) except for echothiphate, not charged except for carbaryl
-used for insecticide and biochemical warfare

-organophosphate binds the strongest, then carbamates and edrophonium
Term
cholinesterase inhibitor with longest duration of action
Definition
echothiophate (echo my fate) - 100 hrs, strongest binding
Term
cholinesterase inhibitor with shortest duration of action
Definition
edrophonium (ed phone him) - 5-15 min), bound less strongly
Term
how to reverse carbamate effect
Definition
give 1 atropine
Term
how to reverse organophosphate effect
Definition
high-dose prolonged atropine, maybe pralidomine/2-PAM (given to EMT responders in the case of a terrorist attack)
Term
cholinesterase-inhibitor drugs affects
Definition
muscarinic effects same as cholinoreceptor-activating drugs, DUMBBELLS. nicotinic effects of cholinesterase-inhibitor drugs causes prolonged effects of acetylcholine: inc muscle tone, while cholinoreceptor-activating drugs cause dec muscle tone and flaccid paralysis due to rapid depolarization causing muscle twitching then leading to flaccid muscle
Term
acetylcholinesterase-inhibiting drugs cause
Definition
inc skeletal muscle tone
Term
Myasthenia gravis treatment and what is it (common usage)
Definition
(skeletal muscle weakness bc not enough acetylcholine receptors in body) cholinesterase-inhibiting drugs (neostigmine-new stick me and pyridostigmine-pie or stick me (Edrophonium has too short a DOA)(Pysostigmine [not charged, penetrates CNS, not best choice]). acetylcholine-activating drugs wont' work here bc don't have enough functioning cholinergic receptor- Nm)
Term
inducing neuromuscular paralysis drug (common usage)
Definition
cholinoreceptor-activating drug: succinylcholine- make skeletal muscle vibrate, send mult action potentials to it then goes flaccid. when pt needs to be intubated
Term
Alzheimer's disease treatment (common usage)
Definition
cholinesterase-inhibiting drugs- donepezil (don a present) and galantamine (galantly mine)
Term
uncommon drug usage treatment for reflux esophagitis and agent we use now
Definition
uncommon- cholinoreceptor-activating drug: inc tone of lower esophageal sphincter and prevent acid from spilling in from the stomach to the esophagus

today- PPIs
Term
uncommon drug usage treatment for glaucoma and agent we use now
Definition
cholinesterase-inhibiting drugs or cholinoreceptor-activating drug- improves disease by increasing intraocular pressure causing lacrimation

today- topical beta blockers and prostate gland and derivatives
Term
uncommon agent for supraventricular tachyarrythmia
Definition
cholinesterase-inhibitor drugs: inc adrenergic, dec acetylcholine activity

agents today: beta blocker and calcium channel blocker
Term
urinary retention uncommon usage drug
Definition
cholinesterase drugs caused sphincter to relax. now use tamulosin
Term
uncommon indication for antimuscarinic drug intoxication
Definition
drug enhances acetylcholine effects, replaced by benzodiazepines
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