drugs theme 1 Flashcards
What is Physostigmine?
Indirect-acting cholinergic drug
reversible
treat glaucoma
What is organophosphates?
Irreversible indirect acting cholinergic stim
very powerful and used in nerve gas
What are the adverse side effects of Cholinergic stimulants?
Most all are Parasympathetic effects except for one * miosis-pupil constriction urination bradycardia bronchoconstriction lacrimation excitation(CNS) like anxiety diarrhea salivation *sweating
Types of anticholinergics?
Anti-muscarinic
atropine-> pupil dilation
Anti nicotinic
ganglion blockers- work on N2 - treat hypertension
neruomuscular junction blockers- work on N1- use in surgery to relax skeleton muscels
Side effects of Anticholinergic drugs?
Resemble sympathetic effects
dry mouth, blurred vision, urinary retention, constipation, tachycardia
describe alpha 1 GCPR signaling
GCPR signaling that activates phospolipase C -> IP3 and DAG
DAG activates PKC
IP3 cause release of Ca+ -> activates Ca2+ dependent protein kinase
describe alpha 2 and Beta adrenergic signaling set up
They are both are GCPR, but they do the opposite effect
Beta activates the adenyl cyclase to make cAMP that leads to biological effects
Alpha 2 inhibits adenyl cyclase from making cAMP
What is Phenylephrine do? and what are its side effects
It’s a alpa 1 selective agonist
it is used to cause vasoconstriction
side effects: HTN(inc BP), headache, and reflex bradycardia bc baroreceptor is responding to the drugs inc to BP
Whats is Clonidine (catapres)? and what are it’s side effects?
alpha 2 selective agonist
treat some types of hypertensions by causing vasodilation
side effects are dissiness, drowsiness, dry mouth
What is isoproterenol ? What does it do? and what is its main problem?
a non selective beta adrenergic agonist
Its used to treat brochospasms and some carido irrhythemias
You have to look out for if patent has a cardiac issue
since effect both B1 & B2 effect both heart and lungs so it can cause flushing, anginea, and other irrhythemias
What is dobutamine ? and what is it used to treat
a B1 selective agonist
its used to treat ppl in shock, or heart failure bc there’s more B1 receptors on heart tissue
What is Albuterol (proventil)? and what is it used for?
a B2 selective agonists
used to treat the pulmonary issues bc theres more b2 receptors on lung tissue
adverse effects: nervousness/restlessness
What is epinephrine and what is it used for?
Its a non selective alpha beta agonist
used to treat anaphylaxis, can also be used to treat asthma
can have broad side effects
Whats prazosin(minipress)? and what are its side effects
a a1 selective antagonist that cause vasodilation
SE are reflex tachycardia, orthostatic hypotension
Whats Propranolol (inderal) ? and its side effects?
Non- selective B antagonists
SE- bronchoconstriction and dec in cardiac function
Whats metoprolol (lopressor) and whats it side effects?
a B1- selective antagonists
used to treat cardiac condition
SE- if have a pulmonary diagnoses it can cause a few pulmonary side effects
What is Pilocarpine (pilopine)?
Cholinergic agonist -> works on ACh
Used topically to treat glaucoma
it is specific for M receptor, so more parasympathetic effects
Types of bronchodilators
B2-adrenergic agonist
Anticholinergics (via muscarinic antagonist)
Theophylline
What does Muscarinic activity do in the lungs?
cause smooth muscle contraction and is stimulated by ACh
What does B2 adrenergic activity do in the lungs?
works on smooth muscles
reverse bronchoncstriction and is stimulated by NE
SABA and what do they do?
short acting beta2 agonist
cause broncodilation by: inc intracellular cAMP, dec intercellular Ca2+, inhib myosing light chain kinase activation, and stim K+ channels to hyperpolarize. all in an effort to reduce smm contraction
Name the SABAs used?
Salbutamol (albuterol)
Levalbuterol
Terbutaline
Metaproterenol
Difference between LABA and SABA and name a LABA?
LABA last in the body longer because they are highly lipid soluble, so they can get trapped in the plasma membrane. They have a slower kinetics but last longer-> so used for managment not rescue
Formoterol is a LABA
Side Effects of LABA and SABA?
Muscle tremor- activation of B2 on skm, especially old ppl
Tachycardia- indirect due to vasodilation-> bp drop-> in HR to comp
Inc free fatty acid, insulin, and glucose
Hypokalemia- due of stim K+ channels to bring into cell
Paradoxical bronchospasms
Whats Atropine?
a Muscarinic antagonist
used to treat asthma, but it is systemic toxin and binds through out the body
What is ipratropium?
Muscarinic antagonist
a modified version of atropine. Has a stable charged nitrogen making it difficult to be easily absorbed -> giving us just local effects
What is Tiotropium
a long acting Muscarinic antagonist
how do muscarinics antagonist work? what are they used for? what are the side effects
They work in the same fashion as B2 agonist
They are used when people can’t use B2 agonist, or in a synergist way with B2 agonist (dec the side effects)
few side effects: minor rebound effect, & glaucoma in old ppl
Whats Theophylline? MOA ? Administered? side effects
It is a Methylxanthines
To treat only asthma by dec bronchial tone
It inhibits PDE , and inhibits adenosine
taken orally
side effects:
tachycardia, irriability and restlessness, seizures, diarrhea, nausea, vomiting , tremor, diuresis
Whats Roflumilast? MOA? ADME? side effects
It is a Methylxanthines To treat COPD It inhibits PDE4 taken orally side effects: tachycardia, irriability and restlessness, seizures, diarrhea, nausea, vomiting , tremor, diuresis
Whats Budesonide? MOA? ADME? side effects?
Inhaled cortical steroid
To mimic the effect of endogenous hormone of cortisol to promote the synthesis of lipocortins inhibits the synthesis of leukotrienes and prostaglandins whech are bonchoconstrictors
high potency, easily abosrbed in the lung, high first-pass metabolism to take care of the amount of drug that is actually swallowed
Side effects: dysphonia (horse), oropharyngeal candidasis (Thrush)
Cough
Whats fluticasone ? MOA? ADME? side effects?
Inhaled cortical steroid
To mimic the effect of endogenous hormone of cortisol to promote the synthesis of lipocortins inhibits the synthesis of leukotrienes and prostaglandins whech are bonchoconstrictors
high potency, easily abosrbed in the lung, high first-pass metabolism to take care of the amount of drug that is actually swallowed
Side effects: dysphonia (horse), oropharyngeal candidasis (Thrush)
Cough
Whats Beclomethasone dipropionate and ciclesonid? MOA? ADME? side effects
Inhaled cortical steroid
prodrugs cleaved by esterase in the lung to the active form
To mimic the effect of endogenous hormone of cortisol to promote the synthesis of lipocortins inhibits the synthesis of leukotrienes and prostaglandins whech are bonchoconstrictors
high potency, easily abosrbed in the lung, high first-pass metabolism to take care of the amount of drug that is actually swallowed
Side effects: dysphonia (horse), oropharyngeal candidasis (Thrush)
Cough
Whats Hydrocortisone & prednisone? MOA? ADME? side effects?
systemic administerd(IV or oral) cortical steroid, only used when ICS and bronchodilators can’t control the asthma
To mimic the effect of endogenous hormone of cortisol to promote the synthesis of lipocortins inhibits the synthesis of leukotrienes and prostaglandins whech are bonchoconstrictors
high potency, easily abosrbed in the lung, high first-pass metabolism to take care of the amount of drug that is actually swallowed
Side effects: dysphonia (horse), oropharyngeal candidasis (Thrush)
Cough
What effect does leukotrienes have on the lungs? how do they cause the effect?
they are bronchoconstrictors
contribute to the airway hyperresponsiveness, plasma exudation, mucus secretion, eosinophil recruitment
What is Zileuton? MOA? ADME? side effects
Its a leukotriene Antagonists
its an iron chelator that interferes with the activity 5-lipoxygenase enzyme
short half life so has to be taken 4 times a day
side effects: some liver toxicity
Whats Montelukast and Zafirlukats? MOA? ADME? side effects?
Leukotriene antagonists
they are leukotriene receptor (CysTL1) inhibitors
are an effective treatment for aspirin-induced asthma
taken 1-2 times a day orally
Explain aspirin induce asthma? and a possible treatment for it?
When at arachidonic acid aspirin and other NSAIDs inhib the COX pathway so more of the arachidonic acid goes on to make lukotirenes which will cause bronchoconstriction. Leukotriene inhibitors like Montelukast and Zafirlukast, can be a possible treatment even though thats not what they are prescribed for
Whats Cromolyn Sodium? MOA? ADME? side effects?
A release inhibitor working on mast cells, preventing them from releasing granulose.
The work on cl- channels and FceR
It is taken as a prevention it does not reverse bronchospasms… works well for antigen and exercise induced asthma
needs to be taken 2-4 times a day in an inhaled aerosols
side effects : dry mouth, cough, throat irritation
Whats Omalizumab? MOA? ADME? side effects
Its an immunomodulator its a monoclonal humanized anti-IgE antibody only use for chronic severe asthma reduces hypersensitivity of airways is injected subcuataneous- slow absorption stays around for 3-4 weeks side effect : injection site rxn inc incidence of infection allergic rxn bc its a a protein
