anti- inflammatory drugs Flashcards
Leukotrienne antagonist
Montelukast (singulair)
categorized as a leukotrienne receptor antagonist
does not alter leukotrienne production
binds to a leukotrienne receptors and inhibits effect on bronchial smooth muscle
(called CystLT receptors)
PO- Pill form
once daily, when for routine maintenance.
clinical use for leukotrienne antagonist
part of maintenance therapy for asthma add on therapy after on ICS an alter option during therapy escalation can lower use of B2 agents allow lower steroid levels Also effective for EIA
montelukast negatives
only inhibits one pathway of inflammation
must be use as part of a drug regimen
doesn’t stop leukotrienne production
side effect of montelukast
—– Leukotrienne antagonist——-
headache
neuro-psychiatic
eosinophilia
churg- strauss vasculitis (inflammation of the vessels)
Roflumilast (Daxas)
—- Phosphodiesterase 4 inhibitor ——–
Decreases inflammation by decreasing the ability of inflammatory cells to produce mediators
elevated cAMP inside immune
inhibition or prevents fibrotic changes
inhibition of airway infiltration of WBCs
use on mod to severe COPD
maintenance therapy
Daxas (phisphodiestarase 4 inhinitor) dosing
Once daily
Oral (PO)
Pill form
may take up 4-8 months before effects are seen
Roflumilast side effects
significant incidence of neuro- Psychiatric changes Diarrhea (about 12% of patients ) weight loss (avg 10lbs)
monoclonal antibody drugs
Monoclonal Antibodies are lab created antibodies targeting specific human mediators
A significant area of Pharmacology for the treatment of:
Cancers
Autoimmune disorders (transplant rejection)
Inflammatory conditions (Crohn’s, Asthma)
COVID
Omalizumab (xoliar)
monoclonal antibody for asthma
produced by genetically modified chinese hamster ovary cells
binds to IgE and prevents it from binding to mast cells
Omazumab (xolair) dosing
given by SI
usually every 4 weeks (bur as frequent as 2 weeks)
circulatinf IgE starts to decrease within 1 hr after administration
cause 96% of IgE decrease
Omaxumab (xolair ) usage
use for the management of chronic asthma
After ICS, LABA and alternate therapies are inadequate
use less ICS
have less exacerbations
Omalizumab side effects
pain, redness around injection site
very infrequent incidence of anaphylaxis
Methylxanthines
older class of drug
found in coffer, tea and cocoa
added on later for the Tx of COPD and asthma
What are the two drugs in methulxanthines ?
– theophylline—
Used in COPD pts
Caffeine
— used in preterm infants with :apnea of prematurity ___
Theophylline
minimal bronchodilating properties
improves diaphragm strength from increase muscle contractility
mild cardiac improvement
CNS stimulation increase ventilatory drive
Mils diuresis
dosing of theophylline
PO
sustaines release tablet, serum
metabolized by the liver at different rates person to person
may use loading dose to reach serum level then adjust based on lab work
theophyllines (negs)
changes from person to person
high serum variation with hepatic or renal dysfunction
wide range of drug interaction with a wide array of drugs
theophylline side effects
CNS- headaches, anxiety, insomnia, seizures
CVS– dysrhythmias, palpitations
GI– nausea, vomiting, anorexia, diarrhea, GER
Caffeine (methylxanthines )
used in neonates to streghtne drive to breath
apnea of prematurity
diffuses easier into CSF than theophylline
has potent CNS and respiratory stimulants effects
Caffeine use and dosing
given orally or by IV
has a wide therapeutic range
dosing is based of weight
Magnesium sulfate
used in sever asthma exacerbations when respiratory failure is impending
use of MgSO4
Inhibits Calcium uptake into bronchial smooth muscle
Potentiating the effects of Beta2 Agonists
Inhibiting Histamine release from Mast cells
Blocking AcH release in cholinergic nerve endings
only use when other options have been tried
administration of MgSO4
given via IV over 20 mins
dosage is weight based
usually just one dose is given
Torsades de pointes (MgSO4)
a lethal heart rhythm—-may help in converting to stable rhythm
preeclampsia
a syndrome characterized by hypertension in pregnant mothers.
preemclampsia decreases BP and seizure risk, used to prolong pregnancy by 1-2 days
Asthma severity
based on two criteria
symptom control
risk of exacerbation
severity is establish after 1-2 months after drug regimen initiated
assessment of asthma severity
frequency of symptoms recue medication use frequency of exacerbations airflow restriction airflow restriction on pulmonary function resting existing co- morbidities
Reliever therapy
Low dose ICS-LABA
or SABA
maintenance therapy
an increasing escalation of therapy involving multiple drugs
MIld asthma
symptoms less than 2 times a month low ICS-LABA PRN (50-100mg) no routine medication is required Fluticason and salmeterol budenoside/ formoterol mometasone/ formtorerol fluticasone/ vilanterol
Mod Asthma
for symptoms more frequent than twice a month, but not daily maintenance option- low dose ICS, with SABA relieve ( beclomethasone + salbutamol) or PRN ICS LABA combo futher add on daily LTRA (Montelukast reliever therapy PRN low dose ICS- LABA budesonide/ formoterol
Severe Asthma
symptoms most days or symptoms frequently causing night time waking preferred maintenance option Medium dose ICS-LABA combo ( 200-400mg) further maintenance option high dose ICS (500-600) add on : LAMA or LTRA reliever therapy ICS-LABA combo fluticasone/ salmeterol
uncontrolled asthma
severe asthma with the inability to control symptoms
High dose ICS-LABA
momentasone/ formoterol (zenhale) 500-600 mg
add on
LAMA or Omalizumab Xolair
reliever therapy
ICS-LABA combo drug
Gold guidelines
A.) minimal symptoms, low exacerbation risk (SAMA pm or SABA prn )
b. ) moderate symptoms, Low exacerbation risk (LAMA or LABA)
c. ) minimal symptoms, high exacerbation risk (ICS+LABA) or LAMA
d. ) frequent symptoms, high exacerbation risk ICS +LABA and or LAMA
