Autocoid Drugs Flashcards
MOA of omalizumab
Binds to IgE receptors on mast cells and basophils
MOA of diphenhydramine
Blocks the H-1 histamine receptor
MOA of cimetidine
Blocks the H-2 histamine receptors
MOA of the -lukasts
blocks the leukotriene receptor
MOA of cromolyn
inhibits mas cell degranulation
MOA of theophylline and roflumilast
inhibits phosphodiesterases
1st generation antihistamines
diphenhydramine
meclizine - less sedation
cyclizine - less sedation
2nd generation antihistamines
Certizine
Desloratadine
Fexofenadine
Terfenadine
1st generation antihistamines differ from 2nd generation
All 1st generation have anticholinergic effects whereas 2nd generation do not
Busprione
5-HT1A partial agonist
used an as anxiolytic (GAD)
5-HT agonists with serious adverse effect of Pulmonary HTN and valvular lesions
Fenfluramine
Dexfenfluramine
Phentermine
(Fen-Phen)
Cisapride
5-HT4 agonist
use: GERD/GI motility
enhances the release of ACh
cardia arrhythmias
prolongs QT
Tegaserod
partial 5-HT4 agonist used for IBS-C
-triptans
5-HT1D agonist
treatment for migraine headaches
Sumatriptan, naratriptan, rizatriptan, eletriptan, frova triptan, and zolmitriptan
can cause coronary vasospasm and angina
Lorcaserin
5-HT 2c agonist for treatment for of obesity
Lasmiditan
5-HT 1F receptor agonist for migraine headaches (new)
Ondansetron, ganisteron, dolasteron
The -setrons
5-HT3 antagonist used for treatment of nausea and vomiting during cancer chemotherapy
Aloserton
treats IBS-D
Morning sickness preferred treatment drugs
doxylamine/pyridoxine
ergot alkaloids
Erogtamine
Dihydroergotamine
Ergonovine/methylergonovine
treats post partum hemorrhage
Lysergic acid diethylamide
hallucinogen
Topiramate
anticonvulsant that prevents migraine
Valproic acid
anticonvulsant that prevents migraine
prolong and excessive treatment with dihydroergotamine
results in gangrene
Dry hacking cough
ACE inhibitors
Lisinopril
MOA of ACE Inhibitors
reduces angiotensin II formation and lowers BP & cardiovascular disease through 4 mechanisms
1. reduced AT vasoconstrictions = vasodilation lowers BP by reducing PVR w/o reflex tachycardia
2. reduce AT II will decrease aldosterone release from adrenal medulla, decrease fluid volume and decrease CO
3. reduced destruction of bradykinin = increase bradykinin levels - vasodilation to enhance BP lowering
4. decrease vascular and cardia hypertrophy & remodeling
Ramipril
does not negatively effect blood lipids or glucose
does not cause reflex tachycardia
JNC 8 Recommendations
General non-black population: thiazides, CCB, ACEI, or ARB
General black population: thiazides or CCB initially
CKD: treatment should include ACEI or ARB
Do not use ACEI and ARB together for risk of hyperkalemia.
Angina pectoris
use:
beta blocker
diltiazem
verapamil
don’t use:
hydralazine
minoxidil
Asthma & COPD
use:
CCB
ACEI
don’t use:
beta blocker
BPH
use:
alpha blocker
don’t use: none listed
Collagen disease (SLE)
use:
ACEI (but not captopril)
don’t use
hydralazine
methyldopa
Depression
use:
ACEI or ARB
CCB
don’t use:
centrally acting alpha 2 agonists
beta blocker
reserpine
DM
use:
ACEI or ARB
CCB
Angiotensin receptor antagonist
don’t use:
beta blocker
diuretic
Gout
don’t use diuretic
Heart failure
use:
ACEI inhibit or ARB
diuretic
hydralazine
beta blocker
don’t use:
CCB
endoge3nous substances that is thought to produce dry hacking cough in a patient taking enalapril
bradykinin
AT II properties
increase IP3, DAG via AT1 G-protein receptors.
constricts arterioles, increase aldosterone secretion
Bradykinin properties
Increase IP3, DAG, NO, cGMP. Dilates arterioles, increases capillary permeability, stimulates sensory nerve endings
Calcitonin gene-related peptide (CGRP)
an extremely potent vasodilator; causes hypotension and reflex tachycardia
Endothelin properties
increase IP3, DAG via G-protein-coupled ETa and ETb receptors. Synthesized in vascular endothelium. constrict most vessels, may play a pathophysiologic role in pulmonary hypertension
Activation of which of the following receptors in an experimental subject would be responsible for the RELEASE of adrenocorticotropic hormone (ACTH) from pituitary corticotropes?
V1b
Vasopressin receptors
V1a - vascular smooth muscle causing vasoconstriction = Gq pathway
V1b - potentiate release of ACTH by pituitary corticotropes = Gq pathway
V2 - in renal cells produce antidiuresis by increasing water permeability and reabsorption in collecting tubules (insertion of water channels) = Gs pathway
Which of the following prostaglandins is likely to cause bronchoconstriction in a asthmatic man?
TXA2; PGF2alpha, & PGD2
prostaglandin preparations appropriate used as an ophthalmic solution to LOWER intraocular pressure (IOP) in open-angle glaucoma?
Latanoprost (PGF2alpha)
Eicosanoids
Alprostadil
Carboprost tromethamine
Dinoprostone
Epoprostenol
Latanoprost
Misoprostol
Inhibitor of eicosanoid synthesis
corticosteroids
NSAIDs
Leukotriene receptor antagonist
Zafirlukast
Montelukast
Ergot Alkaloids and related compounds
Bromocriptine
Dihydroergotamine
Ergonovine
Ergotamine
Lysergic Acid
diethylamide (LSD)
AT II converting enzyme inhibitors
captopril
enalapril
Serotonin agonists
Sumpatriptan (5-HT1d)
Ciapride, Tegaserod, (5-HT4)
Buspirone (5-HT1A)
Peptides
Bradykinin
Vasopressin
DDAVP
Angiotensin II
Oxytocic actions
PGE1
PGE2
PGF2a
Dinoprostone
used for cervical ripening
PGE2
Misoprostol - abortion
Oxytocin
posterior pituitary hormones use clinically to control postpartum bleeding after delivery of the placenta
Induce milk ejection
Molecular target: terbutaline
Beta-2 recptors
Molecular target: steriods
nuclear receptor driven gene expression
Molecular target: -lukasts
leukotriene receptors
molecular target: zileuton
leukotriene synthesis
molecular target: ipratropium
muscarinic receptor
molecular target: theophylline
phosphodiesterase
Monoclonal antibodies for asthma
Omalizumab
Mepolizumab
Reslizumab
Benraliumab
Glucocorticoids
alter nuclear receptor driven gene expression
beclomethasone
budesonide
flunisolide
fluticasone
mometasone
ciclesonide (prodrug)
Drug critical to keep the plasma concentration within a narrow range
Theophylline
Emergency treatment for severe asthmas or COPD when bronchodilators do not resolved the airway obstruction
Oral steroids - prednisone
Parenteral - methylprednisolone
long acting beta 2 agonist risk
asthma-related deaths r/t down regulation of receptors
Omalizumab
antibodies directed towards the IgE high affinity Fc receptor on mast cells
control moderate to severe asthma not controlled by inhaled steriods