Actions on Smooth Muscle Flashcards
Drug Actions on Smooth Muscle
Syndrome of hypersecretion of gastric acid and pepsin usually caused by gastrinoma; it is associated with severe peptic ulceration and diarrhea
Zollinger-Ellison Syndrome
Inhibitor of lipoxygenase
Zileuton
Inhibitor of leukotrienes (LTD4) receptors and used in asthma
Zafirlukast and montelukast
Reason ergot alkaloids are contraindicated in pregnancy
Uterine contractions
Major indication for H1 receptor antagonist
Use in IgE mediated allergic reaction (allergic rhinitis, urticaria)
5HT-1D/1B agonist used for migraine headaches
Sumatriptan, naratriptan, and rizatriptan
Triptan available in parenteral and nasal formulation
Sumatriptan
MOA and effect of nitric oxide
Stimulates cGMP which leads to vascular smooth muscle relaxation
Disease caused by excess ergot alkaloids
St. Anthony’s Fire
Distribution of histamine receptors H1, H2, and H3
Smooth muscle and mast cells; stomach, heart, and mast cells; nerve endings, CNS respectively
Most common side effect of 1st generation antihistamines
Sedation, anticholinergic
Long acting beta 2 agonist used in asthma
Salmeterol
Prostaglandins that cause abortions
Prostaglandin E1 (misoprostol), PGE2, and PGF2alpha
Enzyme which theophylline inhibits
Phosphodiesterase
Approved for use in severe pulmonary HTN
PGI2 (epoprostenol)
Used in pediatrics to maintain patency of ductus arteriosis
PGE1 (Alprostadil)
Prostaglandin used as 2nd line treatment of erectile dysfunction
PGE1 (Alprostadil)
Methylxanthine derivative used as a remedy for intermittent claudication
Pentoxifylline
Agents for reduction of postpartum bleeding
Oxytocin and ergonovine
Drug that causes contraction of the uterus
Oxytocin
5HT-3 antagonist used in chemotherapeutic induced emesis
Ondansetron, granisetron, dolasetron and palonosetron
Class of drugs that reversibly inhibit COX
NSAIDS
Drug used in ergot alkaloids overdose, ischemia and gangrene
Nitroprusside
Receptors for serotonin (5HT-1) are located
Mostly in the brain, and they mediate synaptic inhibition via increased K+ conductance
Ergot alkaloid used as an illicit drug
LSD
Major SE of zileuton
Liver toxicity
5HT2 antagonist mediate synaptic excitation in the CNS and smooth muscle contraction
Ketanserin, cyproheptadine, and ergot alkaloids (partial agonist of alpha and serotonin receptors)
Muscarinic antagonist used in COPD
Ipratropium, tiotropium
MOA of corticosteroids
Induce lipocortins to 1. inhibit phospholipase A2, 2. repress COX-2 gene and enzyme expression, 3. repress cytokines that activate COX-2
SE of ergot alkaloids
Hallucinations resembling psychosis
Generation of antihistamine that has the most CNS effects
First generation due to being more lipid-soluble
2nd generation antihistamines
Fexofenadine, loratadine, and cetirizine
5ht-3 antagonist that has been MOST associated with QRS and QTc prolongation and should not be used in patients with heart disease
Dolasetron
Antihistamine that is indicated for allergies, motion sickness, and insomnia
Diphenhydramine
1st generation antihistamine that is highly sedating
Diphendydramine
H1 antagonist used in motion sickness
Dimenhydrinate and other 1st generation
H1 blocker that is also a serotonin antagonist
Cyproheptadine
Agents used in treatment of carcinoid tumor
Cyproheptadine
Difference between COX 1 and COX 2
COX 1 is constitutive while COX 2 may be induced during inflammation, although COX 2 is constitutive in some tissues
H2 blocker that causes the most interactions with other drugs
Cimetidine
1st generation antihistamine that is least sedating
Chlorpheniramine
Drug that selectively inhibits COX 2
Celecoxib
Drug causing depletion of substance P (vasodilator)
Capsaicin
Dopamine agonist used in hyperprolactinemia
Bromocriptine
Peptide causing increased capillary permeability and edema
Bradykinin and histamine
Mediator of tissue pain, edema, inactivated by ACE, and may be a contributing factor to the development of angioedema
Bradykinin
MOA action of cromolyn
Blocks opening of Cl channels to prevent mast cell degranulation
Antidote for severe CV toxicity of theophylline
Beta blockers
A class of endogenous substances that include histamine, serotonin, prostaglandins, and vasoactive peptides that work in autocrine or paracrine manner
Autacoids
Irreversible, nonselective COX inhibitor
Aspirin (or other salicylates)
Primary endogenous substrate for Nitric Oxidase Synthase
Arginine
SE of long term (>5 days) corticosteroid therapy and remedy
Adrenal suppression and weaning slowly, respectively
Clinical use for H2 blockers
Acid reflux disease, duodenal ulcer and peptic ulcer disease