Drugs with important actions on smooth muscles Flashcards
Serotonin causes ____________
Bronchospasm
Carcinoid is associated with diarrhea and hyertension
Physiologic antagonist of histamine
Epinephrine
Diphenhydramine is a potent sedative with ____ and ____ Blocking action
H1 and M3
Blockade of H2 receptors causes ___________ in cAMP several tissues
Decreases
H2 receptors are Gs-protein coupled receptors, like B adrenoceptors
Mechanism of fendluramine
5-HT2 agononist action
Banned because it causes pulmonary hypotension and cardiac valve malfunction
Alosetron is indicated in ________
Irritable bowel syndrome
Cetirizine is indicated for _________
Hay fever
_________ effective dopamine agonist in the CNS with the advantage of ral caviry
Bromocriptine
______ an agonist at 5HT 1D/1B receptors indicated for prevention and treatment for migraines
Sumatriptan
__________ is a powerful vasodilator necessary to reverse ergot-induced vasopasm
Nitroprusside
Diphenhydramine
Competitive pharmacologic block of peripheral and CNS H1 receptors plus alpha and M receptor block. Anti motion sickness effect
Used for Hay fever, angioedema, motion sickness
Promethazine
H1 blocker with less anti-motion sickness action and more sedative and autonmic effects
Cyclizine, meclizine
H1 blockers with more anti-motion sickness action and less sedative and autonomic effect
Cetirizine
H1 blockers, second generation
competitive pharmacologic block of peripheral H1 receptors, nO autonomic or anti-motion sickeness effect
Cimetidine/famotidine/ranitidine
H2 blocker
Competitive pharmacologic block. No H1 autonomic or anti-motion sickness effects
used in GERD, stress ulcers
Cimetidine: has drug interactions
suamtriptan
H-HT 1D/1B agonist. causes vasoconstriction. modualtes neurotransmitter release
used in migraine and cluster headache
Ketanserin
5 Ht2 antagonist
competive antagonis and alpha1 blcoker
used in hypertension and carcinoid tumor
Ondansetron
5-HT3 antagonist
pharmacologic antagonits. blocks chemoreceptor trigger zone and enteric nervous system 5-HT3 receptors
AE: QT prolongation, possible arrhythmias
Tegaserod
5-HT4 partial agonist
Used in constipation-dominant, irirtibale bowel syndrome (restricted use)
AE: diarrhea, ischemic colitis
Ergotamine
Partial agonist at 5 HT and alpha adrenoceptors, especially in blood vessels
Used in migraine and cluster headache
AE: nausea, vomiting, diarrhea, severe constripation
Ergonovine
partial agonist at 5HT and alpha adrenoceptors, especially in uterus
Used in postpartum bleeding
_____and _____ both caused marked increase in capillary permeability, often associated with edema, but hsitamine is not a peptide
Histamine and bradykinin
_____ is potent arterial vasodialtor and venoconstrictor
Susbtance P
_____is an atrial and brain peptide found in increased amount in heart failure
BNP
________an endothelin antagonist, is used in pulmonary hypertension
macitenan
_____can be used topically to deplete substance P stores from sensory nerves
Capsaicin
_____octapeptide, increases when blood volume decreases because the compensatory response causes an increase in renin secretion
AT II
______ increases because the enzyme inhibited by captopril, angitensin converting enzyme
bradykinin
Aliskerin
Renin inhibitor. Reduces angiotensin I and II and aldosterone secretion
used in hypertension
AE: angioedema. renal impairment
Ecallantide
Kinin anatagonist
Kallikrein inhibitor. reduces bradykinin levels
Used in hereditary angioedema
AE: hypersensitivity reactions
Icatibant
B2 bradykininreceptor blocker
used in hereditary angioedema
AE: hepatic toxicity, hypersensitivity reactions
Nesitiride
BNP receptor agonist
Sacubitril
Neprilysin inhibitor
Bosentan and macitentan
ETA and ETB receptor antagonist
used in pulmonary hypertension
AE: hepatic impairment
Aprepitant
Tachykinin NK1 receptor antagonist
used in antiemetic for chemotherapy induced vomiting
Capsaicin
Releases substance P from nerve endings
misoprostol is a _____ analog
PGE1
Aspirin blocks ____________
cyclooxygenase
Prostacyclin causes _________________ and may be used in pulmonary hypertension
vasodilation
_______ complains severe dysmenorrhea, a uterine stimulant
Prostaglandin PGF 2a
Leukotriene C ans D series are major eicosanoid components of ___________
SRS-A
Blocks the synthesis of leukotrienes.
Zileuton
LTB4
Chemotactic factor in inflammation
LTC4 and LTD4
Bronchonstrictors importantn in anaphylaxus, asthma
Montelukas/Zafrilukast
Block CysLT1 receptor. reduce bronchonstriction in asthma
used in asthma prophylaxis
An NO-containing molecule that releases nitric oxide in the blood is
Citrulline
The inducible isoform of nitric oxidase synthase (iNOS, isoform 2 ) is found primarily in
MArcophages
The primary endogenous substrate for the enzyme nitric oxide synthase (NOS) is
Arginine
Endogenous inhibitor/inactivator of nitric oxide
Hemoglobin
The inducible form of NOS is associated with
inflammation
Nitric oxide oxide gas
Activates guanylyl cyclase, icnreases cGMP synthesis causes smooth muscle relaxation
used in Pulmonary hypertension
AE: excessive hypotension, methemoglobinemia, conversion to nitrogen dioxide (pulmoanry irritant)
Nitric Oxide synthase activators
Acetylcholine, histamine
Increased IP3 will icnrease increased intraceelular calcium that activates NOS, resulting in conversion of arginine to citrulline plus NO