Autocoids Flashcards
Epinephrine
DOC for Anaphylaxis and other
conditions that involve massive
histamine release
First Generation H1 Antagonists
Chlorpheniramine Cyclizine Dimenhydrinate Diphenhydramine Hydroxyzine Meclizine Promethazine
Cross the BBB-Sedative effects
Inverse Agonist,Also block cholinergic, α-adrenergic, serotonin
and local anesthetic receptor sites (unrelated to
their blocking of H1 receptors
DOC in controlling sxs of allergic
rhinitis and urticaria, also treats motion sickness
AE: sedation, dry mouth, hallucinations
Second generation H1 Antagonist
Less sedating less able to cross BBB
Fexofenadine Loratadine Cetirizine Astemizole Terfenadine
Inverse Agonist!↓ constitutive activity
DOC in controlling sxs of allergic
rhinitis and urticaria
AE:Cardiac toxicity (besides Fexofenadine) ,
H2 Antagonist
Cimetidine
Ranitidine
Famotidine
Nizatidine
Competitively and reversible H2 inhibitors!
↓cAMP! ↓ gastric acid secretion
Used for GERD,Peptic ulcers
AE: extreme safe, Cimetidine via IV can lead to confusion and hallucination, inhibits CYP450 (lower metabolism of other drugs)
Serotonin (5-HT)
No clinical applications as a drug
Sumatriptan
5-HT 1D/1B
Agonist
Reduce both sensory activation in the periphery
and nociceptive transmission in the brainstem
trigeminal nucleus!diminish central sensitization
-cause vasoconstriction
DOC for acute severe migraines
Metoclopramide
5-HT4 Agonist
Prokinetic Agent! promote and organize gut
motility
-facilitates ACh release from enteric neurons
Central anti-dopaminergic actions! antinauseant,
antiemetic
Peripheral anti-dopaminergic actions!enhance
prokinetic activity by counteracting the inhibitory
effect of D2 receptors
Used for Gastroparesis
Emesis GERD
AE:Somnolence, Nervousness, & Dystonic rxns Extrapyramidal effects & tardive dyskinesia, Galactorrhea
Cisapride
5-HT4 Agonist
Prokinetic Agent! promote and organize gut
motility
-facilitates ACh release from enteric neurons
Central anti-dopaminergic actions! antinauseant,
antiemetic
Peripheral anti-dopaminergic actions!enhance
prokinetic activity by counteracting the inhibitory
effect of D2 receptors
Used for Gastroparesis
Emesis GERD
AE:Somnolence, Nervousness, & Dystonic rxns Extrapyramidal effects & tardive dyskinesia, Galactorrhea, NO LONGER USED INCREASES QT
Cyproheptadine
5-HT2 Antagonist
Potent H1 blocking actions
Used for: Allergic rhinitis
vasoactive rhinitis .
Serotonin Syndrome ( ↑5-
Ondansetron
5-HT3 Antagonist
Powerful anti-emetic
used for controls severe nausea and vomiting in
patients undergoing chemotherapy
Dihydroergotamine
Ergot Alkaloids
Used for migraines (Triptans preferred)
Ergotamine
Ergot Alkaloids
Used for migraines (Triptans preferred)
Bromocriptine
Ergot Alkaloids
Used for Hyperprolactinemia d/t pituitary tumor
Cabergoline
Ergot Alkaloids
Used for Hyperprolactinemia d/t pituitary tumor
Ergot Alkaloids
Agonist, partial agonist, and antagonist actions at
α-adrenoceptors and 5-HT receptors
Agonist or partial agonist action at CNS dopamine
receptor
AE: Nausea and vomiting (most common)
Contraindicated in pregnant women, pts with
peripheral vascular disease. CAD, HTN, and impaired
hepatic/renal fxn
Should not be used concurrently with drugs that cause
vasoconstriction
Ergonovine
Ergot Alkaloids
Uses Postpartum Hemorrhage when oxytocin is ineffective Ergonovine: provoke coronary artery
spasm! diagnose variant angina
AE: vasospasms
Methylergonovine
Ergot Alkaloids
Uses Postpartum Hemorrhage when oxytocin is ineffective
AE: vasospasms
Misoprostol
PGE 1 analog (Eicosanoid)
Used in Ripen cervix at or near term
Postpartum hemorrhage
Abortion when used in combination with a progesterone
antagonist (mifepristone/methotrexate)
Prevention of peptic ulcers in patients taking high does of NSAIDS
Eicosanoids
Act in autocrine and paracrine fashion
Bind to G-protein coupled receptors (Gs, Gi or Gq)
Contractile effects on smooth mm. are mediated by release of
Ca2+
Relaxing effects are mediated by elevation in cAMP
Dinoprostone
PGE2 (Eicosanoid)
used for Ripen cervix at or near term, Abortion
Alprostadil
PGE1(Eicosanoid)
Used for maintain patency of the ductus arteriosus in infants with transposition of the great vessels
Impotence
Epoprostenol
PGI2 Prostacyclin(Eicosanoid)
Used in Severe pulmonary HTN (↓ peripheral, pulm, and coronary
resistance)
Prevents platelet aggregation in dialysis machines
Latanoprost
PGF2α(Eicosanoids)
Used for glaucoma
Zileuton
Eicosanoid
Antagonists
Leukotriene inhibitors
Inhibits 5-lipoxygenase
Used for Moderate-severe asthma in pts. who are poorly controlled by
conventional therapy or experience adverse effects with corticoids
