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Autacoid pharmacology Flashcards

1
Q

autacoid

A
  • endogenous substance that mediates inflammation

- seldom used therapeutically themselves, but antagonists and some agonists have uses

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2
Q

histamine

A
  • biosynthesized from histidine

- stored in mast cells, basophils, enterochromaffin cells, neurons

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3
Q

H1 histamine receptors

A 
peripheral nerve endings
CNS
smooth muscle of blood vessels
bronchi
intestine
Gq coupled
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4
Q

H2 histamine receptors

A 
gastric mucosa
heart 
mast cells
CNS
Gs coupled
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5
Q

histamine biosynthesis

A

made from histidine via histidine decarboxylase

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6
Q

Histamine metabolism

A

diamine oxidase

Histamine N-methyl transferase

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7
Q

histamine and immune response

A
  • mast cells and basophils release histamine when exposed to antigen
  • IgG or IgM mediated complement cascade activation triggers histamine release
  • inflammatory cells attracted to release histamine by chemotaxis
  • certain drugs (bezylisoquinoline NMJ blockers, opiods, succinylcholine) can displace histamine from storage cells
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8
Q

Ways to antagonize histamine

A
  • physiologic-drug that produces opposite effect-eg epinephrine-reverse anaphylaxis
  • inhibit release
  • receptor antagonists
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9
Q

Effects of peripheral histamine H1 receptor activation

A
  • vasodilation of small blood vessels (most impt effect)-flushing, decrease BP and total peripheral resistance (TPR)
  • increase vascular permeability-edema, urticaria
  • bronchoconstriction and bronchospasm
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10
Q

H1 antagonists

A

-allergic conditions, urticaria, insomnia, motion sickness, parkinsonian syndromes

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11
Q

diphenhydramine mechanism of action

A
  • H1 receptor inverse agonist, stabilizes inactive form of H1 receptors, blocks effects of histamine on H1 in GI tract, large blood vessels, bronchial muscle, uterus, and suppress edema, flare, pruritis
  • produce sedation via antagonism of CNS H1 receptors
  • has significant anti-muscarinic activity-effective in relief of nausea, vomiting, and vertigo from motion sickness; anti-parkinsonian agent
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12
Q

diphenhydramine adverse reactions

A
  • CNS-dizziness, confusion, sedation
  • antimuscarinic effects- mydriasis, xerostomia, reduced bronchial secretions, tachycardia, constipation, urinary retention
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13
Q

diphenhydramine precautions

A

-asthma, heart disease, hepatic disease, glaucoma, bladder obstruction, urinary retention, infants (sleep apnea and SIDS)

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14
Q

diphenhydramine description

A
  • benadryl, sominex
  • 1st gen antihistamine
  • allergic rhinitis, sneezing, itching, urticaria, motion sickness, insomnia
  • CYP2D6
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15
Q

cetirizine description

A
  • zyrtec
  • 2nd gen antihistamine, active metabolite of 1st gen hydroxyzine
  • for allergic conditions (rhinitis, sneezing, itching, urticaria)
  • less sedating than older H1 antagonists
  • formulated q/ pseudoephedrine as Zyrtec-D
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16
Q

Cetirizine mechanism of action

A
  • H1 receptor inverse agonist; stabilizes inactive form of H1 receptor, blocks effects in GI tract, uterus, large BV, bronchial muscle and suppresses edema, flare, pruritis
  • minimal antimuscarinic activity
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17
Q

cetirizine adverse rxns and precautions

A
  • few
  • CNS (high doses): sedation, fatigue
  • xerostomia
  • if CrCL
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18
Q

Fexofenadine description

A
  • allegra
  • 2nd gen antihistamine, active metabolite terfenadine
  • for allergic conditions (rhinitis, sneezing, itching, urticaria)
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19
Q

Fexofenadine mechanism of action

A
  • H1 receptor inverse agonist; stabilizes inactive form of H1 receptor, blocks effects in GI tract, uterus, large BV, bronchial muscle, and suppresses edema, flare, pruritis
  • virtually no antimuscarinic activity at therapeutic dose
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20
Q

Fexofenadine adverse rxns

A

few
GI-nausea, dyspepsia
CNS-drowsiness, sedation

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21
Q

fexofenadine precautions

A
  • decrease dose in pts with decreased renal function

- avoid taking w/ fruit juice -> decreased absorption

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22
Q

Loratadine description

A
  • Claritin Tavist ND
  • 2nd gen antihistamine
  • allergic reactions
  • formulated w/ pseudophedrine-Claritin D
  • desloratadine (Clarinex)-active metabolite
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23
Q

Loratadine mechanism of action

A

-H1 receptor inverse agonist; stabilizes inactive form of H1 receptor, blocks effects in GI tract, uterus, large BV, bronchial muscle, and suppresses edema, flare, pruritis

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24
Q

Loratadine pharmacokinetics, adverse reactions, and precautions

A
  • CYP3A4
  • few; CNS-HA, sedation, xerostomia
  • hepatic ds; if CrCL
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25
H1 receptor antagonists
diphenhydramine cetirizine fexofenadine loratadine
26
Effects of peripheral H2 receptor activation
- vasodilation of small blood vessels - increase HR-reflex tachycardia and direct stimulation - gastric acid secretion
27
H2 antagonists and gastric acid secretion
- treat peptic ulcer ds - not as effective as PPI but cheap, very safe, and OTC (60-70% decrease in 24hr acid secretion) - especially effective at inhibiting nocturnal acid secretion, less effective on meal stimulated acid secretion
28
Cimetidine description
- Tagamet - 1st commercially available drug for peptic ulcer ds - indicated for GERD, peptic ulcer ds, intermittent dyspepsia
29
cimetidine mechanism of action
- inverse agonist; reduces constitutive activation of H2 receptors on parietal cells - decreases acid secretion by 60-70%
30
cimetidine adverse rxns
- moderate to severe HA | - rare blood dsycrasias: neutropenia, agranulocytosis, leukopenia, thrombocytopenia, pancytopenia
31
cimetidine precautions
-hepatic disease (CYP metabolized), renal insufficiency
32
serotonin
- 5-HT - biosynthesized from tryptophan - stored mostly in enterochromaffin cells, some in platelets and synaptic vesicles - mostly G-protein coupled receptors; one ligand gated ion channel (5-HT3)
33
Serotonin biosynthesis and metabolism
tryptophan -tryphtophan hydroxylase -> 5-hydroxy tryptophan - aromatic AA decarboxylase -> serotonin -MAO->aldehyde dehydrogenase or AANAT->ASMT -> melatonin
34
effects of 5-HT
- CNS: affect mood, appetite, sexual activity, thermoregulation, sensory perception, sleep, memory, cognition; mediates vomiting - GI: suppress (5-HT3) or promote (5-HT4) GI motility - CV-clotting, vasoconstriction ->BP, migraine
35
Migraine
- debilitating headache characterized by unilateral throbbing pain w/ nausea/vomiting, sensitivity to light and sound, visual disturbances, and duration of 4-72 hours - w/ (classic) or w/o (common) aura - neurogenic origin followed by vasodilation - 5-HT key mediator of pathogenesis
36
Ergotamine description
- Ergomar | - ergot alkaloid used to relieve migraines; ~70% effective in controlling acute attacks
37
ergotamine mechanism of action
- complex; some of the pharmacologic actions are unrelated to each other and some actions are even mutually antagonistic - partial agonist of antagonist activity @ 5-HT, dopamine, and a-adrenergic receptors; causes vasoconstriction of arteries and veins and decreased blood flow to peripheries - oxytocic agent-increase force and frequency of uterine contractions, decrease postpartum bleeding by constricting the placental vascular bed
38
ergotamine adverse reactions
- GI: NVD, xerostomia - ergotism: angina, asthenia, coronary vasopasm, cramps, myalgia, paresthesias, change in HR, vasoconstriction-> hyperthermia, necrosis
39
ergotamine precautions
- all absolute - CV-angina, arteriosclerosis, CAD, HTN, peripheral vascular ds, Raynaud's, thrombophlebitis, MI, stroke - hepatic ds, biliary tract ds, cholestasis - renal failure or impairment - FDA pregnancy category X
40
sumatriptan description
- Imitrex - approved for tx of acute migraine w/ or w/o aura; give asap after onset - not for long term migraine prophylaxis
41
sumatriptan mechanism of action
-agonist at presynaptic 5HT1D autoreceptors (shut down serotonin release) and at vascular 5-HT1B receptors -> vasoconstriction
42
sumatriptan adverse rxns
- potentially fatal CV events: coronary artery vasospasm, arrhythmias, MI, cardiac arrest - GI: NVD, vasospastic effects leading to bowel ischemia, abdominal pain, bloody diarrhea, and cramping - injection site rxn (50%): pain, burning
43
sumatriptan description
- Imitrex - approved for tx of acute migraine w/ or w/o aura; give asap after onset - not for long term migraine prophylaxis
44
sumatriptan mechanism of action
-agonist at presynaptic 5HT1D autoreceptors (shut down serotonin release) and at vascular 5-HT1B receptors -> vasoconstriction
45
sumatriptan adverse rxns
- potentially fatal CV events: coronary artery vasospasm, arrhythmias, MI, cardiac arrest - GI: NVD, vasospastic effects leading to bowel ischemia, abdominal pain, bloody diarrhea, and cramping - injection site rxn (50%): pain, burning
46
sumatriptan precautions
* *CV-angina, arteriosclerosis, arrhythmia, CAD, HTN, peripheral vascular ds, Raynauds, thrombophlebitis, MI, stroke * *Ischemic bowel disease - hepatic ds - renal insufficiency
47
serotonin syndrome
- caused by excessive serotonin concentration at its receptors - can be precipitated by the concomitant use of drugs that enhance synaptic serotonin [ ]s, usually developoing in less than 12 hrs (SSRI) (ecstasy) - Sx-anitation, hyperthermia, flushing, GI disturbances, myoclonus, rhabdomyolysis, tremor, seizures
48
Hydrocortisone description
- cortizone-10 - natural steroid hormone secreted by adrenal cortex - main uses are antiinflammatory: anaphylaxis, asthma, COPD, IBS, rheumatic disorders, dermatoses - drug of choice for glucocorticoid replacement therapy in patients w/ adrenal insufficiency - low potency topical corticosteroids are safest for chronic use, may be used in infants and young children
49
Eicosanoids
- from 20-C essential FA-arachidonic acid most abundant precursor - biosynthesis is limited by the availability of free arachidonic acid-released from membrane phospholipids by PLA2
50
hydrocortisone/cortisol
- main glucocorticoid in humans - stimulate GNG, increase glood glucose and insulin secretion - promote lipolysis and lipogenesis, increase fat deposition - stimulate protein and bone catabolism - CNS: improve mood, increase motor activity, decrease sleep, decrease memory * immunosuppressive, antiinflammatory effects (IL-1, 2, 6 and TNF-a all stimulate CRH and activate HPA axis)
51
Hydrocortisone description
-cortizone-10
52
hydrocortisone mechanism
- acts via nuclear receptors to modulate gene expression - anti-inflammatory-represses COX-2 expression; decrease cytokine production, increase formation and release of endogenous inflammatory mediators, apoptosis of eosinophils
53
prednisone mechanism
- prodrug of prenisolone, must be metabolized in vivo prednisolone - acts via nuclear receptors to modulate gene expression - anti-inflammatory-represses COX-2 expression; decrease cytokine production, increase formation and release of endogenous inflammatory mediators; apoptosis of eosinophils
54
hydrocortisone precautions
* *abrupt discontinuation of prolonged systemic therapy * *cushings syndrome - preexisting bacterial, viral, and fungal infections - patients receiving corticosteroids chronically should be assessed periodically for cataracts
55
prednisone description
- sterapred, generic - immunosuppressive oral corticosteroid; most prescribed - tx for autoimmune disorders, allograft rejection, asthma, IBS, rheumatoid arthritis, etc
56
prednisone mechanism
- prodrug of prenisolone, must be metabolized in vivo prednisolone - acts via nuclear receptors to modulate gene expression - anti-inflammatory-represses COX-2 expression; decrease cytokine production, increase formation and release of endogenous inflammatory mediators; apoptosis of eosinophils
57
prednisone adverse rxns
- (more common with high doses or prolonged therapy) - CNS: HA, insomnia, vertigo, depression, anxiety, euphoria, personality changes, psychosis - GI-NVD, anorexia, gastritis - cataracts - opportunistic infections
58
prednisone precautions
* *cushings ds * *high doses and long term therapy can suppress HPA axis-avoid abrupt DC of prolonged therapy - preexisting bacterial, viral, fungal infections - patients receiving corticosteroids chronically should be assessed periodically for cataracts
59
Fluticasone description
- Cutivate, flovent - Medium potency steroid used topically to relieve sx of dermatoses and psoriasis and intranasally for allergic and nonallergic rhinitis; used in tx of asthma, but for prophylaxis only
60
Fluticasone mechanism
- acts via nuclear receptors to modulate gene expression - anti-inflammatory-represses COX-2 expression; decrease cytokine production, increase formation and release of endogenous inflammatory mediators; apoptosis of eosinophils
61
Fluticasone adverse reactions
- pruritis, burning, hypertrichosis-mild and self-limiting | - hoarseness, irritation, secondary infections eg oropharyngeal candidiasis w/ inhaled form
62
NSAIDs mechanism of action
- irreversible inhibition of cyclooxygenase (COX) enzymes involved in prostaglandin biosynthesis - COX-1-constitutively present in almost all tissues - COX-2-constitutively expressed only in brain, kidney, and bone; inducible in response to certain mediators of inflammation
63
Steroid drugs
- hydrocortisone - prednisone - fluticasone
64
Aspririn description
- ASA, Bayer, generic - first NSAID, synthesized in 1853 and marketed late 1890s - Salicylate chemical class - used for thrombosis prevention, prevents or reduces risk of MI in pts w/ a history of MI, coronary bypass, angioplasty, angina, stroke, transient ischemic attacks - 5x more COX 1 vs 2
65
NSAIDs mechanism of action
- inhibition of cyclooxygenase (COX) enzymes involved in prostaglandin biosynthesis - COX-1-constitutively present in almost all tissues - COX-2-constitutively expressed only in brain, kidney, and bone; inducible in response to certain mediators of inflammation
66
NSAID black box warnings
-increased risk of cardiovascular and GI adverse effects
67
Aspririn description
- ASA, Bayer, generic - first NSAID, synthesized in 1853 and marketed late 1890s - Salicylate chemical class - used for thrombosis prevention, prevents or reduces risk of MI in pts w/ a history of MI, coronary bypass, angioplasty, angina, stroke, transient ischemic attacks
68
Aspirin adverse rxns
- GI disturbances: NVD, mucosal damage, bleeding pain - tinnitus or hearing loss w/ high doses - hypersensitivity and anaphylactic rxns-pts w/ chronic urticaria, asthma, chronic rhinitis
69
ketorolac adverse rxns and extra precautions
- CNS: HA, dizziness, drowsiness - GI-NVD, damage to mucosa, gastric bleeding, abdominal pain * *CrCL
70
NSAID precautions
* *Salicylate sensitivity * *aspirin triad - heart ds - renal ds - prior hx of GI bleeds or perforation - bleeding disorders: hemophilia, thrombocytopenia, vit k deficiency
71
Ketorolac description
- Toradol - promoted mainly as strong analgesic, not anti-inflm drug - used short term (
72
Indomethacin adverse rxns and extra precautions
- CNS: dizziness, HA, fatigue/malaise, depression, tremor, ataxia - GI disturbances: NVD, damage to mucosa, gastric bleeding, abd pain - Pregnancy category D risk in 3rd trimester - CNS-seizure disorder, parkinsons, major depression
73
NSAID precautions
* *Salicylate sensitivity * *aspirin triad * *CrCL
74
Indomethacin description
- Indocin - NSAID of indole and indene acetic acid class - in premies, used to accelerate closure of patent ductus arteriosus (need low prostaglandins) - 3-5x more COX 1 vs 2
75
Indomethacin adverse rxns and extra precautions
- CNS: dizziness, HA, fatigue/malaise, depression, tremor, ataxia - GI disturbances: NVD, damage to mucosa, gastric bleeding, abd pain - Pregnancy category D risk in 3rd trimester
76
Naproxen description
- Aleve, Anaprox - Naphthylpropionic acid class - marketed as S-enantiomer - Better for lower back pain?; rheumatoid arthritis - 3-5x more COX 1 vs 2
77
Naproxen adverse rxns
- GI: NVD, damage to mucosa, gastric bleeding, abdominal pain; risk of upper GI bleeding double that of OTC ibuprofen - Derm-rashes, urticaria, alopecia
78
Ibuprofen description
- Advil - phenylpropionic acid class - quite effective as analgesic-dental procedures use - 2x more COX 1 vs 2
79
Ibuprofen adverse rxns
- CNS: dizziness, HA, nervousness - GI: NVD, damage to mucosa, gastric bleeding, abdominal pain - Rash - Tinnitus - Blurred vision
80
Meloxicam description
- Mobic - potent enolcarboxamide NSAID - indicated for rheumatoid arthritis or osteoarthritis - 10x more COX 2 vs 1
81
Meloxicam adverse rxns
GI: pain, dyspepsia, nausea
82
Celecoxib description
- Celebrex - first FDA approved selective COX 2 inhibitor - 10-20x more COX 2 vs 1
83
Celecoxib adverse rxns
- GI disturbances: dyspepsia, NVD, abdominal pain - dizziness - rash
84
Diclofenac description
- phenylacetic acid class | - 10-20x more COX 2 vs 1
85
Diclofenac adverse rxns
- GI: upset stomach, heartburn, bleeding, ulceration, perforation, elevated LFTs - Renal-decreased blood flow, decrease GFR
86
Acetaminophen description
- Tylenol - analgesic and antipyretic activity but no anti-inflammatory activity or platelet effects - preferred analgesic/antipyretic when aspirin contraindicated
87
acetaminophen mechanism
- competitive inhibitor of COX 1 and 2 w/in CNS but not periphery - binds to cannabinoid receptors in spinal cord
88
acetaminophen adverse rxns
- rash, pruritis, urticaria - GI (high doses)-NV, anorexia, and abdominal pain w/in 2-3 hrs after high dose - hepatoxicity- in acute overdose, 2-3 days pass before maximum liver damage becomes apparent, antidote is IV N-acetyl cysteine - renal tubule necrosis w/ high/chronic doses
89
Acetaminophen precautions
- alcoholism - hepatic ds - renal ds-if CrCL
90
Acetaminophen pharmcokinetics
-in liver, 85-90% is harmlessly metabolized but 10-15% is converted via CYP 2E1, 1A2, 3A4 to a chemically reactive, potentially hepatotoxic molecule
91
Alprostadil description
Synthetic PGE1 for erectile dysfunction, maintain patent ductus arteriosus
92
Alprostadil mechanism
Agonist at EP receptor-> increase cAMP -> vasodilation
93
Latanoprost description
Synthetic PGF2a analog prodrug | Used to reduce elevated intraocular pressure in pts with open angle glaucoma or ocular HTN
94
Latanoprost mechanism of action
Selective FP receptor agonist, believed to reduce IOP by increasing outflow of aqueous humor
95
Misoprostol description
- potent synthetic prostaglandin analog for gastric ulcer prevention - pregnancy termination, induce labor
96
Misoprostol mechanism
- agonist @ EP receptors on parietal cells in stomach-> decrease cAMP-> decrease acid secretion, promote mucous and bicarbonate secretion - agonist @ EP receptor in uterus, stimulates and increases amplitude and frequency of uterine contractions, dilates cervix
97
Zileuton description
- leukotriene inhibitor - benzothiophene derivative of N-hydroxyurea - indicated for prophylaxis and chronic treatment of asthma
98
Zileuton mechanism
- Specific 5-LOX inhibitor- decrease leukotriene formation - clinical response is inhibition of neutrophil and eosinophil migration, neutrophil and monocyte aggregation, leukocyte adhesion, decreased capillary permeability, decreases leukotriene induced smooth muscle contractions
99
Zafirlukast description
Synthetic, selective peptide leukotriene receptor antagonist indicated for prophylaxis and chronic tx of asthma in adults and children
100
Zafirlukast mechanism
- antagonist at g-protein coupled cysteinyl leukotriene receptors in airway smooth muscle, mast cells, and neutrophils - inhibits bronchoconstriction, edema, mucous secretion
101
Montelukast description
- asthma maintenance therapy - also tx of allergic rhinitis - singulair
102
Montelukast mechanism
Antagonist at G protein coupled cysteinyl leukotriene receptors in airway smooth muscles, mast cells, neutrophils -inhibit bronchoconstriction, edema, mucous secretion

FM 1 (9 decks)

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