Anti inflammatory Flashcards
H1 activation leads to
- Increase capillary dilation via NO leading to Decrease BP
- Increase capillary permeability leading to edema
- Increased bronchiolar smooth muscle contraction
- Increas activation of peripheral nociceptive receptors increase pain and pruritis
- Decrease AV nodal conduction
H2 activation leads to
- Increas gastic acid secretion leading to ulcers
- Increase SA nodal rate
Diphenhydramine M block, Sedaiton, Antimotion
H1 Antagonist
- M Block: +++
- Sedation: +++
- Antimotion: +++
Promethazine M block, Sedaiton, Antimotion
H1 Blocker
- M Block: +++
- Sedation: +++
- Antimotion: +++
- Some alpha block and local anesthetic action
Chlorpheniramine M block, Sedaiton, Antimotion
H1 Blocker
- M Block: ++
- Sedation: ++
- Antimotion: ++
Meclizine M block, Sedaiton, Antimotion
H1 Block
- M Block: ++
- Sedation: ++
- Antimotion: +++
- Highly effective for motion sickness
Cetirizine M block, Sedaiton, Antimotion
H1 Blocker
- M Block: +/-
- Sedation: +
- Antimotion: 0
- Only sedation
Loratadine M block, Sedaiton, Antimotion
H1 Blocker
- M Block: +/-
- Sedation : 0
- Antimotion: 0
- No CNS entry
Fexofenadine M block, Sedaiton, Antimotion
H1 Blocker
- M Block: +/-
- Sedation: 0
- Antimotion: 0
- No CNS entry
H2 antagonist drugs
- Cimetidine
- Ranitidine
- Famotidine
- -TIDINE
H2 antagonist used for
Peptic Ulcer Disease, GERD, and Zolwinger by suppressing secretory response to food stimulation
Cimetidine adverse affects
- Major P450 inhibitor
- Decrease androgens leading to gynecomastia and decrease libido
Omeprazole (-Prazole) mechanism of action
- Irreversible proton pump in gastric parietal cells
- K/H antiport inhibitor
Misoprostol mechanism of action
PGE1 analog that is cytoprotective by increasing mucus and bicarbonate secretion and decrease HCL secretion
Sucralfate mechanism of action
- Polymerizes on GI luminal surface to form a protective gel-like coating of ulcer bed
- Requires acid pH to activated
Ondansteron (-steron) mechanism of action and use
5HT3 antagonist that prevents Nausea and vomiting in Cancer Pts.
DA antagonists
- Prochlorperazine
- Meoclopramide
DA antagonists used for
Prevent Nausea and vomiting in Cancer Pt.
Aprepitant mechanism of action
NK1 receptor antagonist
(receptor for substance P)
Buspirone mechanism of action
5HT1a partial agonist used for GAD
-TRIPTANS mechanism of action
Agonist at 5HT1d receptors in cerebral vessels leading to decrease migraine pain
-Triptan adverse affects
- Asthenia
- Chest or throat pressure or pain
5HT1(a-h) found in
- CNS (inhibitory)
- Smooth muscle (excitatory or inhibitory)
5HT2(a-c) found in
CNS (excitatory)
Cyproheptadine mechanism of action
5HT2 antagonised used in carcinoid, GI tumors, and Anorexia nervosa
5HT3 found in
- Area prostrema
- Peripheral sensory
- Enteric nerves
Ergotamine mechanism of action
- Partial agonist at both alpha and 5HT2 receptors in the vasculature and possibly in the CNS
- Vasoconstrictive action to decrease pulsation in cerebral vessels may prevent acute action of Ergotamine during migration
Ergotamine used for
Accute attacks of migraine headache
Ergotamine adverse affects
- GI distress
- Prolonged vasoconstriction leading to ischemia and gangrene
- Abortions near term
Glucocorticoids inhibit
Phopholipase A2 decreasing conversion of Membrane phospholipds to Arachidonic acid inhibiting production of both Prostaglandins and Leukotrines
Zileuton inhibits
Lipoxygenase preveting the converstion of Arachidonic acid to hydroperoxides preventing leukotrienes
-Lukast inhibit
Leukotriene receptors
NSAIDs inhibit
Cyclooxgynases preventing converstion of Arachidonic acid to Endoperoxides
Alprostadil mechanism of action and use
- PGE1 analog
- Maintains patency of ductus arteriosus
- Vasodilation used in male impotence
Dinoprostone mechanism of action
PGE2 analog that causes contraction of Uterine smooth muscle
Dinoprostone used for
- Cervical ripening
- abortifacient
Carboprost mechanism of action
PGF2alpha analog
Latanoprost mechanism of action
PGF2alpha analog
Carboprost used for
Abortifacient
Latanoprost used for
Treatment of glaucoma by decreasing interocular pressure
Epoprostenol mechanism of action
PGI2 (Prostacyclin) analog cuasing platelet stabilization and vasodilation
Asprin mechanism of action
Covalent bond via acetylation of a serine hydroxyl group near the active site of COX
Asprin adverse affects
Salicylism: Tinnitus, vertigo, decrease hearing
Bronchoconstriction
HS: Triad of Asthma, nasal polyps, rhinitis
Reye syndrome: Enchephalopathy
Increase BT (antiplatelet)
Renal dysfunction with chronic use
Reversible COX 1 and COX 2 inhibitors
- Ibuprofen
- Naproxen
- Indomethacin
- Ketorolac
- Sulindac
Indomethacin adverse affect
Thrombocytopenia, agranulocytosis
Drugs used for RA
- Hydroxychloroquine
- Methotrexate
- Sulfasalazine
- Glucocorticoids
- Leflunomide
- Etanercept
- Infliximad
- Anakinra
Hydroxychloroquine mechanism of action
Stabilizes lysosomes and decrease chemotaxis
Hydroxychloroquine adverse affects
- GI distress
- Visual dysfunction
- Hemolysis in G6PD
Methotrexate mechanism of action
Cytotoxic to lymphocytes
Methotrexate adverse affects
Hematotoxicity
Sulfasalazine mechanism of action
Sulfapyridine causes decrease in B-cell function
Sulfasalazine adverse affect
Hemolysis in G6PD
Glucocorticoids adverse affect
- ACTH suppression
- Cushingoid state
- Osteoporosis
- GI distress
- Glaucoma
Leflunomide mechanism of action
Inhibit dihydro-orotic acid dehydrogenase cuasing a decrease in UMP and decrease ribonucleotides causing arrested lymphocytes in G1
Leflunomide adverse affects
- Alopecia
- Rash
- Diarrhea
- Hepatotoxicity
Etanercept mechanism of action
Binds to TNF and inhibits it
Infliximad mechanism of action
Monoclonal AB to TNF
Anakinra mechanism of action
IL-1 receptor antagonist
Colchicine mechanism of actioin
Binds to tubulin and decreases microtubular polymerization decreasing migration
Treatment of acute gout
- Colchicine
- Indomethacin
Colchicine adverse affect
ACUTE:
- Diarrhea
- GI pain
CHRONIC:
- Hematuria
- Alopecia
- Myelosuppression
- Gastritis
- Peripheral neuropathy
Allopurinol mechanism of action
Converted by xanthine oxidase
Then inhibits xanthing oxidase decreasing purine metabolixm and decreasing Uric acid
Allopurinol adverse affects
- Rash
- Xanthine stones
Prophylaxis of Chronic Gout
- Allopurinol
- Probenecid
Probenecid mechanism of action
Inhibits proximal tubular reasborption of urate
Probenecid adverse affects
Crystallization of high excretion of uric acid
Glucocotricoids
- Prednisone
- Triamcinolone
- Betamethasone
- Dexamethasone
Theophylline mechanism of action
Bronchodilates via inhibition of phosphodiesterase causing and increase of cAMP
Antagonism of Adenosine (bronchoconstrictor)
Theophylline adverse affects
- Nausea
- Diarrhea
- Increase HR
- CNS
Theophylline toxicity increased by
- Erythromycin
- Cimetidine
- Fluoroquinolones
Cromolyn mechanism of action
Prevent degranulation of mast cells causing a decrease release of histamine
Nedocromil mechanism of action
Prevents degranulation of pulmonary mast cells causing a decrease in release of histamine