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71 Cards in this Set
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Antiinflammatory
MOA |
Prostaglandins, Leukotriens, Thromboxaes.
Eiconasoids In response to Inflammation IgE release Trauma Toxins -Bind to G coupled receptors second messenger to effector system. |
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PGE1
Contraindicated |
Protective on GI mucosa
-Minoprostol--Rx of NSAIDS ulcers. -Alprostadil--Maintains PDA Abortificient |
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PGE2
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Uterine contraction
Dinoprostone-->cervix ripening. Inhibition can give gastritis |
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PGF2 alpha
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Uterine and bronchiolar muscle contraction
-Dinoprost&Carboprost-(abortificient) -Latanoprost(rx of glaucoma) -PGE2 and PGF2alpha elevated in Dysmenorrhea. |
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PGI2(prostacyclin)
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Inhibition of platelet aggregation
-Vasodilator -Epoprostenol--> given in pulmonary HTN. |
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Thromboxanes (TXA2)
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-Promotes platelet aggregation.
vasoconstriction and bronchoconstriction -Binds to IP3 to raise free Ca2+-->platelet aggregation. |
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C. Leukotrienes
LTB4 LTA4.LTC4,LTD4 |
-Mediates inflammation-->cell injury
-Release of slow acting substance of anaphylaxis cause- vasoconstriction and bronchoconstriction. |
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Drugs that affect leukotrienes pathway.
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1. Phospholipase inhibitor
-Corticosteroids. 2. Lipoxygenase inhibitor - Zileuton---(rx of asthma) 3. Leukotrienes inhibitors -Zafirlukast -Montelukast |
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NSAIDS
MOA |
Inhibit cycoloxygenase by blocking COX1 and COX2.
-Decreased production of PGE and TXA2 -Asprin( Acetyl Salicylic Acid). irrevirsible inhibition of both COXs. |
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Pharmacologic effects of Aspirin.
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Analgesics--inhibits PGs to decrease sensitization of pain receptors by producing pain mediators bradykinin and Histamine.
Antipyeretic-- Increase production of PGE2 to prodcue increase levels of IL-1..raise temp |
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Antiinflammatory effect
AntiPlatelet aggregation |
Blocks the signal transduction proteins
-blocks selectins and integrins -Blocks COX2. -Decreases Neutrophil adhesion -Blocks TXA2(normally responsible for platelet aggregations). |
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Uricosuric acid
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-Decrease reabsorption
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What is Rigor Mortis? What is it caused by?
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-Muscles become rigid/stiff
-no ATP, Ca remains -> Actin/Myosin bind |
no ATP is available to pump calcium away so Actin and Myosin filaments remain stuck together and muscles become rigid/stiff
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Acute aspirin toxicity
Aspirin Hypersensitivity |
Resp. Alkalosis then Resp Acidosis
-Hypokalemia -Metabolic Acidosis -Fever Triad--Asthma, Nasal Polyp, atrophic rhinitis |
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Acetaminophen
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-Not an ANTI inflammatory drug.
-Works on central cycloxygenase only no effect on peripheral. Similar to aspirin-- Antipyeretic Analgesics No GI bleed No antiinflammatory No effect on blood coagulation |
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Toxicity
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Hepatotoxicity
Production of a metabolite N-acetylbenzoquinoneimine combines with Glutathione (GSH). Antidote--Acetylcysteine--provides SH groups. |
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Reversible inhibitors of COX1&COX2
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1.Ibuprofen--Doesnt affect warfarin activity or oral hypoglycemics.
2. Naproxen--Gout 3. Etodolac-- 4. Indomethacin-- ---Thrombocytopenia, ---Agranulocytosis |
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5. Sulindac
6. Tolmetin 7. Diclofinac |
No renal effects, cramps or rashes.
-side effects--pancreatitis -No effect on oral hypoglycemics -Hepatotoxicity |
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NSAIDS
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all have anelgesics, antipyretic, antiinflammatory.
Side effects -GI dyspepsia -Renal Interstitial nephritis |
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NSAIDs Drug interactions
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Decrease clearance--> INcrease effect of Methotrexate, Oral Hypoglycemics, Lithium
Decrease effects of Antihypertensive drugs -ACE inhibitors -Beta blockers -Loop diuretics |
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Selective COX2 inhibitors
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Valdecoxib
Celecoxib Rofecoxib Cox 1 receptors -present in BV--platelet aggregation -present in Stomach-protective against ulcers. Cox2 receptors -activated by inflammation |
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Rofecoxib (vioxx)
Celecoxib |
-Selective Cox2 inhibitor
--good for inflammation in Arthritis -Activates Cox2 so clot formation in BV can give MI -Cross allergy with sulfonamide |
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Drugs used for Migraine
MOA Side effects |
Sumatriptan
Zolitriptan Frovatriptan -agonist at 5HTD1 receptor in cerebral BV. -asthenia, throat pressure. |
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2. Ergotamine & Methysergide
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-Agonist at 5HTD2 and alpha1 in BV.
-Vasoconstiction relieves pain in acute migraine attack |
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3. Analgesics
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ASA, Acetaminophen
Butarphanol Migraine Prophylaxis -Betablockers -Carbamezipine -Gabapentin -Ca Channel blockers -Tricyclic antidepressents -Valproic acid |
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Drugs used in Asthma
1. Bronchodilators |
Short acting b2 agonists
-Albuterol -Terbuterol -Metaproterenol Long acting B2 agonist -Salmeterol Alpha1,B1,B2 -->epinephrine B1,B2-->Isoproterenol |
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Mechanism of Action
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Bind to B2 receptors in lung--adenyl cyclase-->increase cAMP-->relaxation of smooth muscles in bronchioles.
Salmeterol-->prophylaxis only. |
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Contraindications
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Uncontrolled arrhythmias
Adverse effects Anxiety, headache,palpitation,htn, arrythmias, tremors, tachycardia |
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2. Xanthine Bronchodilators
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Theophylline
AminoPhylline -inhibit phosphodiesterase which metabolizes cAMP..so increase cAMP leads to muscle relaxation. |
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Theophylline
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Theophylline toxicity increased by
-Macrolides (erythromycin) -Quinolones (Ciprofloxacin Decreased effects by -Smoke and marjuana. -CNS depressents--Phenobarbital -antiepileptics--carbamezipine |
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4.Corticosteroids
Oral Corticosteroids |
Buclomethasone
Fluticasone Triamcinolone -Prednisone |
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MOA
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Antiinflammatory
- inhibit the release of inflammatory mediators--Histamine, Kinins - inhibit the release of leukotries to prevent bronchoconstriction and mucus production. |
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Indications
Contraindications Adverse effect |
Bonchial asthma
Chronic bronchitits Allergic rhinitis -Acute bronchospasm -oral fungal infections -anorexia, abdominal distree |
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Leukotrienes Antagonists
Lipoxygenase inhibitor |
Zafirlukast
Montelukast -inhibit LTD4 receptor Zileuton -antagonist of all leukotrienes. |
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Indications
what does zileuton increase |
chronic treatment of asthma
seasonal allergic reactions -Headache Dental pain GI distress Rash -Increases LFT's. |
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Mast cell stabilizers
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Cromolyn
Nedocromil -Act on pulmonary mast cells to inhibit the release of histamine and leukotrienes. -No bronchodilator effect just prevents bronchospasm. |
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Monoclonal antibody
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Omalizumab
-Binds to IgE receptor on mast cells. Moderate to severe persistent asthma -adverse reactions --No acute attack -irritation at site of injection -increased replication of viral or repiratory tract infection. |
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Status asthmaticus treatment
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1. inhaled o2
2. Albuterol 3. IV methylpredinosone 4.Nebulized Ipratropium(anticholinergic) In severe cases give SC Epinephrine |
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Antitussives
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Opioid-->Codeine
Non-opioid--> Dextromethmorphin Robittussin. Benzonatate -MOA-->inhibits cough reflex only for non productive cough, dry cough. |
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Expectorants
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Guaifenesin-->decreases viscosity of mucus secretions.
-Mucus secretions associated with respiratory infections. Not used for persistent cough associated with smokers,asthma,emphysema. |
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Diluents
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to dilute respiratory secretions
-water -saline |
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Mucolytics
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Acetylcysteine
-breaks down mucus proteins -treatment for mucus production in cystic fibrosis and atelectasis. -Antetode for Acetaminophen toxicity. |
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Dornase alfa
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recombinant human Dnase
Cystic Firbrosis -nebulized |
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Decongestants
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Pseudoephedrine
Phenylephrine Stimulate alpha 1 receptors-->vasoconstriction |
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Rheumatoid Arthritis
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Extra articular involvement
Early morning stiffness for 1 hour or longer for more than 6 weeks. more than 3 joints involved. Check with Xray of joint Wrist PIP not DIP Increased ESR |
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Rx for RA
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1.Always start with NSAIDS or COX2 inhibitors.
2.DMARDS Disease Modifying AntiRheumatic DrugS |
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1.. Methotrexate
Adverse effects |
-inhibits dihyrdofolate reductase.
-cytotoxic to lymphocytes -->Worsen Nodules -BM suppression -Hair loss, Mucositits --Leucovorin--Antidote for methotrexate toxicity. |
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2.Hydroxychloroquine
MOA Adverse Effective |
Stabilizes lysosomes and decreases chemotaxis.
-Adverse effects -Cinochoism--Gi distress with visual loss. -Hemolysis in G6PD. |
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3.Sulfasalazine
Adverse effects |
Inhibits COX2.
-Sulfapyridine--Decreases Bcell functions -GI distress -Hemolysis -Rash -SLE like syndrome |
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4.Corticosteroids
5. Gold Salts |
Decrease activity of LTs, IL2 and PAF
-Decrease ACTH -Decrease function of macrophages and lysosomes. Adverse effects-Stomatitis, rash, Bonemarrow suppression, Prtoeinure, Nephrotic syndrome |
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6. D-penicillamine
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Wilson Disease
-Supresses T-cell and Rheumatoid Factor -Adverse effects -Aplastic Anemia - Myasthania Gravis |
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7.Cyclophosphamide
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-Alkylating agents used in severe cases.
-Hemorrhagic Cystitis. |
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8.Azathioprine
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Immunosuppression in AI dieseas.
-Bone marrow suppression. -Inhibits purine synthesis. |
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New DMARDs
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Infiximab
-Monoclonal antibody. -Decreases TNF Etanercept -Binds to TNF |
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3.Leflunomide
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-Inhibits pyridine synthesis
-dihydro-orotic acid dehydrogenase-->decrease RNA Side effects --Alopecia, rash, hepatotoxicity |
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4.Anakinra
MOA |
IL-1 receptor antagonist
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Osteoarthritis
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joint stiffness less than 30 mins.
-Disruption of the cartilage -2ndary-->Joint deformity. |
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diagnosis of Osteoarthiritis
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X-ray-->unequal loss of joint space
Rx -Acetaminophen -Ibuprofen -Cox2 inhibitor -celecoxib |
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Osteomyelitis
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Not an inflammatory disease
-Bacterial infection--S.aureus -Children--Acute -Adults--Chronic -Can affect any kind of bone. -Never answer culture in Osteomyelitis. Do X-rays |
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If X-ray is +ve
If X-ray is -ve |
--+ve
---Do biopsy and IV antibiotics ---ve --Do a bone scan or MRI.. if negative then its not Osteomyelitis. |
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Why confirmation of bone involvement is necessary in Osteomyelitis?
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Cuz u dont want to put someone on Antibiotics for 6 weeks.
-Staph.A --OX, Clox, Diclox, Naf |
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Fibromyalgia
Lab findings? -Rx |
widespread aching and stiffness for longer than 3 months.
-Normal lab findings -Analgesics and anti depressents |
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Polymyalgia Rheumatica
Lab findings Rx |
Elderly with same complains as Fibromyalgia.
-Raised ESR -check for Giant Temporal Arteritis(biopsy) Rx -give steroids 15mg/day and taper if come back with headache, increase to 40mg/day because they might go blind. |
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Gout
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Involvement of Big Toe.
Uric acid crystals present. -Increased UA production(idiopathic) -Decreased excretion (renal dysfunction) -Elevated Serum URIC ACID |
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Drugs used for Gout
Acute Gout attack |
NSAIDs first
-Indomethacin -Naproxin, Sulindac |
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Acute Gout attack
Adverse affects |
Colchicine
-Binds to tubulin-->decrease formation of LTB4 -GI pain, Diarrhea -Peripheral Neuropathy, Hematuria, Alopecia, Mylosupression. |
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Chronic Gouty Arthritis
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Goal is to prevent Uric acid formation.
1.Allopurinol -Inhibits Xanthine oxidase(suicide substrate).-->decrease production of purine -->decrease production of Uric Acid. |
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Adverse effects of Allopurinol
Which drug is contraindicated? why? |
Rash,Stone formation, Vasculitis, Peripheral Neuropathy.
-Decrease amount of 6-Mercaptopurine. -Severe liver toxicity. |
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2. Probenecid
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-Inhibits tubular reabsorption of urate.
-Inhibits secretion of acidic drugs-->penicillin. -Adverse effect-->Uric crystals in kidney. |
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3.Sulfinpyrazone
MOA |
Similar to probenacid.
GFR dependent. Inhibits Platelet aggregation. -GI distress, rash, nephrotic syndrome. |
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Corticosteroids
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inhibits phospholipase A2
-Inhibits cox2 expression -inhibits PAF -Inhibits IL-2 Adverse effects -Electrolyte imbalance -ACTH suppression:cortical atrophy -Increase glaucoma and cataract. |
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