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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.
PGE1

Contraindicated
Protective on GI mucosa

-Minoprostol--Rx of NSAIDS ulcers.
-Alprostadil--Maintains PDA

Abortificient
PGE2
Uterine contraction

Dinoprostone-->cervix ripening.
Inhibition can give gastritis
PGF2 alpha
Uterine and bronchiolar muscle contraction
-Dinoprost&Carboprost-(abortificient)
-Latanoprost(rx of glaucoma)

-PGE2 and PGF2alpha elevated in Dysmenorrhea.
PGI2(prostacyclin)
Inhibition of platelet aggregation
-Vasodilator
-Epoprostenol--> given in pulmonary HTN.
Thromboxanes (TXA2)
-Promotes platelet aggregation.
vasoconstriction and bronchoconstriction

-Binds to IP3 to raise free Ca2+-->platelet aggregation.
C. Leukotrienes
LTB4

LTA4.LTC4,LTD4
-Mediates inflammation-->cell injury


-Release of slow acting substance of anaphylaxis
cause- vasoconstriction and bronchoconstriction.
Drugs that affect leukotrienes pathway.
1. Phospholipase inhibitor
-Corticosteroids.

2. Lipoxygenase inhibitor
- Zileuton---(rx of asthma)
3. Leukotrienes inhibitors
-Zafirlukast
-Montelukast
NSAIDS
MOA
Inhibit cycoloxygenase by blocking COX1 and COX2.
-Decreased production of PGE and TXA2

-Asprin( Acetyl Salicylic Acid).
irrevirsible inhibition of both COXs.
Pharmacologic effects of Aspirin.
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
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).
Uricosuric acid
-Decrease reabsorption
-
What is Rigor Mortis? What is it caused by?
-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
Acute aspirin toxicity

Aspirin Hypersensitivity
Resp. Alkalosis then Resp Acidosis
-Hypokalemia
-Metabolic Acidosis
-Fever

Triad--Asthma, Nasal Polyp, atrophic rhinitis
Acetaminophen
-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
Toxicity
Hepatotoxicity

Production of a metabolite N-acetylbenzoquinoneimine combines with Glutathione (GSH).

Antidote--Acetylcysteine--provides SH groups.
Reversible inhibitors of COX1&COX2
1.Ibuprofen--Doesnt affect warfarin activity or oral hypoglycemics.

2. Naproxen--Gout

3. Etodolac--
4. Indomethacin--
---Thrombocytopenia, ---Agranulocytosis
5. Sulindac
6. Tolmetin
7. Diclofinac
No renal effects, cramps or rashes.
-side effects--pancreatitis

-No effect on oral hypoglycemics

-Hepatotoxicity
NSAIDS
all have anelgesics, antipyretic, antiinflammatory.

Side effects
-GI dyspepsia
-Renal Interstitial nephritis
NSAIDs Drug interactions
Decrease clearance--> INcrease effect of Methotrexate, Oral Hypoglycemics, Lithium

Decrease effects of Antihypertensive drugs
-ACE inhibitors
-Beta blockers
-Loop diuretics
Selective COX2 inhibitors
Valdecoxib
Celecoxib
Rofecoxib

Cox 1 receptors
-present in BV--platelet aggregation
-present in Stomach-protective against ulcers.

Cox2 receptors
-activated by inflammation
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
Drugs used for Migraine

MOA

Side effects
Sumatriptan
Zolitriptan
Frovatriptan

-agonist at 5HTD1 receptor in cerebral BV.
-asthenia, throat pressure.
2. Ergotamine & Methysergide
-Agonist at 5HTD2 and alpha1 in BV.
-Vasoconstiction relieves pain in acute migraine attack
3. Analgesics
ASA, Acetaminophen
Butarphanol

Migraine Prophylaxis

-Betablockers
-Carbamezipine
-Gabapentin
-Ca Channel blockers
-Tricyclic antidepressents
-Valproic acid
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
Mechanism of Action
Bind to B2 receptors in lung--adenyl cyclase-->increase cAMP-->relaxation of smooth muscles in bronchioles.

Salmeterol-->prophylaxis only.
Contraindications
Uncontrolled arrhythmias

Adverse effects
Anxiety, headache,palpitation,htn, arrythmias, tremors, tachycardia
2. Xanthine Bronchodilators
Theophylline
AminoPhylline

-inhibit phosphodiesterase which metabolizes cAMP..so increase cAMP leads to muscle relaxation.
Theophylline
Theophylline toxicity increased by
-Macrolides (erythromycin)
-Quinolones (Ciprofloxacin

Decreased effects by
-Smoke and marjuana.
-CNS depressents--Phenobarbital
-antiepileptics--carbamezipine
4.Corticosteroids

Oral Corticosteroids
Buclomethasone
Fluticasone
Triamcinolone

-Prednisone
MOA
Antiinflammatory

- inhibit the release of inflammatory mediators--Histamine, Kinins

- inhibit the release of leukotries to prevent bronchoconstriction and mucus production.
Indications

Contraindications

Adverse effect
Bonchial asthma
Chronic bronchitits
Allergic rhinitis

-Acute bronchospasm

-oral fungal infections
-anorexia, abdominal distree
Leukotrienes Antagonists

Lipoxygenase inhibitor
Zafirlukast
Montelukast
-inhibit LTD4 receptor

Zileuton
-antagonist of all leukotrienes.
Indications

what does zileuton increase
chronic treatment of asthma
seasonal allergic reactions

-Headache
Dental pain
GI distress
Rash

-Increases LFT's.
Mast cell stabilizers
Cromolyn
Nedocromil

-Act on pulmonary mast cells to inhibit the release of histamine and leukotrienes.

-No bronchodilator effect just prevents bronchospasm.
Monoclonal antibody
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.
Status asthmaticus treatment
1. inhaled o2
2. Albuterol
3. IV methylpredinosone
4.Nebulized Ipratropium(anticholinergic)

In severe cases give
SC Epinephrine
Antitussives
Opioid-->Codeine

Non-opioid--> Dextromethmorphin
Robittussin.
Benzonatate
-MOA-->inhibits cough reflex
only for non productive cough, dry cough.
Expectorants
Guaifenesin-->decreases viscosity of mucus secretions.
-Mucus secretions associated with respiratory infections.
Not used for persistent cough associated with smokers,asthma,emphysema.
Diluents
to dilute respiratory secretions
-water
-saline
Mucolytics
Acetylcysteine
-breaks down mucus proteins
-treatment for mucus production in cystic fibrosis and atelectasis.
-Antetode for Acetaminophen toxicity.
Dornase alfa
recombinant human Dnase

Cystic Firbrosis

-nebulized
Decongestants
Pseudoephedrine
Phenylephrine

Stimulate alpha 1 receptors-->vasoconstriction
Rheumatoid Arthritis
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
Rx for RA
1.Always start with NSAIDS or COX2 inhibitors.
2.DMARDS
Disease Modifying AntiRheumatic DrugS
1.. Methotrexate

Adverse effects
-inhibits dihyrdofolate reductase.
-cytotoxic to lymphocytes

-->Worsen Nodules
-BM suppression
-Hair loss, Mucositits

--Leucovorin--Antidote for methotrexate toxicity.
2.Hydroxychloroquine

MOA

Adverse Effective
Stabilizes lysosomes and decreases chemotaxis.

-Adverse effects
-Cinochoism--Gi distress with visual loss.
-Hemolysis in G6PD.
3.Sulfasalazine

Adverse effects
Inhibits COX2.
-Sulfapyridine--Decreases Bcell functions

-GI distress
-Hemolysis
-Rash
-SLE like syndrome
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
6. D-penicillamine
Wilson Disease
-Supresses T-cell and Rheumatoid Factor
-Adverse effects
-Aplastic Anemia - Myasthania Gravis
7.Cyclophosphamide
-Alkylating agents used in severe cases.
-Hemorrhagic Cystitis.
8.Azathioprine
Immunosuppression in AI dieseas.
-Bone marrow suppression.
-Inhibits purine synthesis.
New DMARDs
Infiximab
-Monoclonal antibody.
-Decreases TNF

Etanercept
-Binds to TNF
3.Leflunomide
-Inhibits pyridine synthesis
-dihydro-orotic acid dehydrogenase-->decrease RNA

Side effects
--Alopecia, rash, hepatotoxicity
4.Anakinra

MOA
IL-1 receptor antagonist
Osteoarthritis
joint stiffness less than 30 mins.
-Disruption of the cartilage
-2ndary-->Joint deformity.
diagnosis of Osteoarthiritis
X-ray-->unequal loss of joint space

Rx
-Acetaminophen
-Ibuprofen
-Cox2 inhibitor
-celecoxib
Osteomyelitis
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
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.
Why confirmation of bone involvement is necessary in Osteomyelitis?
Cuz u dont want to put someone on Antibiotics for 6 weeks.

-Staph.A
--OX, Clox, Diclox, Naf
Fibromyalgia

Lab findings?

-Rx
widespread aching and stiffness for longer than 3 months.
-Normal lab findings
-Analgesics and anti depressents
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.
Gout
Involvement of Big Toe.
Uric acid crystals present.
-Increased UA production(idiopathic)
-Decreased excretion (renal dysfunction)

-Elevated Serum URIC ACID
Drugs used for Gout

Acute Gout attack
NSAIDs first

-Indomethacin
-Naproxin, Sulindac
Acute Gout attack

Adverse affects
Colchicine
-Binds to tubulin-->decrease formation of LTB4

-GI pain, Diarrhea

-Peripheral Neuropathy, Hematuria, Alopecia, Mylosupression.
Chronic Gouty Arthritis
Goal is to prevent Uric acid formation.
1.Allopurinol
-Inhibits Xanthine oxidase(suicide substrate).-->decrease production of purine -->decrease production of Uric Acid.
Adverse effects of Allopurinol

Which drug is contraindicated? why?
Rash,Stone formation, Vasculitis, Peripheral Neuropathy.

-Decrease amount of 6-Mercaptopurine.
-Severe liver toxicity.
2. Probenecid
-Inhibits tubular reabsorption of urate.
-Inhibits secretion of acidic drugs-->penicillin.

-Adverse effect-->Uric crystals in kidney.
3.Sulfinpyrazone

MOA
Similar to probenacid.
GFR dependent.
Inhibits Platelet aggregation.

-GI distress, rash, nephrotic syndrome.
Corticosteroids
inhibits phospholipase A2
-Inhibits cox2 expression
-inhibits PAF
-Inhibits IL-2

Adverse effects
-Electrolyte imbalance
-ACTH suppression:cortical atrophy
-Increase glaucoma and cataract.