One Liners Pharm Musculoskeletal/important Actions On Smooth Muscles

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Disease caused by excess ergot alkaloids

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St. Anthony's Fire

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MOA of NSAIDS

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inhibit prostaglandin synthesis by inhibiting cyclo-oxygenase (cox)

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Endogenous substances commonly interpreted as histamine, serotonin, prostaglandins, and vasoactive peptides

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Autocoids

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Available bisphosphonates

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Alendronate, etidronate, risedronate, pamidronate, tiludronate, and zoledronic acid

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Syndrome of hypersecretion of gastric acid and pepsin usually caused by gastrinoma; it is associated with severe peptic ulceration and diarrhea

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Zollinger-Ellison Syndrome

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Difference between aspirin and other NSAIDS

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Aspirin irreversibly inhibits cyclooxygenase

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Drug that causes contraction of the uterus

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Oxytocin

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MOA of Bisphosphonates

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Inhibits osteoclast bone resorption

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Distribution of histamine receptors H1, H2, and H3

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Smooth muscle; stomach, heart, and mast cells; nerve endings, CNS respectively

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Four main actions of NSAIDS

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Anti-inflammatory, analgesia, antipyretic and antiplatelet activity

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Prototype antagonist of H1 and H2 receptors

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Diphenhydramine and cimetridine, respectively

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Names of three bisphosphonates available IV

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Pamidronate, zoledronate, ibandronate

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1st generation antihistamine that is highly sedating

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Diphendydramine

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Agent used for closure of patent ductus arteriosus

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Indomethacin

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1st generation antihistamine that is least sedating

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Chlorpheniramine or cyclizine

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Uses of bisphosphonates

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Osteoporosis, Paget's disease, and osteolytic bone lesions, and hypercalcemia from malignancy

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2nd generation antihistamines

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Fexofenadine, loratadine, and cetirizine

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Aspirin is contraindicated in children with viral infection

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Potential for development of Reye's syndrome

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Generation of antihistamine that has the most CNS effects

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First generation due to being more lipid-soluble

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Major SE of bisphosphonates

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Chemical esophagitis

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Major indication for H1 receptor antagonist

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Use in IgE mediated allergic reaction

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SE of salicylates

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Tinnitus, GI bleeding

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Antihistamine that can be used for anxiety and insomnia and is not addictive

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hydroxyzine (Atarax)

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Bisphosphonates that cannot be used on continuous basis because it caused osteomalacia

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Etidronate

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H1 antagonist used in motion sickness

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Dimenhydrinate, meclizine, and other 1st generation

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NSAID also available as an ophthalmic preparation

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Diclofenac

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Most common side effect of 1st generation antihistamines

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Sedation

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Used for prevention of postmenopausal osteoporosis in women

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Estrogen (HRT-Hormone replacement therapy)

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Lethal arrhythmias resulting from concurrent therapy with azole fungals (metabolized by CYP 3A4) and these antihistamines which inhibit the 3A4 iso-enzyme.

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Terfenadine and astemizole (have been removed from the market)

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NSAID available orally, IM and ophthalmically

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Ketorolac

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H2 blocker that causes the most interactions with other drugs

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Cimetidine

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Increase bone density, also being tested for breast CA prophylaxis

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Raloxifene (SERM-selective estrogen receptor modulator)

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Clinical use for H2 blockers

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Acid reflux disease, duodenal ulcer and peptic ulcer disease

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NSAID that is used for acute condition, such as pre-op anesthesia and has limited duration (<5 days) of use due to nephrotoxicity

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Ketorolac

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Receptors for serotonin (5HT-1) are located

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Mostly in the brain, and they mediate synaptic inhibition via increased K+ conductance

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Used intranasally and decreases bone resorption

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Calcitonin (salmon prep)

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5HT-1d agonist used for migraine headaches

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Sumatriptan, naratriptan, and rizatriptan

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Newer NSAID that selectively inhibits COX-2

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Celecoxib

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Triptan available in parenteral and nasal formulation

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Sumatriptan

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Used especially in postmenopausal women, dosage should be 1500 mg

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Calcium

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H1 blocker that is also a serotonin antagonist

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Cyproheptadine

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COX 2 inhibitors may have reduced risk of

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Gastric ulcers and GI Bleeding

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Agents for reduction of postpartum bleeding

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Oxytocin, ergonovine and ergotamine

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Vitamin given with calcium to ensure proper absorption

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Vitamin D

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Agents used in treatment of carcinoid tumor

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Ketanserin cyproheptadine, and phenoxybenzamine

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COX 2 inhibitors should be used cautiously in pts with

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Pre-existing cardiac or renal disease

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5HT-3 antagonist used in chemotherapeutic induced emesis

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Ondansetron, granisetron,
dolasetron and alosetron

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Acetaminophen only has

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Antipyretic and analgesic activity

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5HT-3 antagonist that has been associated with QRS and QTc prolongation and should not be used in patients with heart disease

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Dolasetron

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SE of acetaminophen

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Hepatotoxicity

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DOC to treat chemo-induced nausea and vomiting

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Odansetron

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Antidote for acetaminophen toxicity

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N-acetylcysteine

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Drug used in ergot alkaloids overdose, ischemia and gangrene

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Nitroprusside

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DMARDs are slow acting drugs for

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Rheumatic disease

DMARDS: Drugs-Modifying Anti-Rheumatic Agents

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Reason ergot alkaloids are contraindicated in pregnancy

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Uterine contractions

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MOA of gold salts

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Alter activity of macrophages and suppress phagocytic activity of PMNs

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SE of ergot alkaloids

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Hallucinations resembling psychosis

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SE of gold salts

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Dermatitis of the mouth aplastic anemia and agranulocytosis

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Ergot alkaloid used as an illicit drug

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LSD

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Causes bone marrow suppression

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Methotrexate

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Dopamine agonist used in hyperprolactinemia

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Bromocriptine

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SE of penicillamine

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Aplastic anemia and renal

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Peptide causing increased capillary permeability and edema

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Bradykinin and histamine

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Interferes with activity of T-lymphocytes

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Hydroxychloroquine

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Mediator of tissue pain, edema, inactivated by ACE, and may be a contributing factor to the development of angioedema

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Bradykinin

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Anti-malarial drug used in rheumatoid arthritis (RA)

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Hydroxychloroquine

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Drug causing depletion of substance P (vasodilator)

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Capsaicin

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SE of hydroxychloroquine

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Retinal destruction and dermatitis

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Prostaglandins that cause abortions

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Prostaglandin E1 (misoprostol) PGE2, and PGF2alpha

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MOA of Leflunomide (newer agent)

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Inhibiting dihydroorotate dehydrogenase which leads to decreased pyrimidine synthesis, decreased T cell proliferation and decreased antibody production by B cells

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Difference between COX 1 and COX 2

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COX 1 is found throughout
the body and COX 2 is only
in inflammatory tissue

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Proteins that prevent action of tumor necrosis factor alpha (TNF-alpha)

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Adalimumab, infliximab and etanercept

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Drug that selectively inhibits COX 2

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Celecoxib and rofecoxib

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Anti-rheumatic agent also used for ulcerative colitis

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Sulfasalazine

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Inhibitor of lipoxygenase

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Zileuton

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Anti-rheumatic agent also used for Chron's disease

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Infliximab

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Major SE of zileuton

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Liver toxicity

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NSAID used in gout

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Indomethacin

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Inhibitor of leukotrienes (LTD4) receptors and used in asthma

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Zafirlukast and montelukast

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NSAID contraindicated in gout

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Aspirin

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Used in pediatrics to maintain patency of ductus arteriosis

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PGE1

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MOA of Colchicine (used in acute gout)

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Selective inhibitor of microtubule assembly

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Approved for use in severe pulmonary HTN

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PGI2 (epoprostenol)

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SE of colchicine

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Kidney and liver toxicity, diarrhea

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Prostaglandin used in the treatment of impotence

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Alprostadil

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Agent used to treat chronic gout by increasing uric acid secretion

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Probenecid and sulfinpyrazone

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Irreversible, nonselective COX inhibitor

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Aspirin

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Allopurinol treats chronic gout by inhibiting

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Xanthine oxidase

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Class of drugs that reversibly inhibit COX

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NSAIDS

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Drug ofter used in combination with TNF - alpha inhitors for RA

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Methotrexate

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Primary endogenous substrate for Nitric Oxidase Synthase

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Arginine

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Initial DMARD of choice for patients with RA

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Methotrexate

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MOA and effect of nitric oxide

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Stimulates cGMP which leads to vascular smooth muscle relaxation

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Long acting beta 2 agonist used in asthma

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Salmeterol

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Muscarinic antagonist used in asthma

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Ipratropium

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MOA action of cromolyn

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Mast cell stabilizer

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Methylxanthine derivative used as a remedy for intermittent claudication

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Pentoxifylline

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MOA of corticosteroids

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inhibit phospholipase A2

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SE of long term (>5 days) corticosteroid therapy and remedy

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Adrenal suppression and weaning slowly, respectively