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Pharmacology > Autacoids - DMARDS, NSAID, Gout Drugs > Flashcards

Autacoids - DMARDS, NSAID, Gout Drugs Flashcards

0
Q

Two most important amine autacoids

A

Histamine and Serotonin

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1
Q

Refers to endogenous molecules with powerful pharmacologic effects that do not fall into traditional autonomic groups

A

Autacoids

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2
Q

Histamine is formed from what amino acid?

A

Histidine

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3
Q

Enzymes that metabolizes the histamine

A

Monoamine oxidase and diamine oxidase

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4
Q

Triple response effect of histamine

A

Wheal, flush and flare

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5
Q

H1-receptor antagonists (1st generation): used for hay fever, angioedema, motion sickness, insomnia and dystonia. With drowsiness as sideeffect

A

Diphenhydramine - competitive block of peripheral and CNS H1 receptor

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6
Q

H1-receptor antagonist-2nd gen: used for urticaria, hay fever and angioedema. With no autonomic or anti-motion sickness effects

A

Cetirizine

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7
Q

H2-receptor antagonist used for peptic ulcer disease and Zollinger - Ellison syndrome and GERD. CYP450 inhibitor

A

Cimetidine - block H2 receptor, reduction of gastric acid secretion. Cimetidine has antiandrogen effect like gynecomastia

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8
Q

Serotonin is produced from what amino acid?

A

Tryptophan

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9
Q

Serotonin is metabolized by

A

Monoamine oxidase

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10
Q

Excess serotonin in the body is detected by ___ in the urine.

A

5-hydroxyindole acetic acid (5-HIAA)

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11
Q

5-HT receptor agonist: drug of choice for acute migraine, cluster headache. SE: paresthesias and dizziness

A

Sumatriptan - causes vasoconstriction hence modulates neurotransmitter release

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12
Q

5-HT3-receptor antagonist used for chemotherapy and postoperative vomiting. SE: diarrhea, headache

A

Ondansetron - blocks chemoreceptor trigger zone and enteric nervous system

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13
Q

Area distribution block by Ondansetron

A

Area postrema

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14
Q

Responsible for the St. Anthony’s fire described during middle ages

A

Ergot alkaloids - produced by a fungus found in wet or spoiled grain

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15
Q

5-HT2 vasoselective receptor antagonist used in migraine and cluster headache

A

Ergotamine - agonist causes marked smooth muscle contraction but blocks a-agonist vasoconstriction

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16
Q

Antidote used for Ergotamine

A

Nitroprusside

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17
Q

5-HT uteroselective antagonist used for postpartum bleeding and migraine. SE: IG upset, uterine spasm and abortion

A

Ergonovine

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18
Q

Refers to important group of endogenous fatty acid derivatives that are produced from arachnoid acid

A

Eicosanoids

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19
Q

Eicosanoids: bronchoconstriction, slow-reacting substance of anaphylaxis

A

LTC4 and LTD4

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20
Q

Eicosanoids: protective effects on gastric mucosa, maintain PDA

21
Q

Eicosanoids: maintains PDA, increases uterine tone

22
Q

Eicosanoids: platelet aggregation

23
Q

Prostaglandin E1 analog used for PUD, recurrent NSAID induced gastric mucosal injury and abortifacient. SE: teratogenic effect (Moebius sequence)

A

Misoprostol - activates EP receptors causes uterine contraction and increase HCO3 mucus secretion in stomach

24
Q

Prostaglandin E1 analog, used in maintenance of patent ductus arteriosus and erectile dysfunction.SE: priapism

A

Alprostadil - causes vascular smooth muscle relaxation and vasodilation

25
Q

Prostaglandin E2 analog for induction of labor (cervical ripening), abortifacient

A

Dinoprostone - low concentration contract, higher concentration relax uterine and cervical smooth muscle

26
Q

Prostaglandin F2a analog used for control of postpartum hemorrhage, abortaficient

A

Carboprost - activates FP receptors

27
Q

Prostaglandin F2a analog used for Glaucoma. SE: alters color of the iris, causing permanent eye color change

A

Latanoprost - activates FP receptors increases outflow of aqueous humor, reduces intraocular pressure

28
Q

NSAID not used for patients with gout since it prevents uric acid excretion

29
Q

At what dose of Aspirin follows zero order elimination kinetics?

A

High dose - 2400 to 4000 mg/d will have anti-inflammatory effects

30
Q

At what dose of aspirin, follows first order elimination kinetics, and effective in reducing platelet aggregation

A

Low range - <300mg/d

31
Q

NSAID, nonselective reversible COX-1 and COX-2 inhibitor. And inhibits prostaglandin synthesis used for analgesia, antipyretic and antiinflammatory. Long term use reduces risk for colon cancer

A

Ibuprofen - SIMD: Diclofenac, Meloxicam, Mefenamic acid

32
Q

NSAID drug, nonSelective COX inhibitor, for post - surgical analgesic control. Only IV NSAID, use generally restricted to 72 hours only

33
Q

Nonselective NSAID for closure of the PDA

A

Indomethacin

34
Q

COX-2 selective NSAID, for analgesia, antipyretic and anti inflammatory.

35
Q

COX-3 inhibitor,for mild analgesia and antipyretic. Increased hepatotoxicity with alcohol use. Preferred antipyretic in children

A

Paracetamol - Acetaminophen

36
Q

Antidote for Paracetamol toxicity

A

N - acetylcysteine

37
Q

Toxic and lethal dose of Paracetamol

A

Toxic dose: 150mg/kg

Lethal dose: 15g

38
Q

It is the most common form of chronic inflammatory arthritis

A

Rheumatoid arthritis

39
Q

DMARD, chemotherapeutic drug, first choice to treat rheumatoid arthritis. It may cause pseudolymphomatous reaction

A

Methotrexate

40
Q

Rescue agent for Methotrexate

A

Leucovorin - folinic acid

41
Q

DMARD for Crohn’s disease, RA. May cause reactivation of latent tuberculosis. With synergistic effect with methotrexate

A

Infliximab

42
Q

DMARD, for rheumatoid arthritis, Psoriatic arthritis. May cause bone marrow suppression. Cannot give with Allopurinol

A

Azathiopine

43
Q

DMARD, antimalarial drug, for RA, SLE, Sjogrens syndrome and Malaria. Safe for pregnant women

A

Chloroquine

44
Q

DMARD, chemotherapeutic drug for RA, SLE, vasculitis. May cause hemorrhagic cystitis

A

Cyclophosphamide

45
Q

Rescue agent for Cyclophosphamide?

46
Q

DMARD, for RA, inflammatory bowel disease, JRA and ankylosing spondylitis

A

Sulfasalazine

47
Q

Antigout drug, also a microtubule assembly inhibitor for gout and mediterranean fever. May cause agranulomatosis

A

Colchicine

48
Q

Uricosuric agent, antigout drug cause increase uric acid excretion. May precipitate acute gout during early phase of drug action

A

Probenecid - coadministering colchicine to prevent acute gout

49
Q

Xanthine oxidase inhibitor, first line for chronic gout, tumor lysis syndrome. Inhibits metabolism of mercaptopurine and azathioprine

A

Allopurinol

Pharmacology (11 decks)

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