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97 Cards in this Set

  • Front
  • Back
what inhibits activated X?
1) LMWHeparin
2) fondaparinux
what is HIT?
type 2:
heparin assoc. with platelet factor 4 protein--> IgG binds with this and forms immune complexes --> causes platelet degranulation and more PF4 release-->more IC's form=> THROMBOCYTOPENIA and THROMBOSIS
Heparin (UFH) MOA?
stimulates ANTITHROMBIN III to work faster and inhibit thrombin

* doesn't inhibit thrombin thats already bound to fibrin =DTI's can do that
how do you monitor heparin vs warfarin levels?
Heparin =PPT
Warfarin= PT
what two drug classes work on thrombin?
Heparin- works thru ATIII to inhibit thrombin and therefore coagulation; no effect on fibrin bound thrombin

DTI's-(lepriudin,bivalirudin, argatroban) directly inhibit thrombin including fibrin-bound thrombin
what do you treat HIT (heparin induced thrombocytopenia type II) with?
DTI ==> can inactivate fibrin bound thrombin (can break down already formed clots)

* i.e. lepirudin, bivalirudin, argatroban
heparin vs warfarin
Heparin: parenteral;effective in seconds; doesn't cross placenta; , use PTT to moniter patients; both PT and PTT increased; antagonist is protamine sulfate; LMWH inhibts Xa more than ATIII

Warfarin: Oral; effective 8-12 hours later; crosses placenta; monitor with PT (think PeT="war" dog); both PT and PTT increase; antagonist is Vit.K; narrow TI
causes of B12 def?
pernicious anemia, partial-taotal gasterectomy; malabsorption or resection in distal ileum where B12 absorbed
causes of folate def.?
1) pregnancy
2) alcoholics
3) hemolytic anemia
4) liver dz
5) pts on dialysis
6) drugs (medical)
drugs that cause folic acid def.
1) Methotrexate, Trimethoprim, Pyrimethamine (all inhibit dihydrofolate reductase)
2)long term phenytoin use (rarely causes anemia tho)
ferrous sulfate..oral or parenteral?
Oral
1) ferrous sulfate
2) ferrous gluconate
3) ferrous fumarate

Parenteral
1) iron dextram
2) sodium ferric gluconate complex
3) iron sucrose
Hydroyurea is used to treat ?
1) Sickle Cell
2) CML
3) Polycythemia vera

*increases Fetal Hb and inhibits DNA synthesis
Filgrastim MoA?
G-CSF (stimulates PMN production)
Sargramostin MoA?
GM-CSF ( stimulates myeloid and megakaryocyte progenitors via JAK/STAT receptors)
IL-11...?
Megakaryocyte growth factor
Hydroxycobalamin...?
B12 --> cofactor for many rxns
-treats B12 megaloblastic anemia
Adverse effects of
1) aluminum hydroxide
2) magnesium hydroxide
3) calcium carbonate
1) AlOH -constipation
2)MgOH - diarrhea (Must Go)
3)CaCO3 - kidney stones
which H2 blocker inhibits P450?
Cimetidine

AE-cimetidine binds and inhibits androgen receptors- causes gynecomastia and decreases sperm count (men) and galactorrhea (women)
Omeprazole inhibits metabolism of which drugs?
1)Warfarin
2)Phenytoin
3)Diazepam
4)Cyclosporine
name the Proton Pump Inhibitors
1)Omeprazole
2)Esomeprazole
DOC for erosive gastritis, active duodenal ulcers, long term tx of ZE syndrome?
PPI
1)esomeproazole
2)omeprazole
H2 antagonist MoA?
Competitive and Reversibly blocks the H2 receptor

*histamine receptor on parietal cells of stomach; blocks 90% of acid production with single dose
name cytoprotective drugs?
1) Sucralfate
2) Bismuth Subsalicylate

3) Misoprostol (PGE1 analog)

*all stimulate prostaglandin, mucus and bicarb secretion
what is contraindicated for cytoprotective agents?
-don't take antacids or H2 antagonists b/c cytoprotective agents like bismuth subsalicylate (pepto-bismol) and sucralfate need a low (ACIDIC) pH to become activated
where are PPI absorbed?
- pill has an acid-resistant coat that is removed in alkaline duodenum- pro-drug is absorbed and transported into parietal cell canaliculi --> conversion to active drug

* any enteric coated tablet shouldn't be taken with antacids- coat dissolves too early causing irritation- H2 and PPI)
GPII/III receptor antagonists?
1)Abciximab
2)Eptifibatide
3)Tirofiban
Tirofiban MoA?
-blocks GPII/III receptor on platelets

*receptor normally bind fibronectin, fribrinogen, vitronectin and vWF=>for platelet aggregation
Eptifibatide?
GP II/III recpetor antagonist (blocks platelet aggregation)
name ADP receptor blockers?
1)Clopidogrel
2)Ticlopidine
PDE Inhibitor in platelets?
1)Dipyridamole
Dipyridamole and Warfarin are used together in what condition/situation?
Prophylaxis of thromboemboli in pts with prothetic heart valves

*vaso-dilation and prevention of clot formation respectively
NSAID induced gastric ulcer tx?
1) PPI's
2)H2 blockers
3)misoprostol
PGE1 analog?
Misoprostol--> PGE inhibits secretion of HCL and stimulates mucus and bicarb secretion
what medication that is given for NSAID ulcers is C/I for pregnant patients?
Misoprostol

* causes uterine contractions; often used as an abortive medication
what is used to maintain PDA?
Prostaglandins!

-misoprostol (PGE analog)
name muscarinic agonists used to suppress acid secretion?
1) pirenzepine
2) dicyclomine

*dont confuse dicyclomine with dipyridamole (PDE inhibitor-vasodilator)
irreversible inhibitors of P2Y 12?
ADP receptors (PY2 12) are blocked by
1)Clopidogrel
2)Ticlopidine
when do you use muscarinic antagonists to prevent acid secretion?
pirenzipine -peptic ulcers in refractory cases

dicyclomine- used in IBS
H.Pylori regimens?
1) PPI + clarithromycin+amoxicillan
2)PPI + clarithromycin+metronidazole
3)PPI/Ranitidine + Bismuth+ metronidazole+ tetracycline

* all 10-14 day course
Name the Prokinectic drugs...
1) Metoclopramide
2) Cisapride
Metoclopramide MoA?
D2 receptor antagonist; also mixed 5HT3 antag/5HT4 agonist

*speeds up GI
-used for diabetic gastroparesis; anti-emetic; GERD
-can cause inc. parkinsonian effects;
-C/I in pts with SI obstruction
Cisapride ?
-release Ach in myenteric plexus to increase muscle tone in esophageal sphincter

*used for diabetic gastroparesis (inc. gastric emptying); GERD; bowel constipation
AE: long QT syndrome ->arrthymias
with ketoconazole or erythromycin; diarrhea
name a D2 antagonist that work in the GI?
1)Metoclopramide
Name a drug that increases release of ACH in the myenteric plexus of GI
1) Cisapride
Which GI muscarinic antagonist has poor CNS penetration?
Pirenzepine

*muscarinics work through the M receptors on the parietal cell
What is the difference between pirenzipine and cisapride?
pirenzipine - muscarinic antagonist; used for refractory ulcers

cisapride - prokinectic drug that releases Ach in myenteric plexus
what drugs are given to increase gastric emptying in diabetics?
1) Metoclopramide
2) Cisapride
1) which drug has long QT syndrome?
2) which added drugs predispose these pt to arrthymias?
1)Cisapride
2) Cisapride with erythromycin or ketoconazole

*erthyro and keto are p450 inhibitors
what treats opiod induced constipation?
senna (with docusate)

* stimulant
which laxative is an irritant?
castor oil-->rincinoleic acid-->increases peristalsis

*C/I in pregnant pts
lactulose,PEG, Mg citrate?
osmotic laxatives

PEG- polyethylene gycol is used as coloni lavage for endoscopy/rediological procedures
CHRONIC INGESTION OF THIS ANTACID WITH MILK CAN INDUCE MILK-ALKALI SYNDROME
CALCIUM CARBONATE

(can result in hypercalcemic alkalosis with development of renal calculi)
USED IN THE TX OF GERD, THIS HISTAMINE BLOCKER IN ASSOCIATED WITH GYNECOMASTIA AND GALACTORRHEA
CIMETIDINE

(the stronger blockers, ranitidine and famotidine, don't inhibit P450 system and therefore dont cause anti-androgenic effects)
mechanism of vomiting
1) CTZ of area postrema->outside BBB so can respond to chemicals in blood/CSF
2)vomiting center in medulla-->coordinates motor mechanism of vomiting-->responds from afferent imput from vestibular system,GI, pharynx
HI antagonists..?
1)dimenhydrinate
2)meclizine
3)cyclizine
Procholoroperazine MoA?
class of drug: phenothiazines
- D2 blocker (also metoclopramide)
Emetic Neurotransmitters..?
1)dopamine -->D2 receptors
2) Serotonin --> 5HT3
3)Vagal --> Ach
4)Neurokinin/Sub P in CNS
what do metoclopromide and prochorperazine have in common?
both are D2 blockers

*metoclopromide--> effective against cisplastin which is highly emetogenic; also GERD,Diabetic gastroparesis
prochloroperazine--> used for low/moderate CHEMO vomiting
Tx of motion sickness?
1)scopolamine
2)dimenhydrinate
3)meclizine
4)cyclizine
Chemotherapy anti emetics?
1)5HT3 blockers (Ondansetron, Granisetron, Dolasetron)

2)Phenothiazines (Procholorperazine)

3)Corticosteroids (Dexamethasone, Methyl-prednisolone)

4)Marijuana derivative (Dronabinol, Nabilone)
butyrophenones?
1)Droperidol (prolongs QT)
2)Haloperidol

*block D2 receptors; for refractory cases
benzodiazepines?
1)Lorazepam
2)Alprazolam

(anticipatory vomiting-->low potency)
what blocks Neurokinin/ substance P?
Aprepitant

(usu administered with dexamethasone and palonsetron; extensive CYP3A4 metabolism;can induce it too)
COMMONLY USED ANALGESIC AND ANTI-PYRETIC BUT UNLIKE NSAIDS, HAS NO ANTI-INFLAMMATORY PROPERTIES
ACETAMINOPHEN

(weak inhibitor of COX, it inhibits prstaglandin synthesis in the CNS; a related rpo-drug PHENACITIN, is no longer avaiable due to nephrotoxicity)
USED INT EH MANAGEMENT OF CHRONIC GOUT AND AS AN ADJUNCT TO CANER CHEMO, TO SLOW THE PRODUCTION OF URIC ACID
ALLOPURINOL

(results in suicide inhibition of xanthine oxidase with resultant increase of xanthine and hypoxanthine, both of whihc are more soluable and less likely to for m crystals than uric acid)
NSAID WITH ANTI-PYRECTIC, ANALGESIC, ANTI-PLATELET, AND ANTI-INFLAMMATORY PROPERTIES THAT IRREVERSIBLY INHIBIT COX
ASPRIN

(inhibits the formation of PGE, decreases paina nd fever, and decreases snthesis of PGE in stomach, predisposing to acute gastritis)
USED TOPICALLY FOR THE TREATMENT RHEUMATOID ARTHRITIS BECAUSE IT DEPLETES SUBSTANCE P
CAPSAICIN

(component of chili peppers that impairs release of sub P, the potent neurotranmitter for pain sensation)
NEWLY AVAILABLE NSAID, USED IN THE TX OF RHEUMATOID ARTHRITIS AND OTHER CHRONIC CONDITIOS, WITH A DECREASED RISH OF ULCERS AND OTHER GI BLEEDS
CELECOXIB

(celecoxib and a similar drug, rofecoxib, selectively inhibit cox-2 present only in leukocytes; these agents don't inhibit cox-1 that produces protective prostaglandins int eh stomach; as sulfa drugs they can both cause hypersenitivy reactions)
USED FOR TX OF ACUTE ATTACKS OF GOUTY ARTHRITIS, BECAUSE IT IMPAIRS LEUKOCYTE FUNCTION
CHOLCHICINE

(inhibits microtuble assembly, and therefore leukocyte migration and phagocytosis of uric acid crytals)
USED IN THE TX OF TRANSPLANT PATIENTS AND PATIENTS WITH AUTOIMMUNE DZ'S, AS IT IMPAIRS T CELL PRODUCTION OF IL-2
CYCLOSPORINE

(binds to cyclophilins and inhibits the tanscription of cytokine genes; a similar agent, tacrolimus, binds to the immunophilin FK-binding protein (FKBP) and functions similarly;both display a dose-limiting nephrotoxicity)
A BACTERIAL PRODUCT OF STREP PYOGENES, USED IN THE TX OF CORONARY ARTERY THROMBOSIS
STREPTOKINASE

(complexes with and catalyzes the conversion of plasminogen to plasmin; it is cheaper, although debatably equivalent, agent to tPA)
PLATELET ANTI-AGGREGANT, USED FOR THE PREVENTION OF TRANSIENT ISCHEMIC ATTACKS IN PATIENTS WITH ASPRIN SENSITIVITY
TICLOPIDINE

(interferes with the binding of fibrin to the GPIIa/IIIb receptor blocker (class notes=> ADP blocker))
CREATED THROUGH THE USE OF RECOMBINANT DNA TECHNOLOGY, THIS AGENT IS USED FOR CORONARY ARTERY THROMBOSIS AND ISCHEMIC STROKE
TISSUE PLASMIOGEN ACTIVATOR (tPA) ALTEPLASE/RETEPLASE

(converts fibrin bound plasminogen to plasmin resulting in the dissolution of thrombi)
ORALLY ADMINISTERED ANTICOAGULANT USED IN THE MANAGEMENT AND PROPHYLAXIS OF VENOUS THROMBOSIS, MI AND STROKE
WARFARIN

(coumadin compound that interferes with the vit.k dependent carboxylation of clotting factors 2,7,9,10)
MONOCLONAL ANTIBODY USED AS AN ANTICOAGULANT, PREVENTING RE-STENOSIS AFTER CORONARY ANGIOPLASTY
ABCIXIMAB

(antibodies against the GPII/III receptor on platelets, preventing platelet aggregation)
USED IN THE TREATMENT OF ACUTE BLEEDING IN PATIENTS WITH HEMOPHILIA AND OTHER COAGULAPATHIES
AMINOCAPROIC ACID

(orally active inhibitor of plasminogen activation, thereby inhibiting fibrinolysis, tranexamic acid is a similar agent)
RECOMBINANT PRODUCT USED IN THE TX OF ANEMIA ASSOCIATED WITH RENAL FAILURE
ERYTHROPOIETIN (DARBOPOIETIN/EPOETIN ALPHA)

( also used to tx anemia assoc with bone marrow transplants or toxic drug reactions)
WILL CORRECT THE ANEMIA BUT NOT THE NEUROLOGICAL DEFICITS ASUED BY VIT B12 DEF.
FOLIC ACID
RAPID ACTING IV ADMINISTERED ANTI-COAGULANT USED FOR ACUTE MYOCARDIAL INFARCTION AND PREVENTION OF DVT FOLLOWING PROLONGED IMMOBILIZATION
HEPARIN

(bind to and activate ATIII, resulting in inactivation of thrombin and other clotting factors)
USED IN THE MANAGEMENT OF SICKLE CELL ANEMIA AS WELL AS FOR VARIOUS MYELOID NEOPLASMS
HYDROXYUREA

(increases HbF and als inhibits DNA synthesis by blocking conversion of ribonucleotides to deoxyribinucleotides)
RECOMBINANTLY PRODUCED GRANULOCYTE-MACROPHAGE COLONYSTIMULATIONG FACTOR, USED IN THE MANAGEMENT OF PATIENTS UNDERGOING CHEMO
SARGRAMOSTIM

(similar agent G-CSF filgrastim is used for similar applications but affects on granulocytes)
PROKINETIC DRUF USED TO TX UPPER GI DYSFUNCTION SUCH AS GERD OR GASTROPARESIS WITH DELAYED GASTRIC EMPTYING
CISAPRIDE (aka Propulsid)

(stimulates peristalsis by promoting the release of Ach from post-ganglionic nerves of the myenteric plexus, high does have been assoc with long QT syndrome)
OPIOD DERIVATIVE USED IN TX OF DIARRHEA, B/C THEY SUPPRESS GI MOTILITY
DIPHENOXYLATE, LOPERIMIDE


whereas diphenoxylate is formulated with anti-muscarinic alkaloids; both preparations have minimal abuse potential)
THIS PREPARATION IS USED TO TREAT EMESIS AND NAUSEA ASSOC, WITH CHEMO, AND CONTAINS THE ACTIVE INGREDIENT IN MARIJUANA
DRONABINOL
commonly used pro-emetic agent used in cases of ingestion of caustic substances or mineral oils
ipecac syrup

(orally administered drug that acts directly on the chemoreceptor trigger zone (CTZ) in the medulla)
AMONG THE MOST POPULAR ANTACIDS USED IN THE U.S. NEITHER ABSORBED AND THEREFORE CAUSES NO SYSTEMIC EFFECTS
MG OH or AL OH


(MgOH has a strong laxative effect, AlOH causes constipation
THIS PRO-KINECTIC AGENT IS USED TO PREVENT EMESIS ( I.E. POST-ANESTHESIA OR D/T CHEMO), BECAUSE IT BLOCKS D2 RECEPTORS INT HE AREA POSTREMA THAT TRIGGER VOMITING
METOCLOPRAMIDE

(facilitates Ach, while antagonizing the action of dopamine on teh enteric nervous system. side effects include sedation, diarrhea, and extrapyramidal symptoms)
EICOSANOID PREPARATION USED TO PREVENT PEPTIC ULCERS IN PATIENTS TAKING HIGHER DOSES OF NSAIDS FOR CONDITIONS SUCH AS RHEUMATOID ARTHRITIS
MISOPROSTOL

(PGE analog decreases gastric acid production and increases mucus production, protecting the lining of the stomach)
PPI USED IN THE TX OF GERD, GASTRIC AND DUODENAL ULCERS, H.PYLORI GASTRITIS, AND ZE SYNDROME
OMEPRAZOLE

(irreversibly inhibits the H+/K+ ATPase on the luminal side of the parietal cells)
CENTRAL ACTING ANTI-EMETIC USED TO CONTROL POST-OPERATIVE VOMITING in CHEMO PATIENTS
ONDANSETRON

(5HT3 inhibitor that function at the chemorecoetive area of the area postrema)
USED TO TX PEPTIC ULCERS, BECAUSE IT POLYMERIZES AND SELECTIVELY COATS NECROTIC ULCERATED TISSUE
SUCRALFATE

(requires and acidic envoronment to polymerize, and therefore, can't be used in the presence of antaacids or H2 blockers
USED FOR THE TX OF TRAVELER'S DIARRHEA
BISMUTH SUBSALICYLATE

(helps decrease fluid secretion by the bowel, also used with metronidazole and tetracycline for the tx of H.pylori associated PUD
INHIBITS THE RATE-LIMITING ENZYME OF CHOLESTEROL SYNTHESIS, HMG-CoA REDUCATASE, RESULTING IN DRAMATICALLY DECREASED LDL LEVELS
STATINS (LOVASTATIN,PRAVASTATIN/SIMVASTATIN/ATORVASTATIN)

(may cause elevated liver enzymes, myositis with increased creatine kinase from skeletal muscle and rarely rhabdomyolysis)
ANTI-HYPERLIPIDIDEMIC AGENT THAT MAY PREVENT ATHEROSCLEROSIS BY ACTING AS AN ANTIOXIDANT
PROBUCOL

(rarely used for tx of hyperlipidemia because it decreases HDL's as well as LDLs;may be efficacious in preventing restenosis after angioplasty
LIPID LOWERING AGENT CAUSES CUTANEOUS FLUSHING, WHICH CAN BE AVOIDED BY ADMINISTERING CONCURRENTLY WITH ASPIRIN
NIACIN

(directly reduces secretion of VLDL's from and apoliprotein synthesis by the liver, while increasing HDL's)
AGENTS THAT DECREASE TRIGLYCERIDES DRAMATICALLY BY STIMULATING LIPOPROTEIN LIPASE
GEMFIBROZIL,FENOFIBRATE, CLOFIBRATE


(clofibrate has been associated with gallstones and hepatobiliary neoplasms)
BILE ACID-BINDING RESINS USED IN THE MANAGEMENT OF HYPERLIPIDEMIA
CHOLESTYRAMINE, COLESTIPOL

(bind bile acids, preventing enterohepatic recycling, thus diverting hepatic efforts to renew bile acids, instead of producing plasma lipids)