4th Shifting

C.N. __

SUBJECT : TOPIC : DATE :

PHARMACOLOGY
Blood

20 February 2008

I. Drugs on Blood and Hematopoietic Organs • Hematinic 1. Fe 2+ oral a. Fe fumarate – 100 mg is absorbed b. Fe sulfate c. Fe gluconate 60-65 mg is absorbed -taken daily -induration: minimum of 3 months and maximum of 6 months -disadvantage: only 1/3 is absorbed (elemental iron content) -prescription drugs -overdose toxicity and antidotes: a. Deferoxamine – 500/2000 mg/vial - chelates Fe b. Deferasirox – 125/250/500 mg tab Notes… Iron –Deficiency Anemia – “Hypochromic microcytic anemia” - pallor, weakness -confirmed by: CBC (RBC <4.5 M and Heoglobin <12 g) -double reduction of the iron can lead to severe IDA -treatment: 3-6 mos. • If you lack 1-2 g hemoglobin = 3 mos. tx • If too low hemoglobin = 5-6 mos tx -if taken IV: in gluteus muscle : which causes pain and muscle dystrophy : due to daily administration, can lead to brown and black discoloration of gluteus -effects of food on the absorption of these drugs: a. High protein diet (meat)
BY : SUBJECT : Yna and Kring

- enhance the iron absorption in small intestines - vegetarians (who eat phosphatecontaining veggies) can’t absorb iron b. Antacids - Magnesium aluminum hydroxide inhibits iron absorption (chelation) c. Antibiotic - eg. Tetracycline inhibits iron absorption (chelation) d. Vitamin C/ Ascorbic acid -potentiates 2. Fe parenteral a. Imferon/ Fe Dextran - technique of injxn: “Z” track IM / IV after ANST (a negative skin test) - IV can produce allergy - disadvantage: painful if IM Fe sucrose/ Fe-Na gluconate complex IV - alternative for imferon/Fe dextransensitive patients - by IV only - there may be allergy, but less - Adverse effects: i. chronic iron overload ii. hemorrhagic gastroenteritis iii. melena (due to excess of injectible iron) - Antidote: phlebotomy (popliteal/femoral veins) Notes… • Transferrin – free iron • Myoglobin – iron in the muscles • Ferritin – stored iron • Hemosiderosis – increased iron in reticuloendothelial cells • Hemochromatosis – increased iron in pancreas, liver
PAGE : SUBJECT : 1 of 4

b.

Medicine I- Hemiplegia

Yna and Kring

3. Others  Cu – supplements  Co – as Vitamin B12; combined with folic acid to treat megaloblastic anemia  Blood Products 1. Whole Blood – best; if px did not respond to oral/parenteral iron preparations 2. RBC – mild anemia 3. Platelet concentrate – hemorrhagic dengue; <50,000 platelts 4. plasma expanders or LRS – 100,000-200,000 platelets

-Goal of anticoagulants: To maintain fluidity A. Anticoagulants 1. Indirect Antithrombin - parenterals a. Heparin – high MW b. Enoxaparin c. Delteparin new low MW d. Tinzaparin - monitor dose (aPTT and PT) - toxicity: hemorrhage -safe in pregnancy -reversal of toxicity/antidote for heparin: Protamine Sulfate 2. Direct Anti-thrombin -crosses the BBB; contraindicated for pregnancy a. Hirudin [blocks thrombin] (Lepiridin – from leech)/ Bivalirudin b. Argatrotan (synthetic drug)/ Ximelagatran (active form – “melagatran”) -antidote for a & b is Protamine Sulfate c. Warfarin/Coumarin – oral - adverse effects: hemorrhage, and even the infant is affected (give phytonadione or Vit K1 10 mL) - Toxicity: hemorrhage, affect infants, infarction esp in lower extremity  purple toe infarction - monitor: PT Drug Interactions: - PT: Cimetidine, Amiodarone, Metronidazole, Fluconazole, Cotrimoxazole, ASA, 3rd Gen Cephalosporins - PT: Barbiturates, Cholestyramine, Rifampin, Vitamin K, Diuretics (Furosemide and Thiazide) - reversal/antidote: Vit K1 (Phytonadione) B. Thrombolyitc / Fibrinolytic -IV lahat -MOA: enhance plasminogen conversion to plasmin -From streptococci and urine
PAGE : SUBJECT : 2 of 4

Notes… • Megaloblastic Anemia - dse: due to lack of Vit B12 and folic acid -caused primarily by drugs such as: methotrexate, 5-FU, phenytoin, antifolate drugs -prophylaxis: Leucovorin Ca (Folinic acid) -clinical correlation (Vit B12 def): neurologic (ataxia, paresthesia, sensory deficits) • Pernicious Anemia - due to Vit B12 deficiency (operation in gastric mucosa where secretion of Vit B12 takes place and due to operation in the ileum where absorption takes place) - results to atrophy of the stomach and severe anemia -diagnosis: “Schilling Test” – use radioactive Vit B12

II. Drugs for Coagulation Disorders
BY : SUBJECT : Yna and Kring

Medicine I- Hemiplegia

Yna and Kring

-DOC for AMI a. Anistreplase b. Reteplase c. Alteplase d. Tenecteplase (a,b,c, and d are tPAs + synthetics) e. tPAs (endogenous) – natural - Antithrombotic: prophylaxis against acute coronary syndrome - ASA: inhibit TXA2, PG (irreversible)  80mgdaily -Clopidogrel/ticlopidine: inhibit ADP pathway of coagulation  75mg/daily -Tirofiban(available in the Philippines) / Abciximab / Eptifibatide: Inhibit GPIIBIIIA receptor -Dipyridamole: inhibit phosphodiesterase and CGMP, enhance endogenous adenosine (di na ginagamit) -Cilostazol: antiplatelet vasodilator  intermittent claudication -Doctors recommend combination: ASA+clopidogrel or Clopidogrel+tirofiban -Favors Clotting: Hemorrhage -Coagulant: Vit. K MOA: favors clotting of factors II, VII, IX and X -Vit K1: phytonadione warfarin antidote, for newborn -Vit K2: menaquinone synthesized by bacteria in small intestine -Vit K3: menadione  synthetic -plasma fraction: if one of the above is not effective -monitor: fibrinogen, PT - Cryoprecipitate/Humate-P, Desmopressin acetate, Antoplex+FEIBA (factor VIII inhibitory bypassing action) tx for hemophilia A

- Traxenamic acid (Hemostan) - Aminocaproic acid (Amicar) CI: DIC/Gut bleeding -Serine-Protease-Inhibitor (SERPIN) -Aprotinin -open heart surgery D. Hemopoietic Growth Factor -Erythropoietin (Epoietin-A) in JG cell -DOC for chronic renal failure with anemia -Myeloid Growth Factor -DOC for aplastic anemia -G-CSF (Filgrastin): ADR is bone pain -GM-CSF (Sargramostim): better but has fatal ADR which is capillary leak syndrome -Megakaryocyte Growth Factors -IL-11 (Oprelvekin): DOC for thrombocytopenia -Thrombopoietin IMMUNOLOGICALS (Vaccines) • ACTIVE Immunizations - Bacteria  Typhoid 21-A live bacteria  Typhoid Vi Bacterial polysaccharide  Typhoid heat-phenol inactivated bacteria  PTAP Inactivated Bacterial toxoid  Cholera Inactivated Bacteria  Hib conjugated bacteria polysaccharide  Meningococcal bacteria polysaccharide  Pneumococcal bacteria polysaccharide - VIRUS  Live • MMR
PAGE : SUBJECT : 3 of 4

C. Fibrinolytic Inhibitors -MOA: inhibit plasminogen to plasmin
BY : SUBJECT : Yna and Kring

Medicine I- Hemiplegia

Yna and Kring

• • • 

OPV Varicella Yellow Fever

Inactivated • Hep A • Hep B • IPV • Influenza • Rabies • Rota V

-

PASSIVE Immunizations  Botulism – antitoxin, equine  Diphtheria – antitoxine, equine  Tetanus – antitoxin/IG-IM  Snake Bites – antivenim/equine IV-IM  Varicella – VZ- IG IM  Rubella - IGIM  CMV - IGIV  Hep A - IGIM  Hep B – HIB-IM  HIV infant - IGIV  Kawasaki - IGIV  Measles - IGIM  Rabies - IGIM  RSV – IGIV  RSV pneumonia – palivizumab -IM

BY : SUBJECT :

Yna and Kring

PAGE : SUBJECT :

4 of 4