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Anticoagulants, Antiplateletes & Hematinics
Anticlotting drugs
Anticoagulants - ↓ blood coagulation
• Oral WARFARIN
• Parenteral: HEPARINS & HIRUDIN
Antiplatelets - ↓...
WARFARIN
Mech of action:
•Inhibits the synthesis of Vit K
•Delayed onset of action (8-12hrs) due to presence of
preformed ...
Drug interactions:
Prothrombin Time (  risk of bleeding)
• Hepatic microsomal inhibitors (↓ Metabolism ↑toxicity)
Cimeti...
WARFARIN
Adverse effects:
• Hemorrhage ( Needs lab monitoring)
• Teratogenicity-Craniofacial deformities, Intracranial
hem...
Heparins
UNFRACTIONATED HEPARIN
MOA:
• Binds Antithrombin III & potentiates its action 1000 times
(Antithrombin III inhibi...
Heparins
Uses : Prevention & treatment of Deep vein thrombosis,
Pulmonary embolism, Acute MI, & Unstable angina.
Adverse e...
Heparins
Low Molecular Weight HEPARINS; Enoxaparin, Dalteparin
Advantages
• ↑ Bioavailability from SC inj,
• Long duration...
Direct Thrombin Inhibitors
HIRUDIN obtained from medicinal leeches (Hirudo medicinalis)
• Inhibits Thrombin (IIa)
• Admini...
Antiplatelet drugs
Inhibit Platelet aggregation thereby ↓ thrombus formation
ASPIRIN (Acetyl Salicylic Acid)
• At low dose...
Antiplatelet drugs
CLOPIDOGREL/TICLOPIDINE
• Inhibit ADP mediated platelet aggregation
• Synergistic action with Aspirin
U...
Haematinics
• Substances required in the formation of blood cells& their
deficiency results in anemia.
• Vit B12, Folic ac...
Vitamin B12
Preparations :
Parenteral : Cyanocobalamine & Hydroxycobalamin
Oral : Methylcobalmin
•Prophylaxis & treatment ...
Folic acid
Deficiency:
•Dietary deficiency, ↑ demand (children, pregnancy & lactation).
•Malabsorption
• Drug induced. Met...
Iron
Preparations of iron:
Oral Parenteral
-Ferrous sulfate Iron dextran i.m/i.v
-Ferrous fumerate Iron sorbitol-citric-ac...
Iron
Indications for parenteral iron therapy:
•Intolerance to oral iron.
•Failure to absorb oral iron- severe malabsorptio...
Erythropoietin
• Its secretion ↓in patients with renal failure.
• Preparation : Recombinant human erythropoietin I.V/S.C.
...
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1 anticoagulant, antiplatelets & hematinics for dentistry

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Pharmacology
Third Year

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1 anticoagulant, antiplatelets & hematinics for dentistry

  1. 1. Anticoagulants, Antiplateletes & Hematinics
  2. 2. Anticlotting drugs Anticoagulants - ↓ blood coagulation • Oral WARFARIN • Parenteral: HEPARINS & HIRUDIN Antiplatelets - ↓ platelete aggregation & thrombus formation • TXA2 Inhibitor: ASPIRIN • ADP Inhibitors: CLOPIDOGREL
  3. 3. WARFARIN Mech of action: •Inhibits the synthesis of Vit K •Delayed onset of action (8-12hrs) due to presence of preformed clotting factors in the circulation. •Therapeutic effect is monitored by Prothrombin time & International Normalized Ratio.
  4. 4. Drug interactions: Prothrombin Time (  risk of bleeding) • Hepatic microsomal inhibitors (↓ Metabolism ↑toxicity) Cimetidine, Metronidazole, Ciprofloxacin, Ketoconazole • Displacement from plasma protein ( Sulfonamides ↑toxicity) Prothrombin Time ( therapeutic effects) • Hepatic microsomal Inducers ( ↑ Metabolism & ↓ efficacy) Phenytoin, Carbamazepine, Rifampicin • Cholestyramine (↓ Absorption of Warfarin) WARFARIN
  5. 5. WARFARIN Adverse effects: • Hemorrhage ( Needs lab monitoring) • Teratogenicity-Craniofacial deformities, Intracranial hemorrhage • Fat necrosis - skin, breast, fatty tissues. Antidote : Inj. Vit K1 (Phytonadione). Uses : Prophylaxis of • Thromboembolism in Atrial fibrillation • Deep Vein Thrombosis • Thrombosis on Prosthetic heart valves • Extracorporeal circulation Contraindications; Pregnancy & Lactation
  6. 6. Heparins UNFRACTIONATED HEPARIN MOA: • Binds Antithrombin III & potentiates its action 1000 times (Antithrombin III inhibits thrombin (IIa),VIIa, IXa, & Xa) • Rapid onset of action because it acts on preformed clotting factors. • Therapeutic effect is monitored by Activated Partial Thromboplastin Time PK; Given by SC/IV ( IM = Hematomas, to be avoided) • No transplacental passage - safe during pregnancy
  7. 7. Heparins Uses : Prevention & treatment of Deep vein thrombosis, Pulmonary embolism, Acute MI, & Unstable angina. Adverse effects • Haemorrhage (Needs lab monitoring) • Heparin induced Thrombocytopenia (HIT) – > 8 days of therapy • Hypersensitivity • Alopecia • Osteoporosis (> 6 months of therapy) Antidote : Inj Protamine sulphate
  8. 8. Heparins Low Molecular Weight HEPARINS; Enoxaparin, Dalteparin Advantages • ↑ Bioavailability from SC inj, • Long duration of action • Less thrombocytopenia Contraindications of Heparin: • Hypersensitivity to the drug, • Bleeding disorder, • Severe hypertension, • Intracranial hemorrhage, • Ulcerative lesions of GIT,
  9. 9. Direct Thrombin Inhibitors HIRUDIN obtained from medicinal leeches (Hirudo medicinalis) • Inhibits Thrombin (IIa) • Administered by IV, • Therapeutic effects monitored by aPTT USES: In patients with thrombosis related to Heparin induced thrombocytopenia Adverse effects: Bleeding & Hypersensitivity
  10. 10. Antiplatelet drugs Inhibit Platelet aggregation thereby ↓ thrombus formation ASPIRIN (Acetyl Salicylic Acid) • At low doses (75-100 mg) inhibits Cyclo-oxygenase by irreversible acetylation  ↓TXA2 synthesis – TXA2 stimulates platelet aggregation USES; • Prophylaxis-Post MI, Cerebral thrombosis, TIA Adverse effects: Bleeding, GI upset,
  11. 11. Antiplatelet drugs CLOPIDOGREL/TICLOPIDINE • Inhibit ADP mediated platelet aggregation • Synergistic action with Aspirin Uses: Similar to Aspirin & in patients who can not tolerate Aspirin Adv effects (Ticlopidine): • Bleeding, • Severe neutropenia, • Thrombotic thrombocytopenic purpura.
  12. 12. Haematinics • Substances required in the formation of blood cells& their deficiency results in anemia. • Vit B12, Folic acid & Iron (Maturation factors for blood cells) Vitamin B12 • Essential for the synthesis of DNA. • Deficiency causes Megaloblastic anemia – Immature red cells in the blood & bone marrow. .
  13. 13. Vitamin B12 Preparations : Parenteral : Cyanocobalamine & Hydroxycobalamin Oral : Methylcobalmin •Prophylaxis & treatment of Megaloblastic anemia (B12 def.) •Pernicious anemia – Given by i.m lifelong. •Prophylaxis during pregnancy & lactation ( ↑ demand)
  14. 14. Folic acid Deficiency: •Dietary deficiency, ↑ demand (children, pregnancy & lactation). •Malabsorption • Drug induced. Methotrexate, Cotrimoxazole & Trimethoprim. Manifestations - Megaloblastic anemia, glossitis, diarrhea & weakness Uses: •Treatment of Megaloblastic anemia – given along with vit. B12. •Prophylaxis during pregnancy, lactation, infancy •Prevention of Methotrexate induced toxicity – (Folinic acid or Leucovorin rescue)
  15. 15. Iron Preparations of iron: Oral Parenteral -Ferrous sulfate Iron dextran i.m/i.v -Ferrous fumerate Iron sorbitol-citric-acid i.m -Ferrous gluconate Sodium ferric gluconate i.v. •Ferrous succinate Adverse effects: Oral route: Epigastric pain, vomiting, metallic taste, constipation (due to astringent effect) staining of teeth & black colored stool Parenteral route: pain & discoloration of skin at the injection site, Arthralgia, lymphadenopathy, Urticarial rash & Anaphylaxis
  16. 16. Iron Indications for parenteral iron therapy: •Intolerance to oral iron. •Failure to absorb oral iron- severe malabsorption,etc •Non-compliance to oral iron •Severe anemia (pregnancy). •Severe deficiency with bleeding. •Along with erythropoietin in patients with renal disease. Antidote : Desferroxamine ( Fe chelating agent)
  17. 17. Erythropoietin • Its secretion ↓in patients with renal failure. • Preparation : Recombinant human erythropoietin I.V/S.C. Uses: • Anemia of chronic renal failure • Anemia in AIDS patients treated with Zidovudine • Anemia of Cancer chemotherapy Adverse effects: • Flu like syndrome, Hypertension

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