Drugs affecting blood

Июль 27, 2022

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Drugs affecting blood

Содержание

2. Principal Causes of a Disturbance of Erythropoiesis : 1. Hemoglobin synthesis is impaired - in Fe2+
4. Agents Affecting Erythropoesis I. Agents Stimulating Erythropoiesis 1. Used in Hypochromic Anemias A. IN iron-deficient anemias:
5. 2. In HYPERCHROMIC Anemias: Vitamin B12 (Cyanocobalamin) amp. 0.01%, 0.05%-1 ml Folic Acid [Vit Bc, B9]
6. Iron Agents: Ferrous Sulfate, Ferrous Lactate, Fercoven, Ferrum Lek - contain the divalent Fe2+ that is
7. Fercoven (amp. 5 ml) contains 20 mg of Saccharate Iron and 0.09 mg of Gluconate Cobalt
9. OVERDOSE with Fe2+ COMPOUNDS Manifestation: lethargy, nausea and vomiting green then tarry stools, weak and rapid
10. HEMATOPOIETIC GROWTH FACTORS: ▶ ERYTHROPOETIN ▶ Granulocyte Colony-Stimulating Factor - G-CSF, Filgrastim ▶ Granulocyte-Macrophage Colony-Stimulating Factor
11. Erythropoietin (Epoetin alfa) – vial 2000, 4000, and 10,000 IU/ml IV, SC Human erythropoietin, produced by
12. Filgrastim (G-CSF) is lineage-specific growth factor – ● supports Proliferation, Differentiation and Functional Activity of neutrophils
13. Molgramostim (GM-CSF) has broader actions than G-CSF. ● stimulates Proliferation and Differentiation of Granulocytic Progenitor Cells
14. Folate Deficiency: 1) Increased Demand (pregnancy and lactation) 2) Poor Absorption caused by pathology of the
15. The minimal requirement: ≈ 1 μg/day.
16. AGENTS AFFECTING LEUCOPOIESIS 1. Agents Stimulating Leucopoiesis: Sodium nucleinate Pentoxyl Methyluracil Molgramostim Filgrastim 2. Agents Inhibiting
17. AGENTS USED FOR PROPHYLAXIS AND TREATMENT OF THROMBOSIS 1. PLATELET AGGREGATION INHIBITORS 2. ANTICOAGULANTS 3. THROMBOLYTIC
18. PLATELET AGGREGATION INHIBITORS (ANTIPLATELET AGENTS): Aspirin, Ticlopidine, Dipyridamole, Pentoxifylline, Abciximab Clinical Uses: AMI, Prior MI, Unstable
20. ASPIRIN blocks Thromboxane A2 synthesis from arachidonic acid in platelets by irreversible Acetylation and Inhibition of
21. Ticlopidine and Clopidogrel inhibit the ADP pathway involved in the binding of platelets to fibrinogen and
22. Dipyridamole (Curantil, Persantine) is a coronary vasodilator which was introduced for Angina Pectoris. Mechanism of action:
23. Pentoxifylline (Trental) inhibits PDE, ?Platelet and Erythrocytes Aggregation, has desaggregational properties, enhances fibrinolysis, lowers viscosity, IMPROVES
24. ABCIXIMAB ReoPro 2 mg/ml IV injection a Humanized Monoclonal Antibody directed against the platelet Glycoprotein IIb/IIIa
25. II. ANTICOAGULANTS: 1. DIRECT ACTION HEPARIN - amp 5 ml – 5000 U/ml and 10000 U/ml
26. Heparin Mechanism of action: acts indirectly by binding to Antithrombin III. The Heparin-AT III complex binds
28. CONTRAINDICATIONS to Heparin: Bleeding Disorders, Thrombocytopenia Hypertension, Threatened Abortion, Piles, Ulcers Subacute Bacterial Endocarditis Large Malignancies,
29. ADVERSE EFFECTS of HEPARIN: 1. Bleeding complications. Excessive bleeding may be managed by suspending the drug
30. Clinical uses of Heparin: Pulmonary Embolism and Deep Vein Thrombosis Myocardial Infarction and Unstable Angina Prevention
31. Vitamin K is regenerated from the epoxide by vitamin K Epoxide Reductase. It is the enzyme
32. Clinical Uses of Neodicumarin: Thrombophlebitis Deep Vein Thrombosis Myocardial Infarction Artificial Heart Valves ⮚ Atrial Arrhythmias
33. FIBRINOLYTIC (THROMBOLYTIC) DRUGS I. Non-selective Activators of Profibrinolysin: Streptokinase Urokinase Streptodekase II. Selective activators of Profibrinolysin:
34. Streptokinase (amp 250,000 and 500,000 IU) - a non-selective Activator of Profibrinolysin, the enzyme extracted from
35. Alteplase and Duteplase - recombinant tissue-type Plasminogen Activator (t PA) - act selectively on plasminogen, bound
36. Agents to Treat Bleeding (Hemostatics) 1.Agents enhancing Coagulation of blood: for Local Application: Thrombin - amp
37. Adroxon (amp. 0.025% 1 ml) Hemostatic action It is used to stop capillary and parenchymatous bleeding
38. Ethamsylate (Dicynon) – amp. 12.5% 2 ml IV or IM, Caps. 0.25 g Antihyaluronidase Action –
39. 2. ANTIFIBRINOLYTIC AGENTS Inactivation of the Fibrinolytic System can be achieved by Plasmin Inhibitors : Aminocaproic
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Principal Causes of a Disturbance of Erythropoiesis :
1. Hemoglobin synthesis is

impaired -
in Fe2+ deficiency –
Microcytic Hypochromic Anemia.
2. Cell multiplication is inhibited –
DNA synthesis is insufficient -
in deficiencies of Vitamin B12 or Folic Acid
- Macrocytic [Megalocytic]
Hyperchromic Anemia

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Agents Affecting Erythropoesis
I. Agents Stimulating Erythropoiesis
1. Used in Hypochromic Anemias
A.

IN iron-deficient anemias:
a) Iron Agents:
Ferrous sulfate – caps. 0.25 g
Ferrous Lactate – pulv., PO 1 g
Fercoven – amp. 5 ml
Ferrum Lek - amp 5 ml
b) Cobalt agents:
Coamid – amp. 1%-1 ml
Fercoven
B. Hematopoietic Growth Factor:
Erythropoietin - vial 2000, 4000, 10,000 IU/mL

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2. In HYPERCHROMIC Anemias:
Vitamin B12 (Cyanocobalamin)
amp. 0.01%, 0.05%-1 ml
Folic Acid

[Vit Bc, B9] – Tab. 1 mg
II. AGENTS INHIBITING ERYTHROPOIESIS:
Sodium Phosphate liquor labelled Phosphor-32

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Iron Agents:
Ferrous Sulfate, Ferrous Lactate, Fercoven, Ferrum Lek -
contain the

divalent Fe2+ that is markedly better absorbed than trivalent Fe3+ .
Uptake is efficient in the form of heme (present in hemo- and myoglobin).
Iron is stored in intestinal mucosal cells as ferritin
(an iron/protein complex) until needed by the body and passed on to the transport protein - transferrin,
a β1-glycoprotein.
The transferrin–iron complex undergoes endocytotic uptake mainly into erythroblasts to be utilized for Hb synthesis.

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Fercoven (amp. 5 ml) contains 20 mg of Saccharate Iron and

0.09 mg of Gluconate Cobalt in 1 ml.
It is introduced IM slowly (for 8–10 min) once a day
during 10–15 days; first 2 injections – 2 ml, then – 5 ml.
Ferrum Lek (5 ml containing 100 mg of Saccharate Iron) is administered IM or IV.
Interactions: Antacids inhibit iron absorption.
Adverse effects: GI disturbances (epigastric pain, diarrhea, constipation) caused by local irritation necessitates the intake of iron preparations with or after meals.
Adverse effects with IM injection are persistent pain
at the injection site and skin discoloration;
with IV injection: flushing, hypotension, anaphylactic shock.

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OVERDOSE with Fe2+ COMPOUNDS
Manifestation: lethargy, nausea and vomiting green then

tarry stools, weak and rapid pulse, hypotension, dehydration, acidosis, and coma.
Treatment: support of airway, respiration, and circulation. Gastric lavage, using a 1% Sodium Bicarbonate solution, to convert iron to less irritating, poorly absorbed form.
Deferoxamine (powder for injection: 0.5 g) -chelates IRON by binding ferric ions to
the 3 hydroxamic groups of the molecule
[1 g IM].

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HEMATOPOIETIC GROWTH FACTORS:
▶ ERYTHROPOETIN
▶ Granulocyte Colony-Stimulating Factor -
G-CSF, Filgrastim
▶ Granulocyte-Macrophage Colony-Stimulating

Factor - GM-CSF, Molgramostim

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Erythropoietin (Epoetin alfa) – vial 2000, 4000, and 10,000 IU/ml IV,

Human erythropoietin, produced by
recombinant DNA technology
● Stimulates Erythroid Proliferation and Differentiation by interacting with Specific Erythropoietin Receptors
on red cell progenitors.
● Induces release of Reticulocytes from the bone marrow.
Clinical uses: anaemia caused by end-stage renal disease,
HIV-infection, and anaemia in some cancer patients.

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Filgrastim (G-CSF) is lineage-specific growth factor –
● supports Proliferation, Differentiation and

Functional Activity of neutrophils causing a rapid rise in leucocytes within 2–3 days in patients with normal bone marrow function or 7–14 days in patients with bone marrow suppression.
Clinical uses: to decrease incidence of infection
● after cancer chemotherapy for non-myeloid malignancies,
● chronic severe neutropenia,
● after bone marrow transplantation in cancer patients;
● agranulocytosis, pancytopenia, acute leukaemia, myelodysplastic syndrome,
● hematologic toxicity with drug therapy.

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Molgramostim (GM-CSF) has broader actions than G-CSF.
● stimulates Proliferation and Differentiation

of Granulocytic Progenitor Cells as well as Erythroid and Megakaryocyte progenitors.
● increases functional activity of mature neutrophils, enhancing phagocytosis.
GM-CSF acts together with IL-2 to stimulate T cell proliferation and appears to be a locally active factor
at the site of inflammation.
● mobilizes peripheral blood stem cells, but it is significantly less efficacious than G-CSF in this regard.
● enlarges the extent of expression of “respiratory explosion” (ensuring formation of 90% active forms of O2 and which is one of the most important mechanisms of phagocytosis).

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Folate Deficiency:
1) Increased Demand (pregnancy and lactation)
2) Poor Absorption
caused by

pathology of
the small intestine
3) Alcoholism
4) Treatment with drugs that are Dihydrofolate Reductase Inhibitors –
Methotrexate Trimethoprim
Biseptol
A primary result of folic acid deficiency is Megaloblastic Anemia

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The minimal requirement: ≈ 1 μg/day.

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AGENTS AFFECTING LEUCOPOIESIS
1. Agents Stimulating Leucopoiesis:
Sodium nucleinate
Pentoxyl
Methyluracil
Molgramostim

Filgrastim
2. Agents Inhibiting leucopoiesis:
Cyclophosphamide
Dopan
Chlorambucil
Myelosan
Mercaptopurine
Methotrexate

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AGENTS USED FOR PROPHYLAXIS AND TREATMENT OF THROMBOSIS
1. PLATELET AGGREGATION

INHIBITORS
2. ANTICOAGULANTS
3. THROMBOLYTIC AGENTS

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PLATELET AGGREGATION INHIBITORS (ANTIPLATELET AGENTS):
Aspirin, Ticlopidine, Dipyridamole,
Pentoxifylline, Abciximab
Clinical Uses:

AMI, Prior MI,
Unstable or Stable Angina,
Stroke,
Transient Ischemic Attack,
Arterial Bypass Surgery,
Angioplasty,
Peripheral Vascular Disease.

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ASPIRIN blocks Thromboxane A2 synthesis from arachidonic acid in platelets by

irreversible Acetylation and Inhibition of COX –
a key enzyme in PG and TxA2 synthesis.
ASPIRIN 75 - 325 mg/day
is the Most Widely Tested Regimen.

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Ticlopidine and Clopidogrel inhibit the ADP pathway involved in the binding

of platelets to fibrinogen and
to each other.
Adverse Effects:
Prolonged Bleeding
Neutropenia
They are reserved for patients
who cannot tolerate ASPIRIN.

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Dipyridamole (Curantil, Persantine) is
a coronary vasodilator which was introduced
for

Angina Pectoris.
Mechanism of action: it inhibits PDE and
blocks reuptake of Adenosine to increase platelet cAMP
which inhibits TxA2 synthesis and potentiates the effect of
prostacyclin (PGI2) to
antagonize Platelet
Stickiness and
?Platelet Adhesion to
Thrombogenic
Surface.

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Pentoxifylline (Trental)
inhibits PDE, ?Platelet and Erythrocytes Aggregation, has desaggregational properties,

enhances fibrinolysis, lowers viscosity,
IMPROVES MICROCIRCULATION.

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ABCIXIMAB
ReoPro 2 mg/ml
IV injection
a Humanized Monoclonal Antibody
directed against

the platelet
Glycoprotein IIb/IIIa Receptor Complex and inhibits platelet aggregation.

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II. ANTICOAGULANTS:
1. DIRECT ACTION
HEPARIN - amp 5 ml – 5000

U/ml and 10000 U/ml
FRAXAPARIN - syringe 0.3 ml, 0.5 ml, 1 ml (1 ml-9,500 IU)
ENOXAPARIN
SODIUM HYDROCITRATE
2. INDIRECT ACTION
Neodicumarin - Tab 0.05 and 0.1 g
Warfarin - Tab 2 and 10 mg
Phenylin - Tab 0.03 g
Syncumar - Tab 2 and 4 mg

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Heparin
Mechanism of action:
acts indirectly by binding to Antithrombin III.
The

Heparin-AT III complex binds to
clotting factors of intrinsic pathways –
IIa, Xa, IXa, XIa, XIIa and XIIIa and
inactivates them.

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CONTRAINDICATIONS to Heparin:
Bleeding Disorders, Thrombocytopenia
Hypertension, Threatened Abortion, Piles, Ulcers

Subacute Bacterial Endocarditis
Large Malignancies, Tuberculosis (Hemoptysis)
⮚Ocular and Neurosurgery, lumbar puncture

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ADVERSE EFFECTS of HEPARIN:
1. Bleeding complications.
Excessive bleeding may be

managed by suspending the drug or treating with PROTAMINE SULFATE.
2. Hypersensitivity reactions: chills, fever, urticaria, Anaphylactic Shock.
3. Thrombocytopenia.

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Clinical uses of Heparin:
Pulmonary Embolism and Deep Vein Thrombosis
Myocardial

Infarction and Unstable Angina
Prevention of Thromboembolism
Intravascular Catheters
⮚ Disseminated Intravascular Coagulation Syndrome

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Vitamin K is regenerated from the epoxide by
vitamin K Epoxide

Reductase.
It is the enzyme that is inhibited by Neodicumarin, Syncumar and Warfarin.
Neodicumarin (Tab 0.05 and 0.1 g)
is a coumarin derivative.
It inhibits the hepatic synthesis and activation of
vitamin K-dependent clotting factors II, VII, IX and X, decreasing the blood’s coagulation potential.

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Clinical Uses of Neodicumarin:
Thrombophlebitis
Deep Vein Thrombosis
Myocardial Infarction
Artificial

Heart Valves
⮚ Atrial Arrhythmias

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FIBRINOLYTIC (THROMBOLYTIC) DRUGS
I. Non-selective Activators of Profibrinolysin: Streptokinase
Urokinase
Streptodekase
II. Selective activators of

Profibrinolysin: Alteplase

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Streptokinase (amp 250,000 and 500,000 IU) -
a non-selective Activator of

Profibrinolysin,
the enzyme extracted from cultures of
Hemolytic Streptococci.
It activates Plasminogen (Profibrinolysin) of thrombus and
serum to form Plasmin (Fibrinolysin), which
degrades fibrin
and break up
thrombi.

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Alteplase and Duteplase - recombinant tissue-type Plasminogen Activator (t PA) -

act selectively on plasminogen, bound with thrombus and are
‘CLOT SELECTIVE’

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Agents to Treat Bleeding (Hemostatics)
1.Agents enhancing Coagulation of blood:
for Local Application:

Thrombin - amp 125 AU
Sponges hemostatic
System Action:
Gelatin
Fibrinogen
Calcium chloride, Calcium gluconate
Adroxon
Dicynon (Etamsylat)
Vitamin K
Protamine sulfate

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Adroxon (amp. 0.025% 1 ml)
Hemostatic action
It is used to

stop capillary and parenchymatous bleeding in traumas, during surgery and for prevention of post-operative bleeding and haematomas.
Adroxon is used:
a) Locally – gauze bandage or tampon moistened with 0.025% solution;
b) IM or SC 0.025% 1 ml 1–4 times
during or after surgery.

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Ethamsylate (Dicynon) – amp. 12.5% 2 ml IV or IM, Caps.

0.25 g
Antihyaluronidase Action –
improves Capillary Wall stability
Inhibits PGI2 production
Corrects abnormal platelet function
Clinical uses: Prevention and Treatment of
Capillary Bleeding in:
Menorrhagia
after Abortion, Postpartum Haemorrhage
Epistaxis (nosebleed)
Malena (tarry stool)
Haematuria
after tooth extraction.

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2. ANTIFIBRINOLYTIC AGENTS
Inactivation of the Fibrinolytic System
can be achieved by

Plasmin Inhibitors :
Aminocaproic acid (5% sol.-100 ml)
Tranexamic acid
Amben (Pamba) (amp. 1% sol.-5 ml)
Contrical (Aprotinin, Trasylol)
All agents inhibit
plasminogen activation.

Drugs affecting blood

Содержание

Principal Causes of a Disturbance of Erythropoiesis :1. Hemoglobin synthesis is

Agents Affecting ErythropoesisI. Agents Stimulating Erythropoiesis1. Used in Hypochromic Anemias A.

2. In HYPERCHROMIC Anemias: Vitamin B12 (Cyanocobalamin) amp. 0.01%, 0.05%-1 ml Folic Acid

Iron Agents:Ferrous Sulfate, Ferrous Lactate, Fercoven, Ferrum Lek - contain the

Fercoven (amp. 5 ml) contains 20 mg of Saccharate Iron and

OVERDOSE with Fe2+ COMPOUNDS Manifestation: lethargy, nausea and vomiting green then

HEMATOPOIETIC GROWTH FACTORS:▶ ERYTHROPOETIN▶ Granulocyte Colony-Stimulating Factor - G-CSF, Filgrastim▶ Granulocyte-Macrophage Colony-Stimulating

Erythropoietin (Epoetin alfa) – vial 2000, 4000, and 10,000 IU/ml IV,

Filgrastim (G-CSF) is lineage-specific growth factor –● supports Proliferation, Differentiation and

Molgramostim (GM-CSF) has broader actions than G-CSF.● stimulates Proliferation and Differentiation

Folate Deficiency:1) Increased Demand (pregnancy and lactation)2) Poor Absorption caused by

The minimal requirement: ≈ 1 μg/day.

AGENTS AFFECTING LEUCOPOIESIS1. Agents Stimulating Leucopoiesis: Sodium nucleinate Pentoxyl Methyluracil Molgramostim

AGENTS USED FOR PROPHYLAXIS AND TREATMENT OF THROMBOSIS 1. PLATELET AGGREGATION

PLATELET AGGREGATION INHIBITORS (ANTIPLATELET AGENTS): Aspirin, Ticlopidine, Dipyridamole, Pentoxifylline, Abciximab Clinical Uses:

ASPIRIN blocks Thromboxane A2 synthesis from arachidonic acid in platelets by

Ticlopidine and Clopidogrel inhibit the ADP pathway involved in the binding

Dipyridamole (Curantil, Persantine) is a coronary vasodilator which was introduced for

Pentoxifylline (Trental) inhibits PDE, ?Platelet and Erythrocytes Aggregation, has desaggregational properties,

ABCIXIMAB ReoPro 2 mg/ml IV injection a Humanized Monoclonal Antibody directed against

II. ANTICOAGULANTS:1. DIRECT ACTION HEPARIN - amp 5 ml – 5000

Heparin Mechanism of action: acts indirectly by binding to Antithrombin III.The

CONTRAINDICATIONS to Heparin: Bleeding Disorders, Thrombocytopenia Hypertension, Threatened Abortion, Piles, Ulcers

ADVERSE EFFECTS of HEPARIN: 1. Bleeding complications. Excessive bleeding may be

Clinical uses of Heparin: Pulmonary Embolism and Deep Vein Thrombosis Myocardial

Vitamin K is regenerated from the epoxide by vitamin K Epoxide

Clinical Uses of Neodicumarin: Thrombophlebitis Deep Vein Thrombosis Myocardial Infarction Artificial

FIBRINOLYTIC (THROMBOLYTIC) DRUGSI. Non-selective Activators of Profibrinolysin: Streptokinase Urokinase StreptodekaseII. Selective activators of

Streptokinase (amp 250,000 and 500,000 IU) - a non-selective Activator of