DRUGS ACTING ON THE BLOOD INFLAMMATION AND GOUT Flashcards
Absence of adequate iron result in
small erythrocytes with insufficient hemoglobin are formed resulting in microcytic hypochromic anemia.
What are the causes of Iron Deficiency Anemia?
- Nutritional deficiency
- Chronic blood loss
What is the daily requirement of Iron in male?
Male 10mg
What is the daily requirement of Iron in female?
Female 15 mg
What are the dietary sources of iron?
Meat, cereals
How much total content of Iron in the male adult?
About 4000mg in an adult male
How much total content of Iron in the female adult?
About 2500 mg
Which part of duodenum the iron absorbed?
Duodenum and proximal jejunum.
What are the factors that deceases iron absorption?
Antacids
Gastric resection
Phytates
Iron is stored as
ferritin
Ferritin is a storage form of
Iron
What part of body iron (ferrtin) is stored?
Intestinal mucosal cells
How does iron elimination occurs from human body?
Very small amount are execrated in stool
Trace amounts are execrated in bile
Urine and sweat with total daily excretion not more than 1mg/day
What are oral iron therapy preparations for anemia?
Ferrous sulfate
Ferrous gluconate
Ferrous fumarate
What are the side effects of oral therapy drugs?
Nausea, vomiting
Epigastric discomfort,
Constipation
Diarrhea
What are the drugs used for parenteral administration?
- Iron dextran
- Iron sorbitol
They may be given by deep IM or occasionally IV.
Intravenous iron administration may result
in very severe allergic reactions and thus should be avoided if possible.
Which drug is used in acute iron toxicity?
Deferoxamine - A potent iron chealating compound should be given systemically to bind iron and promote excretion through urine
How does a chealating compound work?
The chelating agent has a structure that allows it to bind to the metal (e.g. ferritin) ion at multiple points, forming a ring-like structure known as a chelate.
What is chelation therapy?
In the case of heavy metal (e.g. ferritin, lead) poisoning, the agent may be given intravenously or orally. During chelation therapy, the chelating agent will bind to the metal ions in the bloodstream and other tissues, and facilitate their excretion through urine or feces.
Vitamin B12 is also called
Cobalamin
What is the synthetic form of vitamin B12?
Cyanocobalamin
What is difference between cobalamin and cyanocobalamin?
Cobalamin and cyanocobalamin are two different forms of vitamin B12. Cobalamin is the natural form of vitamin B12 that is found in foods
Cyanocobalamin is a synthetic form of vitamin B12 that is commonly used in dietary supplements and fortified foods.
The main difference between the two forms is that cyanocobalamin contains a cyanide molecule.
What is the physiologic function of B12?
Acts as a coenzyme in the synthesis of DNA and is also essential for various metabolisms in the body.
How does b12 absorb in human body?
It absorbed after combined with intrinsic factor secreted by stomach
Where B12 is absorb in human body?
Distal ileum
Deficiency of Vit B12 results in:
- Megaloblastic anemia
- Neurological syndrome involving spinal cord and peripheral nerves
What is the reason of megaloblastic anemia?
It occurs due to a deficiency in vitamin B12 or folic acid.
What are the characteristics of megaloblastic anemia?
It is characterized by the production of abnormally large red blood cells (megaloblasts) in the bone marrow, which are immature and unable to function properly.
If intrinsic factor secretion is defective, what type of anemia it will cause?
Pernicious anemia
Intrinsic factor secretion is required to absorb:
B12
Defective Intrinsic factor secretion leads to:
Pernicious anemia
What is required to absorb the B12 in human body?
Intrinsic factor secretion (in stomach)
What are the causes defective secretion of intrinsic factor?
- Partial or total gastrectomy,
- Diseases that affect distal ileum,
- Malabsorption syndrome e.g inflammatory bowel disease
Almost all cases of vit B12 deficiencies are caused by:
Malabsorption
What are the Vit B12 therapeutic preparations?
Cyanocoblamin
Hydroxycobalamin
If case of intrinsic factor deficiency the B12 vitamin should be given:
Parenterally and patients with pernicious anemia will need life-long therapy.
What is daily requirement of Folic acids?
Daily requirement is 50 -100μg.
Why folic acid is important for human body?
Folic acid is needed for the production of DNA and RNA, which are essential for the formation of new cells. This is particularly important during periods of rapid cell growth, such as during pregnancy and infancy.
Folic acid, also known as
Folate
What are the natural sources of folic acids?
Yeast
Liver
Kidney
Green vegetables
Folic acids provide precursors for:
Synthesis of amino acids, purines and DNA
What is the physiologic functions of folate (folic acid)?
It plays a role in the biosynthesis of purines and pyrimidines, i.e., DNA.
Folic acid is absorb in:
Proximal jejunum
How much folate stored in human body?
5 -20 mg of folates are stored in the liver and other tissues
Folate deficiency result in:
Megaloblasiic anemia
Megaloblasiic anemia are due to deficiency of:
Folate
What is the consequences of folate deficiency during pregnancy?
Spina bifida (congenital malformation in newborn)
How much amount of folic acid given in anemia?
Folic acid 1mg orally per day.
What is Hemostasis?
Hemostasis is spontaneous arrest of bleeding from a damaged blood vessel.
Steps: Vascular injury -> vasospasm-> platelate adhesion -> platelate aggregation -> coagulation cascades -> fibrin formation
What are anticoagulants?
Anticoagulants are the drugs which inhibit fibrin formation.
What are the classification of anticoagulants?
- Fast and direct acting - IV or subcutaneous e.g: Heparin
- Slow and indirect acting - Oral anticoagulants e.g Warfarin and Dicumarol
What is the drug used as fast and direct acting anticoagulants?
Heparin
What are the drugs used as slow and indirect acting anticoagulants?
Warfarin
Dicumarol
What is the heparin mechanism of action?
The mechanism of action of heparin involves its ability to enhance the activity of antithrombin III, a natural protein that helps to prevent blood clots.
What are the steps of heparin mechanism of actions?
Blood vessel injury -> Activation of clotting factors, including thrombin -> Thrombin converts fibrinogen to fibrin -> Fibrin forms a mesh-like structure -> Clot formation -> Prevention of further bleeding
What are the clinical uses of heparin?
Prevention and treatment of venous thrombosis
Treatment of coronary occlusion
Acute myocardial infarction
Prevention of post operative thrombosis and embolism
Why heparin is always administered by IV or subcutaneous?
Oral therapy is ineffective because it is inactivated by gastric
acids and absorption is minimal because of large molecular size. Heparin must never be administered intramuscularly because of danger of hematoma formation at injection site.
Why heparin is not administered by IM?
Heparin must never be administered intramuscularly because of danger of hematoma formation at injection site.
Why heparin is not administered by oral route?
Oral therapy is ineffective because it is inactivated by gastric
acids
What are the side effects of heparin?
Bleeding is the major side effect
Thrombocytopenia
Osteoporosis
What are the contraindications of heparin?
If patient
- is actively bleeding
- has hemophilia
- has thrombocytopenia
- has sever hypertension
Which compound was originally employed as a rodent poison?
WARFARIN
What is the drug of choice as an oral anticoagulant?
WARFARIN
What is the warfarin mode of action?
The anticoagulant prevents reductive metabolism of the inactive vitamin K epoxide back to its active form
Warfarin should nor administered during:
Pregnancy.
Which drugs increase the effect of warfarin?
Cimitidine
Metronidazole
Cephalosporin (3rd generations)
Which drugs decrease the effect of warfarin?
Barbiturates
Rifampincin
Diuretics
Vit K
What are the THROMBOLYTIC AGENTS? Name them?
Streptokinase
Urokinase
Anistreptase
Tissue plaminogen activator
How does streptokinase work as THROMBOLYTIC AGENTS?
Streptokinase- a protein synthesized by streptococci, combines with plasminogen to convert it to active plasmin.
How does Urokinase work as THROMBOLYTIC AGENTS?
It is human enzyme synthesized by the kidneys that directly converts plasminogen to active plasmin
What is indications (clinical use) of THROMBOLYTIC AGENTS?
Multiple pulmonary emboli
Central deep vein thrombosis
Acute myocardial infarction
What are ANTIPLATELET DRUGS?
Aspirin
Ticlopidine
Dipyridamole.
What is therapeutic Uses of Aspirin?
Prophylaxis against myocardial infarction
Prevention of stroke in patients at risk e.g. those with transient ischemic attacks.
How does Aspirin work?
Aspirin irreversibly blocks the enzyme cyclooxygenase; the drug
decreases the formation of both the prostaglandins and thromboxane A2.
Aspirin provide the following effects in human body:
Anti-inflammatory Effects
Analgesic Effects
Antipyretic Effects
Platelet Effects - inhibits platelet aggregation
What are the clinical uses of aspirin?
used as analgesic, antipyretics, and anti-inflammatory and Inhibition of platelet aggregation drug.
What is the common side effect of aspirin in GI?
Gastritis
What is the common side effect of aspirin in CNS?
Tinnitus, decreased hearing, and vertigo
Aspirin in a low daily dose usually increases:
Serum uric acid levels
Which NSAIDs have more effect in GI? Aspirin or Ibuprofen?
Ibuprofen effects gastrointestinal irritation and bleeding , though less frequently than with aspirin.
Which NSAIDs is potent cyclooxygenase inhibitor?
Diclofenac
Which NSAIDs is potent cyclooxygenase inhibitor? Diclofenac or naproxen?
The potency of diclofenac as a cyclooxygenase inhibitor is greater than that of naproxen.
What are indication (clinical use) of diclofenac?
Rheumatoid arthritis and
Osteoarthritis
Acute musculoskeletal pain.
What are the adverse effects of diclofenac?
Gastrointestinal distress
Gastric ulceration
Name few Nonsteroidal Anti-Inflammatory Drugs?
Ibuprofen
Diclofenac
Rofecoxib
Sulindac
Mefenamic Acid
Which NSAIDs is slightly more toxic than others?
Indomethacin
What are the clinical uses of Indomethacin?
Patent ductus arteriosus
Acute gouty arthritis
Ankylosing spondylitis, pericarditis
Which NSAIDs possesses no significant anti-inflammatory
effects?
Acetaminophen
What are the indications of acetaminophen?
It is an effective analgesic and antipyretic agent, but it lacks of anti-inflammatory properties.
What is Gout?
Gout is a metabolic disease characterized by recurrent episodes of acute arthritis due to deposits of monosodium urate in joints and cartilage. Formation of uric acid calculi in the kidneys may also occur.
What are the drugs used in gout?
Colchicine
Probenecid
sulfinpyrazone
Allopurinol
Which NSAIDS is used in gout?
Indomethacin
What are the Indications of Allopurinol?
- in chronic tophaceous gout
- for recurrent renal stones
- in patients with renal functional impairment;
- When serum urate levels are grossly elevated.