Current presentation is about the comprehensive literature of Anticoagulants, Bulbs for blood collection and their specific uses intended for Graduate and Post graduate students of Physiology and Pathology in Medical and Health Sciences.
Haemostasis is the physiologic system of competent blood vessels, endothelial cells, platelets and numerous plasma proteins that act in a finely controlled manner to preserve blood vessel integrity and prevent pathologic hemorrhage or thrombosis.
Haemostasis is achieved by :-
Vascular constriction
Formation of platelet plug
Formation of blood clot
Growth of fibrous tissue into the clot
Anticoagulants, commonly referred to as blood thinners, are chemical substances that prevent or reduce coagulation of blood, prolonging the clotting time.
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Current presentation is about the comprehensive literature of Anticoagulants, Bulbs for blood collection and their specific uses intended for Graduate and Post graduate students of Physiology and Pathology in Medical and Health Sciences.
Haemostasis is the physiologic system of competent blood vessels, endothelial cells, platelets and numerous plasma proteins that act in a finely controlled manner to preserve blood vessel integrity and prevent pathologic hemorrhage or thrombosis.
Haemostasis is achieved by :-
Vascular constriction
Formation of platelet plug
Formation of blood clot
Growth of fibrous tissue into the clot
Anticoagulants, commonly referred to as blood thinners, are chemical substances that prevent or reduce coagulation of blood, prolonging the clotting time.
Similar to DRUGS AFFECTING COAGULATION,BLEEDING AND THROMBOSIS.pptx (20)
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263778731218 Abortion Clinic /Pills In Harare ,ABORTION WOMEN’S CLINIC +27730423979 IN women clinic we believe that every woman should be able to make choices in her pregnancy. Our job is to provide compassionate care, safety,affordable and confidential services. That’s why we have won the trust from all generations of women all over the world. we use non surgical method(Abortion pills) to terminate…Dr.LISA +27730423979women Clinic is committed to providing the highest quality of obstetrical and gynecological care to women of all ages. Our dedicated staff aim to treat each patient and her health concerns with compassion and respect.Our dedicated group ABORTION WOMEN’S CLINIC +27730423979 IN women clinic we believe that every woman should be able to make choices in her pregnancy. Our job is to provide compassionate care, safety,affordable and confidential services. That’s why we have won the trust from all generations of women all over the world. we use non surgical method(Abortion pills) to terminate…Dr.LISA +27730423979women Clinic is committed to providing the highest quality of obstetrical and gynecological care to women of all ages. Our dedicated staff aim to treat each patient and her health concerns with compassion and respect.Our dedicated group of receptionists, nurses, and physicians have worked together as a teamof receptionists, nurses, and physicians have worked together as a team wwww.lisywomensclinic.co.za/
Title: Sense of Taste
Presenter: Dr. Faiza, Assistant Professor of Physiology
Qualifications:
MBBS (Best Graduate, AIMC Lahore)
FCPS Physiology
ICMT, CHPE, DHPE (STMU)
MPH (GC University, Faisalabad)
MBA (Virtual University of Pakistan)
Learning Objectives:
Describe the structure and function of taste buds.
Describe the relationship between the taste threshold and taste index of common substances.
Explain the chemical basis and signal transduction of taste perception for each type of primary taste sensation.
Recognize different abnormalities of taste perception and their causes.
Key Topics:
Significance of Taste Sensation:
Differentiation between pleasant and harmful food
Influence on behavior
Selection of food based on metabolic needs
Receptors of Taste:
Taste buds on the tongue
Influence of sense of smell, texture of food, and pain stimulation (e.g., by pepper)
Primary and Secondary Taste Sensations:
Primary taste sensations: Sweet, Sour, Salty, Bitter, Umami
Chemical basis and signal transduction mechanisms for each taste
Taste Threshold and Index:
Taste threshold values for Sweet (sucrose), Salty (NaCl), Sour (HCl), and Bitter (Quinine)
Taste index relationship: Inversely proportional to taste threshold
Taste Blindness:
Inability to taste certain substances, particularly thiourea compounds
Example: Phenylthiocarbamide
Structure and Function of Taste Buds:
Composition: Epithelial cells, Sustentacular/Supporting cells, Taste cells, Basal cells
Features: Taste pores, Taste hairs/microvilli, and Taste nerve fibers
Location of Taste Buds:
Found in papillae of the tongue (Fungiform, Circumvallate, Foliate)
Also present on the palate, tonsillar pillars, epiglottis, and proximal esophagus
Mechanism of Taste Stimulation:
Interaction of taste substances with receptors on microvilli
Signal transduction pathways for Umami, Sweet, Bitter, Sour, and Salty tastes
Taste Sensitivity and Adaptation:
Decrease in sensitivity with age
Rapid adaptation of taste sensation
Role of Saliva in Taste:
Dissolution of tastants to reach receptors
Washing away the stimulus
Taste Preferences and Aversions:
Mechanisms behind taste preference and aversion
Influence of receptors and neural pathways
Impact of Sensory Nerve Damage:
Degeneration of taste buds if the sensory nerve fiber is cut
Abnormalities of Taste Detection:
Conditions: Ageusia, Hypogeusia, Dysgeusia (parageusia)
Causes: Nerve damage, neurological disorders, infections, poor oral hygiene, adverse drug effects, deficiencies, aging, tobacco use, altered neurotransmitter levels
Neurotransmitters and Taste Threshold:
Effects of serotonin (5-HT) and norepinephrine (NE) on taste sensitivity
Supertasters:
25% of the population with heightened sensitivity to taste, especially bitterness
Increased number of fungiform papillae
Couples presenting to the infertility clinic- Do they really have infertility...Sujoy Dasgupta
Dr Sujoy Dasgupta presented the study on "Couples presenting to the infertility clinic- Do they really have infertility? – The unexplored stories of non-consummation" in the 13th Congress of the Asia Pacific Initiative on Reproduction (ASPIRE 2024) at Manila on 24 May, 2024.
The prostate is an exocrine gland of the male mammalian reproductive system
It is a walnut-sized gland that forms part of the male reproductive system and is located in front of the rectum and just below the urinary bladder
Function is to store and secrete a clear, slightly alkaline fluid that constitutes 10-30% of the volume of the seminal fluid that along with the spermatozoa, constitutes semen
A healthy human prostate measures (4cm-vertical, by 3cm-horizontal, 2cm ant-post ).
It surrounds the urethra just below the urinary bladder. It has anterior, median, posterior and two lateral lobes
It’s work is regulated by androgens which are responsible for male sex characteristics
Generalised disease of the prostate due to hormonal derangement which leads to non malignant enlargement of the gland (increase in the number of epithelial cells and stromal tissue)to cause compression of the urethra leading to symptoms (LUTS
Flu Vaccine Alert in Bangalore Karnatakaaddon Scans
As flu season approaches, health officials in Bangalore, Karnataka, are urging residents to get their flu vaccinations. The seasonal flu, while common, can lead to severe health complications, particularly for vulnerable populations such as young children, the elderly, and those with underlying health conditions.
Dr. Vidisha Kumari, a leading epidemiologist in Bangalore, emphasizes the importance of getting vaccinated. "The flu vaccine is our best defense against the influenza virus. It not only protects individuals but also helps prevent the spread of the virus in our communities," he says.
This year, the flu season is expected to coincide with a potential increase in other respiratory illnesses. The Karnataka Health Department has launched an awareness campaign highlighting the significance of flu vaccinations. They have set up multiple vaccination centers across Bangalore, making it convenient for residents to receive their shots.
To encourage widespread vaccination, the government is also collaborating with local schools, workplaces, and community centers to facilitate vaccination drives. Special attention is being given to ensuring that the vaccine is accessible to all, including marginalized communities who may have limited access to healthcare.
Residents are reminded that the flu vaccine is safe and effective. Common side effects are mild and may include soreness at the injection site, mild fever, or muscle aches. These side effects are generally short-lived and far less severe than the flu itself.
Healthcare providers are also stressing the importance of continuing COVID-19 precautions. Wearing masks, practicing good hand hygiene, and maintaining social distancing are still crucial, especially in crowded places.
Protect yourself and your loved ones by getting vaccinated. Together, we can help keep Bangalore healthy and safe this flu season. For more information on vaccination centers and schedules, residents can visit the Karnataka Health Department’s official website or follow their social media pages.
Stay informed, stay safe, and get your flu shot today!
New Directions in Targeted Therapeutic Approaches for Older Adults With Mantl...i3 Health
i3 Health is pleased to make the speaker slides from this activity available for use as a non-accredited self-study or teaching resource.
This slide deck presented by Dr. Kami Maddocks, Professor-Clinical in the Division of Hematology and
Associate Division Director for Ambulatory Operations
The Ohio State University Comprehensive Cancer Center, will provide insight into new directions in targeted therapeutic approaches for older adults with mantle cell lymphoma.
STATEMENT OF NEED
Mantle cell lymphoma (MCL) is a rare, aggressive B-cell non-Hodgkin lymphoma (NHL) accounting for 5% to 7% of all lymphomas. Its prognosis ranges from indolent disease that does not require treatment for years to very aggressive disease, which is associated with poor survival (Silkenstedt et al, 2021). Typically, MCL is diagnosed at advanced stage and in older patients who cannot tolerate intensive therapy (NCCN, 2022). Although recent advances have slightly increased remission rates, recurrence and relapse remain very common, leading to a median overall survival between 3 and 6 years (LLS, 2021). Though there are several effective options, progress is still needed towards establishing an accepted frontline approach for MCL (Castellino et al, 2022). Treatment selection and management of MCL are complicated by the heterogeneity of prognosis, advanced age and comorbidities of patients, and lack of an established standard approach for treatment, making it vital that clinicians be familiar with the latest research and advances in this area. In this activity chaired by Michael Wang, MD, Professor in the Department of Lymphoma & Myeloma at MD Anderson Cancer Center, expert faculty will discuss prognostic factors informing treatment, the promising results of recent trials in new therapeutic approaches, and the implications of treatment resistance in therapeutic selection for MCL.
Target Audience
Hematology/oncology fellows, attending faculty, and other health care professionals involved in the treatment of patients with mantle cell lymphoma (MCL).
Learning Objectives
1.) Identify clinical and biological prognostic factors that can guide treatment decision making for older adults with MCL
2.) Evaluate emerging data on targeted therapeutic approaches for treatment-naive and relapsed/refractory MCL and their applicability to older adults
3.) Assess mechanisms of resistance to targeted therapies for MCL and their implications for treatment selection
Prix Galien International 2024 Forum ProgramLevi Shapiro
June 20, 2024, Prix Galien International and Jerusalem Ethics Forum in ROME. Detailed agenda including panels:
- ADVANCES IN CARDIOLOGY: A NEW PARADIGM IS COMING
- WOMEN’S HEALTH: FERTILITY PRESERVATION
- WHAT’S NEW IN THE TREATMENT OF INFECTIOUS,
ONCOLOGICAL AND INFLAMMATORY SKIN DISEASES?
- ARTIFICIAL INTELLIGENCE AND ETHICS
- GENE THERAPY
- BEYOND BORDERS: GLOBAL INITIATIVES FOR DEMOCRATIZING LIFE SCIENCE TECHNOLOGIES AND PROMOTING ACCESS TO HEALTHCARE
- ETHICAL CHALLENGES IN LIFE SCIENCES
- Prix Galien International Awards Ceremony
New Drug Discovery and Development .....NEHA GUPTA
The "New Drug Discovery and Development" process involves the identification, design, testing, and manufacturing of novel pharmaceutical compounds with the aim of introducing new and improved treatments for various medical conditions. This comprehensive endeavor encompasses various stages, including target identification, preclinical studies, clinical trials, regulatory approval, and post-market surveillance. It involves multidisciplinary collaboration among scientists, researchers, clinicians, regulatory experts, and pharmaceutical companies to bring innovative therapies to market and address unmet medical needs.
ARTIFICIAL INTELLIGENCE IN HEALTHCARE.pdfAnujkumaranit
Artificial intelligence (AI) refers to the simulation of human intelligence processes by machines, especially computer systems. It encompasses tasks such as learning, reasoning, problem-solving, perception, and language understanding. AI technologies are revolutionizing various fields, from healthcare to finance, by enabling machines to perform tasks that typically require human intelligence.
Explore natural remedies for syphilis treatment in Singapore. Discover alternative therapies, herbal remedies, and lifestyle changes that may complement conventional treatments. Learn about holistic approaches to managing syphilis symptoms and supporting overall health.
2. Learn about coagulation cascade and coagulation factors
How the blood clots are broken down
What drugs can be used to regulate clotting
How to rectify clotting deficiencies
Objectives
3. Terms
Hemostasis(vasoconstriction +coagulation + platelet aggregation)
Coagulation cascade and clotting factors
Thrombosis
Aptt, pt
Antithrombin , Protein C & S
Zymogens
Scaffolding
Disorders like Hemophilia, Deep vein Thrombosis, Ecchymosis, epistaxis etc
CVA(cerebro vascular accident), ACS( acute coronary syndrome)
4. Commonly asked questions
1. Role of heparin in Ischaemic heart disease
2. Role of streptokinase in Acute myocardial infarction
3. Enumerate anticoagulants used for DVT
4. Low mol. Weight Heparin preferred over conventional heparin for
therapeutic uses
5. Heparin is useful both in vivo and in vitro-explain
6. Short notes- a)thrombolytic drugs, b)Warfarin Sod., c)
EACA/Tranexamic acid
7. Advantages of newer oral anti coagulants over warfarin
6. Coagulants
Haemostasis(arrest of blood loss) and blood
coagulation involve complex interactions between the
injured vessel wall, platelets and coagulation factors.
For coagulation, a cascading series of proteolytic
reaction started by-
a)Contact activation of Hageman factor(Intrinsic
system)
b)Tissue thromboplastin(extrinsic system)
7.
8.
9. Clotting factors are of 3 types-
1. Contact Family (XII, XI, HMWK,
Prekallikrein)
2. Vt K dependent factors( II, VII, IX, X)
3. Fibrinogen family(I,V,VIII,XIII)
Liver produces all factors except III, IV and VIII
10.
11. 1.Vitamin k
Nature :- It is a fat-soluble dietary principle required for
the synthesis of clotting factors.
Chemistry and source :-Vit K has a basic naphthoquinone
structure, with or without a side chain (R) at position 3.
The side chain in K1 is phytyl; in K2 prenyl ;while in K3 there is no side
chain.
Dietary sources :-Green leafy vegetables, such as cabbage. spinach; and
liver, cheese etc.
Daily requirement :-Even 3-10 µg/day external
source may be sufficient. However, the total requirement
of an adult has been estimated to be 50-100 µg/day
12. Action :- Vt k helps in gamma carboxylation of glutamate
residue and activates coagulation factors II, VII,IX, X.
USE :-
1.Vt K requires in dietary deficiency
2.Vt K is administered in case of prolonged
antimicrobial therapy
3.Obstructive jaundice or malabsorption syndromes(sprue, regional ileitis,
steatorrhoea, etc.)
13. 4. It is used in liver diseases (cirrhosis, viral hepatitis)
5. vit k( 1mg) i.m. soon after birth has been recommended
routinely. Some prefer administering 5- 10 mg
i.m. to the mother 4 -12 hours before delivery.
6. Haemorrhagic disease or the newborn can be
selectively prevented/treated by such medication.
Menadione (K,) should not be used for this
purpose
7. Overdose of oral (coumarin) anticoagulants is the most important indication of vit K.
Phytonadione (K1) is the preparation of choice,
14. Severe deficiency: 10 mg i.m followed by 5 mg 4 hourly;
bleeding generally stops in 6-12 hours, but normal levels of
coagulation factors are restored only after 24 hr. This dose of vit
K will block anticoagulant action for 7- 10 days.
Moderate deficiency: IO mg i.M. Followed by 5 mg once or
twice according to response.
Mild deficiency: Lust omit a few doses of the anticoagulant.
15. Adverse effects:-
1. Severe anaphylactoid reactions can occur on i. V. Injection of
emulsified formulation; this route should not be used
2. Menadione and its water-soluble derivatives can cause haemolysis
in a dose-dependent manner. Patients with G-6-PD deficiency and
neonates are especially susceptible.
3. In the newborn menadione or its salts can precipitate kernicterus:
(a) by inducing haemolysis and increasing bilirubin load.
(b) by competively inhibiting glucuronidation of bilirubin.
Glucuronide conjugation is, as such, inadequate in neonates.
16. 2. Fibrinogen
The fibrinogen fraction is synthesized from of human plasma
.
It is employed to control bleeding in haemophilia,
Antihaemophilic globulin (AHG) deficiency and acute
afibrinogenemic states:
It is given at dose of 0.5 g i.V.
17. 3.Antihaemophilic factor
It is concentrated human AHG (factor VIII) prepared from pooled human
plasma.
It is indicated (along with human fibrinogen) in haemophilia which is due
to AHG deficiency.
It is highly effective in controlling bleeding episodes,
Its action is short-lasting ( I to 2 days).
Dose: 5-10 U/kg by i.V. Infusion. Repeated 6-12 hourly
18. 4.Desmopressin
This synthetic peptide is a selective V2 agonist;
It is 12 times more potent antidiuretic than AVP, but has negligible vasoconstrictor activity.
It releases factor VIII and Von willebrand's factor from vascular endothelium and checks
bleeding in haemophilia and Von willebrand’s disease
It is also longer acting because enzymatic degradation is slow; t½ 1- 2 hours, and the
duration of action is 8- 12 hours.
Desmopressin is the preparation of choice for a ll Y2 receptor related indication s. The
intranasal route is preferred.
Though bioavailability is only IO 20% . an oral formulation has been marketed with a
bioavailability of 1- 2%.
19. 5. Adrenochrome
monosemicarbazone
It is believed to reduce capillary fragility, controlling from raw
surfaces and prevent microvessel bleeding, e.g. epistaxis,
haematuria, secondary haemorrhage from wounds. Etc.
Its efficacy is uncernain.
Dose: I 5 mg oral, i.M.
20. 6.Rutin
It is a plant glycoside claimed to reduce capillary bleeding.
It has been used in a dose of 60 mg oral bd/tds along with vit
C which is believed to facilitate its action.
Its efficacy is uncertain.
21. 7. Ethamsylate
Ethamsylate reduces capillary bleeding when platelets arc adequate
It probably corrects abnormalities of platelet adhesion, but does not mobilize fibrin
(not an antifibrinolytic).
Ethamsylate has been used in the prevention and treatment of capillary bleeding
in menorrhagia, after abortion, epistaxis. Malena, hematuria and after tooth
extraction.
Its efficacy is unsubstantiated, therefore not recommended now.
Side effects are nausea, rash, headache and fall in bp (only after i.v Injection).
Dose: 250- S00 mg tds oral/i.v
22. Local haemostatics (styptics)
Local haemostatics (styptics) that are substances used to stop bleeding from a
local and approachable site.
They are particularly effective on oozing surfaces, e.g. Tooth socket, abrasions, etc.
Absorbable materials like fibrin (prepared from human plasma and derived as
sheet or foam). Gelatin foam, oxidized cellulose (as strips which can be cut and
placed in the wound).
M.O.A :- It provide a meshwork which activates the clotting mechanism and checks
bleeding.
Uses:- 1. Thrombin obtained from bovine plasma may be applied as dry powder to
use in hemophilas.
2. Vasoconstrictors like 0. 1 % ad r solution may be soaked in sterile cotton-
gauze used in broken tooth, epistaxis etc.
3. Astringents such as tannic acid or metallic salts are occasionally applied for
bleeding gums, bleeding piles, etc.
23. Sclerosing agents
These are irritants.
They cause inflammation. Coagulation and ultimately fibrosis.
These are injected into haemarroids (piles} or varicose vein mass.
They are used only for local injection.
1. Sod. Tetradecyl sulfate (3% with benzyl alcohol 2%): 0.5-2 ml at each site.
SETROL 2 m l inj.
2. Polidocanol (3% inj): 2 ml; ASKLEROL 2 ml inj.
27. 1.Heparin
Chemistry and occurrence :-
Heparin is a non-uniform mixture of straight chain rnucopolysaccharides with MW I 0,000
to 20,000.
It contains polymers of two sulfated disaccharide units-
D-glucosamine-L-iduronic acid + D-glucosamine-D-glucuronic acid
Heparin carries strong electronegative charges and is the strongest organic acid present
in the body.
It occurs in mast cells as a much bigger molecule (MW ~75,000) loosely bound to the
granular protein.
Thus, heparin is present in all tissues containing mast cells; richest sources are lung, liver
and intestinal mucosa.
Commercially it is produced from ox lung and pig intestinal mucosa.
28.
29.
30. Actions
A. Anticoagulants :-Heparin indirectly activates plasma AT III by –
1. Providing scaffolding for the clotting factors (mainly xa and Ila) on one hand
and AT-Ill on the other, so that they interact with each other.
2. Inducing conformational change in AT-Ill to expose its interactive sites. A
specific pentasaccharide sequence, which is present in only some of the heparin
molecules, binds to AT III with high affinity to induce the conformational change needed
for rapid interaction with clotting factors.
B. Antiplatelet :-
Heparin in higher doses inhibits platelet aggregation and prolongs bleeding time.
C. Lipaemia cleaning :-Injection of heparin clears turbid post-prandial Iipaemic plasma by
releasing a lipoprotein lipase from the vessel wall and tissues, which hydrolyses
triglycerides of chylomicra and very low density lipoproteins to free fatty acids (FFAs).
31. Pharmacokinetics
Heparin is a large, highly ionized molecule; therefore not absorbed orally.
Bioavailability of s.c. Heparin is inconsistent.
Heparin does not cross blood-brain barrier or placenta (it is the anticoagulant of
choice during pregnancy).
It is metabolized in liver by heparinase and fragments are excreted in urine.
After i.V. Injection of doses < 100 U/kg, the t½ averages 1 hr. It is prolonged to 4-
10 hrs in case of cirrhosis and kidney failure
UFH is safer than LMW heparins or fondaparinux in kidney failure patients.
32. Adverse reaction
Bleeding due to overdose is the most serious complication of heparin therapy.
Heparin-induced thrombocytopenia (HIT) is another common problem(due to
formation of antibody against heparin-platelet complex)
Transient and reversible alopecia is infrequent.
Serum transaminase levels may rise.
Osteoporosis may develop on long-term use of relatively high doses.
Hypersensitivity reactions are rare; manifestations are urticaria, rigor, fever and
anaphylaxis.
Patients with allergic diathesis are more liable.
33. Contraindications
Bleeding disorders, history of HIT.
Severe hypertension (risk of cerebral haemorrhage),
Threatened abortion, piles, g.i. Ulcers (risk of aggravated bleeding).
Subacute bacterial endocarditis (risk of embolism), large malignancies (risk of
bleeding in the central necrosed area of the tumour), tuberculosis (risk of
haemoptysis).
Ocular and neurosurgery, lumbar puncture.
Chronic alcoholics, cirrhosis, renal failure.
Aspirin and other antiplatelet drugs should be used very cautiously during heparin
therapy.
34. Heparin antagonist
Protamine sulfate
It is a strongly basic, low molecular weight protein obtained from the sperm of certain
fish.
I mg is needed for every 100 u of heparin for the treatment of heparin induced
bleeding,
Protamine is more commonly used when heparin action needs to be terminated rapidly,
e.g. After cardiac or vascular surgery.
Adverse reactions :-
In the absence o f heparin, protamine itself acts as a weak anticoagulant by interacting
with platelets and fibrinogen.
Being basic in nature it can release histamine in the body. Hypersensitivity reactions
have occurred.
35. Q. Low mol. Weight Heparin preferred over
conventional heparin for therapeutic uses
Advantage over M.O.A :-
I) LMWH selectively inhibits factor xa with little effect on IIa.
2) They act only by inducing conformational change in AT ill and not by providing a scaffolding
for interaction of AT ill with thrombin.
3) LMW heparins have smaller eftect on aptt and whole blood clotting time than unfractionated
heparin (UFH) with less chance of thrombocytopenia.
Advantage of pharmacokinetics :-
Better subcutaneous bioavailability (70-90%) compared to UFH (20- 30%)
Longer and more consistent monoexponential t½ (4- 6 hours)
Laboratory monitoring is not needed; dose is calculated on body weight basis.
Risk of osteoporosis after long term use is much less with LMW heparin.
36. Indications of LMWH
1.Prophylaxis of deep vein thrombosis (DVT) and pulmonary embolism (PE) in high-
risk patients undergoing surgery; stroke or other immobilized patients.
2. Treatment of established DVT.
3. Unstable angina (UA) and M l: they have largely replaced continuous infusion o f
UFH.
4. To maintain patency of cannula and shunts in dialysis patients.
37. Direct thrombin inhibitors
1. Bivaluridin :-
20 amino acid peptide congener of the larger polypeptide
anticoagulant hirudin secreted by the salivary glands of leech.
It is a specific a nd reversible DT I with quick onset a nd short
lasting anticoagulant action.
Bivalirudin is indicated as an anticoagulant in patients
undergoing percutaneous coronary intervention (PC!)
For STEMI. It is to be used along with an antiplatelet drug viz.
Aspirin and/ or clopidogrel or a glycoprotein llb/ la inhibitor
(Gpl).
It can also be used in unstable angina (UA) and NSTEMI when
urgent or early PC! Is planned. It is specifically o f value in
patients at risk of HIT.
38. 2. Argatroban :-
This is a synthetic non peptide compound which binds reversibly 10 the catalytic site of
thrombin.
Not to the substrate recognition site, it acts as a DTI.
Administered by i.v. bolus (350 µg/kg over 3-5 min) followed by 25 µg/kg/min infusion.
It produces a rapid onset short-lasting antithrombin action.
Argatroban prolongs APTT and its dose is regulated by measuring INR. As such. Care
needs to be exercised while shfiting patients to warfarin prophylaxis.
It is indicated for prophylaxis and treatment of thrombosis and for PCI in patients with
HIT or in those who arc al risk of developing I IIT.
Argatroban is cleared by liver with a biological t½ of 45 min. Thus, it can be given 10
patients with renal disease
40. 1.Vitamin K antagonists
Oral anticoagulant' refers to the warfarin-
like drugs which act by blocking synthesis
of clotting factors.
Mechanism of action :-
They competitively inhibit the enzyme vit
K epoxide reductase (VKOR) and interfere
with regeneration of the active
hydroquinone form of vit K which is a co
factor for gamma carboxylation of factor
II,VII,IX,X.
41. Adverse reactions
A. Bleeding as a result of extension o f the desired pharmacological
action is the most important problem
B. It causes ecchymosis, epistaxis, hematuria, bleeding in the g.I.t.
C. Intracranial or other internal haemorrhages may even be fatal.
Bleeding is more likely if therapy is not properly monitored, or when the
international normalized ratio (I R) exceeds 4, or interacting
drugs/contraindications are present.
42. Q.Advantages of newer oral anti
coagulants over warfarin
• Rapid onset and offset of therapeutic effect
• Short half life
• No laboratory monitoring required
• Fixed dosage guidelines depending on the indication
• Antithrombotic efficacy equal to/better than warfarin.
• Lower risk of bleeding compared to warfarin
• Fewer drug interactions.
43. DIRECT FACTOR Xa INHIBITORS
1. Rivaroxaban :-
It is an orally active direct inhibitor of activated factor Xa
Its anticoagulant action develops rapidly within 3-4 hours of ingestion and lasts for ~24
hours.
It is largely metabolized, but also excreted unchanged in urine
Plasma t½ is 7- 11 hours.
It requires no laboratory monitoring of PT or aPTT.
Use:- a)Prophylaxis anticoagulant used in venous thromboembolism following total
knee/hip surgery;
b) Rivaroxaban has also been found equally effective as warfarin for preventing stroke
patients with atrial fibrillation.
c) 2.5 mg/day for coadministration with aspirin and clopidogrel for prophylaxis of ACS.
Side effects:-Bleeding, nausea. Hypotension, tachycardia and edema.
44. Cont.
2. Apixaban :-
This is another oral factor Xa inhibitor having properties and indications similar to
rivaroxaban.
The oral bioavailability of apixaban is 85% and peak effects are produced in 3 hours.
It is partly metabolized by CYP3A4 and eliminated in both faeces as well as urine.
The plasma t½ is 12 hours.
Use :- a)Prophylaxis of VTE following knee/hip replacement (dose: 2.5 mg BO)
b)prophylaxis of stroke in AF patients (dose: 5 mg 80).
c)Treatment of DVT and PE (dose: IO mg BO for 7 days followed by 5 mg 8D).
Drug interaction :-Drug interactions with inducers and inhibitors o f CYP3A4 are possible
and it should not be used in patients with hepatic or renal impairment.
45. ORAL DIRECT THROMBIN INHIBITOR
Dabigatran etexilate :-
It is a prodrug which after oral administration is rapidly hydrolysed to dabigatran.
This direct thrombin inhibitor which reversibly blocks the catalytic site of thrombin
Though oral bioavailability is low i.e. enhanced by P-gp (efflux transporter)
inhibitors (verapamil, amiodarone, etc.)
Plasma t½ is 14 hours and duration of action 24 hours.
There is no drug interactions and any laboratory monitoring required .
Use :-Prevention of VTE following hip/knee joint replacement surgery and
prevention of embolism and stroke in patients of atrial fibrillation.
Side effects :- Bleeding, dyspepsia, ocaational hepatobiliary disorders.
46. Fibrinolytics
These are d rugs used to lyse
thrombi/clot to recanalize occluded
blood vessels (mainly coronary artery).
The fibrinolytic drugs are:
streptokinase, urokinase, alteplase (rt-
pa) reteplase, tenecteplase etc.
M.O.A :-They are therapeutic rather
than prophylactic and work by
activating the natural fibrinolytic
System (SEE THE PICTURE)
47. Q. Role of streptokinase in Acute myocardial
infarction
The chief indication for fibrinolytic therapy is STEMI
These are the tissue plasminogen activators which forms plasmin from
plasminogen and plasmin degrades the fibrin . In this way they helps in recanalizes
the coronary artery and removes the plaque formation.
Recanalization of thrombosed coronary artery has been achieved in 50-90% cases.
In STEM! Fibrinolytics are an alternative first line approach to emergency
percutaneous coronary intervention (PC I) with stent placement.
Best results are obtained if perfusion can be restored within the first hour (the
golden hour).
48. Q. Role of streptokinase in Acute myocardial
infarction
The chief indication for fibrinolytic therapy is STEMI
These are the tissue plasminogen activators which forms plasmin from
plasminogen and plasmin degrades the fibrin . In this way they helps in recanalizes
the coronary artery and removes the plaque formation.
Recanalization of thrombosed coronary artery has been achieved in 50-90% cases.
In STEM! Fibrinolytics are an alternative first line approach to emergency
percutaneous coronary intervention (PC I) with stent placement.
Best results are obtained if perfusion can be restored within the first hour (the
golden hour).
49. Uses of fibrinolytics
1. Acute myocardial infarction
2. Deep vein thrombosis (DVT) in leg, pelvis, shoulder etc.;
3. Fibrinolytic therapy is indicated in large, life-threatening pulmonary
embolism.
4. Fibrinolytics canalise - 40% limb artery occlusions.
5. Alteplase is approved for use in ischaemic stroke.
50. Contraindications
1. H/o intracranial haemorrhage
2. H/o ischaemic stroke in past 3 months
3. H/o head injury in past 3 months
4. Intracranial tumour/vascular abnormality/ Aneurysms
5. Active bleeding/bleeding disorders
6. Patients receiving anticoagulants
7. Peptic ulcer, esophageal varices
8. Any wound or recent fracture or tooth extraction
9. H/o major surgery within 3 weeks
10. Uncontrolled hypertension
11. Pregnancy
51.
52. Antifibrinolytics
1. Epsilon amino-caproic acid (EACA) :-
It is a lysine analogue which combines with the lysine-binding sites of plasminogen
and plasmin so that the latter is not able lo bind to fibrin and lyse it.
It has been used in many hyperplasminaemic states associated with excessive
intravascular fibrin o lysis resulting in bleeding.
The primary indication of EACA is to counteract the effect of fibrinolytic drugs and
bleeding in case of tooth extraction, prostatectomy, trauma, etc of the
hemophiliacs.
EACA is active orally and can be infused i.V. As well. It is excreted by the kidney.
Side effects:- Hypotension, bradycardia, arrhythmia, ureteric obstruction,myopathy
etc. Not used in renal impairment.
53. 2. Tranexamic acid :-
Like EACA, it binds to the lysine binding site on plasminogen and prevents its
combination with fibrin leading to fibrinolysis.
It is 7 times more potent than EACA,
It is preferred for prevention/ control of
• excessive bleeding due to fibrinolytic drngs.
• Cardio-pulmonary bypass surgery.
• Tonsillectomy, prostatic surgery, tooth extraction in haemophiliacs.
• Menorrhagia, especially due lo i uco.
• Recurrent epistaxis, hyphema due lo ocular trauma, peptic ulcer.
Side effects :- Nausea, diarrhoea. thromboembolic events, disturbed colour vision
allergic reactions etc. Thrombophlebitis occurs due to rapid injection.
54. Notes
Please read the chapter from any standard text book
Prepare the questions arrived in previous years
Write the short notes according to 3-4 points(nature of drug, M.O.A,
pharmacokinetics, indications, side effects etc.)
Read the topics on
A)Adverse effect and management of warfarin
B)Short details on LMWH drugs
C)Advantages of alteplase over Streptokinase
Give flow charts or diagram for writing M.O.A of any drug
For other informations ,please search from other sources(reference books, google,
slideshare etc)