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Maharana Pratap College of Dentistry
Maharana Pratap College of Dentistry
Important alert- teach patients to read labels of all over the counter and prescription drugs to
determine whether they contain aspirin
Oral Anticoagulants
WARFARIN: first anticoagulant
- Mechanism of action: Warfarin and its congeners act as anticoagulants only in vivo because
they act by interfering with the synthesis of vitamin K dependent clotting factors in the liver.
They block the y carboxylation of glutamate residues in prothrombin, factors VII, IX and X. y
carboxylation is necessary for these factors to participate in coagulation
- Pharmacokinetics: Warfarin is completely absorbed orally and is 99% bound to plasma
proteins.
Adverse effects
• Hemorrhage is the main side effect. Bleeding in the intestines or brain can be troublesome.
Minor episodes of epistaxis and bleeding gums are common
• Treatment depends on the severity: Stop the anticoagulant Fresh blood transfusion is given
• supply clotting factors
Antidote: The specific antidote is vitamin K, oxide. It allows the synthesis of clotting factors.
However, even on IV administration, the response to vitamin K, oxide needs several hours. Hence
in emergency, fresh whole blood is necessary to counter the effects of oral anticoagulants.
• Other adverse effects include allergic reactions, gastrointestinal disturbances and teratogenicity.
Drug Interactions
• Many drugs potentiate warfarin action
• Drugs that inhibit platelet function-NSAIDS like aspirin increase the risk of bleeding Drugs that
inhibit hepatic drug metabolism like cimetidine, chloramphenicol and metronidazole,
allopurinol, erythromycin enhance plasma levels of warfarin.
• Some drugs reduce the effect of oral Drugs that enhance the metabolism of anticoagulants.
• oral anticoagulants-microsomal enzyme embolism. inducers like barbiturates, rifampicin,
griseofulvin enhance the metabolism of oral anticoagulants. When these drugs are suddenly
withdrawn, excess anticoagulantactivity may result in hemorrhages Drugs that increase the
synthesis of clotting factors counter the effect of oral contraceptives.
Factor Xa inhibitor:
• Rivaroxaban directly binds to factor Xa and inactivates it. Since the binding is direct, its onset
of action is faster (3-4 h). Constant laboratory monitoring is not required and is orally effective.
It is useful in the prophylaxis of postoperative deep vein thrombosis and following stroke.
Oral direct thrombin inhibitor
•Dabigatran binds directly to thrombin andto inactivates it.
•Advantage are
•Orally effective (given as dabigatranetexilate)
• Fast onset of action (<2 hr)
•No need for constant lab monitoring
•Long-acting; given once daily
•An antidote idarucizumab is recentlyits effectsmade available which can quickly reverse
Through currently, dabigatran is being used for the prevention of deep vein thrombosis
postoperatively, it could soon be one of thepopular anticoagulants.
COAGULANTS
Coagulants are drugs that promote coagulation (procoagulants) and control bleeding. They are also called hemostatics.
They may be used locally or systemically. Local hemostatics are called styptics. Physical methods like local application
of pressure, tourniquet or ice can control bleeding.
Styptics are used on bleeding sites like tooth socket and wounds.
They are:
1. Adrenaline: Sterile cotton soaked in 1:10,000 solution of adrenaline is com- monly used in tooth sockets and as nasal
packs for epistaxis. Adrenaline arrests bleeding by vasoconstriction.
2. Thrombin powder: It is dusted over the bleeding surface following skin grafting. It is obtained from bovine plasma.
3. obtained from human plasma is available as sheets. It is used for covering or packing bleeding surfaces.
4. Gelatin foam is porous spongy gelatin used with thrombin to control bleeding from wounds. It gets completely
absorbed in 4 to 6 weeks and can be left in place after suturing of the wound.
5.Thromboplastin powder: Is used in surgery as a styptic.
6. Astringents: Like tannic acid are used onbleeding gums.(alum)
Coagulants Used Systemically are
Vitamin K
Vitamin K
FibrinogenSpecific deficient factor-factors, II, VII, VIII, IX, X
Ethamsylate
Vitamin K: Vitamin K is a fat-soluble vitamin essential for the biosynthesis of clotting factors. There are three
compounds:
Vitamin K1-present in food from plant source
Vitamin K2-produced in the gut bybacteria
Vitamin K3 a synthetic compound used therapeutically.
Actions: Vitamin K is essential for thebiosynthesis of clotting factors-prothrombinand factors VII, IX and X by
the liver.
Human requirement: Not clearly known- recommended intake in adults is 50-70 mg/day.
Deficiency: Vitamin K deficiency results from liver diseases, malabsorption, long-term antibiotic therapy and
rarely by dietary deficiency. It is manifested as bleeding tendencies.
Vitamin K
• Adverse reactions are seen on parenteral administration of vitamin K-allergic reactions and
jaundice can occur.
• Uses
• Vitamin K deficiency
• Newborn babies lack intestinal flora and have low levels of prothrombin and other clotting
factors. Routine administration of vitamin K-1 mg IM prevents hemorrhagic disease of the
newborn
• Oral anticoagulant toxicity.
Other Coagulants
• Fresh plasma or whole blood is useful in most coagulation disorders as it contains all the clotting factors
• Concentrated plasma fractions likefibrinogen, factors VIII, II, VII, IX and Xare available for the treatment of
specific deficiencies
• Snake venom: Some venoms like Russelsviper venom stimulate thrombokinase andpromote coagulation
• Ethamsylate is used orally to arrest bleeding.
• The exact mode of action is not known but it is thought that it acts by inhibiting the synthesis of prostacycline
(PGI,) and correct the abnormal platelet function.
• It may also stabilize the wall of the capillaries and reduce capillary bleeding. Ethamsylate is given orally to
control bleeding in:
• Dental extraction and other proceduresin patients with coagulation disorders
• Menorrhagia
• Postpartum hemorrhage
• Hematemesis and malena.
Dentistry and Drugs Affecting Coagulation
• Most dental procedures including minor ones like scaling and tooth extraction involve some
bleeding stops by itself. However, even minor dental procedures may result in continuous
bleeding from the site in the following patients:
• Patients receiving drugs that inhibit coagulation
• Thrombocytopenic purpura
• Vitamin C deficiency
• Hemophiliacs
• Long-term glucocorticoid therapy. For management of bleeding.
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