Drug information of Anisindione

Anisindione

Drug group: Anticoagulants

Anisindione is indicated for the prophylaxis and treatment of venous thrombosis and its extension, the treatment of atrial fibrillation with embolization, the prophylaxis and treatment of pulmonary embolism, and as an adjunct in the treatment of coronary occlusion.

Mechanism of effect

Like phenindione, to which it is related chemically, anisindione exercises its therapeutic action by reducing the prothrombin activity of the blood. By inhibiting the vitamin K–mediated gamma-carboxylation of precursor proteins, the formation of active procoagulation factors II, VII, IX, and X, as well as the anticoagulant proteins C and S is prevented. Anisindione has no direct thrombolytic effect and does not reverse ischemic tissue damage, although it may limit extension of existing thrombi and prevent secondary thromboembolic complications.

Pharmacodynamic

Anisindione is a synthetic anticoagulant and an indanedione derivative. It is prescribed only if you cannot take coumarin-type anticoagulants such as coumadin as anisindione is a powerful drug with serious potential side effects. Anticoagulants decrease the clotting ability of the blood and therefore help to prevent harmful clots from forming in the blood vessels. These medicines are sometimes called blood thinners, although they do not actually thin the blood. They also will not dissolve clots that already have formed, but they may prevent the clots from becoming larger and causing more serious problems.

Pharmacokinetics

Absorption:Accumulation does not occur with repeated dosing

PLASMA HALF-LIFE: 3-5 DAYS

Drug indications

pulmonary embolism , atrial fibrillation , Coronary Artery Disease (CAD

For the prophylaxis and treatment of venous thrombosis and its extension, the treatment of atrial fibrillation with embolization, the prophylaxis and treatment of pulmonary embolism, and as an adjunct in the treatment of coronary occlusion.

Dosage

Initial dosage of anisindione Tablets is 300 mg the first day, 200 mg the second day, and 100 mg the third day. With initiation of treatment, prothrombin activity decreases rapidly to 50 percent of baseline values within 6 hours; thereafter it decreases slowly until it reaches 15 to 30 percent of baseline values in 48 to 72 hours. Maintenance dosage is established from daily prothrombin-time determinations for each patient, although with anisindione Tablets, the uniform, predictable action of the drug makes it possible to reduce the frequency of prothrombin-time determinations in some cases. Maintenance dosage will vary between 25 to 250 mg a day and should be set to keep the prothrombin time one and one-half to two times the normal value. The dose may be repeated for many days; anisindione does not accumulate in the body.

Drug contraindications

underweight , surgery , High Blood Pressure , Hemorrhagic tendencies , Bacterial endocarditis , Pericarditis , Threatened abortion , eclampsia

-Hemorrhagic Tendencies or Blood Dyscrasias

- active ulceration of the gastrointestinal tract

-recent or contemplated brain, eye, or spinal cord surgery or prostatec-tomy, and in those undergoing regional or lumbar block anesthesia or continuous tube drainage of the small intestine

-severe renal or hepatic disease, subacute bacterial endocar-ditis, pericarditis, polyarthritis, diverticulitis, visceral carcinoma, or aneurysm, severe or malignant hypertension, eclampsia or preeclampsia, threatened abortion, emaciation, malnutrition, and vitamin C or K deficiencies

Side effects

Diarrhea , Headache , nausea , vomiting , Blurred vision , urticaria , anorexia , hemorrhage , renal tubular necrosis , jaundice , Agranulocytosis , mouth ulcers , Sore mouth , skin necrosis , Leukopenia , Rash , Pure red cell aplasia , Anuria

Hemorrhage , necrosis , rash ,diarrhea. Dermatitis , nausea, pyrexia, exfoliative dermatitis, urticaria, alopecia, and sore mouth or mouth ulcers, vomiting, abdominal cramps, anorexia, priapism, erythema and necrosis of the skin and other tissues, manifesting as purple toes and cutaneous gangrene, headache, sore throat, blurred vision, paralysis of accommodation, steatorrhea, hepatitis, jaundice, liver damage, renal tubular necrosis, albuminuria, anuria, myeloid immaturity, agranulocytosis, leukocyte agglutinins, red cell aplasia, atypical mononuclear cells, leukopenia, leukocytosis, anemia, thrombo-cytopenia, and eosinophilia, Phenprocoumon-induced delayed callus formation following bone fracture

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Alerts

-Oral anticoagulants are potent drugs with prolonged and cumulative effects. Treatment must be individualized according to patient response, and the benefit expected from anticoagulant therapy should be weighed against the possible hazards associated with the use of these drugs.

-Oral anticoagulants should not be used in the treatment of acute completed strokes due to the risk of fatal cerebral hemorrhage

-Because agranulocytosis and hepatitis have been associated with the use of anisindione, liver function and blood studies should be performed periodically

-Relatively minor bleeding episodes and hemorrhage occur in 2% to 10% of patients treated with oral anticoagulants.

-fatal hemorrhages can occur. Massive hemorrhage from organ systems may involve cerebral, pericardial, pulmonary, adrenal, hepatic, spinal, gastrointestinal, or genitourinary sites.

-Hemorrhagic necrosis and/or gangrene of the skin and subcutaneous tissue, petechial and purpuric hemorrhage, ecchymosis, epistaxis, hematemesis, or hemoptysis, may also occur.

Points of recommendation

-If leuko-penia or evidence of hypersensitivity occurs, the drug should be discontinued

-Because of the possibility of renal damage associated with the use of phenindione, the urine should be tested periodically for albumin whenever phenindione or any indanedione anticoagulant is used.

-Periodic determination of prothrombin time or other suitable coagulation test is essential.

-Since heparin prolongs the one-stage prothrombin time, a period of at least 5 hours should elapse after the last intravenous dose and after the last subcutaneous dose of heparin before drawing blood to determine the prothrombin time when heparin and anisindione have been given together

-In addition to adequate laboratory facilities, a supply of oral or parenteral phytonadione (vitamin K1) and a source of whole blood or plasma should be available when emergency treatment of acute overdosage is required

-Factors which increase sensitivity to the drug and lengthen prothrombin time include:initial hypo-prothrombinemia, increased age, poor nutritional status, vitamin K deficiency or malabsorption, congestive heart failure or vascular damage, hepatic disorders including hepatitis or obstructive jaundice, biliary fistula, febrile states, hyperthyroidism, preparatory bowel sterilization, recent surgery, and X-ray therapy

-Factors which may decrease the response to oral anticoagulants and shorten the prothrombin time include: pregnancy, diabetes mellitus, hyper-lipidemia, hypothyroidism, hypercholesterolemia, and hereditary or acquired resistance.

-The stool guaiac test should be used to detect occult gastrointestinal bleeding.

-In long-term therapy with anticoagulants, periodic laboratory evaluation of organ systems, including hematopoietic, renal, and hepatic studies, should be performed .

 

Pregnancy level

X

X
Anisindione is contraindicated in pregnancy. If oral anticoagulants are used in pregnant women, they should not be administered during the first trimester, and should be discontinued prior to labor and delivery.

Breast feeding warning

Oral anticoagulants or their metabolites are excreted in the milk of nursing mothers, possibly in amounts sufficient to cause a prothrombopenic state and bleeding in the newborn. As a general rule, nursing should not be undertaken while a patient is receiving an oral anticoagulant.

Drug forms

MIRADON

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