7. Pharmacokinetics:
After administration, Menadione is moderately absorbed in the GIT
via the biliary route. Menadione accumulates in the liver. Menadione
does not cross the placental barrier.
Adverse Drug Reactions:
Liver damage
Brain damage
Death occurs in rare cases
This drug is banned by US FDAbecause of toxic effects
Hemolytic anemia
Therapeutic Uses:
Used as nutritional supplements in animal feed.
In research, it is used in combination with vitamin-C for the
treatment of prostate cancer. 9
9. Pharmacokinetics:
Oral, I.V route of administration, metabolized in liver, undergoes
renal elimination.
Adverse Drug Reactions:
Dizziness, Flushing
Irritation of skin, respiratory tract
Hypersensitivity, Hyperbilirubinemia in premature infants
Therapeutic Uses:
It is used to prevent, control, treat, the coagulant disorder due to
vitamin-K deficiency
9
10. Dose:
Adults:
By Mouth:
For osteoarthritis: A combination product (Wobenzym PS),
providing 600 mg of rutin, 288 mg of trypsin, and 540 mg of
bromelain in divided doses has been used.
10
12. INTRODUCTION
Anti-platelets drugs are the
agents that act against platelet
function.
Anti-platelets drugs prevent the
formation of clot in case of
vascular injuries.
They inhibit platelet aggregation
and thrombus formation .
Antiplatelet are more effective
in arterial circulation where as
Anticoagulants are ineffective.
12
15. Pharmacokinetics:
More than 50% 0f drug gets absorbed upon oral administration. It is
a Prodrug which is metabolized by cytochrome enzyme P450 to give
an active metabolite that is responsible for antiplatelet activity. Oral
dose is excreted in urine, faeces.
Adverse Drug Reactions:
Headaches or dizziness.
Nausea.
Diarrhea or constipation.
Indigestion (dyspepsia)
Stomach ache or abdominal pain.
Nosebleeds.
Increased bleeding (your blood taking longer to clot – for example,
when you cut yourself), or easy bruising.
15
16. Therapeutic Uses:
It is prescribed for the prevention of heart attack, stroke or transient
ischaemic attack (TIA)
Clopidogrel when combined with aspirin is beneficial for acute
coronary syndrome (minor heart attack or unstable angina), a
coronary stent (a device to open up a blocked artery to the heart)
It is used in an open heart operation
It is used in the treatment of peripheral arterial disease
It is used in a vascular operation.
Dose:
75mg/day without taking food.
16
18. ANTI-COAGULANT:
Anti- Coagulants are the drugs
which extend or prolong the
coagulation time of blood.
Anticoagulants are indicated
for the patients which acute
myocardial infarction in the
long term therapy and in
treatment of pulmonary and
venous thrombosis. When
prevention or extension of
thrombus formation is desired
anticoagulant therapy serves
as the best option.
ANTI-COAGULANT
18
19. Ideal characteristics for anti-coagulants agents:
19
It should have rapid Onset of action.
Wide therapeutic index and long duration of action.
Minimal adverse drug effects.
Minimal interaction with drugs and food and should not result into
any life threatening complications.
Pharmacokinetics, pharmacodynamics aspects of drug should be
reproducible such that monitoring blood coagulation is not essential.
20. CLASSIFICATION
20
A. Based on action:
1. DirectlyActingAnticoagulants:
High MolecularWeight Heparin (HMWH)
Low Molecular Weight Heparin (LMWH):
Enoxaparin
New Heparin Derivatives: Fondaparinux, Idraparinux
Dalteparins,
2. In DirectlyActingAnticoagulants:
Coumarin Derivative: Dicumarol, Warfarin
Indanedione Derivative: Phenindione,
Anisindione
21. B. Based on route of administration:
1. InjectableAnticoagulants:
Heparin
Low Molecular Weight Heparin
Heparinoids: Heparin sulphate, Danaparoid,Ancrod, Lepirudin
Miscellaneous Drugs: Bivalirudin, Hirudin
2. OralAnticoagulants:
Coumarin Derivative: Dicumarol, Warfarin sodium,Acenocumarol
Indanedione Derivative: Phenindione,Anisindione
21
25. Mechanism ofAction:
The activation of factors II, VII, IX, and X depends upon reduced
form of vitamin K and enzyme carboxylase. Due to structural
similarity of warfarin with vitamin K, competes with the latter for
reductase an enzyme which activates vitamin K is inhibited and
therefore post translational ϒ-carboxylation of glutamic acid
residues of factors II, VII, IX, and X I also inhibited.
25
26. Pharmacokinetics:
Upon oral administration the drug gets completely absorbed from
GIT. Pharmacological effects reach maximum level after 2 days of
ingestion of the drug. It is metabolized in the liver mixed function
oxidase P450 system.
Adverse Drug Reactions:
unusual bruising, such as: unexplainable bruises, bruises that grow
in size
Nosebleeds, bleeding gums, coughing up blood
bleeding from cuts that takes a long time to stop
heavier than normal menstrual or vaginal bleeding
pink or brown urine, red or black stools
Purple toes syndrome. Symptoms may include: pain and purple or
dark color in your toe
Death of skin tissue. This may happen when blood clots form and
block blood flow to an area of your body. Symptoms may include:
pain, color or temperature change to any area of your body,
29
27. Therapeutic Uses:
Warfarin is used to treat blood clots and to lower the chance of blood
clots forming in your body. Blood clots can cause a stroke, heart
attack, or other serious conditions if they form in your legs or lungs.
reduce the risk of risk of heart attack, stroke, or death
prevent and treat blood clots with atrial fibrillation or heart valve
replacement
prevent and treat blood clots in parts of the body such as the legs
(deep vein thrombosis) and in the lungs (pulmonary embolism)
Dose:
Warfarin is given in a dose of 10-15mg/day from the 3rd or 4th day of
heparin therapy
27
30. Therapeutic Uses:
It prevents the formation of active procoagulation factors II, VII, IX,
X.
Dose:
Anticoagulation:
Adult: PO 300mg day1, 200mg day2, and then 100mg q.d. adjust
dose to maintain desired PT level (dose range 25-250 mg)
30