Vitamin K

It can be used for oral anti-coagulants.

Mechanism of action:
It causes post-translational modification of factors VII, IX and X.

Therapeutic uses:
It is usually administered to all newborn babies in order to prevent vitamin K deficiency leading to hemorrhagic diseases which is common in premature infants.

It is also used as an antidote of warfarin.

Adverse effects:
Rapid infusion of vitamin K may lead to chest pain, back pain and dyspnea.

Protamine sulfate

It is an antidote for heparin.

It is obtained from fish sperm.

It is strongly basic macromolecule due to the presence of more amount of arginine.

In this positive charge of protamine forms complex with negative charge of heparin (a polyanionic macromolecule) neutralizing its activity.

It is administered IV after proper dilution with physiological salt solution. Its duration of affect is 2 hours.

Hypersensitivity reactions may develop. On rapid injection, flushing, dyspnea, hypotension, and bradycardia may be caused.

Aminocaproic acid and Tranexamic acid

These are synthetic inhibitors of plasminogen activator with antiplasmin activity.

These are active orally and excreted in urine. Tranexamic acid can cross placenta.

Therapeutic uses:
Aminocaproic acid is effective in the treatment of complications caused by fibrinolysis such as in the treatment of cardiac bypass or major thoracic surgery. It is also found useful in the treatment of subarachnoid hemorrhage and angioedema.

The most important use of tranexamic acid is in the treatment of ovarian tumor which is malignant.

Adverse effects:
They may cause IV thrombosis.

Aminocaproic acid may cause rash, erythema, nausea, diarrhea and heartburn. It also some of the antiadrenergic effects leading to hypotension and nasal stuffiness.

Dosage:
Tranexamic acid is administered as 15mg/kg orallyas a loading dose then 30 mg/kg four times a day.

Classification of Coagulants

Introduction:

These are the substances which are helpful in the coagulation of the blood.

Bleeding can be caused by
1. Fibrinolytic states arising after prostatectomy or gastrointestinal surgery.
2. Hemophilia

In this case, hemophilia can be caused due to decrease of plasma coagulation factors such as factor VIII or IX.

Classification of Coagulants:
Protamine sulfate, Vitamin K, Aprotinin

Fibrinolytic inhibitors:
Aminocaproic acid, Tranexamic acid

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Atorvastatin

Salt form of Atorvastatin is used i.e. atorvastatin calcium. It belongs to a drug calss of Statins.

Structure:

Credit: Drugbank.ca

Mechanism of Action:
It works by inhibiting the enzyme HMG-CoA (Hydroxymethyl glutaryl Coenzyme-A) reductase, which is present in the tissues of the liver and is responsible for the production of cholesterol in the body via mevalonate pathway.

Pharmacokinetics:
Maximum plasma concentrations is found within 1 to 2 hours. Absorption increases with increasing the dose of the drug. The absolute bioavailability is found to be 14%.

Uses:

It is used for the treatment of Cholesterol i.e. hyperlipidemia, dyslipidemia and hypercholesterolemia. It is used to reduce the risk of myocardial infarction, stroke and angina.

Side effects:
It may cause diarrhea, apin in extremeties and urinary tract infections.

Brand Names:

• Atogal (Ingers (Czech Republic))
• Atorpic
• Cardyl (Pfizer (Spain))
• Faboxim (Fabop (Argentina))
• Hipolixan (Pasteur (Chile))
• Lipitor (Pfizer, Elea (Argentina))
• Lipotropic (Drugtech (Chile))
• Lipovastatinklonal (Klonal (Argentina))
• Liprimar (Pfizer (Hungary, Ukraine), Goedecke (Russia))
• Lowden (Saval (Chile))
• Normalip (Quesada (Argentina))
• Sincol (Indeco (Argentina))
• Sortis (Pfizer (Austria, Czech Republic, Germany, Hungary, Poland, Portugal, Switzerland), Godecke (Germany), Parke, Davis (Germany))
• Sotis
• Torvacard (Zentiva (Czech Republic, Hungary, Poland, Russia, Ukraine))
• Torvast (Pfizer (Italy))
• Totalip (Guidotti (Italy))
• Tozalip
• Tulip (Lek (Czech Republic, Russia), Wermar (Mexico), Sandoz (Poland, Ukraine), Pharmacia (Spain))
• Vastina (Penn (Argentina))
• Xanator (Sieger (Greece))
• Xarator (Parke, Davis (Italy))
• Xavator
• Zurinel (Prater (Chile))

It is also available in the combination with amlodipine with the name of "Caduet".

Serotonin receptor blockers

5-HT3 serotonin receptor blockers include Ondansetron and granisetron.

Action:
It blocks 5-HT3 receptors in the periphery (visceral afferent fibers) and in the brain (chemorecptor trigger zone).

Pharmacokinetics:
• Orally or IV
• Prevents vomiting in 50 – 60% of patients treated with Cisplatin.

Clinical Uses:
It is used as prophylaxis of nausea and vomiting associated with cancer chemotherapy.

Side affects:
Headache.

5-HT1c and 5-HT2 receptor blockers include Ketanserin.

Action:

This drug potently blocks vascular α1-adrenoceptors resulting in hypotensive action. It antagonizes platelet aggregation caused by serotonin by blocking 5-HT2 receptors on platelets.

Uses:
It is used in hypertension and vasospastic conditions.