1.

What is anticoagulant ( Blood Pharmacology )

Blood coagulates by transformation of soluble fibrinogen into insoluble fibrin. Circulating

proteins interact in a “cascade”, where clotting factors undergo limited proteolysis to become
active serine proteases.

Anticoagulants are drugs that decrease the formation of fibrin clots

2. Compare Heparine and Warfarin

Feature Heparin(s) Warfarin (Coumarins)

Chemical Nature Large polysaccharide, water-soluble Small molecule, lipid-soluble

derivatives of vitamin K

Kinetics Given parenterally(IV,/SC), hepatic Given orally, 98% protein bound,

and reticuloendothelial elimination, PO, liver metabolism, half-
half-life=2h, no placental across life=30+h, placental across

3. Which properties of heparin involve hypersensitivity and half-life?

Heparin is a mixture of sulfated polysaccharides with molecular weights of 15-20000 daltons.

Low-molecular-weight (LMW) heparins (eg., enoxaparin) have potential adventage of longer
half-life, less thrombocytopenia, and possibly enhanced activity against factor Xa

Danaparoid, a heparin of different structure, may be safer in hypersensitivity to heparin

4. Which mechanism of aspirin in anticoagulation?

The major well-documented antithrombotic action of aspirin is to acetylate cyclooxygenase-1

(COX-1) in platelets, leading to the inhibition of thromboxane A2 (TXA2) synthesis.
Decreased production of this lipid platelet agonist impairs platelet aggregation.

5. Can warfarin be used in combination with sulfonamide for anticoagulant?

Yes, the combination of warfarin and sulfonamide drugs can potentially increase the risk of
bleeding. Sulfonamide antibiotics, such as sulfamethoxazole-trimethoprim, can inhibit the
metabolism of warfarin, leading to an increase in the anticoagulant effect of warfarin and a
higher risk of bleeding complications. Therefore, caution should be exercised, and close
monitoring of the international normalized ratio (INR) is necessary if these medications need
to be used together. It is important to consult with a healthcare professional to assess the
potential risks and benefits before combining warfarin and sulfonamide drugs for
anticoagulant therapy.
6. Can warfarin be used in combination with Vitamin K for anticoagulant?

No, Warfarin interferes with the action of vitamin K and therefore prolongs the time it takes
to form a clot. This is the intended effect of this therapy. Increasing vitamin K intake while
you are on warfarin will work against the action of this medication.

7. Why can warfarin cause to bleed in patients?

Warfarin can cause bleeding in patients because of its anticoagulant, or blood-thinning,

effects. Warfarin works by inhibiting the production of certain clotting factors in the liver that
depend on Vitamin K. These clotting factors are essential for the normal formation of blood
clots to prevent excessive bleeding.

8. Mention 3 anticoagulants which can be used to reduce hypersensitivity?

Heparin / Urokinase / tPA

9. What are mechanisms of antigoagulants?

Anticoagulants derive their effect by acting at different sites of the coagulation cascade.
Some act directly by enzyme inhibition, while others indirectly, by binding to antithrombin or
by preventing their synthesis from the liver (vitamin K dependent factors)

10. Streptokinase is an anticoagulant. Why does it cause hypersensitivity?

High antibody titres are associated with hypersensitivity reactions to streptokinase. This has
important implications in reinfarction thrombolysis. In patients whose antistreptokinase
antibody titres are likely to be raised the avoidance of streptokinase-related thrombolytic
agents should be considered.

11. Can warfarin combine with aspirin for anticoagulants?

Yes, This combination can help prevent both clot formation within blood vessels
(anticoagulation) and platelet aggregation (antiplatelet effect).

However, combining warfarin and aspirin increases the risk of bleeding. Both medications
individually can increase the risk of bleeding, and when used together, the risk is further
amplified.

12. Mention hormones in male and female?

Female : Estrogen and Progesterone

Male : Testosterone

13. Mention three drugs used in antidiabetes?

Sulfonylureas / Metformin / Thiazolidinediones

14. Mention one drug can not be used with ketoconazole?

Methadone

15. What happens when using antidiabetes drugs for a long time?

When using antidiabetes drugs for a long time, potential effects include improved blood sugar
control, possible tolerance or reduced effectiveness, side effects such as gastrointestinal
issues or weight gain, and a decreased risk of long-term complications when properly
managed. Regular monitoring and communication with a healthcare professional are
important for optimal management.

16. What are the functions of Adrenosteroids?

For use in inflammatory disorders (and adverse effects)

17. Mention 2 drugs of Antidiabetes which can be combined together?

Sulfonylureas + Metformin

18. Which drug can be treated in osteoporosis?

Oral Contraceptives (Combinations of estrogens (ethinyl estradiol, mestranol) with progestins

(norgestrel, norethindrome)

19. Mention a product that can be used in tumor treatment of thyroid gland?

Radioiodine

20. What are side effect of Adrenal Asteroids?

The most common side effects of hydrocortisone tablets are feeling dizzy, headaches, swollen
ankles and feeling weak or tired. Taking hydrocortisone tablets can affect your immune
system so you're more likely to get infections.

21. Can we use Prednisolone for a long time? Explain

No, When taking corticosteroids by mouth for a longer term, you may experience: Problems
with the eyes, such as glaucoma or cataracts. A round face, which is sometimes called moon
face. High blood sugar, which can trigger or worsen diabetes.

22. ADME (Mention four processes of pharmacokinetics)

Absorption

Distribution

Metabolism

Excretion

23. Why a drug need to gr though four steps? Explain

Going through the cell walls (cross the membrane) to go into the plasma.

To be distributed because it needs to go to the exact target organs.

To be converted to the soluble (hydrophilic) metabolites to be excreted easily. Less

pharmacological compounds / more activity metabolites than pro-drugs

To remove toxins and remaining compounds

24. Important of biotransformation?

Same with the metabolism

25. How many phases in biotransformation?

Two phases: Oxidation/Reduction/Hydrolation (Cytochrome P450/Transferase)

Conjugation with endogenous compounds 600mg initial, excretion time 60 mg/h, draw
elimination curve of this drug in 5 hours

Zero order:

After 5h - 300 mg of drug be excreted - 300 mg remaining

26. What do you think about the study about ionized and non-ionized drugs?

Needs to study for drug absorption, drug distribution & drug elimination

Applications of ionized and non-ionized to develop drug and usage of drug

27. Why you need to ionization of drugs?

Ionization of drugs is important for their solubility, absorption, distribution, receptor binding,
and elimination in the body. It affects their ability to cross biological barriers, interact with
target sites, and be excreted.

28. Properties of drug to permeate the membrane?

Drug solubility

Gradient Concentration

Something

29. Types of drug uptake. Which one do not perform the absorption?

Intravenous

Intramuscular

Oral

Properties of ionized and non-ionized (Study the calculation equations)

 Pharmacodynamics

30. Affinity + Potency + Efficacy of Drug

Affinity: The closer the drug curve, the stronger it interacts

Potency: Nearer the y axis - higher potency

Efficacy: The highest point (along the y axis) of the drug

31. Quality of Partial Agonists

Full agonist + another partial agonist - antagonist (reduce the efficacy of drug)

32. Person uses 500g of Vitamin C. How long it has been eliminated almost?

First order: t1/2 à divided over time

33. What we do to eliminate calcium oxalate?

People who are more likely to form calcium oxalate stones should avoid foods high in oxalate
such as beets, spinach, many types of berries, sweet potatoes, soy, nuts, chocolate, brewed
tea, and colas.

34.

Pharmacokinetics and Pharmacodynamics

Pharmacokinetics

ADME (Mention four processes of pharmacokinetics)

· Absorption:

•Drug entry into the systemic circulation from site of administration

•Determinants are those for drug permeation

•Intravascular administration (IV) does not involve absorption

•With extravascular administration (eg. PO, IM, SC, inhalation) less than 100% of a
dose may reach the sytemic circulation, due to variations in bioavailability
· Distribution:

•Depends on drug solubility and binding to plasma proteins

•Equilibrium between bound and free drug molecules

•Only unbound drug (free fraction) exerts pharmacological effects

· Metabolism

· Excretion

Why a drug need to gr though four steps? Explain

• Going through the cell walls (cross the membrane) to go into the plasma.

• To be distributed because it needs to go to the exact target organs.

• To be converted to the soluble (hydrophilic) metabolites to be excreted easily. Less

pharmacological compounds / more activity metabolites than pro-drugs

• To remove toxins and remaining compounds