Pharmacology

Question 1

What are the top 10 drugs by daily defined dose, per thousand population in Australia?

Answer 1

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1. Atorvastatin - statin class; lowers cholesterol
2. Perindopril - ACE inhibitor class; treats hypertension, heart failure
3. Rosuvastatin
4. Amlodipine- Ca2+ channel blocker; Hypertension, Angina Pectoris
5. Paracetamol- analgesic; pain and fever
6. Irbesartan - angiotensin II antagonist; hypertension
7. Candesartan
8. Ramipril
9. Telmisartan
10. Esomezeprazole - proton pump inhibitor; lowers gastric acid secretion

Tips: Any drugs with -statin suffix is a statin, -sartan is a ang II anta, -pril is an ACE inhibitor

Question 2

What is a blockbuster drug? Name the top 5 by revenue.

Answer 2

• a drug that generates more than USD 1 billion per year. Usually for chronic conditions

Top 5 in 2015

1. Adalimumab - rheumatoid arthritis - Abbvie
2. Ledipasvir - Hepatitis C - Gilead Sciences
3. Etanercept- Rheumatoid arthritis
4. Infliximab - rheumatoid arthritis
5. Retuximab- lymphoma and leukemia autoimmune disorders

Question 3

What is pharmacokinetics?

Answer 3

• fate of substances administered externally to a living organism.

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1. Administration
2. Liberation - release of active ingredient from vehicle
3. Absorption - enters circulation
4. Distribution - disperses through tissues
5. Metabolism - biotransformation
6. Elimination

Question 4

What are the four types of receptors for drug activity and its mode of action?

Answer 4

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1. Ligand-gated Ion channel - Ach receptors —> hyper or depolarization = cellular effects
2. G-protein coupled receptors - Ach receptors —> G-proteins binds with second messengers to initiate protein phosphorylation = cellular effects
3. Kinase linked receptors - e.g. Tyrosine Kinase receptors —> protein phosphorylation, gene transcription, protein synthesis = cellular effects
4. Nuclear receptors - e.g Oestrogen receptors. Gene transcription —> protein synthesis = cellular effects

Question 5

What are properties of drugs affecting absorption, distribution and elimination?

Answer 5

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1. Lipid solubility
2. Formulation of Drug
3. pka—> negative log of acid dissociation constant

Question 6

What are factors affecting drug distribution in the body?

Answer 6

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1. Organisms’ physical volume
2. Removal rate —> portion of drug removed from circulation by each organ; affected by factors like lipid solubility
3. Degree of binding to plasma proteins and other tissues.