Pharmacokinetics Malarkey & Inorganic chemistry

Question 1

What is AUC?

Answer 1

Area under the serum concentration time curve.

Question 2

What is AUC a measure of?

Answer 2

A measure of the body’s exposure to drug reflecting both input and elimination

Question 3

What is bioavailability affected by?

Answer 3

Formulation
Permeability
Solubility
Transit time/available absorption surface
Lability

Question 4

How is AUC 0-inf calculated?

Answer 4

Area of a single trapezoid

Question 5

What is inorganic chemistry?

Answer 5

What is inorganic chemistry?

Question 6

What is medicinal inorganic chemistry?

Answer 6

The application of inorganic chemistry to therapy or diagnosis of disease

Question 7

Which metals are vital for many enzymes?

Answer 7

Calcium
Iron
Lithium
Magnesium
Chromium
Zinc
Selenium

Question 8

What are the deficiency diseases caused by a lack of metals?

Answer 8

Calcium - rickets
Iron - anaemia
Lithium - manic depression
Magnesium - convulsions
Chromium - defective glucose metabolism
Zinc - anorexia, dwarfism, anaemia, immune depression, teratogenic effects
Selenium - liver necrosis, cardiomyopathy

Question 9

What are the diseases caused by too much metal in the diet?

Answer 9

Calcium - atherosclerosis, gall stones
Iron - cardiac failure, cancer
Lithium - thyroid disorder
Magnesium - muscular paralysis
Chromium - contact dermatitis, allergy
Zinc - anaemia, metal fume fever
Selenium - hepatic and renal damage, cancer

Question 10

What are inorganic compounds made of?

Answer 10

Salts
- pure inorganic
Organic metal salt
- inorganic and organic part
- sodium acetate
Organometallic
- direct carbon-metal bond
- Grignard
Metal complex
- metal bound to ligands by coordinate covalent bonds
- haemoglobin

Question 11

What are antacids?

Answer 11

Medicines that counteract the acid in your stomach to relieve indigestion and heartburn

• neutralise stomach acid
• alleviate heartburn
• acid reflux
• stomach ulcers

Question 12

What is lithium carbonate and lithium citrate used for?

Answer 12

In the prophylaxis and/or treatment of

• mania
• bipolar
• manic depression)
• recurrent depression
• unipolar depression

Question 13

How does lithium treat mania, bipolar disorder and unipolar depression?

Answer 13

Multiple levels of action

• macroscopic neuroprotection
• intracellular changes

Question 14

What is cis-platin?

Answer 14

Frequently used anti-cancer drug

• best known inorganic drug
• no carbon at all!

Question 15

What is the structure of cis-platin?

Answer 15

Square planar diammino dichloroplatinum complex

• two pairs of ligands (dative covalent bonds)
• same side of complex
• cis stereochemistry

Question 16

What is cis-platin used to treat?

Answer 16

Independently - testicular and ovarian cancer

Combination - wider range of cancer conditions

Question 17

How was cis-platin discovered?

Answer 17

Scientists exploring the effect on electrical currents on the growth of E. coli bacteria

• bacteria stopped growing
• traces of cis-platin formed by the reaction of the platinum electrodes with the growth medium

Question 18

How is cis-platin activated?

Answer 18

Reaction with water

Question 19

How is cis-platin used as a cancer treatment?

Answer 19

The platinum complex binds to DNA in the tumour cell, distorting the double helix structure
DNA replication is blocked
- the cell can no longer divide
- cell death occurs

Question 20

What are the disadvantages of cis-platin?

Answer 20

Can only be given IV
Causes many side effects
- nausea
- vomiting
- kidney damage

Question 21

What second generation platinum drugs have been developed?

Answer 21

Carboplatin

Oxaliplatin

Question 22

What are the advantages of carboplatin and oxaliplatin?

Answer 22

Still requires outpatient IV administration but reduced nausea, vomiting and kidney damage