Pharmacokinetics Malarkey & Inorganic chemistry Flashcards
What is AUC?
Area under the serum concentration time curve.
What is AUC a measure of?
A measure of the body’s exposure to drug reflecting both input and elimination
What is bioavailability affected by?
Formulation Permeability Solubility Transit time/available absorption surface Lability
How is AUC 0-inf calculated?
Area of a single trapezoid
What is inorganic chemistry?
What is inorganic chemistry?
What is medicinal inorganic chemistry?
The application of inorganic chemistry to therapy or diagnosis of disease
Which metals are vital for many enzymes?
Calcium Iron Lithium Magnesium Chromium Zinc Selenium
What are the deficiency diseases caused by a lack of metals?
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
What are the diseases caused by too much metal in the diet?
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
What are inorganic compounds made of?
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
What are antacids?
Medicines that counteract the acid in your stomach to relieve indigestion and heartburn
- neutralise stomach acid
- alleviate heartburn
- acid reflux
- stomach ulcers
What is lithium carbonate and lithium citrate used for?
In the prophylaxis and/or treatment of
- mania
- bipolar
- manic depression)
- recurrent depression
- unipolar depression
How does lithium treat mania, bipolar disorder and unipolar depression?
Multiple levels of action
- macroscopic neuroprotection
- intracellular changes
What is cis-platin?
Frequently used anti-cancer drug
- best known inorganic drug
- no carbon at all!
What is the structure of cis-platin?
Square planar diammino dichloroplatinum complex
- two pairs of ligands (dative covalent bonds)
- same side of complex
- cis stereochemistry
What is cis-platin used to treat?
Independently - testicular and ovarian cancer
Combination - wider range of cancer conditions
How was cis-platin discovered?
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
How is cis-platin activated?
Reaction with water
How is cis-platin used as a cancer treatment?
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
What are the disadvantages of cis-platin?
Can only be given IV Causes many side effects - nausea - vomiting - kidney damage
What second generation platinum drugs have been developed?
Carboplatin
Oxaliplatin
What are the advantages of carboplatin and oxaliplatin?
Still requires outpatient IV administration but reduced nausea, vomiting and kidney damage
