Clinical Pharmacology of Statins + Lipase Inhibitors

Question 1

Obesity

Answer 1

BMI > 30kg/m2

Waist circumference

Question 2

ORLISTAT - clinical indications of use

Answer 2

used to maintain weight loss rather than loose further weight
cease treatment after 12 weeks if weight loss has not exceeded 5% since the start of treatment

Question 3

ORLISTAT - mechanism of action

Answer 3

Antagonises lipase enzyme - stops fat being passively absorbed by duodenum

Question 4

ORLISTAT - side effects

Answer 4

Oily spotting
Flatus with discharge
Faecal urgency 
Fatty/Oily stool 
Increased defecation + faecal incontinence

Question 5

ORLISTAT - pharmacokinetics

Answer 5

ABSORPTION 
minimal 
onset of action = 24- 48 hrs
peak = 8 hrs 
duration of action = 48-72 hrs 
half life elimination = 1-2 hrs 
protein binding = >99% 
METABOLISM 
GI wall = forms inactive metabolites 
EXCRETION
faeces - majority unchanged drug

Question 6

METHYLCELLULOSE - clinical indications for use

Answer 6

constipation
diarrhoea 
obesity 
- produces feeling of satiety 
- attempted use for control of appetite 
- little evidence of efficacy

Question 7

METHYLCELLULOSE - mechanism of action

Answer 7

powder or gel
polysaccharide polymer - not absorbed from the GIT
forms a gel within intestine - distends it
stimulates peristaltic activity
acts mainly in colon - take 1-2 day to work

Question 8

METHYLCELLULOSE - side effects

Answer 8

few side effects
mild laxative effects
flactulence

Question 9

METHYLCELLULOSE - pharmacokinetics

Answer 9

ABSORPTION
- unabsorbed - uncovered in faeces
volume of distribution = accumulation in liver/spleen/lymph nodes/kidney/vascular walls
METABOLISM
n/a
route of elimination = appear unchanged in faeces

Question 10

ATROVASTATIN/SIMVASTATIN - clinical indications of use

Answer 10

lower LDL- C 
familial& non-familial 
hypercholesteremia & mixed dyslipidemia 
hypertriglyceridaemia 
prevention of cardiovascular events