General Medicine Flashcards
Biguanide MoA
Decerase insulin resistance and hepatic glcose production.
Limit weight gain.
Biguanide Efficacy
- 1-2%
- Can be used with others
- Little side effects
- Low cost
- No hypoglycaemia
Biguanide side effect
- Little or no weight gain
- GI
- Lactic acidosis (with resp, CVD, Renal) HRH
- Vit B12 (absorption)
Sulphonylureas drugs used`
Gliclazide
Glibenclamide
Glimepiride
Tolbutamide
Sulphonylureas MoA
Stimulate B cells to release insulin. Antagonise B cell K/ATP channel activity, increase in K (as it accumulates) so depolarisation. Increased Ca, increased release
Sulphonylureas efficacy
- 1-2%
- Low cost
- Tolbutamide has good post prandial control as it has a short half life so taken 30mins before.
- Others have higher half life and more potent
Sulphonylureas side effect
- Weight gain
* Hypoglycaemia (especially CKD)
Glitazone (TZDs) example
Pioglitazone
Glitazone (TZDs) MoA
Increase sensitivity in muscle and adipose tissue. (via upregulation of signals/ genes)
Glitazone ADRs
• Wegith • Fluid (HF) • Bone metab (osteoporosis) • Bladder cancer • Hoever don’t get hypos • Increase in LDL and HDL Rarely used now
Describe Gliptins and e.gs
Sitagliptin Vildagliptin Saxagliptin Linagliptin • 0.5-0.8 • Weight loss
Gliptins ADRs
• GI symptoms • High cost so 2nd line • Infection Pancreatitis Hypos rare
GLP-1 agonists e.g.s MoA, efficacy
Exenatide Liraglutide
GLP from intestine increases insulin secretion and biosynthesis, decreases glucagon secretion, decreases liver glucose production (indirectly).
Decreases satiety, decreases gastric emptying.
Increases glucose uptake into muscles (indirect)
1-=1.5%
GLP-1 ADRS
- GI, nausea, loose stools, diarrhoea
- GORD
- Painful to inject
SGLT2 e.g.s
Dapagliflozin
Canagliflozin
Empagliflozin
SGLT2 MoA and efficacy
Prevents glucose absorption in the the PCT by SGLT2 (90%)
0.5-1%
SGLT2 ADRS
• Only one extra void a day • UTI, thrush • Polyuria • Hypo (low risk) Urosepsis One one episode of above
Rapid acting insulin onset and name
Insulin Aspart (Novorapid) Insulin Lispro (Humalog) Insulin Glulisine (Apidra) o 5-15 P: 30-60min D: 3-4hr
Short acting
Humulin S
Actrapid
Insuman Rapid
O: 30-60
P: 2-3
D: 6-8
Intermediate acting
Humulin I
Insuman Basal
Insulatard
Isophane (NPH)
O: 1-2
P: 4-6
D: 14-16h
Long acting
Insulin glargine (Lantus); Abasaglar
O: 2-4h
No peak
D@ 20-24h
Insulin Detemir (levimer) Analogue
O:2-4
P: 6-14
D: 16-20
Importance of insulin Toujeo(R)
High strength insulin
Basal once daily
exlusive units
Glargine but flatter peak than other glargine products e.g. Lantus
Always prescribe by brand name and include the concentration of insulin
What is Degludec
Long acting
U100 and U200
What is Humulin R (resistant)
Very potent U500 - 5x stronger than normal insulin For insulin resistant patients Normally TDS before meals Prescribed in marks not U Marks based on 0.3 or 0.5ml insulin syringe. 1 mark = 0.01ml = 5 units