Endocrinology drugs Flashcards
Name one ultrafast acting inuslin
FiAsp (aspartate insulin)
Name one fast acting insulin
Actrapid
Name one short acting insulin
Novorapid, Humulin S, hypurin bovine or procine insulin
Name home intermediate acting insulin
humulin 1- isophane insulin
Name one long acting and ultra long acting insulin
Long acting- Glargine
Ultra long acting- Glarudec
Name one combination insulin or rapid and intermediate insluns given together
Novomix 30, Humulin M3
What class of drugs does metformin belong to?
Biguanides
Give an example of a sulphonylurea used to treat type 2 diabetes?
Gliclazide
Give an example of a glitazone which were used to treat type 2 diabetes?
poiglitazone
How do acarbose work to treat type 2 diabetes?
Inhibit a- glucosidase so inhibit breakdown of carbohydrates to glucose in gut, this lowering blood glucose.
How do glifozins such as dapagliflozin work to treat type 2 diabetes?
Inhibits SGLT2 in the PCT of the kidneys, so more glucose is excreted and less is absorbed into blood.
Name 3 classes of drugs which increase insulin release from beta cells of islets of langerhans
glucagon like peptide 1, sulphonylureas, gliptins/ DDP-4 inhibitors
Name 2 classes of drugs which decrease resistance to insulin?
Biguanide (metformin), glitazones
Ethinyestradiol, mestranol and valerate are examples of synthetic versions of which hormone?
oestrogen
Levonorgestrel, Norethindrone and medroxyprogesterone are synthetic versions of which hormone?
progesterones (progestins- are synthetic progesterones)
What oestrogen antagonist can be used to treat infertility and how does it work?
Clomiphene- inhibits oestrogen and its negative feedback on the anterior pituitary, causing ovulation
Give an example of an oestrogen antagonist used to treat ER+ve breast cancer
Tamoxifen
Give an example of an antiprogestin and state its uses
Mifepristerone
Inuduces labour and used in abortions
State one drug which can be used to prevent hair loss, treat male pattern balding and BPH, describe how it works
Finasteride
Inhibits breakdown of testosterone to dihydrotestosterone, so increases testosterone levels
name two compounds used in HRT
oestradiol, medroxyprogesterone
Name two emergency contraceptions
Levonorgestrel, ulipristal acetate
Give 3 adverse effects of insulin
- hypoglycaemia (insulin levels inappropriately high)
- hyperglycaemia
- lipodystrophy (fat hypertrophy or atrophy at injection site-more so with older insulins)
- Painful injections (more with long acting insulins as are prepared in acid to help preserve them)
- allergies
Describe 2 insulin regimes
- long acting insulin (eg glargine) twice a day, with rapid acting insulin (actrapid, aspart) before meal times
- rapid actin insulin (novorapid) 5-10 mins before meals, maybe delivered by a pump w/ continous low background dose
- low doses of intermediate insulin and rapid insulin, with higher doses of insulin delivered at night time
What is the Hba1c target in those with T2 diabetes?
<7.5%
Give 2 non pharmacological treatments of T2 diabetes
Bariatric surgery, exercise programmes, dieticians
How does metformin work?
- decreases insulin resistance, so more glucose enters tissues
- decreases hepatic production of glucose
- limits weight gain
- decreases CVS events
Give 2 side effects of metformin
- Gi upset
- cant be used in severe CKD
- hypoglycaemia
- lactic acidosis rare but possible
How do sulphonylureas such as gliclazide treat T2 diabetes?
They stimulate beta cells to secrete insulin
What are the 2 main side effects of gliclazide?
- weight gain
- hypoglycaemia
What are the side effects of acarbose?
Flatualance and diarrhoea, so severe that this drug is rarely used now
How do the thiazolidinediones (glitazones) eg pioglitazone work?
- increase sensitivity to insulin
- decrease hepatic gluconeogenesis
- By binding to one or more of the peroxisome proliferator activated receptors (PPARs)
Give 3 side effects of pioglitazone
- weight gain
- fluid retention
- heart failure
- bladder cancer
- effects on bone metabolism
- For these reasons theyre hardly used now
How do glucagon like peptide 1 analogues work in diabetes?
- increase insulin secretion from beta cells
- decrease production of glucagon from alpha cells
- also increase satiety and gastic emptying–> this leads to weight loss
Describe 3 disadvatages and side effects to Glucagon like peptide 1 analogues
- they have to be injected
- GI uset
- GORD
- avoid is CKD
- generally well tolerated however
How do gliptins of DPP- 4 inhibitors work?
They increase glucagon like peptide 1 levels, thus having similar effects to synthetic GLP1 analogues, however arn’t as good at causing weight gain and are more expensive
How do glifozins like dapaglifozin work? What are the 2 common side effects?
inhibits SGLT2 in proximal tubule, so more glucose is excreted however will therefor cause polyuria and increased risk of UTIs and thrush.
How does carbimazole work? What is it used for?
Used to treat hyperthyroidism, it is converted to methimazole by the liver, which inhibits thyroid peroxidases from coupling iodine and thyroglobulin so inhibits T3 and T4 production
give 2 common side effects of carbimazole?
- rashes and pruritis
- GI upset
- headaches, joint pain
- can also get bone marrow surpression but this is rare
When is levothyroxine used and how does it work?
synthetic T4, used to treat hypothyroidism
Give 3 side effects of levothyroxine
palpitations, weight loss, heat intolerance, sweating, anxiety, tremour, increased appetite
What characteristics of synthetic sex hormones give them a long half life?
- 99% bound to albumin and sex hormone binding globulin
- very lipophilic so large Vd
Describe the 3 regimes of COCP you can take?
- monophasic (most common)- O and P taken continiously for 21 days, then 7 day break
- biphasic- continious conc of O, P will increase gradually in second phase of cycle
- triphasic- O conc may change, P conc increases in 3 phases
How 4 adverse effects of the COCP
- increase coagulability –> increase VTE, PE, MI, Stroke risk
- hypertension
- decrease glucose tolerance
- headaches
- weight gain (water retention)
- mood swings
- gall stones
Give 3 absolute and 2 relative contraindications of the COCP?
Absolute: age over 35 and smoking >15p/d, migranes, Hx VTE diseases, breast cancer, Major immobility
Relative: overweight, FHx VTE disease in 1st degree relative <45 yrs, breast feeding
What effect do carbemazepine and rifamicin have on the COCP?
both induce CYP450, so increase COCP metabolism, so decrease efficacy of COCP
List 3 adverse effects of the POP
- weight gain
- fluid retention
- acne
- N+ V
- irritable, PMS, depression
What is the advice if one pill is missed?
take miss pill immediatly, even if means taking 2 in one day, continue taking rest of pack as normal, you should be fine
What is the advice is 2 pills are missed?
Take last pill immediatly, even if means taking two in one day, take rest of pack as normal but use extra contraception for next 7 days.
If in last 7 days of pack, miss break and keep taking the pills
What are the benefits of HRT?
- can reduce vasomotor symptoms and osteoporosis risk
- can improve sleep and QoL
- can improve mood
- Can improve uro- genital symptoms
What are the risks of HRT?
- increase endometrial and ovarian cancer with ERT
- breast cancer risk with HRT
- Can increase risk of stroke and IHD
- Increases risk of VTE
- breast tenderness, headaches, bloating common side effects
What are the two HRT regimes
- O and P continuously for 28 days
- O continuously and P for last 14 days only- if last menstural period >1 yr ago
When is HRT indicated?
- when benefits outweigh risks
- for women with early menopause (before 51), even if asymptomatic
- women under age of 60 with osteoporotic risk
What is raloxifene and when is it used?
A selective oestorgen receptor modulator (SERM) used to reduce osteoporsis risk, which doesnt have any effect on breast or endometrium, but may increase hot flushes
How can HRT be administered?
oral, transdermal, implant, transvaginal, nasal
Why may unopposed oestrogens (ERT) be given to pts who have had radial hysterectomy?
Theyve had ovaries and uterus removed, so no risk of endometrial or ovarian cancer. This will help delay menopause. However they will have to keep taking ERT until the age of normal menopause at age 51.
Describe how insulin release is controlled?
More glucose= more atp production, ATP inhibits ATP sensitive K+ channels, so less K+ efflux, so membrane depolarises, so Ca2+ enters and vesicles of insulin can be released.
How does gliclazide (sulphonylureas) work?
Antagonise ATP sensitive K+ channels so less K+ efflux, so membrane depolarises more so more insulin release
How does metformin work?
Reduces cellular stores of ATP, this increases AMPK, which stimulates glycogen storage, decreases gluconeogenesis and increases tissue sensitivity to insulin
