Block 7 Endocrine - Drugs And Management

Front 1

Pharmacological treatment of thyrotoxicosis?

MOA?

Back 1

THIONAMIDES:
1. Methimazole (MMI, Tapazole®)
2. Carbimazole (Neomercazole®)
3. Propylthiouracil (PTU)

Drug of choice in Aust = Neomercazole®

MOA = block activity of peroxidase
--> prevent organification of I-
--> prevent coupling of DIT/MIT to form T3/T4

PTU also blocks 5'-deiodinase (which converts T4 to T3)

Front 2

Indications and contraindications, advantages and disadvantages for radioactive iodine in thyrotoxicosis?
Does the thyroid status of the Pt matter?

Back 2

INDICATIONS: newly diagnosed Graves', relapsed Graves', toxic nodular hyperthyroidism

CONTRAINDICATIONS: pregnancy!!

ADV: effective cure, outpatient, easily applicable, reduced goitre

DISADV: slow effect over months, permanent hypothyroidism in >60% pts, deferral of pregnancy for 6mo

NB: Pt should be euthyroid before commence treatment

Front 3

Indications and contraindications, advantages and disadvantages of SURGERY in thyrotoxicosis?
Does the thyroid status of the Pt matter?

Back 3

ABSOLUTE INDICATIONS: thyroid cancer, obstructive symptoms
RELATIVE INDICATIONS:
failure or non-compliance with medical treatment, large goitre, pregnancy if clinically sig. drug side effects

ADV: rapid control hyperthyroidism, 100% cure

DISADV: invasive, expensive, permanent hypothyroidism, pain, scarring, complication risk (hypoparathyroidism, recurrent laryngeal n.)

Front 4

carbimazole

Back 4

anti-thyroid drug
brand name = neomercazole

Front 5

Anti-thyroid drug regime

Back 5

Therapy for hyperthyroidism generally starts at a high daily dose of 15 - 40mg continued until the patient has normal thyroid function, and then reduced to a maintenance dose of 5 - 15mg. Treatment is usually given for 12 - 18 months followed by a trial withdraw.

Front 6

proylthiouracil

Back 6

PTU = anti-thyroid drug

Front 7

Treatment options hyperthyroidism

Back 7

1. Anti-thyroid drugs
2. Radioactive iodine
3. Surgery

Front 8

Treatment for hypothyroidism

Back 8

Thyroxine (levothyroxine)

Front 9

Treatment options for pituitary tumour

Back 9

1. surgery
2. radiotherapy
3. medical therapy

Front 10

medical therapy for prolactinoma.
MOA?

Back 10

dopamine receptor agonists (cabergoline).

MOA = binds D2 receptors. Inhibits synthesis and release of prolactin

Front 11

cabergoline = ?

Back 11

potent dopamine receptor agonist on D2 receptors.
First-line agent in the management of prolactinomas

Front 12

octreotide = ?

Back 12

Somatostatin analogue. Inhibits growth hormone. Also decreases tumour size of GH-secreting adenoma

Front 13

medical therapy for GH-secreting adenoma?

Back 13

Octreotide (somatostatin analogue)

Front 14

medical therapy for corticotropin-secreting adenoma?

Back 14

Ketoconazole (=anti-fungal agent that inhibits adrenal steroidogenesis). Not effective LT treatment. Usually reserved for patients unsuitable for surgery, or whose tumour has recurred post-surgery/radiation.

Front 15

Ketoconazole = ?

Back 15

anti-fungal agent that inhibits adrenal steroidogenesis

Front 16

Radiation therapy for pituitary tumours. When and how is it used?

Back 16

used in patients with recurrent or incompletely excised tumours, or patients that are unable to tolerate trans-sphenoidal surgery or medical therapy.

can be delivered by conventional external beam techniques, stereotactic radiosugery techniques, or isotope-labelled radiopharmaceuticals

Front 17

route used for surgical excision of pituitary adenoma? when wouldn't you use this route?

Back 17

Transphenoidal microsurgery.

May have to use a transcranial route if tumour has extended into subfrontal, retrochiasmatic or middle cranial fossae

Front 18

describe route of administration for the following:
1. steroids
2. thyroid hormone
3. insulin
4. testosterone
5. gonadal steroids
6. DDAVP (desmopressin)

Back 18

1. steroids = oral
2. thyroid hormone = oral
3. insulin = subQ injection, pump
4. testosterone = depot IM injection
5. gonadal steroids = transdermal
6. DDAVP = intranasal spray, solution, oral

Front 19

DDAVP= ?

Back 19

Desmopressin (trade names: DDAVP, Stimate, Minirin) is a synthetic replacement for vasopressin

Front 20

Addison's disease treatment

Back 20

Gluucocorticoid dose is 25 mg cortisone acetate mane and 12.5 mg nocte to mimic diurnal rhythm. Cortisone acetate is given at a minimum of two doses per day in Addison's disease. The half life of cortisone acetate is not long enough to sustain a once a day dose. In active individuals a third (midday) dose may be required.

PLUS fludrocortisone dose which is generally fixed

Front 21

Atosibar = ?

Back 21

oxytocin antagonist used to prevent premature birth

Front 22

syntocinon = ?

Back 22

Synthetic oxytocin - used to induce labour or induce ejection of the placenta after birth

Front 23

Glucocorticoid and mineralocorticoid relative potency of:
hydrocortisone
dexamethasone
prednisone
betamethasone

Back 23

hydrocortisone G=1, M=1
prednisone G=4, M=0.25
betamethasone G=25, M<0.01
dexamethasone G=30-40, M<0.01

Front 24

give doses of prednisone and dexamethasone equivalent to 20mg hydrocortisone

Back 24

20mg hydro
= 5mg pred
= 0.5mg dex

Front 25

what do you give in emergency anaphylaxis

Back 25

endogenous hydrocortisone IV

Front 26

what steroid do you give to prevent cerebral oedema?

Back 26

dexamethasone

Front 27

what are the basal needs of hydrocortisone per day?
when does this increase?

Back 27

20-25mg
mild illness x2-3
major stress x10

Front 28

management of hypoglycaemia if conscious

Back 28

"15 rule"
15g fast acting CHO (7 jelly beans, 150mL soft drink, 100mL glucozade, 3 tsp honey)

15g complex CHO (1 pce fruit, 1 slice bread, 2 buscuits)

15 mins later - re check BGL and if still low, give more fast acting

Front 29

management of hypoglycaemia if unconscious

Back 29

IV injection 50% glucose (20-25mL)
IV injection glucagon
then 15g complex CHO once awake

Front 30

after treatment of severe hypoglycaemia, what do you do if BGL are then really high?

Back 30

BGL may rebound - do NOT treat hyperglycaemia aggressively in the first 24-48 hrs

Front 31

rapid acting insulin = ?

Back 31

analogues, absorbed rapidly, injection immediately before food, less likely to cause hypo
acting time = 2-3 hrs
onset = 0-20 mins

brands = Apidra, NovoRapid, Humalog

Front 32

short acting insulin = ?

Back 32

solution of human insulin
onset of action w/in 30 min
Duration 6-8 hrs

brands = Actrapid, Humulin R

Front 33

intermediate acting insulin = ?

Back 33

isophane aka NPH insulin
(complex of insulin bound to protamine which is a non-immunogenic fish protein)
insulin released gradually into tissues
onset = 1.5hr
duration up to 24hr
differs bw brands

Brands = protaphane, humulin NPH

Front 34

Long acting insulin = ?

Back 34

human insulin complexed with zinc
rarely used - replaced by analogues

Front 35

very long acting insulin = ?

Back 35

analogue, replaced long-acting
there are 2: glargine and detemir
24 hr duration
peak 3-14 hours

Glargine = Lantus
chemically modified so insoluble after injection

Detemir = Levemir
insulin binds to albumin from which it is slowly released

Front 36

management DKA

Back 36

rehydration
restore normoglycaemia (insulin)
look for infection
replace K+ to prevent hypokalaemia
monitor K+, glucose, HCO3-, creatinine hourly

Front 37

treatment candidiasis

Back 37

topical, poorly absorbed antifungals
= IMIDAZOLE group, or AMPHOTERIUN

or single oral dose imidazole

occ. IV for serious infection

Front 38

treatment cellulitis
oral or IV? why?

Back 38

Oral therapy. For staph: FLUCLOXACILLIN or DICLOXACILLIN monotherapy.

Or can use cephalexin (didn't really understand what you're supposed to use)

more severe or strep --> phenoxymethylpenicillin

can give IV if unsuitable for oral, vital signs indicate septicaemia, rapidly progressing, immobile

Front 39

pharmacological treatment of obesity?

Back 39

1. Phentermine (duromine)
2. Orlistat (Xenical)
3. Sibutramine (Meridia)

Front 40

phentermine = ?

Back 40

chemically related to amphetamine - works predominantly on noradrenaline to reduce appetite.
central stimulant --> HTN, tachycardia, nervousness, headache, insomnia, tremor

Front 41

orlistat = ?

Back 41

pancreatic lipase inhibitor
reduces the absorption of fat by roughly 30%
not absorbed in bloodstream, not an appetite suppressant.
can't eat high-fat meal or get incontinence and greasy stools.
average weight loss 7-8%

Front 42

sibutramine = ?

Back 42

combination noradrenaline and serotonin reuptake blocker.
no serotonin-releasing action therefore pharmacologically more like SSRIs.
weight loss av. 5-8%
has been ass'd with incr. BP - shouldn't be used in people with poorly controlled HTN

Front 43

oral hypoglycaemic therapy classes

Back 43

1. Sulphonylureas
2. Biguanides
3. alpha-glucosidase inhibitors
4. meglitinides
5. thiazolidinediones
6. DPP-4 inhibitors

Front 44

Sulphonylureas = ?

SE?

Back 44

potentiate glucose-stimulated insulin release.
combine with sulfonylurea receptors of beta-cells.
close potassium channels (like glucose!)
depol of cell
calcium influx
insulin released

SE= weight gain, hypoglycaemia

Front 45

Biguanides = ?

SE?
Contraindications?
Adv?

Back 45

Metformin is the only one currently available.
increased glucose uptake into skeletal muscle and fat
appetite suppression (?gastric irritation)
decreased intestinal glucose absorption
decreased gluconeogenesis

DOES NOT STIMULATE INSULIN

SE= transient nausea, diarrhoea. Also LACTIC ACIDOSIS - check renal fn

CONTRA = significant renal failure (excreted entirely by kidneys)

ADV = prevents weight gain, may assist weight loss

Front 46

metformin = ?

Back 46

Biguanide oral hypoglycaemic agent

Front 47

T/F metformin stimulates insulin release

Back 47

FALSE

Front 48

T/F big side effect of metformin is risk of hypoglycaemia

Back 48

false

Front 49

alpha-glucosidase inhibitors = ?

SE?

Back 49

most widely used = ACARBOSE!
inhibit enzyme that breaks down dietary complex carbs to sugars.
reduces quantity of glucose available for abs'n across intestinal wall.
less effective - use in combination with sulphonylureas or metformin

SE = not well tolerated --> abdo distension, pain, flatulence

Front 50

first line OHA?

Back 50

metformin

Front 51

meglitinides = ?

Back 51

only drug = REPAGLINIDE

stimulate same R as sulphonylureas but at diff site.
actions/se similar to sulphonylureas

short acting take bd

Front 52

thiazolidinediones = ?

SE = ?

Back 52

Act on PPAR-g (peroxisome proliferator receptors) in fat cells.

can cause SUBSTANTIAL WEIGHT GAIN

Front 53

DPP-4 inhibitors = ?

Back 53

Dipeptidyl dipeptidase inhibitors - they INHIBIT the activity of the enzymes that break down INCRETINS!

incretins = gut hormones GLP-1 and GIP. These incretins normally stimulate insulin-mediated glucose release from the pancreas following an oral glucose load.

GLP-1 also inhibits secretion of glucagon, inhibits gastric emptying and thus delays glucose absn

Front 54

melatonin

Back 54

light dark cycle regulation

sleep disorders, blind persons

Front 55

budenoside, ciclesonide

Back 55

long term asthma

action of GCS

Front 56

fluticasone

Back 56

long term asthma

action of GCS

Front 57

metyrapone

Back 57

Dx of adrenal insufficiency, sometimes Tx of cushings

inhibits cortisol synthesis via 11 β hydroxylase

Front 58

what makes steroid myopathy worse?

Back 58

9-α fluorinated corticosteroids


changing to prednisone produces improvement

Front 59

Prostaglandin synthetase inhibitors

Back 59

Abnormal uterine bleeding

inhibit synthesis of prostaglandin, also interfere with myometrial prostaglandin E2 binding

Front 60

Tranexamic acid (antifibrinolytic)

Back 60

Abnormal uterine bleeding

inhibit plasminogne activator

Front 61

Norethisterone

Back 61

Abnormal uterine bleeding

Is a progesterone, can be used in combo or stand alone

Front 62

Dydrogesterone

Back 62

Abnormal uterine bleeding

Front 63

Depo Provera

Back 63

Abnormal uterine bleeding/contraception

progesterone only contraceptive

Front 64

Implanon

Back 64

inhibit ovulation

abnormal bleeding, contraception

Front 65

Danazol

Back 65

abnormal uterine bleeding

inhibits endometrial proliferation causing endometrial atrophy

androgenic side effects

Front 66

Goserelin, Nafarelin

Back 66

(GnRH agonist)


initial agonist of pituitary, followed by 'exhaustion' --> hypogonadotrophic hypogonadism


long term use complicated by decreased bone mass