CH6: ENDO DRUGS Flashcards

1
Q

vasopressin

A
  • antidiuretic hormone
  • treatment used for limited time = trauma/pituitary surgery
  • doses are tailored to produce slight diuresis every 24 hours & avoid water intoxication.
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2
Q

desmopressin

A
  • potent analogue of vasopressin
  • no vasoconstriction
  • more potent & longer DOA compared to vasopressin
  • post-op/unconscious = injection
  • maintenance = PO/ intranasal
  • 2nd line can be used as nocturnal enuresis
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3
Q

side effects of desmopressin

A
  • hyponatremia (risk of convulsions if not fluid restricted)
  • fluid retention
  • D/V
  • headache
  • stomach pain
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4
Q

tolvaptan

A
  • ADH/vasopressin antagonist
  • avoid rapid treatment = CNS effects
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5
Q

demeclocycline

A
  • ADH antagonist
  • blocks the renal tubular effect of ADH
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6
Q

what are the drug interactions of ADH antagonists

A
  • lamotrigine
  • chlorpromazine
  • drugs that can cause hyponatraemia = carbamazepine
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7
Q

name corticosteroids (high to low activity)

A

Dexamethasone (HIGHEST)
Betamethasone
Fludrocortisone
Prednisolone
Hydrocortisone (LOWEST)

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8
Q

name mineralocorticoid (high to low activity)

A

Fludrocortisone (HIGHEST)
Hydrocortisone
Prednisolone (LOWEST)

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9
Q

fludrocortisone (indications & side effects)

A
  • HIGH glucocorticoid activity
  • Minimal anti-inflammatory effect
  • High fluid retention
  • IND: postural hypotension, septic shock from adrenal insufficiency
  • SE:
    -> Loss of sodium & water = hypertension
    -> hypokalaemia & hypocalcaemia
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10
Q

what are the main side effects of glucocorticoids?

A
  • diabetes
  • muscle wasting
  • osteoporosis
  • GI ulceration and perforation
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11
Q

What are the side effects of all corticosteroids

A

‘ACHING BOSOM’

Adrenal suppression
Cushing syndrome, cataracts
Hyperglycaemia, hyperlipidaemia
Infections, insomnia
Nervous system; Psychiatric reactions
Glaucoma, GI ulcers

Blood pressure (hypertension)
Osteoporosis
Skin lining
Obesity
Muscle wasting

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12
Q

advise in managing side effects of corticosteroids

A
  • Px lowest effective dose for the shortest duration
  • Single dose in the morning = reduce suppression
  • Alternate day dose = reduce suppression
  • intermediate use with short courses
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13
Q

Name a MILD potency topical corticosteroid drug

A

hydrocortisone

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14
Q

Name a MODERATE potency topical corticosteroid drug

A

clobetasone

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15
Q

Name a POTENT topical corticosteroid drug

A

betametasone

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16
Q

Name a VERY POTENT topical corticosteroid drug

A

clobetasol

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17
Q

are corticosteroids appropriate for pregnancy/breastfeeding patients?

A
  • generally safe
  • monitor for fluid retention
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18
Q

ketoconazole

A
  • cortisol inhibiting drug = tumor based cushing syndrome
  • monitor for hepatotoxicity signs; jaundice, dark urine, pale stool, anorexia, abdominal pain, itching, N/V
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19
Q

Name the bisphosphonate drug that has the greatest risk of osteonecrosis of the jaw

A

Zolendronic acid (IV)

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20
Q

risedronate

A
  • 1st line prevention/treatment for osteoporosis
  • PO, can have foods/drinks/other meds after 2 hours of ingestion
  • sit upright while taking and for 30 mins after
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21
Q

alendronic acid

A
  • 1st line prevention/treatment for osteoporosis
  • PO, have with empty stomach 30 mins before having any food/drinks/other medications
  • sit upright while taking and for 30 mins after
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22
Q

side effects of bisphosphonates

A
  1. Osteonecrosis of;
    - jaw = greater risk with IV bisphos. counsel on dental hygiene. Report; dental pain, swelling and immobility.
    - auditory canal = rare but more likely in long term patients. Counsel on ear pain, discharge and infection
  2. Oesophageal reactions =
    - STOP use if dysphagia or experiencing new/worsening of heartburn.
    - Take with full glass of water while standing and stay upright to reduce risk
  3. Atypical femoral fractures
    - report hip/thigh/groin pain
    - rare but more likely with long term pts.
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23
Q

strontium

A
  • severe treatment of post-menopausal osp and male osp
  • used in pts with high risk of fractures
  • MoA: stimulates bone formation & reduces bone resorption
  • initiated by specialists
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24
Q

side effects of strontium

A
  • increased risk of CVD; MI and VTE (baseline assessments and 6-12 mo)
  • severe allergic reactions: DRESS
    DRESS starts with; rash, swollen glands, fever, increased WBC and can affect the liver, kidney and lungs
  • consult GP and stop use immediately once development of a RASH
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25
Q

counselling advice for taking strontium

A
  • avoid food/drinks 2 hours after/before ingestion
    especially Ca/Al/Mg based antacids.
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26
Q

indication of raloxifene

A

used for secondary prevention and treatment of vertebral fractures in post-meno osteoporosis

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27
Q

indication of teriparatide

A

used for the treatment of post-menopausal osteoporosis
- increases Ca2+ levels and reduces PO4+ levels by negative feedback

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28
Q

indication for calcitriol

A

vitamin D3
used for the treatment of post-menopausal osteoporosis

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29
Q

calcitonin is not recommended because?

A

risk of malignancy with long term use

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30
Q

examples of natural oestrogen

A
  • oestradiol
  • oestrone
  • oestriol
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31
Q

examples of synthetic oestrogen

A
  • ethinyloestradiol
  • mestranol
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32
Q

examples of progestogens

A
  • norethisterone
  • levonorgestrel
  • desogestrel
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33
Q

clonidine

A
  • antihypertensives
  • not 1st line
  • has lots of SE
  • CI: CVD events
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34
Q

tibolone

A
  • treatment for post-menopause
  • increases the risk of endometriosis cancer
  • increases the risk of stroke by 2.2 x in 1st year
  • NOT to use in the peri-menopausal phase
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35
Q

indications for ethinylestradiol

A
  • Short term treatment of oestrogen deficiency
  • Osteoporosis prophylaxis if unable to tolerate other drugs
  • Female hypogonadism
  • Menstrual disorders
  • Palliative treatment of prostate cancer
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36
Q

raloxifene

A

• Treatment and prevention of post-menopausal osteoporosis
• Doesn’t help with vasomotor symptoms

37
Q

clomifene

A

• Anti-oestrogen
• Ovulation stimulant
• Used to treat infertility/ absent periods
• Use 6 cycles only- risk of ovarian cancer
• SE: multiple pregnancy

38
Q

cyproterone

A
  • anti-testosterone
  • used in hyper sexuality
  • used for metastatic prostate cancers
  • MHRA: risk of meningioma (brain tumour)
39
Q

ulipristal acetate

A
  • progesterone receptor modulator
  • Intermittent ulipristal used to treat mod-severe symptoms of uterine fibroids in post-menopausal women where surgery unsuitable/ failed
  • Also used as EHC
40
Q

metformin

A
  • 1st line treatment for T2DM
  • Biguanide class
  • MoA= increases insulin sensitivity via GLUT
41
Q

what are the cautions/ CI of metformin

A
  • DKA
  • Contrast media
  • Surgery/ anaesthesia
  • renal impairment CrCl <30ml/min
  • tissue hypoxia - acute HF, MI, respiratory & liver failure
42
Q

what are the cautions/ CI of metformin?

A
  • DKA
  • Contrast media
  • Surgery/ anaesthesia
  • renal impairment CrCl <30ml/min
  • tissue hypoxia - acute HF, MI, respiratory & liver failure
43
Q

what are the side effects of metformin?

A
  • reduces Vitamin b12 absorption
  • GI disturbances - switch to MR prep
  • lactic acidosis: increased risk in renal failure/tissue hypoxia
44
Q

in what circumstances do we advise to stop the use of metformin

A
  • AKI
  • Dehydration
  • Nausea
  • Vomiting
  • Diarrhoea
  • Fever
45
Q

advantages of metformin

A
  • weight neutral
  • reduce CV morbidity in long-term use
  • does not cause hypoglycaemia unless used with hypo-causing drugs
  • cheap
46
Q

DPP4 inhibitors (examples & MOA)

A
  • Used among 1st line treatment options for T2DM
  • MOA: prevents the breakdown of GLP (a hormone that stimulates insulin secretion & inhibits glucagon)
  • examples (‘gliptin’)
    Sitagliptin, Linagliptin, Vildagliptin
47
Q

what are the advantages of DPP4-i?

A
  • Can be taken with or without food
  • weight neutral
  • does not cause hypoglycaemia
48
Q

what are the side effects of DPP4-i?

A
  • headaches
  • GI disturbances
  • Pancreatitis = report abdominal pain, stop use
  • Vildagliptin - hepatotoxic
    (report; abdominal pain, dark urine, fatigue, N/V)
49
Q

what are the cautions/ CI of DPP4-i?

A
  • Reduce dose in renal impairment (except for linagliptin)
  • liver impairment = Vildagliptin
    (linagliptin & sitagliptin are liver safe)
  • Avoid use with GLP-1 agonists
50
Q

pioglitazone

A
  • Used among 1st line treatment options for T2DM
  • MoA: PPAR agonist, increases insulin sensitivity and reduces hepatic glucose output
51
Q

what are the advantages of pioglitazone?

A
  • taken with or without food
  • does not cause hypoglycemia
52
Q

what are the side effects of pioglitazone?

A
  • bladder cancer (report if having urinary problems)
  • heart failure if on insulin
  • bone fractures: caution in elderly = increased risk of falls
  • liver toxicity: monitor LFTs, and report signs of toxicity. Stop if jaundice
53
Q

caution & CI of pioglitazone

A
  • CI in bladder cancer/hematuria
  • CI in HF
  • CI in DKA
  • Caution in CVD
  • if continued use when HbA1c levels have reduced to 0.5% within the last 2-3 months
54
Q

name the combination of anti-diabetic drugs that are NOT recommended to be taken together on a triple therapy

A

pioglitazone + Dapaglipflozin (SGLT-2i)

55
Q

sulfonylurea (SU)

A
  • Used among 1st line treatment options for T2DM
  • MOA: stimulates insulin sensitivity
  • e.g. gliclazide, glipizide, tolbutamide, glibenclamide (LA) and glimepiride (LA)
56
Q

advantages of sulfonylurea

A
  • taken with or without food
  • SU short acting - Pts with renal impairment/ elderly
  • potent
  • cheap
  • target HbA1c levels are 7% (53 mmol/mol)
57
Q

side effects of sulfonylurea

A
  • cause hypoglycaemia = to avoid skipping meals
  • Avoid driving
  • LA SU- increases prolonged hypoglycaemia effect esp in elderly
  • Weight gain
  • Jaundice
  • hypersensitivity = skin rash
  • hyponatremia = glipizide or glimepiride
58
Q

CI/ cautions of sulfonylurea

A
  • CI in DKA or porphyria
  • Renal/liver failure= increase risk of hypoglycaemia
  • SU-induced hypo- = visit the hospital
  • Avoid LA SU in elderly
59
Q

what are the drug interactions with sulfonylurea

A
  • warfarin & ACE i = hypoglycemia
  • NSAIDs (reduce renal excretion)
60
Q

what are the drug interactions with sulfonylurea?

A
  • warfarin & ACE i = hypoglycemia
  • NSAIDs (reduce renal excretion)
61
Q

name the drug that is to be AVOIDED to use with sulfonylurea

A

meglitinides (e.g. Repaglinide
Nateglinide)

62
Q

SGLT2-i (MOA, examples)

A
  • Used for T2DM if SU is CI/not tolerated
  • MOA: reduces glucose absorption & increases glucose urine output.
  • e.g. empagliflozin, canagliflozin and dapagliflozin
63
Q

what are the advantages of SGLT2-i?

A
  • weight loss
  • reduces CVD risk (esp empagliflozin and canagliflozin)
  • taken with or without food
  • does not cause hypoglycemia
64
Q

side effects of SGLT2-i

A
  • polyuria
  • polydipsia
  • genital/urinary infection (Fourier’s gangrene)
  • associated with DKA
  • hypotension = increases risk of falls in elderly
  • increases the risk of lower limb amputation (report leg ulcers when using canagliflozin)
  • correct hypovolemia before starting
65
Q

cautions/CI of SGLT2-i

A
  • CI in DKA = stop treatment
  • Monitor ketones and renal function
  • CI in liver failure
  • Avoid in renal impairment = dehydration
  • Caution use with diuretics as it can cause hypovolemia or hypotension
66
Q

GLP-1 agonists (MOA, examples)

A

‘ides’
- Used in triple therapy with metformin + SU
examples; Exenatide (S/C) BD before large meals, MR = OW
Liraglutide (S/C) anytime
Lixisenatide (S/C) anytime
Dulaglutide (S/C) OW
Semaglutide (ORAL OD/ S/C OW)

MoA: Slows gastric emptying
Suppresses glucagon secretion
Increases insulin secretion

67
Q

advantages of GLP 1 agonists

A

• Weight loss (feeling full)
• CVD benefit with liraglutide)

68
Q

side effects of GLP 1 agonist

A

• GI side effects
- Can cause dehydration
• Risk of pancreatitis- report severe persistent abdominal pain =stop
• Liraglutide: gall bladder disorders

69
Q

name the drugs of GLP 1 agonists that affect the absorption of oral drugs

A

Lixisenatide and exenatide affect the absorption of oral drugs so take 1 hour before oral or 4 hours before for S/C

70
Q

CI/ cautions of GLP 1 agonist

A

• Do not use with DPP-4I
• MHRA: DKA: Reports of DKA when insulin reduced/ stopped too quick
• GI disease (exenatide/ lixisenatide/ liraglutide)
• Oral semeglutide needs to be taken on empty stomach and 30 mins before other meds/ food. GI SE may reduce after 1 month. Interacts with thyroxine so monitor thyroid levels.
• Review after 6 months, continue if HbA1c reduced by 1%/11mmol/mol and weight loss by 3% of initial wt
• Use contraception
• Do not administer after meal

71
Q

acarbose

A

MOA: Delays starch and sucrose absorption
Dose: 50mg daily increased to TDS then to 100mg TDS if necessary. Max 200mg TDS

72
Q

advantages of acarbose

A

• Low risk of hypo
• Weight loss
• Take when having meals- allows flexibility (chew with 1st bite or take before with water)

73
Q

side effects of acarbose

A

• GI side effects- antacids don’t help, flatulence improves with time but diarrhoea = reduce/ withdraw
• Liver failure (rare): monitor LFT’s

74
Q

CI/ cautions of acarbose

A

• GI disorders e.g., hernia, IBD/ surgery
• Liver failure
• CrCl <25ml/min
• Treat hypoglycaemia with GLUCOSE not sucrose
• Monitor liver function

75
Q

MEGLITINIDES

A

MOA: Stimulates insulin secretion
Rapid onset and short DOA.

E.g:Repaglinide
Nateglinide

76
Q

advantages of meglitinides

A

• Sulphonylurea alternative
• Variable meal pattern (take 30 mins before, max QDS (if pt has 4th meal)

77
Q

side effects of meglitinides

A

• May cause hypoglycaemia
• Weight gain
• Hypersensitivity reactions e.g., skin rashes

78
Q

CI/ cautions of meglitinides

A

• Repaglinide as monotherapy or used with metformin – not with any others
• Nateglinide cannot be used with SU
• Renal failure
• Severe liver failure (increased risk of hypo)
• DKA
• If they skip a meal, must OMIT dose.
• Rapid onset and short DOA
• If stress: stop treatment and replace with insulin

79
Q

rapid-acting (insulin analogues)
- Onset, DoA, examples and when to take it

A
  • Onset: 15 mins
  • DoA: 2-5 hours
  • Examples: Lispro (Humalog I), Aspart (Novo rapid/ fiasp) and glulisine
  • Taken immediately before meals, discourage after meals.
  • A better option than soluble - as it improves glycemic control and protects against nocturnal hypoglycaemia.
80
Q

Soluble short-acting (human insulin)
- Onset, DoA, examples and when to take it

A
  • Onset: 30-60 minutes
  • DoA: 9 hours
  • Examples: Humulin S and actrapid
  • Take 15-30 mins before meals
  • Can be given via IV in emergencies such as DKA
81
Q

Intermediate insulin
- Onset, DoA, examples and when to take it

A
  • Onset: 1-2 hours (peaks at 3-12 hours)
  • DoA: 11-24 hours
  • Examples: Isophane (Humulin I)
  • Given to patients who experience hyperglycaemia overnight/morning
  • Given before bed
82
Q

Long-acting insulin
- Onset, DoA, examples and when to take it

A
  • Onset: 2-4 days (no peak)
  • DoA: 36 hours
  • Examples: Glargine (Lantus), Detemir (Levemir) and Degludec (Tresiba)
  • Given to patients who experience hyperglycemia during the day or night
  • Given before bed
83
Q

Levothyroxine

A
  • 1st line treatment for hypothyroidism
  • MHRA warning: some patients want to remain brand specific, Perform TFT’s if this occurs
    If persistent symptoms, consider maintaining or same brand
  • Take 30-60 mins before breakfast/ other caffeine containing food/ medication
84
Q

Monitoring requirements for levothyroxine

A

• Every 3 months until stable TSH
• Then yearly
• Monitor T4 if symptomatic
• Baseline ECG

85
Q

Liothyronine

A
  • more rapid & potent compared to levothyroxine
    (20-25mcg = 100mcg of Levo)
  • Not routinely offered
  • Ideal in hypothyroid emergencies
  • Brand specific – non UK brands not bioequivalent
86
Q

Briefly explain the metabolism effect of initial dose of levothyroxine

A

Initial dosage: if metabolised too quickly => excess dosage => hyperthyroid symptoms

Reduce dose OR withhold for 1-2 days then restart at lower dose

87
Q

Briefly explain the use of levothyroxine in pregnancy

A

• Advise delaying conception until stable on levothyroxine
• TFT’s may be inaccurate in pregnancy so use trimester related reference ranges

88
Q

Diazoxide

A
  • Tx for chronic hypoglycaemia
  • Dx: Initially 5 mg/kg daily in 2–3 divided doses, adjusted according to response; maintenance 3–8 mg/kg daily in 2–3 divided doses.
  • monitor FBCs (WBC and platelets), blood pressure
  • CI: established or unstable CVD