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Y5 Drug Profiles > BASIC - RESPIRATORY > Flashcards

BASIC - RESPIRATORY Flashcards

1
Q

Names of short/long-acting beta-2-agonists?

A
  • Short-Acting
    o Salbutamol, Terbutaline
  • Long-Acting
    o Salmeterol, formoterol
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2
Q

Indications of beta-2-agonists?

A
  • Asthma – short acting as step 1, long-acting as step 3 (must be given with inhaled corticosteroids)
  • Hyperkalaemia – nebulised salbutamol (in addition to insulin, glucose, calcium gluconate) in emergency treatment
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3
Q

Mechanisms of beta-2-agonists?

A
  • Beta2-receptors found in smooth muscle of bronchi, GI tract, uterus, blood vessels
  • Stimulation of GPCR leads to smooth muscle relaxation – improves airflow
  • Stimulate Na/K/ATPase pump causing K+ to move into cells – treat hyperkalaemia in addition to insulin
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4
Q

Side effects of beta-2-agonists?

A
  • ‘Fight-or-flight’ effects
    o Tachycardia, palpitations, anxiety, tremor
  • Gluconeogenesis, may increase serum glucose
  • High doses
    o Serum lactate levels increased
  • Long-acting
    o Muscle cramps
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5
Q

Interactions of beta-2-agonists?

A
  • Beta-blockers reduce effectiveness
  • Hypokalaemia
    o Concomitant use with theophylline, corticosteroids
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6
Q

What must long-acting beta-agonist be prescribed with?

A
  • Long-acting only prescribed in asthma with inhaled corticosteroid
    o As associated with increased asthma deaths
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7
Q

Cautions of beta-2-agonists?

A

o CVD – tachycardia promote angina, arrhythmias
o Hypokalaemia
o Diabetes

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8
Q

Prescription of beta-2-agonists?

A
  • PRN prescription
    o Use 2 puffs every 4 hours, up to 10 if needed
    o If more, then hospital
  • Can be administered aerosol (MDI), dry powder, nebulised, in combination with steroid (Symbicort, Seretide)
  • Spacer provided to improve airway deposition and treatment efficacy
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9
Q

Monitoring asthma?

A
  • Monitored via peak expiratory flow rate (PEFR)
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10
Q

Names of antimuscarinics?

A

Ipratropium, tiotropium, glycopyrronium

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11
Q

Indications of antimuscarinics?

A
  • Acute exacerbation (short-acting)

- Added in step 4 of chronic asthma (long-acting)

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12
Q

Mechanism of antimuscarinics?

A
  • Bind to muscarinic receptor, competitive inhibitor of acetylcholine
  • Stimulation of muscarinic receptor causes ‘rest and digest’ effects
  • Blockage has opposite effects:
    o Reduced smooth muscle tone
    o Reduced secretions
    o Relaxation of pupillary constrictor and ciliary muscles – pupil dilatation and preventing accommodation – blurred vision
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13
Q

Side effects of antimuscarinics?

A
  • Little systemic absorption

- Blurred vision, urinary retention, constipation, dry mouth

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14
Q

Cautions of antimuscarinics?

A

o Angle-closure glaucoma

o Arrhythmias

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15
Q

Contraindications of antimuscarinics?

A

o Hypersensitivity to atropine or derivatives

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16
Q

Prescription of antimuscarinics?

A
  • Short-acting used QDS or PRN
  • In acute asthma
    o 0.25mg in 4mL saline
    o Every 20-30 mins for 1st 2 hours then every 8 hours if needed
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17
Q

Indications of theophylline?

A
  • Chronic asthma
  • Severe acute asthma
  • Reversible airway obstruction (COPD)
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18
Q

Mechanism of theophylline?

A
  • Xanthine derivative
  • Competitively inhibits PDE 3 and 4 and also binds to adenosine A2B receptor
  • Smooth muscle relaxation (bronchodilation) and suppression of airway response to histamine, methacholine, adenosine, allergens
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19
Q

Side effects of theophylline?

A
  • Narrow therapeutic window
  • GI upset – nausea, diarrhoea
  • Tachycardia, Arrhythmias
  • Headaches, insomnia, dizziness
  • Hypokalaemia
  • Overdose (>10mg/litre)
    o Vomiting, agitation, dilated pupils, sinus tachycardia, convulsions
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20
Q

Cautions of theophylline?

A
  • Arrhythmias
  • Elderly
  • Epilepsy
  • Risk of hypokalaemia
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21
Q

Interactions of theophylline?

A
  • Affected by CYP450 enzymes

- Reduce dose in hepatic impairment

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22
Q

Advice on taking theophylline?

A
  • Avoid alcohol, excessive caffeine

- Take with food, swallow whole

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23
Q

Monitoring of theophylline?

A

o Plasma theophylline concentrations measured 5 days after oral treatment and >3 days after dose changes

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24
Q

Names of inhaled corticosteroids?

A

Beclomethasone (Clenil Modulite 50mcg lower-potency, Clenil 200mcg), budesonide, fluticasone

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25
Q

Indications of inhaled corticosteroids?

A

Step 2 of therapy in chronic asthma – not controlled by short-acting B2 agonists
Chronic obstructive pulmonary disease (COPD) – usually with LABA/LAMA

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26
Q

Mechanism of inhaled corticosteroids?

A
  • Pass through plasma membrane and activate receptor which:
    o Upregulation of anti-inflammatory proteins
    o Downregulates pro-inflammatory interleukins, cytokines, chemokines
  • Effects
    o Reduces mucosal inflammation
    o Widens the airways
    o Reduces mucus secretion
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27
Q

Side effects of inhaled corticosteroids?

A
  • Occur locally in the airway
    o Oral candidiasis
    o Hoarse Voice
  • Few systemic effects unless at very high dose which may cause adrenal suppression, growth retardation and osteoporosis
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28
Q

Doses of inhaled corticosteroids?

A 
-	Inhalation of powder (circle one)
o	Child 5-11 years
	100-200mcg BDS
o	Child 12-17 years & adults
	200-400mcg BDS, can be increased up to 800mcg
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29
Q

Communication to patient on inhaled corticosteroids?

A
  • Reassure them that hardly any of the steroid is absorbed into the body so, except in very high-dose treatment, there are unlikely to be any serious side effects (or weight gain)
  • Advise them to rinse their mouth and gargle after taking the inhaler to prevent development of a sore mouth or hoarse voice
  • Show your patient how to use the device
30
Q

Name of mucolytic?

A

Carbocysteine

31
Q

Indications of mucolytics?

A

Clear secretions easier in COPD, bronchiectasis and CF

32
Q

Mechanism of mucolytics?

A
  • Reduce sputum viscosity
33
Q

Side effects of mucolytics?

A
  • Nausea and vomiting
  • Itchy skin, rash
  • GI bleeding
  • Anaphylaxis reaction
34
Q

Contraindications of mucolytics?

A
  • Peptic ulcer
35
Q

Names of alpha-adrenoreceptor antagonists?

A

Tamsulosin, doxazosin, alfuzosin

36
Q

Indications of alpha-adrenoreceptor antagonists?

A
  • 1st line medical option in BPH

- Add on treatment in resistant hypertension when CCB, ACEi and thiazide diuretics failed

37
Q

Mechanism of alpha-adrenoreceptor antagonists?

A
  • Alpha-1-adrenoreceptor blockers
    o Found in smooth muscle, including blood vessels and urinary tract (bladder neck and prostate)
    o Blockade induces relaxation causing vasodilatation and fall in BP and reduced resistence to bladder outflow
38
Q

Side effects of alpha-adrenoreceptor antagonists?

A
  • Postural hypotension
  • Dizziness
  • Syncope
  • Sexual dysfunction
  • Particularly prominent after first dose
39
Q

When to avoid alpha-adrenoreceptor antagonists?

A
  • Avoid in patients with postural hypotension, history of micturition syncope
40
Q

Interactions of alpha-adrenoreceptor antagonists?

A
  • Additive effect of antihypertensive drugs

o To avoid first-dose hypotension – omit dose of existing antihypertensives on day of first alpha blocker

41
Q

Prescription of alpha-adrenoreceptor antagonists?

A
  • Oral
  • Doxazocin – BPH and hypertension – 1mg daily and increased after 1-2 weeks
  • Tamsulosin – BPH – 400 micrograms daily
  • Take at bedtime
42
Q

Monitoring of alpha-adrenoreceptor antagonists?

A
  • Lying and standing blood pressure
43
Q

Names of PDE-5 inhibitors?

A

Sildenafil

44
Q

Indications of PDE-5 inhibitors?

A
  • Erectile dysfunction

- Primary pulmonary hypertension

45
Q

Mechanisms of PDE-5 inhibitors?

A
  • Selective phosphodiesterase type-5 inhibitor
    o Found in smooth muscle of corpus cavernosum of penis and arteries of lung
  • For an erection to occur:
    o Sexual stimulation releases NO, producing cGMP and causing arterial smooth muscle relaxation, vasodilatation and penile engorgement
    o PDE5 responsible for breakdown of cGMP so sildenafil increases concentrations and erection quality
    o Does not cause an erection without sexual stimulation
  • In pulmonary vasculature, causes arterial vasodilatation
46
Q

Side effects of PDE-5 inhibitors?

A
  • Flushing, headache, dizziness, nasal congestion
  • Hypotension, tachycardia, palpitations
  • Small risk of vascular events – MI, stroke
  • If erection fails to subside for prolonged period of time despite absence of stimulation (priapism) – need urgent medical attention
  • Colour distortion need urgent review
47
Q

Contraindications of PDE-5 inhibitors?

A
  • Recent stroke, ACS or significant history of CVD

- SBP <90mmHg

48
Q

Cautions of PDE-5 inhibitors?

A
  • Other antihypertensive drugs – hypotension

- Sickle cell, myeloma, leukaemia

49
Q

Interactions of PDE-5 inhibitors?

A
  • Do not prescribe with nitrates, nicorandil as can cause cardiovascular collapse
50
Q

Prescription of PDE-5 inhibitors?

A
  • Viagra (Sildenafil 25-100mg tablets) used as required 1 hour before sex
    o Starting dose usually 50mg, maximum one per day
    o Seek medical advice if erection persists two hours after sexual activity has finished
  • Tadalafil is longer-acting and can be used regularly for spontaneous sexual activity when frequent sex
  • Revatio used for pulmonary hypertension
51
Q

Names of GU antimuscarinics?

A

Oxybutynin, tolterodine, solifenacin

52
Q

Indications of oxybutynin?

A
  • Reduce urinary frequency, urgency and urge incontinence in overactive bladder (first-line if bladder training ineffective)
53
Q

Mechanism of oxybutynin?

A
  • Bind to muscarinic receptors and act as competitive inhibitor of acetylcholine
    o Promotes bladder relaxation, reduce urinary frequency, urgency and urge incontinence
  • Selective for M3 receptor in bladder
54
Q

Side effects of oxybutynin?

A
  • Dry mouth, tachycardia, constipation, blurred vision
  • Drowsiness, flushing, headache, nausea and vomiting
  • Urinary retention
55
Q

Contraindications of oxybutynin?

A
  • UTI
  • GI obstruction, intestinal atony
  • BPH
56
Q

Cautions of oxybutynin?

A
  • Elderly
  • Dementia
  • Angle-closure glaucoma
  • Arrhythmias/Acute MI/Cardiac surgery
57
Q

Interactions of oxybutynin?

A
  • Risk of adverse effects increased with other antimuscarinics - TCAs
58
Q

Prescription of oxybutynin?

A
  • Oxybutynin 5mg orally every 8-12 hours, dose increased as needed every week
59
Q

Monitoring of oxybutynin?

A
  • Prior to starting – urinalysis

- Review within a month and then every 6-12 months once stable

60
Q

Indications of N-acetylcysteine? (Parvolex)

A
  • Paracetamol poisoning antidote

- Prevent renal injury due to contract nephropathy

61
Q

Mechanism of N-acetylcysteine?

A
  • Paracetamol metabolised by conjugation with glucuronic acid and sulfate
  • Small amount converted to N-acetyl-p-benzoquinone imine (NAPQI), which is hepatotoxic
    o This is normally quickly detoxified by conjugation with gluthathione
    o In overdose NAPQI causes liver damage
  • Acetylcysteine replenishes body’s supply of glutathione
62
Q

Side effects of N-acetylcysteine?

A
  • Diarrhoea, headache
  • Anaphylactoid reaction (nausea, tachycardia, rash, wheeze)
    o Histamine release independent of IgE
    o Need to stop acetylcysteine and restart at slower rate
63
Q

Caution of N-acetylcysteine?

A
  • Asthma – do not delay treatment

- Increase PT and INR

64
Q

Prescription of N-acetylcysteine?

A
  • 150mg/kg over 1 hour (200ml 5% glucose)
  • 50mg/kg over 4 hours (500ml 5% glucose)
  • 100mg/kg over 16 hours (1L 5% glucose)
  • Max dose for 110kg
65
Q

Communication of N-acetylcysteine?

A
  • If started within 8 hours, very effective

- Need to have continuous treatment for 21 hours

66
Q

Monitoring of N-acetylcysteine?

A
  • Serum paracetamol levels at 4 hours after ingestion as well as LFTs, U&Es, FBC and INR and repeated after the course of acetylcysteine
67
Q

Names of 5-alpha reductase inhibitors?

A

Finasteride

68
Q

Indications of 5-alpha reductase inhibitors?

A

2nd line treatment to BPH (after alpha blockers)

69
Q

Mechanism of 5-alpha reductase inhibitors?

A

Inhibits 5-alpha reductase which converts testosterone into more active dihydrotestosterone which stimulates prostate growth

Reduce size of prostate

70
Q

Side effects of 5-alpha reductase inhibitors?

A 
Impotence
Reduced libido
Gynaecomastia
Hair growth
Breast cancer
71
Q

Warnings of 5-alpha reductase inhibitors?

A

Exposure of a male foetus to 5α-reductase inhibitors may cause abnormal development of the external genitalia

Pregnant women do not take these drugs and are not exposed to them (e.g. by handling broken or damaged tablets or through semen during unprotected intercourse with a man taking these drugs)

72
Q

Dose of 5-alpha reductase inhibitors?

A

Finasteride 5mg OD

Y5 Drug Profiles (17 decks)

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